药物耐药性和伪耐药性:肠道涂层阿司匹林的意外后果
Tilo Grosser1, Susanne Fries, John A Lawson
1Institute for Translational Medicine and Therapeutics, Perelman School of Medicine, University of Pennsylvania, Philadelphia, PA 19104, USA.
Circulation
|December 6, 2012
概括
真正的抗阿司匹林药物耐药性是罕见的. 显而易见的阿司匹林耐药性往往是由于可变的吸收,特别是肠膜阿司匹林,而不是真正的药物耐药性.
科学领域:
- 心血管医学 心血管医学
- 药理学 药理学是指药理学的学科.
- 遗传学 是一个遗传学.
背景情况:
- 低剂量阿司匹林对于预防二次心肌梗塞和中风至关重要.
- 阿司匹林耐药性可能导致治疗失败,但其定义和发病率尚不清楚.
- 这项研究调查了对阿司匹林的真正药理性耐药性,可能与遗传因素有关.
研究的目的:
- 为了确定一个稳定的,特定的表型的真实药理学耐药性阿司匹林的流行.
- 要区分真正的阿司匹林耐药性和由吸收问题引起的伪抗药性.
主要方法:
- 查了400名健康志愿者对一次325毫克剂量即时释放或肠膜阿司匹林的反应.
- 评估了阿司匹林的分子标环氧化酶-1活性.
- 对于明显耐药的个体,使用了重复测试和多种类型的阿司匹林配方 (81mg肠涂层) 和克洛皮多格雷尔 (75mg).
主要成果:
- 可变的吸收导致对单剂量肠膜涂层阿司匹林 (高达49%) 的明显耐药性高频率,但不是即时释放阿司匹林 (0%).
- 所有参与者在重复测试,延长剂量间隔或ex vivo血小板添加后对阿司匹林有反应.
- 没有发现真正抗阿司匹林药物耐药性的病例.
结论:
- 真正的抗阿司匹林药物耐药性是罕见的.
- 由药物吸收延迟和减少引起的伪抗药性是一个重要的因素,特别是与肠膜阿司匹林.
- 立即释放阿司匹林的使用避免了与吸收变异性相关的伪抵抗.
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