trospium ๐Ÿถ Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
quaternary ammonium compounds 2776 10405-02-4

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • trospium
  • trospium chloride
  • relaspium
  • Molecular weight: 392.52
  • Formula: C25H30NO3
  • CLOGP: -1.16
  • 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 ยตM/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 114.04 19.70 25 6015 991 63481991
Lymphatic fistula 103.17 19.70 22 6018 764 63482218
Femoral hernia incarcerated 101.69 19.70 22 6018 819 63482163
Aortic valve stenosis 98.13 19.70 28 6012 3271 63479711
Arterial haemorrhage 95.97 19.70 24 6016 1693 63481289
Wound infection pseudomonas 91.68 19.70 22 6018 1306 63481676
Seroma 81.35 19.70 22 6018 2109 63480873
Tachyarrhythmia 77.43 19.70 25 6015 4425 63478557
Haemarthrosis 77.10 19.70 23 6017 3138 63479844
Fall 74.09 19.70 133 5907 392201 63090781
Faecaloma 73.97 19.70 28 6012 7913 63475069
Wound dehiscence 71.09 19.70 24 6016 4879 63478103
Urinary tract infection 70.64 19.70 105 5935 264579 63218403
Diverticulum intestinal 67.37 19.70 25 6015 6688 63476294
Hepatic cyst 66.04 19.70 23 6017 5131 63477851
Inflammatory marker increased 63.29 19.70 24 6016 6815 63476167
Eructation 62.12 19.70 25 6015 8308 63474674
Aortic arteriosclerosis 58.21 19.70 22 6018 6187 63476795
Coronary artery disease 58.16 19.70 37 6003 32340 63450642
Anuria 55.35 19.70 26 6014 12525 63470457
General physical health deterioration 55.25 19.70 81 5959 201321 63281661
Lactic acidosis 54.85 19.70 38 6002 38249 63444733
Hyponatraemia 54.60 19.70 60 5980 111840 63371142
Cardiovascular disorder 53.73 19.70 25 6015 11787 63471195
Urinary retention 52.86 19.70 34 6006 30267 63452715
Mitral valve incompetence 52.52 19.70 29 6011 19565 63463417
Aplastic anaemia 52.23 19.70 23 6017 9546 63473436
Labelled drug-drug interaction medication error 50.73 19.70 25 6015 13374 63469608
Escherichia infection 48.89 19.70 24 6016 12730 63470252
Groin pain 47.67 19.70 22 6018 10181 63472801
Left ventricular dysfunction 47.27 19.70 23 6017 11965 63471017
Postoperative wound infection 46.23 19.70 22 6018 10903 63472079
Hyperkalaemia 45.16 19.70 39 6001 54164 63428818
Pulmonary hypertension 44.35 19.70 33 6007 37090 63445892
Tricuspid valve incompetence 42.96 19.70 23 6017 14598 63468384
Myelodysplastic syndrome 42.72 19.70 24 6016 16730 63466252
Acute kidney injury 40.54 19.70 82 5958 263333 63219649
Hiatus hernia 39.57 19.70 25 6015 21569 63461413
Joint dislocation 37.57 19.70 23 6017 18777 63464205
Haematemesis 36.25 19.70 27 6013 30385 63452597
Cardiogenic shock 35.99 19.70 22 6018 17910 63465072
Bladder trabeculation 35.75 19.70 6 6034 54 63482928
Product monitoring error 35.22 19.70 14 6026 4502 63478480
Haematuria 35.00 19.70 26 6014 29131 63453851
Fracture 34.21 19.70 22 6018 19562 63463420
Osteopenia 34.01 19.70 22 6018 19763 63463219
Therapeutic drug monitoring analysis not performed 33.67 19.70 10 6030 1342 63481640
Multiple sclerosis relapse 27.16 19.70 28 6012 48450 63434532
Dry mouth 26.82 19.70 35 6005 77828 63405154
Oedema peripheral 26.77 19.70 57 5983 189454 63293528
Face oedema 26.47 19.70 19 6021 20193 63462789
Portal fibrosis 26.26 19.70 6 6034 287 63482695
Drug ineffective 25.17 19.70 38 6002 1044727 62438255
Distal intestinal obstruction syndrome 24.14 19.70 6 6034 412 63482570
Spinal pain 23.54 19.70 15 6025 13124 63469858
Gait disturbance 23.48 19.70 53 5987 183125 63299857
Postmortem blood drug level increased 21.95 19.70 6 6034 598 63482384
Upper airway obstruction 21.05 19.70 6 6034 697 63482285
Dementia 20.87 19.70 16 6024 18778 63464204
Product prescribing error 20.05 19.70 18 6022 26271 63456711
Left ventricular failure 19.72 19.70 10 6030 5677 63477305

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
General physical health deterioration 74.17 25.39 71 2870 128198 34825792
Product prescribing error 65.67 25.39 34 2907 22893 34931097
Anticholinergic syndrome 49.56 25.39 13 2928 1256 34952734
Hyperkinesia 45.29 25.39 13 2928 1755 34952235
Arteriosclerotic gangrene 41.73 25.39 7 2934 72 34953918
Bladder spasm 38.79 25.39 10 2931 902 34953088
Freezing phenomenon 38.03 25.39 11 2930 1525 34952465
Mucosal haemorrhage 37.42 25.39 11 2930 1614 34952376
Fall 35.39 25.39 62 2879 202823 34751167
Skin swelling 34.80 25.39 10 2931 1355 34952635
Labelled drug-drug interaction medication error 33.91 25.39 19 2922 14920 34939070
Therapeutic product effect variable 32.95 25.39 11 2930 2445 34951545
Atrioventricular block second degree 31.88 25.39 12 2929 3776 34950214
Confusional state 29.00 25.39 47 2894 144113 34809877
Disorientation 28.36 25.39 23 2918 33165 34920825
Pallor 26.86 25.39 20 2921 25460 34928530
Thrombophlebitis 26.37 25.39 10 2931 3212 34950778

FDA Adverse Event Reporting System (Geriatric)

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
General physical health deterioration 120.73 18.49 144 7963 275094 79461187
Pancreatic steatosis 104.04 18.49 24 8083 1121 79735160
Lymphatic fistula 101.24 18.49 22 8085 781 79735500
Femoral hernia incarcerated 100.20 18.49 22 8085 820 79735461
Wound infection pseudomonas 85.86 18.49 22 8085 1599 79734682
Fall 85.04 18.49 166 7941 487463 79248818
Arterial haemorrhage 84.87 18.49 24 8083 2537 79733744
Aortic valve stenosis 83.23 18.49 28 8079 5266 79731015
Labelled drug-drug interaction medication error 79.95 18.49 44 8063 27606 79708675
Seroma 78.24 18.49 22 8085 2278 79734003
Faecaloma 74.96 18.49 32 8075 11532 79724749
Product prescribing error 74.47 18.49 50 8057 44763 79691518
Wound dehiscence 69.82 18.49 26 8081 6569 79729712
Urinary tract infection 66.46 18.49 108 7999 274404 79461877
Urinary retention 66.13 18.49 51 8056 56579 79679702
Tachyarrhythmia 64.86 18.49 25 8082 6937 79729344
Haemarthrosis 61.84 18.49 23 8084 5789 79730492
Diverticulum intestinal 59.73 18.49 25 8082 8580 79727701
Hepatic cyst 57.20 18.49 22 8085 6067 79730214
Hyponatraemia 55.81 18.49 79 8028 177769 79558512
Inflammatory marker increased 54.40 18.49 25 8082 10715 79725566
Eructation 54.03 18.49 25 8082 10884 79725397
Escherichia infection 52.98 18.49 29 8078 17988 79718293
Groin pain 49.71 18.49 25 8082 13055 79723226
Aortic arteriosclerosis 49.09 18.49 22 8085 8896 79727385
Cardiovascular disorder 44.83 18.49 26 8081 17999 79718282
Distal intestinal obstruction syndrome 43.25 18.49 11 8096 776 79735505
Product monitoring error 42.83 18.49 20 8087 8886 79727395
Postoperative wound infection 41.28 18.49 22 8085 12939 79723342
Anuria 41.20 18.49 26 8081 20937 79715344
Hyperkinesia 41.19 18.49 14 8093 2715 79733566
Mitral valve incompetence 40.68 18.49 29 8078 28536 79707745
Arteriosclerotic gangrene 40.23 18.49 7 8100 74 79736207
Dementia 39.72 18.49 27 8080 24632 79711649
Lactic acidosis 39.58 18.49 42 8065 70317 79665964
Gait disturbance 38.89 18.49 73 8034 207433 79528848
Joint dislocation 38.37 18.49 23 8084 16916 79719365
Anticholinergic syndrome 37.36 18.49 14 8093 3597 79732684
Aplastic anaemia 37.19 18.49 23 8084 17882 79718399
Haematuria 36.80 18.49 40 8067 68796 79667485
Hiatus hernia 36.30 18.49 25 8082 23287 79712994
Bladder spasm 35.28 18.49 12 8095 2331 79733950
Tricuspid valve incompetence 35.16 18.49 23 8084 19689 79716592
Bladder trabeculation 34.97 18.49 6 8101 58 79736223
Haematemesis 34.47 18.49 34 8073 52230 79684051
Disorientation 34.47 18.49 37 8070 62739 79673542
Osteopenia 34.16 18.49 22 8085 18342 79717939
Mucosal haemorrhage 34.12 18.49 12 8095 2574 79733707
Freezing phenomenon 33.59 18.49 11 8096 1903 79734378
Left ventricular dysfunction 33.10 18.49 22 8085 19339 79716942
Therapeutic product effect variable 33.06 18.49 11 8096 1998 79734283
Dizziness 32.34 18.49 122 7985 526319 79209962
Coronary artery disease 31.48 18.49 36 8071 65438 79670843
Pallor 30.14 18.49 31 8076 50031 79686250
Therapeutic drug monitoring analysis not performed 29.48 18.49 10 8097 1926 79734355
Confusional state 28.70 18.49 84 8023 317913 79418368
Fracture 28.46 18.49 21 8086 21780 79714501
Myelodysplastic syndrome 28.38 18.49 24 8083 30277 79706004
Atrioventricular block second degree 27.85 18.49 14 8093 7298 79728983
Urogenital haemorrhage 27.21 18.49 8 8099 969 79735312
Dysuria 26.17 18.49 29 8078 50922 79685359
Urinary incontinence 25.84 18.49 26 8081 40883 79695398
Orthostatic intolerance 25.66 18.49 9 8098 1915 79734366
Pyelonephritis 25.19 18.49 19 8088 20369 79715912
Subileus 25.05 18.49 12 8095 5642 79730639
Syncope 24.02 18.49 55 8052 179394 79556887
Hydronephrosis 23.20 18.49 17 8090 17437 79718844
Skin swelling 22.40 18.49 10 8097 4004 79732277
Face oedema 21.77 18.49 20 8087 28116 79708165
Portal fibrosis 21.39 18.49 6 8101 615 79735666
Disturbance in attention 21.22 18.49 26 8081 50775 79685506
Asthenia 20.94 18.49 105 8002 511584 79224697
Pulmonary hypertension 20.72 18.49 25 8082 48055 79688226
Drug ineffective 19.96 18.49 51 8056 1080862 78655419
Postmortem blood drug level increased 19.82 18.49 6 8101 803 79735478
Nocturia 19.73 18.49 14 8093 13667 79722614
Fractured sacrum 19.32 18.49 7 8100 1636 79734645
Pulmonary haematoma 18.77 18.49 4 8103 129 79736152
Pollakiuria 18.75 18.49 21 8086 37296 79698985
Hyperkalaemia 18.67 18.49 38 8069 114360 79621921

FDA Adverse Event Reporting System (Pediatric)

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 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
MeSH PA D064804 Urological Agents
FDA EPC N0000175700 Cholinergic Muscarinic Antagonist
CHEBI has role CHEBI:48876 muscarinic antagonists
CHEBI has role CHEBI:53784 antispasmodics

Drug Use | Suggest Off label Use Form| |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




๐Ÿถ Veterinary Drug Use

None

๐Ÿถ Veterinary products

None

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 M2 GPCR ANTAGONIST Ki 8.94 CHEMBL CHEMBL
Muscarinic acetylcholine receptor M3 GPCR ANTAGONIST Ki 8.99 CHEMBL CHEMBL
Muscarinic acetylcholine receptor M1 GPCR Ki 8.46 CHEMBL
Muscarinic acetylcholine receptor M4 GPCR Ki 8.84 CHEMBL
Muscarinic acetylcholine receptor M5 GPCR Ki 8.22 CHEMBL

External reference:

IDSource
4021473 VUID
N0000148857 NUI
D01103 KEGG_DRUG
4021473 VANDF
C0772089 UMLSCUI
CHEBI:32270 CHEBI
CHEMBL1888176 ChEMBL_ID
DB00209 DRUGBANK_ID
CHEMBL3084748 ChEMBL_ID
C003330 MESH_SUPPLEMENTAL_RECORD_UI
5284632 PUBCHEM_CID
7480 IUPHAR_LIGAND_ID
T4Y8ORK057 UNII
236778 RXNORM
107689 MMSL
17758 MMSL
d04929 MMSL
006793 NDDF
006794 NDDF
326557004 SNOMEDCT_US
359380005 SNOMEDCT_US
412604005 SNOMEDCT_US
3001 INN_ID
47608-32-2 SECONDARY_CAS_RN

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 HUMAN PRESCRIPTION DRUG LABEL 1 23155-530 TABLET, FILM COATED 20 mg ORAL ANDA 20 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 ER HUMAN PRESCRIPTION DRUG LABEL 1 35573-446 CAPSULE 60 mg ORAL ANDA 26 sections
TROSPIUM CHLORIDE HUMAN PRESCRIPTION DRUG LABEL 1 50090-5994 CAPSULE, EXTENDED RELEASE 60 mg ORAL ANDA 22 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 62135-742 TABLET, FILM COATED 20 mg ORAL ANDA 19 sections
TROSPIUM CHLORIDE HUMAN PRESCRIPTION DRUG LABEL 1 63629-8457 TABLET, FILM COATED 20 mg ORAL ANDA 29 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 ChlorideER HUMAN PRESCRIPTION DRUG LABEL 1 63629-8458 CAPSULE, EXTENDED RELEASE 60 mg ORAL ANDA 28 sections
TROSPIUM CHLORIDE HUMAN PRESCRIPTION DRUG LABEL 1 63629-9279 TABLET, FILM COATED 20 mg ORAL ANDA 29 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 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 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 70436-174 CAPSULE, EXTENDED RELEASE 60 mg ORAL ANDA 22 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 71205-917 CAPSULE, EXTENDED RELEASE 60 mg ORAL ANDA 26 sections
TROSPIUM CHLORIDE HUMAN PRESCRIPTION DRUG LABEL 1 71205-917 CAPSULE, EXTENDED RELEASE 60 mg ORAL ANDA 26 sections
TROSPIUM CHLORIDE HUMAN PRESCRIPTION DRUG LABEL 1 72789-348 TABLET, FILM COATED 20 mg ORAL ANDA 30 sections