Importance of establishing the presence of drug active metabolites

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Drugs are frequently effective because they are biotransformed into metabolites. The presence of these metabolites may be suspected when the parent compound is found in a target organ for a shorter time than the duration of the biochemical, pharmacological or toxicological effect or when a given activity in vivo cannot be observed in vitro. In some cases the metabolite may be easily detected whereas in other cases it may be highly reactive and bound to macromolecules. Examples of different drugs whose biotransformation results in active metabolites are given.

Original languageEnglish
Pages (from-to)97-108
Number of pages12
JournalEuropean Journal of Drug Metabolism and Pharmacokinetics
Issue number2
Publication statusPublished - Apr 1983


  • active metabolites
  • adriamycin
  • benzodiazepines
  • cyclophosphamide
  • fenfluramine
  • trazodone

ASJC Scopus subject areas

  • Pharmacology
  • Pharmacology (medical)
  • Pharmacology, Toxicology and Pharmaceutics(all)


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