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31 Cards in this Set

  • Front
  • Back
methyldopa
tx HTN
centrally acting sympathoplegic
prodrug, T 1/2 = 2 hrs
use in pregnancy
lowers BP by acting to decrease sympathetic vasomotor tne, either as central agonists - stimulate medullary receptors, or peripheral antagonists that block receptors at nerve endings
interrupt efferent symp pathway at different sites form medullary centers, autonomic ganglia, symp neurons, and adrenergic receptors
agonists at presynaptic alpha2 receptors in brainstem, reduces peripheral vascular resistance
reduces renin secretion
side effects:
not recommended for monotherapy b/c --> postural hypotension
sodium retention (add a diuretic
clonidine
orally, clonidine also has a transdermal patch, T 1/2 = 8-12 hrs
lowers BP by acting on adrenergic receptors to decrease symp tone, either as central agonists or peripheral antagonists, interrups efferent symp pathway at different sites from medullary centers, autonomic ganglia, symp neurons and adrenergic receptors
agonist on presynaptic alpha2 receptors in brainstem, reduces TPR
reduces renin secretion
acts directly!
side effects:
not recommended for monotherapy --> postural hypotension, sodium retention, clonidine, specifically: sedation, dry mouth - dose at bedtime
sudden withdrawal of clonidine --> HTN crisis, HA, tremor, abdominal pain, sweating, tachycardia
sudden withdrawal of cloniti
guanabenz
tx HTN
sympathoplegic drugs
guanfacine
sympathoplegic drugs
propranolol
tx HTN
nonselective beta blockers
specifically: used in caucasions, young
generally:
lower BP by blocking beta-adrenergic receptors in heart - reduce CO, kidney - reduce renin, CNS - reduce symp tone, combined with other anti-HTN to counteract reflex tachycardia by vasodilators, increased renin secretion by thiazide and loop diuretics
side effects:
may worsen sx in pts with reduced myocardial reserve, asthma, peripheral, vascular insufficiency, diabetes
usu increased exercise tolerance when used to tx angina, but may decr exercise tolerance in pts with HF by reducing CO
may predispose to atherogenesis by increasing atherogenesis by incr plasma triglycerides, decr HDL-cholesterol
delayed recovery of normoglycemia
significant risk of new-onset diabetes
minor: GI, CNS, skeletal muscle tumors
nadolol
tx HTN
nonselective beta blockers
specifically: used in caucasions, young
generally:
lower BP by blocking beta-adrenergic receptors in heart - reduce CO, kidney - reduce renin, CNS - reduce symp tone, combined with other anti-HTN to counteract reflex tachycardia by vasodilators, increased renin secretion by thiazide and loop diuretics
side effects:
may worsen sx in pts with reduced myocardial reserve, asthma, peripheral, vascular insufficiency, diabetes
usu increased exercise tolerance when used to tx angina, but may decr exercise tolerance in pts with HF by reducing CO
may predispose to atherogenesis by increasing atherogenesis by incr plasma triglycerides, decr HDL-cholesterol
delayed recovery of normoglycemia
significant risk of new-onset diabetes
minor: GI, CNS, skeletal muscle tumors
penbutolol
tx HTN
nonselective beta blockers
specifically: used in caucasions, young
generally:
lower BP by blocking beta-adrenergic receptors in heart - reduce CO, kidney - reduce renin, CNS - reduce symp tone, combined with other anti-HTN to counteract reflex tachycardia by vasodilators, increased renin secretion by thiazide and loop diuretics
side effects:
may worsen sx in pts with reduced myocardial reserve, asthma, peripheral, vascular insufficiency, diabetes
usu increased exercise tolerance when used to tx angina, but may decr exercise tolerance in pts with HF by reducing CO
may predispose to atherogenesis by increasing atherogenesis by incr plasma triglycerides, decr HDL-cholesterol
delayed recovery of normoglycemia
significant risk of new-onset diabetes
minor: GI, CNS, skeletal muscle tumors
pindolol
tx HTN
nonselective beta blockers
specifically: used in caucasions, young
generally:
lower BP by blocking beta-adrenergic receptors in heart - reduce CO, kidney - reduce renin, CNS - reduce symp tone, combined with other anti-HTN to counteract reflex tachycardia by vasodilators, increased renin secretion by thiazide and loop diuretics
side effects:
may worsen sx in pts with reduced myocardial reserve, asthma, peripheral, vascular insufficiency, diabetes
usu increased exercise tolerance when used to tx angina, but may decr exercise tolerance in pts with HF by reducing CO
may predispose to atherogenesis by increasing atherogenesis by incr plasma triglycerides, decr HDL-cholesterol
delayed recovery of normoglycemia
significant risk of new-onset diabetes
minor: GI, CNS, skeletal muscle tumors
timolol
tx HTN
nonselective beta blockers
specifically: used in caucasions, young
generally:
lower BP by blocking beta-adrenergic receptors in heart - reduce CO, kidney - reduce renin, CNS - reduce symp tone, combined with other anti-HTN to counteract reflex tachycardia by vasodilators, increased renin secretion by thiazide and loop diuretics
side effects:
may worsen sx in pts with reduced myocardial reserve, asthma, peripheral, vascular insufficiency, diabetes
usu increased exercise tolerance when used to tx angina, but may decr exercise tolerance in pts with HF by reducing CO
may predispose to atherogenesis by increasing atherogenesis by incr plasma triglycerides, decr HDL-cholesterol
delayed recovery of normoglycemia
significant risk of new-onset diabetes
minor: GI, CNS, skeletal muscle tumors
acebutolol
tx HTN
beta1 selective blocker
specifically: preferred for asthmatic or diabetic HTN;
generally:
Caucasians, young
lower BP by blocking beta-adrenergic receptors in heart - reduce CO, kidney - reduce renin, CNS - reduce symp tone, combined with other anti-HTN to counteract reflex tachycardia by vasodilators, increased renin secretion by thiazide and loop diuretics
side effects:
may worsen sx in pts with reduced myocardial reserve, asthma, peripheral, vascular insufficiency, diabetes
usu increased exercise tolerance when used to tx angina, but may decr exercise tolerance in pts with HF by reducing CO
may predispose to atherogenesis by increasing atherogenesis by incr plasma triglycerides, decr HDL-cholesterol
delayed recovery of normoglycemia
significant risk of new-onset diabetes
minor: GI, CNS, skeletal muscle tumors
atenolol
tx HTN
beta1 selective blocker
specifically: preferred for asthmatic or diabetic HTN;
generally:
Caucasians, young
lower BP by blocking beta-adrenergic receptors in heart - reduce CO, kidney - reduce renin, CNS - reduce symp tone, combined with other anti-HTN to counteract reflex tachycardia by vasodilators, increased renin secretion by thiazide and loop diuretics
side effects:
may worsen sx in pts with reduced myocardial reserve, asthma, peripheral, vascular insufficiency, diabetes
usu increased exercise tolerance when used to tx angina, but may decr exercise tolerance in pts with HF by reducing CO
may predispose to atherogenesis by increasing atherogenesis by incr plasma triglycerides, decr HDL-cholesterol
delayed recovery of normoglycemia
significant risk of new-onset diabetes
minor: GI, CNS, skeletal muscle tumors
bisoprolol
tx HTN
beta1 selective blocker
specifically: preferred for asthmatic or diabetic HTN;
generally:
Caucasians, young
lower BP by blocking beta-adrenergic receptors in heart - reduce CO, kidney - reduce renin, CNS - reduce symp tone, combined with other anti-HTN to counteract reflex tachycardia by vasodilators, increased renin secretion by thiazide and loop diuretics
side effects:
may worsen sx in pts with reduced myocardial reserve, asthma, peripheral, vascular insufficiency, diabetes
usu increased exercise tolerance when used to tx angina, but may decr exercise tolerance in pts with HF by reducing CO
may predispose to atherogenesis by increasing atherogenesis by incr plasma triglycerides, decr HDL-cholesterol
delayed recovery of normoglycemia
significant risk of new-onset diabetes
minor: GI, CNS, skeletal muscle tumors
esmolol
tx HTN
beta1 selective blocker
specifically: preferred for asthmatic or diabetic HTN;
generally:
Caucasians, young
lower BP by blocking beta-adrenergic receptors in heart - reduce CO, kidney - reduce renin, CNS - reduce symp tone, combined with other anti-HTN to counteract reflex tachycardia by vasodilators, increased renin secretion by thiazide and loop diuretics
side effects:
may worsen sx in pts with reduced myocardial reserve, asthma, peripheral, vascular insufficiency, diabetes
usu increased exercise tolerance when used to tx angina, but may decr exercise tolerance in pts with HF by reducing CO
may predispose to atherogenesis by increasing atherogenesis by incr plasma triglycerides, decr HDL-cholesterol
delayed recovery of normoglycemia
significant risk of new-onset diabetes
minor: GI, CNS, skeletal muscle tumors
metoprolol
tx HTN
beta1 selective blocker
specifically: preferred for asthmatic or diabetic HTN;
generally:
Caucasians, young
lower BP by blocking beta-adrenergic receptors in heart - reduce CO, kidney - reduce renin, CNS - reduce symp tone, combined with other anti-HTN to counteract reflex tachycardia by vasodilators, increased renin secretion by thiazide and loop diuretics
side effects:
may worsen sx in pts with reduced myocardial reserve, asthma, peripheral, vascular insufficiency, diabetes
usu increased exercise tolerance when used to tx angina, but may decr exercise tolerance in pts with HF by reducing CO
may predispose to atherogenesis by increasing atherogenesis by incr plasma triglycerides, decr HDL-cholesterol
delayed recovery of normoglycemia
significant risk of new-onset diabetes
minor: GI, CNS, skeletal muscle tumors
carteolol
tx HTN
mixed beta blcoker
also has NO production
more effective in caucasian and young
carvediol
tx HTN
mixed beta blocker + alpha 1 antagonists, blocks Ca entry
more effective in caucasian and young
mainly used orally for chronic
used in hypertensive emergencies, pheochromocytoma
side effects:
orthostatic hypotension, bronchospasm, hepatotoxicity
labetolol
Tx HTN
mixed beta blocker + alpha1 antagonist
more effective in caucasian and young
IV - in ER
beta:alpha block ratio of 3:1 for oral labetalol
tx: hypertensive emergencies, pheochromocytoma
side effects: orthostatic hypotension, bronchospasm, hepatotoxicity
betaxolol
tx HTN
beta1 specific, blocks Ca entry
more effective in caucasian and young
nebivolol
tx HTN
mixed beta blocker, beta1 specific, NO production
more effective in caucasian and young
prazosin
terazosin
doxazosin
tx HTN
alpha1 blockers
reduces norepi induced vasoconstriction to dilate both arteries and veins
BP falls because of decreased peripheral resistance
less reflex tachycardia than vasodialtors b/c the alpha2 receptors that inhibit norepi release are unaffected
side effects: postural hypotension, may be pronounced with 1st dose
mild, infrequent - drowsiness, dizziness, palpitations, HA, easy fatigability
hydralazine
tx HTN
vasodilators
specifically, orally - chronic treatment or IV for eclampsia/preeclampsia
acts on vascular SM to cause relaxation and reduce vascular R --> lower Bp
hydralazine (and minoxidil and diazoxid) dilate arteries selectively without affecting SM
should NOT be used for monotherapy
hydralazine (and minoxidil) - combined with diuretics, avoid fluid retention, or combined with beta blockers to diminish renin secretion and reflex tachycardia
side effects: antiHTN effects diminish with time b/c relfex tachycardia and increased renin secretion
most effective when combined with other drugs
hypotension accompanied by reflex tachycardia, increased myocardial contractions, incr renin secretion, fluid retnetion, HA, flushing, palpitations, dizziness
in elderly with CAD hydralazine (and minoxidil) - induce angina attacks and MIs
hydralazine - causes lupus-like syndrome
minoxidil
tx HTN
vasodilators, K+ channel opener
specifically, orally - chronic treatment
acts on vascular SM to cause relaxation and reduce vascular R --> lower BP
minoxidil (and hydralazine and diazoxid) dilate arteries selectively without affecting SM
should NOT be used for monotherapy
minoxidil (and hydralazine) - combined with diuretics, avoid fluid retention, or combined with beta blockers to diminish renin secretion and reflex tachycardia
side effects: antiHTN effects diminish with time b/c relfex tachycardia and increased renin secretion
most effective when combined with other drugs
hypotension accompanied by reflex tachycardia, increased myocardial contractions, incr renin secretion, fluid retnetion, HA, flushing, palpitations, dizziness
in elderly with CAD minoxidil (and hydralazine) - induce angina attacks and MIs
minoxidil - causes hypertrichosis (topical ointment - Rogaine - tx male baldness)
nitroprusside
tx HTN
vasodilators
specifically, IV - emergencies
acts on vascular SM to cause relaxation and reduce vascular R --> lower Bp
nitroprusside, spec: non-selective and balanced - dilates both arteries and veins
should NOT be used for monotherapy
side effects: antiHTN effects diminish with time b/c relfex tachycardia and increased renin secretion
most effective when combined with other drugs
hypotension accompanied by reflex tachycardia, increased myocardial contractions, incr renin secretion, fluid retnetion, HA, flushing, palpitations, dizziness
diazoxide
tx HTN
vasodilators, K channel opener
IV - emergencies
acts on vascular SM to cause relaxation and reduce vascular R --> lower Bp
diazoxide (hydralazine, minoxidil) dilate arteries selectively without affecting SM
should NOT be used for monotherapy
side effects: antiHTN effects diminish with time b/c relfex tachycardia and increased renin secretion
most effective when combined with other drugs
hypotension accompanied by reflex tachycardia, increased myocardial contractions, incr renin secretion, fluid retnetion, HA, flushing, palpitations, dizziness
in elderly with CAD
fenoldopam
tx HTN
vasodilators
specifically, IV - emergencies
acts on vascular SM to cause relaxation and reduce vascular R --> lower Bp
dilates arteries by acint as a dopamine D1 agonist
should NOT be used for monotherapy
side effects: antiHTN effects diminish with time b/c reflex tachycardia and increased renin secretion
most effective when combined with other drugs
hypotension accompanied by reflex tachycardia, increased myocardial contractions, incr renin secretion, fluid retnetion, HA, flushing, palpitations, dizziness
in elderly with CAD
verapamil
tx HTN
calcium channel blocker
used in elderly, african americans
contraindicated in pts with SA/AV node abnormalities or CHF
block slow Ca channels, reduce intracellulra Ca --> relax arteriolar SM --> vasodialtion, lower BP
equally effective for monotherapy in mild to mod HTN
verapamil - strongest cardiac effects, least vasodilation
with diltiazem - doesn't cause reflex tachycardia because depresses the SA and AV node
side effects:
verapamil (diltiazem) --> myocardial depression, possibly bradycardia with SA node dysfxn
contraindicated in pts with SA/AV node abnorms, CHF
verpapamil - constipation
diltiazem
tx HTN
calcium channel blocker
used in elderly, african americans
contraindicated in pts with SA/AV node abnormalities or CHF
block slow Ca channels, reduce intracellulra Ca --> relax arteriolar SM --> vasodialtion, lower BP
equally effective for monotherapy in mild to mod HTN
in between verapamil and -dipines on cardiac and vasodilation effects
diltiazem (and verapamil) - don't cause reflex tachycardia b/c depresses AV/SA node
side effects: diltiazem (verapamil) --> myocardial depression, possibly bradycardia w/ SA node dysfxn
-dipines
dihydropyridines
tx HTN
calcium channel blocker
used in elderly, african americans
contraindicated in pts with SA/AV node abnormalities or CHF
block slow Ca channels, reduce intracellulra Ca --> relax arteriolar SM --> vasodilation, lower BP
equally effective for monotherapy in mild to mod HTN
-dipines: strongest vasodilators, most likely to produce reflex tachycardia
side effects:
-dipines: reflex tachycardia, HA, flushing, dizziness, peripheral edema
alisikrein
renin inhibitors
orally active
dose dependent reduction of plasma renin
dose dependent reduction of BP
safety/tolerability - similar to ACE inhibitors
-prils
tx HTN
ACE inhibitors
orally effective for monotherapy
captopril - active drug, all others - prodrugs
most effective in young, middle aged caucasions
1st choice for pts with diabetes, chronic renal disease, LVH
lowers BP by inhibiting ACE
BP lowering due to decrease in peripheral vasc resistance
vasodilation b/c reduced ang-induced vasoconstriction
increased bradykinin --> vasodilation contributes to antiHTN effect
lowers BP w/o compromising blood supply to heart, brain, or kidneys
don't cause symp activation (or tachycardia) b/c of concurrent baroreceptor resetting or vagal activation
lower BP in 50% of pts with mild to mod HTN
side effects:
bradykinin --> dyr, hacking, nonproductive cough, angioneurotic edema
mild, fewer, and w/o lipid changes
hyperkalemia b/c inhibited aldosterone secretion
anaphylaxis
acute renal failure in pts with bilateral renal artery stenosis
tast disturbances interfering with nutrition
nonallergic, pruritic maculopapular rash
-sartans
tx HTN
angiotensin receptor antagonists
2 types of ang II receptors - AT1 - receptors in vasc SM --> known actions in ang II
all available AT II antagonsists block AT1, no effects on AT2
more specific than ACE inhibitors, do not effect bradykinin metabolism
more complete inhibition of angiotensin action b/c other enzymes can generate ang II
side effects:
do not cause cough or angioneurotic edema (except losartan - uricosuric)
otherwise, adverse effects are like ACE inhibitors - hyperkalemia, reduced renal function