General
Preferred name
PROPIVERINE
Synonyms
Propiverine hydrochloride ()
Propiverine (hydrochloride) ()
NSC-172140 ()
Mictonorm ()
Detrunorm XL ()
Detrunorm ()
Mictonetten ()
P&D ID
PD014174
CAS
54556-98-8
60569-19-9
Tags
available
drug
Drug Status
investigational
approved
Drug indication
Urinary incontinence
Max Phase
Phase 4
Structure
Probe scores
P&D probe-likeness score
[[ v.score ]]%
Structure formats
[[ format ]]
[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]
Description
(extracted from source data)
TOXICITY The most common adverse reactions reported in patients treated with propiverine include dry mouth, headache, accommodation disorder, constipation, abdominal pain, dyspepsia and fatigue [L2315].; ; Propiverine may cause drowsiness and blurred vision. This may impair the ability to exert activities that require mental alertness such as operating a motor vehicle or other machinery, or to perform hazardous work while taking this drug [L2315].; ; There have been reports of QT interval prolongation with antimuscarinic medications in the same class of drugs of propiverine hydrochloride. Some drugs that may cause QT/QTc interval prolongation may increase the risk of a rare, but serious ventricular arrhythmia called _torsades de pointes_. Patients at risk for QT/QTc interval prolongation, such as those with diagnosed heart failure, long QT syndrome, recent significant hypokalemia episodes or receiving other drugs known to prolong QT/QTc, should be closely monitored while treated with propiverine. Patients who experience prolonged QT/QTc or symptoms of possible arrhythmias including dizziness, palpitations or fainting should be electrocardiographically evaluated and monitored for electrolyte disturbances [L2315].; ; Propiverine, like other anticholinergics, induces mydriasis. Therefore, the risk to induce acute angle-closure glaucoma in individuals predisposed with narrow angles of the anterior chamber may be increased. Drugs of this class, including propiverine, have been reported to induce or precipitate acute angle-closure glaucoma [L2315].; ; No clinical data are available on the use of propiverine in pregnant women. Studies in animals have shown reproductive toxicity [L2315]. ;
METABOLISM The major metabolites were found to be as follows; 4-piperidyl diphenylpropoxyacetate (DM-P-4), 1-methyl-4-piperidyl benzilate (Dpr-P-4) and 1-methyl-4-piperidyl diphenyl-(2 carboxy) ethoxyacetate (ω-COOH-P-4) in the liver, Dpt-p-4, DM-P-4 in the kidney, and DM-P-4, DPr-P-4 in the lung [L2323]. In the same pharmacokinetic study, All pharmacologically active compounds such as the unchanged compound, 1-methyl-4-piperidyl benzilate N-oxide (DPr-P-4 (N→O)), Dpt-p-4 and 1-methyl-4-piperidyl diphenylpropoxyacetate N-oxide (P-4 (N→O)) were present in the urinary bladder, a target organ for P-4, at higher concentrations than in the plasma [L2323].; ; Propiverine is metabolized by both intestinal and hepatic enzymes. The main metabolic pathway involves the oxidation of the _piperidyl-N _and is mediated by _CYP 3A4_ and _flavin-containing monooxygenases (FMO) _1 and 3 and results in the formation of the second main metabolite M-5, the plasma concentration of which is greater in concentration that of the parent substance propiverine. Four metabolites have been identified in the urine following propiverine ingestion; 3 them are pharmacologically active metabolites that may contribute to its therapeutic effect (M-5, M-6, M-23) [L2325].; ; The mean absolute bioavailability of propiverine IR 15 mg is 40.5% [L2315].
ABSORPTION Propiverine is rapidly absorbed from the gastrointestinal tract with maximum plasma concentrations attained after 2.3 hours. the; mean absolute bioavailability of mictonorm 15 mg tablets (propiverine) is 40.5 %. It undergoes heavy first-pass metabolism in the liver [L2315].;
PHARMACODYNAMICS Propiverine hydrochloride inhibits abnormal contractions of bladder smooth muscle in vivo through not only its anticholinergic activity but also its concurrent calcium antagonistic activity [L2319]. Through the above-mentioned mechanism, propiverine is able to relieve the symptoms of overactive bladder.; ; In animal models, this administration of this drug leads to a dose-dependent decrease in intravesical pressure of the bladder and an increase in bladder capacity [L2315]. In patients with symptoms of OAB resulting from idiopathic detrusor muscle overactivity (IDO) or neurogenic detrusor overactivity (NDO), propiverine showed dose-dependent efficacy and tolerability [A32576].
HALF-LIFE In three studies including a total of 37 healthy volunteers mean elimination half-life was 14.1, 20.1 and; 22.1 hours, respectively [L2315].
Compound Sets
18
Cayman Chemical Bioactives
36049
ChEMBL Approved Drugs
CHEMBL1078261
ChEMBL Drugs
CHEMBL1078261
Drug Repurposing Hub
DrugBank
DB12278
DrugBank Approved Drugs
DB12278
DrugCentral
2300
DrugCentral Approved Drugs
2300
DrugMAP
DMUWBIJ
DrugMAP Approved Drugs
DMUWBIJ
DrugMatrix
Mcule NIBR MoA Box Subset
MCULE-8131441035
MedChem Express Bioactive Compound Library
HY-116408A
Novartis Chemogenetic Library (NIBR MoA Box)
NPC Screening Collection
ReFrame library
Selleckchem Bioactive Compound Library
propiverine-hydrochloride
TargetMol Bioactive Compound Library
T5023
External IDs
40
Properties
(calculated by RDKit )
Molecular Weight
367.21
Hydrogen Bond Acceptors
4
Hydrogen Bond Donors
0
Rotatable Bonds
7
Ring Count
3
Aromatic Ring Count
2
cLogP
3.99
TPSA
38.77
Fraction CSP3
0.43
Chiral centers
0.0
Largest ring
6.0
QED
0.69
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Member status
member
MOA
Muscarinic Antagonists
acetylcholine receptor antagonist
Indication
urinary incontinence
Target
CHRM1
Calcium Channel
mAChR
AChR,Calcium Channel
Pathway
GPCR/G protein
Membrane Transporter/Ion Channel
Neuronal Signaling
Source data