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.
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。
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