Brodie Martin J, Wilson Elaine A, Wesche David L, Alvey Christine W, Randinitis Edward J, Posvar Edward L, Hounslow Neil J, Bron Nicola J, Gibson G L, Bockbrader Howard N
Pfizer, Global Research and Development, Ann Arbor, Michigan 48105, USA.
Epilepsia. 2005 Sep;46(9):1407-13. doi: 10.1111/j.1528-1167.2005.19204.x.
Pregabalin (PGB) is an alpha2-delta ligand with demonstrated efficacy in epilepsy, neuropathic pain, and anxiety disorders. PGB is highly efficacious as adjunctive therapy in patients with refractory partial seizures.
Given its efficacy as adjunctive therapy, the potential for interaction of PGB with other antiepileptic drugs (AEDs) was assessed in patients with partial epilepsy in open-label, multiple-dose studies. Patients received PGB, 600 mg/day (200 mg q8h) for 7 days, in combination with their individualized maintenance monotherapy with valproate (VPA), phenytoin (PHT), lamotrigine (LTG), or carbamazepine (CBZ).
Trough steady-state concentrations of CBZ (and its epoxide metabolite), PHT, LTG, and VPA were unaffected by concomitant PGB administration. Likewise, PGB steady-state pharmacokinetic parameter values were similar among patients receiving CBZ, PHT, LTG, or VPA and, in general, were similar to those observed historically in healthy subjects receiving PGB alone. The PGB-AED combinations were generally well tolerated. PGB may be added to VPA, LTG, PHT, or CBZ therapy without concern for pharmacokinetic drug-drug interactions.
普瑞巴林（PGB）是一种α2-δ配体，已证明在癫痫、神经性疼痛和焦虑症治疗中有效。PGB作为难治性部分性癫痫患者的辅助治疗药物具有高效性。
鉴于其作为辅助治疗的有效性，在开放性、多剂量研究中，对部分癫痫患者评估了PGB与其他抗癫痫药物（AEDs）相互作用的可能性。患者接受PGB，600毫克/天（200毫克，每8小时一次），共7天，同时结合丙戊酸盐（VPA）、苯妥英（PHT）、拉莫三嗪（LTG）或卡马西平（CBZ）个体化维持单药治疗。
CBZ（及其环氧化物代谢物）、PHT、LTG和VPA的谷稳态浓度不受同时给予PGB的影响。同样，接受CBZ、PHT、LTG或VPA治疗的患者中，PGB的稳态药代动力学参数值相似，总体上与历史上单独接受PGB治疗的健康受试者中观察到的值相似。PGB与AEDs的联合用药通常耐受性良好。PGB可添加到VPA、LTG、PHT或CBZ治疗中，无需担心药代动力学药物相互作用。
