Details
| Stereochemistry | ACHIRAL |
| Molecular Formula | C23H29NO3.ClH |
| Molecular Weight | 403.942 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
Cl.CCCOC(C(=O)OC1CCN(C)CC1)(C2=CC=CC=C2)C3=CC=CC=C3
InChI
InChIKey=KFUJMHHNLGCTIJ-UHFFFAOYSA-N
InChI=1S/C23H29NO3.ClH/c1-3-18-26-23(19-10-6-4-7-11-19,20-12-8-5-9-13-20)22(25)27-21-14-16-24(2)17-15-21;/h4-13,21H,3,14-18H2,1-2H3;1H
| Molecular Formula | C23H29NO3 |
| Molecular Weight | 367.4813 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ACHIRAL |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Optical Activity | NONE |
| Molecular Formula | ClH |
| Molecular Weight | 36.461 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ACHIRAL |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Optical Activity | NONE |
DescriptionCurator's Comment: description was created based on several sources, including
http://www.ncbi.nlm.nih.gov/pubmed/23288694
Curator's Comment: description was created based on several sources, including
http://www.ncbi.nlm.nih.gov/pubmed/23288694
Propiverine is a well established antimuscarinic agent. It’s indicated in adults for the symptomatic treatment of urinary incontinence and/or increased urinary frequency and urgency in patients with overactive bladder syndrome or neurogenic detrusor overactivity (detrusor hyperreflexia) from spinal cord injuries, e.g. transverse legion paraplegia. As well as blocking muscarinic receptors in the detrusor muscle, the drug also inhibits cellular calcium influx, thereby diminishing muscle spasm. Overdose with the muscarinic receptor antagonist propiverine hydrochloride can potentially result in central anticholinergic effects, e.g. restlessness, dizziness, vertigo, disorders in speech and vision and muscular weakness. Moreover, severe dryness of mucosa, tachycardia and urinary retention may occur.
Originator
Approval Year
Targets
| Primary Target | Pharmacology | Condition | Potency |
|---|---|---|---|
Target ID: CHEMBL2094109 Sources: http://www.ncbi.nlm.nih.gov/pubmed/26676219 |
Conditions
| Condition | Modality | Targets | Highest Phase | Product |
|---|---|---|---|---|
| Primary | Detrunorm Approved UseTablets & capsules: Treatment of urinary incontinence, urgency and frequency in patients with idiopathic detrusor overactivity (overactive bladder).
Tablets only: Neurogenic detrusor overactivity (detrusor hyperrefexia) from spinal cord injuries, e.g. transverse lesion paraplegia. |
|||
| Primary | Detrunorm Approved UseTablets & capsules: Treatment of urinary incontinence, urgency and frequency in patients with idiopathic detrusor overactivity (overactive bladder).
Tablets only: Neurogenic detrusor overactivity (detrusor hyperrefexia) from spinal cord injuries, e.g. transverse lesion paraplegia. |
Cmax
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
155 ng/mL |
15 mg 3 times / day multiple, oral dose: 15 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
PROPIVERINE serum | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FED |
|
221 ng/mL |
15 mg 3 times / day multiple, oral dose: 15 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
PROPIVERINE serum | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FED |
|
645 ng/mL |
15 mg 3 times / day multiple, oral dose: 15 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
PROPIVERINE N-OXIDE serum | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FED |
|
819 ng/mL |
15 mg 3 times / day multiple, oral dose: 15 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
PROPIVERINE N-OXIDE serum | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FED |
|
97.58 ng/mL |
10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered: |
PROPIVERINE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
102.18 ng/mL |
20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered: |
PROPIVERINE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
48.5 ng/mL |
10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered: |
PROPIVERINE serum | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
62.9 ng/mL |
15 mg single, oral dose: 15 mg route of administration: Oral experiment type: SINGLE co-administered: |
PROPIVERINE serum | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
136 ng/mL |
30 mg single, oral dose: 30 mg route of administration: Oral experiment type: SINGLE co-administered: |
PROPIVERINE serum | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
56 ng/mL |
15 mg single, oral dose: 15 mg route of administration: Oral experiment type: SINGLE co-administered: |
PROPIVERINE serum | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
196 ng/mL |
15 mg single, intravenous dose: 15 mg route of administration: Intravenous experiment type: SINGLE co-administered: |
PROPIVERINE serum | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
393 ng/mL |
10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered: |
PROPIVERINE N-OXIDE serum | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
562 ng/mL |
15 mg single, oral dose: 15 mg route of administration: Oral experiment type: SINGLE co-administered: |
PROPIVERINE N-OXIDE serum | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
1100 ng/mL |
30 mg single, oral dose: 30 mg route of administration: Oral experiment type: SINGLE co-administered: |
PROPIVERINE N-OXIDE serum | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
508 ng/mL |
15 mg single, oral dose: 15 mg route of administration: Oral experiment type: SINGLE co-administered: |
PROPIVERINE N-OXIDE serum | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
281 ng/mL |
15 mg single, intravenous dose: 15 mg route of administration: Intravenous experiment type: SINGLE co-administered: |
PROPIVERINE N-OXIDE serum | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
AUC
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
177 ng × h/mL |
15 mg 3 times / day multiple, oral dose: 15 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
PROPIVERINE serum | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FED |
|
630 ng × h/mL |
15 mg 3 times / day steady-state, oral dose: 15 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
PROPIVERINE serum | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FED |
|
209 ng × h/mL |
15 mg 3 times / day multiple, oral dose: 15 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
PROPIVERINE serum | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FED |
|
657 ng × h/mL |
15 mg 3 times / day steady-state, oral dose: 15 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
PROPIVERINE serum | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FED |
|
1345 ng × h/mL |
15 mg 3 times / day multiple, oral dose: 15 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
PROPIVERINE N-OXIDE serum | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FED |
|
2512 ng × h/mL |
15 mg 3 times / day steady-state, oral dose: 15 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
PROPIVERINE N-OXIDE serum | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FED |
|
1139 ng × h/mL |
15 mg 3 times / day multiple, oral dose: 15 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
PROPIVERINE N-OXIDE serum | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FED |
|
3200 ng × h/mL |
15 mg 3 times / day steady-state, oral dose: 15 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
PROPIVERINE N-OXIDE serum | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FED |
|
1886.4 ng × h/mL |
10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered: |
PROPIVERINE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
1799.67 ng × h/mL |
20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered: |
PROPIVERINE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
483 ng × h/mL |
10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered: |
PROPIVERINE serum | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
615 ng × h/mL |
15 mg single, oral dose: 15 mg route of administration: Oral experiment type: SINGLE co-administered: |
PROPIVERINE serum | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
1348 ng × h/mL |
30 mg single, oral dose: 30 mg route of administration: Oral experiment type: SINGLE co-administered: |
PROPIVERINE serum | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
558 ng × h/mL |
15 mg single, oral dose: 15 mg route of administration: Oral experiment type: SINGLE co-administered: |
PROPIVERINE serum | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
1403 ng × h/mL |
15 mg single, intravenous dose: 15 mg route of administration: Intravenous experiment type: SINGLE co-administered: |
PROPIVERINE serum | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
3578 ng × h/mL |
10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered: |
PROPIVERINE N-OXIDE serum | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
4557 ng × h/mL |
15 mg single, oral dose: 15 mg route of administration: Oral experiment type: SINGLE co-administered: |
PROPIVERINE N-OXIDE serum | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
9519 ng × h/mL |
30 mg single, oral dose: 30 mg route of administration: Oral experiment type: SINGLE co-administered: |
PROPIVERINE N-OXIDE serum | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
4058 ng × h/mL |
15 mg single, oral dose: 15 mg route of administration: Oral experiment type: SINGLE co-administered: |
PROPIVERINE N-OXIDE serum | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
5107 ng × h/mL |
15 mg single, intravenous dose: 15 mg route of administration: Intravenous experiment type: SINGLE co-administered: |
PROPIVERINE N-OXIDE serum | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
T1/2
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
25.87 h |
10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered: |
PROPIVERINE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
28.21 h |
20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered: |
PROPIVERINE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
11.4 h |
10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered: |
PROPIVERINE serum | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
12.8 h |
15 mg single, oral dose: 15 mg route of administration: Oral experiment type: SINGLE co-administered: |
PROPIVERINE serum | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
14.1 h |
30 mg single, oral dose: 30 mg route of administration: Oral experiment type: SINGLE co-administered: |
PROPIVERINE serum | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
16.3 h |
15 mg single, oral dose: 15 mg route of administration: Oral experiment type: SINGLE co-administered: |
PROPIVERINE serum | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
13.9 h |
15 mg single, intravenous dose: 15 mg route of administration: Intravenous experiment type: SINGLE co-administered: |
PROPIVERINE serum | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
11.1 h |
10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered: |
PROPIVERINE N-OXIDE serum | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
11.7 h |
15 mg single, oral dose: 15 mg route of administration: Oral experiment type: SINGLE co-administered: |
PROPIVERINE N-OXIDE serum | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
13.3 h |
30 mg single, oral dose: 30 mg route of administration: Oral experiment type: SINGLE co-administered: |
PROPIVERINE N-OXIDE serum | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
10.3 h |
15 mg single, oral dose: 15 mg route of administration: Oral experiment type: SINGLE co-administered: |
PROPIVERINE N-OXIDE serum | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
13.2 h |
15 mg single, intravenous dose: 15 mg route of administration: Intravenous experiment type: SINGLE co-administered: |
PROPIVERINE N-OXIDE serum | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
Funbound
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
15.1% |
PROPIVERINE serum | Homo sapiens |
||
17.19% |
PROPIVERINE N-OXIDE serum | Homo sapiens |
||
40% |
PROPIVERINE N-OXIDE serum | Homo sapiens |
||
5% |
PROPIVERINE serum | Homo sapiens |
Doses
| Dose | Population | Adverse events |
|---|---|---|
15 mg 3 times / day multiple, oral Recommended Dose: 15 mg, 3 times / day Route: oral Route: multiple Dose: 15 mg, 3 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
|
20 mg 4 times / day multiple, oral Recommended Dose: 20 mg, 4 times / day Route: oral Route: multiple Dose: 20 mg, 4 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
Disc. AE: Flushing, Gastralgia... AEs leading to discontinuation/dose reduction: Flushing (2.3%) Sources: Gastralgia (2.3%) |
AEs
| AE | Significance | Dose | Population |
|---|---|---|---|
| Flushing | 2.3% Disc. AE |
20 mg 4 times / day multiple, oral Recommended Dose: 20 mg, 4 times / day Route: oral Route: multiple Dose: 20 mg, 4 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
| Gastralgia | 2.3% Disc. AE |
20 mg 4 times / day multiple, oral Recommended Dose: 20 mg, 4 times / day Route: oral Route: multiple Dose: 20 mg, 4 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
PubMed
| Title | Date | PubMed |
|---|---|---|
| Efficacy and safety of low-dose propiverine in patients with lower urinary tract symptoms/benign prostatic hyperplasia with storage symptoms: a prospective, randomized, single-blinded and multicenter clinical trial. | 2011-04 |
|
| Propiverine-induced Parkinsonism: a case report and a pharmacokinetic/pharmacodynamic study in mice. | 2000-05 |
Patents
Sample Use Guides
Adults: Tablets: One 15 mg tablet twice a day, which may be increased to three
times a day. Some patients may respond to one 15 mg tablet a day. For neurogenic detrusor overactivity: One 15 mg tablet three times a day; this may be increased
to four times a day (maximum recommended daily dose). Capsules: One 30 mg capsule daily.
Route of Administration:
Oral
In Vitro Use Guide
Sources: http://www.ncbi.nlm.nih.gov/pubmed/8133908
propiverine (3-10 uM) inhibited carbachol-induced contractions in the presence of verapamil and Ca(2+)-induced contractions in excess K+ medium containing atropine, suggesting it has both anticholinergic and Ca2+ channel blocking actions
| Substance Class |
Chemical
Created
by
admin
on
Edited
Mon Mar 31 18:16:49 GMT 2025
by
admin
on
Mon Mar 31 18:16:49 GMT 2025
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| Record UNII |
DC4GZD10H3
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| Record Status |
Validated (UNII)
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| Record Version |
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41125
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m9215
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DTXSID1046847
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54556-98-8
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100000085092
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DBSALT002169
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55176
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172140
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SUB04087MIG
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CHEMBL1078261
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DC4GZD10H3
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PARENT -> SALT/SOLVATE |