Carbamazepine is an iminostilbene derivative that is used as both an anticonvulsant and for the relief of pain associated with trigeminal neuralgia (tic douloureux) as well as for various psychiatric disorders. The anticonvulsant activity of carbamazepine, like phenytoin, principally involves limitation of seizure propagation by reduction of posttetanic potentiation (PTP) of synaptic transmission. Carbamazepine appears to provide relief of pain in trigeminal neuralgia by reducing synaptic transmission within the trigeminal nucleus.
藥動學
Carbamazepine is slowly absorbed from the GI tract. Carbamazepine is widely distributed in the body; the drug has been detected in CSF (approximately 15–22% of serum concentrations), the brain (at autopsy), duodenal fluids, bile, and saliva. A major metabolic pathway appears to be oxidation by microsomal enzymes in the liver (principally cytochrome P-450 isoform 3A4) to form carbamazepine 10,11-epoxide (CBZ-E). Carbamazepine and its metabolites are excreted in urine. Only about 1–3% of the drug is excreted in urine unchanged. Carbamazepine has a relatively long plasma half-life, variously reported to be 8–72 hours.
禁忌症
Patients with previous bone marrow depression, hypersensitivity to carbamazepine and with a hisotry of cardiac, hepatic, or renal disease. Allergic reaction: Tegretol has been reported to cause type I (immediate) hypersensitivity reactions, including rash, itching, hives, angioedema.<20240130>
懷孕分類
D Carbamazepine may cause fetal neurodevelopmental disorders and malformations(including spina bifida, craniofacial defects, cardiovascular malformations, and hypospadias).<20240130>
哺乳分類
Safe. The milk/plasm ratio is low (0.24-0.69). However, the drug should be discontinued if signs and symptoms occur in infant (jaundice, poor sucking, vomiting, or tiredness).
Epilepsy: initial dose 100-200 mg, 1-2 times daily, gradually increased of 200 mg/day to a usual maintenance dose of 0.8 to 1.2 g daily in 2-4 divided doses up to 1.6 g/day. Trigeminal neuralgia: initial dose 100 mg BID, increased by 200 mg daily up to 1.2 g daily, usual maintenance dose 400-800 mg daily in 2-4 divided doses. Tegretol controlled release Tab can be divided into two parts butcould not be crashed. For shifting from conventional tablet to controlled release form, increasing of 10-20% dose is recommended.