Brivaracetam is an orphan drug for the treatment of symptomatic myoclonus. It is a novel high-affinity SV2A ligand that also displays inhibitory activity at neuronal voltage-dependent sodium channels. It possesses a selective binding affinity for SV2A, 13 times higher than that of levetiracetam, and also shows an ability to inhibit sodium channels.
Brivaracetam has nearly complete bioavailability after oral administration. The half-life is approximately 8 h. Brivaracetam is primarily metabolized via hydrolysis of the acetamide group and CYP2C8-mediated hydroxylation. Its metabolites are not pharmacologically active. Brivaracetam is weakly bound to plasma proteins, at approximately 17.5%. Excretion of over 95% of the dose, including metabolites, occurs renally within 72 h of administration.
The pharmacokinetic profile of brivaracetam is unaltered in patients with impaired renal function or by hemodialysis. It is not necessary to adjust treatment initiation doses or to administer supplemental doses after hemodialysis.
Expert Rev Neurother. 2012;12(1):99-105. © 2012 Expert Reviews Ltd.