Antihypertensives Flashcards

1
Q

What are the first line agents, second line agents and other agents for treatment of HTN?

A

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
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2
Q

ACE inhibitors

A

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

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3
Q

Angiotensin Receptor Blockers (ARB’s)

A

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

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4
Q

Renin Inhibitor

A

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

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5
Q

Calcium Channel Blockers

A

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

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6
Q

Diuretics (in general)

A

Thizide, Loop, K+ sparing

MOA:

CE: decrease PVR, Na+ and H2O retention

CA: HTN, CHF, edema

AE: hypotension, hyponatremia, hypokalemia (hyperkalemia if K+ sparing)

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7
Q

Beta-Blockers

A

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

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8
Q

Alpha-1 Antagonists

A

Prazosin, Doxazosin

MOA: antagonist at a1-receptors

CE: decrease PVR

CA: HTN, Benign Prostatic Hyperplasia

AE: orthostatic hypotension (first use), diziness, drowsiness, nausea

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9
Q

Alpha and Beta Blockers

A

Lavetalol

MOA: antagonists at alpha-1 and beta-1 receptors

CE: decrease in PVR, inotropy, chornotropy

CA: HTN, hypertensive emergencies

AE: orthrostatic hypotension

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10
Q

Central Alpha-2 Agonist

A

Clonidine, Methyldopa

MOA: agonist at alpha-2 receptors

CE: decrease sympathetic outflow, PVR, inotropy, chronotropy

CA: HTN, hypertensive emergencies

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11
Q

Direct Vasodilators

A

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

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12
Q

What are the drugs used to treat pulmonary HTN?

A
  • Prostaglandins (Epoprostenol)
  • Enothelin Synthesis and Receptor Blocker (Bosentan)
  • Phosphodiesterase 5 Inhibitor (Sildenafil)
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13
Q

Prostaglandins

A

Epoprostenol

MOA: synthetic PGI2

CE: decrease peripheral pulmonary and coronary resistance

CA: pulmonary HTN

AE: flushing, headache, jaw pain, diarrhea, arthralgias

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14
Q

Endothelin Receptor Blocker

A

Bosentan

MOA: blocks ETA and ETB responses to endothelin

CE: decrease pulmonary resistance

CA: pulmonary HTN

AE: anemia, hepatotoxicity

TCo: pregnancy (Cat X)

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15
Q

Phosphodiesterase 5 Inhibitor

A

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

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16
Q

What drugs are used for treatment of hypertensive emergency?

A
  • Sodium Nitroprusside (arterial and venous dilator)
  • Labetalol (A1 and B1 blocker)
  • Fenoldopam (dopamine agonsit)
  • Nicardipine (calcium channel blocker)
  • Nitroglycerin (mostly venous vasodilator)
  • Diazoxide (potassium channel activator)
  • Phentolamine (non-selective alpha agonist)
  • Esmolol (beta1 blocker)
  • Hydralazine (arteriolar vasodilator)
17
Q

What are the two nitrates?

A

Sodium Nitroprusside, Nitroglycerin

18
Q

Sodium Nitroprusside

A

MOA: direct vasodilator

CE: peripheral vasodilator (arterial and venous smooth muscle)

CA: hypertensive emergencies

AE: hypotension, reflex tachycardia, cyanide toxicity, abdominal cramping, nausea, vomiting

TCo: hypotension

19
Q

Nitroglycerin

A

MOA: direct vasodilator

CE: peripheral vasodilator (mainly venous)

CA: hypertensive emergencies in pts with cardiac ischemia or angina, or after bypass surgery

AE: hypotension

20
Q

Dopamine Agonist

A

Fenoldopam

MOA: agonist at D1 receptors

CE: arteriolar dilation, maintains renal perfusions as BP lowers

CA: hypertensive emergencies

AE: hypotension

TCo: glaucoma

21
Q

Nicardipine

A

MOA: inhibits vascular L-type Ca2+ channels

CE: decrease in PVR

CA: hypertensive emergencies

AE: hypotension, refelx tachycardia

22
Q

Potassium Channel Activator

A

Diazoxide

MOA: opens K+ channels, stabilizes membrane potential preventing smooth muscle contraction

CE: arteriolar dilation

CA: hypertensive emergencies

AE: hypotension, reflex tachycardia, Na+ and H2O retention, inhibiton of insulin relase

23
Q

Non-selective Alpha Antagonist

A

Phentolamine

MOA: antagonist of alpha1/2 receptors

CE: decrease PVR

CA: catecholamine-related hypertensive emergencies

AE: orthostatic hypotension, dizziness, drowsiness, nausea

24
Q

Esmolol

A

MOA: short acting B1 receptor antagonist

CE: decrease inotropy, chornotropy, renin secretion, PVR, Na+ and H2O retention

CA: aortic dissection or p/o hypertension

AE: bradycardia, CNS effects (fatigue, sexual dysfunction, ect.), mask signs of hypoglycemia in diabetics

TCo: pts taking CCBs, 2nd/3rd degree heart block, or severe left ventricular dysfunction

25
Q

Cardiac Glycoside

A

Digoxin

MOA: inhibition of Na+/K+ ATPase and vagal stimulation

CE: increase inotropy, decrease chronotropy

CA: add on therapy to improve heart failure symptoms but not survival; A-fib; 1st line for A-fib + Heart failure

AE: arrhythmias, nausea, vomiting, anorexia, headache ,fatigue, confusion, alteration of color perception (yellow/green hues), blurred vision

TCo: diastolic or right sided heart failure, uncontrolled HTN, bradyarrhythmias, non-responders/interolerant pts, increased toxicity in pts with hypokalemia

26
Q

What are the 4 inotropic agents used to treat acute heart failure?

A
  • Phosphodiesterase III Inhibitors (Inamrinone, Milrinone)
  • Dopamine
  • Dobutamine
  • Glucagon
27
Q

Phosphodiesterase III Inhibitors

A

Inamrinone, Milrinone

MOA: inhibit myocardial cAMP PDE activity > increase cAMP

CE: increase inotropy and chronotropy leading to increase in CO, decrease preload and afterload

CA: short-term therapy for patients with intractable heart failure

AE: arrhythmias, HTN, angiona thrombocytopenia

28
Q

Dopamine

A

MOA: activates dopaminergic and adrenergic receptors

CE: increase inotropy and chronotropy leading to increase in CO, renal vasodilation at therapeutic doses

CA: shock (which persists after fluid replacement)

AE: high doses can cause vasoconstriction

29
Q

Dobutamine

A

MOA: at therapeutic doses major effects is B1 receptor stimulation

CE: increase inotropy and chronotropy leading to increase in CO

CA: acute managment of heart failure

AE: HTN, angina, arrhythmias

30
Q

Glucagon

A

MOA: stimulates adenylyl cyclase > cAMP

CE: increase inotropy and chronotropy > increase CO

CA: B-blockers overdosage

AE: HTN, angina, arrhythmias