U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS
This repository is under review for potential modification in compliance with Administration directives.

Details

Stereochemistry RACEMIC
Molecular Formula C23H27FN4O3
Molecular Weight 426.4839
Optical Activity ( + / - )
Defined Stereocenters 0 / 1
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of PALIPERIDONE

SMILES

CC1=C(CCN2CCC(CC2)C3=NOC4=C3C=CC(F)=C4)C(=O)N5CCCC(O)C5=N1

InChI

InChIKey=PMXMIIMHBWHSKN-UHFFFAOYSA-N
InChI=1S/C23H27FN4O3/c1-14-17(23(30)28-9-2-3-19(29)22(28)25-14)8-12-27-10-6-15(7-11-27)21-18-5-4-16(24)13-20(18)31-26-21/h4-5,13,15,19,29H,2-3,6-12H2,1H3

HIDE SMILES / InChI
Molecular Formula C23H27FN4O3
Molecular Weight 426.4839
Charge 0
Count
Stereochemistry RACEMIC
Additional Stereochemistry No
Defined Stereocenters 0 / 1
E/Z Centers 0
Optical Activity ( + / - )

Description
Curator's Comment: description was created based on several sources, including http://dx.doi.org/10.4172/2161-1459.1000117

Paliperidone (9-OH-risperidone) is the primary active metabolite of the older antipsychotic risperidone. While its specific mechanism of action is unknown, it is believed that paliperidone and risperidone act via similar if not the same pathways. It has been proposed that the drug's therapeutic activity in schizophrenia is mediated through a combination of central dopamine Type 2 (D2) and serotonin Type 2 (5HT2A) receptor antagonism. Paliperidone is also active as an antagonist at alpha 1 and alpha 2 adrenergic receptors and H1 histaminergic receptors, which may explain some of the other effects of the drug. Paliperidone was approved by the FDA for treatment of schizophrenia on December 20, 2006. Very common adverse effects are: headache, tachycardia, somnolence and insomnia.

CNS Activity

CNS Penetrant
2588
Curator's Comment: Due to a hydroxyl group in position 9, paliperidone is less lipophilic than risperidone and crosses the blood-brain barrier less easily the parent drug. Experiments in knock-out mice have suggested that the brain entry of both risperidone and paliperidone may be limited by the presence in the blood-brain barrier of the P-glycoprotein, a multidrug efflux transporter, which has a slightly greater affinity for paliperidone than risperidone.

Originator

Approval Year

2006
190
Targets

Targets

Primary TargetPharmacologyConditionPotency
Antagonist
2849
Antagonist
2849
Antagonist
2849
Antagonist
2849
Blocker
555
 0.57 µM [IC50]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Approved
8583
INVEGA

Approved Use

INVEGA SUSTENNA® (paliperidone palmitate) is indicated for the treatment of: Schizophrenia [see Clinical Studies 14.1

Launch Date

2006
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
7.5 ng/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/20589922/
3 mg single, oral
dose: 3 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
PALIPERIDONE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
10.1 ng/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/26189570/
75 mg × eq single, intramuscular
dose: 75 mg × eq
route of administration: Intramuscular
experiment type: SINGLE
co-administered:
PALIPERIDONE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
257.3 ng × h/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/20589922/
3 mg single, oral
dose: 3 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
PALIPERIDONE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
22.214 ng × h/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/26189570/
75 mg × eq single, intramuscular
dose: 75 mg × eq
route of administration: Intramuscular
experiment type: SINGLE
co-administered:
PALIPERIDONE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
410 ng × h/mL
EXPERIMENT
https://www.researchgate.net/profile/An_Vermeulen/publication/267692020_Population_Pharmacokinetics_of_Paliperidone_ER_in_Healthy_Subjects_and_Patients_With_Schizophrenia/links/5493e2b40cf22d7925da3fa6/Population-Pharmacokinetics-of-Paliperidone-ER-in-Healthy-Subjects-and-Patients-With-Schizophrenia.pdf
6 mg 1 times / day steady-state, oral
dose: 6 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
PALIPERIDONE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
22.8 h
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/20589922/
3 mg single, oral
dose: 3 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
PALIPERIDONE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
44.9 day
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/26189570/
75 mg × eq single, intramuscular
dose: 75 mg × eq
route of administration: Intramuscular
experiment type: SINGLE
co-administered:
PALIPERIDONE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
23 h
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/label/2010/021999s018lbl.pdf
single, oral
 PALIPERIDONE plasma
Homo sapiens
population: UNKNOWN
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
Funbound

Funbound

ValueDoseCo-administeredAnalytePopulation
26%
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/label/2010/021999s018lbl.pdf
single, oral
 PALIPERIDONE plasma
Homo sapiens
population: UNKNOWN
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
Doses

Doses

DosePopulationAdverse events​
180 mg single, oral
Overdose
Dose: 180 mg
Route: oral
Route: single
Dose: 180 mg
Sources:
https://pubmed.ncbi.nlm.nih.gov/24580061
unhealthy, 12
Health Status: unhealthy
Age Group: 12
Sex: M
Sources:
https://pubmed.ncbi.nlm.nih.gov/24580061
Disc. AE: Lethargy, Tachycardia...
AEs leading to
discontinuation/dose reduction:
Lethargy
Tachycardia
Hypokalemia
Dyskinesia
Dystonia
Sources:
https://pubmed.ncbi.nlm.nih.gov/24580061
252 mg single, oral
Overdose
Dose: 252 mg
Route: oral
Route: single
Dose: 252 mg
Sources:
https://pubmed.ncbi.nlm.nih.gov/31308582
unhealthy, 16
Health Status: unhealthy
Age Group: 16
Sex: M
Sources:
https://pubmed.ncbi.nlm.nih.gov/31308582
Disc. AE: Loss of consciousness...
AEs leading to
discontinuation/dose reduction:
Loss of consciousness
Sources:
https://pubmed.ncbi.nlm.nih.gov/31308582
15 mg 1 times / day multiple, oral
Studied dose
Dose: 15 mg, 1 times / day
Route: oral
Route: multiple
Dose: 15 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/24556260
unhealthy, 30
Health Status: unhealthy
Age Group: 30
Sex: M
Sources:
https://pubmed.ncbi.nlm.nih.gov/24556260
DLT: Motor tic...
Dose limiting toxicities:
Motor tic
Sources:
https://pubmed.ncbi.nlm.nih.gov/24556260
234 mg 2 times / month multiple, intramuscular
Recommended
Dose: 234 mg, 2 times / month
Route: intramuscular
Route: multiple
Dose: 234 mg, 2 times / month
Sources:
https://pubmed.ncbi.nlm.nih.gov/25938474
unhealthy, 37.7
Health Status: unhealthy
Age Group: 37.7
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/25938474
Disc. AE: Depressive symptom, Psychotic disorder...
AEs leading to
discontinuation/dose reduction:
Depressive symptom (0.9%)
Psychotic disorder (0.9%)
Anxiety (0.4%)
Insomnia (0.4%)
Agitation (0.4%)
Abnormal dreams (0.4%)
Libido decreased (0.4%)
Substance abuse (0.4%)
Suicidal ideation (0.4%)
Paranoid schizophrenia (0.4%)
Akathisia (0.9%)
Headache (0.9%)
Dystonia (0.4%)
Dizziness (0.4%)
Tardive dyskinesia (0.4%)
Dyskinesia (0.4%)
Oromandibular dystonia (0.4%)
Extrapyramidal disorder (0.4%)
Erectile dysfunction (0.9%)
Amenorrhea (0.4%)
Ejaculation failure (0.4%)
Galactorrhea (0.4%)
Gynecomastia (0.4%)
Injection site pain (0.9%)
Chest discomfort (0.4%)
Weight increased (0.9%)
Semen volume decreased (0.4%)
Sources:
https://pubmed.ncbi.nlm.nih.gov/25938474
9 mg 1 times / day multiple, oral
Recommended
Dose: 9 mg, 1 times / day
Route: oral
Route: multiple
Dose: 9 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/24580061
unhealthy, 38
Health Status: unhealthy
Age Group: 38
Sex: M
Sources:
https://pubmed.ncbi.nlm.nih.gov/24580061
Disc. AE: Dyskinesia, Dystonia...
AEs leading to
discontinuation/dose reduction:
Dyskinesia
Dystonia
Tremor
Diaphoresis
Tachycardia
Sources:
https://pubmed.ncbi.nlm.nih.gov/24580061
12 mg 1 times / day multiple, oral
Recommended
Dose: 12 mg, 1 times / day
Route: oral
Route: multiple
Dose: 12 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021999s036lbl.pdf
unhealthy
Health Status: unhealthy
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021999s036lbl.pdf
Disc. AE: Cerebrovascular disorder (NOS), Stroke...
AEs leading to
discontinuation/dose reduction:
Cerebrovascular disorder (NOS)
Stroke
Transient ischemic attack (grade 3-5)
Neuroleptic malignant syndrome
QT interval prolonged
Tardive dyskinesia
Hyperglycemia
Dyslipidemia
Weight gain
Hyperprolactinemia
Intestinal stricture NOS
Orthostatic hypotension
Syncope
Leukopenia
Neutropenia
Agranulocytosis
Cognitive impairment
Motor dysfunction NOS
Seizures
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021999s036lbl.pdf
234 mg 2 times / month multiple, intramuscular
Recommended
Dose: 234 mg, 2 times / month
Route: intramuscular
Route: multiple
Dose: 234 mg, 2 times / month
Sources:
https://www.janssenlabels.com/package-insert/product-monograph/prescribing-information/INVEGA+SUSTENNA-pi.pdf
unhealthy
Health Status: unhealthy
Sources:
https://www.janssenlabels.com/package-insert/product-monograph/prescribing-information/INVEGA+SUSTENNA-pi.pdf
Disc. AE: Cerebrovascular disorder (NOS), Stroke...
AEs leading to
discontinuation/dose reduction:
Cerebrovascular disorder (NOS)
Stroke
Transient ischemic attack
Neuroleptic malignant syndrome
QT interval prolonged
Tardive dyskinesia
Hyperglycemia
Dyslipidemia
Weight gain
Hyperprolactinemia
Seizures
Orthostatic hypotension
Syncope
Leukopenia
Neutropenia
Agranulocytosis
Cognitive impairment
Motor dysfunction NOS
Sources:
https://www.janssenlabels.com/package-insert/product-monograph/prescribing-information/INVEGA+SUSTENNA-pi.pdf
AEs

AEs

AESignificanceDosePopulation
Dyskinesia Disc. AE
180 mg single, oral
Overdose
Dose: 180 mg
Route: oral
Route: single
Dose: 180 mg
Sources:
https://pubmed.ncbi.nlm.nih.gov/24580061
unhealthy, 12
Health Status: unhealthy
Age Group: 12
Sex: M
Sources:
https://pubmed.ncbi.nlm.nih.gov/24580061
Dystonia Disc. AE
180 mg single, oral
Overdose
Dose: 180 mg
Route: oral
Route: single
Dose: 180 mg
Sources:
https://pubmed.ncbi.nlm.nih.gov/24580061
unhealthy, 12
Health Status: unhealthy
Age Group: 12
Sex: M
Sources:
https://pubmed.ncbi.nlm.nih.gov/24580061
Hypokalemia Disc. AE
180 mg single, oral
Overdose
Dose: 180 mg
Route: oral
Route: single
Dose: 180 mg
Sources:
https://pubmed.ncbi.nlm.nih.gov/24580061
unhealthy, 12
Health Status: unhealthy
Age Group: 12
Sex: M
Sources:
https://pubmed.ncbi.nlm.nih.gov/24580061
Lethargy Disc. AE
180 mg single, oral
Overdose
Dose: 180 mg
Route: oral
Route: single
Dose: 180 mg
Sources:
https://pubmed.ncbi.nlm.nih.gov/24580061
unhealthy, 12
Health Status: unhealthy
Age Group: 12
Sex: M
Sources:
https://pubmed.ncbi.nlm.nih.gov/24580061
Tachycardia Disc. AE
180 mg single, oral
Overdose
Dose: 180 mg
Route: oral
Route: single
Dose: 180 mg
Sources:
https://pubmed.ncbi.nlm.nih.gov/24580061
unhealthy, 12
Health Status: unhealthy
Age Group: 12
Sex: M
Sources:
https://pubmed.ncbi.nlm.nih.gov/24580061
Loss of consciousness Disc. AE
252 mg single, oral
Overdose
Dose: 252 mg
Route: oral
Route: single
Dose: 252 mg
Sources:
https://pubmed.ncbi.nlm.nih.gov/31308582
unhealthy, 16
Health Status: unhealthy
Age Group: 16
Sex: M
Sources:
https://pubmed.ncbi.nlm.nih.gov/31308582
Motor tic DLT
15 mg 1 times / day multiple, oral
Studied dose
Dose: 15 mg, 1 times / day
Route: oral
Route: multiple
Dose: 15 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/24556260
unhealthy, 30
Health Status: unhealthy
Age Group: 30
Sex: M
Sources:
https://pubmed.ncbi.nlm.nih.gov/24556260
Abnormal dreams 0.4%
Disc. AE
234 mg 2 times / month multiple, intramuscular
Recommended
Dose: 234 mg, 2 times / month
Route: intramuscular
Route: multiple
Dose: 234 mg, 2 times / month
Sources:
https://pubmed.ncbi.nlm.nih.gov/25938474
unhealthy, 37.7
Health Status: unhealthy
Age Group: 37.7
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/25938474
Agitation 0.4%
Disc. AE
234 mg 2 times / month multiple, intramuscular
Recommended
Dose: 234 mg, 2 times / month
Route: intramuscular
Route: multiple
Dose: 234 mg, 2 times / month
Sources:
https://pubmed.ncbi.nlm.nih.gov/25938474
unhealthy, 37.7
Health Status: unhealthy
Age Group: 37.7
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/25938474
Amenorrhea 0.4%
Disc. AE
234 mg 2 times / month multiple, intramuscular
Recommended
Dose: 234 mg, 2 times / month
Route: intramuscular
Route: multiple
Dose: 234 mg, 2 times / month
Sources:
https://pubmed.ncbi.nlm.nih.gov/25938474
unhealthy, 37.7
Health Status: unhealthy
Age Group: 37.7
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/25938474
Anxiety 0.4%
Disc. AE
234 mg 2 times / month multiple, intramuscular
Recommended
Dose: 234 mg, 2 times / month
Route: intramuscular
Route: multiple
Dose: 234 mg, 2 times / month
Sources:
https://pubmed.ncbi.nlm.nih.gov/25938474
unhealthy, 37.7
Health Status: unhealthy
Age Group: 37.7
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/25938474
Chest discomfort 0.4%
Disc. AE
234 mg 2 times / month multiple, intramuscular
Recommended
Dose: 234 mg, 2 times / month
Route: intramuscular
Route: multiple
Dose: 234 mg, 2 times / month
Sources:
https://pubmed.ncbi.nlm.nih.gov/25938474
unhealthy, 37.7
Health Status: unhealthy
Age Group: 37.7
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/25938474
Dizziness 0.4%
Disc. AE
234 mg 2 times / month multiple, intramuscular
Recommended
Dose: 234 mg, 2 times / month
Route: intramuscular
Route: multiple
Dose: 234 mg, 2 times / month
Sources:
https://pubmed.ncbi.nlm.nih.gov/25938474
unhealthy, 37.7
Health Status: unhealthy
Age Group: 37.7
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/25938474
Dyskinesia 0.4%
Disc. AE
234 mg 2 times / month multiple, intramuscular
Recommended
Dose: 234 mg, 2 times / month
Route: intramuscular
Route: multiple
Dose: 234 mg, 2 times / month
Sources:
https://pubmed.ncbi.nlm.nih.gov/25938474
unhealthy, 37.7
Health Status: unhealthy
Age Group: 37.7
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/25938474
Dystonia 0.4%
Disc. AE
234 mg 2 times / month multiple, intramuscular
Recommended
Dose: 234 mg, 2 times / month
Route: intramuscular
Route: multiple
Dose: 234 mg, 2 times / month
Sources:
https://pubmed.ncbi.nlm.nih.gov/25938474
unhealthy, 37.7
Health Status: unhealthy
Age Group: 37.7
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/25938474
Ejaculation failure 0.4%
Disc. AE
234 mg 2 times / month multiple, intramuscular
Recommended
Dose: 234 mg, 2 times / month
Route: intramuscular
Route: multiple
Dose: 234 mg, 2 times / month
Sources:
https://pubmed.ncbi.nlm.nih.gov/25938474
unhealthy, 37.7
Health Status: unhealthy
Age Group: 37.7
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/25938474
Extrapyramidal disorder 0.4%
Disc. AE
234 mg 2 times / month multiple, intramuscular
Recommended
Dose: 234 mg, 2 times / month
Route: intramuscular
Route: multiple
Dose: 234 mg, 2 times / month
Sources:
https://pubmed.ncbi.nlm.nih.gov/25938474
unhealthy, 37.7
Health Status: unhealthy
Age Group: 37.7
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/25938474
Galactorrhea 0.4%
Disc. AE
234 mg 2 times / month multiple, intramuscular
Recommended
Dose: 234 mg, 2 times / month
Route: intramuscular
Route: multiple
Dose: 234 mg, 2 times / month
Sources:
https://pubmed.ncbi.nlm.nih.gov/25938474
unhealthy, 37.7
Health Status: unhealthy
Age Group: 37.7
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/25938474
Gynecomastia 0.4%
Disc. AE
234 mg 2 times / month multiple, intramuscular
Recommended
Dose: 234 mg, 2 times / month
Route: intramuscular
Route: multiple
Dose: 234 mg, 2 times / month
Sources:
https://pubmed.ncbi.nlm.nih.gov/25938474
unhealthy, 37.7
Health Status: unhealthy
Age Group: 37.7
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/25938474
Insomnia 0.4%
Disc. AE
234 mg 2 times / month multiple, intramuscular
Recommended
Dose: 234 mg, 2 times / month
Route: intramuscular
Route: multiple
Dose: 234 mg, 2 times / month
Sources:
https://pubmed.ncbi.nlm.nih.gov/25938474
unhealthy, 37.7
Health Status: unhealthy
Age Group: 37.7
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/25938474
Libido decreased 0.4%
Disc. AE
234 mg 2 times / month multiple, intramuscular
Recommended
Dose: 234 mg, 2 times / month
Route: intramuscular
Route: multiple
Dose: 234 mg, 2 times / month
Sources:
https://pubmed.ncbi.nlm.nih.gov/25938474
unhealthy, 37.7
Health Status: unhealthy
Age Group: 37.7
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/25938474
Oromandibular dystonia 0.4%
Disc. AE
234 mg 2 times / month multiple, intramuscular
Recommended
Dose: 234 mg, 2 times / month
Route: intramuscular
Route: multiple
Dose: 234 mg, 2 times / month
Sources:
https://pubmed.ncbi.nlm.nih.gov/25938474
unhealthy, 37.7
Health Status: unhealthy
Age Group: 37.7
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/25938474
Paranoid schizophrenia 0.4%
Disc. AE
234 mg 2 times / month multiple, intramuscular
Recommended
Dose: 234 mg, 2 times / month
Route: intramuscular
Route: multiple
Dose: 234 mg, 2 times / month
Sources:
https://pubmed.ncbi.nlm.nih.gov/25938474
unhealthy, 37.7
Health Status: unhealthy
Age Group: 37.7
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/25938474
Semen volume decreased 0.4%
Disc. AE
234 mg 2 times / month multiple, intramuscular
Recommended
Dose: 234 mg, 2 times / month
Route: intramuscular
Route: multiple
Dose: 234 mg, 2 times / month
Sources:
https://pubmed.ncbi.nlm.nih.gov/25938474
unhealthy, 37.7
Health Status: unhealthy
Age Group: 37.7
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/25938474
Substance abuse 0.4%
Disc. AE
234 mg 2 times / month multiple, intramuscular
Recommended
Dose: 234 mg, 2 times / month
Route: intramuscular
Route: multiple
Dose: 234 mg, 2 times / month
Sources:
https://pubmed.ncbi.nlm.nih.gov/25938474
unhealthy, 37.7
Health Status: unhealthy
Age Group: 37.7
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/25938474
Suicidal ideation 0.4%
Disc. AE
234 mg 2 times / month multiple, intramuscular
Recommended
Dose: 234 mg, 2 times / month
Route: intramuscular
Route: multiple
Dose: 234 mg, 2 times / month
Sources:
https://pubmed.ncbi.nlm.nih.gov/25938474
unhealthy, 37.7
Health Status: unhealthy
Age Group: 37.7
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/25938474
Tardive dyskinesia 0.4%
Disc. AE
234 mg 2 times / month multiple, intramuscular
Recommended
Dose: 234 mg, 2 times / month
Route: intramuscular
Route: multiple
Dose: 234 mg, 2 times / month
Sources:
https://pubmed.ncbi.nlm.nih.gov/25938474
unhealthy, 37.7
Health Status: unhealthy
Age Group: 37.7
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/25938474
Akathisia 0.9%
Disc. AE
234 mg 2 times / month multiple, intramuscular
Recommended
Dose: 234 mg, 2 times / month
Route: intramuscular
Route: multiple
Dose: 234 mg, 2 times / month
Sources:
https://pubmed.ncbi.nlm.nih.gov/25938474
unhealthy, 37.7
Health Status: unhealthy
Age Group: 37.7
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/25938474
Depressive symptom 0.9%
Disc. AE
234 mg 2 times / month multiple, intramuscular
Recommended
Dose: 234 mg, 2 times / month
Route: intramuscular
Route: multiple
Dose: 234 mg, 2 times / month
Sources:
https://pubmed.ncbi.nlm.nih.gov/25938474
unhealthy, 37.7
Health Status: unhealthy
Age Group: 37.7
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/25938474
Erectile dysfunction 0.9%
Disc. AE
234 mg 2 times / month multiple, intramuscular
Recommended
Dose: 234 mg, 2 times / month
Route: intramuscular
Route: multiple
Dose: 234 mg, 2 times / month
Sources:
https://pubmed.ncbi.nlm.nih.gov/25938474
unhealthy, 37.7
Health Status: unhealthy
Age Group: 37.7
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/25938474
Headache 0.9%
Disc. AE
234 mg 2 times / month multiple, intramuscular
Recommended
Dose: 234 mg, 2 times / month
Route: intramuscular
Route: multiple
Dose: 234 mg, 2 times / month
Sources:
https://pubmed.ncbi.nlm.nih.gov/25938474
unhealthy, 37.7
Health Status: unhealthy
Age Group: 37.7
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/25938474
Injection site pain 0.9%
Disc. AE
234 mg 2 times / month multiple, intramuscular
Recommended
Dose: 234 mg, 2 times / month
Route: intramuscular
Route: multiple
Dose: 234 mg, 2 times / month
Sources:
https://pubmed.ncbi.nlm.nih.gov/25938474
unhealthy, 37.7
Health Status: unhealthy
Age Group: 37.7
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/25938474
Psychotic disorder 0.9%
Disc. AE
234 mg 2 times / month multiple, intramuscular
Recommended
Dose: 234 mg, 2 times / month
Route: intramuscular
Route: multiple
Dose: 234 mg, 2 times / month
Sources:
https://pubmed.ncbi.nlm.nih.gov/25938474
unhealthy, 37.7
Health Status: unhealthy
Age Group: 37.7
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/25938474
Weight increased 0.9%
Disc. AE
234 mg 2 times / month multiple, intramuscular
Recommended
Dose: 234 mg, 2 times / month
Route: intramuscular
Route: multiple
Dose: 234 mg, 2 times / month
Sources:
https://pubmed.ncbi.nlm.nih.gov/25938474
unhealthy, 37.7
Health Status: unhealthy
Age Group: 37.7
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/25938474
Diaphoresis Disc. AE
9 mg 1 times / day multiple, oral
Recommended
Dose: 9 mg, 1 times / day
Route: oral
Route: multiple
Dose: 9 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/24580061
unhealthy, 38
Health Status: unhealthy
Age Group: 38
Sex: M
Sources:
https://pubmed.ncbi.nlm.nih.gov/24580061
Dyskinesia Disc. AE
9 mg 1 times / day multiple, oral
Recommended
Dose: 9 mg, 1 times / day
Route: oral
Route: multiple
Dose: 9 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/24580061
unhealthy, 38
Health Status: unhealthy
Age Group: 38
Sex: M
Sources:
https://pubmed.ncbi.nlm.nih.gov/24580061
Dystonia Disc. AE
9 mg 1 times / day multiple, oral
Recommended
Dose: 9 mg, 1 times / day
Route: oral
Route: multiple
Dose: 9 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/24580061
unhealthy, 38
Health Status: unhealthy
Age Group: 38
Sex: M
Sources:
https://pubmed.ncbi.nlm.nih.gov/24580061
Tachycardia Disc. AE
9 mg 1 times / day multiple, oral
Recommended
Dose: 9 mg, 1 times / day
Route: oral
Route: multiple
Dose: 9 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/24580061
unhealthy, 38
Health Status: unhealthy
Age Group: 38
Sex: M
Sources:
https://pubmed.ncbi.nlm.nih.gov/24580061
Tremor Disc. AE
9 mg 1 times / day multiple, oral
Recommended
Dose: 9 mg, 1 times / day
Route: oral
Route: multiple
Dose: 9 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/24580061
unhealthy, 38
Health Status: unhealthy
Age Group: 38
Sex: M
Sources:
https://pubmed.ncbi.nlm.nih.gov/24580061
Agranulocytosis Disc. AE
12 mg 1 times / day multiple, oral
Recommended
Dose: 12 mg, 1 times / day
Route: oral
Route: multiple
Dose: 12 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021999s036lbl.pdf
unhealthy
Health Status: unhealthy
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021999s036lbl.pdf
Cerebrovascular disorder (NOS) Disc. AE
12 mg 1 times / day multiple, oral
Recommended
Dose: 12 mg, 1 times / day
Route: oral
Route: multiple
Dose: 12 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021999s036lbl.pdf
unhealthy
Health Status: unhealthy
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021999s036lbl.pdf
Cognitive impairment Disc. AE
12 mg 1 times / day multiple, oral
Recommended
Dose: 12 mg, 1 times / day
Route: oral
Route: multiple
Dose: 12 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021999s036lbl.pdf
unhealthy
Health Status: unhealthy
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021999s036lbl.pdf
Dyslipidemia Disc. AE
12 mg 1 times / day multiple, oral
Recommended
Dose: 12 mg, 1 times / day
Route: oral
Route: multiple
Dose: 12 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021999s036lbl.pdf
unhealthy
Health Status: unhealthy
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021999s036lbl.pdf
Hyperglycemia Disc. AE
12 mg 1 times / day multiple, oral
Recommended
Dose: 12 mg, 1 times / day
Route: oral
Route: multiple
Dose: 12 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021999s036lbl.pdf
unhealthy
Health Status: unhealthy
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021999s036lbl.pdf
Hyperprolactinemia Disc. AE
12 mg 1 times / day multiple, oral
Recommended
Dose: 12 mg, 1 times / day
Route: oral
Route: multiple
Dose: 12 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021999s036lbl.pdf
unhealthy
Health Status: unhealthy
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021999s036lbl.pdf
Intestinal stricture NOS Disc. AE
12 mg 1 times / day multiple, oral
Recommended
Dose: 12 mg, 1 times / day
Route: oral
Route: multiple
Dose: 12 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021999s036lbl.pdf
unhealthy
Health Status: unhealthy
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021999s036lbl.pdf
Leukopenia Disc. AE
12 mg 1 times / day multiple, oral
Recommended
Dose: 12 mg, 1 times / day
Route: oral
Route: multiple
Dose: 12 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021999s036lbl.pdf
unhealthy
Health Status: unhealthy
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021999s036lbl.pdf
Motor dysfunction NOS Disc. AE
12 mg 1 times / day multiple, oral
Recommended
Dose: 12 mg, 1 times / day
Route: oral
Route: multiple
Dose: 12 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021999s036lbl.pdf
unhealthy
Health Status: unhealthy
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021999s036lbl.pdf
Neuroleptic malignant syndrome Disc. AE
12 mg 1 times / day multiple, oral
Recommended
Dose: 12 mg, 1 times / day
Route: oral
Route: multiple
Dose: 12 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021999s036lbl.pdf
unhealthy
Health Status: unhealthy
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021999s036lbl.pdf
Neutropenia Disc. AE
12 mg 1 times / day multiple, oral
Recommended
Dose: 12 mg, 1 times / day
Route: oral
Route: multiple
Dose: 12 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021999s036lbl.pdf
unhealthy
Health Status: unhealthy
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021999s036lbl.pdf
Orthostatic hypotension Disc. AE
12 mg 1 times / day multiple, oral
Recommended
Dose: 12 mg, 1 times / day
Route: oral
Route: multiple
Dose: 12 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021999s036lbl.pdf
unhealthy
Health Status: unhealthy
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021999s036lbl.pdf
QT interval prolonged Disc. AE
12 mg 1 times / day multiple, oral
Recommended
Dose: 12 mg, 1 times / day
Route: oral
Route: multiple
Dose: 12 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021999s036lbl.pdf
unhealthy
Health Status: unhealthy
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021999s036lbl.pdf
Seizures Disc. AE
12 mg 1 times / day multiple, oral
Recommended
Dose: 12 mg, 1 times / day
Route: oral
Route: multiple
Dose: 12 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021999s036lbl.pdf
unhealthy
Health Status: unhealthy
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021999s036lbl.pdf
Stroke Disc. AE
12 mg 1 times / day multiple, oral
Recommended
Dose: 12 mg, 1 times / day
Route: oral
Route: multiple
Dose: 12 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021999s036lbl.pdf
unhealthy
Health Status: unhealthy
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021999s036lbl.pdf
Syncope Disc. AE
12 mg 1 times / day multiple, oral
Recommended
Dose: 12 mg, 1 times / day
Route: oral
Route: multiple
Dose: 12 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021999s036lbl.pdf
unhealthy
Health Status: unhealthy
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021999s036lbl.pdf
Tardive dyskinesia Disc. AE
12 mg 1 times / day multiple, oral
Recommended
Dose: 12 mg, 1 times / day
Route: oral
Route: multiple
Dose: 12 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021999s036lbl.pdf
unhealthy
Health Status: unhealthy
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021999s036lbl.pdf
Weight gain Disc. AE
12 mg 1 times / day multiple, oral
Recommended
Dose: 12 mg, 1 times / day
Route: oral
Route: multiple
Dose: 12 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021999s036lbl.pdf
unhealthy
Health Status: unhealthy
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021999s036lbl.pdf
Transient ischemic attack grade 3-5
Disc. AE
12 mg 1 times / day multiple, oral
Recommended
Dose: 12 mg, 1 times / day
Route: oral
Route: multiple
Dose: 12 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021999s036lbl.pdf
unhealthy
Health Status: unhealthy
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021999s036lbl.pdf
Agranulocytosis Disc. AE
234 mg 2 times / month multiple, intramuscular
Recommended
Dose: 234 mg, 2 times / month
Route: intramuscular
Route: multiple
Dose: 234 mg, 2 times / month
Sources:
https://www.janssenlabels.com/package-insert/product-monograph/prescribing-information/INVEGA+SUSTENNA-pi.pdf
unhealthy
Health Status: unhealthy
Sources:
https://www.janssenlabels.com/package-insert/product-monograph/prescribing-information/INVEGA+SUSTENNA-pi.pdf
Cerebrovascular disorder (NOS) Disc. AE
234 mg 2 times / month multiple, intramuscular
Recommended
Dose: 234 mg, 2 times / month
Route: intramuscular
Route: multiple
Dose: 234 mg, 2 times / month
Sources:
https://www.janssenlabels.com/package-insert/product-monograph/prescribing-information/INVEGA+SUSTENNA-pi.pdf
unhealthy
Health Status: unhealthy
Sources:
https://www.janssenlabels.com/package-insert/product-monograph/prescribing-information/INVEGA+SUSTENNA-pi.pdf
Cognitive impairment Disc. AE
234 mg 2 times / month multiple, intramuscular
Recommended
Dose: 234 mg, 2 times / month
Route: intramuscular
Route: multiple
Dose: 234 mg, 2 times / month
Sources:
https://www.janssenlabels.com/package-insert/product-monograph/prescribing-information/INVEGA+SUSTENNA-pi.pdf
unhealthy
Health Status: unhealthy
Sources:
https://www.janssenlabels.com/package-insert/product-monograph/prescribing-information/INVEGA+SUSTENNA-pi.pdf
Dyslipidemia Disc. AE
234 mg 2 times / month multiple, intramuscular
Recommended
Dose: 234 mg, 2 times / month
Route: intramuscular
Route: multiple
Dose: 234 mg, 2 times / month
Sources:
https://www.janssenlabels.com/package-insert/product-monograph/prescribing-information/INVEGA+SUSTENNA-pi.pdf
unhealthy
Health Status: unhealthy
Sources:
https://www.janssenlabels.com/package-insert/product-monograph/prescribing-information/INVEGA+SUSTENNA-pi.pdf
Hyperglycemia Disc. AE
234 mg 2 times / month multiple, intramuscular
Recommended
Dose: 234 mg, 2 times / month
Route: intramuscular
Route: multiple
Dose: 234 mg, 2 times / month
Sources:
https://www.janssenlabels.com/package-insert/product-monograph/prescribing-information/INVEGA+SUSTENNA-pi.pdf
unhealthy
Health Status: unhealthy
Sources:
https://www.janssenlabels.com/package-insert/product-monograph/prescribing-information/INVEGA+SUSTENNA-pi.pdf
Hyperprolactinemia Disc. AE
234 mg 2 times / month multiple, intramuscular
Recommended
Dose: 234 mg, 2 times / month
Route: intramuscular
Route: multiple
Dose: 234 mg, 2 times / month
Sources:
https://www.janssenlabels.com/package-insert/product-monograph/prescribing-information/INVEGA+SUSTENNA-pi.pdf
unhealthy
Health Status: unhealthy
Sources:
https://www.janssenlabels.com/package-insert/product-monograph/prescribing-information/INVEGA+SUSTENNA-pi.pdf
Leukopenia Disc. AE
234 mg 2 times / month multiple, intramuscular
Recommended
Dose: 234 mg, 2 times / month
Route: intramuscular
Route: multiple
Dose: 234 mg, 2 times / month
Sources:
https://www.janssenlabels.com/package-insert/product-monograph/prescribing-information/INVEGA+SUSTENNA-pi.pdf
unhealthy
Health Status: unhealthy
Sources:
https://www.janssenlabels.com/package-insert/product-monograph/prescribing-information/INVEGA+SUSTENNA-pi.pdf
Motor dysfunction NOS Disc. AE
234 mg 2 times / month multiple, intramuscular
Recommended
Dose: 234 mg, 2 times / month
Route: intramuscular
Route: multiple
Dose: 234 mg, 2 times / month
Sources:
https://www.janssenlabels.com/package-insert/product-monograph/prescribing-information/INVEGA+SUSTENNA-pi.pdf
unhealthy
Health Status: unhealthy
Sources:
https://www.janssenlabels.com/package-insert/product-monograph/prescribing-information/INVEGA+SUSTENNA-pi.pdf
Neuroleptic malignant syndrome Disc. AE
234 mg 2 times / month multiple, intramuscular
Recommended
Dose: 234 mg, 2 times / month
Route: intramuscular
Route: multiple
Dose: 234 mg, 2 times / month
Sources:
https://www.janssenlabels.com/package-insert/product-monograph/prescribing-information/INVEGA+SUSTENNA-pi.pdf
unhealthy
Health Status: unhealthy
Sources:
https://www.janssenlabels.com/package-insert/product-monograph/prescribing-information/INVEGA+SUSTENNA-pi.pdf
Neutropenia Disc. AE
234 mg 2 times / month multiple, intramuscular
Recommended
Dose: 234 mg, 2 times / month
Route: intramuscular
Route: multiple
Dose: 234 mg, 2 times / month
Sources:
https://www.janssenlabels.com/package-insert/product-monograph/prescribing-information/INVEGA+SUSTENNA-pi.pdf
unhealthy
Health Status: unhealthy
Sources:
https://www.janssenlabels.com/package-insert/product-monograph/prescribing-information/INVEGA+SUSTENNA-pi.pdf
Orthostatic hypotension Disc. AE
234 mg 2 times / month multiple, intramuscular
Recommended
Dose: 234 mg, 2 times / month
Route: intramuscular
Route: multiple
Dose: 234 mg, 2 times / month
Sources:
https://www.janssenlabels.com/package-insert/product-monograph/prescribing-information/INVEGA+SUSTENNA-pi.pdf
unhealthy
Health Status: unhealthy
Sources:
https://www.janssenlabels.com/package-insert/product-monograph/prescribing-information/INVEGA+SUSTENNA-pi.pdf
QT interval prolonged Disc. AE
234 mg 2 times / month multiple, intramuscular
Recommended
Dose: 234 mg, 2 times / month
Route: intramuscular
Route: multiple
Dose: 234 mg, 2 times / month
Sources:
https://www.janssenlabels.com/package-insert/product-monograph/prescribing-information/INVEGA+SUSTENNA-pi.pdf
unhealthy
Health Status: unhealthy
Sources:
https://www.janssenlabels.com/package-insert/product-monograph/prescribing-information/INVEGA+SUSTENNA-pi.pdf
Seizures Disc. AE
234 mg 2 times / month multiple, intramuscular
Recommended
Dose: 234 mg, 2 times / month
Route: intramuscular
Route: multiple
Dose: 234 mg, 2 times / month
Sources:
https://www.janssenlabels.com/package-insert/product-monograph/prescribing-information/INVEGA+SUSTENNA-pi.pdf
unhealthy
Health Status: unhealthy
Sources:
https://www.janssenlabels.com/package-insert/product-monograph/prescribing-information/INVEGA+SUSTENNA-pi.pdf
Stroke Disc. AE
234 mg 2 times / month multiple, intramuscular
Recommended
Dose: 234 mg, 2 times / month
Route: intramuscular
Route: multiple
Dose: 234 mg, 2 times / month
Sources:
https://www.janssenlabels.com/package-insert/product-monograph/prescribing-information/INVEGA+SUSTENNA-pi.pdf
unhealthy
Health Status: unhealthy
Sources:
https://www.janssenlabels.com/package-insert/product-monograph/prescribing-information/INVEGA+SUSTENNA-pi.pdf
Syncope Disc. AE
234 mg 2 times / month multiple, intramuscular
Recommended
Dose: 234 mg, 2 times / month
Route: intramuscular
Route: multiple
Dose: 234 mg, 2 times / month
Sources:
https://www.janssenlabels.com/package-insert/product-monograph/prescribing-information/INVEGA+SUSTENNA-pi.pdf
unhealthy
Health Status: unhealthy
Sources:
https://www.janssenlabels.com/package-insert/product-monograph/prescribing-information/INVEGA+SUSTENNA-pi.pdf
Tardive dyskinesia Disc. AE
234 mg 2 times / month multiple, intramuscular
Recommended
Dose: 234 mg, 2 times / month
Route: intramuscular
Route: multiple
Dose: 234 mg, 2 times / month
Sources:
https://www.janssenlabels.com/package-insert/product-monograph/prescribing-information/INVEGA+SUSTENNA-pi.pdf
unhealthy
Health Status: unhealthy
Sources:
https://www.janssenlabels.com/package-insert/product-monograph/prescribing-information/INVEGA+SUSTENNA-pi.pdf
Transient ischemic attack Disc. AE
234 mg 2 times / month multiple, intramuscular
Recommended
Dose: 234 mg, 2 times / month
Route: intramuscular
Route: multiple
Dose: 234 mg, 2 times / month
Sources:
https://www.janssenlabels.com/package-insert/product-monograph/prescribing-information/INVEGA+SUSTENNA-pi.pdf
unhealthy
Health Status: unhealthy
Sources:
https://www.janssenlabels.com/package-insert/product-monograph/prescribing-information/INVEGA+SUSTENNA-pi.pdf
Weight gain Disc. AE
234 mg 2 times / month multiple, intramuscular
Recommended
Dose: 234 mg, 2 times / month
Route: intramuscular
Route: multiple
Dose: 234 mg, 2 times / month
Sources:
https://www.janssenlabels.com/package-insert/product-monograph/prescribing-information/INVEGA+SUSTENNA-pi.pdf
unhealthy
Health Status: unhealthy
Sources:
https://www.janssenlabels.com/package-insert/product-monograph/prescribing-information/INVEGA+SUSTENNA-pi.pdf
Overview

Overview

CYP3A4CYP2C9CYP2D6hERG
substrate
1946

inhibitor
2252
inhibitor
2438
substrate
1388

inhibitor
2507
inhibitor
2217

OverviewOther

Other InhibitorOther SubstrateOther Inducer
CYP1A2
2153

CYP2A6
879

CYP2C8
1057

CYP4A
20

CYP2E1
1060

P-gp
1741
UGT1A1
479

UGT1A6
343

BCRP
697

P-gp
2052
Drug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
CYP2D6
2546
 no [IC50 61.9 uM]
no (co-administration study)
Comment: examination of inhibition by paliperidone using CYP isozyme probe detromethorphan
Page: 41, 81
CYP2A6
911
 no [Inhibition >30 uM]
no (co-administration study)
Comment: examination of inhibition by paliperidone using CYP isozyme probe coumarin
Page: 41, 81
CYP2E1
1146
 no [Inhibition >30 uM]
no (co-administration study)
Comment: examination of inhibition by paliperidone using CYP isozyme probe chlorzoxazone
Page: 41, 81
CYP4A
34
 no [Inhibition >30 uM]
no (co-administration study)
Comment: examination of inhibition by paliperidone using CYP isozyme probe lauric acid
Page: 41, 81
CYP1A2
2333
 no [Inhibition >60 uM]
no (co-administration study)
Comment: examination of inhibition by paliperidone using CYP isozyme probe Caffeine
Page: 41, 81
CYP2C8
1117
 no [Inhibition >60 uM]
no (co-administration study)
Comment: examination of inhibition by paliperidone using CYP isozyme probe phenytoin
Page: 41, 81
CYP2C9
2497
 no [Inhibition >60 uM]
no (co-administration study)
Comment: examination of inhibition by paliperidone using CYP isozyme probe phenytoin
Page: 41, 81
CYP3A4
2633
 no [Inhibition >60 uM]
no (co-administration study)
Comment: examination of inhibition by paliperidone using CYP isozyme probe testosterone
Page: 41, 81
P-gp
1932
 weak [IC50 63.26 uM]
Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
BCRP
697
 yes
CYP2D6
1388
 yes
CYP3A4
1946
 yes
P-gp
2052
 yes
UGT1A1
479
 yes
UGT1A6
343
 yes
Tox targets

Tox targets

TargetModalityActivityMetaboliteClinical evidence
hERG
2263
Sourcing

Sourcing

Vendor/AggregatorIDURL
001 Chemical
DY10226
https://www.001chemical.com/chem/144598-75-4
3B Scientific (Wuhan) Corp
3B3-032531
http://www.3bsc.com/index/pro_info.php?id=53795
AA Blocks
AA001JQR
https://www.aablocks.com/goods/Goods/detail?id=AA001JQR
Aaron Chemicals
AR001KIJ
http://www.aaronchem.com/144598-75-4
abcr GmbH
AB457979
http://www.abcr.com/shop/en/AB457979
AbMole Bioscience
M5848
http://www.abmole.com/products/paliperidone.html
Acadechem
ACDC-030009
http://acadechemical.com/product/1779
Aceschem
ACF023126
https://www.aceschem.com/catalog/144598-75-4.html
Achemo Scientific Limited
AC-64208
http://www.achemo.com/search/?Keyword= 144598-75-4
Achemtek
0102-022120
http://www.achemtek.com/144598-75-4
Acorn PharmaTech
ACN-050765
http://www.acornpharmatech.com/
Acros Organics
AC456250010
https://www.fishersci.com/shop/products/9-hydroxyrisperidone-98-acros-organics/AC456250010
Active Biopharma
ABP000395
http://www.activebiopharma.com/144598-75-4
AHH Chemical co.,ltd
MT-01921
http://www.ahhchemical.com/product/MT-01921.html
AK Scientific, Inc. (AKSCI)
J10457
http://www.aksci.com/item_detail.php?cat=J10457
AK Scientific, Inc. (AKSCI)
S451
http://www.aksci.com/item_detail.php?cat=S451
Alfa Chemistry
AP1020719554
https://reagents.alfa-chemistry.com/product/9-hydroxyrisperidone-d4-solution-cas-1020719-55-4-756.html
Alsachim
1560
http://www.alsachim.com/product-C2633-glo.bal-view.html
Ambinter
Amb19132718
http://www.ambinter.com/reference/19132718
Angel Pharmatech
AG-11540
http://www.angelpharmatech.com/144598-75-4.html
Angene
AGN-PC-04XSV9
http://www.angenechemical.com/productshow/AGN-PC-04XSV9.html
Anward
ANW-42875
http://www.anward.com/pro_result/28250
Ark Pharm
AK-77508
http://www.arkpharminc.com/products/144598-75-4.html
Aurora Fine Chemicals LLC
A13.105.665
http://online.aurorafinechemicals.com/info?ID=A13.105.665
Aurum Pharmatech LLC
Q-4343
http://www.Aurumpharmatech.com/Product/ProductDetails/Q_4343
AvaChem Scientific
2244
http://www.avachem.com/productSearch.asp?2244
BioChemPartner
BCP02338
http://www.biochempartner.com/144598-75-4-BCP02338
BioCrick
BCC3834
http://www.biocrick.com/Paliperidone-BCC3834.html
BioSynth
Q-101425
https://www.biosynth.com/en/products/life-science/other-biochemicals/products/Q-101425.html
BLD Pharm
BD111798
http://www.bldpharm.com/products/144598-75-4.html
BOC Sciences
130049-85-3
https://www.bocsci.com/r-9-hydroxy-risperidone-r-paliperidone-cas-130049-85-3-item-262137.html
BOC Sciences
147663-01-2
https://www.bocsci.com/s-9-hydroxy-risperidone-s-paliperidone-cas-147663-01-2-item-262138.html
Boerchem
BC228519
http://www.boerchem.com/?product_38518.html
Boerchem
BC677689
http://www.boerchem.com/?product_42087.html
Chem Scene
CS-0386
http://www.chemscene.com/144598-75-4.html
Chemenu
CM110058
http://www.chemenu.com/products/CM110058
ChemMol
30108656
http://www.chemmol.com/chemmol/30108656.html
ChemMol
44008670
http://www.chemmol.com/chemmol/44008670.html
ChemMol
44009994
http://www.chemmol.com/chemmol/44009994.html
ChemMol
49400035
http://www.chemmol.com/chemmol/49400035.html
ChemMol
81412039
http://www.chemmol.com/chemmol/81412039.html
Chemspace
CSSB00000693926
https://chem-space.com/CSSB00000693926
Clearsynth
CS-EB-01587
https://www.clearsynth.com/en/CSEB01587.html
Clearsynth
CS-ER-01579
https://www.clearsynth.com/en/CSER01579.html
Clearsynth
CS-O-02070
https://www.clearsynth.com/en/CSO02070.html
Combi-Blocks
OR-2275
http://www.combi-blocks.com/cgi-bin/find.cgi?OR-2275
Coresyn
CM14424
http://www.coresyn.com/Cas144598-75-4.html
CSNpharm
CSN10189
https://www.csnpharm.com/products/paliperidone.html
DAOGE BIOPHARMA
DG21-12007
https://www.daogechem.com/product/144598-75-4.html
eNovation Chemicals
D522284
http://www.enovationchem.com/productDetails.asp?productID=D522284
Finetech
FT-0600425
http://www.finetechnology-ind.com/prod/detail/pub/144598-75-4.html
Finetech
FT-0670101
http://www.finetechnology-ind.com/prod/detail/pub/1020719-55-4.html
Finetech
FT-0670102
http://www.finetechnology-ind.com/prod/detail/pub/130049-85-3.html
Fluoropharm
YF10040
http://www.fluoropharm.com/product/YF10040.html
Glentham Life Sciences
GP3914
http://www.glentham.com/products/product/GP3914/
Hello Bio
HB1798
https://www.hellobio.com/paliperidone.html
iChemical
EBD54215
http://www.ichemical.com/products/144598-75-4.html?utm_source=PubChem&utm_medium=website&utm_campaign=product%20catalogs
Lab Network
LN00188652
https://labnetwork.com/frontend-app/p/#!/moleculedetails/LN00188652
LGC Standards
LGCAMP0491.03-01
https://www.lgcstandards.com/US/en/p/LGCAMP0491.03-01
LGC Standards
LGCFOR0491.03
https://www.lgcstandards.com/US/en/p/LGCFOR0491.03
LGC Standards
MM0491.03
https://www.lgcstandards.com/US/en/p/MM0491.03
Matrix Scientific
125342
https://www.matrixscientific.com/125342.html
mcule
MCULE-5597043685
https://mcule.com/MCULE-5597043685/
MedChem Express
HY-A0019
https://www.medchemexpress.com/Paliperidone.html
Molcore
MC10226
https://www.molcore.com/product/144598-75-4
MolPort
MolPort-020-313-413
https://www.molport.com/shop/molecule-link/MolPort-020-313-413
MuseChem
A000313
https://www.musechem.com/product/A000313.html
OChem
22777
http://www.ocheminc.com/index.php?act=psearch&pid=598P754
Renno Tech
RL01805
http://www.rennotech.com/product_show.asp?id=2054
Shanghai Send Pharmaceutical Technology Co., Ltd
send21033
http://shsendpharm.com/
Sigma-Aldrich
1491809_USP
https://www.sigmaaldrich.com/catalog/product/usp/1491809?utm_source=pubchem&utm_campaign=pubchem_2017&utm_medium=referral
Sigma-Aldrich
H-076_CERILLIAN
https://www.sigmaaldrich.com/catalog/product/cerillian/h076?utm_source=pubchem&utm_campaign=pubchem_2017&utm_medium=referral
Sigma-Aldrich
P0099_SIGMA
https://www.sigmaaldrich.com/catalog/product/sigma/p0099?utm_source=pubchem&utm_campaign=pubchem_2017&utm_medium=referral
Smolecule
S538546
http://www.smolecule.com/products/s538546
Synblock Inc
PB27526
http://www.synblock.com/product/144598-75-4.html
TCI (Tokyo Chemical Industry)
P1897
http://www.tcichemicals.com/eshop/en/us/commodity/P1897/index.html
THE BioTek
bt-278646
https://www.thebiotek.com/product/inhibitors/bt-278646
THE BioTek
bt-318627
https://www.thebiotek.com/product/others/bt-318627
Tocris
4493
https://www.tocris.com/products/paliperidone_4493
VladaChem
VL281908-10MG
https://www.vladachem.com/product.php?products=144598-75-4
Yuhao Chemical
M0403394
http://www.chemyuhao.com/144598-75-4.html
PubMed

PubMed

TitleDatePubMed
Possible relationship between combined plasma concentrations of risperidone plus 9-hydroxyrisperidone and extrapyramidal symptoms. Preliminary study.
2001
Effects of two atypical neuroleptics, olanzapine and risperidone, on the function of the urinary bladder and the external urethral sphincter in anesthetized rats.
2001
Relationship between plasma risperidone and 9-hydroxyrisperidone concentrations and clinical response in patients with schizophrenia.
2001 Jan 1
Different enantioselective 9-hydroxylation of risperidone by the two human CYP2D6 and CYP3A4 enzymes.
2001 Oct
The effect of fluoxetine on the pharmacokinetics and safety of risperidone in psychotic patients.
2002 Mar
Three-dimensional quantitative structure-activity relationship for inhibition of human ether-a-go-go-related gene potassium channel.
2002 May
Effects of CYP2D6 genotypes on plasma concentrations of risperidone and enantiomers of 9-hydroxyrisperidone in Japanese patients with schizophrenia.
2003 Feb
Correlation between scores on Continuous Performance Test and plasma concentration for schizophrenic patients on risperidone.
2004 Apr
Risperidone plasma levels, clinical response and side-effects.
2005 Aug
Dose-dependent interaction of paroxetine with risperidone in schizophrenic patients.
2005 Dec
Effect of verapamil on pharmacokinetics and pharmacodynamics of risperidone: in vivo evidence of involvement of P-glycoprotein in risperidone disposition.
2005 Jul
Predominant role of the 9-hydroxy metabolite of risperidone in elevating blood prolactin levels.
2005 May
Cytochrome P450 3A inhibitor itraconazole affects plasma concentrations of risperidone and 9-hydroxyrisperidone in schizophrenic patients.
2005 Nov
P-glycoprotein interaction with risperidone and 9-OH-risperidone studied in vitro, in knock-out mice and in drug-drug interaction experiments.
2005 Oct
Pharmacokinetic profile of long-acting injectable risperidone at steady-state: comparison with oral administration.
2005 Sep-Oct
Membrane transporter proteins: a challenge for CNS drug development.
2006
[Paliperidone].
2006 Aug
Serum concentrations of risperidone and 9-OH risperidone following intramuscular injection of long-acting risperidone compared with oral risperidone medication.
2006 Jul
[Trazodone for the treatment of behavioral and psychological symptoms of dementia (BPSD) in Alzheimer's disease: a retrospective study focused on the aggression and negativism in caregiving situations].
2006 Jun
A PET study evaluating dopamine D2 receptor occupancy for long-acting injectable risperidone.
2006 Mar
Multiple dose pharmacokinetics of risperidone and 9-hydroxyrisperidone in Chinese female patients with schizophrenia.
2006 Mar
Intestinal uptake and biodistribution of novel polymeric micelles after oral administration.
2006 Mar 10
Optimization of the separation of some psychotropic drugs and their respective metabolites by liquid chromatography.
2006 May 3
Effect of adjunctive lamotrigine treatment on the plasma concentrations of clozapine, risperidone and olanzapine in patients with schizophrenia or bipolar disorder.
2006 Oct
Paliperidone: quo vadis?
2007 Apr
Risperidone and paliperidone inhibit p-glycoprotein activity in vitro.
2007 Apr
Paliperidone extended-release tablets for prevention of symptom recurrence in patients with schizophrenia: a randomized, double-blind, placebo-controlled study.
2007 Feb
Treatment of schizophrenia with paliperidone extended-release tablets: a 6-week placebo-controlled trial.
2007 Feb
FDA approves new antipsychotic.
2007 Feb 1
Valproic acid improves psychotic agitation without influencing plasma risperidone levels in schizophrenic patients.
2007 Jan
Maintenance therapy with once-monthly administration of long-acting injectable risperidone in patients with schizophrenia or schizoaffective disorder: a pilot study of an extended dosing interval.
2007 Jan 29
Efficacy, safety and early response of paliperidone extended-release tablets (paliperidone ER): results of a 6-week, randomized, placebo-controlled study.
2007 Jul
Molecule of the month. Paliperidone.
2007 Jun
Determination of risperidone and enantiomers of 9-hydroxyrisperidone in plasma by LC-MS/MS.
2007 Jun 1
Paliperidone (Invega) for schizophrenia.
2007 Mar 12
A study of genetic (CYP2D6 and ABCB1) and environmental (drug inhibitors and inducers) variables that may influence plasma risperidone levels.
2007 May
Paliperidone extended-release tablets: a new atypical antipsychotic.
2007 May
Sensitive liquid chromatography/tandem mass spectrometry method for the simultaneous determination of olanzapine, risperidone, 9-hydroxyrisperidone, clozapine, haloperidol and ziprasidone in rat brain tissue.
2007 Oct 15
Absorption, metabolism, and excretion of paliperidone, a new monoaminergic antagonist, in humans.
2008 Apr
Paliperidone extended-release tablets for the acute and maintenance treatment of schizophrenia.
2008 Feb
Paliperidone-ER: first atypical antipsychotic with oral extended release formulation.
2008 Feb
Paliperidone for treatment of schizophrenia.
2008 May
Secondary delusional parasitosis treated with paliperidone.
2009 Apr
Paliperidone suppresses the development of the aggressive phenotype in a developmentally sensitive animal model of escalated aggression.
2009 May
Inhibition of cloned hERG potassium channels by risperidone and paliperidone.
2017 Jun
Patents

Patents

20020146456
3

Sample Use Guides

In Vivo Use Guide
In adults is 6 mg administered once daily In adolescents 12-17 years of age is 3 mg administered once daily
Route of Administration: Oral
In Vitro Use Guide
Paliperidone has dual hyperprolactinemic actions in lactotrophs i) by preserving the coupling of spontaneous electrical activity and prolactin secretion in the presence of dopamine and ii) by inhibiting intrinsic dopamine receptor activity in the absence of dopamine, leading to enhanced calcium signaling and secretion.
Substance Class Chemical
Created
by admin
on Mon Mar 31 18:24:10 GMT 2025
Edited
by admin
on Mon Mar 31 18:24:10 GMT 2025
Record UNII
838F01T721
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
PALIPERIDONE
EMA EPAR   INN   JAN   MART.   MI   ORANGE BOOK   USAN   USP-RS   VANDF   WHO-DD  
INN   USAN  
Official Name English
INVEGA
Preferred Name English
PALIPERIDONE [USAN]
Common Name English
4H-PYRIDO(1,2-A)PYRIMIDIN-4-ONE, 3-(2-(4-(6-FLUORO-1,2-BENZISOXAZOL-3-YL)-1-PIPERIDINYL)ETHYL)-6,7,8,9-TETRAHYDRO-9-HYDROXY-2-METHYL-
Systematic Name English
3-(2-(4-(6-FLUORO-1,2-BENZISOXAZOL-3-YL)-1-PIPERIDINYL)ETHYL)-6,7,8,9-TETRAHYDRO-9-HYDROXY-2-METHYL-4H-PYRIDO(1,2-A)PYRIMIDIN-4-ONE
Systematic Name English
PALIPERIDONE [USP MONOGRAPH]
Common Name English
PALIPERIDONE [MART.]
Common Name English
PALIPERIDONE [EMA EPAR]
Common Name English
RISPERIDONE IMPURITY C [EP IMPURITY]
Common Name English
9-HYDROXYRISPERIDONE
Common Name English
RO76477
Code English
paliperidone [INN]
Common Name English
PALIPERIDONE [VANDF]
Common Name English
(9RS)-3-[2-[4-(6-Fluoro-1,2-benzisoxazol-3-yl)piperidin-1-yl]]ethyl]-9-hydroxy-2-methyl-6,7,8,9-tetrahydro-4H-pyrido[1,2-a]pyrimidin-4-one
Common Name English
NSC-759623
Code English
PALIPERIDONE [ORANGE BOOK]
Common Name English
RISPERIDONE IMPURITY, 9-HYDROXYRISPERIDONE- [USP IMPURITY]
Common Name English
PALIPERIDONE [USP-RS]
Common Name English
PALIPERIDONE [MI]
Common Name English
Paliperidone [WHO-DD]
Common Name English
R-76477
Code English
RO-76477
Code English
PALIPERIDONE [JAN]
Common Name English
Classification Tree Code System Code
WHO-ATC N05AX13
Created by admin on Mon Mar 31 18:24:10 GMT 2025 , Edited by admin on Mon Mar 31 18:24:10 GMT 2025
WHO-VATC QN05AX13
Created by admin on Mon Mar 31 18:24:10 GMT 2025 , Edited by admin on Mon Mar 31 18:24:10 GMT 2025
LIVERTOX NBK548506
Created by admin on Mon Mar 31 18:24:10 GMT 2025 , Edited by admin on Mon Mar 31 18:24:10 GMT 2025
NDF-RT N0000175430
Created by admin on Mon Mar 31 18:24:10 GMT 2025 , Edited by admin on Mon Mar 31 18:24:10 GMT 2025
EMA ASSESSMENT REPORTS INVEGA (AUTHORIZED: PSYCHOTIC DISORDERS)
Created by admin on Mon Mar 31 18:24:10 GMT 2025 , Edited by admin on Mon Mar 31 18:24:10 GMT 2025
EMA ASSESSMENT REPORTS INVEGA (AUTHORIZED: SCHIZOPHRENIA)
Created by admin on Mon Mar 31 18:24:10 GMT 2025 , Edited by admin on Mon Mar 31 18:24:10 GMT 2025
NCI_THESAURUS C66883
Created by admin on Mon Mar 31 18:24:10 GMT 2025 , Edited by admin on Mon Mar 31 18:24:10 GMT 2025
Code System Code Type Description
DRUG CENTRAL
4137
Created by admin on Mon Mar 31 18:24:10 GMT 2025 , Edited by admin on Mon Mar 31 18:24:10 GMT 2025
PRIMARY
LACTMED
Paliperidone
Created by admin on Mon Mar 31 18:24:10 GMT 2025 , Edited by admin on Mon Mar 31 18:24:10 GMT 2025
PRIMARY
ChEMBL
CHEMBL1621
Created by admin on Mon Mar 31 18:24:10 GMT 2025 , Edited by admin on Mon Mar 31 18:24:10 GMT 2025
PRIMARY
EPA CompTox
DTXSID7049059
Created by admin on Mon Mar 31 18:24:10 GMT 2025 , Edited by admin on Mon Mar 31 18:24:10 GMT 2025
PRIMARY
RS_ITEM_NUM
1491809
Created by admin on Mon Mar 31 18:24:10 GMT 2025 , Edited by admin on Mon Mar 31 18:24:10 GMT 2025
PRIMARY
WIKIPEDIA
PALIPERIDONE
Created by admin on Mon Mar 31 18:24:10 GMT 2025 , Edited by admin on Mon Mar 31 18:24:10 GMT 2025
PRIMARY
DRUG BANK
DB01267
Created by admin on Mon Mar 31 18:24:10 GMT 2025 , Edited by admin on Mon Mar 31 18:24:10 GMT 2025
PRIMARY
USAN
QQ-13
Created by admin on Mon Mar 31 18:24:10 GMT 2025 , Edited by admin on Mon Mar 31 18:24:10 GMT 2025
PRIMARY
INN
7977
Created by admin on Mon Mar 31 18:24:10 GMT 2025 , Edited by admin on Mon Mar 31 18:24:10 GMT 2025
PRIMARY
DAILYMED
838F01T721
Created by admin on Mon Mar 31 18:24:10 GMT 2025 , Edited by admin on Mon Mar 31 18:24:10 GMT 2025
PRIMARY
CAS
144598-75-4
Created by admin on Mon Mar 31 18:24:10 GMT 2025 , Edited by admin on Mon Mar 31 18:24:10 GMT 2025
PRIMARY
SMS_ID
100000092109
Created by admin on Mon Mar 31 18:24:10 GMT 2025 , Edited by admin on Mon Mar 31 18:24:10 GMT 2025
PRIMARY
IUPHAR
7258
Created by admin on Mon Mar 31 18:24:10 GMT 2025 , Edited by admin on Mon Mar 31 18:24:10 GMT 2025
PRIMARY
PUBCHEM
115237
Created by admin on Mon Mar 31 18:24:10 GMT 2025 , Edited by admin on Mon Mar 31 18:24:10 GMT 2025
PRIMARY
RXCUI
679314
Created by admin on Mon Mar 31 18:24:10 GMT 2025 , Edited by admin on Mon Mar 31 18:24:10 GMT 2025
PRIMARY RxNorm
NCI_THESAURUS
C66293
Created by admin on Mon Mar 31 18:24:10 GMT 2025 , Edited by admin on Mon Mar 31 18:24:10 GMT 2025
PRIMARY
FDA UNII
838F01T721
Created by admin on Mon Mar 31 18:24:10 GMT 2025 , Edited by admin on Mon Mar 31 18:24:10 GMT 2025
PRIMARY
EVMPD
SUB23268
Created by admin on Mon Mar 31 18:24:10 GMT 2025 , Edited by admin on Mon Mar 31 18:24:10 GMT 2025
PRIMARY
MERCK INDEX
m8357
Created by admin on Mon Mar 31 18:24:10 GMT 2025 , Edited by admin on Mon Mar 31 18:24:10 GMT 2025
PRIMARY Merck Index
CHEBI
82978
Created by admin on Mon Mar 31 18:24:10 GMT 2025 , Edited by admin on Mon Mar 31 18:24:10 GMT 2025
PRIMARY
NSC
759623
Created by admin on Mon Mar 31 18:24:10 GMT 2025 , Edited by admin on Mon Mar 31 18:24:10 GMT 2025
PRIMARY
HSDB
8148
Created by admin on Mon Mar 31 18:24:10 GMT 2025 , Edited by admin on Mon Mar 31 18:24:10 GMT 2025
PRIMARY
Related Record Type Details
MUSCARINIC ACETYLCHOLINE RECEPTOR M3
OFF-TARGET->NON-INHIBITOR
NON-INHIBITOR
Ki
CYTOCHROME P450 2D6
METABOLIC ENZYME -> SUBSTRATE
HISTAMINE H1 RECEPTOR
TARGET -> INHIBITOR
INHIBITOR
Ki
ALPHA-1A ADRENERGIC RECEPTOR
TARGET -> INHIBITOR
INHIBITOR
Ki
MUSCARINIC ACETYLCHOLINE RECEPTOR M5
OFF TARGET->NON-INHIBITOR
NON-INHIBITOR
Ki
D(4) DOPAMINE RECEPTOR
TARGET -> INHIBITOR
INHIBITOR
Ki
ALPHA-2C ADRENERGIC RECEPTOR
TARGET -> INHIBITOR
INHIBITOR
Ki
Structure of PALIPERIDONE
EXCRETED UNCHANGED
AMOUNT EXCRETED
URINE
5-HYDROXYTRYPTAMINE RECEPTOR 1D
TARGET -> INHIBITOR
INHIBITOR
Ki
HISTAMINE H2 RECEPTOR
TARGET->WEAK INHIBITOR
INHIBITOR
Ki
5-HYDROXYTRYPTAMINE RECEPTOR 2A
TARGET -> INHIBITOR
INHIBITOR
Ki
5-HYDROXYTRYPTAMINE RECEPTOR 1E
TARGET -> INHIBITOR
INHIBITOR
Ki
MUSCARINIC ACETYLCHOLINE RECEPTOR M4
OFF TARGET->NON-INHIBITOR
NON-INHIBITOR
Ki
D(2) DOPAMINE RECEPTOR
TARGET -> INHIBITOR
INHIBITOR
Ki
5-HYDROXYTRYPTAMINE RECEPTOR 5A
TARGET -> INHIBITOR
INHIBITOR
Ki
MULTIDRUG RESISTANCE PROTEIN 1
TRANSPORTER -> SUBSTRATE
TRANSPORTER
IC50
MUSCARINIC ACETYLCHOLINE RECEPTOR M2
OFF TARGET->NON-INHIBITOR
NON-INHIBITOR
Ki
PLASMA PROTEIN FRACTION (HUMAN)
BINDER->LIGAND
Structure of Paliperidone monohydrochloride
SALT/SOLVATE -> PARENT
5-HYDROXYTRYPTAMINE RECEPTOR 4
TARGET -> INHIBITOR
INHIBITOR
Ki
ALPHA-2B ADRENERGIC RECEPTOR
TARGET -> INHIBITOR
INHIBITOR
Ki
5-HYDROXYTRYPTAMINE RECEPTOR 1A
TARGET -> INHIBITOR
INHIBITOR
Ki
D(1B) DOPAMINE RECEPTOR
TARGET -> INHIBITOR
INHIBITOR
Ki
MUSCARINIC ACETYLCHOLINE RECEPTOR M1
OFF TARGET->NON-INHIBITOR
NON-INHIBITOR
Ki
5-HYDROXYTRYPTAMINE RECEPTOR 7
TARGET -> INHIBITOR
INHIBITOR
Ki
5-HYDROXYTRYPTAMINE RECEPTOR 6
TARGET -> INHIBITOR
INHIBITOR
Ki
CYTOCHROME P450 3A4
METABOLIC ENZYME -> SUBSTRATE
5-HYDROXYTRYPTAMINE RECEPTOR 1B
TARGET -> INHIBITOR
INHIBITOR
Ki
5-HYDROXYTRYPTAMINE RECEPTOR 2C
TARGET -> INHIBITOR
INHIBITOR
Ki
D(3) DOPAMINE RECEPTOR
TARGET -> INHIBITOR
INHIBITOR
Ki
Related Record Type Details
Structure of R-93725
METABOLITE -> PARENT
Trace in feces
URINE
Structure of R-84852
METABOLITE -> PARENT
FECAL
Structure of Paliperidone ketone
METABOLITE -> PARENT
URINE
Structure of RISPERIDONE
PARENT -> METABOLITE ACTIVE
Related Record Type Details
Structure of 3-(2-CHLOROETHYL)-2-METHYL-9-HYDROXY-6,7,8,9-TETRAHYDRO-4H-PYRIDO (1,2-A) PYRIMIDIN-4-ONE
IMPURITY -> PARENT
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
Structure of 6,7,8,9-TETRAHYDRO-9-HYDROXY-3-(2-HYDROXYETHYL)-2-METHYL-4H-PYRIDO(1,2-A)PYRIMIDIN-4-ONE
IMPURITY -> PARENT
Structure of R-84852
IMPURITY -> PARENT
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
Structure of 3-ETHYL-6,7,8,9-TETRAHYDRO-9-HYDROXY-2-METHYL-4H-PYRIDO(1,2-A)PYRIMIDIN-4-ONE
IMPURITY -> PARENT
Structure of R-56109
IMPURITY -> PARENT
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
Structure of Paliperidone ketone
IMPURITY -> PARENT
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
Structure of RISPERIDONE
PARENT -> IMPURITY
Related Record Type Details
Structure of PALIPERIDONE
ACTIVE MOIETY
Name Property Type Amount Referenced Substance Defining Parameters References
ORAL BIOAVAILABILITY PHARMACOKINETIC
Biological Half-life PHARMACOKINETIC
Volume of Distribution PHARMACOKINETIC
Tmax PHARMACOKINETIC
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