Etorphine ( M99) is a semi-synthetic opioid possessing an analgesic potency approximately 1,000–3,000 times that of morphine. It was first prepared in 1960 from oripavine, which does not generally occur in opium poppy extract but rather the related plants oriental poppy and Papaver bracteatum.
The human antidote is generally naloxone, not diprenorphine, and is always prepared before the preparation of etorphine to be immediately administered following accidental human exposure to etorphine. The in humans is 3 μg which led to the requirement that the medicine include an equivalent dose of an antidote.
One of its main advantages is its speed of operation, and more importantly, the speed that diprenorphine reverses its effects. The high incidence of side effects, including severe cardiopulmonary depression, has caused etorphine to fall into disfavor in general veterinary practice. However, its high potency, combined with the rapid action of both etorphine and its antagonist, diprenorphine, means that it has found a place for use in the capture of large mammals, such as rhinoceroses and elephants, where rapid onset and rapid recovery are both very important. The high potency of etorphine means that sufficient etorphine can be administered to large wild mammals by projectile syringe (dart).
Large Animal Immobilon is a combination of etorphine plus acepromazine maleate. An etorphine antidote Large Animal Revivon contains mainly diprenorphine for animals and a human-specific naloxone-based antidote, which should be prepared prior to the etorphine. A 5–15 mg dose is enough to immobilise an African elephant and a 2–4 mg dose is enough to immobilise a black rhinoceros.
In the Netherlands etorphine is a Schedule I drug of the Opium Law. It is used only for veterinary purposes in zoos to immobilise large animals.
In the United States etorphine is listed as a Schedule I drug with an ACSCN of 9056, although its hydrochloride salt is classified as Schedule II with an ACSCN of 9059.
In the United Kingdom, under the Misuse of Drugs Act 1971, etorphine is controlled as a Class A substance.
In Italy etorphine is illegal, as are the parent compounds Dihydroetorphine and Acetorphine. (Data from 2022)
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