Clonidine and Related Drugs

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Clonidine (Catapres) is effective orally and is used primarily for the treatment of moderate hypertension. It is structurally related to the a-adrenoceptor antagonists phentolamine and tolazoline. Clonidine, however, is not an a-blocker, but is actually an a-agonist. Its antihyper-tensive effectiveness appeared paradoxical until it was recognized that clonidine activated central a2-receptors, thus reducing sympathetic outflow to the periphery.

Guanabenz (Wytensin) and guanfacine (Tenex) are two drugs with considerable structural similarity to clonidine. These agents also are central a2-agonists and exhibit an antihypertensive profile similar to that of clonidine.

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