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Ketobemidone: Difference between revisions
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{{headerpanel|{{DepressantOD|opiates}}}} | {{headerpanel|{{DepressantOD|opiates}}{{approval}}}} | ||
{{SummarySheet}} | {{SummarySheet}} | ||
{{SubstanceBox/Ketobemidone}} | {{SubstanceBox/Ketobemidone}} | ||
'''Ketobemidone''' (also known by the brand names '''Ketogan''', and '''Ketorax''') is | '''Ketobemidone''' (also known by the brand names '''Ketogan''', and '''Ketorax''') is an [[psychoactive class::opioid]] substance of the [[chemical class::piperidine]] class. It belongs to a group of synthetic opioids. The mechanism of action involves [[agonist|binding activity]] at [[opioid]] [[receptors]]. | ||
It is marketed in Denmark, Iceland, Norway and Sweden | It is commonly prescribed to treat severe pain (i.e. cancer pain, postoperative pain, gallstone pain, and kidney pain). It is marketed in Denmark, Iceland, Norway and Sweden for this purpose.<ref>Brayfield A, ed. (9 January 2017). "Ketobemidone Hydrochloride: Martindale: The Complete Drug Reference". ''MedicinesComplete''. London, UK: Pharmaceutical Press.</ref> | ||
[[Subjective effects]] include [[sedation]], [[pain relief]], [[muscle relaxation]], [[compulsive redosing]], and [[euphoria]]. Its effectiveness against pain is in the same range as morphine, and it also has some NMDA-antagonist properties imparted, in part, by its metabolite norketobemidone.<ref>Ebert B, Thorkildsen C, Andersen S, Christrup LL, Hjeds H (September 1998). "Opioid analgesics as noncompetitive N-methyl-D-aspartate (NMDA) antagonists". ''Biochemical Pharmacology''. '''56''' (5): 553–9. doi:10.1016/S0006-2952(98)00088-4. <nowiki>PMID 9783723</nowiki>.</ref> | |||
It has high abuse potential comparable to that of [[morphine]]. Chronic use is associated with psychological dependence and addiction. It is highly advised to use harm reduction practices if using this substance. | |||
==History and culture== | ==History and culture== | ||
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The synthesis occurs by alkylating (3-methoxyphenyl)acetonitrile with bis(2-chloroethyl)methylamine, followed by a reaction with ethylmagnesium bromide, and finally O-demethylation with hydrobromic acid. | The synthesis occurs by alkylating (3-methoxyphenyl)acetonitrile with bis(2-chloroethyl)methylamine, followed by a reaction with ethylmagnesium bromide, and finally O-demethylation with hydrobromic acid. | ||
==Pharmacology== | ==Pharmacology== | ||
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The elimination half-life of ketobemidone is 2 to 2.5 hours for both intravenous and oral administration.<ref name=":0" /> Analgesia after 5-10 mg orally or 5-7.5 mg intravenously lasts 3–5 hours. Ketobemidone is also available in preparations with a spasmolytic, which can improve the analgesia. | The elimination half-life of ketobemidone is 2 to 2.5 hours for both intravenous and oral administration.<ref name=":0" /> Analgesia after 5-10 mg orally or 5-7.5 mg intravenously lasts 3–5 hours. Ketobemidone is also available in preparations with a spasmolytic, which can improve the analgesia. | ||
==Subjective effects== | ==Subjective effects== | ||
{{effectStub}}{{Preamble/SubjectiveEffects}} | {{effectStub}} | ||
{{Preamble/SubjectiveEffects}} | |||
{{effects/base | {{effects/base | ||
|{{effects/physical| | |||
{{effects/physical| | |||
*'''[[Effect::Sedation]]''' | *'''[[Effect::Sedation]]''' | ||
*'''[[Effect::Dizziness]]''' | *'''[[Effect::Dizziness]]''' | ||
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*'''[[Effect::Pain relief]]''' | *'''[[Effect::Pain relief]]''' | ||
*'''[[Effect::Pupil constriction]]''' | *'''[[Effect::Pupil constriction]]''' | ||
*'''[[Effect::Itchiness]]''' | |||
*'''[[Effect::Respiratory depression]]''' | *'''[[Effect::Respiratory depression]]''' | ||
*'''[[Effect::Decreased blood pressure]]''' | *'''[[Effect::Decreased blood pressure]]''' | ||
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}} | }} | ||
{{effects/cognitive| | |{{effects/cognitive| | ||
*'''[[Effect::Cognitive euphoria]]''' | *'''[[Effect::Cognitive euphoria]]''' | ||
*'''[[Effect::Anxiety suppression]]''' | *'''[[Effect::Anxiety suppression]]''' | ||
*'''[[Effect::Confusion]]''' | *'''[[Effect::Confusion]]''' | ||
*'''[[Effect::Irritability]]''' - While opioids are well known for their ability to improve mood, they can also have the paradoxical effect of increasing the user's sensitivity to irritable stimuli. This can manifest as aloofness and sudden outbursts of anger and aggression (colloquially known as "opiate rage"). It appears to occur more frequently during the comedown of the experience and/or with heavy use. | *'''[[Effect::Irritability]]''' - While opioids are well known for their ability to improve mood, they can also have the paradoxical effect of increasing the user's sensitivity to irritable stimuli. This can manifest as aloofness and sudden outbursts of anger and aggression (colloquially known as "opiate rage"). It appears to occur more frequently during the comedown of the experience and/or with heavy use. | ||
}} | |||
{{effects/disconnective| | |||
Ketobemidone is thought to have disconnective effects due to its affinity for the [[NMDA_receptor_antagonist|NMDA]] receptor. | |||
*'''[[Effect::Cognitive disconnection]]''' | |||
*'''[[Effect::Physical disconnection]]''' | |||
}} | }} | ||
{{effects/visual| | {{effects/visual| | ||
====Suppressions==== | ====Suppressions==== | ||
*'''[[Effect::Double vision]]''' - At high doses, the eyes unfocus and re-focus uncontrollably. This creates a blurred effect and double vision that is present no matter where one focuses their eyes. This can be so intense it becomes impossible to read or drive. | *'''[[Effect::Double vision]]''' - At high doses, the eyes unfocus and re-focus uncontrollably. This creates a blurred effect and double vision that is present no matter where one focuses their eyes. This can be so intense it becomes impossible to read or drive. | ||
*'''[[Effect::Acuity suppression]]''' | *'''[[Effect::Acuity suppression]]''' | ||
====Hallucinatory States==== | ====Hallucinatory States==== | ||
*'''[[Effect::Internal hallucination]]''' - One may experience a state of semi-consciousness and [[hypnagogia]] during heavy dosage nodding which results in dream-like states and up to level 3 [[Lucid_dreaming#Internally_sourced_sensory_input|imagery]]. This is often accompanied by ill-defined [[geometry]]. | *'''[[Effect::Internal hallucination]]''' - One may experience a state of semi-consciousness and [[hypnagogia]] during heavy dosage nodding which results in dream-like states and up to level 3 [[Lucid_dreaming#Internally_sourced_sensory_input|imagery]]. This is often accompanied by ill-defined [[geometry]]. | ||
}} | |||
}} | }} | ||
}} | |||
===Experience reports=== | |||
Anecdotal reports which describe the effects of this compound within our [[experience index]] include: | |||
{{#ask: [[Category:Ketobemidone]][[Category:Experience]]|format=ul|Columns=1}} | |||
Additional experience reports can be found here: | |||
*[https://www.erowid.org/experiences/subs/exp_Ketobemidone.shtml Erowid Experience Vaults: Ketobemidone] | |||
==Toxicity and harm potential== | ==Toxicity and harm potential== | ||
{{toxicityStub}} | |||
=== | ===Dependence and abuse potential=== | ||
===Dangerous interactions=== | ===Dangerous interactions=== | ||
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==Legal status== | ==Legal status== | ||
{{legalStub}} | |||
*'''Australia:''' S9 (Prohibited substance) | *'''Australia:''' S9 (Prohibited substance).{{citation needed}} | ||
*'''Canada:''' Schedule I | *'''Canada:''' Schedule I.{{citation needed}} | ||
*'''Germany:''' Anlage II (Authorized trade only, not prescriptible) | *'''Germany:''' Anlage II (Authorized trade only, not prescriptible).{{citation needed}} | ||
*'''United States:''' Schedule I | *'''United States:''' Ketobemidone is a Schedule I substance.{{citation needed}} | ||
*'''European Union:''' | *'''European Union:''' Available by prescription only<ref>https://www.ema.europa.eu/en/documents/psusa/ketobemidone-list-nationally-authorised-medicinal-products-psusa/0001807/202005_en.pdf</ref> | ||
==See also== | ==See also== | ||