Fentanyl is a monocarboxylic acid amide resulting from the formal condensation of the aryl amino group of N-phenyl-1-(2-phenylethyl)piperidin-4-amine with propanoic acid. It has a role as an opioid analgesic, a mu-opioid receptor agonist, an anaesthesia adjuvant, an intravenous anaesthetic, an adjuvant and an anaesthetic. It is a member of piperidines, an anilide and a monocarboxylic acid amide.

Fentanyl is a DEA Schedule II controlled substance. Substances in the DEA Schedule II have a high potential for abuse which may lead to severe psychological or physical dependence. It is a Opiates substance.

Fentanyl, a potent opioid agonist, was developed in the 1950s to fill a need for strong and rapid analgesia. Because of these characteristics, fentanyl is commonly used to treat chronic cancer pain or in anesthesia. Fentanyl is related to other opioids like [morphine] and [oxycodone]. Fentanyl’s high potency has also made it a common adulterant in illicit drugs, especially heroin. In 2017, 47600 overdose deaths in the United States involved some opioid (over 2/3 of all overdose deaths). Opioid overdoses kill an average of 11 Canadians daily. Fentanyl was FDA approved in 1968.

Fentanyl is an Opioid Agonist. The mechanism of action of fentanyl is as a Full Opioid Agonist.

Fentanyl is a synthetic, lipophilic phenylpiperidine opioid agonist with analgesic and anesthetic properties. Fentanyl selectively binds to and activates the mu-receptor in the central nervous system (CNS) thereby mimicking the effects of endogenous opiates. Activation of the mu-subtype opioid receptor stimulates the exchange of GTP for GDP on the G-protein complex and subsequently inhibits adenylate cyclase. This causes a decrease in intracellular cAMP which inhibits cAMP-mediated calcium influx into the cell via the calcium channels and thereby results in hyperpolarization and reduced neuronal excitability.

FENTANYL is a small molecule drug with a maximum clinical trial phase of IV (across all indications) that was first approved in 1968 and has 6 approved and 38 investigational indications. This drug has a black box warning from the FDA.

A potent narcotic analgesic, abuse of which leads to habituation or addiction. It is primarily a mu-opioid agonist. Fentanyl is also used as an adjunct to general anesthetics, and as an anesthetic for induction and maintenance. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1078)