Details
Stereochemistry | ACHIRAL |
Molecular Formula | C25H30NO3.Cl |
Molecular Weight | 427.964 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 3 / 3 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
[Cl-].OC(C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)[N@@+]23CCCC3)(C4=CC=CC=C4)C5=CC=CC=C5
InChI
InChIKey=RVCSYOQWLPPAOA-QKYUOBHYSA-M
InChI=1S/C25H30NO3.ClH/c27-24(25(28,19-9-3-1-4-10-19)20-11-5-2-6-12-20)29-23-17-21-13-14-22(18-23)26(21)15-7-8-16-26;/h1-6,9-12,21-23,28H,7-8,13-18H2;1H/q+1;/p-1/t21-,22+,23+;
DescriptionCurator's Comment: Description was created based on several sources, including https://www.drugbank.ca/drugs/DB00209
Curator's Comment: Description was created based on several sources, including https://www.drugbank.ca/drugs/DB00209
Trospium is an antispasmodic, antimuscarinic agent indicated for the treatment of overactive bladder with symptoms of urge urinary incontinence, urgency, and urinary frequency. Receptor assays showed that trospium has negligible affinity for nicotinic receptors as compared to muscarinic receptors at concentrations obtained from therapeutic doses. Trospium antagonizes the effect of acetylcholine on muscarinic receptors in cholinergically innervated organs. Its parasympatholytic action reduces the tonus of smooth muscle in the bladder. Trospium is marketed under the brand name Sancturain the US, Tropez OD in India,Trosec in Canada, Regurin and Flotros in the United Kingdom and Spasmex in Germany, Russia, Turkey, Argentina, Chile and Israel.
CNS Activity
Sources: https://www.ncbi.nlm.nih.gov/pubmed/15482001
Curator's Comment: Trospium chloride is hydrophilic and does not cross the normal blood-brain barrier in significant amounts and, therefore, has minimal central anticholinergic activity.
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | SANCTURA Approved UseTrospium chloride tablets are a muscarinic antagonist indicated for the treatment of overactive bladder (OAB) with symptoms of urge urinary incontinence, urgency, and urinary frequency. Trospium chloride tablets are a muscarinic antagonist indicated for the treatment of overactive bladder (OAB) with symptoms of urge urinary incontinence, urgency, and urinary frequency. (1) Launch Date2004 |
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
3.5 ng/mL |
20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered: |
TROSPIUM plasma | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
AUC
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
36.4 ng × h/mL |
20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered: |
TROSPIUM plasma | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
T1/2
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
18.3 h |
20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered: |
TROSPIUM plasma | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
Funbound
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
32.5% |
20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered: |
TROSPIUM plasma | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
Doses
Dose | Population | Adverse events |
---|---|---|
360 mg single, oral Highest studied dose Dose: 360 mg Route: oral Route: single Dose: 360 mg Sources: |
healthy n = 8 Health Status: healthy Sex: M Population Size: 8 Sources: |
|
20 mg 2 times / day multiple, oral Recommended Dose: 20 mg, 2 times / day Route: oral Route: multiple Dose: 20 mg, 2 times / day Sources: Page: p.3 |
unhealthy n = 591 Health Status: unhealthy Condition: Overactive bladder Population Size: 591 Sources: Page: p.3 |
Disc. AE: Dry mouth... AEs leading to discontinuation/dose reduction: Dry mouth (1.9%) Sources: Page: p.3 |
20 mg 2 times / day multiple, oral Recommended Dose: 20 mg, 2 times / day Route: oral Route: multiple Dose: 20 mg, 2 times / day Sources: Page: p.1 |
unhealthy Health Status: unhealthy Condition: Overactive bladder Sources: Page: p.1 |
Disc. AE: Face angioedema, Lip angioedema... AEs leading to discontinuation/dose reduction: Face angioedema Sources: Page: p.1Lip angioedema Oedema tongue Angioedema of larynx Somnolence |
AEs
AE | Significance | Dose | Population |
---|---|---|---|
Dry mouth | 1.9% Disc. AE |
20 mg 2 times / day multiple, oral Recommended Dose: 20 mg, 2 times / day Route: oral Route: multiple Dose: 20 mg, 2 times / day Sources: Page: p.3 |
unhealthy n = 591 Health Status: unhealthy Condition: Overactive bladder Population Size: 591 Sources: Page: p.3 |
Angioedema of larynx | Disc. AE | 20 mg 2 times / day multiple, oral Recommended Dose: 20 mg, 2 times / day Route: oral Route: multiple Dose: 20 mg, 2 times / day Sources: Page: p.1 |
unhealthy Health Status: unhealthy Condition: Overactive bladder Sources: Page: p.1 |
Face angioedema | Disc. AE | 20 mg 2 times / day multiple, oral Recommended Dose: 20 mg, 2 times / day Route: oral Route: multiple Dose: 20 mg, 2 times / day Sources: Page: p.1 |
unhealthy Health Status: unhealthy Condition: Overactive bladder Sources: Page: p.1 |
Lip angioedema | Disc. AE | 20 mg 2 times / day multiple, oral Recommended Dose: 20 mg, 2 times / day Route: oral Route: multiple Dose: 20 mg, 2 times / day Sources: Page: p.1 |
unhealthy Health Status: unhealthy Condition: Overactive bladder Sources: Page: p.1 |
Oedema tongue | Disc. AE | 20 mg 2 times / day multiple, oral Recommended Dose: 20 mg, 2 times / day Route: oral Route: multiple Dose: 20 mg, 2 times / day Sources: Page: p.1 |
unhealthy Health Status: unhealthy Condition: Overactive bladder Sources: Page: p.1 |
Somnolence | Disc. AE | 20 mg 2 times / day multiple, oral Recommended Dose: 20 mg, 2 times / day Route: oral Route: multiple Dose: 20 mg, 2 times / day Sources: Page: p.1 |
unhealthy Health Status: unhealthy Condition: Overactive bladder Sources: Page: p.1 |
Overview
CYP3A4 | CYP2C9 | CYP2D6 | hERG |
---|---|---|---|
OverviewOther
Other Inhibitor | Other Substrate | Other Inducer |
---|---|---|
Drug as perpetrator
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2004/21-595_Sanctura_BioPharmr_P1.pdf Page: 47.0 |
inconclusive | |||
Page: 22.0 |
no [IC50 11928 uM] | |||
Page: 22.0 |
no [IC50 14857 uM] | |||
Page: 22.0 |
no [IC50 1756.3 uM] | |||
Page: 22.0 |
no [IC50 2000 uM] | |||
Page: 22.0 |
no [IC50 2600 uM] | |||
Page: 22.0 |
no [IC50 27 uM] | |||
Page: 22.0 |
no [IC50 8432 uM] |
Drug as victim
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
Page: 22.0 |
likely |
Tox targets
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
Page: 5, 13 |
Sample Use Guides
The recommended dose of SANCTURA (Trospium) is one 20 mg tablet twice daily. SANCTURA should be dosed with water on an empty stomach, at least one hour before a meal.
For patients with severe renal impairment (creatinine clearance less than 30 mL/min), the recommended dose is 20 mg once daily at bedtime.
In geriatric patients greater than or equal to 75 years of age, dose may be titrated down to 20 mg once daily based upon tolerability.
Route of Administration:
Oral
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/20022086
After cumulative administration of increasing concentrations of trospium (1, 3, and 5 uM), agonist-induced contractions decreased significantly in bladder strips.
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Classification Tree | Code System | Code | ||
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NCI_THESAURUS |
C29704
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NCI_THESAURUS |
C29698
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3001
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32270
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CHEMBL1888176
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C61995
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NN-09
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100000092335
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DB00209
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Trospium chloride
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C003330
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233-875-4
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1699300
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38891
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SUB11349MIG
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10405-02-4
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PRIMARY | https://en.wikipedia.org/wiki/Trospium_chloride | ||
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1E6682427E
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m11236
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DTXSID7023724
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ACTIVE MOIETY
SUBSTANCE RECORD