Etorphine
Encyclopedia
Etorphine is a semi-synthetic opioid
possessing an analgesic
potency approximately 200 times that of morphine
. It was first prepared in 1960 from oripavine
, which does not generally occur in opium poppy
extract but rather in "poppy straw" and in related plants, Papaver orientale
and Papaver bracteatum
. It was later reproduced in 1963 by a research group at Macfarlan-Smith and Co. in Edinburgh, led by Professor Kenneth Bentley. It can also be produced from thebaine
.
Etorphine is often used to immobilize elephant
s and other large mammals. Etorphine is available legally only for veterinary
use and is strictly governed by law. Diprenorphine
(M5050), also known as Revivon, is an opioid receptor antagonist that can be administered in proportion to the amount of etorphine used (1.3 times) to reverse its effects. Veterinary-strength etorphine is fatal to humans. For this reason the package as supplied to vets always includes the human antidote as well as Etorphine.
One of its main advantages in general veterinary work is its speed of operation and, even more important, the speed with which Revivon reverses the effects. For example, operations on valuable animals, such as racehorses, using alternative anesthetics risk the animal injuring itself as the anesthetic wears off. The rapid action of Immobilon and Revivon means the animal can be back on its feet within a relatively short time and aware of its surroundings more quickly, thus reducing any tendency to panic and move around rapidly while still partially under the influence of the anesthetic. For this reason, its use is popular with many vets.
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 close relative, dihydroetorphine
has been used as an opioid painkiller for human usage in China. It is claimed to be less addictive than traditional opioids but this has yet to be confirmed.
, δ
, and κ
opioid receptors. It also has a weak affinity for the ORL1 nociceptin
/orphanin FQ receptor.
, Etorphine is regulated under Schedule 1 of Hong Kong's Chapter 134 Dangerous Drugs Ordinance. It can be used legally only by health professionals and for university research purposes. The substance can be given by pharmacists under a prescription. Anyone who supplies the substance without prescription can be fined $10,000 (HKD
). The penalty for trafficking or manufacturing the substance is a $5,000,000 (HKD) fine and life imprisonment. Possession of the substance for consumption without license from the Department of Health is illegal with a $1,000,000 (HKD) fine and/or 7 years of jail time.
In the Netherlands
, Etorphine is a list I drug of the Opium Law
. It is used only for veterinary purposes in zoos to immobilize large animals.
In the US, Etorphine is listed as a Schedule I drug, although Etorphine hydrochloride
is classified as Schedule II.
, M99 is used by the show's serial-killer protagonist Dexter Morgan
to sedate his victims via injection by a hypodermic needle. The sedative works instantly, rendering the injected immobile and unconscious within a couple of seconds and lasting for several hours. Dexter is able to access the drug through one of his aliases, Patrick Bateman
, M.D.. "Patrick Bateman" is the name of the main character in the novel American Psycho
by Bret Easton Ellis
. Patrick Bateman is also a serial killer.
It was also used on the Blue Bloods (TV series)
television series by a fanatical mother and son serial killer team who prey on prostitutes in the episode "Lonely Hearts Club".
Opioid
An opioid is a psychoactive chemical that works by binding to opioid receptors, which are found principally in the central and peripheral nervous system and the gastrointestinal tract...
possessing an analgesic
Analgesic
An analgesic is any member of the group of drugs used to relieve pain . The word analgesic derives from Greek an- and algos ....
potency approximately 200 times that of morphine
Morphine
Morphine is a potent opiate analgesic medication and is considered to be the prototypical opioid. It was first isolated in 1804 by Friedrich Sertürner, first distributed by same in 1817, and first commercially sold by Merck in 1827, which at the time was a single small chemists' shop. It was more...
. It was first prepared in 1960 from oripavine
Oripavine
Oripavine is an opiate and the major metabolite of thebaine. It is the parent compound from which a series of semi-synthetic opioids are derived, which includes the compounds etorphine and buprenorphine...
, which does not generally occur in opium poppy
Opium poppy
Opium poppy, Papaver somniferum, is the species of plant from which opium and poppy seeds are extracted. Opium is the source of many opiates, including morphine , thebaine, codeine, papaverine, and noscapine...
extract but rather in "poppy straw" and in related plants, Papaver orientale
Oriental poppy
Papaver orientale is a perennialflowering plant native to the Caucasus, northeastern Turkey, and northern Iran, not the Orient as the name implies....
and Papaver bracteatum
Papaver bracteatum
Papaver bracteatum, also known as the Iranian poppy, is a sturdy perennial poppy with large deep red flowers up to 8 inches across on stiff stalks up to 4 feet high with a prominent black spot near the base of the petals...
. It was later reproduced in 1963 by a research group at Macfarlan-Smith and Co. in Edinburgh, led by Professor Kenneth Bentley. It can also be produced from thebaine
Thebaine
Thebaine , its name coming from the Greek Θῆβαι, Thēbai, an ancient city in Upper Egypt, is an opiate alkaloid. A minor constituent of opium, thebaine is chemically similar to both morphine and codeine, but has stimulatory rather than depressant effects, causing convulsions similar to strychnine...
.
Etorphine is often used to immobilize elephant
Elephant
Elephants are large land mammals in two extant genera of the family Elephantidae: Elephas and Loxodonta, with the third genus Mammuthus extinct...
s and other large mammals. Etorphine is available legally only for veterinary
Veterinary medicine
Veterinary Medicine is the branch of science that deals with the prevention, diagnosis and treatment of disease, disorder and injury in non-human animals...
use and is strictly governed by law. Diprenorphine
Diprenorphine
Diprenorphine is an opioid antagonist used to reverse the effects of the super-potent opioid analgesics such as etorphine and carfentanil that are used for tranquilizing large animals in veterinary medicine....
(M5050), also known as Revivon, is an opioid receptor antagonist that can be administered in proportion to the amount of etorphine used (1.3 times) to reverse its effects. Veterinary-strength etorphine is fatal to humans. For this reason the package as supplied to vets always includes the human antidote as well as Etorphine.
One of its main advantages in general veterinary work is its speed of operation and, even more important, the speed with which Revivon reverses the effects. For example, operations on valuable animals, such as racehorses, using alternative anesthetics risk the animal injuring itself as the anesthetic wears off. The rapid action of Immobilon and Revivon means the animal can be back on its feet within a relatively short time and aware of its surroundings more quickly, thus reducing any tendency to panic and move around rapidly while still partially under the influence of the anesthetic. For this reason, its use is popular with many vets.
Large Animal Immobilon is a combination of etorphine plus acepromazine
Acepromazine
Acepromazine or acetylpromazine is a phenothiazine derivative antipsychotic drug. It was first used in humans in the 1950s, but is now little used in humans...
maleate. An etorphine antidote Large Animal Revivon contains mainly diprenorphine for animals and a human-specific naloxone
Naloxone
Naloxone is an opioid antagonist drug developed by Sankyo in the 1960s. Naloxone is a drug used to counter the effects of opiate overdose, for example heroin or morphine overdose. Naloxone is specifically used to counteract life-threatening depression of the central nervous system and respiratory...
-based antidote, which should be prepared prior to the etorphine.
A close relative, dihydroetorphine
Dihydroetorphine
Dihydroetorphine was developed by K.W.Bentley at McFarlan-Smith in the 1960s and is a potent analgesic drug , which is used mainly in China...
has been used as an opioid painkiller for human usage in China. It is claimed to be less addictive than traditional opioids but this has yet to be confirmed.
Pharmacology
Etorphine is an agonist at μMu Opioid receptor
The μ-opioid receptors are a class of opioid receptors with high affinity for enkephalins and beta-endorphin but low affinity for dynorphins. They are also referred to as μ opioid peptide receptors. The prototypical μ receptor agonist is the opium alkaloid morphine; μ refers to morphine...
, δ
Delta Opioid receptor
The δ-opioid receptors, also known as delta opioid receptor or simply delta receptor, abbreviated DOR, is an opioid receptor that has enkephalins as its endogenous ligands.-Function:...
, and κ
Kappa Opioid receptor
The κ-opioid receptor is a protein that in humans is encoded by the OPRK1 gene. The κ-opioid receptor is one of five related receptors that bind opium-like compounds in the brain and are responsible for mediating the effects of these compounds...
opioid receptors. It also has a weak affinity for the ORL1 nociceptin
Nociceptin
Nociceptin or orphanin FQ, a 17 amino acid neuropeptide, is the endogenous ligand for the nociceptin receptor . It is derived from the prepronociceptin protein, as are a further 2 peptides, nocistatin & NocII...
/orphanin FQ receptor.
Legal status
In Hong KongHong Kong
Hong Kong is one of two Special Administrative Regions of the People's Republic of China , the other being Macau. A city-state situated on China's south coast and enclosed by the Pearl River Delta and South China Sea, it is renowned for its expansive skyline and deep natural harbour...
, Etorphine is regulated under Schedule 1 of Hong Kong's Chapter 134 Dangerous Drugs Ordinance. It can be used legally only by health professionals and for university research purposes. The substance can be given by pharmacists under a prescription. Anyone who supplies the substance without prescription can be fined $10,000 (HKD
Hong Kong dollar
The Hong Kong dollar is the currency of the jurisdiction. It is the eighth most traded currency in the world. In English, it is normally abbreviated with the dollar sign $, or alternatively HK$ to distinguish it from other dollar-denominated currencies...
). The penalty for trafficking or manufacturing the substance is a $5,000,000 (HKD) fine and life imprisonment. Possession of the substance for consumption without license from the Department of Health is illegal with a $1,000,000 (HKD) fine and/or 7 years of jail time.
In the Netherlands
Netherlands
The Netherlands is a constituent country of the Kingdom of the Netherlands, located mainly in North-West Europe and with several islands in the Caribbean. Mainland Netherlands borders the North Sea to the north and west, Belgium to the south, and Germany to the east, and shares maritime borders...
, Etorphine is a list I drug of the Opium Law
Opium Law
The Opium Law is the section of the Dutch law which covers nearly all psychotropic drugs. All non-psychotropic, but prescription-only drugs are covered by the Medicine Act.- Origin and history :...
. It is used only for veterinary purposes in zoos to immobilize large animals.
In the US, Etorphine is listed as a Schedule I drug, although Etorphine hydrochloride
Hydrochloride
In chemistry, hydrochlorides are salts resulting, or regarded as resulting, from the reaction of hydrochloric acid with an organic base . This is also known as muriate, derived from hydrochloric acid's other name: muriatic acid....
is classified as Schedule II.
In media
In the Showtime television series DexterDexter (TV series)
Dexter is an American television drama series, which debuted on Showtime on October 1, 2006. The sixth season premiered on October 2, 2011. The series centers on Dexter Morgan , a bloodstain pattern analyst for the Miami Metro Police Department who moonlights as a serial killer...
, M99 is used by the show's serial-killer protagonist Dexter Morgan
Dexter Morgan
Dexter Morgan is a fictional character in a series of novels by Jeff Lindsay, including Darkly Dreaming Dexter , Dearly Devoted Dexter , Dexter in the Dark , Dexter by Design , Dexter is Delicious and Double Dexter...
to sedate his victims via injection by a hypodermic needle. The sedative works instantly, rendering the injected immobile and unconscious within a couple of seconds and lasting for several hours. Dexter is able to access the drug through one of his aliases, Patrick Bateman
Patrick Bateman
Patrick Bateman is a fictional character, the antihero and narrator of the novel American Psycho by Bret Easton Ellis, and its film adaptation. He has also briefly appeared in other Ellis novels.-Biography and profile:...
, M.D.. "Patrick Bateman" is the name of the main character in the novel American Psycho
American Psycho
American Psycho is a psychological thriller and satirical novel by Bret Easton Ellis, published in 1991. The story is told in the first person by the protagonist, serial killer and Manhattan businessman Patrick Bateman. The book's graphic violence and sexual content generated a great deal of...
by Bret Easton Ellis
Bret Easton Ellis
Bret Easton Ellis is an American novelist and short story writer. His works have been translated into 27 different languages. He was regarded as one of the so-called literary Brat Pack, which also included Tama Janowitz and Jay McInerney...
. Patrick Bateman is also a serial killer.
It was also used on the Blue Bloods (TV series)
Blue Bloods (TV series)
Blue Bloods is an American police procedural/drama series on CBS, filmed on location in New York City. The show premiered on September 24, 2010, with episodes airing on Fridays at 10:00 pm Eastern and Pacific/9:00 PM Central and Mountain....
television series by a fanatical mother and son serial killer team who prey on prostitutes in the episode "Lonely Hearts Club".
External links
- Opioids.com page on etorphine
- Etorphine: Molecule of the Month