Drug
Diuretics
Acetazolamide
Hydrochlorothiazide
Chlorhalidone
Indapamide
Metolazone
Furosemide (Lasix)
Amiloride
Triamterene
Spironolactone
Class
Uses
Carbonic anhydrase
inhibitor
(derivative of Sulfonamides)
Thiazide
Thiazide-like long acting
IOP (formation of aqueous
humor); epilepsy;
motion sickness
Edema, HTN (TPR)
Edema, HTN (TPR)
Loop (rapid-acting)
Renal failure, ascites,
nephrotic syndrome,
pulmonary edema, CHF,
HTN, hypercalcemia
Modest diuretic prevents Na+
reabsorption
K+-sparing
(renal epithelial Na+-channel
inhibitors)
K+-sparing
(aldosterone antagonist)
Combo Rx for HTN, prevent
cardiac hypertrophy
(aldosterone-mediated)
Side effects
Metabolic acidosis, sedation,
parasthesia, bone marrow
suppression, allergic rxn
Same as below
Hypokalemia, glucose
tolerance, LDL & TGs,
impotence, arrhythmias
Hypotension, hypokalemia,
ototoxicity, hyperuricemia,
LDL & HDL hyperglycemia,
arrhythmias
Hyperkalemia
CI—DM, renal failure,
concurrent ACE-inhibitors
Anti-androgen (libido,
gynecomastia, impotence)
menstrual irregularities,
female hair growth
NO androgen & progesterone
side effects
Eplerenone
K+-sparing
(aldosterone antagonist)
HTN & CHF
Glycerine
Isosorbide
Mannitol
Urea
Osmotic
Acute renal failure (maintain
renal BF), glaucoma (IOP),
cerebral edema
Total electrolyte imbalance,
exacerbate CHF & pulmonary
edema (ECV)
ACE-inhibitors
CHF & HTN (TPR w/o HR)
AT1-receptor blocker
Arterial-selective vasodilator
(cGMP)
1st-line CHF; HTN
TPR (CO) for LV failure
Nitroprusside
Balanced vasodilator
(arterial & venous)
HTN emergencies
Nesiritide
Balanced vasodilator
B-type natriuretic peptide
Non-selective -agonist
Selective 1-agonist
PDE-inhibitors
Decompensated CHF
(rapid TPR)
Decompensated CHF
Persistent cough,
angioedema, renal fxn
Few side effects
Lupus-like syndrome,
headache, reflex tachycardia,
Na+/H2O retention
Hypotension, cyanide
poisoning (metabolized to
cyanide & thiocyanate)
Hypotension
Carvediol
Metoprolol
Non-selective -blocker
Selective 1-blocker
Digoxin
Digitoxin
Cardiac glycosides
(inhibit Na+/K+ ATPase)
CHF (LV fxn & reverses
hypertrophy); DOC
prophylaxis stable angina
(+)inotropism & antiarrhythmic
Anti-ischemics
Metoprolol
Selective 1-blocker
Nitroglycerine
Organic nitrates
Isosorbide dinitrate
Verapamil
Ca2+-channel blocker
DOC for stable angina
prophylaxis
DOC for stable & variant
angina
Prophylaxis
Angina, HTN, arrhythmias
Diltiazem
Amlodipine
Nifedipine
Ca2+-channel blocker
Ca2+-channel blocker
Dihydropyridines
NOT unstable angina
NOT unstable angina OR
arrhythmias
CHF
Captopril
Enalapril
Losartan
Hydralazine
Dopamine
Dobutamine
Milrinone
Inamrinone
Short-term for refractory CHF
(NOT cardiac Ca2+-channels)
Anti-arrhythmics
Procainamide
Quinidine
Lidocaine
Phenytoin
Flecainide
Features
Crosses BBB
NOT used as diuretic!
Reversible ototoxicity
(Ethacrynic acid)
Prodrug metabolized to
Canrenone
Analog of Spironolactone
Blocks aldosteroneinduced gene expression
Prodrug
Directly block AII activity
Combine w/ -blocker &
diuretic
Light sensitive (short t1/2)
Reconstituted & infused
NO tolerance
Arrhythmias
IV dose (short t1/2)
Arrhythmias, GI upset,
thrombocytopenia
(Milrinone less toxic)
“Withdrawal” syndrome
(rebound tachycardia)
NOT reduce morbidity &
mortality of CHF!
GI upset, visual disturbances,
arrhythmias
Carvediol racemic mixture
antioxidant &
antiproliferative
t1/2=42h, renal metabolism
t1/2=5d, hepatic metabolism
“Withdrawal” syndrome
(rebound tachycardia)
Headaches, hypotension,
reflex tachycardia
(-)inotropism &
(-)chronotropism
Bradycardia, AV nodal block,
hypotension
Better tolerated
Hypotension w/ reflex
tachycardia (mortality),
edema, headache, gingival
hyperplasia
Strongest cardiac effects
Torsade de pointes
CI for structural heart dz &
Class IA
Blocks Na+ & K+-channels
Ventricular tachycardia
Class IB
Weakest Na+-channel
blocker
Class IC
Post-MI ventricular
tachycardia; NOT prophylaxis
Widened QRS complex,
Lupus-like syndrome, bone
marrow depression,
proarrhythmic
Agitation (CNS effects),
proarrhythmic
Prophylaxis of atrial fibrillation
Very proarrhythmic
Spray (short onset & duration)
Patch (slow onset, long duration)
Tablets go bad after 6m
Intermediate effects
Strongest vasodilation
Fast-release capsules
Propranolol
Amiodarone
Sotalol
Verapamil
Adenosine
HTN
Prazosin
Hydralazine
Minoxidil
Nitroprusside
Hyperlipidemia
Simvastatin (Zocor)
Atorvastatin (Lipitor)
Cholestyramine
Colesevelam (WelChol)
Strongest Na+-channel
blocker
Class II
-blocker
Class III
K+-channel blocker
Class III
-blocker & K+-channel
blocker
Class IV
Ca2+-channel blocker
G-protein receptor agonist
(-)inotropism
DOC for rate control of atrial
fibrillation
Most arrhythmias (especially
structural heart dz)
mortality following MI
Warfarin & Digoxin levels
Prophylaxis of atrial fibrillation
(especially ischemic heart dz)
Pulmonary toxicity,
hypothyroidism OR
thyrotoxicosis
Torsade de pointes,
bronchoconstriction
DOC for rate control of atrial
fibrillation
Paroxysmal supraventricular
tachycardia, AV nodal reentry
tachycardia
Flushing, cardiac arrest
(SA/AV nodal block),
bronchoconstriction
A1 (negative inotropism)
A2 (vasodilation)
A3 (histamine release)
ONLY for severe
arrhythmias OR low risk of
proarrhythmias
Diuretics, ACEIs (1st-line), AT1-blockers (1st-line), -blockers (1st-line), Ca2+-channel blockers, 2-agonists
HTN w/ benign prostatic
Fluid retention, 1st-dose
Selective 1-blocker
syncope, orthostatic
hyperplasia (HDL & LDL)
hypotension
Arterial-selective vasodilator
Severe HTN
Lupus-like syndrome,
Combo w/ -blockers &
headache, Na+/H2O retention, diuretics
reflex tachycardia
Direct vasodilator
Severe HTN
Hair growth (Rogaine)
Stimulates K+ channels to
hyperpolarize SM
Balanced vasdodilator
HTN emergency (quickest
IV infusion VS. Diazoxide
Thiocyanate toxicity, ICP
(arterial & venous)
onset & shortest duration)
(IV bolus)
Combo therapy (Statin + Resin + Niacin) can LDL >70%
HMG-CoA reductase
1st-line LDL, HDL, TGs
inhibitor
Upregulate liver LDL
(reversible, competitive)
receptors
BA sequestrants
Moderate LDL (younger
(anion exchange resins)
persons & pregnancy),
slight HDL, NO effect TGs
Niacin
Selective cholesterol
absorption inhibitor
Nicotinic acid
LDL, HDL, TGs
(additive effect w/ Statin)
Atherogenic dyslipidemia,
Modest LDL, HDL,
Marked TGs
Gemfibrozil (Lopid)
Fibrates
Modest LDL, HDL
Marked TGs
Ezetimibe (Zetia)
depressed LV fxn
Minimal
CI—liver dz, pregnancy &
nursing
GI upset, reduced drug
absorption
CI—TGs >400mg/dL
familial dysbetalipoproteinemia
CI—liver dz, pregnancy &
nursing
Flushing, hyperglycemia,
gout, GI upset (combine w/
ASA/NSAID or titer up)
CI—liver dz, PUD, gout, DM
Dyspepsia, GI upset,
gallstones, myopathy
Lovastatin & Pravastatin
prodrugs
Extensive 1st-pass p450
Combo w/ Statins for very
high LDL
NOT absorbed b/c so large
NOT effect fat-soluble
vitamins
Niaspan (extendedrelease)
Mono OR combo therapy
Mono OR combo therapy
risk for acute pancreatitis
CI—liver OR renal insufficiency
Anti-thromboembolics
Aspirin
Irreversible COX-1 & 2
inhibitor
MI, unstable angina, TIA,
stroke
Dipyridamole
Platelet phosphodiesterase
inhibitor (cAMP)
Thienopyridines
Irreversible platelet ADP
receptor inhibitors
Stroke prevention
Abciximab (antibody)
Eptifibatide (peptide)
Glycoprotein IIb/IIIa receptor
inhibitors
Heparin
Unfractionated
anticoagulant
Enoxaparin (Lovenox)
Fractionated (LMWH)
anticoagulant
Acute coronary syndromes,
prevent restenosis following
intervention
DVT, PE, MI, arrhythmias,
CABG or valve replacement,
stroke prevention
Same as above
Fondaparinux
Factor Xa selective inhibitor
(Pentasaccharides)
Direct thrombin inhibitor
(blocks thrombin binding
sites on Factors)
(blocks thrombin receptors
on platelets)
Oral anticoagulants
(vit.K-dependent
carboxylation inhibitor)
Clopidogrel (Plavix)
Ticlopidine
Bivalirudin
Argatroban
Aprotinin
Warfarin (Coumadin)
Stroke prevention (patients
intolerant to ASA)
CI—ulcer, hypersensitivity,
thrombocytopenia, bleeding
disorder, <16yo, concurrent
anticoagulants
GI upset, hypersensitivity
CI—asthma, bleeding
Bone marrow suppression
(Ticlopidine), bleeding, GI
upset
CI—bleeding, liver dz, kids
Bleeding, hypotension,
hypersensitivity
CI—thrombocytopenia
Thrombocytopenia, rash,
osteoporosis
Lower risk thrombocytopenia
Prevention of DVT following
hip/knee surgery
Prevents Heparin-induced
thrombocytopenia (HIT),
prevent bleeding after
intervention
Anemia, GI upset, injection
rxn
Bleeding, hypersensitivity w/
repeated exposure
Long-term (delayed onset)
therapy
Hemorrhage, necrosis (early
thrombosis w/ rapid protein C
loss), GI upset, teratogenic,
7-10d duration
Adjuvant w/ ASA
(Aggrenox)
Expensive
Inhibit platelet aggregation
(fibrinogen binding)
IV dosing
Rapid & short duration
RES elimination
Requires aPTT monitoring
Easier SC dosing, NO
monitoring, longer t1/2
Renal elimination
Synthetic (less variable
prep)
Requires monitoring PT
time (INR)
drug interactions
CI—liver dz
Alteplase
Anistreplase
-Aminocaproic acid
(EACA)
Recombinant tPA
(activates plasmin on fibrin)
Streptokinase-plasminogen
complex
(NOT specific to fibrin)
Competitive inhibitor of
plasminogen & PAs
DOC for acute MI
DVT & PE
Acute MI
Serine protease inhibitor of
plasmin & SK-plasminogen
Antidote for excessive
fibrinolytic therapy &
hemophilia
Antidote for excessive
fibrinolytic therapy & postop
Oral Fe (most common)
Fe-deficiency
Fe-deficiency
Fe-hydroxide dextran
Ferrous gluconate,
fumarate, lactate, cholinate
Parenteral Fe
Deferoxamine
Fe chelator
Cyanocobalamin
Hydroxycobalamin
Stable vit.B12
Leucovorin
Folic acid
Epoetin-
(Epogen or Procrit)
Recombinant erythropoietin
Aprotinin
Anemia
Ferrous sulfate
Organic Fe salts
Antihistamines
Diphenhydramine
(Benadryl)
Fe-deficiency (patients
cannot tolerate OR absorb
oral Fe)
Acute & chronic Fe overload
Dietary deficiency (rare),
achlorohydria, Crohn’s dz,
pernicious anemia
Dietary deficiency,
malabsorption, alcoholism,
drug-induced (esp. due to
antifolates)
Renal failure, chemo, HIV,
frequent blood donations
1st-generation H1-blocker
(oral or topical)
Nasal allergies, allergic
dermatoses, direct
suppression of cough center,
insomnia (OTC sleep aids)
Nasal allergies, dermatoses
Fexofenadine
(Allegra)
2nd-generation H1-blocker
(oral)
2nd-generation H1-blocker
(oral)
2nd-generation H1-blocker
(oral)
Promethazine
(Phenergan)
H1-blocker (less selective
than 2nd-generation)
Motion sickness, vomiting
Proton pump inhibitors
(selective, irreversible H+/K+
ATPase inhibitors in gastric
parietal cells)
Selective H2-blockers
(competitive, reversible)
GERD, combo therapy for
H.pylori ulcers
Cetirizine (Zyrtec)
Loratadine (Claritin)
GI
Omeprazole (Prilosec)
Pantoprazole
(Protonix)
Cimetidine (Tagamet)
Ranitidine (Zantac)
Magnesium hydroxide
(Milk of magnesia)
Aluminum hydroxide
Bismuth
(Pepto Bismol)
Sucralfate (Carafate)
Misoprostol (PG)
Metoclopramide
Cisapride
Tetracyclines
Ondansetron (Zofran)
OTC antacids
Nasal allergies, dermatoses
Nasal allergies, dermatoses
Duodenal ulcer healing,
prevent nocturnal acid
breakthrough (some PPIs)
Acid neutralization
IV dosing w/in 4-6h
Derived from Strep
Cheap
GI upset, heartburn,
constipation
Fewer SE
Anaphylaxis
Allergic rxn, hypotension,
ocular defects (histamine
release)
Cheap
More expensive
Complex dosing forms
IM or IV (rapid buildup of
Fe stores)
IM or slow IV (prevent SE)
Oral (IM for pernicious
anemia)
Rare
Oral or IV
Recovery w/in 10d
HTN, seizure, headache, GI
upset, edema, fatigue
MUST maintain Fe levels
w/ long-term therapy
Sedation (crosses BBB),
antimuscarinic (dry mouth,
tachycardia, blurred vision,
constipation), ED, appetite
loss
CI—nursing, babies
Dose-dependent sedation
(liver dz)
Non-sedative (NOT cross
BBB), NO tachycardia
Minimal sedation,
antimuscarinic, NO QT
prolongation
BP effects (central anti-ACh),
rash, sedative
Most effective prior to
histamine release
4-6h duration
Hypochlorhydria w/ gastric
bacterial overgrowth,
hypergastrinemia, gastric
cancer (long-term)
Mental confusion, renal
disturbances, inhibits p450
(Cimetidine)
GI upset, renal problems,
altered drug absorption
Protonix acid stable
Omeprazole inhibits drug
metabolism
12-24h duration
>24h duration
1-12h duration
Combo w/ cold meds
Quick onset, 2-8h duration
Structure similar to
histamine
basal acid secretion
Diazepam absorption  w/
AlOH &  w/ MgOH
(Amphojel)
Mucosal protection & healing
AlOH & sulfated sucrose
complex
Inhibits acid production
(binds parietal cell receptor
& cAMP)
Serotonin receptor agonists
Mucosal protection, promotes
PG synthesis
mucosal thickness,
mucosal BF, HCO3secretion
GERD (rarely used)
Antibiotics
5-HT3-receptor blockers
NOT neutralize acid
Constipation, altered drug
absorption
Diarrhea, uterine stimulant
CI—pregnancy
Forms viscous suspension
that binds mucosa
H.pylori-associated PUD
Parkinson’s-like Sx
(Metoclopramide)
Disruption of GI flora
N&V (esp. w/ chemo)
Constipation, diarrhea,
Cisapride removed from
market for arrhythmias
Triple-component regimen
(TCN, PPI, Bismuth,
Metronidazole) for 14d
Extensive p450
Granisetron (Kytril)
Metoclopramide
(Reglan)
Prochlorperazine
(Compazine)
Sulfasalizine
(Azulfidine)
Prednisone
Budenoside
6-Mercaptopurine
Infliximab (Remicade)
Entanercept (Enbrel)
Mineral oil
Docusates
Phenolphthalein
Bisacodyl
Loperamide
(Imodium)
Diphenoxylate
headache, light-headedness
Extrapyramidal effects,
restlessness, sedation,
fatigue, nausea, diarrhea
Masks gag reflex,
tranquilizer, jaundice
Fever, malaise, N&V,
headaches, epigastric
discomfort, diarrhea, allergic
rxns
metabolism
Promote gastric emptying
(peripheral) & suppress
vomiting (central)
Bone marrow loss,
opportunistic infection,
teratogenic
SLE & lymphoma (long-term)
May take 3-6m to work
D2-receptor blocker, 5-HT3receptor blocker, &
5-HT4 agonist
D2-receptor blocker (in CTZ)
N&V (esp. w/ chemo)
5-aminosalicylates
(inhibits arachidonic acid
metabolism, scavenges
ROS, immune effects)
Glucocorticoids
(outside US)
Immunosuppressive
(inhibits lymphocyte
proliferation)
Chimeric Ig
(binds & neutralizes TNF-)
Fusion protein of TNF-R &
IgG1 Fc portion
Stool softeners (lower ST)
Mild UC & IBS
Diphenylmethane derivative
Constipation
Removed from market over
concerns w/ long-term use
Diphenylmethane derivative
(stimulates mucosal nerve
plexus of colon)
Opioid
(improves anal sphincter
tone)
Opioid
(metabolized to Difenoxin)
Constipation & pre-op colonic
cleanse
Severe intestinal cramps,
damaged colonic tone (longterm)
CNS effects (overdose, esp.
in kids)
N&V
90% remission UC &
60-90% Crohn’s dz
Severe UC & maintain UC
remission
Crohn’s dz
Prodrug metabolized to
Sulfapyridine (causes SE)
& 5-ASA mesalamine
(active portion) in colon
Crohn’s dz
Neutralizes TNF-
Constipation
Little efficacy
Diarrhea
(activity against cholera &
some E.coli toxins)
Diarrhea
CNS effects
Induce low-grade
inflammation, fluid
accumulation, & motility
Stomach (>6h onset)
Rectal (30-60min)
Binds peripheral -opioid
receptors & relaxes
intestinal contractions
Marketed w/ Atropine
(Lomotil or Motofen) to
discourage abuse