The metabolism of carbamazepine in humans: steric course of the enzymic hydrolysis of the 10, 11-epoxide

G Bellucci, G Berti, C Chiappe, A Lippi…

Index: Belluci, Giuseppe; Berti, Giancarlo; Chiappe, Cinzia; Lippi, Annalisa; Marioni, Franco Journal of Medicinal Chemistry, 1987 , vol. 30, # 5 p. 768 - 773

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Citation Number: 66

Abstract

Carbamazepine 10, ll-oxide (la, lOb-dihydro-6H-dibenzo [b, floxireno [d] azepine-6- carboxamide), a key intermediate in carbamazepine metabolism, was found to be unusually resistant to enzymatic hydrolysis when incubated with microsomal and cytosolic fractions from rabbit, rat, and guinea pig livers. However, its hydrolysis product, trans-lO, ll-dihydro-l0, 1 l-dihydroxy-5H-dibenzo [b, flazepine-5-carboxamide, was excreted, as previously ...