Anti-HTN Drugs Flashcards
Captopril / Enalapril / Lisinopril
ACE Inhibitors
MOA: prevent conversion of angiotensin I to II =👇🏽BP by 👇🏽PVR
Effects: decrease afterload, prevent Na+ and H2O retention by dec release of aldosterone
*👆🏽bradykinin levels = dry cough
Losartan / Valsartan
Angiotensin Receptor Blockers (ARBs)
*First-line agents
MOA: blocking angiotensin II type 1 receptors, block aldosterone secretion
Effects: 👇🏽BP by causing arteriolar and venous dilation, decrease Na+ and H2O retention
Aliskiren
Renin inhibitor
MOA: inhibits renin prevents conversion of angiotensinogen to angiotensin I
Effects:👇🏽production of angiotensin II and aldosterone
SE: hyperkalemia, hypotension, acute renal failure (NO dry cough)
Verapamil
MOA: Ca2+ channel blocker (non-dihydropyridines)
Use: angina, supraventricular tachyarrhythmias, HTN, migraine and cerebral vasospasm
SE: constipation, negative inotropic effects, gingival hyperplasia
Contra: pt’s taking β-blockers, or who have 2nd or 3rd degree AV block, or severe LV systolic dysfunction
Diltiazem
MOA: Ca2+ blocker (non-dihydropyridine)
Use: angina, HTN, SVT, cerebral vasospasm
Contra: pt’s taking β-blockers, or who have 2nd or 3rd degree AV block, or severe LV systolic dysfunction
Amlodipine / Nifedipine
Ca2+ blockers (dihydropyridines)
MOA: reduce Ca2+ entry into smooth muscle to cause coronary and peripheral vasodilation and lower BP
Use: HTN, angina
*higher affinity for vascular Ca2+ channels than for cardiac Ca2+ channels
SE: hypotension, pedal edema, dizziness, HA, fatigue, gingival hyperplasia, flushing, reflex tachycardia (esp in short-acting preparations)
Propranolol
Non-selective β1 and β2 antagonist
Metoprolol / Atenolol
Selective β1 antagonist
*most widely used
Pindolol
Non-selective β1 and 2 partial agonist w/ intrinsic sympathomimetic activity
*preferred β blocker in pregnancy
Prazosin / Doxazosin
Competitive α1 blockers
MOA: relaxing arterial and venous smooth muscle
Effects:👇🏽arterial BP by 👇🏽PVR w/ no long-term tachycardia, no Na+ and H2O retention
Use: BPH
SE: orthostatic hypotension (leads to syncope) upon first-dose or Lg increase in dose, dizziness/drowsiness/HA/nausea/palpitations
Labetalol
Mixed α and β blockers
Use: HTN emergencies, safe in pregnancy
SE: orthostatic hypotension (first use or high doses)
Clonidine
Central α2 agonist
MOA: activation of α2 causing reduce in SANS outflow
Effects: 👇🏽BP d/t 👇🏽PVR and CO, spares renal blood flow and GFR
Use: HTN management and HTN crisis
SE: rebound HTN following abrupt withdrawal, drowsiness/xerostomia/dizziness/HA/sexual dysfunction
Methyldopa
Central α2 agonist
MOA: diminish SANS outflow
Effects: 👇🏽BP d/t 👇🏽PVR (but NO👇🏽in CO, and spares renal blood flow and GFR)
Use: DOC in pregnancy-induced HTN
SE: +ve Coomb’s Test, sedation/drowsiness/nausea/HA/weakness/fatigue/sexual dysfunction/nightmares/vertigo
Hydralazine
Direct vasodilator
MOA: arteriolar dilation
Use: pregnancy included HTN / pre-eclampsia, last-line therapy for HTN management
SE: fluid retention and reflex tachycardia, SLE-like syndrome, HA/nausea/sweating/flushing
*usually administered w/ β-blocker and thiazide (oral or IV)
Minoxidil (Rogaine)
Direct vasodilator
MOA: vasodilation of arterioles
Use: oral tx for severe malignant HTN
SE: hypertrychosis, reflex tachycardia and fluid retention (combine w/ Loop diuretic and β-blocker)
Epoprostenol
Synthetic PGI2
MOA: 👇🏽peripheral, pulmonary and coronary resistance
PK: given fia continuous infusion
AE: flushing, HA, jaw pn, diarrhea, arthralgias
Bosentan
Nonselective endothelin receptor blocker
MOA: blocks initial transient depressors (ETa) and prolonged pressure (ETb) responses to endothelin
Pregnancy category X
Sildenafil
PDE5 inhibitor MOA: increased cGMP Effects: smooth muscle relaxation SE: HA, flushing, dyspepsia, cyanopsia Contra: nitrates
Sodium Nitroprusside
DOC for HTN emergency
PK: t1/2 = 1-2min req continuous infusion
MOA: prompt vasodilation by direct effect on arterial and venous smooth muscle
SE: cyanide toxicity, hypotension (OD), goose bumps, abd cramping, N/V, HA
Labetalol
Combined α and β blocker
PK: given IV bolus or infusion, t1/2 = 3-6h
Contra: asthma, COPD, 2nd or 3rd degree AV block or bradycardia
Fenoldopam
Peripheral D1 agonist MOA: arteriolar dilation PK: given IV, t1/2 = 30 min Action: maintains or increases renal perfusion as lowers BP, promotes naturesis Contra: glaucoma
Nicardipine
Ca2+ channel blocker
PK: given IV, t1/2 = 30 min
SE: reflex tachycardia
Nitroglycerin
Vasodilator
*DOC for HTN emergency in pt w/ cardiac ischemia or angina, or after CABG
PK: t1/2 = 2-5 min
SE: hypotension
Diazoxide
Arteriolar dilator
MOA: prevents vascular smooth muscle contraction by opening K+ channels and stabilizing membrane potential
PK: t1/2 = ~24h
SE: hypotension, reflex tachycardia, Na+ and H2O retention
Use: inhibits insulin release and can be used to tx hypoglycemia 2° to insulinoma
Phentolamine
*DOC for pt w/ catecholamine-related HTN emergency
Esmolol
Use: aortic dissection or post-op HTN
Hydralazine
DOC in tx HTN emergency in pregnancy related to eclampsia
Enalapril
Enalaprilat is active drug metabolite
ACE Inhibitors Use
HTN (+ diuretic), CHF, nephropathy pt, s/p MI
ACE Inhibitors SE
Dry cough, hyperkalemia, hypotension, angioedema, acute renal failure (in pt w/ b/l renal artery stenosis), rash, fever, AMS
Losartan (re: gout)
Reduces plasma uric acid levels by inhibiting URAT1 transporter
*can be useful in tx pt w/ Gout
β-blockers
“-olol”
Use: add-on therapy to first line agents in primary prevention pt’s
*first-line only in pt’s w/ CAD, CHF or post-MI
Doxazosin SE
shown to increase rate of CHF
