Pethidine: Difference between revisions

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[[Opioid]]s exert their effects by binding to and activating the [[Opioid#Mu_.28.CE.BC.29|μ-opioid]] [[receptor]]. This occurs because opioids structurally mimic endogenous endorphins which are naturally found within the body and also work upon the μ-opioid receptor set. The way in which opioids structurally mimic these natural endorphins results in their [[physical euphoria|euphoria]], [[pain relief]] and [[anxiolytic]] effects. This is because endorphins are responsible for reducing pain, causing sleepiness, and feelings of pleasure. They can be released in response to pain, strenuous exercise, orgasm, or general excitement. The bioavailability of orally administered pethidine can vary from 50% to around 60%.
[[Opioid]]s exert their effects by binding to and activating the [[Opioid#Mu_.28.CE.BC.29|μ-opioid]] [[receptor]]. This occurs because opioids structurally mimic endogenous endorphins which are naturally found within the body and also work upon the μ-opioid receptor set. The way in which opioids structurally mimic these natural endorphins results in their [[physical euphoria|euphoria]], [[pain relief]] and [[anxiolytic]] effects. This is because endorphins are responsible for reducing pain, causing sleepiness, and feelings of pleasure. They can be released in response to pain, strenuous exercise, orgasm, or general excitement. The bioavailability of orally administered pethidine can vary from 50% to around 60%.


Compared to traditional opioids, pethidine has a very unique pharmacological profile. In addition to being an opioid, pethidine is also a muscarinic [[acetylcholine]] [[receptor]] [[antagonist]]. Pethidine is also a [[dopamine]] [[reuptake inhibitor]] and [[norepinephrine]] reuptake inhibitor. Pethidine is a κ-opioid agonist and its metabolite norpethidine is also an extremely powerful [[serotonin]] reuptake inhibitor.<ref> Meperidine: A Critical Review | https://www.researchgate.net/publication/11575123_Meperidine_A_Critical_Review</ref>
Compared to traditional opioids, pethidine has a very unique pharmacological profile. In addition to being an opioid, pethidine is also a muscarinic [[acetylcholine]] [[receptor]] [[antagonist]]. Pethidine is also a [[dopamine]] [[reuptake inhibitor]] and [[norepinephrine]] reuptake inhibitor. Pethidine is a κ-opioid agonist and its metabolite norpethidine is also an extremely powerful [[serotonin]] reuptake inhibitor.<ref>Meperidine: A Critical Review | https://www.researchgate.net/publication/11575123_Meperidine_A_Critical_Review</ref>


==Subjective effects==
==Subjective effects==
{{Preamble/SubjectiveEffects}} Many users note that they find pethidine just as, or more euphoric than [[oxycodone]].<ref> Subjective, Psychomotor, and Physiological Effects of Cumulative Doses of Opioid μ Agonists in Healthy Volunteers | http://jpet.aspetjournals.org/content/289/3/1454.long </ref>
{{Preamble/SubjectiveEffects}} Many users note that they find pethidine just as, or more euphoric than [[oxycodone]].<ref>Subjective, Psychomotor, and Physiological Effects of Cumulative Doses of Opioid μ Agonists in Healthy Volunteers | http://jpet.aspetjournals.org/content/289/3/1454.long </ref>
{{effects/base
{{effects/base
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Pethidine has a [[Toxicity::high toxicity]] relative to dose. 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]]]] and generally has a wider range of substances which it is [[pethidine#Dangerous interactions|dangerous to combine with]] in comparison to other opioids.  
Pethidine has a [[Toxicity::high toxicity]] relative to dose. 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]]]] and generally has a wider range of substances which it is [[pethidine#Dangerous interactions|dangerous to combine with]] in comparison to other opioids.  


One of pethdine's metabolites, norpethidine has little to no opioid action, but is known to cause seizures. Pethidine should not be taken during [[Benzodiazepine#Discontinuation|benzodiazepine withdrawals]] as this can potentially cause [[seizure]]s. In 1984, Libby Zion, a teenager was brought to the emergency room due to a "flu-like" ailment. She was previously prescribed and taking phenelzine, a [[MAOI |monoamine oxidase inhibitor]], which in combination caused fatal serotonin syndrome.<ref> Serotonin Syndrome and the Libby Zion Affair | http://epmonthly.com/article/serotonin-syndrome-and-the-libby-zion-affair/ </ref>
One of pethdine's metabolites, norpethidine has little to no opioid action, but is known to cause seizures. Pethidine should not be taken during [[Benzodiazepine#Discontinuation|benzodiazepine withdrawals]] as this can potentially cause [[seizure]]s. In 1984, Libby Zion, a teenager was brought to the emergency room due to a "flu-like" ailment. She was previously prescribed and taking phenelzine, a [[MAOI |monoamine oxidase inhibitor]], which in combination caused fatal serotonin syndrome.<ref>Serotonin Syndrome and the Libby Zion Affair | http://epmonthly.com/article/serotonin-syndrome-and-the-libby-zion-affair/ </ref>


It is strongly recommended that one use [[responsible drug use|harm reduction practices]] when using this drug.
It is strongly recommended that one use [[responsible drug use|harm reduction practices]] when using this drug.
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==Legal issues==
==Legal issues==
{{LegalStub}}
{{LegalStub}}
*'''Germany:''' Pethidine is a controlled substance under Anlage III of the BtMG. It can only be prescribed on a narcotic prescription form.<ref>http://www.gesetze-im-internet.de/btmg_1981/anlage_iii.html</ref>
*'''United States:''' Pethidine is a Schedule II Controlled Substance.<ref>DEA Controlled Substances | https://www.deadiversion.usdoj.gov/schedules/orangebook/e_cs_sched.pdf</ref>
*'''United States:''' Pethidine is a Schedule II Controlled Substance.<ref>DEA Controlled Substances | https://www.deadiversion.usdoj.gov/schedules/orangebook/e_cs_sched.pdf</ref>
*'''United Kingdom:''' Pethidine is a Class A, Schedule 2 drug in the United Kingdom.<ref>UK Controlled Drugs | https://www.gov.uk/government/publications/controlled-drugs-list--2/list-of-most-commonly-encountered-drugs-currently-controlled-under-the-misuse-of-drugs-legislation</ref>
*'''United Kingdom:''' Pethidine is a Class A, Schedule 2 drug in the United Kingdom.<ref>UK Controlled Drugs | https://www.gov.uk/government/publications/controlled-drugs-list--2/list-of-most-commonly-encountered-drugs-currently-controlled-under-the-misuse-of-drugs-legislation</ref>
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==References==
==References==
<references />
<references />
[[Category:Substance]][[Category:Psychoactive substance]][[Category:Depressant]][[Category:Opioid]]
[[Category:Substance]]
[[Category:Psychoactive substance]]
[[Category:Depressant]]
[[Category:Opioid]]