Drug Name
Drug Class
Mechanism
Special side effects
Use
esomeprazole
- Proton Pump Inhibitors
- Irreversible H/K ATPase inhibit
- rebound hypergastrinemia, CYP enz->increase in warfarin levels & decreased clopidogrel levels,
- All stomach acid things (GERD, gastric/duodenal ulcer, Zollinger-Ellison, erosive esophagitis, H. Pylori treatment, NSAID ulcers)
lansoprazole
- Proton Pump Inhibitors
- Irreversible H/K ATPase inhibit
- rebound hypergastrinemia, CYP enz->increase in warfarin levels & decreased clopidogrel levels,
- All stomach acid things (GERD, gastric/duodenal ulcer, Zollinger-Ellison, erosive esophagitis, H. Pylori treatment, NSAID ulcers)
omeprazole
- Proton Pump Inhibitors
- Irreversible H/K ATPase inhibit
- rebound hypergastrinemia, CYP enz->increase in warfarin levels & decreased clopidogrel levels,
- All stomach acid things (GERD, gastric/duodenal ulcer, Zollinger-Ellison, erosive esophagitis, H. Pylori treatment, NSAID ulcers)
cimetidine
- H2 receptor antagonists
- H2 block (from ECL cell)
- long-term: down testosterone & estradiol (gynecomastia, impotence, galactorrhea), rarely CNS effects parenterally, tolerance in 3 days, rebound
- Zollinger-Ellison, decrease nocturnal acid secretion (requires 4 wks)
famotidine
- H2 receptor antagonists
- H2 block (from ECL cell)
- rarely CNS effects parenterally, tolerance in 3 days, rebound
- Zollinger-Ellison, decrease nocturnal acid secretion (requires 4 wks)
ranitidine
- H2 receptor antagonists
- H2 block (from ECL cell)
- rarely CNS effects parenterally, tolerance in 3 days, rebound
- Zollinger-Ellison, decrease nocturnal acid secretion (requires 4 wks)
sucralfate
- Misc. (coating)
- sticky neutral pH coating
- block absorption of other drugs (but requires acid activation)
- stress ulcers (sticks to duodenum better)
aluminum hydroxide
-delays gastric emptying, slows motility, rebound
-slow-acting acid neut.
calcium carbonate
-rebound
-acid neut.
magnesium hydroxide
-stim gastric emptying, rebound
-fast-acting acid neut.
magnesium trisilicate
-stim gastric emptying, renal stones, rebound
-fast-acting acid neut.
misoprostol
- prostaglandin analog
- PGE1 analog
- exacerbate inflam. bowel disease, abortion (uterine contract)
- Prevent NSAID gastric injury (PPI’s better)
pirenzepine
- M1 antagonists
- stops signal from vagal nerve (down acid secretion)
- anticholinergic effects
- rarely used
bethanechol
- cholinergic ag (prokinetic agent)
- general constriction of whole intestine
- anti-ACh effects
- help urinate, prokinetic motility
erythromycin
- antibiotic (prokinetic agent)
- motilin agonist
- fast painful dumps
- counter an ileus
metoclopramide
- DA antagonist (prokinetic agent)
- block DA->increased coordinated ACh release
- Parkinson’s-like, dyskinesia
- antiemetic, up esophageal sphincter tone (GERD), up GI motility
neostigmine
- AChE inhibitor (prokinetic agent)
- general constriction of whole intestine
- ACh effects
- counter an ileus
tegaserod
- 5-HT4 agonist
- stim intestinal sensory neurons
- fatal arrythmias
- females w/ irritable bowel syndrome
cisapride
- 5-HT4 agonist (prokinetic agent)
- stim intestinal sensory neurons via 5-HT4 & adenylate cyclase
- fatal arrythmias
- GERD
heparin sulfate
- anticoagulant- indirect thrombin inhibitor
- binds antithrombin up flexibility catalyzes activity (blocks IIA,IXa,Xa)
- Bleeding, allergy, thrombosis, osteoporosis. NEVER GIVE INTRAMUSC!
- Acute Tx of DVT and PE. Sometime venous thrombosis and DIC
protamine sulfate
- heparin antagonist
- cationic peptide binds heparin and inhibits anticoagulant activity
- allergies (fish)?
- reverse heavy heparin after surgery
rivaroxaban
-anticoagulants
-Factor Xa inhibitor, liver/renal/faecal-biliary clearance
-
-
warfarin
- anticoagulant
- inh. Vit K metab–> disrupts gamma-carboxylation of II, VII, IX, X, C, S.
- bleeding, skin necrosis, teratogen, thrombosis
- prevent blood clots- 3 day warfarinization needs heparin start
menadione
-warfarin antidote- vit K
-
-
-
dalteparin
- low molecular weight heparins- indirect thrombin inhibitor
-enhances antithrombin action on factor X
-
-Tx=MI, angina, thrombophlebitis Prevent=clots etc.
enoxaparin
-low molecular weight heparins- indirect thrombin inhibiotor
-enhances antithrombin action on factor X
-
-Tx=MI, angina, thrombophlebitis Prevent=clots etc.
fondaparinux
- Xa inhibitor- indirect thrombin inhibitor
- pentasaccharide inhibits Xa, renal clearance
- bleeding hemmorhage
- SubQ for DVT, PE prevention following surg,
argatroban
-direct thrombin inhibitors
-inhibits thrombin, hepatic clearance
-
-parenteral in heparin contraindicated individuals
bivalirudin
-direct thrombin inhibitors
-inhibits thrombin, hepatic and renal clearance
-
-parenteral in heparin contraindicated individuals
lepirudin
-direct thrombin inhibitors
-inhibits thrombin, renal clearance
-
-parenteral in heparin contraindicated individuals
dabigatran
- direct thrombin inhibitors
- inhibits thrombin, 80% renal clearance
- GI BLEEDS!
- Oral
tissue plasminogen activator
- thrombolytics
- serine protease, plasminogen to plasmin
- intracranial hemmorhage
- massive venous thrombosis or PE, acute MI
streptokinase
- thrombolytics
- binds and activates plasminogen
- allergic reactions, intracranial hemmorhage
- massive venous thrombosis or PE, acute MI
urokinase
- thrombolytics
- promotes plasminogen to plasmin
- intracranial hemmorhage
- massive venous thrombosis or PE, acute MI
abciximab
- antiplatelet drugs
- chimeric monoclonal Ab targets platelet Iib/IIIa
- bleeding/hemorrhage
- parenteral, prevent blood clot during vessel procedure
aspirin
- antiplatelet drugs
- irrev. Acetylates cyclooxygenase inhibits TXA2 syn
- excessive bleeding (aneurysm in brain)
- prevention MI, TIA, stroke, restenosis (most common used)
clopidogrel
- antiplatelet drugs
- thienopyridine deriv–>irrev blocks P2Y receptor–>blocks plat. Agg.
- less than ticlopidine, less dosing so preferred
- coronary stent placement- also for patients non tolerant of aspirin
prasugrel
-antiplatelet drugs
-thienopyridine deriv–>irrev blocks P2Y receptor–>blocks plat. Agg
-
-prevent stroke MI, coronary intervention (more eff/rapid HYDROLYSIS not CYP)
ticlopidine
- antiplatelet drugs
- thienopyridine deriv–>irrev blocks P2Y receptor–>blocks plat. Agg
- nausea, dyspepsia, diarrhea, hemorrhage LEUKOPENIA
- coronary stent placement- also for patients non tolerant of aspirin
tirofiban
- antiplatelet drugs
- carboxy fibrinogen terminal targets platelet IIb/IIIa receptor
- bleeding/hemorrhage
- parenteral, prevent blood clot during vessel procedure
Chlorothiazide
- Thiazide Diuretics
- Block Na-Cl symporter in DCT
- Hypokalemia, increased uric acid, sulfa crossreactivity
- antihypertensive, heart failure
Chlorthalidone
- Thiazide Diuretics
- Block Na-Cl symporter in DCT
- Hypokalemia, increased uric acid, sulfa crossreactivity
- antihypertensive, heart failure
Hydrochlorothiazide
- Thiazide Diuretics
- Block Na-Cl symporter in DCT
- Hypokalemia, increased uric acid, sulfa crossreactivity
- antihypertensive, heart failure
Furosemide
- Loop diuretic
- Blocks Na-K-2Cl cotransporter in ascending loop of Henle
- Hypokalemia, increased uric acid, deafness, sulfa cross reactivity
- Hypertension, heart failure
Ethacrynic Acid
- Loop diuretic
- Blocks Na-K-2Cl cotransporter in ascending loop of Henle
- Hypokalemia, increased uric acid, deafness (especially this drug)
- Hypertension, heart failure
Bumetanide
- Loop diuretic
- Blocks Na-K-2Cl cotransporter in ascending loop of Henle
- Hypokalemia, increased uric acid, deafness, sulfa cross reactivity
- Hypertension, heart failure
Torsemide
- Loop diuretic
- Blocks Na-K-2Cl cotransporter in ascending loop of Henle
- Hypokalemia, increased uric acid, deafness, sulfa cross reactivity
- Hypertension, heart failure
Spironolactone
- Aldosterone Receptor Blockers (mild diuretic)
- Block sodium and water reabsorption in collecting ducts
- Hyperkalemia
- Resistant hypertension, congestive heart failure with hypertension
Eplerenone
- Aldosterone Receptor Blockers (mild diuretic)
- Block sodium and water reabsorption in collecting ducts
- Hyperkalemia
- Resistant hypertension, congestive heart failure with hypertension
Triamterene
- Potassium sparing diuretic
- Sodium channel blocker in DCT and collecting duct
- Hyperkalemia
- Diuresis, antihypertensive
Amiloride
- Potassium sparing diuretic
- Sodium channel blocker in DCT and collecting duct
- Hyperkalemia
- Diuresis, antihypertensive
Captopril
- ACE inhibitors
- Block conversion of Ang I to Ang II & bradykinin breakdown
- Dry cough, hyperkalemia, angioedema, hypotension, rash, fetal renal damage
- Mild/moderate hypertension, heart failure (1st line tx), for HF usually combo with B-blocker; prevent progression of heart failure after MI
Enalapril
- ACE inhibitors
- Block conversion of Ang I to Ang II & bradykinin breakdown
- Dry cough, hyperkalemia, angioedema, hypotension, rash, fetal renal damage
- Mild/moderate hypertension, heart failure (1st line tx), for HF usually combo with B-blocker; prevent progression of heart failure after MI
Lisinopril
- ACE inhibitors
- Block conversion of Ang I to Ang II & bradykinin breakdown
- Dry cough, hyperkalemia, angioedema, hypotension, rash, fetal renal damage
- Mild/moderate hypertension, heart failure (1st line tx) for HF usually combo with B-blocker; prevent progression of heart failure after MI
Fosinopril
- ACE inhibitors
- Block conversion of Ang I to Ang II & bradykinin breakdown
- Dry cough, hyperkalemia, angioedema, hypotension, rash, fetal renal damage
- Mild/moderate hypertension, heart failure
Conivaptan
- Vasopressin Receptor Antagonist (intravenous)
- Blocks V1 (reduces afterload) and V2 receptors (for hyponatremia)
- Blood pressure can fall abruptly in patients with impared sympathetic nervous system (due to V1), increased osmolality
- Hyponatremia associated with Syndrome of Inappropriate ADH (SIADH) and heart failure
Tolvaptan
- Vasopressin Receptor Antagonist (oral)
- Blocks V2 receptor selectively
- increased plasma osmolality
- Hyponatremia associated with heart failure, cirrhosis, and SIADH
Losartan
- ARBs
- Block AT1 receptor, block effects of Ang II
- Hypotension, hyperkalemia, fetal renal toxicity (angioedema and cough < ACEIs
- Hypertension and heart failure
Valsartan
- ARBs
- Block AT1 receptor, block effects of Ang II
- Hypotension, hyperkalemia, fetal renal toxicity (angioedema and cough < ACEIs
- Hypertension and heart failure
Candesartan
- ARBs
- Block AT1 receptor, block effects of Ang II
- Hypotension, hyperkalemia, fetal renal toxicity (angioedema and cough < ACEIs
- Hypertension and heart failure
Irbesartan
- ARBs
- Block AT1 receptor, block effects of Ang II
- Hypotension, hyperkalemia, fetal renal toxicity (angioedema and cough < ACEIs
- Hypertension and heart failure
Aliskiren
- Renin Inhibitor
- Competitive inhibitor of renin
- Hypotension, cough, hyperkalemia
- Hypertension
Verapamil
- Cardioselective calcium channel Blocker
- Blocks L-type Calcium channels
- Headache, don’t use in heart failure w/ edema (depressive A-V conductance and contractility
- Hypertension and heart failure (negative ionotropic)
Diltiazem
- Cardioselective calcium channel Blocker
- Blocks L-type Calcium channels
- Headache, don’t use in heart failure w/ edema (depressive A-V conductance and contractility
- Hypertension and heart failure (negative ionotropic)
Nifedipine
- Vascular smooth muscle selective calcium channel Blocker
- Blocks L-type Calcium channels
- Headache, don’t use in heart failure w/ edema (depressive A-V conductance and contractility
- Hypertension and heart failure
Nicardipine
- Vascular smooth muscle selective calcium channel Blocker
- Blocks L-type Calcium channels
- Headache, don’t use in heart failure w/ edema (depressive A-V conductance and contractility
- Hypertension and heart failure
Amlodipine
- Vascular smooth muscle selective calcium channel Blocker
- Blocks L-type Calcium channels
- Headache, don’t use in heart failure w/ edema (depressive A-V conductance and contractility
- Hypertension and heart failure
Atenolol
- Beta Blocker
- Blocks Beta 1 receptors
- Inability to elevate glucose, nausea, vomiting, confusion, dizziness, fatigue, sleep disorders
- Hypertension
Terazosin
- Alpha blocker
- Blocks alpha 1 receptors
- Reflex tachycardia, orthostatic hypotension, fluid retention, palpitations, tinnitus, GI upset, headaches, urinary incontinence
- Hypertension (pheochromocytoma)
Prazosin
- Alpha blocker
- Blocks alpha 1 receptors
- Reflex tachycardia, orthostatic hypotension, fluid retention, palpitations, tinnitus, GI upset, headaches, urinary incontinence
- Hypertension (pheochromocytoma)
Doxazosin
- Alpha blocker
- Blocks alpha 1 receptors
- Reflex tachycardia, orthostatic hypotension, fluid retention, palpitations, tinnitus, GI upset, headaches, urinary incontinence
- Hypertension (pheochromocytoma)
Labetalol
- Mixed Adrenergic Blocker
- Blocks beta receptors and alpha 1 receptors
- (none mentioned)
- Chronic Hypertension, hypertensive emergencies
Carvedilol
- Mixed Adrenergic Blocker
- Blocks beta receptors and alpha 1 receptors
- (none mentioned)
- CHypertension and heart failure
Reserpine
- Adrenergic Transmission Blockers
- Depletes Norepinephrine from adrenergic nerve terminals, blocks its reuptake
- Postural hypotension, sedation, dry mouth, night mares, sodium and water retention
- Mild to moderate hypertension
Clonidine
- Centrally mediated agents
- Alpha 2 agonists
- Withdrawal syndrome - rebound hyertension, sedation, dry mouth, depression, drowsiness, sodium and water retention, postural hypotension
- Resistant hypertension
Alpha-methyldopa
- Centrally mediated agents
- Alpha 2 agonists
- Withdrawal syndrome - rebound hyertension, sedation, dry mouth, depression, drowsiness, sodium and water retention, postural hypotension
- Pregnancy Induced hypertension
Guanabenz
- Centrally mediated agents
- Alpha 2 agonists
- Withdrawal syndrome - rebound hyertension, sedation, dry mouth, depression, drowsiness, sodium and water retention, postural hypotension
- Resistant hypertension
Hydralazine
- Vasodilators
- Unknown mechanism (reduces intracell calcium in arterioles
- Headache, anorexia, nausea, dizziness, sweating, reflex tachcardia (angina and ischemic arrhythmias, Lupus
- Hypertension
Minoxidil
- Vasodilators
- Activates Potassium channels preferentially In arterioles
- Fluid retention, reflex tachycardia, abnormal hair growth, pericardial effusion and cadiac tamponande
- Resistant hypertension
Nitroprusside
- Vasodilators
- Generates nitric oxide, increases cGMP in veins and arteries
- Rapid decrease in MAP, cyanide accumulation
- Hypertensive crisis, cause hypotension during surgery
Riociguat
- Vasodilators
- Direct stimulation of guanylyl cyclase, increases cGMP
- Headaches, dizziness, nausea, diarrhea, hypotension, birth defects
- Pulmonary hypertension, thromboembolic hypertension
Nitroglycerin
- Vasodilators
- Generates nitric oxide, increases cGMP in veins
- Headache
- hypertensive crisis, cause hypotension during surgery
Epoprostenol
- Vasodilators
- Direct vasodilation via cAMP (drug is prostacyclin, counters TXA2)
- (none mentioned)
- Pulmonary hypertension (continuous IV admin)
Bosentan
- Vasodilators
- Non selective endothelin receptor blocker
- Edema, headache, blocks spermatogenesis, resp. tract infection, decreased hematocrit, hepatic effects
- Pulmonary hypertension
Ambrisentan
- Vasodilators
- ET-A (endothelin A) receptor blocker
- Edema, headache, blocks spermatogenesis, resp. tract infection, decreased hematocrit, hepatic effects
- Pulmonary hypertension
Rizatriptan
- Serotonin Receptor Agonist
- Activate prejunctional 5-HT1B/D receptors on sensory nerves, block trigemnovascular system, inhibit release of inflammatory peptides (CGRP) and 5-HT1D receptors promote vasoconstriction in cranial blood vessels
- Coronary spasm in patients with CV disease. Contraindicated in liver failure.
- Acute migraines, cluster headaches
Sumatriptan
- Serotonin Receptor Agonist
- Activate prejunctional 5-HT1B/D receptors on sensory nerves, block trigemnovascular system, inhibit release of inflammatory peptides (CGRP) and 5-HT1D receptors promote vasoconstriction in cranial blood vessels
- Coronary spasm in patients with CV disease. Contraindicated in liver failure.
- Acute migraines, cluster headaches
Zolmitriptan
- Serotonin Receptor agonist (more lipophilic and longer half life than sumatriptan)
- Activate prejunctional 5-HT1B/D receptors on sensory nerves, block trigemnovascular system, inhibit release of inflammatory peptides (CGRP) and 5-HT1D receptors promote vasoconstriction in cranial blood vessels
- Coronary spasm in patients with CV disease. Contraindicated in liver failure.
- Acute migraines, cluster headaches
Cyproheptadine
- Serotonin Receptor Antagonist
- nonselective 5-HT1, 5-HT2 antagonist and H1 receptor antagonist
- Drowsiness, GI disturbances, prolonged vasospasm
- Treats symptoms resulting from carcinoid tumors
Ketanserin
- Serotonin Receptor Antagonist
- Selective 5-HT2 (smooth muscle) receptor antagonist (5HT2A>5HT2C), blocks alpha1 adrenergic R too
- none specified in lecture
- Lowers arterial pressure in hypertensives (not approved in U.S.)
Ergonovine
- Serotonin Receptor Partial Agonist
- 5HT2 R partial agonist, weak antagonist activity
- Prolonged vasospasm, GI disturbances
- Postpartum and postabortal hemorrhage, diagnostic tool for vasospastic angina
Ergotamine
- Serotonin Receptor Partial Agonist
- Partial agonist at 5-HT1/2 R
- Prolonged vasospasm, GI disturbances
- Acute migraines, postpartum bleeding
Methysergide
- Serotonin Receptor Partial Agonist
- Antagonist at 5-HT2 R and partial agonist at 5-HT1 R
- Prolonged vasospasm, GI disturbances, CNS disturbances (hallucination)
- Symptoms of carcinoid tumors
Amlodipine
- Vasoselective Ca channel blocker
- Block L-type Ca channels (down cytosolic Ca)
- gingival hyperplasia, arrhythmia, heart failure (but not as bad as the other 3 drugs)
- Hypertension, chronic for coronary heart disease to vasodilate, prevent vasospasm post-stroke
Nicardipine
- Vasoselective Ca channel blocker
- Block L-type Ca channels (down cytosolic Ca)
- gingival hyperplasia, arrhythmia, heart failure
- Hypertension, chronic for coronary heart disease to vasodilate, prevent vasospasm post-stroke
Nifedipine
- Vasoselective Ca channel blocker
- Block L-type Ca channels (down cytosolic Ca)
- gingival hyperplasia, arrhythmia, heart failure
- (avoid post-MI!), Hypertension, chronic for coronary heart disease to vasodilate, prevent vasospasm post-stroke
Nimodipine
- Vasoselective Ca channel blocker
- Block L-type Ca channels (down cytosolic Ca)
- gingival hyperplasia, arrhythmia, heart failure
- ONLY for post-subarachnoid hemorrhage prevention of vasospasm (cuz more lipophilic)
Isosorbide Dinitrate
-Nitrovasodilators
-reduce O2 demand, up O2 supply to heart (relaxes arteries & veins!), inhibit platelet agg.
-
-angina/CHD
Isosorbide Mononitrate
- Nitrovasodilators
- reduce O2 demand, up O2 supply to heart (relaxes arteries & veins!), inhibit platelet agg.
- minimal first-pass metab!
- angina/CHD (longer action)
Nitroglycerin
- Nitrovasodilators
- reduce O2 demand, up O2 supply to heart (relaxes large arteries & veins!), inhibit platelet agg.
- first-pass hepatic metab.
- vasodilate distal to a stenosis (heart) for angina, CHD
Nitroprusside Sodium
-Nitrovasodilators
-reduce O2 demand, up O2 supply to heart (relaxes arteries & veins!), inhibit platelet agg.
-
-angina/CHD
Aspirin
-
-Acute coronary syndrome, MI, stroke in combo w/ a P2Y12 inhibitor
Clopidogrel
- Miscellaneous vasoactive (anticoagulant)
- Inhibit Platelet P2Y12 to reduce platelet activation, down ADP activation of GPIIb/IIIa
- Neutropenia!, genetic variability
- Acute coronary syndrome, MI, stroke in combo w/ aspirin
Prasugrel
- Miscellaneous (anticoagulant)
- Inhibit Platelet P2Y12 to reduce platelet activation, down ADP activation of GPIIb/IIIa
- Fewest drug interactions!
- Acute coronary syndrome, MI, stroke in combo w/ aspirin
Ranolazine
- Miscellaneous vasoactive
- down late Na current (reduce Na, Ca overload in ischemic myocytes), shift ATP production to glycolysis
- NO negative chrono/ino effects, better exercise tolerance!
- Angina
Ticagrelor
-Miscellaneous vasoactive (anticoagulant)
-Inhibit Platelet P2Y12 to reduce platelet activation, down ADP activation of GPIIb/IIIa
-
-Acute coronary syndrome, MI, stroke in combo w/ aspirin
cholestyramine
- bile acid sequestrants
- cationic binds bile acids prevent reabsorption, up LDL rec., up VLDL prod
- dyspepsia and other GI, Malabsorp vit K, impaired absorption of drugs
- lower cholesterol levels
colesevelam HCl
- bile acid sequestrants
- cationic binds bile acids prevent reabsorption, up LDL rec., up VLDL prod
- DOWN HYPERGLYCEMIA. dyspepsia and other GI, Malabsorp vit K, impair absorption of drugs
- lower cholesterol
atorvastatin
- HMG CoA reductase inhibitors- CYP3A4
- competitive inhibit–> decrease chol. Syn, UP LDL rec. –> dec. LDL
- liver tox, inc. Creat. Kinase–>myopathy/rhabdomyolysis
- lower cholesterol and prevent cardiac disease
fluvastatin
- HMG CoA reductase inhibitors- CYP2C9
- competitive inhibit–> decrease chol. Syn, UP LDL rec. –> dec. LDL
- liver tox, inc. Creat. Kinase–>myopathy/rhabdomyolysis
- lower cholesterol and prevent cardiac disease
lovastatin
- HMG CoA reductase inhibitors- CYP3A4
- competitive inhibit–> decrease chol. Syn, UP LDL rec. –> dec. LDL
- liver tox, inc. Creat. Kinase–>myopathy/rhabdomyolysis
- lower cholesterol and prevent cardiac disease
simvastatin
- HMG CoA reductase inhibitors-CYP3A4
- competitive inhibit–> decrease chol. Syn, UP LDL rec. –> dec. LDL
- liver tox, inc. Creat. Kinase–>myopathy/rhabdomyolysis
- lower cholesterol and prevent cardiac disease
pravastatin
- HMG CoA reductase inhibitors-CYP3A4
- competitive inhibit–> decrease chol. Syn, UP LDL rec. –> dec. LDL
- liver tox, inc. Creat. Kinase–>myopathy/rhabdomyolysis
- lower cholesterol and prevent cardiac disease
clofibrate
- fibric acids
- PPAR ligand–>UP lipase, apo AI,II–>Clears chylomicrons and VLDL and raises HDL
- Rashes, GI, arrhythmias (lowers potassium), myopthathy, galls stones
- treat hypertriglyceridemias (VLDL)
fenofibrate
- fibric acids
- PPAR ligand–>UP lipase, apo AI,II–>Clears chylomicrons and VLDL and raises HDL
- Rashes, GI, arrhythmias (lowers potassium), myopthathy, galls stones
- treat hypertriglyceridemias (VLDL)
gemfibrozil
- fibric acid (increase blood conc. statins)
- PPAR ligand–>UP lipase, apo AI,II–>Clears chylomicrons and VLDL and raises HDL
- Rashes, GI, arrhythmias (lowers potassium), myopthathy, galls stones -treat hypertriglyceridemias (VLDL)
ezetimibe
- misc. agents for atherosclerosis (not CYP substrate)
- inhibits NPC1L1-impairs intestinal absorption of cholesterol
- Non specific- headache diarrhea etc. (similar to others that lower chol.)
- lowers cholesterol (not CYP substrate)
nicotinic acid (niacin)
- misc. agents for atherosclerosis
- G prot. Down cAMP, prevents VLDL secretion and subseq. Decreases LDL production
- cutaneous vasodilat, insulin resistance, hyperuricemia, liver tox.
- lowers triglycerides>cholesterol
quinapril
- ACE inhibitors
- Block conversion of Ang I to Ang II & bradykinin breakdown
- Dry cough, hyperkalemia, angioedema, hypotension, rash, fetal renal damage
- Mild/moderate hypertension, heart failure (1st line tx) for HF usually combo with B-blocker; prevent progression of heart failure after MI
candesartan
- ARB (AT1 Receptor antag)
- competitive antagonist of AT1 recept (supress Ang2 & Ang 3 actions & incr Ang1-7 actions)
- (none listed)
- reasonable alternative to ACE inhib for HF (not in combo)
losartan
- ARB (AT1 Receptor antag)
- competitive antagonist of AT1 recept (supress Ang2 & Ang 3 actions & incr Ang1-7 actions)
- (none listed)
- reasonable alternative to ACE inhib for HF (not in combo
valsartan
- ARB (AT1 Receptor antag)
- competitive antagonist of AT1 recept (supress Ang2 & Ang 3 actions & incr Ang1-7 actions)
- (none listed)
- reasonable alternative to ACE inhib for HF (not in combo
Loop diuretics
- ## --preferred diuretic in most HF patients for management of fluid retention (symptomatic benefit); no mortality benefit in HF, should not be used alone in stage C HF patients
thiazides
- ## --preferred in hypertensive patients with HF for management of fluid retention (symptomatic benefit) & anti-hypertensive actions; no mortality benefit in HF, should not be used alone in stage C HF patients
bisoprolol
- beta R antagonists
- selective beta-1 R antag (mechanism not fully known but likely impairs SNS-mediated incr in automaticity and hypoK, improves L ventricular structure and fx by preventing remodeling in HF, and improves abnormal Ca handling in HF by preventing hyperphosphorylation of RYR)
- fluid retention, fatigue, bradycardia (heart block), hypotension; contraindications: bradycardia or reactive airway disease
- all patients with stage C HF (reduce death)
carvedilol
- beta R antagonists
- alpha-1, beta-1, & beta-2 R antag (mechanism not fully known but likely impairs SNS-mediated incr in automaticity and hypoK, improves L ventricular structure and fx by preventing remodeling in HF, and improves abnormal Ca handling in HF by preventing hyperphosphorylation of RYR)
- fluid retention, fatigue, bradycardia (heart block), hypotension; contraindications: bradycardia or reactive airway disease
- all patients with stage C HF (significantly reduce death compared to metoprolol)
metoprolol
- beta-1 R antagonists; class II anti-arrhythmic drug
- selective beta-1 R antag; decr phase 4 slope (reduced automaticity)
- fluid retention, fatigue, bradycardia (heart block), hypotension, Inability to elevate glucose, nausea, vomiting, confusion, dizziness, fatigue, sleep disorders; contraindications: bradycardia or reactive airway disease
- all patients with stage CHF (reduce death); atrial arrhythmias, slow AV node conduction, prevent sudden cardiac death post-MI
digoxin
- cardiac glycosides
- Cardiac tissue action: inhib Na/K ATPase (incr intracellular free Ca > incr CO > decr reflex SNS activity & incr renal perfusion); Non-cardiac action: sensitizes cardiac baroreceptors (sense P as higher), incr vagal tone and incr SA node sensitivity to ACh > decr SNS and incr PSNS activity; inhib Na-K ATPase in hidney > reduce reabsorption of Na > incr Na release to distal tubules > decr renin
- electrical cardiac toxicity (arrhythmias, heart block), therapeutic range (2ng/mL) deleterious effects on heart with long-term use; toxicity treated with anti-digoxin immunotherapy
- arrhythmias; no longer 1st line therapy for HF; tx patient with HF & atrial fibrillation or persistent, severe symptoms despite ACEI/ARB & B-blocker tx
digitoxin
-cardiac glycosides
-No other info not specific to digoxin
-
-
eplerenone
-
-addition to ACEI/ARBs in patient with moderately severe HF (class C/D) or with L ventricular dysfunction after MI
spironolactone
-
-addition to ACEI/ARBs in patient with moderately severe HF (class C/D) or with L ventricular dysfunction after MI
hydralazine
-vasodilators
-arterial vasodilator > reduced renal vasc resistance & incr renal blood flow
-
-used as combo with isosorbide dinitrate (incr survival but not as good as enalapril); used in patients who cannot tolerate ACEIs; may provide hemodynamic improvement in advanced HF already treated with ACEI, digoxin, & diuretics
isosorbide dinitrate
-vasodilators
-short acting, venodilation > incr venous capacitance > reduce preload; also incr coronary artery flow
-
-used as combo with hydralazine
nitroglycerine
-vasodilators
-sublingual quick acting; IV NO source selective for venous capacitance vessels
-
-L sided HF due to acute myocardial ischemia or when prompt reduct. of ventricular fillling P required
dobutamine
- beta agonists
- Beta agonist; does not activate DA R; improve cardiac performance, facilitate diuresis, & promote clinical stability in SHORT TERM use
- tolerance limits efficacy with longer term use; tachycardia & arrhythmias
- systolic dysfuntion & congestion w/ HF; refractory HF (hospitalized frequently for clinical deterioration)
dopamine
- beta agonists
- Beta agonist (low conc > stim cardiac contractility); alpha-agonist (high conc > periph arterial/venous constriction); improve cardiac performance, facilitate diuresis, & promote clinical stability in SHORT TERM use
- tachycardia (can provoke ischemia in CAD); arterial vasoconstriction incr afterload, not helping HF
- circulatory failure; refractory HF (hospitalized frequently for clinical deterioration)
inamrinone
- cAMP PDE inhib
- prevent cAMP degradation > more active PKA > incr cytosolic Ca > stimulate myocardial contraction & accelerate relaxation; stimulate balanced arterial/venous dilation (reduce afterload & preload); longer half life & less selective
- worse SE profile than milrinone
- short term support of circulation in advanced HF (parenteral inotropic support)
milrinone
- cAMP PDE inhib
- prevent cAMP degradation > more active PKA > incr cytosolic Ca > stimulate myocardial contraction & accelerate relaxation; stimulate balanced arterial/venous dilation (reduce afterload & preload); shorter half life & more selective for PDE3
- more favorable SE profile, best PDE inhib
- short term support of circulation in advanced HF (parenteral inotropic support)
disopyramide
- Na channel blocker, class IA anti-arrhythmic drug
- block Na channels > incr threshold (prolong action potential), oral admin, dissociate from Na channels with medium kinetics
- negative inotrope; contraindications: HF
- ventricular arrhythmias, recurrent atrial arrhythmias
procainamide
- Na channel blocker, class IA anti-arrhythmic drug
- block Na channels > incr threshold (prolong action potential), oral/IV admin, dissociate from Na channels with medium kinetics
- lupus-like effect, nausea
- ventricular arrhythmias & recurrent atrial arrhythmias
quinidine
- Na channel blocker, class IA anti-arrhythmic drug
- block Na channels > incr threshold (prolong action potential), oral/IV admin, dissociate from Na channels with medium kinetics
- diarrhea
- ventricular arrhythmias & recurrent atrial arrhythmias
lidocaine
- Na channel blocker, class IB anti-arrhythmic drug
- block Na channels > incr threshold (shorten action potential), IV admin, dissociate from Na channels with fast kinetics
- CNS toxicity
- Acute ventricular arrhythmias
mexiletine
- Na channel blocker, class IB anti-arrhythmic drug
- block Na channels > incr threshold (shorten action potential), oral admin, dissociate from Na channels with fast kinetics
- CNS toxicity
- Chronic ventricular arrhythmias
flecainide
- Na channel blocker, class IC anti-arrhythmic drug
- block Na channels > incr threshold (minimal effect on action potential duration), oral admin, dissociate from Na channels with slow kinetics
- arrhythmogenic (avoid in patients with underlying structural heart disease or post-MI)
- Recurrent atrial arrhythmias
propafenone
- Na channel blocker, class IC anti-arrhythmic drug
- block Na channels > incr threshold (minimal effect on action potential duration), oral admin, dissociate from Na channels with slow kinetics
- arrhythmogenic (avoid in patients with underlying structural heart disease or post-MI)
- Recurrent atrial arrhythmias
amiodarone
- K channel blocker, class III anti-arrhythmic drug
- incr action potential duration, oral/IV admin
- bradycardia (beta blocking effects)
- atrial and ventricular arrhythmias (less arrhythmogenic in patients with HF/post-MI)
dofetilide
- K channel blocker, class III anti-arrhythmic drug
- incr action potential duration, oral admin
- marked QT prolongation (torsades de pointes)
- atrial arrhythmias
dronedarone
-K channel blocker, class III anti-arrhythmic drug
-incr action potential duration
-
-
ibutilide
-K channel blocker, class III anti-arrhythmic drug
-incr action potential duration
-
-
sotalol
-K channel blocker, class III anti-arrhythmic drug
-incr action potential duration
-
-
diltiazem
-
-decr phase 4 slope & incr threshold
-
-class IV anti-arrhythmic drug
verapamil
-
-decr phase 4 slope & incr threshold
-
-class IV anti-arrhythmic drug
atenolol
- beta-R blocker, class II anti-arrhythmic drug
- decr phase 4 slope (reduced automaticity), oral/IV admin
- bradycardia, negative inotrope
- atrial arrhythmias, slow AV node conduction, prevent sudden cardiac death post-M
esmolol
- beta-R blocker, class II anti-arrhythmic drug
- decr phase 4 slope (reduced automaticity), IV admin, short half-life
- bradycardia, negative inotrope
- atrial arrhythmias, slow AV node conduction
propranolol
- beta-R blocker, class II anti-arrhythmic drug
- block beta-1 & beta-2 receptors; decr phase 4 slope (reduced automaticity), oral/IV admin
- bradycardia, negative inotrope, bronchospasm; Inability to elevate glucose, Nausea, vomiting, confusion, dizziness, fatigue, sleep disorders
- hypertension; atrial arrhythmias, slow AV node conduction
digoxin
-
-
adenosine
-
-incr max diastolic potential
-
-
acebutolol
- Beta 1 antagonist (cardioselective)
- inhibits SNS input to heart decreasing O2 demand
- contraindicated: COPD, asthma, diabetes
atenolol
- Beta 1 antagonist (cardioselective)
- inhibits SNS input to heart decreasing O2 demand
- contraindicated: COPD, asthma, diabetes
esmolol
- Beta 1 antagonist (cardioselective)
- inhibits SNS input to the heart decreasing O2 demand
- Contraindicated: COPD, asthma, diabetes
metoprolol
- Beta 1 antagonist (cardioselective)
- inhibits SNS input to the heart decreasing O2 demand
- Contraindicated: COPD, asthma, diabetes
nadolol
- Beta antagonist (non selective)
- B1 and B2 antagonist
- Contraindicated: COPD, asthma, diabetes
pindolol
- Beta antagonist (non selective)
- B1 and B2 antagonist, partial Beta agonist
- Contraindicated: COPD, asthma, diabetes
propranolol
- Beta antagonist (non selective)
- B1 and B2 antagonist
- Contraindicated: COPD, asthma, diabetes
timolol
- Beta antagonist (non selective)
- B1 and B2 antagonist
- Contraindicated: COPD, asthma, diabetes
avanafil
- PDE5 inhibitor
- increase levels of cGMP
- Do not take with nitrates or alpha receptor blocker vision changes
tadalafil
- PDE5 inhibitor
- increase levels of cGMP
- Do not take with nitrates or alpha receptor blocker (17 Hr T1/2) vision changes
sildenafil
- PDE5 inhibitor
- increase levels of cGMP
- Do not take with nitrates or alpha receptor blocker. Vision changes
vardenafil
- PDE5 inhibitor
- increase levels of cGMP
- Do not take with nitrates or alpha receptor blocker. Vision changes
verapamil
- Ca+ channel blocker (cardioselective)
- Block L type Ca+ channels in heart
- Can cause heart failure, gingival inflammation
diltiazem
- Ca+ channel blocker (cardioselective)
- Block L type Ca+ channels in heart
- can cause bradycardia/heartblock