司替戊醇
Stiripentol.
作者信息
Chiron Catherine
机构信息
INSERM, U663, Service de Neurologie et Métabolisme, Hôpital Necker, 149 rue de Sèvres, 75015 Paris, France.
出版信息
Neurotherapeutics. 2007 Jan;4(1):123-5. doi: 10.1016/j.nurt.2006.10.001.
Stiripentol (STP) is a new antiepileptic compound made by Biocodex. It recently proved to increase the GABAergic transmission in vitro in an experimental model of immature rat. Clinical studies were based on the fact that STP also acts as an inhibitor of CYP3A4, CYP1A2, and CYP2C19 in vivo in epileptic patients. Whereas the studies in adult patients were disappointing, the trials conducted in pediatric populations demonstrated a specific efficacy of STP in severe myoclonic epilepsy in infancy, Dravet syndrome, when combined with valproate and clobazam. Based on these results, STP was granted orphan drug status in the European Union for the treatment of Dravet syndrome. The French experience in compassionate use suggests that STP might also be of benefit when combined with carbamazepine in pediatric patients with pharmacoresistant partial epilepsy. The interactions of STP with a large number of drugs need to be carefully taken into account, with doses of the combined antiepileptic drugs adjusted to improve the tolerability of the therapeutic association.
司替戊醇（STP）是百康公司生产的一种新型抗癫痫化合物。最近在未成熟大鼠实验模型中证实，它能在体外增强γ-氨基丁酸能传递。临床研究基于这样一个事实，即STP在癫痫患者体内还可作为细胞色素P450 3A4、细胞色素P450 1A2和细胞色素P450 2C19的抑制剂。尽管在成年患者中的研究结果令人失望，但在儿科人群中进行的试验表明，STP与丙戊酸盐和氯巴占联合使用时，对婴儿严重肌阵挛性癫痫（德拉韦特综合征）具有特效。基于这些结果，STP在欧盟被授予孤儿药地位，用于治疗德拉韦特综合征。法国的同情用药经验表明，STP与卡马西平联合用于药物难治性部分性癫痫的儿科患者时，可能也有益处。需要仔细考虑STP与大量药物之间的相互作用，并调整联合使用的抗癫痫药物剂量，以提高治疗组合的耐受性。
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