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Carbamazepine: Urine
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Carbamazepine can induce its own metabolism. It is metabolized in the liver to an epoxide and several other metabolites. A major metabolic pathway is oxidation by microsomal enzymes to form carbamazepine 10, 11 epoxide. This is an active compound and is almost completely metabolized to an inactive metabolite, trans-10,11-dihydroxy-10,11- dihydrocarbamazepine (trans-carbamazepine-diol), and excreted in the urine mainly in an unconjugated form. Carbamazepine is ... inactivated by conjugation and hydroxylation.
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Carbamazepine is metabolized in the liver, where the epoxide pathway of biotransformation is the most important one, yielding the 10,11-transdiol derivative and its glucuronide as the main metabolites. Cytochrome P4503A4 has been identified as the major isoform responsible for the formation of the pharmacologically active carbamazepine-10,11 epoxide from carbamazepine. 9-Hydroxy-methyl-10-carbamoyl acridan is a minor metabolite related to this pathway. After a single oral dose of carbamazepine about 30% appears in the urine as end-products of the epoxide pathway. Other important biotransformation pathways for carbamazepine lead to various monohydroxylated compounds, as well as to the N-glucuronide of carbamazepine produced by UGT2B7.
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C-Carbamazepine, 72% of the administered radioactivity was found in the urine and 28% in the feces. This urinary radioactivity was composed largely of hydroxylated and conjugated metabolites, with only 3% of unchanged Carbamazepine.
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