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Cardic drugs
Question | Answer | |
---|---|---|
Diltiazem, verapamil | Ca+2 channels blockers (non-dihydropyridines) block the voltage gated L type Ca+2 channels of cardiac muscles | Heart: verapamil> diltiazem> amlodipine= nifedipine Uses: HT, angina, atrial fibrilation/fluttter S.E: cardiac depression, AV block, Hyperprolactenemia, constipation |
Hydralazine | Antihypertensive increase cGMP--> s.m. relaxation Vasodilates arterioles>veins --> decrease afterload | Severe HT(acute) HF(with organic nitrate). SAFE TO USE DURING PREGNANCY. Freq coad. with beta blocker to prevent Reflex tachycardia. S.E: compensatory tachycardia, fluid retention, headache, angina, Lupus like syndrome |
Nitroprusside | Antihypertensive in emergency Short acting---: increase cGMP via direct release fo NO. Venous and arterial vasodilator--> decrease PL and AL | |
Fenoldopam | Dopamine 1 receptor agonist--> coronary, peripheral, renal and splachnic vasodilation---> decrease BP and increase natriuresis. | Antihypertensive used postoperatively S.E: hypotension and tachycardia |
Nitroglycerin, isosorbide dinitrate, isosorbide mononitrate | Nitrates vasodilates by increase NO in vascular smooth m. --> increase cGMP and s.m. relaxation Dilate veins>>arteries--> decrease PL | Uses: angina. acute coronary syndrome, pulmonary edema. S.E.: Reflex tachycardia(tx with Beta blockers), hypotension, flushing, headache, Monday dx--industrial exposure---> development of tolerance over week and loss of tolerance-->tachycardia, dizziness |
Ranolazine | inhibits the late phase of Na current thereby reducing diastolic wall tension and O2 consumption. Does not affect HR and contractility | Uses: angina refractory to other medical therapies. S.E: constipation, dizziness, headache, nausea, QT prolongation |
Milrinone | Selective PD- inhibitor In cardiac cells: increase cAMP accumulation--> increase Ca influx--> increase inotropy and chronotropy vascular s.m-->increase cAMP accumulation--> inhibition of MLCK activity---general vasodilation. | Uses: short term use in acute decompensated HF S.E: arrhythmias, hypotension |
lovastatin, pravastatin | HMG-CoA reductase inhibitors inhibits conversin of HMG-CoA to mevalonate---cholesterol precursor Decrease mortality in CAD pts | Decrease LDL; increase HDL and decrease TG S.E: hepatotoxicity; myopathy (when is combined with fibrates or niacin) |
Cholestyramine, colestipol, colesvelam | Bile acids resins prevents intestinal reabsorption of bile acids--liver must use cholesterol to make more | Decrese LDL; slightly increase HDL and TG S.E: GI upset, decrease absorption of other drugs and fat soluble vitamins |
Ezetimibe | Prevent cholesterol absorption at small intestine brush border | Decrese LDL, increase HDL and TG Rare increase LFTs, diarrhea |
Gembfibrozil, bezafibrate, fenofibrate | Fibrates (inhibits cholesterol 7alpha hydroxylase) upregulate LPL--increase TG clearance activates PPAR-alpha to induce HDL synthesis | decrease LDL; increase HDL, decrease greatly TG Myopathy( increase risk with statins) cholesterol gallstones. Pts with very high TG (>150), this medication would be inappropriate |
Niacin ( vitamin B3) | inhibits lipolysis(hormone sensitve lipase) in adipose tissue---> reduces hepatic VLDL synthesis | decrease LDL; increase HDL; decrease TG Red, flushed face, which in decrease by NSAIDs or long term use HYperglycemia HYperuricemia |
Airocumab Evolocumab | PCSK9 inhibitors inactivation of LDL receptor degradation---> increase amount of LDL removed from bloodstream | Decrease greatly LDL; increase HDL and decrease TG S.E: myalgias, delirium, demetia, other neurocognitive effects |
Digoxin | Cardiac glycoside direct inhibition of Na/K ATPase indirect inhbition of Na/Ca exchanger---increase Ca intracellular--- + inotropy STIMULATES VAGUS N. ---> HR | Uses: HF(increase contractility); AF(decrease conduction at AVN and depression of SAN) SE: Cholinergic(nausea, vomiting, diarrhea, blurry yellow vision, arrhythmia, AV block) Can predispose to hyperkalemia---indicates poor px. |
Factors that predispose digoxin toxicity | renal failure(decrease excretion) hypokalemia(permissive for digoxin binding at K binding site on Na/K ATPase) displacement of digoxin:verapamil, amiodarone, quinidine | antidote: slowly normalize K, cardiac pacer, anti digoxin Fab fragments, Mg |
Antiarrhythmics Na channel blockers (class 1) | Mechanism | slow or block conduction (especially in depolarized cells) Decrease slope of phase 0 depolarization. Are state dependent (selectively depress tissue that is frequently depolarized eg tachycardia) NA CHANNEL BINDING STRENGTH: 1C>1A>1B |
Quinidine, Procainamide, Disopyramide | Class IA Block the Na channels in phase )---leading to increase AP duration, ERP in ventricular action potential. Increase QT interval(torsade de pointes), some K channels blocking effects. | Uses: Atrial and ventricular arrhythmias---especially re-entrant SVT and VT SE: Cinchonism(headache, tinnitus, blurred vision, disorientation, psychosis-->Quinidine) Reversible SLE-like syndrome--> procainamide;HF--->disopyramide,Thrombocytopenia |
Lidocaine, Mexiletine | Class IB Blockade of Na channels---decrease AP; preferentially affect ischemic or depolarized Purkinje and ventricular tissue. Shortens Phase 3 (repolarization) Phenytion can also fall in this category. | Uses: Acute ventricular arrhythmias (post MI), digitalis induced arrhythmias SE: CNS stimulation/ depression, CV depression |
Flecainide, Propafenone | Class IC.Prolongs ERP in AV node and accessory bypass tract. NO EFFECT on ERP in Purkinje and Ventricular tissue. Minimal effect on AP duration. Prolong QRS duration.SLOW DISSOCIATION FROM NA CHANNELS ALLOW THE BLOCKING EFFECT TO ACCUMULATE | Uses: SVTs including including atrial fibrillation. ONLY as last resort in refractory VT. SE: Proarrhythmic---> especially post-MI (contraindicated). |
Beta blockers Metoprolol(dyslipidemia), propranolol(exarcerbate Prinzmetal angina), esmolol, atenolol, timolol, carvedilol | Antiarrhythmics class II Decrease SA and AV nodal activity by decrease cAMP, Ca currents. Suppress abnormal pacemaker by decrease slope of phase 4. AV node particularly sensitive--> increase PR internal. Overdose: saline, atropine, glucagon | Uses: SVT, ventricular rate control for atrial fibrillation and atrial flutter. SE: Impotence, exacerbation of asthma and COPD, bradycardia,AVblock, HF, mask hypoglycemia. No use in cocaine overdose or pheochromocytoma(alone) |
Amiodarione, Ibutilide, Dofetilide, Sotalol | Antiarhythmics class III Block K channels---> increase AP duration, ERP, QT interval | Uses: AF, A flutter, Ventricular tachycardia(sotalol, amiodarone) SE: Sotalol--torsades de pointes, excessive beta blockade Ibutilide--torsade de pointes Amiodarone-- Pulmonary fibrosis, hepatotoxicity, hypo/hyperthyroidism(act as hapten) |
Verapamil, diltiazem | Antiarrhythmics class IV Block Ca channels---> decrease conduction velocity, increase ERP and PR interval | Uses: Prevention of nodal arrhythmias, rate control in atrial fibrillation S.E: Constipation, flushing, edema, CV effects( HF, AV block, sinus node depression) |
Adenosine | Efflux of K---hyperpolarizing the cell and decrease Ca, decrease AV node conduction. Effects blunted by theophylline and caffeine (both are adenosine receptor antagonist) | DOC in dx/terminating certain forms of SVT. Very short acting(15 sec) SE: flushing, hypothyroidism, hypotension, chest pain, sense of impending doom, bronchospasm. |
Mg2+ | Effective in torsades de pointes and digoxin toxicity | |
Ivabradine | Selective inhibition of funny Na channels-- prolonging slow depolarization phase (phase 4), decrease SA node firing; negative chronotropic effect without inotropy. Reduces cardiac O2 requirement. | Uses: Chronic stable angina in pts who cannot take beta blockers. Chronic HF with reduced ejection fraction. SE: Luminous phenomena? visual brightness, HT, bradycardia. |
Amlidipine, clevidipine, nicardipine, nifedipine | Ca+2 channels blockers (dihydropyridines) block the voltage gated L type Ca+2 channels of smooth muscle | Amlodipine=nifedipine Uses: Hypertension, angina, Raynaud phenomenon Nimodipin: subarachnoid hemorrhage(prevents cerebral vasospam) Nicardipine, clevidipine: Hypertensive urgency or ER S.E: Peripheral edema, flushing, dizziness, gingival hyperplasia |