Antihypertensive agents Flashcards Preview

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Flashcards in Antihypertensive agents Deck (18):
1

Hydrochlorothiazide, chlorthalidone

  • 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

Furosemide

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

3

Spironolactone, eplerenone

  • 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

Clonidine, methyldopa

  • 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

Reserpine

  • 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

Guanethidine

  • 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

Prazosin, terazosin, doxazosin

  • 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

Metoprolol, carvedilol, nebivolol

  • 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

Verapamil, diltiazem

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

10

Nifedipine, amlodipine, other dihydropyridines

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

11

Hydralazine, minoxidil

  • 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

Nitroprusside

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

13

Fenoldopam

  • MOA
    - activates D1 receptors
  • Effects
    - powerful vasodilation
  • The rest same as nitroprusside

14

Diazoxide

  • MOA
    - opens K channels
  • Effects
    - powerful vasodilation
  • The rest same as nitroprusside

15

Labetalol

  • MOA
    - α, β blocker
  • Effects
    - powerful vasodilation
  • The rest same as nitroprusside

16

Captopril, many others

  • 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

Losartan, many others

  • 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

Aliskiren

  • 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