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Acetorphine is a potent
opioid Opioids are a class of Drug, drugs that derive from, or mimic, natural substances found in the Papaver somniferum, opium poppy plant. Opioids work on opioid receptors in the brain and other organs to produce a variety of morphine-like effects, ...
analgesic An analgesic drug, also called simply an analgesic, antalgic, pain reliever, or painkiller, is any member of the group of drugs used for pain management. Analgesics are conceptually distinct from anesthetics, which temporarily reduce, and in s ...
, up to 8700 times stronger than
morphine Morphine, formerly also called morphia, is an opiate that is found naturally in opium, a dark brown resin produced by drying the latex of opium poppies (''Papaver somniferum''). It is mainly used as an analgesic (pain medication). There are ...
by weight. It is a
derivative In mathematics, the derivative is a fundamental tool that quantifies the sensitivity to change of a function's output with respect to its input. The derivative of a function of a single variable at a chosen input value, when it exists, is t ...
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 re ...
, 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 non-human animals. The scope of veterinary medicine is wide, covering all animal species, both ...
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 t ...
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, currently branded as Reckitt, formerly known as Reckitt Benckiser, is a British multinational consumer goods company headquartered in Slough, United Kingdom. It is a producer of health, hygiene and nutrition pro ...
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, formerly sold under the brand name Wildnil, is an extremely potent opioid analgesic used in veterinary medicine to anesthetize large animals such as elephants and rhinoceroses. It is a structural analogue of the ...
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 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 6.0 g is the amount required determining a court of trial, 2.0 g is considered intent to sell and supply.


Germany

Acetorphine is illegal in Germany (
Anlage I The following drugs are controlled by the German Narcotic Drugs Act ( or ). Trade and possession of these substances without licence or prescription is considered illegal; prescription is illegal for drugs on ''Anlage I'' and II and drugs on ''Anl ...
).


Indonesia

Acetorphine is considered as a class 1 narcotic drug in Indonesia, along with etorphine 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 medi ...
. A class 1 narcotic drug can only be used for scientific development purposes and not be used in therapy.


Italy

In Italy acetorphine is illegal, as are the parent compounds etorphine and dihydroetorphine.


Romania

Acetorphine is prohibited in Romania.


United Kingdom

Acetorphine is considered a Class A drug by the
UK Misuse of Drugs Act The Misuse of Drugs Act 1971 (c. 38) 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 Uni ...
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.


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