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Dihydroetorphine



Dihydroetorphine
Systematic (IUPAC) name
(5R,6R,7R,9R,13S,14R)-7-[(R)-2-Hydroxypentan-2-yl] -6-methoxy-17-methyl-4,5-epoxy-6,14-ethanomorphinan-3-ol
Identifiers
CAS number 14357-76-7
ATC code  ?
PubChem 107765
Chemical data
Formula C25H35NO4 
Mol. mass 413.5497 g/mol
Pharmacokinetic data
Bioavailability  ?
Metabolism  ?
Half life  ?
Excretion  ?
Therapeutic considerations
Pregnancy cat.

?

Legal status

Schedule II

Routes  ?

Dihydroetorphine is a potent analgesic drug (painkiller),[1] which is used mainly in China. It is a derivative of the more well-known opioid etorphine, which is used as a very potent veterinary painkiller and anesthetic medication, primarily for the sedation of large animals such as elephants, giraffes and rhinos.

Additional recommended knowledge

Dihydroetorphine is a semi-synthetic opioid, used mainly as a strong painkiller for humans.[2] It is several thousand times stronger than morphine (between 1000x and 12000x more potent depending what method is used for comparison), although it is poorly absorbed when taken orally. Sublingual forms of dihydroetorphine are used in China at doses ranging from 20 to 180µg, and are reported to cause strong analgesia and relatively mild side effects compared to other opioids, although all the usual opioid side effects such as dizziness, sedation, nausea, constipation, and respiratory depression can occur. Transdermal patches of dihydroetorphine have also been developed.[3]

Dihydroetorphine is considered to be somewhat less addictive than many other opioids, and is also sometimes used in China as a substitute maintenance drug for opioid addicts,[4] in a similar way to how the related drug buprenorphine is used in western nations.[5][6]

References

  1. ^ Martin TJ, Hairston CT, Lutz PO, et al. Anti-allodynic actions of intravenous opioids in the nerve injured rat: Potential utility of heroin and dihydroetorphine against neuropathic pain. European Journal of Pharmacology 1998;357:25-32.
  2. ^ Lewis JW, Husbands SM. The orvinols and related opioids--high affinity ligands with diverse efficacy profiles. Current Pharmaceutical Design. 2004;10(7):717-32.
  3. ^ Ohmori S, Morimoto Y. Dihydroetorphine: a potent analgesic: pharmacology, toxicology, pharmacokinetics, and clinical effects. CNS Drug Reviews. 2002 Winter;8(4):391-404.
  4. ^ Qin Bo-Yi (1998). "Advances in dihydroetorphine: From analgesia to detoxification". Drug Development Research 39 (2): 131-134. Link
  5. ^ Gerak LR, Gauthier CR, France CR. Discriminative stimulus and antinociceptive effects of dihydroetorphine in rhesus monkeys. Psychopharmacology (Berlin). 2003 Apr;166(4):351-9.
  6. ^ Husbands SM, Lewis JW. Opioid ligands having delayed long-term antagonist activity: potential pharmacotherapies for opioid abuse. Mini Reviews in Medicinal Chemistry. 2003 Mar;3(2):137-44.
  • http://www.deadiversion.usdoj.gov/21cfr/cfr/1308/1308_12.htm


 
This article is licensed under the GNU Free Documentation License. It uses material from the Wikipedia article "Dihydroetorphine". A list of authors is available in Wikipedia.
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