Talk:Oxymorphazone: Difference between revisions

 

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    |IntravenousROA_Bioavailability=[[Intravenous min bioavailability::x1]]% - [[Intravenous max bioavailability::x2]]%<ref>APA formatted citation</ref>

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Oxymorphazone was first synthesised in 1979 by a team of Chemists at Rockefeller University, New York. Recent attempts to build effective irreversible opioid [[agonists]] encouraged the team to develop a hydrazone derivative of oxymorphone.

Oxymorphazone is an opioid of the morphinan class. Oxymorphazone and other molecules of this class contain a polycyclic core of three benzene rings fused in a zig-zag pattern called phenanthrene. A fourth nitrogen containing ring is fused to the phenanthrene at R₉ and R₁₃ with the nitrogen member looking at R₁₇ of the combined structure. This structure is called morphinan. Oxymorphazone is structurally similar to Oxymorphone, with a C₆ substitution of oxygen with a hydrazone group.

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.

If applicable, a brief paragraph summary of the substance's physical effects may be included here.

 

You may select physical effects to add below [[Subjective effect index#Physical effects|here]].

 

*'''[[Effect::Physical effect]]'''  

*'''[[Effect::Physical effect2]]'''

*'''[[Effect::Physical effect3]]'''

If applicable, a brief paragraph summary of the substance's cognitive effects may be included here.

 

You may select from a list of cognitive effects to add below [[Subjective effect index#Cognitive effects|here]].

 

*'''[[Effect::Cognitive effect1]]'''  

*'''[[Effect::Cognitive effect2]]'''  

*'''[[Effect::Cognitive effect3]]'''  

 

{{effects/multisensory|

 

You may select from a list of multisensory effects to add below [[Subjective effect index#Multisensory effects|here]].

 

*'''[[Effect::Multisensory effect1]]'''  

*'''[[Effect::Multisensory effect2]]'''

 

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.

When addiction has developed, cravings and [[Opioids#Discontinuation|withdrawal symptoms]] may occur if a person suddenly stops their usage.

 

Oxymorphazone presents cross-tolerance with [[Cross-tolerance::all other [[opioids]]]], meaning that after the consumption of oxymorphazone all [[opioid]]s will have a reduced effect.

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>

*'''United Kingdom''' - Oxymorphone is a Class A, Schedule 2 drug in the United Kingdom. It has no medical uses. <ref>Psychoactive Substances Act 2016. (2016). Retrieved from http://www.legislation.gov.uk/ukpga/2016/2/schedule/2/enacted</ref>

* [https://en.wikipedia.org/wiki/SUBSTANCE SUBSTANCE (Wikipedia)]

 

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