Inhibition by erythromycin of the conversion of carbamazepine to its active 10,11-epoxide metabolite.
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.
Department of Internal Medicine and Therapeutics, University of Pavia, Italy.
N
N
Barzaghi
G
G
Gatti
F
F
Crema
M
M
Monteleone
C
C
Amione
L
L
Leone
E
E
Perucca
D000328:Adult; D001711:Biotransformation / Q000187:drug effects; D002220:Carbamazepine / Q000031:analogs & derivatives* / Q000378:metabolism* / Q000493:pharmacokinetics; D003864:Depression, Chemical; D004917:Erythromycin / Q000494:pharmacology*; D006801:Humans; D008297:Male
D002220:Carbamazepine; D004917:Erythromycin; C012227:carbamazepine epoxide