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| Trade names | Revivon |
| Other names | Diprenorfin; M5050 |
| AHFS/Drugs.com | International Drug Names |
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| ECHA InfoCard | 100.034.826 |
| Chemical and physical data | |
| Formula | C26H35NO4 |
| Molar mass | 425.569 g·mol−1 |
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Diprenorphine (brand nameRevivon; former developmental code nameM5050),[1] also known asdiprenorfin, is anon-selective, high-affinity, weakpartial agonist of theμ- (MOR),κ- (KOR), andδ-opioid receptor (DOR) (with equal affinity) which is used inveterinary medicine as anopioid antagonist.[2][3][4] It is used to reverse the effects of super-potentopioidanalgesics such asetorphine andcarfentanil that are used fortranquilizing large animals. The drug is not approved for use in humans.[5]
Diprenorphine is the strongest opioid antagonist that is commercially available (some 100 times more potent thannalorphine),[6] and is used for reversing the effects of very strong opioids for which the binding affinity is so high thatnaloxone does not effectively or reliably reverse the narcotic effects.[7] These super-potent opioids, with the single exception ofbuprenorphine (which has an improved safety-profile due to its partial agonism character[8]), are not used in humans because the dose for a human is so small that it would be difficult to measure properly[citation needed], so there is an excessive risk ofoverdose leading to fatalrespiratory depression. However conventional opioid derivatives are not strong enough to rapidly tranquilize large animals, like elephants and rhinos, so drugs such as etorphine and carfentanil are available for this purpose.
Diprenorphine is considered to be the specific reversing agent/antagonist for etorphine and carfentanil,[9] and is normally used to remobilise animals once veterinary procedures have been completed.[10] Since diprenorphine also has partial agonistic properties of its own, it should not be used on humans if they are accidentally exposed to etorphine or carfentanil. Naloxone or naltrexone is the preferred human opioid receptor antagonist.[11]
In theory, diprenorphine could also be used as an antidote for treating overdose of certain opioid derivatives which are used in humans, particularlybuprenorphine 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 etorphine or carfentanil specifically for reversing the effects of the drug, so the use of diprenorphine for treating a buprenorphine overdose is not usually carried out in practice.
Because diprenorphine is a weak partial agonist of theopioid receptors rather than asilent antagonist, it can produce some opioid effects in the absence of other opioids at sufficient doses.[12] Moreover, due to partial agonism of the KOR, where it appears to possess significantly greaterintrinsic activity relative to the MOR, diprenorphine can producesedation as well as, in humans,hallucinations.[3][5][13][14][15]