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129 Cards in this Set
- Front
- Back
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MoA of hydralazine
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cGMP ® SM relax
vasodilates ARTERIOLES > veins ¯ AFTERLOAD |
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Use of hydralazine
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Severe HTN, CHF
1st line tx for HTN in pregnancy |
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Tox of hydralazine
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Compensatory tachy (co-admin w/β-blocker)
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non-DHPR Ca-channel blockers
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Verapamil
Diltiazem |
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DHPR Ca-channel blockers
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Nifedipine
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MoA of non-DHPR Ca-channel blockers (class IV antiarrhythmics)
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Block cardiac voltage-dependent L-type Ca-channels
¯ conduction velocity PR interval ERP (effects similar to β-blockers) |
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MoA of DHPR Ca-channel blockers
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Block voltage-dependent L-type Ca-channels of SM
¯ contractility (effects similar to nitrates) |
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Use of non-DHPR Ca-channel blockers
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Prevention of nodal arrhythmias
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Use of DHPR Ca-channel blockers
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HTN
Angina Prinzmetals's angina Raynaud's |
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Tox of non-DHPR Ca-channel blockers
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Edema, flushing
CHF, AV block, sinus node depression |
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Tox of DHPR Ca-channel blockers
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Edema, flushing
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Nitrates
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Nitroglcerin
Isosorbide dinitrate |
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MoA of nitrates
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cGMP & releases NO ® SM relax
venodilates VEINS >> arteries ¯ PRELOAD |
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Use of nitrates
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Angina
Pulmonary edema (Aphrodesiac & erection enhancer) |
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Tox of nitrates
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Reflex tachy, hypotension, flushing
Tolerance ('skip' dose 1x daily to prevent) Do NOT use w/sildenafil/vardenafil (accumlation of cGMP) |
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MoA of nitroprusside
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cGMP via direct release of NO
Short-acting |
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Use of nitroprusside
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Malignant HTN
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Tox of nitroprusside
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Cyanide (CN) toxicity ® tx w/sulfates
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MoA of fenoldopam
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Dopamine D1 receptor agonist
Relaxes RENAL vascular SM ( renal perfusion & diuresis while ¯ HTN) |
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MoA of diazoxide
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K-channel OPENer
Hyperpolarizes & relaxes vascular SM |
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Tox of diazoxide
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Hyperglycemia (due to insulin release)
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MoA of statins
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HMG-CoA reductase inhibitors
¯¯¯ LDL (cause LDL endocytosis into liver) |
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Tox of statins
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Rhabdomyolysis
Hepatotoxicity |
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MoA of niacin
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Inhibits lipolysis in adipose, ¯ VLDL secretion by liver
HDL, ¯¯ LDL |
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Tox of niacin
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Flushing (prevent w/aspirin or long-term use)
Hyperglycemia ® acanthosis nigricans Hyperuricemia ® gout exacerbation |
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Bile acid resins
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Cholestyramine
Colestipol Colesevelam |
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MoA of bile acid resins
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Prevent intestinal Reabsorption of bile acids
¯¯ LDL |
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Tox of bile acid resins
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Cholesterol gallstones
¯ absorption of fat-soluble vit's |
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MoA of ezetimibe
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Prevent cholesterol Reabsorption @ intestine brush border
¯¯ LDL |
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Fibrates
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Gemfibrozil
-fibrate |
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MoA of fibrates
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Upregulate LPL ® TG clearance
¯¯¯ TG |
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Tox of fibrates
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Cholesterol gallstones
Myostitis Hepatotoxicity |
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MoA of digoxin
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Inhibit Na/K-ATPase ® indirect inhibition of Na/Ca-exchanger ® [Ca]in ® (+) inotropy ( contractility)
Stimulates vagus nerve ® parasympathetic stim of nodes |
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Use of digoxin
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CHF ( contractility)
Atrial fibrillation (¯ conduction @ AV node & depression of SA node) |
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Tox of digoxin
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Blurry yellow vision, nausea vomiting (cholinergic)
PR, ¯ QT, T-wave inversion Arrhythmia Hyperkalemia (worsened by renal fail., hypokalemia, quinidine) Antidote: normalize K, lidocaine (if tachy), atropine (if brady), anti-dig Fab fragments, Mg |
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MoA of Class I antiarrhythmics
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Na-channel blockers
Slow/block conduction ¯ slope of pase 0 depolarization (Na+ in) firing threshold State-dependent (selectively depress frequently depolarized tissue, as in fast tachy) |
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Class IA antiarrhythmics
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Quinidine
Procainamide Disopyramide |
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Effects of IA antiarrhythmics
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AP duration, ERP, QT interval
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Use of IA antiarrhythmics
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Reentrant & ectopic SVTs
Ventricular tachy |
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Class IB antiarrhythmics
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Lidocaine
Mexiletine Tocainide |
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Effects of IB antiarrhythmics
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¯ AP duration
Preferentially effect ischemic Purkinje & ventricular tissue |
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Use of IB antiarrhythmics
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Acute vertricular arrhythmias (post-MI)
Digitalis-induced arrhythmias |
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Class IC antiarrhythmics
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Flecainide
Encainide Propafenone |
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Effects of IC antiarrhythmics
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No effect on AP duration
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Use of IC antiarrhythmics
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V-tachs that progress to VF
Intractable SVT Last resort Contraindicated post-MI |
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Class II antiarrhythmics (Beta-blockers)
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Propranolol
Esmolol Metoprolol Atenolol Timolol |
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MoA of β-blockers (Class II antiarrhythmics)
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¯ cAMP, ¯ Ca2+ currents
¯ slope of phase 4 (suppress abnormal pacemakers) PR interval (AV node particularly sensitive) Esmolol very short acting |
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Use of β-blockers (Class II antiarrhythmics)
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V-tach
SVT Slowing ventricular rate during A-fib/flutter |
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Tox of β-blockers (Class II antiarrhythmics)
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Contraindicated in asthma & acute exacerbations of CHF
Metoprolol: dyslipidemia Tx OD w/glucagon |
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Class III antiarrhythmics (K-channel blockers)
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Sotalol
Ibutilide Dofetilide Bretylium Amiodarone |
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MoA of K-channel blockers (Class III)
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AP duration
ERP QT interval Used when other arrhythmics fail |
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Tox of amiodarone
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Pulmonary fibrosis
Hepatotoxicity Hypo/hyper-thyroidism Blue/grey skin ® photodermatitis (has class I, II, III, & IV effects because it alters the lipid membrane) |
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Distinguish btw the primary sites of axn of the anti-arrhythmics)
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Class I & III primarily act on ventricular cells
Class II & IV primarily act on the nodes |
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MoA of adenosine
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K out of cells ® hyperpolarization
¯ Ca currents Very short acting |
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Use of adenosine
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Drug of choice in diagnosing/abolishing SUPERVENTRICULAR TACHYCARDIA
Effects blocked by theophylline |
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Use of K & Mg
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K: depress ectopic pacemakers in hypokalemia (e.g. digoxin tox)
Mg: torsades de pointes & digoxin tox |
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Use of indomethacin
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Close patent ductus arteriosis (inhibits PGE2)
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Anti-HTN drugs of choice in diabetes
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ACEi
ARB |
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Anti-HTN drugs of choice in CHF
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ACEi
β-blockers Diuretics (thiazides) ARB |
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Anti-HTN drugs of choice in systolic HTN
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DHPR Ca-channel blocker (verapamil)
Thiazide diuretic |
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Anti-HTN drugs of choice in MI
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β-blocker
ACEi |
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Contraindications for β-blockers
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Asthma
COPD Depression Non-selective β-blockers: hyperkalemia |
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Contraindications for diuretics
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Gout
K-sparing diuretics: renal insufficiency, hyperkalemia |
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Contraindications for ACEi's & ARBs
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Pregnancy
Renovascular dysfxn Hyperkalemia |
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Tx for hyperthyroidism
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Propylthiouracil, methimazole
MoA: inhbits organification of iodide & coupling of thyroid hormone synthesis; PPT also ¯ T4 ® T3 conversion |
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Tx for hypothyroidism
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Levothyroixine, triiodothyronine
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Use for GH
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GH deficiency
Turner syndrome |
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Octreotide (somatostatin analog)
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Acromegaly
Carcinoid Gastrinoma Glucagonoma |
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Oxytocin
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Stimulate labor (uterine contractions)
Milk let-down Ctrls uterine hemorrhage |
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ADH (desmopressin)
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Pituitary DI (central, not nephrogenic)
Stimulate vWF release from endothelial cells (von Willebrand's) |
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Tx for SIADH
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Demeclocycline (a tetracycline)
MoA: ADH antagonist Tox: nephrogenic DI, photosensitivity, abnl's of bone/teeth |
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Tx for pheochromocytoma
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Phenoxybenzanine (to shrink tumor prior to surgical removal)
MoA: non-selective α-antagonist |
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Tx for prolactinoma
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Bromocriptine, cabergolin
MoA: dopamine agonists |
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Bugs assoc'd w/endocarditis
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Acute: S. aureus
Subacute: viridans streptococci Assoc'd w/colon cancer: S. bovis Assoc'd w/prosthetic valves: S. epidermidis |
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Tx for diabetes insipidus
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Adequate fluid intake
Central: intranasal desmopressin Nephrogenic: thiazide diuretic, indomethacin, amiloride |
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1st generation H1 blockers
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Diphenhydramine
Dimenhydrinate Chlorpheniramine (reversible inhibitors of H1 histamine receptors) |
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2nd generation of H1 blockers
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Loratadine
Fexofenadine Desloratadine Cetirizine (reversible inhibitors of H1 histamine receptors; less sedating) |
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Asthma drugs that target inflammatory processes
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Cromolyn
Corticosteroids Antileukotrienes |
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Asthma drugs that target sympathetic tone
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Beta agonists
Theophylline (methylxanthines) Ipratropium |
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Uses of β-agonists
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Isoproterenol (non-specific): relaxes SM (β2); tox = tachycardia (β1)
Albuterol (β2): acute exacerbation Salmeterol (β2): prophylaxis; tox = tremor/arrhythmia |
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MoA of theophylline
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Inhibits phosphodiesterase ® ¯ cAMP hydrolysis ® bronchodilation
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Tox of theophylline
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Use limited by narrow therapeutic index
Cardiotox, neurotox Metabolized by P450 Blocks axns of adenosine |
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MoA & use of Ipratropium
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Competitive block of mAChR's ® prevents bronchoconstriction
Use: Asthma prophylaxis, COPD |
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MoA & use of cromolyn
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Prevents release of mediators from mast cells
Use: asthma prophylaxis only (not useful for acute attacks) |
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MoA & use of corticosteroids
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Beclomethasone, prednisone
MoA: inactivates NF-kB ® inhibits synthesis of of all cytokines, incl. TNF-α Use: 1st-line tx for chronic asthma |
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Antileukotrienes
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Zileuton
Zafirlukast Montelukast |
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MoA & use of zileuton
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Inhibits 5-lipoxygenase path: blocks arachidonic acid ® leukotrienes
Asthma prophylaxis |
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MoA & use of zafirlukast & motelukast
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Block leukotrience receptors
Use: aspirin-induced asthma |
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Expectorants
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Guaifenesin
N-acetylcysteine |
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MoA & uses of N-acetylcysteine
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Mucolytic
Use: loosen mucous plugs in CF pts; antidote for acetaminophen OD |
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Tx of pulmonary hypertension
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Bosentan
(competitively antagonizes endothelin-1 receptors, decreasing pulmonary vascular resistance) |
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MoA of mannitol
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Osmotic diuretic
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MoA & use & tox of acetazolamide
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MoA: Carbonic anydrase inhibitor ® self-limited bicarb diuresis
Use: Urinary alkalinization, metabolic alkalosis, altitude sickness Tox: hyperchloremic metabolic acidosis, sulfa allergy |
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MoA & use & tox of furosemide
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MoA: sulfonamide LOOP diuretic; inhibits Na/K/2Cl cotransporter (thick ascending LoH)
Use: edema, HTN, hypercalCEMIA Tox: Ototoxicity, hypokalemia, allergy (sulfa), nephritis (interstitial), gout |
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MoA & use & tox of ethacrynic acid
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MoA: NON-sulfonamide LOOP diuretic; inhibits Na/K/2Cl cotransporter (thick ascending LoH)
Use: diuresis in pts allergic to sulfa drugs Tox: similar to furosemide but does not cause gout |
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MoA & use & tox of thiazide diuretics
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MoA: inhibits NaCl reabsorption in early DCT
Use: HTN, CHF, hypercalciURIA, nephrogenic DI Tox: Hypokalemic metabolic alkalosis, hyperglycemia, hyperlipidemia, hyperuricemia, hypercalcemia; sulfa allergy |
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K-sparing diuretics
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Spironolactone
Triamterene Amiloride |
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MoA of spironolactone
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Competitive aldosterone receptor antagonist (NOT an ARB) in CCT
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MoA of triamterene & amiloride
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Block Na-channels in the CCT
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Use & tox of K-sparing diuretics
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Hyperaldosteronism, hypokalemia, CHF
Tox: hyperkalemia; spironolactone -- endo effects (gynecomastia, anti-androgen effects) |
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Diuretics that can cause acidemia
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Acetazolamide
K-sparing diuretics |
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Diuretics that can cause alkalemia
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Loop diuretics
Thiazides |
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ACE inhibitors
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Captopril
Enalapril Lisinopril |
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MoA of ACEi
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Inhibit angiotensin-converting enzyme (ACE) ® ¯ angiotensin II ® ¯ inactivation of bradykinin (potent vasodilator)
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Use of ACEi
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HTN
CHF DIABETIC renal dz |
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Tox of ACEi
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COUGH
ANGIOEDEMA Proteinuria Hyperkalemia Fetal renal damage (contraindicated) (contraindicated in bilateral renal artery stenosis) |
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MoA of losartan
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ARB (angiotensin II receptor blocker)
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MoA of leuprolide
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GnRH analog
Pulsatile: agonist Continuous: antagonist |
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Use of leuprolide
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Pulsatile: infertility
Continuous: prostate cancer (use w/flutamide), uterine fibroids |
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Antiandrogens
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Finasteride (propecia)
Flutamide Ketoconazole Spironolactone |
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MoA & use of finesteride
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MoA: 5α-reductase inhibitor (¯ testosterone ® DHT conversion)
Use: BPH, male-pattern baldness |
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MoA & use of flutamide
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MoA: nonsteroidal competitive testosterone receptor antagonist
Use: prostate cancer (w/leuprolide) |
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MoA & use of ketoconazole
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MoA: inhibits desmolase (¯ steroid synthesis)
Use: prevent hirsutism in tx of PCOS Tox: gynecomastia & amenorrhea |
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MoA & use of spironolactone
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MoA: inhibits steroid binding
Use: prevent hirsutism in tx of PCOS Tox: gynecomastia & amenorrhea |
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Estrogens
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Ethinyl estradiol
DES Mestranol |
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Tox of estrogens
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risk of endometrial cancer
Bleeding in postmenopausal women risk of thrombi DES: clear cell adenocarcinoma of vagina in females exposed in utero |
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Selective estrogen receptor modulators (SERMs)
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Estrogen partial agonists
Clomiphene Tamoxifen Raloxifene |
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MoA of clomiphene
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Partial agonist @ estrogen receptors in hypothalamus
Prevents normal feedback inhibition & release of LH & FSH from pituitary ® stimulates ovulation |
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Use & tox of clomiphene
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Use: Tx infertility & PCOS
Tox: hot flashes, ovarian enlargement, multiple simultaneous pregnancies |
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MoA & use of tamoxifen
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MoA: estrogen receptor antagonist on breast tissue
Use: tx & prevent recurrence of ER-(+) breast cancer |
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MoA & use of raloxifene
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MoA: estrogen receptor agonist on bone ® reduce resoprtion of bone
Use: tx osteoporosis |
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MoA of oral contraceptives
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Prevent estrogen surge ® no LH surge ® no ovulation
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Contraindications of oral contraceptives
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Smokers > 35y
Hx of thromboembolism Hx of stroke Hx of estrogen-dependent tumor |
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MoA & use of dinoprostone
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MoA: PGE2 analog causing cervical dilation & uterine contraction
Use: Labor induction |
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MoA & use of ritodrine/terbutaline
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MoA: β2-agonsits that relax the uterus
Use: reduce premature uterine contractions (prevent early delivery) |
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MoA & use of tamsulosin
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MoA: α1-antagonist ® inhibit SM contraction; selective for α1A,D receptors (prostate) vs α1B receptors (vascular)
Use: BPH |
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MoA of sildenafil & vardenafil
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Inhibit cGMP phosphodiesterase ® cGMP ® SM relaxation in corpus cavernosum ® blood flow erection
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Tox of sildenafil & vardenafil
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Headache, flushing, dyspepsia
Impaired blue-green color vision Risk of life-threatening hypotension in pts taking nitrates |
