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CSF concentrations and serum protein binding of carbamazepine and carbamazepine-10,11-epoxide in epileptic patients.癫痫患者脑脊液中卡马西平和卡马西平-10,11-环氧化物的浓度及血清蛋白结合率。
Br J Clin Pharmacol. 1976 Aug;3(4):575-82. doi: 10.1111/j.1365-2125.1976.tb04878.x.
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Adverse event load in bipolar participants receiving either carbamazepine immediate-release or extended-release capsules: a blinded, randomized study.
Int Clin Psychopharmacol. 2009 May;24(3):145-9. doi: 10.1097/YIC.0b013e328329b199.
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Efficacy and tolerability of gastric-retentive gabapentin for the treatment of postherpetic neuralgia: results of a double-blind, randomized, placebo-controlled clinical trial.胃内滞留型加巴喷丁治疗带状疱疹后神经痛的疗效和耐受性:一项双盲、随机、安慰剂对照临床试验的结果
Clin J Pain. 2009 Mar-Apr;25(3):185-92. doi: 10.1097/AJP.0b013e3181934276.
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Once-daily extended-release levetiracetam as adjunctive treatment of partial-onset seizures in patients with epilepsy: a double-blind, randomized, placebo-controlled trial.每日一次缓释左乙拉西坦作为癫痫患者部分性发作的辅助治疗:一项双盲、随机、安慰剂对照试验。
Epilepsia. 2009 Mar;50(3):406-14. doi: 10.1111/j.1528-1167.2008.01817.x.
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Getting into the brain: approaches to enhance brain drug delivery.进入大脑:增强脑内药物递送的方法。
CNS Drugs. 2009;23(1):35-58. doi: 10.2165/0023210-200923010-00003.
6
Antiepileptic drugs--best practice guidelines for therapeutic drug monitoring: a position paper by the subcommission on therapeutic drug monitoring, ILAE Commission on Therapeutic Strategies.抗癫痫药物——治疗药物监测的最佳实践指南:国际抗癫痫联盟治疗策略委员会治疗药物监测小组委员会的立场文件
Epilepsia. 2008 Jul;49(7):1239-76. doi: 10.1111/j.1528-1167.2008.01561.x.
7
Lamotrigine extended-release as adjunctive therapy for partial seizures.拉莫三嗪缓释片作为部分性癫痫发作的辅助治疗药物。
Neurology. 2007 Oct 16;69(16):1610-8. doi: 10.1212/01.wnl.0000277698.33743.8b.
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Evaluation of brivaracetam, a novel SV2A ligand, in the photosensitivity model.
Neurology. 2007 Sep 4;69(10):1027-34. doi: 10.1212/01.wnl.0000271385.85302.55.
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Extended-release formulations for the treatment of epilepsy.用于治疗癫痫的缓释制剂。
CNS Drugs. 2007;21(9):765-74. doi: 10.2165/00023210-200721090-00005.
10
An international multicenter randomized double-blind controlled trial of lamotrigine and sustained-release carbamazepine in the treatment of newly diagnosed epilepsy in the elderly.拉莫三嗪与缓释卡马西平治疗老年新诊断癫痫的国际多中心随机双盲对照试验
Epilepsia. 2007 Jul;48(7):1292-302. doi: 10.1111/j.1528-1167.2007.01128.x. Epub 2007 Jun 11.

抗癫痫药物的缓释制剂:原理与比较价值。

Extended-release formulations of antiepileptic drugs: rationale and comparative value.

机构信息

Clinical Trial Center, Institute of Neurology IRCCS C Mondino Foundation Pavia, Italy.

出版信息

Epilepsy Curr. 2009 Nov-Dec;9(6):153-7. doi: 10.1111/j.1535-7511.2009.01326.x.

DOI:10.1111/j.1535-7511.2009.01326.x
PMID:19936129
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC2778358/
Abstract

Extended-release products are designed to prolong the absorption of drugs with short half-lives, thereby allowing longer dosing intervals while minimizing fluctuations in serum drug levels. The relationship between serum drug concentration and clinical effects of antiepileptic drugs (AEDs) can be complex and reducing fluctuations in serum drug levels is not equally advantageous for all AEDs. Extended-release formulations have been shown to be particularly valuable for carbamazepine, whereas for other AEDs advantages, other than prolongation of the dosing interval, have not been clearly demonstrated. Differences in bioavailability may exist between extended-release and immediate-release formulations and among different brands of extended-release products. Therefore, when switching from one formulation to another, careful monitoring of clinical response and attention to the need for dose adjustment are warranted.

摘要

控释产品旨在延长半衰期短的药物的吸收,从而在最小化血清药物水平波动的同时允许更长的给药间隔。抗癫痫药物(AEDs)的血清药物浓度与临床疗效之间的关系可能很复杂,降低血清药物水平的波动并不对所有 AEDs都有利。控释制剂已被证明对卡马西平特别有价值,而对于其他 AEDs,除了延长给药间隔之外,其优势尚未得到明确证明。控释制剂和速释制剂以及不同品牌的控释产品之间可能存在生物利用度的差异。因此,在从一种制剂转换为另一种制剂时,需要仔细监测临床反应并注意调整剂量的必要性。