Name: Clonidine (Catapres)
Class: Centrally Acting Antiadrenergic Agent/Opioid Withdrawal Suppressant
Mechanism: Stim. inhib. a2 receptors in central cardiovasc pathways involving EPI or NE. a2 are G-protein coupled to inhibit adenylyl cyclase ®
¯ cAMP ® ¯ central symp. activity.
Absorption:
Dist.: Act at medullary and spinal sites.
Metabolism.:
Excretion, t½:
Toxicity/S.E.s: Prominent sedation, dry mouth.
Utility: Treat hypertension. DOC for treating opioid w/drawal (probably substitutes for opioid depression of adenylate cyclase in locus coeruleus & pregang. symp. neurons. No abstinence synd. when withdrawn.
Special Features: Direct a2 activation. Very potent (<0.5>