Talk:Clozapine

From PsychonautWiki
Jump to: navigation, search


Songbird-egg.svg

This article is a stub.

As such, it may contain incomplete or wrong information. You can help by expanding it.

Summary sheet: Clozapine
Clozapine
Clozapine.svg
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

WARNING: Always start with lower doses due to differences between individual body weight, tolerance, metabolism, and personal sensitivity. See responsible use section.



Oral
Dosage
Threshold 6.125 - 12.5 mg
Light 12.5 - 25 mg
Common 37.5 - 50 mg
Strong 50 - 100 mg
Heavy 100 mg +
Duration
Total - hours
Onset - minutes









DISCLAIMER: PW's dosage information is gathered from users and resources for educational purposes only. It is not a recommendation and should be verified with other sources for accuracy.

FazaClo and Clozaril 100 mg tablets.

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

Molecule.svg

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

Metacogghjgjvghnition.png
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.

The effects listed below are based upon the subjective effects index and personal experiences of PsychonautWiki contributors. These effects should be taken with a grain of salt and will rarely (if ever) occur all at once, but heavier doses will increase the chances of inducing a full range of effects. Likewise, adverse effects become much more likely on higher doses and may include serious injury or death.

Physical effects
Child.svg

Cognitive effects
User.svg

Visual effects
Eye.svg

Paradoxical effects
Paradox placeholder.svg


Experience reports

There are currently no anecdotal reports which describe the effects of this compound within 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]

Legality

Handcuffs-300px.png

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

References

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

  1. Novartis Corporation, Prescribing Guide For Clozapine (https://www.accessdata.fda.gov/drugsatfda_docs/label/2010/019758s062lbl.pdf)
  2. Jazz Pharmaceuticals (2017) FazaClo Highlights of Prescribing Information
  3. Baldessarini, R. J., & Frankenburg, F. R. (1991). Clozapine: a novel antipsychotic agent. New England Journal of Medicine, 324(11), 746-754.
  4. 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. 5.0 5.1 Clozapine (PubMed.gov / NCBI) | https://www.ncbi.nlm.nih.gov/mesh/68003024
  6. Lieberman, J., Johns, C., Cooper, T., Pollack, S., & Kane, J. (1989). Clozapine pharmacology and tardive dyskinesia. Psychopharmacology, 99(1), S54-S59.
  7. Baldessarini, R. J., & Frankenburg, F. R. (1991). Clozapine: a novel antipsychotic agent. New England Journal of Medicine, 324(11), 746-754.
  8. 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.
  9. 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.
  10. 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