Tribut Olivier, Bentué-Ferrer Danièle, Verdier Marie-Clémence
Laboratoire de Pharmacologie Biologique, CHU Pontchaillou, Rennes, France.
Therapie. 2010 Jan-Feb;65(1):35-8. doi: 10.2515/therapie/2009068. Epub 2010 Mar 8.
Felbamate is a derivative of meprobamate used in second-line partial epilepsy and in the Lennox-Gastaut syndrome. Felbamate is well absorbed and has linear kinetics: C(max) and AUC increasing linearly with dose. The metabolism takes place in the liver. Metabolites represent 40 to 60% of excretion and are eliminated via the urine. The half-life is between 15 and 23 hours. Clearance is dependent on renal function. There is a concentration - efficacy and concentration - toxicity relationship. These arguments are in favour of a TDM but the therapeutic range is not clearly established. Potentially fatal side effects can be caused by felbamate (aplastic anemia, acute liver failure), which limits its use because they are dose-independant.
非氨酯是眠尔通的衍生物,用于二线治疗部分性癫痫和伦诺克斯 - 加斯东综合征。非氨酯吸收良好,具有线性动力学:C(max)和AUC随剂量呈线性增加。代谢在肝脏中进行。代谢产物占排泄量的40%至60%,并通过尿液排出。半衰期在15至23小时之间。清除率取决于肾功能。存在浓度 - 疗效和浓度 - 毒性关系。这些因素支持进行血药浓度监测,但治疗范围尚未明确确定。非氨酯可引起潜在致命的副作用(再生障碍性贫血、急性肝衰竭),由于这些副作用与剂量无关,因此限制了其使用。