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

Stem definitionDrug idCAS RN
2776 10405-02-4

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • trospium
  • trospium chloride
  • relaspium
  • Molecular weight: 392.52
  • Formula: C25H30NO3
  • CLOGP: -1.15
  • LIPINSKI: 0
  • HAC: 4
  • HDO: 1
  • TPSA: 46.53
  • ALOGS: -6.81
  • ROTB: 5

  • Status: OFP

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

Drug dosage:

DoseUnitRoute
40 mg O

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 3 Benet LZ, Broccatelli F, Oprea TI
S (Water solubility) 500 mg/mL Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine) 6 % Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 1.46 ┬ÁM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability) 10 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution) 5.10 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 13.90 mL/min/kg Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma) 0.33 % Lombardo F, Berellini G, Obach RS
t_half (Half-life) 5 hours Lombardo F, Berellini G, Obach RS

Approvals:

DateAgencyCompanyOrphan
May 28, 2004 FDA ALLERGAN

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

None

Pharmacologic Action:

SourceCodeDescription
ATC A03DA06 ALIMENTARY TRACT AND METABOLISM
DRUGS FOR FUNCTIONAL GASTROINTESTINAL DISORDERS
ANTISPASMODICS IN COMBINATION WITH ANALGESICS
Synthetic anticholinergic agents in combination with analgesics
ATC G04BD09 GENITO URINARY SYSTEM AND SEX HORMONES
UROLOGICALS
UROLOGICALS
Drugs for urinary frequency and incontinence
FDA EPC N0000175700 Cholinergic Muscarinic Antagonist
FDA MoA N0000000125 Cholinergic Muscarinic Antagonists
MeSH PA D018678 Cholinergic Agents
MeSH PA D018680 Cholinergic Antagonists
MeSH PA D018727 Muscarinic Antagonists
MeSH PA D018377 Neurotransmitter Agents
MeSH PA D010276 Parasympatholytics
MeSH PA D018373 Peripheral Nervous System Agents
CHEBI has role CHEBI:53784 antispasmodic drug
CHEBI has role CHEBI:48876 muscarinic antagonist
MeSH PA D064804 Urological Agents

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Urgent desire to urinate indication 75088002
Urge incontinence of urine indication 87557004
Bladder muscle dysfunction - overactive indication 236633002
Increased Urinary Frequency indication
Constipation contraindication 14760008 DOID:2089
Atony of colon contraindication 29479008
Acute nephropathy contraindication 58574008
Ulcerative colitis contraindication 64766004 DOID:8577
Myasthenia gravis contraindication 91637004 DOID:437
Gastrointestinal obstruction contraindication 126765001
Disease of liver contraindication 235856003 DOID:409
Bladder outflow obstruction contraindication 236645006
Retention of urine contraindication 267064002
Gastric retention contraindication 307227006
Angle-closure glaucoma contraindication 392291006 DOID:13550
Gastrointestinal hypomotility contraindication 421807004

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 13.67 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 M3 GPCR ANTAGONIST WOMBAT-PK CHEMBL
Muscarinic acetylcholine receptor M2 GPCR ANTAGONIST CHEMBL CHEMBL
Muscarinic acetylcholine receptor M5 GPCR WOMBAT-PK
Muscarinic acetylcholine receptor M1 GPCR WOMBAT-PK

External reference:

IDSource
4021473 VUID
N0000148857 NUI
C0772089 UMLSCUI
D01103 KEGG_DRUG
1E6682427E UNII
3001 INN_ID
359380005 SNOMEDCT_US
236778 RXNORM
412604005 SNOMEDCT_US
4021473 VANDF
d04929 MMSL
006793 NDDF
DB00209 DRUGBANK_ID
CHEBI:32270 CHEBI
CHEMBL1888176 ChEMBL_ID
CHEMBL3084748 ChEMBL_ID
5596 PUBCHEM_CID
7480 IUPHAR_LIGAND_ID
C003330 MESH_SUPPLEMENTAL_RECORD_UI

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Trospium Chloride HUMAN PRESCRIPTION DRUG LABEL 1 0574-0118 CAPSULE, EXTENDED RELEASE 60 mg ORAL ANDA 18 sections
TROSPIUM CHLORIDE HUMAN PRESCRIPTION DRUG LABEL 1 0574-0145 TABLET, FILM COATED 20 mg ORAL ANDA 18 sections
Trospium Chloride HUMAN PRESCRIPTION DRUG LABEL 1 0591-3636 CAPSULE, EXTENDED RELEASE 60 mg ORAL ANDA 17 sections
Trospium Chloride HUMAN PRESCRIPTION DRUG LABEL 1 23155-530 TABLET, FILM COATED 20 mg ORAL ANDA 17 sections
TROSPIUM CHLORIDE HUMAN PRESCRIPTION DRUG LABEL 1 42291-846 TABLET 20 mg ORAL ANDA 18 sections
Trospium Chloride HUMAN PRESCRIPTION DRUG LABEL 1 60429-098 CAPSULE, EXTENDED RELEASE 60 mg ORAL ANDA 17 sections
TROSPIUM CHLORIDE HUMAN PRESCRIPTION DRUG LABEL 1 60505-3454 TABLET 20 mg ORAL ANDA 18 sections
Trospium Chloride HUMAN PRESCRIPTION DRUG LABEL 1 68001-228 CAPSULE, EXTENDED RELEASE 60 mg ORAL ANDA 17 sections
Trospium Chloride HUMAN PRESCRIPTION DRUG LABEL 1 68462-461 TABLET, FILM COATED 20 mg ORAL ANDA 18 sections
Trospium Chloride HUMAN PRESCRIPTION DRUG LABEL 1 69097-912 TABLET, FILM COATED 20 mg ORAL ANDA 17 sections
Trospium Chloride HUMAN PRESCRIPTION DRUG LABEL 1 69150-258 TABLET 20 mg ORAL ANDA 18 sections
Trospium Chloride HUMAN PRESCRIPTION DRUG LABEL 1 76282-336 TABLET, FILM COATED 20 mg ORAL ANDA 17 sections