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

Stem definitionDrug idCAS RN
2293 298-50-0

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • propantheline bromide
  • propantheline
  • propanthelinium
  • probanthine
A muscarinic antagonist used as an antispasmodic, in rhinitis, in urinary incontinence, and in the treatment of ulcers. At high doses it has nicotinic effects resulting in neuromuscular blocking.
  • Molecular weight: 368.50
  • Formula: C23H30NO3
  • CLOGP: 1.49
  • LIPINSKI: 0
  • HAC: 4
  • HDO: 0
  • TPSA: 35.53
  • ALOGS: -6.75
  • ROTB: 7

  • Status: OFP

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

Drug dosage:

DoseUnitRoute
60 mg O
60 mg P

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 1 Benet LZ, Broccatelli F, Oprea TI
S (Water solubility) 50 mg/mL Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine) 3.50 % Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 3.82 ┬ÁM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD

Approvals:

DateAgencyCompanyOrphan
April 2, 1953 FDA

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

None

Pharmacologic Action:

SourceCodeDescription
ATC A03AB05 ALIMENTARY TRACT AND METABOLISM
DRUGS FOR FUNCTIONAL GASTROINTESTINAL DISORDERS
DRUGS FOR FUNCTIONAL GASTROINTESTINAL DISORDERS
Synthetic anticholinergics, quaternary ammonium compounds
ATC A03CA34 ALIMENTARY TRACT AND METABOLISM
DRUGS FOR FUNCTIONAL GASTROINTESTINAL DISORDERS
ANTISPASMODICS IN COMBINATION WITH PSYCHOLEPTICS
Synthetic anticholinergic agents in combination with psycholeptics
FDA EPC N0000175574 Anticholinergic
MeSH PA D000897 Anti-Ulcer Agents
MeSH PA D018678 Cholinergic Agents
MeSH PA D018680 Cholinergic Antagonists
MeSH PA D005765 Gastrointestinal Agents
MeSH PA D018727 Muscarinic Antagonists
MeSH PA D018377 Neurotransmitter Agents

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Peptic ulcer indication 13200003 DOID:750
Irritable bowel syndrome off-label use 10743008 DOID:9778
Urinary incontinence off-label use 165232002
Brain damage contraindication 2470005
Tachyarrhythmia contraindication 6285003
Urinary tract obstruction contraindication 7163005 DOID:5200
Severe chronic ulcerative colitis contraindication 14311001
Toxic megacolon contraindication 28536002 DOID:1770
Atony of colon contraindication 29479008
Hyperthyroidism contraindication 34486009 DOID:7998
Hypertensive disorder contraindication 38341003 DOID:10763
Complete trisomy 21 syndrome contraindication 41040004 DOID:14250
Achalasia of esophagus contraindication 45564002 DOID:9164
Chronic heart failure contraindication 48447003
Paralytic ileus contraindication 55525008 DOID:8442
Peptic reflux disease contraindication 57643001
Ulcerative colitis contraindication 64766004 DOID:8577
Drug AND/OR toxin-induced diarrhea contraindication 65979008
Spastic paralysis contraindication 78403003
Disturbance of salivary secretion contraindication 78948009
Hiatal hernia contraindication 84089009 DOID:12642
Kidney disease contraindication 90708001 DOID:557
Myasthenia gravis contraindication 91637004 DOID:437
Gastrointestinal obstruction contraindication 126765001
Autonomic dysreflexia contraindication 129618003
Bleeding contraindication 131148009
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
Angle-closure glaucoma contraindication 392291006 DOID:13550
Gastric ulcer contraindication 397825006 DOID:10808
Chronic lung disease contraindication 413839001
Disorder of coronary artery contraindication 414024009

Acid dissociation constants calculated using MoKa v3.0.0

None

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 M3 GPCR ANTAGONIST Ki 10 IUPHAR CHEMBL
Muscarinic acetylcholine receptor M1 GPCR ANTAGONIST Ki 9.70 IUPHAR CHEMBL
Muscarinic acetylcholine receptor M2 GPCR ANTAGONIST Ki 9.50 IUPHAR CHEMBL
Muscarinic acetylcholine receptor M4 GPCR ANTAGONIST Ki 10.20 IUPHAR

External reference:

IDSource
4018122 VUID
N0000178964 NUI
C0033448 UMLSCUI
D00481 KEGG_DRUG
36642006 SNOMEDCT_US
8761 RXNORM
372721007 SNOMEDCT_US
d00359 MMSL
4019912 VANDF
004693 NDDF
CHEMBL1240 ChEMBL_ID
DB00782 DRUGBANK_ID
CHEMBL1180725 ChEMBL_ID
UX9Z118X9F UNII
226 INN_ID
50-34-0 SECONDARY_CAS_RN
CHEBI:8481 CHEBI
D011413 MESH_DESCRIPTOR_UI
4934 PUBCHEM_CID
329 IUPHAR_LIGAND_ID

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Propantheline Bromide HUMAN PRESCRIPTION DRUG LABEL 1 0054-4721 TABLET, FILM COATED 15 mg ORAL ANDA 12 sections