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

Stem definition	Drug id	CAS RN
sulpiride derivatives and analogues	2537	15676-16-1

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: sulpiride sulpirid sulpitil sulpyrid sursumid	A dopamine D2-receptor antagonist. It has been used therapeutically as an antidepressant, antipsychotic, and as a digestive aid. (From Merck Index, 11th ed) Molecular weight: 341.43 Formula: C15H23N3O4S CLOGP: 1.15 LIPINSKI: 0 HAC: 7 HDO: 2 TPSA: 101.73 ALOGS: -2.80 ROTB: 6

Molecule

Description

Molfile Inchi Smiles

Synonyms:

sulpiride
sulpirid
sulpitil
sulpyrid
sursumid

A dopamine D2-receptor antagonist. It has been used therapeutically as an antidepressant, antipsychotic, and as a digestive aid. (From Merck Index, 11th ed)

Molecular weight: 341.43
Formula: C15H23N3O4S
CLOGP: 1.15
LIPINSKI: 0
HAC: 7
HDO: 2
TPSA: 101.73
ALOGS: -2.80
ROTB: 6

Drug dosage:

Dose	Unit	Route
0.80	g	O
0.80	g	P

ADMET properties:

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Property	Value	Reference
EoM (Fraction excreted unchanged in urine)	70 %	Benet LZ, Broccatelli F, Oprea TI
t_half (Half-life)	6.50 hours	Lombardo F, Berellini G, Obach RS
BDDCS (Biopharmaceutical Drug Disposition Classification System)	3	Benet LZ, Broccatelli F, Oprea TI
BA (Bioavailability)	27 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
S (Water solubility)	2.28 mg/mL	Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose)	133.89 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
CL (Clearance)	1.90 mL/min/kg	Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma)	1 %	Lombardo F, Berellini G, Obach RS
Vd (Volume of distribution)	0.94 L/kg	Lombardo F, Berellini G, Obach RS

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Approvals:

Date	Agency	Company	Orphan
Jan. 1, 1972	YEAR INTRODUCED

FDA Adverse Event Reporting System (Female)

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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
Torsade de pointes	111.06	24.02	38	3630	13313	63472041
Electrocardiogram QT prolonged	109.71	24.02	58	3610	59472	63425882
Parkinsonism	76.34	24.02	27	3641	10412	63474942
Ventricular fibrillation	65.68	24.02	25	3643	11842	63473512
Cerebellar syndrome	62.85	24.02	18	3650	3521	63481833
Hypokalaemia	62.30	24.02	50	3618	103754	63381600
Serotonin syndrome	61.57	24.02	31	3637	28651	63456703
Suicide attempt	60.93	24.02	40	3628	60878	63424476
Fall	57.40	24.02	90	3578	392244	63093110
Hypomagnesaemia	55.71	24.02	29	3639	28708	63456646

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FDA Adverse Event Reporting System (Male)

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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	58.91	27.79	24	2114	12856	34941937
Schizophrenia	53.23	27.79	20	2118	8646	34946147
Neuroleptic malignant syndrome	42.18	27.79	21	2117	17913	34936880
Suicide attempt	40.97	27.79	27	2111	39089	34915704
Mean cell haemoglobin concentration decreased	38.94	27.79	10	2128	1227	34953566
Eosinophil count decreased	37.52	27.79	10	2128	1418	34953375
Parkinsonism	36.63	27.79	15	2123	8123	34946670
Reduced facial expression	35.23	27.79	9	2129	1082	34953711
Pneumonia aspiration	32.36	27.79	24	2114	41879	34912914
Dissociative disorder	31.52	27.79	7	2131	462	34954331

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FDA Adverse Event Reporting System (Geriatric)

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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
Electrocardiogram QT prolonged	118.46	20.27	77	5807	90309	79648195
Parkinsonism	104.34	20.27	41	5843	16543	79721961
Extrapyramidal disorder	91.95	20.27	41	5843	22638	79715866
Torsade de pointes	91.61	20.27	39	5845	19273	79719231
Suicide attempt	74.31	20.27	56	5828	82876	79655628
Fall	59.92	20.27	119	5765	487510	79250994
Cerebellar syndrome	58.46	20.27	20	5864	5460	79733044
Psychomotor retardation	56.10	20.27	20	5864	6164	79732340
Neuroleptic malignant syndrome	55.56	20.27	31	5853	27528	79710976
Serotonin syndrome	50.82	20.27	35	5849	44992	79693512

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	N05AL01	NERVOUS SYSTEM PSYCHOLEPTICS ANTIPSYCHOTICS Benzamides
CHEBI has role	CHEBI:35469	antidepressants
CHEBI has role	CHEBI:35476	neuroleptics
CHEBI has role	CHEBI:48561	dopaminergic antagonists
CHEBI has role	CHEBI:50919	antiemetico
MeSH PA	D000928	Antidepressive Agents
MeSH PA	D018687	Antidepressive Agents, Second-Generation
MeSH PA	D014150	Antipsychotic Agents
MeSH PA	D002491	Central Nervous System Agents
MeSH PA	D002492	Central Nervous System Depressants

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

Disease	Relation	SNOMED_ID	DOID
Schizophrenia	indication	58214004	DOID:5419

🐶 Veterinary Drug Use

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🐶 Veterinary products

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Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	9.47	acidic
pKa2	12.66	acidic
pKa3	8.85	Basic

Orange Book patent data (new drug applications)

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Orange Book exclusivity data (new drug applications)

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Bioactivity Summary:

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Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
D(2) dopamine receptor	GPCR	P14416	DRD2_HUMAN	ANTAGONIST	Ki	8.12	CHEMBL	IUPHAR
Alpha-2A adrenergic receptor	GPCR	P08913	ADA2A_HUMAN		Ki	6.12	DRUG MATRIX
D(3) dopamine receptor	GPCR	P35462	DRD3_HUMAN		Ki	8.10	CHEMBL
D(4) dopamine receptor	GPCR	P21917	DRD4_HUMAN		Ki	5.68	CHEMBL
Carbonic anhydrase 2	Enzyme	P00918	CAH2_HUMAN		IC50	7.40	WOMBAT-PK
Carbonic anhydrase 1	Enzyme	P00915	CAH1_HUMAN		Ki	5.92	CHEMBL
Carbonic anhydrase 9	Enzyme	Q16790	CAH9_HUMAN		Ki	7.51	CHEMBL
Carbonic anhydrase 12	Enzyme	O43570	CAH12_HUMAN		Ki	8.41	CHEMBL
Carbonic anhydrase 5A, mitochondrial	Enzyme	P35218	CAH5A_HUMAN		Ki	6.76	CHEMBL
Carbonic anhydrase 5B, mitochondrial	Enzyme	Q9Y2D0	CAH5B_HUMAN		Ki	7.74	CHEMBL

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External reference:

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ID	Source
003764	NDDF
10239	RXNORM
2359	INN_ID
321506004	SNOMEDCT_US
395891007	SNOMEDCT_US
5355	PUBCHEM_CID
5501	IUPHAR_LIGAND_ID
7MNE9M8287	UNII
C0038803	UMLSCUI
CHEBI:32168	CHEBI

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Pharmaceutical products:

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