Clozapine

Atypical Antipsychotic — NERVOUS SYSTEM

Key facts

Clozapine is an ofp drug in the Atypical Antipsychotic class catalogued in DrugCentral. It was first approved by the FDA in 1989. DrugCentral lists 87 molecular targets, including HRH1, H1F0 and Htr2c|Htr2a|Htr2b. Recorded indications include Suicidal Behavior in Schizoaffective Disorder, Suicidal Behavior in Schizophrenia and Treatment-Resistant Schizophrenia.

• Approval status: ofp (first approved 1989 by the FDA).
• Drug class: Atypical Antipsychotic.
• Molecular targets: HRH1, H1F0, Htr2c|Htr2a|Htr2b and Chrm1 (87 listed in DrugCentral).
• Indications: Suicidal Behavior in Schizoaffective Disorder, Suicidal Behavior in Schizophrenia and Treatment-Resistant Schizophrenia.
• ATC code: N05AH02 (Diazepines, oxazepines, thiazepines and oxepines).
• Molecular formula: C18H19ClN4; molecular weight 326.83 g/mol.

Indications & contraindications

Drug–disease relationships curated by DrugCentral (OMOP / SNOMED concepts).

Indications (3)

• Suicidal Behavior in Schizoaffective Disorder
• Suicidal Behavior in Schizophrenia
• Treatment-Resistant Schizophrenia

Off-label uses (2)

• Bipolar affective disorder, current episode manic
• Bipolar disorder in remission

Contraindications (47)

• Agranulocytosis
• Alcohol-induced psychosis
• Angle-closure glaucoma
• At risk for aspiration
• Benign prostatic hyperplasia
• Bone marrow depression
• Breastfeeding (mother)
• Central nervous system depression
• Cerebrovascular accident
• Cerebrovascular disease
• Coma
• Conduction disorder of the heart
• Constipation
• Decreased respiratory function
• Deep venous thrombosis
• Dehydration
• Diabetes mellitus
• Disease of liver
• Disorder of coronary artery
• Drug-induced neutropenia
• Eosinophil count raised
• Fecal impaction
• Gastrointestinal hypomotility
• Hyperglycemia
• Hyperlipidemia
• Leukopenia
• Liver function tests abnormal
• Low blood pressure
• Lowered convulsive threshold
• Metabolic syndrome X
• + 17 more

Mechanism & targets

• Established pharmacologic class: Atypical Antipsychotic

Molecular targets (87)

Target	Gene	Action	Activity
Histamine H1 receptor	HRH1	unknown	Ki 9.20
Histone H1.0	H1F0	unknown	Ki 9.00
Serotonin 2 (5-HT2) receptor	Htr2c|Htr2a|Htr2b	unknown	Ki 8.74
Muscarinic acetylcholine receptor M1	Chrm1	unknown	Ki 8.68
Histamine H1 receptor	Hrh1	unknown	Ki 8.54
Alpha-2C adrenergic receptor	ADRA2C	unknown	Ki 8.54
5-hydroxytryptamine receptor 2A	HTR2A	unknown	IC50 8.52
Alpha-1B adrenergic receptor	Adra1b	unknown	Ki 8.45
Histamine H1 receptor	HRH1	unknown	Ki 8.42
5-hydroxytryptamine receptor 6	Htr6	antagonist	Ki 8.40
5-hydroxytryptamine receptor 2A	HTR2A	antagonist	Ki 8.30
5-hydroxytryptamine receptor 2B	HTR2B	unknown	Ki 8.26
Histamine H4 receptor	HRH4	unknown	Ki 8.23
5-hydroxytryptamine receptor 2A	Htr2a	unknown	Ki 8.22
5-hydroxytryptamine receptor 7	Htr7	unknown	Ki 8.20
5-hydroxytryptamine receptor 1A	HTR1A	unknown	Ki 8.20
Muscarinic acetylcholine receptor M1	CHRM1	unknown	IC50 8.18
5-hydroxytryptamine receptor 2C	Htr2c	unknown	Ki 8.10
Alpha-1A adrenergic receptor	ADRA1A	unknown	Ki 8.10
5-hydroxytryptamine receptor 2C	HTR2C	unknown	Ki 8.05

Regulatory approvals (1)

Date	Agency	Marketed as	Applicant	Orphan
1989-09-26	FDA	—	NOVARTIS

ATC classification

ATC code	Therapeutic hierarchy
N05AH02	NERVOUS SYSTEM › PSYCHOLEPTICS › ANTIPSYCHOTICS › Diazepines, oxazepines, thiazepines and oxepines

Pharmacogenomics

Drug-label and guideline annotations from PharmGKB and CPIC.

• FDA label: CYP2D6 · Actionable PGx
• HCSC label

Reported adverse-event signals

Strongest FDA FAERS disproportionality signals (log-likelihood ratio). A signal is a statistical association in spontaneous reports, not proof that the drug causes the event.

MedDRA term	LLR
Neutropenia	34664.3
Hospitalisation	23557.5
Neutrophilia	10708.4
Neutrophil count increased	9929.1
Death	7601.4
White blood cell count increased	7535.1
Granulocytopenia	6658.7
Differential white blood cell count abnormal	5427.6
Antipsychotic drug level increased	5240.0
Psychotic disorder	4979.9
Mental impairment	4718.4
Treatment noncompliance	4685.0

Chemical structure

Full physicochemical, ADMET and 3D-structure analysis of Clozapine is on its molecule page.

• Molecular formula: C₁₈H₁₉ClN₄
• Molecular weight: 326.83 g/mol
• CAS number: 5786-21-0
• InChIKey: QZUDBNBUXVUHMW-UHFFFAOYSA-N
• PubChem CID: 135398737

CN1CCN(CC1)C1=NC2=CC(Cl)=CC=C2NC2=C1C=CC=C2

Frequently asked questions

Answers are generated from the structured data on this page, not written by hand.

What is Clozapine used for?

DrugCentral lists the following indications for Clozapine: Suicidal Behavior in Schizoaffective Disorder, Suicidal Behavior in Schizophrenia and Treatment-Resistant Schizophrenia.

How does Clozapine work?

Its molecular targets in DrugCentral include HRH1, H1F0, Htr2c|Htr2a|Htr2b and Chrm1.

When was Clozapine first approved?

Clozapine was first approved by the FDA in 1989.

What drug class does Clozapine belong to?

Clozapine is in the Atypical Antipsychotic class.

What is the chemical formula of Clozapine?

Clozapine has the molecular formula C18H19ClN4 and a molecular weight of 326.83 g/mol.

Sources

• DrugCentral drug card 722 — structure, indications, targets, approvals, pharmacologic classes (CC BY-SA 4.0)
• ChEMBL CHEMBL42 — compound record and bioactivity
• PubChem CID 135398737 — chemical identifiers
• DrugBank DB00363 — drug record
• FDA UNII J60AR2IKIC — substance identity
• DailyMed: FDA labels for Clozapine — current prescribing information (label search)
• UniProt P35367 (HRH1) — target protein
• UniProt P07305 (H1F0) — target protein
• UniProt P18825 (ADRA2C) — target protein
• UniProt P28223 (HTR2A) — target protein
• UniProt P41595 (HTR2B) — target protein
• UniProt Q9H3N8 (HRH4) — target protein
• FDA Adverse Event Reporting System (openFDA FAERS) — adverse-event signals, as aggregated by DrugCentral
• PharmGKB / CPIC — pharmacogenomic label annotations

How this page is built: methodology · editorial policy & corrections.