trospium Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| 2776 | 10405-02-4 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 40 | mg | O |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| 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 µM/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:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| May 28, 2004 | FDA | ALLERGAN |
FDA Adverse Event Reporting System (Female)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients 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 term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients 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:
| Source | Code | Description |
|---|---|---|
| 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)
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| 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 level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 13.67 | acidic |
Orange Book patent data (new drug applications)
None
Orange Book exclusivity data (new drug applications)
None
Bioactivity Summary:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA 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:
| ID | Source |
|---|---|
| 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:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| 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 |