Fentanyl: Receptor pharmacology, abuse potential, and implications for treatment

NEUROSCIENCE AND BIOBEHAVIORAL REVIEWS

卷:106

Review

Comer, Sandra D.^1,2  Cahill, Catherine M.³ 

[1] New York State Psychiat Inst & Hosp, New York, NY 10027 USA

[2] Columbia Univ, New York, NY 10027 USA

[3] Univ Calif Los Angeles, Semel Inst Neurosci & Human Behav, Los Angeles, CA 90095 USA

关键词: Fentanyl;    Heroin;    Illicit;    Pharmacology;    Beta-arrestin;    Abuse;    Efficacy;    Subjective effects;    Self-administration;    Pain;    Methadone;    Naltrexone;    Buprenorphine;    Treatment;   

DOI  :  10.1016/j.neubiorev.2018.12.005

来源: Elsevier

【 摘 要 】

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.

【 授权许可】

Free