奥卡西平治疗创伤性癫痫的临床疗效分析

目的：分析和研究奥卡西平治疗创伤性癫痫的临床疗效。方法选取2011年6月~2013年2月创伤性癫痫患者64例,其中36例患者为单药治疗;28例患者为添加治疗,将64例患者的临床资料进行回顾性的分析与总结。结果单药治疗组的治疗总有效率94.4%;添加治疗组的治疗总有效率78.6%。结论将奥卡西平应用于创伤性癫痫患者的治疗中,效果较显著,其能够有效改善患者的癫痫症状,可将其做为首选用药,也可做为联合用药,并且不良反应症状较轻,相对安全,是值得临床推荐应用的新型抗癫痫类药物。     

奥卡西平致皮疹7例分析

目的 分析奥卡西平引起皮疹的相关因素. 方法 收集首都医科大学宣武医院2006～2008年由奥卡西平引起皮疹的患者资料.对患者的性别、年龄、临床表现、奥卡西平的用法用量、皮疹出现的时间和严重程度以及转归进行调查分析. 结果 应用奥卡西平出现皮疹的癫痫患者共7例, 起始剂量大于常规剂量上限3例; 2例患者加量速度过快; 局部皮疹1例, 全身皮疹4例, 躯干皮疹、剥脱性皮炎各1例; 3例患者经抗组胺药物、糖皮质激素、外用药物等治疗后好转.结论 奥卡西平引起皮疹与起始剂量过大或加量速度过快有关.     

国产奥卡西平治疗癫痫70例

［摘要］目的观察国产奥卡西平（OXC）单药治疗癫部分性发作/继发全面性强直 阵挛发作（PS/SGTCS）或特发性全面性强直 阵挛发作（GTCS）的疗效、耐受性和安全性.方法新诊断的和未经正规治疗的PS/SGTCS或GTCS患者70例.成人OXC起始量均为每次150 mg,早晚各1次,维持剂量900～1 500 mg&;#8226;d 1,分2次服用;儿童起始量4～5 mg&;#8226;kg 1,早晚各1次,维持剂量25～30 mg&;#8226;kg 1&;#8226;d 1.进行自身对比开放性观察,同时分析单药治疗1,2,3,6个月内的疗效、不良反应、耐受性和安全性.结果6个月时总有效率为92.86%,控制率为80.00%,累积退出率为7.14%,其中2例（2.86%）失访,2例（2.86%）因皮疹退出,经济原因退出1例（1.43%）.最常见的不良反应：乏力、头昏、头痛、嗜睡、恶心、呕吐,且均为暂时性的.结论国产奥卡西平单药治疗PS/SGTCS或GTCS 6个月的疗效明显,不良反应轻,耐受性好,安全性高.     

奥卡西平治疗癫痫的临床研究

目的观察奥卡西平（OXCP）治疗癫痫的临床疗效和安全性。方法选择2008年1月至2009年12月在我院治疗的44例癫痫患者,随机将其分为治疗组和对照组各22例,治疗组用奥卡西平治疗,对照组用苯妥英钠治疗,比较两组疗效和不良反应。结果治疗组总有效率为86.4%,对照组总有效率为63.6%,两组疗效比较差异有统计学意义（P〈0.05）;治疗组患者有1例出现不良反应,不良反应发生率为4.5%,对照组有4例患者出现不良反应,不良反应发生率为18.2%,差异有统计学意义（P〈0.05）。结论奥卡西平治疗癫痫临床效果显著,且安全性好,值得在临床更多应用。     

奥卡西平用于癫痫治疗的效果分析

目的:探究奥卡西平用于癫痫治疗的效果,为临床提供指导.方法:以2015年8月12日～2016年12月20日来我院接受救治的66例癫痫患儿作为观察对象,使用单双号编号法进行分组.奥卡西平组33例应用奥卡西平治疗,苯妥英钠组33例应用苯妥英钠治疗,随访半年,研究对比两组临床疗效及不良反应发生率.结果:奥卡西平组总有效率为90.91％,相比苯妥英钠组(72.73％)明显更高,P<0.05,奥卡西平组不良反应发生率为9.09％,相比苯妥英钠组(27.27％)明显更低,P<0.05.结论:奥卡西平用于癫痫治疗具有较显著的效果,且毒副作用较小.     

奥卡西平联合用药治疗癫痫和三叉神经痛的研究进展

奥卡西平是常见的癫痫类用药,常用于治疗癫痫和三叉神经痛,具有较好的耐受性,在联合用药方面前景广阔。本文就近年来关于奥卡西平联合用药治疗癫痫及三叉神经痛的情况进行综述,为临床用药提供参考。     

奥卡西平治疗癫痫44例的临床研究

目的观察奥卡西平(OCBZ)治疗癫痫的临床疗效和安全性。方法选择2008年1月至2009年12月在我院治疗的44例癫痫患者,随机将其分为治疗组和对照组各22例,治疗组用奥卡西平治疗,对照组用苯妥英钠治疗,比较两组疗效和不良反应。结果治疗组总有效率为86.4%,对照组总有效率为63.6%,两组疗效比较差异有统计学意义(P<0.05);治疗组患者有1例出现不良反应,不良反应发生率为4.5%,对照组有4例患者出现不良反应,不良反应发生率为18.2%,差异有统计学意义(P<0.05)。结论奥卡西平治疗癫痫临床效果显著,且安全性好,值得在临床更多应用。     

奥卡西平治疗癫痫的临床观察

目的：观察奥卡西平（OCBZ）治疗癫痫的疗效、耐受性和安全性。方法：对36例癫痫患者采用单用和添加奥卡西平治疗,其中19例未经过抗癫痫治疗进入单药治疗组,17例曾使用一线抗癫痫药物无效而进入添加治疗组,两组服用奥卡西平疗程均达6个月。成人起始剂量为剂量为0．15g,qn,维持剂量600～1200mg·d^-1,最大未超过1．5g;儿童按10mg·kg^-1·d^-1,分两次服用,增加剂量每周不超过10mg·kg^-1·d^-1。分两次服用,最大不超过30mg·kg^-1·d^-1。分析两组6月以上的疗效、耐受性和安全性。结果：本组总有效率为88．9％,完全控制为36．1％;其中单药治疗组控制率42．1％,总有效率为94．7％,添加治疗组控制率为29．4％,总有效率为82．4％。最常见的不良反应为头昏、头痛、嗜睡、皮疹、纳差等。单治组不良反应总发生率为31．6％,添加治疗组不良反应发生率为58．8％。结论：奥卡西平治疗癫痫安全、稳定、有效。     

Oxcarbazepine: current status and clinical applications

Oxcarbazepine (OXC) was introduced in 1990 and is now registered in 54 countries worldwide as monotherapy, as add-on treatment for partial seizures, with or without secondarily generalised seizures, and primary generalised tonic-clonic seizures. OXC and its active metabolite, monohydroxy derivative (MHD), block voltage-dependent sodium channels and may effect potassium and calcium channels. In animal models of epilepsy, OXC and MHD have efficacy similar to that of CBZ. There is no evidence for clinically important teratogenicity, mutagenicity or carcinogenicity. OXC has no effect on serum concentrations of hepatically metabolised anti-epileptic drugs (AEDs) and no clinically important interactions with common non-AEDs, other than hormonal contraceptives. MHD has low protein binding and linear pharmacokinetics. Adverse effects (AEs) are usually related to the central nervous system. Approximately three-quarters of patients who experience adverse effects with CBZ improve when switched to OXC, without loss of seizure control. The incidence of rash appears to be less than that expected with CBZ. While hyponatraemia may occur more often with OXC than with CBZ, it is rarely symptomatic. OXC is an effective and safe drug for the treatment of partial-onset and primary generalised tonic-clonic seizures. Placebo- and low-dose controlled double-blind monotherapy studies prove that OXC has anticonvulsant activity and that therapeutic dosages may be obtained with a 24 h titration in hospitalised patients, if necessary. Comparative double-blind trials show that OXC has similar efficacy to VPA, CBZ and PHT, but has advantages compared to those agents in terms of pharmacokinetics, side-effects and tolerability.     

HLA-B基因多态性与抗癫痫药拉莫三嗪致皮肤不良反应关系的meta分析

目的 系统评价人类白细胞抗原B(human leukocyte antigen B,HLA-B)基因多态性与抗癫痫药拉莫三嗪致皮肤不良反应(lamotrigine-cutaneous adverse reactions,LTG-cADRs)的相关性。方法 通过计算机全面检索中国期刊全文数据库、万方数字化期刊全文库、中国科技期刊全文数据库、PubMed、Web of Science、Science Direct数据库,检索时间截至2022年7月15日,采用RevMan5.4软件进行meta分析。结果 共纳入16篇病例对照研究,331例LTG-cADRs癫痫患者,其中94例拉莫三嗪致史-约综合征/中毒性表皮坏死松懈症(lamotrigine-Stevens-Johnson syndrome/toxic epidermal necrolysis,LTG-SJS/TEN)患者,232例拉莫三嗪致斑丘疹(lamotrigine-maculopapule,LTG-MPE)患者,5例伴嗜酸粒细胞增多和系统症状的药疹(lamotrigine-drug rash with eosinophilia and systemic symptoms,LTG-DRESS)患者;612例拉莫三嗪耐受癫痫患者。Meta分析结果显示：HLA-B*1502等位基因与LTG-SJS/TEN存在显著相关性(OR=3.03,95%CI：1.70~5.39,P=0.000 2)。HLA-B*1502、HLA-B*5801、HLA-B*1302等位基因均与LTG-MPE无显著相关性。结论 HLA-B*1502等位基因与LTG-SJS/TEN存在相关性,可能是LTG-SJS/TEN风险基因;HLA-B*1502、HLA-B*5801和HLA-B*1302等位基因与LTG-MPE无相关性。     

Oxcarbazepine extended-release formulation in epilepsy

Oxcarbazepine (OXC) is a 10-keto-analogue of carbamazepine, which was developed and labeled as a follow-up antiepileptic drug, that was intended to overcome some of the pharmacological drawbacks of carbamazepine with similar efficacy. The main advantage is the nonoxidative metabolic pathway that allows a lower enzyme-induction profile and fewer drug interactions. OXC is rapidly and extensively reduced by cytosolic hepatic enzymes to its monohydroxylated derivative (MHD), thus OXC may be regarded as a prodrug with MHD representing the active antiepileptic agent. The immediate-release (IR) formulation of OXC (Trileptal^®, Timox^®) has an almost complete bioavailibilty. It is rapidly absorbed and reaches peak concentrations after 1–3 h. MHD peak concentrations are measured within 4–12 h. Elimination half-life in healthy subjects is 1–5 h for OXC and 7–20 h for MHD. The OXC plasma concentration peak may have been responsible for side effects, such as dizziness, vertigo, coordination problems or blurred vision, which appeared more often with this formulation in individual cases than with the formulation available prior to 2000, or with another formulation that has been distributed in Scandinavian countries. Both possibilities offer a profile approaching the characteristics of an extended-release (ER) formulation. ER OXC was labeled in Germany in 2008 (Apydan^® extent, Desitin Arzneimittel GmbH, Hamburg, Germany). Under steady-state conditions, Phase I studies show bioequivalence between IR and ER OXC. With ER OXC, OXC plasma peak concentrations and both OXC and MHD peak–trough fluctuations are markedly reduced. In clinical trials, comparisons between IR OXC twice daily versus ER OXC once daily failed to show significant differences; efficacy tended to be better with IR OXC, whereas OXC ER showed insignificant tolerability advantages. Another study is currently ongoing to compare the tolerability of both formulations under twice-daily administration conditions in patients with difficult-to-treat epilepsies who require a dosage increase of OXC and who are randomized to IR or ER OXC.     

药物代谢酶和转运体基因多态性与中国癫痫患儿服用奥卡西平的活性代谢物血药浓度关联性研究

目的 研究代谢酶和转运体基因多态性对中国癫痫患儿服用奥卡西平的活性代谢物10-羟基卡马西平(monohydroxycarbazepine,MHD)血药浓度是否有显著影响。方法 前瞻性收集年龄0~14岁服用奥卡西平达稳态的谷浓度血浆样本,酶放大免疫法测定患者MHD血药浓度,双脱氧链终止法检测患儿代谢酶基因UGT2B7 802T>C、UGT1A9 I399C>T,以及转运体基因ABCB1 3435C>T和ABCC2 1249G>A多态性,应用单因素方差分析与Fisher最小显著差检验法分析代谢酶和转运体基因多态性与奥卡西平活性代谢物血药浓度的关联性。结果 研究共收集161例癫痫患儿的谷浓度血浆样本,单因素方差分析显示,转运体基因ABCB1 3435C>T与MHD血药浓度显著相关(P<0.05)。随后进行Fisher最小显著差检验,携带ABCB1 3435C>T突变等位基因患儿的血浆MHD浓度明显高于非携带者,未见其他代谢酶和转运体基因多态性显著影响MHD血药浓度。结论 转运体基因ABCB1 3435C>T与中国癫痫患儿奥卡西平活性代谢物血药浓度存在显著关联性,对癫痫患儿给予奥卡西平时可作该位点基因多态性检测,为临床个体化给药提供参考。     

奥卡西平的合成

奥卡西平（oxcarbazepine，1），化学名为10，11-二氢-10-氧代-5H-二苯[b，f]氮杂[艹卓]-5-甲酰胺，由瑞士Novartis公司研发，1990年首次在丹麦上市，现已在多国上市。1是治疗癫痫的一线药物，疗效与卡马西平（carbamazepine）相当，疲乏、运动失调、男性阳萎等不良反应较少。本品还具有较强的抗三叉神经痛作用。     

Oxcarbazepine

Oxcarbazepine (OXC) (Trileptal^®, Novartis) is one of the recently introduced anti-epileptic drugs (AEDs) in the US. This drug has demonstrated efficacy as adjunctive therapy in adults and children, and as monotherapy in adults for the treatment of seizures of partial onset. There is also convincing evidence of its efficacy in patients with newly diagnosed and refractory trigeminal neuralgia. In addition, the initial efficacy results of oxcarbazepine in other neuropathic pain conditions and in bipolar disorders are encouraging. In this review, recommendations on the optimal clinical use of OXC are given based on its pharmacokinetic profile, efficacy and tolerability in those various conditions.     

基因多态性对药品不良反应影响的研究进展

个体差异是药品不良反应产生的重要影响因素,随着人类基因图谱描绘的完成以及遗传药理学、药物基因组学等学科的快速发展,基因多态性导致个体差异逐步得到证实。本文综述了基因多态性对药品不良反应影响研究的发展历史、作用机制以及发展现状,为探讨预防药品不良反应的产生提供思路,为临床合理用药提供参考。     

谷胱甘肽S-转移酶M1基因多态性与个体化给药的研究进展

目的:介绍谷胱甘肽S-转移酶M1(GSTM1),为建立个体化给药方案提供参考.方法:通过文献检索和资料汇总,对目前有关GSTM1基因多态性影响药物疗效的研究进行综述.结果:GSTM1基因多态性与不同肿瘤易感性的研究比较多,而对药物代谢动力学的影响研究较少,部分研究显示,抗癌药物的临床反应受到GsTM1基因的多态性的影响,但研究结果却不完全一致.结论:目前没有研究显示GSTM1基因多态性显著影响抗癌药物的药物代谢动力学,但不同GSTM1基因型可表达不同活性的GST相关酶,从而影响治疗效果.     

奥卡西平的药代动力学及其立体选择性

奥卡西平是一种治疗癫痫部分发作和全身强直阵孪性癫痫发作的新药。与传统抗癫痫药物相比，奥卡西平有不良反应少、自身诱导及对肝药酶的诱导作用小等优点。本文系统地介绍了奥卡西平在人体内吸收、分布、代谢和排泄的药代动力学特征，对年龄、性别、肝肾功能损伤等影响因素进行了描述，同时综述了奥卡西平及其活性代谢产物10-羟基卡马西平在动物及人体内药代动力学的立体选择性。     

Oxcarbazepine in bipolar disorder: a critical review of the literature

Oxcarbazepine (OXC) is a keto-congener of carbamazepine, which has fewer side effects and drug interactions. However, the efficacy of OXC in treating bipolar disorder is not as well established as that of carbamazepine. This article is a systematic literature review of all studies regarding OXC and bipolar disorders, with particular attention to papers published in the last 6 years. Using the terms ‘oxcarbazepine and bipolar disorder’, ‘oxcarbazepine and mania’ or ‘oxcarbazepine and bipolar depression’, a computer-aided search of MEDLINE for the years 2000 – 2006 has been conducted. Since its introduction as an antiepileptic drug in early 2000, clinical research regarding the potential role of OXC in the treatment of bipolar disorder remains limited. There is a lack of double-blind, placebo-controlled studies. Studies recently published have small samples of patients, with insufficient follow-up periods and other methodological weaknesses. The efficacy of OXC in bipolar disorder has not been widely studied. Some authors recommend using OXC as monotherapy or as add-on therapy in refractory mania, although results are not conclusive. It is unknown whether OXC has efficacy in the maintenance treatment of bipolar disorder. OXC can be particularly useful as an add-on treatment in bipolar disorder patients for whom previous treatments have failed, or in patients who have difficulty tolerating adequate dosages of standard approved treatments.