Acetorphine
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Acetorphine is a potent
opioid Opioids are substances that act on opioid receptors to produce morphine-like effects. Medically they are primarily used for pain relief, including anesthesia. Other medical uses include suppression of diarrhea, replacement therapy for opioid us ...
analgesic An analgesic drug, also called simply an analgesic (American English), analgaesic (British English), pain reliever, or painkiller, is any member of the group of drugs used to achieve relief from pain (that is, analgesia or pain management). It ...
, up to 8700 times stronger than
morphine Morphine is a strong opiate that is found naturally in opium, a dark brown resin in poppies (''Papaver somniferum''). It is mainly used as a analgesic, pain medication, and is also commonly used recreational drug, recreationally, or to make ...
by weight. It is a
derivative In mathematics, the derivative of a function of a real variable measures the sensitivity to change of the function value (output value) with respect to a change in its argument (input value). Derivatives are a fundamental tool of calculus. F ...
of the more well-known opioid
etorphine 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 r ...
, which is used as a very potent
veterinary Veterinary medicine is the branch of medicine that deals with the prevention, management, diagnosis, and treatment of disease, disorder, and injury in animals. Along with this, it deals with animal rearing, husbandry, breeding, research on nutri ...
painkiller and
anesthetic An anesthetic (American English) or anaesthetic (British English; see spelling differences) is a drug used to induce anesthesia ⁠— ⁠in other words, to result in a temporary loss of sensation or awareness. They may be divided into two ...
medication, primarily for the sedation of large animals such as elephants, giraffes and rhinos. Acetorphine was developed in 1966 by the
Reckitt Reckitt Benckiser Group plc, trading as Reckitt, is a British multinational consumer goods company headquartered in Slough, England. It is a producer of health, hygiene and nutrition products. The company was formed in March 1999 by the merge ...
research group that developed etorphine. Acetorphine was developed for the same purpose as etorphine itself, namely as a strong tranquilizer for use in immobilizing large animals in veterinary medicine. Despite showing some advantages over etorphine, for instance producing less toxic side effects in giraffes, acetorphine was never widely adopted for veterinary use, and etorphine (along with other tranquilizers such as
carfentanil Carfentanil or carfentanyl, sold under the brand name Wildnil, is a very 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 ...
and
azaperone Azaperone is a pyridinylpiperazine and butyrophenone neuroleptic drug with sedative and antiemetic effects, which is used mainly as a tranquilizer in veterinary medicine. It is uncommonly used in humans as an antipsychotic drug. Azaperone acts ...
) remains the drug of choice in this application.


Legal Status


Australia

Acetorphine is a schedule 9 substance in Australia under the Poisons Standard (February 2017). A schedule 9 drug is outlined in the
Poisons Act 1964 Poison is a chemical substance that has a detrimental effect to life. The term is used in a wide range of scientific fields and industries, where it is often specifically defined. It may also be applied colloquially or figuratively, with a broa ...
as "Substances which may be abused or misused, the manufacture, possession, sale or use of which should be prohibited by law except when required for medical or scientific research, or for analytical, teaching or training purposes with approval of the CEO." Under the Misuse of Drugs Act 1981 6.0g is the amount required determining a court of trial, 2.0g is considered intent to sell and supply.


Germany

Acetorphine is illegal in Germany (
Anlage I Anlage may refer to: * Allele, a specific version of a gene, as used by Gregor Mendel * Anlage Süd, a headquarters facility of the German Third Reich in Strzyżów, Poland * Primordium, the initial clustering of embryonic cells from which a body ...
)


United Kingdom

Acetorphine is considered a Class A drug by the
UK Misuse of Drugs Act The Misuse of Drugs Act 1971 is an Act of the Parliament of the United Kingdom. It represents action in line with treaty commitments under the Single Convention on Narcotic Drugs, the Convention on Psychotropic Substances, and the United Nation ...
since 1971, making its unlawful possession and distribution illegal. Class A drugs are deemed to be the most dangerous.


United States

Acetorphine is a Schedule I controlled substance in the United States. Its DEA Administrative Controlled Substances Control Number is 9319 and the one salt in use, acetorphine hydrochloride, has a freebase conversion ratio of 0.93.


Italy

In Italy Acetorphine is illegal, as are the parent compounds
Etorphine 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 r ...
and
Dihydroetorphine Dihydroetorphine was developed by K. W. Bentley at McFarlan-Smith in the 1960s and is a potent opioid analgesic used mainly in China. It is a derivative of the better-known opioid etorphine, a very potent veterinary painkiller and anesthetic med ...
. (Data from 2022)


See also

*
6,14-Endoethenotetrahydrooripavine 6,14-Endoethenotetrahydrooripavine is the central nucleus, or backbone, of a class of morphinan opioids known as the Bentley compounds and may be considered their "privileged scaffold". These include but are not limited to etorphine and buprenor ...


References


External links


Space filling 3D model and ball & stick 3D model full motion animated rotating of Acetorphine/Acetyletorphine

2D nonanimated/nonmoving rendering of Acetorphine/Acetyletorphine as a flat diagram
Semisynthetic opioids Mu-opioid receptor agonists 4,5-Epoxymorphinans Tertiary alcohols Ethers Acetate esters {{analgesic-stub