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Opioids: Difference between revisions
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While opioid is a more general term for substances that act primarily on opioid receptors, including natural occurring alkaloids, synthetic substances and opioid peptides.<ref name=":17">{{Cite book|url=https://books.google.com/books?id=s8CXrbimviMC&pg=PA268|title=Pharmacology and Physiology for Anesthesia: Foundations and Clinical Application: Expert Consult - Online and Print|last=Hemmings|first=Hugh C.|last2=Egan|first2=Talmage D.|publisher=Elsevier Health Sciences|year=2013|isbn=1437716792|page=253|quote=Opiate is the older term classically used in pharmacology to mean a drug derived from opium. Opioid, a more modern term, is used to designate all substances, both natural and synthetic, that bind to opioid receptors (including antagonists).}}</ref> | While opioid is a more general term for substances that act primarily on opioid receptors, including natural occurring alkaloids, synthetic substances and opioid peptides.<ref name=":17">{{Cite book|url=https://books.google.com/books?id=s8CXrbimviMC&pg=PA268|title=Pharmacology and Physiology for Anesthesia: Foundations and Clinical Application: Expert Consult - Online and Print|last=Hemmings|first=Hugh C.|last2=Egan|first2=Talmage D.|publisher=Elsevier Health Sciences|year=2013|isbn=1437716792|page=253|quote=Opiate is the older term classically used in pharmacology to mean a drug derived from opium. Opioid, a more modern term, is used to designate all substances, both natural and synthetic, that bind to opioid receptors (including antagonists).}}</ref> | ||
Opioid dependence can develop with ongoing administration, leading to a withdrawal syndrome with abrupt discontinuation.<ref>Cammarano, W. B., Pittet, J. F., Weitz, S., Schlobohm, R. M., | Opioid dependence can develop with ongoing administration, leading to a withdrawal syndrome with abrupt discontinuation.<ref>{{cite journal | vauthors=((Cammarano, W. B.)), ((Pittet, J.-F.)), ((Weitz, S.)), ((Schlobohm, R. M.)), ((Marks, J. D.)) | journal=Critical Care Medicine | title=Acute withdrawal syndrome related to the administration of analgesic and sedative medications in adult intensive care unit patients: | volume=26 | issue=4 | pages=676–684 | date= April 1998 | url=http://journals.lww.com/00003246-199804000-00015 | issn=0090-3493 | doi=10.1097/00003246-199804000-00015}}</ref> Opioids are not only well known for their addictive properties, but also for their ability to produce a feeling of euphoria, motivating some to use opioids recreationally. | ||
==Chemistry== | ==Chemistry== | ||
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===Receptor types=== | ===Receptor types=== | ||
Opioids act on the three main classes of opioid receptor in the nervous system, μ, κ, δ (mu, kappa, and delta).<ref name="receptors">Opioid - Chapter 2: The Endogeneous Opioid Systems | Opioids act on the three main classes of opioid receptor in the nervous system, μ, κ, δ (mu, kappa, and delta).<ref name="receptors">Opioid - Chapter 2: The Endogeneous Opioid Systems | ||
(http://www.stoppain.org / Beth Israel Medical Center's Department of Pain Medicine and Palliative Care) | https://web.archive.org/web/20110719072413/http://www.stoppain.org/pcd/_pdf/OpioidChapter2.pdf</ref> Each opioid is measured by its [[agonist]]ic or [[antagonist]]ic effects towards the receptors, with the responses to the different receptor sub-types (e.g., μ1 and μ2) providing even more effects. Opioid receptors are found mainly within the brain, but also within the spinal cord and digestive tract.<ref>Opioid receptors in the gastrointestinal tract | (http://www.stoppain.org / Beth Israel Medical Center's Department of Pain Medicine and Palliative Care) | https://web.archive.org/web/20110719072413/http://www.stoppain.org/pcd/_pdf/OpioidChapter2.pdf</ref> Each opioid is measured by its [[agonist]]ic or [[antagonist]]ic effects towards the receptors, with the responses to the different receptor sub-types (e.g., μ1 and μ2) providing even more effects. Opioid receptors are found mainly within the brain, but also within the spinal cord and digestive tract.<ref>{{cite journal | vauthors=((Holzer, P.)) | journal=Regulatory peptides | title=Opioid receptors in the gastrointestinal tract | volume=155 | issue=1–3 | pages=11–17 | date=5 June 2009 | url=https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3163293/ | issn=0167-0115 | doi=10.1016/j.regpep.2009.03.012}}</ref> | ||
====='''Delta (δ)'''===== | ====='''Delta (δ)'''===== | ||
The delta receptor is responsible for the [[analgesia]], antidepressant and convulsant effects as well as physical dependence.<ref name="receptors" /> | The delta receptor is responsible for the [[analgesia]], antidepressant and convulsant effects as well as physical dependence.<ref name="receptors" /> | ||
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====='''Mu (μ)'''===== | ====='''Mu (μ)'''===== | ||
The mu receptor is responsible for [[analgesia]], physical dependence, [[respiratory depression]], [[euphoria]], and possible [[vasodilation]].<ref name="receptors" /> | The mu receptor is responsible for [[analgesia]], physical dependence, [[respiratory depression]], [[euphoria]], and possible [[vasodilation]].<ref name="receptors" /> | ||
Agonists of mu opioid receptors produce sedative, euphoric, and anxiolytic effects largely through the interaction of the mu receptors with serotonin, dopamine, and norepinephrine. Activation of mu receptors allows for the disinhibition of serotonin and dopamine neurons by blocking the inhibitory effects of GABA on serotonin and dopamine neurons, thus increasing activity and release of serotonin and dopamine.<ref>https://www.sciencedirect.com/science/article/abs/pii/S1043661818306145</ref> Mu receptors additionally inhibit the activity of norepinephrine neurons, leading to sedation, anxiolysis, and respiratory depression.<ref>https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3274960/</ref> | |||
====='''Nociceptin'''===== | ====='''Nociceptin'''===== | ||
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|{{effects/physical| | |{{effects/physical| | ||
*'''[[Sedation]]''' | *'''[[Stimulation]] or [[Sedation]]''' - At light doses, mu opioid agonists often produce mild to moderate stimulation due to enhancing dopamine and serotonin signaling, which gradually changes to sedation with higher doses due to inhibition of norepinephrine. Opioids with stronger activity at kappa and nociceptin opioid receptors such as [[fentanyl]] and [[morphine]] tend to be more sedating than opioids which primarily act on mu opioid receptors like [[kratom]] and [[tianeptine]] | ||
*'''[[Respiratory depression|Respiratory depression]]''' - At low to moderate doses, this effect results in the sensation that the breath is slowed down mildly to moderately, but does not cause noticeable impairment. At high doses and overdoses, opioid-induced respiratory depression can result in a shortness of breath, abnormal breathing patterns, semi-consciousness, or unconsciousness. Severe overdoses can result in a coma or death without immediate medical attention. | *'''[[Respiratory depression|Respiratory depression]]''' - At low to moderate doses, this effect results in the sensation that the breath is slowed down mildly to moderately, but does not cause noticeable impairment. At high doses and overdoses, opioid-induced respiratory depression can result in a shortness of breath, abnormal breathing patterns, semi-consciousness, or unconsciousness. Severe overdoses can result in a coma or death without immediate medical attention. | ||
*'''[[Pain relief]]''' | *'''[[Pain relief]]''' | ||
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}} | }} | ||
|{{effects/cognitive| | |{{effects/cognitive| | ||
*'''[[Cognitive euphoria | *'''[[Cognitive euphoria]]''' - This can be described as a powerful and overwhelming feeling of emotional bliss, contentment, and happiness. | ||
*'''[[ | *'''[[Motivation enhancement]]''' - Some opioids (such as [[kratom]]) are more stimulating than others and seem to enhance motivation. | ||
*'''[[ | *'''[[Anxiety suppression]]''' | ||
*'''[[Compulsive redosing]]''' | *'''[[Compulsive redosing]]''' | ||
*'''[[Dream potentiation]]''' | *'''[[Dream potentiation]]''' | ||
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*'''[[Tramadol]]''' | *'''[[Tramadol]]''' | ||
*'''[[Tianeptine]]''' | *'''[[Tianeptine]]''' | ||
*'''[[Tilidine]]''' | |||
*'''[[Pethidine]]''' (Meperidine) | *'''[[Pethidine]]''' (Meperidine) | ||
*'''[[O-Desmethyltramadol]]''' | *'''[[O-Desmethyltramadol]]''' | ||
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===Long term effects=== | ===Long term effects=== | ||
The long-term use of opioids causes hormonal imbalance in both men and women.<ref>The effect of opioid therapy on endocrine function. | The long-term use of opioids causes hormonal imbalance in both men and women.<ref>{{cite journal | vauthors=((Brennan, M. J.)) | journal=The American Journal of Medicine | title=The effect of opioid therapy on endocrine function | volume=126 | issue=3 Suppl 1 | pages=S12-18 | date= March 2013 | issn=1555-7162 | doi=10.1016/j.amjmed.2012.12.001}}</ref> In men, this opioid-induced androgen deficiency results in abnormally low levels of sex hormones, particularly testosterone.<ref>{{cite journal | vauthors=((Smith, H. S.)), ((Elliott, J. A.)) | journal=Pain Physician | title=Opioid-induced androgen deficiency (OPIAD) | volume=15 | issue=3 Suppl | pages=ES145-156 | date= July 2012 | issn=2150-1149}}</ref> | ||
This negative change in endocrine function in males can lead to: reduced libido, erectile dysfunction, fatigue, depression, reduced facial and body hair, decreased muscle mass, and weight gain. | This negative change in endocrine function in males can lead to: reduced libido, erectile dysfunction, fatigue, depression, reduced facial and body hair, decreased muscle mass, and weight gain. | ||
Another often observed long-term effect is hyperalgesia, an increase in the pain sensitivity of the person. This is specially seen in chronic pain patients on high dose opioid regimes. There is some evidence that NMDA antagonists like [[ketamine]] and opoids that are also weak NMDA antagonist such as [[methadone]], [[levorphanol]] and [[tramadol]] may help delay the onset of hyperalgesia or even revert it.<ref>A comprehensive review of opioid-induced hyperalgesia | Another often observed long-term effect is hyperalgesia, an increase in the pain sensitivity of the person. This is specially seen in chronic pain patients on high dose opioid regimes. There is some evidence that NMDA antagonists like [[ketamine]] and opoids that are also weak NMDA antagonist such as [[methadone]], [[levorphanol]] and [[tramadol]] may help delay the onset of hyperalgesia or even revert it.<ref>{{cite journal | vauthors=((Lee, M.)), ((Silverman, S. M.)), ((Hansen, H.)), ((Patel, V. B.)), ((Manchikanti, L.)) | journal=Pain Physician | title=A comprehensive review of opioid-induced hyperalgesia | volume=14 | issue=2 | pages=145–161 | date= April 2011 | issn=2150-1149}}</ref> | ||
It is strongly recommended that one use [[responsible drug use|harm reduction practices]] when using this class of substances. | It is strongly recommended that one use [[responsible drug use|harm reduction practices]] when using this class of substances. | ||
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Due to the highly euphoric nature of these substances, the recreational use and abuse of opioids has an extremely high rate of addiction and dependence. This is combined with a tolerance which builds up quickly, necessitates that the user take increasingly high dosages in order to get the same effects. | Due to the highly euphoric nature of these substances, the recreational use and abuse of opioids has an extremely high rate of addiction and dependence. This is combined with a tolerance which builds up quickly, necessitates that the user take increasingly high dosages in order to get the same effects. | ||
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., | 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>{{cite journal | vauthors=((Siegel, S.)), ((Hinson, R. E.)), ((Krank, M. D.)), ((McCully, J.)) | journal=Science | title=Heroin “Overdose” Death: Contribution of Drug-Associated Environmental Cues | volume=216 | issue=4544 | pages=436–437 | date=23 April 1982 | url=https://www.science.org/doi/10.1126/science.7200260 | issn=0036-8075 | doi=10.1126/science.7200260}}</ref> | ||
===Dangerous interactions=== | ===Dangerous interactions=== | ||
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*[https://en.wikipedia.org/wiki/Opioid Opioid (Wikipedia)] | *[https://en.wikipedia.org/wiki/Opioid Opioid (Wikipedia)] | ||
*[https://erowid.org/chemicals/opiates/opiates.shtml Opiates (Erowid Vault)] | *[https://erowid.org/chemicals/opiates/opiates.shtml Opiates (Erowid Vault)] | ||
* | *[https://en.wikipedia.org/wiki/List_of_benzimidazole_opioids List of benzimidazole opioids (Wikipedia)] | ||
==References== | ==References== | ||
<references /> | <references /> | ||
[[Category:Anaphrodisiac]] | |||
[[Category:Psychoactive class]] | [[Category:Psychoactive class]] | ||
[[Category:Opioid| ]] | [[Category:Opioid| ]] | ||
[[Category:Pharmacology]] | [[Category:Pharmacology]] | ||
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