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22 Cards in this Set
- Front
- Back
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Drugs which inhibit adrenergic transmission are used to treat?
-mechanisms |
-hypertension
-inhibit presynaptic NE release -inhibit postsynaptic adrenoreceptors |
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clonidine, guanabenz:
-what -peripheral and central actions |
-a2-adrenoceptor agonist
-stimulate a2 receptors involved in negative feedback = unable to release NE (peripheral) -inhibit frequency of neuronal impulses (central) **MAIN action |
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What is neuronal frequency specificity
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-drug action is overcome by strong sympathetic activation (NE displaces drugs from receptor)
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Uses of clonidine
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-antihypertensive
-ease withdrawal symptoms -ADHD, tourette's |
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What is a long-term side effect of alpha2-adrenoceptor agonists
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-adaptation to adrenergic blockers can cause postsynaptic receptor supersensitivity --> important to discontinue use gradually to avoid hypertensive crisis
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Bromocriptine:
-what -how it works -uses |
-DA2 receptor agonist
-stimulates DA2 receptors = inhibition of NE release -parkinsons, type II diabetes |
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a2-agonists and DA2 agonists have more/less activity at high frequency nerve AP
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-les activity
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metyrosine
-what -effectiveness -uses |
-competitive inhibitor of tyrosine hydroxylase
-decreases catecholamines by 80% -treatment of pheochromocytomas |
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Reserpine and guanethidine:
-what they do |
-reduced concentration of NE in synaptic vesicles and amount released
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T/F - reserpine and guanethidine have the same mechanism
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-false
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Reserpine:
-mechanism -uses -side effects |
-irreversibly inactivates the vesicular monoamine transporter
-first antihypertensive drug -depression, ulcers (not used today) |
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Guanethidine:
-mechanism -uses |
-competes with NE for the NE transporter
-orally effective antihypertensive (rarely used) |
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bretylium, guanethidine, guanadrel
-what -how -action |
-membrane stabilizing compounds
-structurally similar to NE -act like LA b/c the neuronal impulse fails to release NE -also prevent fusion of vesicles with membrane |
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Ephedrine:
-what |
-false transmitter = indirect agonist, replaces NE in SV but lower efficacy at receptors
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Aldomet:
-what -receptors |
-false transmitter/precursor --> converted to MNE in terminal
-a2 agonist (potent); weak at a1/b1 |
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What is intrinsic sympathomimetic activity?
-dependent on |
-inhibition of amine I transport and indirect agonist activities
-dose, time, administration, interactions |
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phenoxybenzamine:
-what -can also produce -uses |
-noncompetitive alpha-1 antagonist
-reflex tachycardia b/c B1 in heart is not inhibited -not widely used b/c of severe side effec |
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Prazosin:
-what -causes -antidote for |
-competitive alpha1 antagonist
-vasodilation --> tx hypertension -scorpion sting -second line drug |
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Phentolamine:
-what -used to diagnose -dental use |
-non-selective alpha receptor blocker
-pheochromocytoma -reverse LA (oraverse) |
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Which type of drugs are good to use in patients with asthma being treated for hypertension
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-selective beta-1 blcokers (less prone to inducing bronchoconstriction)
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timolol, metoprolol, propanolol
-used for what -what are they |
-prophylaxis to prevent recurrence of MI
-beta-adrenoceptor antagonists |
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timolol
-what -uses |
-beta-adrenoceptor antagonist
-relieve intraocular pressure in glaucoma |
