Propoxyphene (dextropropoxyphene): a critical review of a weak opioid analgesic that should remain in antiquity.
Propoxyphene (dextropropoxyphene): a critical review of a weak opioid analgesic that should remain in antiquity.
复制标题
DOI：
10.1097/01.mjt.0000253850.86480.fb
复制
发表时间：
2006-11-01
影响因子：
4.2
通讯作者：
Barkin, Diana S
中科院分区：
文献类型：
--
作者：
Barkin, Robert L;Barkin, Stacie J;Barkin, Diana S
丙氧芬（右旋丙氧芬）是一种合成的弱阿片类药物，于 1957 年引入美国。它最常与对乙酰氨基酚和/或阿司匹林联合使用。在其无处不在的介绍阶段之后，很快就发现这种药物的医源性事件（心脏毒性、癫痫发作等）远远超过了任何感知到的治疗益处。丙氧芬镇痛作用独立地等同于仅对乙酰氨基酚或阿司匹林。丙氧芬的欣快成分在其处方中造成了问题。由于其复杂的药代动力学和药效学，应避免在老年人中使用该药物。本文详细讨论了该药物的药代动力学、药效学和药理学，包括其致心律失常性。描述了产生 QTc 延长或致心律失常的其他非心血管药物疗法。本文提供了与丙氧芬相互作用的细胞色素 P450 2D6 药物疗法列表。强烈建议不要使用此代理。本文详细讨论了这样做的基本原理。该药物的毒性部分与去甲丙氧芬（一种非阿片类心脏毒性代谢物）有关。包装说明书中仅对死亡的警告就应该提醒任何谨慎的处方者该药物的危险性，并削弱其处方潜力。
Propoxyphene (dextropropoxyphene) is a synthetic weak opioid introduced into the United States in 1957. It is most frequently prescribed in combination with acetaminophen and/or aspirin. After its ubiquitous introductory phase, it was soon discovered that this drug's iatrogenic events (cardiotoxicity, seizures, etc.) far outweighed any perceived therapeutic benefit. Propoxyphene analgesia was equated with that of merely acetaminophen or aspirin independently. The propoxyphenes euphorigenic component has created a problem in its prescribing. Use of this agent in the elderly should be avoided because of its complex pharmacokinetics and pharmacodynamics. The pharmacokinetics, pharmacodynamics, and pharmacology of this drug are discussed thoroughly in this article, including its arrhythmogenicity. Additional noncardiovascular pharmacotherapies that produce QTc prolongation or arrhythmogenicity are described. A list of the cytochrome P450 2D6 pharmacotherapies that will interact with propoxyphene is provided in the article. The use of this agent is highly discouraged. The rationale for this is discussed fully within this article. The toxicity of this drug is partially related to nor-propoxyphene a non-opioid cardiotoxic metabolite. The mere warnings of fatalities within the package insert should alert any cautious prescriber on the dangers of this agent and dampen its prescribing potential.