HUMAN IN VITRO GLUTATHIONYL AND PROTEIN ADDUCTS OF CARBAMAZEPINE-10,11-EPOXIDE, A STABLE AND PHARMACOLOGICALLY ACTIVE METABOLITE OF CARBAMAZEPINE

• Published in: Drug metabolism and disposition Vol. 33; no. 12; pp. 1920 - 1924
• Main Authors: Bu, Hai-Zhi, Kang, Ping, Deese, Alan J, Zhao, Ping, Pool, William F
• Format: Journal Article
• Language: English
• Published: Bethesda, MD American Society for Pharmacology and Experimental Therapeutics 01.12.2005
• Subjects: Biological and medical sciences; Carbamazepine - analogs & derivatives; Carbamazepine - metabolism; Glutathione - metabolism; Humans; Medical sciences; Microsomes, Liver - metabolism; Pharmacology. Drug treatments; Protein Binding; Human; Metabolite; Mood stabilizer; Epoxide; Anticonvulsant; Tricyclic compound; In vitro; Molecular adduct; Carbamazepine; Adduct; Protein

The clinical use of carbamazepine (CBZ), an anticonvulsant, is associated with a variety of idiosyncratic adverse reactions that are likely related to the formation of chemically reactive metabolites. CBZ-10,11-epoxide (CBZE), a pharmacologically active metabolite of CBZ, is so stable in vitro and i...