Identification

Name
Propiverine
Accession Number
DB12278
Type
Small Molecule
Groups
Approved, Investigational
Description

Propiverine is a widely used antimuscarinic drug with a mixed mode of action in the treatment of symptoms associated with overactive bladder (OAB) [1].

Overactive bladder (OAB) is a chronic condition of the lower urinary tract characterized by urinary urgency, increased frequency of urination, and nocturia (frequent waking during the night to urinate). OAB has a negative impact on quality of life and may lead to leakage and inconvenient urinary accidents [15], [16]. Overactive bladder syndrome affects millions of elderly individuals in the United States and shows equal prevalence in men and women. The impact of OAB on quality of life is sometimes devastating, especially to elderly patients with other medical conditions [16].

Propiverine hydrochloride is a bladder detrusor muscle relaxant drug with dual antimuscarinic and calcium-modulating properties for the treatment of OAB [7].

Structure
Thumb
Synonyms
Not Available
Product Ingredients
IngredientUNIICASInChI Key
Propiverine hydrochlorideDC4GZD10H354556-98-8KFUJMHHNLGCTIJ-UHFFFAOYSA-N
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
MictorylCapsule, extended release30 mgOralDuchesnay Inc.2017-05-08Not applicableCanada
MictorylCapsule, extended release45 mgOralDuchesnay Inc.2017-05-08Not applicableCanada
Mictoryl PediatricTablet5 mgOralDuchesnay Inc.2017-04-13Not applicableCanada
Categories
UNII
468GE2241L
CAS number
60569-19-9
Weight
Average: 367.4813
Monoisotopic: 367.214743799
Chemical Formula
C23H29NO3
InChI Key
QPCVHQBVMYCJOM-UHFFFAOYSA-N
InChI
InChI=1S/C23H29NO3/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
IUPAC Name
1-methylpiperidin-4-yl 2,2-diphenyl-2-propoxyacetate
SMILES
CCCOC(C(=O)OC1CCN(C)CC1)(C1=CC=CC=C1)C1=CC=CC=C1

Pharmacology

Indication

Indicated for symptomatic treatment of urinary incontinence and/or increased urinary frequency and urgency in patients with overactive bladder (OAB) [6]. Propiverine may also be used in patients with neurogenic bladder as a result of spinal cord injury [5].

Structured Indications
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 [8]. 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 [6]. 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 [1].

Mechanism of action

Propiverine demonstrates both anticholinergic and calcium-modulating properties. The efferent connection of the pelvic nerve is inhibited due to the anticholinergic action exerted by this drug, leading to relaxation of bladder smooth muscle. Propiverine blocks calcium ion influx and modulates the intracellular calcium in urinary bladder smooth muscle cells, resulting in the inhibition of muscle spasm [6]. The bladder contains several muscarinic receptors. Acetylcholine is the main contractile neurotransmitter in the human bladder detrusor muscle, and antimuscarinics such as propiverine exert their effects by competitively inhibiting the binding of acetylcholine at muscarinic receptors on detrusor smooth muscle cells and other structures within the bladder wall [17]. In one study, After oral treatment with propiverine, the bladder showed the highest concentration of M-2, indicating a targeted distribution of this metabolite into the bladder. Therefore, muscarinic receptor-2 may highly contribute to the relatively selective and long-lasting occupation of bladder muscarinic receptors after oral ingestion of propiverine [19].

TargetActionsOrganism
AMuscarinic acetylcholine receptor M1
antagonist
Human
AMuscarinic acetylcholine receptor M2
antagonist
Human
AMuscarinic acetylcholine receptor M3
antagonist
Human
UMuscarinic acetylcholine receptor M4
antagonist
Human
AMuscarinic acetylcholine receptor M5Not AvailableHuman
AVoltage-dependent L-type calcium channel subunit alpha-1C
antagonist
Human
AAlpha-1A adrenergic receptor
antagonist
Human
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 [6].

Volume of distribution

In one study, the volume of distribution was calculated in 21 healthy volunteers after intravenous (IV) administration of propiverine hydrochloride was measured to range from 125 to 4731 (average 2791) indicating, that a large amount of available propiverine is distributed to peripheral compartments [13].

Protein binding

90-95% for the parent compound and about 60% for the main metabolite [13].

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 [12]. 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 [12].

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) [14].

The mean absolute bioavailability of propiverine IR 15 mg is 40.5% [6].

Route of elimination

Following the ingestion of 30 mg propiverine, 60% radioactivity was recovered in urine and 21% was recovered in feces within 12 days. Less than 1% of an oral dose is excreted unchanged in the urine [6].

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 [6].

Clearance

Mean total clearance after single dose administration of 30 mg is 371 mL/min (191 – 870 mL/min) [6].

Toxicity

The most common adverse reactions reported in patients treated with propiverine include dry mouth, headache, accommodation disorder, constipation, abdominal pain, dyspepsia and fatigue [6].

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 [6].

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 [6].

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 [6].

No clinical data are available on the use of propiverine in pregnant women. Studies in animals have shown reproductive toxicity [6].

Affected organisms
  • Humans and other mammals
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteractionDrug group
1,10-PhenanthrolineThe therapeutic efficacy of Propiverine can be decreased when used in combination with 1,10-Phenanthroline.Experimental
Acetyl sulfisoxazoleThe metabolism of Propiverine can be decreased when combined with Acetyl sulfisoxazole.Approved, Vet Approved
AclidiniumPropiverine may increase the anticholinergic activities of Aclidinium.Approved
AlcuroniumThe risk or severity of adverse effects can be increased when Propiverine is combined with Alcuronium.Experimental
AlfentanilThe risk or severity of adverse effects can be increased when Propiverine is combined with Alfentanil.Approved, Illicit
AlphacetylmethadolThe risk or severity of adverse effects can be increased when Propiverine is combined with Alphacetylmethadol.Experimental, Illicit
AlphaprodineThe risk or severity of adverse effects can be increased when Propiverine is combined with Alphaprodine.Illicit
AmbenoniumThe therapeutic efficacy of Propiverine can be decreased when used in combination with Ambenonium.Approved
AmiodaroneThe metabolism of Propiverine can be decreased when combined with Amiodarone.Approved, Investigational
Anisotropine MethylbromideThe risk or severity of adverse effects can be increased when Anisotropine Methylbromide is combined with Propiverine.Approved
ApalutamideThe serum concentration of Propiverine can be decreased when it is combined with Apalutamide.Approved, Investigational
AprepitantThe serum concentration of Propiverine can be increased when it is combined with Aprepitant.Approved, Investigational
AtazanavirThe metabolism of Propiverine can be decreased when combined with Atazanavir.Approved, Investigational
AtomoxetineThe metabolism of Propiverine can be decreased when combined with Atomoxetine.Approved
AtracuriumThe risk or severity of adverse effects can be increased when Propiverine is combined with Atracurium.Approved, Experimental, Investigational
Atracurium besylateThe risk or severity of adverse effects can be increased when Atracurium besylate is combined with Propiverine.Approved
AtropineThe risk or severity of adverse effects can be increased when Atropine is combined with Propiverine.Approved, Vet Approved
BenactyzineThe risk or severity of adverse effects can be increased when Benactyzine is combined with Propiverine.Withdrawn
BendroflumethiazideThe serum concentration of Bendroflumethiazide can be increased when it is combined with Propiverine.Approved
BenzatropineThe risk or severity of adverse effects can be increased when Benzatropine is combined with Propiverine.Approved
BezitramideThe risk or severity of adverse effects can be increased when Propiverine is combined with Bezitramide.Experimental, Illicit, Withdrawn
BiperidenThe risk or severity of adverse effects can be increased when Biperiden is combined with Propiverine.Approved, Investigational
BoceprevirThe metabolism of Propiverine can be decreased when combined with Boceprevir.Approved, Withdrawn
BornaprineThe risk or severity of adverse effects can be increased when Bornaprine is combined with Propiverine.Experimental
BortezomibThe metabolism of Propiverine can be decreased when combined with Bortezomib.Approved, Investigational
BosentanThe serum concentration of Propiverine can be decreased when it is combined with Bosentan.Approved, Investigational
Botulinum Toxin Type APropiverine may increase the anticholinergic activities of Botulinum Toxin Type A.Approved, Investigational
Botulinum Toxin Type BPropiverine may increase the anticholinergic activities of Botulinum Toxin Type B.Approved, Investigational
BuprenorphineThe risk or severity of adverse effects can be increased when Propiverine is combined with Buprenorphine.Approved, Illicit, Investigational, Vet Approved
ButorphanolThe risk or severity of adverse effects can be increased when Propiverine is combined with Butorphanol.Approved, Illicit, Vet Approved
ButylscopolamineThe risk or severity of adverse effects can be increased when Butylscopolamine is combined with Propiverine.Approved, Investigational, Vet Approved
CarbamazepineThe metabolism of Propiverine can be increased when combined with Carbamazepine.Approved, Investigational
CarfentanilThe risk or severity of adverse effects can be increased when Propiverine is combined with Carfentanil.Illicit, Investigational, Vet Approved
CeritinibThe serum concentration of Propiverine can be increased when it is combined with Ceritinib.Approved
ChlorothiazideThe serum concentration of Chlorothiazide can be increased when it is combined with Propiverine.Approved, Vet Approved
ChlorphenoxamineThe risk or severity of adverse effects can be increased when Chlorphenoxamine is combined with Propiverine.Withdrawn
ChlorthalidoneThe serum concentration of Chlorthalidone can be increased when it is combined with Propiverine.Approved
CimetropiumPropiverine may increase the anticholinergic activities of Cimetropium.Experimental, Investigational
ClarithromycinThe metabolism of Propiverine can be decreased when combined with Clarithromycin.Approved
ClemastineThe metabolism of Propiverine can be decreased when combined with Clemastine.Approved, Investigational
ClotrimazoleThe metabolism of Propiverine can be decreased when combined with Clotrimazole.Approved, Vet Approved
CobicistatThe metabolism of Propiverine can be decreased when combined with Cobicistat.Approved
CodeineThe risk or severity of adverse effects can be increased when Propiverine is combined with Codeine.Approved, Illicit
ConivaptanThe serum concentration of Conivaptan can be increased when it is combined with Propiverine.Approved, Investigational
CoumaphosThe therapeutic efficacy of Propiverine can be decreased when used in combination with Coumaphos.Vet Approved
CrizotinibThe metabolism of Propiverine can be decreased when combined with Crizotinib.Approved
CyclopenthiazideThe serum concentration of Cyclopenthiazide can be increased when it is combined with Propiverine.Experimental
CyclopentolateThe risk or severity of adverse effects can be increased when Cyclopentolate is combined with Propiverine.Approved
CyclosporineThe metabolism of Propiverine can be decreased when combined with Cyclosporine.Approved, Investigational, Vet Approved
DabrafenibThe serum concentration of Propiverine can be decreased when it is combined with Dabrafenib.Approved, Investigational
DarifenacinThe risk or severity of adverse effects can be increased when Darifenacin is combined with Propiverine.Approved, Investigational
DarunavirThe metabolism of Propiverine can be decreased when combined with Darunavir.Approved
DasatinibThe serum concentration of Propiverine can be increased when it is combined with Dasatinib.Approved, Investigational
DecamethoniumThe therapeutic efficacy of Propiverine can be decreased when used in combination with Decamethonium.Approved
DeferasiroxThe serum concentration of Propiverine can be decreased when it is combined with Deferasirox.Approved, Investigational
DelavirdineThe metabolism of Propiverine can be decreased when combined with Delavirdine.Approved
DemecariumThe therapeutic efficacy of Propiverine can be decreased when used in combination with Demecarium.Approved
DesloratadineThe risk or severity of adverse effects can be increased when Desloratadine is combined with Propiverine.Approved, Investigational
DexetimideThe risk or severity of adverse effects can be increased when Dexetimide is combined with Propiverine.Withdrawn
DextromoramideThe risk or severity of adverse effects can be increased when Propiverine is combined with Dextromoramide.Experimental, Illicit
DextropropoxypheneThe risk or severity of adverse effects can be increased when Propiverine is combined with Dextropropoxyphene.Approved, Illicit, Investigational, Withdrawn
DezocineThe risk or severity of adverse effects can be increased when Propiverine is combined with Dezocine.Approved, Investigational
DichlorvosThe therapeutic efficacy of Propiverine can be decreased when used in combination with Dichlorvos.Vet Approved
DicyclomineThe risk or severity of adverse effects can be increased when Dicyclomine is combined with Propiverine.Approved
DihydrocodeineThe risk or severity of adverse effects can be increased when Propiverine is combined with Dihydrocodeine.Approved, Illicit
DihydroergotamineThe metabolism of Propiverine can be decreased when combined with Dihydroergotamine.Approved, Investigational
DihydroetorphineThe risk or severity of adverse effects can be increased when Propiverine is combined with Dihydroetorphine.Experimental, Illicit
DihydromorphineThe risk or severity of adverse effects can be increased when Propiverine is combined with Dihydromorphine.Experimental, Illicit
DiltiazemThe metabolism of Propiverine can be decreased when combined with Diltiazem.Approved, Investigational
DiphenhydramineThe risk or severity of adverse effects can be increased when Diphenhydramine is combined with Propiverine.Approved, Investigational
DiphenoxylateThe risk or severity of adverse effects can be increased when Propiverine is combined with Diphenoxylate.Approved, Illicit
DistigmineThe therapeutic efficacy of Propiverine can be decreased when used in combination with Distigmine.Experimental
DonepezilThe therapeutic efficacy of Propiverine can be decreased when used in combination with Donepezil.Approved
DoxycyclineThe metabolism of Propiverine can be decreased when combined with Doxycycline.Approved, Investigational, Vet Approved
DPDPEThe risk or severity of adverse effects can be increased when Propiverine is combined with DPDPE.Experimental
DronabinolPropiverine may increase the tachycardic activities of Dronabinol.Approved, Illicit
DronedaroneThe metabolism of Propiverine can be decreased when combined with Dronedarone.Approved
EchothiophateThe therapeutic efficacy of Propiverine can be decreased when used in combination with Echothiophate.Approved
EdrophoniumThe therapeutic efficacy of Propiverine can be decreased when used in combination with Edrophonium.Approved
EluxadolinePropiverine may increase the constipating activities of Eluxadoline.Approved, Investigational
EmeproniumThe risk or severity of adverse effects can be increased when Propiverine is combined with Emepronium.Experimental
EnzalutamideThe serum concentration of Propiverine can be decreased when it is combined with Enzalutamide.Approved
EpitizideThe serum concentration of Epitizide can be increased when it is combined with Propiverine.Experimental
ErythromycinThe metabolism of Propiverine can be decreased when combined with Erythromycin.Approved, Investigational, Vet Approved
EtanautineThe risk or severity of adverse effects can be increased when Propiverine is combined with Etanautine.Experimental
EthopropazineThe risk or severity of adverse effects can be increased when Ethopropazine is combined with Propiverine.Approved
EthylmorphineThe risk or severity of adverse effects can be increased when Propiverine is combined with Ethylmorphine.Approved, Illicit
EtorphineThe risk or severity of adverse effects can be increased when Propiverine is combined with Etorphine.Illicit, Vet Approved
EtybenzatropineThe risk or severity of adverse effects can be increased when Propiverine is combined with Etybenzatropine.Experimental
FentanylThe risk or severity of adverse effects can be increased when Propiverine is combined with Fentanyl.Approved, Illicit, Investigational, Vet Approved
FenthionThe therapeutic efficacy of Propiverine can be decreased when used in combination with Fenthion.Vet Approved
FesoterodineThe risk or severity of adverse effects can be increased when Fesoterodine is combined with Propiverine.Approved
FlavoxateThe risk or severity of adverse effects can be increased when Flavoxate is combined with Propiverine.Approved
FluconazoleThe metabolism of Propiverine can be decreased when combined with Fluconazole.Approved, Investigational
FluvoxamineThe metabolism of Propiverine can be decreased when combined with Fluvoxamine.Approved, Investigational
FosamprenavirThe metabolism of Propiverine can be decreased when combined with Fosamprenavir.Approved
FosaprepitantThe serum concentration of Propiverine can be increased when it is combined with Fosaprepitant.Approved
FosphenytoinThe metabolism of Propiverine can be increased when combined with Fosphenytoin.Approved, Investigational
Fusidic AcidThe serum concentration of Propiverine can be increased when it is combined with Fusidic Acid.Approved, Investigational
GalantamineThe therapeutic efficacy of Propiverine can be decreased when used in combination with Galantamine.Approved
GallamineThe risk or severity of adverse effects can be increased when Propiverine is combined with Gallamine.Experimental
Gallamine TriethiodideThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Propiverine.Approved
Glucagon recombinantThe risk or severity of adverse effects can be increased when Propiverine is combined with Glucagon recombinant.Approved
GlycopyrroniumPropiverine may increase the anticholinergic activities of Glycopyrronium.Approved, Investigational, Vet Approved
HeroinThe risk or severity of adverse effects can be increased when Propiverine is combined with Heroin.Approved, Illicit, Investigational
HomatropineThe risk or severity of adverse effects can be increased when Propiverine is combined with Homatropine.Approved
Human secretinThe therapeutic efficacy of Human secretin can be decreased when used in combination with Propiverine.Approved
Huperzine AThe therapeutic efficacy of Propiverine can be decreased when used in combination with Huperzine A.Approved, Investigational
HydrochlorothiazideThe serum concentration of Hydrochlorothiazide can be increased when it is combined with Propiverine.Approved, Vet Approved
HydrocodoneThe risk or severity of adverse effects can be increased when Propiverine is combined with Hydrocodone.Approved, Illicit
HydroflumethiazideThe serum concentration of Hydroflumethiazide can be increased when it is combined with Propiverine.Approved, Investigational
HydromorphoneThe risk or severity of adverse effects can be increased when Propiverine is combined with Hydromorphone.Approved, Illicit
HyoscyamineThe risk or severity of adverse effects can be increased when Hyoscyamine is combined with Propiverine.Approved
IdelalisibThe metabolism of Propiverine can be decreased when combined with Idelalisib.Approved
ImatinibThe metabolism of Propiverine can be decreased when combined with Imatinib.Approved
IndapamideThe serum concentration of Indapamide can be increased when it is combined with Propiverine.Approved
IndinavirThe metabolism of Propiverine can be decreased when combined with Indinavir.Approved
IpidacrineThe therapeutic efficacy of Propiverine can be decreased when used in combination with Ipidacrine.Experimental
Ipratropium bromideThe risk or severity of adverse effects can be increased when Ipratropium bromide is combined with Propiverine.Approved
IsavuconazoleThe serum concentration of Propiverine can be increased when it is combined with Isavuconazole.Approved, Investigational
IsavuconazoniumThe metabolism of Propiverine can be decreased when combined with Isavuconazonium.Approved, Investigational
IsoflurophateThe therapeutic efficacy of Propiverine can be decreased when used in combination with Isoflurophate.Approved, Investigational, Withdrawn
IsradipineThe metabolism of Propiverine can be decreased when combined with Isradipine.Approved, Investigational
ItoprideThe therapeutic efficacy of Itopride can be decreased when used in combination with Propiverine.Investigational
ItraconazoleThe metabolism of Propiverine can be decreased when combined with Itraconazole.Approved, Investigational
IvacaftorThe serum concentration of Propiverine can be increased when it is combined with Ivacaftor.Approved
KetobemidoneThe risk or severity of adverse effects can be increased when Propiverine is combined with Ketobemidone.Approved, Investigational
KetoconazoleThe metabolism of Propiverine can be decreased when combined with Ketoconazole.Approved, Investigational
Levomethadyl AcetateThe risk or severity of adverse effects can be increased when Propiverine is combined with Levomethadyl Acetate.Approved, Investigational
LevorphanolThe risk or severity of adverse effects can be increased when Propiverine is combined with Levorphanol.Approved
LofentanilThe risk or severity of adverse effects can be increased when Propiverine is combined with Lofentanil.Illicit
LopinavirThe metabolism of Propiverine can be decreased when combined with Lopinavir.Approved
LorpiprazoleThe serum concentration of Propiverine can be increased when it is combined with Lorpiprazole.Approved
LovastatinThe metabolism of Propiverine can be decreased when combined with Lovastatin.Approved, Investigational
LuliconazoleThe serum concentration of Propiverine can be increased when it is combined with Luliconazole.Approved
LumacaftorThe metabolism of Propiverine can be increased when combined with Lumacaftor.Approved
MalathionThe therapeutic efficacy of Propiverine can be decreased when used in combination with Malathion.Approved, Investigational
MazaticolThe risk or severity of adverse effects can be increased when Propiverine is combined with Mazaticol.Experimental
MecamylamineThe risk or severity of adverse effects can be increased when Mecamylamine is combined with Propiverine.Approved, Investigational
MefloquineThe therapeutic efficacy of Propiverine can be decreased when used in combination with Mefloquine.Approved, Investigational
MemantineThe therapeutic efficacy of Propiverine can be decreased when used in combination with Memantine.Approved, Investigational
MeptazinolThe risk or severity of adverse effects can be increased when Propiverine is combined with Meptazinol.Experimental
MethadoneThe risk or severity of adverse effects can be increased when Propiverine is combined with Methadone.Approved
Methadyl AcetateThe risk or severity of adverse effects can be increased when Propiverine is combined with Methadyl Acetate.Approved, Illicit
Methanesulfonyl FluorideThe therapeutic efficacy of Propiverine can be decreased when used in combination with Methanesulfonyl Fluoride.Investigational
MethanthelineThe risk or severity of adverse effects can be increased when Methantheline is combined with Propiverine.Approved, Investigational
MethscopolamineThe risk or severity of adverse effects can be increased when Propiverine is combined with Methscopolamine.Approved
MethyclothiazideThe serum concentration of Methyclothiazide can be increased when it is combined with Propiverine.Approved
Methylscopolamine bromideThe risk or severity of adverse effects can be increased when Propiverine is combined with Methylscopolamine bromide.Approved
MetixeneThe risk or severity of adverse effects can be increased when Propiverine is combined with Metixene.Approved
MetoclopramideThe therapeutic efficacy of Propiverine can be decreased when used in combination with Metoclopramide.Approved, Investigational
MetolazoneThe serum concentration of Metolazone can be increased when it is combined with Propiverine.Approved
MianserinMianserin may increase the anticholinergic activities of Propiverine.Approved, Investigational
MifepristoneThe serum concentration of Propiverine can be increased when it is combined with Mifepristone.Approved, Investigational
MinaprineThe therapeutic efficacy of Propiverine can be decreased when used in combination with Minaprine.Approved
MirabegronThe risk or severity of adverse effects can be increased when Propiverine is combined with Mirabegron.Approved
MitotaneThe serum concentration of Propiverine can be decreased when it is combined with Mitotane.Approved
MorphineThe risk or severity of adverse effects can be increased when Propiverine is combined with Morphine.Approved, Investigational
NabilonePropiverine may increase the tachycardic activities of Nabilone.Approved, Investigational
NalbuphineThe risk or severity of adverse effects can be increased when Propiverine is combined with Nalbuphine.Approved
NefazodoneThe metabolism of Propiverine can be decreased when combined with Nefazodone.Approved, Withdrawn
NelfinavirThe metabolism of Propiverine can be decreased when combined with Nelfinavir.Approved
NeostigmineThe therapeutic efficacy of Propiverine can be decreased when used in combination with Neostigmine.Approved, Vet Approved
NetupitantThe serum concentration of Propiverine can be increased when it is combined with Netupitant.Approved, Investigational
NevirapineThe metabolism of Propiverine can be increased when combined with Nevirapine.Approved
NicomorphineThe risk or severity of adverse effects can be increased when Propiverine is combined with Nicomorphine.Experimental
NilotinibThe metabolism of Propiverine can be decreased when combined with Nilotinib.Approved, Investigational
NormethadoneThe risk or severity of adverse effects can be increased when Propiverine is combined with Normethadone.Approved, Illicit
OlaparibThe metabolism of Propiverine can be decreased when combined with Olaparib.Approved
OpiumThe risk or severity of adverse effects can be increased when Propiverine is combined with Opium.Approved, Illicit
OrphenadrineThe risk or severity of adverse effects can be increased when Orphenadrine is combined with Propiverine.Approved
OsimertinibThe serum concentration of Propiverine can be increased when it is combined with Osimertinib.Approved
OtiloniumThe risk or severity of adverse effects can be increased when Propiverine is combined with Otilonium.Experimental, Investigational
OxitropiumThe risk or severity of adverse effects can be increased when Propiverine is combined with Oxitropium.Investigational
OxybutyninThe risk or severity of adverse effects can be increased when Oxybutynin is combined with Propiverine.Approved, Investigational
OxycodoneThe risk or severity of adverse effects can be increased when Propiverine is combined with Oxycodone.Approved, Illicit, Investigational
OxymorphoneThe risk or severity of adverse effects can be increased when Propiverine is combined with Oxymorphone.Approved, Investigational, Vet Approved
OxyphenoniumThe risk or severity of adverse effects can be increased when Oxyphenonium is combined with Propiverine.Approved
PalbociclibThe serum concentration of Propiverine can be increased when it is combined with Palbociclib.Approved, Investigational
PancuroniumThe risk or severity of adverse effects can be increased when Pancuronium is combined with Propiverine.Approved
ParaoxonThe therapeutic efficacy of Propiverine can be decreased when used in combination with Paraoxon.Experimental
PentazocineThe risk or severity of adverse effects can be increased when Propiverine is combined with Pentazocine.Approved, Vet Approved
PentobarbitalThe metabolism of Propiverine can be increased when combined with Pentobarbital.Approved, Investigational, Vet Approved
PentoliniumThe risk or severity of adverse effects can be increased when Pentolinium is combined with Propiverine.Approved
PethidineThe risk or severity of adverse effects can be increased when Propiverine is combined with Pethidine.Approved
PhenazocineThe risk or severity of adverse effects can be increased when Propiverine is combined with Phenazocine.Experimental
PhenglutarimideThe risk or severity of adverse effects can be increased when Phenglutarimide is combined with Propiverine.Experimental
PhenobarbitalThe metabolism of Propiverine can be increased when combined with Phenobarbital.Approved, Investigational
PhenoperidineThe risk or severity of adverse effects can be increased when Propiverine is combined with Phenoperidine.Experimental
PhenytoinThe metabolism of Propiverine can be increased when combined with Phenytoin.Approved, Vet Approved
PhysostigmineThe therapeutic efficacy of Propiverine can be decreased when used in combination with Physostigmine.Approved, Investigational
PipecuroniumThe risk or severity of adverse effects can be increased when Pipecuronium is combined with Propiverine.Approved
PirenzepineThe risk or severity of adverse effects can be increased when Pirenzepine is combined with Propiverine.Approved
PiritramideThe risk or severity of adverse effects can be increased when Propiverine is combined with Piritramide.Approved, Investigational
PitolisantThe serum concentration of Propiverine can be decreased when it is combined with Pitolisant.Approved, Investigational
PolythiazideThe serum concentration of Polythiazide can be increased when it is combined with Propiverine.Approved
PosaconazoleThe metabolism of Propiverine can be decreased when combined with Posaconazole.Approved, Investigational, Vet Approved
Potassium ChloridePropiverine may increase the ulcerogenic activities of Potassium Chloride.Approved, Withdrawn
PramlintidePramlintide may increase the anticholinergic activities of Propiverine.Approved, Investigational
PrimidoneThe metabolism of Propiverine can be increased when combined with Primidone.Approved, Vet Approved
ProcyclidineThe risk or severity of adverse effects can be increased when Procyclidine is combined with Propiverine.Approved
PropanthelineThe risk or severity of adverse effects can be increased when Propantheline is combined with Propiverine.Approved
PyridostigmineThe therapeutic efficacy of Propiverine can be decreased when used in combination with Pyridostigmine.Approved, Investigational
QuinethazoneThe serum concentration of Quinethazone can be increased when it is combined with Propiverine.Approved
QuinidineThe risk or severity of adverse effects can be increased when Quinidine is combined with Propiverine.Approved, Investigational
RamosetronPropiverine may increase the constipating activities of Ramosetron.Approved, Investigational
RanolazineThe metabolism of Propiverine can be decreased when combined with Ranolazine.Approved, Investigational
RemifentanilThe risk or severity of adverse effects can be increased when Propiverine is combined with Remifentanil.Approved
RifabutinThe metabolism of Propiverine can be increased when combined with Rifabutin.Approved, Investigational
RifampicinThe metabolism of Propiverine can be increased when combined with Rifampicin.Approved
RifapentineThe metabolism of Propiverine can be increased when combined with Rifapentine.Approved, Investigational
RivastigmineThe therapeutic efficacy of Propiverine can be decreased when used in combination with Rivastigmine.Approved, Investigational
RucaparibThe metabolism of Propiverine can be decreased when combined with Rucaparib.Approved, Investigational
SaquinavirThe metabolism of Propiverine can be decreased when combined with Saquinavir.Approved, Investigational
SarilumabThe therapeutic efficacy of Propiverine can be decreased when used in combination with Sarilumab.Approved, Investigational
ScopolamineThe risk or severity of adverse effects can be increased when Scopolamine is combined with Propiverine.Approved, Investigational
SecretinThe therapeutic efficacy of Secretin can be decreased when used in combination with Propiverine.Approved, Investigational
SildenafilThe metabolism of Propiverine can be decreased when combined with Sildenafil.Approved, Investigational
SiltuximabThe serum concentration of Propiverine can be decreased when it is combined with Siltuximab.Approved, Investigational
SimeprevirThe serum concentration of Propiverine can be increased when it is combined with Simeprevir.Approved
SolifenacinThe risk or severity of adverse effects can be increased when Solifenacin is combined with Propiverine.Approved
St. John's WortThe serum concentration of Propiverine can be decreased when it is combined with St. John's Wort.Approved, Investigational, Nutraceutical
StiripentolThe serum concentration of Propiverine can be increased when it is combined with Stiripentol.Approved
SufentanilThe risk or severity of adverse effects can be increased when Propiverine is combined with Sufentanil.Approved, Investigational
SulfisoxazoleThe metabolism of Propiverine can be decreased when combined with Sulfisoxazole.Approved, Vet Approved
SulpiridePropiverine may increase the anticholinergic activities of Sulpiride.Approved, Investigational
TacrineThe therapeutic efficacy of Propiverine can be decreased when used in combination with Tacrine.Investigational, Withdrawn
TapentadolThe risk or severity of adverse effects can be increased when Propiverine is combined with Tapentadol.Approved
TelaprevirThe metabolism of Propiverine can be decreased when combined with Telaprevir.Approved, Withdrawn
TelithromycinThe metabolism of Propiverine can be decreased when combined with Telithromycin.Approved
TiclopidineThe metabolism of Propiverine can be decreased when combined with Ticlopidine.Approved
TilidineThe risk or severity of adverse effects can be increased when Propiverine is combined with Tilidine.Experimental
TiotropiumPropiverine may increase the anticholinergic activities of Tiotropium.Approved
TocilizumabThe serum concentration of Propiverine can be decreased when it is combined with Tocilizumab.Approved
TolterodineThe risk or severity of adverse effects can be increased when Tolterodine is combined with Propiverine.Approved, Investigational
TopiramateThe risk or severity of adverse effects can be increased when Propiverine is combined with Topiramate.Approved
TramadolThe risk or severity of adverse effects can be increased when Propiverine is combined with Tramadol.Approved, Investigational
TrichlorfonThe therapeutic efficacy of Propiverine can be decreased when used in combination with Trichlorfon.Vet Approved
TrichlormethiazideThe serum concentration of Trichlormethiazide can be increased when it is combined with Propiverine.Approved, Vet Approved
TrihexyphenidylThe risk or severity of adverse effects can be increased when Trihexyphenidyl is combined with Propiverine.Approved
TrimethaphanThe risk or severity of adverse effects can be increased when Trimethaphan is combined with Propiverine.Approved, Investigational
TropatepineThe risk or severity of adverse effects can be increased when Propiverine is combined with Tropatepine.Experimental
TropicamideThe risk or severity of adverse effects can be increased when Tropicamide is combined with Propiverine.Approved, Investigational
TrospiumThe risk or severity of adverse effects can be increased when Trospium is combined with Propiverine.Approved
TubocurarineThe risk or severity of adverse effects can be increased when Tubocurarine is combined with Propiverine.Approved
TyrothricinThe therapeutic efficacy of Propiverine can be decreased when used in combination with Tyrothricin.Approved
UmeclidiniumPropiverine may increase the anticholinergic activities of Umeclidinium.Approved
VecuroniumThe risk or severity of adverse effects can be increased when Vecuronium is combined with Propiverine.Approved
VemurafenibThe serum concentration of Propiverine can be decreased when it is combined with Vemurafenib.Approved
VenlafaxineThe metabolism of Propiverine can be decreased when combined with Venlafaxine.Approved
VerapamilThe metabolism of Propiverine can be decreased when combined with Verapamil.Approved
VoriconazoleThe metabolism of Propiverine can be decreased when combined with Voriconazole.Approved, Investigational
ZiprasidoneThe metabolism of Propiverine can be decreased when combined with Ziprasidone.Approved
Food Interactions
Not Available

References

General References
  1. McKeage K: Propiverine: a review of its use in the treatment of adults and children with overactive bladder associated with idiopathic or neurogenic detrusor overactivity, and in men with lower urinary tract symptoms. Clin Drug Investig. 2013 Jan;33(1):71-91. doi: 10.1007/s40261-012-0046-9. [PubMed:23288694]
  2. Haustein KO, Huller G: On the pharmacokinetics and metabolism of propiverine in man. Eur J Drug Metab Pharmacokinet. 1988 Apr-Jun;13(2):81-90. [PubMed:3208795]
  3. Chess-Williams R: Muscarinic receptors of the urinary bladder: detrusor, urothelial and prejunctional. Auton Autacoid Pharmacol. 2002 Jun;22(3):133-45. [PubMed:12452898]
  4. Maruyama S, Oki T, Otsuka A, Shinbo H, Ozono S, Kageyama S, Mikami Y, Araki I, Takeda M, Masuyama K, Yamada S: Human muscarinic receptor binding characteristics of antimuscarinic agents to treat overactive bladder. J Urol. 2006 Jan;175(1):365-9. [PubMed:16406943]
  5. Sakakibara F, Takahama K, Nanri M, Sasaki E: Pharmacological Properties of Propiverine Contribute to Improving Lower Urinary Tract Dysfunctions in Rats with Spinal Cord Injuries. Drug Res (Stuttg). 2016 Sep;66(9):464-469. doi: 10.1055/s-0042-110855. Epub 2016 Oct 17. [PubMed:27750360]
  6. Mictoryl monograph [Link]
  7. CDR CLINICAL REVIEW REPORT FOR MICTORYL [Link]
  8. The Efficacy and Safety of Propiverine Hydrochloride in Patients with Overactive Bladder Symptoms Who Poorly Responded to Previous Anticholinergic Agents [Link]
  9. Propiverine hydrochloride [Link]
  10. Propiverine Hydrochloride PubChem [Link]
  11. Public assessment report [Link]
  12. Pharmacokinetic Studies on Propiverine Hydrochloride [Link]
  13. Mictonorm [Link]
  14. The muscarinic receptor antagonist propiverine exhibits α1-adrenoceptor antagonism in human prostate and porcine trigonum [Link]
  15. Mayo Clinic, Overactive Bladder [Link]
  16. Maximizing the Treatment of Overactive Bladder in the Elderly [Link]
  17. Muscarinic receptor antagonists for overactive bladder [Link]
  18. Propiverine overview [Link]
  19. The N-Oxide Metabolite Contributes to Bladder Selectivity Resulting from Oral Propiverine: Muscarinic Receptor Binding and Pharmacokinetics [Link]
External Links
Human Metabolome Database
HMDB0041999
KEGG Drug
D08441
KEGG Compound
C07852
PubChem Compound
4942
PubChem Substance
347828547
ChemSpider
4773
ChEBI
8493
ChEMBL
CHEMBL1078261
Wikipedia
Propiverine
ATC Codes
G04BD06 — Propiverine
AHFS Codes
  • 86:12.04 — Antimuscarinics
MSDS
Download (168 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
2CompletedNot AvailableOveractive Bladder1
3CompletedTreatmentBladder Disorder, Neurogenic / Neurogenic Bladder Disorder / Neurogenic Urinary Bladder Disorder / Overactive Detrusor Function / Urinary Bladder Disorder, Neurogenic / Urinary Bladder Neurogenic Dysfunction / Urinary Bladder, Neurogenic / Urinary Incontinence (UI) / Urologic Diseases1
3CompletedTreatmentOveractive Bladder1
3CompletedTreatmentUrinary Bladder, Overactive1
4CompletedNot AvailableOveractive Bladder Syndrome1
4CompletedTreatmentOveractive Bladder1
4CompletedTreatmentOveractive Bladder (OAB)1
Not AvailableCompletedTreatmentUrinary Incontinence (UI)1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage forms
FormRouteStrength
Capsule, extended releaseOral30 mg
Capsule, extended releaseOral45 mg
TabletOral5 mg
Prices
Not Available
Patents
Not Available

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)224-226http://www.chemicalbook.com/ChemicalProductProperty_EN_CB3855472.htm
boiling point (°C)484.2 MSDS
water solubility5mg/mLhttp://www.chemicalbook.com/ChemicalProductProperty_EN_CB3855472.htm
Predicted Properties
PropertyValueSource
Water Solubility0.00635 mg/mLALOGPS
logP4.16ALOGPS
logP4.25ChemAxon
logS-4.8ALOGPS
pKa (Strongest Basic)8.72ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count3ChemAxon
Hydrogen Donor Count0ChemAxon
Polar Surface Area38.77 Å2ChemAxon
Rotatable Bond Count8ChemAxon
Refractivity107.73 m3·mol-1ChemAxon
Polarizability41.88 Å3ChemAxon
Number of Rings3ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Predicted ADMET features
Not Available

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSNot Available
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available

Taxonomy

Description
This compound belongs to the class of organic compounds known as diphenylmethanes. These are compounds containing a diphenylmethane moiety, which consists of a methane wherein two hydrogen atoms are replaced by two phenyl groups.
Kingdom
Organic compounds
Super Class
Benzenoids
Class
Benzene and substituted derivatives
Sub Class
Diphenylmethanes
Direct Parent
Diphenylmethanes
Alternative Parents
Benzylethers / Piperidines / Trialkylamines / Carboxylic acid esters / Amino acids and derivatives / Monocarboxylic acids and derivatives / Dialkyl ethers / Azacyclic compounds / Organopnictogen compounds / Organic oxides
show 2 more
Substituents
Diphenylmethane / Benzylether / Piperidine / Amino acid or derivatives / Carboxylic acid ester / Tertiary amine / Tertiary aliphatic amine / Carboxylic acid derivative / Dialkyl ether / Ether
show 13 more
Molecular Framework
Aromatic heteromonocyclic compounds
External Descriptors
diarylmethane (CHEBI:8493)

Targets

Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Antagonist
General Function
Phosphatidylinositol phospholipase c activity
Specific Function
The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the...
Gene Name
CHRM1
Uniprot ID
P11229
Uniprot Name
Muscarinic acetylcholine receptor M1
Molecular Weight
51420.375 Da
References
  1. Maruyama S, Oki T, Otsuka A, Shinbo H, Ozono S, Kageyama S, Mikami Y, Araki I, Takeda M, Masuyama K, Yamada S: Human muscarinic receptor binding characteristics of antimuscarinic agents to treat overactive bladder. J Urol. 2006 Jan;175(1):365-9. [PubMed:16406943]
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Antagonist
General Function
G-protein coupled acetylcholine receptor activity
Specific Function
The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the...
Gene Name
CHRM2
Uniprot ID
P08172
Uniprot Name
Muscarinic acetylcholine receptor M2
Molecular Weight
51714.605 Da
References
  1. Maruyama S, Oki T, Otsuka A, Shinbo H, Ozono S, Kageyama S, Mikami Y, Araki I, Takeda M, Masuyama K, Yamada S: Human muscarinic receptor binding characteristics of antimuscarinic agents to treat overactive bladder. J Urol. 2006 Jan;175(1):365-9. [PubMed:16406943]
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Antagonist
General Function
Receptor activity
Specific Function
The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the...
Gene Name
CHRM3
Uniprot ID
P20309
Uniprot Name
Muscarinic acetylcholine receptor M3
Molecular Weight
66127.445 Da
References
  1. Maruyama S, Oki T, Otsuka A, Shinbo H, Ozono S, Kageyama S, Mikami Y, Araki I, Takeda M, Masuyama K, Yamada S: Human muscarinic receptor binding characteristics of antimuscarinic agents to treat overactive bladder. J Urol. 2006 Jan;175(1):365-9. [PubMed:16406943]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Antagonist
General Function
Guanyl-nucleotide exchange factor activity
Specific Function
The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the...
Gene Name
CHRM4
Uniprot ID
P08173
Uniprot Name
Muscarinic acetylcholine receptor M4
Molecular Weight
53048.65 Da
References
  1. Maruyama S, Oki T, Otsuka A, Shinbo H, Ozono S, Kageyama S, Mikami Y, Araki I, Takeda M, Masuyama K, Yamada S: Human muscarinic receptor binding characteristics of antimuscarinic agents to treat overactive bladder. J Urol. 2006 Jan;175(1):365-9. [PubMed:16406943]
Kind
Protein
Organism
Human
Pharmacological action
Yes
General Function
Phosphatidylinositol phospholipase c activity
Specific Function
The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the...
Gene Name
CHRM5
Uniprot ID
P08912
Uniprot Name
Muscarinic acetylcholine receptor M5
Molecular Weight
60073.205 Da
References
  1. Maruyama S, Oki T, Otsuka A, Shinbo H, Ozono S, Kageyama S, Mikami Y, Araki I, Takeda M, Masuyama K, Yamada S: Human muscarinic receptor binding characteristics of antimuscarinic agents to treat overactive bladder. J Urol. 2006 Jan;175(1):365-9. [PubMed:16406943]
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Antagonist
General Function
Voltage-gated calcium channel activity
Specific Function
Voltage-sensitive calcium channels (VSCC) mediate the entry of calcium ions into excitable cells and are also involved in a variety of calcium-dependent processes, including muscle contraction, hor...
Gene Name
CACNA1C
Uniprot ID
Q13936
Uniprot Name
Voltage-dependent L-type calcium channel subunit alpha-1C
Molecular Weight
248974.1 Da
References
  1. Maruyama S, Oki T, Otsuka A, Shinbo H, Ozono S, Kageyama S, Mikami Y, Araki I, Takeda M, Masuyama K, Yamada S: Human muscarinic receptor binding characteristics of antimuscarinic agents to treat overactive bladder. J Urol. 2006 Jan;175(1):365-9. [PubMed:16406943]
  2. The muscarinic receptor antagonist propiverine exhibits α1-adrenoceptor antagonism in human prostate and porcine trigonum [Link]
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Antagonist
General Function
Protein heterodimerization activity
Specific Function
This alpha-adrenergic receptor mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system. Its effect is mediated by G(q) and G(11) prot...
Gene Name
ADRA1A
Uniprot ID
P35348
Uniprot Name
Alpha-1A adrenergic receptor
Molecular Weight
51486.005 Da
References
  1. The muscarinic receptor antagonist propiverine exhibits α1-adrenoceptor antagonism in human prostate and porcine trigonum [Link]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
No
Actions
Substrate
General Function
Vitamin d3 25-hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation react...
Gene Name
CYP3A4
Uniprot ID
P08684
Uniprot Name
Cytochrome P450 3A4
Molecular Weight
57342.67 Da
References
  1. Mictoryl monograph [Link]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Nadp binding
Specific Function
This protein is involved in the oxidative metabolism of a variety of xenobiotics such as drugs and pesticides. Form I catalyzes the N-oxygenation of secondary and tertiary amines.
Gene Name
FMO1
Uniprot ID
Q01740
Uniprot Name
Dimethylaniline monooxygenase [N-oxide-forming] 1
Molecular Weight
60310.285 Da
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Trimethylamine monooxygenase activity
Specific Function
Involved in the oxidative metabolism of a variety of xenobiotics such as drugs and pesticides. It N-oxygenates primary aliphatic alkylamines as well as secondary and tertiary amines. Plays an impor...
Gene Name
FMO3
Uniprot ID
P31513
Uniprot Name
Dimethylaniline monooxygenase [N-oxide-forming] 3
Molecular Weight
60032.975 Da
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen
Specific Function
Not Available
Gene Name
CYP2B
Uniprot ID
Q14097
Uniprot Name
CYP2B protein
Molecular Weight
43147.81 Da

Drug created on October 20, 2016 15:48 / Updated on May 22, 2018 23:58