Talk:Clozapine
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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. --Corticosteroid (talk) 02:56, 5 October 2017 (CEST) |
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| Summary sheet: Clozapine |
| Clozapine | |||||||||||||||||||||||||
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| Chemical Nomenclature | |||||||||||||||||||||||||
| Common names | Clozaril, FazaClo | ||||||||||||||||||||||||
| Substitutive name | Clozapine | ||||||||||||||||||||||||
| Systematic name | 8-Chloro-11-(4-methylpiperazin-1-yl)-5H-dibenzo[b,e][1,4]diazepine | ||||||||||||||||||||||||
| Class Membership | |||||||||||||||||||||||||
| Psychoactive class | Antipsychotic | ||||||||||||||||||||||||
| Chemical class | Dibenzodiazepine | ||||||||||||||||||||||||
| Routes of Administration | |||||||||||||||||||||||||
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Clozapine, sold Clozaril and FazaClo, is an 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.[1] It is also used for schizoaffective disorder, a similar condition. FazaClo is an orally disintegrating tablet. [2]
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
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This chemistry section is incomplete. You can help by adding to it. |
Clozapine is a tricyclic dibenzodiazepine. Its main structure is of two benzene rings fused to a 1,3-diazepine ring, one benzene being chlorinated. [3][4]
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-HT2A and 5-HT2C receptor subtypes.[5] 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.[6]
It also displays a strong affinity as an antagonist to several dopaminergic receptors, but shows only weak antagonism at the dopamine D2 receptor, which is commonly thought to modulate neuroleptic activity.[5]
Agranulocytosis (severely low white blood cell count) is a major adverse effect associated with the administration of this agent.[7][8]
Subjective effects
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This subjective effects section is a stub. As such, it is still in progress and may contain incomplete or wrong information. You can help by expanding or correcting it. |
Disclaimer: The effects listed below cite the Subjective Effect Index (SEI), an open research literature based on anecdotal user reports and the personal analyses of PsychonautWiki contributors. As a result, they should be viewed with a healthy degree of skepticism.
It is also worth noting that these effects will not necessarily occur in a predictable or reliable manner, although higher doses are more liable to induce the full spectrum of effects. Likewise, adverse effects become increasingly likely with higher doses and may include addiction, severe injury, or death ☠.
Physical effects 
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- Sedation
- Itchiness
- Constipation
- Tremors
- Salivation - Clozapine can cause hypersalivation, or "drooling." [9]
- Increased perspiration
- Perception of increased weight
- Dehydration
- Acuity suppression
- Dizziness
- Seizure
- Headaches
- Increased heart rate - Clozapine's anticholinergic activity increases heart rate.
- Motor control loss - This effect is usually mild.
- Weight gain
Cognitive effects 
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- Anxiety suppression & Anxiety - At theraputic doses, clozapine suppresses anxiety, but at higher dosages it may cause anxiety due to its anticholinergic activity.
- Sleepiness
- Delusions
- Amnesia
- Irritability
- Confusion and delirium
- Cognitive fatigue
- Emotion suppression
- Cognitive euphoria - This effect is generally very mild and better described as a mood lift. It is rare.
- Cognitive dysphoria
Visual effects 
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- Hallucinations - These only occur in very high doses and as a result of clozapine's anticholinergic activity.
Paradoxical effects 
- 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
There are currently 0 experience reports which describe the effects of this substance in our experience index.
Additional experience reports can be found here:
Toxicity and harm potential
Clozapine is associated with a rare but potentially fatal effect called agranulocytosis (dangerously low white blood cell count).[10] Therefore, lower doses and self-monitoring for this condition are encouraged if taken outside of supervised medical context.
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
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This legality section is a stub. As such, it may contain incomplete or wrong information. You can help by expanding it. |
- 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.
- Australia: Clozapine is a schedule four substance, meaning it is a prescription-only medicine.
See also
External links
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
- ↑ Novartis Corporation, Prescribing Guide For Clozapine (https://www.accessdata.fda.gov/drugsatfda_docs/label/2010/019758s062lbl.pdf)
- ↑ Jazz Pharmaceuticals (2017) FazaClo Highlights of Prescribing Information
- ↑ Baldessarini, R. J., & Frankenburg, F. R. (1991). Clozapine: a novel antipsychotic agent. New England Journal of Medicine, 324(11), 746-754.
- ↑ 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.
- ↑ 5.0 5.1 Clozapine (PubMed.gov / NCBI) | https://www.ncbi.nlm.nih.gov/mesh/68003024
- ↑ Lieberman, J., Johns, C., Cooper, T., Pollack, S., & Kane, J. (1989). Clozapine pharmacology and tardive dyskinesia. Psychopharmacology, 99(1), S54-S59.
- ↑ Baldessarini, R. J., & Frankenburg, F. R. (1991). Clozapine: a novel antipsychotic agent. New England Journal of Medicine, 324(11), 746-754.
- ↑ 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.
- ↑ 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.
- ↑ 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