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

Stem definition	Drug id	CAS RN
	1784	14008-44-7

Description:

Molecule

Description

Molfile Inchi Smiles

Synonyms:

metopimazine hydrochloride
metopimazine HCl
metopimazine
vogalene

Molecular weight: 445.60
Formula: C22H27N3O3S2
CLOGP: 1.30
LIPINSKI: 0
HAC: 6
HDO: 1
TPSA: 83.71
ALOGS: -4.37
ROTB: 6

Drug dosage:

Dose	Unit	Route
15	mg	O
15	mg	P

ADMET properties:

Property	Value	Reference
BA (Bioavailability)	20 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
CL (Clearance)	12.14 mL/min/kg	Lombardo F, Berellini G, Obach RS
t_half (Half-life)	4 hours	Lombardo F, Berellini G, Obach RS

Approvals:

None

FDA Adverse Event Reporting System (Female)

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
Acute kidney injury	78.08	36.80	54	1211	263361	63224396
Cholestasis	58.51	36.80	22	1243	29412	63458345
Febrile bone marrow aplasia	50.11	36.80	14	1251	7311	63480446
Drug reaction with eosinophilia and systemic symptoms	48.62	36.80	20	1245	33816	63453941
Hyperkalaemia	45.56	36.80	22	1243	54181	63433576
Poisoning deliberate	40.11	36.80	13	1252	11205	63476552

FDA Adverse Event Reporting System (Male)

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
Analgesic drug level increased	52.82	49.92	10	760	846	34955315

FDA Adverse Event Reporting System (Geriatric)

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
Acute kidney injury	102.83	34.48	95	2045	519309	79222939
Coma	57.61	34.48	35	2105	100614	79641634
Cholestasis	57.48	34.48	28	2112	52081	79690167
Poisoning deliberate	54.16	34.48	20	2120	18808	79723440
Drug reaction with eosinophilia and systemic symptoms	51.94	34.48	28	2112	64216	79678032
Febrile bone marrow aplasia	41.79	34.48	15	2125	13005	79729243
Hepatitis	41.46	34.48	23	2117	55704	79686544
Hyperkalaemia	39.35	34.48	29	2111	114369	79627879
Analgesic drug level increased	37.75	34.48	10	2130	3168	79739080
Thrombocytopenia	36.42	34.48	40	2100	265219	79477029
Hepatocellular injury	36.38	34.48	20	2120	47573	79694675

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	A04AD05	ALIMENTARY TRACT AND METABOLISM ANTIEMETICS AND ANTINAUSEANTS ANTIEMETICS AND ANTINAUSEANTS Other antiemetics
MeSH PA	D000932	Antiemetics
MeSH PA	D002491	Central Nervous System Agents
MeSH PA	D005765	Gastrointestinal Agents
MeSH PA	D018373	Peripheral Nervous System Agents

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

None

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	13.41	acidic
pKa2	8.95	Basic
pKa3	3.45	Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Mechanism action	Bioact source	MoA source
D(2) dopamine receptor	GPCR	P14416	DRD2_HUMAN		Ki	10.15		CHEMBL
D(3) dopamine receptor	GPCR	P35462	DRD3_HUMAN		Ki	9.21		CHEMBL
Histamine H1 receptor	GPCR	P35367	HRH1_HUMAN		Ki	8.08		CHEMBL

External reference:

ID	Source
D05010	KEGG_DRUG
C0066469	UMLSCUI
CHEBI:135726	CHEBI
CHEMBL398615	ChEMBL_ID
DB13591	DRUGBANK_ID
C005260	MESH_SUPPLEMENTAL_RECORD_UI
11140	IUPHAR_LIGAND_ID
2178	INN_ID
238S75V9AV	UNII
26388	PUBCHEM_CID
29954	RXNORM
005826	NDDF

Pharmaceutical products:

None