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Cardiovascular

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Nitroglycerin
MECH: NO --> inc cGMP; dilates veins and inc venous capacitance; may also inc O2 supply by dec coronary vasospasm USES: angina, CHF, HTN SE:hypoTN, tachycardia, throbbing headaches (meningeal arterial dilatation), tolerance OTHER: isosorbide dinitrate, isosorbide mononitrate longer-acting oral forms
Nitroprusside
MECH: NO --> inc cGMP; dilates arteries AND veins USES: HTN crises, acute aortic dissection (give with B blocker), decompensated CHF SE: hypoTN, reflex tachycardia; can ppt angina in CAD pts; can cause hypoxemia in COPD pts; cyanide toxicity (inhibition of cellular respiration --> lactic acidosis, arrhythmias, hypoTN, cytotoxic hypoxia); thiocyanate toxicity (weakness, disorientation, psychosis, muscle spasms) CI: hepatic or renal dz OTHER: IV, 30s onset, peak effect 2 min, duration 3 min
Nesitiride
MECH: recombinant BNP USES: short-term tx of decompensated CHF SE: hypoTN OTHER: IV
Hydralazine
MECH: opens K channels(?), dilates arteries USES: HTN (HTN urgency, pregnancy, refractory HTN; NOT first-line); CHF (often in renal failure pts who cannot tolerate ACEI) SE: -headache, nausea, flushing -lupus-like syndrome in 10% -reflex inc HR, renin activity, fluid retention (give with B blocker) OTHER: added to ACEI or ARB in black pts; metabolized by hepatic acetylation
Captopril
MECH: ACEI (reversible); ACE is expressed on endothelial cells in pulmonary and other vascular beds; dilates arteries AND veins; natriuresis USES: HTN, CHF (dec AL and remodeling), diabetic and nondiabetic nephropathy, ischemic HD SE: hypoTN (Na-depleted pts), cough (5%), angioedema, ARF, hyperK CI: renal insufficiency, bilateral renal artery stenosis, pregnancy OTHER: PO
Losartan
MECH: competitive ATII receptor blocker USES: HTN, CHF, diab etic/nondiabetic nephropathy SE: hypoTN (Na-depleted pts), ARF, hyperK; NO cough or angioedema CI: renal insufficiency, bilateral renal artery stenosis, pregnancy
Nifedipine
MECH: dihydropyridine CCB, selective for vascular SM; dilates arteries USES: HTN, primary pulmonary HTN, relief of vasospasm in Prinzmetal's angina and Raynaud's phenomenon, ischemic HD (long-acting preps only) SE: hypoTN, CHF, flushing, headaches, dizziness, peripheral edema CI: short-acting CCB in CAD can --> reflex tachycardia --> angina OTHER: amlopidine, felodipine, etc; nimopidine = 2nd generation lipophilic CCB used after subarachnoid hemorrhages
Verapamil
MECH: CCB that binds to both types of Ca channels; dec HR, dec inotropy, coronary vasoD, mild peripheral arterial vasoD; Class IV antiarrhythmic (dec phase 4 slope, dec rate of rate of phase 0 slope, inc refractoriness at SA and AV nodes) USES: HTN, supraventricular tachycardias (PSVT, AF, AFL), ischemic HD, relief of vasospasm in Prinzmetal's angina, hypertrophic cardiomyopathy SE: heart block, bradycardia, CHF, edema, constipation, inc digitalis levels OTHER: diltiazem
Digoxin
MECH: block Na/K ATPase (inc intracellular Na --> inc intracellular Ca), (+) inotropy, dec sympathetic tone and inc vagal tone - slows impulse conduction through AV node USES: CHF, AF, AFL SE: atrial tachycardias, AV block, dig delirium (nausea, blurred vision, yellow-green hallucinations) CI: hypoK, 2nd or 3rd degree heart block (WPW pts who develop AF: inc impulse transmission through accessory pathway --> VF) OTHER: long t1/2, renal excretion; quinidine, amiodarone, verapamil, NSAIDs can inc serum levels Note: also causes ECG changes - scooping of ST segment, inverted T waves; inc PR, dec QT
Milrinone
MECH: PDE3 inhibitor; inc cAMP --> inc cardiac contractility and dilates arteries AND veins USES: decompensated CHF SE: potentially life-threatening ventricular arrhythmias, hypoTN, hepatotoxicity, thrombocytopenia OTHER: IV; inamrinone, cilostazol (treat claudication)
Sildenafil
MECH: PDE5 inhibitor; inc cGMP --> SM relaxation USES: erectile dysfunction, pulmonary arterial HTN SE: headache, flushing, priapism; potentiates effect of nitrates; blue-tinged vision OTHER: tadalafil, vardenafil have longer t1/2
Epoprostenol
MECH: PGI2 analog --> inc cAMP --> vasoD USES: pulmonary arterial HTN SE: nausea, diarrhea, headache, flushing, jaw pain; infxn from indwelling catheter OTHER: very short t1/2 (3 min), light and temp sensitive
Bosentan
MECH: endothelin antagonist --> vasoD USES: pulmonary arterial HTN SE: headache, facial flushing, leg edema; hepatitis at higher doses, teratogenic OTHER: induces CYP2C9 and CYP3A4 --> dec warfarin levels Note: ET-A mediates vasoC and ET-B mediates vasoD; overall effect of bosentan is vasoD
Procainamide
MECH: class IA antiarrhythmic, MODERATE Na blockade; prolong repolarization; use dependence USES: maintain sinus rhythm in pts with AF, AFL, PSVT; emergent tx of VT and wide-cplx tachycardias SE: -prolong QT interval and potentially proarrhythmic -lupus-like syndrome -hypoTN OTHER: metabolized by N-acetylation -quinidine: moderate anticholinergic effects, can cause cinchonism (GI upset, tinnitus, hemolytic anemia, thrombocytopenia) -disopyramide: marked anticholinergic effects and (-)inotropic properties, used in hypertrophic cardiomyopathy
Lidocaine
MECH: -class IB antiarrhythmic, MILD Na blockade; shortens repolarization (in addition to decreasiing slope of phase 4 and raising threshold) -blocks activated and inactivated, but not resting channels; preferential effect on arrhythmogenic tissue USES: acute ventricular arrhythmias caused by myocardial ischemia, cardiac surgery, digitalis SE: CNS (paresthesias, tremor, nausea, slurred speech, agitation, seizures), mild dec cardiac contractility CI: WPW (can facilitate conduction down bypass tract), severe heart block OTHER -IV, IM, NOT PO -mexiletine (PO)
Flecainide
MECH: class IC antiarrhythmic; MARKED Na blockade; NO effect on repolarization or refractory period USES: supraventricular arrhythmias (AF, WPW) in pts with structurally nl hearts SE: proarrhythmic CI: -preexisting 2nd or 3rd degree heart block -structural HD -pacemakers OTHER: -propafenone: also has class II activity; SE are metallic taste, constipation -moricizine
Amiodarone
MECH: primarily class III (block K channel, prolong repolarization); also has class I, II, IV effects; also vasoD USES: -ventricular arrhythmias (VT, VF) -AF, paroxysmal AF SE: -inc QT interval (torsades de pointes rare) -thyoid dysfct -inc serum transaminases (hepatic injury rare) -pulmonary fibrosis (10-15%) -microcrystalline deposits in cornea and skin -cutaneous photosensitivity (25%)
Ibutilide
MECH: class III antiarrhythmic, prolong repolarization USES: pharmacologic cardioversion of AF or AFL SE: prolong QT internval, torsades de pointes CI: concomitant use of other meds that prolong QT interval (TCAs, phenothiazines) OTHER: -dofetilide (PO) -sotalol: some class II activity
Adenosine
MECH: dec cAMP and inc outward K current --> membrane hyperpolarization and suppression of Ca-dependent APs; dec rate of discharge of pacemaker cells and dec rate of conduction through AV node; dilate coronary and cerebral blood vessels, bronchoconstrict USES: -supraventricular tachyarrhythmias (therapy and dx) -pharmacologic stress tests SE: transient high-grade AV block, flushing, SOB, CP, bronchoconstriction CI: AV block, sick sinus syndrome, ventricular tachycardia OTHER: given IV, t1/2 = 10 s
Which drugs are used to treat pulmonary arterial HTN?
-sildenafil -epoprostenol -bosentan
Which drugs increase cAMP?
-milrinone (PDE3 inhibitor) -epoprostenol
Which drugs increase cGMP?
-nitrates -sildenafil -nesiritide
Which drugs prolong the QT interval?
-procainamide (class IA) -amiodarone (class III) -ibutilide (class III)
Lovastatin, pravastatin, simvastatin, atorvastatin
MECH: inhibit HMG-CoA reductase USES: DEC LDL >>> INC HDL = DEC TG SE: reversible inc LFTs, rhabdomyolysis
Which drugs are proarrhythmic?
-procainamide (class IA) -flecainide (class IC) -milrinone
Niacin
MECH: inhibit lipolysis in adipose tissue; reduce VLDL secretion into circulation USES: DEC LDL = INC HDL >> DEC TG SE: red, flushed face which is dec by aspirin
Cholestyramine, colestipol, colesevelam
MECH: prevent intestinal reabs of bile acids; liver must use XOL to make more USES: DEC LDL SE: GI discomfort, dec abs of fat-soluble vitamins CI: pts with gallstones
Ezetimibe
MECH: prevent XOL reabs at SI brush border USES: DEC LDL SE: rare inc LFTs
Gemfibrozil, clofibrate, bezafibrate, fenofibrate ("fibrates")
MECH: upregulate LPL --> inc TG clearance USES: DEC TG >>> DEC LDL = INC HDL SE: myositis, inc LFTs
Which drugs are used for SUPRAVENTRICULAR arrhythmias?
-procainamide (AF, AFL, PSVT) -flecainide (AF, WPW in pts with structurally nl hearts) -amiodarone (paroxsymal AF) -ibutilide -verapamil -adenosine -digoxin
Which drugs are used for VENTRICULAR arrhythmias?
-procainamide (emergent tx of VT) -lidocaine (acute arrhythmias caused by surgery, dig, myocardial ischemia) -amiodarone (VT, VF)
Which drugs cause a lupus-like syndrome?
-procainamide -hydralazine
Which drugs are used in ischemic HD?
-nifedipine -verapamil -captopril
Which drugs have a short t1/2?
-nitroprusside -epoprostenol -adenosine
Which drugs are used in hypertrophic cardiomyopathy?
-disopyramide -verapamil
Which drugs can cause AV block?
-digoxin -verapamil -adenosine

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