Princess Jovelyn Gutierez

NERVOUS SYSTEM AGENTS

REVIEW OF ANATOMY AND PHYSIOLOGY

NERVOUS SYSTEM

A. CENTRAL NERVOUS SYSTEM B. PERIPHERAL NERVOUS SYSTEM

1. Brain
2. Spinal cord
Parasympathetic Nerves {Rest and digest}
 Constrict pupils
 Stimulate saliva
 Slow heart beat
 Constrict airways
 Stimulate activity of stomachs
 Inhibit release of glucose
 Stimulate gallbladder
 Stimulate activity of intestines
 Contract bladder
 Promote erection of genitals
1.SOMATIC NERVOUS SYSTEM- voluntary;
skeletal muscles and sensory information
 AFFERENT –SENSORY NEURON
 EFFERENT –MOTOR NEURONS
2. AUTONOMIC NERVOUS SYSTEM-
involuntary; cardiac and smooth muscles;
glandular secretions
A. Sympathetic (Fight or Flight System)
B. Parasympathetic (Energy Conservation)
Sympathetic Nerves {Fight or Flight}
 dilate pupils
 inhibits saliva
 increase beat
 relax airways
 inhibits activity of stomachs
 stimulate release of glucose
 inhibit gallbladder
 inhibit activity of intestines
 relax bladder
 Promote ejaculation

SYMPATHETIC NERVOUS SYSTEM

• Adrenergic system has norephinepine the neurotransmitter that innervated the smooth muscles.

• alpha1

• alpha2

• beta1

• beta2

• Allows the body to function under stress

• Fight or fight system

Adrenoreceptor
A1 A2 B1
 Vasoconstriction  Inhibition of  Tachycardia
 Increased peripheral norepinephrine  Increased lipolysis
resistance release  Increased myocardial contractility
 Increase blood  Inhibition of  Increased release of renin
receptors acetylcholine
 Mydriasis release
 Increased closure of  Inhibition of
internal sphincter of insulin release
the bladder
Drugs that can cross BBB

Blood brain barrier – prevents drugs from entering cns

 1. Chemotherapeutic drugs
2. Opioid
3. Analgesic

Sympathetic

• Sympathomimetic (adrenergic) = sympathetic stimulants

• Sympatholytic (adrenergic blockers) = sympathetic depressant

• norepinephrine bitartrate, (Levophed)epinephrine, (adrenalin)dopamine (Inotroopin)

• dobutamine (Dobutrext)isoproterenol (Isuprel)

A. SYMPATHOMIMETIC (ADRENERGIC) B. SYMPATHOLYTICAGENTS (ADRENERGIC

AGENTS BLOCKERS)
• Affect both alpha- and beta-adrenergic • Drugs that block the effect of the
receptors sympathetic NS
• Actions: • (LIKE TAKING YOUR FOOT OFF THE GAS)
+ inotropic: increase force of contraction
of heart
+ chronotropic: increase rate of
heartbeat
+ dromotropic: increase conduction of
impulse
1. Alpha Adrenergic Blockers

• Drug classes:

non-selective:

• phentolamine
• phenoxybenzamine
• labetalol

selective:

• α1  prazosin (Minipress)terazosin (Hytrin)

• α2  yohimbine

• Actions: interrupt or antagonize the sympathomimetic agents

• Vasodilate vascular smooth muscle

• Lower peripheral vascular resistance

2. Beta adrenergic blockers

• Drug classes:

non-selective:

• propranolol (Inderal)
• timolol
• pindolol (Visken)

• selective (β1):

• Metoprolol (Neobloc, Betaloc, Cardiosel)

• atenolol (Tenormin, Cardioten, Durabeta)
• esmolol (Brevibloc)

• Action: block sympathetic response by competing for beta receptors; also block stimulation of
the heart and have the potential to block bronchodilation.
 • Uses: hypertension migraine, headaches, angina, myocardial infraction, tachyarrhythmias,
anxiety

• Side effects: bradycardia, hypoglycemia, orthostatic hypotension, impotence, bronchospasm,

depression

• Nursing implications:

• Monitor vital signs for bradycardia and hypotension

• Monitor blood glucose for hypoglycemia

• Advise the client about the possibility of impotence

• Advise the client not to use OTC drugs such as decongestants

• Action: block sympathetic response by competing for beta receptors; also block stimulation of
the heart and have the potential to block bronchodilation.

• Uses: hypertension migraine, headaches, angina, myocardial infraction, tachyarrhythmias,

anxiety

• Side effects: bradycardia, hypoglycemia, orthostatic hypotension, impotence, bronchospasm,

depression

• Nursing implications:

• Monitor vital signs for bradycardia and hypotension

• Monitor blood glucose for hypoglycemia

• Advise the client about the possibility of impotence

• Advise the client not to use OTC drugs such as decongestants

PARASYMPATHETIC NERVOUS SYSTEM

• Cholinergic system –

acetylcholine –

neurotransmitter that innervates the muscles.

• nicotinic
• muscarinic

Regulates vegetative functions

Rest and Digest

• These two systems work in constant opposition to control organ response

Parasympathetic

• Parasympathomimetic(cholinergic) = parasympathetic stimulants

• Parasympatholytic(anticholinergics) = parasympathetic depressants

Nicotinic Receptors
N1 or Nm N2 o Nn
Neuromuscular junction Autonomic ganglia
Central Nervous System
Adrenal Medulla
 Muscarinic Receptor
M1 M2 M3 M4
Striatum Forebrain Brain Striatum Dopaminergic
Cortex Thalamus Hypothalamus Cortex neurons
Hippocampus Heat Pupils Hippocampus Basal ganglia
Pupil Exocrine Spinal cord Brain
Spinal Cord Peripheral arteries vasculature
Exocrine

C.PARASYMPATHOMIMETIC AGENTS (CHOLONERGIC AGENTS}

Drugs that causes the same effect as stimulation of parasympathetic CNS (LIKE PUTTING
YOUR FOOT ON THE BRAKE)

Direct-acting cholinergic agonists

• Action: mimics acetylcholine to produce parasympathetic stimulation (binds directly with Ach
receptors)

• Prototype drugs:

• Bethanicol chloride for bladder

• atony,
• pilocarpineHCI (Pilomann, Pilogel)for glaucoma

Causes: salivation, urination, defecation, sweating, vomiting, and abdominal cramps. • Uses:
glaucoma, bladder atony

• Side effects: hypotension, hypersalivation, hyperhidrosis, nausea, vomiting, diarrhea.

1. Muscarinic Antagonists

• atropine->preop med; for organophosphate poisoning

• scopolamine->motion sickness

• oxybotin->urinary incontinence

• ipratropium->for asthma

• dicyclomine->for GI spasms

action: compete with acetylcholine at muscarinic receptors

uses: preoperatively given to reduce salivation and gastric secretions

 Increase heat rate force

 Relaxation of smooth muscle
 Secretion of glands
 Restlessness and amnesia

Side Effects:

 Hot as Hare- high temp

 Mad as Hatter- confusion delirium
 Red as beet- flushed face
 Dry as Bone- Decreased secretion, thirsty

Nursing implications:

• provide comfort measures for side effects

• encourage fluids to decrease risk of constipation

• monitor vital signs

• 2. Nicotinic Antagonists

• a. Ganglion-blocking drugs

action: block ganglionic nicotinic receptors in both sympathetic and Parasympathetic NS

• hexamethonium
• Mecamylamine
• Trimethaphan-> Used for hypertensive crisis

used: hypertensive crisis-> produce hypotension

effects: PS-> salivation, peristalsis, gastric acid

• S-> inc.HR, dec.SV, inc. PVR, inc.

awareness, Dec. Fatigue, Dec. Appetite

Side effects: marked venous pooling-> postural hypotension

• b. Neuromuscular blocking drugs

• action: block nicotinic receptors at muscle level->producing muscle paralysis.

tubocurarine, vecuroniumpancuronium, gallamine, atracurium

• compete with Ach for the receptor sites on motor end plates or by blocking depolarization

• uses: facilitate endotracheal intubation decrease the number of anesthetics to be used relaxed
skeletal muscles of intubated patients

• side effects: hypotension, tachycardia, dysrhythmia, respiratory depression

3. Ganglionic blockers

• Prototype drugs: trimethaphan, mecamylamine

• Not commonly used because it is non-selective

• Action: compete with acetylcholine and affect both sympathetic and parasympathetic systems

• Uses: hypertension especially hypertensive crisis

• Pulmonary edema resulting from pulmonary hypertension

• Side effects: hypotension, bradycardia, anticholinergic effects (dry mouth, dilated pupils,
tachycardia, decreased GI and urinary motility)

CENTRAL NERVOUS SYSTEM (CNS) MEDICATIONS

A. CNS Stimulants

• Drugs used are limited to the treatment of narcolepsy, attention deficit disorder in children,
obesity and reversal of respiratory distress.

• STIMULANT –a substance that quickens the activity of the CNS by increasing the rate of
neuronal discharge or by blocking an inhibitory neurotransmitter.

• Classification: CNS Stimulants

• Amphetamines
• Anorexiants
• Analeptics

1. AMPHETAMINES AND AMPHETAMINE-LIKE DRUGS

Action: stimulate the release of norepinephrine, which causes increased alertness, less fatigue
and elevate the mood.

Common drugs:
 • Methylphenidate (Ritalin, Concerta) –for ADHD most commonly
• Pemoline (Cylert)
• Dextroamphetamine
• sulfate (Dexedrine, Adderall)
• Methamphetamine HCL (Desoxyn)

Uses:

Narcolepsy- Characterized by sudden sleep attack

Endogenous obesity - Obesity resulting from dysfunction of the endocrine or metabolic systems.
Amphetamines suppress the appetite

Attention Deficit hyperactivity Disorder (ADHD) - Childhood condition involving inattention,

impulsivity and hyperactivity

Amphetamine increase attention span while decreasing the hyperactivity

Mental depression – elevate the mood.

• Major side effects:

• Tolerance, dependence, abusive

• Nervousness, irritability, increased motor activity
• Headaches, dizziness, insomnia
• CV: HPN, palpitations, dysrhythmia
• Weight loss and fatigue from prolonged use
• Drug –drug Interactions:

• Antidepressants-increase the effect

Nursing Applications:

• Weight reduction diet and exercise program should accompany the use of these
agents for obesity. Short term is recommended
• Check with pharmacist about all OTC medications
• Do not abruptly stop taking the drugs
• Do not try to make up dose if one is skipped
• If diabetic, check whether insulin or hypoglygemicagents may be reduced
• Avoid other stimulants while on these drugs
• Avoid taking the last dose after 4 to 6 PM to prevent insomnia

2. ANOREXIANTS

Action: suppress the appetite by acting on the hypothalamus

Use: weight reduction when accompanied by medical complications

Tolerance and abuse are possible

Common drugs:

Benzphetamine HCL (Didrex)

Diethylpropion (tenuate, Tepanil, Dospan)

Phenmetrazine HCL (Preludin)

Phentermine HCL (Adipex-P, lonamin)

Dextroamphetamine sulfate (Dexedrine)

3. ANALEPTICS

Action: stimulates the CNS by acting on the cerebral cortex and the medulla

Uses:
• Respiratory stimulation primary use

Common drugs:

• Methylxanthines: theophylline (used for asthma), theobromide

• Respiratory stimulant: DoxapramHCL (Dopram)
• caffeine (85 mg/cup of coffee, 50 mg/cup of tea or cola),

Major side Effects:

CV: dysrhythmias, heart attacks, tachycardia, HPN, tachypnea

• Caffeinism: restlessness, insomnia, nervousness, muscle twitching, headache

• Seizures

• Tolerance and abuse

Nursing implication

• Monitor the dietary intake of caffeine

• Assess respiratory and CV systems
• Watch for withdrawal symptoms: nausea, vomiting, headache
• Avoid other foods and drinks that contain stimulants

CNS DEPRESSANTS

• Sedative-hypnotics • Anesthetics
• Analgesics
• Anticonvulsants
• Anxiolytics
• Antidepressants

1. SEDATIVE-HYPNOTICS

• SEDATIVE- agent that produces a state of calmness

• HYPNOTIC- an agent given at bedtime to induce sleep (usually in a larger dosage than a sedative

CATEGORIES OF SEDATIVE-HYPNOTICS:

a. Barbiturates

Common drugs:

• Phenobarbital (Luminal), mephobarbital

• amobarbital (Amytal), butarbital
• secobarbital (Seconal)
 pentobarbital (Nembutal)
• thiopental sodium (Pentothal)

Methohexital

Action: produce various levels of CNS depression by decreasing the excitability of synaptic
membranes in the cerebral cortex

Uses:

• Sedative and hypnotic

• Preoperatively and as anesthetic
• Anticonvulsant (e.g. phenobarbital)

Major side Effects:

• Excessive CNS depression: dizziness, drowsiness, hang-over effect, convulsion

• Rebound insomnia, respiratory depression
• Anxiety, hypersensitivity
 • Interacts with alcohol and narcotics which may further depress the CNS

Nursing implications:

• Teach safety precautions to clients

• Assess level of consciousness, respiratory status, and effectiveness of the agent
• Hold if respirations are <10/min.
o Do not abruptly stop the medication for those on chronic use.

b. Benzodiazepines

Common drugs:

• flurazepam (Dalmane)
• estozolam (Esilgan)
• temazepam
• triazolam
• quazepam

• Action: increase in GABA (inhibitor)calming effect

Uses:

• Insomnia
• Preoperative medication
• Anxiety
• Sleep induction
• Prolonged hypnotic therapy
• Withdrawal syndromes

Major side effects:

• Drowsiness, hypertension, slurred speech, memory impairment, hangover effect, dizziness,

respiratory depression

2. ANESTHETICS

ANESTHESIA- the loss of sensation as a result of reversible CNS depression

Classification of anesthetics

a. General

• Agents which cause reversible loss of consciousness due to loss of CNS activity
• Depress the CNS, alleviate pain and cause a great loss of consciousness

b. Local

Agents which cause reversible loss of pain sensation without loss of consciousness

Blocks pain at the site where the drug is administered

1. Barbiturates

• e.g. thiopental sodium (Pentothal)

• most commonly used IV anesthetic

• 2. Benzodiazepine

• diazepam, lorazepam, midazolam • can cause anterograde amnesia

3. Ketamine hydrochloride

• for children and patients with hypotension • used for short surgical procedures

4. Propofol

• produce anesthesia at a rate similar to that of barbiturate • can cause respiratory depression
Major side effects: hangover effect, apnea, laryngospasm, bronchospasm, coughing, CVS
depression

Nursing implication

• Have emergency equipment and IV fluids ready • Know each individual drug
• Practice and stress safety measures
• Monitor vital signs
• Monitor elimination and status (urine output)
• Cautiously administer analgesics

LOCAL ANESTHETICS

• These drugs are given to block nerve impulses and decrease the ability of the cell to depolarize
which is necessary for impulse transmission, block the pain at the site where the drug is
administered, allowing consciousness to be maintained •

Uses: dental procedures

• Suturing skin lacerations

• Performing minor surgery
• Blocking the nerve impulse
• Performing diagnostic procedures

3. ANALGESICS

ANALGESICS – drugs that relieve the sensation of pain

Types of Analgesics:

a. Nonnarcotic Analgesics

• not addictive and are less potent than narcotic analgesics

• used to treat mild to moderate pain have analgesic and antipyretic action

actions:

• inhibits cyclooxygenase (produces COX-1 and 2)

• COX –1  protects stomach lining increases temperature, promotes platelet
aggregation
• COX –2  triggers pain and inflammation
• Inhibit the formation or reactivity of prostaglandins and thus also control fever.

types:

a.1. Salicylates

• e.g. aspirin  oldest nonnarcotic analgesic

• contraindicated in children < 12 years of age (danger of Reye’s syndrome)
• effect: analgesic, antipyretic, anti-inflammatory, decreases platelet aggregation

a.2. Non-steroidal anti-inflammatory drugs (NSAIDs)

• non-selective: ibuprofen, naproxen

• COX-2 selective: celecoxib, meloxicam

a.3. Para-aminophenol’s

• e.g. acetaminophen (administered q4h as needed with a maximum dose of 4g/day)

• effect: analgesic and antipyretic • (NOT anti-inflammatory)

nursing implication:

• assess temperature every 4 hours

• check liver enzymes for those taking high doses
• evaluate the degree of pain relief obtain
b. Narcotic or opioid

analgesics:

• act mostly on the CNS

• uses: analgesia (moderate to severe pain)

• cough suppression (antitussive) • anesthesia

Examples:

• meperidine (Demerol)  diphenoxylate

• codeine  dextromethorphan
• methadone
• fentanyl (Sublimaze)
• oxycodone (Percocet)
• nalbuphine (Nubain)
• butorphanol tartrate (Stanol)
• naloxone (Narcan)

• drug interactions: CNS depressants 

additive effect

• smoking  decreased effect

Nursing implications

• assess respiratory status

• assess for hypotension
• monitor bowel elimination
• evaluate pain response to medication
• implement and teach client about safety
• do not administer to client with head injuries.

4. Anticonvulsants

• ANTICONVULSANT –substance that prevents, reduces, or stops the severity of epileptic or

other convulsive disorders.

Mechanisms:

• Suppress sodium influx → prolonging channel inactivation → prevents neuron firing

• Suppress calcium influx → prevents electric current generated
• Increase the action of GABA

Pathophysiology

GABA- main inhibitory neuro transmitter

Glutamate-the major excitatory neurotransmitter

ANTISEIZURE DRUGS

Tonic-clonic And Absence Seizures Broad Spectrum Adjunct

Partial Seizures
Carbamazepine Ethosuximide Valproic Acid (Lamotrigine)
Phenytoin [and broad (Clonazepam) Gabapentin
Phenobarbital spectrum]
[and broad
spectrum]
LORAZEPAM or DIAZEPAM i.v RX tonic-clonic epilepticus

CLONAZEPAM is an alternative drug due to sedation and intolerance

Benzodiazepine mechanism of action

 If seizure does not resolve after a few minutes give a benzodiazepine

 Enhances the inhibitory effect of GABA
 Reduces excessive neuronal firing.

Sodium Valproate mechanism of action

 Inhibits GABA transaminase (inhibits GABA breakdown)

 Enhances the inhibitory effect of GABA
 Reduces excessive neuronal firing.

NURSING CONSIDERATIONS

o CNS: dizziness
o Eat food with drug
o Antacids decrease
o Support group for epileptics
o Alert tag indicating specific drug
o Report adverse effects

• Anxiolytics or Antianxiety Drugs • Action: to enhance the effect of GABA (Gamma Aminobutyric
Acid), an inhibitory neurotransmitter to decrease impulses in the synapses of the brain,
therefore decreasing conduction of rapid impulses causing symptoms of anxiety. Depression of
the CNS, produces relaxation.

• Common Drugs:

• Benzodiazepines: diazepam (Valium)

• Alprazolam (Xanor)
• Lorazepam (Ativan)
• Antihistamines: diphenhydramine (Benadryl)
• Other agents: hydroxyzine HCL (iterax)

Mechanism of action

 Barbiturates increases duration

 Benzodiazepines increases opening of cl channel
 At higher dose barbiturates can act as a gaba mimetic

NURSING CONSIDERATIONS

• Avoid abrupt discontinuation after prolonged use

• Not given if BP is decreased, with renal/hepatic dysfunction, or history of drug
abuse
• Xanax (Alprazolam), Ativan (Lorazepam), Serax (Oxazepam) -examples with brand
names
• Increase in 3Ds -drowsiness, dizziness, and decrease in BP
• Enhance action of GABA
• Teach to rise slowly from supine
• Yes, alcohol and caffeine should be avoided

Antidepressants and Mood Stabilizers

a. Tricyclic antidepressants (TCAs)

Common drugs: amitriptyline doxepin imipramine (Tofranil)

Action: increases neurotransmitter concentration levels of NE and serotonin.

Major side effects: sedation, orthostatic

hypotension, anticholinergic effect
Nursing implication

• It will take 1 to 3 weeks before the drug will take effect.

• Drug can mask suicidal tendencies.
• Institute safety measures.

• b. Monoamine oxidase inhibitors (MAOIs)

• Common drugs:

• Phenelzine sulfate
• Tranylycprominesulphate
• • Isocarboxazid

• Action: inhibit MAO enzymes (present in the brain, blood platelets, liver, spleen and kidneys)
that metabolizes NE and serotonin.

• Uses: 2nd line antidepressant

• Side effects: hypertensive crisis (if given with tyramine rich foods like cheese, yogurt, red
wines), CNS stimulation (anxiety, agitation, mania), orthostatic hypotension.

C. Selective serotonin reuptake inhibitors (SSRIs)

• Common drugs: fluoxetine (Prozac)

• Sertraline (Zoloft)

• Paroxetine (Seroxat)

• Action: antidepressant response is from the inhibition of the serotonin uptake

• Uses: depression, obsessive-

compulsive disorders disorders

• Side effects: nausea, diarrhea, CNS stimulation insomnia, headache, nervousness, dizziness),
skin rash

• Nursing implication:

• administer with meals to reduce nausea

• use cautiously in patients with impaired renal function

Upper Respiratory Tract Infections (URTI)

URTI includes:

 Common cold
 Acute rhinitis
 Sinusitis
 Acute pharyngitis

Common cold:

  The common cold is a viral infection of your nose and throat. (nasopharynx)
  Caused by rhinovirus (most common), influenza, parainfluenza, adenovirus.

Acute rhinitis

- acute inflammation of the mucous membranes of the nose.

 Sinusitis

- an inflammation or swelling of the tissue lining the sinuses. Healthy sinuses are filled with air.

 Acute pharyngitis
- is an inflammation of the back of the throat, otherwise known as the pharynx.

I. DRUGS FOR UPPER RESPIRATORY DISORDER

1. Antihistamines (H1 blockers or H1 antagonists)

Histamine- a compound found in cells and released in allergic, inflammatory reaction with
resultant dilatation of capillaries, decreased BP, increased gastric secretion and constriction of
the smooth muscle of the bronchi and uterus. H1 receptors –Found in lungs (binding results in
bronchoconstriction).

H2 receptors- found in stomach (binding results in increase gastric acid secretion)

Action of antihistamines: blocks H1 receptors thereby decreasing allergic response.

A. 1st generation antihistamines

 diphenhydramine (Benadryl AH)

 brompheniramine (Dimetapp, Nasatapp)

 chlorpheniramine (Decolgen, Neozep)

 hydroxyzine (Iterax)

 meclizine (Bonamine)

B. 2nd generation antihistamines:

 cetirizine (Virlix, Zyrtec)

 fexofenadine (Telfast)

 loratadine (Claritin, Lordex, Claricort, Clarinase)

Indications:

1. Allergic rhinitis

2. Common colds.

3. Allergic responses: itchy, watery eyes.

4. Sinusitis

5. Prevent motion sickness.

6. Sleep aid.

Nursing implications:  Take at bedtime if possible, to avoid sedation during the day.

 If taken during the day, caution the client about safety measure with driving, operating
machinery and ambulating. Sedation usually decreases with repeated doses.

 Caution older adults in particular about sedation effects.

 Avoid alcohol and other CNS depressants.

 Give with food to decrease gastric distress.

2. DECONGESTANTS (sympathomimetic amines)

 A substance that eliminates or reduces congestion or swelling, especially in the mucous

membrane

Action: stimulate the alpha-adrenergic receptors → vasoconstriction of capillaries within nasal

mucosa →

shrink nasal mucous membranes →

↓ fluid secretion
Indications: sinusitis, allergic rhinitis, acute coryza (profuse nasal discharge), otitis media

Common Decongestants:

Vicks Sinex(oxymetazoline)

Sudafed PE, (phenylephrine)

Sudafed, Suphedrin

(pseudoephedrine)

3. EXPECTORANT

 an agent that promotes expectoration by reducing the viscosity of pulmonary secretion or by

decreasing the tenacity with which exudates adhere to the lower respiratory tract

Action:

 Guaifenesin- reduces adhesiveness and surface tension of fluids thinning of secretions →more
productive cough

 Iodide preparation act directly on bronchial tissue to increase the secretion of respiratory
fluids and decrease the viscosity of mucus

Indications: bronchitis, persistent cough, common colds

Common drugs:

 guaifenesin-Benadryl expectorant, Robitussin

 potassium iodide solution

 dextromenthorphan hydrobromide+ benzocaine -Formula 44, Vicks cough syrup 

ambroxolhydrochloride -Myracof

4. ANTITUSSIVE

 any of the large group of narcotic or nonnarcotic drug that act on the CNS peripheral nervous
system to suppress the cough reflex

 Nonnarcotic –suppress the cough reflex by numbing the stretch receptors in the respiratory
tract and preventing the cough reflex from being stimulated.

dextromethorphan (Robitussin DM. Streptuss)

diphenhydramineHCL (BenadrylAH) butamiratecitrate (Sinecod)

 Narcotic -suppress the cough reflex by direct action on the cough center in the medulla.
Codeine sulfate (CodiprontN)

Hydrocodone

Indication: mostly for nonproductive and irritating cough

Major side effects: dry secretions, drowsiness without respiratory depression, constipation,
narcotic abuse (for codeine and hydrocodone) Nursing implication:

 Waits 15 to 20 minutes after taking the syrup before drinking any liquid  Monitor use because
these are controlled substances

 Taken at bedtime

 Monitor bowel elimination

 Humidify air during sleep time to improve effectives

Interaction: a synergistic effect with alcohol and CNS depressant

II. DRUGS FOR LOWER RESPIRATORY DISORDER

Lower Respiratory Tract disorder

Common disorder:

 Infective: Pneumonia

 Non-infective: COPD

 Chronic bronchitis

 Bronchial asthma.

PNEUMONIA

 Infection of pulmonary parenchyma.

CHRONIC OBSTRUCTIVE PULMONARY DISEASE (COPD)

 A disease state characterized by the presence of airflow obstruction due to the chronic
bronchitis or emphysema.

CHRONIC BRONCHITIS a.k. a blue bloater, tussive or type B COPD)

 Excessive mucus secretion in the bronchial tree leading to productive cough for at least 3
months of two successive years.

BRONCHIAL ASTHMA

 Reversible airway obstruction that is characterized by hyperirritability and inflammation of the

airways.

 Chronically inflamed airway is hyperresponsive; they become obstructed and airflow is limited
(by bronchoconstriction, mucus plugs, and increased inflammation) when airways are exposed to
various risk factors.

 History of any of the following:

 Cough, worse particularly at night  Recurrent wheezing

 Recurrent difficult breathing

 Recurrent chest tightness

DRUGS USED TO TREAT LOWER RESPIRATORY DISORDERS

Bronchodilators

 1. Sympathomimetic

 2. Xanthine derivatives

 3. Anticholinergics

1. Sympathomimetics (Beta 2-Adrenergic Agonists)

-smooth muscle relaxation

Beta2 Agonist SMART

 Salmeterol
 Metaproterenol
 Albuterol-relaxes the bronchial smooth muscle and peripheral vasculative
 Ritodrine
 Terbutaline

B2 agonist short acting- 3-4 hrs. terbutaline salbutamol

B2 agonist long acting- 12 hrs. salmeterol formoterol

Nursing Considerations
 B – breathing and coughing techniques

 R – relaxation techniques

 E – evaluate vital signs

 A – appropriate positioning

 T – tremors

 H – have 8 or more glasses of fluids

 E – emphasize no smoking

2. Xanthine derivatives (Methylxanthines)

Common drugs:

 aminophylline–available only in IV

 theophylline (theo-dur, Nuelin, Uni-dur)

Side effects:

 Cardiac stimulation: tachyarrhythmias, tachycardia, angina, hypotension.

 GI distress: nausea (first sign of toxicity), vomiting, anorexia.

Drug interactions:

 Increased side effects with high intake of caffeine.

 Altered cardiac status with most of cardiac agents.

 Herbal interactions: ephedramay increase effect of theophylline.

Nursing implications:

 Give during the daytime to prevent insomnia.

 Monitor blood levels for toxicity: therapeutic blood level is 10 to 20ug/ml toxicity may
occur with small increase> 20ug/ml.

 > 20 ug/ml = nausea –1st sign

 > 35 ug/ml -tremors –late sign

3. Anticholinergics

Action: blocks Ach-muscarinic receptors; bronchodilation

Common drugs: Ipratropium bromide (Atrovent, Combivent)

 often in inhalation forms

Anti-Inflammatory

 Glucocorticoids

 Mast cell Stabilizers

 Leukotriene receptor Antagonist

Glucocorticoids

Action: anti-

inflammatory effect

 decrease inflammatory substances

 reduce mucus plugs and edema secondary to vascular permeability

Common drugs:

 oral:  prednisone (Pred, Organon)

methylprednisolone (Solumedrol, Depomedrol)

 parenteral: hydrocortisone, methyl prednisone

 inhaled: beclomethasone (Cyclocaps)

budesonide (Budecort, Symbicort*)

fluticasone (Flixotide, Seretide)

Nursing interventions:

 Do not administer the drug to treat an acute attack.

 Use bronchodilator before corticosteroid aerosol.

 Hold the inhaled drug for a few seconds before exhaling.

 Allow 1-3 minutes to elapse between each inhalation.

 Have the patient rinse the mouth after using the inhaler.

 Monitor for any sign of respiratory infection like sore throat or mouth sores.

 Must taper off gradually under provided supervision.

Mast Cell Stabilizers

 Anti-inflammatory agents

a. Cromlynsodium (Intal)

Action: inhibits the release of histamine Preparation: inhaler, nebulizing solutions

 Frequent daily dosing is required.

 May take 4-6 weeks for maximum effect.

b. Nedocromilsodium

Action: inhibits release of histamine and leukotrienes.

Indications: prevent bronchospasm and acute attack of asthma.

Nursing interventions:

 Drink water before and after inhalation (to lessen bad taste).

Leukotriene Receptor Antagonist

 a new class of drugs for asthma treatment, available in tablet form.  Mechanism of
action -

combination of both bronchodilator and anti-inflammatory effects.

 Common Drugs:

 zafirlukast (Accolate) and montelukast

(Singulair);

Nursing Considerations:

 assess respiratory status

 assess liver function tests

 medication does not treat acute asthma attacks

 GASTROINTESTINAL AGENTS

ANTIEMETICS

VOMITING (emesis) – the forceful expulsion of gastric contents thru the mouth  activation of
chemoreceptor trigger zone (CTZ) which lies near medulla → impulses to vomiting center (in
medulla) → vomiting

 activated by dopamine

 direct stimulation of vomiting center can trigger emesis

 stimulated by odor, smell, taste, gastric mucosal irritation, acetylcholine

Pathway Potentially Beneficial Drugs

Chemoreceptor trigger zone Dopamine and 5-HT3 serotonin receptor
Vestibular Cholinergic muscarinic receptors
Vomiting center pathways Histamine and cholinergic muscarinic
receptors
Gastric Stasis Dopamine and 5-HT$ serotine in receptor

1. Antihistamines

Action: act primarily on vomiting center

Common drugs: Antihistamines – meclizine (Bonamine)

promethazine (Phenergan)

hydroxyzine (Vistaril, Atarex)

Side effects:

 Drowsiness
 Confusion
 Dry mouth
 Dizziness
 Headaches

2. Anticholinergics

Action: act primarily on vomiting center

Common drugs: Anticholinergics – scopolamine (TransdermScoop)

3. Dopamine-antagonists

Action: block dopamine2 receptors in the CTZ depressing the medullary vomiting center.

Common drugs:  phenothiazine–chlorpromazine (Thorazine)

perphenazine (Trifalon)

 butyrophenone–e.g. haloperidol (Haldol)  metoclopramide (Plasil, Reglan)

Side effects: extra-pyramidal effect

 Pseudo parkinsonism
 Acute dystonia
 Tardive dyskinesia
 Akathisia

4. Serotonin (5-HT3) receptor antagonists

Action: block serotonin receptors (5-HT3) in the CTZ and the afferent vagusnerve terminals in
the upper GI tract
Common drugs: ondansetron (Zofran)

granisetron (Kytril)

dolasetron

 effective in suppressing nausea/vomiting caused by cancer chemotherapy

DRUGS USED TO TREAT DIARRHEA

DIARRHEA

Definition: passage of abnormally liquid or unformed stools at an increased frequency

 Fecal output > 200g/day on low-fiber diet

Anti-diarrheal Drugs

Common drugs:  loperamide (Imodium)

 opiates/ opiate derivates: codeine, diphenoxylate (Lomotil–with atropine)

 Adsorbents: kaolin pectin (kaopectate)

Action: block stimulation of GI tract  bismuth subsalicylate  inhibit local reflexes by coating
the lining of GI tract

 Loperamide  direct muscles of the GI tract to slow activity and allow increased time for
absorption of fluid and electrolytes

 opiates  action on CNS centers that cause GI spasm

1. Absorbents- drugs that increases the viscosity of luminal contents

2. Antimotility- Drugs that delay passage of gut contents

Side effects

  constipation
  abuse potential for opiates

Nursing implications:

  Check for dehydration

  Monitor response
  Administer drug after each unformed stool to ensure therapeutic effectiveness.

LAXATIVES

CONSTIPATION – persistent, difficult, infrequent or seemingly incomplete defecation

 Contributory factors: inactivity, low roughage diet and inadequate allotment of time for
defecation

Type of Laxatives

1. Bulk forming  natural fibrous, non-absorbable substances

Action: fluid in the intestinal contents →enlarges bulk →

stimulates local stretch receptors→ GI motility

Common drugs: methylcellulose (Cologel)

psyllium (Metamucil)

dietary fiber (Fibrosine)

lactulose (Duphalac)

2. Surfactant laxatives
 also known as emollients or lubricant laxatives Action: lowers surface tension and promote
water accumulation in the intestine

Common drugs: glycerin, mineral oil

Emollient: Stool softeners

Common drugs: docusate sodium (Colace)

docusate potassium (Dialose)

3. Stimulant/Contact laxatives

Action: directly stimulate the nerve plexus in the intestinal wall –stimulation of local reflexes
→ GI motility

Common drugs:

senna (Senokot)

castor oil

bisacodyl (Dulcolax)

4. Osmotic laxatives

Action: water retention (osmotic effect) –soft bulky stool -peristalsis -defecation

Common drugs: Magnesium OH-milk of Magnesia

 Magnesium citrate-citrate of Magnesia

 Sodium phosphate w/ sodium biphosphate-Fleet Enema

 Lactulose-Cephulac

Nursing implications

 Administer only as a temporary measure

 Arrange for appropriate dietary measures

 Do not administer in the presence of acute abdominal pain, nausea, or vomiting

 Monitor bowel function and side effects

 Assess fluid and electrolytes levels

DRUGS USED TO TREAT PEPTIC ULCER DISEASE and RELATED DISORDERS

ULCER – disruption of mucosal integrity of the stomach and or duodenum leading to defect or
excavation due to active inflammation.

 develop as a result of imbalance between defensive factors (mucosal protection and repair)
and aggressive factors (gastric acid, pepsin).

Pharmacologic Treatment

Acid-suppressing drugs

 Antacids

 H2 receptor antagonists

 Proton-pump inhibitors

Mucosal protective agents

 Sucralfate

 Prostaglandin analogue
 Bismuth-containing compounds
 A. Acid-Suppressing Drugs

1. Antacids

Action: neutralization of secreted acid

Common drugs:

 sodium bicarbonate (Alka-Seltzer)

 calcium carbonate (Tums)
 aluminum hydroxide (Amphogel)
 magnesium hydroxide
 aluminum hydroxide + magnesium hydroxide (Kremalin

S, Maalox)

Side effects

•  rebound acidity: stomach produces more acid in response to an alkaline

environment
•  constipation: if aluminum products are used  diarrhea: if magnesium product
used
•  fluid retention if sodium bicarbonate products are used
•  milk-alkali syndrome (alkalosis, renal calcium deposits, severe electrolyte
disorders): if calcium salts are used

Nursing implications:

•  Administer the drug apart from any other oral medications (1 hour before or 2
hours after) to ensure adequate absorption of other medications
•  Have patients chew tablets thoroughly and follow with water to ensure
therapeutic levels reach stomach (to decrease acid)
•  Periodically monitor serum electrolytes (to evaluate drug effects)
•  Assess patients for any signs of acid-base or electrolyte imbalance

2. H2 receptor antagonists

Action: selectively block histamine H2 receptor sites→

decrease gastric acid secretion and reduction in overall pepsin production.

Common drugs: cimetidine (Tagamet) → has antiandrogenic effects

ranitidine (Zantac)

famotidine (Pepcidin, H2 Bloc)

 cimetidine: anti-androgenic effects

 gynecomastia, galactorrhea, decreased libido, impotence

3. Proton-Pump Inhibitors (PPIs)

Action: inhibits the hydrogen/ potassium ATPaseenzyme system located in the gastric parietal
cells suppressing gastric acid secretion

 100% greater acid suppression than H2 blockers

Common drugs:

 omeprazole (Losec)
 lansoprazole (Lanz, Prevacid)
 rabeprazole (Pariet)
 pantoprazole (Pantoloc, Ulcepraz)
 esomeprazole (Nexium)

Nursing implications
 Should be taken before the meals (to ensure therapeutic effectiveness)

 Monitor patient response to drug and adverse effects

DRUGS AFFECTING THE CARDIOVASCULAR SYSTEM

HEART

chambers:

Right atrium → Tricuspid Valve

receives deoxygenated blood.

Right ventricle → Pulmonic valve

pumps blood to the pulmonary

artery.

Left atrium → Mitral valve

receives oxygenated blood.

Left ventricle → aortic valve

pumps blood into aorta for

systemic circulation.

Cardiac output the amount of blood ejected by each ventricle per min

CO = vol /min

Factors that affect the CO

1.Stroke Volume: the volume of blood pumped by the ventricles per beat

SV= ml/beat

contractility, preload and afterload

2.Heart Rate: the conduction system of the heart

HR=beats/min

FACTORS THAT AFFECT CARDIAC OUTPUT

CO= SV x HR

CO= SV (70ml/beat) x HR (65 beats/min)

CO=4,550ml/min

The amount of blood passing through the heart is about 4-8 liters/min

EFFECTS OF DRUGS ON HEART

1. Inotropic

•affects the force of contraction

•positive inotropic effect: ↑ myocardial contraction, ↑ renal blood flow

2. Chronotropic

•interferes with the rate of heart beat

•positive chronotropic effect: ↑ heart rate

3. Dromotropic

•pertains to conduction

•positive dromotropic effect: speeds up conduction

CARDIAC DRUGS

•Used in Hypertension

•Used in Angina Pectoris and Myocardial Infarction

•Used in Shock

•Used in Arrhythmias

•Used in CHF

HYPERTENSION

excessive high blood pressure

Factors the affect BP:

1.Contraction of the LV

2.Peripheral Vascular resistance

3.Elasticity of the arterial walls

4.Blood volume

BP HOMEOSTASIS

1.Baroreceptors

mechanoreceptors located in the carotid sinus and in the aortic arch.

bara receptors sense pressure changes and respond to change in the tension/stretch of the
arterial wall.

The baroreflex mechanism is a fast response to changes in blood pressure

HOW BARORECEPTORS REGULATE BLOOD PRESSURE

BARORECEPTORS
BP decreases ----- Baroreceptors signals to the adrenal medulla -------

releases catecholamines ------activates Alpha and beta receptors ----- increase in

the sympathetic activion -----activation of Beta 1 receptors HR & stroke
volume --------------------- CO --------BP

activation of Apha1 receptors --------vasoconstriction and vascular resistance

increase in BP

BP HOMEOSTASIS

2.RAAS Renin-Angiotensin-Aldosterone-System

it is regulated by the rate of renal blood flow

a classic endocrine system that helps to regulate BP and extracellular volume of the body.

ANTIHYPERTENSIVE DRUGS

•Goal: to decrease BP to normal

CLASSIFICATIONS OF ANTIHYPERTENSIVE DRUGS:

1.ACE-INHIBITORS

2.ANGIOTENSIN II –RECEPTOR BLOCKERS

3.CALCIUM CHANNEL BLOCKERS (CCB)

4.VASODILATORS

5.DIURETICS

6.RENIN INHIBITORS

7.SYMPHATETIC NERVOUS SYSTEM BLOCKER

A. BETA BLOCKERS

ACE INHIBITORS

are heart medications inhibit ACE

increases the amount of blood the heart pumps and lowers blood pressure

raise blood flow, which helps to lower heart's workload

ANGIOTENSIN-CONVERTING ENZYME (ACE) INHIBITOR

•no direct positive inotropic action

•reduce aldosterone secretion, salt and water retention, and vascular resistance

•first line drugs for heart failure, along with diuretics and digitalis

ACE INHIBITORS

captopril (Capoten) → 1stACE inhibitor

benazepril ( Cibacen)

perindopril (Coversyl)

enalapril (Renitec, Vasopress)

quinapril (Accupril)

eosinophil (BPNorm)
ramipril (Tritace)

lisinopril (Zestril)

trandolapril

moexipril (Univasc)

…Pril=Chill =decrease BP

NURSING RESPONSIBILITIES

1.The nurse should encourage the patient to implement lifestyle changes such as weight
reduction, smoking cessation, decreased intake of alcohol, dietary restriction of salt/fats
and increased exercise.

2. Give the drug on an empty stomach, either 1 hour before or 2 hours after

meals to ensure proper drug absorption

3. Stress the importance of NOT abruptly stopping the medication if

symptoms are improving

ANGIOTENSIN II –RECEPTOR BLOCKERS

also known as angiotensin II receptor antagonists

ARBs reduce the action of the hormone angiotensin II.

They are also used for chronic kidney disease and prescribed following a heart attack.

ANGIOTENSIN II –RECEPTOR BLOCKERS (… SARTAN)

EXAMPLE:

Losartan (Prototype)

Candesartan

Irbesartan

Valsartan

Telmisartan

CALCIUM CHANNEL BLOCKERS

They work by slowing the movement of calcium into the cells of the heart and blood vessel
walls, which makes it easier for the heart to pump and widens blood vessels.

As a result, the heart doesn't have to work as hard, and blood pressure lowers

CCB calms the heart

CALCIUM CHANNEL BLOCKERS

2 CLASSIFICATIONS:

1.Dihydropyridines:

•Selectively inhibit the L type of calcium Channels in the vascular smooth muscle

•blocks the entry of Calcium into the vascular smooth muscle decreasing the contraction and
decrease BP.

Amlodipine (Norvasc)

Felodipine (Plendil)
Nicardipine

Nifedipine (Calcibloc, Adalat) Long acting

CALCIUM CHANNEL BLOCKERS

2. Nonhydropyridines

non selectively block the cardiac cells on the SA and AV node that decreases myocardial
contractility, decrease the CO and HR

Diltiazem

Verapamil (isoptin)

Side Effect:

1.excessive bradycardia

2. Cardiac conduction abnormality

3. Verapamil inhibits CC in the smooth muscle of the GIT: constipation

VASODILATORS

medicines that dilate (open) blood vessels by relaxing the smooth muscle

allows blood to flow more easily.

They affect the muscles in the walls of the arteries and veins, preventing the muscles
from tightening and the walls from narrowing.

As a result, blood flows more easily through the blood vessels.

Used to treat severe hypertension

VASODILATORS

Example:

•Hydrala

•Zine

•Diazoxide (Hyperstat)

•Hydralazine (Apresoline)

•Minoxidil (Loniten)

•Sodium Nitroprusside (Nitropress) (P)

•Tolazoline (Priscoline)

CONTRAINDICATIONS

•The vasodilators are contraindicated in the presence of known allergy to the drug

•with pregnancy and lactation because of the potential for adverse effects on the fetus and
neonate

•and with any condition that could be exacerbated by a sudden fall in blood pressure, such
as cerebral insufficiency

NURSING CONSIDERATIONS

•Monitor blood glucose and serum electrolytes to avoid potentially serious adverse effects.
•Monitor the patient carefully in any situation that might lead to a drop in fluid volume
(e.g., excessive sweating, vomiting, diarrhea, dehydration) to detect and treat excessive
hypotension that may occur.

DIURETICS

also called water pills

increases the amount of water and sodium excretion from the body as urine.

first line agent in

mild hypertension

RENIN INHIBITOR

: inhibits/ antagonist renin production

: inhibits to the conversion of angiotensinogen to angiotensin 1

Results to relaxed blood vessels, improves cardiac output

EXAMPLE:

ALISKIREN

Enalliren

Remikiren

SYMPATHETIC NERVOUS SYSTEM BLOCKERS

•Blocks fight and flight response

1. BETA BLOCKERS (…olol)

AKA beta-adrenergic agents

block the hormones adrenaline and

noradrenaline in the sympathetic

nervous system.

sympatholytic

Example

 Acebutolol
 Atenolol
 Betaxolol
 Bisoprolol
 Metoprolol

BETA-BLOCKERS

Cardiac Effects

•Decrease contractility (negative inotropy)

•Decrease relaxation rate (negative lusitropy)

•Decrease heart rate (negative chronotropy)

•Decrease conduction velocity (negative dromotropy)

Vascular Effects

•Smooth muscle contraction (mild vasoconstriction)

NURSING RESPONSIBILITIES

1.Monitor BP, ECG

2.Monitor I&O

3.Monitor compliance

4.Advise to change position slowly to prevent orthostatic hypotension

ALPHA-ADRENERGIC BLOCKERS

•A substance that relaxes muscle tissue in blood vessels, which improves the flow of urine
and blood.

•Also called Alpha-adrenergic antagonist

EXAMPLE: PHENTOLAMINEPHENOXYBENZAMINE

Pharmacodynamics:

Inhibits the postsynaptic alpha1-adrenergic receptors, preventing the feedback control of

norepinephrine release

ALPHA-AND BETA-BLOCKERS

have a combined effect. They block the binding of catecholamine hormones to both alpha-
and beta-receptors.

Therefore, they can decrease the constriction of blood vessels likealpha-blockersdo.

They also slow down the rate and force of the heartbeat like beta-blockers do.

EXAMPLE:

 Clonidine
 Guanfacine
 Methyldopa

ALPHA

2 ADRENERGIC AGONISTS

Pharmacodynamics

 stimulates the alpha2 adrenergic receptors in the

 CNS and inhibit the cardiovascular centers
 decrease in sympathetic outflow from the CNS
 decrease in norepinephrine release
 weakening the sympathetic nervous system effects that results in
 increase in the reflex tachycardia

ADVERSE EFFECTS AND TOXICITY ASSOCIATED

WITH ANTIHYPERTENSIVE DRUGS

 Syncope, dizziness,
 headache
 Alopecia, rash
 Cough
ADVERSE EFFECTS AND TOXICITY ASSOCIATED

WITH ANTIHYPERTENSIVE DRUGS

 Renal damage
 proteinuria
 Renal failure
 Tachycardia
 Heart failure
 Arrythmias
 hypotension

ADVERSE EFFECTS AND TOXICITY ASSOCIATED

WITH ANTIHYPERTENSIVE DRUGS

 Constipation
 GI upset
 Loss of libido

2. ANGINA PECTORIS

 refers to a strangling or pressure like pain caused by cardiac ischemia.

 The pain is usually located substernal, sometimes with radiation to the neck,
shoulder and arm, or epigastrium.
 Drugs used in angina exploit two main strategies: reduction of
oxygen demand and increase of oxygen delivery to the myocardium.

DRUGS USED FOR ANGINA

1.NITRATES: NITROGLYCERINE

2.BETA BLOCKERS

3.CALCIUM CHANNEL BLOCKERS

NITROGLYCERINE

EXAMPLE

Isosorbide dinitrate

Isosorbide mononitra
• Pharmacodynamics:

relaxes vascular smooth muscle with a resultant decrease in venous return and
decrease in arterial blood pressure, reducing the left ventricular workload and
decreasing myocardial oxygen

drug of choice for treating an acute anginal attack

BETA-BLOCKERS

EXAMPLE:

Metoprolol

Nadolol

Propranolol

• Pharmacodynamics:

competitively blocks beta-adrenergic receptors in the heart and kidneys, decreasing

the influence of the sympathetic nervous system on these tissues and the excitability
of the heart;

decreases cardiac output, which results in a lowered blood pressure and decreased
cardiac workload

CALCIUM CHANNEL BLOCKERS

EXAMPLE: Diltiazem

• Pharmacodynamics:

inhibits the movement of calcium ions across the membranes of myocardial and
arterial muscle cells

alters the action potential and blocking muscle cell contraction

depresses myocardial contractility

slows cardiac impulse formation in the conductive tissues, and relaxes and dilates
arteries

fall in BP and a decrease in venous return

decreases the workload of the heart and myocardial oxygen consumption

3. ARRHYTHMIA

irregular rhythm of the heart

A. Pathophysiology:

involves changes to the automaticity or conductivity of the heart cells

CLASS 1 ANTIARRHYTHMIC DRUGS

•Drugs used for Arrhythmia:

CLASS I ANTIARRHYTHMIC DRUGS

Class Ia: Procainamide Quinidine

Class Ic Flecainide Propafenone

Class Ib Lidocaine Mexiletine

CLASS 1 ANTIARRHYTHMIC DRUGS

•Pharmacodynamics:

blocks sodium channels

decreases depolarization, decreasing automaticity of the ventricular cells

increases ventricular fibrillation threshold

• Indications:

management of acute ventricular arrhythmias during cardiac surgery or MI

CLASS II ANTIARRHYTHMIC DRUGS

•EXAMPLE

Acebutolol

Esmolol

Propranolol

• Pharmacodynamics:

competitively blocks beta-adrenergic receptors in the heart and kidney, has a

membrane-stabilizing effect, and decreases the influence of the sympathetic nervous
system

CLASS III ANTIARRHYTHMIC DRUGS

EXAMPLE
Amiodarone

Dofetilide

• Pharmacodynamics:

acts directly on heart muscle cells to prolong repolarization and the refractory
period, increasing the threshold for ventricular fibrillation; also acts on peripheral
smooth muscle to decrease peripheral resistance

CLASS IV ANTIARRHYTHMIC DRUGS

•EXAMPLE: Diltiazem Verapamil

•Pharmacodynamics:

blocks the movement of calcium ions across the cell membrane, depressing the
generation of action potentials, delaying phases 1 and 2 of repolarization, and slowing
conduction through the AV node.

• Indications:

Treatment of paroxysmal supraventricular tachycardia

atrial fibrillation

atrial flutter.

HEART FAILURE

a condition where the heart is not pumping effectively and blood backs up so the
system becomes congested

results from conditions that impair the ability of the heart to fill with, or to pump
out, sufficient blood.

•Either side of the heart may be affected, or both sides may be affected in some
patients.

AGENTS USED FOR HEART FAILURE

CARDIOTONIC DRUGS (INOTROPIC DRUGS)

drugs that affect the intracellular calcium levels in the heart muscle that results in;

1.increased contractility, increase in contraction, increased cardiac output

2.increased renal blood flow, increased urine production, decreases renin release
3.interfering with the effects of the renin–angiotensin–aldosterone system increases
urine output decreased blood volume

4.decrease in the heart’s workload

5.relief of HF

CARDIOTONIC DRUGS (INOTROPIC DRUGS)

CARDIAC GLYCOSIDES

1.Digoxin (Lanoxin)

derived from digitalis plant

most often used drug to treat HF

They increase the level of CALCIUM inside the cell by inhibiting the Sodium-
Potassium pump.

More calcium will accumulate inside the cell during cellular depolarization

CARDIAC GLYCOSIDES

•Negative chronotropic effect-the heart rate is slowed due to decreased rate of

cellular repolarization

•Bradycardia

•Decreased conduction velocity through the AV node

CARDIAC GLYCOSIDES

•Nursing considerations:

1.monitor apical pulse for 1 full minute before administering the drug to monitor for
adverse effects.

2.hold the dose if the pulse is less than 60 beats/min in an adult or less than 90
beats/min in an infant; retake the pulse in 1 hour. If the pulse remains low,
document it, withhold the drug, and notify the prescriber because the pulse rate
could indicate digoxin toxicity

3.monitor the pulse for any change in quality or rhythm to detect arrhythmias or
early signs of toxicity

4.monitor the patient for therapeutic digoxin level (0.5–2 ng/mL)

5.Patient teaching on the antidote in case of toxicity: DIGOXINE IMMUNE FAB

VASODILATORS
1. Ace inhibitors … pril (captopril, enalapril)

2. Nitrates: nitroglycerine

•Pharmacodynamics:

relax vascular smooth muscle that results in

•a decrease afterload

•a venous pooling: a decrease preload of

the heart, decrease workload,

(+) inotropic effect

DRUGS FOR CIRCULATORY DISORDERS

Five major groups:

1. antilipidemics-hypolipidemics; antihyperlipidemic; increase blood lipid concentration.

2. Anticoagulants -prevent the formation of clots that inhibit the circulation

3. thrombolytics-dissolve blood clots that have already formed

4. antiplatelets(antithrombotic) -prevent platelets aggregation (clumping together of

platelets to form a clot)

5. Peripheral vasodilation-promote dilation of blood vessels narrowed by vasospasm

ANTIHYPERLIPIDEMICAGENTS

1. HMG CoA reductase inhibitors (statins)

Action: blocks HMG CoA reductase inhibits cholesterol biosynthesis in the liver↓
total cholesterol, ↓ LDL, ↑ HDL

Drugs: lovastatin

Fluvastatin (Lescol)

pravastatin (Lippstadt)

atorvastatin (Lipitor)

simvastatin (Zocor, Vidastat)

Side effects: myopathy, increase liver enzymes

Contraindication: active or chronic liver disease

•use in caution in patient taking cyclosporine, macrolide antibiotics, antifungal agents

•may increase statin serum level

2. BILE ACID SEQUESTRANTS

Action: binds with bile acids in the intestine

Drugs: cholestyramine

cholestipol

Side effects: gastrointestinal distress, constipation, decreased absorption of other

drugs

Contraindication:

•cannot be used in patients with elevated triglyceride (>400mg/dl)

PARENTERAL (SC OR IV)

A. Heparin

•Combines with antithrombinIII -> inactivates thrombin inhibits conversion of

fibrinogen to fibrin (clot) clot is prevented

•Poorly absorbed through Glmucosa -> give SC or IV

•Can be used to prevent clot from forming (SC) or to treat acute thrombosis (IV)

HEPARIN

Side effects:

•Prolongs clotting time (monitor partial thromboplastin time or PTT and activated
partial thromboplastin time or aPTT)

•Thrombocytopenia (decrease in platelet count)

•Bleeding antidote: protamine sulfate

•Before discontinuing, oral therapy is begun (warfarin)

B. LOW MOLECULAR WEIGHT HEPARINS

•Lower risk of bleeding than heparin

Use: to prevent thromboembolism

•Frequent laboratory is not required

Drug examples: enoxaparin sodium (Clexane)

dalteparinsodium (Fragmin)

ardeparin

nadroparincalcium (Fraxiparine)

tinzaparinsodium (Innohep)

•average treatment duration: 7-14 days

Side effect:

•bleeding is rare antidote: protamine sulfate

•contraindicated for strokes (hemorrhagic), peptic ulcers and blood anomalies

ORAL ANTICOAGULANTS

Drug examples:

warfarin (Coumadin) →most prescribed

dicumarol

anisidine→ more side effects noted

Action:

•inhibit hepatic synthesis of vitamin K → affect vitamin K dependent clotting factors

•well absorbed in Glmucosa but food will delay absorption

•long half-life and highly-protein bound →cumulative effect →bleeding and other side
effects

Side effects:

•bleeding: monitor prothrombintime (PT) and International Normalized Ratio (INR)

•antidote for side effects: parenteral vitamin K

•for severe bleeding may give fresh-frozen plasma or platelets

ANTIPLATELETS

Action: used to prevent thrombosis in the arteries by suppressing platelet aggregation

Indications:
•for prophylaxis against myocardial infarction and stroke

Drugs: aspirin (Aspilet)

dipyridamole (Persantin)

ticlodipine (Ticlid)

clopidogrel (Plavix)

Platelet glycoprotein (GP) IIb/IIIareceptor antagonists

abciximab–drug of choice for angioplasty

eptifibatide

tirofiban (Aggrastat)

dipyridamole+ aspirin (Aggrenox)

PERIPHERAL VASODILATORS

Peripheral Vascular Disease

S/Sx: numbness and coolness of extremities, intermittent claudication, leg ulcers

•caused by arteriosclerosis and hyperlipidemia

•e.g. Raynaud’s disease, arteriosclerosis obliterans, cerebrovascular insufficiency

Action of peripheral vasodilators: increased blood flow to the extremities

•acts directly on vascular smooth muscle (isoxsuprine)

Drugs: tolazoline

isoxsuprine (Duvadilan)

nicotinylalcohol

papaverine

prazosin (Minipress)

nifedipine (Adalat, Calcibloc)

ENDOCRINE

● Anti-Diabetic Drugs
Insulin - increases glucose transport into cells and promotes conversion of glucose to
glycogen decreasing serum glucose levels

Different type of insulin

Type Name Onset Peak Duration

Rapid acting NovoLog, 5-15 min 30-120 min 3-5 hours
Humalog,
apidra
Short-acting U100: 2-4 hours 5-8 hours
(regular/r) Humulin-R, 30 min
Novolin-R.
U500: 4-8 hours 14-15 hours
Humulin-R, U-
500
Intermediate- Humulin N, 2-4 hours 4-10 Hours 10-18 hours
acting Novolin N
Long-acting Levemir 1-3 hours 6-8 hours 18-20 hours
Lantus 2-4 hours No peak 20-24 hours
Toujeo 2-4 hours No peak 24 hours

Pre Mixed Insulin

Brand Basal Prandial

Novolog 70/30 Aspart protamine Aspart
Humalog 75/25 Lispro protamine Lispro
Humalog 50/50 Lispro protamine Lispro
Humulin 70/30 NPH Regular
Novolin 70/30 NPH Regular

1st number= percentage of intermediate-acting insulin

2nd number= percentage of short/rapid-acting insulin

Example: Novolog 70/30, inject 50 units BID

Each injection would contain

 35 units (70% of 50) of aspart protamine (basal)

 15 units (30 % of 50) of aspart (prandial /rapid)

Pros Cons
Less injection Less dosing flexibility
cheaper (Set Basal/prandial ratios)
 Oral Hypoglycemic Agents – OHA

1. Sulfonylureas

MOA: stimulates the beta cells secrete more insulin  insulin cell receptors  inc.
ability of cells to bind insulin for glucose metabolism

2. Biguanides

MOA: Increases insulin receptor sensitivity and peripheral glucose uptake at the
cellular level

3. Alpha-glucosidase inhibitors

MOA: inhibits the digestive enzyme (alpha-glucosidase) in the small intestine

(responsible for the release of glucose from the complex carbohydrates (CHO) in the
diet) → CHO cannot be absorbed → CHO passed into the large intestine.

It stimulates the pancreas to produce insulin and increase peripheral receptors

sensitivity to insulin decreasing serum glucose levels.