Dmd #6866 Human in Vitro Glutathionyl and Protein Adducts of Carbamazepine- 10,11-epoxide, a Stable and Pharmacologically Active Metabolite of Carbamazepine
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Human in vitro glutathionyl and protein adducts of carbamazepine-10,11-epoxide, a stable and pharmacologically active metabolite of carbamazepine.
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 in vivo that the potential for the epoxide to covalently interact with macromolecules has not been...
متن کاملAccelerated Communication HUMAN IN VITRO GLUTATHIONYL AND PROTEIN ADDUCTS OF CARBAMAZEPINE- 10,11-EPOXIDE, A STABLE AND PHARMACOLOGICALLY ACTIVE METABOLITE OF CARBAMAZEPINE
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 in vivo that the potential for the epoxide to covalently interact with macromolecules has not been...
متن کاملPlasma concentrations of carbamazepine and carbamazepine 10,11-epoxide during pregnancy and after delivery.
Plasma concentrations of carbamazepine were monitored in 9 pregnant epileptic patients treated with the drug alone at constant doses during pregnancy and for at least 3 months after delivery. In addition, plasma concentrations of the metabolite, carbamazepine 10,11-epoxide were measured in 6 of the 9 patients. Plasma carbamazepine concentrations were fairly stable during pregnancy, and carbamaz...
متن کاملCarbamazepine-viloxazine interaction in patients with epilepsy.
In six depressed epileptic patients stabilised on carbamazepine therapy, addition of the antidepressant agent viloxazine (300 mg/day for three weeks) induced a marked (average 55%) increase in steady-state plasma carbamazepine concentration. The concentration of the active metabolite carbamazepine-10,11-epoxide also increased during viloxazine therapy, but to a lesser extent (16%). In three pat...
متن کاملThe mechanism of the carbamazepine-valproate interaction in humans.
AIMS The study investigated the mechanism of the interaction between valproate and carbamazepine which causes raised plasma carbamazepine-10,11-epoxide concentrations with unchanged plasma carbamazepine concentrations. This interaction has usually been attributed to valproate inhibiting epoxide hydrolase, the enzyme that catalyses the biotransformation of carbamazepine-10,11-epoxide to carbamaz...
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تاریخ انتشار 2005