Inhibition by erythromycin of the conversion of carbamazepine to its active 10,11-epoxide metabolite

Br J Clin Pharmacol. 1987 Dec;24(6):836-8. doi: 10.1111/j.1365-2125.1987.tb03257.x.

Abstract

The serum levels of carbamazepine (CBZ) and its 10,11-epoxide metabolite (CBZ-E) were determined in seven subjects after a single dose of CBZ (400 mg) in the control state and during co-administration of erythromycin (500 mg three times daily for 10 days). Erythromycin treatment was associated with a decrease in CBZ clearance and a prolongation of CBZ half-life, while CBZ-E levels were markedly reduced. These data provide evidence that erythromycin inhibits the conversion of CBZ to its epoxide metabolite.

Publication types

  • Clinical Trial
  • Randomized Controlled Trial

MeSH terms

  • Adult
  • Biotransformation / drug effects
  • Carbamazepine / analogs & derivatives*
  • Carbamazepine / metabolism*
  • Carbamazepine / pharmacokinetics
  • Depression, Chemical
  • Erythromycin / pharmacology*
  • Humans
  • Male

Substances

  • Carbamazepine
  • Erythromycin
  • carbamazepine epoxide