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Metabolism of carvedilol in man

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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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Authors and Affiliations

  1. Department of Clinical Pharmacology, Boehringer Mannheim GmbH, Sandhofer Stra Be 116, D-6800, Mannheim 31, Germany

    G. Neugebauer & P. Neubert

  2. Department of Bioanalytics, Boehringer Mannheim GmbH, Mannheim, Germany

    G. Neugebauer & P. Neubert

Authors
  1. G. Neugebauer
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  2. P. Neubert
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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

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