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Ketobemidone

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Subjective Effects
Interactions
Tolerance
Legality
Ketobemidone molecule structureKetobemidone molecule structure
Open in Piru
Chemical Class
Piperidine

Ketobemidone is an opioid analgesic of the phenylpiperidine class1 used to treat severe pain.1 Its pain-relieving effectiveness is comparable to morphine,2 and it may help with some types of pain that respond poorly to other opioids.3 It has a high risk of substance use disorder. Overdose can cause respiratory depression1 and death.4 Combining it with other central nervous system depressants is strongly discouraged.

Dosage & Duration

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Dosage

Doses are population estimates that vary widely between individuals.

Threshold~5 mg
Light5 mg
Moderate5-10 mg
Strong10-15 mg
Heavy15+ mg

Duration

After Effects1-8 hours

Subjective Effects

Subjective Effects not written up yet

Reagent Testing

Expected colorimetric results for common reagent tests. Colors show reaction change over 1–2 minutes.

Marquis(MQ)
white → orange1
Mecke(ME)
white → blue2 → green2
Mandelin(MD)
yellow2 → blue2 → green2
Froe(FR)
white → blue1 → black2
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Pharmacology

Pharmacodynamics

Ketobemidone is an opioid analgesic with additional NMDA receptor antagonist activity.5 Its NMDA antagonism is partly attributable to an active metabolite and may contribute to analgesia in pain that responds poorly to other opioids.

Pharmacokinetics

Ketobemidone is metabolized mainly through conjugation of its phenolic hydroxyl group and N-demethylation. Its metabolism produces a metabolite with NMDA antagonist activity. About 13-24% is excreted unchanged after intravenous administration.6 Its reported elimination half-life is 2.25-2.45 hours.7

Interactions

Interactions not written up yet

An unlisted combination is an unknown one, not a safe one. Check a dedicated combination chart before mixing.

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Tolerance

Tolerance not written up yet

Harm Potential

Addiction & Dependence

Psychological

High

Ketobemidone has a high risk of substance use disorder; experiments in people with prior opioid addiction suggested substantial addictiveness and potentially greater abuse potential at high doses in people with current or prior opioid addiction. A separate study found it no more addictive than morphine and suggested a lower addiction risk under qualified clinical supervision because analgesia occurred at doses well below those producing euphoria.

Toxicity

Respiratory system

Ketobemidone overdose can cause respiratory depression8 that may progress to death.9

History & Culture

Ketobemidone was first synthesized in 1942 by Eisleb and colleagues in the I.G. Farbenindustrie laboratory at Hoechst during the Second World War. The first human study was published in 1946, and the compound entered clinical medicine shortly afterward.…

Legality

Legality not written up yet

References

Citations

  1. Ketogan Novum 5 mg tabletter — Produktresumé. Läkemedelsverket (2023). https://docetp.mpa.se/LMF/Ketogan%20Novum%20tablet%20SmPC_09001bee807a494f.pdf123
  2. Morfin, petidin eller ketobemidon ved akutt smerte – er det forskjeller av betydning?. Tidsskrift for Den norske legeforening (2000). https://tidsskriftet.no/2000/09/legemidler-i-praksis/morfin-petidin-eller-ketobemidon-ved-akutt-smerte-er-det-forskjeller-av1
  3. The opioid ketobemidone has a NMDA blocking effect. Pain / PubMed (1996). https://doi.org/10.1016/0304-3959(96)03123-51
  4. Fatal poisoning among patients with drug addiction. Danish Medical Journal (2015). https://ugeskriftet.dk/dmj/fatal-poisoning-among-patients-drug-addiction1
  5. Ketobemidone plus (RS)-3-dimethylamino-1,1-diphenylbut-1-ene (A29) is More Potent at NMDA Receptors than Ketobemidone Alone: Evidence for A29 as a Non-Competitive NMDA Receptor Antagonist. Pharmacology & Toxicology (1998). https://doi.org/10.1111/j.1600-0773.1998.tb01417.x1
  6. Quantitative determination of the urinary excretion of ketobemidone and four of its metabolites after intravenous and oral administration in man. Drug Metabolism and Disposition (1981). https://pubmed.ncbi.nlm.nih.gov/61148381
  7. Single-Dose Kinetics and Bioavailability of Ketobemidone. Acta Anaesthesiologica Scandinavica (1982). https://doi.org/10.1111/j.1399-6576.1982.tb01848.x1
  8. Ketogan Novum - Produktresumé. iMeds (2012). https://imeds.se/ketogan-novum/produktresume1
  9. Risiko for alvorlige bivirkninger ved bruk av ketobemidon (Ketorax). RELIS (2011). https://relis.no/artikler/28408/1
  10. Narcotic Drugs: Estimated World Requirements for 2002; Statistics for 2000. International Narcotics Control Board (2001). https://www.incb.org/documents/Narcotic-Drugs/Technical-Publications/2001/narcotic_drugs_2001_full.pdf1

Article Status

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