Topiramate is a sulfamate-substituted monosaccharide, antiepileptic drug. Topiramate is indicated as adjunctive therapy for the treatment of patients with partial onset seizures or generalized tonic-clonic seizures. It cannot be used in children<2ys.
藥理
Potential advantages of topiramate are its lack of effect conventional antiepileptic agents (although phenytoin and carbamazepine can decrease topiramate serum concentrations), relatively long elimination half-life, and overall better tolerability compared to conventional agents; hematotoxicity or hepatotoxicity has not been reported in available trials. One disadvantage is its propensity to induce cognitive disturbances.
藥動學
Topiramate is well absorbed after oral doses; peak serum concentrations occur in 2 to 4 hours. Food alters the rate of absorption but not the extent. The plasma protein binding of topiramate is minimal (9% to 17%); its volume of distribution is 0.7 L/kg. Most of an oral dose is excreted unchanged in the urine. The elimination half-life of topiramate is 18 to 24 hours.
禁忌症
Hypersensitivity to topiramate;precaution in the following condition: Behavioral disorders or cognitive deficits, urolithiasis, paresthesia, renal impairment or hepatic impairment, topiramate and other antiepileptic drugs should be gradually withdrawn
懷孕分類
D
哺乳分類
No data available
副作用
Adverse effects of topiramate include cognitive dysfunction, paresthesias, sedation, dizziness, fatigue, weight loss, diarrhea, and urolithiasis. The drug appears better tolerated in regard to hematotoxicity and hepatic dysfunction.
劑量和給藥方法
Adults: partial seizures or generalized tonic-clonic seizures: 400 mg/day PO BID Children: the initial dose is topiramate 25 mg or less (1 to 3 mg/kg/day) nightly for 1 week. The dosage should then be increased by increments of 1-3 mg/kg/day administered in 2 divided doses at 1- to 2-week intervals.