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Concept
Carfentanil
Summary
Carfentanil or carfentanyl, sold under the brand name Wildnil, is an extremely potent opioid analgesic which is used in veterinary medicine to anesthetize large animals such as elephants and rhinoceroses. It is typically administered in this context by tranquilizer dart. Carfentanil has also been used in humans for imaging of opioid receptors. It has additionally been used as a recreational drug, typically by injection, insufflation, or inhalation. Deaths have been reported in association with carfentanil.
Effects and side effects of carfentanil in humans are similar to those of other opioids and include euphoria, relaxation, pain relief, pupil constriction, drowsiness, sedation, slowed heart rate, low blood pressure, lowered body temperature, loss of consciousness, and suppression of breathing. The effects of carfentanil, including overdose, can be reversed by the opioid antagonists naloxone and naltrexone, though higher or more doses than usual may be necessary compared to other opioids. Carfentanil is a structural analogue of the synthetic opioid analgesic fentanyl. It acts as an ultrapotent and highly selective agonist of the μ-opioid receptor.
Carfentanil was first synthesized in 1974 by a team of chemists at Janssen Pharmaceutica which included Paul Janssen. It was introduced into veterinary medicine in 1986. Carfentanil is legally controlled in most jurisdictions.
Chosen for its high therapeutic index, carfentanil was first sold in 1986 under the brand name "Wildnil" for use in combination with an α2-receptor agonist as a tranquilizing agent for large mammals like hippos, rhinos, and elephants. Commercial production of Wildnil ceased in 2003; the drug is now available only in compounded form.
Carfentanil has been used at doses of less than 7 μg as a radiotracer for positron emission tomography imaging of the μ-opioid receptor in the brain in humans.
Carfentanil acts as a highly selective agonist of the μ-opioid receptor. It showed affinity values (Ki) of 0.051 nM for the μ-opioid receptor, 4.
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