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. 1976 Oct;3(5):849-55.
doi: 10.1111/j.1365-2125.1976.tb00637.x.

Assessment of alpha- and beta-adrenoceptor blocking actions of labetalol

Assessment of alpha- and beta-adrenoceptor blocking actions of labetalol

D A Richards et al. Br J Clin Pharmacol. 1976 Oct.

Abstract

Isoprenaline dose-response curves plotting increases in heart rate before and after labetalol are suggestive of competitive antagonism at beta-adrenoceptor sites. Phenylephrine dose-response curves using increases in systolic pressure before and after labetalol are suggestive of competitive antagonism at alpha-adrenoceptor sites. The ratio of alpha:beta-adrenoceptor antagonism induced by labetalol is approximately 1:3. Peak pharmacological responses after a single oral dose of labetalol (400 mg) occurred between 90-120 min after administration.

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