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

Details

Stereochemistry ACHIRAL
Molecular Formula C18H19ClN4
Molecular Weight 326.823
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of CLOZAPINE

SMILES

CN1CCN(CC1)C2=NC3=C(NC4=C2C=CC=C4)C=CC(Cl)=C3

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
Molecular Formula C18H19ClN4
Molecular Weight 326.823
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

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
115
Targets

Targets

Primary TargetPharmacologyConditionPotency
Antagonist
2778
 160.0 nM [Ki]
Antagonist
2778
 5.4 nM [Ki]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Approved
8429
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
1737
substrate
1037

inhibitor
1767
substrate
1217

inhibitor
1852
inhibitor
1612

OverviewOther

Other InhibitorOther SubstrateOther Inducer
CYP3A
214

CYP2C19
1478

BCRP
699

P-gp
1461

OATP1B1
788

OATP1B3
706
UGT1A4
347

CYP1A1
349

CYP1A2
1054

CYP3A5
395

CYP2C8
693

CYP2C19
991

CYP2E1
667

FMO3
67

UGT1A1
418

P-gp
1537

OCT1
327

OCT3
80

OCTN1
47

OCTN2
50

OATP1B1
406

OATP1B3
350
Drug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
OATP1B1
803
 no
OATP1B3
715
 no
BCRP
773
 yes [IC50 42 uM]
CYP2D6
1891
 yes [Ki 19 uM]
CYP2C9
1819
 yes [Ki 31 uM]
CYP2C19
1553
 yes [Ki 69 uM]
CYP3A
298
 yes [Ki 99 uM]
P-gp
1650
 yes
Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
CYP1A2
1054
 major
yes (co-administration study)
Comment: co-administration with fluvoxamin lead to 3x increase in clozapine Cmin
CYP2C19
991
 minor
CYP2C9
1037
 minor
CYP2D6
1217
 minor
CYP3A4
1737
 minor
weak (co-administration study)
Comment: co-administration studies indicate modest (<2x) increase in clozapine exposure when co-administered with CYP3A4 inhibitors
CYP1A1
349
 no
OATP1B1
406
 no
OATP1B3
350
 no
OCT1
327
 no
OCT3
80
 no
OCTN1
47
 no
OCTN2
50
 no
P-gp
1537
 no
CYP2C8
693
 yes
CYP2E1
667
 yes
CYP3A5
395
 yes
FMO3
67
 yes
UGT1A4
347
 yes
UGT1A1
418
 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
1647
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
Panic disorder associated with clozapine.
2000 Dec
Reemergence of tardive dyskinesia after discontinuation of clozapine treatment.
2000 Dec 15
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
Myotoxicity and neurotoxicity during clozapine treatment.
2000 Sep-Oct
Antipsychotic medications and the elderly: effects on cognition and implications for use.
2001
Olanzapine: an updated review of its use in the management of schizophrenia.
2001
Effects of systemic injections of dopaminergic agents on the habituation of rats submitted to an open field test.
2001
Evidence for an association between polymorphism in the serotonin-2A receptor variant (102T/C) and increment of N100 amplitude in schizophrenics treated with clozapine.
2001
Atypical antipsychotics: new directions and new challenges in the treatment of schizophrenia.
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
Is generic really the same?
2001 Feb
Possible serotonin syndrome associated with clomipramine after withdrawal of clozapine.
2001 Feb
Effects of newer atypical antipsychotics on autonomic neurocardiac function: a comparison between amisulpride, olanzapine, sertindole, and clozapine.
2001 Feb
Mitchell B. Balter Award. Human leukocyte antigen-A1 predicts a good therapeutic response to clozapine with a low risk of agranulocytosis in patients with schizophrenia.
2001 Feb
FosB in rat striatum: normal regional distribution and enhanced expression after 6-month haloperidol administration.
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 increases apolipoprotein D expression in rodent brain: towards a mechanism for neuroleptic pharmacotherapy.
2001 Feb
Subspecialty training in schizophrenia.
2001 Feb
Increased dopamine d(2) receptor occupancy and elevated prolactin level associated with addition of haloperidol to clozapine.
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
Bodyweight gain with atypical antipsychotics. A comparative review.
2001 Jan
Clozapine for the treatment of drug-induced psychosis in Parkinson's disease: results of the 12 week open label extension in the PSYCLOPS trial.
2001 Jan
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
Fatty acid derivatives of clozapine: prolonged antidopaminergic activity of docosahexaenoylclozapine in the rat.
2001 Jan
The effect of clozapine on caudate nucleus volume in schizophrenic patients previously treated with typical antipsychotics.
2001 Jan
Double-blind comparison of olanzapine versus clozapine in schizophrenic patients clinically eligible for treatment with clozapine.
2001 Jan 1
Lack of association between the T-->C 267 serotonin 5-HT6 receptor gene (HTR6) polymorphism and prediction of response to clozapine in schizophrenia.
2001 Jan 15
Clozapine, but not haloperidol, reverses social behavior deficit in mice during withdrawal from chronic phencyclidine treatment.
2001 Jan 22
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
5-HT(2A) and D(2) receptor blockade increases cortical DA release via 5-HT(1A) receptor activation: a possible mechanism of atypical antipsychotic-induced cortical dopamine release.
2001 Mar
Atypical antipsychotics and hyperglycaemia.
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
Cloning, expression, and pharmacological characterization of a novel human histamine receptor.
2001 Mar
Cloning and pharmacological characterization of a fourth histamine receptor (H(4)) expressed in bone marrow.
2001 Mar
Double activity imaging reveals distinct cellular targets of haloperidol, clozapine and dopamine D(3) receptor selective RGH-1756.
2001 Mar
Patents

Patents

JP2002511409A
23
JP2005528380A
6
JP2006505569A
69
JP2007514770A
75
JP2008528532A
12
JP2011526251A
112
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.
Substance Class Chemical
Created
by admin
on Fri Dec 15 15:07:36 UTC 2023
Edited
by admin
on Fri Dec 15 15:07:36 UTC 2023
Record UNII
J60AR2IKIC
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
CLOZAPINE
EP   HSDB   INN   JAN   MART.   MI   ORANGE BOOK   USAN   USP   VANDF   WHO-DD  
USAN   INN  
Official 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 [WHO-DD]
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 Dec 15 15:07:36 UTC 2023 , Edited by admin on Fri Dec 15 15:07:36 UTC 2023
NCI_THESAURUS C29710
Created by admin on Fri Dec 15 15:07:36 UTC 2023 , Edited by admin on Fri Dec 15 15:07:36 UTC 2023
LIVERTOX NBK548412
Created by admin on Fri Dec 15 15:07:36 UTC 2023 , Edited by admin on Fri Dec 15 15:07:36 UTC 2023
NDF-RT N0000175430
Created by admin on Fri Dec 15 15:07:36 UTC 2023 , Edited by admin on Fri Dec 15 15:07:36 UTC 2023
NCI_THESAURUS C94726
Created by admin on Fri Dec 15 15:07:36 UTC 2023 , Edited by admin on Fri Dec 15 15:07:36 UTC 2023
WHO-VATC QN05AH02
Created by admin on Fri Dec 15 15:07:36 UTC 2023 , Edited by admin on Fri Dec 15 15:07:36 UTC 2023
WHO-ATC N05AH02
Created by admin on Fri Dec 15 15:07:36 UTC 2023 , Edited by admin on Fri Dec 15 15:07:36 UTC 2023
Code System Code Type Description
DRUG CENTRAL
722
Created by admin on Fri Dec 15 15:07:36 UTC 2023 , Edited by admin on Fri Dec 15 15:07:36 UTC 2023
PRIMARY
IUPHAR
38
Created by admin on Fri Dec 15 15:07:36 UTC 2023 , Edited by admin on Fri Dec 15 15:07:36 UTC 2023
PRIMARY
EPA CompTox
DTXSID5022855
Created by admin on Fri Dec 15 15:07:36 UTC 2023 , Edited by admin on Fri Dec 15 15:07:36 UTC 2023
PRIMARY
JAPANESE REVIEW
CLOZARIL
Created by admin on Fri Dec 15 15:07:36 UTC 2023 , Edited by admin on Fri Dec 15 15:07:36 UTC 2023
PRIMARY APPROVED APRIL 2009
MESH
D003024
Created by admin on Fri Dec 15 15:07:36 UTC 2023 , Edited by admin on Fri Dec 15 15:07:36 UTC 2023
PRIMARY
MERCK INDEX
m3676
Created by admin on Fri Dec 15 15:07:36 UTC 2023 , Edited by admin on Fri Dec 15 15:07:36 UTC 2023
PRIMARY Merck Index
DRUG BANK
DB00363
Created by admin on Fri Dec 15 15:07:36 UTC 2023 , Edited by admin on Fri Dec 15 15:07:36 UTC 2023
PRIMARY
HSDB
6478
Created by admin on Fri Dec 15 15:07:36 UTC 2023 , Edited by admin on Fri Dec 15 15:07:36 UTC 2023
PRIMARY
CAS
1333667-72-3
Created by admin on Fri Dec 15 15:07:36 UTC 2023 , Edited by admin on Fri Dec 15 15:07:36 UTC 2023
ALTERNATIVE
CHEBI
3766
Created by admin on Fri Dec 15 15:07:36 UTC 2023 , Edited by admin on Fri Dec 15 15:07:36 UTC 2023
PRIMARY
SMS_ID
100000092795
Created by admin on Fri Dec 15 15:07:36 UTC 2023 , Edited by admin on Fri Dec 15 15:07:36 UTC 2023
PRIMARY
WIKIPEDIA
CLOZAPINE
Created by admin on Fri Dec 15 15:07:36 UTC 2023 , Edited by admin on Fri Dec 15 15:07:36 UTC 2023
PRIMARY
PUBCHEM
135398737
Created by admin on Fri Dec 15 15:07:36 UTC 2023 , Edited by admin on Fri Dec 15 15:07:36 UTC 2023
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LACTMED
Clozapine
Created by admin on Fri Dec 15 15:07:36 UTC 2023 , Edited by admin on Fri Dec 15 15:07:36 UTC 2023
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RS_ITEM_NUM
1142107
Created by admin on Fri Dec 15 15:07:36 UTC 2023 , Edited by admin on Fri Dec 15 15:07:36 UTC 2023
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NSC
757429
Created by admin on Fri Dec 15 15:07:36 UTC 2023 , Edited by admin on Fri Dec 15 15:07:36 UTC 2023
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CAS
5786-21-0
Created by admin on Fri Dec 15 15:07:36 UTC 2023 , Edited by admin on Fri Dec 15 15:07:36 UTC 2023
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INN
2612
Created by admin on Fri Dec 15 15:07:36 UTC 2023 , Edited by admin on Fri Dec 15 15:07:36 UTC 2023
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FDA UNII
J60AR2IKIC
Created by admin on Fri Dec 15 15:07:36 UTC 2023 , Edited by admin on Fri Dec 15 15:07:36 UTC 2023
PRIMARY
EVMPD
SUB06787MIG
Created by admin on Fri Dec 15 15:07:36 UTC 2023 , Edited by admin on Fri Dec 15 15:07:36 UTC 2023
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RXCUI
2626
Created by admin on Fri Dec 15 15:07:36 UTC 2023 , Edited by admin on Fri Dec 15 15:07:36 UTC 2023
PRIMARY RxNorm
ECHA (EC/EINECS)
227-313-7
Created by admin on Fri Dec 15 15:07:36 UTC 2023 , Edited by admin on Fri Dec 15 15:07:36 UTC 2023
PRIMARY
ChEMBL
CHEMBL42
Created by admin on Fri Dec 15 15:07:36 UTC 2023 , Edited by admin on Fri Dec 15 15:07:36 UTC 2023
PRIMARY
NCI_THESAURUS
C28936
Created by admin on Fri Dec 15 15:07:36 UTC 2023 , Edited by admin on Fri Dec 15 15:07:36 UTC 2023
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DAILYMED
J60AR2IKIC
Created by admin on Fri Dec 15 15:07:36 UTC 2023 , Edited by admin on Fri Dec 15 15:07:36 UTC 2023
PRIMARY
Related Record Type Details
ALDEHYDE OXIDASE
METABOLIC ENZYME -> INHIBITOR
IC50
PLASMA PROTEIN FRACTION (HUMAN)
BINDER->LIGAND
BINDING
5-HYDROXYTRYPTAMINE RECEPTOR 2A
TARGET -> INHIBITOR
IC50
CYTOCHROME P450 1A2
METABOLIC ENZYME -> SUBSTRATE
Structure of CLOZAPINE HYDROCHLORIDE
SALT/SOLVATE -> PARENT
D(2) DOPAMINE RECEPTOR
TARGET -> INHIBITOR
Ki
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Structure of NORCLOZAPINE
METABOLITE ACTIVE -> PARENT
ACTIVITY OF NORCLOZAPINE AGAINST DOPAMINE AND SEROTONIN RECEPTOR MAY DIFFER FROM THAT OF CLOZAPINE
MAJOR
Structure of CLOZAPINE N-OXIDE
METABOLITE LESS ACTIVE -> PARENT
MAJOR
Structure of CLOZAPINE N-OXIDE
METABOLITE LESS ACTIVE -> PARENT
APPEARS TO HAVE LESS ACTIVITY THAN CLOZAPINE AND NORCLOZAPINE AGAINST 5HT RECEPTORS
MAJOR
Structure of NORCLOZAPINE
METABOLITE ACTIVE -> PARENT
MAJOR
Significant Metabolite
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Structure of 8-CHLORO-5,10-DIHYDRO-11H-DIBENZO(B,E)(1,4)DIAZEPIN-11-ONE
IMPURITY -> PARENT
CHROMATOGRAPHIC PURITY (HPLC/UV)
CLINICALLY SIGNIFICANT
Structure of 11,11-(PIPERAZINE-1,4-DIYL)BIS(8-CHLORO-5H-DIBENZO(B,E)(1,4)DIAZEPINE)
IMPURITY -> PARENT
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
Structure of NORCLOZAPINE
IMPURITY -> PARENT
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
Structure of (2-((2-AMINO-4-CHLOROPHENYL)AMINO)PHENYL)(4-METHYL-1-PIPERAZINYL)METHANONE
IMPURITY -> PARENT
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
Related Record Type Details
Structure of CLOZAPINE
ACTIVE MOIETY
Name Property Type Amount Referenced Substance Defining Parameters References
Biological Half-life PHARMACOKINETIC
NIH
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