Antihypertensive agents Flashcards

1
Q

Hydrochlorothiazide, chlorthalidone

A
  • MOA
  • thiazide diuretic
  • block Na/Cl transporter in renal distal convoluted tubule
  • Effects
  • reduce blood volume and poorly understood vascular effects
  • Clinical
  • hypertension
  • mild heart failure
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2
Q

Furosemide

A
  • MOA
  • loop diuretic
  • block Na/K/2Cl transporter in renal loop of henle
  • Effects
  • like thiazides, greater efficacy
  • Clinical
  • severe hypertension
  • heart failure
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3
Q

Spironolactone, eplerenone

A
  • MOA
  • diuretic
  • block aldosterone receptor in renal collecting tubule
  • Effects
  • increase Na and decrease K excretion
  • poorly understood reduction in heart failure mortality
  • Clinical
  • aldosteronism
  • heart failure
  • hypertension
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4
Q

Clonidine, methyldopa

A
  • Centrally acting sympathoplegic
  • MOA
  • activates α2 adrenoceptors
  • Effects
  • reduce central sympathetic outflow
  • reduce NE release from noradrenergic nerve endings
  • Clinical
  • hypertension
  • clonidine also used in withdrawal from abused drugs
  • Kinetics, tox, int.
  • oral; clonidine also as patch
  • tox: sedation; methyldopa hemolytic anemia
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5
Q

Reserpine

A
  • Sympathetic nerve terminal blocker
  • MOA
  • blocks vesicular amine transporter in noradrenergic nerves and depletes transmitter stores
  • Effects
  • reduces all sympathetic effects, esp. cardiovascular, and reduce blood pressure
  • Clinical
  • hypertension, rarely used
  • Kinetics, tox, int.
  • oral, long duration (days)
  • tox: psychiatric depression, GI disturbances
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6
Q

Guanethidine

A
  • Sympathetic nerve terminal blocker
  • MOA
  • interferes with amine release and replaces NE in vesicles
  • Effects
  • same as reserpine
  • Clinical
  • same as reserpine
  • Kinetics, tox, int.
  • severe orthostatic hypotension
  • sexual dysfunction
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7
Q

Prazosin, terazosin, doxazosin

A
  • MOA
  • selectively block α1 adrenoceptors
  • Effects
  • prevent sympathetic vasoconstriction
  • reduce prostatic smooth muscle tone
  • Clinical
  • hypertension
  • benign prostatic hyperplasia
  • Kinetics, tox, int.
  • oral
  • tox: orthostatic hypotension
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8
Q

Metoprolol, carvedilol, nebivolol

A
  • MOA
  • block β1 receptors
  • carvedilol also blocks α receptors
  • nebivolol also releases NO
  • Effects
  • prevent sympathetic cardiac stimulation
  • reduce renin secretion
  • Clinical
  • hypertension
  • heart failure
  • coronary disease
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9
Q

Verapamil, diltiazem

A
  • Vasodilator
  • MOA
  • nonselective block of L-type Ca channels
  • Effects
  • reduce cardiac rate and output
  • reduce vascular resistance
  • Clinical
  • hypertension, angina, arrythmias
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10
Q

Nifedipine, amlodipine, other dihydropyridines

A
  • Vasodilators
  • MOA
  • block vascular Ca channels>cardiac Ca channels
  • Effects
  • reduce vascular resistance
  • Clinical
  • hypertension, angina
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11
Q

Hydralazine, minoxidil

A
  • Vasodilators
  • MOA
  • causes NO release
  • metabolite opens K channels in vascular smooth muscle
  • Effects
  • vasodilation
  • reduces vascular resistance
  • arterioles more sensitive than veins
  • reflex tachycardia
  • Clinical
  • hypertension
  • minoxidil also used to treat hair loss
  • Kinetics, tox, int.
  • oral
  • tox: angina, tachycardia, hydralazine lupus-like syndrome, minoxidil hypertrichosis
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12
Q

Nitroprusside

A
  • MOA
  • releases NO
  • Effects
  • powerful vasodilation
  • Clinical
  • hypertensive emergencies
  • Kinetics, tox, int.
  • parenteral, short duration
  • tox: excessive hypotension, shock
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13
Q

Fenoldopam

A
  • MOA
  • activates D1 receptors
  • Effects
  • powerful vasodilation
  • The rest same as nitroprusside
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14
Q

Diazoxide

A
  • MOA
  • opens K channels
  • Effects
  • powerful vasodilation
  • The rest same as nitroprusside
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15
Q

Labetalol

A
  • MOA
  • α, β blocker
  • Effects
  • powerful vasodilation
  • The rest same as nitroprusside
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16
Q

Captopril, many others

A
  • MOA
  • ACE inhibitor
  • Effects
  • reduce ang II levels
  • reduce vasoconstriction and aldosterone secretion
  • increase bradykinin
  • Clinical
  • hypertension, heart failure, diabetes
  • Kinetics, tox, int.
  • oral
  • tox: cough, angioedema, hyperkalemia, renal impairment, teratogenic
17
Q

Losartan, many others

A
  • Angiotensin receptor blockers (ARBs)
  • MOA
  • block AT1 angiotensin receptors
  • Effects
  • same as ACE inhibitors but no increase in bradykinin
  • Clinical
  • hypertension, heart failure
  • Kinetics, tox, int.
  • oral
  • tox: same as ACE inhibitors but less cough
18
Q

Aliskiren

A
  • Renin inhibitor
  • MOA
  • inhibits enzyme activity of renin
  • Effects
  • reduces ang I, II and aldosterone
  • Clinical
  • hypertension
  • Kinetics, tox, int.
  • oral
  • tox: hyperkalemia, renal impairment, potential teratogen