Scroll

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

Stem definition	Drug id	CAS RN
sulpiride derivatives and analogues	1782	364-62-5

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: metoclopramide metoclopramide hydrochloride metochlopramide methochlopramide metoclopramide hydrochloride hydrate metoclopramide monohydrochloride metoclopramide HCl AHR-3070-C metaclopramide	A dopamine D2 antagonist that is used as an antiemetic. Molecular weight: 299.80 Formula: C14H22ClN3O2 CLOGP: 2.34 LIPINSKI: 0 HAC: 5 HDO: 2 TPSA: 67.59 ALOGS: -2.99 ROTB: 7 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

metoclopramide
metoclopramide hydrochloride
metochlopramide
methochlopramide
metoclopramide hydrochloride hydrate
metoclopramide monohydrochloride
metoclopramide HCl
AHR-3070-C
metaclopramide

A dopamine D2 antagonist that is used as an antiemetic.

Molecular weight: 299.80
Formula: C14H22ClN3O2
CLOGP: 2.34
LIPINSKI: 0
HAC: 5
HDO: 2
TPSA: 67.59
ALOGS: -2.99
ROTB: 7

Status: OFP

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

Drug dosage:

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

ADMET properties:

Show entries

Search:

Property	Value	Reference
BA (Bioavailability)	76 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
t_half (Half-life)	7.20 hours	Lombardo F, Berellini G, Obach RS
S (Water solubility)	67 mg/mL	Bocci G, Oprea TI, Benet LZ
CL (Clearance)	5.70 mL/min/kg	Lombardo F, Berellini G, Obach RS
MRTD (Maximum Recommended Therapeutic Daily Dose)	33.36 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
Vd (Volume of distribution)	3.20 L/kg	Lombardo F, Berellini G, Obach RS
EoM (Fraction excreted unchanged in urine)	20 %	Hosey CM, Chan R, Benet LZ
BDDCS (Biopharmaceutical Drug Disposition Classification System)	1	Hosey CM, Chan R, Benet LZ
fu (Fraction unbound in plasma)	0.60 %	Lombardo F, Berellini G, Obach RS

Showing 1 to 9 of 9 entries

Previous1Next

Approvals:

Date	Agency	Company	Orphan
Feb. 7, 1979	FDA	BAXTER HLTHCARE CORP

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
Febrile neutropenia	511.33	10.00	821	111502	117628	63259071
Drug ineffective	487.51	10.00	687	111636	1044078	62332621
Vomiting	403.07	10.00	2003	110320	557614	62819085
Joint swelling	336.48	10.00	83	112240	327583	63049116
Rheumatoid arthritis	294.44	10.00	48	112275	253771	63122928
Contraindicated product administered	289.55	10.00	26	112297	217622	63159077
Arthropathy	284.76	10.00	39	112284	234753	63141946
Synovitis	269.74	10.00	15	112308	186903	63189796
Drug intolerance	260.67	10.00	110	112213	308551	63068148
Hand deformity	257.29	10.00	5	112318	159452	63217247

Showing 1 to 10 of 495 entries

Previous1 2 3 4 5…50Next

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
Febrile neutropenia	484.14	10.28	909	66305	135940	34753777
Vomiting	289.25	10.28	1087	66127	246534	34643183
Drug ineffective	238.52	10.28	319	66895	456432	34433285
Nausea	163.95	10.28	1165	66049	338743	34550974
General physical health deterioration	159.16	10.28	575	66639	127694	34762023
Dehydration	120.47	10.28	532	66682	129437	34760280
Decreased appetite	95.92	10.28	597	66617	165795	34723922
Drug abuse	93.07	10.28	37	67177	99059	34790658
Pyrexia	93.04	10.28	1013	66201	332000	34557717
Product dose omission issue	85.76	10.28	63	67151	119648	34770069

Showing 1 to 10 of 244 entries

Previous1 2 3 4 5…25Next

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
Febrile neutropenia	895.97	9.67	1605	152985	229394	79360404
Vomiting	590.67	9.67	2701	151889	663127	78926671
Drug ineffective	470.93	9.67	864	153726	1080049	78509749
Nausea	350.03	9.67	3097	151493	954099	78635699
Joint swelling	277.87	9.67	106	154484	288540	79301258
Drug intolerance	250.89	9.67	99	154491	264020	79325778
Rheumatoid arthritis	250.05	9.67	50	154540	208420	79381378
Synovitis	248.72	9.67	10	154580	150724	79439074
General physical health deterioration	242.19	9.67	1116	153474	274122	79315676
Neutropenic sepsis	241.53	9.67	280	154310	26784	79563014

Showing 1 to 10 of 529 entries

Previous1 2 3 4 5…53Next

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Show entries

Search:

Source	Code	Description
ATC	A03FA01	ALIMENTARY TRACT AND METABOLISM DRUGS FOR FUNCTIONAL GASTROINTESTINAL DISORDERS PROPULSIVES Propulsives
CHEBI has role	CHEBI:35703	Xenobiotic
CHEBI has role	CHEBI:48561	dopaminergic antagonists
CHEBI has role	CHEBI:50919	antiemetico
CHEBI has role	CHEBI:55324	gastrointestinal drugs
CHEBI has role	CHEBI:78298	environmental contaminants
FDA EPC	N0000175800	Dopamine-2 Receptor Antagonist
FDA MoA	N0000175799	Dopamine D2 Antagonists
MeSH PA	D000932	Antiemetics
MeSH PA	D002491	Central Nervous System Agents

Showing 1 to 10 of 16 entries

Previous1 2Next

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

Show entries

Search:

Disease	Relation	SNOMED_ID	DOID
Diabetic gastroparesis	indication	34140002
Intubation of gastrointestinal tract	indication	235419001
Gastroesophageal reflux disease	indication	235595009	DOID:8534
Chemotherapy-induced nausea and vomiting	indication	236084000
Prevention of Post-Operative Nausea and Vomiting	indication
Gastrointestinal Radiography Adjunct	indication
Suicidal thoughts	contraindication	6471006
Neuroleptic malignant syndrome	contraindication	15244003	DOID:14464
Cirrhosis of liver	contraindication	19943007	DOID:5082
Parkinsonism	contraindication	32798002

Showing 1 to 10 of 25 entries

Previous1 2 3Next

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	13.17	acidic
pKa2	8.94	Basic
pKa3	1.08	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
EQ 15MG BASE/SPRAY	GIMOTI	EVOKE PHARMA INC	N209388	June 19, 2020	RX	SPRAY, METERED	NASAL	11020361	Dec. 22, 2029	NASAL ADMINISTRATION OF METOCLOPRAMIDE FOR TREATMENT OF DIABETIC GASTROPARESIS
EQ 15MG BASE/SPRAY	GIMOTI	EVOKE PHARMA INC	N209388	June 19, 2020	RX	SPRAY, METERED	NASAL	11628150	Dec. 22, 2029	NASAL ADMINISTRATION OF METOCLOPRAMIDE FOR TREATMENT OF DIABETIC GASTROPARESIS
EQ 15MG BASE/SPRAY	GIMOTI	EVOKE PHARMA INC	N209388	June 19, 2020	RX	SPRAY, METERED	NASAL	8334281	May 16, 2030	NASAL ADMINISTRATION OF METOCLOPRAMIDE FOR TREATMENT OF DIABETIC GASTROPARESIS

Showing 1 to 3 of 3 entries

Previous1Next

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
EQ 15MG BASE/SPRAY	GIMOTI	EVOKE PHARMA INC	N209388	June 19, 2020	RX	SPRAY, METERED	NASAL	June 19, 2023	NEW PRODUCT

Showing 1 to 1 of 1 entries

Previous1Next

Bioactivity Summary:

Show entries

Search:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
D(2) dopamine receptor	GPCR	P14416	DRD2_HUMAN	ANTAGONIST	Ki	7.19	WOMBAT-PK	CHEMBL
5-hydroxytryptamine receptor 3A	Ion channel	P46098	5HT3A_HUMAN	ANTAGONIST	Ki	6.70	WOMBAT-PK	CHEMBL
5-hydroxytryptamine receptor 4	GPCR	Q13639	5HT4R_HUMAN	AGONIST	EC50	6	WOMBAT-PK	CHEMBL
5-hydroxytryptamine receptor 2B	GPCR	P41595	5HT2B_HUMAN		Ki	6.40	DRUG MATRIX
5-hydroxytryptamine receptor 2C	GPCR	P28335	5HT2C_HUMAN		Ki	5.90	DRUG MATRIX
D(3) dopamine receptor	GPCR	P35462	DRD3_HUMAN		Ki	7.66	WOMBAT-PK
Muscarinic acetylcholine receptor M1	GPCR	P11229	ACM1_HUMAN				WOMBAT-PK
Aldehyde oxidase	Enzyme	Q06278	AOXA_HUMAN		IC50	4.51	WOMBAT-PK
Cytochrome P450 2D6	Enzyme	P10635	CP2D6_HUMAN		IC50	6.10	DRUG MATRIX
Myeloperoxidase	Enzyme	P05164	PERM_HUMAN		IC50	6.46	CHEMBL

Showing 1 to 10 of 27 entries

Previous1 2 3Next

External reference:

Show entries

Search:

ID	Source
001877	NDDF
004778	NDDF
1062	MMSL
1740	INN_ID
241	IUPHAR_LIGAND_ID
267036	RXNORM
31147000	SNOMEDCT_US
34842	MMSL
372776000	SNOMEDCT_US
4017905	VANDF

Showing 1 to 10 of 27 entries

Previous1 2 3Next

Pharmaceutical products:

Show entries

Search:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Metoclopramide	HUMAN PRESCRIPTION DRUG LABEL	1	0093-2203	TABLET	10 mg	ORAL	ANDA	26 sections
Metoclopramide	HUMAN PRESCRIPTION DRUG LABEL	1	0093-2204	TABLET	5 mg	ORAL	ANDA	26 sections
Metoclopramide	HUMAN PRESCRIPTION DRUG LABEL	1	0121-0576	SOLUTION	5 mg	ORAL	ANDA	28 sections
Metoclopramide	HUMAN PRESCRIPTION DRUG LABEL	1	0121-0576	SOLUTION	5 mg	ORAL	ANDA	28 sections
Metoclopramide	HUMAN PRESCRIPTION DRUG LABEL	1	0121-0576	SOLUTION	5 mg	ORAL	ANDA	28 sections
Metoclopramide	HUMAN PRESCRIPTION DRUG LABEL	1	0121-1576	SOLUTION	5 mg	ORAL	ANDA	28 sections
Metoclopramide	HUMAN PRESCRIPTION DRUG LABEL	1	0121-1576	SOLUTION	5 mg	ORAL	ANDA	28 sections
Metoclopramide	HUMAN PRESCRIPTION DRUG LABEL	1	0121-1576	SOLUTION	5 mg	ORAL	ANDA	28 sections
Metoclopramide	HUMAN PRESCRIPTION DRUG LABEL	1	0404-9910	INJECTION, SOLUTION	5 mg	INTRAVENOUS	ANDA	13 sections
Metoclopramide	HUMAN PRESCRIPTION DRUG LABEL	1	0404-9910	INJECTION, SOLUTION	5 mg	INTRAVENOUS	ANDA	13 sections

Showing 1 to 10 of 30 entries

Previous1 2 3Next