Radulovic L L, Wilder B J, Leppik I E, Bockbrader H N, Chang T, Posvar E L, Sedman A J, Uthman B M, Erdman G R
Department of Pharmacokinetics/Drug Metabolism and Clinical Pharmacology, Parke-Davis Pharmaceutical Research, Division of Warner-Lambert Company, Ann Arbor, Michigan.
Epilepsia. 1994 Jan-Feb;35(1):155-61. doi: 10.1111/j.1528-1157.1994.tb02926.x.
Gabapentin (GBP) studies were conducted in patients with epilepsy receiving carbamazepine (CBZ, n = 12) or valproate (VPA, n = 14) monotherapy. The effects of GBP coadministration on steady-state CBZ or VPA concentrations and of these antiepileptic drugs (AEDs) on GBP pharmacokinetics were investigated. GBP (400 mg) was coadministered every 8 h for 3 1/3 days with CBZ or for 5 1/3 days with VPA. GBP was well tolerated. Mean steady-state plasma CBZ/CBZ-10,11-epoxide (CBZ-E) and serum VPA concentrations before, during, and after GBP administration were not significantly different. Mean steady-state GBP pharmacokinetic parameters during CBZ or VPA coadministration were similar to steady-state parameters reported in healthy subjects. Thus, no pharmacokinetic interaction exists between CBZ or VPA and GBP. No dosage adjustment is necessary when GBP and CBZ or VPA are coadministered.
在接受卡马西平(CBZ,n = 12)或丙戊酸盐(VPA,n = 14)单药治疗的癫痫患者中开展了加巴喷丁(GBP)研究。研究了联合使用GBP对CBZ或VPA稳态浓度的影响,以及这些抗癫痫药物(AEDs)对GBP药代动力学的影响。GBP(400 mg)每8小时与CBZ联合给药3 1/3天,或与VPA联合给药5 1/3天。GBP耐受性良好。在GBP给药前、给药期间和给药后,CBZ/CBZ - 10,11 - 环氧化物(CBZ - E)的平均稳态血浆浓度和血清VPA浓度无显著差异。在CBZ或VPA联合给药期间,GBP的平均稳态药代动力学参数与健康受试者报告的稳态参数相似。因此,CBZ或VPA与GBP之间不存在药代动力学相互作用。当GBP与CBZ或VPA联合使用时,无需调整剂量。