U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

Details

Stereochemistry ACHIRAL
Molecular Formula C18H19ClN4
Molecular Weight 326.8239
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of CLOZAPINE

SMILES

CN1CCN(CC1)C2=Nc3cc(ccc3Nc4ccccc42)Cl

InChI

InChIKey=QZUDBNBUXVUHMW-UHFFFAOYSA-N
InChI=1S/C18H19ClN4/c1-22-8-10-23(11-9-22)18-14-4-2-3-5-15(14)20-16-7-6-13(19)12-17(16)21-18/h2-7,12,20H,8-11H2,1H3

HIDE SMILES / InChI

Description
Curator's Comment:: description was created based on several sources, including https://www.ncbi.nlm.nih.gov/pubmed/10372606

Clozapine was discovered in 1958 by an anesthetist and now it is used for the treatment of schizophrenia. Although the exact mechanism of its action is unknown, the effect of clozapine on schizophrenia is associated with inhibition of dopamine D2 and serotonin 2A receptors.

CNS Activity

Approval Year

1989
116
Targets

Targets

Primary TargetPharmacologyConditionPotency
Antagonist
2575
 160.0 nM [Ki]
Antagonist
2575
 5.4 nM [Ki]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Approved
8043
CLOZARIL

Approved Use

Clozaril is an atypical antipsychotic indicated for: Treatment-resistant schizophrenia.

Launch Date

6.2277118E11
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
98 nM
EXPERIMENT
https://www.ncbi.nlm.nih.gov/pubmed/10606838
12.5 mg single, oral
dose: 12.5 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
CLOZAPINE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
319 ng/mL
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/019758s073lbl.pdf
100 mg 2 times / day steady-state, oral
dose: 100 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
CLOZAPINE plasma
Homo sapiens
population: UNKNOWN
age: UNKNOWN
sex: FEMALE / MALE
food status: UNKNOWN
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
1348 nM × h
EXPERIMENT
https://www.ncbi.nlm.nih.gov/pubmed/10606838
12.5 mg single, oral
dose: 12.5 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
CLOZAPINE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
18.6 h
EXPERIMENT
https://www.ncbi.nlm.nih.gov/pubmed/10606838
12.5 mg single, oral
dose: 12.5 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
CLOZAPINE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
12 h
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/019758s073lbl.pdf
100 mg 2 times / day steady-state, oral
dose: 100 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
CLOZAPINE plasma
Homo sapiens
population: UNKNOWN
age: UNKNOWN
sex: FEMALE / MALE
food status: UNKNOWN
Funbound

Funbound

ValueDoseCo-administeredAnalytePopulation
3%
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/019758s073lbl.pdf
100 mg 2 times / day steady-state, oral
dose: 100 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
CLOZAPINE plasma
Homo sapiens
population: UNKNOWN
age: UNKNOWN
sex: FEMALE / MALE
food status: UNKNOWN
Doses

Doses

DosePopulationAdverse events​
289 mg 1 times / day multiple, oral (mean)
Recommended
Dose: 289 mg, 1 times / day
Route: oral
Route: multiple
Dose: 289 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/10831480/
unhealthy, 41
n = 22
Health Status: unhealthy
Condition: refractory psychotic mania
Age Group: 41
Sex: M+F
Population Size: 22
Sources:
https://pubmed.ncbi.nlm.nih.gov/10831480/
Other AEs: Sedation, Salivation...
Other AEs:
Sedation (14 patients)
Salivation (6 patients)
Constipation (6 patients)
Nausea and vomiting (5 patients)
Dizziness (4 patients)
Fever (4 patients)
Sources:
https://pubmed.ncbi.nlm.nih.gov/10831480/
296 mg 1 times / day multiple, oral (mean)
Recommended
Dose: 296 mg, 1 times / day
Route: oral
Route: multiple
Dose: 296 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/20586532/
unhealthy, 74.2 years (range: 65-89 years)
n = 75
Health Status: unhealthy
Condition: schizophrenia | schizoaffective disorder | Parkinson’ s disease with psychotic symptoms | bipolar disorder | acquired brain injury
Age Group: 74.2 years (range: 65-89 years)
Sex: M+F
Population Size: 75
Sources:
https://pubmed.ncbi.nlm.nih.gov/20586532/
Disc. AE: Orthostatic hypotension, Sedation...
Other AEs: Sedation, Hypersalivation...
AEs leading to
discontinuation/dose reduction:
Orthostatic hypotension (13 patients)
Sedation (1 patient)
Dysphagia (1 patient)
Fever (2 patients)
Tachycardia (2 patients)
Myocarditis (1 patient)
Leukopenia (3 patients)
Parkinsonism (1 patient)
Myocardial infarction (3 patients)
Ataxia (1 patient)
Cardiomyopathy (1 patient)
Other AEs:
Sedation (28 patients)
Hypersalivation (25 patients)
Constipation (16 patients)
Weight gain (8 patients)
Leukopenia (4 patients)
Tachycardia (3 patients)
Leukopenia (2 patients)
Seizure (2 patients)
Dysphagia (1 patient)
Fever (1 patient)
Fatigue (1 patient)
Sources:
https://pubmed.ncbi.nlm.nih.gov/20586532/
450 mg 1 times / day multiple, oral
Recommended
Dose: 450 mg, 1 times / day
Route: oral
Route: multiple
Dose: 450 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/14971863/
unhealthy, adult
n = 10
Health Status: unhealthy
Condition: schizophrenia, treatment-resistant
Age Group: adult
Sex: M+F
Population Size: 10
Sources:
https://pubmed.ncbi.nlm.nih.gov/14971863/
Other AEs: Dry mouth, Urinary hesitancy...
Other AEs:
Dry mouth (20%)
Urinary hesitancy (10%)
Constipation (60%)
Nausea (60%)
Dyspepsia (70%)
Headache (40%)
Somnolence (100%)
Lethargy (90%)
Myoclonus (30%)
Stuttering (20%)
Sialorrhea (80%)
Sweating (50%)
Urinary frequency (40%)
Dysphagia (20%)
Orthostatic hypotension (10%)
Dizziness (60%)
Increased appetite (50%)
Sources:
https://pubmed.ncbi.nlm.nih.gov/14971863/
900 mg 1 times / day multiple, oral (max)
Recommended
Dose: 900 mg, 1 times / day
Route: oral
Route: multiple
Dose: 900 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/3046553/
unhealthy, adult
n = 126
Health Status: unhealthy
Condition: schizophrenia, treatment-resistant
Age Group: adult
Sex: M+F
Population Size: 126
Sources:
https://pubmed.ncbi.nlm.nih.gov/3046553/
Other AEs: Drowsiness, Tachycardia...
Other AEs:
Drowsiness (21%)
Tachycardia (17%)
Constipation (16%)
Dizziness (14%)
Hypotension (13%)
Hyperthermia (13%)
Salivation (13%)
Hypertension (12%)
Headache (10%)
Nausea and vomiting (10%)
Dry mouth (5%)
Sources:
https://pubmed.ncbi.nlm.nih.gov/3046553/
AEs

AEs

AESignificanceDosePopulation
Sedation 14 patients
289 mg 1 times / day multiple, oral (mean)
Recommended
Dose: 289 mg, 1 times / day
Route: oral
Route: multiple
Dose: 289 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/10831480/
unhealthy, 41
n = 22
Health Status: unhealthy
Condition: refractory psychotic mania
Age Group: 41
Sex: M+F
Population Size: 22
Sources:
https://pubmed.ncbi.nlm.nih.gov/10831480/
Dizziness 4 patients
289 mg 1 times / day multiple, oral (mean)
Recommended
Dose: 289 mg, 1 times / day
Route: oral
Route: multiple
Dose: 289 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/10831480/
unhealthy, 41
n = 22
Health Status: unhealthy
Condition: refractory psychotic mania
Age Group: 41
Sex: M+F
Population Size: 22
Sources:
https://pubmed.ncbi.nlm.nih.gov/10831480/
Fever 4 patients
289 mg 1 times / day multiple, oral (mean)
Recommended
Dose: 289 mg, 1 times / day
Route: oral
Route: multiple
Dose: 289 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/10831480/
unhealthy, 41
n = 22
Health Status: unhealthy
Condition: refractory psychotic mania
Age Group: 41
Sex: M+F
Population Size: 22
Sources:
https://pubmed.ncbi.nlm.nih.gov/10831480/
Nausea and vomiting 5 patients
289 mg 1 times / day multiple, oral (mean)
Recommended
Dose: 289 mg, 1 times / day
Route: oral
Route: multiple
Dose: 289 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/10831480/
unhealthy, 41
n = 22
Health Status: unhealthy
Condition: refractory psychotic mania
Age Group: 41
Sex: M+F
Population Size: 22
Sources:
https://pubmed.ncbi.nlm.nih.gov/10831480/
Constipation 6 patients
289 mg 1 times / day multiple, oral (mean)
Recommended
Dose: 289 mg, 1 times / day
Route: oral
Route: multiple
Dose: 289 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/10831480/
unhealthy, 41
n = 22
Health Status: unhealthy
Condition: refractory psychotic mania
Age Group: 41
Sex: M+F
Population Size: 22
Sources:
https://pubmed.ncbi.nlm.nih.gov/10831480/
Salivation 6 patients
289 mg 1 times / day multiple, oral (mean)
Recommended
Dose: 289 mg, 1 times / day
Route: oral
Route: multiple
Dose: 289 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/10831480/
unhealthy, 41
n = 22
Health Status: unhealthy
Condition: refractory psychotic mania
Age Group: 41
Sex: M+F
Population Size: 22
Sources:
https://pubmed.ncbi.nlm.nih.gov/10831480/
Dysphagia 1 patient
296 mg 1 times / day multiple, oral (mean)
Recommended
Dose: 296 mg, 1 times / day
Route: oral
Route: multiple
Dose: 296 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/20586532/
unhealthy, 74.2 years (range: 65-89 years)
n = 75
Health Status: unhealthy
Condition: schizophrenia | schizoaffective disorder | Parkinson’ s disease with psychotic symptoms | bipolar disorder | acquired brain injury
Age Group: 74.2 years (range: 65-89 years)
Sex: M+F
Population Size: 75
Sources:
https://pubmed.ncbi.nlm.nih.gov/20586532/
Fatigue 1 patient
296 mg 1 times / day multiple, oral (mean)
Recommended
Dose: 296 mg, 1 times / day
Route: oral
Route: multiple
Dose: 296 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/20586532/
unhealthy, 74.2 years (range: 65-89 years)
n = 75
Health Status: unhealthy
Condition: schizophrenia | schizoaffective disorder | Parkinson’ s disease with psychotic symptoms | bipolar disorder | acquired brain injury
Age Group: 74.2 years (range: 65-89 years)
Sex: M+F
Population Size: 75
Sources:
https://pubmed.ncbi.nlm.nih.gov/20586532/
Fever 1 patient
296 mg 1 times / day multiple, oral (mean)
Recommended
Dose: 296 mg, 1 times / day
Route: oral
Route: multiple
Dose: 296 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/20586532/
unhealthy, 74.2 years (range: 65-89 years)
n = 75
Health Status: unhealthy
Condition: schizophrenia | schizoaffective disorder | Parkinson’ s disease with psychotic symptoms | bipolar disorder | acquired brain injury
Age Group: 74.2 years (range: 65-89 years)
Sex: M+F
Population Size: 75
Sources:
https://pubmed.ncbi.nlm.nih.gov/20586532/
Ataxia 1 patient
Disc. AE
296 mg 1 times / day multiple, oral (mean)
Recommended
Dose: 296 mg, 1 times / day
Route: oral
Route: multiple
Dose: 296 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/20586532/
unhealthy, 74.2 years (range: 65-89 years)
n = 75
Health Status: unhealthy
Condition: schizophrenia | schizoaffective disorder | Parkinson’ s disease with psychotic symptoms | bipolar disorder | acquired brain injury
Age Group: 74.2 years (range: 65-89 years)
Sex: M+F
Population Size: 75
Sources:
https://pubmed.ncbi.nlm.nih.gov/20586532/
Cardiomyopathy 1 patient
Disc. AE
296 mg 1 times / day multiple, oral (mean)
Recommended
Dose: 296 mg, 1 times / day
Route: oral
Route: multiple
Dose: 296 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/20586532/
unhealthy, 74.2 years (range: 65-89 years)
n = 75
Health Status: unhealthy
Condition: schizophrenia | schizoaffective disorder | Parkinson’ s disease with psychotic symptoms | bipolar disorder | acquired brain injury
Age Group: 74.2 years (range: 65-89 years)
Sex: M+F
Population Size: 75
Sources:
https://pubmed.ncbi.nlm.nih.gov/20586532/
Dysphagia 1 patient
Disc. AE
296 mg 1 times / day multiple, oral (mean)
Recommended
Dose: 296 mg, 1 times / day
Route: oral
Route: multiple
Dose: 296 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/20586532/
unhealthy, 74.2 years (range: 65-89 years)
n = 75
Health Status: unhealthy
Condition: schizophrenia | schizoaffective disorder | Parkinson’ s disease with psychotic symptoms | bipolar disorder | acquired brain injury
Age Group: 74.2 years (range: 65-89 years)
Sex: M+F
Population Size: 75
Sources:
https://pubmed.ncbi.nlm.nih.gov/20586532/
Myocarditis 1 patient
Disc. AE
296 mg 1 times / day multiple, oral (mean)
Recommended
Dose: 296 mg, 1 times / day
Route: oral
Route: multiple
Dose: 296 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/20586532/
unhealthy, 74.2 years (range: 65-89 years)
n = 75
Health Status: unhealthy
Condition: schizophrenia | schizoaffective disorder | Parkinson’ s disease with psychotic symptoms | bipolar disorder | acquired brain injury
Age Group: 74.2 years (range: 65-89 years)
Sex: M+F
Population Size: 75
Sources:
https://pubmed.ncbi.nlm.nih.gov/20586532/
Parkinsonism 1 patient
Disc. AE
296 mg 1 times / day multiple, oral (mean)
Recommended
Dose: 296 mg, 1 times / day
Route: oral
Route: multiple
Dose: 296 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/20586532/
unhealthy, 74.2 years (range: 65-89 years)
n = 75
Health Status: unhealthy
Condition: schizophrenia | schizoaffective disorder | Parkinson’ s disease with psychotic symptoms | bipolar disorder | acquired brain injury
Age Group: 74.2 years (range: 65-89 years)
Sex: M+F
Population Size: 75
Sources:
https://pubmed.ncbi.nlm.nih.gov/20586532/
Sedation 1 patient
Disc. AE
296 mg 1 times / day multiple, oral (mean)
Recommended
Dose: 296 mg, 1 times / day
Route: oral
Route: multiple
Dose: 296 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/20586532/
unhealthy, 74.2 years (range: 65-89 years)
n = 75
Health Status: unhealthy
Condition: schizophrenia | schizoaffective disorder | Parkinson’ s disease with psychotic symptoms | bipolar disorder | acquired brain injury
Age Group: 74.2 years (range: 65-89 years)
Sex: M+F
Population Size: 75
Sources:
https://pubmed.ncbi.nlm.nih.gov/20586532/
Orthostatic hypotension 13 patients
Disc. AE
296 mg 1 times / day multiple, oral (mean)
Recommended
Dose: 296 mg, 1 times / day
Route: oral
Route: multiple
Dose: 296 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/20586532/
unhealthy, 74.2 years (range: 65-89 years)
n = 75
Health Status: unhealthy
Condition: schizophrenia | schizoaffective disorder | Parkinson’ s disease with psychotic symptoms | bipolar disorder | acquired brain injury
Age Group: 74.2 years (range: 65-89 years)
Sex: M+F
Population Size: 75
Sources:
https://pubmed.ncbi.nlm.nih.gov/20586532/
Constipation 16 patients
296 mg 1 times / day multiple, oral (mean)
Recommended
Dose: 296 mg, 1 times / day
Route: oral
Route: multiple
Dose: 296 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/20586532/
unhealthy, 74.2 years (range: 65-89 years)
n = 75
Health Status: unhealthy
Condition: schizophrenia | schizoaffective disorder | Parkinson’ s disease with psychotic symptoms | bipolar disorder | acquired brain injury
Age Group: 74.2 years (range: 65-89 years)
Sex: M+F
Population Size: 75
Sources:
https://pubmed.ncbi.nlm.nih.gov/20586532/
Leukopenia 2 patients
296 mg 1 times / day multiple, oral (mean)
Recommended
Dose: 296 mg, 1 times / day
Route: oral
Route: multiple
Dose: 296 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/20586532/
unhealthy, 74.2 years (range: 65-89 years)
n = 75
Health Status: unhealthy
Condition: schizophrenia | schizoaffective disorder | Parkinson’ s disease with psychotic symptoms | bipolar disorder | acquired brain injury
Age Group: 74.2 years (range: 65-89 years)
Sex: M+F
Population Size: 75
Sources:
https://pubmed.ncbi.nlm.nih.gov/20586532/
Seizure 2 patients
296 mg 1 times / day multiple, oral (mean)
Recommended
Dose: 296 mg, 1 times / day
Route: oral
Route: multiple
Dose: 296 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/20586532/
unhealthy, 74.2 years (range: 65-89 years)
n = 75
Health Status: unhealthy
Condition: schizophrenia | schizoaffective disorder | Parkinson’ s disease with psychotic symptoms | bipolar disorder | acquired brain injury
Age Group: 74.2 years (range: 65-89 years)
Sex: M+F
Population Size: 75
Sources:
https://pubmed.ncbi.nlm.nih.gov/20586532/
Fever 2 patients
Disc. AE
296 mg 1 times / day multiple, oral (mean)
Recommended
Dose: 296 mg, 1 times / day
Route: oral
Route: multiple
Dose: 296 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/20586532/
unhealthy, 74.2 years (range: 65-89 years)
n = 75
Health Status: unhealthy
Condition: schizophrenia | schizoaffective disorder | Parkinson’ s disease with psychotic symptoms | bipolar disorder | acquired brain injury
Age Group: 74.2 years (range: 65-89 years)
Sex: M+F
Population Size: 75
Sources:
https://pubmed.ncbi.nlm.nih.gov/20586532/
Tachycardia 2 patients
Disc. AE
296 mg 1 times / day multiple, oral (mean)
Recommended
Dose: 296 mg, 1 times / day
Route: oral
Route: multiple
Dose: 296 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/20586532/
unhealthy, 74.2 years (range: 65-89 years)
n = 75
Health Status: unhealthy
Condition: schizophrenia | schizoaffective disorder | Parkinson’ s disease with psychotic symptoms | bipolar disorder | acquired brain injury
Age Group: 74.2 years (range: 65-89 years)
Sex: M+F
Population Size: 75
Sources:
https://pubmed.ncbi.nlm.nih.gov/20586532/
Hypersalivation 25 patients
296 mg 1 times / day multiple, oral (mean)
Recommended
Dose: 296 mg, 1 times / day
Route: oral
Route: multiple
Dose: 296 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/20586532/
unhealthy, 74.2 years (range: 65-89 years)
n = 75
Health Status: unhealthy
Condition: schizophrenia | schizoaffective disorder | Parkinson’ s disease with psychotic symptoms | bipolar disorder | acquired brain injury
Age Group: 74.2 years (range: 65-89 years)
Sex: M+F
Population Size: 75
Sources:
https://pubmed.ncbi.nlm.nih.gov/20586532/
Sedation 28 patients
296 mg 1 times / day multiple, oral (mean)
Recommended
Dose: 296 mg, 1 times / day
Route: oral
Route: multiple
Dose: 296 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/20586532/
unhealthy, 74.2 years (range: 65-89 years)
n = 75
Health Status: unhealthy
Condition: schizophrenia | schizoaffective disorder | Parkinson’ s disease with psychotic symptoms | bipolar disorder | acquired brain injury
Age Group: 74.2 years (range: 65-89 years)
Sex: M+F
Population Size: 75
Sources:
https://pubmed.ncbi.nlm.nih.gov/20586532/
Tachycardia 3 patients
296 mg 1 times / day multiple, oral (mean)
Recommended
Dose: 296 mg, 1 times / day
Route: oral
Route: multiple
Dose: 296 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/20586532/
unhealthy, 74.2 years (range: 65-89 years)
n = 75
Health Status: unhealthy
Condition: schizophrenia | schizoaffective disorder | Parkinson’ s disease with psychotic symptoms | bipolar disorder | acquired brain injury
Age Group: 74.2 years (range: 65-89 years)
Sex: M+F
Population Size: 75
Sources:
https://pubmed.ncbi.nlm.nih.gov/20586532/
Leukopenia 3 patients
Disc. AE
296 mg 1 times / day multiple, oral (mean)
Recommended
Dose: 296 mg, 1 times / day
Route: oral
Route: multiple
Dose: 296 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/20586532/
unhealthy, 74.2 years (range: 65-89 years)
n = 75
Health Status: unhealthy
Condition: schizophrenia | schizoaffective disorder | Parkinson’ s disease with psychotic symptoms | bipolar disorder | acquired brain injury
Age Group: 74.2 years (range: 65-89 years)
Sex: M+F
Population Size: 75
Sources:
https://pubmed.ncbi.nlm.nih.gov/20586532/
Myocardial infarction 3 patients
Disc. AE
296 mg 1 times / day multiple, oral (mean)
Recommended
Dose: 296 mg, 1 times / day
Route: oral
Route: multiple
Dose: 296 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/20586532/
unhealthy, 74.2 years (range: 65-89 years)
n = 75
Health Status: unhealthy
Condition: schizophrenia | schizoaffective disorder | Parkinson’ s disease with psychotic symptoms | bipolar disorder | acquired brain injury
Age Group: 74.2 years (range: 65-89 years)
Sex: M+F
Population Size: 75
Sources:
https://pubmed.ncbi.nlm.nih.gov/20586532/
Leukopenia 4 patients
296 mg 1 times / day multiple, oral (mean)
Recommended
Dose: 296 mg, 1 times / day
Route: oral
Route: multiple
Dose: 296 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/20586532/
unhealthy, 74.2 years (range: 65-89 years)
n = 75
Health Status: unhealthy
Condition: schizophrenia | schizoaffective disorder | Parkinson’ s disease with psychotic symptoms | bipolar disorder | acquired brain injury
Age Group: 74.2 years (range: 65-89 years)
Sex: M+F
Population Size: 75
Sources:
https://pubmed.ncbi.nlm.nih.gov/20586532/
Weight gain 8 patients
296 mg 1 times / day multiple, oral (mean)
Recommended
Dose: 296 mg, 1 times / day
Route: oral
Route: multiple
Dose: 296 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/20586532/
unhealthy, 74.2 years (range: 65-89 years)
n = 75
Health Status: unhealthy
Condition: schizophrenia | schizoaffective disorder | Parkinson’ s disease with psychotic symptoms | bipolar disorder | acquired brain injury
Age Group: 74.2 years (range: 65-89 years)
Sex: M+F
Population Size: 75
Sources:
https://pubmed.ncbi.nlm.nih.gov/20586532/
Orthostatic hypotension 10%
450 mg 1 times / day multiple, oral
Recommended
Dose: 450 mg, 1 times / day
Route: oral
Route: multiple
Dose: 450 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/14971863/
unhealthy, adult
n = 10
Health Status: unhealthy
Condition: schizophrenia, treatment-resistant
Age Group: adult
Sex: M+F
Population Size: 10
Sources:
https://pubmed.ncbi.nlm.nih.gov/14971863/
Urinary hesitancy 10%
450 mg 1 times / day multiple, oral
Recommended
Dose: 450 mg, 1 times / day
Route: oral
Route: multiple
Dose: 450 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/14971863/
unhealthy, adult
n = 10
Health Status: unhealthy
Condition: schizophrenia, treatment-resistant
Age Group: adult
Sex: M+F
Population Size: 10
Sources:
https://pubmed.ncbi.nlm.nih.gov/14971863/
Somnolence 100%
450 mg 1 times / day multiple, oral
Recommended
Dose: 450 mg, 1 times / day
Route: oral
Route: multiple
Dose: 450 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/14971863/
unhealthy, adult
n = 10
Health Status: unhealthy
Condition: schizophrenia, treatment-resistant
Age Group: adult
Sex: M+F
Population Size: 10
Sources:
https://pubmed.ncbi.nlm.nih.gov/14971863/
Dry mouth 20%
450 mg 1 times / day multiple, oral
Recommended
Dose: 450 mg, 1 times / day
Route: oral
Route: multiple
Dose: 450 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/14971863/
unhealthy, adult
n = 10
Health Status: unhealthy
Condition: schizophrenia, treatment-resistant
Age Group: adult
Sex: M+F
Population Size: 10
Sources:
https://pubmed.ncbi.nlm.nih.gov/14971863/
Dysphagia 20%
450 mg 1 times / day multiple, oral
Recommended
Dose: 450 mg, 1 times / day
Route: oral
Route: multiple
Dose: 450 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/14971863/
unhealthy, adult
n = 10
Health Status: unhealthy
Condition: schizophrenia, treatment-resistant
Age Group: adult
Sex: M+F
Population Size: 10
Sources:
https://pubmed.ncbi.nlm.nih.gov/14971863/
Stuttering 20%
450 mg 1 times / day multiple, oral
Recommended
Dose: 450 mg, 1 times / day
Route: oral
Route: multiple
Dose: 450 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/14971863/
unhealthy, adult
n = 10
Health Status: unhealthy
Condition: schizophrenia, treatment-resistant
Age Group: adult
Sex: M+F
Population Size: 10
Sources:
https://pubmed.ncbi.nlm.nih.gov/14971863/
Myoclonus 30%
450 mg 1 times / day multiple, oral
Recommended
Dose: 450 mg, 1 times / day
Route: oral
Route: multiple
Dose: 450 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/14971863/
unhealthy, adult
n = 10
Health Status: unhealthy
Condition: schizophrenia, treatment-resistant
Age Group: adult
Sex: M+F
Population Size: 10
Sources:
https://pubmed.ncbi.nlm.nih.gov/14971863/
Headache 40%
450 mg 1 times / day multiple, oral
Recommended
Dose: 450 mg, 1 times / day
Route: oral
Route: multiple
Dose: 450 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/14971863/
unhealthy, adult
n = 10
Health Status: unhealthy
Condition: schizophrenia, treatment-resistant
Age Group: adult
Sex: M+F
Population Size: 10
Sources:
https://pubmed.ncbi.nlm.nih.gov/14971863/
Urinary frequency 40%
450 mg 1 times / day multiple, oral
Recommended
Dose: 450 mg, 1 times / day
Route: oral
Route: multiple
Dose: 450 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/14971863/
unhealthy, adult
n = 10
Health Status: unhealthy
Condition: schizophrenia, treatment-resistant
Age Group: adult
Sex: M+F
Population Size: 10
Sources:
https://pubmed.ncbi.nlm.nih.gov/14971863/
Increased appetite 50%
450 mg 1 times / day multiple, oral
Recommended
Dose: 450 mg, 1 times / day
Route: oral
Route: multiple
Dose: 450 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/14971863/
unhealthy, adult
n = 10
Health Status: unhealthy
Condition: schizophrenia, treatment-resistant
Age Group: adult
Sex: M+F
Population Size: 10
Sources:
https://pubmed.ncbi.nlm.nih.gov/14971863/
Sweating 50%
450 mg 1 times / day multiple, oral
Recommended
Dose: 450 mg, 1 times / day
Route: oral
Route: multiple
Dose: 450 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/14971863/
unhealthy, adult
n = 10
Health Status: unhealthy
Condition: schizophrenia, treatment-resistant
Age Group: adult
Sex: M+F
Population Size: 10
Sources:
https://pubmed.ncbi.nlm.nih.gov/14971863/
Constipation 60%
450 mg 1 times / day multiple, oral
Recommended
Dose: 450 mg, 1 times / day
Route: oral
Route: multiple
Dose: 450 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/14971863/
unhealthy, adult
n = 10
Health Status: unhealthy
Condition: schizophrenia, treatment-resistant
Age Group: adult
Sex: M+F
Population Size: 10
Sources:
https://pubmed.ncbi.nlm.nih.gov/14971863/
Dizziness 60%
450 mg 1 times / day multiple, oral
Recommended
Dose: 450 mg, 1 times / day
Route: oral
Route: multiple
Dose: 450 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/14971863/
unhealthy, adult
n = 10
Health Status: unhealthy
Condition: schizophrenia, treatment-resistant
Age Group: adult
Sex: M+F
Population Size: 10
Sources:
https://pubmed.ncbi.nlm.nih.gov/14971863/
Nausea 60%
450 mg 1 times / day multiple, oral
Recommended
Dose: 450 mg, 1 times / day
Route: oral
Route: multiple
Dose: 450 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/14971863/
unhealthy, adult
n = 10
Health Status: unhealthy
Condition: schizophrenia, treatment-resistant
Age Group: adult
Sex: M+F
Population Size: 10
Sources:
https://pubmed.ncbi.nlm.nih.gov/14971863/
Dyspepsia 70%
450 mg 1 times / day multiple, oral
Recommended
Dose: 450 mg, 1 times / day
Route: oral
Route: multiple
Dose: 450 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/14971863/
unhealthy, adult
n = 10
Health Status: unhealthy
Condition: schizophrenia, treatment-resistant
Age Group: adult
Sex: M+F
Population Size: 10
Sources:
https://pubmed.ncbi.nlm.nih.gov/14971863/
Sialorrhea 80%
450 mg 1 times / day multiple, oral
Recommended
Dose: 450 mg, 1 times / day
Route: oral
Route: multiple
Dose: 450 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/14971863/
unhealthy, adult
n = 10
Health Status: unhealthy
Condition: schizophrenia, treatment-resistant
Age Group: adult
Sex: M+F
Population Size: 10
Sources:
https://pubmed.ncbi.nlm.nih.gov/14971863/
Lethargy 90%
450 mg 1 times / day multiple, oral
Recommended
Dose: 450 mg, 1 times / day
Route: oral
Route: multiple
Dose: 450 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/14971863/
unhealthy, adult
n = 10
Health Status: unhealthy
Condition: schizophrenia, treatment-resistant
Age Group: adult
Sex: M+F
Population Size: 10
Sources:
https://pubmed.ncbi.nlm.nih.gov/14971863/
Headache 10%
900 mg 1 times / day multiple, oral (max)
Recommended
Dose: 900 mg, 1 times / day
Route: oral
Route: multiple
Dose: 900 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/3046553/
unhealthy, adult
n = 126
Health Status: unhealthy
Condition: schizophrenia, treatment-resistant
Age Group: adult
Sex: M+F
Population Size: 126
Sources:
https://pubmed.ncbi.nlm.nih.gov/3046553/
Nausea and vomiting 10%
900 mg 1 times / day multiple, oral (max)
Recommended
Dose: 900 mg, 1 times / day
Route: oral
Route: multiple
Dose: 900 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/3046553/
unhealthy, adult
n = 126
Health Status: unhealthy
Condition: schizophrenia, treatment-resistant
Age Group: adult
Sex: M+F
Population Size: 126
Sources:
https://pubmed.ncbi.nlm.nih.gov/3046553/
Hypertension 12%
900 mg 1 times / day multiple, oral (max)
Recommended
Dose: 900 mg, 1 times / day
Route: oral
Route: multiple
Dose: 900 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/3046553/
unhealthy, adult
n = 126
Health Status: unhealthy
Condition: schizophrenia, treatment-resistant
Age Group: adult
Sex: M+F
Population Size: 126
Sources:
https://pubmed.ncbi.nlm.nih.gov/3046553/
Hyperthermia 13%
900 mg 1 times / day multiple, oral (max)
Recommended
Dose: 900 mg, 1 times / day
Route: oral
Route: multiple
Dose: 900 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/3046553/
unhealthy, adult
n = 126
Health Status: unhealthy
Condition: schizophrenia, treatment-resistant
Age Group: adult
Sex: M+F
Population Size: 126
Sources:
https://pubmed.ncbi.nlm.nih.gov/3046553/
Hypotension 13%
900 mg 1 times / day multiple, oral (max)
Recommended
Dose: 900 mg, 1 times / day
Route: oral
Route: multiple
Dose: 900 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/3046553/
unhealthy, adult
n = 126
Health Status: unhealthy
Condition: schizophrenia, treatment-resistant
Age Group: adult
Sex: M+F
Population Size: 126
Sources:
https://pubmed.ncbi.nlm.nih.gov/3046553/
Salivation 13%
900 mg 1 times / day multiple, oral (max)
Recommended
Dose: 900 mg, 1 times / day
Route: oral
Route: multiple
Dose: 900 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/3046553/
unhealthy, adult
n = 126
Health Status: unhealthy
Condition: schizophrenia, treatment-resistant
Age Group: adult
Sex: M+F
Population Size: 126
Sources:
https://pubmed.ncbi.nlm.nih.gov/3046553/
Dizziness 14%
900 mg 1 times / day multiple, oral (max)
Recommended
Dose: 900 mg, 1 times / day
Route: oral
Route: multiple
Dose: 900 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/3046553/
unhealthy, adult
n = 126
Health Status: unhealthy
Condition: schizophrenia, treatment-resistant
Age Group: adult
Sex: M+F
Population Size: 126
Sources:
https://pubmed.ncbi.nlm.nih.gov/3046553/
Constipation 16%
900 mg 1 times / day multiple, oral (max)
Recommended
Dose: 900 mg, 1 times / day
Route: oral
Route: multiple
Dose: 900 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/3046553/
unhealthy, adult
n = 126
Health Status: unhealthy
Condition: schizophrenia, treatment-resistant
Age Group: adult
Sex: M+F
Population Size: 126
Sources:
https://pubmed.ncbi.nlm.nih.gov/3046553/
Tachycardia 17%
900 mg 1 times / day multiple, oral (max)
Recommended
Dose: 900 mg, 1 times / day
Route: oral
Route: multiple
Dose: 900 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/3046553/
unhealthy, adult
n = 126
Health Status: unhealthy
Condition: schizophrenia, treatment-resistant
Age Group: adult
Sex: M+F
Population Size: 126
Sources:
https://pubmed.ncbi.nlm.nih.gov/3046553/
Drowsiness 21%
900 mg 1 times / day multiple, oral (max)
Recommended
Dose: 900 mg, 1 times / day
Route: oral
Route: multiple
Dose: 900 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/3046553/
unhealthy, adult
n = 126
Health Status: unhealthy
Condition: schizophrenia, treatment-resistant
Age Group: adult
Sex: M+F
Population Size: 126
Sources:
https://pubmed.ncbi.nlm.nih.gov/3046553/
Dry mouth 5%
900 mg 1 times / day multiple, oral (max)
Recommended
Dose: 900 mg, 1 times / day
Route: oral
Route: multiple
Dose: 900 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/3046553/
unhealthy, adult
n = 126
Health Status: unhealthy
Condition: schizophrenia, treatment-resistant
Age Group: adult
Sex: M+F
Population Size: 126
Sources:
https://pubmed.ncbi.nlm.nih.gov/3046553/
Overview

Overview

CYP3A4CYP2C9CYP2D6hERG
substrate
1601
substrate
936

inhibitor
1604
substrate
1118

inhibitor
1702
inhibitor
1475

OverviewOther

Other InhibitorOther SubstrateOther Inducer
CYP3A
191

CYP2C19
1325

BCRP
643

P-gp
1330

OATP1B1
733

OATP1B3
657
UGT1A4
330

CYP1A1
325

CYP1A2
972

CYP3A5
367

CYP2C8
634

CYP2C19
910

CYP2E1
606

FMO3
64

UGT1A1
393

P-gp
1400

OCT1
302

OCT3
75

OCTN1
41

OCTN2
44

OATP1B1
370

OATP1B3
319
Drug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
OATP1B1
748
 no
OATP1B3
666
 no
BCRP
713
 yes [IC50 42 uM]
CYP2D6
1738
 yes [Ki 19 uM]
CYP2C9
1648
 yes [Ki 31 uM]
CYP2C19
1392
 yes [Ki 69 uM]
CYP3A
271
 yes [Ki 99 uM]
P-gp
1514
 yes
Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
CYP1A2
972
 major
yes (co-administration study)
Comment: co-administration with fluvoxamin lead to 3x increase in clozapine Cmin
CYP2C19
910
 minor
CYP2C9
936
 minor
CYP2D6
1118
 minor
CYP3A4
1601
 minor
weak (co-administration study)
Comment: co-administration studies indicate modest (<2x) increase in clozapine exposure when co-administered with CYP3A4 inhibitors
CYP1A1
325
 no
OATP1B1
370
 no
OATP1B3
319
 no
OCT1
302
 no
OCT3
75
 no
OCTN1
41
 no
OCTN2
44
 no
P-gp
1400
 no
CYP2C8
634
 yes
CYP2E1
606
 yes
CYP3A5
367
 yes
FMO3
64
 yes
UGT1A4
330
 yes
UGT1A1
393
 yes
yes (pharmacogenomic study)
Comment: UGT1A1*28 and UGT1A4*3 alleles contribute significantly to inter-individual variability in CLZ and dmCLZ metabolism
Tox targets

Tox targets

TargetModalityActivityMetaboliteClinical evidence
hERG
1507
Sourcing

Sourcing

Vendor/AggregatorIDURL
ChEBI
CHEBI:3766
https://www.ebi.ac.uk/chebi/searchId.do?chebiId=CHEBI:3766
ChemicalBook
CB7776111
https://www.chemicalbook.com/ChemicalProductProperty_EN_CB7776111
MolPort
MolPort-001-728-041
https://www.molport.com/shop/molecule-link/MolPort-001-728-041
Selleck Chemicals
Clozapine(Clozaril)
http://www.selleckchem.com/products/Clozapine(Clozaril).html
ZINC
ZINC000019796155
http://zinc15.docking.org/substances/ZINC000019796155
eMolecules
536309
https://www.emolecules.com/cgi-bin/more?vid=536309
PubMed

PubMed

TitleDatePubMed
Hepatic encephalopathy associated with combined clozapine and divalproex sodium treatment.
1997 Apr
A selective dopamine D4 receptor antagonist, NRA0160: a preclinical neuropharmacological profile.
1999
Clozapine lacks previous clinical efficacy when restarted after a period of discontinuation: a case series.
1999 Dec
Clozapine pretreatment modifies haloperidol-elicited forebrain Fos induction: a regionally-specific double dissociation.
1999 Jun
New and old antipsychotics versus clozapine in a monkey model: adverse effects and antiamphetamine effects.
1999 Jun
Seizures after discontinuation of low-dose lorazepam from originally seizure-free clozapine regimen: combined effects?
1999 Jun
Clozapine and obsessions in patients with recent-onset schizophrenia and other psychotic disorders.
1999 Jun
[Presentation of obsessive-compulsive symptoms in a patient with schizophrenia treated with clozapine].
1999 May
Quinpirole, 8-OH-DPAT and ketanserin modulate catalepsy induced by high doses of atypical antipsychotics.
1999 Nov
Worsening of motor features of parkinsonism with olanzapine.
1999 Nov
[The concept of supersensitivity psychosis. The particular case of clozapine].
1999 Nov-Dec
Clozapine, neuroleptic malignant syndrome, and pancerebellar syndrome.
1999 Nov-Dec
Hypotension associated with clozapine after cardiopulmonary bypass.
1999 Oct
Clozapine-induced acute interstitial nephritis.
1999 Oct 2
Transient syncope and ECG changes associated with the concurrent administration of clozapine and diazepam.
1999 Sep
Reemergence of tardive dyskinesia after discontinuation of clozapine treatment.
2000 Dec 15
An unexpected and serious complication of treatment with the atypical antipsychotic drug clozapine.
2000 Jul
Clozapine-associated extrapyramidal reaction.
2000 May
Significant interaction between clozapine and cocaine in cocaine addicts.
2000 May 1
Ciprofloxacin increases serum clozapine and N-desmethylclozapine: a study in patients with schizophrenia.
2000 Nov
A case of pharmacokinetic interference in comedication of clozapine and valproic acid.
2000 Nov
Hyperglycemia, hyperlipemia, and periodic paralysis: a case report of new side effects of clozapine.
2000 Nov
Risperidone-associated hyperprolactinemia.
2000 Nov-Dec
Inverse agonist activity of atypical antipsychotic drugs at human 5-hydroxytryptamine2C receptors.
2000 Oct
Effects of antipsychotic drugs on cholecystokinin and preprotachykinin (substance P) mRNA expression in the rat hippocampal formation.
2000 Sep
Myotoxicity and neurotoxicity during clozapine treatment.
2000 Sep-Oct
Antipsychotic medications and the elderly: effects on cognition and implications for use.
2001
Combinations of clozapine and phencyclidine: effects on drug discrimination and behavioral inhibition in rats.
2001
Protein thiol oxidation by haloperidol results in inhibition of mitochondrial complex I in brain regions: comparison with atypical antipsychotics.
2001 Apr
New onset diabetes and atypical antipsychotics.
2001 Feb
Effects of newer atypical antipsychotics on autonomic neurocardiac function: a comparison between amisulpride, olanzapine, sertindole, and clozapine.
2001 Feb
Uncompetitive antagonists of the N-methyl-D-aspartate (NMDA) receptors alter the mRNA expression of proteins associated with the NMDA receptor complex.
2001 Feb
Clozapine-associated reduction in arrest rates of psychotic patients with criminal histories.
2001 Feb
Haloperidol and clozapine increase neural activity in the rat prefrontal cortex.
2001 Feb 9
Olanzapine-induced leukopenia with human leukocyte antigen profiling.
2001 Jan
Pharmacokinetic-pharmacodynamic modelling in the early development phase of anti-psychotics: a comparison of the effects of clozapine, S 16924 and S 18327 in the EEG model in rats.
2001 Jan
Genetic determinants of clozapine-induced agranulocytosis: recent results of HLA subtyping in a non-jewish caucasian sample.
2001 Jan
Trimethoprim-sulfamethoxazole and clozapine.
2001 Jan
Clozapine therapy for a patient with a history of Hodgkin's disease.
2001 Jan
The clozapine access project.
2001 Jan
Pharmacology of [3H]R(+)-7-OH-DPAT binding in the rat caudate-putamen.
2001 Jan
Double-blind comparison of olanzapine versus clozapine in schizophrenic patients clinically eligible for treatment with clozapine.
2001 Jan 1
Antipsychotic drugs classified by their effects on the release of dopamine and noradrenaline in the prefrontal cortex and striatum.
2001 Jan 26
A proposed pathological model in the hippocampus of subjects with schizophrenia.
2001 Jan-Feb
Electroconvulsive therapy in rehabilitation: the Hong Kong experience.
2001 Mar
Clozapine and pulmonary embolus.
2001 Mar
Does fast dissociation from the dopamine d(2) receptor explain the action of atypical antipsychotics?: A new hypothesis.
2001 Mar
Pharmacological characterization of locomotor sensitization induced by chronic phencyclidine administration.
2001 Mar
Double activity imaging reveals distinct cellular targets of haloperidol, clozapine and dopamine D(3) receptor selective RGH-1756.
2001 Mar
The dynamin-dependent, arrestin-independent internalization of 5-hydroxytryptamine 2A (5-HT2A) serotonin receptors reveals differential sorting of arrestins and 5-HT2A receptors during endocytosis.
2001 Mar 16
Patents

Patents

JP2002511409A
21
JP2005528380A
6
JP2006505569A
64
JP2007514770A
72
JP2008528532A
12
JP2011526251A
110
JP2013544838A
2
JPH10175865A
4

Sample Use Guides

In Vivo Use Guide
Start with 12.5 mg once daily or twice daily, then increase the total daily dosage in increments of 25 mg to 50 mg per day (if well-tolerated) in order to reach 300 mg to 450 mg per day, in divided doses, by the end of 2 weeks.
Route of Administration: Oral
In Vitro Use Guide
The effects of antipsychotic medication on the energy metabolism of OLN-93 cells were analyzed by adding a vehicle (0.01% HCl, same dissolving solution used to solubilize the antipsychotics), 1 or 10 ug/ml of clozapine to the cell culture for 6 or 24 h.
Name Type Language
CLOZAPINE
EP   HSDB   INN   JAN   MART.   MI   ORANGE BOOK   USAN   USP   VANDF   WHO-DD  
USAN   INN  
Official Name English
CLOZAPINE [WHO-DD]
Common Name English
CLOZAPINE [JAN]
Common Name English
LEPONEX
Brand Name English
8-CHLORO-11-(4-METHYL-1-PIPERAZINYL)-5H-DIBENZO(B,E)(1,4)DIAZEPINE
Systematic Name English
CLOZAPINE [USP-RS]
Common Name English
CLOZAPINE [MI]
Common Name English
CLOZAPINE (CLOZARIL) [VANDF]
Common Name English
CLOZAPINE (FAZACLO) [VANDF]
Common Name English
CLOZAPINE [USAN]
Common Name English
CLOZAPINE RESOLUTION MIXTURE [USP-RS]
Common Name English
CLOZARIL
Brand Name English
CLOZAPINE [USP MONOGRAPH]
Common Name English
CLOZAPINE [HSDB]
Common Name English
HF-1854
Code English
FAZACLO
Brand Name English
CLOZAPINE [INN]
Common Name English
CLOZAPINE (VERSACLOZ) [VANDF]
Common Name English
CLOZAPINE [EP MONOGRAPH]
Common Name English
CLOZAPINE RESOLUTION MIXTURE
USP-RS  
Common Name English
CLOZAPINE (IVAX) [VANDF]
Common Name English
5H-DIBENZO(B,E)(1,4)DIAZEPINE, 8-CHLORO-11-(4-METHYL-1-PIPERAZINYL)-
Systematic Name English
NSC-757429
Code English
CLOZAPINE (CARACO) [VANDF]
Common Name English
HF 1854
Code English
CLOZAPINE (MYLAN) [VANDF]
Common Name English
CLOZAPINE [VANDF]
Common Name English
CLOZAPINE (UDL) [VANDF]
Common Name English
CLOZAPINE (TEVA) [VANDF]
Common Name English
CLOZAPINE [MART.]
Common Name English
CLOZAPINE [ORANGE BOOK]
Common Name English
Classification Tree Code System Code
FDA ORPHAN DRUG 357411
Created by admin on Fri Jun 25 21:00:20 UTC 2021 , Edited by admin on Fri Jun 25 21:00:20 UTC 2021
NCI_THESAURUS C29710
Created by admin on Fri Jun 25 21:00:20 UTC 2021 , Edited by admin on Fri Jun 25 21:00:20 UTC 2021
LIVERTOX 230
Created by admin on Fri Jun 25 21:00:20 UTC 2021 , Edited by admin on Fri Jun 25 21:00:20 UTC 2021
NDF-RT N0000175430
Created by admin on Fri Jun 25 21:00:20 UTC 2021 , Edited by admin on Fri Jun 25 21:00:20 UTC 2021
NCI_THESAURUS C94726
Created by admin on Fri Jun 25 21:00:20 UTC 2021 , Edited by admin on Fri Jun 25 21:00:20 UTC 2021
WHO-VATC QN05AH02
Created by admin on Fri Jun 25 21:00:20 UTC 2021 , Edited by admin on Fri Jun 25 21:00:20 UTC 2021
WHO-ATC N05AH02
Created by admin on Fri Jun 25 21:00:20 UTC 2021 , Edited by admin on Fri Jun 25 21:00:20 UTC 2021
Code System Code Type Description
DRUG CENTRAL
722
Created by admin on Fri Jun 25 21:00:20 UTC 2021 , Edited by admin on Fri Jun 25 21:00:20 UTC 2021
PRIMARY
IUPHAR
38
Created by admin on Fri Jun 25 21:00:20 UTC 2021 , Edited by admin on Fri Jun 25 21:00:20 UTC 2021
PRIMARY
EPA CompTox
5786-21-0
Created by admin on Fri Jun 25 21:00:20 UTC 2021 , Edited by admin on Fri Jun 25 21:00:20 UTC 2021
PRIMARY
JAPANESE REVIEW
CLOZARIL
Created by admin on Fri Jun 25 21:00:20 UTC 2021 , Edited by admin on Fri Jun 25 21:00:20 UTC 2021
PRIMARY APPROVED APRIL 2009
MESH
D003024
Created by admin on Fri Jun 25 21:00:20 UTC 2021 , Edited by admin on Fri Jun 25 21:00:20 UTC 2021
PRIMARY
MERCK INDEX
M3676
Created by admin on Fri Jun 25 21:00:20 UTC 2021 , Edited by admin on Fri Jun 25 21:00:20 UTC 2021
PRIMARY Merck Index
DRUG BANK
DB00363
Created by admin on Fri Jun 25 21:00:20 UTC 2021 , Edited by admin on Fri Jun 25 21:00:20 UTC 2021
PRIMARY
HSDB
6478
Created by admin on Fri Jun 25 21:00:20 UTC 2021 , Edited by admin on Fri Jun 25 21:00:20 UTC 2021
PRIMARY
CAS
1333667-72-3
Created by admin on Fri Jun 25 21:00:20 UTC 2021 , Edited by admin on Fri Jun 25 21:00:20 UTC 2021
ALTERNATIVE
USP_CATALOG
1142107
Created by admin on Fri Jun 25 21:00:20 UTC 2021 , Edited by admin on Fri Jun 25 21:00:20 UTC 2021
PRIMARY USP-RS
WIKIPEDIA
CLOZAPINE
Created by admin on Fri Jun 25 21:00:20 UTC 2021 , Edited by admin on Fri Jun 25 21:00:20 UTC 2021
PRIMARY
PUBCHEM
135398737
Created by admin on Fri Jun 25 21:00:20 UTC 2021 , Edited by admin on Fri Jun 25 21:00:20 UTC 2021
PRIMARY
LACTMED
Clozapine
Created by admin on Fri Jun 25 21:00:20 UTC 2021 , Edited by admin on Fri Jun 25 21:00:20 UTC 2021
PRIMARY
CAS
5786-21-0
Created by admin on Fri Jun 25 21:00:20 UTC 2021 , Edited by admin on Fri Jun 25 21:00:20 UTC 2021
PRIMARY
INN
2612
Created by admin on Fri Jun 25 21:00:20 UTC 2021 , Edited by admin on Fri Jun 25 21:00:20 UTC 2021
PRIMARY
FDA UNII
J60AR2IKIC
Created by admin on Fri Jun 25 21:00:20 UTC 2021 , Edited by admin on Fri Jun 25 21:00:20 UTC 2021
PRIMARY
EVMPD
SUB06787MIG
Created by admin on Fri Jun 25 21:00:20 UTC 2021 , Edited by admin on Fri Jun 25 21:00:20 UTC 2021
PRIMARY
RXCUI
2626
Created by admin on Fri Jun 25 21:00:20 UTC 2021 , Edited by admin on Fri Jun 25 21:00:20 UTC 2021
PRIMARY RxNorm
ECHA (EC/EINECS)
227-313-7
Created by admin on Fri Jun 25 21:00:20 UTC 2021 , Edited by admin on Fri Jun 25 21:00:20 UTC 2021
PRIMARY
ChEMBL
CHEMBL42
Created by admin on Fri Jun 25 21:00:20 UTC 2021 , Edited by admin on Fri Jun 25 21:00:20 UTC 2021
PRIMARY
NCI_THESAURUS
C28936
Created by admin on Fri Jun 25 21:00:20 UTC 2021 , Edited by admin on Fri Jun 25 21:00:20 UTC 2021
PRIMARY
USP_CATALOG
1142108
Created by admin on Fri Jun 25 21:00:20 UTC 2021 , Edited by admin on Fri Jun 25 21:00:20 UTC 2021
PRIMARY USP-RS
ACTIVE MOIETY
Structure of CLOZAPINE
METABOLITE ACTIVE (PARENT)
Structure of NORCLOZAPINE
METABOLITE LESS ACTIVE (PARENT)
Structure of CLOZAPINE N-OXIDE
SALT/SOLVATE (PARENT)
Structure of CLOZAPINE HYDROCHLORIDE
NIH
NCATS
PRIVACY ACT
ACCESSIBILITY
DISCLAIMER
HHS VULNERABILITY DISCLOSURE
For language access assistance, contact the NCATS Public Information Officer
National Center for Advancing Translational Sciences (NCATS),
6701 Democracy Boulevard, Bethesda MD 20892-4874 • 301-594-8966