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- W2290708766 abstract "Topiramate is rapidly and almost completely absorbed after oral ingestion, with a bioavailability of 81-95%. Absorption is slowed, but not decreased, by food, and therefore topiramate can be administered without regard to meal times. The pharmacokinetics of topiramate are linear, with plasma concentrations increasing in proportion to dose over the clinically relevant dosage range. The drug distributes primarily to body water. It is minimally bound to plasma proteins (13-17%). Topiramate is not extensively metabolized, <15% being metabolized to six metabolites, all of which are pharmacologically inactive. It is eliminated, mainly unchanged via the kidneys, with an elimination half-life in healthy volunteers of 19-25 h. In patients comedicated with hepatic enzyme-inducing antiepileptic drugs, elimination half-life values of 9-12 h can be expected. The plasma and renal clearances of topiramate are decreased in patients with significant renal impairment, so that dosage reductions would be necessary in these patients. Furthermore, topiramate plasma concentration may rise modestly (20-30%) in patients with hepatic impairment. In children, the pharmacokinetics of topiramate are similar to those of adults except that clearance is 50% faster, resulting in topiramate plasma concentrations that are 33% lower. Hepatic enzyme-inducing antiepileptic drugs, such as phenytoin, phenobarbitone and carbamazepine, induce the metabolism of topiramate, so that topiramate plasma concentrations can be expected to decrease by approximately 40% in the presence of such drugs. In addition, topiramate can increase phenytoin concentrations by as much as 25% and this can prove to be clinically significant in patients whose phenytoin metabolism is at, or near, saturation. Topiramate enhances the metabolism of digoxin and the oestrogen component of oral contraceptives. Overall, topiramate demonstrates favourable pharmacokinetics, which should aid its clinical use." @default.
- W2290708766 created "2016-06-24" @default.
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- W2290708766 title "The pharmacokinetic profile of topiramate" @default.
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