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Anti-HTN drugs (Exam 5)
Anti-HTN drugs
15
Pharmacology
Graduate
12/01/2010

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Term
Reserpine
Definition
Transmitter depleter
Crosses BBB so central effects as well as depleting NE in SNS
Many SEs including depression
Long acting
Term
Guanethidine
Definition
Transmitter depleter
Depletes NE peripherally
Potent
Many SEs
Term
Clonidine
Definition
Centrally-acting alpha-2 agonist
MOA: act on post-synaptic alpha-2A receptors in NTS and Imidazoline receptors in RVLM
SE: sedation, dry mouth, decreased libido, no CNS SEs like alpha-methyl-DOPA, some minimal ortho-hypo, rebound HT (abrupt withdrawal)
USE: drug and nicotine plans
Reduce left-ventricle hypertrophy and lower total cholesterol w/o reducing HDL
Term
Alpha-methyl-DOPA
Definition
Centrally-acting alpha-2 agonist
MOA: prodrug metabolized to alpha-methyl-NE intra-neuronally -> released as false NT
Activity @ alpha-2A receptor > alpha-1 receptor
USE: decreases SNS, moderately potent anti-HT, can be used safely during pregnancy
SE: dry mouth, nasal congestion, + Coombs test (resolves), sedation, EPS, lactation, decreased libido, ortho-hypotension
Reduce left-ventricle hypertrophy and lower total cholesterol w/o reducing HDL
Term
Prazosin, Doxazosin
Definition
Alpha-1 antagonists
MOA: alpha-1 and alpha-2B selective
SE: syncope (during 1st admin and dose increases), minimal ortho-hypo, headaches, priapism
USE: more severe HT, usually in combo
Decreases total cholesterol w/o effect on HDL
Caution: arrythmias -> sudden death
Term
Propanolol and Labetolol (nonselective)
Acebutolol, Atenolol, Metoprolol (beta-1 cardioselective)
Definition
Beta-blockers
MOA: decrease renin, decrease CO, block presynaptic beta receptors?
May produce rapid drop in BP, or have more slowly developing anti-HT effect
Used for mild to moderate HT, and in combo for more severe HT
SE: myocardial depression, bronchial constriction, potentiation of hypoglycemia, withdrawal rebound, impaired exercise tolerance, increase TGs and decrease HDLs
DI: NSAIDs may block or reduce anti-HT effect of beta-blockers
Not good at preventing stroke like ACE inhibitors, ARBs, Ca2+ channel blockers -> use other first unless pt has cardiac issues for which you need to use beta-blockers
Term
Hydrochorothiazide, Chlorthalidone, Spironolactone, Amiloride
Definition
thiazides
MOA: mild diuretic effect, possibly reduce Na+ in VSM to reduce contractility
Very well tolerated, very inexpensive, as good/better than more expensive agents for mild HT and in combo for more severe HT
Chlorthalidone as effective as Ca2+ channel blocker or ACE inhibitor in preventing fatal CHD or non-fatal MI, also more effective in preventing heart failure
No orthostatic hypotension
Many options available

Hydrochlorthiazide: overall anti-HT effect is mild and plateaus (ceiling effect-efficacy maxed out at 15mmHg)
Does not lower BP in normotensive, high sodium intake can reverse anti-HT effects
SE: hypokalemia, hyperglycemia, hyperuricemia, increased cholesterol and TGs
Term
Hydralazine
Definition
Smooth muscle vasodilator
MOA: increased NO, increased K+ permeability
SEs (if used alone): tachycardia, headache, fluid retention, edema, nausea, lupus-like syndrome (resolves with DQ)
USE: generally used with severe HT in combo
Reflexes intact, little or no otho-hypo
-give with beta blocker to counter tachycardia
Term
Minoxidil
Definition
Smooth muscle vasodilator
MOA: increased K+ channel opening
USE: very potent, used in severe HT-usually in combo
SEs like hydralazine, also hirsutism and edema
-give with diuretic and beta blocker
Term
Nitroprusside
Definition
Smooth muscle vasodilator
MOA: metabolized to NO
Very potent, unstable compound, prepared fresh and given IV
SE: headache and nausea
Used for HT crisis, gives moment to moment control of BP, cheap
Term
Captopril, Enalapril, Fosinopril
Definition
ACE inhibitors
MOA: prevent conversion of A1 to A2, increase bradykinin, increase PGI and NO
USE: mild or moderate HT, well tolerated
Do not interfere with reflexes -> no ortho-hypotension
SE: cough, bronchospasm, ageusia (mainly captopril), renal complications (long term, kidney excretion), hypotension with volume depletion, fetal mortality (2nd and 3rd trimesters), birth defects seen in 1st trimester, angioedema: rare -> DQ drug, resolves in hours
DI: dangerous hyperkalemia if combined w/ K+ sparing agent, oral contraceptives increase A1 levels, NSAIDs can reduce anti-HT and may increase kidney complications, increase Li2+ retention (bipolar pts)
In heart failure -> slow progession of disease and prolong survival
In diabetics -> decrease development of glomerulopathies
Less effective in African Americans
Term
Losartan, Valsartan
Definition
Angiotension receptor blockers (ARBs)
In terms of efficacy, patient tolerance, and SEs -> similar to ACE-Is
Advantage: no cough
SE: dizziness, fetal toxicity, hyperkalemia
Less effective in African Americans
Term
Aliskerin
Definition
Renin inhibitor
MOA: binds renin, inhibits cleaving of angiotensinogen to produce angio-1
Does not increase plasma renin activity
BP reduction similar to ARBs
Expect other effects similar to ACE-Is and ARBs (heart, kidney) -> but not known
No or little cough
Long ½ life=24 hrs
SE: rash, increased uric acid , gout (low incidence)
Do not use during pregnany
-sometimes see unexpected beneficial effects or deleterious effects
Term
Nifedipine (arteriolar)
Verapamil and Diltiazem (arteriolar and cardiac)
Definition
Calcium channel blockers
MOA: reduce VSM tone to decrease PR
Numerous SEs including adverse cardiac events including sudden death (more common in short acting)
Nifedipine-good vasodilation with little cardiac depression, but significant reflex tachycardia
Verapamil and Diltiazem-little reflex tachycardia, but do produce cardiac depression
Works well in African Americans
Term
Sildenifil
Definition
PDE5 inhibitor
MOA: prolongs cGMP presence, vasodilation
USE: pulmonary arterial HT
Danger: unexpected presence of NO
Limitation: requires cognitive activation
SE: retinal cGMP
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