Diprenorphine

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Image:Diprenorphine.png
Diprenorphine
Systematic (IUPAC) name
(5α,7α)-17-(Cyclopropylmethyl) -4,5-epoxy-18,19-dihydro-3-hydroxy-6-methoxy -α,α-dimethyl-6,14-ethenomorphinan-7-methanol
Identifiers
CAS number 14357-78-9
ATC code  ?
PubChem 443408
Chemical data
Formula C26H35NO4 
Mol. mass 425.56 g/mol
SMILES eMolecules & PubChem
Pharmacokinetic data
Bioavailability  ?
Metabolism  ?
Half life  ?
Excretion  ?
Therapeutic considerations
Pregnancy cat.

?

Legal status
Routes  ?

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Diprenorphine (Revivon, M5050) is an opiate antagonist[1] 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.

Diprenorphine is the strongest opiate antagonist that is commercially available (some 100 times more potent as an antagonist than nalorphine),[1] and is used for reversing the effects of very strong opioids for which the binding affinity is so high that naloxone does not effectively or reliably reverse the narcotic effects.[1] These super-potent opioids are not used in humans because the dose for a human is so small that it would be difficult to measure properly, so there is an excessive risk of overdose leading to fatal respiratory depression. However conventional opioid derivatives are not strong enough to rapidly tranquilize large animals such as elephants and rhinos, so drugs such as etorphine or carfentanil are available for this purpose.

Diprenorphine is considered the specific antagonist for etorphine and carfentanil,[1] and is normally used to remobilise animals once veterinary procedures have been completed,[1] however it may also be used on humans in the event that they are accidentally exposed to etorphine or carfentanil, for instance if someone working with large animals suffered a needlestick injury with a dart from a tranquiliser dart gun that was loaded with etorphine or carfentanil, they would be given diprenorphine as an antidote.

In theory diprenorphine could also be used as an antidote for treating overdose of certain opioid derivatives which are used in humans, such as buprenorphine, for which the binding affinity is so high that naloxone does not reliably reverse the narcotic effects. However diprenorphine is not generally available in hospitals, instead a vial of diprenorphine is supplied with the etorphine or carfentanil specifically for reversing the effects of these drugs, so use of diprenorphine for treating buprenorphine overdose is not carried out in practice although it would work in theory.

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Acknowledgement and Attribution Regarding Sources of Content

Some of the initial content on this page may be incorporated in part from copyleft sources in the public domain including wikis such as Wikipedia and AskDrWiki. Drug information for patients came from the The National Library of Medicine. Infectious disease information may have come from the Centers for Disease Control (CDC). Differential Diagnoses are drawn from clinicians as well as an amalgamation of 3 sources: 1.The Disease Database; 2. Kahan, Scott, Smith, Ellen G. In A Page: Signs and Symptoms. Malden, Massachusetts: Blackwell Publishing, 2004:3; 3. Sailer, Christian, Wasner, Susanne. Differential Diagnosis Pocket. Hermosa Beach, CA: Borm Bruckmeir Publishing LLC, 2002:7 .

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