Relationship between plasma concentrations and pharmacological effects of labetalol.

Abstract:

:In healthy normal subjects following the administration of labetalol the pharmacological effects were measured and compared with the plasma concentrations achieved. The inhibition of exercise induced tachycardia and inhibition of exercise induced increases in systolic pressure were significantly related to the administered dose of labetalol. Labetalol was rapidly absorbed from the gastrointestinal tract and peak plasma concentrations occurred two hours after oral administration. There was a linear correlation (r = 0.84) between the logarithm of the plasma concentration and the maximum inhibition of exercise tachycardia at two hours. After intravenous administration there was an immediate reduction in systolic and diastolic blood pressure with a concomitant small increase in heart rate. There was a rapid decline in the associated plasma concentration but the pharmacological effects were maintained in excess of two hours. Our findings are consistent with those of others who have studied the relationship between pharmacological events and plasma concentrations after single doses of other adrenoceptor blocking drugs.

journal_name

Eur J Clin Pharmacol

authors

Richards DA,Maconochie JG,Bland RE,Hopkins R,Woodings EP,Martin LE

doi

10.1007/BF00562897

subject

Has Abstract

pub_date

1977-01-03 00:00:00

pages

85-90

issue

2

eissn

0031-6970

issn

1432-1041

journal_volume

11

pub_type

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