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)

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
Pancreatic steatosis 106.65 21.03 24 4828 981 46680229
Lymphatic fistula 92.88 21.03 21 4831 877 46680333
Femoral hernia incarcerated 92.62 21.03 21 4831 888 46680322
Arterial haemorrhage 84.13 21.03 22 4830 1696 46679514
Wound infection pseudomonas 82.80 21.03 21 4831 1434 46679776
Seroma 75.09 21.03 21 4831 2086 46679124
Haemarthrosis 72.05 21.03 22 4830 2971 46678239
Aortic valve stenosis 71.13 21.03 22 4830 3102 46678108
Tachyarrhythmia 70.36 21.03 24 4828 4608 46676602
Faecaloma 68.70 21.03 27 4825 7725 46673485
Wound dehiscence 66.85 21.03 23 4829 4531 46676679
Diverticulum intestinal 64.13 21.03 24 4828 6017 46675193
Inflammatory marker increased 62.71 21.03 23 4829 5452 46675758
Hepatic cyst 62.00 21.03 22 4830 4744 46676466
Urinary tract infection 60.77 21.03 93 4759 220173 46461037
General physical health deterioration 56.97 21.03 65 4787 115704 46565506
Eructation 56.29 21.03 23 4829 7272 46673938
Fall 54.49 21.03 111 4741 328986 46352224
Aortic arteriosclerosis 54.49 21.03 21 4831 5700 46675510
Aplastic anaemia 53.32 21.03 22 4830 7131 46674079
Anuria 52.41 21.03 25 4827 11406 46669804
Escherichia infection 50.64 21.03 24 4828 10793 46670417
Urinary retention 49.82 21.03 32 4820 26029 46655181
Postoperative wound infection 49.04 21.03 22 4830 8731 46672479
Cardiovascular disorder 47.92 21.03 24 4828 12163 46669047
Left ventricular dysfunction 45.71 21.03 22 4830 10233 46670977
Groin pain 45.17 21.03 21 4831 9044 46672166
Joint dislocation 43.90 21.03 22 4830 11164 46670046
Pulmonary hypertension 40.51 21.03 32 4820 35961 46645249
Hyperkalaemia 40.48 21.03 37 4815 50672 46630538
Tricuspid valve incompetence 39.67 21.03 22 4830 13695 46667515
Myelodysplastic syndrome 39.52 21.03 23 4829 15688 46665522
Hiatus hernia 38.80 21.03 24 4828 18278 46662932
Mitral valve incompetence 35.65 21.03 23 4829 18829 46662381
Lactic acidosis 33.62 21.03 28 4824 33881 46647329
Cardiogenic shock 33.50 21.03 21 4831 16363 46664847
Osteopenia 32.83 21.03 21 4831 16940 46664270
Haematuria 32.65 21.03 25 4827 26833 46654377
Product used for unknown indication 31.76 21.03 8 4844 531 46680679
Acute kidney injury 28.18 21.03 70 4782 235785 46445425
Impaired healing 27.74 21.03 26 4826 36717 46644493
Coronary artery disease 27.65 21.03 25 4827 33727 46647483
Multiple sclerosis relapse 26.55 21.03 27 4825 42098 46639112
Hyponatraemia 25.36 21.03 41 4811 101291 46579919
Gait disturbance 25.10 21.03 50 4802 145213 46535997
Dry mouth 23.90 21.03 29 4823 54897 46626313
Face oedema 23.65 21.03 18 4834 19135 46662075
Oedema peripheral 22.97 21.03 51 4801 159655 46521555
Pulmonary haematoma 21.67 21.03 4 4848 59 46681151

FDA Adverse Event Reporting System (Male)

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
Product prescribing error 62.92 26.63 28 2015 16705 29933730
Anticholinergic syndrome 57.87 26.63 13 2030 811 29949624
General physical health deterioration 49.02 26.63 46 1997 99898 29850537
Labelled drug-drug interaction medication error 44.02 26.63 19 2024 10519 29939916
Arteriosclerotic gangrene 43.20 26.63 7 2036 72 29950363
Hyperkinesia 41.33 26.63 12 2031 2086 29948349
Mucosal haemorrhage 40.90 26.63 11 2032 1447 29948988
Skin swelling 40.51 26.63 10 2033 937 29949498
Therapeutic product effect variable 36.71 26.63 10 2033 1379 29949056
Bladder spasm 36.19 26.63 9 2034 869 29949566
Pallor 34.20 26.63 20 2023 21029 29929406
Freezing phenomenon 33.43 26.63 10 2033 1926 29948509
Confusional state 31.25 26.63 42 2001 134792 29815643
Fall 31.05 26.63 49 1994 181823 29768612
Micturition disorder 29.56 26.63 9 2034 1840 29948595
Disturbance in attention 28.19 26.63 18 2025 22111 29928324
Impaired quality of life 26.89 26.63 8 2035 1511 29948924
Haematoma 26.89 26.63 18 2025 23935 29926500

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 MoA N0000000125 Cholinergic Muscarinic Antagonists
FDA EPC N0000175700 Cholinergic Muscarinic Antagonist
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
MeSH PA D064804 Urological Agents
CHEBI has role CHEBI:48876 antimuskarinika
CHEBI has role CHEBI:53784 antispasmodics

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
D01103 KEGG_DRUG
47608-32-2 SECONDARY_CAS_RN
4021473 VANDF
C0772089 UMLSCUI
CHEBI:32270 CHEBI
CHEMBL1888176 ChEMBL_ID
CHEMBL3084748 ChEMBL_ID
C003330 MESH_SUPPLEMENTAL_RECORD_UI
3001 INN_ID
DB00209 DRUGBANK_ID
T4Y8ORK057 UNII
5284631 PUBCHEM_CID
7480 IUPHAR_LIGAND_ID
236778 RXNORM
107689 MMSL
17758 MMSL
d04929 MMSL
006793 NDDF
006794 NDDF
326557004 SNOMEDCT_US
359380005 SNOMEDCT_US
412604005 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Trospium ChlorideER HUMAN PRESCRIPTION DRUG LABEL 1 0574-0118 CAPSULE, EXTENDED RELEASE 60 mg ORAL ANDA 29 sections
TROSPIUM CHLORIDE HUMAN PRESCRIPTION DRUG LABEL 1 0574-0145 TABLET, FILM COATED 20 mg ORAL ANDA 30 sections
Trospium Chloride HUMAN PRESCRIPTION DRUG LABEL 1 0591-3636 CAPSULE, EXTENDED RELEASE 60 mg ORAL ANDA 26 sections
Trospium Chloride HUMAN PRESCRIPTION DRUG LABEL 1 0904-7059 TABLET, FILM COATED 20 mg ORAL ANDA 21 sections
Trospium Chloride HUMAN PRESCRIPTION DRUG LABEL 1 23155-530 TABLET, FILM COATED 20 mg ORAL ANDA 20 sections
TROSPIUM CHLORIDE ER HUMAN PRESCRIPTION DRUG LABEL 1 35573-446 CAPSULE 60 mg ORAL ANDA 26 sections
TROSPIUM CHLORIDE HUMAN PRESCRIPTION DRUG LABEL 1 42291-846 TABLET 20 mg ORAL ANDA 28 sections
Trospium Chloride HUMAN PRESCRIPTION DRUG LABEL 1 60429-098 CAPSULE, EXTENDED RELEASE 60 mg ORAL ANDA 26 sections
TROSPIUM CHLORIDE HUMAN PRESCRIPTION DRUG LABEL 1 63629-8457 TABLET, FILM COATED 20 mg ORAL ANDA 29 sections
Trospium ChlorideER HUMAN PRESCRIPTION DRUG LABEL 1 63629-8458 CAPSULE, EXTENDED RELEASE 60 mg ORAL ANDA 28 sections
Trospium Chloride HUMAN PRESCRIPTION DRUG LABEL 1 68001-228 CAPSULE, EXTENDED RELEASE 60 mg ORAL ANDA 26 sections
TROSPIUM CHLORIDE HUMAN PRESCRIPTION DRUG LABEL 1 68001-427 CAPSULE, EXTENDED RELEASE 60 mg ORAL ANDA 26 sections
Trospium Chloride HUMAN PRESCRIPTION DRUG LABEL 1 68462-461 TABLET, FILM COATED 20 mg ORAL ANDA 29 sections
Trospium Chloride HUMAN PRESCRIPTION DRUG LABEL 1 69097-912 TABLET, FILM COATED 20 mg ORAL ANDA 28 sections
Trospium Chloride HUMAN PRESCRIPTION DRUG LABEL 1 69150-258 TABLET 20 mg ORAL ANDA 28 sections
TROSPIUM CHLORIDE HUMAN PRESCRIPTION DRUG LABEL 1 70010-027 CAPSULE, EXTENDED RELEASE 60 mg ORAL ANDA 26 sections
TROSPIUM CHLORIDE HUMAN PRESCRIPTION DRUG LABEL 1 70436-174 CAPSULE, EXTENDED RELEASE 60 mg ORAL ANDA 22 sections
Trospium Chloride HUMAN PRESCRIPTION DRUG LABEL 1 76282-336 TABLET, FILM COATED 20 mg ORAL ANDA 27 sections