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78 Cards in this Set
- Front
- Back
- 3rd side (hint)
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How does clonidine work?
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It is an alpha-2 agonist. It stimulates central and peripheral alpha-2 receptors, decreasing central sympathetic outflow.
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An IV injection of clonidine may cause what side effect?
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transient increase in BP
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When is clonidine used?
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moderate-to-severe essential hypertension, renal hypertension, dx pheochromocytoma
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What are the side effects of clonidine?
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sedation, dry mouth, orthostatic hypotension, fluid retention
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An abrupt withdrawal of clonidine may cause what side effect?
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rebound hypertensive crisis
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What drugs interact with clonidine and methyldopa?
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tricyclic antidepressants (they block reuptake of norepinephrine); Ca2+ blockers decrease HR and contractibility and will have an additive effect
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How does methyldopa work?
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It is an alpha-2 agonist. It stimulates central alpha-2 receptors, diminishing sympathetic outflow.
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When is methyldopa used?
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moderate essential hypertension; hypertension in pregnancy
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What are the side effects of methyldopa? (h for hint)
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sedation, dry mouth, postural hypotension, fluid retention, positive direct Coombs reaction in 10-20%
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they are the same as clonidine with one addition: it involves a blood test...
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Name three alpha-2 agonists
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clonidine, methyldopa, guanabenz
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Name five selective beta-1 blockers.
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acebutolol, betaxolol, esmolol, atenolol, metoprolol
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Name two ISA beta-blockers. What does ISA mean?
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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
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When would you use an ISA?
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in patients with decreased cardiac functioning or a tendency for bradycardia
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How do beta-blockers work?
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They decrease cardiac output and decrease renin secretion
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What is special about labetalol?
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it is a mixed antagonist; it blocks both beta and alpha receptors
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What is the longest-acting beta-blocker?
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nadolol, 24 hours
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What is the shortest-acting beta-blocker?
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esmolol, half-life of 10 minutes
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Which beta-blocker is lipid-soluble and causes CNS effects? What endocrine disorder would this drug be used in?
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propranolol; hyperthyroidism
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Which beta-blocker has high oral bioavailability?
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pindolol
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When are beta-blockers used?
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mild-to-severe essential hypertension, supraventricular and ventricular tachyarrhythmias, treatment of angina, acute MI, hypertrophic cardiomyopathies, hypertensive emergencies
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Which two beta-blockers are used topically for glaucoma?
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timolol and betaxolol
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Which tumor does labetalol help treat?
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pheochromocytoma
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What are the side effects of beta-blockade?
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bronchospasm, masking of sympathetic responses to hypoglycemia, negative inotropic effect (exacerbates CHF), heart block or bradycardia, aggravation of vasospasm
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Who should not receive a beta-blocker?
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asthmatics, diabetics, patients with COPD
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Name three selective alpha-1 blockers.
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prazosin, terazosin, and doxazosin
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How do alpha-1 blockers work?
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They block vasoconstriction of vascular smooth muscle (both arteriolar and venous), decreasing both afterload and preload
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When are alpha-1 blockers used?
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mild-to-moderate essential hypertension, CHF, pheo (prazosin), and BPH
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Why are alpha-1 blockers used to treat BPH?
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they promote relaxation of the urethra and trigone, and decrease urinary retention
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What are the side effects of alpha-1 blockers?
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postural hypotension and reflex tachycardia
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Name three nonselective alpha-blockers.
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phentolamine, tolazoline, phenoxybenzamine
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Which alpha-blocker binds irreversibly and is therefore noncompetitive?
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phenoxybenzamine
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When is phentolamine used?
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diagnose pheo, prevent dermal necrosis and sloughing from infiltrated drugs such as norepinephrine, autonomic hyperreflexia
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When is tolazoline used?
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peripheral vascular disease, Raynaud's phenomenon, autonomic hyperreflexia
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When is phenoxybenzamine used?
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Raynaud's phenomenon, autonomic hyperreflexia
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What are the side effects of alpha-blockers?
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sedation, miosis, postural hypotension, reflex tachycardia
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How do nonselective alpha-blockers lower blood pressure?
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They block catecholamine-induced vasoconstriction
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How does reserpine work? What is its classification?
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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
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When is reserpine used?
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mild-to-moderate hypertension, but rarely used at all clinically
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What are the side effects of reserpine?
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sedation, bradycardia, vasodilation, diarrhea, depression
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Who should not take reserpine?
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patients with a history of depression
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How does guanethidine work? What is its classification?
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It displaces norepinephrine from synaptic vesicles and inhibits its release from nerve endings; adrenergic neuron blocker
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How does guanethidine enter the nerve terminal and what drugs would block this if given concurrently?
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It uses uptake 1; uptake blockers (like tricyclic antidepressants... and what other antihypertensive do TCAs counteract? clonidine/methydopa!)
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When is guanethidine used?
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severe hypertension, but rarely used clinically
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What are the side effects of guanethidine?
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severe orthostatic hypotension, sexual dysfunction, fluid retention
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Name three ganglionic blockers.
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hexamethonium, trimethapham, mecamylamine
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What do ganglionic blockers block? What does this achieve physiologically?
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nicotinic receptors of autonomic ganglia; block of sympathetic and parasympathetic outflow
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How does guanethidine enter the nerve terminal and what drugs would block this if given concurrently?
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It uses uptake 1; uptake blockers (like tricyclic antidepressants... and what other antihypertensive do TCAs counteract? clonidine/methydopa!)
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When is guanethidine used?
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severe hypertension, but rarely used clinically
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What are the side effects of guanethidine?
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severe orthostatic hypotension, sexual dysfunction, fluid retention
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Name three ganglionic blockers.
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hexamethonium, trimethapham, mecamylamine
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What do ganglionic blockers block? What does this achieve physiologically?
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nicotinic receptors of autonomic ganglia; block of sympathetic and parasympathetic outflow
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Ganglionic blockers are rarely used as antihypertensives today. Which drug is the exception to this rule, and in what case is it used?
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trimethaphan; hypertension secondary to acute dissecting aortic aneurysm
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Which reflexes do ganglionic blockers prevent?
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baroreceptor reflexes
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What effect does hydralazine cause and how does it achieve that?
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direct relaxation of arteriolar smooth muscle; release of EDRF (nitric oxide) and interference with Ca2+ metabolism
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When is hydralazine used?
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moderate-to-severe hypertension (with beta-blockers and diuretic), CHF (with oral nitrates)
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What are the side effects of hydralazine?
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reflex tachycardia, increased myocardial oxygen consumption (MC ischemia, prevent with beta-blocker), headache, edema
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What important side effect of hydralazine is related to the acetylation capacity of the patient?
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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) |
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What effect does minoxidil have and how does it achieve that?
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direct arterial vasodilation; opens K+ channels, which hyperpolarizes and relaxes vascular smooth muscle
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When is minoxidil used? What should it be given with?
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severe hypertension when nothing else works; beta-blocker and diuretic
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What are the side effects of minoxidil?
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salt and water retention, reflex tachycardia, hypertrichosis (defined as human werewolf syndrome LOL), pericardial effusion
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How does diazoxide work?
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It opens K+ channels and dilates arterioles; inhibits insulin release (K+ channels on B cells of pancreas)
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What is diazoxide used for?
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hypertensive emergencies (malignant hypertension), and hyperinsulinemia (esp. insulinoma)
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When is diazoxide contraindicated?
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CAD, pulmonary edema, aortic aneurysm, intracranial hemorrhage
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What are the side effects of diazoxide?
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excessive hypotension, salt and water retention, hyperglycemia
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How does sodium nitroprusside work?
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It releases NO, balanced vasodilation
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When is sodium nitroprusside used?
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hypertensive emergencies, acute CHF, severe mitral regurgitation with pulmonary congestion
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What are the side effects of sodium nitroprusside?
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hypotension, headache, diaphoresis, thiocyanate poisoning
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Name the calcium-channel blockers.
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dihydropyridines (-dipines), verapamil, dilitiazem; mibefradil, bepridil
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How do calcium-channel blockers work? (now that's a hard one)
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they block Ca2+ entry into cells, which inhibits excitation-contraction coupling of vascular smooth muscle (blah, blah, they decrease PVR)
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Dilitiazem and verapamil have another effect. What is it?
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They slow conduction through the AV node
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What are the uses of Ca2+-channel blockers?
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mild-to-moderate hypertension, coronary vasospasm (Prinzmetal), supraventricular tachyarrhythmias (V&D)
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What are the side effects of cc blockers?
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heart block (esp. verapamil), exacerbation of CHF, hypotension (esp. verapamil) *DHPs cause gingival hyperplasia and verapamil increases plasma digoxin levels
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What is the suffix of ACE inhibitors?
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-pril
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What is the mechanism of action of captopril?
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it inhibits ACE, which potentiates the vasodilatory effects of bradykinin... leads to decrease in peripheral resistance
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What other effects does captopril have? (Hint: on the kidney)
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reduces filtration pressure and GFR because the vasodilation of the efferent arterioles is greater than that of the afferent arterioles because aldosterone is decreased
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When is captopril used?
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CHF, mild-to-moderate essential hypertension; use with a thiazide diuretic
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ACE inhibitors decrease proteinuria and the rate of pregression of renal failure in what patient population?
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diabetics
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What are the side effects of ACE inhibitors?
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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) |
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