Anti-HTN Drugs

Question 1

Captopril / Enalapril / Lisinopril

Answer 1

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

Question 2

Losartan / Valsartan

Answer 2

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

Question 3

Aliskiren

Answer 3

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)

Question 4

Verapamil

Answer 4

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

Question 5

Diltiazem

Answer 5

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

Question 6

Amlodipine / Nifedipine

Answer 6

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)

Question 7

Propranolol

Answer 7

Non-selective β1 and β2 antagonist

Question 8

Metoprolol / Atenolol

Answer 8

Selective β1 antagonist

*most widely used

Question 9

Pindolol

Answer 9

Non-selective β1 and 2 partial agonist w/ intrinsic sympathomimetic activity
*preferred β blocker in pregnancy

Question 10

Prazosin / Doxazosin

Answer 10

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

Question 11

Labetalol

Answer 11

Mixed α and β blockers
Use: HTN emergencies, safe in pregnancy
SE: orthostatic hypotension (first use or high doses)

Question 12

Clonidine

Answer 12

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

Question 13

Methyldopa

Answer 13

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

Question 14

Hydralazine

Answer 14

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)

Question 15

Minoxidil (Rogaine)

Answer 15

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)

Question 16

Epoprostenol

Answer 16

Synthetic PGI2
MOA: 👇🏽peripheral, pulmonary and coronary resistance
PK: given fia continuous infusion
AE: flushing, HA, jaw pn, diarrhea, arthralgias

Question 17

Bosentan

Answer 17

Nonselective endothelin receptor blocker
MOA: blocks initial transient depressors (ETa) and prolonged pressure (ETb) responses to endothelin
Pregnancy category X

Question 18

Sildenafil

Answer 18

PDE5 inhibitor 
MOA: increased cGMP
Effects: smooth muscle relaxation
SE: HA, flushing, dyspepsia, cyanopsia
Contra: nitrates

Question 19

Sodium Nitroprusside

Answer 19

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

Question 20

Labetalol

Answer 20

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

Question 21

Fenoldopam

Answer 21

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

Question 22

Nicardipine

Answer 22

Ca2+ channel blocker
PK: given IV, t1/2 = 30 min
SE: reflex tachycardia

Question 23

Nitroglycerin

Answer 23

Vasodilator
*DOC for HTN emergency in pt w/ cardiac ischemia or angina, or after CABG
PK: t1/2 = 2-5 min
SE: hypotension

Question 24

Diazoxide

Answer 24

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

Question 25

Phentolamine

Answer 25

*DOC for pt w/ catecholamine-related HTN emergency

Question 26

Esmolol

Answer 26

Use: aortic dissection or post-op HTN

Question 27

Hydralazine

Answer 27

DOC in tx HTN emergency in pregnancy related to eclampsia

Question 28

Enalapril

Answer 28

Enalaprilat is active drug metabolite

Question 29

ACE Inhibitors Use

Answer 29

HTN (+ diuretic), CHF, nephropathy pt, s/p MI

Question 30

ACE Inhibitors SE

Answer 30

Dry cough, hyperkalemia, hypotension, angioedema, acute renal failure (in pt w/ b/l renal artery stenosis), rash, fever, AMS

Question 31

Losartan (re: gout)

Answer 31

Reduces plasma uric acid levels by inhibiting URAT1 transporter
*can be useful in tx pt w/ Gout

Question 32

β-blockers

Answer 32

“-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

Question 33

Doxazosin SE

Answer 33

shown to increase rate of CHF