RISPERIDONE HEXANOATE

Details

Stereochemistry	ACHIRAL
Molecular Formula	C23H27FN4O2.C6H12O2
Molecular Weight	526.6428
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

CCCCCC(O)=O.CC1=C(CCN2CCC(CC2)C3=NOC4=C3C=CC(F)=C4)C(=O)N5CCCCC5=N1

InChI

InChIKey=KBFKXAXGRPWQON-UHFFFAOYSA-N

InChI=1S/C23H27FN4O2.C6H12O2/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;1-2-3-4-5-6(7)8/h5-6,14,16H,2-4,7-13H2,1H3;2-5H2,1H3,(H,7,8)

HIDE SMILES / InChI

Molecular Formula	C6H12O2
Molecular Weight	116.1583
Charge	0
Count

Stereochemistry	ACHIRAL
Additional Stereochemistry	No
Defined Stereocenters	0 / 0
E/Z Centers	0
Optical Activity	NONE

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

Description
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

Approval Year

Targets

Primary Target	Pharmacology	Potency
Adrenergic receptor alpha-1 169 Target ID: CHEMBL2094251 Sources: https://www.ncbi.nlm.nih.gov/pubmed/11132243	Antagonist 2760	2.7 nM [Kd]
Dopamine D2 receptor 297 Target ID: CHEMBL217 Sources: https://www.ncbi.nlm.nih.gov/pubmed/11132243	Antagonist 2760	3.8 nM [Kd]
Serotonin 1d (5-HT1d) receptor 52 Target ID: CHEMBL1983 Sources: https://www.ncbi.nlm.nih.gov/pubmed/11132243	Antagonist 2760	3.9 nM [Kd]
Serotonin 2a (5-HT2a) receptor 230 Target ID: CHEMBL224 Sources: https://www.ncbi.nlm.nih.gov/pubmed/11132243 http://www.accessdata.fda.gov/drugsatfda_docs/label/2016/020272s077,020588s065,021346s055,021444s051lbl.pdf	Antagonist 2760	0.15 nM [Kd]

Conditions

Condition	Modality	Highest Phase	Product
Schizophrenia 295 Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2016/020272s077,020588s065,021346s055,021444s051lbl.pdf	Primary	Approved 8360	RISPERDAL Approved Use INDICATIONS & USAGE Risperidone tablets are indicated for the acute and maintenance treatment of schizophrenia [see Clinical Studies (14.1) Launch Date 7.5712319E11
Acute manic or mixed episodes associated with Bipolar I disorder 2 Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2016/020272s077,020588s065,021346s055,021444s051lbl.pdf	Primary	Approved 8360	RISPERDAL Approved Use INDICATIONS & USAGE Risperidone tablets are indicated for the acute and maintenance treatment of schizophrenia [see Clinical Studies (14.1) Launch Date 7.5712319E11
Irritability associated with autistic disorder 2 Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2016/020272s077,020588s065,021346s055,021444s051lbl.pdf	Primary	Approved 8360	RISPERDAL Approved Use INDICATIONS & USAGE Risperidone tablets are indicated for the acute and maintenance treatment of schizophrenia [see Clinical Studies (14.1) Launch Date 7.5712319E11

C_max

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

T_1/2

Value	Dose	Co-administered	Analyte	Population
20 h DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2010/020588s046lbl.pdf	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

F_unbound

Value	Dose	Co-administered	Analyte	Population
10% DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2010/020588s046lbl.pdf	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: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/020272s056,020588s044,021346s033,021444s03lbl.pdf	unhealthy, adult n = 198 Health Status: unhealthy Condition: Schizophrenia Age Group: adult Population Size: 198 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/020272s056,020588s044,021346s033,021444s03lbl.pdf	Disc. AE: Dizziness, Agitation... AEs leading to discontinuation/dose reduction: Dizziness (1%) Agitation (1%) Somnolence (0.5%) Hypotension postural (0.5%) Tachycardia (0.5%) Akathisia (1%) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/020272s056,020588s044,021346s033,021444s03lbl.pdf
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: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/020272s056,020588s044,021346s033,021444s03lbl.pdf	unhealthy, adult n = 448 Health Status: unhealthy Condition: Bipolar Mania Age Group: adult Population Size: 448 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/020272s056,020588s044,021346s033,021444s03lbl.pdf	Disc. AE: Parkinsonism, Somnolence... AEs leading to discontinuation/dose reduction: Parkinsonism (0.4%) Somnolence (0.2%) Dizziness (0.2%) Dystonia (0.2%) SGOT increased (0.2%) SGPT increased (0.2%) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/020272s056,020588s044,021346s033,021444s03lbl.pdf
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: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/020272s056,020588s044,021346s033,021444s03lbl.pdf	unhealthy, adult n = 366 Health Status: unhealthy Condition: Schizophrenia Age Group: adult Population Size: 366 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/020272s056,020588s044,021346s033,021444s03lbl.pdf	Disc. AE: Dizziness, Nausea... AEs leading to discontinuation/dose reduction: Dizziness (1.4%) 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%) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/020272s056,020588s044,021346s033,021444s03lbl.pdf
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: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/020272s056,020588s044,021346s033,021444s03lbl.pdf	unhealthy, child n = 106 Health Status: unhealthy Condition: Schizophrenia Age Group: child Population Size: 106 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/020272s056,020588s044,021346s033,021444s03lbl.pdf	Disc. AE: Somnolence, Dizziness... AEs leading to discontinuation/dose reduction: Somnolence (2%) Dizziness (2%) Anorexia (1%) Anxiety (1%) Ataxia (1%) Hypotension (1%) Palpitation (1%) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/020272s056,020588s044,021346s033,021444s03lbl.pdf
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: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/020272s056,020588s044,021346s033,021444s03lbl.pdf	unhealthy, child n = 111 Health Status: unhealthy Condition: Bipolar Mania Age Group: child Population Size: 111 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/020272s056,020588s044,021346s033,021444s03lbl.pdf	Disc. AE: Somnolence, Nausea... AEs leading to discontinuation/dose reduction: Somnolence (5%) Nausea (3%) Abdominal pain (2%) Vomiting (2%) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/020272s056,020588s044,021346s033,021444s03lbl.pdf

AEs

Overview

CYP3A4	CYP2C9	CYP2D6	hERG
substrate 1709	substrate 1010	substrate 1193 inhibitor 1837	inhibitor 1599

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
BCRP 691 P-gp 1437	CYP3A5 391 CYP1A1 348 CYP1A2 1032 CYP2C8 688 CYP2C19 985 P-gp 1527 BCRP 555 UGT 187

Drug as perpetrator

Target	Modality	Activity	Clinical evidence
BCRP 765	inhibitor 3240 Sources: https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2637613/ Page: 1.0	moderate [IC50 38.1 uM]
CYP2D6 1875	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/021346s061lbl.pdf#page=37 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 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/021346s061lbl.pdf#page=37 Page: 37.0
P-gp 1626	inhibitor 3240 Sources: https://www.nature.com/articles/1301181	yes [IC50 15.78 uM]

Drug as victim

Target	Modality	Activity	Clinical evidence
CYP2D6 1193	substrate 3326 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/021346s061lbl.pdf#page=36 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 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/021346s061lbl.pdf#page=36 Page: 36.0
CYP3A5 391	substrate 3326 Sources: https://link.springer.com/article/10.1007/PL00005334 Page: 3.0	minor
CYP3A4 1709	substrate 3326 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
BCRP 555	substrate 3326 Sources: https://peerj.com/articles/2081/	no
CYP1A1 348	substrate 3326 Sources: https://link.springer.com/article/10.1007/PL00005334 Page: 3.0	no
CYP1A2 1032	substrate 3326 Sources: https://link.springer.com/article/10.1007/PL00005334 Page: 3.0	no
CYP2C19 985	substrate 3326 Sources: https://link.springer.com/article/10.1007/PL00005334 Page: 3.0	no
CYP2C8 688	substrate 3326 Sources: https://link.springer.com/article/10.1007/PL00005334 Page: 3.0	no
CYP2C9 1010	substrate 3326 Sources: https://link.springer.com/article/10.1007/PL00005334 Page: 3.0	no
UGT 187	substrate 3326 Sources: https://academic.oup.com/ijnp/article-pdf/6/1/57/1794310/6-1-57.pdf Page: 8.0	no
P-gp 1527	substrate 3326 Sources: https://pubmed.ncbi.nlm.nih.gov/16936711/ Page: 1.0	yes

Tox targets

Target	Modality	Activity	Metabolite	Clinical evidence
hERG 1632	inhibitor 1613 Sources: https://pubmed.ncbi.nlm.nih.gov/28265686/

Sourcing

Vendor/Aggregator	ID	URL
ChEBI	CHEBI:8871	https://www.ebi.ac.uk/chebi/searchId.do?chebiId=CHEBI:8871
ChemicalBook	CB41565182	https://www.chemicalbook.com/ChemicalProductProperty_EN_CB41565182
ChemicalBook	CB63154711	https://www.chemicalbook.com/ChemicalProductProperty_EN_CB63154711
ChemicalBook	CB9131730	https://www.chemicalbook.com/ChemicalProductProperty_EN_CB9131730
MolPort	MolPort-002-885-858	https://www.molport.com/shop/molecule-link/MolPort-002-885-858
MolPort	MolPort-047-151-613	https://www.molport.com/shop/molecule-link/MolPort-047-151-613
Selleck Chemicals	Risperidone(Risperdal)	http://www.selleckchem.com/products/Risperidone(Risperdal).html
ZINC	ZINC000000538312	http://zinc15.docking.org/substances/ZINC000000538312
eMolecules	902418	https://www.emolecules.com/cgi-bin/more?vid=902418

PubMed

Title	Date	PubMed
In vivo effects of olanzapine on striatal dopamine D(2)/D(3) receptor binding in schizophrenic patients: an iodine-123 iodobenzamide single-photon emission tomography study.	1999 Aug	10436199
Dopamine receptor responsivity in schizophrenic patients before and after switch from haloperidol to risperidone.	1999 Dec 20	10646830
Hyperprolactinemia and male sexual dysfunction.	1999 Feb	10084644
Opioid withdrawal during risperidone treatment.	1999 Jun	10350033
Catatonia under medication with risperidone in a 61-year-old patient.	1999 Mar	10100918
Risperidone-induced tardive dystonia and psychosis.	1999 Mar 20	10459911
Quinpirole, 8-OH-DPAT and ketanserin modulate catalepsy induced by high doses of atypical antipsychotics.	1999 Nov	10669905
Risperidone in treatment-refractory schizophrenia.	1999 Sep	10484947
Risperidone in the treatment of elderly patients with psychotic disorders.	1999 Spring	10322240
Risperidone treatment of behavioral disturbances in outpatients with dementia.	1999 Summer	10440009
Case report of withdrawal syndrome after olanzapine discontinuation.	2000 Aug	10917413
Use of the dopamine agonists bromocriptine and cabergoline in the management of risperidone-induced hyperprolactinemia in patients with psychotic disorders.	2000 Dec	11194712
Attention deficit-hyperactivity disorder may be a risk factor for treatment-emergent tardive dyskinesia induced by risperidone.	2000 Feb	10653224
Further evidence that behavioral tests and neuropeptide mRNA and tissue level alterations can differentiate between typical and atypical antipsychotic drugs.	2000 Jul	10869885
Acute confusional states during treatment with risperidone.	2000 Jun	10861920
Subjective experience and striatal dopamine D(2) receptor occupancy in patients with schizophrenia stabilized by olanzapine or risperidone.	2000 Jun	10831489
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	10868556
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	10847307
[Valproic acid in prophylaxis of bipolar disorder. A case of valproate-induced encephalopathy].	2000 May	10846716
Serotonin and dopamine antagonism in obsessive-compulsive disorder: effect of atypical antipsychotic drugs.	2000 Nov	11147933
The serotonin 5-HT(2A) receptor subtype does not mediate apomorphine-induced aggressive behaviour in male Wistar rats.	2000 Oct	11124399
Inverse agonist activity of atypical antipsychotic drugs at human 5-hydroxytryptamine2C receptors.	2000 Oct	10991983
The effects of olanzapine, risperidone, and haloperidol on plasma prolactin levels in patients with schizophrenia.	2000 Sep	11048906
A naturalistic comparison of clozapine, risperidone, and olanzapine in the treatment of bipolar disorder.	2000 Sep	11030483
Weight change and atypical antipsychotic treatment in patients with schizophrenia.	2001	11232752
Evidence for the effectiveness of olanzapine among patients nonresponsive and/or intolerant to risperidone.	2001	11232749
Antipsychotic medications and the elderly: effects on cognition and implications for use.	2001	11232738
Atypical antipsychotics: new directions and new challenges in the treatment of schizophrenia.	2001	11160792
Novel treatments for bipolar disorder.	2001 Apr	11281816
Dynamic dopamine-antagonist interactions at recombinant human dopamine D(2short) receptor: dopamine-bound versus antagonist-bound receptor states.	2001 Apr	11259537
Treatment of psychogenic polydipsia: comparison of risperidone and olanzapine, and the effects of an adjunctive angiotensin-II receptor blocking drug (irbesartan).	2001 Feb	11270459
Priapism associated with polypharmacy.	2001 Feb	11247100
Weight gain with risperidone among patients with mental retardation: effect of calorie restriction.	2001 Feb	11247096
A case of risperidone-induced stuttering.	2001 Feb	11199937
Atypical antipsychotics and cardiovascular risk in schizophrenic patients.	2001 Feb	11199934
Adverse drug interaction between risperidone and carbamazepine in a patient with chronic schizophrenia and deficient CYP2D6 activity.	2001 Feb	11199933
Rehospitalization rates of chronically ill schizophrenic patients discharged on a regimen of risperidone, olanzapine, or conventional antipsychotics.	2001 Feb	11156809
Risperidone versus pimozide in Tourette's disorder: a comparative double-blind parallel-group study.	2001 Jan	11235929
Acute and long-term treatment of catatonia with risperidone.	2001 Jan	11229618
Risperidone-induced cholestatic hepatitis.	2001 Jan	11204814
Relationship between plasma risperidone and 9-hydroxyrisperidone concentrations and clinical response in patients with schizophrenia.	2001 Jan 1	11205425
Consistency of atypical antipsychotic superiority to placebo in recent clinical trials.	2001 Jan 1	11163781
Dopamine transporter density in young patients with schizophrenia assessed with [123]FP-CIT SPECT.	2001 Jan 15	11163545
Antipsychotic drugs classified by their effects on the release of dopamine and noradrenaline in the prefrontal cortex and striatum.	2001 Jan 26	11165224
Effects of dopamine antagonists with different receptor blockade profiles on morphine-induced place preference in male mice.	2001 Jun	11275296
Effectiveness of ECT combined with risperidone against aggression in schizophrenia.	2001 Mar	11281510
Does fast dissociation from the dopamine d(2) receptor explain the action of atypical antipsychotics?: A new hypothesis.	2001 Mar	11229973
Estrogen - a potential treatment for schizophrenia.	2001 Mar 1	11278160
Effects of olanzapine and other antipsychotics on cognitive function in chronic schizophrenia: a longitudinal study.	2001 Mar 1	11278151

Patents

Sample Use Guides

In Vivo Use Guide

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

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 `Thu Jul 06 21:36:09 UTC 2023` Edited by `admin` on `Thu Jul 06 21:36:09 UTC 2023`
Record UNII	FQ117R8W8H
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

RISPERIDONE HEXANOATE

Common Name

English

HEXANOIC ACID, COMPD. WITH 3-(2-(4-(6-FLUORO-1,2-BENZISOXAZOL-3-YL)-1-PIPERIDINYL)ETHYL)-6,7,8,9-TETRAHYDRO-2-METHYL-4H-PYRIDO(1,2-A)PYRIMIDIN-4-ONE

Systematic Name

English

Code System Code Type Description

FDA UNII

FQ117R8W8H

Created by admin on Thu Jul 06 21:36:09 UTC 2023 , Edited by admin on Thu Jul 06 21:36:09 UTC 2023

PRIMARY

CAS

1587586-95-5

Created by admin on Thu Jul 06 21:36:09 UTC 2023 , Edited by admin on Thu Jul 06 21:36:09 UTC 2023

NON-SPECIFIC STOICHIOMETRY

PUBCHEM

70675271

Created by admin on Thu Jul 06 21:36:09 UTC 2023 , Edited by admin on Thu Jul 06 21:36:09 UTC 2023

PRIMARY

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					L6UH7ZF8HC

RISPERIDONE

PARENT -> SALT/SOLVATE

Amount:

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					L6UH7ZF8HC

RISPERIDONE

ACTIVE MOIETY

Amount:

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: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/020272s056,020588s044,021346s033,021444s03lbl.pdf	unhealthy, adult n = 198 Health Status: unhealthy Condition: Schizophrenia Age Group: adult Population Size: 198 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/020272s056,020588s044,021346s033,021444s03lbl.pdf
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: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/020272s056,020588s044,021346s033,021444s03lbl.pdf	unhealthy, adult n = 198 Health Status: unhealthy Condition: Schizophrenia Age Group: adult Population Size: 198 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/020272s056,020588s044,021346s033,021444s03lbl.pdf
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: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/020272s056,020588s044,021346s033,021444s03lbl.pdf	unhealthy, adult n = 198 Health Status: unhealthy Condition: Schizophrenia Age Group: adult Population Size: 198 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/020272s056,020588s044,021346s033,021444s03lbl.pdf
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: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/020272s056,020588s044,021346s033,021444s03lbl.pdf	unhealthy, adult n = 198 Health Status: unhealthy Condition: Schizophrenia Age Group: adult Population Size: 198 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/020272s056,020588s044,021346s033,021444s03lbl.pdf
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: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/020272s056,020588s044,021346s033,021444s03lbl.pdf	unhealthy, adult n = 198 Health Status: unhealthy Condition: Schizophrenia Age Group: adult Population Size: 198 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/020272s056,020588s044,021346s033,021444s03lbl.pdf
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: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/020272s056,020588s044,021346s033,021444s03lbl.pdf	unhealthy, adult n = 198 Health Status: unhealthy Condition: Schizophrenia Age Group: adult Population Size: 198 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/020272s056,020588s044,021346s033,021444s03lbl.pdf
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: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/020272s056,020588s044,021346s033,021444s03lbl.pdf	unhealthy, adult n = 448 Health Status: unhealthy Condition: Bipolar Mania Age Group: adult Population Size: 448 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/020272s056,020588s044,021346s033,021444s03lbl.pdf
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: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/020272s056,020588s044,021346s033,021444s03lbl.pdf	unhealthy, adult n = 448 Health Status: unhealthy Condition: Bipolar Mania Age Group: adult Population Size: 448 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/020272s056,020588s044,021346s033,021444s03lbl.pdf
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: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/020272s056,020588s044,021346s033,021444s03lbl.pdf	unhealthy, adult n = 448 Health Status: unhealthy Condition: Bipolar Mania Age Group: adult Population Size: 448 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/020272s056,020588s044,021346s033,021444s03lbl.pdf
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: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/020272s056,020588s044,021346s033,021444s03lbl.pdf	unhealthy, adult n = 448 Health Status: unhealthy Condition: Bipolar Mania Age Group: adult Population Size: 448 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/020272s056,020588s044,021346s033,021444s03lbl.pdf
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: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/020272s056,020588s044,021346s033,021444s03lbl.pdf	unhealthy, adult n = 448 Health Status: unhealthy Condition: Bipolar Mania Age Group: adult Population Size: 448 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/020272s056,020588s044,021346s033,021444s03lbl.pdf
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: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/020272s056,020588s044,021346s033,021444s03lbl.pdf	unhealthy, adult n = 448 Health Status: unhealthy Condition: Bipolar Mania Age Group: adult Population Size: 448 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/020272s056,020588s044,021346s033,021444s03lbl.pdf
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: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/020272s056,020588s044,021346s033,021444s03lbl.pdf	unhealthy, adult n = 366 Health Status: unhealthy Condition: Schizophrenia Age Group: adult Population Size: 366 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/020272s056,020588s044,021346s033,021444s03lbl.pdf
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: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/020272s056,020588s044,021346s033,021444s03lbl.pdf	unhealthy, adult n = 366 Health Status: unhealthy Condition: Schizophrenia Age Group: adult Population Size: 366 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/020272s056,020588s044,021346s033,021444s03lbl.pdf
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: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/020272s056,020588s044,021346s033,021444s03lbl.pdf	unhealthy, adult n = 366 Health Status: unhealthy Condition: Schizophrenia Age Group: adult Population Size: 366 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/020272s056,020588s044,021346s033,021444s03lbl.pdf
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: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/020272s056,020588s044,021346s033,021444s03lbl.pdf	unhealthy, adult n = 366 Health Status: unhealthy Condition: Schizophrenia Age Group: adult Population Size: 366 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/020272s056,020588s044,021346s033,021444s03lbl.pdf
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: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/020272s056,020588s044,021346s033,021444s03lbl.pdf	unhealthy, adult n = 366 Health Status: unhealthy Condition: Schizophrenia Age Group: adult Population Size: 366 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/020272s056,020588s044,021346s033,021444s03lbl.pdf
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: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/020272s056,020588s044,021346s033,021444s03lbl.pdf	unhealthy, adult n = 366 Health Status: unhealthy Condition: Schizophrenia Age Group: adult Population Size: 366 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/020272s056,020588s044,021346s033,021444s03lbl.pdf
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: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/020272s056,020588s044,021346s033,021444s03lbl.pdf	unhealthy, adult n = 366 Health Status: unhealthy Condition: Schizophrenia Age Group: adult Population Size: 366 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/020272s056,020588s044,021346s033,021444s03lbl.pdf
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: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/020272s056,020588s044,021346s033,021444s03lbl.pdf	unhealthy, adult n = 366 Health Status: unhealthy Condition: Schizophrenia Age Group: adult Population Size: 366 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/020272s056,020588s044,021346s033,021444s03lbl.pdf
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: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/020272s056,020588s044,021346s033,021444s03lbl.pdf	unhealthy, adult n = 366 Health Status: unhealthy Condition: Schizophrenia Age Group: adult Population Size: 366 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/020272s056,020588s044,021346s033,021444s03lbl.pdf
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: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/020272s056,020588s044,021346s033,021444s03lbl.pdf	unhealthy, child n = 106 Health Status: unhealthy Condition: Schizophrenia Age Group: child Population Size: 106 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/020272s056,020588s044,021346s033,021444s03lbl.pdf
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: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/020272s056,020588s044,021346s033,021444s03lbl.pdf	unhealthy, child n = 106 Health Status: unhealthy Condition: Schizophrenia Age Group: child Population Size: 106 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/020272s056,020588s044,021346s033,021444s03lbl.pdf
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: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/020272s056,020588s044,021346s033,021444s03lbl.pdf	unhealthy, child n = 106 Health Status: unhealthy Condition: Schizophrenia Age Group: child Population Size: 106 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/020272s056,020588s044,021346s033,021444s03lbl.pdf
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: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/020272s056,020588s044,021346s033,021444s03lbl.pdf	unhealthy, child n = 106 Health Status: unhealthy Condition: Schizophrenia Age Group: child Population Size: 106 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/020272s056,020588s044,021346s033,021444s03lbl.pdf
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: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/020272s056,020588s044,021346s033,021444s03lbl.pdf	unhealthy, child n = 106 Health Status: unhealthy Condition: Schizophrenia Age Group: child Population Size: 106 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/020272s056,020588s044,021346s033,021444s03lbl.pdf
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: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/020272s056,020588s044,021346s033,021444s03lbl.pdf	unhealthy, child n = 106 Health Status: unhealthy Condition: Schizophrenia Age Group: child Population Size: 106 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/020272s056,020588s044,021346s033,021444s03lbl.pdf
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: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/020272s056,020588s044,021346s033,021444s03lbl.pdf	unhealthy, child n = 106 Health Status: unhealthy Condition: Schizophrenia Age Group: child Population Size: 106 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/020272s056,020588s044,021346s033,021444s03lbl.pdf
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: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/020272s056,020588s044,021346s033,021444s03lbl.pdf	unhealthy, child n = 111 Health Status: unhealthy Condition: Bipolar Mania Age Group: child Population Size: 111 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/020272s056,020588s044,021346s033,021444s03lbl.pdf
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: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/020272s056,020588s044,021346s033,021444s03lbl.pdf	unhealthy, child n = 111 Health Status: unhealthy Condition: Bipolar Mania Age Group: child Population Size: 111 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/020272s056,020588s044,021346s033,021444s03lbl.pdf
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: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/020272s056,020588s044,021346s033,021444s03lbl.pdf	unhealthy, child n = 111 Health Status: unhealthy Condition: Bipolar Mania Age Group: child Population Size: 111 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/020272s056,020588s044,021346s033,021444s03lbl.pdf
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: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/020272s056,020588s044,021346s033,021444s03lbl.pdf	unhealthy, child n = 111 Health Status: unhealthy Condition: Bipolar Mania Age Group: child Population Size: 111 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/020272s056,020588s044,021346s033,021444s03lbl.pdf

Details

SMILES

InChI

CNS Activity

Originator

Approval Year

Targets

Conditions

Approved Use

Launch Date

Approved Use

Launch Date

Approved Use

Launch Date

Cmax

AUC

T1/2

Funbound

Doses

AEs

Overview

OverviewOther

Drug as perpetrator​

Drug as victim

Tox targets

Sourcing

PubMed

Patents

Sample Use Guides

C_max

T_1/2

F_unbound

Drug as perpetrator