Drug intelligence / Profile preview

fentanyl

Development stage
Approved
Lead developer
Janssen Pharmaceutica
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Transdermal, Buccal, Intravenous, Intramuscular, Epidural, Intrathecal
01

Overview

Fentanyl is a highly potent synthetic opioid analgesic of the 4-anilinopiperidine class. It acts primarily as a strong agonist at the mu-opioid receptor in the central nervous system. Fentanyl is approximately 50 to 100 times more potent than morphine and about 30 to 50 times more potent than heroin. It was first synthesized in 1960 by Belgian pharmacologist Paul Janssen and introduced for medical use in Europe in the mid-1960s and approved in the United States in 1968[2][6][8]. Medically, fentanyl is used for managing severe pain (such as cancer pain or post-surgical pain) that does not respond well to other opioids. Its high potency also makes it a major drug of abuse with significant risk of overdose and death due to respiratory depression[3][7][10]. Fentanyl is available as injectable formulations, transdermal patches, sublingual tablets/lozenges/buccal films, and nasal sprays[8].

Brand names
DuragesicSublimazeActiqFentoraAbstralLazanda
Other names
芬太尼N-phenyl-N-[1-(2-phenylethyl)piperidin-4-yl]propanamide
02

Targets

MOR (Mu opioid receptor)

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