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Mirtazapine: Difference between revisions
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{{SummarySheet}} | {{SummarySheet}} | ||
{{SubstanceBox/Mirtazapine}} | {{SubstanceBox/Mirtazapine}} | ||
'''Mirtazapine''' (trade name '''Remeron''', among others) is an [[psychoactive class::antidepressant]] substance of the [[Chemical class::piperazinoazepine]] class. At high doses, it has been reported to act as an atypical [[psychedelic]] and [[sedative]]. It is classified as a noradrenergic and specific serotonergic antidepressant (NaSSA). | '''Mirtazapine''' (trade name '''Remeron''', among others) is an [[psychoactive class::antidepressant]] substance of the [[Chemical class::piperazinoazepine]] class. At high doses, it has been reported to act as an atypical [[psychedelic]] and [[sedative]]. It is classified as a noradrenergic and specific serotonergic antidepressant (NaSSA).<ref>Roland A. Carlstedt (14 December 2009). ''Handbook of Integrative Clinical Psychology, Psychiatry, and Behavioral Medicine: Perspectives, Practices, and Research''. Springer Publishing Company. p. 290. [[ISBN (identifier)|ISBN]] [[Special:BookSources/978-0-8261-1094-7|<bdi>978-0-8261-1094-7</bdi>]]. Retrieved 23 April 2012.</ref> | ||
Mirtazapine was developed in the Netherlands and introduced in the United States in 1996.<ref> "REMERON (mirtazapine) tablet, film coated [Organon Pharmaceuticals USA]". DailyMed. Organon Pharmaceuticals USA. October 2012. Retrieved 24 October 2013.</ref> Its patent expired in 2004 and generic versions have been widely available since.<ref name="Schatzberg">{{cite book | vauthors=((Schatzberg, A. F.)), ((Cole, J. O.)), ((DeBattista, C.)) | date= 2010 | title=Manual of clinical psychopharmacology | publisher=American Psychiatric Pub | volume=3 | edition=7th ed | isbn=9781585623778}}</ref> It is used primarily in the treatment of major depressive disorder and other mood disorders.<ref>{{cite journal | vauthors=((Gorman, J. M.)) | journal=The Journal of Clinical Psychiatry | title=Mirtazapine: clinical overview | volume=60 Suppl 17 | pages=9–13; discussion 46-48 | date= 1999 | issn=0160-6689}}</ref><ref>{{cite journal | journal=Expert Opinion on Pharmacotherapy | title=Review of the use of mirtazapine in the treatment of depression | url=https://informahealthcare.com/doi/abs/10.1517/14656566.2011.585459}}</ref> It has also been prescribed off-label for the treatment of | Mirtazapine was developed in the Netherlands and introduced in the United States in 1996.<ref> "REMERON (mirtazapine) tablet, film coated [Organon Pharmaceuticals USA]". DailyMed. Organon Pharmaceuticals USA. October 2012. Retrieved 24 October 2013.</ref> Its patent expired in 2004 and generic versions have been widely available since.<ref name="Schatzberg">{{cite book | vauthors=((Schatzberg, A. F.)), ((Cole, J. O.)), ((DeBattista, C.)) | date= 2010 | title=Manual of clinical psychopharmacology | publisher=American Psychiatric Pub | volume=3 | edition=7th ed | isbn=9781585623778}}</ref> It is used primarily in the treatment of major depressive disorder and other mood disorders.<ref>{{cite journal | vauthors=((Gorman, J. M.)) | journal=The Journal of Clinical Psychiatry | title=Mirtazapine: clinical overview | volume=60 Suppl 17 | pages=9–13; discussion 46-48 | date= 1999 | issn=0160-6689}}</ref><ref>{{cite journal | journal=Expert Opinion on Pharmacotherapy | title=Review of the use of mirtazapine in the treatment of depression | url=https://informahealthcare.com/doi/abs/10.1517/14656566.2011.585459}}</ref> It has also been prescribed off-label for the treatment of | ||
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==Pharmacology== | ==Pharmacology== | ||
Mirtazapine | Mirtazapine inhibits presynaptic serotonin (5-HT)-2 and alpha-2 adrenergic auto- and hetero-receptors, thereby increasing serotonergic and noradrenergic neurotransmission. The increased amount of 5-HT released interacts with postsynaptic 5-HT1 receptors, which may be relevant to the antidepressant effects of the drug. The affinity of mirtazapine for central alpha-2 adrenoreceptors is 10 times higher than for peripheral receptors, resulting in fewer peripheral effects related to increased blood pressure. Mirtazapine is an antagonist at postsynaptic 5-HT2A, 5-HT2C, and 5-HT3 receptors. The blockade of these receptors may result in a lower incidence of certain adverse effects (e.g., anxiety, insomnia, nausea) than occurs with antidepressants that do not antagonize these receptors. Mirtazapine significantly antagonizes histamine H1 receptors at low doses, and this activity is associated with sedation and appetite stimulation. Higher doses have a greater effect on norepinephrine release relative to antihistamine effects, which may offset the sedative potential and appetite stimulation observed at low doses. Mirtazapine has muscarinic antagonist properties, which may be associated with xerostomia, constipation, and other anticholinergic effects. Orthostatic hypotension is the result of the peripheral alpha-1 adrenergic antagonism of the drug. Mirtazapine does not have clinically significant receptor affinity for dopamine, 5-HT1A, or 5-HT1B, and has no effects on the central reuptake of either norepinephrine or serotonin.:<ref name="Fernandez2005">{{cite journal | vauthors=((Fernández, J.)), ((Alonso, J. M.)), ((Andrés, J. I.)), ((Cid, J. M.)), ((Díaz, A.)), ((Iturrino, L.)), ((Gil, P.)), ((Megens, A.)), ((Sipido, V. K.)), ((Trabanco, A. A.)) | journal=Journal of Medicinal Chemistry | title=Discovery of New Tetracyclic Tetrahydrofuran Derivatives as Potential Broad-Spectrum Psychotropic Agents | volume=48 | issue=6 | pages=1709–1712 | date=1 March 2005 | url=https://pubs.acs.org/doi/10.1021/jm049632c | issn=0022-2623 | doi=10.1021/jm049632c}}</ref><ref>{{cite journal | vauthors=((Boer, Th. de)), ((Maura, G.)), ((Raiteri, M.)), ((Vos, C. J. de)), ((Wieringa, J.)), ((Pinder, R. M.)) | journal=Neuropharmacology | title=Neurochemical and autonomic pharmacological profiles of the 6-aza-analogue of mianserin, org 3770 and its enantiomers | volume=27 | issue=4 | pages=399–408 | date=1 April 1988 | url=https://www.sciencedirect.com/science/article/pii/0028390888901499 | issn=0028-3908 | doi=10.1016/0028-3908(88)90149-9}}</ref> | ||
*[[serotonin|5-HT<sub>2A</sub> receptor]]<ref name="Fernandez2005" /> | *[[serotonin|5-HT<sub>2A</sub> receptor]]<ref name="Fernandez2005" /> | ||
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*'''[[Effect::Bronchodilation]]''' - This can cause swallowing to be extremely difficult and uncomfortable, as with some other [[deliriants|anticholinergics]] such as [[diphenhydramine]]. As with [[diphenhydramine]], it is most prominent during the onset phase of the experience and often fades away as the peak sets in. | *'''[[Effect::Bronchodilation]]''' - This can cause swallowing to be extremely difficult and uncomfortable, as with some other [[deliriants|anticholinergics]] such as [[diphenhydramine]]. As with [[diphenhydramine]], it is most prominent during the onset phase of the experience and often fades away as the peak sets in. | ||
*'''[[Effect::Muscle relaxation]]''' | *'''[[Effect::Muscle relaxation]]''' | ||
*'''[[Effect::Restless legs]]''' - This effect is considered slightly less apparent than it is with [[diphenhydramine]] | *'''[[Effect::Restless legs]]''' - This effect is considered slightly less apparent than it is with [[diphenhydramine]]. | ||
*'''[[Effect::Nausea suppression]]''' | *'''[[Effect::Nausea suppression]]''' | ||
}} | }} | ||
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*'''[[Effect::Increased music appreciation]]''' | *'''[[Effect::Increased music appreciation]]''' | ||
*'''[[Effect::Irritability]]''' | *'''[[Effect::Irritability]]''' | ||
*'''[[Effect::Emotion suppression]]''' - Mirtazapine | *'''[[Effect::Emotion suppression]]''' - Mirtazapine can have a dulling effect on emotions and it is sometimes difficult to express them. | ||
*'''[[Effect::Anxiety suppression]]''' - This effect is much stronger and more rapidly acting than that of SSRIs. | *'''[[Effect::Anxiety suppression]]''' - This effect is much stronger and more rapidly acting than that of SSRIs. | ||
}} | }} | ||
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*[http://www.erowid.org/pharms/mirtazapine/mirtazapine.shtml Mirtazapine (Erowid Vault)] | *[http://www.erowid.org/pharms/mirtazapine/mirtazapine.shtml Mirtazapine (Erowid Vault)] | ||
*[https://isomerdesign.com/PiHKAL/explore.php?domain=pk&id=9430 Mirtazapine (Isomer Design)] | *[https://isomerdesign.com/PiHKAL/explore.php?domain=pk&id=9430 Mirtazapine (Isomer Design)] | ||
*[http://www.drugs.com/mirtazapine.html Mirtazapine (Drugs.com)] | *[http://www.drugs.com/mirtazapine.html Mirtazapine (Drugs.com)] | ||