Drug intelligence / Profile preview

carfentanil

Development stage
Phase 1
Lead developer
Janssen Pharmaceutica
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Intramuscular, Intravenous
01

Overview

Carfentanil is an extremely potent synthetic opioid, structurally related to fentanyl and classified as a fentanyl analogue. It was originally developed in 1974 for veterinary use as a tranquilizer for large animals such as elephants and other large mammals, but it is not approved for human use due to its extraordinary potency and risk profile. Carfentanil acts primarily as a mu-opioid receptor agonist, with some activity at kappa- and delta-opioid receptors. Its effects include profound analgesia, sedation, respiratory depression, miosis (pinpoint pupils), and suppression of the cough reflex. Carfentanil is estimated to be approximately 10,000 times more potent than morphine and about 100 times more potent than fentanyl. Even minute quantities can cause fatal overdose in humans; multiple high doses of naloxone may be required to reverse its effects in cases of poisoning or overdose[1][2][5][6]. Illicitly manufactured carfentanil has been found mixed with heroin or pressed into counterfeit pills on the illegal drug market, contributing significantly to opioid overdose deaths[1][4]. Due to its extreme potency and lethality at very low doses (potentially lethal at amounts equivalent to a few grains of salt), carfentanil poses significant risks not only to users but also first responders who may accidentally come into contact with it[7][9]. Routes of administration for veterinary use include intramuscular and intravenous. Illicit exposure typically occurs via injection, inhalation/snorting, or oral ingestion.

Brand names
Wildnil
Other names
carfentanyl
02

Targets

MOR (Mu opioid receptor)KOR (Kappa opioid receptor)DOR (Opioid Receptor Delta 1)

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