Effect of oxidative polymorphism (debrisoquine/sparteine type) on hepatic first-pass metabolism of bufuralol

Eur J Clin Pharmacol. 1985;28(3):317-20. doi: 10.1007/BF00543330.


Bufuralol is a beta-adrenoceptor blocking drug whose oxidative metabolism is under the same genetic control as debrisoquine and sparteine. The pharmacokinetics of bufuralol were studied in 10 healthy subjects (7 extensive and 3 poor metabolizers of debrisoquine) after oral and intravenous administration. In extensive metabolizers the systemic availability of bufuralol was 43%. Poor metabolizers were characterized by a considerable increase in systemic availability due to a corresponding decrease in hepatic first-pass metabolism. After oral administration of bufuralol non-linear kinetics may occur.

MeSH terms

  • Adrenergic beta-Antagonists / metabolism*
  • Adult
  • Debrisoquin / metabolism
  • Ethanolamines / metabolism*
  • Humans
  • Kinetics
  • Liver / metabolism*
  • Oxidation-Reduction
  • Polymorphism, Genetic
  • Sparteine / metabolism


  • Adrenergic beta-Antagonists
  • Ethanolamines
  • Sparteine
  • bufuralol
  • Debrisoquin