Antipyrine metabolism is not affected by terbinafine, a new antifungal agent

Eur J Clin Pharmacol. 1989;37(3):231-3. doi: 10.1007/BF00679775.


The potential to inhibit drug metabolism of the new antifungal agent terbinafine has been studied using antipyrine (single oral dose of 10 mg/kg) as a probe drug. In a cross-over study in 8 healthy volunteers, antipyrine was administered prior to, during and after 8 days of oral terbinafine 125 mg b.d. Antipyrine, its major metabolites 4-hydroxyantipyrine (4-OH-AP), 3-hydroxymethylantipyrine (3-OH-CH3-AP) and norantipyrine (Nor-AP) were analyzed by specific HPLC assays in multiple plasma and urine samples. During all three parts of the study, the pharmacokinetics of antipyrine viz. t1/2 (11.7 h), total plasma (38.5 and renal clearance (1.6, and its clearance rates to metabolites (CLM), eg. CLM for 4-OH-AP (12.3, CLM for 3-OH-CH3-AP (4.2 and CLM for Nor-AP (6.7 did not differ from the control values. Thus, all the cytochrome P-450-dependent isozymes involved in the metabolism of antipyrine and many other drugs should not be affected by therapeutic doses of terbinafine.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adult
  • Antifungal Agents / pharmacology*
  • Antipyrine / metabolism*
  • Antipyrine / pharmacokinetics
  • Biotransformation
  • Female
  • Half-Life
  • Humans
  • Liver / drug effects
  • Liver / metabolism
  • Male
  • Middle Aged
  • Naphthalenes / pharmacology*
  • Terbinafine


  • Antifungal Agents
  • Naphthalenes
  • Terbinafine
  • Antipyrine