Meredith P A
University Department of Medicine and Therapeutics, Western Infirmary, Gardiner Institute, Glasgow, Scotland.
Drug Saf. 1996 Oct;15(4):233-42. doi: 10.2165/00002018-199615040-00001.
For economic reasons, the use of generic substitution is increasingly being supported by health authorities. Potentially, this may be problematic for drugs with a narrow therapeutic window if quality control and/or bioequivalence is not optimal. Many developing countries do not have the resources or expertise to carry out appropriate quality control resulting in widespread distribution of substandard or even counterfeit drugs. Even in countries where procedures are well regulated, substandard drugs reach the market from time to time. Interchangeability of drugs is determined by bioequivalence studies comparing the serum concentration versus time curves for the products following single dose administration to fasting volunteers in a randomised crossover design. A number of reports, largely anecdotal, of treatment failure or increased adverse events after switching brands has cast some doubts upon whether bioequivalence testing is sufficient in all cases. These reports have covered cardiovascular, respiratory, hormonal, psychotropic, anticonvulsant, anti-infective and anti-inflammatory drugs. Equivalence is particularly difficult to obtain with many sustained-release formulations. The WHO has initiated programs to prevent the distribution of substandard preparations and has drafted guidelines for testing bioequivalence based on internationally accepted reference products. Until such time as means can be provided-first, to enforce internationally accepted production standards, and second, to permit uniform testing of therapeutic agents-the safest clinical choice, particularly in countries where registration requirements and quality control are minimal, must remain the branded product.
出于经济原因,卫生当局越来越支持使用非专利药品替代。对于治疗窗较窄的药物而言,如果质量控制和/或生物等效性不理想,这可能会带来问题。许多发展中国家没有资源或专业知识来进行适当的质量控制,导致不合格甚至假冒药品广泛流通。即使在程序监管良好的国家,不合格药品也不时进入市场。药物的可互换性是通过生物等效性研究来确定的,该研究采用随机交叉设计,比较单剂量给药后空腹志愿者体内产品的血清浓度与时间曲线。大量主要是传闻的报告称,更换品牌后出现治疗失败或不良事件增加的情况,这让人对生物等效性测试在所有情况下是否足够产生了一些怀疑。这些报告涵盖了心血管、呼吸、激素、精神、抗惊厥、抗感染和抗炎药物。对于许多缓释制剂来说,尤其难以实现等效性。世界卫生组织已启动相关项目以防止不合格制剂的流通,并根据国际认可的参比产品起草了生物等效性测试指南。在能够提供手段——首先是执行国际认可的生产标准,其次是允许对治疗药物进行统一测试——之前,最安全的临床选择,尤其是在注册要求和质量控制最低的国家,仍必须是品牌产品。