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Talk:Clozapine

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Summary sheet: Clozapine
Clozapine
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 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.


Clozapine (trade names Clozaril and FazaClo) is an atypical 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). Therefore, it is a drug of last resort (DoLR).

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. However, its only approved (on-label) use is in treatment-resistant schizophrenia.[1] Clozapine was first synthesized in 1958 by Wander AG, a Swiss pharmaceutical company, based on the chemical structure of the tricyclic antidepressant imipramine.

Chemistry

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Clozapine is a tricyclic dibenzodiazepine. Its main structure is of two benzene rings fused to a 1,3-diazepine ring, one benzene being chlorinated.

Pharmacology

Cloazapine 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.

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.

Agranulocytosis (severely low white blood cell count) is a major adverse effect associated with the administration of this agent.

Subjective effects

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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 ☠.



Experience reports

Anecdotal reports which describe the effects of this compound within our experience index include:

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).[2] 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

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  • 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.
  • Australia: Clozapine is a schedule four substance, meaning it is a prescription-only medicine.

See also

References

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. 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