Cardiovascular Module Drug Lists

Card Set Information

Cardiovascular Module Drug Lists
2011-11-21 22:08:00
Ross University Med Medical School s3 s3m3 pharmacology cardiovascular

All the drug lists for the Cardiovascular module and important facts about individual drugs on those lists. Use for name recognition.
Show Answers:

  1. 6 classes of Diuretics and their sites of action
    • Carbonic Anhydrase Inhibitors: proximal tubule
    • Osmotic Diuretics: thin descending loop of Henle
    • Loop Diuretics: thin ascending loop of Henle
    • Thiazides and Congeners: early distal tubule
    • Potassium-Sparing Diuretics: late distal tubule and cortical collecting duct
    • Vasopressin/ADH Antagonists: medullary collecting duct
  2. Two Carbonic Anhydrase inhibitors (diuretics)
    • Acetazolamide: PO, IV; 90% tubular secretion
    • Dorzolamide: topical eye drops; binds CA in RBCs and eliminated over 5 months
    • both drugs bind carbonic anhydrase, preventing bicarb breakdown in the tubule and alkalizing urine
  3. 1 Osmotic diuretic
    Mannitol: freely filtered, not reabsorbed; osmotically draws water out in TDL and PCT
  4. 2 Loop Diuretics
    • Furosemide: can give IM in emergencies, 60% bioavailable
    • Ethacrynic acid: NOT a sulfonamide; 100% bioavailable
    • Both inhibit Na/K/Cl symporter, inhibit macula densa detection of ions; cause alkalosis
  5. 2 Thiazides/cogeners (diuretics)
    • Hydrochlorothiazide: 70% available, T1/2 6-15hr, 100% excreted in urine
    • Indapamide: 93% available, T1/2 16hr, completely metabolized
    • Cause alkalosis; inhibit Na/Cl symporter (NCC) in the DCT; also weak carbonic anhydrase inhibitors (alkaline urine)
  6. 3 Potassium-sparing Diuretics
    • Triamterene: blocks epithelial sodium channel (ENaC) in late DCT and CCT
    • Amiloride: same as triamterene, but lower oral availablility and longer T1/2
    • Spironolactone: aldosterone receptor antagonist; canrenone active metabolite; blocks production of ENaCs and Na/K-ATPases
    • All cause NaCl wasting while sparing K reabsorption; can lead to hyperkalemia, slight acidosis
  7. 2 Vasopressin/ADH antagonists (diuretics)
    • Conivaptan: IV, also hits V1a, helping diuresis
    • Tolvaptan: PO, slightly longer T1/2
    • Both target basolateral V2 receptor in principle cells, downregulating insertion of aquaporin channels
  8. Four classes of Antihypertensives
    • Diuretics: reduce volume, reduce pressure
    • Sympatholytics: regulate sANS signaling (α/β blockers)
    • Vasodilators: lower peripheral resistance
    • Inhibitors/antagonists of Renin-Angiotensin system: block end-effects of angiotensin (ups peripheral resistance, lowers diuresis, vascular/cardiac remodeling)
  9. 4 Diuretics for hypertension
    • Hydrochlorothiazide: 1st line drug, hits biporter
    • Indapamide: 1st line drug, thiazide drug
    • Furosemide: preferred only in malignant hypertension, concomitant chronic kidney disease (loop diuretic)
    • Spironolactone: combine with thiazides to prevent hypokalemia; tx hypertension of hyperaldosteronism
  10. 6 Sympatholytics for hypertension
    • Clonidine: α2 and imidozoline receptor agonist; centrally acting (NTS, rostral ventrolateral medulla)
    • Methyldopa: indirect adrenergic agonist (pre-synaptic neuron metabolizes to α2 agonist)
    • Prazosin: α1 antagonist in resistance and capacitance vessels
    • Propanolol: selective β-block; decrease HR, CO
    • Labetalol: α/β-block; decrease TPR, venous tone
    • Esmolol: similar to labetalol
  11. 8 Vasodilators for hypertension
    • Hydralazine: uncertain MOA,
    • Nitroprusside:
    • Minoxidil: opens arteriole smooth muscle K+ channel, hyperpolarizing membrane
    • Diazoxide: K+ channel opener similar to minoxidil
    • Nifedipine: dihydropyridine Ca2+ channel blocker; see anti-arrythmics
    • Verapamil: class IV Ca2+ channel blocker; see anti-angina
    • Diltiazem: class IV Ca2+ channel blocker; see anti-angina
    • Fenoldopam: D1-dopamine receptor agonist; renal and mesenteric vessel dilator
  12. 4 antihypertensive Renin/Angiotensin modifiers
    • Aliskiren: competitive inhibitor of renin, prevents angiotensinI conversion (rate-limiting step)
    • Captopril: ACE inhibitor; prevents angiotensinI -> angiotensinII conversion
    • Enalapril/enalaprilat: prodrug/metabolite ACE inhibitor
    • Losartan: competitive, selective angiotensinII receptor antagonist
  13. 5 classes of Anti-Arrhythmic Drugs
    • Class I: 3 subclasses (abc), all Na+ channel blockers
    • Class II: β-adrenoreceptor blockers
    • Class III: K+ channel blockers
    • Class IV: Ca2+ channel blockers
    • Miscellaneous: different MOAs
  14. 2 Class Ia anti-arrhythmics
    • Quinidine: blocks activated Na+ channels, at high doses K+, Ca2+, and α1; a-flutter and fib, ectopic vent beats, recurrent suprav- and v-tach
    • Procainamide: Blocks activated Na+ channels, some K+ channels; WPW and arrhythmias when others are poorly tolerated
  15. 3 Class Ib anti-arrhythmics
    • Lidocaine: blocks inactivated > activated Na+ channels; least cardiotoxic; acute vent arrhythmia, digitalis arrhythmias
    • Mexiletine: oral lidocaine analogue for v-tach
    • Phenytoin: mainly inactivated Na+ channel block; digitalis-induced arrhythmias
  16. 1 Class Ic anti-arrhythmic
    Flecainide: blocks activated Na+, some K+ channels; rhythm control of a-flutter, fib, and chronic supravent arrhythmias
  17. 4 Class II anti-arrhythmics
    • Esmolol: used in ICU for short T1/2
    • Metoprolol
    • Sotalol
    • All are selective β1 blockers in cardiac tissue; depress contractility and slow HR; control a-flutter/fib, hypertrophic cardiomyopathy, prophylaxis of v-fib
  18. 3 Class III anti-arrhythmics
    • Amiodarone: K+ channel block, inactivated Na+ channels; most effective antiarrhythmic, used in chronic control, sustained v-tach, and hypertrophic cardiomyopathy; can lead to pulmonary fibrosis, many other toxicities
    • Sotalol: nonselective β-block and K+ channel block; supravent and vent arrhythmias
    • Ibutilide: blocks K+ and causes inward Na+; used only in a-flutter/fib
  19. 3 Class IV anti-arrhythmics
    • Verapamil: see anti-angina
    • Diltiazem: see anti-angina
    • both are activated and inactivated Ca2+ channel blockers used in acute tx of suprav-tach and acute tx, chronic control of a-flutter/fib
  20. 3 Miscellaneous anti-arrhythmics
    • Adenosine: hyperpolarization of SA and AV nodes, decreasing SA automaticity and AV conduction; 1st choice for paroxysmal supravent-tach
    • Magnesium Sulfate: unknown MoA, effective prevention of recurrent torsade de pointes and digitalis induced arrhythmias
    • Digoxin: see drugs for heart failure; useful in a-flutter/fib in cardiac failure where Ca2+ blockers could worsen situation
  21. 5 classes of Heart Failure Drugs
    • Inotropic Drugs: modulate contractility (inotropy) of the heart to affect preload/afterload
    • Renin-Angiotensin-Aldosterone modulators: reduce afterload (angiotensin) and preload (aldosterone); cornerstone tx in all stages of heart failure
    • Diuretics: prevent Na+ and H2O retention to stabilize hemodynamic decompensation
    • β-Blockers: unknown MoA, possibly dangerous due to negative inotropic effect
    • Vasodilators: reduce preload and afterload by reversing vasoconstriction associated with heart failure
  22. 4 Inotropic Drugs for heart failure
    • Digoxin: cardiac glycoside that blocks Na+/K+-ATPase; many actions, but primarily improves efficiency of myocyte contraction, reducing O2 demand in failure
    • Dobutamine: selective β1 agonist, very + inotropy (greater than digoxin) and + dromotropy (conduction velocity)
    • Dopamine: MoA dependent on dose; mid-dose gives + inotropic effects, in addition ot vasodilation from lower doses (D-1 and β1/2 agonist); especially useful in poor renal perfusion
    • Milrinone: inhibitor of specific cardiac phosphodiesterase; leads to + inotropy and peripheral vasodilation
  23. 4 Renin-Angiotensin-Aldosterone modulating drugs for heart failure
    • Captopril: ACE inhibitor (hypertension)
    • Enalaprilat: ACE inhibitor (hypertension)
    • Losartan: AngiotensinII receptor antagonist (hypertension)
    • Spironolactone: aldosterone receptor antagonist, stops ENaC insertion (diuretics); attenuate pathologic remodeling at sub-diuretic doses and synergistic with above 3
  24. 2 Diuretics for heart failure
    • Furosemide: triporter loop diuretic
    • Thiazides: Na/Cl biporter DCT diuretic
    • Main use for these is to prevent water and NaCl retention to reduce preload and edema
  25. 3 β-Blockers for heart failure
    • Metoprolol
    • Carvedilol
    • Bisoprolol
    • NOT A CLASS EFFECT. They decrease HR, reduce myocardial remodeling, inhibit renin secretion, and upreg β1 receptors otherwise downregulated in failure.
    • CARBIME: mnemonic
  26. 3 Vasodilators for heart failure
    • Nitrates: very large reduction in preload/afterload
    • Hydralazine: direct vasodilator, unknown MoA
    • Nesiritide: ANF analogue (recomb brain natriuretic peptide); arteriolar and venous vasodilator
    • Arteriolar dilators preferred in 1* low CO
    • Venous dilators preferred in 1* pulmonary congestion
    • Losartan, Milrinone, and Captopril also considered vasodilators
  27. 5 classes of Anti-Hyperlipidemic drugs
    • HMG-CoA inhibitors: prevents mevalonic acid formation (rate-limiting step)
    • Bile Acid Binding Resins: increase excretion of bile acids by up to 10x
    • VLDL Secretion Inhibitors: prevent lipolysis in adipose tissue
    • Fibric Acid Derivatives: activate nuclear transcription receptor PPAR-α, increasing LPL synth and VLDL hydrolysis
    • Intestinal Sterol Absorption Inhibitors: selectively inhibits absorption of sterols at small intestine brush border
  28. 1 HMG-CoA Inhibitor for hyperlipidemia
    • Lovastatin: 20-55% drop of LDL, 10-35% drop of triglycerides, 5-10% increase in HDL
    • includes any drug with '-statin'
    • Good for high cholesterol or LDL, atherosclerosis, prevention of coronary artery disease and stroke
  29. 1 Bile-Acid Binding Resin for hyperlipidemia
    • Cholestyramine: 10-35% reduction of LDL; little effect on HDL, VLDL, or triglycerides
    • all resins basically just bind and remove cholesterol from the GI tract
    • Good for all isolated increases of LDL
  30. 1 VLDL Secretion Inhibitor for hyperlipidemia
    • Niacin: 15-25% drop of LDL, 15-40% drop of VLDL, 30-50% drop of triglycerides, and 15-30% bump of HDL
    • Strongly inhibits adipose lipolysis and reduces catabolism of apo-A1 from HDL
    • Good high VLDL, LDL, and low HDL
  31. 1 Fibric Acid Derivative for hyperlipidemia
    • Gemfibrozil: 30-60% drop of triglycerides, 20-30% drop of VLDL, 5-10% bump of HDL, and variable effect on LDL
    • Drug of choice for Hyperlipoproteinemia Type III
  32. 1 Intestinal Sterol Absorption Inhibitor for hyperlipidemia
    • Ezetimibe: 15-20% drop of LDL, 5-8% drop of triglycerides, 16% drop of Apo-B, little effect on HDL
    • Used for hyperlipidemias in conjunction with statins
  33. 3 classes of Anti-Anginal Drugs
    • Nitrates and Nitrites: marked relaxation of large veins and large arteries to lesser extent, decreasing preload and afterload respectively
    • Ca2+ Channel Blockers: cause vasodilation (decrease afterload), decrease conduction, automaticity, and contractility, and increase refractoriness
    • β-Adrenoreceptor Blockers: reduction in heart rate, contractility, and blood pressure lead to decreased O2 demand and increase subendocardial perfusion
  34. 3 Nitrates/Nitrites for angina
    • Amyl Nitrite: 3-5min duration
    • Nitroglycerin: many RoA with variant onset and duration
    • Isosorbide Mononitrate: oral RoA, 15-40min onset with 6-10hr duration
  35. 2 Subclasses of Ca2+ Channel Blockers for angina
    • Dihydropyridines: selectively block vessel Ca2+ channels (no direct cardiac action)
    • Others: block Ca2+ channels in heart and vessels (nonselective)
    • Also good for Raynaud's phenomenon
  36. 2 Dihydropyridines for angina
    • Nifedipine: high vascular selectivity
    • Nicardipine: very high vascular selectivity
    • Both Ca2+ channel blockers; decrease afterload; also dilate cerebral vessels, inhibiting delayed reactive vasospasm from subarachnoid hemorrhage
  37. 3 "other" Ca2+ channel blockers for angina
    • Verapamil: low vascular selectivity
    • Diltiazem: low vascular selectivity; improves diastolic compliance
    • Bepridil: no selectivity
    • All have cardiac effects in addition to vascular effects
  38. 3 β-Blockers for angina
    • Propanolol: nonselective β-blockade
    • Metoprolol: selective β1-blockade
    • Atenolol: selective β1-blockade