methscopolamine Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
1757 13265-10-6

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • methscopolamine
  • methylscopolamine
  • N-Methylhyoscine
  • N-Methylscopolamine
  • methscopolamine bromide
  • methscopolamine nitrate
  • methylscopolamine bromide
A muscarinic antagonist used to study binding characteristics of muscarinic cholinergic receptors.
  • Molecular weight: 318.39
  • Formula: C18H24NO4
  • CLOGP: -2.47
  • LIPINSKI: 0
  • HAC: 5
  • HDO: 1
  • TPSA: 59.06
  • ALOGS: -4.39
  • ROTB: 5

  • Status: OFP

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

Drug dosage:

DoseUnitRoute
12 mg O
12 mg P

ADMET properties:

None

Approvals:

DateAgencyCompanyOrphan
April 9, 1953 FDA FOUGERA PHARMS

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

None

Pharmacologic Action:

SourceCodeDescription
ATC A03BB03 ALIMENTARY TRACT AND METABOLISM
DRUGS FOR FUNCTIONAL GASTROINTESTINAL DISORDERS
BELLADONNA AND DERIVATIVES, PLAIN
Belladonna alkaloids, semisynthetic, quaternary ammonium compounds
ATC A03CB01 ALIMENTARY TRACT AND METABOLISM
DRUGS FOR FUNCTIONAL GASTROINTESTINAL DISORDERS
ANTISPASMODICS IN COMBINATION WITH PSYCHOLEPTICS
Belladonna and derivatives in combination with psycholeptics
ATC S01FA03 SENSORY ORGANS
OPHTHALMOLOGICALS
MYDRIATICS AND CYCLOPLEGICS
Anticholinergics
FDA EPC N0000175574 Anticholinergic
FDA MoA N0000175370 Cholinergic Antagonists
MeSH PA D010276 Parasympatholytics
MeSH PA D018373 Peripheral Nervous System Agents

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Vasomotor rhinitis indication 8229003 DOID:4730
Irritable bowel syndrome indication 10743008 DOID:9778
Cough indication 49727002
Allergic rhinitis indication 61582004
Nasal discharge indication 64531003
Nasal congestion indication 68235000
Common cold indication 82272006 DOID:10459
Rhinitis off-label use 70076002 DOID:4483
Seasonal allergic rhinitis off-label use 367498001
Brain damage contraindication 2470005
Ocular hypertension contraindication 4210003 DOID:9282
Tachyarrhythmia contraindication 6285003
Suicidal thoughts contraindication 6471006
Urinary tract obstruction contraindication 7163005 DOID:5200
Peptic ulcer contraindication 13200003 DOID:750
Chronic obstructive lung disease contraindication 13645005 DOID:3083
Severe chronic ulcerative colitis contraindication 14311001
Disorder of lung contraindication 19829001 DOID:850
Myocardial infarction contraindication 22298006 DOID:5844
Glaucoma contraindication 23986001 DOID:1686
Ventricular tachycardia contraindication 25569003
Alcohol intoxication contraindication 25702006
Shock contraindication 27942005
Toxic megacolon contraindication 28536002 DOID:1770
Atony of colon contraindication 29479008
Hyperthyroidism contraindication 34486009 DOID:7998
Depressive disorder contraindication 35489007
Acute hepatitis contraindication 37871000
Hypertensive disorder contraindication 38341003 DOID:10763
Complete trisomy 21 syndrome contraindication 41040004 DOID:14250
Hyperactive behavior contraindication 44548000
Achalasia of esophagus contraindication 45564002 DOID:9164
Chronic heart failure contraindication 48447003
Bradycardia contraindication 48867003
Acidosis contraindication 51387008
Coronary arteriosclerosis contraindication 53741008 DOID:3393
Paralytic ileus contraindication 55525008 DOID:8442
Peptic reflux disease contraindication 57643001
Ulcerative colitis contraindication 64766004 DOID:8577
Arterial thrombosis contraindication 65198009
Drug AND/OR toxin-induced diarrhea contraindication 65979008
Substance abuse contraindication 66214007
Psychotic disorder contraindication 69322001
Arteriosclerotic vascular disease contraindication 72092001
Diabetes mellitus contraindication 73211009 DOID:9351
Sleep apnea contraindication 73430006 DOID:0050847
Spastic paralysis contraindication 78403003
Disturbance of salivary secretion contraindication 78948009
Chronic idiopathic constipation contraindication 82934008
Hiatal hernia contraindication 84089009 DOID:12642
Kidney disease contraindication 90708001 DOID:557
Myasthenia gravis contraindication 91637004 DOID:437
Hypoalbuminemia contraindication 119247004
Gastrointestinal obstruction contraindication 126765001
Autonomic dysreflexia contraindication 129618003
Bleeding contraindication 131148009
Partial atrioventricular block contraindication 195039008
Acute pancreatitis contraindication 197456007 DOID:2913
Myocardial dysfunction contraindication 233928007
Disease of liver contraindication 235856003 DOID:409
Bladder outflow obstruction contraindication 236645006
Pyloric obstruction contraindication 244815007
Benign prostatic hyperplasia contraindication 266569009
Retention of urine contraindication 267064002
Drowsy contraindication 271782001
Pregnancy, function contraindication 289908002
Severe chronic obstructive pulmonary disease contraindication 313299006
Hypoxia contraindication 389086002
Angle-closure glaucoma contraindication 392291006 DOID:13550
Gastric ulcer contraindication 397825006 DOID:10808
Breastfeeding (mother) contraindication 413712001
Chronic lung disease contraindication 413839001
Disorder of coronary artery contraindication 414024009
Porphyria contraindication 418470004
Hypertensive urgency contraindication 443482000

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 13.24 acidic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Muscarinic acetylcholine receptor M1 GPCR ANTAGONIST Ki 9.90 IUPHAR CHEMBL
Muscarinic acetylcholine receptor M3 GPCR ANTAGONIST Ki 10.40 IUPHAR IUPHAR
Muscarinic acetylcholine receptor M4 GPCR Ki 10.01 CHEMBL
Muscarinic acetylcholine receptor M2 GPCR Ki 9.82 CHEMBL
Muscarinic acetylcholine receptor M5 GPCR Ki 9.68 CHEMBL

External reference:

IDSource
4019830 VUID
N0000147918 NUI
C0301374 UMLSCUI
28415002 SNOMEDCT_US
001720 NDDF
89785 RXNORM
372690005 SNOMEDCT_US
d00989 MMSL
4019830 VANDF
CHEMBL376897 ChEMBL_ID
DB00462 DRUGBANK_ID
K0813KQM3V UNII
6106-46-3 SECONDARY_CAS_RN
CHEBI:135361 CHEBI
71183 PUBCHEM_CID
CHEMBL1201024 ChEMBL_ID
CHEMBL1201268 ChEMBL_ID
CHEMBL1354199 ChEMBL_ID
D019832 MESH_DESCRIPTOR_UI
DB11315 DRUGBANK_ID

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Methscopolamine Bromide HUMAN PRESCRIPTION DRUG LABEL 1 0168-0482 TABLET 2.50 mg ORAL NDA authorized generic 14 sections
Methscopolamine Bromide HUMAN PRESCRIPTION DRUG LABEL 1 0168-0483 TABLET 5 mg ORAL NDA authorized generic 14 sections
Pamine HUMAN PRESCRIPTION DRUG LABEL 1 10337-061 TABLET 2.50 mg ORAL NDA 14 sections
Pamine Forte HUMAN PRESCRIPTION DRUG LABEL 1 10337-062 TABLET 5 mg ORAL NDA 14 sections
METHSCOPOLAMINE BROMIDE HUMAN PRESCRIPTION DRUG LABEL 1 43063-740 TABLET 2.50 mg ORAL ANDA 14 sections
METHSCOPOLAMINE BROMIDE HUMAN PRESCRIPTION DRUG LABEL 1 43063-741 TABLET 5 mg ORAL ANDA 14 sections
Methscopolamine Bromide HUMAN PRESCRIPTION DRUG LABEL 1 51991-191 TABLET 2.50 mg ORAL ANDA 14 sections
Methscopolamine Bromide HUMAN PRESCRIPTION DRUG LABEL 1 51991-192 TABLET 5 mg ORAL ANDA 14 sections
Methscopolamine Bromide HUMAN PRESCRIPTION DRUG LABEL 1 64376-603 TABLET 2.50 mg ORAL ANDA 14 sections
Methscopolamine Bromide HUMAN PRESCRIPTION DRUG LABEL 1 64376-604 TABLET 5 mg ORAL ANDA 14 sections
METHSCOPOLAMINE BROMIDE HUMAN PRESCRIPTION DRUG LABEL 1 76385-100 TABLET 2.50 mg ORAL ANDA 14 sections
METHSCOPOLAMINE BROMIDE HUMAN PRESCRIPTION DRUG LABEL 1 76385-101 TABLET 5 mg ORAL ANDA 14 sections