Antihypertensives Flashcards
What are the first line agents, second line agents and other agents for treatment of HTN?
First-line agents:
- ACE-inhibitors, ARBs, calcium channel blockers, thiazide diuretics
Second-line agents:
- B-blockers, aldosterone antagonists
Other agents:
- Loop diuretics, alpha-blockers, direct vasodilators, central alpha2-agonists, renin inhibitors
ACE inhibitors
Captopril, Enalapril, Lisinopril
MOA: inhibition of ACE enzyme preventing conversion of angiotensin I to angiotensin II (also prevent bradykinin degradation)
CE: Catopril will decrease PVR; Enalapril/Lisinopril decrease Na+ and H2O retention
CA: perserve renal function in diabetic/non-diabetic nephropathy pts; Captopril HTN; Enalapril heart failure; Lisinopril post MI
AE: dry cough, angioedema, hyperkalemia, hypotension, rash, fever, altered taste
TCo: pregnancy, bilateral renal artery stenosis
Angiotensin Receptor Blockers (ARB’s)
Losartan
MOA: block angiotensin II type 1 receptors
CE: decrease PVR, Na+ and H2O retention
CA: HTN, heart failure, post MI
AE: hyperkalemia, hypotension, rash, fever, altered taste
TCo: pregnancy, bilateral renal artery stenosis
Renin Inhibitor
Aliskirin
MOA: renin inhibitor
CE: decrease PVR, Na+ and H2O retention
CA: alternative agent in HTN (3rd line)
AE: hyperkalemia, hypotension, rash, fever, altered taste
TCo: pregnancy, bilateral renal artery stenosis
Calcium Channel Blockers
Amlodipine, Nifedipine; Diltiazem, Verapamil
MOA: inhibit vascular L-type Ca2+ channels; inhibit vascular and cardiac L-type Ca2+ channels
CE: Amlodipine/Nifedipine (Dihydropyridine) decrease PVR; Diltiazem/Verapamil decrease PVR, inotropy, chronotropy
CA: Dihydropyridine HTN, angina; Diltiazem/Verapamil HTN, angina, supraventricular tachyarrhythmias, migraine, cerebral vasospasm
AE: Dihydropyridine reflex tachycardia, peripheral edema, hypotension, gingival hyperplasia, fatigue, flushing; Verapamil constipation, negative inotropic effects
TCo: Verapamil pts taking B-blockers, 2nd/3rd degree heart block, or severe left ventricular dysfunction
Diuretics (in general)
Thizide, Loop, K+ sparing
MOA:
CE: decrease PVR, Na+ and H2O retention
CA: HTN, CHF, edema
AE: hypotension, hyponatremia, hypokalemia (hyperkalemia if K+ sparing)
Beta-Blockers
Propanolol (B1/2), Metoprolol (B1), Atenolol (B1), Pindolol (B1/2P)
MOA: antagonist at B-receptors
CE: decrease inotropy, chronotropy, renin secretion (decrease PVR and Na+ and H2O retention)
CA: HTN, angina, heart failure, arrhythmias
AE: airway constriction (Propanolol), bradycardia, CNS effects (fatigue, sexual dysfunction, ect.), disrupt lipid metabolism decrease in HDL/increase in TAGs, mask signs of hypoglycemia in diabetics
TCo: pt taking CCB, 2nd/3rd degree heart block, or severe left ventricular dysfunction; Propanolol asthmatics and COPD; cant stop abruptly becasue of rebound HTN
Alpha-1 Antagonists
Prazosin, Doxazosin
MOA: antagonist at a1-receptors
CE: decrease PVR
CA: HTN, Benign Prostatic Hyperplasia
AE: orthostatic hypotension (first use), diziness, drowsiness, nausea
Alpha and Beta Blockers
Lavetalol
MOA: antagonists at alpha-1 and beta-1 receptors
CE: decrease in PVR, inotropy, chornotropy
CA: HTN, hypertensive emergencies
AE: orthrostatic hypotension
Central Alpha-2 Agonist
Clonidine, Methyldopa
MOA: agonist at alpha-2 receptors
CE: decrease sympathetic outflow, PVR, inotropy, chronotropy
CA: HTN, hypertensive emergencies
Direct Vasodilators
Hydralazine, Minoxidil
MOA: arterial vasodilators (smooth muscle relaxants)
CE: decrease PVR
CA: HTN, hypertensive emergencies
AE: fluid retention, reflex tachycardia; Hydralazine reversible lupus-like syndrome; Minoxidil hypertrichosis
What are the drugs used to treat pulmonary HTN?
- Prostaglandins (Epoprostenol)
- Enothelin Synthesis and Receptor Blocker (Bosentan)
- Phosphodiesterase 5 Inhibitor (Sildenafil)
Prostaglandins
Epoprostenol
MOA: synthetic PGI2
CE: decrease peripheral pulmonary and coronary resistance
CA: pulmonary HTN
AE: flushing, headache, jaw pain, diarrhea, arthralgias
Endothelin Receptor Blocker
Bosentan
MOA: blocks ETA and ETB responses to endothelin
CE: decrease pulmonary resistance
CA: pulmonary HTN
AE: anemia, hepatotoxicity
TCo: pregnancy (Cat X)
Phosphodiesterase 5 Inhibitor
Sildenafil
MOA: inhibit PDE5 to increase cGMP levels > smooth muscle relaxation
CE: decrease pulmonary resistance
CA: pulmonary HTN, erectile dysfunction
AE: headache, flushing, dyspepsia, cyanopsia
TCo: nitrates