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Talk:Clozapine: Difference between revisions
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{{decree|type= | {{decree|type=notice|message=This article is in the 'Talk' namespace because it is an unfinished draft. This section is used to host drafts for unpublished articles as well as discussions for published ones. If you'd like to use this area to discuss this draft, please do so in the 'Discussion' section at the very bottom of the page. This notice will be removed once this draft has been approved for publication by an administrator.}} | ||
{{decree|type=style|message=Please help by contributing so that this article can be published. It would be appreciated if the substancebox was verified and the references at the bottom were located and formatted. --[[User:Corticosteroid|Corticosteroid]] ([[User talk:Corticosteroid|talk]]) 02:56, 5 October 2017 (CEST)}} | |||
{{headerpanel|{{ | {{headerpanel|{{approval}}}} | ||
{{SummarySheet}} | {{SummarySheet}} | ||
{{SubstanceBox/Clozapine}} | {{SubstanceBox/Clozapine}} | ||
[[File:FazaClo and Clozaril 100 mg each side by side.png|400px|thumbnail|right|FazaClo and Clozaril 100 mg tablets.]] | |||
'''Clozapine''' | '''Clozapine''', sold '''Clozaril''' and '''FazaClo''', is an [[antipsychotic|atypical antipsychotic]] substance of the tricyclic dibenzodiazepine chemical class that produces antipsychotic, hypnotic, and dulling effects when administered. It is used for treatment-resistant schizophrenia and is considered to be a "drug of last resort," reserved for when all other agents have failed.<ref> Novartis Corporation, Prescribing Guide For Clozapine (https://www.accessdata.fda.gov/drugsatfda_docs/label/2010/019758s062lbl.pdf)</ref> It is also used for schizoaffective disorder, a similar condition. FazaClo is an orally disintegrating tablet. <ref>Jazz Pharmaceuticals (2017) FazaClo Highlights of Prescribing Information</ref> | ||
Clozapine may also be used to help reduce the risk of suicidal tendencies in people with schizophrenia or other disorders that can be similar, such as acute delirium, bipolar disorder, and extreme cases of anxiety.{{citation needed}} However, it is only approved for use (on-label) in treatment-resistant schizophrenia. Clozapine was first synthesized in 1958 by Wander AG, a Swiss pharmaceutical company, based on the structure of the tricyclic antidepressant imipramine. | |||
==Chemistry== | ==Chemistry== | ||
{{chemistry}} | {{chemistry}} | ||
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==Pharmacology== | ==Pharmacology== | ||
Clozapine is classified as and was the first atypical antipsychotic agent. It binds to several types of central nervous system receptors and displays a unique pharmacological profile. It is a [[serotonin]] antagonist, with strong binding to the 5-HT<sub>2A</sub> and 5-HT<sub>2C</sub> receptor subtypes. | Clozapine is classified as and was the first atypical [[antipsychotic]] agent. It binds to several types of central nervous system receptors and displays a unique pharmacological profile. It is a [[serotonin]] [[antagonist]], with strong binding to the 5-HT<sub>2A</sub> and 5-HT<sub>2C</sub> [[receptor]] subtypes.<ref name="Clozapine">Clozapine (PubMed.gov / NCBI) | https://www.ncbi.nlm.nih.gov/mesh/68003024</ref> Clozapine has clinically significant anticholinergic activity, and this activity may make clozapine one of the few, if any other antipsychotic agents to have very low induction rates of tardive dyskinesia.<ref>Lieberman, J., Johns, C., Cooper, T., Pollack, S., & Kane, J. (1989). Clozapine pharmacology and tardive dyskinesia. Psychopharmacology, 99(1), S54-S59.</ref> | ||
It also displays a strong affinity as an antagonist to several [[dopamine|dopaminergic]] receptors, but shows only weak antagonism at the dopamine D2 receptor, which is commonly thought to modulate neuroleptic activity. | It also displays a strong affinity as an [[antagonist]] to several [[dopamine|dopaminergic]] receptors, but shows only weak antagonism at the [[dopamine]] D2 [[receptor]], which is commonly thought to modulate neuroleptic activity.<ref name="Clozapine"/> | ||
[https://en.wikipedia.org/wiki/Agranulocytosis Agranulocytosis] (severely low white blood cell count) is a major adverse effect associated with the administration of this agent.<ref>Baldessarini, R. J., & Frankenburg, F. R. (1991). Clozapine: a novel antipsychotic agent. New England Journal of Medicine, 324(11), 746-754.</ref><ref>Smits, R. A., Lim, H. D., Stegink, B., Bakker, R. A., de Esch, I. J., & Leurs, R. (2006). Characterization of the histamine H4 receptor binding site. Part 1. Synthesis and pharmacological evaluation of dibenzodiazepine derivatives. Journal of medicinal chemistry, 49(15), 4512-4516.</ref> | [https://en.wikipedia.org/wiki/Agranulocytosis Agranulocytosis] (severely low white blood cell count) is a major adverse effect associated with the administration of this agent.<ref>Baldessarini, R. J., & Frankenburg, F. R. (1991). Clozapine: a novel antipsychotic agent. New England Journal of Medicine, 324(11), 746-754.</ref><ref>Smits, R. A., Lim, H. D., Stegink, B., Bakker, R. A., de Esch, I. J., & Leurs, R. (2006). Characterization of the histamine H4 receptor binding site. Part 1. Synthesis and pharmacological evaluation of dibenzodiazepine derivatives. Journal of medicinal chemistry, 49(15), 4512-4516.</ref> | ||
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|{{effects/physical| | |{{effects/physical| | ||
*'''[[Effect::Sedation]]''' | |||
*'''[[Effect::Itchiness]]''' | *'''[[Effect::Itchiness]]''' | ||
*'''[[Effect::Constipation]]''' | *'''[[Effect::Constipation]]''' | ||
*'''[[Effect::Tremors]]''' | *'''[[Effect::Tremors]]''' | ||
*'''[[Effect:: | *'''[[Effect::Salivation]]''' - Clozapine can cause hypersalivation, or "drooling." <ref>Chengappa, K. R., Pollock, B. G., Parepally, H., Levine, J., Kirshner, M. A., Brar, J. S., & Zoretich, R. A. (2000). Anticholinergic differences among patients receiving standard clinical doses of olanzapine or clozapine. Journal of clinical psychopharmacology, 20(3), 311-316.</ref> | ||
*'''[[Effect::Increased perspiration]]''' | *'''[[Effect::Increased perspiration]]''' | ||
*'''[[Effect::Perception of increased weight]]''' | *'''[[Effect::Perception of increased weight]]''' | ||
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*'''[[Effect::Seizure]]''' | *'''[[Effect::Seizure]]''' | ||
*'''[[Effect::Headaches]]''' | *'''[[Effect::Headaches]]''' | ||
*'''[[Effect::Increased heart rate]]''' - Clozapine's anticholinergic activity increases heart rate. | |||
*'''[[Effect::Motor control loss]]''' - This effect is usually mild. | |||
*'''[[Effect::Weight gain]]''' | |||
}} | }} | ||
|{{effects/cognitive| | |{{effects/cognitive| | ||
*'''[[Effect::Anxiety suppression]] & [[Effect::Anxiety]]''' - At theraputic doses, clozapine suppresses anxiety, but at higher dosages it may cause anxiety due to its anticholinergic activity. | |||
*'''[[Effect::Sleepiness]]''' | *'''[[Effect::Sleepiness]]''' | ||
*'''[[Effect::Delusions]]''' | *'''[[Effect::Delusions]]''' | ||
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*'''[[Effect::Confusion]]''' and '''[[Effect::Delirium|delirium]]''' | *'''[[Effect::Confusion]]''' and '''[[Effect::Delirium|delirium]]''' | ||
*'''[[Effect::Cognitive fatigue]]''' | *'''[[Effect::Cognitive fatigue]]''' | ||
*'''[[Effect::Emotion suppression]]''' | |||
*'''[[Effect::Cognitive euphoria]]''' - This effect is generally very mild and better described as a mood lift. It is rare. | |||
*'''[[Effect::Cognitive dysphoria]] | |||
}} | }} | ||
{{effects/visual| | {{effects/visual| | ||
*'''[[Effect::External hallucinations|Hallucinations]]''' | *'''[[Effect::External hallucinations|Hallucinations]]''' - These only occur in very high doses and as a result of clozapine's anticholinergic activity. | ||
}} | |||
{{effects/paradoxical| | |||
Paradoxical reactions to antipsychotics such as worsened psychosis, violent behavior, loss of impulse control, irritability, and suicidal behavior sometimes occur (although they are rare in the general population).{{citation needed}} | |||
}} | }} | ||
}} | }} | ||
===Experience reports=== | ===Experience reports=== | ||
There are currently {{#ask:[[Category:SUBSTANCE]][[Category:Experience]] | format=count}} experience reports which describe the effects of this substance in our [[experience index]]. | |||
{{#ask: [[Category: | {{#ask: [[Category:SUBSTANCE]][[Category:Experience]]|format=ul|Columns=1}} | ||
Additional experience reports can be found here: | Additional experience reports can be found here: | ||
* https://erowid.org/experiences/subs/exp_Clozapine_.shtml Erowid Experience Vaults: Clozapine] | * [https://erowid.org/experiences/subs/exp_Clozapine_.shtml Erowid Experience Vaults: Clozapine] | ||
==Toxicity and harm potential== | ==Toxicity and harm potential== | ||
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Clozapine can also cause NMS, or neuroleptic malignant syndrome. This reaction is rare, but serious and includes dysfunctions such as muscle rigidity, hyperthermia, paleness, psychomotor agitation, respiratory distress (tachypnea), among others.{{citation needed}} | Clozapine can also cause NMS, or neuroleptic malignant syndrome. This reaction is rare, but serious and includes dysfunctions such as muscle rigidity, hyperthermia, paleness, psychomotor agitation, respiratory distress (tachypnea), among others.{{citation needed}} | ||
== | ==Legal status== | ||
{{LegalStub}} | {{LegalStub}} | ||
*'''United States:''' Clozapine is not a controlled substance, but is a prescription-only medicine. Bloodwork for a condition called agranulocytosis is often done for safety before prescribing and sometimes while on the medication. | *'''United States:''' Clozapine is not a controlled substance, but is a prescription-only medicine. Bloodwork for a condition called agranulocytosis is often done for safety before prescribing and sometimes while on the medication. | ||
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*[[Quetiapine]] | *[[Quetiapine]] | ||
*[[Prochlorperazine]] | *[[Prochlorperazine]] | ||
==External links== | ==External links== | ||
*[https:// | *[https://en.wikipedia.org/wiki/Clozapine Clozapine (Wikipedia)] | ||
*[https:// | *[https://isomerdesign.com/PiHKAL/explore.php?id=9413 Clozapine (TiHKAL / Isomer Design)] | ||
*[https://www.drugs.com/clozapine.html Clozapine (Drugs.com)] | |||
== | ==Literature== | ||
format these fuckers correctly please. and where are the <ref> tags ele-mayo | format these fuckers correctly please. and where are the <ref> tags ele-mayo | ||
http://www.accessdata.fda.gov/drugsatfda_docs/appletter/2002/19758se1-047ltr.pdf | http://www.accessdata.fda.gov/drugsatfda_docs/appletter/2002/19758se1-047ltr.pdf | ||
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https://www.ncbi.nlm.nih.gov/mesh/68003024 | https://www.ncbi.nlm.nih.gov/mesh/68003024 | ||
==References== | |||
<references /> | |||
[[Category:Psychoactive substance]] | |||
[[Category:Psychoactive substance]] | [[Category:Proofread]] | ||