a Department of Neurosciences, Biomedicine and Movement Sciences , University of Verona , Verona , Italy.
b Department of Neurology , Franz Tappeiner Hospital , Merano , Italy.
Expert Opin Pharmacother. 2018 May;19(7):743-747. doi: 10.1080/14656566.2018.1462338. Epub 2018 Apr 12.
Recently, an intravenous formulation of carbamazepine (CBZ) (sulphobutylether-7-beta-cyclodextrine carbamazepine, SBECD CBZ) has been developed and approved by the U.S. Food and Drug Administration. It is indicated as a short-term replacement therapy for oral CBZ formulations, when oral administration is temporarily not feasible and in adults with focal seizures with complex symptomatology as well as generalized tonic-clonic seizures and mixed seizure patterns. Areas covered: This review focuses on the drug development, pharmacokinetics and pharmacodynamics of intravenous CBZ and provides a comprehensive overview of the studies assessing its clinical efficacy, tolerability and safety in adults with epilepsy. Expert opinion: Intravenous CBZ has favorable pharmacokinetics and is well tolerated and safe when used as a short-term substitution for oral CBZ. Seizure control was unchanged after switching from oral to IV formulations. Overall, this new formulation represents a useful option to enhance continuity of care in adults with focal or generalized tonic-clonic seizures when oral CBZ administration is temporarily unfeasible. Further studies are needed to assess the efficacy and tolerability of IV CBZ used at larger doses (above 1600 mg/day), for a period longer than 7 days or for other indications not approved by FDA, such as prolonged convulsive seizures and status epilepticus.
最近,美国食品和药物管理局批准了一种卡马西平(CBZ)的静脉制剂(磺丁基醚-β-环糊精 CBZ,SBECD CBZ)。它被指示为口服 CBZ 制剂的短期替代疗法,当口服暂时不可行时,以及用于具有复杂症状的局灶性发作以及全身性强直阵挛发作和混合发作模式的成年患者。
本综述重点介绍了静脉 CBZ 的药物开发、药代动力学和药效学,并全面评估了评估其在癫痫成人中的临床疗效、耐受性和安全性的研究。
静脉内 CBZ 具有良好的药代动力学特性,并且在作为口服 CBZ 的短期替代物使用时具有良好的耐受性和安全性。从口服转为 IV 制剂后,癫痫发作得到了控制。总体而言,这种新制剂为在口服 CBZ 暂时不可行时增强局灶性或全身性强直阵挛性癫痫成人的护理连续性提供了一种有用的选择。需要进一步研究来评估大剂量(超过 1600mg/天)、超过 7 天或其他未获得 FDA 批准的适应症(如延长的惊厥性癫痫发作和癫痫持续状态)使用 IV CBZ 的疗效和耐受性。