Rheims Sylvain, Ryvlin Philippe
Department of Functional Neurology and Epileptology, Hospices Civils de Lyon, Lyon, France.
Expert Rev Neurother. 2009 Feb;9(2):167-73. doi: 10.1586/14737175.9.2.167.
In order to improve patient compliance and decrease toxicity of antiepileptic drugs (AEDs), the recent strategy for epilepsy management has been to expand the use of extended-release (XR) formulations. Lamotrigine (LTG), an AED with broad efficacy, is available as a twice-daily immediate-release formulation. A once-daily XR formulation of LTG (LTG-XR) is currently being developed. LTG-XR tablets contain a modified-release eroding matrix formulation designed to control the dissolution rate of LTG. The bioavailability of LTG-XR is similar to that of LTG-IR, except in patients taking enzyme-inducing AEDs in whom the bioavailability of LTG-XR is 21% lower. In adult drug-resistant partial epilepsy, adjunctive LTG-XR effectively reduces the seizure frequency and is well tolerated. Trials in an elderly population with partial epilepsy as well as in adults with refractory primary tonic-clonic seizures are underway. Once-daily LTG-XR may represent a future option for patients with poor compliance to twice-daily immediate-release LTG.
为了提高患者的依从性并降低抗癫痫药物(AEDs)的毒性,癫痫管理的最新策略是扩大缓释(XR)制剂的使用。拉莫三嗪(LTG)是一种疗效广泛的AED,有每日两次的速释制剂。目前正在研发LTG的每日一次的XR制剂(LTG-XR)。LTG-XR片剂含有一种控释侵蚀性基质制剂,旨在控制LTG的溶解速率。LTG-XR的生物利用度与LTG-IR相似,但服用酶诱导性AEDs的患者除外,在这些患者中,LTG-XR的生物利用度低21%。在成人耐药性部分性癫痫中,辅助使用LTG-XR可有效降低癫痫发作频率,且耐受性良好。针对老年部分性癫痫患者以及难治性原发性强直-阵挛性发作的成人患者的试验正在进行中。对于每日两次速释LTG依从性差的患者,每日一次的LTG-XR可能是一种未来选择。