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78 Cards in this Set

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How does clonidine work?
It is an alpha-2 agonist. It stimulates central and peripheral alpha-2 receptors, decreasing central sympathetic outflow.
An IV injection of clonidine may cause what side effect?
transient increase in BP
When is clonidine used?
moderate-to-severe essential hypertension, renal hypertension, dx pheochromocytoma
What are the side effects of clonidine?
sedation, dry mouth, orthostatic hypotension, fluid retention
An abrupt withdrawal of clonidine may cause what side effect?
rebound hypertensive crisis
What drugs interact with clonidine and methyldopa?
tricyclic antidepressants (they block reuptake of norepinephrine); Ca2+ blockers decrease HR and contractibility and will have an additive effect
How does methyldopa work?
It is an alpha-2 agonist. It stimulates central alpha-2 receptors, diminishing sympathetic outflow.
When is methyldopa used?
moderate essential hypertension; hypertension in pregnancy
What are the side effects of methyldopa? (h for hint)
sedation, dry mouth, postural hypotension, fluid retention, positive direct Coombs reaction in 10-20%
they are the same as clonidine with one addition: it involves a blood test...
Name three alpha-2 agonists
clonidine, methyldopa, guanabenz
Name five selective beta-1 blockers.
acebutolol, betaxolol, esmolol, atenolol, metoprolol
Name two ISA beta-blockers. What does ISA mean?
acebutolol and pindolol; ISA means intrinsic sympathomimetic activity; these drugs have less negative inotropic and chronotropic effects, and they don't increase serum triglyercides or decrease HDL
When would you use an ISA?
in patients with decreased cardiac functioning or a tendency for bradycardia
How do beta-blockers work?
They decrease cardiac output and decrease renin secretion
What is special about labetalol?
it is a mixed antagonist; it blocks both beta and alpha receptors
What is the longest-acting beta-blocker?
nadolol, 24 hours
What is the shortest-acting beta-blocker?
esmolol, half-life of 10 minutes
Which beta-blocker is lipid-soluble and causes CNS effects? What endocrine disorder would this drug be used in?
propranolol; hyperthyroidism
Which beta-blocker has high oral bioavailability?
pindolol
When are beta-blockers used?
mild-to-severe essential hypertension, supraventricular and ventricular tachyarrhythmias, treatment of angina, acute MI, hypertrophic cardiomyopathies, hypertensive emergencies
Which two beta-blockers are used topically for glaucoma?
timolol and betaxolol
Which tumor does labetalol help treat?
pheochromocytoma
What are the side effects of beta-blockade?
bronchospasm, masking of sympathetic responses to hypoglycemia, negative inotropic effect (exacerbates CHF), heart block or bradycardia, aggravation of vasospasm
Who should not receive a beta-blocker?
asthmatics, diabetics, patients with COPD
Name three selective alpha-1 blockers.
prazosin, terazosin, and doxazosin
How do alpha-1 blockers work?
They block vasoconstriction of vascular smooth muscle (both arteriolar and venous), decreasing both afterload and preload
When are alpha-1 blockers used?
mild-to-moderate essential hypertension, CHF, pheo (prazosin), and BPH
Why are alpha-1 blockers used to treat BPH?
they promote relaxation of the urethra and trigone, and decrease urinary retention
What are the side effects of alpha-1 blockers?
postural hypotension and reflex tachycardia
Name three nonselective alpha-blockers.
phentolamine, tolazoline, phenoxybenzamine
Which alpha-blocker binds irreversibly and is therefore noncompetitive?
phenoxybenzamine
When is phentolamine used?
diagnose pheo, prevent dermal necrosis and sloughing from infiltrated drugs such as norepinephrine, autonomic hyperreflexia
When is tolazoline used?
peripheral vascular disease, Raynaud's phenomenon, autonomic hyperreflexia
When is phenoxybenzamine used?
Raynaud's phenomenon, autonomic hyperreflexia
What are the side effects of alpha-blockers?
sedation, miosis, postural hypotension, reflex tachycardia
How do nonselective alpha-blockers lower blood pressure?
They block catecholamine-induced vasoconstriction
How does reserpine work? What is its classification?
It blocks the uptake of neurotransmitters into their storage vesicles, leading to the depletion of catecholamine and serotonin stores... it also decreases cardiac output and peripheral vascular resistance; adrenergic neuron blocker
When is reserpine used?
mild-to-moderate hypertension, but rarely used at all clinically
What are the side effects of reserpine?
sedation, bradycardia, vasodilation, diarrhea, depression
Who should not take reserpine?
patients with a history of depression
How does guanethidine work? What is its classification?
It displaces norepinephrine from synaptic vesicles and inhibits its release from nerve endings; adrenergic neuron blocker
How does guanethidine enter the nerve terminal and what drugs would block this if given concurrently?
It uses uptake 1; uptake blockers (like tricyclic antidepressants... and what other antihypertensive do TCAs counteract? clonidine/methydopa!)
When is guanethidine used?
severe hypertension, but rarely used clinically
What are the side effects of guanethidine?
severe orthostatic hypotension, sexual dysfunction, fluid retention
Name three ganglionic blockers.
hexamethonium, trimethapham, mecamylamine
What do ganglionic blockers block? What does this achieve physiologically?
nicotinic receptors of autonomic ganglia; block of sympathetic and parasympathetic outflow
How does guanethidine enter the nerve terminal and what drugs would block this if given concurrently?
It uses uptake 1; uptake blockers (like tricyclic antidepressants... and what other antihypertensive do TCAs counteract? clonidine/methydopa!)
When is guanethidine used?
severe hypertension, but rarely used clinically
What are the side effects of guanethidine?
severe orthostatic hypotension, sexual dysfunction, fluid retention
Name three ganglionic blockers.
hexamethonium, trimethapham, mecamylamine
What do ganglionic blockers block? What does this achieve physiologically?
nicotinic receptors of autonomic ganglia; block of sympathetic and parasympathetic outflow
Ganglionic blockers are rarely used as antihypertensives today. Which drug is the exception to this rule, and in what case is it used?
trimethaphan; hypertension secondary to acute dissecting aortic aneurysm
Which reflexes do ganglionic blockers prevent?
baroreceptor reflexes
What effect does hydralazine cause and how does it achieve that?
direct relaxation of arteriolar smooth muscle; release of EDRF (nitric oxide) and interference with Ca2+ metabolism
When is hydralazine used?
moderate-to-severe hypertension (with beta-blockers and diuretic), CHF (with oral nitrates)
What are the side effects of hydralazine?
reflex tachycardia, increased myocardial oxygen consumption (MC ischemia, prevent with beta-blocker), headache, edema
What important side effect of hydralazine is related to the acetylation capacity of the patient?
lupus-like syndrome
BONUS: What other drugs cause lupus-like syndrome?
BONUS: What antibodies are seen in drug-induced lupus?



(A: procainamide, D-penicillamine; antihistone antibodies)
What effect does minoxidil have and how does it achieve that?
direct arterial vasodilation; opens K+ channels, which hyperpolarizes and relaxes vascular smooth muscle
When is minoxidil used? What should it be given with?
severe hypertension when nothing else works; beta-blocker and diuretic
What are the side effects of minoxidil?
salt and water retention, reflex tachycardia, hypertrichosis (defined as human werewolf syndrome LOL), pericardial effusion
How does diazoxide work?
It opens K+ channels and dilates arterioles; inhibits insulin release (K+ channels on B cells of pancreas)
What is diazoxide used for?
hypertensive emergencies (malignant hypertension), and hyperinsulinemia (esp. insulinoma)
When is diazoxide contraindicated?
CAD, pulmonary edema, aortic aneurysm, intracranial hemorrhage
What are the side effects of diazoxide?
excessive hypotension, salt and water retention, hyperglycemia
How does sodium nitroprusside work?
It releases NO, balanced vasodilation
When is sodium nitroprusside used?
hypertensive emergencies, acute CHF, severe mitral regurgitation with pulmonary congestion
What are the side effects of sodium nitroprusside?
hypotension, headache, diaphoresis, thiocyanate poisoning
Name the calcium-channel blockers.
dihydropyridines (-dipines), verapamil, dilitiazem; mibefradil, bepridil
How do calcium-channel blockers work? (now that's a hard one)
they block Ca2+ entry into cells, which inhibits excitation-contraction coupling of vascular smooth muscle (blah, blah, they decrease PVR)
Dilitiazem and verapamil have another effect. What is it?
They slow conduction through the AV node
What are the uses of Ca2+-channel blockers?
mild-to-moderate hypertension, coronary vasospasm (Prinzmetal), supraventricular tachyarrhythmias (V&D)
What are the side effects of cc blockers?
heart block (esp. verapamil), exacerbation of CHF, hypotension (esp. verapamil) *DHPs cause gingival hyperplasia and verapamil increases plasma digoxin levels
What is the suffix of ACE inhibitors?
-pril
What is the mechanism of action of captopril?
it inhibits ACE, which potentiates the vasodilatory effects of bradykinin... leads to decrease in peripheral resistance
What other effects does captopril have? (Hint: on the kidney)
reduces filtration pressure and GFR because the vasodilation of the efferent arterioles is greater than that of the afferent arterioles because aldosterone is decreased
When is captopril used?
CHF, mild-to-moderate essential hypertension; use with a thiazide diuretic
ACE inhibitors decrease proteinuria and the rate of pregression of renal failure in what patient population?
diabetics
What are the side effects of ACE inhibitors?
loss of taste, dry cough, ANGIOEDEMA, orthostatic hypotension, proteinuria (ha), eosinophilia, bone marrow toxicity (rare)
BONUS: what class of androgen treats hereditary angioedema?



(A: 17-alkyl derivatives like danazol)