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

Stem definition	Drug id	CAS RN
antipsychotics, risperidone derivatives	945	57808-66-9

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: domperidone betadex domperidone betacyclodextrin domperidone motilium peridon domperidone maleate	A specific blocker of dopamine receptors. It speeds gastrointestinal peristalsis, causes prolactin release, and is used as antiemetic and tool in the study of dopaminergic mechanisms. Molecular weight: 425.92 Formula: C22H24ClN5O2 CLOGP: 3.87 LIPINSKI: 0 HAC: 7 HDO: 2 TPSA: 67.92 ALOGS: -3.66 ROTB: 5

Molecule

Description

Molfile Inchi Smiles

Synonyms:

domperidone betadex
domperidone betacyclodextrin
domperidone
motilium
peridon
domperidone maleate

A specific blocker of dopamine receptors. It speeds gastrointestinal peristalsis, causes prolactin release, and is used as antiemetic and tool in the study of dopaminergic mechanisms.

Molecular weight: 425.92
Formula: C22H24ClN5O2
CLOGP: 3.87
LIPINSKI: 0
HAC: 7
HDO: 2
TPSA: 67.92
ALOGS: -3.66
ROTB: 5

Drug dosage:

Dose	Unit	Route
30	mg	O
30	mg	P
0.12	g	R

ADMET properties:

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Property	Value	Reference
CL (Clearance)	9.50 mL/min/kg	Lombardo F, Berellini G, Obach RS
t_half (Half-life)	7.50 hours	Lombardo F, Berellini G, Obach RS
Vd (Volume of distribution)	3.40 L/kg	Lombardo F, Berellini G, Obach RS
BDDCS (Biopharmaceutical Drug Disposition Classification System)	2	Benet LZ, Broccatelli F, Oprea TI
BA (Bioavailability)	15 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
MRTD (Maximum Recommended Therapeutic Daily Dose)	0.34 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
fu (Fraction unbound in plasma)	0.08 %	Lombardo F, Berellini G, Obach RS
S (Water solubility)	0.01 mg/mL	Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine)	0 %	Benet LZ, Broccatelli F, Oprea TI

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Approvals:

Date	Agency	Company	Orphan
Jan. 1, 1982	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
Premature labour	174.73	11.75	106	41051	12398	63435467
Derealisation	134.07	11.75	44	41113	1164	63446701
Gastric pH decreased	131.30	11.75	39	41118	735	63447130
Blepharospasm	130.55	11.75	68	41089	5928	63441937
Depersonalisation/derealisation disorder	120.82	11.75	42	41115	1330	63446535
Sensory loss	99.25	11.75	69	41088	10169	63437696
H1N1 influenza	96.82	11.75	38	41119	1701	63446164
Pulmonary malformation	96.69	11.75	25	41132	274	63447591
Cogwheel rigidity	92.23	11.75	38	41119	1932	63445933
Pemphigus	89.65	11.75	8	41149	183718	63264147

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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
Regurgitation	78.56	13.25	28	13094	1671	34942138
On and off phenomenon	68.08	13.25	28	13094	2469	34941340
Oropharyngeal discomfort	55.20	13.25	26	13096	3170	34940639
Vitamin B12 deficiency	52.34	13.25	27	13095	4004	34939805
Eructation	51.02	13.25	28	13094	4703	34939106
Drug ineffective	40.05	13.25	69	13053	456682	34487127
Pulmonary vasculitis	39.98	13.25	13	13109	586	34943223
Intentional medical device removal by patient	39.05	13.25	11	13111	302	34943507
Stoma site discharge	37.89	13.25	15	13107	1198	34942611
Vomiting	36.31	13.25	186	12936	247435	34696374

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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
Gastric pH decreased	122.16	11.22	38	51283	848	79692219
Derealisation	120.97	11.22	44	51277	1605	79691462
Completed suicide	115.43	11.22	12	51309	245755	79447312
Depersonalisation/derealisation disorder	108.60	11.22	42	51279	1820	79691247
Vomiting	102.77	11.22	756	50565	665072	79027995
Premature labour	102.16	11.22	65	51256	8325	79684742
On and off phenomenon	92.27	11.22	44	51277	3196	79689871
H1N1 influenza	86.67	11.22	39	51282	2480	79690587
Sensory loss	85.03	11.22	69	51252	12922	79680145
Hypoaesthesia oral	82.02	11.22	70	51251	14054	79679013

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FDA Adverse Event Reporting System (Pediatric)

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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
Generalised tonic-clonic seizure	47.22	24.38	9	7	131	89645

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Pharmacologic Action:

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Source	Code	Description
ATC	A03FA03	ALIMENTARY TRACT AND METABOLISM DRUGS FOR FUNCTIONAL GASTROINTESTINAL DISORDERS PROPULSIVES Propulsives
CHEBI has role	CHEBI:48561	dopaminergic antagonists
CHEBI has role	CHEBI:50919	antiemetico
MeSH PA	D000932	Antiemetics
MeSH PA	D002491	Central Nervous System Agents
MeSH PA	D015259	Dopamine Agents
MeSH PA	D018492	Dopamine Antagonists
MeSH PA	D005765	Gastrointestinal Agents
MeSH PA	D018377	Neurotransmitter Agents
MeSH PA	D018373	Peripheral Nervous System Agents

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

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Disease	Relation	SNOMED_ID	DOID
Nausea and vomiting	indication	16932000
Acute gastric ulcer with perforation	contraindication	19850005
Torsades de pointes	contraindication	31722008
Acute nephropathy	contraindication	58574008
Acute gastric ulcer with hemorrhage	contraindication	89748001
Prolonged QT interval	contraindication	111975006
Gastrointestinal obstruction	contraindication	126765001
Disease of liver	contraindication	235856003	DOID:409
Pregnancy, function	contraindication	289908002
Congenital long QT syndrome	contraindication	442917000

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🐶 Veterinary Drug Use

Species	Use	Relation
Horses	Prevention of fescue toxicosis in periparturient mares	Indication

🐶 Veterinary products

Product	Applicant	Ingredients
Equidone Gel	Dechra, Ltd.	1

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	9.45	acidic
pKa2	10.04	acidic
pKa3	7.79	Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

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	8.40	IUPHAR	IUPHAR
Alpha-2A adrenergic receptor	GPCR	P08913	ADA2A_HUMAN		Ki	5.99	DRUG MATRIX
Potassium voltage-gated channel subfamily H member 2	Ion channel	Q12809	KCNH2_HUMAN		IC50	6.79	WOMBAT-PK
Multidrug resistance protein 1	Transporter	P08183	MDR1_HUMAN				WOMBAT-PK
Sodium-dependent serotonin transporter	Transporter	P31645	SC6A4_HUMAN		Ki	5.79	DRUG MATRIX
Sodium-dependent noradrenaline transporter	Transporter	P23975	SC6A2_HUMAN		Ki	5.59	DRUG MATRIX
5-hydroxytryptamine receptor 2A	GPCR	P28223	5HT2A_HUMAN		Ki	7.96	DRUG MATRIX
5-hydroxytryptamine receptor 2B	GPCR	P41595	5HT2B_HUMAN		Ki	5.78	DRUG MATRIX
5-hydroxytryptamine receptor 2C	GPCR	P28335	5HT2C_HUMAN		Ki	6.16	DRUG MATRIX
Alpha-1A adrenergic receptor	GPCR	P35348	ADA1A_HUMAN		Ki	6.65	WOMBAT-PK

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External reference:

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ID	Source
003454	NDDF
005091	NDDF
203007	RXNORM
3151	PUBCHEM_CID
32955006	SNOMEDCT_US
384972001	SNOMEDCT_US
387181004	SNOMEDCT_US
4025225	VUID
4025225	VANDF
4110	INN_ID

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Pharmaceutical products:

None