Debruyne Danièle, Pailliet-Loilier Magalie, Lelong-Boulouard Véronique, Coquerel Antoine, Bentué-Ferrer Danièle
Service de Pharmacologie-Toxicologie, CHU Côte de Nacre, Caen, France.
Therapie. 2010 May-Jun;65(3):219-24. doi: 10.2515/therapie/2010027. Epub 2010 Aug 11.
Clonazepam is a 1-4 benzodiazepine mainly used to treat epilepsy and epileptiform convulsion state. Rapidly absorbed after oral administration, it is widely distributed in the organism and is extensively converted in metabolites, poorly or not active, eliminated mainly in urine (70%) and feces. Elimination half-life is long, around 40 h. In adult and child, several studies showed a concentration-effect relation. Meanwhile, a large inter-individual variability in the dose-concentration relation was observed. A 15-50 microg/L range of clonazepam blood concentrations appears to be retained as an acceptable target to control a majority of epileptic seizures. The Therapeutic Drug Monitoring (TDM) of clonazepam can be considered as possibly useful in case of association with CYP450 inducers or inhibitors, suspicion of poor observance, or toxicity signs.
氯硝西泮是一种1,4 - 苯二氮䓬类药物,主要用于治疗癫痫和癫痫样惊厥状态。口服后迅速吸收,广泛分布于机体中,并在代谢产物中大量转化,代谢产物活性低或无活性,主要通过尿液(70%)和粪便排出。消除半衰期较长,约为40小时。在成人和儿童中,多项研究显示了浓度 - 效应关系。同时,观察到剂量 - 浓度关系存在较大的个体间差异。氯硝西泮血药浓度在15 - 50微克/升范围内似乎可作为控制大多数癫痫发作的可接受目标。在与CYP450诱导剂或抑制剂联合使用、怀疑服药依从性差或出现毒性体征的情况下,氯硝西泮的治疗药物监测(TDM)可能有用。