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Ketobemidone: Difference between revisions
>IJUSTPOPPEDAXAN Added basic subjective effects |
>IJUSTPOPPEDAXAN Added basic history and culture information |
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{{SubstanceBox/Ketobemidone}} | {{SubstanceBox/Ketobemidone}} | ||
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'''Ketobemidone''' (also known by the brand names '''Ketogan''', and '''Ketorax''') is a synthetic [[Opioids|opioid]] substance of the [[Substituted piperidines|piperidine]] class. It is used to treat severe pain (like cancer pain, postoperative pain, gallstone pain, and kidney pain). | '''Ketobemidone''' (also known by the brand names '''Ketogan''', and '''Ketorax''') is a synthetic [[Opioids|opioid]] substance of the [[Substituted piperidines|piperidine]] class. It is used to treat severe pain (like cancer pain, postoperative pain, gallstone pain, and kidney pain). | ||
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==History and culture== | ==History and culture== | ||
Ketobemidone was first synthesized during World War II by German scientists at the I.G. Farbenindustrie laboratory in Höchst, 1942.<ref>[https://worldwide.espacenet.com/patent/search/family/004472963/publication/GB609763A?q=pn%3DGB609763 GB patent 609763], "Manufacture of piperidyl ketones", published 1948-10-06, assigned to Ciba Ltd.</ref> | |||
Today, Pfizer produces ketobemidone under the brand names Ketogan and Ketorax in tablet and suppository form as well as injection liquids.{{citation needed}} | |||
==Chemistry== | ==Chemistry== | ||
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==Pharmacology== | ==Pharmacology== | ||
Ketobemidone is metabolized in the liver by N- | Ketobemidone is metabolized in the liver by N-demethylation, ringhydroxylation, O-methylation, and O-conjugation. The principal phase 1 reaction is N-demethylation, and it is also metabolized by conjugation of the phenolic hydroxyl group.<ref>Bondesson U, Hartvig P, Danielsson B (1981). "Quantitative determination of the urinary excretion of ketobemidone and four of its metabolites after intravenous and oral administration in man". ''Drug Metabolism and Disposition.'' '''9''' (4): 376–80. PMID [https://pubmed.ncbi.nlm.nih.gov/6114838 6114838].</ref> Primary metabolites of ketobemidone are norketobemidone, 4'-hydroxyketobemidone, and hydroxymethoxyketobemidone. The metabolites' pharmacological activity is unknown.<ref name=":0">https://bok.fass.se/LIF/product?userType=0&nplId=19930507000075</ref> | ||
The elimination half-life of ketobemidone is 2 to 2.5 hours for both intravenous and oral administration.<ref name=":0" /> | The elimination half-life of ketobemidone is 2 to 2.5 hours for both intravenous and oral administration.<ref name=":0" /> | ||
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==Subjective effects== | ==Subjective effects== | ||
* Euphoria | *Euphoria | ||
* Confusion | *Confusion | ||
* Sedation | *Sedation | ||
* Dizziness | *Dizziness | ||
* Headache | *Headache | ||
* Blurred vision | *Blurred vision | ||
* Bradycardia | *Bradycardia | ||
* Respiratory depression | *Respiratory depression | ||
* Dry mouth | *Dry mouth | ||
* Nausea | *Nausea | ||
* Vomiting | *Vomiting | ||
* Constipation | *Constipation | ||
* Difficulty urinating | *Difficulty urinating | ||
* Decreased blood pressure | *Decreased blood pressure | ||
==Toxicity and harm potential== | ==Toxicity and harm potential== | ||