Talk:Oxymorphazone: Difference between revisions

Oxymorphazone is estimated to be 50-100% as potent as [[oxymorphone]]<ref name = "a">[Ling, G., Galetta, S., & Pasternak, G. (1984). Oxymorphazone: A long-acting opiate analgesic. Cellular And Molecular Neurobiology, 4(1), 1-13. doi: 10.1007/bf00710938]</ref>. Although oxymorphazone is active on its own, research suggests that oxymorphazone's extremely long duration of effects and irreversible binding is a result of rapid degradation to oxymorphonazine. Oxymorphonazine is some 20-40x more potent and forms a covalent bond with the MOR, causing extensively long clearance.

Due to strong binding affinity and it's long action, tolerance to oxymorphazone builds very rapidly<ref name= "a" /> and physical dependence is guaranteed, even from just one administration of the substance.

Oxymorphazone has a [[Toxicity::low toxicity]] relative to dose. It is estimated to be half to 100% as potent as oxymorphpne, suggesting that 10mg Oxymorphazone is equivalent to approximately 30mg morphine <ref>[Pergolizzi Jr., J., & Raffa, R. (2009). Oxymorphone and Opioid Rotation. Pain Medicine, 10(Suppl 1), S39-S48.]</ref>. As with all opioids, long-term effects can vary but can include diminished libido, apathy, and memory loss. It is also [[Toxicity::potentially [[respiratory depression|lethal]] when mixed with [[depressants]] like [[alcohol]] or [[benzodiazepines]]]].

Oxymorphazone use is considered '''extremely''' dangerous. This is because if overdose occurs, anatagonism of the [[μ-opioid]] [[receptor]] is not possible. Drugs such as [[naloxone]] are unable to knock oxymorphazone off the MOR, and as such are useless in treating oxymorphazone overdose. There are no MOR hydrazone antagonists (that would knock oxymorphazone off the MOR) on the market. Treatment of oxymorphazone overdose would be supportive care (such as mechanical ventilation) and ensuring the patient does not aspirate on their vomit.

A single administration of oxymorphazone results in physical dependence in rats<ref name= "a" /> . Tolerance also builds extremely rapidly, due to its prolonged effects. Thus, although oxymorphazone may have similar subjective effects to oxymorphone, it is likely addiction would develop in a much larger proportion of users.

The risk of fatal opioid overdoses rise sharply after a period of cessation and [[relapse]], largely because of reduced tolerance.<ref>Why Heroin Relapse Often Ends In Death - Lauren F Friedman (Business Insider) | http://www.businessinsider.com.au/philip-seymour-hoffman-overdose-2014-2</ref> To account for this lack of tolerance, it is safer to only dose a fraction of one's usual [[dosage]] if relapsing. It has also been found that the environment one is in can play a role in opioid tolerance. In one scientific study, rats with the same history of heroin administration were significantly more likely to die after receiving their dose in an environment not associated with the drug in contrast to a familiar environment.<ref>Siegel, S., Hinson, R., Krank, M., & McCully, J. (1982). Heroin “overdose” death: contribution of drug-associated environmental cues. Science, 216(4544), 436–437. https://doi.org/10.1126/science.7200260</ref>