传统和新型抗癫痫药的合理选择

目的:面对日益复杂的抗癫痫药应用状况,对传统及新型抗癫痫药的临床应用状况进行评价以期为临床合理用药提供参考。方法:从6个传统抗癫痫药和9个新型抗癫痫药的临床适应证及其药动学特点、不良反应和药物相互作用,患者的年龄、性别和疾病状态以及经济因素等方面对影响抗癫痫药合理选择的因素作一探讨。结果及结论:传统抗癫痫药仍被广泛应用,新型抗癫痫药与传统抗癫痫药相比具有药代动力学更好、药物相互作用更少、耐受性更好等优势,但临床资料和用药经验相对缺乏,临床应用时应权衡利弊,合理选择。     

1996～2006年我院抗癫痫药的用药状况分析

目的了解我院1996～2006年抗癫痫药的应用状况及变化趋势。方法采用WHO推荐的以DDD数为指标的药物利用研究方法,计算我院抗癫痫药的销售金额、用药频度、日用金额等指标并进行排序。结果我院抗癫痫药的销售金额和DDDs值大体上呈逐渐增长趋势。并且以传统抗癫痫药物为主,丙戊酸盐、卡马西平、苯妥英钠三种传统的抗癫痫药物临床使用频度约占95%。结论我们应该对药物的使用情况进行定期分析比较,为合理用药、开发新型抗癫痫药提供科学依据和思路。     

新型抗癫痫药的安全性评价

新型抗癫痫药与传统抗癫痫药相比,具有较理想的药代动力学特性,不良反应和药物相互作用较少,耐受性和安全性较好。由于新型抗癫痫药上市时间较短,临床资料和用药经验相对较少,其安全性问题尤其值得人们关注。本文对9种新型抗癫痫药从作用机制、药代动力学、不良反应、相互作用等方面作一综合评价。     

2005-2007年我院抗癫痫药使用回顾分析

目的：统计分析我院2005—2007年抗癫痫药物的应用情况。方法：采用回顾性调查方法，对我院2005—2007年抗癫痫药物销售金额、用药频度进行统计分析。结果：2005—2007年，我院抗癫痫药物临床用药稳步增长，丙戊酸钠等传统药物仍是主要品种，但托吡酯等新型抗癫痫药增长很快。药品销售金额大幅上涨，主要是因为新型抗癫痫药来源于进口和合资，价格昂贵。结论：我院抗癫痫药应用合理。目前新型抗癫痫药物市场前景广阔，但国产药物少，必须加大研制开发和生产。     

新抗癫痫药的不良反应

目的：为指导临床合理用药,综述了近年来新的抗癫痫药物的不良反应。方法：查阅国内外献,探讨了加巴喷丁、非氨酯、拉莫三嗪、奥卡西平、替加宾等新的抗癫痫药在各个系统的不良反应。结果：各类抗癫痫药均具不同程度的不良反应。结论：掌握新的抗癫痫药的不良反应,有助于临床医师选适当的药物治疗癫痫,从而达到合理用药的目的。     

新型抗癫痫药加巴喷丁

加巴喷丁（gabapentin）是一种新型抗癫痫药，为γ-氨基丁酸（GABA）类似物，口服易吸收，与其他抗癫痫药物相互作用小，且耐受性好。临床研究表明，其作为添加用药治疗癫痫具有良好的临床疗效和安全性。现对其作用机制、药动学、药物相互作用、临床应用和药物不良反应等作一综述。     

儿童抗癫痫药过敏反应36例

抗癫痫药过敏反应是一种抗癫痫药所致的药物剂量无关的副反应,多为皮疹、发热、淋巴结肿大、内脏损害等表现,多见于服用芳香族抗癫痫药（如苯巴比妥、苯妥英钠及卡马西平等）的患者。其中部分病例可以表现为抗癫痫药过敏综合征（antiepileptic drug hypersensitive syndrome,AHS）,临床主要表现为发热、皮疹和内脏损害。抗癫痫药过敏反应早期临床表现各异,如不重视易延误诊断加重病情,一旦出现严重肝损害、     

高原低氧环境影响抗癫痫药物的研究进展

高原低氧环境通过改变机体胃肠排空速率、器官血流量、药物血浆蛋白结合率、药物代谢酶和转运体表达等影响药物的药代谢动力学过程。癫痫是一种需长期用药的脑部疾病,而大多数抗癫痫药物的治疗指数低、有效血药浓度范围窄。临床上常用治疗药物监测(therapeutic drug monitoring, TDM)来寻找抗癫痫药物的最佳个体化用药方法。该文对临床上常用抗癫痫药及其治疗窗进行归纳总结,并分析高原低氧环境对抗癫痫药物药代动力学的影响,为高原抗癫痫药物临床用药提供参考。     

儿童抗癫痫药物的血药浓度监测

目的儿童抗癫痫药物的血药浓度测定可提高疗效，减少毒副作用，指导临床合理使用抗癫痫药物。方法对单种药和两药联用的８６例癫痫患儿，用荧光偏振免疫法（ＦＴＩＡ）和稳态血药浓度一点法监测血药浓度并进行疗效分析。结果单用一药能控制症状不宜并用两药；必须两药联用时应注意药物相互作用。结论儿童的抗癫痫药物的血药浓度监测，能及早发现不易觉察的中毒，并结合疗效调整给药剂量与方法。     

抗癫痫药的研究进展

本文综述了欧美国家近１０年来应用于临床的抗癫痫药在体内吸收，分布，排泄的方式，相互间的作用及适用癫痫的类型，临床上抗癫痫药的选择原则。对于抗癫痫药耐受癫痫，药物开发重点应集中于压制神经元高兴奋性及阻止原发灶的进一步传播。     

Long-term neurocognitive adverse effects of prenatal antiepileptic drug exposure

Most women with epilepsy use antiepileptic medication during pregnancy because of seizure-related risks to mother and fetus. Most of the children exposed prenatally to antiepileptic medication are born healthy; however, there is increased risk for major congenital malformations and also unfavorable neurocognitive long-term development of the offspring. The increased risk has been correlated mainly with prenatal exposure to polytherapy and certain antiepileptic medications. Many confounding risk factors make it difficult to correlate the prenatal exposure and neurodevelopmental problems, and data of newer antiepileptic medications are lacking. In the future, larger prospective, controlled studies with extended follow-up are required to evaluate the long-term neurocognitive effects of prenatal antiepileptic medication exposure.     

Long-term neurocognitive adverse effects of prenatal antiepileptic drug exposure

Most women with epilepsy use antiepileptic medication during pregnancy because of seizure-related risks to mother and fetus. Most of the children exposed prenatally to antiepileptic medication are born healthy; however, there is increased risk for major congenital malformations and also unfavorable neurocognitive long-term development of the offspring. The increased risk has been correlated mainly with prenatal exposure to polytherapy and certain antiepileptic medications. Many confounding risk factors make it difficult to correlate the prenatal exposure and neurodevelopmental problems, and data of newer antiepileptic medications are lacking. In the future, larger prospective, controlled studies with extended follow-up are required to evaluate the long-term neurocognitive effects of prenatal antiepileptic medication exposure.     

Current oral and non-oral routes of antiepileptic drug delivery

Antiepileptic drugs are commonly given orally for chronic treatment of epilepsy. The treatment of epilepsy requires administration of medications for both acute and chronic treatment using multiple types of formulations. Parenteral routes are used when the oral route is unavailable or a rapid clinical response is required. Lorazepam and midazolam can be administered by the buccal, sublingual or intranasal routes. Consensus documents recommend rectal diazepam, buccal midazolam or intranasal midazolam for the out-of-hospital treatment of early status epilepticus. In the United States, diazepam is the only FDA approved rectal formulation. With the lack of parenteral, buccal or intranasal formulations for many of the antiepileptic drugs, the use of the rectal route of delivery to treat acute seizures or to maintain therapeutic concentrations is suitable for many, but not all antiepileptic medications. There is a significant need for new non-oral formulations of the antiepileptic drugs when oral administration is not possible.     

Estimation of apparent clearance of valproic acid in adult Saudi patients

International Journal of Clinical Pharmacy - Background Valproic acid is one of several antiepileptic medications requiring therapeutic drug monitoring due to its complex and wide pharmacokinetic...     

抗癫痫药的药物经济学研究进展

癫痫为慢性发作性疾病,需长期坚持药物治疗,抗癫痫药物治疗是癫痫治疗的主要手段,并取得了良好临床疗效.治疗过程中,在保证疗效的前提下,同时如何尽可能地为病人节省费用是一大难题,故经济因素也常常影响抗癫痫药的选择.随着新型抗癫痫药物在临床中的广泛应用,为选择治疗药物提供优良备选方案和应用思路.本文旨在对抗癫痫药物进行药物经济学评价,为临床合理用药提供参考.     

Increased seizures after discontinuing carbamazepine: results from the gabapentin monotherapy trial

Studies in patients with epilepsy undergoing telemetry evaluation for surgery have suggested that discontinuation of carbamazepine (CBZ) is associated with increased seizures. The period of observation in that setting, however, was limited to a few days. The authors reviewed the occurrence of seizures in patients with epilepsy who had all their antiepileptic medications discontinued during an 8-week period, converted to gabapentin monotherapy, and observed for 26 weeks as part of the gabapentin trial #945-082. Two hundred and seventy-five patients were enrolled. Kaplan-Meier estimates of time to exit for all patients showed that 18% of patients previously treated with CBZ completed the study as compared with 30% of the patients receiving other antiepileptic medications. Increase in the frequency of seizures was maximal in the 2 weeks following CBZ discontinuation. Seizures increased both in frequency and severity but no new seizure types were observed. The findings in this study show that removal of CBZ is associated with increased frequency of seizures in patients with a previous history of epilepsy with incompletely controlled seizures. The period of maximal increase was the first 2 weeks after CBZ discontinuation.     

Therapeutic strategies for treating epilepsy during pregnancy

Introduction: Counseling for women with epilepsy of childbearing potential surrounding pregnancy issues is of the utmost importance and should be done when antiepileptic medications are prescribed and reviewed regularly at clinic visits. Physicians must be familiar with risks associated with antiepileptic medication, and endeavor to minimize risks to a fetus while selecting best medications for epilepsy type.

Areas covered: The authors discuss the role of folic acid, updated evidence relating to the occurrence of major congenital malformations and neurocognitive risks associated with antiepileptic medication. They also examine the rationale for monitoring drug levels, optimum delivery strategies, and evidence for the safety of breastfeeding while taking antiepileptic medication.

Expert opinion: Valproate carries the highest known teratogenic risk in pregnancy and should only be prescribed to women of child-bearing potential in a specialist setting. There is a need for the ongoing register collection of risks associated with newer AEDs which lack substantial (major) data. Choosing these newer medications can create a dilemma for physicians, particularly when seizures are not well controlled or where treatment options are limited. The authors advocate a multidisciplinary team approach to managing women with epilepsy so that pregnancies in such women can be well managed in an optimum and individualized fashion.     

A Rare Case of Levetiracetam and Drug-Induced Idiopathic Aseptic Meningitis in a Pediatric Patient

Levetiracetam (LEV) is a pyrrolidine derivative antiepileptic medication used for the treatment of seizures in pediatric and adult patients. We report a case of probable LEV-induced aseptic meningitis in a 13-year-old girl. The patient received LEV for a generalized seizure disorder and presented with symptoms 5 days after medication initiation. Ten days after LEV initiation, the patient presented to the hospital for further management. During her hospital course, infectious etiologies were ruled out with clinical and diagnostic testing. Upon discontinuation of LEV, the patient's symptoms resolved. Although select antiepileptic medications have been associated with drug-induced aseptic meningitis (DIAM), to date, no reports have been published about DIAM following the administration of LEV. We describe and categorize the probability of DIAM in association with LEV, as observed in a patient case.     

New and investigational antiepileptic drugs

In the last fifteen years, new antiepileptic medications have been offered for the treatment of patients with epilepsy. Nevertheless, despite optimal medical treatment, up to 30% of patients still experience recurrent seizures and the challenge for new, more efficacious and better-tolerated drugs continues. New antiepileptic drugs include the evolution of pre-existing drugs and new compounds identified through the investigation of additional molecular targets, such as SV2A synaptic vesicle protein, voltage-gated potassium channels, ionotropic and metabotropic glutamate receptors, and gap junctions. This paper reviews the available information on various classes of molecules that are in the pipeline as well as on the innovative approaches to the treatment of epilepsy.     

Treatment of partial seizures in childhood : an overview

The treatment of partial seizures in children is based on the use of first generation and recently introduced antiepileptic drugs as well as nonpharmacological treatments such as the ketogenic diet, vagus nerve stimulation and surgical therapy. The present review discusses the efficacy and tolerability of different treatment options for partial seizures in childhood. Few adjunctive or monotherapy, placebo-controlled or comparative trials of the first-generation antiepileptic drugs and some of the more recently introduced antiepileptic drugs have been performed in children. This can be explained by the fact that it is only relatively recently (1989) that the International League against Epilepsy proposed that randomised, controlled trials be included among the required criteria for assessing the efficacy and tolerability of an antiepileptic agent. This led to controlled, comparative trials among older antiepileptic drugs (phenobarbital, phenytoin, carbamazepine and valproic acid), both in adults and in paediatric patients, being performed relatively 'late', based on when these drugs were first introduced. Carbamazepine and valproic acid may still be considered as first-line antiepileptic therapies for children with partial seizures. Phenobarbital and phenytoin are mostly considered as last choice drugs because of their adverse event profiles. The new generation of antiepileptic agents has added to the first- and second-line treatment options for paediatric partial seizures. To date, there are sufficient data to support the clinical use of some of the recently introduced antiepileptic drugs (e.g. oxcarbazepine, topiramate, gabapentin and lamotrigine) as adjunctive or first-line monotherapy. Because of the risk of visual field constriction with vigabatrin, the use of this drug is currently limited to patients refractory to other medications. Tiagabine, felbamate, levetiracetam and zonisamide have been shown to be effective in adults with partial seizures; however, at present there are not yet enough data on the efficacy of these drugs in children to support consideration of their use as either first-line or add-on therapy in this patient population, although controlled studies are expected shortly. Furthermore, the use of felbamate is considerably limited by rare, but severe, hepatic and haematological toxicity. Controlled trials for paediatric partial seizures are still lacking for the ketogenic diet and vagus nerve stimulation, though they may represent, in given patients, useful adjunctive alternative treatments for refractory partial seizures. In conclusion, further trials are needed to determine an optimal sequence of first- and second-line therapies and to establish whether other newer antiepileptic drugs merit consideration as initial therapy in children with partial seizures.