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
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
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 | ( + / - ) |
DescriptionCurator's Comment: description was created based on several sources, including
http://dx.doi.org/10.4172/2161-1459.1000117
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
Sources: https://www.ncbi.nlm.nih.gov/pubmed/23861636
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.
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL217 Sources: https://www.ncbi.nlm.nih.gov/pubmed/7520908 |
|||
Target ID: CHEMBL224 Sources: https://www.ncbi.nlm.nih.gov/pubmed/7542676 |
|||
Target ID: CHEMBL240 Sources: https://www.ncbi.nlm.nih.gov/pubmed/28265686 |
0.57 µM [IC50] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | INVEGA Approved UseINVEGA SUSTENNA® (paliperidone palmitate) is indicated for the treatment of: Schizophrenia [see Clinical Studies 14.1 Launch Date2006 |
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
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 |
|
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 |
AUC
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
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 |
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 |
|
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 |
T1/2
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
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 |
|
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 |
|
23 h |
single, oral |
PALIPERIDONE plasma | Homo sapiens population: UNKNOWN age: ADULT sex: UNKNOWN food status: UNKNOWN |
Funbound
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
26% |
single, oral |
PALIPERIDONE plasma | Homo sapiens population: UNKNOWN age: ADULT sex: UNKNOWN food status: UNKNOWN |
Doses
Dose | Population | Adverse events |
---|---|---|
180 mg single, oral Overdose Dose: 180 mg Route: oral Route: single Dose: 180 mg Sources: Page: p.210 |
unhealthy, 12 n = 1 Health Status: unhealthy Condition: Developmental delay Age Group: 12 Sex: M Population Size: 1 Sources: Page: p.210 |
Disc. AE: Lethargy, Tachycardia... AEs leading to discontinuation/dose reduction: Lethargy Sources: Page: p.210Tachycardia Hypokalemia Dyskinesia Dystonia |
252 mg single, oral Overdose Dose: 252 mg Route: oral Route: single Dose: 252 mg Sources: Page: p.47 |
unhealthy, 16 n = 1 Health Status: unhealthy Condition: Conduct disorder Age Group: 16 Sex: M Population Size: 1 Sources: Page: p.47 |
Disc. AE: Loss of consciousness... AEs leading to discontinuation/dose reduction: Loss of consciousness Sources: Page: p.47 |
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: |
unhealthy, 30 n = 1 Health Status: unhealthy Condition: Schizophrenia Age Group: 30 Sex: M Population Size: 1 Sources: |
DLT: Motor tic... |
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: Page: p.565 |
unhealthy, 37.7 n = 226 Health Status: unhealthy Condition: Schizophrenia Age Group: 37.7 Sex: M+F Population Size: 226 Sources: Page: p.565 |
Disc. AE: Depressive symptom, Psychotic disorder... AEs leading to discontinuation/dose reduction: Depressive symptom (0.9%) Sources: Page: p.565Psychotic 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%) |
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: Page: p.210 |
unhealthy, 38 n = 1 Health Status: unhealthy Condition: Schizophrenia Age Group: 38 Sex: M Population Size: 1 Sources: Page: p.210 |
Disc. AE: Dyskinesia, Dystonia... AEs leading to discontinuation/dose reduction: Dyskinesia Sources: Page: p.210Dystonia Tremor Diaphoresis Tachycardia |
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: Page: p.1 |
unhealthy Health Status: unhealthy Condition: Schizophrenia Sources: Page: p.1 |
Disc. AE: Cerebrovascular disorder (NOS), Stroke... AEs leading to discontinuation/dose reduction: Cerebrovascular disorder (NOS) Sources: Page: p.1Stroke 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 |
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: Page: p.1 |
unhealthy Health Status: unhealthy Condition: Schizophrenia|Schizoaffective disorder Sources: Page: p.1 |
Disc. AE: Cerebrovascular disorder (NOS), Stroke... AEs leading to discontinuation/dose reduction: Cerebrovascular disorder (NOS) Sources: Page: p.1Stroke 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 |
AEs
AE | Significance | Dose | Population |
---|---|---|---|
Dyskinesia | Disc. AE | 180 mg single, oral Overdose Dose: 180 mg Route: oral Route: single Dose: 180 mg Sources: Page: p.210 |
unhealthy, 12 n = 1 Health Status: unhealthy Condition: Developmental delay Age Group: 12 Sex: M Population Size: 1 Sources: Page: p.210 |
Dystonia | Disc. AE | 180 mg single, oral Overdose Dose: 180 mg Route: oral Route: single Dose: 180 mg Sources: Page: p.210 |
unhealthy, 12 n = 1 Health Status: unhealthy Condition: Developmental delay Age Group: 12 Sex: M Population Size: 1 Sources: Page: p.210 |
Hypokalemia | Disc. AE | 180 mg single, oral Overdose Dose: 180 mg Route: oral Route: single Dose: 180 mg Sources: Page: p.210 |
unhealthy, 12 n = 1 Health Status: unhealthy Condition: Developmental delay Age Group: 12 Sex: M Population Size: 1 Sources: Page: p.210 |
Lethargy | Disc. AE | 180 mg single, oral Overdose Dose: 180 mg Route: oral Route: single Dose: 180 mg Sources: Page: p.210 |
unhealthy, 12 n = 1 Health Status: unhealthy Condition: Developmental delay Age Group: 12 Sex: M Population Size: 1 Sources: Page: p.210 |
Tachycardia | Disc. AE | 180 mg single, oral Overdose Dose: 180 mg Route: oral Route: single Dose: 180 mg Sources: Page: p.210 |
unhealthy, 12 n = 1 Health Status: unhealthy Condition: Developmental delay Age Group: 12 Sex: M Population Size: 1 Sources: Page: p.210 |
Loss of consciousness | Disc. AE | 252 mg single, oral Overdose Dose: 252 mg Route: oral Route: single Dose: 252 mg Sources: Page: p.47 |
unhealthy, 16 n = 1 Health Status: unhealthy Condition: Conduct disorder Age Group: 16 Sex: M Population Size: 1 Sources: Page: p.47 |
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: |
unhealthy, 30 n = 1 Health Status: unhealthy Condition: Schizophrenia Age Group: 30 Sex: M Population Size: 1 Sources: |
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: Page: p.565 |
unhealthy, 37.7 n = 226 Health Status: unhealthy Condition: Schizophrenia Age Group: 37.7 Sex: M+F Population Size: 226 Sources: Page: p.565 |
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: Page: p.565 |
unhealthy, 37.7 n = 226 Health Status: unhealthy Condition: Schizophrenia Age Group: 37.7 Sex: M+F Population Size: 226 Sources: Page: p.565 |
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: Page: p.565 |
unhealthy, 37.7 n = 226 Health Status: unhealthy Condition: Schizophrenia Age Group: 37.7 Sex: M+F Population Size: 226 Sources: Page: p.565 |
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: Page: p.565 |
unhealthy, 37.7 n = 226 Health Status: unhealthy Condition: Schizophrenia Age Group: 37.7 Sex: M+F Population Size: 226 Sources: Page: p.565 |
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: Page: p.565 |
unhealthy, 37.7 n = 226 Health Status: unhealthy Condition: Schizophrenia Age Group: 37.7 Sex: M+F Population Size: 226 Sources: Page: p.565 |
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: Page: p.565 |
unhealthy, 37.7 n = 226 Health Status: unhealthy Condition: Schizophrenia Age Group: 37.7 Sex: M+F Population Size: 226 Sources: Page: p.565 |
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: Page: p.565 |
unhealthy, 37.7 n = 226 Health Status: unhealthy Condition: Schizophrenia Age Group: 37.7 Sex: M+F Population Size: 226 Sources: Page: p.565 |
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: Page: p.565 |
unhealthy, 37.7 n = 226 Health Status: unhealthy Condition: Schizophrenia Age Group: 37.7 Sex: M+F Population Size: 226 Sources: Page: p.565 |
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: Page: p.565 |
unhealthy, 37.7 n = 226 Health Status: unhealthy Condition: Schizophrenia Age Group: 37.7 Sex: M+F Population Size: 226 Sources: Page: p.565 |
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: Page: p.565 |
unhealthy, 37.7 n = 226 Health Status: unhealthy Condition: Schizophrenia Age Group: 37.7 Sex: M+F Population Size: 226 Sources: Page: p.565 |
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: Page: p.565 |
unhealthy, 37.7 n = 226 Health Status: unhealthy Condition: Schizophrenia Age Group: 37.7 Sex: M+F Population Size: 226 Sources: Page: p.565 |
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: Page: p.565 |
unhealthy, 37.7 n = 226 Health Status: unhealthy Condition: Schizophrenia Age Group: 37.7 Sex: M+F Population Size: 226 Sources: Page: p.565 |
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: Page: p.565 |
unhealthy, 37.7 n = 226 Health Status: unhealthy Condition: Schizophrenia Age Group: 37.7 Sex: M+F Population Size: 226 Sources: Page: p.565 |
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: Page: p.565 |
unhealthy, 37.7 n = 226 Health Status: unhealthy Condition: Schizophrenia Age Group: 37.7 Sex: M+F Population Size: 226 Sources: Page: p.565 |
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: Page: p.565 |
unhealthy, 37.7 n = 226 Health Status: unhealthy Condition: Schizophrenia Age Group: 37.7 Sex: M+F Population Size: 226 Sources: Page: p.565 |
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: Page: p.565 |
unhealthy, 37.7 n = 226 Health Status: unhealthy Condition: Schizophrenia Age Group: 37.7 Sex: M+F Population Size: 226 Sources: Page: p.565 |
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: Page: p.565 |
unhealthy, 37.7 n = 226 Health Status: unhealthy Condition: Schizophrenia Age Group: 37.7 Sex: M+F Population Size: 226 Sources: Page: p.565 |
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: Page: p.565 |
unhealthy, 37.7 n = 226 Health Status: unhealthy Condition: Schizophrenia Age Group: 37.7 Sex: M+F Population Size: 226 Sources: Page: p.565 |
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: Page: p.565 |
unhealthy, 37.7 n = 226 Health Status: unhealthy Condition: Schizophrenia Age Group: 37.7 Sex: M+F Population Size: 226 Sources: Page: p.565 |
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: Page: p.565 |
unhealthy, 37.7 n = 226 Health Status: unhealthy Condition: Schizophrenia Age Group: 37.7 Sex: M+F Population Size: 226 Sources: Page: p.565 |
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: Page: p.565 |
unhealthy, 37.7 n = 226 Health Status: unhealthy Condition: Schizophrenia Age Group: 37.7 Sex: M+F Population Size: 226 Sources: Page: p.565 |
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: Page: p.565 |
unhealthy, 37.7 n = 226 Health Status: unhealthy Condition: Schizophrenia Age Group: 37.7 Sex: M+F Population Size: 226 Sources: Page: p.565 |
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: Page: p.565 |
unhealthy, 37.7 n = 226 Health Status: unhealthy Condition: Schizophrenia Age Group: 37.7 Sex: M+F Population Size: 226 Sources: Page: p.565 |
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: Page: p.565 |
unhealthy, 37.7 n = 226 Health Status: unhealthy Condition: Schizophrenia Age Group: 37.7 Sex: M+F Population Size: 226 Sources: Page: p.565 |
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: Page: p.565 |
unhealthy, 37.7 n = 226 Health Status: unhealthy Condition: Schizophrenia Age Group: 37.7 Sex: M+F Population Size: 226 Sources: Page: p.565 |
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: Page: p.565 |
unhealthy, 37.7 n = 226 Health Status: unhealthy Condition: Schizophrenia Age Group: 37.7 Sex: M+F Population Size: 226 Sources: Page: p.565 |
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: Page: p.565 |
unhealthy, 37.7 n = 226 Health Status: unhealthy Condition: Schizophrenia Age Group: 37.7 Sex: M+F Population Size: 226 Sources: Page: p.565 |
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: Page: p.210 |
unhealthy, 38 n = 1 Health Status: unhealthy Condition: Schizophrenia Age Group: 38 Sex: M Population Size: 1 Sources: Page: p.210 |
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: Page: p.210 |
unhealthy, 38 n = 1 Health Status: unhealthy Condition: Schizophrenia Age Group: 38 Sex: M Population Size: 1 Sources: Page: p.210 |
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: Page: p.210 |
unhealthy, 38 n = 1 Health Status: unhealthy Condition: Schizophrenia Age Group: 38 Sex: M Population Size: 1 Sources: Page: p.210 |
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: Page: p.210 |
unhealthy, 38 n = 1 Health Status: unhealthy Condition: Schizophrenia Age Group: 38 Sex: M Population Size: 1 Sources: Page: p.210 |
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: Page: p.210 |
unhealthy, 38 n = 1 Health Status: unhealthy Condition: Schizophrenia Age Group: 38 Sex: M Population Size: 1 Sources: Page: p.210 |
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: Page: p.1 |
unhealthy Health Status: unhealthy Condition: Schizophrenia Sources: Page: p.1 |
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: Page: p.1 |
unhealthy Health Status: unhealthy Condition: Schizophrenia Sources: Page: p.1 |
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: Page: p.1 |
unhealthy Health Status: unhealthy Condition: Schizophrenia Sources: Page: p.1 |
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: Page: p.1 |
unhealthy Health Status: unhealthy Condition: Schizophrenia Sources: Page: p.1 |
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: Page: p.1 |
unhealthy Health Status: unhealthy Condition: Schizophrenia Sources: Page: p.1 |
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: Page: p.1 |
unhealthy Health Status: unhealthy Condition: Schizophrenia Sources: Page: p.1 |
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: Page: p.1 |
unhealthy Health Status: unhealthy Condition: Schizophrenia Sources: Page: p.1 |
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: Page: p.1 |
unhealthy Health Status: unhealthy Condition: Schizophrenia Sources: Page: p.1 |
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: Page: p.1 |
unhealthy Health Status: unhealthy Condition: Schizophrenia Sources: Page: p.1 |
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: Page: p.1 |
unhealthy Health Status: unhealthy Condition: Schizophrenia Sources: Page: p.1 |
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: Page: p.1 |
unhealthy Health Status: unhealthy Condition: Schizophrenia Sources: Page: p.1 |
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: Page: p.1 |
unhealthy Health Status: unhealthy Condition: Schizophrenia Sources: Page: p.1 |
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: Page: p.1 |
unhealthy Health Status: unhealthy Condition: Schizophrenia Sources: Page: p.1 |
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: Page: p.1 |
unhealthy Health Status: unhealthy Condition: Schizophrenia Sources: Page: p.1 |
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: Page: p.1 |
unhealthy Health Status: unhealthy Condition: Schizophrenia Sources: Page: p.1 |
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: Page: p.1 |
unhealthy Health Status: unhealthy Condition: Schizophrenia Sources: Page: p.1 |
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: Page: p.1 |
unhealthy Health Status: unhealthy Condition: Schizophrenia Sources: Page: p.1 |
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: Page: p.1 |
unhealthy Health Status: unhealthy Condition: Schizophrenia Sources: Page: p.1 |
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: Page: p.1 |
unhealthy Health Status: unhealthy Condition: Schizophrenia Sources: Page: p.1 |
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: Page: p.1 |
unhealthy Health Status: unhealthy Condition: Schizophrenia|Schizoaffective disorder Sources: Page: p.1 |
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: Page: p.1 |
unhealthy Health Status: unhealthy Condition: Schizophrenia|Schizoaffective disorder Sources: Page: p.1 |
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: Page: p.1 |
unhealthy Health Status: unhealthy Condition: Schizophrenia|Schizoaffective disorder Sources: Page: p.1 |
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: Page: p.1 |
unhealthy Health Status: unhealthy Condition: Schizophrenia|Schizoaffective disorder Sources: Page: p.1 |
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: Page: p.1 |
unhealthy Health Status: unhealthy Condition: Schizophrenia|Schizoaffective disorder Sources: Page: p.1 |
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: Page: p.1 |
unhealthy Health Status: unhealthy Condition: Schizophrenia|Schizoaffective disorder Sources: Page: p.1 |
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: Page: p.1 |
unhealthy Health Status: unhealthy Condition: Schizophrenia|Schizoaffective disorder Sources: Page: p.1 |
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: Page: p.1 |
unhealthy Health Status: unhealthy Condition: Schizophrenia|Schizoaffective disorder Sources: Page: p.1 |
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: Page: p.1 |
unhealthy Health Status: unhealthy Condition: Schizophrenia|Schizoaffective disorder Sources: Page: p.1 |
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: Page: p.1 |
unhealthy Health Status: unhealthy Condition: Schizophrenia|Schizoaffective disorder Sources: Page: p.1 |
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: Page: p.1 |
unhealthy Health Status: unhealthy Condition: Schizophrenia|Schizoaffective disorder Sources: Page: p.1 |
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: Page: p.1 |
unhealthy Health Status: unhealthy Condition: Schizophrenia|Schizoaffective disorder Sources: Page: p.1 |
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: Page: p.1 |
unhealthy Health Status: unhealthy Condition: Schizophrenia|Schizoaffective disorder Sources: Page: p.1 |
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: Page: p.1 |
unhealthy Health Status: unhealthy Condition: Schizophrenia|Schizoaffective disorder Sources: Page: p.1 |
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: Page: p.1 |
unhealthy Health Status: unhealthy Condition: Schizophrenia|Schizoaffective disorder Sources: Page: p.1 |
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: Page: p.1 |
unhealthy Health Status: unhealthy Condition: Schizophrenia|Schizoaffective disorder Sources: Page: p.1 |
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: Page: p.1 |
unhealthy Health Status: unhealthy Condition: Schizophrenia|Schizoaffective disorder Sources: Page: p.1 |
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: Page: p.1 |
unhealthy Health Status: unhealthy Condition: Schizophrenia|Schizoaffective disorder Sources: Page: p.1 |
Overview
CYP3A4 | CYP2C9 | CYP2D6 | hERG |
---|---|---|---|
Drug as perpetrator
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2006/021999s000_ClinPharmR_Part1.pdf Page: 41, 81 |
no [IC50 61.9 uM] | no (co-administration study) Comment: examination of inhibition by paliperidone using CYP isozyme probe detromethorphan Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2006/021999s000_ClinPharmR_Part1.pdf Page: 41, 81 |
||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2006/021999s000_ClinPharmR_Part1.pdf Page: 41, 81 |
no [Inhibition >30 uM] | no (co-administration study) Comment: examination of inhibition by paliperidone using CYP isozyme probe coumarin Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2006/021999s000_ClinPharmR_Part1.pdf Page: 41, 81 |
||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2006/021999s000_ClinPharmR_Part1.pdf Page: 41, 81 |
no [Inhibition >30 uM] | no (co-administration study) Comment: examination of inhibition by paliperidone using CYP isozyme probe chlorzoxazone Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2006/021999s000_ClinPharmR_Part1.pdf Page: 41, 81 |
||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2006/021999s000_ClinPharmR_Part1.pdf Page: 41, 81 |
no [Inhibition >30 uM] | no (co-administration study) Comment: examination of inhibition by paliperidone using CYP isozyme probe lauric acid Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2006/021999s000_ClinPharmR_Part1.pdf Page: 41, 81 |
||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2006/021999s000_ClinPharmR_Part1.pdf Page: 41, 81 |
no [Inhibition >60 uM] | no (co-administration study) Comment: examination of inhibition by paliperidone using CYP isozyme probe Caffeine Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2006/021999s000_ClinPharmR_Part1.pdf Page: 41, 81 |
||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2006/021999s000_ClinPharmR_Part1.pdf Page: 41, 81 |
no [Inhibition >60 uM] | no (co-administration study) Comment: examination of inhibition by paliperidone using CYP isozyme probe phenytoin Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2006/021999s000_ClinPharmR_Part1.pdf Page: 41, 81 |
||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2006/021999s000_ClinPharmR_Part1.pdf Page: 41, 81 |
no [Inhibition >60 uM] | no (co-administration study) Comment: examination of inhibition by paliperidone using CYP isozyme probe phenytoin Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2006/021999s000_ClinPharmR_Part1.pdf Page: 41, 81 |
||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2006/021999s000_ClinPharmR_Part1.pdf Page: 41, 81 |
no [Inhibition >60 uM] | no (co-administration study) Comment: examination of inhibition by paliperidone using CYP isozyme probe testosterone Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2006/021999s000_ClinPharmR_Part1.pdf Page: 41, 81 |
||
weak [IC50 63.26 uM] |
Drug as victim
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
yes | ||||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2006/021999s000_ClinPharmR_Part1.pdf Page: 40.0 |
yes | |||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2006/021999s000_ClinPharmR_Part1.pdf Page: 40.0 |
yes | |||
Page: 41, 67 |
yes | |||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2006/021999s000_ClinPharmR_Part3.pdf Page: 19.0 |
yes | |||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2006/021999s000_ClinPharmR_Part3.pdf Page: 19.0 |
yes |
Tox targets
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
Page: 8, 17, 24 |
PubMed
Title | Date | PubMed |
---|---|---|
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 |
|
Positive modulation of glutamatergic receptors potentiates the suppressive effects of antipsychotics on conditioned avoidance responding in rats. | 2006 Jun |
|
Effect of adjunctive lamotrigine treatment on the plasma concentrations of clozapine, risperidone and olanzapine in patients with schizophrenia or bipolar disorder. | 2006 Oct |
|
Evaluation of antipsychotic drugs as inhibitors of multidrug resistance transporter P-glycoprotein. | 2006 Sep |
|
Paliperidone extended release. | 2007 |
|
Extended-release paliperidone: efficacy, safety and tolerability profile of a new atypical antipsychotic. | 2007 Apr |
|
Paliperidone: quo vadis? | 2007 Apr |
|
Risperidone and paliperidone inhibit p-glycoprotein activity in vitro. | 2007 Apr |
|
Enantioselective analysis of the antipsychotic 9-hydroxyrisperidone, main metabolite of risperidone, by chiral capillary EKC using dual CDs. | 2007 Aug |
|
Efficacy and safety of paliperidone extended-release tablets: results of a 6-week, randomized, placebo-controlled study. | 2007 Dec 15 |
|
Possible neuroleptic malignant syndrome associated with paliperidone. | 2007 Fall |
|
Rapidly disintegrating risperidone in subjects with schizophrenia or schizoaffective disorder: a summary of ten phase I clinical trials assessing taste, tablet disintegration time, bioequivalence, and tolerability. | 2007 Feb |
|
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 |
|
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 |
|
Pharmacokinetics study for hyperprolactinemia among schizophrenics switched from risperidone to risperidone long-acting injection. | 2007 Jun |
|
Treatment with risperidone for 4 weeks increased plasma 3-methoxy-4-hydroxypnenylglycol (MHPG) levels, but did not alter plasma brain-derived neurotrophic factor (BDNF) levels in schizophrenic patients. | 2007 Jun 30 |
|
Paliperidone (Invega) for schizophrenia. | 2007 Mar 12 |
|
New drug for schizophrenia. | 2007 Mar-Apr |
|
New drugs: paliperidone, dasatinib, and decitabine. | 2007 Mar-Apr |
|
Effect of topiramate on plasma concentrations of clozapine, olanzapine, risperidone, and quetiapine in patients with psychotic disorders. | 2007 Mar-Apr |
|
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 |
|
The pharmacology and safety of paliperidone extended-release in the treatment of schizophrenia. | 2007 Nov |
|
Paliperidone: a new extended-release oral atypical antipsychotic. | 2007 Oct |
|
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 |
|
A double-blind, placebo-controlled, randomized study evaluating the effect of paliperidone extended-release tablets on sleep architecture in patients with schizophrenia. | 2007 Sep |
|
Analytical and semipreparative enantioseparation of 9-hydroxyrisperidone, the main metabolite of risperidone, using high-performance liquid chromatography and capillary electrophoresis. Validation and determination of enantiomeric purity. | 2007 Sep 7 |
|
Upcoming agents for the treatment of schizophrenia: mechanism of action, efficacy and tolerability. | 2008 |
|
Dose-finding study of paliperidone ER based on striatal and extrastriatal dopamine D2 receptor occupancy in patients with schizophrenia. | 2008 Apr |
|
Effect of rifampin, an inducer of CYP3A and P-glycoprotein, on the pharmacokinetics of risperidone. | 2008 Jan |
|
Gateways to clinical trials. July-August 2008. | 2008 Jul-Aug |
|
Metabolism of atypical antipsychotics: involvement of cytochrome p450 enzymes and relevance for drug-drug interactions. | 2008 Jun |
|
Efficacy and tolerability of oral paliperidone extended-release tablets in the treatment of acute schizophrenia: pooled data from three 6-week, placebo-controlled studies. | 2008 May |
|
Efficacy and safety of oral paliperidone extended-release tablets in the treatment of acute schizophrenia: pooled data from three 52-week open-label studies. | 2008 Nov |
|
Apparent seizure and atrial fibrillation associated with paliperidone. | 2008 Nov 15 |
|
Gateways to clinical trials. | 2008 Oct |
|
Antipsychotic drugs inhibit the function of breast cancer resistance protein. | 2008 Oct |
|
Paliperidone extended-release for the treatment of schizophrenia. | 2008 Oct |
|
ABCB1 polymorphisms influence steady-state plasma levels of 9-hydroxyrisperidone and risperidone active moiety. | 2008 Oct |
|
Choreatic symptoms during and after treatment with paliperidone and escitalopram. | 2008 Sep |
|
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 |
Patents
Sample Use Guides
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
Sources: https://www.ncbi.nlm.nih.gov/pubmed/25754735
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
Edited
Fri Dec 15 16:17:28 GMT 2023
by
admin
on
Fri Dec 15 16:17:28 GMT 2023
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Record UNII |
838F01T721
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Record Status |
Validated (UNII)
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Record Version |
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Classification Tree | Code System | Code | ||
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WHO-ATC |
N05AX13
Created by
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WHO-VATC |
QN05AX13
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LIVERTOX |
NBK548506
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NDF-RT |
N0000175430
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EMA ASSESSMENT REPORTS |
INVEGA (AUTHORIZED: PSYCHOTIC DISORDERS)
Created by
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EMA ASSESSMENT REPORTS |
INVEGA (AUTHORIZED: SCHIZOPHRENIA)
Created by
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NCI_THESAURUS |
C66883
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Paliperidone
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CHEMBL1621
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PALIPERIDONE
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C66293
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838F01T721
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SUB23268
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m8357
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82978
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759623
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8148
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Related Record | Type | Details | ||
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OFF-TARGET->NON-INHIBITOR |
NON-INHIBITOR
Ki
|
||
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METABOLIC ENZYME -> SUBSTRATE | |||
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TARGET -> INHIBITOR |
INHIBITOR
Ki
|
||
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TARGET -> INHIBITOR |
INHIBITOR
Ki
|
||
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OFF TARGET->NON-INHIBITOR |
NON-INHIBITOR
Ki
|
||
|
TARGET -> INHIBITOR |
INHIBITOR
Ki
|
||
|
TARGET -> INHIBITOR |
INHIBITOR
Ki
|
||
|
EXCRETED UNCHANGED |
AMOUNT EXCRETED
URINE
|
||
|
TARGET -> INHIBITOR |
INHIBITOR
Ki
|
||
|
TARGET->WEAK INHIBITOR |
INHIBITOR
Ki
|
||
|
TARGET -> INHIBITOR |
INHIBITOR
Ki
|
||
|
TARGET -> INHIBITOR |
INHIBITOR
Ki
|
||
|
OFF TARGET->NON-INHIBITOR |
NON-INHIBITOR
Ki
|
||
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TARGET -> INHIBITOR |
INHIBITOR
Ki
|
||
|
TARGET -> INHIBITOR |
INHIBITOR
Ki
|
||
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TRANSPORTER -> SUBSTRATE |
TRANSPORTER
IC50
|
||
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OFF TARGET->NON-INHIBITOR |
NON-INHIBITOR
Ki
|
||
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BINDER->LIGAND |
|
||
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TARGET -> INHIBITOR |
INHIBITOR
Ki
|
||
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TARGET -> INHIBITOR |
INHIBITOR
Ki
|
||
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TARGET -> INHIBITOR |
INHIBITOR
Ki
|
||
|
TARGET -> INHIBITOR |
INHIBITOR
Ki
|
||
|
OFF TARGET->NON-INHIBITOR |
NON-INHIBITOR
Ki
|
||
|
TARGET -> INHIBITOR |
INHIBITOR
Ki
|
||
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TARGET -> INHIBITOR |
INHIBITOR
Ki
|
||
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METABOLIC ENZYME -> SUBSTRATE | |||
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TARGET -> INHIBITOR |
INHIBITOR
Ki
|
||
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TARGET -> INHIBITOR |
INHIBITOR
Ki
|
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TARGET -> INHIBITOR |
INHIBITOR
Ki
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Related Record | Type | Details | ||
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METABOLITE -> PARENT |
Trace in feces
URINE
|
||
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METABOLITE -> PARENT |
FECAL
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METABOLITE -> PARENT |
URINE
|
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|
PARENT -> METABOLITE ACTIVE |
MAJOR
PLASMA
|
Related Record | Type | Details | ||
---|---|---|---|---|
|
IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
|
||
|
PARENT -> IMPURITY |
not more than the area of the principal peak in the chromatogram obtained with reference solution (b)
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
|
||
|
IMPURITY -> PARENT |
|
||
|
IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
|
||
|
IMPURITY -> PARENT |
|
||
|
IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
|
||
|
IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
|
Related Record | Type | Details | ||
---|---|---|---|---|
|
ACTIVE MOIETY |
Name | Property Type | Amount | Referenced Substance | Defining | Parameters | References |
---|---|---|---|---|---|---|
ORAL BIOAVAILABILITY | PHARMACOKINETIC |
|
|
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Biological Half-life | PHARMACOKINETIC |
|
|
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Volume of Distribution | PHARMACOKINETIC |
|
|
|||
Tmax | PHARMACOKINETIC |
|
|
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