Details
Stereochemistry | ACHIRAL |
Molecular Formula | C23H27FN4O2 |
Molecular Weight | 410.4854 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
Cc1c(CCN2CCC(CC2)c3c4ccc(cc4on3)F)c(=O)n5CCCCc5n1
InChI
InChIKey=RAPZEAPATHNIPO-UHFFFAOYSA-N
InChI=1S/C23H27FN4O2/c1-15-18(23(29)28-10-3-2-4-21(28)25-15)9-13-27-11-7-16(8-12-27)22-19-6-5-17(24)14-20(19)30-26-22/h5-6,14,16H,2-4,7-13H2,1H3
Molecular Formula | C23H27FN4O2 |
Molecular Weight | 410.4854 |
Charge | 0 |
Count |
|
Stereochemistry | ACHIRAL |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Optical Activity | NONE |
DescriptionSources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2016/020272s077,020588s065,021346s055,021444s051lbl.pdfCurator's Comment:: description was created based on several sources, including:
https://www.drugs.com/risperidone.html
http://www.wikidoc.org/index.php/Risperidone_(oral)
http://www.rxlist.com/risperdal-drug.htm
Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2016/020272s077,020588s065,021346s055,021444s051lbl.pdf
Curator's Comment:: description was created based on several sources, including:
https://www.drugs.com/risperidone.html
http://www.wikidoc.org/index.php/Risperidone_(oral)
http://www.rxlist.com/risperdal-drug.htm
Risperidone, a benzisoxazole derivative, is an atypical antipsychotic drug with high affinity for 5-hydrotryptamine (5-HT) and dopamine D2 receptors. It is FDA approved for the treatment of schizophrenia, bipolar mania, irritability associated with autistic disorder. Carbamazepine and other enzyme inducers decrease plasma concentrations of risperidone. Vice versa, Fluoxetine, paroxetine, and other CYP 2D6 enzyme inhibitors increase plasma concentrations of risperidone. Common adverse reactions include increased mortality in elderly patients with dementia-related psychosis, cerebrovascular adverse events, including stroke, in elderly patients with dementia-related psychosis, neuroleptic malignant syndrome, tardive dyskinesia , metabolic Changes (hyperglycemia and diabetes mellitus, dyslipidemia, weight gain), hyperprolactinemia, orthostatic hypotension, leukopenia, neutropenia, agranulocytosis, potential for cognitive and motor impairment, seizures, dysphagia, priapism, disruption of body temperature regulation.
CNS Activity
Originator
Sources: https://www.google.com/patents/US4804663
Curator's Comment:: # Janssen Pharmaceutica N.V.
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL2094251 Sources: https://www.ncbi.nlm.nih.gov/pubmed/11132243 |
2.7 nM [Kd] | ||
Target ID: CHEMBL217 Sources: https://www.ncbi.nlm.nih.gov/pubmed/11132243 |
3.8 nM [Kd] | ||
Target ID: CHEMBL1983 Sources: https://www.ncbi.nlm.nih.gov/pubmed/11132243 |
3.9 nM [Kd] | ||
0.15 nM [Kd] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | RISPERDAL Approved UseINDICATIONS & USAGE Risperidone tablets are indicated for the acute and maintenance treatment of schizophrenia [see Clinical Studies (14.1) Launch Date7.5712319E11 |
|||
Primary | RISPERDAL Approved UseINDICATIONS & USAGE Risperidone tablets are indicated for the acute and maintenance treatment of schizophrenia [see Clinical Studies (14.1) Launch Date7.5712319E11 |
|||
Primary | RISPERDAL Approved UseINDICATIONS & USAGE Risperidone tablets are indicated for the acute and maintenance treatment of schizophrenia [see Clinical Studies (14.1) Launch Date7.5712319E11 |
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
17 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11985287/ |
2 mg 2 times / day steady-state, oral dose: 2 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
RISPERIDONE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
7.77 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25042870/ |
1 mg single, oral dose: 1 mg route of administration: Oral experiment type: SINGLE co-administered: |
RISPERIDONE plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
AUC
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
83.1 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11985287/ |
2 mg 2 times / day steady-state, oral dose: 2 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
RISPERIDONE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
53.86 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25042870/ |
1 mg single, oral dose: 1 mg route of administration: Oral experiment type: SINGLE co-administered: |
RISPERIDONE plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
T1/2
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
20 h |
1 mg single, oral dose: 1 mg route of administration: Oral experiment type: SINGLE co-administered: |
RISPERIDONE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
4.88 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25042870/ |
1 mg single, oral dose: 1 mg route of administration: Oral experiment type: SINGLE co-administered: |
RISPERIDONE plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
Funbound
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
10% |
1 mg single, oral dose: 1 mg route of administration: Oral experiment type: SINGLE co-administered: |
RISPERIDONE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
Doses
Dose | Population | Adverse events |
---|---|---|
16 mg 1 times / day multiple, oral (max) Recommended Dose: 16 mg, 1 times / day Route: oral Route: multiple Dose: 16 mg, 1 times / day Sources: |
unhealthy, adult n = 198 Health Status: unhealthy Condition: Schizophrenia Age Group: adult Population Size: 198 Sources: |
Disc. AE: Dizziness, Agitation... AEs leading to discontinuation/dose reduction: Dizziness (1%) Sources: Agitation (1%) Somnolence (0.5%) Hypotension postural (0.5%) Tachycardia (0.5%) Akathisia (1%) |
6 mg 1 times / day multiple, oral (max) Recommended Dose: 6 mg, 1 times / day Route: oral Route: multiple Dose: 6 mg, 1 times / day Sources: |
unhealthy, adult n = 448 Health Status: unhealthy Condition: Bipolar Mania Age Group: adult Population Size: 448 Sources: |
Disc. AE: Parkinsonism, Somnolence... AEs leading to discontinuation/dose reduction: Parkinsonism (0.4%) Sources: Somnolence (0.2%) Dizziness (0.2%) Dystonia (0.2%) SGOT increased (0.2%) SGPT increased (0.2%) |
8 mg 1 times / day multiple, oral (max) Recommended Dose: 8 mg, 1 times / day Route: oral Route: multiple Dose: 8 mg, 1 times / day Sources: |
unhealthy, adult n = 366 Health Status: unhealthy Condition: Schizophrenia Age Group: adult Population Size: 366 Sources: |
Disc. AE: Dizziness, Nausea... AEs leading to discontinuation/dose reduction: Dizziness (1.4%) Sources: Nausea (1.4%) Agitation (1.1%) Parkinsonism (0.8%) Somnolence (0.8%) Dystonia (0.5%) Abdominal pain (0.5%) Hypotension postural (0.3%) Tachycardia (0.3%) |
6 mg 1 times / day multiple, oral (max) Recommended Dose: 6 mg, 1 times / day Route: oral Route: multiple Dose: 6 mg, 1 times / day Sources: |
unhealthy, child n = 106 Health Status: unhealthy Condition: Schizophrenia Age Group: child Population Size: 106 Sources: |
Disc. AE: Somnolence, Dizziness... AEs leading to discontinuation/dose reduction: Somnolence (2%) Sources: Dizziness (2%) Anorexia (1%) Anxiety (1%) Ataxia (1%) Hypotension (1%) Palpitation (1%) |
6 mg 1 times / day multiple, oral (max) Recommended Dose: 6 mg, 1 times / day Route: oral Route: multiple Dose: 6 mg, 1 times / day Sources: |
unhealthy, child n = 111 Health Status: unhealthy Condition: Bipolar Mania Age Group: child Population Size: 111 Sources: |
Disc. AE: Somnolence, Nausea... AEs leading to discontinuation/dose reduction: Somnolence (5%) Sources: Nausea (3%) Abdominal pain (2%) Vomiting (2%) |
AEs
AE | Significance | Dose | Population |
---|---|---|---|
Hypotension postural | 0.5% Disc. AE |
16 mg 1 times / day multiple, oral (max) Recommended Dose: 16 mg, 1 times / day Route: oral Route: multiple Dose: 16 mg, 1 times / day Sources: |
unhealthy, adult n = 198 Health Status: unhealthy Condition: Schizophrenia Age Group: adult Population Size: 198 Sources: |
Somnolence | 0.5% Disc. AE |
16 mg 1 times / day multiple, oral (max) Recommended Dose: 16 mg, 1 times / day Route: oral Route: multiple Dose: 16 mg, 1 times / day Sources: |
unhealthy, adult n = 198 Health Status: unhealthy Condition: Schizophrenia Age Group: adult Population Size: 198 Sources: |
Tachycardia | 0.5% Disc. AE |
16 mg 1 times / day multiple, oral (max) Recommended Dose: 16 mg, 1 times / day Route: oral Route: multiple Dose: 16 mg, 1 times / day Sources: |
unhealthy, adult n = 198 Health Status: unhealthy Condition: Schizophrenia Age Group: adult Population Size: 198 Sources: |
Agitation | 1% Disc. AE |
16 mg 1 times / day multiple, oral (max) Recommended Dose: 16 mg, 1 times / day Route: oral Route: multiple Dose: 16 mg, 1 times / day Sources: |
unhealthy, adult n = 198 Health Status: unhealthy Condition: Schizophrenia Age Group: adult Population Size: 198 Sources: |
Akathisia | 1% Disc. AE |
16 mg 1 times / day multiple, oral (max) Recommended Dose: 16 mg, 1 times / day Route: oral Route: multiple Dose: 16 mg, 1 times / day Sources: |
unhealthy, adult n = 198 Health Status: unhealthy Condition: Schizophrenia Age Group: adult Population Size: 198 Sources: |
Dizziness | 1% Disc. AE |
16 mg 1 times / day multiple, oral (max) Recommended Dose: 16 mg, 1 times / day Route: oral Route: multiple Dose: 16 mg, 1 times / day Sources: |
unhealthy, adult n = 198 Health Status: unhealthy Condition: Schizophrenia Age Group: adult Population Size: 198 Sources: |
Dizziness | 0.2% Disc. AE |
6 mg 1 times / day multiple, oral (max) Recommended Dose: 6 mg, 1 times / day Route: oral Route: multiple Dose: 6 mg, 1 times / day Sources: |
unhealthy, adult n = 448 Health Status: unhealthy Condition: Bipolar Mania Age Group: adult Population Size: 448 Sources: |
Dystonia | 0.2% Disc. AE |
6 mg 1 times / day multiple, oral (max) Recommended Dose: 6 mg, 1 times / day Route: oral Route: multiple Dose: 6 mg, 1 times / day Sources: |
unhealthy, adult n = 448 Health Status: unhealthy Condition: Bipolar Mania Age Group: adult Population Size: 448 Sources: |
SGOT increased | 0.2% Disc. AE |
6 mg 1 times / day multiple, oral (max) Recommended Dose: 6 mg, 1 times / day Route: oral Route: multiple Dose: 6 mg, 1 times / day Sources: |
unhealthy, adult n = 448 Health Status: unhealthy Condition: Bipolar Mania Age Group: adult Population Size: 448 Sources: |
SGPT increased | 0.2% Disc. AE |
6 mg 1 times / day multiple, oral (max) Recommended Dose: 6 mg, 1 times / day Route: oral Route: multiple Dose: 6 mg, 1 times / day Sources: |
unhealthy, adult n = 448 Health Status: unhealthy Condition: Bipolar Mania Age Group: adult Population Size: 448 Sources: |
Somnolence | 0.2% Disc. AE |
6 mg 1 times / day multiple, oral (max) Recommended Dose: 6 mg, 1 times / day Route: oral Route: multiple Dose: 6 mg, 1 times / day Sources: |
unhealthy, adult n = 448 Health Status: unhealthy Condition: Bipolar Mania Age Group: adult Population Size: 448 Sources: |
Parkinsonism | 0.4% Disc. AE |
6 mg 1 times / day multiple, oral (max) Recommended Dose: 6 mg, 1 times / day Route: oral Route: multiple Dose: 6 mg, 1 times / day Sources: |
unhealthy, adult n = 448 Health Status: unhealthy Condition: Bipolar Mania Age Group: adult Population Size: 448 Sources: |
Hypotension postural | 0.3% Disc. AE |
8 mg 1 times / day multiple, oral (max) Recommended Dose: 8 mg, 1 times / day Route: oral Route: multiple Dose: 8 mg, 1 times / day Sources: |
unhealthy, adult n = 366 Health Status: unhealthy Condition: Schizophrenia Age Group: adult Population Size: 366 Sources: |
Tachycardia | 0.3% Disc. AE |
8 mg 1 times / day multiple, oral (max) Recommended Dose: 8 mg, 1 times / day Route: oral Route: multiple Dose: 8 mg, 1 times / day Sources: |
unhealthy, adult n = 366 Health Status: unhealthy Condition: Schizophrenia Age Group: adult Population Size: 366 Sources: |
Abdominal pain | 0.5% Disc. AE |
8 mg 1 times / day multiple, oral (max) Recommended Dose: 8 mg, 1 times / day Route: oral Route: multiple Dose: 8 mg, 1 times / day Sources: |
unhealthy, adult n = 366 Health Status: unhealthy Condition: Schizophrenia Age Group: adult Population Size: 366 Sources: |
Dystonia | 0.5% Disc. AE |
8 mg 1 times / day multiple, oral (max) Recommended Dose: 8 mg, 1 times / day Route: oral Route: multiple Dose: 8 mg, 1 times / day Sources: |
unhealthy, adult n = 366 Health Status: unhealthy Condition: Schizophrenia Age Group: adult Population Size: 366 Sources: |
Parkinsonism | 0.8% Disc. AE |
8 mg 1 times / day multiple, oral (max) Recommended Dose: 8 mg, 1 times / day Route: oral Route: multiple Dose: 8 mg, 1 times / day Sources: |
unhealthy, adult n = 366 Health Status: unhealthy Condition: Schizophrenia Age Group: adult Population Size: 366 Sources: |
Somnolence | 0.8% Disc. AE |
8 mg 1 times / day multiple, oral (max) Recommended Dose: 8 mg, 1 times / day Route: oral Route: multiple Dose: 8 mg, 1 times / day Sources: |
unhealthy, adult n = 366 Health Status: unhealthy Condition: Schizophrenia Age Group: adult Population Size: 366 Sources: |
Agitation | 1.1% Disc. AE |
8 mg 1 times / day multiple, oral (max) Recommended Dose: 8 mg, 1 times / day Route: oral Route: multiple Dose: 8 mg, 1 times / day Sources: |
unhealthy, adult n = 366 Health Status: unhealthy Condition: Schizophrenia Age Group: adult Population Size: 366 Sources: |
Dizziness | 1.4% Disc. AE |
8 mg 1 times / day multiple, oral (max) Recommended Dose: 8 mg, 1 times / day Route: oral Route: multiple Dose: 8 mg, 1 times / day Sources: |
unhealthy, adult n = 366 Health Status: unhealthy Condition: Schizophrenia Age Group: adult Population Size: 366 Sources: |
Nausea | 1.4% Disc. AE |
8 mg 1 times / day multiple, oral (max) Recommended Dose: 8 mg, 1 times / day Route: oral Route: multiple Dose: 8 mg, 1 times / day Sources: |
unhealthy, adult n = 366 Health Status: unhealthy Condition: Schizophrenia Age Group: adult Population Size: 366 Sources: |
Anorexia | 1% Disc. AE |
6 mg 1 times / day multiple, oral (max) Recommended Dose: 6 mg, 1 times / day Route: oral Route: multiple Dose: 6 mg, 1 times / day Sources: |
unhealthy, child n = 106 Health Status: unhealthy Condition: Schizophrenia Age Group: child Population Size: 106 Sources: |
Anxiety | 1% Disc. AE |
6 mg 1 times / day multiple, oral (max) Recommended Dose: 6 mg, 1 times / day Route: oral Route: multiple Dose: 6 mg, 1 times / day Sources: |
unhealthy, child n = 106 Health Status: unhealthy Condition: Schizophrenia Age Group: child Population Size: 106 Sources: |
Ataxia | 1% Disc. AE |
6 mg 1 times / day multiple, oral (max) Recommended Dose: 6 mg, 1 times / day Route: oral Route: multiple Dose: 6 mg, 1 times / day Sources: |
unhealthy, child n = 106 Health Status: unhealthy Condition: Schizophrenia Age Group: child Population Size: 106 Sources: |
Hypotension | 1% Disc. AE |
6 mg 1 times / day multiple, oral (max) Recommended Dose: 6 mg, 1 times / day Route: oral Route: multiple Dose: 6 mg, 1 times / day Sources: |
unhealthy, child n = 106 Health Status: unhealthy Condition: Schizophrenia Age Group: child Population Size: 106 Sources: |
Palpitation | 1% Disc. AE |
6 mg 1 times / day multiple, oral (max) Recommended Dose: 6 mg, 1 times / day Route: oral Route: multiple Dose: 6 mg, 1 times / day Sources: |
unhealthy, child n = 106 Health Status: unhealthy Condition: Schizophrenia Age Group: child Population Size: 106 Sources: |
Dizziness | 2% Disc. AE |
6 mg 1 times / day multiple, oral (max) Recommended Dose: 6 mg, 1 times / day Route: oral Route: multiple Dose: 6 mg, 1 times / day Sources: |
unhealthy, child n = 106 Health Status: unhealthy Condition: Schizophrenia Age Group: child Population Size: 106 Sources: |
Somnolence | 2% Disc. AE |
6 mg 1 times / day multiple, oral (max) Recommended Dose: 6 mg, 1 times / day Route: oral Route: multiple Dose: 6 mg, 1 times / day Sources: |
unhealthy, child n = 106 Health Status: unhealthy Condition: Schizophrenia Age Group: child Population Size: 106 Sources: |
Abdominal pain | 2% Disc. AE |
6 mg 1 times / day multiple, oral (max) Recommended Dose: 6 mg, 1 times / day Route: oral Route: multiple Dose: 6 mg, 1 times / day Sources: |
unhealthy, child n = 111 Health Status: unhealthy Condition: Bipolar Mania Age Group: child Population Size: 111 Sources: |
Vomiting | 2% Disc. AE |
6 mg 1 times / day multiple, oral (max) Recommended Dose: 6 mg, 1 times / day Route: oral Route: multiple Dose: 6 mg, 1 times / day Sources: |
unhealthy, child n = 111 Health Status: unhealthy Condition: Bipolar Mania Age Group: child Population Size: 111 Sources: |
Nausea | 3% Disc. AE |
6 mg 1 times / day multiple, oral (max) Recommended Dose: 6 mg, 1 times / day Route: oral Route: multiple Dose: 6 mg, 1 times / day Sources: |
unhealthy, child n = 111 Health Status: unhealthy Condition: Bipolar Mania Age Group: child Population Size: 111 Sources: |
Somnolence | 5% Disc. AE |
6 mg 1 times / day multiple, oral (max) Recommended Dose: 6 mg, 1 times / day Route: oral Route: multiple Dose: 6 mg, 1 times / day Sources: |
unhealthy, child n = 111 Health Status: unhealthy Condition: Bipolar Mania Age Group: child Population Size: 111 Sources: |
Overview
CYP3A4 | CYP2C9 | CYP2D6 | hERG |
---|---|---|---|
Drug as perpetrator
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
Page: 1.0 |
moderate [IC50 38.1 uM] | |||
Page: 37.0 |
weak | no (co-administration study) Comment: RISPERDAL did not significantly affect the pharmacokinetics of donepezil and galantamine, which are metabolized by CYP2D6 Page: 37.0 |
||
Sources: https://www.nature.com/articles/1301181 |
yes [IC50 15.78 uM] |
Drug as victim
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
Page: 36.0 |
major | yes (co-administration study) Comment: Fluoxetine and paroxetine (CYP 2D6 inhibitors) have been shown to increase the plasma concentration of risperidone 2.5-2.8 fold and 3-9 fold, respectively Page: 36.0 |
||
Sources: https://link.springer.com/article/10.1007/PL00005334 Page: 3.0 |
minor | |||
Sources: https://pubmed.ncbi.nlm.nih.gov/15270204/ Page: 4.0 |
minor | yes (co-administration study) Comment: Carbamazepine co-administration with oral RISPERDAL decreased the steady-state plasma concentrations of risperidone by about 50%; Sources: https://pubmed.ncbi.nlm.nih.gov/15270204/ Page: 4.0 |
||
Sources: https://peerj.com/articles/2081/ |
no | |||
Sources: https://link.springer.com/article/10.1007/PL00005334 Page: 3.0 |
no | |||
Sources: https://link.springer.com/article/10.1007/PL00005334 Page: 3.0 |
no | |||
Sources: https://link.springer.com/article/10.1007/PL00005334 Page: 3.0 |
no | |||
Sources: https://link.springer.com/article/10.1007/PL00005334 Page: 3.0 |
no | |||
Sources: https://link.springer.com/article/10.1007/PL00005334 Page: 3.0 |
no | |||
Page: 8.0 |
no | |||
Sources: https://pubmed.ncbi.nlm.nih.gov/16936711/ Page: 1.0 |
yes |
Tox targets
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
PubMed
Title | Date | PubMed |
---|---|---|
Cytochrome P450 2D6 genotype and steady state plasma levels of risperidone and 9-hydroxyrisperidone. | 1999 Dec |
|
Two cases of risperidone-induced tardive dyskinesia and a review of the literature. | 1999 Jul |
|
Risperidone-induced tardive dystonia and psychosis. | 1999 Mar 20 |
|
Risperidone-induced absence of ejaculation. | 1999 Sep |
|
Risperidone in treatment-refractory schizophrenia. | 1999 Sep |
|
Case report of withdrawal syndrome after olanzapine discontinuation. | 2000 Aug |
|
Risperidone versus haloperidol in psychotic patients with disturbing neuroleptic-induced extrapyramidal symptoms: a double-blind, multi-center trial. | 2000 Dec 15 |
|
Attention deficit-hyperactivity disorder may be a risk factor for treatment-emergent tardive dyskinesia induced by risperidone. | 2000 Feb |
|
Further evidence that behavioral tests and neuropeptide mRNA and tissue level alterations can differentiate between typical and atypical antipsychotic drugs. | 2000 Jul |
|
Acute confusional states during treatment with risperidone. | 2000 Jun |
|
Subjective experience and striatal dopamine D(2) receptor occupancy in patients with schizophrenia stabilized by olanzapine or risperidone. | 2000 Jun |
|
Relation between cholinesterase inhibitor and Pisa syndrome. | 2000 Jun 24 |
|
Risperidone treatment of drug-related psychosis in patients with parkinsonism. | 2000 Mar |
|
Effects of atypical neuroleptics on sustained attention deficits in schizophrenia: a trial of risperidone versus haloperidol. | 2000 Mar |
|
Doses of olanzapine, risperidone, and haloperidol used in clinical practice: results of a prospective pharmacoepidemiologic study. EFESO Study Group. Estudio Farmacoepidemiologico en la Esquizofrenia con Olanzapina. | 2000 May |
|
The safety of olanzapine compared with other antipsychotic drugs: results of an observational prospective study in patients with schizophrenia (EFESO Study). Pharmacoepidemiologic Study of Olanzapine in Schizophrenia. | 2000 May |
|
[Valproic acid in prophylaxis of bipolar disorder. A case of valproate-induced encephalopathy]. | 2000 May |
|
Lack of specific effects of selective D(1) and D(2) dopamine antagonists vs. risperidone on morphine-induced hyperactivity. | 2000 May |
|
Serotonin and dopamine antagonism in obsessive-compulsive disorder: effect of atypical antipsychotic drugs. | 2000 Nov |
|
Risperidone-associated hyperprolactinemia. | 2000 Nov-Dec |
|
Risperidone and tardive dyskinesia: a case of blepharospasm. | 2000 Oct |
|
Inverse agonist activity of atypical antipsychotic drugs at human 5-hydroxytryptamine2C receptors. | 2000 Oct |
|
The effects of olanzapine, risperidone, and haloperidol on plasma prolactin levels in patients with schizophrenia. | 2000 Sep |
|
Long-term risperidone for pervasive developmental disorder: efficacy, tolerability, and discontinuation. | 2000 Summer |
|
Weight change and atypical antipsychotic treatment in patients with schizophrenia. | 2001 |
|
Atypical antipsychotics: new directions and new challenges in the treatment of schizophrenia. | 2001 |
|
Effective treatment of aggression and impulsivity in antisocial personality disorder with risperidone. | 2001 Apr |
|
Risperidone-induced retrograde ejaculation. | 2001 Apr |
|
An MRI study of basal ganglia volumes in first-episode schizophrenia patients treated with risperidone. | 2001 Apr |
|
Dynamic dopamine-antagonist interactions at recombinant human dopamine D(2short) receptor: dopamine-bound versus antagonist-bound receptor states. | 2001 Apr |
|
Health care utilization in patients with schizophrenia maintained on atypical versus conventional antipsychotics. | 2001 Feb |
|
Dose relationship of limbic-cortical D2-dopamine receptor occupancy with risperidone. | 2001 Feb |
|
Treatment of psychogenic polydipsia: comparison of risperidone and olanzapine, and the effects of an adjunctive angiotensin-II receptor blocking drug (irbesartan). | 2001 Feb |
|
Addition of risperidone to clozapine therapy in chronically psychotic inpatients. | 2001 Feb |
|
Weight gain with risperidone among patients with mental retardation: effect of calorie restriction. | 2001 Feb |
|
Drug induced akathisia, suicidal ideation and its treatment in the elderly. | 2001 Feb |
|
Combination risperidone and quetiapine therapy in refractory schizophrenia. | 2001 Feb |
|
A case of risperidone-induced stuttering. | 2001 Feb |
|
Rehospitalization rates of chronically ill schizophrenic patients discharged on a regimen of risperidone, olanzapine, or conventional antipsychotics. | 2001 Feb |
|
Hyperthermia and chronic pancerebellar syndrome after cocaine abuse. | 2001 Feb 26 |
|
Acute and long-term treatment of catatonia with risperidone. | 2001 Jan |
|
Does risperidone have a place in the treatment of nonschizophrenic patients? | 2001 Jan |
|
Consistency of atypical antipsychotic superiority to placebo in recent clinical trials. | 2001 Jan 1 |
|
Hyperfunction of dopaminergic and serotonergic neuronal systems in mice lacking the NMDA receptor epsilon1 subunit. | 2001 Jan 15 |
|
Antipsychotic drugs classified by their effects on the release of dopamine and noradrenaline in the prefrontal cortex and striatum. | 2001 Jan 26 |
|
[Viewpoint of schizophrenic patients: a European survey]. | 2001 Jan-Feb |
|
The evaluation of multiple surrogate endpoints. | 2001 Mar |
|
Fixed-dosed risperidone in mania: an open experimental trial. | 2001 Mar |
|
Does fast dissociation from the dopamine d(2) receptor explain the action of atypical antipsychotics?: A new hypothesis. | 2001 Mar |
|
Pharmacological characterization of locomotor sensitization induced by chronic phencyclidine administration. | 2001 Mar |
Sample Use Guides
Initial dosing is generally 2 mg/day. Dose increases should then occur at intervals not less than 24 hours, in increments of 1–2 mg/day, as tolerated, to a recommended dose of 4–8 mg/day. Effective dose range - 0.5-16 mg (disease dependent).
Route of Administration:
Other
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/18755815
Measurement of ATP contents in the neuronal cell line showed significantly increased levels after a 24-h treatment with 25 microg/mL risperidone.
Substance Class |
Chemical
Created
by
admin
on
Edited
Fri Jun 25 21:03:09 UTC 2021
by
admin
on
Fri Jun 25 21:03:09 UTC 2021
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Record UNII |
L6UH7ZF8HC
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Record Status |
Validated (UNII)
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Record Version |
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Common Name | English | ||
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Common Name | English | ||
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Code | English | ||
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Common Name | English | ||
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Code | English | ||
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Code | English | ||
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Common Name | English | ||
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Common Name | English |
Classification Tree | Code System | Code | ||
---|---|---|---|---|
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WHO-ATC |
N05AX08
Created by
admin on Fri Jun 25 21:03:09 UTC 2021 , Edited by admin on Fri Jun 25 21:03:09 UTC 2021
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NDF-RT |
N0000175430
Created by
admin on Fri Jun 25 21:03:09 UTC 2021 , Edited by admin on Fri Jun 25 21:03:09 UTC 2021
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||
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NCI_THESAURUS |
C29710
Created by
admin on Fri Jun 25 21:03:09 UTC 2021 , Edited by admin on Fri Jun 25 21:03:09 UTC 2021
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WHO-VATC |
QN05AX08
Created by
admin on Fri Jun 25 21:03:09 UTC 2021 , Edited by admin on Fri Jun 25 21:03:09 UTC 2021
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LIVERTOX |
852
Created by
admin on Fri Jun 25 21:03:09 UTC 2021 , Edited by admin on Fri Jun 25 21:03:09 UTC 2021
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|
FDA ORPHAN DRUG |
326110
Created by
admin on Fri Jun 25 21:03:09 UTC 2021 , Edited by admin on Fri Jun 25 21:03:09 UTC 2021
|
Code System | Code | Type | Description | ||
---|---|---|---|---|---|
|
CHEMBL85
Created by
admin on Fri Jun 25 21:03:09 UTC 2021 , Edited by admin on Fri Jun 25 21:03:09 UTC 2021
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PRIMARY | |||
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Risperidone
Created by
admin on Fri Jun 25 21:03:09 UTC 2021 , Edited by admin on Fri Jun 25 21:03:09 UTC 2021
|
PRIMARY | |||
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106266-06-2
Created by
admin on Fri Jun 25 21:03:09 UTC 2021 , Edited by admin on Fri Jun 25 21:03:09 UTC 2021
|
PRIMARY | |||
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2389
Created by
admin on Fri Jun 25 21:03:09 UTC 2021 , Edited by admin on Fri Jun 25 21:03:09 UTC 2021
|
PRIMARY | |||
|
7580
Created by
admin on Fri Jun 25 21:03:09 UTC 2021 , Edited by admin on Fri Jun 25 21:03:09 UTC 2021
|
PRIMARY | |||
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M9631
Created by
admin on Fri Jun 25 21:03:09 UTC 2021 , Edited by admin on Fri Jun 25 21:03:09 UTC 2021
|
PRIMARY | Merck Index | ||
|
5073
Created by
admin on Fri Jun 25 21:03:09 UTC 2021 , Edited by admin on Fri Jun 25 21:03:09 UTC 2021
|
PRIMARY | |||
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RISPERIDONE
Created by
admin on Fri Jun 25 21:03:09 UTC 2021 , Edited by admin on Fri Jun 25 21:03:09 UTC 2021
|
PRIMARY | |||
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D018967
Created by
admin on Fri Jun 25 21:03:09 UTC 2021 , Edited by admin on Fri Jun 25 21:03:09 UTC 2021
|
PRIMARY | |||
|
6085
Created by
admin on Fri Jun 25 21:03:09 UTC 2021 , Edited by admin on Fri Jun 25 21:03:09 UTC 2021
|
PRIMARY | |||
|
SUB10335MIG
Created by
admin on Fri Jun 25 21:03:09 UTC 2021 , Edited by admin on Fri Jun 25 21:03:09 UTC 2021
|
PRIMARY | |||
|
1604654
Created by
admin on Fri Jun 25 21:03:09 UTC 2021 , Edited by admin on Fri Jun 25 21:03:09 UTC 2021
|
PRIMARY | USP-RS | ||
|
106266-06-2
Created by
admin on Fri Jun 25 21:03:09 UTC 2021 , Edited by admin on Fri Jun 25 21:03:09 UTC 2021
|
PRIMARY | |||
|
35636
Created by
admin on Fri Jun 25 21:03:09 UTC 2021 , Edited by admin on Fri Jun 25 21:03:09 UTC 2021
|
PRIMARY | RxNorm | ||
|
C29416
Created by
admin on Fri Jun 25 21:03:09 UTC 2021 , Edited by admin on Fri Jun 25 21:03:09 UTC 2021
|
PRIMARY | |||
|
96
Created by
admin on Fri Jun 25 21:03:09 UTC 2021 , Edited by admin on Fri Jun 25 21:03:09 UTC 2021
|
PRIMARY | |||
|
DB00734
Created by
admin on Fri Jun 25 21:03:09 UTC 2021 , Edited by admin on Fri Jun 25 21:03:09 UTC 2021
|
PRIMARY | |||
|
L6UH7ZF8HC
Created by
admin on Fri Jun 25 21:03:09 UTC 2021 , Edited by admin on Fri Jun 25 21:03:09 UTC 2021
|
PRIMARY |
Related Record | Type | Details | ||
---|---|---|---|---|
|
TARGET -> INHIBITOR |
INHIBITOR
Ki
|
||
|
TARGET -> INHIBITOR |
INHIBITOR
Ki
|
||
|
TARGET -> INHIBITOR |
INHIBITOR
Ki
|
||
|
TARGET -> INHIBITOR |
INHIBITOR
Ki
|
||
|
TARGET -> INHIBITOR |
INHIBITOR
Ki
|
||
|
TARGET -> INHIBITOR |
INHIBITOR
Ki
|
||
|
TARGET -> INHIBITOR |
INHIBITOR
Ki
|
||
|
TARGET -> INHIBITOR |
INHIBITOR
Ki
|
||
|
BASIS OF STRENGTH->SUBSTANCE |
ASSAY (TITRATION)
EP
|
||
|
BASIS OF STRENGTH->SUBSTANCE |
ASSAY (HPLC)
USP
|
||
|
NON-INHIBITOR->OFF-TARGET |
|
||
|
TARGET -> INHIBITOR |
INHIBITOR
Ki
|
||
|
METABOLIC ENZYME -> SUBSTRATE | |||
|
TARGET -> INHIBITOR |
INHIBITOR
Ki
|
||
|
TARGET -> INHIBITOR |
INHIBITOR
Ki
|
||
|
TARGET -> INHIBITOR |
INHIBITOR
|
||
|
NON-AGONIST->OFF-TARGET |
Ki
|
||
|
INHIBITOR -> TARGET |
INHIBITOR
Ki
|
||
|
TARGET -> INHIBITOR |
INHIBITOR
Ki
|
||
|
BINDER->LIGAND |
|
||
|
NON-INHIBITOR->OFF-TARGET |
Ki
|
||
|
TARGET -> ACTIVATOR |
INHIBITOR
Ki
|
||
|
TARGET -> INHIBITOR |
INHIBITOR
Ki
|
||
|
SALT/SOLVATE -> PARENT | |||
|
TARGET -> INHIBITOR |
INHIBITOR
Ki
|
||
|
NON-INHIBITOR->OFF-TARGET |
Ki
|
||
|
NON-INHIBITOR->OFF-TARGET |
|
||
|
TARGET -> INHIBITOR |
INHIBITOR
Ki
|
||
|
TRANSPORTER -> SUBSTRATE |
INHIBITOR
IC50
|
Related Record | Type | Details | ||
---|---|---|---|---|
|
METABOLITE ACTIVE -> PARENT |
MAJOR
PLASMA
|
||
|
METABOLITE ACTIVE -> PARENT |
in vitro mediators are CYP2D6 and CYP3A4
MAJOR
|
Related Record | Type | Details | ||
---|---|---|---|---|
|
IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
|
||
|
IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
|
||
|
IMPURITY -> PARENT |
UNSPECIFIED
EP
|
||
|
IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
|
||
|
IMPURITY -> PARENT |
not more than the area of the principal peak in the chromatogram obtained with reference solution (b)
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
|
||
|
IMPURITY -> PARENT |
UNSPECIFIED
EP
|
||
|
IMPURITY -> PARENT |
not more than the area of the principal peak in the chromatogram obtained with reference solution (b)
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
|
||
|
IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
|
||
|
IMPURITY -> PARENT |
UNSPECIFIED
EP
|
||
|
IMPURITY -> PARENT |
UNSPECIFIED
EP
|
||
|
IMPURITY -> PARENT |
UNSPECIFIED
EP
|
||
|
IMPURITY -> PARENT |
not more than the area of the principal peak in the chromatogram obtained with reference solution (b)
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
|
||
|
IMPURITY -> PARENT |
not more than the area of the principal peak in the chromatogram obtained with reference solution (b)
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
|
||
|
IMPURITY -> PARENT |
UNSPECIFIED
EP
|
||
|
IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
|
||
|
IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
|
||
|
IMPURITY -> PARENT |
not more than the area of the principal peak in the chromatogram obtained with reference solution (b)
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
|
Related Record | Type | Details | ||
---|---|---|---|---|
|
ACTIVE MOIETY |