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 |
---|---|---|---|---|
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
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
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 |
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
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
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 |
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 |
unhealthy, 12 |
Disc. AE: Lethargy, Tachycardia... AEs leading to discontinuation/dose reduction: Lethargy Sources: Tachycardia Hypokalemia Dyskinesia Dystonia |
252 mg single, oral Overdose |
unhealthy, 16 |
Disc. AE: Loss of consciousness... AEs leading to discontinuation/dose reduction: Loss of consciousness Sources: |
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 |
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: |
unhealthy, 37.7 |
Disc. AE: Depressive symptom, Psychotic disorder... AEs leading to discontinuation/dose reduction: Depressive symptom (0.9%) Sources: 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%) |
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: |
unhealthy, 38 |
Disc. AE: Dyskinesia, Dystonia... AEs leading to discontinuation/dose reduction: Dyskinesia Sources: Dystonia 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: |
unhealthy Health Status: unhealthy Sources: |
Disc. AE: Cerebrovascular disorder (NOS), Stroke... AEs leading to discontinuation/dose reduction: Cerebrovascular disorder (NOS) Sources: 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 |
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: |
unhealthy Health Status: unhealthy Sources: |
Disc. AE: Cerebrovascular disorder (NOS), Stroke... AEs leading to discontinuation/dose reduction: Cerebrovascular disorder (NOS) Sources: 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 |
AEs
AE | Significance | Dose | Population |
---|---|---|---|
Dyskinesia | Disc. AE | 180 mg single, oral Overdose |
unhealthy, 12 |
Dystonia | Disc. AE | 180 mg single, oral Overdose |
unhealthy, 12 |
Hypokalemia | Disc. AE | 180 mg single, oral Overdose |
unhealthy, 12 |
Lethargy | Disc. AE | 180 mg single, oral Overdose |
unhealthy, 12 |
Tachycardia | Disc. AE | 180 mg single, oral Overdose |
unhealthy, 12 |
Loss of consciousness | Disc. AE | 252 mg single, oral Overdose |
unhealthy, 16 |
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 |
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: |
unhealthy, 37.7 |
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: |
unhealthy, 37.7 |
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: |
unhealthy, 37.7 |
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: |
unhealthy, 37.7 |
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: |
unhealthy, 37.7 |
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: |
unhealthy, 37.7 |
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: |
unhealthy, 37.7 |
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: |
unhealthy, 37.7 |
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: |
unhealthy, 37.7 |
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: |
unhealthy, 37.7 |
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: |
unhealthy, 37.7 |
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: |
unhealthy, 37.7 |
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: |
unhealthy, 37.7 |
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: |
unhealthy, 37.7 |
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: |
unhealthy, 37.7 |
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: |
unhealthy, 37.7 |
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: |
unhealthy, 37.7 |
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: |
unhealthy, 37.7 |
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: |
unhealthy, 37.7 |
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: |
unhealthy, 37.7 |
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: |
unhealthy, 37.7 |
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: |
unhealthy, 37.7 |
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: |
unhealthy, 37.7 |
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: |
unhealthy, 37.7 |
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: |
unhealthy, 37.7 |
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: |
unhealthy, 37.7 |
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: |
unhealthy, 37.7 |
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: |
unhealthy, 38 |
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: |
unhealthy, 38 |
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: |
unhealthy, 38 |
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: |
unhealthy, 38 |
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: |
unhealthy, 38 |
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: |
unhealthy Health Status: unhealthy Sources: |
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: |
unhealthy Health Status: unhealthy Sources: |
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: |
unhealthy Health Status: unhealthy Sources: |
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: |
unhealthy Health Status: unhealthy Sources: |
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: |
unhealthy Health Status: unhealthy Sources: |
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: |
unhealthy Health Status: unhealthy Sources: |
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: |
unhealthy Health Status: unhealthy Sources: |
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: |
unhealthy Health Status: unhealthy Sources: |
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: |
unhealthy Health Status: unhealthy Sources: |
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: |
unhealthy Health Status: unhealthy Sources: |
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: |
unhealthy Health Status: unhealthy Sources: |
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: |
unhealthy Health Status: unhealthy Sources: |
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: |
unhealthy Health Status: unhealthy Sources: |
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: |
unhealthy Health Status: unhealthy Sources: |
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: |
unhealthy Health Status: unhealthy Sources: |
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: |
unhealthy Health Status: unhealthy Sources: |
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: |
unhealthy Health Status: unhealthy Sources: |
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: |
unhealthy Health Status: unhealthy Sources: |
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: |
unhealthy Health Status: unhealthy Sources: |
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: |
unhealthy Health Status: unhealthy Sources: |
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: |
unhealthy Health Status: unhealthy Sources: |
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: |
unhealthy Health Status: unhealthy Sources: |
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: |
unhealthy Health Status: unhealthy Sources: |
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: |
unhealthy Health Status: unhealthy Sources: |
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: |
unhealthy Health Status: unhealthy Sources: |
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: |
unhealthy Health Status: unhealthy Sources: |
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: |
unhealthy Health Status: unhealthy Sources: |
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: |
unhealthy Health Status: unhealthy Sources: |
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: |
unhealthy Health Status: unhealthy Sources: |
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: |
unhealthy Health Status: unhealthy Sources: |
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: |
unhealthy Health Status: unhealthy Sources: |
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: |
unhealthy Health Status: unhealthy Sources: |
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: |
unhealthy Health Status: unhealthy Sources: |
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: |
unhealthy Health Status: unhealthy Sources: |
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: |
unhealthy Health Status: unhealthy Sources: |
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: |
unhealthy Health Status: unhealthy Sources: |
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: |
unhealthy Health Status: unhealthy Sources: |
Overview
CYP3A4 | CYP2C9 | CYP2D6 | hERG |
---|---|---|---|
OverviewOther
Other Inhibitor | Other Substrate | Other Inducer |
---|---|---|
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 |
---|---|---|
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
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
Mon Mar 31 18:24:10 GMT 2025
by
admin
on
Mon Mar 31 18:24:10 GMT 2025
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Record UNII |
838F01T721
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Record Status |
Validated (UNII)
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WHO-ATC |
N05AX13
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WHO-VATC |
QN05AX13
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LIVERTOX |
NBK548506
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NDF-RT |
N0000175430
Created by
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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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Code System | Code | Type | Description | ||
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4137
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Paliperidone
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CHEMBL1621
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DTXSID7049059
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1491809
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PALIPERIDONE
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DB01267
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QQ-13
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7977
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838F01T721
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144598-75-4
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100000092109
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7258
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115237
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679314
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C66293
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838F01T721
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SUB23268
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m8357
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PRIMARY | Merck Index | ||
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82978
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759623
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8148
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Related Record | Type | Details | ||
---|---|---|---|---|
|
OFF-TARGET->NON-INHIBITOR |
NON-INHIBITOR
Ki
|
||
|
METABOLIC ENZYME -> SUBSTRATE | |||
|
TARGET -> INHIBITOR |
INHIBITOR
Ki
|
||
|
TARGET -> INHIBITOR |
INHIBITOR
Ki
|
||
|
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
|
||
|
TARGET -> INHIBITOR |
INHIBITOR
Ki
|
||
|
TARGET -> INHIBITOR |
INHIBITOR
Ki
|
||
|
TRANSPORTER -> SUBSTRATE |
TRANSPORTER
IC50
|
||
|
OFF TARGET->NON-INHIBITOR |
NON-INHIBITOR
Ki
|
||
|
BINDER->LIGAND |
|
||
|
SALT/SOLVATE -> PARENT |
|
||
|
TARGET -> INHIBITOR |
INHIBITOR
Ki
|
||
|
TARGET -> INHIBITOR |
INHIBITOR
Ki
|
||
|
TARGET -> INHIBITOR |
INHIBITOR
Ki
|
||
|
TARGET -> INHIBITOR |
INHIBITOR
Ki
|
||
|
OFF TARGET->NON-INHIBITOR |
NON-INHIBITOR
Ki
|
||
|
TARGET -> INHIBITOR |
INHIBITOR
Ki
|
||
|
TARGET -> INHIBITOR |
INHIBITOR
Ki
|
||
|
METABOLIC ENZYME -> SUBSTRATE | |||
|
TARGET -> INHIBITOR |
INHIBITOR
Ki
|
||
|
TARGET -> INHIBITOR |
INHIBITOR
Ki
|
||
|
TARGET -> INHIBITOR |
INHIBITOR
Ki
|
Related Record | Type | Details | ||
---|---|---|---|---|
|
METABOLITE -> PARENT |
Trace in feces
URINE
|
||
|
METABOLITE -> PARENT |
FECAL
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||
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METABOLITE -> PARENT |
URINE
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||
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PARENT -> METABOLITE ACTIVE |
Related Record | Type | Details | ||
---|---|---|---|---|
|
IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
|
||
|
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
|
||
|
PARENT -> IMPURITY |
Related Record | Type | Details | ||
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|
ACTIVE MOIETY |
Name | Property Type | Amount | Referenced Substance | Defining | Parameters | References |
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ORAL BIOAVAILABILITY | PHARMACOKINETIC |
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Biological Half-life | PHARMACOKINETIC |
|
|
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Volume of Distribution | PHARMACOKINETIC |
|
|
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Tmax | PHARMACOKINETIC |
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