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
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
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
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
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
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
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
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
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
10
Q
Nifedipine, amlodipine, other dihydropyridines
A
- Vasodilators
- MOA
- block vascular Ca channels>cardiac Ca channels
- Effects
- reduce vascular resistance
- Clinical
- hypertension, angina
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
12
Q
Nitroprusside
A
- MOA
- releases NO
- Effects
- powerful vasodilation
- Clinical
- hypertensive emergencies
- Kinetics, tox, int.
- parenteral, short duration
- tox: excessive hypotension, shock
13
Q
Fenoldopam
A
- MOA
- activates D1 receptors
- Effects
- powerful vasodilation
- The rest same as nitroprusside
14
Q
Diazoxide
A
- MOA
- opens K channels
- Effects
- powerful vasodilation
- The rest same as nitroprusside
15
Q
Labetalol
A
- MOA
- α, β blocker
- Effects
- powerful vasodilation
- The rest same as nitroprusside