Remacemide: current status and clinical applications

Remacemide (RMC) is a non-competitive, low-affinity N-methyl-D-aspartate (N MDA) receptor antagonist that does not cause the behavioural and neuropatho logical side effects seen with other NMDA receptor antagonists. RMC and its active metabolite, AR-R 12495 AR, which has moderate affinity for the NMDA receptor, also interact with voltage-dependent neuronal sodium channels. B oth agents show efficacy in a variety of animal models of epilepsy, parkins onism and cerebral ischaemia. There is no evidence for teratogenicity or ge notoxicity. RMC delays the absorption of L-dopa and elevates the concentrat ions of drugs metabolised by the hepatic cytochrome P450 3A4 isoform. RMC a nd AR-R 12495 AR have moderate protein binding and linear pharmacokinetics. Controlled studies show evidence of efficacy in treating epilepsy and Park inson's disease. Post-surgical outcomes in RMC-treated patients at risk for intra-operative cerebral ischaemia are also encouraging. Adverse effects a re related to the gastrointestinal and central nervous systems. RMC is a pr omising drug with numerous potential applications for both acute or chronic conditions associated with glutamate-mediated neurotoxicity.