Scroll

risperidone 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definition	Drug id	CAS RN
antipsychotics, risperidone derivatives	2389	106266-06-2

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: risperidone ripedon rispadal risperdal risperidal R 64,766 okedi	A selective blocker of DOPAMINE D2 RECEPTORS and SEROTONIN 5-HT2 RECEPTORS that acts as an atypical antipsychotic agent. It has been shown to improve both positive and negative symptoms in the treatment of SCHIZOPHRENIA. Molecular weight: 410.49 Formula: C23H27FN4O2 CLOGP: 2.71 LIPINSKI: 0 HAC: 6 HDO: 0 TPSA: 61.94 ALOGS: -3.38 ROTB: 4 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

risperidone
ripedon
rispadal
risperdal
risperidal
R 64,766
okedi

A selective blocker of DOPAMINE D2 RECEPTORS and SEROTONIN 5-HT2 RECEPTORS that acts as an atypical antipsychotic agent. It has been shown to improve both positive and negative symptoms in the treatment of SCHIZOPHRENIA.

Molecular weight: 410.49
Formula: C23H27FN4O2
CLOGP: 2.71
LIPINSKI: 0
HAC: 6
HDO: 0
TPSA: 61.94
ALOGS: -3.38
ROTB: 4

Status: OFP

Legend:
OFP - off patent
OFM - off market
ONP - on patent

Drug dosage:

Dose	Unit	Route
5	mg	O
2.70	mg	P

ADMET properties:

Show entries

Search:

Property	Value	Reference
BA (Bioavailability)	66 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
CL (Clearance)	5.40 mL/min/kg	Lombardo F, Berellini G, Obach RS
t_half (Half-life)	3.20 hours	Lombardo F, Berellini G, Obach RS
EoM (Fraction excreted unchanged in urine)	3 %	Benet LZ, Broccatelli F, Oprea TI
Vd (Volume of distribution)	1.10 L/kg	Lombardo F, Berellini G, Obach RS
BDDCS (Biopharmaceutical Drug Disposition Classification System)	1	Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose)	0.56 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
S (Water solubility)	0.29 mg/mL	Bocci G, Oprea TI, Benet LZ
fu (Fraction unbound in plasma)	0.10 %	Lombardo F, Berellini G, Obach RS

Showing 1 to 9 of 9 entries

Previous1Next

Approvals:

Date	Agency	Company	Orphan
Dec. 29, 1993	FDA	JANSSEN PHARMS
Feb. 14, 2022	EMA	LABORATORIOS FARMACEUTICOS ROVI, S.A.

FDA Adverse Event Reporting System (Female)

Show entries

Search:

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Hyperprolactinaemia	1584.88	11.55	468	95775	3432	63389347
Extrapyramidal disorder	1544.03	11.55	625	95618	12659	63380120
Suicide attempt	1493.23	11.55	1006	95237	59912	63332867
Neuroleptic malignant syndrome	1400.37	11.55	567	95676	11489	63381290
Blood prolactin increased	1138.63	11.55	354	95889	3149	63389630
Galactorrhoea	1135.92	11.55	368	95875	3787	63388992
Dystonia	989.16	11.55	462	95781	13357	63379422
Sedation	910.06	11.55	624	95619	38185	63354594
Intentional overdose	855.46	11.55	785	95458	73367	63319412
Dyskinesia	806.22	11.55	538	95705	31464	63361315

Showing 1 to 10 of 740 entries

Previous1 2 3 4 5…74Next

FDA Adverse Event Reporting System (Male)

Show entries

Search:

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Gynaecomastia	3595.01	13.03	1299	104886	8881	34841865
Extrapyramidal disorder	1914.56	13.03	884	105301	11996	34838750
Neuroleptic malignant syndrome	1617.63	13.03	877	105308	17057	34833689
Aggression	1045.03	13.03	899	105286	38065	34812681
Dystonia	1043.83	13.03	554	105631	10291	34840455
Psychotic disorder	1035.23	13.03	739	105446	23713	34827033
Sedation	952.17	13.03	662	105523	20344	34830402
Suicide attempt	838.98	13.03	796	105389	38320	34812426
Hyperprolactinaemia	832.62	13.03	273	105912	1323	34849423
Treatment noncompliance	811.97	13.03	677	105508	27423	34823323

Showing 1 to 10 of 700 entries

Previous1 2 3 4 5…70Next

FDA Adverse Event Reporting System (Geriatric)

Show entries

Search:

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Extrapyramidal disorder	3027.41	11.31	1292	165795	21387	79555914
Neuroleptic malignant syndrome	2785.76	11.31	1292	165795	26267	79551034
Gynaecomastia	2272.68	11.31	782	166305	6899	79570402
Hyperprolactinaemia	2029.04	11.31	636	166451	4040	79573261
Dystonia	1780.63	11.31	878	166209	20521	79556780
Aggression	1722.05	11.31	1162	165925	49796	79527505
Sedation	1522.56	11.31	1085	166002	50810	79526491
Suicide attempt	1435.48	11.31	1271	165816	81661	79495640
Psychotic disorder	1415.16	11.31	951	166136	40451	79536850
Blood prolactin increased	1271.01	11.31	430	166657	3581	79573720

Showing 1 to 10 of 1,019 entries

Previous1 2 3 4 5…102Next

FDA Adverse Event Reporting System (Pediatric)

Show entries

Search:

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Tricuspid valve incompetence	31.30	27.29	12	405	61	89314

Showing 1 to 1 of 1 entries

Previous1Next

Pharmacologic Action:

Show entries

Search:

Source	Code	Description
ATC	N05AX08	NERVOUS SYSTEM PSYCHOLEPTICS ANTIPSYCHOTICS Other antipsychotics
CHEBI has role	CHEBI:35471	psychotropic drugs
CHEBI has role	CHEBI:37890	alpha-adrenergic receptor blockaders
CHEBI has role	CHEBI:37955	H1 receptor antagonists
CHEBI has role	CHEBI:48279	serotonin antagonists
CHEBI has role	CHEBI:48561	dopaminergic antagonists
CHEBI has role	CHEBI:65191	atypical antipsychotic agent
CHEBI has role	CHEBI:76779	post-proline endopeptidase inhibitors
FDA EPC	N0000175430	Atypical Antipsychotic
MeSH PA	D014150	Antipsychotic Agents

Showing 1 to 10 of 19 entries

Previous1 2Next

Drug Use | Suggest Off label Use Form| |View source of the data|

Show entries

Search:

Disease	Relation	SNOMED_ID	DOID
Mixed bipolar I disorder	indication	16506000	DOID:3312
Schizophrenia	indication	58214004	DOID:5419
Bipolar disorder in remission	indication	85248005
Bipolar affective disorder, current episode manic	indication	191618007
Infantile autism	indication	408857007
Bipolar affective disorder, current episode depression	off-label use	191627008	DOID:3312
Toxoplasmosis associated with acquired immunodeficiency syndrome	off-label use	421666009
Depression Treatment Adjunct	off-label use
Priapism	contraindication	6273006	DOID:9286
Suicidal thoughts	contraindication	6471006

Showing 1 to 10 of 51 entries

Previous1 2 3 4 5 6Next

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	7.78	Basic
pKa2	3.45	Basic

Orange Book patent data (new drug applications)

Show entries

Search:

Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Patent number	Patent expiration date	Patent use
100MG/0.28ML (100MG/0.28ML)	UZEDY	TEVA	N213586	April 28, 2023	RX	SUSPENSION, EXTENDED RELEASE	SUBCUTANEOUS	9439905	Jan. 12, 2025	TREATMENT OF SCHIZOPHRENIA
100MG/0.28ML (100MG/0.28ML)	UZEDY	TEVA	N213586	April 28, 2023	RX	SUSPENSION, EXTENDED RELEASE	SUBCUTANEOUS	8221778	Nov. 12, 2027	TREATMENT OF SCHIZOPHRENIA
100MG/0.28ML (100MG/0.28ML)	UZEDY	TEVA	N213586	April 28, 2023	RX	SUSPENSION, EXTENDED RELEASE	SUBCUTANEOUS	8741327	Nov. 12, 2027	TREATMENT OF SCHIZOPHRENIA
12.5MG	RYKINDO	SHANDONG LUYE	N212849	Jan. 13, 2023	RX	FOR SUSPENSION, EXTENDED RELEASE	INTRAMUSCULAR	10098882	April 10, 2032	TREATMENT OF SCHIZOPHRENIA IN ADULTS
12.5MG	RYKINDO	SHANDONG LUYE	N212849	Jan. 13, 2023	RX	FOR SUSPENSION, EXTENDED RELEASE	INTRAMUSCULAR	10406161	April 10, 2032	TREATMENT OF SCHIZOPHRENIA IN ADULTS
12.5MG	RYKINDO	SHANDONG LUYE	N212849	Jan. 13, 2023	RX	FOR SUSPENSION, EXTENDED RELEASE	INTRAMUSCULAR	9446135	April 10, 2032	TREATMENT OF SCHIZOPHRENIA IN ADULTS
12.5MG	RYKINDO	SHANDONG LUYE	N212849	Jan. 13, 2023	RX	FOR SUSPENSION, EXTENDED RELEASE	INTRAMUSCULAR	9532991	April 10, 2032	TREATMENT OF SCHIZOPHRENIA IN ADULTS
120MG	PERSERIS KIT	INDIVIOR	N210655	July 27, 2018	RX	FOR SUSPENSION, EXTENDED RELEASE	SUBCUTANEOUS	10406160	June 26, 2026	METHOD OF TREATING SCHIZOPHRENIA
120MG	PERSERIS KIT	INDIVIOR	N210655	July 27, 2018	RX	FOR SUSPENSION, EXTENDED RELEASE	SUBCUTANEOUS	10058554	Sept. 26, 2026	ADMINISTRATION OF RISPERIDONE
120MG	PERSERIS KIT	INDIVIOR	N210655	July 27, 2018	RX	FOR SUSPENSION, EXTENDED RELEASE	SUBCUTANEOUS	11110093	Nov. 5, 2026	TREATING SCHIZOPHRENIA

Showing 1 to 10 of 49 entries

Previous1 2 3 4 5Next

Orange Book exclusivity data (new drug applications)

Show entries

Search:

Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Exclusivity date	Description
100MG/0.28ML (100MG/0.28ML)	UZEDY	TEVA	N213586	April 28, 2023	RX	SUSPENSION, EXTENDED RELEASE	SUBCUTANEOUS	April 28, 2026	NEW PRODUCT
125MG/0.35ML (125MG/0.35ML)	UZEDY	TEVA	N213586	April 28, 2023	RX	SUSPENSION, EXTENDED RELEASE	SUBCUTANEOUS	April 28, 2026	NEW PRODUCT
150MG/0.42ML (150MG/0.42ML)	UZEDY	TEVA	N213586	April 28, 2023	RX	SUSPENSION, EXTENDED RELEASE	SUBCUTANEOUS	April 28, 2026	NEW PRODUCT
200MG/0.56ML (200MG/0.56ML)	UZEDY	TEVA	N213586	April 28, 2023	RX	SUSPENSION, EXTENDED RELEASE	SUBCUTANEOUS	April 28, 2026	NEW PRODUCT
250MG/0.7ML (250MG/0.7ML)	UZEDY	TEVA	N213586	April 28, 2023	RX	SUSPENSION, EXTENDED RELEASE	SUBCUTANEOUS	April 28, 2026	NEW PRODUCT
50MG/0.14ML (50MG/0.14ML)	UZEDY	TEVA	N213586	April 28, 2023	RX	SUSPENSION, EXTENDED RELEASE	SUBCUTANEOUS	April 28, 2026	NEW PRODUCT
75MG/0.21ML (75MG/0.21ML)	UZEDY	TEVA	N213586	April 28, 2023	RX	SUSPENSION, EXTENDED RELEASE	SUBCUTANEOUS	April 28, 2026	NEW PRODUCT

Showing 1 to 7 of 7 entries

Previous1Next

Bioactivity Summary:

Show entries

Search:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
5-hydroxytryptamine receptor 2A	GPCR	P28223	5HT2A_HUMAN	ANTAGONIST	Ki	9.36	WOMBAT-PK	CHEMBL
D(2) dopamine receptor	GPCR	P14416	DRD2_HUMAN	ANTAGONIST	Ki	8.49	WOMBAT-PK	CHEMBL
D(1A) dopamine receptor	GPCR	P21728	DRD1_HUMAN		Ki	7.68	CHEMBL
Alpha-2A adrenergic receptor	GPCR	P08913	ADA2A_HUMAN		Ki	8	WOMBAT-PK
Sigma non-opioid intracellular receptor 1	Membrane receptor	Q99720	SGMR1_HUMAN		Ki	5.37	CHEMBL
Potassium voltage-gated channel subfamily H member 2	Ion channel	Q12809	KCNH2_HUMAN		IC50	6.79	WOMBAT-PK
Sodium-dependent serotonin transporter	Transporter	P31645	SC6A4_HUMAN		Ki	5.85	CHEMBL
5-hydroxytryptamine receptor 1A	GPCR	P08908	5HT1A_HUMAN		Ki	6.44	WOMBAT-PK
5-hydroxytryptamine receptor 2B	GPCR	P41595	5HT2B_HUMAN		Ki	7.42	WOMBAT-PK
5-hydroxytryptamine receptor 2C	GPCR	P28335	5HT2C_HUMAN	ANTAGONIST	Ki	7.70	WOMBAT-PK

Showing 1 to 10 of 59 entries

Previous1 2 3 4 5 6Next

External reference:

Show entries

Search:

ID	Source
004392	NDDF
108386000	SNOMEDCT_US
1259	MMSL
146973	MMSL
152318	RXNORM
386840002	SNOMEDCT_US
4020840	VUID
4020840	VANDF
5073	PUBCHEM_CID
5429	MMSL

Showing 1 to 10 of 22 entries

Previous1 2 3Next

Pharmaceutical products:

Show entries

Search:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Risperidone	HUMAN PRESCRIPTION DRUG LABEL	1	0054-0063	SOLUTION	1 mg	ORAL	ANDA	33 sections
Risperidone	HUMAN PRESCRIPTION DRUG LABEL	1	0054-0063	SOLUTION	1 mg	ORAL	ANDA	33 sections
Risperidone	HUMAN PRESCRIPTION DRUG LABEL	1	0054-0063	SOLUTION	1 mg	ORAL	ANDA	33 sections
Risperidone	HUMAN PRESCRIPTION DRUG LABEL	1	0615-8196	TABLET	0.25 mg	ORAL	ANDA	33 sections
Risperidone	HUMAN PRESCRIPTION DRUG LABEL	1	0615-8196	TABLET	0.25 mg	ORAL	ANDA	33 sections
Risperidone	HUMAN PRESCRIPTION DRUG LABEL	1	0615-8196	TABLET	0.25 mg	ORAL	ANDA	33 sections
Risperidone	HUMAN PRESCRIPTION DRUG LABEL	1	0615-8197	TABLET	0.50 mg	ORAL	ANDA	33 sections
Risperidone	HUMAN PRESCRIPTION DRUG LABEL	1	0615-8197	TABLET	0.50 mg	ORAL	ANDA	33 sections
Risperidone	HUMAN PRESCRIPTION DRUG LABEL	1	0615-8197	TABLET	0.50 mg	ORAL	ANDA	33 sections
Risperidone	HUMAN PRESCRIPTION DRUG LABEL	1	0615-8198	TABLET	1 mg	ORAL	ANDA	33 sections

Showing 1 to 10 of 30 entries

Previous1 2 3Next