Tiagabine (Gabitril) is a GABA reuptake inhibitor resulting in higher levels of cerebral GABA available for inhibition of the epileptic excitatory activity. With a relatively short half-life of 5 to 8 h ultimate dosage should be administered tid. Absorption is slower and the drug more easily tolerated when given with meals. Metabolism is via the P-450 mechanism and, as a result, the half-life is significantly reduced by coadministration with enzyme inducers such as carbamazepine, phenytoin, and phenobarbital. The maximum effective dose in children at this time is estimated to be 1 mg/kg/day. This dose should be started at 0.1 mg/kg/day and gradually increased over the next 6 to 10 weeks. Because of high protein binding, free levels of coadministered AEDs should be monitored (phenytoin, carbamazepine, and valproate). Most common side effects are sedation and behavioral. Activation of myoclonic seizures can also occur.
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