Pharmacokinetics and bioavailability of carvedilol, a vasodilating beta-blocker.
The pharmacokinetics and absolute bioavailability of carvedilol have been studied in 20 male healthy volunteers in a randomised 4-period, cross-over trial. Carvedilol 12.5 mg was given i.v., 50 mg was administered p.o. as a suspension and 25 and 50 mg were given in a capsule formulation. For the 50 mg capsule Cmax was 66 micrograms.l-1, tmax 1.2 h, t1/2 6.4 h. The t1/2 after i.v. administration was 2.4 h, CL 589 ml/min and VZ 132 l. The absolute bioavailability was 24% (50 mg capsule). The kinetics after the 25 and 50 mg capsules were consistent with dose linearity.
Clinical Pharmacology, Boehringer Mannheim GmbH, Federal Republic of Germany.
E
E
von Möllendorff
K
K
Reiff
G
G
Neugebauer
D000284:Administration, Oral; D000328:Adult; D001682:Biological Availability; D002214:Capsules; D002227:Carbazoles / Q000008:administration & dosage / Q000493:pharmacokinetics*; D000077261:Carvedilol; D006207:Half-Life; D006801:Humans; D007262:Infusions, Intravenous; D007408:Intestinal Absorption; D008297:Male; D011412:Propanolamines / Q000008:administration & dosage / Q000493:pharmacokinetics*; D011897:Random Allocation; D013535:Suspensions; D014665:Vasodilator Agents / Q000008:administration & dosage / Q000493:pharmacokinetics*
D002214:Capsules; D002227:Carbazoles; D011412:Propanolamines; D013535:Suspensions; D014665:Vasodilator Agents; D000077261:Carvedilol