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Encyclopedia > Etorphine
Etorphine
Systematic (IUPAC) name
6,14-endoetheno – 7 a (1-(R)-hydroxy-1 methylbutyl)-tetrahydro-nororipavine
Identifiers
CAS number 14521-96-1
ATC code  ?
PubChem  ?
Chemical data
Formula C25H33NO4 
Mol. mass 411.53 g/mol
Pharmacokinetic data
Bioavailability  ?
Metabolism  ?
Half life  ?
Excretion  ?
Therapeutic considerations
Pregnancy cat.

? IUPAC nomenclature is a system of naming chemical compounds and of describing the science of chemistry in general. ... CAS registry numbers are unique numerical identifiers for chemical compounds, polymers, biological sequences, mixtures and alloys. ... The Anatomical Therapeutic Chemical Classification System is used for the classification of drugs. ... PubChem is a database of chemical molecules. ... A chemical formula is an easy way of expressing information about the atoms that constitute a particular chemical compound. ... For other uses, see Carbon (disambiguation). ... This article is about the chemistry of hydrogen. ... General Name, symbol, number nitrogen, N, 7 Chemical series nonmetals Group, period, block 15, 2, p Appearance colorless gas Standard atomic weight 14. ... This article is about the chemical element and its most stable form, or dioxygen. ... The molecular mass (abbreviated Mr) of a substance, formerly also called molecular weight and abbreviated as MW, is the mass of one molecule of that substance, relative to the unified atomic mass unit u (equal to 1/12 the mass of one atom of carbon-12). ... In pharmacology, bioavailability is used to describe the fraction of an administered dose of unchanged drug that reaches the systemic circulation, one of the principal pharmacokinetic properties of drugs. ... Drug metabolism is the metabolism of drugs, their biochemical modification or degradation, usually through specialized enzymatic systems. ... The biological half-life of a substance is the time required for half of that substance to be removed from an organism by either a physical or a chemical process. ... The kidneys are important excretory organs in vertebrates. ... The pregnancy category of a pharmaceutical agent is an assessment of the risk of fetal injury due to the pharmaceutical, if it is used as directed by the mother during pregnancy. ...

Legal status

List 1NL Schedule I/II(see text)US The regulation of therapeutic goods, that is drugs and therapeutic devices, varies by jurisdiction. ... NL can stand for: NL (complexity), a computational complexity class Netherlands, its alpha-2 country code Dutch language, its alpha-2 language code Shaheen Air International, its IATA airline designator National League, US baseball league Newfoundland and Labrador, its Canada Post provincial abbreviation New Line, film production studio No liability... United States may refer to: Places: United States of America SS United States, the fastest ocean liner ever built. ...

Routes  ?

Etorphine (Immobilon or M99) is a semi-synthetic opioid possessing an analgesic potency approximately 10,000 times that of morphine and 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.[1] It was later reproduced in 1963 by a research group at McFarlan-Smith and Co. in Edinburgh, led by Professor Kenneth Bentley.[2][3] It can also be produced from thebaine. In pharmacology and toxicology, a route of administration is the path by which a drug, fluid, poison or other substance is brought into contact with the body. ... An opioid is a chemical substance that has a morphine-like action in the body. ... An analgesic (colloquially known as a painkiller) is any member of the diverse group of drugs used to relieve pain (achieve analgesia). ... This article is about the drug. ... Oripavine is an opiate and the major metabolite of thebaine. ... Binomial name L. The opium poppy, Papaver somniferum, is the type of poppy from which opium and all refined opiates such as morphine, thebaine, codeine, papaverine, and noscapine are extracted. ... Binomial name Papaver orientale (L.) The Oriental poppy (Papaver orientale) is a perennial poppy of the genus Papaver. ... A minor constituent of opium, thebaine or paramorphine (C19H21NO3) is chemically similar to both morphine and codeine, but produces stimulatory rather than depressant effects. ...


Etorphine is most often used to immobilize elephants and other large mammals. Etorphine is only available legally for veterinary use and is strictly governed by law. Diprenorphine (M5050) 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; one drop on the skin can cause death within a few minutes.[4] Genera and Species Loxodonta Loxodonta cyclotis Loxodonta africana Elephas Elephas maximus Elephas antiquus † Elephas beyeri † Elephas celebensis † Elephas cypriotes † Elephas ekorensis † Elephas falconeri † Elephas iolensis † Elephas planifrons † Elephas platycephalus † Elephas recki † Stegodon † Mammuthus † Elephantidae (the elephants) is a family of pachyderm, and the only remaining family in the order Proboscidea... Veterinary medicine is the application of medical, diagnostic, and therapeutic principles to companion, domestic, exotic, wildlife, and production animals. ... Diprenorphine (Revivon, M5050) is an opiate 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. ...


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. Acepromazine or Acetylpromazine is one of the phenothiazine derivative psychotropic drugs, used little in humans, however frequently in animals as a means of chemical restraint. ... Diprenorphine (Revivon, M5050) is an opiate 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. ... Naloxone is a drug used to counter the effects of opioid overdose, for example heroin and morphine overdose. ...


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. China is one of the only countries in the world to prescribe Dihydroetorphine, (a close relative of Etorphine) to humans. ...

Contents

Pharmacology

Etorphine is an agonist at μ, δ, and κ opioid receptors. It also has a weak affinity for the ORL1 nociceptin/orphanin FQ receptor.[5] The μ opioid receptors (MOR) are a class of opioid receptors with high affinity for enkephalins and beta-endorphin but low affinity for dynorphins. ... δ-Opioid receptor activation produces analgesia. ... κ-Opioid receptors are involved with analgesia, but activation also produces marked nausea and dysphoria. ... Opioid receptors are a group of G-protein coupled receptors with opioids as ligands. ... Opioid receptors are a group of G-protein coupled receptors with opioids as ligands. ...


Legal status

In Hong Kong, Etorphine is regulated under Schedule 1 of Hong Kong's Chapter 134 Dangerous Drugs Ordinance. It can only be used legally by health professionals and for university research purporses. The substance can be given by pharmacists under a prescription. Anyone who supplies the substance without prescription can be fined $10000(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. ISO 4217 Code HKD User(s) Hong Kong Inflation 2. ...


In the Netherlands, Etorphine is a list I drug of the Opium Law. It is only used for veterinary purposes in zoos to immobilise large animals.


In the US, Etorphine is listed as a Schedule I drug, although Etorphine hydrochloride is classified as Schedule II. In chemistry, hydrochlorides are salts resulting, or regarded as resulting, from the reaction of hydrochloric acid with an organic base (mostly amines). ...


References

  1. ^ Opium: the king of narcotics
  2. ^ Bentley KW, Hardy DG. "New potent analgesics in the morphine series." Proceedings of the Chemical Society. 1963;220.
  3. ^ Bentley KW, Hardy DG. "Novel analgesics and molecular rearrangements in the morphine-thebaine group. 3. Alcohols of the 6,14-endo-ethenotetrahydrooripavine series and derived analogs of N-allylnormorphine and -norcodeine." Journal of the American Chemical Society. 1967 Jun 21;89(13):3281-92. PMID 6042764
  4. ^ Zoo Vet At Large - Sky Travel (8 July 2007, Part 10 of 26)
  5. ^ Hawkinson JE, Acosta-Burruel M, Espitia SA. "Opioid activity profiles indicate similarities between the nociceptin/orphanin FQ and opioid receptors." European Journal of Pharmacology. 2000 Feb 18;389(2-3):107-14. PMID 10688973

Sky Travel is a channel from BSkyB that shows extensive programmes about travel, adverts for travel agencies, and documentries. ... is the 189th day of the year (190th in leap years) in the Gregorian calendar. ... Year 2007 (MMVII) was a common year starting on Monday of the Gregorian calendar in the 21st century. ...

External links

  • Opioids.com page on etorphine
  • Etorphine: Molecule of the Month

  Results from FactBites:
 
ZooPharm » Drug Information » Etorphine hydrochloride (806 words)
Etorphine revolutionized the ability of biologists and veterinarians to safely capture and restrain many species that previously could not be handled.
Etorphine has been used in almost every wild and free-ranging group with the exception of members of the family Felidae which have severe and adverse reactions to all opiate agonists.
Etorphine has had limited use in domestic species in the United States due to its high opiate agonist potency and the level of DEA control on this substance.
Etorphine (6686 words)
The syndrome manifests as pink froth from the trunk and is caused by pulmonary edema and capillary bleeding.
Group 1 (n=71) was immobilized with 4-8 mg etorphine; group 2 (n=109) was immobilized with 4-8 mg etorphine and 50-90 mg azaperone; and group 3 (n=26) was immobilized with 4-8 mg carfentanil and 50-90 mg azaperone.
Following immobilization with etorphine hydrochloride or carfentanil citrate, six of seven elephants were intubated and maintained on a 1-1.5% halothane in oxygen mixture; one elephant was maintained in lateral recumbency by multiple i.v.
  More results at FactBites »


 

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