Relationship of N-demethylation of amiflamine and its metabolite to debrisoquine hydroxylation polymorphism

Clin Pharmacol Ther. 1984 Oct;36(4):515-9. doi: 10.1038/clpt.1984.212.

Abstract

The metabolism of the new reversible A-selective monoamine oxidase inhibitor amiflamine was studied in relation to polymorphic hydroxylation of debrisoquine in 24 healthy subjects. Amiflamine is metabolized by two consecutive N-demethylations. By construction of urinary recovery ratios analogous to that of debrisoquine/4-hydroxydebrisoquine, correlations between debrisoquine metabolic ratio and amiflamine/demethylated metabolites were significant and consistent within slow and rapid hydroxylators of debrisoquine. It is concluded that debrisoquine hydroxylation and amiflamine N-demethylation might be under common genetic regulation.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Administration, Oral
  • Adult
  • Biotransformation
  • Debrisoquin / metabolism*
  • Debrisoquin / urine
  • Humans
  • Hydroxylation
  • Isoquinolines / metabolism*
  • Male
  • Phenethylamines / metabolism*
  • Phenethylamines / urine
  • Polymorphism, Genetic

Substances

  • Isoquinolines
  • Phenethylamines
  • amiflamine
  • Debrisoquin