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clozapine

File:Clozapine.svg · Wikimedia Commons · See Wikimedia Commons

EntityQ221361· pop 38· linked from 2,889 articles

Also known as LEX123, HF-1854

Clozapine, sold under the brand name Clozaril among others, is a psychiatric medication and was the first atypical antipsychotic to be discovered. It is used primarily to treat people with schizophrenia and schizoaffective disorder who have had an inadequate response to two other antipsychotics, or who have been unable to tolerate other drugs due to extrapyramidal side effects. In the US, clozapine is also approved for use in people with recurrent suicidal behavior in people with schizophrenia or schizoaffective disorder. It is also used for the treatment of psychosis in Parkinson's disease.

Key facts

Drug.Watchedfields
changed
Drug.verifiedrevid
443538511
Drug.image
Clozapine.svg
Drug.image_class
skin-invert-image
Drug.width
200
Drug.alt
Skeletal formula of clozapine
Drug.image2
Clozapine_3d-ball_and_stick.png
Drug.image_class2
bg-transparent
Drug.width2
240
Drug.alt2
Stick-and-ball model of the clozapine molecule
Drug.tradename
Clozaril, others
Drug.MedlinePlus
a691001
Drug.DailyMedID
Clozapine
Drug.pregnancy_AU
C
Drug.routes_of_administration
By mouth, intramuscular
Drug.class
Atypical antipsychotic
Drug.ATC_prefix
N05
Drug.ATC_suffix
AH02

via Wikipedia infobox

Chemical data

Formula
C18H19ClN4
Molecular weight
326.8 g/mol
IUPAC name
3-chloro-6-(4-methylpiperazin-1-yl)-11H-benzo[b][1,4]benzodiazepine
SMILES
CN1CCN(CC1)C2=NC3=C(C=CC(=C3)Cl)NC4=CC=CC=C42
InChIKey
QZUDBNBUXVUHMW-UHFFFAOYSA-N
XLogP
3.1
Polar surface area
30.9 Ų
H-bond donors
1
H-bond acceptors
3
Formal charge
0

via PubChem

~44 min read

Encyclopedic overview

40 sections
Contents
  • Medical uses
  • Schizophrenia
  • Personality disorder
  • Bipolar disorder
  • Administration
  • Initiation
  • Enforced
  • Treatment optimization
  • Blood sampling
  • Benign ethnic neutropenia
  • Adverse effects
  • Mortality
  • Neutropenia and agranulocytosis
  • Pharmacogenetics
  • Cost-effectiveness monitoring
  • Restarting (rechallenge)
  • Cardiac toxicity
  • Gastrointestinal hypomotility
  • Hypersalivation
  • Central nervous system
  • Urinary incontinence
  • Withdrawal
  • Weight gain and diabetes
  • Pneumonia
  • Overdose
  • Drug interactions
  • Pharmacology
  • Pharmacodynamics
  • Pharmacokinetics
  • Chemistry
  • History
  • Society and culture
  • Underuse
  • Racial disparity
  • Economics
  • Brand names
  • Research
  • Severe personality disorders
  • References
  • Further reading

Clozapine, sold under the brand name Clozaril among others, is a psychiatric medication and was the first atypical antipsychotic to be discovered. It is used primarily to treat people with schizophrenia and schizoaffective disorder who have had an inadequate response to two other antipsychotics, or who have been unable to tolerate other drugs due to extrapyramidal side effects. In the US, clozapine is also approved for use in people with recurrent suicidal behavior in people with schizophrenia or schizoaffective disorder. It is also used for the treatment of psychosis in Parkinson's disease.

Clozapine is recommended by multiple international treatment guidelines, after resistance to two other antipsychotic medications, and is the only treatment likely to result in improvement if two (or one) other antipsychotic has not had a satisfactory effect. Long term follow-up studies from Finland show significant improvements in terms of overall mortality including from suicide and all causes. Clozapine is on the World Health Organization's List of Essential Medicines. It is available as a generic medication. Common adverse effects include drowsiness, constipation, hypersalivation (increased saliva production), tachycardia, low blood pressure, blurred vision, significant weight gain, and dizziness. Clozapine is not normally associated with tardive dyskinesia and is recommended as the drug of choice when this is present, although some case reports describe clozapine-induced tardive dyskinesia. Serious adverse effects include agranulocytosis, seizures, myocarditis (inflammation of the heart), and hyperglycemia (high blood glucose levels). The use of clozapine may result rarely in clozapine-induced, gastric hypomotility syndrome, which may lead to bowel obstruction and death. The mechanism of action is not clear.

Excerpted from Wikipedia’s “clozapine” article, available under the CC BY-SA 4.0 licence.

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