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{{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.]]
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'''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/Summary|Summary sheet: Clozapine]]''
 
Clozapine (trade name '''Clozaril''') is an antipsychotic medication that is used to treat severe schizophrenia. However, it only applies to those that have not responded to other medications (studies demonstrated that clozapine was more effective against treatment-resistant schizophrenia than other antipsychotics). Clozapine may also be used to help reduce the risk of suicidal tendencies in people with schizophrenia or similar disorders (Delirium, bipolar disorder, extreme cases of anxiety). Clozapine was first synthesized in 1958 by Wander AG, a Swiss pharmaceutical company, based on the chemical structure of the tricyclic antidepressant imipramine.  
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==
A tricylic dibenzodiazepine, classified as an atypical antipsychotic agent. It binds several types of central nervous system receptors, and displays a unique pharmacological profile. Clozapine is a serotonin antagonist, with strong binding to 5-HT 2A/2C receptor subtype. It also displays strong affinity to several dopaminergic receptors, but shows only weak antagonism at the dopamine D2 receptor, a receptor commonly thought to modulate neuroleptic activity. Agranulocytosis is a major adverse effect associated with administration of this agent.  
{{chemistry}}
Year introduced: 1991(1975)
Clozapine is a tricyclic dibenzodiazepine. Its main structure is of two benzene rings fused to a 1,3-diazepine ring, one benzene being chlorinated. <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>
===Physical effects===
 
==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.<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.<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>
 
==Subjective  effects==
{{effectStub}}
{{Preamble/SubjectiveEffects}}
{{effects/base
 
|{{effects/physical|
*'''[[Effect::Sedation]]'''
*'''[[Effect::Itchiness]]'''
*'''[[Effect::Itchiness]]'''
*'''[[Effect::Constipation]]'''
*'''[[Effect::Constipation]]'''
*'''[[Effect::Shaking ]]'''
*'''[[Effect::Tremors]]'''
*'''[[Effect::Drooling]]'''
*'''[[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]]'''
*'''[[Effect::Dehydration]]'''
*'''[[Effect::Dehydration]]'''
*'''[[Effect::Blurred Vision]]'''
*'''[[Effect::Acuity suppression]]'''
*'''[[Effect::Dizziness]]'''
*'''[[Effect::Dizziness]]'''
*'''[[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]]'''


===Cognitive effects===
 
}}
|{{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]]'''
*'''[[Effect::Hallucinations]]'''
*'''[[Effect::Amnesia]]'''
*'''[[Effect::Amnesia]]'''
*'''[[Effect::Agitation]]'''
*'''[[Effect::Irritability]]'''
*'''[[Effect::Confusion]]'''*
*'''[[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|
*'''[[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===
Anecdotal reports which describe the effects of this compound within our [[experience index]] include:
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:Clozapine]][[Category:Experience]]|format=ul|Columns=1}}
{{#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
* [https://erowid.org/experiences/subs/exp_Clozapine_.shtml Erowid Experience Vaults: Clozapine]
 
==Toxicity and harm potential==
Clozapine is associated with a rare but potentially fatal effect called agranulocytosis (dangerously low white blood cell count).<ref>Mebanga Ojong and Shari N. Allen (2013) Management and prevention of agranulocytosis in patients receiving clozapine. Mental Health Clinician: September 2013, Vol. 3, No. 3, pp. 139-143. https://doi.org/10.9740/mhc.n166825</ref> Therefore, lower doses and self-monitoring for this condition are encouraged if taken outside of supervised medical context.


==Legal issues==
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}}
*'''US:''' Special permission/perscription.  
*'''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.
*'''AUS:''' Schedule 4, prescription only.
*'''Australia:''' Clozapine is a schedule four substance, meaning it is a prescription-only medicine.  


==See also==
==See also==
* [[Responsible use]]
*[[Responsible use]]
* [[Antipsychotic]]
*[[Antipsychotic]]
*[[Delusions]]
*[[Delusions]]
*[[Quetiapine]]
*[[Quetiapine]]
*[[Prochlorperazine]]
*[[Prochlorperazine]]
==External links==
==External links==
*[https://www.drugs.com/clozapine.html (Drugs.com)]
*[https://en.wikipedia.org/wiki/Clozapine Clozapine (Wikipedia)]
*[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
http://www.accessdata.fda.gov/drugsatfda_docs/appletter/2002/19758se1-047ltr.pdf
https://www.ncbi.nlm.nih.gov/pubmedhealth/PMHT0009695/?report=details#side_effects
https://www.ncbi.nlm.nih.gov/mesh/68003024


==References==
==References==
# 1 - http://www.accessdata.fda.gov/drugsatfda_docs/appletter/2002/19758se1-047ltr.pdf
<references />
 
# 2 - https://www.ncbi.nlm.nih.gov/pubmedhealth/PMHT0009695/?report=details#side_effects


# 3 - https://www.ncbi.nlm.nih.gov/mesh/68003024
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