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Drug Charts

 Eicosanoids
 NSAIDs
 Immunopharmacology
 Adrenergic Agonists
 Adrenergic Antagonists
 PsNS Agents
 Anti-Hypertensives
 Antibiotics
 Cancer Drugs
 Movement Disorders
 Anti-Convulsants
 Anxiolytics
 Anti-Psychotics
 Anti-Depressants
 Alcoholism
 Opioids
 General Anesthetics
 Local Anesthetics
 GI Drugs
 Anti-Virals
 Anti-Virals: HIV
 Anti-Arrhythmics
 Cardiotonics
 Diuretics
 Alternative Medications
 Pituitary Hormones
 Estrogens/Progestins
 Thyroid/Parathyroid/Adrenal Hormones
 Anti-Malarials
 Anti-Parasitics
 Pulmonary Drugs
 Caloric Regulation
 Diabetes Drugs
 Lipid Drugs
 Dermatology Drugs
 Gout Drugs

S. Carr
Drug Eye Clotting Vasculature Lungs GI Reproductive Organs CNS Treats
PGI vasodilation bronchodilation ↓ acid, ↑ mucus, Kidney: ↑ blood, Primary pulmonary
↓ plt aggregation ↓ tone
(↑ cAMP) (↑ cAMP) ↑ blood ↑ diuresis HTN
PGE1 ↓ intraocular vasodilation bronchodilation ↓ acid, ↑ mucus, Kidney: ↑ blood, ↑ body temp Misoprostol
↓ plt aggregation ↓ tone
pressure (↑ cAMP) (↑ cAMP) ↑ blood ↑ diuresis, ↓ ADH ↓ NE Alprostadil
PGE2 ↓ intraocular vasodil + vasocx bronchodilation ↓ acid, ↑ mucus, ↓ tone Kidney: ↑ blood, ↑ body temp
↓ plt aggregation Dinoprostone
pressure (↑ IP3 & ↑ Ca2+) (↑ cAMP) ↑ blood (+ ↑ oxy CX) ↑ diuresis, ↓ ADH ↓ NE
PGF2α ↓ intraocular vasocx bronchocx ↑ CX Latanoprost
pressure (↑ IP3 & ↑ Ca2+) (↑ IP3 & ↑ Ca2+) (↑ oxytocin) Carboprost
TXA vasocx bronchocx Kidney: ↓ blood
↑ plt aggregation ↑ CX
(↑ IP3 & ↑ Ca2+) (↑ IP3 & ↑ Ca2+)
LTC ↑ permeability bronchocx
Zileuton
(↓ BP) (↑ IP3 & ↑ Ca2+)
Zafirlukast
LTD ↑ permeability bronchocx
Montelukast
(↓ BP) (↑ IP3 & ↑ Ca2+)
Epoprostenol (PGI) vasodilation Primary pulmonary
(Epopro = IV / Trepro = subQ) (vasculature = vasodilates to relieve pulmonary HTN)
Treprostinil (↑ cAMP) HTN
Misoprostol ↓ acid, ↑ mucus, ↑ CX NSAID-ulcer
(GI = cytoprotective at low doses, ↓ acid at high doses) (during pregnancy = dinoprostone)
(PGE1) ↑ blood (↑ oxytocin) Abortifacient
Alprostadil vasodilation Impotence
(male = erection injection) (vasculature = vasodilates to maintain PDA until surgical correction)
(PGE1) (↑ cAMP) Maintain PDA
Dinoprostone ↑ CX Abortifacient
(administered vaginally, uterine contractions & ↑ collagenase activity)
(PGE2) (↑ oxytocin) Labor induction
Latanoprost ↓ intraocular Open angle
(stable, long acting, SE: brown pigmentation, dry eyes)
(PDF2 α) pressure glaucoma
Carboprost ↑ CX
(administered vaginally, uterine contractions & ↑ collagenase activity) Abortifacient
(PGF2 α) (↑ oxytocin)
Zileuton bronchodilation
(inhibits leukotrienes) Asthma
(↓lipoxygenase) (blocks LT synth)
Zafirlukast (↓LTR) bronchodilation
(blocks leukotriene receptors) Asthma
Montelukast (blocks LT synth)
Indomethacin vasocx
(NSAID indole derivative) (vasculature = vasoconstricts to close PDA in premies) Close PDA
(COX inh.) (↓ PG synth)
Drug Inhibits Metabolism Duration What Makes it Unique Side Effects Treats
Aspirin Low = 15 min 1) binds serum proteins (depends on dose) 1) salicylism, respirary alkalosis, met. acid
COX-1 RA
High = 4 h 2) irreversibly acetylates COX-1&2, 3) 2) NSAID-asthma
COX-2 Chronic inflm
↑ High = 13 h irreversibly inhibits platelet aggregation 3) Reyes syndome
Non-acetylated COX-1 Less side effects, no renal toxicity, RA
Less effective at COX inhibition than ASA
COX-2 no NSAID-asthma Chronic inflm
salicylates
Ibuprofen COX-1 Liver Short Low dose = analgesic (no anti-inflam) GI, rash, tinnitis, fluid retention RA
COX-2 CYP2C8 (2hr) High dose = analgesic & anti-inflam kidney failure, hepatitis Chronic inflm

Diclofenac Liver
COX-1 Short 1)↑ serum aminotransferase activity in liver RA
CYP3A4 Typical NSAID
COX-2 (2hr) 2) Renal dysfx doesn't impair clearance Chronic inflm
CYP2C9
Etodolac COX-1 Intermediate RA
Affects COX-2 > COX-1 by 10:1 Less GI
COX-2 (5 hr) Chronic inflm

Indomethacin COX-1 30% have to discontinue RA


Very potent indole derivative
COX-2 (psychosis & hallucination) Chronic inflm

Ketoprofen COX-1 1) Short (2 hr) RA


Also inhibits lipoxygenase Typical NSAID
COX-2 2) Slow release Chronic inflm

Naproxen COX-1 Long RA


Free fraction is 40% higher in females Typical NSAID
COX-2 (12 hr) Chronic inflm

Sulindac COX-1 Long 1) ↑ serum aminotransferases RA


Cholestatic liver damage
COX-2 (12 hr) 2) Treats familial intestinal polyposis Chronic inflm

Celecoxib 1) Least potent of COX-2 inhibitors Can interfere w/antihypertensive therapy RA


COX-2 2) Does not affect platelet aggregation Still contraindicated in pts w/GI ulcers Chronic inflm

Rofecoxib RA
COX-2 Most COX-2 selective → CV problems Still contraindicated in pts w/GI ulcers
Chronic inflm
Valdecoxib
Acetaminophen 1) COX inhibitory effects primarily in CNS
COX-1 1) Less GI irritation & bleeding RA
2) Best anti-pyretic/analgesic in children
COX-2 2) Liver toxicity (↓ glutathione) Chronic inflm
3) No anti-inflammatory or anti-coagulant
Analgesia Anti-pyretic Anti-inflamatory Anti-coagulant COX-2 Pro-coagulant
NSAID Effects (low grade pain) (PG inhibition) (MSK, RA, OA) (other NSAIDs can block long-lasting ASA) (↓ COX-2 PGI but not COX-1 TXA)
GI irritation ↑ bleeding time Pregnancy Hypersensitivity
NSAID Side Effects (ASA espclly) (inhib. TXA)
Kidney effects
(delayed onset of labor from ↓ PGE & PGF) (↓ COX → arachidonate → ↑ lipoxygenase)
Drug Action Response What Makes it Unique Treats
Prednisone Autoimmune disease
Immunosuppression Chronic use associated with: ↑infections, ulcers,
Down-regulate inflammation Transplantation inflm
Prednisolone Anti-inflammatory hyperglycemia, osteoporosis
Hypersensitivity
GVHD (bone marrow trxpnt)
T-cell Inhibitor

Cyclosporine Inhibits calcineurin phosphatase


Impairs T-cell response to antigen Tacrolimus is 100x more potent Aplastic anemia (ineligible)
Tacrolimus → ↓ cytokines
Autoimmune disease
Sirolimus Transplant rejection
Inhibits T-cell activation Renal transplant have surgical complications
↓ T-cell response GVHD
& proliferation May produce an immunosupp tolerance
Autoimmune disease
Azathioprine Competitive inhibition of inosinate Myelosuppression Transplant rejection
Cytotoxic

Converted to thioinosinate
S phase inhibitor Coadministration w/allopurinol is toxic Rheumatoid arthritis

Mycophenolate Inhibits inosine monophosphate Inhibits T-cell & B-cell cell cycle & Coadminister: cyclosporine & corticosteroids
Transplant rejection
dehydrogenase proliferation Do not coadminister: antacids

FTY720 Reversibly sequesters lymphocytes in Graft is protected from T-cell attack


Sphingosine 1-P receptor agonist Transplant rejection
2° lymph organs ↑ HR in 30% of patients

Antithymocyte Ig
Ig against T-cells Removes T-cells from system Coadminister: azathioprine & corticosteroids Transplant rejection (kidney)

Immune globulin Immunodeficiencies


Human plasma Ig Replaces missing Ig Toxicity: autoimmune hemolytic anemia Lymphocytic leukemia
Immunoglobulins

Kawasake disease
Anti-CD3 Ig
Ig against CD3 on T-cells Blocks antigen recognition site Toxicity: cytokine release syndrome Transplant rejection

Basiliximab Coadminister: cyclosporine & corticosteroids


Ig against IL-2 receptor Blocks activation of T-cells by IL-2 Transplant rejection (kidney)
Daclizumab Toxicity: none!

Infliximab Rheumatoid arthritis


Ig against TNF-α Blocks immune activation of TNF Coadminister: methotrexate for RA
Etanercept Crohn's disease

Rho Immune Ig Administered to Rh- mother pregnant with Rh+ Hemolytic disease of the
Ig against anti-D antibodies Blocks anti-Rh antibodies
fetus newborn (prevention)
Biological Response Modifiers

Bacillis Calmette-
Strain of myobacterium bovis Stimulates T-cells & NK cells Toxicity: severe hypersensitivity & shock Bladder cancer
Guerin
Thymic Factors
Promotes T-cell differentiation Enhanced T-lymphocytic function Stem cells rushed through boot camp SCID

Interleukin-2 Promotes T & B-cell proliferation, AIDS


↑T-cells, ↑B-cells, ↑NK cells Natural cytokine
differentiation Cancer

GM-CSF ↑ WBC recovery Cancer


Stimulates clonal expansion Natural cytokine
G-CSF in pts with ↓ hematopoiesis Congenital
Drug Receptors Heart Vasculature Lungs GI Reproductive Organs Treats
Epinephrine α1 [high] Reflex bradycardia ↑ DBP (↓ MSK) ↑ uterine CX
↓ mucus congestion Eye: ↓ intraocular Asthma
α2 [high] ↓ ACh (α2A)
pressure Anaphylaxis
β1 [low] ↑HR, ↑CX, ↑CO ↑ SBP (indirect) ↓ motility Metabolism: ↑ Cardiac arrest
β2 [low] ↓ DBP (↑ MSK) bronchodilation ↓ motility ↓ uterine CX
Phenylephrine α1 Reflex bradycardia ↑DBP & ↑SBP Nasal deconges.
Levarterenol similar to EPI…potent vasoconstrictor used to treat hypotension & shock Shock
Norepinephrine α1 Reflex bradycardia ↑ DBP (vasocx)
α2
β1 ↑HR, ↑CX, ↑CO ↑ SBP (indirect) Kidney: ↑ renin
Dopamine D1 [low] vasodilation 1) shock caused by
β1 [high] ↑HR, ↑CX, ↑CO ↑ SBP (indirect) Kidney: ↑ renin ↓ CO & ↓ renal fxn
2) Parkinson's
α1 [↑ high] ↑ DBP (vasocx)
Amphetamine 1) displaces NE from vesicles….2) competitively inhibts NE reuptake….3) inhibits MAO activity → NE lingers Narcolepsy
Arbutamine α1
β1 ↑HR, ↑CX, ↑CO ↑ SBP (indirect) Kidney: ↑ renin (Experimental)

β2
α-methyl-DOPA α1 some activity, but less effective than NE SE: hepatotoxicity & autoimmune hemolytic anemia HTN during
α2 ↓ SNS outflow ↓ BP pregnancy

Tyramine α1 Reflex bradycardia ↑ DBP (vasocx) If MAO inhib: 1) displaces NE from vesicles, 2) competes w/NE for reuptake
β1 ↑HR, ↑CX, ↑CO ↑ SBP (indirect) Initially potentiates NE effects, then eventually depletes NE Kidney: ↑ renin
Guanethidine α1 Depletes NE in the SNS (but does not cross the BBB)
α2
β1
Ephedrine 1) displaces NE from vesicles….2) competitively inhibts NE reuptake….3) inhibits MAO activity → NE lingers (acts like amphetamine)
Clonidine α2 ↓ SNS outflow ↓ BP HTN
Brimonidine α2 ↓ SNS outflow ↓ BP ↓ humor production & ↑ uveoscleral outflow OA glaucoma
Tizanidine α2 ↓ SNS outflow ↓ MSK spasticity Multiple sclerosis
Isoproterenol β1 ↑HR, ↑CX, ↑CO ↑ SBP (indirect) Kidney: ↑ renin Bronchodilator
β2 ↓ cardiac efficiency ↓DBP vasodilation bronchodilation ↓ motility Cardiac arrest

Dobutamine α1 [high] ↑ cardiac efficiency ↑ DBP (vasocx) Decompensated


β1 [low] ↑HR, ↑CX, ↑CO ↑ SBP (indirect) Kidney: ↑ renin heart failure

Metaproterenol β2 M = medium bronchodilation Medium duration (oral administration) Bronchospasm


Salmeterol β2 S = steroid & slow bronchodilation Long-lasting (inhalation) must be accompanied by steroid Bronchospasm
Formoterol β2 F = fast bronchodilation Long-lasting (inhalation) fast-acting Bronchospasm
Terbutaline β2 T = tachycardia bronchodilation Minimal tachycardia Bronchospasm
Albuterol β2 A = acute bronchodilation Short-acting (inhalation) acute relief Bronchospasm
Drug Receptors Heart Vasculature Lungs GI Reproductive Organs Treats
α-methyl-paratyrosine competitive inhibitor of tyrosine hydroxylase → depletes NE, EPI, DA pre-operatively in pheochromocytoma

Reserpine binds VMAT-2 irreversibly inhibits vesicular concentration of NE & DA → transient ↑ at receptors → SNS depletion

Cocaine reversibly inhibits NET & DAT (CNS) → anesthetic, CNS stimulant, sympathomimetic

Phenoxybenzamine Anti α1 Reflex tachycardia ↓ vasocx


Pheochromocytoma
Anti α2 ↑ SNS outflow
Carvedilol Anti α1
Anti β1 Heart failure

Anti β2
Prazosin Anti α1 Reflex tachycardia ↓ vasocx smooth muscle RX Hypertension
BPH
Anti α2B Reflex tachycardia ↓ vasocx
Tamsulosin Anti α1A Reflex tachycardia ↓ vasocx Hypertension
Alfuzosin Anti α1 smooth muscle RX BPH
Yohimbine Anti α2 Male impotence
Propranolol Anti β1 ↓HR, ↓CX, ↓CO ↓SBP Kidney: ↓ renin Hypertension
Migraine
Anti β2 bronchocx
Metoprolol Anti β1 [low] ↓HR, ↓CX, ↓CO ↓SBP Kidney: ↓ renin
Hypertension
Anti β2 [high] bronchocx
Atenolol Anti β1 ↓HR, ↓CX, ↓CO ↓SBP Long-lasting, specific, reduced CNS activity, no bronchocx Kidney: ↓ renin Hypertension
Acebutolol Anti β1 ↓HR, ↓CX, ↓CO ↓SBP β1 specific, partial agonist → less exercise intolerance Hypertension
Timolol Anti β1 ↓HR, ↓CX, ↓CO ↓SBP ↓ intraocular pressure w/o affecting pupil or ciliary body Kidney: ↓ renin Open angle
glaucoma
Anti β2 bronchocx
Labetalol Anti β1 ↓HR, ↓CX, ↓CO ↓SBP Kidney: ↓ renin
Hypertension
Anti β2 bronchocx
Sotalol Anti β1 ↓HR, ↓CX, ↓CO ↓SBP anti-arrhythmic, anti-atrial fibrillation Kidney: ↓ renin Arrhythmia
Atrial fibrillation
Anti β2 bronchocx
Carbachol ACh musc Ciliary muscle CX → widens trabecular network → ↑ drainage of aqueous humor OA glaucoma
Pilocarpine ACh musc Ciliary muscle CX → widens trabecular network → ↑ drainage of aqueous humor OA glaucoma
Physostigmine AChE inhib Ciliary muscle CX → widens trabecular network → ↑ drainage of aqueous humor OA glaucoma
Echothiophate AChE inhib Ciliary muscle CX → widens trabecular network → ↑ drainage of aqueous humor OA glaucoma
Brimonidine α2 Inhibits aqueous humor production OA glaucoma
Latanoprost PDF2α Enhance uveoscleral outflow OA glaucoma
Cholinomimetics
Drug Mechanism Heart Vasculature Lungs GI GU Organs Treats
Bethanechol Choline Ester M2 M1 M1 Eye : M1
M3 ↑ secretions C: OA glaucma
PsNS agonist [Lo] = reflx tach ↑ motility (B) Detrussor CX Circular M. CX
vasodil (B & C) bronchoCX B: GI/GU retentn
Carbachol M1, M2, M3 [Hi] = AV block ↑ secretions (B & C) Ciliary M. CX
Natural alkaloid
Pilocarpine Treats OA glaucoma: (1) pupillary CX, (2) spasm of accom., (3) transient ↑ IOP → persistent ↓ IOP, (4) impaired night vision
M1, M2, M3
M2 (ant) GI spasms
Muscarinic blockade
Atropine (M1, M2, M3)
[Lo] = brady
M1 (ant) M1 (ant) Eye: M1 (ant)
Eye exams
[Normal] = ↑ HR M3 (ant) ↓ secretions ChEI toxicity
Parasympathetic Antagonists

↓ motility Detrussor RX Circular M. RX


M2 (ant) vasocx bronchodil Anesth adjunct
Muscarinic blockade ↓ secretions Urine retention Ciliary M. RX
Scopalamine (M1, M2, M3)
[Lo] = ↑brady Motion sickness
[Hi] = ↑ HR Overax bladder

Pirenzepine M1 antagonist Used w/H-2 blockers to reduce gastric acid secretion to promote gastric ulcer healing Gastric ulcer

Tolterodine
Overactive
Trospium Anti-muscarinic
bladder
Oxybutynin

Ipratropium Muscarinic blockade


↓ secretions
(M1, M2, M3) COPD
bronchodil
[No ↓ cilia motility]
Tiotropium

Reversible ChE Diagnosis of MG


Edrophonium inhibitor PAT

Atropine toxicity
Physostigmine Reversible ChE (crosses BBB)
Eye : M1
inhibitor (competitive) Circular M. CX Paralytic ileus
Physo : block nACh? Ciliary M. CX
Neostigmine Direct: Treatment of MG
~ Xerostomia
M2 M1
Cholinesterase Inhibitors

Skel Muscle :
Echothiophate ↓HR M3 Detrussor CX
M1 Nm
Indirect: NO-cGMP ↑ secretions Trigone RX
↑ motility ↓ Caused by
DFP M3 ↓ bronchoCX Ex. sphincter RX
↑ secretions fasciculations exposure to
vasodil vasodil ↓
Irreversible ChE ~ toxins
↓ micturition
Malathion inhibitor CNS : *Atropine can
reflex tachy
(phosphorylate ChE) Stimulation reverse
Parathion ↓ *Pralidoxime can
depression reverse

Soman
Reverses ChEI
Pralidoxime Splits covalent bond → forming oxime-phosphonate → splits off → leaves regenerated ChE
toxicity

Tacrine Non-competitive
Also: (1) blocks DA, NE, 5-HT uptake (2) MAO inhibitor (3) block Na+ & K+ channels…hepatotoxicity
Alzheimer's
reversible ChE inhib.
disease
(centrally-acting)
Donepezil ↑ AChE selectivity in CNS (minimal peripheral activity)…no hepatotoxicity

Nm (ant) Nm (ant) Resp. paralysis


Drug intrx: aminoglycosides & tetracyclines
Neuromuscular Junction Blockers (nAChR)

Tubocurarine Steroid nucleus


↑ HR ↓ BP BronchoCX
Contraind.: asthma, MG
(↓PsNS + rx tach) (↓SNS + hstmne) (histamine)
competitive NMJ
blocker (NmX)
Mivacurium ↓ cardiac effects (less tachycardia)...↑ histamine release (more bronchoCX) Used during
procedures that
Vecuronium Isoquinoline require muscle
competitive NMJ ↑ cardiac effects (more tachycardia)...↓ histamine release (less bronchoCX) paralysis
Rocuronium blocker (NmX)
Depolarizing NMJ Nn Nn
Resp. paralysis w/halothane + RyR defect → malig. Hyperthermia
Succinylcholine blocker ↓ HR ↑ BP
Slight histamine (give sodium dantrolene)
(↑ open freq. & dur.) (↑PsNS + rx brad) (↑SNS)
Competitive / Nn (ant) Nn (ant) Nn (ant)
Nn (ant) Eye : mydriasis Surg: ↓ bleeding
Ganglion blockers Depolarizing Nn ↑ HR (PsNS)
↓ BP
↓ motility ↓ secr Urinary reten
Skin : ↓ sweat SCI: ↑ reflexia
blockers ↓ CX (SNS) (PsNS) ♂ impotence
Prevent ACh release Dystonia
Botulinum toxin from the motor nerve Cleaves synaptobrevin & SNAP to prevent ACh vesicle fusion & release Spasticity
terminal Hyperhidrosis
Partial nicotine agonist
Varenicline May help prevent rewarding aspects of nicotine administration Nicotine addiction
at α4β2 Nn
Drug Mechanism Duration Renin What Makes it Unique Side Effects Treats
Guanethidine Depletes NE Long lasting Initial: ↓ Reserpine: central depletion of 5-HT, DA, Nasal cong, ortho hypo, miosis, brady,
HTN (?)
SNS Inhibitors Reserpine ↓ SNS w/residual Eventual: ↑ NE…Parkinsonism & depression diarrhea, cramps, ♂ imp

α-methyl DOPA Stimulate NTS Post-syn α2A Initial: ↓ Metabolized to α-methyl NE (false NT) and Common…+...hemolytic anemia, Moderate HTN
α2 receptors ↑ NTS → ↓ SNS Eventual: ? acts mostly α2, little α1 centrally sedation, ♂ imp, ↑ lactation, EP signs (LVH)

Clonidine Stimulate NTS Initial: ↓


No DA problems (↑ lactation, EP signs) Less ortho hypo, rebound W/D HTN HTN (?)
α2 receptors Eventual: ~

Hydralazine ↑ NO Initial: ↑ Tachycardia, fluid retention, edema,


Can produce a lupus-like syndrome Severe HTN
Direct on VSM

↑ K+ permeability Eventual: ? headache, nausea

Minoxidil Initial: ↑ Preference for resistance (over capacitance) Same as hydralazine Severe HTN
↑ K+ permeability
Eventual: ? vessels….↓ venous pooling (should use w/β-blocker & diuretic) w/ renal disease

Sodium Metabolized to NO Initial: ↑ Unstable: degrades → thiocyanate & CN


Very short Nausea & headache HTN Crisis!
↑ cGMP Eventual: ? IV only: moment to moment control
nitroprusside
Thiazide

Hydrochlorothiazide
Diuretic

↓ Na+ reabsorption Initial: ↑ Hypokalemia, hyperglycemia,


Ceiling effect of 15 mmHg Mild HTN
in DCT → ↑ urine Eventual: ~ hyperuricemia, ↑ chol & ↑ TAG
Chlorthalidone
Sparing
Diuretic

Amiloride Aldosterone Initial: ? Used with thiazide diuretic to avoid Hyperkalemia (in renal disease) Not anti-HTN by
K+

antagonist Eventual: ? hypokalemia Gynecomastia themselves…


Spironolactone
Proproanolol Mild-Moderate
Initial: ↓
HTN
↓ CX, ↓ CO, ↓ renin Recommended use: w/ CHF or angina
Atenolol ↓ pre-syn. (+) fdbk NSAIDs interfere w/anti-HTN effect
β Blockers

Mild-Moderate
Initial: ↓
↓ Heart, bronchial CX, hypoglycemia, HTN
W/D rebound, exercise intol.
Acebutolol Same as above Partial agonist activity: ↑ TAG & ↓ HDL Mild-Moderate
Initial: ↓
(+ partial agonist) less ↓ HDL & less exercise intolerance HTN

Labetalol
α1/β1/β2 blocker Initial: ↓ HTN Crisis!

Prazosin
Antag

Block α1 Syncope (initial trx), ortho hypo, Mild-Moderate


α1

t1/2 = 3-4 hr Initial: ↑ Could cause cardiac events


(& some α2B) tachycardia, headache, depression HTN

Captopril Prevent A1 → A2 Also inhibit bradykinin metabolism


Ca2+ Channel Blockers Angiotensin

Short Initial: ? Cough, rash, leukopenia, renal, Moderate HTN


Inhibitors

conversion …leads to PGI2 production → cough


Renin-

Long (prodrug) Eventual: ? ageusia, fetal ab, no ortho hypo, (LVH)


Enalapril (ACE inhibitors) Good in diabetics (renal)/CHF
K+ diuretic, BC, NSAID, lithium intaxn
Losartan Vasculature A-2 Initial: ? Hypotension in volume-depleted pts
Similar to ACE inhib. but no cough HTN (?)
receptor blocker Eventual: ? Less effective in Afr.Americans

Nifedipine DHP Ca2+ Initial: ? Reflex tachycardia


Good vasodilation w/ less cardiodepression
channel blocker Eventual: ? Adverse cardiac events
Should use
Verapamil L-type Ca2+ channel long-acting Initial: ? Little reflex tachycardia HTN (?)
Cardiodepression: ↓ HR & ↓ CO
blocker (short acting → ↑ Eventual: ? Adverse cardiac events (Not first-line)
toxicities)
Diltiazem Ca2+ channel Initial: ? Little reflex tachycardia
Similar to Verapamil…but less ↓ HR & ↓ CO
blocker Eventual: ? Adverse cardiac events

Sildenafil
PDE5
inhib

PDE-5 inhibitor Initial: ? Requires ACh to initiate process: Rx interaction: (in cardiac pts) ♂ impotence
→ ↑ cGMP Eventual: ? M3 → NOS → GMP cyclase → ↑ cGMP Nitrates → ↑ NO → hypotension Pulm. Art. HTN
Drug Action Resistance Pharmacodynamics Adverse Reactions
Ciprofloxacin 1) Target modification

quinolones
Inhibitors of Nucleic Acid Synthesis

Fluoro
Inhibit DNA gyrase & topo IV 2) Altered uptake/efflux Administer: oral or IV Arthopathy (no preg or children)
Levofloxacin (Bactericidal) 3) Plasmid-mediated modification by Drug Intrxn: antacids ↓ oral avail. QT interval prolongation
quinolone transacetylase

Rifampin Inhibit RNA polymerase Administer: oral or IV Liver problems, induces cyt p450
Target site mutation in rpoB subunit
(Bactericidal) Distribution: great, CNS, intracellular (HIV meds), turns fluids orange
Metronidazole Produces compounds Administer: oral or IV ↓ elimination of lithium & ergot
(Rare, unknown mechanisms)
toxic to DNA Distribution: great, CNS derivatives...(no alcohol!)
Sulfanilamide PABA analog that binds DHP
synthetase → ↓ folic acid Allergy
Administer: oral or IV
Target site mutation, up-regulation, Not given to: G6P or folic acid
Drugs
Sulfa

Trimethoprim DHF acid analog that binds DNF Sulfa & trimethoprim given together
new genes, altered uptake/efflux deficiency, or pregnant
acid reductase → ↓ folic acid (TMX-SMX = Bactrim)
(Plasmid/Chromosomal) HIV: prophylaxis → neutropenia &
Sulfa given w/silver ions in cream
Dapsone PABA analog that binds DHP exfoliative dermatitis
synthetase → ↓ folic acid
Penicillin G/V
Penicillins

1) Altered transpeptidases Administer: oral or IV


Bind transpeptidase & prevent Allergy
2) ↓ permeability Distribution: good bioavailability
Artificial penicillin cross-linking (Can be desensitized)
3) β-lactamases Crosses BBB

Ticaricillin-
Clavulanic Acid
w/β-lactamase

Amoxicillin-
Penicillins

inhibitors

1) Bind transpeptidase & prevent 1) Altered transpeptidases Administer: oral or IV


Clavulanic Acid Allergy
cross-linking 2) ↓ permeability Distribution: good bioavailability
(Can be desensitized)
Inhibitors of the Bacterial Cell Wall

Piperacillin- 2) Bind & inhibit β-lactamase 3) β-lactamases Crosses BBB


Tazobactam
Ampicillin-Sulbactam
peptide peptide

Vancomycin
Poly Glyco

Binds D-alanine dimer in cross- Transposon: enzymes use D-serine or Administer: IV Red man syndrome: histamine
linking peptide in peptidoglycan D-lactate to make cell wall Distribution: good, CNS (inflam.) mediated w/rapid IV admin.
Bacitracin Binds membrane lipid carrier Administer: topical
Allergy (rare)
molecule → ↓ cell wall comp. (often w/neomycin & polymyxin B)
Cephalexin
Cephalosporins

Cefotaxime
Allergy
Bind transpeptidase & prevent
(5-10% PCN-allergy cross-
Ceftazidime cross-linking
hypersensitivity)

Ceftriaxone
penem bactam

Aztreonam
Carba Mono

Bind transpeptidase & prevent No PCN-allergy cross-


cross-linking hypersensitivity
Imipenem-Cilastatin Bind transpeptidase & prevent Cilastatin = inhibits renal Allergy
Ertapenem cross-linking dihydropeptidase I to prolong t1/2 (PCN-allergy cross-hypersen.)
Drug Action Resistance Pharmacodynamics Adverse Reactions
Streptomycin
Aminoglycosides
Neomycin Administer: IM or IV
1) Block protein synthesis by
1) Modifying enzymes (most com .) Post-ABX Effect: persistent Nephrotoxicity
bacterial ribosomes
2) Efflux pumping suppression after drug removal Ototoxicity
Gentamycin 2) Disrupt magnesium bridges in
3) Altered ribosome binding Conc.-Dependent Killing: (Particularly Streptomycin)
LPS
↑ concentrations → better killing
Tobramycin

Tetracycline
Inhibitors of Bacterial Protein Synthesis

Tetracyclines

1) Efflux pumping (most common ) Administer: oral or IV Nausea


Doxycycline Block protein synthesis by bacterial 2) Altered ribosome binding Distribution: good, including CNS Photosensitivity
ribosomes Drug Intx: food → ↓ absorption Can discolor teeth
Antagonizes β-lactams (not given to children or pregnant)
Tigecycline
Not affected by resistance

Erythromycin
More nausea & ↑ QT prolongation
Macrolides

Azithromycin Administer: oral or IV


1) Methylation of ribosomes
Block protein synthesis by bacterial Distribution: good
(most common )
Clarithromycin ribosomes Azithromycin: long intracellular
2) Efflux pumping
half-life, given to children, pregnant

Telithromycin
Severe hepatotoxicity
dinone samide

Clindamycin Block protein synthesis by bacterial 1) rRNA methylation/adenylation Administer: oral or IV or topical
Oxazoli Linco

Allergy
ribosomes 2) altered ribosomal proteins Distribution: good, but no CNS
Linezolid Block protein synthesis by bacterial Administer: oral or IV Thrombocytopenia
ribosomes Distribution: good Contraindication: SSRI
Chloramphenicol Block protein synthesis by bacterial 1) acetylation (most common ) Aplastic anemia, BM suppression
Administer: oral or IV
ribosomes 2) efflux pumping Gray syndrome (shock, coma)
Strepto

Quinupristin-
gramin

Block protein synthesis by bacterial Arthralgias


Occurs if only one of the two is given Administer: IV
Dalfopristin ribosomes Myalgias
Polymyxins Administer: Topical or IM or IV
Disrupts bacterial membranes Few
(often w/neomycin & bacitracin)
Miscellaneous

Daptomycin Cyclic lipopeptide: interferes ↑ liver fx tests


Administer: IV
w/bacterial membrane muscle weakness & pain (↑CPK)
Nitrofurantoin Radiomimetic Administer: oral Turns urine brown
Altered levels of reduction enzymes
(IC enzymatic redctn required) (drug concentrated in urine) Lung problems w/chronic use
Mupirocin
Disrupts protein synthesis
Drug MOA Treats Toxicity What Makes it Unique Mnemonic
Mechlorethamine Bone marrow Interesting N-(CH2-CH2-Cl)2
Hodgkin lymphoma
GI structure activates to ring
Monofx: modify DNA base
Cyclophosphamide Bifx: DNA cross-link or DNA-protein Bone marrow (immunosupp) Tall lean cyclist has bladder
Non-Hodgkin Lymphoma Acrolein byproduct toxic but
Alopecia problems & needs a mens
Breast/Ovary Carcinoma rescued by MESNA
Ifosfamide Hemorrhagic cystitis room!
Carmustine Bone marrow (immunosupp) We must preserve the brain
↑ lipophilic → crosses BBB Brain tumors
Nephrotoxicity (long-term trx) to maintain life!
Lomustine
(Phase non-specific)

Streptozocin Insulin shock


Pancreatic islet cell Retained in β cells of islets of
Alkylating Agents

Inhibits DNA synthesis Nephrotoxicity


carcinoma Langerhans
Hepatotoxicity
Busulfan
CML Pulmonary fibrosis

Dacarbazine Active metabolite monomethyl triazeno Dcarb: Hodgkin lymphoma Bone marrow (immunosupp)
methylates DNA Temozo: malignant glioma Nausea
Temozolomide
Procarbazine Hodgkin/Non lymphoma Bone marrow (immunosupp)
Drinking, driving, & drugs
Inhibits DNA/RNA/protein synthesis SCLC, Melanoma Neurotoxic & leukemia
don't mix!
Brain tumors Contraindx: EtOH/Drugs
Cis-platinum Forms intrastrand & interstrand DNA CURES: testicular tumor Ototoxicity Testes & ovaries are
cross-links → ↓ DNA/RNA synthesis Ovarian cancer Nephrotoxicity precious, & platinum is a
Carboplatin Produces DNA breaks Also: SCLC & bladder CA Electrolyte disturbances precious metal!
Oxaliplatin Bone marrow (immunosupp)
Forms platinum-DNA cross-links → Colorectal cancer (malig.) CRC: w/5-FU & Leucovorin Good for ovaries & your
Nausea/diarrhea/fatigue
↓ DNA synthesis Ovarian cancer (adv.) Ovary C: w/Cisplatin & Paclitaxel o-ring
Neurotoxicity (glutathione helps)
Methotrexate CURES: osteosarcoma & Bone marrow (immunosupp) Develops resistance via DHFR ,
Inhibits DHFR → ↓ thymidylate, ↓ Luke to the rescue
choriocarcinoma GI transport, MPs
purines, ↓ methionine, ↓ serine (meth lab)!
ALL, Burkitt's, Non-H, Blad Nephro & Hepatotoxicity Also treats RA & psoriasis
6-Mercaptopurine Converted to 6-MPRP by HGPRT → Bone marrow (immunosupp) Thiopurine methyltransferase
ALL MP controls ALL
↓ purine synthesis 6-MP can → gout (give Allopurinol) mutation → ↓ 6-MP metabolism

6-Thioguanine Converted to nucleotide → inhibits


PRPP amidotrx → ↓ DNA synthesis
(S phase specific)
Antimetabolites

Fludarabine Unnatureal purine → incorporated into


Leukemia Bone marrow (immunosupp)
DNA & RNA → ↓ synthesis & ↓ function

Pentostatin

5-Fluorouracil Converted to 5FdUMP → Breast cancer Bone marrow (immunosupp)


Patients on Cimetidine have
↓ thymidylate synthetase → Colorectal cancer GI
↑ survival rate
↓ TMP → ↓ DNA synthesis Basal cell carcinoma Mod: Cispt/IFN/Luke/MTX/PALA/Uridine
Cytarabine Converted to AraCTP → incoporated Acute leukemia
Bone marrow (immunosupp)
into DNA → terminates elongation (w/6-TG)

Gemcitabine Bone marrow (immunosupp)


Converted to dFdCTP → incorporated Pancreatic cancer (1st line)
Flu-like syndrome Not S-phase specific
into DNA → terminates elongation Non-SC lung cancer
Elevated liver enzymes (transaminases)
Vincristine ALL (1st line) Vinocristine = treats
Hodgkin/Non-H lymphoma Peripheral neuropathy children
Acute myelo leukemia Vinocristine = Christ PN
Vinblastine CURES: testicular tumor
Binds tubulin to ↓ polymerization into Vinoblastine = bone marrow
Hodgkin/Non-H lymphoma
microtubules supp.
Choriocarcinoma
Bone marrow (immunosupp)
Vinorelbine Non-SC lung cancer (adv.) Vinorelbine = bone marrow
Breast cancer (adv.) supp.
Antimitotics

Paclitaxel Neutropenia (give G-CSF)


Promotes microtubule formation & Ovarian cancer (met.) Abraxane = albumin-bound Taxol
Hypersensitivity (give
stabilizes the polymer Breast cancer (met.) (give ↑ doses)
dexameth/diphen/H2)
Etoposide Testicular cancer
Etoposide = topoisomerase
Prostate cancer
II
Inhibit topoisomerase II → Oat cell lung cancer
Bone marrow (immunosupp)
Teniposide ↓ DNA replication Teniposide =
ALL topoisomerase II
Teniposide = ten year-olds
Topotecan Colorectal cancer (met.) Bone marrow (immunosupp) Topotecan =
Inhibit topoisomerase I →
Ovarian cancer (met.) Alopecia & skin bronzing & cholinergic sx topoisomerase I
↓ DNA replication
Irinotecan SC lung cancer (adv.) Nausea/vomiting/diarrhea/mucositis Both "tecans" do the same
Actinomycin D CURES: Wilm's tumor
& rhabdomyosarcoma Bone marrow (immunosupp) Flat ring structure
MTX-res. Choriocarcinoma
Doxorubicin Myeloma
Sarcoma
Intercalates between GC bp → binds Lymphoma
Of the Rubicin sisters, Epi is
Daunorubicin DNA → ↓ DNA/RNA synthesis Bone marrow (immunosupp)
less likely to break your
Acute leukemia Alopecia
heart (she is "above"
Cardiotoxicity
Antibiotics

that….Epi)!
Epirubicin

Plicamycin Bone marrow (immunosupp) Specific to osteoclasts →


Inhibits RNA synthesis Bone cancer (met.) Hepatotoxicity ↓ [Ca2+] in hypercalcemic
Nephrotoxicity patients
Bleomycin Glycopeptides that bind DNA → CURES: testicular cancer Bleomycin = DNA breaks
Pneumonitis & Pulmonary fibrosis
produce free radicals → strand breaks Squamous carcinoma Least myelosuppressive
Hyperpigmentation, alopecia, stomatitis
Inhibits DNA ligase → ↓ DNA repair Lymphoma activity
Mitomycin Cervical cancer Bone marrow (immunosupp)
Mighty Mitomycin is the one
Cross-links DNA → ↓ DNA synthesis GI cancer (stomach/anus) Nephrotoxicity
treating cervical cancer!
Lung cancer Interstitial pneumonia
Drug MOA Treats Toxicity What Makes it Unique Mnemonic
Tyrosine Kinase Inhibitors Miscellaneous
L-asparaginase Metabolizes L-asparagine required by Hypersensitivity, hyperglycemia,
Sometimes interferes w/other
tumor cells with ↓ asparagine ALL Coagulation defects, hypoalbuminemia ALL disparaging
drugs activity
synthetase …due to ↓ normal protein
Tretinoin Nasty drug….retinoic acid syndrome:
Stimulate transcription of retinoic acid CURES: Prostate cancer
fever, wt gain, SOB, heart, photosens., Can become resistant
receptor genes Leukemia
skin, hearing, diarrhea, liver enzymes,
Imatinib mesylate ↑ [Warfarin]
Nausea, diarrhea, edema, cramps, rash
Binds to Bcr-Abl kinase → ↓ activity CML Itraconz & Erythro → ↑ [IM]
Neutropenia, thrombocytopenia
Phenytoin → ↓ [IM]
Gefitinib EGFR mutations correlate with
Inhibits EGFR tyrosine kinase → (Well tolerated!) Asian non-smokers Get fit
Non-SC lung cancer drug's efficacy
↓ cell proliferation & survival Diarrhea, acne-like rash without lung cancer
Works best in Asian non-
Sunitinib RCC (adv.) Fatigue, anorexia Ketoconz → ↑ [Sunitinib] Sunni are vegetarians &
Inhibits VEGFR & PDGFR kinase
GI stromal tumors Nausea, diarrhea, mucositis, stomatitis Rifampin → ↓ [Sunitinib] pretty darn good

Sorafenib Inhibits cell surface & intracellular Fatigue, diarrhea, dermatologic


RCC (adv.)
kinases Hypertension, neutropenia, bleeding

Bortezomib Nausea, diarrhea, anorexia, fever, weak


Protea
some
Inhib.

Reversible 26S proteasome inhibitor → My llama is a bore, I've had


Multiple myeloma Neuropathy, neutropenia,
↓ activation of NFκB enough (NF)!
thrombocytopenia
Trastuzumab Fever & chills
Antibody that blocks (amplified) HER2/neu is overexpressed in Adam Trask's wife broke his
Breast cancer (met.) Cardiotoxic (if given w/Adriamycin)
Specialty Antibodies

HER2/neu receptor → ↓ growth signal breast cancer heart with her new pistol
Respiratory problems
Rituximab Antibody that blocks CD20 antigen on Fever & chills Does not deplete stem cells Ritu has 20 CD's which will
Non-H B-cell lymphoma
B-cells → ↓ B-cells in blood Nausea w/first infusion (which lack CD20) be selled.

Cetuximab Antibody that blocks (amplified) EGFR is overexpressed in Can see (C) Colorectal
Colorectal cancer Acne-like skin rash
EGF receptor → ↓ growth signal colorectal cancer cancer in situ (Cetu)

Bevacizumab Antibody that blocks VEGF → prevents


Nausea, constipation, GI bleed, abd. pain The color of a very good
binding to endothelium → ↓ Colorectal cancer (met.) In combo w/ 5-FU & leucovorin
Hypertension, ↓ wound healing beverage
angiogenesis
Interferons 1) Stim. 5-oligoadenylate synthetase Hairy cell leukemia Bone marrow (immunosupp)
Harry interferes and should
2) ↓ c-myc 3) ↓ protein synthesis Kaposi's sarcoma Fever & chills Antiviral activity
mellow out.
Biological Response

4) Activates nuclease degrades dsRNA Melanoma (malig.) Neurotoxicity


Interleukin-2 Nausea, diarrhea, fever, ↑ liver function
Induce T-cell response → kill tumor Melanoma (malig.)
Modifiers

Anemia, hypotension, edema, arrhythmia


cells RCC
Thrombocytopenia
G-CSF Induce neutrophil & granulocyte Chemotherapy-induced
Bone pain Doesn't treat cancer
precursor formation neutropenia

GM-CSF Rescue bone marrow graft failure Bone marrow Fever


Speed bone marrow graft recovery transplantation Bone pain

Diethylstilbesterol Block production of LH → Hypercalcemia Prostate cancer is still the


Prostate cancer (met.)
↓ testosterone Vaginal carcinomas in offsprings best.
Ethinyl Estradiol
Tamoxifen ↓ osteoporosis
Binds ER → estrogen antagonist Breast cancer Nausea, hot flash, rash, vag bleed, ↑ Ca
↓ serum & LDL cholesterol
Depletes ER, EGF, IGF-1 (Post-men; in ER+ tumors) May cause endometrial cancer
Toremifene ↑ apolipoprotein A1
Fulvestrant Breast cancer Indicated for pre-menopausal
Binds ER → prevents dimerization Nausea, hot flashes, pain, headaches
(Pre-men; in ER+ tumors) breast cancer

Aminoglutethimide Post-menopause women The breast way to treat


Inhibits aromatase & desmolase → Breast cancer CNS depression
produce estrogen in adrenal Tammy, Ethyl, Anna, and
↓ estradiol (Post-men; in ER+ tumors) (drowsiness, blurry vision, ataxia)
cortex….. Medical Lenny is by aromatherapy.
Hormones

Anastrozole Reduced incidence of blood clots


Breast cancer GI, weakness, headaches, bone/back
& vaginal bleeding compared to
(Post-men; in ER+ tumors) pain
Tamoxifen
Inhibits aromatase → ↓ estradiol
Letrozole Breast cancer Nausea
(Post-men; in ER+ tumors) Musculoskeletal pain

Prednisone ALL, CLL


Converted to prednisolone → binds Cushing's syndrome ALL pretty girls should get
Hodgkin/Non-H lymphoma
receptor Immunosuppression phone CaLLs
Breast cancer
Leuprolide LHRH analog that initially ↑ FSH & LH A goose named Lou was
Transient flare w/initial dose
secretion → desensitization → ↓ FSH & Prostate cancer Sexual dysfunction sick with the flu, but still
(give flutamide)
Goserelin LH → ↓ testosterone/estrogen showed flare at the pro state
Flutamide Converted to dihydroxyflutamide → Dwight (DHT) plays the
Prostate cancer GI distress
blocks DHT binding to receptors flute but he's still a man
Drug Mechanism Metabolism Toxicity What makes it unique Treats

Periph: N/V, OH, arrhythmia


Dopamine agonist (→ DA)
CNS: On-off, wear-off, dyskin ↑ SNS tone peripherally
Levodopa L-DOPA −(AADC)→ DA L-DOPA → DA (AADC)
Psych: hallucin, delusion, sleep N/V/anorexia via CTZ stimulation
Carbidopa ↑ DA in striatum DA (MAO-B, DBH, COMT)
Peak-Dose: grimace/writhe Tubero-infund DA → ↓ prolactin
C-DOPA: ↓ peripheral AADC
Neuroleptic malignant syndrome
Dopamine Agonists
Used in "frozen" cases
Apomorphine Dopamine agonist (Reverses "off" state)
Advanced PD on ↑ dose L-DOPA

Bromocriptine B: D2 agonist / D1 antagonist B: short half-life Bromo only works in L-DOPA Pergolide
Pergolide P: D2 agonist / D1 agonist P: better w/L-DOPA (D1 & lipophilic) allows ↓ L-DOPA dose
Nausea, somnolence, dry mouth, edema,
insomnia, postural/OH
Peak-dose, on-off,
depr., anxiety, hallucinations Reduce on-off in late PD
Pramipexole Parkinson's Disease
D2 agonist Pramipexole can delay L-DOPA by 2
Ropinirole years
Inhibitors
MAO

Selegiline Used when L-DOPA effects are starting to


Inhibits MAO-B → ↑ striatal DA
Deprenyl decline
Anticholinergic

Treats influenza A & hepatits C


May: alter DA release/reuptake Restlessness, agitation, insomnia,
Amantadine Block NMDA receptors confusion, hallucinations, OH
No effect on tremor
Block mACh receptors
Inhibitors
COMT

Tolcapone Produce 2x ↑ in bioavailability & half-life Competes w/L-DOPA → BBB May


Inhibits COMT → ↑ DA in cleft Tolcapone: fatal hepatoxicity
Entacapone of L-DOPA cause "wear-off" / "on-off"
Psychotics Depressant

SSRI
Anti

Block 5-HT reuptake

Anxiolytics
Fatigue, restlessness, hyperexcitability,
tardive dyskinesia
Butyrophenone Huntington's Disease
Anti

Block DA receptors (D2) Help with tics

Phenothiazine

Reserpine Deplete DA vesicles → ↓ chorea Hypotension, depression, sedation, GI

Clonidine Don't w/d suddenly


α2 agonists Tachycardia, sweating, restlessness Tourette's Syndrome
Guanfacine Improve tics in 50% of children
Miscellaneous

Antipsychotics Block DA receptors (D2) ↑ dose APD helps


Neuroleptic malignant syndrome Tardive Dyskinesia
Bromocriptine Some 5-HT receptor block Balancing DA agonist helps

Primidone Anticonvulsant Abuse potential Congener of phenobarbital Benign Essential Tremor

Drowsiness, loss of coordination,


Baclofen GABA-B receptor agonist
confusion, nausea, seizures
Amyotrophic Lateral
Prolong time before tracheostomy
Sclerosis
Riluzole Reduces glutamate release Dizziness, GI, pain, diarrhea, weakness
Drug Mechanism Metabolism Toxicity What makes it unique Treats

Acute: nystagmus, diplopia, ataxia, GI, conf.


Admin: oral / IV (status epilepticus) Congeners (mepheny/etho-toin) more toxic Partial seizures
Chronic: Gingival hyperplasia, hirsutism,
Block Na+ channel 90% protein bound Phenacemide very toxic (refractory partial) Gen. tonic-clonic seizures
Phenytoin (prolong inactive state) First order (low) → Zero order (high)
osteomalacia, rash, agranulocytosis,
Fosphenytoin = more soluble (injection) Status epilepticus
megaloblastic anemia
Displaced by other protein-bound Rx ↓ BC effectiveness & birth defects (not absence)
High IV: arrhythmia, CNS depression

Partial seizures
Block Na+ channel Acute: stupor, coma, convulsions, irritability Accelerates metabolism: phenytoin, Gen. tonic-clonic seizures
Induces liver microsomes
Carbamazepine (prolong inactive state)
Produces active 10,11 epoxide metabolite
Chronic: diplopia, ataxia, GI, sedation, fluid reten primadone, ethosuximide, valproate, BC Trigeminal neuralgia
Enhance GABA activity Major: aplastic anemia, agranulocytosis Congener (oxcarb) less toxic, less potent Bipolar Disorder
(not absence)

Block Na+ channel


Partial & Generalized Tonic-Clonic Seizures

Partial seizures
(prolong inactive state) Sedation, ataxia, respiratory depression, rash,
Phenobarbital Prolongs GABA-A channel activity nystagmus, porphyria, tolerance, withdrawal
Congeners (mephobarbital & primidone) Gen. tonic-clonic seizures
(not absence)
Block AMPA receptor

Vigabatrin Enhance GABA

Partial seizures
Block Na+ channel
Generalized seizures
Lamotrigine (prolong inactive state) Headache, diplopia, rash, nausea, dizziness, ataxia Life-threatening rash in 1-2% of patients
Absence seizures
May block Ca2+ channel
Myoclonic seizures

NMDA antagonist Aplastic anemia Partial seizures


Felbamate Enhance GABA Severe hepatitis (poorly controlled)

Partial seizures
GABA analog
Gabapentin (↑ release of GABA?)
Renal excretion of unchanged drug Somnolence, dizziness, ataxia No liver involvement! Neuropathic pain
Alcoholism

Block Na+ channel


Somnolence, dizziness, fatigue, cognitive slowing, Partial seizures
Topiramate (prolong inactive state)
weight loss
Used for weight loss
Gen. tonic-clonic seizures
Enhance GABA activity

Tiagabine GABA reuptake inhibitor

Can produce euphoria


Partial seizures
Pregabalin GABA analog Neuropathic pain: post-herpetic neuralgia &
Neuropathic pain
diabetic neuropathy

Block T-type Ca2+ channel (↓ threshold) Good absorption orally (stomach irritation)
Generalized

Ethosuximide GI, lethargy, fatigue, rash, bone marrow suppression Phensuximide & methsuximide not as good Absence seizures
Seizures

↓ rhythmic thalamic activity 75% liver metabolized

Block Na+ channel Absence seizures


Well absorbed
(prolong inactive state) Nausea, vomiting, GI, hepatotoxicity, birth defects, Preferred over ethosuximide if absence + Myoclonic seizures
Valproic Acid ↑ GABA (↑ GAD) ↓GABA-T activity
90% protein bound
Sedation (w/phenobarbital) generalized tonic-clonic seizures Atonic seizures
Liver metabolized
Block T-type Ca2+ channel Partial seizures
Miscellaneous

Diazepam Status epilepticus

Absence seizures
Clonazepam Sedation, tolerance, withdrawal Myoclonic seizures
Infantile spasms
Drug Mechanism Metabolism Toxicity What makes it unique Treats

Anxiety
Alprazolam Short acting
Depression

Rapidly absorbed Anxiety


Chlordiazepoxide Short acting Alcohol withdrawal

REM suppression
Rapidly absorbed
Triazolam Short acting (very )
REM rebound upon W/D Insomnia
Tolerance
Bind α1γ2 on GABA-A receptor ~
→ ↑ GABA binding freq. Rapidly absorbed Sedation, lethargy, fatigue, mental Don't induce their own metabolism Anxiety
Diazepam → ↑ Cl- conductance Long acting clouding, fine motor incoord, ataxia, (MDOS) Status epilepticus
Benzodiazepines

→ neuron hyperpolarizaiton W/D, convulsions Difficult to produce respiratory arrest


→ ↓ neuron activity ~ alone
Slowly absorbed
Oxazepam ~ Physio/Psycho dependence ~ Anxiety
Short acting
Anxiolytic-sedative ~ King Midas and Lora found a tri-
Hypnotic Anterograde amnesia color ox on their short trip to the
Anesthesia Slowly absorbed Paradoxical hostility Alps
Lorazepam Anticonvulsant Short acting ~ ~
Anxiety
Muscle relaxation Toxicity reversed by flumazenil Flur Diaz longed to be a clown
Alcohol withdrawal -BZ-1 & BZ-2 antagonist
Flurazepam Long acting -Not effective w/other agents Insomnia
-Short acting
-Must be given IV
Steep dose-response curve
Midazolam Short acting
Water soluble

Clonazepam Long acting Status epilepticus

?: 5-HT1A or DA receptor Palpitations, tachycardia No sedation, dependence, abuse,


Generalized anxiety D/O
Buspirone Major metabolite blocks α2 Slowly developing anxiolysis GI distress W/D, amnesia, CNS interx, motor
Anxiety w/MDD
(Not GABA receptor) Miosis, ↑BP (w/MAOIs)
(Non-Benzo/Non-Barb)

Meprobamate Propanediols indistinguishable from barbiturates in their drawbacks Muscle relaxant


Carisiprodol
Anxiolytics

Zolpidem Short acting

Bizarre night-time behavior


Acts just like Benzos (BZ-1) but Get some ZZZ's….
Zaleplon Short acting Less SE than benzos/barbs Insomnia
structually unrelated E-long-ate
Reversed by flumazenil

Eszoplicone Long acting

Thiopental
Ultra short acting Thio huxtable was ultra short Anesthesia adjuct
Methohexital Induce own metabolism (MDOS)
Barbiturates

Excessive sedation, confusion,


lethargy, motor incoordination
Pentobarbital Act at GABA-A receptor → prolong
Tolerance
Short-intermediate acting Drugs of abuse
Secobarbital Cl channel opening → inhibition
Phys/Psych dependence → W/D
Respiratory arrest
↑ ALA synthase → AIP
Phenobarbital Long acting Fennel seeds are long Anticonvulsant

Melatonin-1 & 2 agonist → Insomnia


Ramelteon ↓ sleep onset (sleep onset problems)
Drug Mechanism Metabolism Toxicity What makes it unique Treats

Antipsychotics
High dose, low potency DA: EPS, ↑ prolactin, wt gain
Blocks: α1=5-HT2A > D2 Jaundice, photosensitivity, Schizophrenia
Chlorpromazine Liver metabolized mACh: "anti-cholinergic effects"
Typical

mAChR, histamine receptors Parkinsonism, NMS, TD Schizoaffective D/O


Interax: produce sedation α1: orthostatic hypotension
Bipolar D/O
Haloperidol Mania
Blocks: D2 > 5HT2A Low dose, high potency Less CV & anti-cholinergic effects IM preparation Tourette's syndrome
Fluphenazine
Ortho hypotension, ~EPS
Blocks: D4=α1 > 5-HT2A > D2 Causes sialorrhea
Clozapine Weak agonist at M4 ACh receptor
↓ seizure threshold
Have to keep their mouth clozed
Atypical Antipsychotics

Agranulocytosis
Low doses → ↓EPS
Blocks: 5-HT2A > D2 Schizophrenia
Risperidone (potent @ D2…looks typical)
Therapeutic doses → EPS & DA: EPS, ↑ prolactin, wt gain
prolactin Schizoaffective D/O
Bipolar D/O
Weight gain prominent Especially good for negative SX of Mania
Olanzapine Blocks: 5-HT2A > D2 > α
(Metabolic syndrome) schizophrenia Tourette's syndrome
Less SE's

Aripiprazole Partial agonist at: D2 & 5-HT2A Minimal or no weight gain

Na+ or Mg2+ replacement Oral absorption Acute: fatigue, weakness, tremor Only drug that ↓suicide
Lithium ↓IP3/DAG, ↓cAMP Kidney excretion (↑ in preggo) Chronic: ↓thyroid, diabetes insipidus, Breast milk (Ebstein anomaly) Mania
↓NT release Narrow therapeutic window nephritis, edema ↑ dietary sodium can ↓ effect
Sedation, GI
Used for early mania Mania
Valproic Acid Hepatotoxicity As effective as lithium in early mania
Mood Stabilizers

Used as lithium adjunct (early)


Anti-convulsant Birth defects
Block Na+, enhance GABA Diplopia, ataxia, GI
Use anti-convulsant dose
Carbamazepine Used if lithium inadequate
Aplastic anemia, birth defects
Agranulocytosis

Anti-convulsant
Lamotrigine Used as lithium adjunct Mania
Block Na+

Sedation
Clonazepam Benzodiazepine Amnesia
Abuse, dependence
Drug Mechanism Metabolism Toxicity What makes it unique Treats

Inhibits NE & 5-HT reuptake Sedation


Imipramine Metabolized to desipramine Orthostasis
Tricycic Antidepressants

Blocks: α1, mAChR, histamine


Cardiotoxicity
Inhibits NE & 5-HT reuptake Anti-cholinergic effects
Pronounced anti-ACh visual effects: Depression
Amitriptyline (5-HT>NE) Metabolized to nortriptyline Hypomania
mydriasis & ↓accom. ~
Blocks: α1, mAChR, histamine Rash, photosensitivity
Enuresis
↓seizure threshold
(anti-ACh)
α1: hypotension → reflex SNS
Pain
Desipramine Inhibits NE reuptake Tachycardia Sudden death in children
ADHD
Arrhythmia
Angina, infarct
Inhibits NE & 5-HT reuptake Suicide
Nortriptyline (NE>5-HT) Impotence

↓CV SE's
2nd & 3rd Generation

Depression
Buproprion Inhibits DA reuptake (?) ↓sexual complications Psychomotor activation
Nicotine withdrawal
↓seizure threshold

↓CV SE's
Venlafaxine Inhibits NE & 5-HT reuptake
↑BP
Depression

Trazodone Trazodone: Sedation (in a tranz) Trazodone can cause priapism & Depression
Nefazodone Nefazodone: Hypnotic orgasms w/yawning (Nef>Traz)

Long acting Akathisia


Fluoxetine Active metabolite Behaviorally activating ↓ food intake → weight loss
SSRIs

Inhibits P450 system Depression


Nervousness, insomnia, N/V
Inhibition of 5-HT reuptake OCD
Sertraline Shorter acting (than fluox) Headache, anorgasmia
Bulimia
Suicide
Paroxetine No active metabolites (like fluox)
No inhibition of P450 system MAOI Interax: serotonin syndrome
Fluvoxamine
MAO Inhibitors

Phenelzine Irreversibly inhibit MAO-A & B → Interax: tyramine-containing foods →


↑NE & ↑5-HT & ↑DA Inhibit SIF ganglion cells → ↓BP Depression
Tranylcypromine hypertensive crisis
Headache Narcolepsy
~
Sexual dysfunction Phobia anxiety D/O
Reversibly inhibit MAO-A → Mood elevations in depressed &
Hypertension/hypotension OCD
Moclobemide ↑NE & ↑5-HT normal individuals

Interax: ↑ levels of…cyclosporine,


Partially inhibit NE & 5-HT reuptake Photosensitivity
St. John's Wort Bind GABA receptors
warfarin, indinavir, digoxin,
Induces liver enzymes
Depression?
Miscellaneous

amitriptyline

Substance P
Needs confirmation Depression?
antagonist

Psychotic major
Mifepristone Glucocorticoid receptor antagonist
depression
Drug Mechanism Metabolism Toxicity What makes it unique Treats

Irreversibly inhibit ALDH → Converted to active metabolites Acetaldehyde syndrome →


Disulfiram ↑acetaldehyde (which inhibit ALDH) alcohol flush reaction

Opiate µOR antagonist Reduces craving


Naltrexone Blocks alcohol reinforcement Reduces relapse rates by 50%
Alcoholism Treatment

Interacts with NMDA & GABA-A Reduces hyperexcitability during


Acamprosate receptors
Taurine derivative
withdrawal
Alcoholism

Facilitates GABA-A function


Topiramate Blocks AMPA & kainate receptors

Tiapride D2 dopamine antagonist

Alcoholism
Ondansetron 5-HT effects
(early-onset)
Toxic Alcohols

Headache, vertigo, vomiting,


Methanol −ADH→ formaldehyde
Methanol −ALDH→ formic acid
abd/back pain, dyspnea, met. Can cause blindness (15mL) Toxic
Acidosis, coma, resp. failure
Ethgly −ADH→ glycoaldehyde
Metabolic acidosis Treat with EtOH
Ethylene glycol −ALDH→ glycolic acid →
Renal failure (oxalate deposits) Treat w/fomepizole: ADH inhibitor
Antifreeze
glyoxylic & oxalic acid
Drug Mechanism Metabolism Toxicity What makes it unique Treats

Analgesia, sedation, euphoria, Mod-severe pain


30% absorbed in gut Pinpoint pupils = opioid OD
Morphine 90% first pass metabolism
dysphoria, miosis, N/V, OH,
Constipation
Myocardial infarction
Strong Opioid Agonists

resp. & cough suppression Dyspnea, anxiety

Fentanyl Sufentanyl = ↑ fentanyl Post-op pain


80x morphine potency Less nausea
Su & Alfentanil Alfentanyl = ↓ fentanyl Anesthetic (w/droperidol)
Potent MOR agonist
No cough suppression
1/5 morphine potency OB/Surg analgesia
Meperidine 1/4 morphine duration
Less constipation
Mod-severe pain
No labor prolongation
Same potency as morphine
No euphoria Mod-severe pain
Methadone ↑bioavailability than morphine
Prevents W/D signs Opioid addiction
Long acting

Metabolized in part to morphine Mild-moderate pain


Codeine Few SE
Moderate Opioid

Excellent bioavailability Cough


Agonists

1/2 codeine potency


Propoxyphene Weaker MOR agonist Given w/acetaminophen
Interax: alcohol/sedatives (fatal)
Mild-moderate pain

Oxycodone Given w/aspirin or acetaminophen Abuse

Given w/naloxone IV to avoid Combined w/tripelennamine


Pentazocine analgesic & euphoric effects ("T's & blues") → heroin-like
Moderate pain
Agonist-Antagonists
Mixed Opioid

30x pentazocine antagonism Mod-severe pain


Butorphanol 20x pentazocine analgesia Sedation (KOR) (acute)
KOR agonist Sweating, dizziness
MOR antagonist Psychotomimetic effects
Same potency as morphine Anxiety, nausea, vomiting Less psychotomimetic effects
Nalbuphine 5x pentazocine potency Less MOR antagonist activity
Mod-severe pain
Worse sedation & resp. depression
Buprenorphine 25-50x morphine potency (pain) than morphine
Binds MOR w/high affinity
Antagonists

T-REX is bigger than an OX, and a


Naloxone Fast onset
T-REX is more orally active!
Precipitates opioid W/D Opioid overdose
Opioid

Competitive opioid antagonist


(MOR) 3-5x naloxone potency
Opioid addiction
Naltrexone Long acting
(highly motivated)
Orally active (moreso)
Dental pain
Weak MOR agonist 1/10 codeine MOR affinity Less potential for abuse &
Tramadol Inhibits NE & 5-HT reuptake 6000x less morphine MOR affinity respiratory depression
Dual mechanism of action Acute MSK pain
Cancer pain
Drug Mechanism Metabolism Toxicity What makes it unique Mnemonic
Hepatotoxicity (free radicals)
Slow induction (↑ blood:gas)
Halothane Most potent (↓MAC)
Sensitizes myocardium to NE/EPI Halo = Heart
↑cerebral blood flow
General Anesthetics
(Inhalation)

Enflurane
Nonspecific interactions w/ lipid bilayer Fluranes (fluoride) can be nephrotoxic
Intermediate induction Fluranes fluoride floppy
Block K+ channels → hyperpolarization ↓minute volume
Intermediate potency muscles
Activate or facilitate GABA Muscle relaxation
Isoflurane

Fast induction (↓ blood:gas)


Nitrous oxide Least potent (↑MAC)
NO potency

Ultra short acting May produce "hangover"


Thiopental Barbiturate Rapid onset, short anesthesia Myocardial/Respiratory depression Thio huxtable is ultra short
Diffuses out of brain ↓cerebral/renal blood flow, ↓GFR
Not analgesic
Diazepam Slower onset Prolonged post-op. recovery
Benzodiazepines
Loraz/Midaz Long acting Anterograde amnesia
General Anesthetics (IV)

Morphine Analgesic
High potency opioid Can be reversed w/naloxone Respiratory depression
Fentanyl Only anesthetic @ ↑ doses

Rapid onset
Respiratory depression
Propofol Rapid recovery
Hypotension
Most popular IV anesthetic Be proper, don't puke
Anti-emetic
CV stimulation: ↑HR, ↑BP, ↑CO Analgesic
Ketamine Blocks NMDA receptors ↑cerebral blood flow, ↑ICP Amnesia Ketamine = catatonic
Disorientation, illusions, vivid dreams Catatonia
Analgesia
Can talk to the patient from
Droperidol Antipsychotic Given w/opioid (fentanyl) Pt. can respond to commands
behind the drape
(no loss of consciousness)
Nausea & vomiting
Rapid onset
Etomidate Rapid recovery
Pain Not analgesic He tummy ache
(Minimal CV/repspiratory Depression)
Drug Mechanism Metabolism Toxicity What makes it unique Use
Local Anesthetics (Esters)
Absorb via mucous membranes Produces vasoconstriction
Cocaine Block V-G Na+ channels Topical use
CNS stimulation & euphoria (abuse)
(All other LA's produce vasodilation)
Topical LA
in high frequency pain fibers
(spend lots of time "open") Short acting Infiltration
~ Aunt Ester had allergies
Procaine (metabolized by plasma ChE)
…but she was a peach! (PChE)
Nerve block
Weak bases (pKa=8-9) Given w/EPI Spinal anesthesia
1) uncharged into axoplasm
2) ionized & trapped inside More lipophilic than Pro/Coke:
Spinal anesthesia
Tetracaine 3) binds open Na+ channel Rapider onset, potenter Most commonly used drug for Spinals
Topical LA
~ Longer acting
Dusting powder
Quickly metabolized by PChE So poorly water soluble that systemic toxicity
Benzocaine Poorly water soluble
potential is zero.
Ointment
(burns/ulcerations)
LA
Lidocaine More lipophilic than Pro/Coke:
Drowsiness Used in ester-allergic individuals
Cardiac arrhythmias
Block V-G Na+ channels
Local Anesthetics

Rapider onset, potenter


in high frequency pain fibers
(Intermediate) Longer acting
(Amides)

Mepivacaine (spend lots of time "open") Lassitude in neonate OB LA


~
Weak bases (pKa=8-9) More lipophilic than Mep/Lido: Particularly long acting
Epidural anesthesia (OB)
Bupivacaine 1) uncharged into axoplasm Long acting Cardiotoxic (some nerve blocks last 24+ hrs!)
Nerve blocks
2) ionized & trapped inside Highly plasma protein bound Analgesia + abdominal muscle control
3) binds open Na+ channel
Procainamide Cardiac arrhythmias
Drug Mechanism Metabolism Toxicity What makes it unique Treats

Degranulation
Cromolyn Sodium

Inhibitors
Inhibit immunologically triggered mast Bronchial asthma
Ineffective after asthma attack has started
cell degranulation (prophylaxis)
Nedocromil

Block H1 receptor → ↓ histamine ax


H1 Receptor Antagonists

Rapidly absorbed orally Ineffective in bronchial asthma (mediated by Seasonal allergic rhinitis
Chlorpheniramine Allergies Metabolized by CYP3A4 more than just ol' histamine) Urticaria
First Generation

Motion sickness
Sedation Strong sedation! Allergies
Diphenhydramine Antiparkinsonian effects Ototoxicity Motion sickness
Promethazine Anti-cholinergic effects (newborns or ABX) Sedation
Anti-serotonergic effects
α receptor blocking Drug interax: cardiotoxic w/ conazoles or Metabolized to fexofenadine (not cardiotoxic),
Terfenadine Local anesthetic effects macrolides if CYP3A4 inhibited, terfenadine accumulates
Allergies
H1 Receptor Antagonists

Fexofenadine Lower risk of arrhythmia


Second Generation

Loratadine Block H1 receptor → ↓ histamine ax Long acting Little to NO sedation No significant side effects Allergies

Cyproheptadine Strong 5-HT blocking

Inhibits P450 system Diarrhea, muscle pain


Cimetidine Drug interax: ↑chlordiazepoxide, EtOH, Headache, dizziness
H2 Receptor Antagonists

propranolol, theophylline, warfarin Gynecomastia, impotence

4-10x more effective than cimetidine Less side effects than cimetidine
Ranitidine Does not interfere with P450 No antiandrogenic effects Gastric/duodenal ulcers
Competitive inhibitor of histamine (H2)-
Ci me, I ran ti dine with my family & my nizce ZE syndrome
stimulated gastric HCl secretion
GERD
Famotidine Not metabolized by P450 Don't use in renal disease

Nizatidine Don't use with salicylates


Inhibitor

Gastric/duodenal ulcers
Proton
Pump

Active form irreversibly binds & inhibits Absorbed in alkaline SI pH Diarrhea, nausea Heals duodenal ulcers more rapidly than H2
Omeprazole proton pump in parietal cells Use >2 months not advisable Dizziness, headache blockers
ZE syndrome
GERD
Aluminum salt of sucrose sulfate → Short acting
Constipation Additionally: inhibits pepsin & bile aciton
Protectants

Sucralfate binds plasma proteins in crater → Drug interax: blocks tetracycline & PO4 Duodenal ulcer
Mucosal

Nausea Also: ↑ prostaglandin release


protective barrier absorption

React w/proteins in acid medium → Black stools, black tongue


Colloidal bismuth protective barrier in ulcer crater Don't use in renal disease
May have ABX activity against H. pylori Gastric/duodenal ulcers
Protect

Prostaglandin E1 analog → ↓ H+ Nausea, diarrhea Gastric/duodenal ulcers


Cyto

Misoprostol ↑mucus & ↑bicarbonate secretion Abortion in preggos NSAID-induced damage


75% reaches colon Nausea, vomiting
Bacteria split azo bond → 5-ASA (& Ulcerative colitis (85%)
Sulfasalazine 5-ASA = active metabolite Headache Can cause ↓ folate absorption
Inflammatory Bowel Disease

sulfapyridine) → ↓ inflammation Colonic Crohn's Dz


Sulfapyridine = SEs Allergy

Hydrocortisone Corticosteroid → ↓ inflammation Acute episodes

Azathioprine Ulcerative colitis


Mercaptopurine Crohn's disease
Cytotoxins Low dose used for prophylaxis Toxicity may limit chronic use Used in nonresponsive cases

Cyclosporine Severe refractory IBD

Nausea
Monoclonal antibody against TNF-α → ↓
Infliximab inflammatory action
Single IV infusion → remission Serum sickness Crohn's disease
Infections, autoimmunity, cancer
Drug Mechanism Metabolism Toxicity What makes it unique Mnemonic Treats
Resistance: altered/deficient viral
Acyclovir Nausea, vomiting, diarrhea HSV
Valacyclovir −(rapidly)→ acyclovir thymidine kinase or
Valacyclovir Guanine nucleoside analog Headache, renal dysfx VZV
viral DNA polymerase
Viral thymidine kinase produces analog →
binds viral DNA polymerase & inactivates Myelosuppression, neutropenia vision CMVertables are fos
Ganciclovir CMV
disturbances, carcinogenic More toxic than acyclovir cars, cid so you ganci
Valganciclovir (retinitis)
CNS effects the road fomi
Nausea, diarrhea
Famciclovir Guanine nucleoside analog Famciclovir is a prodrug metabolized to
Headache Acute herpes zoster
Penciclovir Inhibits viral DNA synthesis active penciclovir
Tumors, testicular toxicity
Herpes / Varicella / CMV

Nausea, fever, headaches, hypocalcemia, CMV (retinitis)


Inorganic pyrophosphate analog
Foscarnet Reversibly inhibits viral DNA & RNA polymerases
hypomagnesemia, nephrotoxicity, anemia, More toxic than gancyclovir HSV
genital ulcer (acyclovir resist.)

HSV
Tri flurting w/Kera's
Trifluridine Pyrimidine analog Cornea inflammation
tits & HSV
(Keratoconjunctivitis)
(Epithelial keratitis)

Nephrotoxicity, neutropenia, metabolic


Cidofovir acidosis
CMV (retinitis)

Iritis, vitritis, ↑ intraocular pressure Don't give to patients who have taken CMV (retinitis)
Fomivirsen Antisense oligonucleotide
Vision changes cidofovir in past month (in HIV patients unresp)

For herpes, tri giving


Only effective if given at first symptoms
Docosanol Prevents viral fusion → ↓ viral entry acyclovir, doc (or HSV
(ineffective at papule stage)
dox)!

Iodinated thymidine analog


Pain, inflammation, edema HSV
Idoxuridine Incorporated into viral & cellular DNA →
of eyes or eyelids (keratitis)
susceptible to breaks & error in trx
Anorexia, nausea, peripheral edema Reduces duration & severity of influenza
Amantadine Metabolized by kidney CNS effects infection
Inhibits viral uncoating & blocks influenza A M2 (in renal failure dz) 90% of influenza is resistant! Influenza A
Viral Respiratory Infections

protein (↓ dissociation of RNP complex in


Parkinson's disease
replication)
Rimantadine Metabolized by liver

Nasal/throat discomfort, headache,


Zanamivir bronchospasm (asthmatics)
Inhibits neuraminidase → ↓ release of virus → Orally inhaled If taken within ~30 hrs of SX onset →
Influenza A & B
↑ viral aggregates & ↓ viral spread Used once taily to prevent flu ↓ duration & respiratory complications
Oseltamivir Nausea, vomiting, headache

Dexamethasone Croup

Ade for viruses Hepatitis B


Adefovir Inhibits viral reverse transcriptase Nephrotoxicity
Viral Hepatitis Infection

makes me hep B! (chronic)

IFNα & IFNβ bind cellular receptors → activate JAK- Flu-like symptoms, bone marrow HPV
Interferons STAT → ↑ 2,5-oligoadenylate synthetase & kinase IM or SC injection suppression, fatigue, infections, anorexia, Hepatits B & C
→ ↓ protein syn diarrhea, depr, anxiety Kaposi's sarcoma, MS

Renal dysfunction Tell bi he's a dead


Telbivudine Myopathy (↑ CK) hepatitis…..
Hepatitis B

Conjunctiva irritation, wheezing, rash Hepatitis C


Synthetic guanosine nucleoside analog Ribavirin blocks RNA
Ribavirin Alters nucleotide pool → ↓ viral mRNA syn
Anemia, bone marrow suppression
of virin
RSV , Influenza, HIV
Teratogenic Parainflu, Paramyxo

Induces IFNα & TNFα Local erythema, flaking, itching


Imquimod (and other cytokines) (topical)
I'm quiet about warts HPV
Drug Mechanism Metabolism Toxicity What makes it unique Mnemonic Treats
Converted via human thymidine kinase → AZT-TP Anemia, leukopenia, headaches, lactic Protects fetuses from infection
↑ toxicity w: probenecid, tylenol,
Zidovudine → incorporated into viral DNA → terminates chain
lorazepam, indomethacin, cimetidine
acidosis, hepatic steatosis, lipoatropy, Resistance: mutated RT w/↓ affinity for HIV
Nucleoside Reverse Transcriptase Inhibitors
elongation central fat, ↑lipids AZT-TP
Orally in buffered tablets HIV
Didanosine ↑ toxicity w: stavudine
Pancreatitis, peripheral neuropathy
(AZT resistant)
Resistance: mutated RT
Given w/AZT or alone
Zalcitabine (if can't tolerate AZT)
Stomatitis, peripheral neuropathy, rash HIV

Peripheral neuropathy
Stavudine Lactic acidosis, hepatic steatosis,
Zitty Zal went nuclear
HIV
lipoatropy, central fat, ↑lipids
& did stab a baby
Inhibits viral reverse transcriptase → terminates Resistance to AZT develops more slowly lamb he tends.
Lamivudine DNA chain elongation
Pancreatitis (pediatric patients)
if you add lamivudine
HIV
Hepatitis B
Emtricitabine Hyperpigmentation

Given w/AZT or Lamivudine or


Abacavir protease inhibitor
Hypersensitivity, fever, GI, malaise, rash HIV

Do not give w/didanosine, lamivudine, Flatulence HIV


Tenofovir abacavir Renal toxicity Hepatitis B
↓ [phenobarb, phenytoin, carbmzpne,
Dizziness, headache, insomnia, rash
Non-Nucleoside

Efavirenz Given w/AZT & lamivudine methadone, rifabutin]


RT Inhibitors

Nightmares, hallucinations
Rifampin → ↓ efav
↑ [rifampin, rigabutin, ergot, triazolam,
Binds next to RT activation site → change Given w/AZT & didanosine Never ever tell a nun
Delavirdine Rash midazolam, cisapride] HIV
conformation → inhibit RT activity Least potent a lie.
Efavirenz Rx & SJW → ↓ dela
↓ [rifampin, ketoconazole, ethinyl
Nevirapine Given w/didanosine & stavudine Rash, fever, nausea, hepatotoxicity estradiol (BC)]
SJW → ↓ nevir

Indinavir
Diarrhea, nausea, vomiting, lipodystrophy,
hyperglycemia
Saquinavir SJW lowers concentration

Ritonavir Diarrhea, nausea, fatigue, headache, Administered together:


Protease Inhibitors

hyperlipidemia, hyperglycemia, altered Ritonavir inhibits CYP3A4 →


body fat ↑ Lopinavir
Lopinavir Nel is a LIAR. She is
Interferes w/proteolysis of gag-pol viral protein a professional tease
HIV
precursor → nonfunctional virions and will inhibit or slow
Nelfinavir your fost progress

Although HIV cross-resistance occurs,


Inhibits CYP34A (Rx toxicity)
Amprenavir Rifampin induces CYP3A4
most likely to still be Amprenavir
Diarrhea, nausea, vomiting, lipodystrophy, susceptible
hyperglycemia
Atazanavir

Fosamprenavir

Binds viral envelope glycoprotein to prevent


Fusion

Pain, erythema, nodules, cysts


Inh.

Enfuvirtide conformational change when binding host cell


(at injection site)
Injected twice a day Binds enfulope HIV
membrane
Drug Mechanism Metabolism Toxicity What makes it unique Treats

Blocks V-G Na+ channels GI, hepatic granulomas, torsades, ↑ ventricular

(Intermediate τ)
↓ automaticity, prolonged QT, widened Can cause paradoxical ↑ in heart rate in

Na+ blocker
Quinidine & K+ channels rate w/A flutter, cinchonism, lupus-like Chronic SVT
Class 1A Blocks α-adren. & vagus
QRS, ↑ SA & AV node conduction velocity
syndrome
atrial flutter

Blocks V-G Na+ channels ↓ automaticity GI, hypotension, torsades, Converted to active metabolite NAPA →
Ventricular tachycardia
Procainamide & K+ channels ↑ refractory period heart block, agranulocytosis, lupus-like no Na+ channel activity but blocks K+
SVT
(no ANS effects) ↓ conduction velocity syndrome channels
IV use only (↑ first pass metab) Seizures
Na+ blocker

Lidocaine ↓automaticity, ↓ action potential, Nystagmus, tremor, dysarthria, altered


Class 1B

(Rapid τ)

Blocks Na+ channels, ↑ gK in fast ↓ conduction velocity sernsorium Ventricular tachycardia


fibers during phase 3 & 4 Ventricular fibrillation
Mexiletine Same, but orally effective Nausea, tremor, CNS effects Orally active

Blocks Na+ channels Proarrhythmic (after MI)


Atrial arrhythmia
(Very long τ)
Na+ blocker

Flecainide Blocks K+ channels Exacerbate CHF by ↓ LV fxn


Class 1C

↓ conduction velocity, widened QRS, ↑ (if no other strx disease)


Blocks Ca2+ channels Heart block (in AV node dz)
action potential,
Blocks Na+ channels prolonged QT, prolonged PR Proarrhythmic (after MI)
Propafenone Blocks K+ channels Exacerbate CHF by ↓ LV fxn Bradycardia & bronchospasm (β block) Atrial arrhythmia
Blocks β-adrenergic Heart block (in AV node dz), torsades
Non-selective β blocker Myocardial depression, heart block,
↓ AV conduction velocity, prolonged PR, ↓
Propranolol Na+ blocker at ↑ dose
automaticity in ectopic foci
bronchospasm, ↑ insulin hypoglycemia,
(membrane stabilization) depression, rebound SNS if w/d

Metoprolol β1 blocker
Class II - β Blockers

Non-selective β blocker
Carvedilol α blocker
Antioxidant properties Atrial flutter
Atrial fibrilliation
Ventricular arrhythmia (post-MI)
Intrinsic SNS activity, but no membrane Angina
Acebutolol Lupus-like syndrome
stabilizing effects

Atenolol β1 blocker Longer acting Less polar → less CNS effects

Used IV when immediate block is needed


Esmolol Cleared quickly

Blocks K+ channels Prolonged QT, ↓ automaticity, ↓ Corneal deposits (100%), liver dz, hypo &
Miscellaneous Ca2+ channel Class III - K+ channel blockers

First line agent in ACLS code Atrial tachycardia


Amiodarone Blocks Na+ & Ca2+ channels conduction velocity, hyperthyroidism, pulmonary fibrosis,
Active metabolite: desethyl-amio Ventricular tachycardia
Non-competitive SNS blocker widened QRS, prolonged PR vasodilation, photosensitivity/skin color
↑ action potential, ↓ automaticity, Renal excretion of unchanged drug
Blocks K+ channels Torsades (especially in hypokalemia) Atrial arrhythmias
Sotalol Non-selective β blocker
↓ conduction velocity (AV only), prolongs
β blocker SE's
β blocker w/Class III effects
(chronic)
AV refractory period
IV use only
Blocks K+ channels Torsades Atrial arrhythmias
Ibutilide Non-selective β blocker
Delays repolarization,
Contraindicated in hypokalemia
IV use only
(acute)
↓ action potential
Rx Interax: ↑ [Dofetilide]
Blocks K+ channels Atrial arrhythmias
Dofetilide (rapid delayed rectifier K+ current)
Greater effect on atria than ventricles Torsades Interfere w/cation trx in kidney, prolong QT
(chronic)
interval, use liver metab.

Given orally but IV is better


Class IV -

Verapamil
blockers

Hypotension → reflex tachy, neg. inotropy, More active L-isomer first pass met.
↓ HR, ↓ CX, ↓ conduction velocity (AV), SVT
Blocks L-type Ca2+ channels heart block (AV conduction dz), bradycardia
prolongs AV refractory period (acute or chronic)
(SA conduction dz), GI Less negative inotropic effects
Diltiazem (less ↓ CX)
Arrhythmias SVT
Direct: Blocks Na+/K+ ATPase ↑ CX (↑ Ca2+) Rx Interax: ↑ [Digoxin]
Digoxin Indirect: vagal stimulation Vagal: ↓ atrial AP & ↑ AV refractory
Nausea
quinidine & verapamil
(acute or chronic)
CNS effects CHF (↑ CO)
Binds adenosine receptors → opens Shortens atrial AP, ↓ automaticity, Transient: asystole, dyspnea, bronchoCX IV use only Atrial tachycardia
Adenosine ACh-sens. K+ channels (in ↑ AV refractory period, Atrial fibrillation Rx Interax: theophylline & caffeine block Atrial fibrillation
SA/AV/atria) ↓ AV conduction velocity Flushing adenosine receptors Produce controlled hypotension
Drug Mechanism Metabolism Toxicity What makes it unique Treats

Inhibit Na+/K+ ATPase binding 25% plasma protein bound


Glycosides

Digoxin Renal elimination Fatigue, malaise, dizziness, confusion,


extracellularly on α subunit
Digitalis

2 day half-life delirium, anorexia, N/V, abdominal pain, Aglycone portion = for cardiac activity
Prefers E1-P form → stabilize to E2-P
color vision, halos, bradycardia, AV Monosaccharide chain = metab. Heart failure
form >90% plasma protein bound block, ectopic beats, SA arrest, Eubacterium lentum in gut inactivates
Na & Mg favor binding
Digitoxin Hepatic elimination ventricular arrhythmias, EKG changes
K favors release 7 day half-life
Miscellaneous

Dopamine: tachycardia, arrhymthia


Dopamine Dopamine vasodilates renal vasculature via
Simulate β1 receptors → ↑ CX
Inotropes

Dobutamine: tolerance, vasodilation (via


Dobutamine D1 receptors
β2 receptors) Heart failure
Nausea, vomiting (serious)
Inhibits phosphodiesterase-III → PDE-III selectively found in cardiac & smooth Does more harm than good when used long-
Amrinone vasodilation & ↑ CX muscle
Thrombocytopenia, liver damage
term
Arrhythmia

Hyponatremia, hypokalemia,
Furosemide Diuresis & peripheral vasodilation → Short acting
hypocalcemia, hypomagnesemia, Heart failure
Bumetamide ↓ cardiac workload Very potent
hypophosphatemia
Diuretics

Hyrdochlorothiazide Hyponatremia, hypokalemia, Kidneys can adapt Heart failure


Diuresis Synergistic with loop diuretics
Chlorothiazide hypocalcemia, hypophosphatemia Ineffective at GFR < 30 ml/min (mild)

Add to other diuretics Hyperkalemia, anti-androgenic effects


Spironolactone Diuresis
(to help w/diuresis & to spare K+) (gynecomastia)
Avoids K+ wasting Heart failure

Captopril Venous & arterial vasodilation →


Abrupt ↓ in BP w/first dose (vol dep)
Enalapril ↓ preload & afterload
Rash, loss of taste, cough
Heart failure
Lisinopril (+ ↑ bradykinin)

Cyanide → thiocyanate
Hypotension, coronary steal, angina, Heart failure
Sodium nitroprusside cyanide toxicity, thiocyanate toxicity
(eliminated kidneys)
Angina
Metabolized to NO → venous & arterial No tolerance (different NOS from NG)
Isosorbide dinitrate vasodilation → ↓ preload & afterload CHF (acute & chronic)
Vasodilators

Flushing, headache, hypotension, reflex Fast first pass metabolism


Nitroglycerin tachycardia, Tolerance develops rapidly
Vasospastic Angina
Isosorbide 5-mononitrate (w/Ca2+ blockers)

Arterial vasodilation → ↓ afterload


Hypotension
Hydralazine ↑ CX
Reflex SNS activity
Heart failure
renal dilation → ↑ renal blood flow
Carvedilol Myocardial depression, bronchoCX,
Blocks β receptors in heart → counteracts May allow gradual up-regulation of β receptors
Metoprolol SNS input to heart to occur in the heart
hypoglycemia, fatigue, depression, Heart failure
Bisoprolol impotence, rebound SNS if W/D
Verapamil Worsening angina, worsening HF, heart Heart failure / HTN
Blocks L-type Ca2+ channel → Highly protein bound (~90%) Not helpful for systolic dysfx
Diltiazem vasodilation & ↓HR & ↓CX Liver metabolized
block (in AV dz), bradycardia,
Helpful for diastolic dysfx (cardiac filling)
Reentry arrhythmia
Nifedipine hypotension, edema, resp, GI Angina (vasospastic/exer)
Drug Mechanism Metabolism Toxicity What makes it unique Treats

Secreted into lumen via OA trx Metabolic acidosis, renal CaPO4 stones, CHF edema, Glaucoma
Inhibits CA in the PCT →
Acetazolamide Inhibits 85% of PCT HCO3 reabs hypokalemia, CNS, allergy Urine alkalinization
Anhydrase
Inhibitors ↓ Na & HCO3- reabsorption
Carbonic

Inhibits 45% of total HCO3 reabs Contraind: cirrhosis (encephalopathy) Mountain sickness

Used more often for glaucoma than


Dorzolamide Inhibits CA in the eye Topical application Minimal
acetazolamide
Glaucoma

Secreted into lumen via OA trx Decrease luminal (+) potential


Furosemide Eliminated via kidney (↓ K+ pushed out) → ↓Ca2+ & Mg2+ reabs
Hyponatremia/dehydration
Loop Diuretics

Shorter acting Hypocalcemia


Inhibits Na+/K+/2Cl- trx in TAL →
Bumetanide ↓Na & K & 2Cl reabsorption
50% liver elimination Hypokalemia 40x more potent Pulmonary edema
(50% kidney elimination) Metabolic alkalosis Edema (CH, renal, cirrhosis)
Hypomagnesemia Hypercalcemia
Longer acting
Hyperuricemia Hyperkalemia
Torasemide Faster absorption
Ototoxicity
80% liver elimination
Allergy
No sulfur group in its structure
Ethacrynic Acid Only if allergic to other loops
Worst ototoxicity

Low Na in cell sucks Na through basolateral


Secreted into lumen via OA trx
Hydrochlorothiazide Absorbed orally
Na/Ca exchanger → ↑ Ca2+
reabsorption

Chlorothiazide
Thiazide Diuretics

Shorter acting Hyponatremia/dehydration 10x less potent than HCT


Hypokalemia
Hypertension
Metabolic alkalosis
CHF
Inhibits NaCl cotrx in DCT → Hypercalcemia 10x more potent than HCT
Metolazone Longer acting Idiopathic hypercalciuria
↓Na & Cl reabsorption Hyperglycemia Different structure from thiazides
(renal stones)
Hyperuricemia
Nephrogenic diabetes insipidus
Longer acting Allergy
Weakness 20x more potent than HCT
Indapamide Excellent oral absorption
Different structure from thiazides
Eliminated via liver

Same potency as HCT


Chlorthalidone Longer acting
Different structure from thiazides

Competitive aldosterone receptor in DCT & ↓ Na+ reabsorption & ↓ K+ secretion Also inhibits DHT receptor → Cirrhosis (ascites)
Potassium-Sparing Diuretics

Hyperkalemia, metabolic acidosis, gynecomastia,


Spironolactone CT → ↓ in Na+ channels & ↓ in Principal cells
impotence, ↓ libido, GI, CNS effects
↓ testosterone Hyperaldosteronism
out K+ channels (Princ.) ↑ H+ secretion Intercalated cells Only diuretic not acting in lumen Hypertension

Less anti-androgenic effects (less DHT &


Eplerenone Epoxy-spironolactone derivative
progesterone receptor binding)
Heart failure

Secreted unchanged into lumen via Hyperkalemia (NSAIDs ↑ likelihood)


Amiloride organic base transporter Nausea, vomiting, diarrhea, leg cramps, headache,
Blocks Na+ channels in Principal cells in Eliminated unchanged via kidney dizziness Edema
DT & CT →
Hypertension
↓ Na+ reabs & ↓ K+ secretion Shorter acting
Triamterene Metabolized in liver → into kidney lumen Photosensitivity 10x less potent than amiloride
→ insoluble & ppts out

Must be given IV
Filtered & excreted exerting osmotic pull in Headache, nausea, vomiting, Intracranial pressure
Mannitol PCT & loop of henle
↑ flow → ↑ urea excretion →
hypernatremia/dehydration, pulmonary edema
Initial rapid expansion of plamsa volume
Renal excretion of toxins
↓ ability to concentrate urine

Demeclocycline Nephrotoxic Tetracycline antibiotic SIADH


Blocks ADH action in the CT →
↓ aquaporins
Bipolar disorder
Lithium Not very good Usually used to treat mania
Miscellaneous

(~SIADH)

Recombinant form of ANF →


Nesiritide ↑ Na+ excretion
Hypotension CHF

ADH V2 receptor antagonist →


Tolvaptan ↑ free H2O excretion & Heart failure
↓ urea & Na+ reabsorption
ADH V2 receptor antagonist →
ADH V1a antagonist →
Conivaptan ↓ vasocx & ↓ smooth muscle growth
↑ free H2O excretion &
↓ urea & Na+ reabsorption
Drug Mechanism Metabolism Toxicity What makes it unique Treats

Flu-like, hepatitis, asthma, rash, May contain organocholine


Echinacea Proposed immune stimulant
nausea, urticaria, anaphyaxis pesticides
URI or "Colds"

Contains ephedrine 16x risk of hemorrhagic stroke Weight loss


Ephedra (sympathomimetic)
Stroke, arrhythmias, hypertension
(w/phenylpropanolamine) Energy

Contains melatonin
May inhibit PLA2 → arachadonic Contraind: anti-coagulants Dizziness, nausea, indigestion, Migraines
Feverfew acid (may inhibit platelet aggregation) heartburn, oral ulcer, rash
Does work, but not better than
Arthritis
traditional treatment
Lowers blood pressure
GI distress, allergy, dermatitis,
Garlic Lowers cholesterol
bleeding, odor
Culture media for C. botulinum Hypertension
(small & brief)
Herbal medications & Nutrient supplements

Effective anti-nausea Contraind: anti-coagulants As effective as antihistaminics in Motion sickness


Ginger Inhibit thromboxane synthase (may inhibit platelet aggregation) nausea Morning sickness

Contraind: anti-coagulants Ginseng abuse syndrome:


Ginseng Many have NO donor capability (may inhibit platelet aggregation) CNS, arousal, HTN, nervous, Dementia
Phenelzine insomnia, vaginal bleeding
↑ACh activity
Dementia
Ginko biloba Effects 5-HT & NE Contraind: anti-coagulants GI, headache, allergy, bleeding
Circulatory disorders
VasoRX….Antioxidant...↓coag
Dry flaking skin, puffy face, red eyes,
Can cause serious cirrhosis & liver Anxiety
Kava Enhances GABA activty weakness, oral tingling, GI, SOB,
failure! Insomnia
EKG abnormalities

Inhibit 5α-reductase → ↓DHT


Saw Palmetto Block α1 receptors
Headache, GI, hypertension, ↓libido Trad. > Saw palmetto > placebo BPH

↑metabolism of: cyclosporine,


Contains hyperforin → activates
St. John's Wort PXR → ↑CYP450
indinavir, digoxin, phenobarbital, Photosensitivity Depression
tamoxifen, BC

Morning drowsiness, headache,


Valerian Small hypnotic effect
excitability, cardiac, odor
Insomnia

Gi discomfort, nausea,
Stimulate cartilage cells → GAG & Osteoarthritis
Glucosamine proteoglycans
photosensitivity, systolic HTN,
Wound healing
proteinuria
DHEA →androstenedione & Rash, dyspnea, N/V, diarrhea,
Creatine Athletic performance
testosterone & androsterone nervousness, fatigue, migraine,
Androstenedione Weight loss
Creatine → phosphocreatine myopathy, seizures, a-fib, testo
Drug Mechanism Metabolism Toxicity What makes it unique Treats

Growth Hormone ↑IGF-1, ↑ECM, ↑muscle, ↑soft


Administered daily in evening
Children: few
Childhood deficiency
Somatropin tissue, ↑urinary retention of nitrogen, Adults: per. edema, arthralgia,
(mimics normal pattern) Adult deficiency
Growth Hormone Associated Agents Somatotropin PO4, K+, anti-insulin myalgia, carpal tunnel syndrome

IGF Mitogenic & anti-apoptotic Should not be used after closure of


May induce hypoglycemia
SPIGFD: mutations in GH receptor, Severe primary IGF
Mecasermin Skeletal, muscle, organ growth epiphyses or in neoplasia post GHR defect, IGF-1 defects deficiency

GHRH Binds GHRH receptor → ↑cAMP → 40-80% of GH deficienct children Hexorelin: ↑cardiac performance Dx pituitary defect
Sermorelin ↑GH synthesis & release respond normally to GHRH (dilated cardiomyopathy) Hypothalamic GH deficiency
Hexa/Capromorelin
Binds SRIF receptor → ↓cAMP → Synthetic SRIF is resistant to Acromegaly
Somatostatin ↓GH release (synthesis intact) enzymes (t1/2: 3min→2hr)
↓GI motility & secretions, ↓bile PVR of hypothalamus = 14 AAs
Carcinoid tumors
Octreotide production, ↓gallbladder CX δ cells of pancreas = 28 AAs
Also inhibits TSH secretion Selective for GH (vs. insulin) VIPomas
PEGylated to ↑t1/2,
GH lysine replaced by glycine → GH ↑hepatic aminotransferase Does not reduce size of GH tumor or
Pegvisomant antagonist
↓immunogenicity…but ↓affinity
(otherwise well-tolerated) lower GH levels
Acromegaly
(8 AA substitutions fix that)
Bromocriptine
Paradoxical inhibitory effect on Headache, N/V, dizziness, postural
Cabergoline somatroph adenomas (↓GH)
Cabergoline > bromocriptine
hypotension, insomnia
Most useful in ↑GH & ↑prolactin Somatroph adenomas
Pergolide
CRH (hypothalamus) → ACTH (ant.
ACTH
HPA Axis

pituitary) → cortisol & aldosterone & Dx adrenal insufficiency


Cosyntropin sex hormones

CRH Binds CRH receptor → ↑cAMP → Ovine CRH = ↑t1/2 & potency Flushing, SOB, tachycardia, Blood drawn from inferior petrosal Dx ACTH-secreting tumor
Corticorelin ↑POMC → ↑ACTH (over synthetic) hypotension sinus after CRH stimulation location

TSH Binds TSH receptor → ↑cAMP → Dx residual thyroid


HPT Axis

Thyrotropin-α ↑iodide uptake & TH syn/secr'n carcinoma

TRH Binds TRH receptor → ↑Ca2+ → Admin: IV over 15-30 seconds Transient nausea, hypo/HTN, Dx 2° hypothyroidism
Protirelin ↑TSH & ↑prolactin (TSH → 2-5x basal in 30 min) flushing, palpitations Measure PRL reserves

Male infertility
hCG Used for LH activity (acts at same
Cryptorchidism
Choriogonadotropin-α receptor as LH, but longer t1/2)
Dx Leydig cell failure

hMG Used for LH & FSH activity IM


Derived from urine of Male infertility
Menotropin postmenopausal women Female infertility
Gonadotropins

FSH Used for FSH activity (merotropin Urofollitropin: IM/subQ


Multiple births, ovarian
Urofollitropin hyperstimulation syndrome, fluid Female infertility
w/LH component removed) rFSH: subQ
rFSH accumulation in cavities

Partial estrogen agonist (competitive Ovarian enlargement, vasomotor ↑amplitude (not frequency) of Induce ovulation
Clomiphene inhibitor of ER)
Admin: oral x5 days
flushing, OHSS pulsatile LH & FSH secretion Dx gonadotropin secr'n

GnRH Binds GnRH receptor → ↑Ca2+ →


Long-acting agents (leuprolide,
Hypogonadism, ↓bone Pulsatile: ↑LH & FSH release
GnRH deficiency
Gonadorelin histrelin, nafarelin, goserelin) have D- Delayed/precoc. Puberty
PLC → ↑FSH & ↑LH mineralization, ↑lipids Continuous: ↓LH & FSH release
Leuprolide, Goserelin AA's at cleavage site Gn-depen. Disease
No transient rise in gonadotropin
Ganirelix Competitive antagonists binding Inhibit premature LH surge
subQ secretion as with continuous GnRH
Cetrorelix GnRH receptor → ↓LH > ↓FSH in ovary stim.
administration
Pituitar

Binds V1a receptors → GI/vasoCX Desmopressin challenge: urine Osm Central diabetes insipidus
Post.

Vasopressin VasoCX
Binds V1b receptors → ↑ACTH Nasal spray, subQ should ↑50% w/central DI Dx central/nephro DI
y

Desmopressin ↑GI muscle, ↑uterine muscle


Binds V2 receptors → ↑aquaporins SIADH: Rx w/loop/demeclocycline Post-op ileus...eso varices
Drug Mechanism Metabolism Toxicity What makes it unique Treats

Admin: transdermal patch


17 β-estradiol Most potent natural steroid
Ethinyl estradiol = #1 estrogen
Extensive first pass metabolism
Norethidrone = #1 progestin
Endometrial hyperplasia
Low-dose mono-triphasic = #1 Hormone replacement
Conjugated & esterified natural Endometrial cancer
Esterified estradiol steroids
Admin: IM
Breast tenderness
~ (Primary hyogonadism)
Suppress ovulation by negative Prostate cancer
Feminization in males
Estrogens

feedback on gonadotropin release


Cholestasis (GB disease)
Ethinyl estradiol Admin: PO
Hepatic adenomas
~
Mestranol ↓ first pass metabolism (ethinyl) Progestins = thicken cervical mucus Oral contraceptive
↑plasma TAG
Synthetic steroidal estrogens ~ Hormone replacement
Thromboembolic disease/MI
Thin endometrium (Primary hypogonadism)
Admin: IM (x1/month) Headache, migraine
Estradiol cypionate ↓ ovum transport
Insoluble in water BC Interax: ABX, phenytoin,
~
barbiturates
↑hormone binding proteins
Admin: PO ↑insulin secretion & resistance
Diethylstilbesterol Advanced prostate
Synthetic non-steroidal estrogens As potent as estradiol
Methallenestril carcinoma
Longer t1/2 than estradiol

Progesterone
↑fat deposition & weight gain
The only role of the progestin
Progestins

Acne
component of combination oral
Admin: IM Menstrual abnormalities Endometriosis
Medroxyprogesterone contraceptives is to protect
>oral activity than progesterone Uterine cramps Dys/amenorrhea
endometrium from estrogen-induced
Hirsutism (androgenic preps)
hyperplasia & cancer
Norethindrone ↑risk of breast cancer
Oral contraceptive
Norgestrel Suppress gonadotropins
Levonorgestrel
Pure estrogen receptor antagonist → Admin: IM (x1/month) ER+ metastatic breast
Estrogen Receptor

Fulvestrant ER downregulation As effective as anastrozole cancer


Modulators

Breast: estrogen antagonist


Tamoxifen Lipids, bones, uterus: agonist
ER+ breast cancer

↓total cholesterol Osteoporosis


Raloxifene ↓risk of breast cancer (in post-menopausal)

Binds irreversibly to aromatase →


Synthesis

Exemestane Structure similar to androstenedione


Inhibitors
Estrogen

inhibiting conversion to estrogen Breast cancer


(unresponsive to
tamoxifen)
Anastrozole Nonsteroidal aromatase inhibitor

Competitive binding to progesterone


Progestin

Inh. prog receptor & ↑PG → uteroCX Abortifacient


Anti

Mifepristone receptor & ↓prostaglandin


Given w/misoprostol 2 days later
Also blocks glucocorticoid receptor
Cushing syndrome
dehydrogenase
Drug Mechanism Metabolism Toxicity What makes it unique Treats
Intrx: steroids, tmxfn, opioid, 5-FU,
Nervousness, arrhythmia, HTN,
Identical to endogenous T4 phenytoin, CPZ, salicylate, benzos ↑TBG in children & preggos →
Levothyroxine Converted to T3 Contraind: adrenal insufficiency
SOB, N/V, diarrhea, heat intolerance,
↑doses required
Thyroid hormone replacement
↓reproductive fx

Rash, agranulocytosis, arthralgia,


Propylthiouracil Inhibit thyroid peroxidase → Propyl: Preggos Graves disease
myalgia, hepatic necrosis (P), Propylthiouracil ↓T4→T3 conversion
Thyroid Methimazole ↓TH synthesis Methim: longer duration Thyrotoxicosis
cholestatic jaundice (M)
Coadmin: β-blockers or Ca2+
Doesn't increase cancer risk or
Radioactive iodine Selectively destroys thyroid tissue channel blockers for Sx Hypothyroidism
fertility or effect offspring
Hyperthyroidism
Contraind: preggo

Traps thyroid iodide & blocks thyroid Coadmin: β-blockers & Ca2+ channel
Sodium Iodide hormone release blockers & thionamide
Thyrotoxic crisis

Binds PTH receptors → ↑Ca2+ bone Daily intermittent admin ↑osteoblasts Hypoparathyroidism
PTH mobilization & ↑renal Mg & Ca (↓PO4) & bone formation Not used to treat hypocalcemia Dx pseudohyperPTH
Teriparatide acetate
Calcium Homeostasis

reabsorption & ↑vit.D production (not bone resorption!) Osteoporosis

Binds VitD receptor + RXR → HypoPTH, pseudohypoPTH


Vitamin D ↑calbindins & ↑osteocalcin & Stored for prolonged periods in fat Hypervitaminosis D: hypercalcemia Rickets, osteomalacia
Calcitriol ↑osteoclast formation & ↑Ca2+ Osteoporosis
Binds calcitonin receptors → ↑cAMP Hypercalcemia
Nausea, facial flushing, hand Salmon CT is ↑potent and ↑t1/2
Calcitonin → ↓osteoclast-mediated Ca2+
swelling, urticaria, resistance 20% develop resistance
HyperPTH, ↑VitD, Bone mets
mobilization & ↑ excretion Osteoporosis, Paget's Dz
Etidronate Bisphosphonates (pyroPO4 analogs) Paget's Dz
Absorbed IV much better than PO Hypocalcemia, hypophosphatemia
Alendronate Bind OH-apatite → ↓osteoclasts
PO: take w/full glass of water Upper GI distress
Osteoporosis
Risedronate ↑bone mass Malignancy ↑Ca2+

Hydrocortisone
Short-acting
Cortisone
Bind glucocorticoid receptors →
Prednisone Short-acting
↑gluconeogenesis Addison's disease
Glucocorticoids

Prednisolone 4x anti-inflammatory ↑susceptibility to infx


↑glycogenesis
Inhibits growth in kids
↑hormone-sensitive lipase
Intermediate-acting Myopathy
↑blood glucose
Triamcinolone 5x anti-inflammatory Osteoporosis
↓cytokines
5x topical Cataracts
↑vasoCX
Adrenocortical atrophy
demarginalized PMNs Long-acting Dx of hypercortisolism
Iatrogenic Cushing's
Dexamethasone ↓vitamin D → ↓Ca2+ absorption & 30x anti-inflammatory Congenital adrenal
↑Ca2+ clearance & ↑bone resorption 10x topical hyperplasia

Betamethasone Inhaled Asthma


ACTH

ACTH analog w/complete biological Plasma cortisol measured 30-60 min Replaced therapeutically with steroid
Cosyntropin activity after IM/IV administration hormones
Dx of adrenal insufficiency

Hypernatremia, hypokalemia
Binds mineralocorticoid receptor → Primary adrenocortical
Fludrocortisone ↑Na+ reabs. & ↑K+ secretion
Metabolic alkalosis, hypervolemia
deficiency
Hypertension
Corticosteroid Antagonists

Metyrapone Blocks cortisol synthesis

Blocks conversion of cholesterol →


Aminoglutethimide pregnenalone
Cushing's syndrome

Inhibit P450 enzymes required for


Ketoconazole steroid synthesis

Spironolactone Competitive mineralocorticoid receptor


Primary hyperaldosteronism
Drospirenone antagonist
Drug Mechanism Metabolism Toxicity What makes it unique Treats

Schizonticide → terminates fever & Pruritus, nausea, anorexia, blurring


Resistance: mutant PfCRT trx PF malaria
Chloroquine parasitemia
(reversed by verapamil & desipramine)
Hemolysis in G6PD, Wide QRS
Hepatic amebic abscess
Buildup of free heme Agranulocytosis, oto/retinopathy
Metabolized by liver, excreted by kidney Cardiotoxicity, hematologic Does not eliminate liver forms
Quinine
Main Drugs

Unknown Coadmin: doxycycline Cinchonism, hypersensitivity (P. vivax & P. ovale) PF malaria
Quinidine Only used in chloroquin-resistant Blackwater fever, ↓glucose, uteroCX No P. falciparum gametocyte kill

GI
Schizonticide PF malaria
Mefloquine Used as prophylaxis
Long half-life (~20 days) Neuropsychiatric
(chloroquine resistant)
Cardiac & blood dyscrasias
GI, methemoglobinemia Only agent active against dormant
Absorbed GI
Primaquine Synthetic 8-aminiquinoline
Half-life: 3-8 hours
Hemolysis in G6PD hypnozoite liver form
Cardiac & blood dyscrasias (P. vivax & P. ovale)
Folate
Inhib.

Pyrimethamine Active against RBC forms Coadmin: sulfa drugs GI


Proguanil Inhibit DHF reductase → ↓folate (inh. DHP synthase = synergy) Pruritus

Tetracycline Doxycycline added to quinine trx


ABX

Action is too slow to be used as


Doxycycline monotherapy
Clindamycin instead of doxy for Malaria
Clindamycin preggos

Not to be used alone


Atovaquone Active against RBC forms Combined w/proguanil (malarone) GI
(Resistance & toxicity)
Miscellaneous

Halofantrine

Sesquiterpene lactone peroxide → PF malaria


Artemisin dihydroartemisin (drug-resistant)
Drug Mechanism Metabolism Toxicity What makes it unique Treats

GI
Admin: IV Adding pentamidine may increase Early hemolymphatic

Trypanosomiasis & Leishmaniasis


Suramin Does not cross BBB
Neurological
efficacy African trypanosomiasis
Cardiovascular, blood dyscrasias
Reactive encephalopathy
Admin: IV
Melarsoprol Trivalent arsenical compound
Does cross BBB
Renal & cardiac toxicity
Hypersensitivity CNS advanced
Mammalian OC enzyme very short African trypanosomiasis
Inhibits ornithine decarboxylase → blocks GI
Eflornithine conversion of ornithine → putrescine
Admin: IV
Blood dyscrasias
half-life…trypanosome OC enzyme
much more stable
Decreases severity of acute disease,
GI Acute American
Nifurtimox Nitrofuran structure Admin: oral
CNS
but many times fails to eradicate the
trypanosomiasis
parasite

GI
Admin: IM or IV Cutaneous & visceral
Stibogluconate Pentavalent antimonial
(daily)
Fever, arthralgias First line therapy
leishmaniasis
T wave changes, QT prolong

Nausea, headache, metallic taste Giardiasis


Causes multiple-strand breaks, disruption of
Metronidazole DNA replication & trx & inhibits DNA repair
Admin: oral GI, CNS, hematologic May potentiate oral anticoagulants Entamebiasis
Disulfiram-like reaction Trichomoniasis
Contraind: Optic neuropathy
GI
Iodoquinol Coadmin: metronidazole
Pruritis
Renal or thyroid disease
Effective against intraluminal E. hystolytica Iodine intolerance
Other Protozoa

(not tissue)
Little GI absorption
Paromomycin Renal excretion
GI Entamebiasis

Effective against tissue E. hystolytica Heart failure Use limited to severe amebiasis
Emetine trophozoites Hypotension when metronidazole unavailable

Admin: IM or IV Cardiovascular
Injectable (trypanosomatid) Trypanosomes
Pentamidine Effective against trypanosoma & P. carinii Half-life: ~6 hr Pancreatic, hepatic, renal, blood
Inhalation (pneumocystis) P. carinii
Accumulates in tissues (12 days) Bronchospasm, dyspnea
Giardiasis
Blocks pyruvate:ferredoxin oxidoreductase Useful in trx metro-resistant protozoa
Nitazoxanide pathway
Converted to active tizoxanide
& tapeworms
Cryptosporidiasis
(+ tapeworms)
Direct GABA agonist
Admin: oral
Piperazine Blocks ACh at NMJ to produce nematode
Excretion: w/in 24 hrs
GI Cure rate of ascariasis (>90%) Ascariasis
flacid paralysis

Ascariasis
Tetrahydropyrimidine derivative Admin: oral GI ACh release & AChE inhibition
Pyrantel pamoate NMJ blocking agent → paralyzes & expels Poorly absorbed from GI (good!) Insomnia Cure rates >90%
Pinworm
Anti-Helminths

Hookworm
Admin: oral Ascariasis
Hypersensitivity reactions
Mebendazole Inhibits microtubule synthesis Poorly absorbed from GI
Alopecia
Wide-spectrum Trichuriasis
(effect ↑w/fatty meal) Pin & Hookworm
Mild GI Admin fasting: luminal parasite Cysticercosis
Admin: oral
Albendazole Active albendazole sulfoxide
Metabolized in liver to active form
Long-term use (hydatid): Admin fatty meal: tissue parasite Hydatid disease
↑liver enzyme & blood dyscrasia Coadmin: corticosteroids (cyst) Round, Pin, Hook

Salicylamide derivative
Niclosamide Inhibits oxidative phosphorylation
Admin: oral Mild GI Tapeworm

Schistosomiasis
Isoquinoline-pyrazine derivative Admin: oral
Mild: headache, dizziness, GI, Hydatid disease
Praziquantel ↑cell membrane permeability to Ca2+ → [↑]: cimetidine or carbs Bitter taste (don't chew)
Anti-Trematodes

myalgia, pruritis, fever Neurocysticercosis


paralysis [↓]: steroids or antiepileptics
Trematodes & Cestodes

GI
Bithionol Admin: oral
Skin rash
Fascioliasis

Synthetic piperazine derivative Admin: oral


Mild: headache, dizziness, GI, fever, Give w/antihistaminics
Diethylcarbamazepine Immobilizes & alters microfilament surface Half-life: 2-3 hrs (acidic urine)
rash, blood dyscrasias (↓allergic reactions)
Filariasis
structure 10 hrs (alkaline urine)
Drug Mechanism Metabolism Toxicity What makes it unique Treats

Amphetamine derivative
Phentermine Inhibits NE reuptake Coadmin: fenfluramine Fenfluramine releases 5-HT &
Noradrenergic Targets

(Pulmonary HTN & valve problems) Drug mouth, insomnia, constipation, inhibits 5-HT reputake
Diethylproprion Interax: MAOI, guaneth, stim, EtOH, ↑BP, ↑HR, abuse Contraind: hyperthyroid, HTN, CVD,
sibutramine, TCA glaucoma, anxiety
Phendimetrazine Inhibit NE reuptake Obesity
Benzphetamine
Withdrawn in 2000 due to Only approved OTC appetite
Phenylpropanolamine NE target
hemorrhagic strokes in women suppressant

Obesity
Cardiac arrest, HTN, arrhythmia,
Ephedra Appetite suppressant & weight loss ↑weight loss w/: caffeine & aspirin
stroke, seizure, MI
Found in the herb Ma Huang Asthma
URI
Target

Interax: MAOI, SSRI, triptans, Lose 10-15% of weight


Mixed

Drug mouth, insomnia, constipation,


Sibutramine Inhibits NE, 5-HT, DA reuptake ergotamines, dextromethorphan, Contraind: HTN, renal/liver impair,
s

↑BP, ↑HR, abuse


opioids, lithium, tryptophan addx, CAD, CHF, arrhythmia, stroke
Obesity
Metab.

Lose 8-10% of weight


Inhibits GI lipases → ↓dietary fat Gas, oily stools, ↑defecation
Fat

Orlistat absorption
Interax: cyclosporine
↓absorption of ADEK & β-carotene
Improves H1Ac & sulfonylurea dose
Contraind: malabsorption, cholestitis
Drug Mechanism Metabolism Toxicity What makes it unique Treats

Able to stay as monomer, because


Lispro insulin proline & lysine AA's are swapped
Ultra-fast & short-acting

Short-acting
Zinc insulin crystals in a neutral,
Regular insulin unbuffered suspension
Admin: IV or subQ Hypoglycemia
(30-60 min before meal) (Counter-reg. often impaired)
Mild: juice/glucose
Insulin(-) complexed w/protamine(+) Severe: glucagon Insulin requirements ↑ during 2nd
NPH insulin & zinc
Insulin

~ half of pregnancy
Intermediate-acting Allergy ~ Type 1 diabetes
30% semilente insulin + 70% (insulin or protamine) If impaired renal fx: ↓insulin
Lente insulin ultralente insulin crystals in acetate ~ clearance
buffer Insulin resistance (IgG)
~
Excess zinc (produces large Lipohypertrophy
Ultralente insulin crystals) in acetate buffer
Long-acting

Peakless recombinant insulin that Ultra-long-acting


Glargine insulin precipitates in neutral subQ tissues Delayed onset of action

Amylin analog → ↓gastric emptying Admin: subQ w/mealtime insulin ↑Insulin-induced severe Type 1 diabetes
Pramlintide
Peptides

& ↑satiety & ↓post-pran glucagon Don't use w/acarbose hypoglycemia Contraind: hypersensitivity, Type 2 diabetes
gastroparesis, hypoglycemia
Glucagon-like peptide agonist → GLP-1 secreted in response to food unawareness
Exenatide ↓gastric emptying & ↓post-pran to potentiate glucose-stim insulin N/V, diarrhea Type 2 diabetes
glucagon & ↑insulin secretion release

First generation:
Tolbutamide Shortest acting
Least potent
First generation: May induce SIADH
Chlorpropamide Longest acting (60 hours) Severe hypoglycemia or alcohol flush reaction
Sulfonylureas

Intermediate potency (chlorpropamide & glyburide) Recurring hypoglycemia


Weight gain
Bind SUR receptors associated w/
Skin reactions & erythema Extended release form does not
Glipizide ATP-sensitive K+ channels → Second generation: Type 2 diabetes
Blood dyscrasias induce weight gain!
↓K+ current → ↑insulin secretion
Hepatic dysfunction
(All are liver metabolized)
GI disturbances Does not cross placenta
Glyburide Once daily dosing
(can use for gestational diabetes)

Binds a site on K+ channel different


Highest potency
Glimepiride Once daily dosing
from all other sulfonylureas
↑muscle insulin sensitivity
Meglitinides

Metabolized by liver
Repaglinide Bind SUR receptors associated w/ Half-life: 1 hour
ATP-sensitive K+ channels (diff. site Hypoglycemia
Used for post-pran hyperglycemia Type 2 diabetes
from sulfonylureas) → ↓K+ current Weight gain
→ ↑insulin secretion Metabolized by liver
Nateglinide Half-life: even shorter & rapider

↓ gluconeogenesis
Biguanides

Phenformin ↑insulin-stimulated GLUT4 Not significantly metabolized Do not cause hypoglycemia


Lactic acidosis
trafficking to membrane 90% oral dose gone in 24 hours (even at high doses) Type 2 diabetes
(Even less with 2nd generation)
↑cAMP-act. protein kinase Half-life: 2 hours ↓TAG, ↓cholesterol, ↓LDL, ↑HDL (obese)
Cardiovascular disorders
(Increase tissue sensitivity to Low potency Weight loss & ↓BP
Metformin
insulin)

Metabolized to inactive metabolites


Rosiglitazone Bind PPAR-γ receptor + RXR → Half-life: 3-4 hours
Troglitazone: hepatotoxicity Do not cause hypoglycemia
TZDs

↑GLUT1 & GLUT4 ↑albumin bound


Heart failure Current TZD's do not cause Type 2 diabetes
↑lipoprotein lipase, FABPaP2 Metabolized to weak metabolites Angina, MI hepatotoxicity
↓TNFα, ↓leptin
Pioglitazone Half-life: 3-7 hours
↑albumin bound
Pptdase glcsdase

Competitive α-glucosidase inhibitors


Acarbose
inhib.

Low systemic bioavailability Flatulence, nausea, diarrhea Do not cause hypoglycemia, lactic
→ ↓carbohydrate digestion/absorb Type 2 diabetes
α

Miglitol Taken with a meal Contraind: IBS, obstruction, ulcer acidosis, or weight gain
Blunted post-prandial glucose
4 inhib
Dipep

Blocks dipeptidyl peptidase IV → With: diet & exercise


Sitagliptin ↓GLP-1 & GIP → ↑post-pran insulin With: metformin or TZD
Type 2 diabetes
Hyperglycemic

↑ open time of ATP-sensitive K+ Metabolized in liver Nausea/vomiting Does not inhibit the synthesis of
Diazoxide channel → ↓insulin release Half-life: 48 hours Fluid & salt retention insulin, only the release
Insulinoma
s

Binds glucagon receptor → ↑cAMP Admin: subQ, IM, IV Inotropic & chronotropic Severe hypoglycemia
Glucagon → ↑(P) glycogen phosphorylase & Half-life: 3-6 minutes Nausea & vomiting RX of GI smooth muscle Shock & GI RX
synthase Metabolism: 25% first-pass Release catecholamines & CT Dx pheochr-cytoma
Drug Mechanism Metabolism Toxicity What makes it unique Treats

Vitamin B3 → ↓hepatic TAG Half-life: 1 hour Flushing, pruritis HyperTAG


Most effective agent to ↑HDL
Niacin synthesis & ↑lipoprotein lipase → Used w/: bile acid binding resin Nausea, diarrhea, peptic ulcer
Only agnet to ↓Lp(a)
Familial hyperTAG
↓apoB → ↓VLDL → ↓LDL
Triglycerides

Used w/: HMG CoA reductase inh. Hepatotoxic, glucose intol., gout FC hyperTAG
Gemfibrozil Bind PPAR-α+ RXR → ↓apoC-III & GI disturbances HyperTAG
Half-life: 1.5 hours
Fenofibrate apoB & ↑lipoprotein lipase → ↓VLDL
Highly albumin bound
Rash, myopathy, arrhythmia Dysbetalipoproteinemia
Clofibrate → ↓LDL & ↑apoA Fatigue FC hyperTAG
(+) charged resins that bind bile
Cholestipol HyperTAG Negligible systemic bioavailability Familial HyperTAG
acids → ↓reabsorption of bile acids Taken with meals PO
Cholestyramine GI (constipation) Approved for use in children FC hyperTAG
→ ↓cholesterol & ↑LDL receptors
Inhibit HMG CoA reductase (HMG First pass metabolism Myopathy (↑CK)
↑BMP-2 → ↑osteoblasts → Hypercholesterolemia
Statins CoA → mevalonate) → ↓cholesterol Cytochrome P450 metabolized Renal dysfx (myoglobinuria)
↓fracture risk (& familial)
& ↑LDL receptors Extensively protein bound Rhabdomyolysis (w/gemfribrozil)
↓cholesterol transport at brush Enterohepatic recycling
Cholesterol lowering effect limited
Ezetimibe border in small intestine lumen → Half-life: 22 hours
by ↑liver cholesterol synthesis
Hypercholesterolemia
↓cholesterol & ↓LDL-C & ↑HDL Low systemic bioavailability
↓lipid oxidation Progestins have undesirable effects
Estrogen
Cholesterol

↑TAG, ↑HDL on plasma lipids


replacement ↓LDL, ↓cholesterol (CAD & stroke)

Plant stanol
↓absorption of dietary cholesterol
esters

Omega-3 fatty ↓endothelial inflammation Monosaturated fatty acids (oleic):


acids ↓LDL & ↓TAG ↓LDL but not HDL

Ethanol ↑HDL & ↓LDL No association with beverage types


Drug Mechanism Metabolism Toxicity What makes it unique Treats

Ointment
Gram (+) bacteria
Bacitracin Used w/neomycin or polymyxin Allergic contact dermatitis
Anaerobes (cocci)
Absorbed through skin

Bacterial Infections
PEG vehicle can irritate nasal Impetigo
Mupirocin Effective against most gram (+) Intranasal preparation
mucosa (S. aureus & S. pyogenes)

P. aeruginosa
Polymyxin B E. coli, enterobacter
Klebsiella
Effective against most gram (-) Topical
Sensitization
Neomycin
Cross-sensitivity to streptomycin,
Gentamycin kanamycin, gentamycin

10% of topical application is Bloody diarrhea


Clindamycin absorbed Pseudomembranous colitis
Acne vulgaris
Acne Vulgaris

Effective against Burning


Erythromycin Propionibacterium acnes Irritation

Topical Acne vulgaris


Sulfacetamine Alone or with sulfur preparation
Contraind: sulfa allergy
Acne rosacea

Effective against Dermodex brevis Possible carcinogen


Metronidazole Anti-inflammatory Contraind: pregnancy & lactation
Acne rosacea

Effective against dermatophyte Cream, shampoo, lotion, vagial Seborrheic dermatitis


Azoles infection tablets, suppositories Candidiasis

Dermatophytes
Use in onychomycosis only effective
Topical Antifungals

Ciclopiroxolamine in ~10% of patients


Candida
P. obiculare

Naftifine Allylamines
Dermatophytes
Terbinafine Inhibit ergosterol synthesis

Cessation of therapy generally


Tolfnaftate Well tolerated
followed by infection recurrence

Amphotericin B
Well tolerated Superficial candidiasis
Nystatin
Diarrhea
Effective against growing cells
Antifungals

Griseofulvin Inhibits fungal cell wall synthesis


Fine microcystal suspension Photosensitivity Contraind: porphyria, liver dysfx Tinea infections
Headaches
Oral

Gynecomastia
Interax: benzos → ↑sedation Chronic gen. MC candidiasis
Ketoconazole statins → rhabdomyolysis
Hepatitis
Dermatophytes
Ventricular dysfx

Primary cutaneous HSV


Acyclovir Decreases viral shedding Ointment
Antivirals
Topical

Limited MC HSV

Decreases viral shedding (time) & Cream


Pencyclovir ↓time to healing Applied at first sign of infection
Recurrent orolabial HSV

Shampoo or lotion Pediculosis capitis


Antiparasites

Hematotoxicity
Lindane ~Absorbed via skin, ↑in fatty tissue,
Neurotoxicity
Pediculosis pubis
excreted in urine in 5 days Scabies

Skin staining Lack of systemic effects


Sulfur Unpleasant odor (good for kids and preggos)
Scabies
Pigmentation

Hydroquinone Inhibit tyrosinase → ↓melanin → Hydroquinone = temporary Local irritation


Monobenzone ↓skin hyperpigmentation Monobenzone = permanent Allergy
Skin

Produce repigmentation of
Trioxsalen Skin cancer
depigmented macules Vitiligo
Methoxsalen Cataracts
Psoralens intercalate w/DNA
Tretinoin (ATRA) Erythema May appear worse in the first month,
Admin: topical Acne vulgaris (comedones)
Retinoic acid ↓epidermis cohesion
Applied to dry skin only
Dryness as quiescent comedones emerge &
Light-damaged skin
↑cell turnover Sunlight sensitivity rupture

Similar to retinoic acid but less


Adapalene Naphtoic acid analog
irritation
Mild to moderate acne
Acne

Similar to hypervitaminosis A:
Synthetic retinoid-like drug
Isotretinoin Decreases sebaceous gland function
Admin: oral dryness, itching, IBS Severe cystic acne
IBS, muscle pain, teratogen

Converted to benzoic acid


Benzoyl peroxide Effective against P. acnes
Admin: topical Skin irritation Acne vulgaris

Acitretin Admin: oral


Psoriasis

Anti-inflammatory
Tazarotene Extreme caution in young women Psoriasis
Antiproliferative

Skin dryness
Calcipotriene Synthetic vitamin D3
Itching

Skin atrophy, rosacea


inflammatory

Anti-inflammatory Keloids, cystic acne, alopecia areata


Corticosteroids Antimitotic
↑IO pressure
= triamcinolone injection
Anti-

Cushing's syndrome, growth

Byproducts of petrol distillation Irritant folliculitis Psoriasis


Tar compounds Antipruritic Allergic contact dermatitis Chronic lichenified dermatitis

Anaphylactic shock
Salicylic acid Solubilize cell surface protein debris Irritation & inflammation
Salicylism
Keratolytics

Used for elimination of keratolytic


Propylene glycol debris
Alone or with: salicylic acid Allergic contact dermatitis

Xerosis
↑prekeratin & keratin solubility →
Urea ↑elimination
Hyperkeratosis
(palms & soles)
Pruritis

Potent histamine receptor (H1 & H2) SE's & contraindications similar to Atopic dermatitis
Doxepin antagonist
Admin: oral or topical Allergic contact dermatitis
anticholinergics Lichen simplex chronicus

Reverses progressive ↓ of terminal Discontinuation causes continued hair


Tricogenics

Minoxidil scalp hairs


Admin: topical
loss in 4-6 months
Androgenic alopecia
↓libido
Blocks 5α-reductase → inhibits Pregnant women should not be
Finasteride conversion of testosterone → DHT
Admin: oral Ejaculation disorders
exposed (hypospadias)
Eretctile dysfunction
Drug Mechanism Metabolism Toxicity What makes it unique Treats

Binds microtubule tubulin → Admin: oral GI Gouty arthritis attacks


Colchicine ↓polymerization → ↓WBC migration Accumulates in WBCs Blood dyscrasias Pseudogout
Misc.

& urate phagocytosis Deacetylated in liver CNS depression, shock Familial Med. fever

Not to be used in chronic gout or


Indomethacin Anti-inflammatory
prophylaxis
Acute gouty attacks

Admin: oral GI
Inhibits proximal tubule reabsorption
Uricosuric

Probenecid Half-life: 6-12 hours Dermatitis Not to be used in acute gout attacks
Agents

of urate
Interax: PCN, ASA, sulfa, allopurinol Nephrotic syndrome
Hyperuricemia control
Inhibits proximal tubule reabsorption
Potentiates insulin & oral
Sulfinpyrazone of urate Very highly plasma protein bound
hypoglycemics
No anti-inflammatory or analgesia
Comp. inhibits xanthine oxidase Metabolized to oxipurinol (active) Maculopapular rash (pruritus)
Inhib.
Urate

Not useful for acute gout attacks


Allopurinol ↓conversion of hypoxanthine → Depletes purine precursors GI, hepatotoxicity
Inhibits kidney reperfusion injury
Chronic tophaceus gout
xanthine → uric acid (5'-PRPP) Fever, hypersensitivity
Drug Mechanism Metabolism Toxicity What makes it unique Treats

Albuterol Albuterol is the most used


Admin: Metered dose inhaler Anxiety, tremor, restlessness, ↑HR,
Terbutaline Nebulizers hypokalemia
Metered dose inhaler is most Acute asthma attack
Metaproterenol β2-agonists → Gs → ↑cAMP → common
bronchoRX Long-acting Salmeterol is not useful in acute Severe refract asthma
Salmeterol
Salmeterol = slow-acting asthma attacks! COPD
Formoterol Formoterol = fast-acting (Slow onset of action) Chronic bronchitis
Antagonist at adenosine A1 receptor Headache, CNS stimulation
Admin: IV
Theophylline → ↓Gi → ↑cAMP & ↓PLC →
Low therapeutic index
N/V, epigastric pain Nocturnal asthma
bronchoRX Arrhythmias, seizures

Ipratropium mACh receptor antagonist → ↓Gi → Chronic bronchitis


Admin: dry powder inhalation
Tiotropium ↑cAMP & ↓PLC → bronchoRX Limited in asthma

Cromolyn No role in acute asthma!


Admin: metered dose inhaler
Prevents mast cell degranulation Asthma
Spinhaler Virtually no side effects
(asthma prophylaxis) Greater potency than cromolyn (maintenance)
4x day regimen
Nedocromil Additive therapeutic effects with
corticosteroids

Prednisone
Admin: oral
Methylprednisone Systemic corticosteroid effects
Inhibit late-phase reactions of Hoarseness
inflammation Oropharyngeal candidiasis
Methylprednisone
Decrease bronchial reactivity Admin: IV Coughing, wheezing Acute asthma
Hydrocortisone Most potent anti-asthma agents HPA axis suppression
available Long-term therapy (>3weeks) only if
Beclomethasone
refractory to other trx Reformulated as HFA inhaler
Flunisolide Admin: inhalation
systems (+MDI)
Triamcinolone
Troleandomycin
TAO = macrolide antibiotic → inhibit
Gold salts corticosteroid metabolism
Steroid-sparing therapy
Methotrexate
Weak anti-inflammatory & Best if added to ICS therapy Asthma
Montelukast bronchodilator actions (allows lower doses) (maintenance)

Allowed lower doses of ICS &


Omalizumab Monoclonal anti-IgE antibody
↓hospitalizations & ER visits

Mucolytic that improves


Tumorigenicity forced removal from
Iodinated glycerol expectoration, cough, chest
the market
Chronic bronchitis
discomfort, duration of attack