metoclopramide indications/contra

Stem definitionDrug idCAS RN
sulpiride derivatives 1782 364-62-5

Description:

MoleculeDescription

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: 2.23
  • LIPINSKI: 0
  • HAC: 5
  • HDO: 2
  • TPSA: 67.59
  • ALOGS: -2.99
  • ROTB: 7

Drug dosage:

DoseUnitRoute
30 mg O
30 mg P
30 mg R

Approvals:

DateAgencyCompanyOrphan
Feb. 7, 1979 FDA BAXTER HLTHCARE CORP

FDA Adverse Event Reporting System

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MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Drug hypersensitivity 855.30 30.58 259 2134 35421 3348045
Dystonia 545.91 30.58 116 2277 3651 3379815
Tardive dyskinesia 478.03 30.58 97 2296 2414 3381052
Serotonin syndrome 398.47 30.58 96 2297 5327 3378139
Vomiting 339.59 30.58 171 2222 89360 3294106
Dyskinesia 293.87 30.58 80 2313 7205 3376261
Toxicity to various agents 293.10 30.58 127 2266 46927 3336539
Nausea 275.05 30.58 169 2224 129476 3253990
Drug interaction 257.93 30.58 116 2277 46696 3336770
Extrapyramidal disorder 257.89 30.58 63 2330 3680 3379786
Parkinsonism 237.04 30.58 54 2339 2324 3381142
Neuroleptic malignant syndrome 232.48 30.58 60 2333 4381 3379085
Tremor 221.78 30.58 90 2303 28054 3355412
Restlessness 210.61 30.58 62 2331 7376 3376090
Torsade de pointes 198.51 30.58 49 2344 2980 3380486
Akathisia 189.33 30.58 46 2347 2617 3380849
Cardiac arrest 183.48 30.58 78 2315 27241 3356225
Anxiety 179.80 30.58 86 2307 39543 3343923
Tachycardia 177.98 30.58 73 2320 23298 3360168
Drug abuse 159.31 30.58 63 2330 18267 3365199
Electrocardiogram QT prolonged 156.21 30.58 54 2339 10741 3372725
Completed suicide 142.39 30.58 68 2325 31046 3352420
Muscle twitching 134.78 30.58 38 2355 3859 3379607
Economic problem 129.41 30.58 25 2368 472 3382994
Cardio-respiratory arrest 126.88 30.58 51 2342 15389 3368077
Agitation 124.63 30.58 54 2339 19652 3363814
Hypotension 120.54 30.58 71 2322 49443 3334023
Dyspnoea 116.99 30.58 92 2301 102842 3280624
Exposure during pregnancy 116.24 30.58 57 2336 27506 3355960
Fatigue 115.80 30.58 93 2300 107147 3276319

Pharmacologic Action:

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SourceCodeDescription
ATC A03FA01 ALIMENTARY TRACT AND METABOLISM
DRUGS FOR FUNCTIONAL GASTROINTESTINAL DISORDERS
PROPULSIVES
Propulsives
FDA MoA N0000175799 Dopamine D2 Antagonists
FDA EPC N0000175800 Dopamine-2 Receptor Antagonist
CHEBI has role CHEBI:50919 antiemetic
CHEBI has role CHEBI:48561 dopaminergic antagonist
CHEBI has role CHEBI:55324 gastrointestinal drug
MeSH PA D000932 Antiemetics
MeSH PA D001337 Autonomic Agents
MeSH PA D002491 Central Nervous System Agents
MeSH PA D015259 Dopamine Agents
MeSH PA D018492 Dopamine Antagonists
MeSH PA D065127 Dopamine D2 Receptor Antagonists
MeSH PA D005765 Gastrointestinal Agents
MeSH PA D018377 Neurotransmitter Agents
MeSH PA D018373 Peripheral Nervous System Agents

Drug Use (View source of the data)

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DiseaseRelationSNOMED_IDDOID
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 DOID:13548
Depressive disorder contraindication 35489007 DOID:2848
Hypertensive disorder contraindication 38341003 DOID:10763
Body fluid retention contraindication 43498006
Mechanical ileus contraindication 46420000
Chronic heart failure contraindication 48447003
Gastrointestinal perforation contraindication 51875005
Gastrointestinal hemorrhage contraindication 74474003
Tardive dyskinesia contraindication 102449007
Deficiency of cytochrome-b>5< reductase contraindication 124184009
Seizure disorder contraindication 128613002 DOID:1826
Impaired renal function disorder contraindication 197663003
Anastomosis of intestine contraindication 235407009
Pheochromocytoma contraindication 302835009
Porphyria contraindication 418470004 DOID:13268
Acquired torsion dystonia contraindication 433493000

Acid dissociation constants calculated using MoKa v3.0.0

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Dissociation levelDissociation constantType (acidic/basic)
pKa1 13.17 acidic
pKa2 8.94 Basic
pKa3 1.08 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

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TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
D(2) dopamine receptor GPCR ANTAGONIST Ki 7.19 WOMBAT-PK CHEMBL
5-hydroxytryptamine receptor 3A Ion channel ANTAGONIST Ki 6.70 WOMBAT-PK CHEMBL
5-hydroxytryptamine receptor 4 GPCR AGONIST EC50 6 WOMBAT-PK CHEMBL
5-hydroxytryptamine receptor 2B GPCR Ki 6.40 DRUG MATRIX
5-hydroxytryptamine receptor 2C GPCR Ki 5.90 DRUG MATRIX
Cytochrome P450 2D6 Enzyme IC50 6.10 DRUG MATRIX
Solute carrier family 22 member 1 Transporter IC50 4.02 CHEMBL
Aldehyde oxidase Enzyme IC50 4.51 WOMBAT-PK
Muscarinic acetylcholine receptor M1 GPCR WOMBAT-PK
D(3) dopamine receptor GPCR Ki 7.66 WOMBAT-PK
Serotonin 3 (5-HT3) receptor Ion channel Kd 7.30 CHEMBL
Alpha-2A adrenergic receptor GPCR Ki 5.99 DRUG MATRIX
5-hydroxytryptamine receptor 2A GPCR Ki 5.98 DRUG MATRIX
Serotonin 2 (5-HT2) receptor GPCR IC50 4.88 CHEMBL
Serotonin 3 receptor (5HT3) Ion channel Ki 6.70 CHEMBL
Adrenergic receptor alpha-2 GPCR IC50 5.11 CHEMBL
Serotonin 1 (5-HT1) receptor GPCR IC50 5.11 CHEMBL
D(2) dopamine receptor GPCR Ki 6.98 CHEMBL
Serotonin 3 (5-HT3) receptor Ion channel Ki 6.68 CHEMBL
Adrenergic receptor alpha-1 GPCR IC50 4.48 CHEMBL
D(2) dopamine receptor GPCR Ki 7.10 CHEMBL
D(3) dopamine receptor GPCR IC50 7.21 CHEMBL
5-hydroxytryptamine receptor 4 GPCR Ki 6.05 CHEMBL
5-hydroxytryptamine receptor 4 GPCR Ki 6.26 CHEMBL
D(2) dopamine receptor GPCR ANTAGONIST Ki 7.54 IUPHAR
5-hydroxytryptamine receptor 4 Unclassified AGONIST Ki 6 IUPHAR

External reference:

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IDSource
241 IUPHAR_LIGAND_ID
4019835 VUID
N0000147923 NUI
C0025853 UMLSCUI
D00726 KEGG_DRUG
CHEMBL86 ChEMBL_ID
4019835 VANDF
6915 RXNORM
372776000 SNOMEDCT_US
56549003 SNOMEDCT_US
d00298 MMSL
N0000005745 NDFRT
N0000147923 NDFRT
004778 NDDF
4168 PUBCHEM_CID
CHEBI:107736 CHEBI
CHEMBL1200940 ChEMBL_ID
CHEMBL1256771 ChEMBL_ID
DB01233 DRUGBANK_ID
D008787 MESH_DESCRIPTOR_UI
L4YEB44I46 UNII
1740 INN_ID
54143-57-6 SECONDARY_CAS_RN

Pharmaceutical products:

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ProductCategoryIngredientsNDCFormQuantityRoute MarketingLabel
Metoclopramide HUMAN PRESCRIPTION DRUG LABEL 1 0093-2203 TABLET 10 mg ORAL ANDA 18 sections
Metoclopramide HUMAN PRESCRIPTION DRUG LABEL 1 0093-2204 TABLET 5 mg ORAL ANDA 18 sections
Metoclopramide Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0115-1651 TABLET 10 mg ORAL ANDA 19 sections
Metoclopramide Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0115-1652 TABLET 5 mg ORAL ANDA 19 sections
Metoclopramide HUMAN PRESCRIPTION DRUG LABEL 1 0121-0576 SOLUTION 5 mg ORAL ANDA 19 sections
Metoclopramide HUMAN PRESCRIPTION DRUG LABEL 1 0121-1576 SOLUTION 5 mg ORAL ANDA 19 sections
Metoclopramide HUMAN PRESCRIPTION DRUG LABEL 1 0409-3414 INJECTION, SOLUTION 5 mg INTRAMUSCULAR ANDA 14 sections
Metoclopramide HUMAN PRESCRIPTION DRUG LABEL 1 0440-1771 TABLET 10 mg ORAL ANDA 13 sections
Metoclopramide Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0591-2467 TABLET 5 mg ORAL ANDA 14 sections
Metoclopramide Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0591-2468 TABLET 10 mg ORAL ANDA 14 sections
Metoclopramide HUMAN PRESCRIPTION DRUG LABEL 1 0615-2536 TABLET 10 mg ORAL ANDA 14 sections
Metoclopramide HUMAN PRESCRIPTION DRUG LABEL 1 0615-7698 TABLET 5 mg ORAL ANDA 13 sections
Metoclopramide HUMAN PRESCRIPTION DRUG LABEL 1 0615-7752 TABLET 10 mg ORAL ANDA 12 sections
Metoclopramide HUMAN PRESCRIPTION DRUG LABEL 1 0615-7932 TABLET 10 mg ORAL ANDA 13 sections
Metoclopramide Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0615-8038 TABLET 10 mg ORAL ANDA 14 sections
Metoclopramide Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0615-8071 TABLET 10 mg ORAL ANDA 14 sections
Metoclopramide HUMAN PRESCRIPTION DRUG LABEL 1 0703-4502 INJECTION, SOLUTION 5 mg INTRAVENOUS ANDA 13 sections
Metoclopramide HUMAN PRESCRIPTION DRUG LABEL 1 12634-112 TABLET 10 mg ORAL ANDA 13 sections
METOCLOPRAMIDE HUMAN PRESCRIPTION DRUG LABEL 1 16590-150 TABLET 5 mg ORAL ANDA 14 sections
METOCLOPRAMIDE HUMAN PRESCRIPTION DRUG LABEL 1 16590-151 TABLET 10 mg ORAL ANDA 14 sections
REGLAN HUMAN PRESCRIPTION DRUG LABEL 1 16590-906 TABLET 10 mg ORAL NDA 14 sections
Metoclopramide HUMAN PRESCRIPTION DRUG LABEL 1 17856-0537 SOLUTION 5 mg ORAL ANDA 14 sections
Metoclopramide HUMAN PRESCRIPTION DRUG LABEL 1 17856-0576 SOLUTION 5 mg ORAL ANDA 14 sections
Metoclopramide HUMAN PRESCRIPTION DRUG LABEL 1 17856-3727 SOLUTION 5 mg ORAL ANDA 14 sections
Metoclopramide HUMAN PRESCRIPTION DRUG LABEL 1 21695-346 TABLET 10 mg ORAL ANDA 11 sections
Metoclopramide HUMAN PRESCRIPTION DRUG LABEL 1 21695-485 TABLET 5 mg ORAL ANDA 11 sections
Metoclopramide HUMAN PRESCRIPTION DRUG LABEL 1 23155-240 INJECTION 5 mg INTRAMUSCULAR ANDA 13 sections
Metoclopramide HUMAN PRESCRIPTION DRUG LABEL 1 33261-166 TABLET 10 mg ORAL ANDA 13 sections
METOCLOPRAMIDE hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 40032-581 TABLET, ORALLY DISINTEGRATING 5 mg ORAL ANDA 17 sections
Metoclopramide Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 42254-196 TABLET 5 mg ORAL ANDA 14 sections