Summary
The metabolism of carvedilol was investigated in plasma and urine of 3 healthy male volunteers after administration of 50mg of [14C]-labeIled drug. Rapid and extensive biotransformation occurred. After 1.5h 9% of total radioactivity in plasma consisted of unchanged drug, 22% of carvedilol-glucuronide and another 20% of oxidative cleavage products of the beta-blocking side chain. Urinary excretion of radioactivity amounted to 16% of which 2% represented unchanged drug, 32% carvedilol-glucuronide and about 25% side chain oxidation products. Ring-hydroxylated metabolites of Carvedilol accounted for 18% of the radioactive compounds in the urine.
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Sponer G., Bartsch W., Strein K., Müller-Beckmann B. (1982) The pharmacological profile of BM 14.190, a compound with beta-blocking and vasodilating properties. Arch. Pharmacol., 321 (Suppl), R21.
Sponer G., Müller-Beckmann B. (1983) Studies on the mechanism of the vasodilating activity of BM 14.190. Arch. Pharmacol., 322 (Suppl), R46.
Strein K., Abshagen U., von Möllendorff E., Bartsch W., von Möllendorff E., Müller-Beckmann B., Sponer G. (1983) Pharmakologische und klinisch-pharmakologische Grundlagen für die antihypertensive und antianginöse Therapie mit den vasodilatierenden β-Blockern BM 14.190 (A) und BM 12.434 (B). Z. Kardiol., 72 (Suppl), 1: 103.
von Möllendorff E., Abshagen U., Akpan W., Neugebauer G., Schröter E. (1986) Clinical pharmacological investigations with carvedilol, a new beta-blocker with direct vasodilator activity. Clin. Pharmacol. Ther., 39, 677–682.
von Möllendorff E., Reiff K., Neugebauer G. (1987) Pharmacokinetics and bioavailability of carvedilol, a vasodilating beta-blocker. Eur. J. Clin. Pharmacol., 33, 511–551
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Neugebauer, G., Neubert, P. Metabolism of carvedilol in man. European Journal of Drug Metabolism and Pharmacokinetics 16, 257–260 (1991). https://doi.org/10.1007/BF03189969
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DOI: https://doi.org/10.1007/BF03189969