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Carfentanil or carfentanyl is a structural analog of the synthetic opioid analgesic fentanyl. Carfentanyl was first synthesized in 1974 by a team of chemists at Janssen Pharmaceutica which included Paul Janssen. The effects of carfentanil, including overdose, can be reversed by naloxone. Carfentanil is legally controlled in most jurisdictions, but has veterinary uses for anaesthetising large animals. 

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Carfentanil was sold starting in 1986 under the brand name “Wildnil” for use in tranquilizer darts in combination with an α2-adrenoreceptor agonist for large mammals including elk and elephants. It was chosen for its high therapeutic index. Commercial production of Wildnil ceased in 2003, and the drug is available only as a compounded dosage form. Radiolabelled. carfentanyl is widely used as a selective radiotracer in animal and human positron emission tomography (PET) imaging studies of the μ-opioid system due to its high affinity for receptors. 

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Carfentanil is a lipophilic chemical, and can easily cross the blood-brain barrier. It has very rapid onset of effects, but is also shorter acting than fentanyl. For pain relief, a unit of carfentanyl is 100 times as potent as the same amount of fentanyl, 5,000 times as potent as a unit of heroin and 10,000 times as potent as a unit of morphine. This is despite only having 14-135 times higher affinity for the μ receptor. Despite its higher potency, carfentanil is less fatal than fentanyl in rats. 

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China’s unregulated narcotic“, fentanyl, carfentanil and other highly potent derivatives of fentanyl were actively marketed by several Chinese chemical companies. Carfentanyl was not a controlled substance in China until 1 March 2017, and until then was manufactured legally and sold openly over the Internet. 

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