Details
Stereochemistry | ACHIRAL |
Molecular Formula | C23H27FN4O2 |
Molecular Weight | 410.4845 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
CC1=C(CCN2CCC(CC2)C3=NOC4=C3C=CC(F)=C4)C(=O)N5CCCCC5=N1
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 | 410.4845 |
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 Date1993 |
|||
Primary | RISPERDAL Approved UseINDICATIONS & USAGE Risperidone tablets are indicated for the acute and maintenance treatment of schizophrenia [see Clinical Studies (14.1) Launch Date1993 |
|||
Primary | RISPERDAL Approved UseINDICATIONS & USAGE Risperidone tablets are indicated for the acute and maintenance treatment of schizophrenia [see Clinical Studies (14.1) Launch Date1993 |
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 |
---|---|---|---|
OverviewOther
Other Inhibitor | Other Substrate | Other Inducer |
---|---|---|
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 |
---|---|---|
Dopamine receptor responsivity in schizophrenic patients before and after switch from haloperidol to risperidone. | 1999 Dec 20 |
|
A case of delayed NMS induced by risperidone. | 2000 Feb |
|
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 |
|
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 |
|
Risperidone-associated hyperprolactinemia. | 2000 Nov-Dec |
|
The serotonin 5-HT(2A) receptor subtype does not mediate apomorphine-induced aggressive behaviour in male Wistar rats. | 2000 Oct |
|
The effects of olanzapine, risperidone, and haloperidol on plasma prolactin levels in patients with schizophrenia. | 2000 Sep |
|
A naturalistic comparison of clozapine, risperidone, and olanzapine in the treatment of bipolar disorder. | 2000 Sep |
|
Weight change and atypical antipsychotic treatment in patients with schizophrenia. | 2001 |
|
Evidence for the effectiveness of olanzapine among patients nonresponsive and/or intolerant to risperidone. | 2001 |
|
Antipsychotic medications and the elderly: effects on cognition and implications for use. | 2001 |
|
Olanzapine: an updated review of its use in the management of schizophrenia. | 2001 |
|
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 |
|
Protein thiol oxidation by haloperidol results in inhibition of mitochondrial complex I in brain regions: comparison with atypical antipsychotics. | 2001 Apr |
|
Health care utilization in patients with schizophrenia maintained on atypical versus conventional antipsychotics. | 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 |
|
Priapism associated with polypharmacy. | 2001 Feb |
|
Weight gain with risperidone among patients with mental retardation: effect of calorie restriction. | 2001 Feb |
|
Long-term treatment of chronic schizophrenia with risperidone: a study with plasma levels. | 2001 Feb |
|
Drug induced akathisia, suicidal ideation and its treatment in the elderly. | 2001 Feb |
|
Tolerability and effectiveness of atypical antipsychotics in male geriatric inpatients. | 2001 Feb |
|
Combination risperidone and quetiapine therapy in refractory schizophrenia. | 2001 Feb |
|
A case of risperidone-induced stuttering. | 2001 Feb |
|
Atypical antipsychotics and cardiovascular risk in schizophrenic patients. | 2001 Feb |
|
Adverse drug interaction between risperidone and carbamazepine in a patient with chronic schizophrenia and deficient CYP2D6 activity. | 2001 Feb |
|
Rehospitalization rates of chronically ill schizophrenic patients discharged on a regimen of risperidone, olanzapine, or conventional antipsychotics. | 2001 Feb |
|
Receptor-mediated regulation of serotonin output in the rat dorsal raphe nucleus: effects of risperidone. | 2001 Jan |
|
Risperidone versus pimozide in Tourette's disorder: a comparative double-blind parallel-group study. | 2001 Jan |
|
Acute and long-term treatment of catatonia with risperidone. | 2001 Jan |
|
Bodyweight gain with atypical antipsychotics. A comparative review. | 2001 Jan |
|
Risperidone-induced cholestatic hepatitis. | 2001 Jan |
|
Does risperidone have a place in the treatment of nonschizophrenic patients? | 2001 Jan |
|
Relationship between plasma risperidone and 9-hydroxyrisperidone concentrations and clinical response in patients with schizophrenia. | 2001 Jan 1 |
|
Consistency of atypical antipsychotic superiority to placebo in recent clinical trials. | 2001 Jan 1 |
|
Dopamine transporter density in young patients with schizophrenia assessed with [123]FP-CIT SPECT. | 2001 Jan 15 |
|
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 |
|
5-HT(2A) and D(2) receptor blockade increases cortical DA release via 5-HT(1A) receptor activation: a possible mechanism of atypical antipsychotic-induced cortical dopamine release. | 2001 Mar |
|
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 |
|
Estrogen - a potential treatment for schizophrenia. | 2001 Mar 1 |
|
Effects of olanzapine and other antipsychotics on cognitive function in chronic schizophrenia: a longitudinal study. | 2001 Mar 1 |
|
Risperidone addition and psychotic exacerbation. | 2001 Winter |
|
Full remission of panic attacks in a schizophrenic patient after switching from haloperidol to risperidone. | 2001 Winter |
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
Sat Dec 16 17:26:08 GMT 2023
by
admin
on
Sat Dec 16 17:26:08 GMT 2023
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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 |
Classification Tree | Code System | Code | ||
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WHO-ATC |
N05AX08
Created by
admin on Sat Dec 16 17:26:12 GMT 2023 , Edited by admin on Sat Dec 16 17:26:12 GMT 2023
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NDF-RT |
N0000175430
Created by
admin on Sat Dec 16 17:26:12 GMT 2023 , Edited by admin on Sat Dec 16 17:26:12 GMT 2023
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NCI_THESAURUS |
C29710
Created by
admin on Sat Dec 16 17:26:12 GMT 2023 , Edited by admin on Sat Dec 16 17:26:12 GMT 2023
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WHO-VATC |
QN05AX08
Created by
admin on Sat Dec 16 17:26:12 GMT 2023 , Edited by admin on Sat Dec 16 17:26:12 GMT 2023
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LIVERTOX |
NBK548906
Created by
admin on Sat Dec 16 17:26:12 GMT 2023 , Edited by admin on Sat Dec 16 17:26:12 GMT 2023
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FDA ORPHAN DRUG |
326110
Created by
admin on Sat Dec 16 17:26:12 GMT 2023 , Edited by admin on Sat Dec 16 17:26:12 GMT 2023
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Code System | Code | Type | Description | ||
---|---|---|---|---|---|
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CHEMBL85
Created by
admin on Sat Dec 16 17:26:12 GMT 2023 , Edited by admin on Sat Dec 16 17:26:12 GMT 2023
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PRIMARY | |||
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Risperidone
Created by
admin on Sat Dec 16 17:26:12 GMT 2023 , Edited by admin on Sat Dec 16 17:26:12 GMT 2023
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PRIMARY | |||
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DTXSID8045193
Created by
admin on Sat Dec 16 17:26:12 GMT 2023 , Edited by admin on Sat Dec 16 17:26:12 GMT 2023
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PRIMARY | |||
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2389
Created by
admin on Sat Dec 16 17:26:12 GMT 2023 , Edited by admin on Sat Dec 16 17:26:12 GMT 2023
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PRIMARY | |||
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7580
Created by
admin on Sat Dec 16 17:26:12 GMT 2023 , Edited by admin on Sat Dec 16 17:26:12 GMT 2023
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PRIMARY | |||
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100000092091
Created by
admin on Sat Dec 16 17:26:12 GMT 2023 , Edited by admin on Sat Dec 16 17:26:12 GMT 2023
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PRIMARY | |||
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m9631
Created by
admin on Sat Dec 16 17:26:12 GMT 2023 , Edited by admin on Sat Dec 16 17:26:12 GMT 2023
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PRIMARY | Merck Index | ||
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5073
Created by
admin on Sat Dec 16 17:26:12 GMT 2023 , Edited by admin on Sat Dec 16 17:26:12 GMT 2023
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PRIMARY | |||
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RISPERIDONE
Created by
admin on Sat Dec 16 17:26:12 GMT 2023 , Edited by admin on Sat Dec 16 17:26:12 GMT 2023
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PRIMARY | |||
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BB-19
Created by
admin on Sat Dec 16 17:26:12 GMT 2023 , Edited by admin on Sat Dec 16 17:26:12 GMT 2023
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PRIMARY | |||
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D018967
Created by
admin on Sat Dec 16 17:26:12 GMT 2023 , Edited by admin on Sat Dec 16 17:26:12 GMT 2023
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PRIMARY | |||
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6085
Created by
admin on Sat Dec 16 17:26:12 GMT 2023 , Edited by admin on Sat Dec 16 17:26:12 GMT 2023
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PRIMARY | |||
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1604654
Created by
admin on Sat Dec 16 17:26:12 GMT 2023 , Edited by admin on Sat Dec 16 17:26:12 GMT 2023
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PRIMARY | |||
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SUB10335MIG
Created by
admin on Sat Dec 16 17:26:12 GMT 2023 , Edited by admin on Sat Dec 16 17:26:12 GMT 2023
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PRIMARY | |||
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8871
Created by
admin on Sat Dec 16 17:26:12 GMT 2023 , Edited by admin on Sat Dec 16 17:26:12 GMT 2023
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PRIMARY | |||
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106266-06-2
Created by
admin on Sat Dec 16 17:26:12 GMT 2023 , Edited by admin on Sat Dec 16 17:26:12 GMT 2023
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PRIMARY | |||
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L6UH7ZF8HC
Created by
admin on Sat Dec 16 17:26:12 GMT 2023 , Edited by admin on Sat Dec 16 17:26:12 GMT 2023
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PRIMARY | |||
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35636
Created by
admin on Sat Dec 16 17:26:12 GMT 2023 , Edited by admin on Sat Dec 16 17:26:12 GMT 2023
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PRIMARY | RxNorm | ||
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C29416
Created by
admin on Sat Dec 16 17:26:12 GMT 2023 , Edited by admin on Sat Dec 16 17:26:12 GMT 2023
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PRIMARY | |||
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96
Created by
admin on Sat Dec 16 17:26:12 GMT 2023 , Edited by admin on Sat Dec 16 17:26:12 GMT 2023
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PRIMARY | |||
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DB00734
Created by
admin on Sat Dec 16 17:26:12 GMT 2023 , Edited by admin on Sat Dec 16 17:26:12 GMT 2023
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PRIMARY | |||
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L6UH7ZF8HC
Created by
admin on Sat Dec 16 17:26:12 GMT 2023 , Edited by admin on Sat Dec 16 17:26:12 GMT 2023
|
PRIMARY | |||
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759895
Created by
admin on Sat Dec 16 17:26:12 GMT 2023 , Edited by admin on Sat Dec 16 17:26:12 GMT 2023
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PRIMARY |
Related Record | Type | Details | ||
---|---|---|---|---|
|
TARGET->WEAK INHIBITOR |
INHIBITOR
Ki
|
||
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METABOLIC ENZYME -> SUBSTRATE | |||
|
TARGET -> INHIBITOR |
INHIBITOR
Ki
|
||
|
TARGET->WEAK INHIBITOR |
INHIBITOR
Ki
|
||
|
TARGET -> INHIBITOR |
INHIBITOR
Ki
|
||
|
TARGET -> INHIBITOR |
INHIBITOR
Ki
|
||
|
TARGET->WEAK 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
|
||
|
OFF TARGET->NON-INHIBITOR |
|
||
|
TARGET->WEAK INHIBITOR |
INHIBITOR
Ki
|
||
|
TARGET -> INHIBITOR |
INHIBITOR
Ki
|
||
|
TARGET->WEAK INHIBITOR |
INHIBITOR
Ki
|
||
|
TARGET -> INHIBITOR |
INHIBITOR
|
||
|
OFF-TARGET->NON-AGONIST |
Ki
|
||
|
TARGET -> INHIBITOR |
INHIBITOR
Ki
|
||
|
TARGET -> INHIBITOR |
INHIBITOR
Ki
|
||
|
BINDER->LIGAND |
|
||
|
OFF TARGET->NON-INHIBITOR |
Ki
|
||
|
TARGET -> ACTIVATOR |
INHIBITOR
Ki
|
||
|
TARGET -> INHIBITOR |
INHIBITOR
Ki
|
||
|
SALT/SOLVATE -> PARENT |
|
||
|
TARGET->WEAK INHIBITOR |
INHIBITOR
Ki
|
||
|
OFF TARGET->NON-INHIBITOR |
Ki
|
||
|
OFF-TARGET->NON-INHIBITOR |
|
||
|
TARGET->WEAK 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
|
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 |
|
||
|
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 | ||
---|---|---|---|---|
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ACTIVE MOIETY |
|