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外観
白色～ほとんど白色粉末～結晶
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効能
抗てんかん薬
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商品名
イノベロン (エーザイ)
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説明
Approximately 2.5 million people worldwide are afflicted with epilepsy, a
devastating neurological disorder diagnosed by the tendency toward recurrent,
unprovoked seizures, often of unknown etiology. Rufinamide has been launched primarily as adjunctive
therapy of LGS. Its proposed mechanism of action involves the limitation of
firing of sodium-dependent action potentials. The ultimate result is membrane
stabilization. Since it does not exhibit measurable binding to monoamine,
acetylcholine, histamine, glycine, AMPA/kainate, NMDA, or GABA receptors or
systems, these receptor-mediated pathways are not anticipated to be involved in
the exertion of rufinamide’s effects. Rufinamide displayed efficacy in several
electrical and chemical animal seizure models.
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化学的特性
White Solid
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使用
Labelled Rufinamide (R701552). Antiepileptic triazole derivative which decreases firing by neurons at sodium channels. Anticonvulsant.
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一般的な説明
An antiepileptic drug and anticonvulsant, Rufinamide is approved for the treatment of partial seizures associated with Lennox-Gastaut syndrome in adults and children 4 years and older. Rufinamide is marketed as Banzel® in the US and Inovelon® in the EU.
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生物活性
Board spectrum anticonvulsant. Prolongs the inactivation of sodium channels and limits the frequency of action potential firing in cultured and acutely isolated neurons. Displays anticonvulsive activity in a range of animal seizure models.
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副作用
Rufinamide was well tolerated with the most common adverse events including fatigue, somnolence, tremors, mild-to-moderate dizziness, nausea, headache, and diplopia. Since rufinamide is not metabolized by the CYP450 system, it is anticipated to have a low potential for interaction with drugs metabolized by the CYP isozymes. Rufinamide, however, does exhibit clinically relevant interactions with other antiepileptic drugs; concomitant treatment with valproate results in a reduction in rufinamide clearance while concomitant treatment with phenytoin, primidone, phenobarbital, carbamazepine, or vigabatrin causes an increase in rufinamide clearance. In these situations, rufinamide dosage adjustment may be required.
