Opioid overdoses, many of which are attributed to use of illicit fentanyl, are currently one of the leading causes of death in the U.S. Although fentanyl has been used safely for decades in clinical settings, the widespread use of illicit fentanyl is a recent phenomenon. Starting in 2013, illicitly manufactured fentanyl and its analogs began to appear on the streets. These substances were added to or sold as heroin, often unbeknownst to the user. Because fentanyl is so potent, only small amounts are needed to produce pharmacological effects, but the margin between safe and toxic doses is narrow. Surprisingly little is known about the exact signaling mechanisms underlying fentanyl-related respiratory depression or the effectiveness of naloxone in reversing this effect. Similarly, little is known about the ability of treatment medications such as buprenorphine, methadone, or naltrexone to reduce illicit fentanyl use. The present article reviews the receptor, preclinical and clinical pharmacology of fentanyl, and how its pharmacology may predict the effectiveness of currently approved medications for treating illicit fentanyl use.

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芬太尼：受体药理学，潜在滥用和对治疗的影响。

阿片类药物过量（其中许多归因于非法芬太尼的使用）目前是美国的主要死亡原因之一。尽管芬太尼已在临床环境中安全使用了数十年，但非法芬太尼的广泛使用是最近的现象。从2013年开始，非法生产的芬太尼及其类似物开始出现在街头。这些物质被添加到海洛因中或作为海洛因出售，这通常是用户所不知道的。由于芬太尼是如此有效，因此仅需少量即可产生药理作用，但安全剂量与毒性剂量之间的差很窄。令人惊讶的是，关于芬太尼相关呼吸抑制的确切信号机制或纳洛酮逆转这种作用的有效性知之甚少。相似地，关于丁丙诺啡，美沙酮或纳曲酮等治疗药物减少非法芬太尼使用的能力知之甚少。本文综述芬太尼的受体，临床前和临床药理学，以及其药理学如何预测目前批准的治疗非法使用芬太尼的药物的有效性。