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Cholinergic
Adrenergic
Afferent
Efferent
There are four types of adrenergic receptors. These are lpha-1 and lpha-2 and eta-1 and
eta-2. Alpha-receptors are located mainly in the blood vessels and pupils. eta-1 receptors
are in the heart and eta-2 receptors are mainly in the lungs, skeletal muscles and uterus.
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Sympathetic (adrenergic)
Originate in the thoracic and lumbar region
Post ganglionic nerve fibre very long
Preganglionic nerve fibre very short
Ganglia is near spinal cord
Neurotransmitters
Norepinephrine (NE)
Epinephrine (epi)
Dopamine (D)
ACh
Receptors:
Norepinephrine (NE) a1,a2, b1 (Not on b2)
Epinephrine (epi)a1, a2, b1, b2
DopamineD1 > b > a
ACh M1
Functions
Increase heart rate
Increase blood pressure
Increase blood flow to skeletal muscle and heart
Dilation of pupil and bronchioles
Adjust in response to stressful situation (trauma,
cold, fear, hypoglycemia, exercise)
Changes in emergencies (Fight or flight response)
Receptors
AChM1, M2, M3, M4 and M5
Functions
Maintains essential body functions
(Digestive, waste elimination).
Oppose or balance the action of
sympathetic.
Dominant over sympathetic in rest and
digest situation
Both the sympathetic and parasympathetic nerves innervate the same structures. Their actions are opposing
but not equal in scope.
Vessels
Brain (postsynaptic)
Site
Presynaptic
Membrane
Penis
1
2
1
2
2
2
Heart
Kidney
Juxtamedullary apparatus
Cerebral vessels
Bladder (including Longitudinal muscle)
Fat cells
Bronchial muscles
Vessels (Venules)
Pancreas
D1, D2
D1, D2
D1
D1
D1
D2
Nigrostriatal pathway
Median eminence, anterior pituitary
Nucleus accumbens, limbic system
Renal and mesenteric vessels
Chemoreceptive trigger zone
Ganglia presynaptic membrane
Effect
Strong vasoconstriction
Neurotransmission
Contraction
Auto inhibition of norepinephrine
release
Ejaculation
Stimulation
Renin release
Dilation (?)
Relaxation
Lipolysis
Bronchodilation
Weak vasodilation
Relaxation
Insulin release
Gluconeogenesis,
Glycogenolysis,
Lipolysis
Motor coordination
Inhibition of prolactin release
Control of emotions
Dilation
Nausea
Auto inhibition of dopamine release
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Effector Organ
Adipose
Sympathetic
Arterioles
Skin and mucosa
Skeletal Muscle
Bladder
Detrusor
Sphincter
Eye
Radial Muscle, iris
Sphincter muscle, iris
Ciliary muscle
Constriction (a1)
Usually relaxation (2, M)
Lipolysis (3)
Heart
Sinoatrial node
Atrioventricular node
Atria
Ventricles
Kidney
Lacrimal glands
Liver
Lung (bronchial muscle)
Male sex organs
Nasopharyngeal glands
Pancreas
Salivary Glands
Stomach & intestine
Motility
Sphincters
Secretion
Sweat glands
Uterus
Veins (systemic)
Spleen
Relaxation (2)
Contraction (a1)
Contraction (M)
Relaxation (M)
Accommodation
(Relaxation, 2)
Miosis (M)
Contraction for near
vision (M)
?
Renin secretion (1)
Mucus secretion
Fluid secretion (M)
Marked water secretion
(M)
Increase (M)
Relaxation (M)
Stimulation (M)
Secretion (M)
Contraction (a1) Relaxes detrusor
muscles
Relaxation (2)
Dilation (2)
Contraction (a1)
Secretion (M)
-
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Epipen, Anapen
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Adrenergic Drugs
Adrenergic Drugs
(Sympathetic Drugs)
Ach
Adrenergic agonists
Alpha agonist
Alpha 1 agonist
Alpha 2 agonist
Beta agonist
Beta 1 agonist
Beta 2 agonist
Adrenergic antagonists
Alpha antagonists
(a-blockers)
Beta antagonists
(b-blockers)
a1agonists
a1 agonists
Pharmacological
actions
Therapeutic use
Epinephrine
(in blood)
Norepinephrine
Adrenergic
Receptor
Adrenergic
Receptor
Phenylephrine
Pseudoephridine
Methoxamine
Bronchodilation
Blood Pressure
Peripheral Resistance
Closure Sphincter bladder
Mydriasis
Vasoconstriction
Dimetapp Cold (Night time) extra strength contains
Phenylephrine + chlorpheniramine + acetaminophen
Dimetapp Daytime Cold extra strength contains
Pseudoephedrine + Acetaminophen
Methyldopa
Clonidine
Guanabenz
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Mechanism
Therapeutic use
Common side effects
Adrenergic Drugs
Therapeutic use
Contraindication
Dobutamine (b1>b2)
Isoproterenol (b1 = b2)
Tachycardia
Increase lipolysis
+ve Inotropic effect (increase force of contraction of heart)
Increase Cardiac output (CO)
Increase Heart rate (HR)
Bronchodilation
Dobutamine (Dobutrex) the treatment of adults with cardiac
decompensation due to depressed contractility resulting from
organic heart disease or following cardiac surgical procedures in
which parenteral therapy is necessary for inotropic support.
Tachycardia and ventricular fibrillation
Beta 2 agonist
Beta2 agonist
Mechanism
Therapeutic use
Short acting beta 2
agonist
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Adrenergic Drugs
Inhalation route has less toxic side effects than systemic routes.
Have less tachycardia, hyperglycemia, and hypokalemia effects with
inhalations routes.
Short acting are best reserved for treatment of acute exacerbations and
prophylaxis of exercise induce asthma
Salmeterol has long duration of action, providing bronchodilation for at
least 12 hours, and slow onset of action.
Indicated in maintenance treatment in combination with corticosteroids
especially for nocturnal asthma, EIA, and COPD
Not indicated in acute asthmatic attacks
Dopamine
Epinephrine
Norepinephrine
a1, a2, b1 agonist
Vasoconstriction
Cardiac contractility
Systolic Blood Pressure (SBP)
Diastolic Blood Pressure (DBP)
Peripheral Resistance (PR)
Reflex bradycardia
Vasoconstriction causes peripheral resistance
Baroreceptor reflex stimulates cardiac contractility
Epinephrine (Adrenaline)
Action
Cardiovascular
Respiratory
Hyperglycemia
Therapeutic use
Side effects
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Adrenergic Drugs
Dopamine (Inotropin)
Mechanism
Major affects
Act on D1, D2, D3, D4, D5, and Mixed a and b agonist
Has +ve inotropic and +ve chronotropic effects
Dilates renal arterioles by increasing blood flow to kidney
Dopamine is drug of choice for shock given by continuous infusion.
Adrenergic Blockers
Adrenergic antagonists
Alpha-blockers
(Adrenergic blockers)
Nonselective
(1 and 2
blockade)
Selective (1
Doxazocin (1)
Terazocin (1)
Tamsulosin (1a)
Reversible
Phentolamine
Beta blockers
1 , 2 , &
blockade
Carvedelol
Labetelol
Neuronal blockers
Selective ( 1
blockade)
Esmolol
Metoprolol
Atenolol
Acebutolol
Irreversible
Phenoxybenzamine
Nonselective
(1and 2
blockade)
Propanolol
Pindalol
Nadolol
Timolol
Levobutalol
a1-antagonists
a1-antagonists
Mechanism
Therapeutics use
Prazosin
Terazosin
Doxazosin
Tamsulosin ( 1A)
Alfuzosin ( 1A)
BP orthostatic hypotension
Total Peripheral Resistance
No Reflex tachycardia
Vasodilations
First dose effect (syncope) Fainting
Miosis
Antihypertensive
Symptomatic Benign Prostate Hyperplasia
Side effects
Comments
Starting dose for doxazocin 1mg once daily and titrate slowly
Tamsulosin has no postural hypotension
Tamsulosin is a selective 1A receptor blocker
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Adrenergic Drugs
a2-antagonist
Yohimbine
Pharmacological
actions
Therapeutic use
Side effects
Contraindications
Mirtazepine
Used as antidepressant
a1 & a2 antagonists
a1 & a2 antagonist
Phentolamine
(Reversible)
Therapeutic use
Phenoxybenzamine
(Irreversible)
Pheochromocytoma
b-blockers
Mixed b1 and b2antagonists (non
selective)
Mechanism
b1 antagonists
(cardioselective or
selective)
Propranolol
ProPiNaTionaLe
Pindolol
Nadolol
Timolol
Levobutolol
Reduce intra ocular pressure Decrease secretion of aqueous humor
Bradycardia
Bronchoconstriction (Bronchospasm)
Esmolol
Metoprolol
Acebutolol
Atenolol
Selective EMAA
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Mechanism
Mixed and
-antagonists
Mechanism
Partial agonist and
antagonist
Mechanism
ISA: Intrinsic
Sympathomimetic
Activity:
Adrenergic Drugs
Vasoconstriction
No bronchoconstriction
Labetalol: acts 1, 1 and 2 receptor (Non-ISA/alpha)
Carvedilol: acts 1, 1 and 2 receptors (Non-ISA/alpha)
Produce vasodilation BP
Peripheral vasoconstriction
Does not alter serum lipid levels
Acebutolol
Pindolol
Oxprenolol
Intrinsic sympathomimetic activity (ISA)
Minimized disturbances of lipid and carbohydrate metabolism.
The partial agonist stimulates the beta-receptors to which they
are bound; yet inhibit stimulation by the more potent endogenous
catecholamines, epinephrine and norepinephrine.
1 agonist
Phenylephrine
Pseudoephridine
Beta agonist
2 agonist
Clonidine
Methyl dopa
1 agonist
2 agonist
Tremors
Palpitations
Hyperglycemia
Tachycardia
1 antagonists (a1-blockers)
Doxazocin
Prazocin
Terazocin
Tamsulosin
2 antagonists (a2-blockers)
Orthostatic hypotension
Tachycardia (No reflex tachycardia)
Vertigo
Sexual dysfunction
First dose effects (syncope)
Hypotension
Orthostatic hypotension
Reflex tachycardia
CNS insomnia, fatigue,
hallucinations, impotency (libido)
CVSDecrease HDL and increase
TG, bradycardia, orthostatic
hypotension
Beta antagonists
(b-blockers)
Increase BP
Inrease TPR
Vasoconstriction
Mydriasis
Decrease lipolysis
Decrease insulin secretions
Sexual dysfunction
1 and 2 antagonist
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Adrenergic Drugs
Cardioselective b-blockers
Esmolol
Metaprolol
Atenolol
Acebutalol
Partial alpha and beta blockers
Carvedilol
Labetelol
Partial agonist and antagonist
Acebutalol
Pindolol
Oxyprenolol
Drugs that have +ve inotropic and +ve chronotropic effect is: dopamine.
Inotropic is: force of contraction (+ve increase in force of contraction)
Chronotropic is: heart rate (+ve increase in heart rate)
Drugs that have +ve inotropic and ve chronotropics is: Digoxin
Drugs that have +ve inotropic are: ACE Inhibitors.
Epinephrine is used for: Anophylactic reaction or hypersensitive reactions.
Epinephrine is: 1, 2, 1 and 2 agonist
Xylometazoline action is on alpha-adrenergic receptors.
Salbutamol is 2 agonist
Summary of 2 agonist:
2 agonist drugs have no anti-inflammatory effect and act as branchodilators
SABA always used as prn and tolerance can occur with regular use and also mask the symptoms
of inflammation.
SABA has additive effect with anticholinergic drugs (Ipratropium)
LABA always used as daily dose.
LABA has same effect as SABA but long duration of action.
LABA has synergistic effect with corticosteroids. (Products available: Fluticosone + Salmeterol
= Advair)
SABA and LABA are branchodilators.
Beta-blockers are drug of choice for uncomplicated hypertension in patient age under 65 years
old.
Beta-blockers are used cautiously in: Asthma, CHF, Diabetes and sever peripheral vascular
diseases.
Diabetic patient taking beta-blockers monitor? Blood sugar levels
Digoxin, non-DHP CCB may cause additive Bradycardia with beta blockers.
-blockers are drug of choice for orthostatic hypotension.
What adrenergic blockers are useful in treating Tachycardia? blockers (Propranolol)
The longest acting beta-blockers is? Nadolol
Example of irreversible and noncompetitive 1 and 2 blocker is Phenoxybenzamine
Examples of drugs that reverse effect of epinephrine associated vasocontriction 1 blockers.
Examples of sympathomimetic that should be avoided in Glaucoma Phenylephrine,
pseudoephridines.
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Adrenergic Drugs
Norepinephrine
Central Nervous System
Cardiac Output
Heart Rate
Catechol Amine O-Methyl Transferase
Exercise Induce Asthma
Systolic Blood Pressure
Diastolic Blood Pressure
Peripheral Resistance
Total Peripheral Resistance
Benign Prostate Hyperplasia
Intra Ocular Pressure
Blood Pressure
Esmalot, Metopralol, Acebutalot, Atenalol
Intrinsic Sympathomimetic Activity
High density Lipoperteins
Angiotism Converting Enzymes
Short Acting 2 Agonist
Long Acting 2 Agonist
Congestive Heart Failure
Dihydropyridine
Calcium Channel Blockers
Otrivin
Advair
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Cholinergic Drugs
Cholinergic Drugs
(Parasympathetic Drugs)
Cholinergic
agonists
Direct
cholinergic
agonist
Acetylcholine
agonists
Pilocarpine
Cevimeline
Choline
estere
Bethanechol
Carbachol
Indirect
cholinergic
agonists
Antiacetylcholinesterases
Quarternary
alcohols
Edrophonium
Tacrine
Donepezil
Carbamate
Physostigmone
Neostigmine
Demecarium
Pyridostigmine
Organophosphate
Echothiophate
Malathion
Parathion
Sarin
Soman
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Cholinergic Drugs
Side Effects
Cholinergic drugs
Myopic accommodation
Bradycardia
Salivation
Lacrimation
Flushing
Diarrhea
Hypotension
Tremors
Choline
Anticholinergic
Hyper optic
accommodation and
increased intraocular
pressure
Tachycardia
Dry mouth
Blurred vision and
mydriasis
Constipation
Urinary retention
Dizziness and
drowsiness
Acetylcholine
CoA
Acetylcholine
Synaptic
vesicle
Presynaptic
receptor
Choline
Acetylcholine
Acetate
INTRACELLULAR
RESPONSE
Acetylcholine
Pilocarpine
Bethanechol
Carbachol
Methacholine
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Pharmacological
actions
Cholinergic Drugs
Heart rate
Cardiac output
Blood pressure
saliva secretion
Miosis
Bethanecol: used clinically for its therapeutic effects in postoperative atony of the bowel, for abdominal
distention and urinary retention. Other drugs in this group are pilocarpine and carbachol, used in the
eye to treat glaucoma.
Urinary retention is the inability to empty the bladder. It can be due to a number of conditions such
as old age, prolonged surgery, tumours, distended bladder without voiding for long periods, exposure
to cold or anemia.
Glaucoma is disease of the eye characterized by increased intraocular pressure resulting in damage
to the optic nerve and the retina. It can lead to blindness if left untreated.
Pilocarpine is a cholinergic agent most often used to treat glaucoma since it produces a reduction in
intraocular pressure.
Side effects: cramps, diarrhea, and increased gastric acid. May cause bradycardia, flushing and a
fall in blood pressure, bronchoconstriction-causing difficulty in breathing, sweating and salivation.
If you look at the chart that showed the effects of the parasympathetic system, you should not be
surprised to see the side effects mimic the action of the parasympathetic system.
Miosis
Effects on muscarinic and nicotinic receptors.
Effects on NMJ and brain
Wide range of actions
Insecticides
Parathion
Malathion
Echothiophate
Physostigmine
Neostigmine
Pyridostigmine
Edrophonium
Donepezil
Tacrine
Neostagmine is used to treat myasthenia gravis. This disease is a disorder of skeletal (voluntary
striated) muscle due to excessive cholinesterase or lack of acetylcholine. It is characterized by
increasing fatigue and muscle weakness; some cases are mild, some are severe. Death usually
occurs due to respiratory depression.
Side effects: diarrhea, cramps, increased salivation, increased bronchial secretions, miosis, sweating
and muscle cramps.
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Cholinergic Drugs
Muscarinic antagonists
Anticholinergic
drugs
Pharmacological
actions
Anticholinergic
side effects
Atropine
Muscarinic antagonist
Ipratropium
Scopolamine
Benztropine
Tertiary amines
Quarternary amine
Tropicamide
Atropine
Ipratropium
Glycopyrrolate
Scopalamine
Tiotropium
Trihexyphenidyl
in salivation cause
dry mouth (xerostomia)
intestinal secretion Constipation
Increase HR Tachycardia
Mydriasis Pupil dilatation
Relaxation of detrussor muscle Urinary retention
Blurred vision
Dry mouth
Blurred vision
Tachycardia
Constipation
Urinary retention
NMJ blockers
These agents are used for surgical patients to relax the muscles during surgery. .
Pharmacological actions:
Blocks the cholinergic transmission between motor nerve and nicotinic receptors.
Antagonizes (non depolarizing type) and agonist (polarizing) the effect of acetycholine.
Classified as two categories of NMJ blockers:
Depolarizing: Succinylcholine
Depolarizing drug attaches to nicotinic receptors and act like acetylcholine to depolarize the
junction.
Causes opening of sodium channel associated with nicotinic receptors, which results in
depolarization of receptors.
Non-depolarizing:
Prevents the binding of acetylcholine.
Inhibits muscular contraction
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Cholinergic Drugs
Sinoatrial Node
Atroventricular Node
Peripheral Resistance
a -Bungarotoxin
Acetyl Choline
Neuro Muscular Junction
Blood Pressure
Heart Rate
IsotoCarpine
Atreza, AtroPen, Atropine Care, Atropisol
Atrovent, Atrovent HFA
Isopto Hyoscine, Maldemar, Scopace
Cogentin
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Tropicamide
Glycopyrrolate
Trihexyphenidyl
Atracurium
Tubocurarine
Doxacurium
Pancuronium
Vecuronium
Mivacurium
Succinylcholine
Physostigmine
Neostigmine
Pyridostigmine
Edrophonium
Donepezil
Tacrine
Malathion
Echothiophate
Neostigmine
Edrophonium
Cholinergic Drugs
Mydriacyl
Robinul, Robinul Forte
Artane
Tracrium
Tubarine. Metubine. Jex
Nuromax
Pavulon
Norcuron
Mivacron
Anectine, Quelicin, Sucostrin
Mestinon, Regonol
Prostigmin
Pyridostigmine
Enlon, Reversol, Tensilon
Aricept, Aricept ODT
Cognex
Ovide
Phospholine Iodide
Prostigmin
Enlon, Reversol, Tensilon
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Blood Pressure
Diuretics
Antihypertensive drugs
Antihypertensive Drugs
= Cardiac Output (CO)
Beta
Blockers
Calcium
Channel
Blockers
Alpha1
Blocker
Alpha2
agonists
ACE inhibitors
Angiotensin
antagonist
AT1 Receptor
Blocker
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Antihypertensive drugs
By altering blood volume: Sympathetic stimulation releases the enzyme renin. Angiotensinogen and
angiotensin I & angiotensin II.
Angiotensin II is the bodies most potent circulating vasoconstrictor causing increases BP.
Angiotensin II stimulates aldosterone (ADH) secretion leading to increase kidney sodium reabsorption
and increase in blood volume, which contributes to increase in BP.
Systemic blood pressure depends upon cardiac output and resistance to flow
Angiotensin I
ACE
Angiotensin II
PR
BP
Aldosterone
Na/H2O retension
Blood
Volume
b-blockers
Beta-blockers are used to treat hypertension and angina. These drugs act by slowing the heartbeat,
which results in lowered blood pressure since blood pressure is affected by the heart rate and
peripheral resistance. Because of its action on the lining of arteries, propranolol is also used to treat
migraines.
Nonselective (
& 2)
1
Propranolol
Pindolol
Nadolol
Timolol
Levobutolol
Vasoconstriction
Reduce intra
ocular pressure
(IOP) =
secretion of
aqueous humor
Bradycardia
Cardioselective
( 1 only)
Esmolol
Metoprolol
Acebutolol
Atenolol
Bisoprolol
Betoxalol
Labetalol
Carvedilol
Acebutolol
Pindolol
Oxprenolol
Alpha receptors
Produce
vasodilatation =
BP
Beta blocker
cause Peripheral
vasoconstriction
Does not alter
serum lipid
levels
Intrinsic
sympathomimetic
activity (ISA)
Minimized
disturbances
of lipid and
carbohydrate
metabolism
Beta Blockers
Beta & Alpha
blockers
Partial agonist
& antagonist
CardioSelective
(b 1 only)
Nonselective (b1
& b2)
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Mixed b1 and b2antagonists (non
selective)
Mechanism
b1 antagonists
(cardioselective)
Mechanism
Mixed a and
b-antagonists
Mechanism
Partial agonist and
antagonist
Mechanism
ISA: Intrinsic
Sympathomimetic
Activity:
Side effects
Antihypertensive drugs
Propranolol
ProPiNaTionaLe
Pindolol
Nadolol
Timolol
Levobutolol
Reduce intra ocular pressure Decrease
secretion of aqueous humor
Bradycardia
Bronchoconstriction (Bronchospasm)
Esmolol
EMAA Selective
Metoprolol
Acebutolol
Atenolol
Vasoconstriction
No bronchoconstriction
Labetalol
Carvedilol
Produce vasodilation BP
Peripheral vasoconstriction
Does not alter serum lipid levels
Acebutolol
Pindolol
Oxprenolol
Intrinsic sympathomimetic activity
Minimized disturbances of lipid and
carbohydrate metabolism.
The partial agonist stimulates the betareceptors to which they are bound; yet
inhibit stimulation by the more potent
endogenous catecholamines, epinephrine and
norepinephrine.
The result of opposing actions is a muchdiminished effect on cardiac rate and cardiac
output.
Compared to b-blocker without ISA.
1 receptors
blood
CO
HR
Force
receptors
peripheral
vasodilation
Cardiac output
Renin
Preripheral
resistant
Angiotensin II
BP
Aldosterones
Na, H2O levels
Blood volume
Cardiac output
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Contraindications
Antihypertensive drugs
Beta-blockers therapeutic uses:
Bradycardia
Propranolol
Heart blockage
Asthma and bronchospasm (avoid non selective)
Peripheral vascular diseases such as Raynauds
phenomenon and intermittent claudication except
carvedilol and labetelol can be tried.
Timolol
Caution in congestive heart failure.
Left ventricular dysfunction
Drug and food interactions
Pindolol
Metaprolol
Cardioselective, used for
Propranolol is best absorbed with food but
hypertension, angina
consistency is the most important factor
Metoprolol is best taken with meals
Atenolol
Cardioselective, used for
These drugs should be taken at about same
hypertension
time every day
Esmolol
Cardioselective used for
Beta blocekers that have Ist pass metabolism;
hypertension, tachycardias
propranolol, timolol
Beta blocekers that have no biotransformation; Acebutolol Cardioselective, used for
hypertension, angina
atenolol
Beta blocekers that have blockadeeffect:
Decrease in contractility of heart and decrease
labetalol, carvedilol
in oxygen consumption
Beta blocekers that act as membrane stabilizer;
propranolol
-receptors
Indication
Contraindication
Side Effects
1-antagonist
2-agonist
Orthostatic hypotension
Tachycardia
Vertigo
Sexual dysfunction
Decrease lipolysis
Decrease insulin secretion
Sexual dysfunction
Hypertension
Benign Prostatic Hypertrophy
(BPH or enlarged prostate)
DOC for pheochromacytoma
hypertension
Hypertension
Treat withdrawal
symptoms in recovering
drug and alcohol abusers
(Clonidine)
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Antihypertensive drugs
pheochromacytoma hypertension.
Pharmacological actions of 1 anatagonist:
BP
Total Peripheral Resistance (TPR)
No Reflex tachycardia
Vasodilations
First dose effect (syncope)
Miosis
Side effects: Orthostatic hypotension, Tachycardia (No reflex tachycardia), Vertigo, Sexual dysfunction
to avoid the first dose effect of hypotension and occasional syncope, the starting doses should be small
and given at bedtime.
Methyldopa
Clonidine
Guanabenz
ATP
Methyldopa (Aldomet)
Mechanism
Therapeutic use
a2 agonists
Inhibit norepinephrine release
Inhibit insulin release
Indicated in moderate to sever hypertension
Produced active metabolite (Methyl dopa Alpha methyl
norepinephrine)
Methyl dopa is prodrug
Drug of choice for hypertension in pregnancy.
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Side effects
Antihypertensive drugs
Clonidine (Cataprex)
Chemistry
Clonidine contain imidazoline ring.
Therapeutic use Used in non complicated hypertension to lower BP.
Indicated in opioids and benzodiazepine withdrawal symptoms (CNS
symptom)
Side effects
CVS bradycardia orthostatic hypotension, severe rebound hypertension
CNS drowsiness, dizziness, agitation
Dosage
Precautions
Counselling
Transdermal patch
Pruritus and rash at the site of transdermal
Patch (TT1 (release 0.1 mg/24 h), TT2 (0.2 mg 24/h). TT3 (0.3 mg/24 h)
Dont discontinue abruptly, reduce dose over 2-3 days to reduce sever
hypertension
Dont miss any pill, Dont stop suddenly
Causes drowsiness
Need gradual withdrawal
Classification of Diuretics
Thiazide
Diuretics
Loop
Diuretics
K-sparing
diuretics
Carbonic acid
Inhibitor
Osmotic
diuretic
Chlorothiazide
Hydrochlorothiazide
Chlothalidone
Furosemide
Ethacrynic acid
Bemetanide
Spirolactone
Triamterene
Amiloride
Acetazolamide
Mannitol
Diuretics
Often called water-pills, diuretics increase urine production,
Reducing the body of sodium and water, thereby reducing the volume of blood that the heart
must pump, and in this manner decreasing blood pressure.
Side effects: stomach upset, frequent urination, potassium depletion, and dizziness.
Potassium blood levels should be monitored.
Foods rich in potassium may be ingested (eaten) daily. These are potatoes, bananas, cantaloupe,
and citrusfruit.
If potassium levels are very low, potassium chloride or potassium oral liquids may be used.
Mechanism of hypokalemia induced by CA inhibitors, loops and thiazide diuretics: Because of
upstream blockade of NaCl reabsorption there is Na+ consequently there is reuptake of Na+.
+ve charge in the cell. The increase +ve charge then pushes out K+ into the lumen.
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Antihypertensive drugs
Thiazide Diuretics
Thiazides
Pharmacological
actions
Therapeutic uses
Side effects
Loop Diuretics
Loop
Mechanism
Therapeutic use
Side effects
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Antihypertensive drugs
Nephritis (intestinal)
Gout arthritis
Sequence of ototoxicity (etharynic acid>furosemide>bumetanide)
Do not use
Ethacrynic Acid Does not contain sulfonamide functional group no sulfa allergy
Potassium sparing
Pharmacyprep.com
Amiloride (Midamor)
Potassium sparing diuretics
Triamterene (Dyrenium)
Spironolactone (Aldactone)
The K+ STAys
Na+
Spironolactone
H+ K+
Triamterene
blue color urine
Amiloride
Inhibit Na+ reabsorption and K+, H+ excretion in
Act in the early collecting duct to
distal convoluted tubule and net results is
descreased Na+ reabsortion and K+, H+ excretion
inhibit the electrogenic reabsorption
of Na+ by blocking the Na channels
and hence the exchange of sodium for potassium.
After administration: Na+, Cl- elimination, K+, Ca++ (amiloride).
Increase Na, H2O, HCO3 excretion (decrease levels in body)
Decrease K+, H+ excretion
Alkaline urinary pH Increase excretion of HCO3
Spironolactone (Aldactone): competitive inhibits aldosterone at minor
Aldocorticoid receptors. Decreases potassium excretion.
Amiloride and triamterene
Act directly on late distal tubule and collecting duct. They disrupt
sodium exchange with Potassium and hydrogen by blocking sodium
channel
Decrease in the driving force for secretion of potassium and hydrogen.
Used in nephrogenic diabetic insipidus
Potassium sparing
Mechanism
Aldosterone
antagonist
Non aldosterone
antagonist
Osmotic Diuretics
Osmotic
Mechanism
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Antihypertensive drugs
Acetazolamide
Increase excretion of H2O, Na, K, and HCO3 (Decrease levels in body)
Increase alkaline pH Inc. exc-HCO3
Cause metabolic acidosis
Type of diuretic
Ca
Mg
Na
Uric acid
Blood sugar
Lipids
Metabolic Disturbances
Thiazide
Loop
K-sparing
Hyperchloremic
metabolic acidosis (CO2)
Intracellular alkalosis
CAI
Heperchloremic metabolic
acidosis
Osmotic
Diuretics Tips
ACE Inhibitors
Angiotensin II is a substance produced in the body that causes the blood vessels to constrict (become
smaller in diameter). ACE inhibitors inhibit Angiotensin II formation. These drugs represent a
major advance in hypertensive treatment and have most displaced digoxin as the drug of choice in
congestive heart failure. ACE inhibitors are used to treat hypertension and congestive heart failure.
ACE inhibitors also tend to protect the kidneys of diabetics from developing renal failure when used
in the early stages of diabetic nephropathy.
Side effects: profound low pressure, taste abnormalities, dry cough, blood cell abnormalities, and
kidney problems. They are contraindicated in pregnancy. A persistent dry cough may necessitate
discontinuing the drug. Use of potassium supplements and ACE inhibitors increase the risk of
hyperkalemia.
ACE Inhibitors
Captopril, Benazepril, Cilazapril, Enalapril,
Fosinopril, Lisinopril, Perindopril, Quinapril,
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Ramipril, Trandolapril
Pharmacological actions
Antihypertensive drugs
Liver
Angiotensinogen
sympathetic output
Bloodstream
Vasodilation of smooth muscles
Renin
levels of bradykinincauses dry cough
Angiotensin I
and vasodilation
retention of Na and H2O
Angiotensin
converting
Above combined effect produce in preload
enzyme
Kidney
Lung
and after load
Angiotensin II
cardiac output (CO).
Dilation of venous blood vessels leads to
Vasoconstriction
decrease in cardiac preload by venous
Aldosterone secretion
capacitance.
ADH secretion
Arterial dilator reduces systemic arteriolar
Thirst
resistance and after load.
Angiotensin II Formation
Lower BP by reducing peripheral vascular
resistance with reflexly increasing cardiac output rate.
By reducing circulating angiotensin II levels ACE the secretion of aldosterone, resulting
retention of Na and H2O.
Little change in HR, or GFR.
Therapeutic use
Sympathetic action
Vasodilation
BP
Bradykinin
Side effects
Contra
Indications:
Pregnancy (absolute): Can produce hypotension in the fetus leading renal failure
and death, skull hypoplasia and death.
Documented angioedema-secondary angioedema,
Bilateral renal artery stenosis.
Captopril should be taken one hour before meals.
High fat meals may reduce absorption of Accupril
Food does not effect the other drugs in this class
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Tips
Antihypertensive drugs
ARB Inhibitors
These drugs are used to control high blood pressure and appear to have the same benefits as ACE
inhibitors, without producing the common side effect (experienced by as many as 30% of patients)
of a dry cough. These drugs block the effects of Angiotensin II, a naturally occurring substance that
causes blood vessels to narrow (constrict). When these drugs are administered, blood vessels dilate,
thereby lowering blood pressure and decreasing the workload of the heart.
Mechanism: Angiotensin binds to its own receptors, AT-1 receptors are found on vascular muscle and
in the adrenals. Stimulation leads to vasoconstriction and release of aldosterone in the adrenal gland.
ARB Inhibitors
Losartan
Candesartan
Valsartan
Irbesartan
Telmisartan
Side effects
Less dry cough (cough associated with ACE inhibitors does appear with these drugs),
Bradykinin causes vasodilation of arterioles and venules results TPR.Less Dry cough
Dizziness,
Hypotension/syncope
Renal dysfunction. (Reversible renal failure)
Hyperkalemia
Angioedema
Contraindications
Pregnancy (Renal fetal toxicity),
Bilateral renal artery stenosis (stenosis = abnormal narrowing of passage or opening, such blood
vessels or heart valve.
Vasodilators
Preload: Volume
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Antihypertensive drugs
Minoxidil (Rogaine)
Mechanism
Therapeutic use
Side effects
For alopecia
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Side effects
Antihypertensive drugs
Salt and water retention, which may lead to CHF (use a diuretic).
Hematologic-neutropenia,
Leucopenia,
Agranulocytosis,
Muscle cramps,
Orthostatic hypotension
Tachycardia
Lupus like syndrome (Systemic Lupus Erythromatus)
Diazoxide (Hyperstat)
Mechanism
Therapeutic use
Side effects
Sodium Nitroprusside
Mechanism
Therapeutic use
Side effects
Thiocyanate
toxicity
Summary of b - blockers
Pharmacological actions
b1 = decrease heart rate
b2 = bronchoconstriction
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Antihypertensive drugs
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Antihypertensive drugs
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Antihypertensive drugs
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Antihyperlipidemics Drugs
Antihyperlipedemic Drugs
Classification of Antihyperlipidemic Drugs
HMG-CoA
reductase
inhibitors
Lovastatin
Simvastatin
Pravastatin
Fluvastatin
Atorvastatin
Cervastatin
Nicotinic
acid
Bile acid
sequeste-rants
Fibric acid
derivatives
Niacin
Cholestyramine
Cholestipol
Cholesterol
Absorption
inhibitors
Ezetimibe
Ezetrol
LDL
HDL
VLDL-TG
(TG)
Statins
Statins
Mechanism
Therapeutic use
Contraindicated
Side Effects
Drug interactions
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Monitor
Antihyperlipidemics Drugs
FLS
Known Metabolizing
Enzyme(s)
Grapefruit juice
Take
Food
Statin
Atorvastatin Fluvastatin Lovastatin Pravastatin Rosuvastatin Simvastatin
CYP3A4
CYP2C9
CYP3A4 Not Known CYP2C9 CYP3A4
Avoid
With or
without
At night
With or
after
Avoid
At night
With or
after
With or
without
With or
without
Avoid
At night
With or without
Antihyperlipidimocs/Dyslipidimics/Antihypercholesteremia
Cholesterol
D
O
F
I
n
t
e
s
t
i
n
e
Bile acid
Liver
Resins
Prevent
reabsorption
of bile acids
VLDL
Liver
Adipose
TG
Free VLDL Tissue
Fatty
Acids
sue
Ti s
Blood
circulation
TG-chylomicron
LDL
LDL
Therapeutic use
Side Effects
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Management
No-flush prep
Antihyperlipidemics Drugs
Bezafibrate
Fenofibrate
Gemfibrozil
Decrease TG levels
Increase HDL levels (moderately)
Decrease LDL levels
Inhibit cholesterol synthesis
Fibric acid derivatives
Treatment of choice in hypertriglyceridemia + diabetic patients.
HDL increase 10 20%
TG decrease 20 50% (Effective for TG)
Mild GI disturbances.
Lithiasis: because these drug increase bilary cholesterol excretion
predispose gallstone formation.
Sever hepatic and renal dysfunction, potentiates warfarin activity.
Preexisting gall bladder disease.
Liver Function test
Creatinin Kinase
Complete Blood Count
Renal function test
At 3, 6 and 12 mo, and yearly
Combination with Statins may lead to rhabdomyolysis
Fibrates
Fibrates
Mechanism
Therapeutic use
Side Effects
Contraindication
Monitoring
Drug interactions
Resins
Resins
Mechanism
Therapeutic use
Cholestyramine
Colestipol
Prevents absorption of cholesterol.
Anion-exchange resins bind with the enzymes in intestine and inhibit
the synthesis of cholesterol. Bile acids are synthesized from cholesterol.
Decrease LDL 15 30%
Increase HDL 3 10%
No change or increase in TG (disadvantage)
Drug of choice in pregnancy
Cholestyramine also relieves pruritis caused by accumulation of bile
acids in patients with biliary obstruction in cholestasis
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Side Effects
Drug-Drug
interactions
Antihyperlipidemics Drugs
Ezetimibe (Zetia)
Mechanism
Therapeutic use
Side Effects
Advantage
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TG
CBC
HMG
LFT
CPK or CK
ADEK
DM
HMG
Antihyperlipidemics Drugs
Lipitor
Lescol
Mevacor
Pravachol
Crestor
Zocor
Bezalip
Lipidil
Lopid
Questran
Colestid
Zetia
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Antihyperlipidemics Drugs
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Prinzmetal angina
Or
Vasospastic angina
Nocturnal Angina
Other causes that limit coronary blood flow include: Arterial thrombi and Spasm
Angina Pectoris
Angina are those symptoms of myocardial ischemia that occur when myocardial oxygen availability
is insufficient to meet myocardial oxygen demand.
These symptoms include:
Chest discomfort often described as heaviness, pressure, and squeezing. The sensation is
localized typically in the sternal region.
Symptoms often last one to five minutes. Angina can radiate to the left shoulder, to both arms
(ulnar surfaces of the forearm and hand), and can radiate to the neck, jaw, teeth, epigastrium and
back.
Types of angina
Angina Pectoris
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Types of angina
pectoris
Stable angina or
classical
Unstable
angina/resting/
Crescendo
Nocturnal
angina (angina
decubitus)
Prinzmetal
angina
(vasospastic or
variant angina)
Vasodilators
Nitrates
Cardiac depressants
Short duration
Inhaled amyl nitrite
Sublingual
Nitroglycerine
Isosorbide dinitrite
Intermediate
Oral regular or sustainedrelease Nitroglycerine
Isosorbide dinitrite
-blockers
Proponolol
Long duration
Transdermal
Ntiroglycerine patch
Treatment of angina
The following beta-blockers are used in treatment of angina:
Beta-blockers with Selective Intrinsic Sympathomimetic Activity (ISA):
Acebutolol hydrochloride Beta-blockers with Non-ISA: Atenolol
and Metoprolol tartrate can be used.
Beta-blockers with Nonselective, ISA: Pindolol
Beta-blockers with Nonselective, Non-ISA: Nadolol, Propranolol hydrochloride,
Timolol maleate
Calcium Channel Blockers are used in treatment of angina:
Amlodipine besylate, Diltiazem hydrochloride, Nifedipine, Verapamil hydrochloride
The following Coronary Vasodilators, Nitrates are used in treatment of angina:
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cGMP
Dephosphorylation of
myosin light chain
Nitrates
Organic nitrates act primarily by vasodilation (especially venodilation), which reduces
myocardial preload and therefore myocardial oxygen demand.
Nitrates also promote redistribution of blood flow to relative ischemic areas.
Mechanism
Side effects
Storage
Conditions
Drug
interactions
Dosage forms
Nitrites
Therapeutic use
Side effects
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calcium-channel blocking agents block the entrance of calcium into the muscle, the muscle will not
contract. This will allow themuscle to relax and subsequently reduce the blood pressure. Other
therapeutic uses: angina, migraine, antiarrhythmic.
Non
dihydropyridines
Diltiazem hydrochloride
Verapamil hydrochloride
Mechanism
NDHP
Diltiazem
Veropamil
Av conducting
decrease
Coronary Dilatation
Side effects: flushing, profound low blood pressure, swelling of legs and feet, constipation and
stomach upset. If edema (swelling) of the legs and feet occur, a diuretic may be added to the
regimen.
Nifedipine (Adalat)
Mechanism
Therapeutic use
Side Effects
Amlodipine (Norvasc)
Mechanism
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Therapeutic use
Side Effects
Diltiazem (Cardizem)
Mechanism
Therapeutic use
Side Effects
ASA
Post MI
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Low-density Lipoprotein
Angiotensin-Converting Enzyme
Acetyl Saliaylate
ST-Segment Elevation MI
non-ST-Segment Elevation MI
Verdanafil
Sildenafil
Tadanafil
Nitroprusside
Levitra
Viagra
Cialis
Nitropress
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Cardioic
glycosides
Digoxin
Digitoxin
Quabain
-agonists,
Dobutamine
PDE inhibitors
Amrinone
ACE inhibitors
Captopril
Enalapril
Lisinopril
Nitrates,
Nitroprusside,
Hydralazine,
PDE inhibitors
Milrinone
Congestive heart failure is characterized by reduced cardiac output so that the heart is not able to
pump sufficient oxygenated blood strongly enough to reach the tissues. The heart beat is weak and
rapid and the heart muscles may hypertrophy (grow larger) to compensate for reduced cardiac output.
Atrial fibrillation occurs when the atria beat rapidly and out of sequence.
Cardiac Heart failure due to:
Increased sympathetic activity
Fluid retention (edema)
Decrease in heart muscle contractility
Due to negative (-ve) inotropic effect
Due to +ve chronotropic effects
Left systolic dysfunction
Left sided failure (systolic failure)
This is the most common type of heart failure, Often due to hypertension. Due left ventricular
(systolic) dysfunction leads to pulmonary edema; Symptoms: SOB (Dyspnea), Wheezing. Can be
treated by ACE I, and beta blockers (rarely in chronic), only carvedilol (1, 2 and 1).
The Most common etiology of left sided heart failure is:
Due to impaired pumping ability of the heart
Usually occurs in Left ventricular ejection fraction
May be present without CHF
Ejection fraction is lower than 35%, it is Left ventricular dysfunction (systolic failure)
Right Sided Heart failure (diastolic failure)
Due to chronic lung disease, Diastolic filling is impaired this can leads to peripheral edema.
Symptoms: edema in veins, legs, bowel. Diuretics or Dihydropyridine CCBs treats right-sided
heart failure.
Ejection fraction is greater than 45%, it is Right ventricular dysfunction (Diastolic failure)
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PP
B
CO
CHF
Aldosterone
Venous
Pressure
Capillary
Filtration
Na/H2O retension
EDEMA
Cardiac glycosides
Mechanism
Positive Inotropic
effect
Negative
chronotropic effect
Vagomimetic effect
Side effects
Digoxin (Lanoxin)
Digoxin
Bioavailability
Therapeutic use
[K]i
Inhibits (slows)
Na/K ATPase
K
Na/K
ATPase
Na
[Na]i
Na/Ca
X-ch
Na Reduced Na
gradient slows
Ca removal
Ca
Digoxin Mechanism of Action
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Side effects
Monitor
Counselling
Improves Oxygenation
Inotropy
(Desired)
Tachyarrhythmias
(Side effect)
Bradyarrhythmias
(Side effect)
Ca i
Heart Rate
(Desired)
Digitalis toxicity
Digitalis
toxicity
Predisposing
factors
Toxicities of digoxin
increased by renal failure
(decrease excretion)
Hypokalemia, or
hyperkalemia (potentiates
drug effect)
Hypothyroidism, hypoxia,
renal failure and myocarditis
also predisposing factors for
digitalis toxicities.
Drugs that K+
levels
Thiazides
Loop diuretics
Corticosteroids
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Digitalis
toxicity
Management
Antidote
Digitoxin
Binds strongly to
proteins extravascular
space, resulting in
large volume of
distribution.
Digoxin eliminated
largely unchanged in
urine
Extensively
metabolized by liver
before it excrete in
feces.
CHF Tips
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Antiarrhythmic Drugs
Class II
-blockers
Esmolol
(Propranolol)
Timolol
Atenolol
Metoprolol
Nadolol
Class I
Ia-Na+ channel
blockers
Quinidine
Procainamide
Disopyramide
Amiodarone
Ib: Lidocaine
Mexiletine
Tocainide
Ic: Flecainide
ropafenone
1a
1b
1c
II
III
IV
Arrhythmias
Class III
K+ channel
inhibitors
Amiodarone
(Cordarone)
Bretylium
Dofetilide
Sotolol
Class IV
Ca 2+ channel
blockers
Verapamil
Diltiazem
Nifedipine
(Procardia, Adalat)
Miscellaneous
Adenosine
Magnesium
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Antiarrhythmic Drugs
Heart blockade:
The electrical impulses are partially or fully blocked between the atria and the ventricles. The SA
node in the right atrium fires at the normal rate, but the rate at which the ventricles contract (pulse
rate) depends on how many impulses get through to the ventricles.
Three types:
1st degree ---blockage of pulsation
2nd degree ----blockage of pulsation
3rd degree---complete heart block
First-degree heart block means there is a slight delay in each impulse going from the atria to the
ventricles. But, each impulse does get through and the heart rate is normal.
Second-degree heart block means that some impulses from the atria are not conducted through to
the ventricles. The rate that the ventricles contract can then be slow.
Third degree or complete heart block means that no impulses are conducted through. The
ventricles then contract at their own intrinsic rate of about 20-40 beats per minute. So, you have a
very slow pulse.
Myocardial Action Potential Curve
Myocardial action potential curve reflects action potential, which describe electrical activity of five
phases.
This occurs in atrial and ventricular myocytes and Purkinje fibers
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Antiarrhythmic Drugs
Torsade de pointes
A problem in one of the ion channels can prolong the Q-T interval. A prolonged Q-T interval can
increase risk for a type of arrhythmia called torsade de pointes. When torsade de pointes occurs,
heart cannot pump enough oxygen-rich blood to the rest of body, especially your brain. Torsade de
pointes can also lead to ventricular fibrillation, a dangerous form of arrhythmia that causes rapid,
uncoordinated contractions in the muscle fibers of the ventricles. With ventricular fibrillation, the
heart cannot pump oxygen-rich blood to the rest of the body, which can lead to death.
Drugs and diseases that can lead to QT-prolongation
Phenothiazines and haloperidol antipsychotics
Type III antiarrhythmic drugs
In patients with hepatic failure.
Electrocardiograph Wave Forms
The electrical activity occurred during depolarization and
repolarization transmitted through electrodes attached to
the body and transformed by an electrocardiograph (ECG)
in to series of waveforms;
P WAVE: indicated atrial depolarization
PR INTERVAL: indicates the spread of the impulse from the atria through Purkenje fibres.
QRS complex: indicates ventricular depolarization
ST segment: indicates phase 2 of the action potential- the absolute refractory period.
T wave: shows phase 3 of the action potential-ventricular repolarization.
Q-T interval mechanical contraction of the ventricles (Torse de pointes)
U wave caused by hypokalemia
Arrhythmias Treatment
Class I
Class Ia
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Class Ia
Therapeutic use
Class Ib
Therapeutic use
Class Ic
Therapeutic use
Class II
Beta blockers
Therapeutic use
Class III
K+ channel
blockers
Class IV
Ca2+ channel
blockers
Therapeutic use
Digoxin
Therapeutic use
Antiarrhythmic Drugs
Pharmacological action;
Slow the phase 0 (slow entry of Sodium ion)
Prolong re-polarization
Prolong effective refractory period
Indicated to treat SVT, VT
Lidocaine
Tocainamide
Mexiletine
Pharmacological action:
Minimal effect on Phase 0 Slow phase III repolarization (decrease K
pump out)
Indicated to treat VT, VA
iv Lidocaine: used to treat cardioversion related arrhythmias
Encainide,
Propafenone decrease 25-50% digoxin
Flecainide
Pharmacological action:
Very effective on slowing phase 0 depolarization
Little effect on repolarization
Indicated to treat VA
Propranolol
Atenolol
Timolol
Pharmacological action:
Competitively block catecholamine induced stimulation of Beta
receptor thereby
Suppress phase IV depolarization
Indicated to treat AT, SVT, VT, VA
Amiodarone blue skin, photosensitivity, photophobia
Bretylium
Sotalol
Prolong Phase III repolarization (Prolong QT interval)Torose de
pointes
Indicated to treat VA
Verapamil
Diltiazem
Nifedipine
Pharmacological action: Shortens action potential
Indicated to treat SVA, VA
Pharmacological action: Effects vagotonic response (vegomimetic)
thereby increases AV nodal refractoriness.
It is contraindicated in ventricular fibrillation.
Ventricular tachycardia may result from digitalis toxicities
Indicated to treat SVA (atrial arrhythmias) only
Contraindicated in ventricular arrhythmias
Quinidine (Quinaglute)
Mechanism
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Antiarrhythmic Drugs
Therapeutic use
Drug-Drug
interaction
Side Effects
Counselling
Procainamide (Pronestyl)
Mechanism
Side Effects
Amiodarone (Cordarone)
Therapeutic use
Counseling
Digoxin (Lanoxin)
Therapeutic use
Contraindicated
Atrial arrhythmias
Ventricular fibrillation and hypokalimic patients
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Counseling
Antiarrhythmic Drugs
Cordarone
Lanoxin
Procaine SR
Norpace CR
Enkaid
Rhythmol
Lanoxin
Quinaglute, Quinidex
Pronestyl, Procan, Procanbid
Tambocor
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Anticoagulants
Anticoagulants
Anticoagulants
Antithrombin III
Mucopolysaccharide
Vitamin K
analogue
Protein C
Endogenous
Anticoagulant
LMWH
Warfarin
Heparin
Intrinsic Pathway
Damaged surface
Extrinsic Pathway
Kininogen,Kallikrein
Xll
Trauma
Xlla
Xl a
Xl
lX
Prothrombin (ll)
Tissue factor
Va
Trauma
Xa
Final
Common
Pathway
Vll
Vlla
lXa
Vllla
Thrombin (lla)
Fibrinogen (l)
Fibrin (la)
Xllla
Cross-linked
fibrin clot
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Anticoagulants
Heparin
Mechanism
Therapeutic use
Drug-Drug
interaction
Side Effects
Contraindications
Monitoring
Advantage
Enoxaparin
Dalteparin
Tinzaparin
Ardeparin
LMWH are not interchangeable with heparin in their actions and
use. Because these highly acidic. These administered parenterally as
sodium salt. Because poorly absorbed from GI tract.
The prevention of DVT or PE
Does not change Prothrombin Levels
Act longer and do not require close blood monitoring as Heparin does
Hypersensitivity reaction (chills, fever, urticaria etc),
Bleeding
Heparin induce Thrombocytopenia
Osteoporosis
Warfarin (Coumadin)
Mechanism
War farin
Vitamin K epoxide reductase
Polypeptides Vitamin K
O
CO2
HOOC
NH2
Precursor of clotting Factors
II, VII, IX, X
VitaminK epoxide
O
HOOC
COONH2
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Therapeutic
Drug-Drug
interactions
Side Effects
Monitoring
Antidote
Anticoagulants
Metronidazole
Phenylbutazone
Warfarin
INR
Due to decrease
synthesis of clotting
factor
Cefamindole
Cefaprazone
Cefatetan
Cefametazole
Due to additive
effects
Heparin
LMWH
Thrombolytic
agents
Parenteral
Mech
Enhances the
serum protease
antithrombin
III results in
inactivation of
fators IIa, IXa, Xa,
XIa, XIIa, XIIIa
Protamin sulfate
Antidote
Site of
action
In vitro, In vivo
Vitamin K,
phytanadione
In vivo only (liver)
Onset of
Faster (minutes)
Slower (6-8 hours)
action
Pregnancy Yes
NO (Terotogenic)
Protamine sulfate: Works by acid base neutralization
INR
Warfarin
Chronic
alcohol
Barbiturates
Rifampin
Vitamin K
Dark green
Vegetables
Heparin antidote
Patient taking heparin monitored for
Heparin action include
What is the safest anticoagulant in pregnancy
What are the factors heparin inhibits
Monitor warfarin through
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Anticoagulants
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Antiplatelet Drugs
10
Antiplatelet Drugs
Antiplatelet Drugs
ASA
Dipyridamole
Ticlopidine
&
Clopidogrel
Glycoprotein
inhibitors
Eptifibatide
Tirrofiban
Prostaglandin
analogs
Epoprostenol
Platelets, of the elements of blood cells, tend to clump together. The following drugs interfere with
the coagulation by inhibiting platelet aggregation. Heart attacks and strokes occur when a blood
clot that forms in a narrowed portion of an artery blood flow and cuts off the supply of oxygen and
nutrients to the tissue that lies beyond the site of the clot.
ASA (Salicylates)
Clopidogrel
Ticlopidine
Theonopyridine
Dipyridamole
Dipiperdino-dinitro pyrimidine
Fab fragments of human monoclonal antibody to the Glycoproteine (GPIIb/IIIa) receptors
(Abciximab, tirofiban, eptifibatide).
Ticlopidine (Ticlid)
Mechanism
Therapeutic use
Side effects
Contraindications
Storage conditions
Dosage
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Food and drug
interactions
Antiplatelet Drugs
Clopidogrel (Plavix)
Mechanism
Therapeutic use
Side Effects
Drug-Drug
interaction
Contraindication
Monitoring
Antiplatelet summary
Drug of choice in STEMI
Patient cannot take aspirin due stomach ulcers for MI prophylaxis, what is an alternate drug
of choice
If patient is allergic to aspirin what is alternate drug
Drug of choice for transient Ischemic attack (TIA)
What is the effect of aspirin on warfarin
What dose of aspirin act as Antiplatelet
Acetyl Saliaylate
Transient Ischemic attack
Nonsteroidal Anti-Inflammatory Drug
Ticlid
Plavix
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Thrombolytic Drugs
11
Thrombolytic Drugs
Thrombolytic Drugs
Streptok inase
(Strepto protein from
Group C-B-hemplytic
steptococci bacteria
tissue
plasminogen
activator tPA
Clot selective
Mechanism
Therapeutic
Side Effects
Anistreptase (Aminase)
Prodrug of streptokinase
Uro k inase
(Abbokinase)
t-pa
(tissue type
plasminogen activator)
Alteplase (activase)
Directly degrade
Reteplase (Retevase)
fibrin and
very high affinity to
fibrinogen
plasminogen, bound to
thrombus
Alteplase
Reteplase
Tenecteplase
Streptokinase
VIIa
Blood
Urokinase
IX
X
Anistreplase
Xa
X
Prothrombin (II)
Thrombin IIa
Facilitate conversion of
plasminogen to plasmin that
Thrombolytics:
XII
Streptokinase
subsequently hydrolyzes fibrin
Urokinase
to dissolve clots
Alteplase
Fibrinogen
Recombinant DNA derivatives
Catalyzation
of tissue plasminogen activator
(tPA).
Plasminogen
Plasmin Fibrin (Soluble)
They contain 527 and 355 amino
XIIa
acids of natural tPA.
Fibrin degradation product
Fibrin (insoluble)
tPA catalyzes the conversion of
Site of injury
plasminogen to plasmin.
Acute MI and acute massive
pulmonary embolism (PE), DVT
Hypersensitivity reactions
Internal GI bleeding, retroperitoneal
bleeding, superficial bleeding at catheter injection site.
Nausea and vomiting
Streptokinase (Streptase)
Mechanism
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Therapeutic use
Drug-Drug
interactions
Side Effects
Monitoring
Thrombolytic Drugs
Urokinase (Abbokinase)
Mechanism
Therapeutic use
Side effects
Anistreplase (Eminase)
Mechanism
Therapeutic use
Thrombolytics Tips
t-PAs are
DOC for ST segment elevation myocardial infarction (STEMI)
Embolus
Streptase
Abbokinase
Eminase
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Antidepressants
12
Antidepressants
Classification of Antidepressants
Amine reuptake
inhibitors drugs
Non-selective
5HT, NE, D
5HT, NE
Dual action
Tricyclics (TCAs)
SNRI
Venlafaxine
a2 receptor inhibitors
Mirtazapine (SARI)
5HT only
Selective serotonin
Reuptake inhibitors (SSRIs)
Fluoxetine (Prozac)
Fluvoxamine
Paroxetine
Sertraline
Citalopram
e-citalopram
sNDRI
Bupropion
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Antidepressants
Classes of antidepressant drugs include: tricyclic compounds (TCAs), monoamine oxidase inhibitors
(MAOIs), selective serotonin re-uptake inhibitors (SSRIs) and reversible inhibitors of monoamine
oxidase (RIMAs).
Mechanism
Metabolic enzymes
Therapeutic use
Side effects
Advantage
Serotonergic
syndrome
(Contraindications)
Discontinued
syndrome
Citalopram (Celexa)
E-citalopram
Fluoxetine (Prozac)
Fluvoxamine (Luvox)
Paroxetine (Paxil)
Sertraline (Zoloft)
Selective serotonin reuptake inhibitors:Increase serotonin levels
Most common metabolizing enzymes
SSRI inhibit CYP 2D6
CYP3A4
CYP 1A9
Antidepressant
Antianxiety
Sexual dysfunction (orgasmic delay)Alprostadil may be helpful
GI Nausea (Most common)
Headache
Insomnia
Nervousness
Fatigue
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Tips
Antidepressants
Most anorexicFluoxetine
Most nauseating Fluvoxamine
Most weight gain Mirtazapine
Citalopram SE: Somnolence
All SSRIs have common SE: Nausea
Antidepressants with Less sexual dysfunction Bupropion,
Mirtazapine, moclobemide
Onset of action
It normally takes 2-4 weeks for antidepressant to have an effect.
Wash out period
Two SSRIs or SSRI with TCA or MAOI should not combine
If switch from one SSRI to other (SSRI, TCA or MAOI), waiting period
required (washout period)
All SSRIs have washout period for 2 weeks, Except: Fluoxetine (require
5 weeks)
Tramadol
Meperidine
Amphetamine
Dopamine
Cocaine
Methyldopa
MAO Inhibitors
Dextromethorphan
SSRI
Caffeine
TCA
Lithium
SSRI
MAO Inhibitors
TCAs
St.John wort
Serotonergic symptoms
Hyperpyrexia (Fever)
Agitation
Hypotension
Tremors / Shivering
Seizure
Coma, and death
Tricyclic Antidepressants
TCA
Mechanism
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Therapeutic use
Side effects
Contraindications
Overdose symptoms
Overdose treatment
Tips
Antidepressants
Antidepressant
Neuropathy painAmitriptyline
Enuresis in children (Bedwetting) Imipramine
Anxiety disorder (OCD)
CVD effects Orthostatic Hypotension, Tachycardia (AV blockade)
Weight Gain
Sexual Dysfunction
Confusion/Delirium
Bone marrow depression
Mania with manic depressive illnesses
Anticholinergic side effects
Constipation
Blurred vision
Urinary retention
Dry mouth
MAO inhibitors, SSRI
Nausea
Constipation
Confusion
Sleepiness
Palpitation
Dizziness
Dry mouth
Blurred vision
Fever
Contact physician immediatelyif any such symptoms appears.
Activated charcoal
Less hypotensive TCA
Nortriptyline (Aventyl)
Most Anticholinergic and
sedative TCAAmitriptyline
(Elavil)
Least sedative of TCA
Nortriptyline
Less anticholinergic TCANortriptyline
Take medication daily
Antidepressants must be taken for two to four weeks for a noticeable
effect
Continue to take medication even if you are feeling better
Do not stop taking the antidepressant without checking with the
physician
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MAO Inhibitors
Mechanism
Therapeutic use
Side effects
Drug interactions
Can cause
Serotonergic
syndrome
Serotonergic
syndrome
Hypertensive
crisis
Food to avoid
Antidepressants
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Antidepressants
Bupropion
Venlafaxine
Mirtazapine
Bupropion
Venlafaxine
Mirtazapine
Trazodone and Nefazadone
Serotonin (very little), Dopamine and Norepinephrine reuptake inhibitor
(sNDRI)
SE: Stimulant affect (tachycardia, agitation), aggravation of psychosis,
aggravation of seizure (Reduce seizure threshold)
Also used for smoking cessation (Zyban)
1st line treatment for Major depression
Least sexual dysfunction and weight gain
Inhibits Serotonin and Norepinephrine, Some degree of dopamine reuptake
inhibitor (SNRI)
Stimulant affect Anxiety, agitation, headache, insomnia
At higher dose 225 mg / day, it has cardiovascular side effects, such as dose
dependent hypertension.
At lower dose (75 and 150mg) it acts on 5HT only, higher dose (225mg)
5HT ,NE and Dopamine.
Alpha2 antagonist and potent 5HT2 receptor antagonist
Increases release of norepinephrine and serotonins.
Side effects: Increase appetite, Sedation
Increase serum cholesterol levels
Lithium (Lithobid)
Therapeutic use
Pharmacokinetics
Therapeutic levels
Dose
Side effects
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Toxic symptoms
(Over 1.5 mEq/L)
Monitoring
Drug interactions
Antidepressants
Antidepressant Tips
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Antidepressants
Citalopram
E-citalopram
Fluoxetine
Fluvoxamine
Paroxetine
Sertraline
Amitriptyline
Clomipramine
Desipramine
Doxepin
Imipramine
Maprotiline
Nortriptyline
Trimipramine
Phenelzine
Tranylcypromine
Isocarboxazid
Bupropion
Venlafaxine
Mirtazapine
Trazodone
Nefazadone
Lithium
Monoamine Oxidase
Selective serotonin reuptake inhibitor
Dopamine
Norepinephrine
Serotonin Norepinephrine Reuptake Inhibitors
Norepinephrine Dopamine Reuptake Inhibitor
Reversible Inhibitors of Monoamine oxidase
Tricyclic Antidepressants
Obsessive-Compulsive Disorder
Cardiovascular Disease
General Anxiety Disorde
5-hydroxy tryptamine (Serotonin)
Celexa
Proxac
Luvox
Paxil
Zoloft
Anafranil
Norpramin
Sinequan
Tofranil
Aventyl
Surmontil
Nardil
Parnate
Wellbutrin SR
Effexor
Remeron
Desyrel
Lithobid
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13
Benzodiazepines
Long action
Diazepam
Fluorazepam
Clorazepate
Intermediat
Alprazolam
Lorazepam
Temazepam
Estazolam
Short acting
Oxazepam
Triazolam
Midazolam
Ultra-short
action
Thiopental
Non-benzodiazepines
Zaleplon
Zopiclone
Zolpidem
Other anxiolytics:
Buspirone, Hydroxyzine
Intermediate
Amobarbital
Secobarbital
Pentobarbital
Long action
Phenobarbital
Sedatives (anxiolytic agents): Reduce anxiety with little effect on motor or mental functions.
Hypnotics: Produce drowsiness and reduce onset of sleep.
Insomnia disturbed or fragmented sleep, often associated with physical or emotional illness
Anxiolytic a drug that decreases anxiety
Sedatives
Benzodiazepines
Aldehyde
derivative
Antihistamine
Barbiturates
Others sedatives
Cyclopyrolones
Pyrazolopyrimidines
Hypnotic &
Sedatives
Benzodiazepines
Short acting
Midazolam
Estazolam
Triazolam (Halcion)
Intermediate acting
Alprazolam (Xanax)
Lorazepam (Ativan)
Oxazepam (generics)
Temazepam (Restoril)
Nitrazepam
Long acting
Diazepam (generics)
Flurazepam (Dalmane)
Clonazepam,
Chlordiazepoxide
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Benzodiazepines
Benzodiazepine are minor tranquilizers are used to treat insomnia and anxiety. The following are
terms that are used to describe some conditions dealing with anxiety or sleep disorders. Anxiolytic a
drug that decreases anxiety: insomnia disturbed or fragmented sleep, often associated with physical
or emotional illness: sedative a drug which causes drowsiness but not sleep, reduces anxiety and
irritability; hypnotic a drug which will produce sleep. Sometimes a larger dose of a sedative will
cause a hypnotic action.
Mechanism
Benzodiazepine
therapeutic actions
Anticonvulsant action
Muscle relaxant action
Dependence
Withdrawal symptoms
Benzodiazepine antidote
Reduce anxiety
Insomnia; Sedative and hypnotic action
Anticonvulsant action
Muscle relaxant action
Flurazepam (no rebound insomnia)
Quazepam (No rebound insomnia)
Temazepam
Triazolam used for insomnia often rebound insomnia
Alprazolam (used in treatment of panic disorders)
Clonazepam (useful in treating absence seizures)
Diazepamstatus epilepticus
Diazepammuscle spasm, muscle degenerative disease
Physical and psychological dependence (at high doses)
Withdrawal symptoms upon abrupt discontinuation
Long acting withdrawal symptoms occurs after number of days
Short acting benzodiazepine associated with immediate withdrawal
symptoms if it is stopped abruptly.
Confusion, anxiety, agitation, restlessness, insomnia, and tension.
Rapid development of tolerance and withdrawl symptoms occurs
with short acting.
Flumazenil
Other sedatives
Mechanism
Therapeutic use
Zaleplon
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Zopiclone
Zolpidem
Zolpidem (Ambien)
Mechanism
Therapeutic use
Advantages
Side effects
Barbiturates
Barbiturates
Ultra-short action
Thiopental
Short acting
Amobarbital
Secobarbital
Pentobarbital
Long action
Phenobarbital
Barbiturates are used much less commonly than before. They are effective only for a few weeks
since they alter the length of time spent in R.E.M. sleep. They should only be used for short-term
therapy as sedative or hypnotics.
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Barbiturates
Mechanism
Metabolic Enzymes
Therapeutic use
Withdrawal
symptoms
Poisoning
Poisoning
management
Barbiturates
antagonist
Miscellaneous
Non-barbiturate
sedatives
Chloralhydrate
Antihistamine
Chloralhydrate
Alcohol
Antihistamine
Buspirone
Tri chlorinated derivative of acetaldehyde
Doxylamine and other antihistamine are used as OTC treatment of sleep
disorders
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Hydroxyzine
Mechanism
Therapeutic use
Advantages
Buspirone
Ethanol
Anxiolytics
Azaspirodecanedione
Derivatives
Benzodiazepines
Various Anxiolytics
Buspirone hydrochloride
Alprazolam
Bromazepam
Chlordiazepoxide hydrochloride
Clorazepate dipotassium
Diazepam
Lorazepam
Oxazepam
Hydroxyzine hydrochloride Antihistamine
Paroxetine SSRI
Trifluoperazine hydrochloride Antipsychotics
Venlafaxine antidepressant
Alternate
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Benzodiazepines (BDZs)
Alprazolam 0.25mg TID or QID or
clonazepam 0.25 to 0.5mg BID
Obsessive-Compulsive
Disorder (OCD)
Post-traumatic Stress
Disorder (PTSD)
Clomipramine
SSRIs
Citalopram
Generalized Anxiety
Disorder (GAD)
Attention Deficit
Hyperactivity Disorder
(ADHD)
(SSRIs) fluoxetine,
fluvoxamine, paroxetine,
sertraline and citalopram
Gamma-Aminobutyric Acid
Benzodiazepine
5-hydroxy tryptamine (Serotonin)
Over The Counter
Cognitive Behavior Therapy
Selective Serotonin Reuptake Inhibitor
Tricyclic Antidepressants
Post-traumatic Stress Disorder
Obsessive Compulsive Disorder
Generalized Anxiety Disorder
Social Anxiety Disorder
Panic Disorder
Attention Deficit Hyperactivity Disorder
Ambien
Luminal, Solfoton
Amytal
Butisol
Nembutal
Seconal
Pentothal
Myidone, Mysoline
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CNS Stimulants
14
CNS stimulants
These drugs have a stimulating effect on the CNS. As a side effect, they decrease appetite and for
many years were used as appetite suppressants. Addiction and abuse were side effects of taking these
drugs. Furthermore, they are known as uppers and people hooked on them needed downers to
be able to sleep, causing more problems. Today, they are used mainly to treat hyperkinetic children
(attention deficit syndrome) where the child is unable to concentrate. It would seem that the drugs
would soup up the patient, but the opposite occurs.
These drugs are also used to treat narcolepsy, a condition where the patient lapses into momentary
sleep while sitting. This may occur as many as 20 times a day and is dangerous if it were to happen
while the patient is driving or operating machinery.
CNS Stimulants
Psychomotor:
Methylxanthines
Cocaine
Nicotine
Amphetamines
Methylphenidate
Psychomimetic:
Phencyclidine
Lysergic acid diethylamide
Tetrahydrocannabinol
Psychomtor Stimulants
Mechanism
Cocaine
Amphetamines
Dexamphetamine
Methylxanthines
Excitement
Euphoria
Decrease feeling of fatigue
Increase motor activity
Ester type Local anesthetic
Blockade of voltage sodium ion activated channel
Side effects Anxiety, depression, seizures, cardiac arrhythmias.
Therapeutic use: Attention Deficit Hyperactivity Disorder (ADHD)
Psychological and physical dependency addiction potential
Development of tolerance to euphoric and anorectic effects of chronic use.
Less tolerant to convulsions and toxic CNS effect
Amphetamine are classified as controlled drugs
Theophylline tea
Caffeine coffee
Theobromine cocoa
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CNS Stimulants
Psychomimetic stimulants
Mechanism
Hallucinogens
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Antipsychotics Drugs
15
Thioxanthenes:
*Chlorprothixene
*Thiothixene
Butyrophenones
*Haloperidol
*Droperidol
Typical
Diphenylbutyrylpiperidine
*Pimozide
Dibenzoxazepine
* Loxapine
Dihydroidolon
* Molindone
The schizophrenic individual is out of touch with reality, hallucinates, hears voices and exhibits
bizarre behaviour. These symptoms are only one aspect of schizophrenia. Other symptoms are:
social withdrawal, and an inability to communicate or to concentrate.
Schizophrenia Symptoms (Psychosis)
Positive Symptoms
Reality distortions
Delusions persecution
Grandiosity
Thought broadcasting
Thought insertion
Loose associations
Gestures
Mind-reading
Being controlled
Hallucinations
Auditory (most common)
Olfactory
Somatic
Visual
Negative Symptoms
Disorganizations
Disorganized speech
Incoherent speech
Tangentiality
Loose association
Blunted affect
Lack of expressed emotion
Poor eye contact and inattentiveness
Reduced spontaneity
Disorganized behavior
Agitation
Hostility
Assaultiveness
Uncooperativeness
Inappropriate sexual/social behavior
Inappropriate dress
Catatonia
Alogia
Lack of spontaneity of conversation
poor ability to concentrate
Avolation /apathy
Lack of interest in activities
No motivation, social withdrawal
Poor hygiene
Anhedonia
Loss of pleasure
Few recreational activates
Attentional impairment
Lack of ability to concentrate on tasks or
conversation
Antipsychotics
Muscarinic
receptor
receptors
Dopamine
Serotonin
receptor
H 1 receptors
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Antipsychotics Drugs
Antipsychotics
1st generation
Chlorpromazine
Prochlorpromazine
Haloperidol
Droperidol
Flupenthixol
Fluphenazine
Thioridazine
2 nd generation
Clozapine (Clozaril)
Olanzapine
Risperidone
Quetiapine
Zuclopenthixol
Therapeutic use
Side effects
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Antipsychotics Drugs
Therapeutic use
Antipsychotics
Side effects
EPS
Sexual Dysfunction
Anticholinergic Side effects
Tardive Diskinesia
Sedation
High weight gain
Low EPS
Low sexual dysfunction
Low anticholinergic side effects
High weight gain
Advantage
Disadvantage
Antipsychotics Tips
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Antipsychotics Drugs
Largactil
Compazine
Haldol, Serenace
Droleptan, Thalamonal
Depixol, Fluanxol
Modecate, Moditen, Motipress, Motival
Melleril
Stelazine, Porstelin
Clopixol
Clozaril
Zyprexa, Zyprexa Zydis
Risperdal, Risperdal Consta, Risperdal M-Tab
Seroquel XR, Seroquel
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Epilepsy
16
Epilepsy
Antiseizure drugs
Reduces NMDA
Receptor activation
Felbamate
Affect GABA
receptors
Reduce Ca2+
current through
T-channels
Phenobarbital
Ethosuximide
Carbamazepine
Diazepam
Phenytoin
Vigabatrin
Fosphenytoin
Topiramate
Lamotrigine
Tiagabine
Primidone
Gabapentine
Valproate
Valproic acid
Seizure: Abnormal electrical discharge from local areas and spread around the brain adjacent areas.
Condition like hypoxia, uremia, bacterial meningitis, genetic predisposition and drugs such as
cocaine, penicillin G, anticholinergics can produce seizure. Withdrawal from chronic use of alcohol,
barbiturates, benzodiazepines and most anti seizure medication can also lead to seizures.
Epilepsy: Epilepsy is a disorder of the brain characterized by recurrent and spontaneous seizures which
are self-limiting. Which usually recur unpredictably.
Convulsions: Involuntary contractions (abrupt) of voluntary muscles.
Seizures (Epilepsy) are characterized as: Partial and Generalized seizures.
Partial Most common (80%)
Comments
Simple partial
Seizures begin locally
Consciousness not impaired
With motor symptoms Jerking, lip smacking,
chewing motions
With autonomic symptomsSweating, pupil dilation,
With behavioral symptoms
Drug of choice
Drug of choice
1st
Carbamazepine
2nd Phenytoin
3rd Primidone
4th Gabapentin
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Complex partial
Generalized seizures
Absence seizures
(Petit mal)
Myoclonic seizures
Tonic-clonic seizure
(grand mal)
Status epilepticus
Epilepsy
Drug of choice:
1st Carbamazepine
2nd Phenytoin
3rd Phenobarbital
4th Valproic acid
Seizure Type
1st Choice
Generalized
Tonic-clonic
(Grand-mal)
Absence
(petit-mal)
Myclonic and Atonic
Partial (simple or complex) with
or without 2 generalization
Alternative therapy
Carbamazepine
Phenytoin
Valproic Acid
Ethosuximide
Valproic Acid
Valproic Acid
Carbamazepine
Phenytoin
Clobazam
Lamotrigine
Levetirecetam
Topiramitrate
- Same as above-Same as aboveGabapentin
Oxcarbazepine
Phenobarbital
Primidone
Valproic Acid
Vigabatrin
Carbamazepine (Tegretol)
Mechanism
Therapeutic use
Side effects
Management
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Epilepsy
Phenytoin (Dilantin)
Phenytoin decreases the sodium content of nerve in the brain and thereby decreases the
hyperexcitability of the cells that are involved in initiating seizures.
Mechanism
Phenobarbital (Luminal)
Primidone
Mechanism
Therapeutic use
Side Effects
Advantage
Disadvantage
Metabolite of phenobarbital
Increase seizure threshold by decreasing postsynaptic excitation by
stimulating postsynaptic GABA-A receptor inhibitor response as CNS
depressant.
Epilepsy
Sleeping and sedative drug
When combined with other drugs it is used in anxiety associated with
menopausal symptoms
Unwanted sedation
Skin rash (Phenobarbital)
Depression
Libido (Primidone)
Long t1/2
Metabolism inhibited by Valproic acid
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Tips
Epilepsy
Clobazam (Frisium)
Mechanism
Therapeutic use
Side effects
Management
Dose
Ethosuximide (Zarontin)
Mechanism
Therapeutic use
Side effects
Management
Gabapentin (Neurontin)
Mechanism
Therapeutic use
Side effects
Advantage:
Disadvantage
Tips
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Epilepsy
Lamotrigine (Lamictal)
Mechanism
Therapeutic use
Side effects
Advantage:
Disadvantage:
Comment:
Inhibit glutamate and aspartate release and blocks sodium channels and
prevents repetitive firing
Anticonvulsant
Rash,
CNS: Somnolence, dizziness, insomnia
Broad spectrum, no enzyme induction, some patients more alert
Metabolism inhibited by valproic acid.
Only available in oral form
Very expensive at high doses
Topiramate (Topamax)
Side Effects
Management
Advantage
Disadvantage:
Valproic Acid
Valproic acid and divalproex are related chemicals. Divalproex is a mixture of valproic acid
and sodium valproate. In the body they are metabolized to separate compounds, and both exert
anticonvulsant effects.
Mechanism
Reduces the propagation of abnormal electrical charge in the brain. It may
enhance GABA action at inhibitory synapses
Therapeutic use
Side Effects
Monitoring
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Epilepsy
Vigabatrin (Sabril)
Side Effects
Advantage
Disadvantages
Gamma-Aminobutyric Acid
Complete Blood Count
Liver Function Test
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Epilepsy
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Epilepsy
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17
Dementia
Definitions:
Dementia is a declined in mental ability that usually progresses slowly, in which memory, thinking,
judgment, and ability to pay attention and learn is impaired, and personality may deteriorate.
Delerium is a potentially reversible condition that usually comes so sudden. The person has diminished
ability to pay attention and often confused, disoriented, and unable to think clearly.
Alzheimers Disease
A progressive form of dementia. Alzheimers disease is a progressive, relentless
loss of mental function, characterized by degeneration of brain tissue, including loss of nerve cells and
the development of senile plaques and neurofibrillary tangles.
Alzheimers disease:
Alzheimer disease occurs due to in Acetylcholine (ACh). It is very rare among people younger than
60. It becomes more common with increasing age. It affects only about 1% of people aged 60 to 64,
but up to 30% of those older than 85.
Treatment: Acetylcholine agonist: Donepezil , Rivastigmine, Tacrine, Galanthamine
These drugs may improve cognitive function temporarily, but they do not slow the progression of
the disease.
Drugs for Alzheimers Disease
Reversible
Acetylcholinesterase inhibitor
Nonselective
Physostigmine
Tacrine
Galanthamine
Selective
Donepezil
Rivastigmine
(relatively selective
Donepezil (Aricept)
Mechanism
Acetylcholinesterase inhibitor
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Side effects
Dosage
Advantage
Drug and Drug
Interactions
Monitor
Dementia
Rivastigmine (Exelon)
Mechanism
Side effects
Therapeutic use
Dosage
Galanthamine
Mechanism
Therapeutic use
Side effects
Dosage
Dementia Tips
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Acetylcholine
Aricept
Exelon
Razadyne, Reminyl, Memeron
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Dementia
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Anti-Parkinsons Drugs
18
Anti-Parkinsons Drugs
Drugs to treat Parkinsons Disease
DA
precursor
L-dopa
Peripheral
dopa
decarboxylase
inhibitor
DA
agonist
MAO B
inhibitor
Anticholinergic
Selegiline
Benztropine
Pramipexole
Ropinirole
Anti-viral
drug
Carbidopa
Combination
Sinemet
COMT
inhibitors
Entacapone Amantadine
Ergots
Bromocriptine
Pergolide
Wearing off effects: After 3-4 years of treatment, drug loose its efficacy.
Parkinsons is a condition, which is characterized by muscle tremors at rest, muscle weakness,
emotionless facial expressions, increased sweating and salivation, disturbances of motion and
increased postural balance difficulty. These patients have a deficiency of the neurotransmitter,
dopamine, allowing acetylcholine to dominate.
Mechanism
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Anti-Parkinsons Drugs
Brain
Peripheral tissues
3-O-Methyldopa
3-O-Methyldopa
Tolcapone
Tolcapone
Striatal neuron
Ldopa
Levodopa
Ldopa
Carbidopa
Dopamine
Dopamine
Pergolide and other agonists
D1 and D2
receptors
Dopamine
Selegiline
Dihydroxyphenylacetic
Acid (DOPAC) + H2O2
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Anti-Parkinsons Drugs
Levodopa preparations
Dyskinesias
Psychosis, confusion,
agitation, hallucinations,
delusions
Orthostatic hypotension
Management Strategies
Add a dopamine agonist
Switch to Sinemet CR
Administer levodopa more frequently
Switch to Sinemet CR
Add or increase dose of a dopamine agonist
Switch to a different dopamine agonist
Decrease dose of levodopa or dopamine agonist
Switch to a different dopamine agonist
Decrease dose of levodopa or dopamine agonist
Discontinue anticholinergic drugs, amantadine, selegiline
Can be caused by anti-parkinsonian medications, other medications
and by Parkinsons disease itself. A lying and standing blood pressure
should be checked at each visit
Decrease dose of levodopa or dopamine agonist, increase gradually
Add salt to diet
Add domperidine or fludrocortisone
Take levodopa with food
Increase dose of levodopa or dopamine agonist gradually over several
weeks
Benztropine (Benztropine)
Therapeutic use
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Side effects
Contraindications
Counseling
Anti-Parkinsons Drugs
Antiviral Agent
Indicated in drug induced PD because levodopa will reverse the beneficial effect of the drug.
Side effects: edema of ankles.
Amantadine (Symmetrel)
Therapeutic use
Drug-Drug interaction
Side Effects
Entracapone (Comtan)
Mechanism
Side Effects
Bromocriptine (Parlodel)
Mechanism
Therapeutic use
Drug-Drug
interaction
Contraindication
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Side Effects
Anti-Parkinsons Drugs
Pergolide (Permax)
Mechanism
Therapeutic use
Pramipexole (Mirapex)
Mechanism
Therapeutic use
Side Effects
Monitoring
Selegline (deprenyl)
Selective inhibitor of MAOB at low doses. Indicated in early stages of PD and as an adjunct to
levodopa in patients who exhibit deterioration in their response.
SE: insomnia, confusion, hallucinations, anorexia, diarrhea, increase dyskinesia,
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Anti-Parkinsons Drugs
Motilium
Tasmar
Benztropine
Symmetrel
Comtan
Parlodel
Permax
Mirapex
Deprenyl
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Anesthetics
19
Anesthetics
Local Anesthetics classification
Amides Type
Esters Type
Long duration
Tetracaine
Medium Duration
Cocaine
Short duration
Procaine
Long duration
Bupivacaine
Ropivacaine
Surface-active
Benzocaine
Cocaine
Medium duration
Lidocaine
Intravenous
Inhaled
Gas
Nitrous oxide
Ether (diethyl ether)
Volatile liquid
Halothane
Enflurane
Isoflurane
Barbiturate
Thiopental
Miscellaneous
Propofol
Dissociative
Ketamine
Benzodiazepines
Midazolam
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Anesthetics
Anesthetic Tips
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Anesthetics
Fluothane
Forane
Ethrane
Sevorane, Ultane
Suprane
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Anesthetics
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Opioids
20
Opioids
Opioid Analgesics Classification
Mixed agonist antagonist
Pentazocine
Nalbuphine
Agonists
Strong
Morphine
Heroin
Meperidine
Methadone
Other agents
Fentanyl
Levorphanol
Moderate
Codeine
Oxycodone
Hydrocodone
Antagonists
Naloxone
Naltrexone
Weak
Propoxyphene
Opioids are used for moderate to severe pain of trauma, post-surgical pain, pain associated with myocardial infarction and pain of terminal illness. Physical and psychological dependence (addiction)
can occur when opiates are administered for some time. When tolerance develops, the patient requires increasing amounts of drug to treat pain. All opioids are habit forming, however, titrated doses
tolerate pain, the risk of addiction is slight.
Opioid receptors and neurotransmitters
Functions
Analgesia-Supraspinal
Analgesia- Spinal
Receptors
Mu (m)/delta (d)
+
+
Respiratory depression
Sedation
Euphoria
Dysphoria
Physical dependence and tolerance
Constipation
++
++
+
+
+
Kappa (k)
+
+
+
+
+
+
Opiate
Receptors
Mu (m)
Kappa (k)
Delta (d)
Neurotransmitters
b-Endorphin
Dynorphin
Enkephalins
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Spinal cord
Opioids
Hypothalamus
Limbic system
Periphery
Immune cells
Opioid Analgesics
Therapeutic use
Side Effects
Overdose
Drug-Drug
interactions
Addiction potential
All opioids
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Oxycodone
Meperidine
Pentazocin
Methadone
Butorphanol
Nalbuphine
Naloxone
Naltrexone
Nalmefene
Opioids
Opioids Tips
Dyspnea is
Avoid opioids in head trauma patients
Morphine active metabolite
Analgesic activity of morphine
Codeine is metabolized by
Patient taking Tylenol # 3 + hydromorphone
Methadone is used for
Morphine over dose symptoms
Which opioids has highest addiction potential
In Angina pain what opioids is used
Drugs used to treat opioids withdrawal symptoms
Opioid antagonist
A patient developed seizure after initiating opioids therapy, which opioids would be
responsible
Opioids least used in
Pinpoint pupil is opioids
Patient on methadone and has already missed dose for three consecutive days, what is
appropriate suggestion
Avoid opioids with MAOI
Opioid induced constipation treated by
Enkephalins are
A patient is on opioids, having constipation, started taking psyllium laxatives but no
improvement, you advise him
How to apply fentanyl transdermal patch
Allergic to morphine can use
What is the antidote for an OxyContin overdose?
Name the antagonist of choice for an opiod overdose.
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Opioids
Talwin, Talwin NX
Nubain
Narcan, Narcan Neonatal
Depade, ReVia, Vivitrol
Demerol, Meperitab
Diskets, Dolophine, Methadose
Actiq, Duragesic, Fentora, Sublimaze
Levo-Dromoran
Endocodone, Eth-OxyDose, OxyContin OxyFast,
Hycodan, Hydromet, Hydropane, Mycodone, Tussigon
Darvon, Darvon-N 100, Darvon-N,
Depade, ReVia, Vivitrol
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21
Analgesics
Acetic acid
derivatives
(including
indole
derivatives)
Fenamates
COX-2
inhibitors
Napthylalkanoes
Celecoxib
Meloxicam
Valdecoxib
Floctafenine
Mefenamic acid
Diclofenac potassium
Diclofenac sodium
Etodolac
Indomethacin
Ketorolac tromethamine
Sulindac
Tolmetin sodium
Salicylic acid
derivatives
Oxicams
Nabumetone
Acetaminophen
Propionic acid
Derivatives
Meloxicam
Piroxicam
Tenoxicam
Fenoprofen Calcium
Flurbiprofen
Ibuprofen
Ketoprofen
Naproxen sodium
Oxaprozin
Tiaprofenic acid
Age > 65
Anticoagulants or oral glucocorticoids
History of peptic ulcer disease
History of upper GI conditions
Comorbid medical conditions
Misoprostol
PGE1 analog
Increases bicarbonate secretions
Increase mucus secretions
Proton pump inhibitor (Omeprazole,lansoprazole)
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Recommendation
ASA
Salicylate allergies
Acetylsalicylic Acid
Mechanism
Therapeutic use
Side Effects
Drug-drug
interaction
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Contraindication
Monitoring
Butalbital
Therapeutic use
Side Effects
Management
Analgesic
Dependence
Additive sedation with other CNS depressants (e.g. alcohol)
Naproxen
Therapeutic use
Side Effects
Management
Ketoprofen
Mechanism
NSAID
Therapeutic use
Side Effects
Drug-drug
interaction
NSAIDs and ASA will increase the risk of bleeding with Ketoprofen
Lithium, digoxin, and methotrexate may raise blood levels with
Ketoprofen.
Alcohol may increase risk of stomach disorders
Quinolone antibiotics may increase the risk of seizures
Contraindication
Diclofenac
Mechanism
Therapeutic use
Side Effects
GI disorders
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Drug-Drug
interaction
Contraindication
Monitoring
Piroxicam
Therapeutic use
Side Effects
Drug-drug
interaction
Contraindication
Monitoring
NSAIDs Tips
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Misoprostol
Sucralfate
Ranitidine
Omeprazole
Ibuprofen
Butalbital
Naproxen
Ketoprofen
Diclofenac
Piroxicam
Cytotec
Sulcrate
Zantac
Losec
Advil, Motrin
Fiorinal with ASA +codein
Naprosyn, Anaprox, Novo-Naprox
Apo-Keto, Noveo-Keto, Orudis SR
Volraren, Cataflam, Solaraze
Apo-Piroxicam, Feldene, Novo-Pirocam
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Autocoids
22
Autocoids
Autocoids (Local hormones): Chemical mediators that the body releases as a response to pathogens
or noxious substances. Produced in the body and has profound pharmacological effects.
Classification of autocoids
Amines type Histamine, Serotonins
No real clinical application in the treatment of diseases however antihistamines are of great
importance.
Endogenous Peptides
Prostaglandins, Prostacyclin, Thromboxane, Leukotrienes, bradykinins
Site of production for endogenous peptides are GIT, kidneys, lungs, pancreas and uterus.
Histamines
Histamine H1-receptor blockers
Particularly
Diphenhydramine,
promethazine
Anti
Cholinergic
(muscarinic)
receptor
Particularly
promethazine
Alpha
Adrenergic
receptor
Dopamine
receptor
Particularly
cyproheptadine
Serotonin
receptor
Histamine H1
receptor
Histamine H2
receptor
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Autocoids
5HT1a
Agonist
Buspirone
(BuSpar)
5-HT1b/1d
Agonist
Triptans
Sumatriptan
Rizatriptan
Zolmitriptan
Naratriptan
5-HT2
5HT3
Ergotamine (DHE)
Antagonist of 5-HT2a
Atypical antipsychotic
Olanzapine, clozapine,
and risperidone
5HT4
Antagonist
Ondansetron
Alosetron
Fabesetron
Ramosetron
Agonist
Cisapride
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Autocoids
Serotonin Agonist
5HT1D/1B receptor agonist
TRIPTANS (all are indole derivatives)
Sumatriptan
Rizatriptan
Naratriptan
Zolmitriptan
Almotriptan
Frovatriptan
5HT1D receptor agonist side effects: Feeling of warmth, dizziness, tightness or heaviness in the chest,
rarely patient may experience chest pain.
5HT4 agonist
Cisapride (a benzamide)
Tagaseride (indole derivative)
Ergotamine-serotonin partial agonist: Ergot alkaloids have agonist and antagonist properties
Serotonin Antagonist
5HT3 receptor antagonist
Ondansetron (indole derivatives),
Granisetron (benzimidazole derivative)
Ergot alkaloids and derivatives with antagonist/partial agonist activity include:
Ergonovine
Dihydroergotamine (DHE)
Methysergide
Bromocriptine
Ondansetron side effects: Constipation, headache, dizziness and Granisetron--diarrhea
Prostaglandin
Prostaglandin chemical classification
Prostaglandin has been classified based presence and absence of keto or hydroxyl groups
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Autocoids
at 9 and 11. Subscripts relate to the number of double bond present in aliphatic chains
Platelet aggregation, Relax bronchial and GI smooth muscles, Relax smooth muscles, Inhibit gastric
acid secretion, Pain, Edema, Inflammation
Prostaglandin analogs
PGF2
PGI2
Latanoprost
Epoprostenol
Thromboxane A2
Branchial &
Branchial &
Branchial &
smooth
smooth
smooth
muscle
muscle
muscle
dilatation
constriction
dilatation
Pharmacological actions of prostaglandins
Blood vessels
dilatation
Platelet
aggregation
PGE2
PGE1
Misoprostol
Alprastadil
Dinoprostone
TxA2
Inhibit
aggregation
Corticosteroids
Receptors
PGI2
Actions
Vasodilation
Decrease platelets aggregation
Maintaining renal blood flow
PGE1
Leukotrienes
Lipoxygenase
Arachinodic acid
Membrane
phospholoipids
PGE2
Pyrogen elevate PGE2
Contraction of uterus
PGF2
Bronchoconstriction
Contraction of uterus
PGD2
Vasodialtion
Inhibition of platelets aggregation
TXA2
Prostaglandins G
Hydroperoxidase
PGH2
Dipyridamole
Prostacyclin (PGI2)
Thromboxane A
Platelet aggregation
Vascular tone
Uterine tone
Paltelet aggrega
Vascular tone
Vascular tone
Bronchial tone
PGE Analogs
Cyclooxygenase
Uterine tone
Bronchial tone
PGE1 analogs
Misoprostol (Cytotec): is used for prevention of NSAID induced GI ulcers.
Chemically it is ecosonides
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Autocoids
Leukotrienes
Physiological functions
LTC and LTD antagonists
Play important role in numerous
physiological functions.
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Autocoids
Montelukast (Singulair)
Similar profile to that of Zafirlukast.
Can be used in children over 2-year age
Montelukast may be taken without regard of food.
Available as chewable tablet (once daily in the evening).
Administer granules directly into mouth or mix with teaspoon of cold or room temperature
applesauce, carrot, rice or ice cream.
Do not take aspirin or NSAIDs while on this medication.
Cytotec
Caverject, Prostin VR pediatrics
Prostin E2, Prepidil, Cervidil
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Latanoprost
Travoprost
Bimatoprost
Unoprostone
Carboprost
Epoprostenol
Zafirlukast
Montelukast
Autocoids
Xalatan
Travatan
Lumigan
Rescula
Hemabate
Prostcyclin, Flolan
Accolate
Singulair
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Autocoids
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23
There are two types of diabetes mellitis, Type I and Type II. For Type I diabetes, patients need insulin
injections. Type I diabetes is known as insulin dependent diabetes mellitis (IDDM). It usually begins
in young people under 40 and of normal weight. Onset is sudden and severe; ketones are found in the
blood and urine.
Types of Insulin
Ultra rapid
Rapid
Intermediate
Long-acting
Ultralente
Protamine
Zinc
Insulin lispro
Glargine
Types of insulin are categorized by their onset of action, and these relative positions hold true for
their effectiveness and their duration of action as well.
NPH
Lente
Regular
Semilente
Sulfonylureas
1 Generation
Tolbutamide
Tolazamide
Chlorpropamide
st
Nonsulfonylurea insulin
secretagogue
Meglitinides
Repaglinide
Neglitinide
Biguanide
Metformin
2 Generation
Glyburide
Glipizide
Glimepiride
nd
-glucosidase
inhibitor
*Acarbose
Thiazolidinedione
*Pioglitazone
*Rosiglitazone
Very short
(fastest)
iv form
Onset
(hours)
Peak
(hours)
5-10
min
30-40
min
Usual Effective
Duration of Action
(hours)
2-3 h
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Regular (R)
(suitable for iv dose). Both
human and animal source
NPH (N) Isophane
Amorphous precipitate of
insulin w/ zinc ion acetate
buffer
Ultralente
Zinc suspension crystals
in acetate buffer contain
large particles that are slow
dissolve
Rapid (short)
-1 h
Subcutaneous
Or iv (in emergencies)
Intermediate
2-4 h
Semilente (30%)
1-3 h
5-7 (dose-dependent;
may be longer)
6-10 h
14-18 h
not suitable for iv
dose
Long
(70%)
Slowest onset of
action but Longest
hypoglycemic effect.
18-28 h
Insulin
Oral
hypoglycemics
4-5 h
Diagnosis (Diabetic)
1-Symptoms
2-Random Blood sugar levels > 14.0 mmol/L
3-Fasting Blood sugar levels > 11.1mmol/L
4-Post prandial BSL > 14.0 mmol/L
5-Glycosylated hemoglobin (HbA1c) > 7%
Normal Blood sugar levels (BSL)
Fasting BSL 5-6 mmol/L
Random BSL 11.1 mmol/L
Post prandial 14.0 mmol/L
HbA1C is 4 - 6%
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Oral antidibetics
Hypglycemic drugs: Sulfonylureas, Meglitinides
Antihyperglycemics: Biguanides, Thizolinediones
Medication
Mechanism
Side effects
Contraindications
Sulfonylureas
Glyburide (DiaBeta)
Chlorpropamide
(Diabinese)
Gliclazide
Stimulate release of
endogenous insulin
Hypoglycemia
Nausea
GI discomfort
Weight gain
Meglitinides
Repaglinide (Gluconorm)
Stimulate release of
endogenous insulin
(rapid-acting, better
post-prandial glucose control): Must
take before meals,
because
Decrease postprandial glucose levels.
1-Reduce gluconeogenesis,
2-increase glucose
utilization
Hepatic or renal
Impairment
Chlorpropamide not a good
choice in elderly (long half
life)
Not used in Type 1 DM
Pregnancy
It is important to Avoid
alcohol, it can cause disulfiram type reactions.
Hypersensitivity
Diabetic Ketoacidosis
(DKA)
Not indicated in type I diabetes
Contraindicated Pregnancy
Biguanides
Metformin (Glucophage)
Lactic acidosis, in
hepatic and renal disease patients
GI discomfort Anorexia, nausea, diarrhea, metallic taste
Due to anorexia
caused by metformin
this drugs used for
weight loss.
Hepatic or renal
Impairment
Alcoholism
Advanced age
Previous lactic acidosis
DOC in obese
Therapeutic uses also include: To treat Infertility
For weight loss
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Thiazolidinediones
Rosiglitazone
(Avandia)
Pioglitazone
(Actos)
Glucosidase
Inhibitors
Acarbose
(Prandase)
1-Increase peripheral
insulin sensitivity,
2-Reduce gluconeogenesis
Flatulence
Abdominal
Cramping, nausea
Diarrhea.
Decrease metformin
bioavailability.
Liver disease,
Congestive heart failure
(CHF)
Gender selective Resume
ovulation in previously anovulatory women (example:
polycystic ovarian syndrome). Increase chances
of pregnancy, if insufficient
contraception not used.
May be taken with or without food
Hypersensitivity,
DKA,
Inflammatory Bowel
Disease (IBD)
Pregnancy & Lactation,
Liver cirrhosis
With first bite of meal.
Skip the dose if you skip
meals.
Diarrhea
Steatorrhea (Fatty
stools)
Abdominal discomfort
Oily leakage
Chlorpropamide (Diabinese)
Mechanism
Therapeutic use
Contraindications
Side Effects
Repaglinide (Gluconorm)
Mechanism
Therapeutic use
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Contraindications
Side Effects
Hypersensitivity
Diabetic Ketoacidosis (DKA)
Hypoglycemia(less frequent than with sulfonylureas)
Gliclazide (Diamicron)
Mechanism
Therapeutic use
Side Effects
Drug-drug
interaction
Contraindication
Monitoring
Stimulates the production and secretion of insulin from the islet cells of
pancreas.
Treat adult (maturity-onset) diabetes mellitus
Faintness and confusion
Weakness and tremor
Sweating, constipation and diarrhea
Corticosteroids, estrogens, diuretics, rifampin, other drugs may reduce
the effect of gliclazide.
Alcohol
Not recommended to pregnant, lactating mothers, and children.
Regular testing of sugar levels in the blood and urine is required.
Periodic assessment of the eyes, heart, and kidneys may also be
advised.
Metformin (Glucophage)
Mechanism
Therapeutic use
Side Effects
Contraindication
Drug-Drug
interactions
Does not stimulate secretion of insulin like sulfonyl ureas. Rather decreases
hepatic glucose output by inhibition of gluconeogenesis.
Reduces LDL, VLDL, cholesterol levels
To control hyperglycemia
For the treatment of obese diabetic patients.
No weight gain side effect.
Preferred in obese patients
Lactic acidosis (in hepatic or renal failure patient), metallic taste, N, D and
anorexia
Contraindicated in renal and hepatic impairments.
During pregnancy
Patient with history of Lactic acidosis, irrespective or precipitating factors
Alcohol potentiates effects, avoid alcohol
Potentiates other oral hypoglycemics
Rosiglitazone (Avandia)
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Mechanism
Therapeutic Effects
Pioglitazone (Actos)
Mechanism
Therapeutic use
Contraindications
Side Effects
Drug-Drug
interactions
Acarbose (Prandase)
Mechanism
Therapeutic
use
Drug-Drug
interaction
Dose
Side Effects
Monitoring
Orlistat (Xenical)
Mechanism
Therapeutic use
Drug-Drug
interaction
Dose
Side Effects
Blocks the action of stomach and pancreatic enzymes (lipases) that digest fats,
so fats and other fat soluble vitamins ADEK are not absorb in the body but pass
through and excreted in the feces.
Reduces fats stores and produce weight loss.
Orlistat increases blood levels and toxicity of pravastatin
120-360mg daily
Diarrhea, abdominal discomfort, oily leakage
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Acarbose mechanism
Orlistat mechanism
Difference between glyburide and glimepride
Antidiabetic drugs taken before or after meals
Insulin works on cell wall
The antidiabetic drug side effect of anorexia
Anticholesterol DOC in diabetic patient
Metformin monitoring
Which antidiabetic drugs are not used in type I DM
What antidiabetic drug of choice in pregnancy
If patient has admitted in surgical ward and her blood glucose levels high, what is drug of
choice
Which of the available forms of insulin should be used IV to correct excessive preprandial
glucose concentrations?
BMI = weight in Kg/ (height in m)2
DiaBeta
Diabinese
Gluconorm
Avandia
Actos
Prandase
Xenical
Orinase, Diabinese, Insulase
Diamicron
Starlix
Glucophage
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Thyroids Disorders
24
Thyroid disorders
Drugs Used In Thyroid Disease
Hypothyroids
Thyroxine (T4)
Dessicated thyroid
hormone.
Synthroid
Thioamides:
Methimazole
Propylthiouracil
Symptoms
Treatment
Monitoring
Pregnancy
Hyperthyroids
Triidothyronine (T3)
Iodide
Lugol solution:
(KI+I)
131
Ipodate
Hypothyroidism
Sensitivity to cold
Constipation
Bradycardia
Weight gain
Dry flaky skin
Coarse hair
Slowed speech
Puffy face, hands, feet
Hearing loss
Decreased libido
Slow return of deep tendon
reflexes
If untreated myxedema and coma
will develop
Thyroxin (T4)
Triiodothyronine (T3)
Hyperthyroidism
Intolerance to heat
Diarrhea
Tachycardia
Weight loss
Nervousness
Heart palpitation
More common in pregnancy
Thioamides
Methimazole
Propylthiouracil
Iodide
Radioactive iodide
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Thyroids Disorders
Drug-drug
interaction
Over dose
Monitoring
Methimazole (Tapazole)
Thioamides
Mechanism
Pharmacokinetics
Similarities between
Carbimazole and
Methimazole
Do not prevent the uptake of I by the gland they inhibit the synthesis of
T3 and T4 by inhibiting the iodination of tyrosine in the thyroglobulin
Blocks the coupling of the iodo thyroxine
Inhibits the conversion of T4 to T3
Therefore thyroid hormone synthesis is decreased.
Obvious effects are very slow since it takes 3-4 weeks before the
hormone levels show a decrease
Well absorbed,
Slow excretion
t1/2 is 6 hours
Both drugs accumulate in the plasma
Both cross the placental barrier and can accumulate in the thyroid gland
of the fetus
Propylthiouracil (Propyl-Thyracil)
Mechanism
Therapeutic use
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Side Effects
Thyroids Disorders
Disadvantage
Contraindication
Monitoring
Pharmacokinetics
Jaundice
Sore throat and fever
Calcitonin is stimulated by
TSH is secreted from
In treatment of hypothyroidism with T4 have effect on
Hypothyroidism is monitored by
DOC in pregnancy for hyperthyroidism
Hypothyroidism symptoms
Hyperthyroidism is
Hypothyroidism is
T4 metabolized to T3 by deiodinase enzyme
Discontinue antithyroid if patient notice even a single rash
Sweating is symptom of
Lugol solution is?
Lugol solution can stain.
Why is it beneficial to add propranolol to a drug regimen of a patient diagnosed with
hyperthyroidism?
Tapazole
Propyl-Thyracil
Drug of Choice
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Thyroids Disorders
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25
Testes
Progesterone
Norethidrone
Norgestrel
Norethynodrel
Norgestimate
Desogestrel
Testosterone
Anti-testosterone drugs
Included in this category are: androgens (male sex hormones), estrogens (female sex hormones) and
progestins. These chemicals are needed for the development, maintenance and function of the sexual
organs and are necessary for normal pregnancy to occur, be maintained and for birth
Clinical Uses for Various Estrogen Preparations
Palliative treatment of
advanced prostate cancer
Diethylstilbestrol
Estrogen
Conjugated estrogens
Estradiol
Estradiol transdermal
Estrogens are female sex hormones that are used primarily to decrease bone loss and to treat the
symptoms of menopause. Estrogen is used to reduce or prevent osteoporosis in susceptible women.
Estrogens decrease the frequency and severity of hot flashes as well as the dryness in the vagina that
many post-menopausal women experience.
Estradiol Exist in body in equilibrium with estrone
Estriol
Estrone
Ethinyl estradiol 17 alpha estradiol
Mestranol
Quinestrol used for estrogen replacement therapy (HRT)
Diethylstilbestrol Non steroidal synthetic estrogen (stilbene derivatives)
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Therapeutic use
Side effects
GI Nausea and vomiting are the most common, weight gain, diarrhea
CNSHeadache, Breast tenderness
CV Edema, Hypertension, stroke, MI, Increased risk of thromboembolic
diseases
Contraindicated in
Antiestrogens
Mechanism
Therapeutic use
Tamoxifen
Clomiphene
Inhibit or modify the action of estrogen
These drugs are non-steroidal antiestrogenic compounds equally effective in
oral or injection.
Tamoxifen Breast cancer
ClomipheneFertility drugs
Tamoxifen
Mechanism
Indication
Side effects
Clomiphene (Clomid)
Mechanism
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Therapeutic use
Contraindication
Side effects
Progestins
Progestins are female sex hormones that may be used with estrogens in oral contraceptive pills,
hormone replacement therapy, and treat menstrual irregularities, and as cancer treatment.
Classification of progestins
Two types of progestins
17-alpha hydroxyprogesterone
A. Medroxyprogesterone acetate
B. Megestrol aceta
17-alpha ethinylandrogens (more potent)
A. Norethindrone
B. Norethynodrel
Commonly used in OCs
Potent oral activity
More lipid soluble
Less first pass metabolism
Mechanism Progestins are produced in males from testes.
Adrenal cortex produced progestins in males and females.
Progestins in females promote the development of a secretor endometrium that
can accommodate implantation of newly formed embryo.
The high level of progestins produced in second half of menstrual cycle inhibits
the production of gonadotropins and thereby further ovulation.
Therapeutic Major clinical use in contraception, generally used with estrogen.
use
Not widely used as alone because of its rapid metabolism results in low
bioavailability.
Progestins are indicated in uterine bleeding, dysmenorrhea, suppression of
postpartum lactone, and endometrium cancer.
Endometriosis
Side Effects Edema
Depression
Menstrual irregularities (breakthrough bleeding, amenorrhea)
Androgen like progestins can increase LDL and HDL ratio cholesterol, weight
gain and edema,
Hirsutism, and acne can cause thrombophlebitis (inflammation of wall of vein)
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Therapeutic use
Side Effects
Androgens
Testosterone is the androgen that leads to the development of male secondary sexual characteristics
and maintains the male reproductive system.
Androgens are used to treat delayed puberty in males who do not develop normal testicular function.
They are also used illegally by athletes to build muscle mass. They are very dangerous when used for
this as they may lead to aggressive behaviour, and may cause liver and/or brain tumours and death.
Androgens
Danazol
Nandrolone
Stanozolol
Fluoxymesterone
Mechanism
Therapeutic use
Side effects
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Antiandrogens- Finasteride
Mechanism
Therapeutic use
Side effects
Dose
Contraindication
Finasteride
Dutasteride
Flutamide
Cyproterone acetate
Inhibit the synthesis of androgen.
Finasteride: steroid like drug approved for BPH treatment.
Finasteride: inhibits the 5-alpha reductase: Competitive and specific
inhibitor of type II 5-alpha reductase
Indicated in BPH, and to treat men who have lost scalp hair.
Decrease libido.
Sexual dysfunction
Breast tenderness
Hirsutism
Hypersensitive reactions like rashes, pruritic, swelling face and lips
Testicular pain
5mg for BPH treatment
1mg daily for 3 months for hair growth in men
Not indicated in woman and children. Woman should not handle or
break tablet when they are pregnant.
Finasteride may cause external genitalia abnormalities in male fetus.
ACTH is secreted by
Example of antiandrogenic drug
What partial antiestrogen cause hot flushes
Metformin + glyburide may cause
Increase in cortisone cause (Hypercorticoids)
Decrease in cortisone cause (Hypocorticoids)
Glutathione is
Diabetic Ketoacedosis (DKA) mainly occurs in
During ovulation increase of
Corpus luteum is stimulated by
Purpose of frequent glucose level monitoring
What steroidal hormone structure have phenolic ring
Decrease in cortisone cause
Aldosterone secreted from
Cortisone is secreted form
Hoshimoto disease
Example of antithyroid drugs
Fineseride (Proscar), Dutasteride (Avodant) is
Vitamin D3 acts as
Myxedema is malfunction of
The effect of vasopressing on kidney
Deficiency (absence) of Antidiuretic Hormone (ADH) or vasopressin cause Diabetes Insipidus
(DI)
Glutathione protects
The endocrine gland plays important rule in calcium metabolism
The major factor that controls Na excretion in kidney
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Nolvadex, Soltamox
Clomid
Mifeprex
Danocrine
Durabolin, Kabolin
Winstrol
Halotestin, Android-F, Ora-Testryl.
Avodart
Eulexin
Diane
Avodant
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Adrenal Corticosteroids
26
Adrenal Corticosteroids
The adrenal hormones, or corticosteroids, are drugs with powerful anti-inflammatory effects. These
are used for replacement therapy in conditions such as, Addisons disease, a condition of adrenal
insufficiency. In replacement therapy, the adverse effects are minimal since hormones are being
replaced and are not added to those already in the body.
Corticosteroids are used for their anti-inflammatory, anti-allergic and anti-stress effects. Prednisone
is used as replacement therapy and also for its anti-inflammatory effects in many conditions, such as
arthritis, allergies and asthma.
Glucocorticoids
Classification
Short acting (8-12 hour)
Intermediate acting (18-36
hours)
Long acting (1-3 days)
Mechanism
Side Effects
Hydrocortisone
Cortisone
Prednisone
Prednisolone
Methylprednisolone
Triamcilone
Betamethasone
Dexamethasone
Paramethasone
Promote normal intermediately metabolism
Increase resistant to stress
Alter blood cell levels in plasma
Anti-inflammatory action by inhibiting IgE
High doses stimulate gastric acid and pepsin production and may
cause peptic ulcers.
Chronic use causes sever bone loss (Due to decrease in calcium)
and myopathy leads to weakness
Concentration of topical Glucocorticoids depends on site of use
on the body.
Take with food
Should not be stopped suddenly, taper off or gradually decrease
dose.
Diabetic drugs glyburide, chlorpropamide, glipizide,
tolbutamide, and tolzamide.
Can rise blood sugar noticeably
Monitor blood sugar levels
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Therapeutic use
Side effects
Adrenal
Corticosteroid
Corticosteroid
biosynthesis
inhibitors
Mechanism
Indications
of Adrenal
corticosteroids
Adrenal Corticosteroids
Cortisone
Hydrocortisone
Betamethasone
Beclomethasone
Prednisolone
Prednisone
Triamcilone
Methylprednisolone
Ketoconazole
Spironolactone
Mifepristone
Metyrapone
Aminoglutethimide
For anti-inflammatory corticoids: Glucocorticoids effects on the distribution,
concentration, and function of leukocytes. These include decrease in
concentration of lymphocytes T and B cells) and increase in concentration of
neutrophils.
Decrease basophils, eosinophils and monocytes, and inhibition of the ability
of leukocyte and macrophages to responds mitogen and antigen.
The above Inhibitory response also results in reduce the amount of histamine
release from basophils to inhibit kinins.
Indications of adrenal corticosteroids
Addisons disease (caused by dysfunction of adrenal cortex)hydrocortisone.
Cushing syndrome (caused by hypersecretion of glucocorticoids that is due
to excess secretion of corticotropin by anterior pituitary to adrenal tumor.
dexamethasone test is used in diagnosis.
Congenital adrenal hyperplasia (CAH)results from enzyme defects
administration of sufficient corticosteroids.
Indicated in inflammatory symptoms of rheumatoid arthritis, osteoarthritis,
skin condition. Redness, swelling, heat, and tenderness that commonly treated
by adrenal corticoids
Indicated in treatment of allergies.
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Adrenal Corticosteroids
Formulations
Systemic:
IM Cortisone, triamcinolone, desoxycorticosterone
IV and IM Dexamethasone, hydrocortisone, methylprednisolone,
prednisolone.
Inhaled Aerosol Beclomethasone, flunisolide, fluticasone, triamcinolone
Topical Hydrocortisone, beclomethasone, dexamethasone, triamcinolone,
Oral: All corticosteroids can be administered orally.
Long term use Osteoporosis --> is due negative calcium balance
Side effects
Increase risk of infection due to impaired wound healing and immunosuppression
associated with Diabetes due to hyperglycemia SE
oral steroids
Increased appetite can cause weight gain
Hypertension is due to increase water retention (Edema)
Peptic ulcers
Euphoria
Psychosis
Immunosuppression due to suppression of IgE.
Adrenocorticoids Tips
Cortone
A-hydroCort, Ala-Cort, Ala-Scalpt, Anu-Med HC
Diprosone, Diprolene
Beclovent, Beconase AQ, Beconase, Qvar , Vancenase
AK-Pred, Bubbli-Pred, Econopred, Econopred Plus
Deltasone, Predone, Sterapred, Sterapred DS
A-Methapred, Cortimed, Depmedalone, Depo-Medrol, Medralone
Extina, Kuric, Nizoral Shampoo, Nizoral, Nizoral A-D, Xolegel
Aldactone, Spirono
Mifeprex
Metopirone
Aminoglutethimide
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Adrenal Corticosteroids
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Oral Contraceptives
27
Oral Contraceptives
Oral contraceptives (birth control pills) are combinations of estrogen and progestins.
The combination preparations may be monophasic, biphasic or triphasic. They contain various
estrogens and progestins. Some common ones are listed:
Drugs that Causes Of
OC Failure
Contraindications
Precautions
Starting Hormonal
Contraceptives
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Starting Hormonal
Contraceptives
Oral Contraceptives
Starting Depo-Provera: im
Should be injected during the first 5 days of menstrual cycle rule out
pregnancy
Repeat injection q12 weeks - effective for up to 14 wks
Oral Contraceptive
Deep Veinthrombosis
Break Through Bleeding
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Oral Contraceptives
Alesse
Brevicon
Demulen
Diane-35
Ortho-Cept
Marvelon
Ortho
Min-Ovral
Triphasil
Synphasic
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Oral Contraceptives
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Osteoarthritis
28
Osteoarthritis
Osteoarthritis
Pain Therapy,
Topical
Synovial Fluid
Replacement
Corticosteroids
Capsaicin
Methyl salicylate
Menthol
Triethanolamine
salicylate
Hylan G-F 20
Hyaluronic acid sodium
Sodium hyaluronate
Betamethasone valerate
Cortisone acetate
Dexamethasone
Dexamethasone sodium
phosphate
Methyl prednisolone
acetate
Prednisolone
Triamcinolone
Triamcinolone diacetate
Glucocorticoids
Antigen
Viscous supplements
Intraarticular injections
NSAIDs
Activation of
macrophages
Prostaglandins
Methotrexate
Activation
of T cells
IL-2
TNF
Activation of
B cells
Induction
of cytotoxic
T cells
Production of
autoimmune
antibodies
Cytokines
Joint
inflammation
Synoviocyte
proliferation,
Bone and
cartilage
destruction
IgRF
complex
es
Diclofenac (Voltaren)
Therapeutic use
Side Effects
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Drug-Drug
interaction
Contraindication
Monitoring
Osteoarthritis
Osteoarthritis Tips
Allergic to aspirin
Aspirin use in children with flu symptoms can cause
Peptobismol (Bismuth subsalicylate) can cause Rye syndrome in childrem.
Ibuprofen is safe in children under 12 years (No Rye syndrome)
Misprostol is
Azotemia
Topical pain relievers
Hylorunan injections (synovial fluid replacement) act as viscous supplement given
Misoprostol is
What type of exercise in osteoarthitis
Acetaminophen is least used in
Risk factors for renal toxicity associated with NSAIDs and COX II inhibitors include .
Counseling of Capscicin
Corticosteroids are used primarily for their action as
Symptoms
Stiffness
Localized
Pain
Inflammation
Risk factor
Osteoarthritis
Morning or after inactivity (last 30
min)
Limited affected joints.
Worsens With Activity Or
After Prolong Use, (weight bearing
activity)
Uncommon
>65 years
Degenerative joint disease caused
by breakdown of the cartilage b/w
bones, degradation of articular
cartilage in synovial joints
Rheumatoid Arthritis
In the morning (last 1 hour)
Not localized
Worsens with prolong inactivity. (Usually
improves with activity).
Common
Autoimmune inflammatory condition
Chronic systemic
Symmetrical synovitis affecting similar
joints bilateral.
Cylco Oxygenase
Osteoarthritis Tips
Diclofenac
Cataflam, Solaraze
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29
DMARDS
Cytotoxics
Gold preparations
Azathioprine
Methotrexate
sodium Gold
Standards for
treatment of RA
Aurothioglucose
Sodium
aurothioglucose
Other DMARDs
Cyclosporine
Hydroxychloroquine
sulfateSE: Corneal &
retinal deposition
Leflunomide C/I in
pregnancy
Penicillamine
Sulfasalazine C/I: ASA
& Sulfa allergy
Biological response
modifiers
Adalimumab
Anakinra
Etanercept
Infliximab
A chronic inflammatory disease with frequent acute attacks. The immune system is involved in
attacking the joints and surrounding structures such as muscle tendons and most other connective
tissue. There is inflammation of the synovial membrane.
Biological
Response Modifiers
Infliximab
Etanercept
Infliximab
Infliximab (Remicade)
Etanercept (Embrel)
Anakinra (Kineret)
Binds to the Tumor Necrosis Factor (TNFa)
Inhibit interleukin-1 (IL-1), a key mediator of inflammatory NF
synovitis as well as bone and cartilage destruction.
Improve the sign and symptom of active RA
Must be given with Methotrexate to prevent formation of antibodies.
Binds to the Tumor Necrosis Factor (TNF alpha and beta)
Given SC twice weekly
Side effects: Most common: Respiratory tract infections
Given every 8 week by iv
Most common SE is Respiratory tract infections (Pneumonitis)
Storage: Refrigerator (2 8oC)
Do not freeze
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Methotrexate (Rheumatrex)
Mechanism
Therapeutic use
Side effects
Dose
Monitoring
Azathioprine (Imuran)
Refractory RA
Metabolism
Therapeutic use
Side effects
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Contraindications
Pregnancy
Children
Patients with rheumatoid arthritis previously treated with alkylating
agents (cyclophosphamide, chlorambucil, melphalan or others) may
have a prohibitive risk of neoplasia if treated with azathioprine.
Hydroxychloroquine (Plaquenil)
Therapeutic use
Side Effects
Overdose
management
Sulfasalazine (Azulfidine)
Mechanism
Therapeutic use
Side effects
Dose
Pharmacokinetics
Contraindications
Allergies
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Counselling
Leflunomide (Arava)
Mechanism
Therapeutic use
Side Effects
Monitoring
Washout
Diarrhea, Nausea
Weight Loss
Flu like syndrome
Skin rash
Alopecia
Hypokalemia
Male patient have possible male mediated fetal toxicity. Reliable
contraception during treatment should be guaranteed.
Pregnancy must be avoided if either partner receiving leflunomide.
Leflunomide should be administered to patients only under careful
medical supervision.
For men having received leflunomide and wishing to have children.
Plasma levels of active metabolite should be less than 0.02 mg/L
Using Cholestyramine resin
Cyclosporine (Neoral)
Cyclosporin PO
Therapeutic use
Side effects
Precautions
Drug interactions
(Cyclosporin is
metabolized by
CYP3A4)
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Drug interactions
(Cyclosporin is
metabolized by
CYP3A4)
Minocycline (Minocin)
Minocycline
Therapeutic use
Side Effects
Contraindication
D-penicillamine (Cuprimine)
Mechanism
Therapeutic use
Side Effects
Non Wilson disease
patients
Chelating agent
Wilsons disease (excess copper)
Chronic lead poisoning
Active Rheumatoid arthritis
For refractory RA, if other drugs fail.
Urticaria, Pruritis, Rashes, Bone marrow depression,
Thrombocytopenia, Leucopenia, Tinnitus, Proteinuria
Diarrhea (17%)
5-10 mg of copper can administered as 5-10 drops of Copper sulphate
solutions in fruit juice twice daily (do not use in Wilson disease patients).
Penicillamine should be given empty stomach. (increase absorption)
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Side Effects
Most common
Skin rashes
Proteinuria (after IM admin.)
Nitritoid reaction (low blood pressure and syncope after injections)
Pruritis (pruriginous), dermatitis
Angioedema
Thrombocytopenia
Aplastic anemia
Diarrhea
Stomatitis
Proteinuria
Arava
Neoral
Cleeravue-M, Dynacin, Minocin, Myrac
Cuprimine
Remicade
Embrel
Kineret
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30
Antimitotics and
anti-inflammatory
action
Colchicine
Corticosteroids
Nonsteroidal
Anti-inflammatory
Drugs (NSAIDs)
UricosuricsIncrease
excretion of uric acid
Xanthine oxidase
inhibitors prevents
conversion of purine to
uric acid
Dexamethasone
Dexamethasone sodium phosphate
Hydrocortisone sodium succinate
Methylprednisolone acetate
Prednisone
Triamcinolone
Allopurinol Take
with full glass of H2O
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Hereditary metabolic disease that is a form of acute arthritis and is marked by inflammation of the
joints.
Gout is associated with increased body stores of uric acid.
Acute attacks involve joint inflammation caused by precipitation of uric acid crystals.
Hyperuricemia
Urate crystal in joints inflammatory response
Acute gout arthritis
Abrupt onset of excruciating pain and inflammation of joint during the night or early morning.
Patient cannot tolerate even light pressure such as a bed sheet on the affected joint.
Attacks often resolve spontaneously over 3- 10 days. 1st line treatment is NSAIDs
For sever pain Intra-articular injection of corticosteroid. (especially in patient with polyarticular
gout)
Colchicine It relieves pain within 24 hours in 90% patients if treated within few hours of attacks.
Side effects: GI abdominal pain, cramps, diarrhea, N and V
Rarely Neuropathy, myopathy, bone marrow suppression
Intercritical gout: Most patient have second attack within 6 24 months.
Chronic tophaceous gout: May occur after 12 year of first attack.
Colchicine
Mechanism
Therapeutic use
Side effects
Drug-Drug
interactions
Indomethacin (Indocin)
Mechanism
Therapeutic use
Side effects
Probenecid (Benemid)
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Mechanism
Therapeutic use
Side effects
Counselling
Sulfinpyrazone (Anturane)
Mechanism
Therapeutic use
Side effects
Counselling
Sulfinpyrazone partially inhibits both the active secretion and the active
reabsorption
Inhibits platelet aggregation
Gout arthritis
Urate crystal formation
Take plenty of water
Allopurinol (Zyloprim)
Mechanism
Metabolism
Therapeutic
use
Side effects
Drug-Drug
interactions
Counselling
Ribose - 5 - P + ATP
Inosinic Acid
Inosine
Hypoxanthine
Hypersensitivity rashes
Peripheral neuritis and necrotizing
vasculitis
GI intolerance, diarrhea
Xanthine oxidase
In condition with large purine turnover xanthine
Xanthine
stone formation may occur
Alkalinize the urine to increase solubility
Xanthine oxidase
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Sulfinpyrazone is used as
A uricosuric drug is one that
Colchicine is mainly used for
xanthine oxidase
Indocin
Benemid, Probalan
Anturane
Zyloprim
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Osteoporosis
31
Osteoporosis
Osteoporosis Treatment
Selected Estrogen
Receptor Modulators
(SERMs)
Calcium Supplements
Anti parathyroid
Hormones
Calcium carbonate
Calcium gluconate
Calcitonin
Benzothiophene
Bisphosphonates
Parathyroid hormones
Alendronate
Etidronate
Risedronate
Raloxifene
hydrochloride
Teriparatide
Non Modifiable
Age > 65 y
Vertebral compression fractures
Postmenopausal woman (not on estrogen
therapy)
Premature menopause (<45 years)
Gender (Female)
Family history
Thin and small boned (overweight is NOT a
risk factor)
Hypogonadism
Race: Caucasians, Asians
Hyperparathyroidism
Hypocalcemia
Ingested
Ca2+
(
(
(
(
)
)
)
)
Fecal
Ca2+
Modifiable
Low calcium intake (<1000 mg
elemental calcium per day)
Inadequate sun exposure.
Cigarette smoking
Excessive Alcohol intake
Caffeine containing beverages.
Sedentary life style
Excessive heparin therapy
Oral Corticosteroid therapy
1,25-Dihydroxycholecalciferol
(+)
Absorption
Secretion
ECF
Ca2+
Bone formation
Bone resorption
(-)
Filtration
(+)
Reabsorption Calcitonin
(+)
PTH,
1,25-Dihydroxycholecalciferol
PTH
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Osteoporosis
Dose of Vitamin D
Bisphosphonates
Bisphosphonates
Mechanism
Therapeutic use
Side Effects
Osteoporosis Prevention
Treatment of post menopause bone loss
Treatment of osteoporosis
Treatment of Glucocorticoid induced osteoporosis
Pagets disease = Excessive activity of osteoclasts.
Metastatic bone cancer
Bisphosphonates have decreased rate of bone fracture in osteoporosis
and Pagets disease patients
Bisphosphonates have anti resorptive activity.
Risedronate has highest anti resorptive activity and than alendronate.
Etidronate has lowest anti resorptive activity
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Dose
Alendronate
Counseling
Osteoporosis
Raloxifene (Evista)
Mechanism
Therapeutic use
Side Effects
Calcitonin salmon
Calcitonin is a hormone secreted from thyroid gland
Calcitonin hormone helps bone formation by transporting Ca from blood to bones
Mechanism: Directly effect on osteoclast and decrease bone resorption through direct effect.
Two products are available
Miacalcin
200 IU/day intranasally
Common SE is nasal irritation
Calcimar, caltine
50 100 IU sc/day or Q 2nd day or 5days/wk
Not approved for osteoporosis
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Osteoporosis
Osteoporosis Tips
Evista
Fosamax
Didronel
Actonel
Alendronate
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32
b2-adrenergic
agonist
Anti-inflammatory drugs
Methyl
xanthene
Aerosol
corticosteroids
Mast cell
stabilizers
Theophylline
Cromolyn sodium
Aminophyllinne
Nedocromil
Muscarinic
Fluticasone
antagonist
Beclamethasone
Ipratropium
Tiotropium (Spiriva)
Leukoteine antagonists
Leukotriene
receptors
antagonist
Zafirlukast
Montelukast
Inhibitory
of 5-lipo
oxygenase
enzyme
Zileuton
Short acting
Long acting
Albuterol (salbutamol)
Formeterol
Isoproterenol
Salmeterol
Isoetharine
Metaproterenol
Terbutaline
Asthma Triggers (factors that increase risk of asthma)
Triggers
Early asthmatic response- Symptoms only (i.e., bronchoconstriction)
Cold air
Exercise
Emotional stress
Late asthmatic response- Worsening asthma
Allergens (Pollens, cockroach, molds, animal dandur)
Respiratory viruses
Occupational chemicals
Drugs ASA, NSAIDs
Food additives sulfites, tartrazine
Air pollution (including cigarette smoke)
GERD
Sinusitis
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Mechanism
Therapeutic use
Short acting beta 2 agonist:
Albuterol, terbutaline,
pirbuterol
SE
Salbutamol (Ventolin)
Mechanism
Therapeutic use
Side effects
Recommendation
Contraindication
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Onset of bronchodilation
10-20 minutes
Duration of
bronchodilation
4-5 hours
Salmeterol (Serevent)
Mechanism
Therapeutic use
Side effects
Drug-drug interaction
Metaproterenol (Alupent)
Mechanism
Therapeutic use
Onset of
bronchodilation
Duration of action
Terbutaline (Bricanyl)
Mechanism
Therapeutic use
Side effects
Drug-drug
interaction
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Corticosteroids
Corticosteroids
Mechanism
Therapeutic use
Side effects
Recommendation
Combination
products
Prednisone/Prednisolone (Inflamase)
Mechanism
Therapeutic use
Side effects
Drug-Drug interaction
Recommendation
Fluticasone (Flovent)
Mechanism
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Mechanism
Therapeutic use
Side effects
Monitoring
Side effects
Drug-Drug
interaction
Monitoring
Beclomethasone (Qvar)
Mechanism
Therapeutic use
Side effects
Recommendation
Monitoring
Anticholinergics
Ipratropium Bromide Atrovent
Mechanism
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Therapeutic use
Side effects
Onset of effect
Duration of action
Tiotropium (Spiriva)
Combivent
All MDI
Leukotriene inhibitors
Zafirlukast
Mechanism
Leukotriene inhibitors
Inhibitors of LTC4 and LTD4 receptors
Steroid sparing properties
Therapeutic use
Side effects
Drug-Food
interaction
Montelukast
Mechanism
Therapeutic use
Side effects
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Drug-Food
interaction
Therapeutic use
Side Effects
Recommendation
Monitoring
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Side Effects
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Acetyl Saliaylate
Non-Steroidal Anti-inflammatory Drugs
Short Acting Beta2 Agonist
Long Acting Beta2 Agonist
Catechol-O-methyl transferase
Exercise Induce Asthma
Chronic Obstructive Pulmonary Diseases
Congestive Heart Failure
Calcium Channel Blocker
Ventolin
Advir, Serevent
Alupent
Brenthin, Bricanyl
Inflamase, Pediapril, Winpred
Flonase, Flovent
Entocort, Pulmicort, Rhinocort, Rhinocort Aqua
Ati-Beclomethasone, Qvar, Rivanase AQ
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33
Action of DNA
Damage DNA
Inhibit
synthesis or
functions
Others
Free radicals:
Alkylation:
Actinomycin D
Bleomycin
Mechlorethamine
Etoposide
Cyclophosphamide
Teniposide
Ifosfamide
Amsacrine
Topoisomerase
Chlorambucil
Antimetabolites
inhibitors
5-fluorouracil
Melphalan
Doxorubicin
Cytarabine
Busulfan
Daunorubicin
Mercaptopurine
Lomustine
Topotecan
Thioguanine
Carmustine
Irinotecan
Thioguanine
Streptozolin
Methotrexate
Cisplatin
Carboplatin
Dacarbazine
Procarbazine
Altretamine/
Hexamethylmelamine
Action on steroid
Mitomycin
Hormones
Agonists
Androgens
Estrogens
Progestins
Leuprolide
Goserelin
Narfarelin
Cancer estimated
deaths in men
Cancer estimated
deaths in women
Warning signs of
cancers
Atagonist
Tamoxifen
Toremifene
Flutamide
Anastrozole
Letrozole
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Cell Cycle Phases
All cells must traverse the cell cycle phases before and during cell division.
Anticancer drugs may act on specific phase. Tumor cells are more
responsive to specific drugs
G0 phase Resting phase
G1 phase Synthesis of enzymes needed for DNA synthesis
S phase DNA replication (DNA synthesis)
G2 phase Synthesis of components needed for mitosis.
M phase Mitotic tubule formation Vincristine and vinblastine
More active against cells that are specific phase of cycle:
G1 phase L-aspraginase and prednisone
S phase Methotrexate, 6-thioguanine, cytarabine
G2 specific Bleomycin and etoposide
M phase Vincristine and vinblastine, peclitaxol
Alkylating agents, Antitumor antibiotic, Cisplatin
phase where
cell divides
G0: resting
state where cell
is not dividing
G1: synthesis
of enzymes
needs for DNA
synthesis
S: DNA is
replicated
Class
Alkylator and alkylatorlike drugs
Antimetabolites
Examples
Melphalan, Chlorambucil,
Cisplatin, Carmustine
Fluoroucil, Methotrexate
cytarabine, Mercaptopurine
fludarabine
Mechanisms
Covalent bonds break with DNA
bases; strand breaks
Inhibit DNA synthesis by inhibiting
enzymes or incorporating into DNA
and RNA.
Antibiotics
Doxorubin, Bleomycin,
Mitomycin C, Dactinomycin
Vincristine, Vinblastine,
Paclitaxel. Docetaxel
Mitotic inhibitors
Topoisomerase
inhibitors
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Alopecia is a counseling issue! The extent of hair loss varies, but is usually starts at 2-4 weeks and
is reversible when the drugs are discontinued. Doxorubicin and paclitaxel tend to cause the most
alopecia, but it is common with most combination regimens. Patients may wear wigs, hats, or may
just go bald.
Neurotoxicity: Vincristine has as its dose-limiting toxicity autonomic dysfunction and peripheral
neuropathy, both sensory and motor.
Pulmonary toxicity: Bleomycin causes a generally irreversible pulmonary fibrosis at higher lifetime
doses.
Clophosphamide (Cytoxan)
Mechanism
Therapeutic use
Side Effects
Drug-Drug
interaction
Contraindication
Monitoring
Side effects
Doxorubicin (Adriamycin)
Mechanism
Therapeutic use
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Side effects
Irreversible cardiotoxicity
Myelosuppression
Stomatitis
Alopecia
Nausea and vomiting
Should be carried in Vertical laminar air flow hood
Compounding
Dactinomycin (Cosmegen)
Mechanism
Side effects
Anticancer antibiotics
Form stable DNA complex and interfere with DNA dependent RNA polymerase
Major dose limiting toxicitybone marrow depression.
Mechlorethamine (Mustargen)
Mechanism
Therapeutic use
Side effects
Alkylating agent
Primarily used in Hodgkins disease (malignant disease of lymphatic tissue) as
part of MOPP regimen (Mechlorethamine, Oncovin, Prednisone, Procarbazine)
Severe nausea and vomiting
Sever bone marrow depression
Myelosuppression
Anorexia
Gonadal dysfunctionz
Side effects
Paclitaxel (Taxol)
Mechanism
Side effects
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Anaphylaxis
Dyspnea
Chemotherapy
The treatment of cancer with drugs is called chemotherapy. Antineoplastic drugs, also referred to as
chemotherapeutic agents, are drugs that are used to treat cancer.
Side effects of chemotherapy:
Acute:
Extravasation (effects the adjacent tissue)
Vessicant drugs (damage to tissue / necrosis) Example: Bleomycin, cisplatin,
dactinomycin, domorubicin, vincristine, vinblastin etc.
Thrombophlebitis (inflammation associated with thrombus): Patient with cancer can
develop thrombosis after chemotherapy. Due to activation of fibrinogen.
Hypersensitive reactions. Example: Etopiside, peclitaxol, rituximab, trastuzumab.
Rapid tumor lysis syndrome
Nausea and vomiting
Skinalopecia, dry skin, nail changes, pigmentation (melanoma), Xerostomia
Alopecia is the loss of hair: Drug that cause alopecia is doxorubicin, daunorubicin,
cyclophosphamide, vincristine, and paclitaxel.
Vessicant agents include: dactinomycin, doxorubicin, mechlorethamine, mitomycin, vincristine, and
vinblastine.
Hair regrowth occurs after 1-2 months after stopping chemotherapy.
Xerostomia: Dry mouth is one of the most common complication associated with radiation therapy.
Reversible after 6-12 months of therapy.
Can be managed by: Sugar free hard candy, chewing sugar free gum stimulate salivation.
Commercially available saliva substitute. Ice chips. Cholinergic agonist Pilocarpine 5mg tab.
Bone marrow depression (Myelosuppression):
Bone marrow depressionNeutropenia, Thrombocytopenia
Neutropenia treated by colony stimulating factors (G-CSF and GM CSF): Filgrastim or
pegfilgrastim
Thrombocytopenia for prevention use Oprelvekin (Inerleukin-11)
Complications: Bone marrow suppression is the most dose limiting side effect of cancer
Myelosuppression in general the onset is 7 10 days and peak is 10 14 days. Recovery count
occurs usually occurs in 2 3 weeks.
Megaloblastic anemia by methotrexateFolinic acid (leucovorin, 5-formyltetrahydrofolic acid)
Neutropenia associated anticancer drugs can be treated by filgrastim (human granulocyte
colony stimulating factor)
Least bone marrow depression anticancer drugs is: Bleomycin
Cancer patient with anemia Erythropoeitins are useful
Cardiotoxicity:
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Pulmonary toxicity:
Pneumonitis, pulmonary fibrosis commonly seen with Bleomycin, Carmustine, Cyclophosphamide,
Mitomycin, Methotrexate, vinca alkaloids,
Symptoms of pulmonary toxicity include: SOB, non-productive cough, and rarely low grade fever.
Neurotoxicity:
Common with vincristine, vinblastine, Cytarabines, Methotrexate (very little), 5FU, interferon
alpha
Peripheral neuropathies associated with: Vincristine, peclitaxel: Peresthesia (numbness and
tingling) can occur with vincristine, which often appears within few weeks of therapy.
High dose of cytarabin may produce cerebllar toxicity that manifest initially as loss of eye-hand
coordination and progress to coma.
Fludrabine cause severe neurotoxicity
Caramustine and other alkylating agents cause little or no neurotoxicity.
GI toxicity
Mucositis or stomatitis:
Mucositis: Generalized burning, and pain on the ventral surface of tongue. Floor of tongue, mouth
looks erythromatus.
Stomatitis: generalized inflammation of oral mucosa.
Mucositis or stomatitis: Common with Doxorubicin, Methotrexate, 5-fluorouracil, Actinomycin,
Bleomycin capecitabine.
Recommend mouth hygiene, xylocaine, viscous sucralfate, nystatin, sodium bicarbonate, for
severe cases peliformin (growth factor) can be used.
Avoid alcohol, antihitamine, steroids, spicy food
Mucositis treatment and prevention:
Topical anesthetics: Viscous Lidocaine, or dyclonineHCL 0.5 or 1%
Corticosteroid provide anti-inflammatory action
Capscisin: Produces burning and pain and ultimately desensitizes pain.
Sucralfate suspension may provide benefit by coating.
For Localized effect: use benzocain in orabase
Mucositis prevention:
Chlorhexidine gluconate 0.12% (Peridex, Periogard) may reduce severity and frequency
of mucositis infections.
Very high emetics anticancer drugs
Cisplatin
Streptozocin
Cyclophosphamide
High emetics anticancer drugs
Doxorubicin
Methotrexate (250 mg to 1000mg)
Cytarabine
Lowest emetic anticancer drugs
Bleomycin
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Hepatotoxicity
Hepatotoxicity monitor LFT, jaundice, or hepatitis: Asparaginase, cytarabine, mercaptopurine, and
methotrexate.
Nephropathy:
Elevate BUN and electrolyte abnormalities: methotrexate may precipitate in kidney. Cisplatin and
streptozocin. Amifostine may be used to protect the kidney from the nephrotoxicity associated
with cisplatin.
Sexual dysfunction:
Cyclophosphamide, melphalan, and procarbazine associated with significant infertility in men and
women.
Hemorrhagic cystitis
It is a bladder toxicity that is seen most commonly after administration of cyclophosphamide and
ifosfamide.
These drugs produce a metabolite called acrolein, which cause chemical irritation in bladder
mucosa, resulting in bleeding.
Hemorrhagic cystitis caused by Acrolein can be prevented by excessive hydration and subsequent
frequent urination. The other method is by administering uroprotecting agent called MESNA,
which bind acroleine and prevent from contacting the bladder mucosa.
Pulmonary toxicities:
The most common with bleomycin, mitomycin, carmustine
Rationale for combination therapy: Overcoming or preventing resistance, Cytotoxicity to resting and
dividing cells Biochemical enhancement of effect. Beneficial drug interactions Rescue host cells
Some agents can be administered intrathecally: Methotrexate, Cytarabine Thiotepa
Warning: Vincristine should be labelled as Intravenous only. Intrathecally vincristine causes death.
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Melonoma is
Metoclopramide and dexamethasone are more effective nausea related to
Methotrexate is used for
Which anticancer drugs cause pulmonary fibrosis
Hypertropy is
Hyperplasia is
Least emetic anticancer drug is
Cancer patient on cancer chemotherapy, reports shortness of breath, non productive cough, she
may be using drug
DOC for delayed Nausea and vomiting
Mesna is
Doxorubicin preparation should be performed in
Hypertropy is
Hyperplasia is
Melatonin
Peclitaxel and docetaxel act on
Alkeran
Leukeran
Platinol
BiCNU
Adrucil, Carac, Efudex, Fluoroplex
Rheumatrex, Trexall
Cytosar
Fludara
Blenoxane
Mitozytrex, Mutamycin
Oncovin, Vincasar PFS
Velban
TaxotereT
Etopophos, Toposar, VePesid
Camptosar
Hycamtin
Oncovin
Cytoxan, Procytox
Purinethol
Adriamycin, Rubex
Cosmegen
Mustargen
Taxol
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Gastrointestinal Drugs
34
Gastrointestinal Drugs
GERD
Mild GERD, relief of symptoms is with antacids, alginates or non-prescription strength H2RA.
Severe GERD: PPI are the Drug of choice. Use PPI for 2 4 weeks
The goal is to raise the intragastric pH 4 during periods when reflux is likely to occur.
Peptic ulcers
Gastric ulcers Due to reflux since has weak pyloric sphincter
Duodenal ulcers Excessive secretion from parietal cells
Acute stress ulcers (Curlings ulcer) Tumors
Pathologic acid-hypersecretory states (Zollinger-Ellison syndrome)
Treatment of peptic ulcers
To eradicate H. pylori
Antacids
Antacids are used to treat stomach upset, acid indigestion (heartburn) and sometimes ulcers. They
are simple chemical compounds that are mildly alkaline, and some also act as chemical buffers. They
act by neutralizing stomach and coating the mucosal lining of the stomach. Simethicone is an agent
added to antacids that helps relieve gas.
Types of antacids
Aluminum
compounds
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Mg bicarbonate
Na bicarbonate
Combined
preparations
Calcium Carbonate
Gastrointestinal Drugs
H2 receptor antagonists
Ach
Atropine
Histamine
Muscarinic receptor
IP3 Ca2+
Cimetidine
H2 receptor
cAMP
PPIs
Gastrin
H+ secretion
H2-receptor antagonists inhibit the action of a special type of histamine receptor present in the
stomach. This reduces the amount of gastric acid production, which helps heal ulcers.
H2 receptor
antagonists
Therapeutic use
Cimetidine (Tagamet)
Ranitidine (Zantac)
Famotidine (Pepcid)
Nizatidine (Axid)
Acid must be produced to digest protein
Gastric acid secretion is controlled by histamine from enterochromaffin-like
cells, acetylcholine neurons and gastrin-G cells in the antrum
90% reduction in acid secretion
Useful in promoting healing of gastric ulcers
Preventing reoccurrence of ulcers
Management of Zollinger-Ellison syndrome
Gastric hypersecretory states in systemic mastocytosis which is a rare
disorder with increase number of mast cells systematically and in skin
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Side effects
Tips
Gastrointestinal Drugs
Ranitidine (Zantac)
Mechanism
Therapeutic use
Side Effects
Drug-drug
interaction
Contraindication
Advantage from
other drugs
Call physician NOW
Cimetidine
Mechanism
Therapeutic use
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Side Effects
Drug-Drug
interaction
Contraindication
Monitoring
Gastrointestinal Drugs
Diarrhea
Dizziness
Increases the effects of anticoagulants. Inhibit CYP 3A4 metabolism,
thereby inhibit metabolism of warfarin, phenytoin, theophylline.
Discuss with physician about using the drugs for pregnant and
lactating mothers.
It is prescribed with caution to people who are receiving
anticoagulants and anticonvulsants
This drug will mask the symptoms of cancer, and delay diagnosis.
Mechanism
Therapeutic use
Duration
Side effects
Omeprazole
Lansoprazole
Rabeprazole
Pantoprazole
Irreversible inhibition of gastric parietal cell proton pump H+/K+ ATPase
Prevention of reoccurrence of duodenal ulcers and esophagitis
Pathology hypersecretory states
Multiple endocrine neoplasias
Healing of NSAID induces peptic ulcers
Systemic mastocytosis
A part of the eradication of H. pylori therapy
Drug of choice for Ellison Zollinger Syndrome
Short term treatment (4-8 weeks)
Abdominal pain
Diarrhea
Headache
Omeprazole (Losec)
Mechanism
Therapeutic use
Side Effects
Drug-drug
interaction
Contraindication
Stop taking drug
NOW
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Gastrointestinal Drugs
Lansoprazole (Prevacid)
Mechanism
Therapeutic use
Side Effects
Drug-drug
interaction
Contraindication
Therapeutic use
Side effects
Dose
Drug interactions
Bismuth Compounds
Mechanism
Therapeutic use
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Contraindications
Gastrointestinal Drugs
GI disorder Tips
Losec
Prevacid
Tagamet
Axid
Zantac
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35
Protein Synthesis
inhibitors
Aminoglycosides
Macrolides
Tetracyclines
Lincosamide
Penicillins
Cephalosporins
Vancomycin
DNA Synthesis
inhibitors
Quinolones/
Fluoroquinolones
Metronidazole
Folate Inhibitors
Sulfonamides
Trimethoprin
Penicillins
Acid labile (acid sensitive)
Penicillin G...b-lactamase sensitive
Methicillinb-lactamase resistant
Nafcillin....b-lactamase resistant
Aminopenicillins
Penicillin G
Penicillin V
Methicillin
Nafcillin
Oxacillin
Carbenicillin
Ticarcillin
Piperacillin
Amoxicillin
Ampicillin
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Mechanism
Therapeutic uses
Side effects
Penicillins G
Mechanism
Therapeutic uses
Side effects
Side effects
management
Drug interactions
Interferes and alters test results for urine and serum protein levels. It
does not interfere with test using bromophenol blue.
Aminoglycoside causes synergistic effect. Most effective endocarditis
infections.
Penicillin V
Mechanism
Uses
Side Effects
SE management
Drug interactions
Amoxicillin (Amoxil)
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Therapeutic use
Side Effects
Drug interaction
Gram + ve (mainly)
Gram ve Neisseria
Synergistic effect with aminoglycoside
Hypersensitivity, Anaphylaxis
GI affects Nausea& Vomiting, P. Colitis (diarrhea).
Blood related
Thrombocytopenia
Leucopenia
Agranulocytosis
AllopurinolIncreases rashes
Hormonal contraceptiveDecreases contraceptive effect.
Methotrexate-effects renal tubular absorption.
Ampicillin (Principen)
Clinical use
Drug interaction
Side Effects
Gram + ve (mainly)
Gram ve Neisseria
AllopurinolIncreases rashes
Hormonal contraceptiveDecreases contraceptive
Hypersensitivity, Anaphylaxis
GI Nausea & Vomiting, P. colitis (diarrhea).
Blood related Thrombocytopenia
Leukopenia
Agranulocytosis
Cephalosporins
1st generation
2nd generation
Cefazolin
Cephalothin
Cephalexin
Cephapirin
Cephradine
Cefadroxin
Cefaclor
Cefamandole
Cefoxitin
Cefuroxime
sodium
Cefuroxime
auxetil
Cefotetan
Cefproxil
Cefonicid
Loracarbef
Oral
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3rd generation
Contain
methylthiotetrazole
side chain. Can cause
hypoprothrombonemia
and bleeding problems
1th generation
Cefixime
Cefoperazone
Cefotaxime
Cefpodoxime
Ceftazidime
Ceftriaxone
Cefdinir
Ceftibuten
Cefepime
Dose
Cefazolin
Cephalothin
Surgical prophylaxis (best for Gram + ve)
Allergic reaction (5-15%)
Anaphylaxis
Skin rash
Fever
Hemolytic anemia
Granulocytopenia
Local irritation at site of injection.
Seizure in high doses in IV form
IV and PO
Clinical use
Side effects
Dose
Cefaclor
Cefamandole
Cefoxitin
Cefuroxime
Gram -ve coverage.
Parenteral administration except: cefaclor
Allergic reaction (5-15%) Skin rash, Anaphylaxis
Fever,
Local irritation at site of injection
Blood related Hemolytic anemia, Granulocytopenia
IV and PO
Cephalosporins-3rd Generation
3rd Generation
Cefixime
Cefoperazone
Cefotaxime
Cefpodoxime
Ceftazidime
Ceftriaxone
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Clinical use
Side effects
Dose
Cefepime
Best for Gram -ve
Higher potency
Side effects
Dose
Vancomycin (Vancocin)
Mechanism
Therapeutic use
Side effects
Precautions
Dosage
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Pfizerpen
Beepen-VK, V-Cillin-K, Veetids
Pipracil
Amoxil, Dipermox, Trimox
Principen
Vancocin, Vancoled
Ancef, Kefzol
Keflin
Ceclor, Ceclor CD, Raniclor, Raniclor
Mefoxin
Alti, Ceftin, Kefurox, Zinacef
Velosef
Duricef
Mefoxin
Ceftin
Cefotan
Cefzil
Lorabid
Suprax
Cefobid
Claforan
Banan, Vantin
Ceptaz, Fortaz, Tazicef, Tazidime
Rocephin
Omnicef
Rocephin
Cedax
Maxipime
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36
Chloramphenicol
Lincosamides
Clindamycin
Lincomycin
Macrolides
Erythromycin
Azithromycin
Clarithromycin
30 S Antibacterial Agents
Aminoglycosides
Gentamycin
Streptomycin
Kanamycin
Tetracyclines
Demeclocycline
Doxycycline
Minocycline
Aminoglycosides
Gentamicin, Streptomycin, Tobramycin, Kanamycin, Amikacin
Pharmacokinetics
All aminoglycosides renally eliminated
Half-life 2 4 hours.
Post dose antibiotic effect (PDAE)
Only Kanamycin and neomycin have oral and topical
Commonly aminoglycosides used as IM or IV
Streptomycin has only IM
Pharmacokinetics is not completely understood
Contain aminosugars structures and have low bioavailablity
Primarily used in infections associated with gram ve.
Aminoglycoside have little activity against anaerobic.
Gentamicin (Garamycin)
Therapeutic Uses
Side Effects
Gram ve
Drug uptake depends of oxygen: active against aerobes
Second line treatment for tuberculosis (mainly streptomycin)
Treatment for plague (streptomycin).
Pseudomonas (streptomycin)
Combined with cephalosporins (2nd and 3rd) to reduce resistance
Respiratory paralysis (decrease Ach at NMJ)
Nephrotoxicity (proximal tubular cell)
Ototoxicity (also occurs in unborn fetus)
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Streptomycin
Uses
Side Effects
Gram -ve
Second line treatment for tuberculosis (mainly streptomycin)
Treatment for plague (streptomycin).
Pseudomonas (streptomycin)
Combined with cephalosporins (2nd and 3rd) to reduce resistance
Otic nerve toxicity-8th cranial nerve (mainly streptomycin)
Highest ototoxicity
Least Nephrotoxic
Ototoxicity
Streptomycin = Kanamycin > amikacin = gentamycin = tobramcycin > netilmycin
Tobramycin (Tobrex)
Uses
Side Effects
Gram -ve
Second line treatment for tuberculosis (mainly streptomycin)
Treatment for plague (streptomycin).
Pseudomonas (streptomycin)
Combined with cephalosporins (2nd and 3rd) to reduce resistance
Respiratory paralysis (decrease Ach at NMJ)
Nephrotoxicity (proximal tubular cell)
Ototoxicity (also occurs in unborn fetus).
Amikacin (Amikin)
Uses
Side Effects
Gram -ve
Second line treatment for tuberculosis (mainly streptomycin)
Treatment for plague (streptomycin).
Pseudomonas (streptomycin)
Combined with cephalosporins (2nd and 3rd) to reduce resistance
Respiratory paralysis (decrease Ach at NMJ)
Nephrotoxicity (proximal tubular cell)
Ototoxicity (also occurs in unborn fetus)
Aminoglycoside summary
Side effects
A = Allergy
M = neuroMascular Blockade
I = Inactivated when physically mixed with b-lactams
N = Nephrotoxicity
O = Ototoxicity, Optic nerve toxicity
Half life is 2 4 h
Aminoglycoside have post antibiotic effect
Highest ototoxicity is with Streptomycin
Highest nephrotoxic is Neomycin
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Ototoxicity symptoms associated with gentamycin and streptomycin are: Vestibular damage this
can cause Tinnitus, vertigo, and ataxia.
Ototoxicity symptoms associated with amikacin and kanamycin are: Auditory damage this can
cause hearing loss.
Tobramycin can cause both vestibular and auditory damage
To prevent serious side effects associated with aminoglycosides monitor: Blood drug levels,
BUN, Serum creatinin levels
Blood levels are monitored by peak and trough levels:
Trough levels of gentamycin greater than 2mcg/ml can cause nephrotoxic.
Macrolides
Erythromycin. Clarithromycin, Azithromycin
Pharmacokinetics:
All of macrolides hepatically eliminated, except: clarithromycin, which is renally eliminated.
All macrolides have oral dosage and erythromycin gluceptate and lactobionate is IV.
Azithromycin has long half-life 68h and used single daily doses.
Erythromycin has short half-life 1.2 2.6 hours.
Erythromycin are preferred drug for treatment of Mycoplasma infection.
Important alternate in patient allergic to penicillins
Erythromycin estolate may cause cholestatic jaundice in-patient used more than 10-14 days.
(Resolved after discontinued treatment)
Erythromycin is inhibitor of CYP3A4, thereby potentiates toxicities of drugs that are metabolized
by CYP3A4, eg: digoxin, corticosteroids, lovastatin or (ALS), Carbamazepine.
Clarithromycin increase warfarin INR (monitor PT), increases digoxin and theophylline levels.
Azithromycin is more active against gram ve H.influenza than erythromycin.
Clarithromycin is effective for H.pylori (used along with PPIs in triple therapy)
Erythromycin
Use
Side effects
Drug
Interactions
Clarithromycin (Biaxin)
Use
Side Effects
Contraindication
Azithromycin (Zithromax)
Use
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Side Effects
Contraindicated
Counselling
Epigastric distress.
Oral has less N and V.
in patient with hepatic dysfunction
Suspension do not refrigerate
Tetracycline
Tetracycline
Therapeutic Uses
Side Effects
Contraindication
Counselling
Doxycycline
Uses
Side Effects
Contraindication
Counseling
Broad spectrum
Prophylaxis in travellers diarrhea
Lyme disease, Chlamydia (lymphogranuloma, Psittacosis), Rickettsia (Rocky
mountain spotted fever)
Mycoplasma pneumonia
Gastric discomfort.
Effect on calcified tissues (deposition in the bone and primary dentination
occurs during growing children.
Discoloration and hypoplasia of the teeth and temporary stunting of growth,
Fetal hepatotoxicity
Phototoxicity-Severe sunburn
Super infection (over growth of candida in vagina or resistance to
Staphylococcus in intestine)
Pregnancy, children under 8 old, breast feeding
Take entire medication even if you feel better
Oral: take with or after meal with glass of water.
(Food decreases GI side effects avoid milk, antacids, iron)
Tell patient to check tongue for fungal infection.
Stress good oral hygiene.
Avoid prolong sun exposure
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Minocycline
Minocycline
Therapeutic use
Side Effects
Contraindication
Clindamycin
Clindamycin
Uses
Side Effects
Contraindication
Counseling
Precaution
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37
Side Effects
Counseling
Auxiliary labels
Phototoxicity
Ofloxacin (Floxin)
Mechanism
Uses
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Side effects
Counseling
Gatifloxacin (Tequin)
Mechanism
Therapeutic use
Side Effects
Drug-drug
interaction
Contraindication
Monitoring
Metronidazole (Flagyl)
Metronidazole
Mechanism
Therapeutic use
Side effects
Drug-Drug
interaction
Precautions
Pregnancy and
lactations
Dosage
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38
Combination
drugs
Mechanism
Therapeutic Use
Sulfamethoxazole
Sulfadiazine
Sulfisoxazole
Sulfasalazine
Trimethoprim
Cotrimoxazole
Folate Antagonists
UTI E. coli
Drug of choice in Traveller diarrhea
Trachoma-chlamydia trachoma-most
common cause of preventable blindness
Topical: Burns and wounds
Side effects
Crystalluria: adequate hydration and
alkalinization prevent this problem
Hypersensitivity: rashes, StevensJohnson syndrome-occurs with longer
acting agents: (diuretics, acetazolamide,
thiazide, furosemide, bumetanide,
diazoxide).
Hemolytic anemia-G6 PD deficiency
Kernicterus: newborns because sulfas
displace bilirubin from binding
Counseling
Sulfasalazine: drugs colors urine and may
color skin orange yellow.
May permanently stain soft lenses
Take drug after meals to reduce GI
distress and to facilitate passage into
intestine.
Stevens-Johnson syndrome
Sulfa Drugs = Antiseizure drugs ; Allopurinol
Management of SJS: by discontinuing medication.
Folate antagonist Mechanism
Pteridine + PABA
Dihydropteroate
synthase
Sulfonamide
Dihydropteroic acid
Dihydrofolic acid
Dihydrofolate
reductase
Trimethoprim,
pyrimethamine
THF cofactors
Thymine
Purines
DNA
DNA
RNA
Methionine
Glycine
f-met-tRNA
Proteins
Sulfasalazine (Salazopyrin)
Mechanism
Therapeutic use
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Side effects
Drug-drug
interactions
Monitoring
Side effects
Counseling
Contraindications
Antibiotics Tips
Steven-Johnsons Syndrome: Rash, skin peeling, and sores on the mucus membrane. In Steven
Jhonsons syndrome, a person has blistering of mucus membrane, typically in mouth, eyes and
vagina. Patchy areas of rash. SJS can occur in all age groups.
Due to: SASPAN
Sulfonylurea
Anticonvulsant (phenytoin)
Sulphonamide
Penicillin
Allopurinol
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NSAIDs
Sulfa drugs Stevens Jhonsons Syndrome
Topical sulfa is contraindicated because it may cause disease like SJS, this disease is life threatening.
Treatment of SJS is Cortisone
Summary of Cell wall synthesis inhibitors
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Antifungals
39
Antifungal agents
Mechanisms of Action and Classification of Antifungal Agents
Antifungal Agents
After cell membrane permeability
Azoles
Allylamine
* Terbinafine
* Naftifine
Imidazoles
* Ketoconazole
* Miconazole
* Clotrimazole
Systemic
antifungals
Triazoles
Pyrimidine
Analog
Polyene
macrolide
antibiotics
* Flucytosine
Penicillin
derivative
* Griseofulvin
* Amphotericin B
*Nystatin
* Fluconazole
* Itraconazole
Allylamines
Antifungal Antibiotics
Echinocandins
Imidazole
Pyrimidines
Triazoles
Topical
Antifungals
Allylamines
Antifungal Antibiotics
Imidazoles
Terbinafine hydrochloride
Amphotericin B
Amphotericin B (lipid-based)
Griseofulvin
Caspofungin acetate
Ketoconazole
Flucytosine
Fluconazole
Itraconazole
Naftifine hydrochloride
Terbinafine hydrochloride
Nystatin
Clotrimazoles
Econazole nitrate
Ketoconazole
Miconazole nitrate
Oxiconazole nitrate
Tioconazole
Chlorphenesin
Ciclopirox olamine
Clioquinol
Selenium sulfide
Tolnaftate
Undecylenic acid
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Antifungals
Amphotericin B (Fungicidal)
Therapeutic use
Mechanism
Side effects
Contraindication
WARNING
Drug interaction
Precaution
Counselling
References
Nystatin
Category
Therapeutic use
Mechanism
Side effects
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Advantage
Drug interaction
Precaution
Counselling
Reference:
Antifungals
Fluconazol
Triazole type antifungal
Inhibitors of Ergosterol synthesis by
binding to CYP
Single doses
Penetrate CNS (AIDS chemotherapy)
CNS SE: dizziness
No interaction with cimetidine, antacids
For systemic infection UTI, peritonitis,
pneumonia
Ketoconazol
Imidazole type antifungal
Inhibitor Ergosterol synthesis
Not a single dose
Doesnt penetrate CNS
SE: Hormonal effects such as gynecomastia and
menstrual disturbances
Interaction with cimetidine, antacids
Require acidic conditions for absorption (avoid
antacids concomitantly)
Ketoconazole (Nizoral)
Ketoconazole (Imidazole type)
Therapeutic use
Miconazole; Clotrimazole
Chronic mucocutaneous candidiasis, systemic and vaginal
candidiasis, Tinea corporis (ringworm), T. cruris (jock itch),
T. pedis (Athletes foot), Tinea versicolor (sun fungus),
histoplasmosis, blastomycosis, paracoccidioidomycosis, oral
thrush
Relative bioavailability: 75 % with meals
Available as tablet, cream
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Antifungals
Mechanism
Side effects
Contraindication
WARNING
Precaution
Counselling
References
Fluconazole (Diflucan)
Mechanism
Therapeutic use
Side effects
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Drug interaction
Precaution
Reference:
Antifungals
Itraconazole (Sporanox)
Therapeutic use
Mechanism
Block the synthesis of ergosterol 14a demethylase in the fungal CYP 450
complexz
Side effects
Contraindication
Warning
Cause CHF; heart attack; irregular heart beat/ dse; lung/ kidney/liver
disease or other serious problems; SOB; coughing up white phlegm;
weakness; excessive tiredness; fast heart beat; swelling of the feet, ankle or
leg; sudden weight gain
Drug interaction
Drug interaction
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Counselling
Reference:
Antifungals
Oral solution: Swish 10ml (2tsp) in the mouth for a few seconds and
swallow. Repeat is necessary until entire dose is taken. The solution is
usually taken on an empty stomach once daily or BID for 1-4 weeks.
Tell Doctor if taking Itraconazole. Do not substitute the capsules for the
liquid because they have different use.
CPS 2004, page 1973-1978
Comprehensive Pharmacy Review, 5th Ed. Page 794-795
Clotrimazole
Therapeutic use
Mechanism
Side effects
Contraindication
Management
Precaution
Reference
Miconazole
Category
Mechanism
Therapeutic use
Side effects
Contraindication
Drug interaction
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Drug interaction
Availability
Application
Reference
Antifungals
Atypical anti-psychotics,
Cyclosporins
Some statins
Topical 2%, aerosol powder, 2 % cream, a kit-2% powder 2y/o and 2%
tincture, 2% vaginal cream and 100 and 200 mg vaginal suppositories
Aerosol powder
Cleanse skin with soap and water.
Dry thoroughly.
Shake aerosol well before using.
Apply or spray a thin layer over the affected area in the morning and up to
bedtime.
Do it from a distance of 6-10 inches to the affected area of the feet. Do not
inhale powder.
If no improvement in 2 weeks time, see doctor But continue fir 1-2
weeks after symptoms disappear to a maximum of 4 weeks. Jock itch and
ringworm is 1-2 weeks resolution; athletes foot-4 weeks.
Cream Apply sparingly, smoothen well and avoid maceration. Massage
area gently. Athletes foot: dry feet, wear cotton socks
CPS, 2004, page 1246
Tolnaftate
Category
Mechanism
Therapeutic use
Side effects
Administration
Administration
Warning
Contraindication
Reference:
Fungistic, fungicidal
Damage hyphae and stunt mycelial growth in susceptible fungi
Jock itch, athletes foot, ringworm; T. pedis, M. canis, Aspergillus niger,
C. albicans, M. gypseum, M. audounii, M. japonicum, T. rubrum, T,
mentagrophytes, T. schonleinii, A. fumigatus
Slight irritation, sting (aerosol solution), burning and itching of athletes
foot and jock itch should decrease with in 2-3 days
Do not apply dressings, or mix cosmetics or other skin medications with
tolnaftate treatment.
Powder: Clean and dry affected area. Sprinkle it b/n toes and in socks and
shoes treated lightly.
Spray should be shaken well before use. Apply it from a distance of at
least six inches away. Continue treatment until symptoms disappear. A
total of 4-6 weeks necessary. Do not inhale powder, bring close to a hot
object or flame
Cream. Thoroughly clean the infected area. Allow it to dry and then rub
gently the medication until most of it disappears. Use sufficient quantity
to cover the affected area. Wash hands after application.
Solution. If it solidifies, dissolve by warming the closed container in
warm water then follow dosage as directed.
Usually, applied in affected areas 2x a day. If no effect in 4 weeks, check
with health care professional.
Aerosols: Flammable
Allergies to tolnaftate or any preservatives, dyes; pregnancy; children, 2
y/o
Comprehensive Pharmacy Review, 5th Ed. Page 801
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Antifungals
Antifungals Tips
Nystatin is indicated
Ketoconazole require acidic conditions for higher bioavailability therefore
Meningitis fungal infections other CNS infections can be treated by
If a child swallowed 5g of nystatin, and parents are panic, comes to your pharmacy, what is
appropriate action
Nystatin is ineffective for
DOC for oral thrush
DOC for vaginal candidasis
Topcal Drug of choice for Atheletes foot
Nystatin suspension counseling
Amphotericin B is act by inhibiting the cell membrane function
Fungistic, Fungicidal
Tri-Statin, Mycolog, Mytrex
Diflucan
Sppranox
Clotrimazole, Cruex, Lotrimin, Mycelex
Aloe Vesta, Cruex, Desenex Jock Itch
Asorbine, Afate, Genaspore, Pitrex
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Anti-Mycobacterial Drugs
40
Anti-Mycobacterial Drugs
Antimycobacterial drugs
Isoniazid
Rifampin
Streptomycin
Pyrazinamide
Ethambutol
Capreomycin
Rifabutin
Tuberculosis treatment:
Goal of treatment is must eradicate mycobacterium.
Important issues in tuberculosis treatment are resistance to drugs.
Drugs that have lowest resistance is:Isoniazid, rifampin, streptomycin and combination of these
drugs with pyrazinamide, or ethambutol.
Drug of choice is combination of Isoniazid + rifampin + pyrazinamide.
Antimycobacterial Drugs
Rifampin
Chemical structure of rifampin is a macrocyclin.
This drugs is bactericidal
Mechanism
Inhibits RNA synthesis
Therapeutic Use
Effective against M. tuberculosis, and M. leprae
Prophylactic for house hold members of exposed to meningitis caused by
meningococci or H. influenza type b
Side Effects
Serious liver toxicity (hepatotoxicity) thereby LFT should be performed
regularly
GI SE: nausea, vomiting, abdominal pain
CNS SE: Headache, drowsiness, confusion, fatigue
Rifampin discolor urine, sweat, tears, saliva and feces to orange-red.
Drug interactions
Rifampin is inducer of CYP 1A2, 2D6, 2C9, 2C19, 3A4
Reduce efficacy oral contraceptive.
Isoniazid (INH)
Mechanism
Therapeutic Use
Side Effects
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Side Effects
Anti-Mycobacterial Drugs
Antimycobacterials Tips
Isoniazid
Liver Funtion Test
Extensive Drug Resistance Tuberculosis.
Pyrazinamide
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Anti-viral Drugs
41
Anti-viral Drugs
Antivir al Agents
Tricyclic
amines
Amantadine
Rimantadine
Guanosine
analogs
Ribavirin
Glycoproteins
Nucleoside
analogs
Nucleoside
RTIs
NNRTIs
Interferon-alfa
Interferon-beta
Acyclovir
Valacyclovir
Ganciclovir
Trifluridine
Vidarabine
Zidovudine
Didanosine
Zalcitabine
Lamivudine
Stavudine
Abacavir
Nevirapine
Delavirdine
Efavirenz
Neuroamindiase inhibitor
Osaltamavir
Zanamavir
Antivirals Drugs classifications
For RNA viruses Amantadine
Ribavirin
Rimantadine
Zidovudine
Didanosine
Zalcitabine
Stavudine
Lamivudine
Nevirapine
For DNA viruses Acyclovir
Ganciclovir
Famciclovir
For RNA and
Foscarnet
DNA viruses
Ribavirin
Mechanism
Therapeutic use
Foscarnet
Protease
inhibitors
Indinavir
Saquinavir
Ritonavir
Amprenavir
Antiretroviral
Acyclovir (zovirax)
Prophosphanate
derivative
Saquinavir
Ritonavir
Indinavir
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Side effects
Advantage
Dosage
Anti-viral Drugs
Antiretroviral drugs:
Retrovirus: Virus that contain reverse transcriptase enzyme such as HIV is referred as retrovirus
There are three classes of antiretroviral drugs: NRTI, NNRTI and Protease Inhibitors;
Nucleoside reverse transcriptase inhibitors (NRTI) phosphorylate by human cellular kinases.
Non nucleoside reverse transcriptase inhibitors (NNRTI)- phosphorylate by human cellular kinases.
Protease inhibitors: viral protease
Zidovudine (AZT)
Mechanism
Therapeutic use
Side effects
Didanosine (ddl)
Mechanism
Therapeutic use
Side effects
Monitor
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Anti-viral Drugs
Zalcitabine (ddc)
Mechanism
Therapeutic use
Side effects
Monitor
Avoid
Stavudine (d4T)
Mechanism
Side effects
Monitor
Lamivudine (3TC)
Mechanism
Therapeutic use
Side effects
Monitor
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Anti-viral Drugs
Zovirax
AZT Retrovir
Videx, Videx EC
Hivid
Zerit
Epivir
Tamiflu
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Anti-Malarial Drugs
42
Anti-Malarial Drugs
Malaria is infection of red blood cells with the single-celled parasite Plasmodium, which causes
fever, an enlarged spleen, and anemia.
Four species of malaria parasites--Plasmodium falciparum, Plasmodium vivax, Plasmodium ovale,
and Plasmodium malariae--can infect people.
Falciparum malaria, caused by Plasmodium falciparum, is the most dangerous form of malaria and
can be fatal.
Blackwater fever is an uncommon complication of falciparum malaria.
Chloroquine is the drug of choice for treatment in a person who has malaria caused by Plasmodium
vivax, Plasmodium ovale, or Plasmodium malariae--except in a very few areas where resistance to
chloroquine in people with Plasmodium vivax has been reported.
Chloroquine is the preferred drug for prevention of malaria caused by Plasmodium falciparum in
Mexico, areas of Central America west of the Panama Canal, Haiti, the Dominican Republic, and
some areas of the Middle East.
Primaquine is added to kill persistent parasites in the liver of a person infected with Plasmodium
vivax or Plasmodium ovale. Before primaquine is given, a blood test is done to look for a relatively
common enzyme deficiency (G6PD deficiency). People with G6PD deficiency who are given
primaquine may have a breakdown of their red blood cells.
Treatment of malaria
Prophylaxis
P. falciparum
P. malariae
P. vivax
P. ovale
Chloroquine resistant
prohylaxis
Treatment
Pyrimethamine/sulfadoxine
Chloroquine
Chloroquine
Chloroquine + primaquine
Chloroquine + primaquine
Primaquine, Quinine + doxycycline: Mefloquine, atovaquoneproguanil.
Quinine or mefloquine or pyrimethamine/sulfoxine
Retinopathy
Nausea, dizziness, and trouble sleeping, may rarely produce seizures
or psychiatric problems. Should also be avoided in people with
certain heart conditions.
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Quinine
Atovaquone-proguanil
Anti-Malarial Drugs
Mefloquin prophylaxis:
Chloroquin resistant area prophylaxis is:
Chloroquin resistant area treatment:.
Plasmodium vivax and ovale infections, treatment must include
Cinchonism is caused by?
Chloroquine side effect include:
Glucose-6-phosphate dehydrogenase
Ara;em
Radical cure
Adoxa Pak, Adoxa, Alodox , Atridox, Bio-Tab
Lariam
Malarone, Malarone Pediatric
Daraprim
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Travellers Diarrhea
43
Travellers Diarrhea
Travellers diarrhea also known as infections diarrhea. Organisms commonly implicated in the
cause of Travellers Diarrhea:
Escherichia coli.
Shigella sp.
Compylobacter jejuni
Shigella diarrhea diarrhea characterized as dysentery (bloody diarrhea).
Effective drugs in the prevention of Travellers Diarrhea:
Ciprofloxacin is the DOC for travelers diarrhea.
Alternate DOC is Cotrimoxazole
PreventionDoxycycline or ciprofloxacin
Traveller to Thailand: Azithromycin is the DOC for travelers diarrhea
The antibiotic most commonly recommended is ciprofloxacin.
Non prescription drugs:
Bismuth subsalicylate, a nonprescription drug. Causes black stools and tongue.
Loperamide (immodium): Treatment of diarrhea.
Bismuth subsalicylate can be used as prophylaxis or treatment. However loparamide is only used
upon appear of symptoms of diarrhea
When symptoms occur, treatment includes drinking plenty of fluids and eating a bland diet (for
example, cooked cereals, bananas, rice, applesauce, and toast). In addition, antibiotics (such as
ciprofloxacin) and antidiarrheal drugs (such as Lopramide or bismuth) are usually recommended.
Travelers are encouraged to seek medical care if they develop fever or blood in the stool.
Drug of Choice
Immodium
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Travellers Diarrhea
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Anti-Helments Drugs
44
Anti-HelminthicDrugs
Helminthic
Species
Common infections
Round worm
Ingestion
Hook worm
Percutaneous
Trichuris trichuria
Whipworm
Ingestion
Enterobius
vermiculars
Strongyloides
Pinworm
Threadworm
Filariasis
Percutaneous
Diethylcarbamzine
River blindness/
onchoceriasis
Trichinosis
Percutaneous
Livermectin
Ingestion
Thiabendazole
Pork
beef
Ingestion
ingestion
Niclosamide
Niclosamide
Fish
ingestion
Niclosamide
Intestinal
nematodes
Ascaris
lumbricoides
Necator
americanus
Tissue nematodes
Wuchereria
bancrofti
Onchocerca
volvulus
Trichinella spiralis
Cestodes
(tapeworms)
Taenia solium
Taenia saginata
Diphyllobothrium
latum
Hymenolepis nana
Trematodes
(flukes)
Schistosoma
mansoni
Schistosoma
haematobium
Clonorchis sinesis
Fasciolopsis
Pragonimus
Dwarf
Blood
Mebendazole
Praziquantel, niclosamide
Percutaneous
bilharziasis
Liver
Intestinal
Lung
Pyrantel pamoate,
mebendazole
Pyrantel pamoate,
mebendazole
Praziquantel
Praziquantel
ingestion
Ingestion
Ingestion
Praziquantel
Praziquantel
Praziquantel
Mebendazole:
Mechanism: Inhibits microtubule synthesis and glucose uptake in nematodes
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Anti-Helments Drugs
44 - 2