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Identification
NameSolifenacin
Accession NumberDB01591  (APRD00168)
TypeSmall Molecule
GroupsApproved
DescriptionSolifenacin (rINN), marketed as solifenacin succinate under the trade name Vesicare, is a urinary antispasmodic of the anticholinergic class. It is used in the treatment of overactive bladder with urge incontinence. [Wikipedia]
Structure
Thumb
SynonymsNot Available
External Identifiers
  • YM-67905
  • YM-905
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Ach-solifenacin SuccinateTablet10 mgOralAccord Healthcare IncNot applicableNot applicableCanada
Ach-solifenacin SuccinateTablet5 mgOralAccord Healthcare IncNot applicableNot applicableCanada
Act SolifenacinTablet10 mgOralActavis Pharma Company2015-09-30Not applicableCanada
Act SolifenacinTablet5 mgOralActavis Pharma Company2015-09-30Not applicableCanada
Auro-solifenacinTablet5 mgOralAuro Pharma Inc2016-01-04Not applicableCanada
Auro-solifenacinTablet10 mgOralAuro Pharma Inc2016-01-04Not applicableCanada
Jamp-solifenacinTablet5 mgOralJamp Pharma Corporation2015-12-29Not applicableCanada
Jamp-solifenacinTablet10 mgOralJamp Pharma Corporation2015-12-29Not applicableCanada
Med-solifenacinTablet5 mgOralGeneric Medical Partners Inc2016-04-18Not applicableCanada
Med-solifenacinTablet10 mgOralGeneric Medical Partners Inc2016-04-18Not applicableCanada
Mint-solifenacinTablet5 mgOralMint Pharmaceuticals Inc2016-04-20Not applicableCanada
Mint-solifenacinTablet10 mgOralMint Pharmaceuticals Inc2016-04-20Not applicableCanada
PMS-solifenacinTablet5 mgOralPharmascience Inc2015-10-28Not applicableCanada
PMS-solifenacinTablet10 mgOralPharmascience Inc2015-10-28Not applicableCanada
Ran-solifenacinTablet10 mgOralRanbaxy Pharmaceuticals Canada Inc.2015-12-29Not applicableCanada
Ran-solifenacinTablet5 mgOralRanbaxy Pharmaceuticals Canada Inc.2015-12-29Not applicableCanada
Sandoz SolifenacinTablet5 mgOralSandoz Canada Incorporated2015-09-30Not applicableCanada
Sandoz SolifenacinTablet5 mgOralSandoz Canada Incorporated2015-09-30Not applicableCanada
Sandoz SolifenacinTablet10 mgOralSandoz Canada Incorporated2015-09-30Not applicableCanada
Sandoz SolifenacinTablet10 mgOralSandoz Canada Incorporated2015-09-30Not applicableCanada
SolifenacinTablet5 mgOralPro Doc LimiteeNot applicableNot applicableCanada
SolifenacinTablet10 mgOralPro Doc LimiteeNot applicableNot applicableCanada
SolifenacinTablet10 mgOralSanis Health Inc2016-11-03Not applicableCanada
Solifenacin SuccinateTablet10 mgOralJubilant Generics LimitedNot applicableNot applicableCanada
Solifenacin SuccinateTablet5 mgOralJubilant Generics LimitedNot applicableNot applicableCanada
Solifenacin Succinate TabletsTablet5 mgOralMda Inc.Not applicableNot applicableCanada
Solifenacin Succinate TabletsTablet10 mgOralMda Inc.Not applicableNot applicableCanada
Teva-solifenacinTablet5 mgOralTeva Canada Limited2015-07-30Not applicableCanada
Teva-solifenacinTablet10 mgOralTeva Canada Limited2015-07-30Not applicableCanada
VesicareTablet10 mgOralAstellas Pharma Canada Inc2006-06-23Not applicableCanada
VesicareTablet, film coated10 mg/1OralPhysicians Total Care, Inc.2007-09-13Not applicableUs
VesicareTablet, film coated5 mg/1OralCardinal Health2005-01-05Not applicableUs
VesicareTablet, film coated5 mg/1OralA S Medication Solutions2005-01-05Not applicableUs
VesicareTablet, film coated5 mg/1OralPhysicians Total Care, Inc.2005-08-29Not applicableUs
VesicareTablet, film coated10 mg/1OralCardinal Health2005-01-05Not applicableUs
VesicareTablet, film coated5 mg/1OralA S Medication Solutions2005-01-05Not applicableUs
VesicareTablet, film coated5 mg/1OralCardinal Health2005-01-05Not applicableUs
VesicareTablet, film coated5 mg/1OralAstellas Pharma Technologies, Inc.2005-01-05Not applicableUs
VesicareTablet5 mgOralAstellas Pharma Canada Inc2006-06-23Not applicableCanada
VesicareTablet, film coated10 mg/1OralCardinal Health2005-01-05Not applicableUs
VesicareTablet, film coated10 mg/1OralAstellas Pharma Technologies, Inc.2005-01-05Not applicableUs
Approved Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Apo-solifenacinTablet5 mgOralApotex IncNot applicableNot applicableCanada
Apo-solifenacinTablet10 mgOralApotex IncNot applicableNot applicableCanada
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
VesikurNot Available
Brand mixturesNot Available
Salts
Name/CASStructureProperties
Solifenacin hydrochloride
Thumb
  • InChI Key: YAUBKMSXTZQZEB-VROPFNGYSA-N
  • Monoisotopic Mass: 398.1761058
  • Average Mass: 398.93
DBSALT001640
Solifenacin succinate
242478-38-2
Thumb
  • InChI Key: RXZMMZZRUPYENV-VROPFNGYSA-N
  • Monoisotopic Mass: 480.226036766
  • Average Mass: 480.5528
DBSALT001639
Categories
UNIIA8910SQJ1U
CAS number242478-37-1
WeightAverage: 362.473
Monoisotopic: 362.199428085
Chemical FormulaC23H26N2O2
InChI KeyFBOUYBDGKBSUES-VXKWHMMOSA-N
InChI
InChI=1S/C23H26N2O2/c26-23(27-21-16-24-13-10-18(21)11-14-24)25-15-12-17-6-4-5-9-20(17)22(25)19-7-2-1-3-8-19/h1-9,18,21-22H,10-16H2/t21-,22-/m0/s1
IUPAC Name
(3R)-1-azabicyclo[2.2.2]octan-3-yl (1S)-1-phenyl-1,2,3,4-tetrahydroisoquinoline-2-carboxylate
SMILES
O=C(O[[email protected]]1CN2CCC1CC2)N1CCC2=CC=CC=C2[C@@H]1C1=CC=CC=C1
Pharmacology
IndicationFor the treatment of overactive bladder with symptoms of urge urinary incontinence, urgency, and urinary frequency.
Structured Indications
PharmacodynamicsSolifenacin is a competitive muscarinic receptor antagonist. Muscarinic receptors play an important role in several major cholinergically mediated functions, including contractions of urinary bladder smooth muscle and stimulation of salivary secretion.
Mechanism of actionSolifenacin is a competitive muscarinic acetylcholine receptor antagonist. The binding of acetylcholine to these receptors, particularly the M3 receptor subtype, plays a critical role in the contraction of smooth muscle. By preventing the binding of acetylcholine to these receptors, solifenacin reduces smooth muscle tone in the bladder, allowing the bladder to retain larger volumes of urine and reducing the number of incontinence episodes.
TargetKindPharmacological actionActionsOrganismUniProt ID
Muscarinic acetylcholine receptor M3Proteinyes
antagonist
HumanP20309 details
Muscarinic acetylcholine receptor M1Proteinunknown
antagonist
HumanP11229 details
Muscarinic acetylcholine receptor M2Proteinunknown
antagonist
HumanP08172 details
Muscarinic acetylcholine receptor M4Proteinunknown
antagonist
HumanP08173 details
Muscarinic acetylcholine receptor M5Proteinunknown
antagonist
HumanP08912 details
Related Articles
AbsorptionThe absolute bioavailability of solifenacin is approximately 90%, and plasma concentrations of solifenacin are proportional to the dose administered.
Volume of distribution
  • 600 L
Protein bindingSolifenacin is approximately 98% (in vivo) bound to human plasma proteins, principally to alpha1-acid glycoprotein.
Metabolism

Solifenacin is extensively metabolized in the liver. The primary pathway for elimination is by way of CYP3A4; however, alternate metabolic pathways exist. The primary metabolic routes of solifenacin are through N-oxidation of the quinuclidin ring and 4R-hydroxylation of tetrahydroisoquinoline ring. One pharmacologically active metabolite (4R-hydroxy solifenacin), occurring at low concentrations and unlikely to contribute significantly to clinical activity, and three pharmacologically inactive metabolites (N-glucuronide and the N-oxide and 4R-hydroxy-N-oxide of solifenacin) have been found in human plasma after oral dosing.

SubstrateEnzymesProduct
Solifenacin
Not Available
4R-hydroxy solifenacinDetails
Solifenacin
Not Available
4R-hydroxy-N-oxide solifenacinDetails
Route of eliminationThe primary pathway for elimination is by way of CYP3A4; however, alternate metabolic pathways exist.
Half lifeThe elimination half-life of solifenacin following chronic dosing is approximately 45-68 hours.
ClearanceNot Available
ToxicityOverdosage with solifenacin can potentially result in severe anticholinergic effects and should be treated accordingly. The highest solifenacin dose given to human volunteers was a single 100 mg dose. Intolerable anticholinergic side effects (fixed and dilated pupils, blurred vision, failure of heel-to-toe exam, tremors and dry skin) occurred on day 3 in normal volunteers taking 50 mg daily (5 times the maximum recommended therapeutic dose).
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
Interactions
Drug Interactions
DrugInteractionDrug group
1,10-PhenanthrolineThe therapeutic efficacy of Solifenacin can be decreased when used in combination with 1,10-Phenanthroline.Experimental
2-HYDROXY-1,4-NAPHTHOQUINONEThe metabolism of Solifenacin can be decreased when combined with 2-HYDROXY-1,4-NAPHTHOQUINONE.Experimental
2-mercaptobenzothiazoleThe metabolism of Solifenacin can be decreased when combined with 2-mercaptobenzothiazole.Vet Approved
AclidiniumAclidinium may increase the anticholinergic activities of Solifenacin.Approved
AlfentanilThe risk or severity of adverse effects can be increased when Solifenacin is combined with Alfentanil.Approved, Illicit
AlphacetylmethadolThe risk or severity of adverse effects can be increased when Solifenacin is combined with Alphacetylmethadol.Experimental, Illicit
AmbenoniumThe therapeutic efficacy of Solifenacin can be decreased when used in combination with Ambenonium.Approved
AmiodaroneThe metabolism of Solifenacin can be decreased when combined with Amiodarone.Approved, Investigational
AmorolfineThe metabolism of Solifenacin can be decreased when combined with Amorolfine.Approved
Amphotericin BThe metabolism of Solifenacin can be decreased when combined with Amphotericin B.Approved, Investigational
AN2690The metabolism of Solifenacin can be decreased when combined with AN2690.Investigational
AnagrelideSolifenacin may increase the QTc-prolonging activities of Anagrelide.Approved
AnidulafunginThe metabolism of Solifenacin can be decreased when combined with Anidulafungin.Approved, Investigational
Anisotropine MethylbromideThe risk or severity of adverse effects can be increased when Anisotropine Methylbromide is combined with Solifenacin.Approved
AprepitantThe serum concentration of Solifenacin can be increased when it is combined with Aprepitant.Approved, Investigational
Arsenic trioxideSolifenacin may increase the QTc-prolonging activities of Arsenic trioxide.Approved, Investigational
ArtemetherThe metabolism of Solifenacin can be decreased when combined with Artemether.Approved
AsenapineSolifenacin may increase the QTc-prolonging activities of Asenapine.Approved
AtazanavirThe metabolism of Solifenacin can be decreased when combined with Atazanavir.Approved, Investigational
AtomoxetineThe metabolism of Solifenacin can be decreased when combined with Atomoxetine.Approved
Atracurium besylateThe risk or severity of adverse effects can be increased when Atracurium besylate is combined with Solifenacin.Approved
AtropineThe risk or severity of adverse effects can be increased when Atropine is combined with Solifenacin.Approved, Vet Approved
AzithromycinSolifenacin may increase the QTc-prolonging activities of Azithromycin.Approved
Bafilomycin A1The metabolism of Solifenacin can be decreased when combined with Bafilomycin A1.Experimental
BedaquilineSolifenacin may increase the QTc-prolonging activities of Bedaquiline.Approved
BenactyzineThe risk or severity of adverse effects can be increased when Solifenacin is combined with Benactyzine.Withdrawn
BendroflumethiazideThe serum concentration of Bendroflumethiazide can be increased when it is combined with Solifenacin.Approved
BenzatropineThe risk or severity of adverse effects can be increased when Benzatropine is combined with Solifenacin.Approved
Benzoic AcidThe metabolism of Solifenacin can be decreased when combined with Benzoic Acid.Approved
BexaroteneThe serum concentration of Solifenacin can be decreased when it is combined with Bexarotene.Approved, Investigational
BezitramideThe risk or severity of adverse effects can be increased when Solifenacin is combined with Bezitramide.Experimental, Illicit, Withdrawn
BifonazoleThe metabolism of Solifenacin can be decreased when combined with Bifonazole.Approved
BiperidenThe risk or severity of adverse effects can be increased when Biperiden is combined with Solifenacin.Approved
BoceprevirThe metabolism of Solifenacin can be decreased when combined with Boceprevir.Approved
BortezomibThe metabolism of Solifenacin can be decreased when combined with Bortezomib.Approved, Investigational
BosentanThe serum concentration of Solifenacin can be decreased when it is combined with Bosentan.Approved, Investigational
Botulinum Toxin Type ASolifenacin may increase the anticholinergic activities of Botulinum Toxin Type A.Approved, Investigational
Botulinum Toxin Type BSolifenacin may increase the anticholinergic activities of Botulinum Toxin Type B.Approved
BuprenorphineThe risk or severity of adverse effects can be increased when Solifenacin is combined with Buprenorphine.Approved, Illicit, Investigational, Vet Approved
ButenafineThe metabolism of Solifenacin can be decreased when combined with Butenafine.Approved
ButoconazoleThe metabolism of Solifenacin can be decreased when combined with Butoconazole.Approved
ButorphanolThe risk or severity of adverse effects can be increased when Solifenacin is combined with Butorphanol.Approved, Illicit, Vet Approved
CandicidinThe metabolism of Solifenacin can be decreased when combined with Candicidin.Withdrawn
CarbamazepineThe metabolism of Solifenacin can be increased when combined with Carbamazepine.Approved, Investigational
CarfentanilThe risk or severity of adverse effects can be increased when Solifenacin is combined with Carfentanil.Illicit, Vet Approved
CaspofunginThe metabolism of Solifenacin can be decreased when combined with Caspofungin.Approved
CeritinibThe serum concentration of Solifenacin can be increased when it is combined with Ceritinib.Approved
CeruleninThe metabolism of Solifenacin can be decreased when combined with Cerulenin.Approved
ChloroquineSolifenacin may increase the QTc-prolonging activities of Chloroquine.Approved, Vet Approved
ChlorothiazideThe serum concentration of Chlorothiazide can be increased when it is combined with Solifenacin.Approved, Vet Approved
ChloroxineThe metabolism of Solifenacin can be decreased when combined with Chloroxine.Approved
ChlorphenoxamineThe risk or severity of adverse effects can be increased when Solifenacin is combined with Chlorphenoxamine.Withdrawn
ChlorpromazineSolifenacin may increase the QTc-prolonging activities of Chlorpromazine.Approved, Vet Approved
ChlorthalidoneThe serum concentration of Chlorthalidone can be increased when it is combined with Solifenacin.Approved
CiclopiroxThe metabolism of Solifenacin can be decreased when combined with Ciclopirox.Approved, Investigational
CimetropiumSolifenacin may increase the anticholinergic activities of Cimetropium.Experimental
CiprofloxacinSolifenacin may increase the QTc-prolonging activities of Ciprofloxacin.Approved, Investigational
CisaprideSolifenacin may increase the QTc-prolonging activities of Cisapride.Approved, Investigational, Withdrawn
CitalopramSolifenacin may increase the QTc-prolonging activities of Citalopram.Approved
ClarithromycinThe metabolism of Solifenacin can be decreased when combined with Clarithromycin.Approved
ClemastineThe metabolism of Solifenacin can be decreased when combined with Clemastine.Approved
ClotrimazoleThe metabolism of Solifenacin can be decreased when combined with Clotrimazole.Approved, Vet Approved
ClozapineSolifenacin may increase the QTc-prolonging activities of Clozapine.Approved
CobicistatThe metabolism of Solifenacin can be decreased when combined with Cobicistat.Approved
CodeineThe risk or severity of adverse effects can be increased when Solifenacin is combined with Codeine.Approved, Illicit
ConivaptanThe serum concentration of Solifenacin can be increased when it is combined with Conivaptan.Approved, Investigational
CordycepinThe metabolism of Solifenacin can be decreased when combined with Cordycepin.Investigational
CoumaphosThe therapeutic efficacy of Solifenacin can be decreased when used in combination with Coumaphos.Vet Approved
CrizotinibSolifenacin may increase the QTc-prolonging activities of Crizotinib.Approved
CyclopentolateThe risk or severity of adverse effects can be increased when Cyclopentolate is combined with Solifenacin.Approved
CyclosporineThe metabolism of Solifenacin can be decreased when combined with Cyclosporine.Approved, Investigational, Vet Approved
DabrafenibThe serum concentration of Solifenacin can be decreased when it is combined with Dabrafenib.Approved
DarifenacinThe risk or severity of adverse effects can be increased when Darifenacin is combined with Solifenacin.Approved, Investigational
DarunavirThe metabolism of Solifenacin can be decreased when combined with Darunavir.Approved
DasatinibThe serum concentration of Solifenacin can be increased when it is combined with Dasatinib.Approved, Investigational
DecamethoniumThe therapeutic efficacy of Solifenacin can be decreased when used in combination with Decamethonium.Approved
Decanoic AcidThe metabolism of Solifenacin can be decreased when combined with Decanoic Acid.Experimental
DeferasiroxThe serum concentration of Solifenacin can be decreased when it is combined with Deferasirox.Approved, Investigational
DelavirdineThe metabolism of Solifenacin can be decreased when combined with Delavirdine.Approved
DemecariumThe therapeutic efficacy of Solifenacin 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 Solifenacin.Approved, Investigational
DexamethasoneThe serum concentration of Solifenacin can be decreased when it is combined with Dexamethasone.Approved, Investigational, Vet Approved
DexetimideThe risk or severity of adverse effects can be increased when Solifenacin is combined with Dexetimide.Withdrawn
DextromoramideThe risk or severity of adverse effects can be increased when Solifenacin is combined with Dextromoramide.Experimental, Illicit
DextropropoxypheneThe risk or severity of adverse effects can be increased when Solifenacin is combined with Dextropropoxyphene.Approved, Illicit, Withdrawn
DezocineThe risk or severity of adverse effects can be increased when Solifenacin is combined with Dezocine.Approved
DichlorvosThe therapeutic efficacy of Solifenacin 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 Solifenacin.Approved
DihydrocodeineThe risk or severity of adverse effects can be increased when Solifenacin is combined with Dihydrocodeine.Approved, Illicit
DihydroergotamineThe metabolism of Solifenacin can be decreased when combined with Dihydroergotamine.Approved
DihydroetorphineThe risk or severity of adverse effects can be increased when Solifenacin is combined with Dihydroetorphine.Experimental, Illicit
DihydromorphineThe risk or severity of adverse effects can be increased when Solifenacin is combined with Dihydromorphine.Experimental, Illicit
DiltiazemThe metabolism of Solifenacin can be decreased when combined with Diltiazem.Approved
DiphenoxylateThe risk or severity of adverse effects can be increased when Solifenacin is combined with Diphenoxylate.Approved, Illicit
DisopyramideSolifenacin may increase the QTc-prolonging activities of Disopyramide.Approved
DofetilideSolifenacin may increase the QTc-prolonging activities of Dofetilide.Approved
DolasetronSolifenacin may increase the QTc-prolonging activities of Dolasetron.Approved
DomperidoneSolifenacin may increase the QTc-prolonging activities of Domperidone.Approved, Investigational, Vet Approved
DonepezilThe therapeutic efficacy of Solifenacin can be decreased when used in combination with Donepezil.Approved
DoxycyclineThe metabolism of Solifenacin can be decreased when combined with Doxycycline.Approved, Investigational, Vet Approved
DPDPEThe risk or severity of adverse effects can be increased when Solifenacin is combined with DPDPE.Investigational
DronabinolSolifenacin may increase the tachycardic activities of Dronabinol.Approved, Illicit
DronedaroneSolifenacin may increase the QTc-prolonging activities of Dronedarone.Approved
DroperidolSolifenacin may increase the QTc-prolonging activities of Droperidol.Approved, Vet Approved
EchothiophateThe therapeutic efficacy of Solifenacin can be decreased when used in combination with Echothiophate.Approved
EconazoleThe metabolism of Solifenacin can be decreased when combined with Econazole.Approved
EdrophoniumThe therapeutic efficacy of Solifenacin can be decreased when used in combination with Edrophonium.Approved
EfavirenzThe serum concentration of Solifenacin can be decreased when it is combined with Efavirenz.Approved, Investigational
EfinaconazoleThe metabolism of Solifenacin can be decreased when combined with Efinaconazole.Approved
EliglustatSolifenacin may increase the QTc-prolonging activities of Eliglustat.Approved
EluxadolineSolifenacin may increase the constipating activities of Eluxadoline.Approved
EnzalutamideThe serum concentration of Solifenacin can be decreased when it is combined with Enzalutamide.Approved
ErythromycinSolifenacin may increase the QTc-prolonging activities of Erythromycin.Approved, Vet Approved
EscitalopramSolifenacin may increase the QTc-prolonging activities of Escitalopram.Approved, Investigational
Eslicarbazepine acetateThe serum concentration of Solifenacin can be decreased when it is combined with Eslicarbazepine acetate.Approved
EthopropazineThe risk or severity of adverse effects can be increased when Ethopropazine is combined with Solifenacin.Approved
EthylmorphineThe risk or severity of adverse effects can be increased when Solifenacin is combined with Ethylmorphine.Approved, Illicit
EtorphineThe risk or severity of adverse effects can be increased when Solifenacin is combined with Etorphine.Illicit, Vet Approved
EtravirineThe serum concentration of Solifenacin can be decreased when it is combined with Etravirine.Approved
FentanylThe risk or severity of adverse effects can be increased when Solifenacin is combined with Fentanyl.Approved, Illicit, Investigational, Vet Approved
FenthionThe therapeutic efficacy of Solifenacin can be decreased when used in combination with Fenthion.Vet Approved
FesoterodineThe risk or severity of adverse effects can be increased when Solifenacin is combined with Fesoterodine.Approved
FlecainideSolifenacin may increase the QTc-prolonging activities of Flecainide.Approved, Withdrawn
FluconazoleThe metabolism of Solifenacin can be decreased when combined with Fluconazole.Approved
FlucytosineThe metabolism of Solifenacin can be decreased when combined with Flucytosine.Approved
FluoxetineSolifenacin may increase the QTc-prolonging activities of Fluoxetine.Approved, Vet Approved
FlupentixolSolifenacin may increase the QTc-prolonging activities of Flupentixol.Approved, Withdrawn
FluvoxamineThe metabolism of Solifenacin can be decreased when combined with Fluvoxamine.Approved, Investigational
FosamprenavirThe metabolism of Solifenacin can be decreased when combined with Fosamprenavir.Approved
FosaprepitantThe serum concentration of Solifenacin can be increased when it is combined with Fosaprepitant.Approved
FosphenytoinThe metabolism of Solifenacin can be increased when combined with Fosphenytoin.Approved
Fusidic AcidThe serum concentration of Solifenacin can be increased when it is combined with Fusidic Acid.Approved
Gadobenic acidSolifenacin may increase the QTc-prolonging activities of Gadobenic acid.Approved
GalantamineThe therapeutic efficacy of Solifenacin can be decreased when used in combination with Galantamine.Approved
Gallamine TriethiodideThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Solifenacin.Approved
GemifloxacinSolifenacin may increase the QTc-prolonging activities of Gemifloxacin.Approved, Investigational
Ginkgo bilobaThe therapeutic efficacy of Solifenacin can be decreased when used in combination with Ginkgo biloba.Approved, Nutraceutical
Glucagon recombinantThe risk or severity of adverse effects can be increased when Solifenacin is combined with Glucagon recombinant.Approved
GlycopyrroniumSolifenacin may increase the anticholinergic activities of Glycopyrronium.Approved, Investigational, Vet Approved
GlyphosateThe metabolism of Solifenacin can be decreased when combined with Glyphosate.Experimental
GoserelinSolifenacin may increase the QTc-prolonging activities of Goserelin.Approved
GranisetronSolifenacin may increase the QTc-prolonging activities of Granisetron.Approved, Investigational
GriseofulvinThe metabolism of Solifenacin can be decreased when combined with Griseofulvin.Approved, Vet Approved
HaloperidolSolifenacin may increase the QTc-prolonging activities of Haloperidol.Approved
HaloproginThe metabolism of Solifenacin can be decreased when combined with Haloprogin.Approved, Withdrawn
HeroinThe risk or severity of adverse effects can be increased when Solifenacin is combined with Heroin.Approved, Illicit
HexamethoniumThe risk or severity of adverse effects can be increased when Solifenacin is combined with Hexamethonium.Experimental
HexetidineThe metabolism of Solifenacin can be decreased when combined with Hexetidine.Approved
HomatropineThe risk or severity of adverse effects can be increased when Solifenacin is combined with Homatropine.Approved
Huperzine AThe therapeutic efficacy of Solifenacin can be decreased when used in combination with Huperzine A.Investigational
HydrochlorothiazideThe serum concentration of Hydrochlorothiazide can be increased when it is combined with Solifenacin.Approved, Vet Approved
HydrocodoneThe risk or severity of adverse effects can be increased when Solifenacin is combined with Hydrocodone.Approved, Illicit
HydroflumethiazideThe serum concentration of Hydroflumethiazide can be increased when it is combined with Solifenacin.Approved
HydromorphoneThe risk or severity of adverse effects can be increased when Solifenacin is combined with Hydromorphone.Approved, Illicit
HyoscyamineThe risk or severity of adverse effects can be increased when Hyoscyamine is combined with Solifenacin.Approved
IbutilideSolifenacin may increase the QTc-prolonging activities of Ibutilide.Approved
IdelalisibThe serum concentration of Solifenacin can be increased when it is combined with Idelalisib.Approved
IloperidoneSolifenacin may increase the QTc-prolonging activities of Iloperidone.Approved
ImatinibThe metabolism of Solifenacin can be decreased when combined with Imatinib.Approved
IndapamideThe serum concentration of Indapamide can be increased when it is combined with Solifenacin.Approved
IndinavirThe metabolism of Solifenacin can be decreased when combined with Indinavir.Approved
Ipratropium bromideThe risk or severity of adverse effects can be increased when Ipratropium bromide is combined with Solifenacin.Approved
IsavuconazoniumThe metabolism of Solifenacin can be decreased when combined with Isavuconazonium.Approved, Investigational
IsoconazoleThe metabolism of Solifenacin can be decreased when combined with Isoconazole.Approved
IsoflurophateThe therapeutic efficacy of Solifenacin can be decreased when used in combination with Isoflurophate.Approved, Withdrawn
IsradipineThe metabolism of Solifenacin can be decreased when combined with Isradipine.Approved
ItoprideThe therapeutic efficacy of Itopride can be decreased when used in combination with Solifenacin.Investigational
ItraconazoleThe metabolism of Solifenacin can be decreased when combined with Itraconazole.Approved, Investigational
IvacaftorThe serum concentration of Solifenacin can be increased when it is combined with Ivacaftor.Approved
KetobemidoneThe risk or severity of adverse effects can be increased when Solifenacin is combined with Ketobemidone.Approved
KetoconazoleThe metabolism of Solifenacin can be decreased when combined with Ketoconazole.Approved, Investigational
LenvatinibSolifenacin may increase the QTc-prolonging activities of Lenvatinib.Approved
LeuprolideSolifenacin may increase the QTc-prolonging activities of Leuprolide.Approved, Investigational
LevofloxacinSolifenacin may increase the QTc-prolonging activities of Levofloxacin.Approved, Investigational
Levomethadyl AcetateThe risk or severity of adverse effects can be increased when Solifenacin is combined with Levomethadyl Acetate.Approved
LevorphanolThe risk or severity of adverse effects can be increased when Solifenacin is combined with Levorphanol.Approved
LofentanilThe risk or severity of adverse effects can be increased when Solifenacin is combined with Lofentanil.Illicit
LopinavirThe metabolism of Solifenacin can be decreased when combined with Lopinavir.Approved
LovastatinThe metabolism of Solifenacin can be decreased when combined with Lovastatin.Approved, Investigational
LuliconazoleThe serum concentration of Solifenacin can be increased when it is combined with Luliconazole.Approved
LumacaftorThe metabolism of Solifenacin can be increased when combined with Lumacaftor.Approved
LumefantrineSolifenacin may increase the QTc-prolonging activities of Lumefantrine.Approved
MalathionThe therapeutic efficacy of Solifenacin can be decreased when used in combination with Malathion.Approved, Investigational
MecamylamineThe risk or severity of adverse effects can be increased when Mecamylamine is combined with Solifenacin.Approved
MefloquineThe therapeutic efficacy of Solifenacin can be decreased when used in combination with Mefloquine.Approved
MemantineThe therapeutic efficacy of Solifenacin can be decreased when used in combination with Memantine.Approved, Investigational
MethadoneSolifenacin may increase the QTc-prolonging activities of Methadone.Approved
Methadyl AcetateThe risk or severity of adverse effects can be increased when Solifenacin is combined with Methadyl Acetate.Approved, Illicit
Methanesulfonyl FluorideThe therapeutic efficacy of Solifenacin 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 Solifenacin.Approved
MethyclothiazideThe serum concentration of Methyclothiazide can be increased when it is combined with Solifenacin.Approved
MetixeneThe risk or severity of adverse effects can be increased when Solifenacin is combined with Metixene.Approved
MetolazoneThe serum concentration of Metolazone can be increased when it is combined with Solifenacin.Approved
MevastatinThe metabolism of Solifenacin can be decreased when combined with Mevastatin.Experimental
MianserinMianserin may increase the anticholinergic activities of Solifenacin.Approved
MicafunginThe metabolism of Solifenacin can be decreased when combined with Micafungin.Approved, Investigational
MiconazoleThe metabolism of Solifenacin can be decreased when combined with Miconazole.Approved, Investigational, Vet Approved
MifepristoneMifepristone may increase the QTc-prolonging activities of Solifenacin.Approved, Investigational
MiltefosineThe metabolism of Solifenacin can be decreased when combined with Miltefosine.Approved
MinaprineThe therapeutic efficacy of Solifenacin can be decreased when used in combination with Minaprine.Approved
MirabegronThe risk or severity of adverse effects can be increased when Mirabegron is combined with Solifenacin.Approved
MitotaneThe serum concentration of Solifenacin can be decreased when it is combined with Mitotane.Approved
ModafinilThe serum concentration of Solifenacin can be decreased when it is combined with Modafinil.Approved, Investigational
MonensinThe metabolism of Solifenacin can be decreased when combined with Monensin.Vet Approved
MorphineThe risk or severity of adverse effects can be increased when Solifenacin is combined with Morphine.Approved, Investigational
MoxifloxacinSolifenacin may increase the QTc-prolonging activities of Moxifloxacin.Approved, Investigational
MyxothiazolThe metabolism of Solifenacin can be decreased when combined with Myxothiazol.Experimental
N-butylscopolammonium bromideThe risk or severity of adverse effects can be increased when Solifenacin is combined with N-butylscopolammonium bromide.Vet Approved
NabiloneSolifenacin may increase the tachycardic activities of Nabilone.Approved, Investigational
NafcillinThe serum concentration of Solifenacin can be decreased when it is combined with Nafcillin.Approved
NaftifineThe metabolism of Solifenacin can be decreased when combined with Naftifine.Approved
NalbuphineThe risk or severity of adverse effects can be increased when Solifenacin is combined with Nalbuphine.Approved
NatamycinThe metabolism of Solifenacin can be decreased when combined with Natamycin.Approved
NefazodoneThe metabolism of Solifenacin can be decreased when combined with Nefazodone.Approved, Withdrawn
NelfinavirThe metabolism of Solifenacin can be decreased when combined with Nelfinavir.Approved
NeostigmineThe therapeutic efficacy of Solifenacin can be decreased when used in combination with Neostigmine.Approved, Vet Approved
NetupitantThe serum concentration of Solifenacin can be increased when it is combined with Netupitant.Approved
NevirapineThe metabolism of Solifenacin can be increased when combined with Nevirapine.Approved
NilotinibSolifenacin may increase the QTc-prolonging activities of Nilotinib.Approved, Investigational
NitroxolineThe metabolism of Solifenacin can be decreased when combined with Nitroxoline.Approved
NormethadoneThe risk or severity of adverse effects can be increased when Solifenacin is combined with Normethadone.Approved, Illicit
NVA237The risk or severity of adverse effects can be increased when Solifenacin is combined with NVA237.Investigational
NystatinThe metabolism of Solifenacin can be decreased when combined with Nystatin.Approved, Vet Approved
OfloxacinSolifenacin may increase the QTc-prolonging activities of Ofloxacin.Approved
OlaparibThe metabolism of Solifenacin can be decreased when combined with Olaparib.Approved
OndansetronSolifenacin may increase the QTc-prolonging activities of Ondansetron.Approved
OpiumThe risk or severity of adverse effects can be increased when Solifenacin is combined with Opium.Approved, Illicit
OrphenadrineThe risk or severity of adverse effects can be increased when Orphenadrine is combined with Solifenacin.Approved
OsimertinibThe serum concentration of Solifenacin can be increased when it is combined with Osimertinib.Approved
OxiconazoleThe metabolism of Solifenacin can be decreased when combined with Oxiconazole.Approved
OxybutyninThe risk or severity of adverse effects can be increased when Oxybutynin is combined with Solifenacin.Approved, Investigational
OxycodoneThe risk or severity of adverse effects can be increased when Solifenacin is combined with Oxycodone.Approved, Illicit, Investigational
OxymorphoneThe risk or severity of adverse effects can be increased when Solifenacin is combined with Oxymorphone.Approved, Investigational, Vet Approved
OxyphenoniumThe risk or severity of adverse effects can be increased when Oxyphenonium is combined with Solifenacin.Approved
pafuramidineThe metabolism of Solifenacin can be decreased when combined with pafuramidine.Investigational
PalbociclibThe serum concentration of Solifenacin can be increased when it is combined with Palbociclib.Approved
PaliperidoneSolifenacin may increase the QTc-prolonging activities of Paliperidone.Approved
PancuroniumThe risk or severity of adverse effects can be increased when Pancuronium is combined with Solifenacin.Approved
PanobinostatSolifenacin may increase the QTc-prolonging activities of Panobinostat.Approved, Investigational
PazopanibSolifenacin may increase the QTc-prolonging activities of Pazopanib.Approved
PentamidineThe metabolism of Solifenacin can be decreased when combined with Pentamidine.Approved
PentazocineThe risk or severity of adverse effects can be increased when Solifenacin is combined with Pentazocine.Approved, Vet Approved
PentobarbitalThe metabolism of Solifenacin can be increased when combined with Pentobarbital.Approved, Vet Approved
PentoliniumThe risk or severity of adverse effects can be increased when Pentolinium is combined with Solifenacin.Approved
PerflutrenSolifenacin may increase the QTc-prolonging activities of Perflutren.Approved
PethidineThe risk or severity of adverse effects can be increased when Solifenacin is combined with Pethidine.Approved
PhenobarbitalThe metabolism of Solifenacin can be increased when combined with Phenobarbital.Approved
PhenytoinThe metabolism of Solifenacin can be increased when combined with Phenytoin.Approved, Vet Approved
PhysostigmineThe therapeutic efficacy of Solifenacin can be decreased when used in combination with Physostigmine.Approved
PimozideSolifenacin may increase the QTc-prolonging activities of Pimozide.Approved
PipecuroniumThe risk or severity of adverse effects can be increased when Pipecuronium is combined with Solifenacin.Approved
PirenzepineThe risk or severity of adverse effects can be increased when Pirenzepine is combined with Solifenacin.Approved
PiritramideThe risk or severity of adverse effects can be increased when Solifenacin is combined with Piritramide.Investigational
PolythiazideThe serum concentration of Polythiazide can be increased when it is combined with Solifenacin.Approved
PosaconazoleThe metabolism of Solifenacin can be decreased when combined with Posaconazole.Approved, Investigational, Vet Approved
Potassium ChlorideSolifenacin may increase the ulcerogenic activities of Potassium Chloride.Approved, Withdrawn
PramlintidePramlintide may increase the anticholinergic activities of Solifenacin.Approved, Investigational
PrimaquineSolifenacin may increase the QTc-prolonging activities of Primaquine.Approved
PrimidoneThe metabolism of Solifenacin can be increased when combined with Primidone.Approved, Vet Approved
ProcainamideSolifenacin may increase the QTc-prolonging activities of Procainamide.Approved
ProcyclidineThe risk or severity of adverse effects can be increased when Procyclidine is combined with Solifenacin.Approved
PromazineSolifenacin may increase the QTc-prolonging activities of Promazine.Approved, Vet Approved
PropafenoneSolifenacin may increase the QTc-prolonging activities of Propafenone.Approved
PropanthelineThe risk or severity of adverse effects can be increased when Propantheline is combined with Solifenacin.Approved
PropiverineThe risk or severity of adverse effects can be increased when Solifenacin is combined with Propiverine.Investigational
PyridostigmineThe therapeutic efficacy of Solifenacin can be decreased when used in combination with Pyridostigmine.Approved
QuetiapineSolifenacin may increase the QTc-prolonging activities of Quetiapine.Approved
QuinethazoneThe serum concentration of Quinethazone can be increased when it is combined with Solifenacin.Approved
QuinidineSolifenacin may increase the QTc-prolonging activities of Quinidine.Approved
QuinineSolifenacin may increase the QTc-prolonging activities of Quinine.Approved
RadicicolThe metabolism of Solifenacin can be decreased when combined with Radicicol.Experimental
RamosetronSolifenacin may increase the constipating activities of Ramosetron.Approved
RanolazineThe metabolism of Solifenacin can be decreased when combined with Ranolazine.Approved, Investigational
RemifentanilThe risk or severity of adverse effects can be increased when Solifenacin is combined with Remifentanil.Approved
RifabutinThe metabolism of Solifenacin can be increased when combined with Rifabutin.Approved
RifampicinThe metabolism of Solifenacin can be increased when combined with Rifampicin.Approved
RifapentineThe metabolism of Solifenacin can be increased when combined with Rifapentine.Approved
RitonavirThe metabolism of Solifenacin can be decreased when combined with Ritonavir.Approved, Investigational
RivastigmineThe therapeutic efficacy of Solifenacin can be decreased when used in combination with Rivastigmine.Approved, Investigational
Salicylhydroxamic AcidThe metabolism of Solifenacin can be decreased when combined with Salicylhydroxamic Acid.Experimental
Salicylic acidThe metabolism of Solifenacin can be decreased when combined with Salicylic acid.Approved, Vet Approved
SaquinavirThe metabolism of Solifenacin can be decreased when combined with Saquinavir.Approved, Investigational
ScopolamineThe risk or severity of adverse effects can be increased when Scopolamine is combined with Solifenacin.Approved
Scopolamine butylbromideThe risk or severity of adverse effects can be increased when Solifenacin is combined with Scopolamine butylbromide.Approved
SecretinThe therapeutic efficacy of Secretin can be decreased when used in combination with Solifenacin.Approved, Investigational
SertaconazoleThe metabolism of Solifenacin can be decreased when combined with Sertaconazole.Approved
SildenafilThe metabolism of Solifenacin can be decreased when combined with Sildenafil.Approved, Investigational
SiltuximabThe serum concentration of Solifenacin can be decreased when it is combined with Siltuximab.Approved
SimeprevirThe serum concentration of Solifenacin can be increased when it is combined with Simeprevir.Approved
SinefunginThe metabolism of Solifenacin can be decreased when combined with Sinefungin.Experimental
SirolimusThe metabolism of Solifenacin can be decreased when combined with Sirolimus.Approved, Investigational
SotalolSolifenacin may increase the QTc-prolonging activities of Sotalol.Approved
St. John's WortThe serum concentration of Solifenacin can be decreased when it is combined with St. John's Wort.Nutraceutical
StiripentolThe serum concentration of Solifenacin can be increased when it is combined with Stiripentol.Approved
SufentanilThe risk or severity of adverse effects can be increased when Solifenacin is combined with Sufentanil.Approved, Investigational
SulconazoleThe metabolism of Solifenacin can be decreased when combined with Sulconazole.Approved
SulfisoxazoleSolifenacin may increase the QTc-prolonging activities of Sulfisoxazole.Approved, Vet Approved
SulpirideThe therapeutic efficacy of Sulpiride can be decreased when used in combination with Solifenacin.Approved
TacrineThe therapeutic efficacy of Solifenacin can be decreased when used in combination with Tacrine.Withdrawn
TapentadolThe risk or severity of adverse effects can be increased when Solifenacin is combined with Tapentadol.Approved
TavaboroleThe metabolism of Solifenacin can be decreased when combined with Tavaborole.Approved
TelaprevirThe metabolism of Solifenacin can be decreased when combined with Telaprevir.Approved
TelavancinSolifenacin may increase the QTc-prolonging activities of Telavancin.Approved
TelithromycinThe metabolism of Solifenacin can be decreased when combined with Telithromycin.Approved
TerbinafineThe metabolism of Solifenacin can be decreased when combined with Terbinafine.Approved, Investigational, Vet Approved
TerconazoleThe metabolism of Solifenacin can be decreased when combined with Terconazole.Approved
TetrabenazineSolifenacin may increase the QTc-prolonging activities of Tetrabenazine.Approved
ThioridazineSolifenacin may increase the QTc-prolonging activities of Thioridazine.Approved
ThymolThe metabolism of Solifenacin can be decreased when combined with Thymol.Approved
TiclopidineThe metabolism of Solifenacin can be decreased when combined with Ticlopidine.Approved
TioconazoleThe metabolism of Solifenacin can be decreased when combined with Tioconazole.Approved
TiotropiumSolifenacin may increase the anticholinergic activities of Tiotropium.Approved
TocilizumabThe serum concentration of Solifenacin can be decreased when it is combined with Tocilizumab.Approved
TolnaftateThe metabolism of Solifenacin can be decreased when combined with Tolnaftate.Approved, Vet Approved
TolterodineThe risk or severity of adverse effects can be increased when Tolterodine is combined with Solifenacin.Approved, Investigational
TopiramateThe risk or severity of adverse effects can be increased when Solifenacin is combined with Topiramate.Approved
ToremifeneSolifenacin may increase the QTc-prolonging activities of Toremifene.Approved, Investigational
TramadolThe risk or severity of adverse effects can be increased when Solifenacin is combined with Tramadol.Approved, Investigational
TrichlorfonThe therapeutic efficacy of Solifenacin can be decreased when used in combination with Trichlorfon.Vet Approved
TrichlormethiazideThe serum concentration of Trichlormethiazide can be increased when it is combined with Solifenacin.Approved, Vet Approved
TrihexyphenidylThe risk or severity of adverse effects can be increased when Trihexyphenidyl is combined with Solifenacin.Approved
TrimethaphanThe risk or severity of adverse effects can be increased when Trimethaphan is combined with Solifenacin.Approved
TrimetrexateThe metabolism of Solifenacin can be decreased when combined with Trimetrexate.Approved, Investigational
TropicamideThe risk or severity of adverse effects can be increased when Tropicamide is combined with Solifenacin.Approved
TrospiumThe risk or severity of adverse effects can be increased when Trospium is combined with Solifenacin.Approved
TubocurarineThe risk or severity of adverse effects can be increased when Tubocurarine is combined with Solifenacin.Approved
UmeclidiniumUmeclidinium may increase the anticholinergic activities of Solifenacin.Approved
VandetanibSolifenacin may increase the QTc-prolonging activities of Vandetanib.Approved
VecuroniumThe risk or severity of adverse effects can be increased when Vecuronium is combined with Solifenacin.Approved
VemurafenibSolifenacin may increase the QTc-prolonging activities of Vemurafenib.Approved
VenlafaxineThe metabolism of Solifenacin can be decreased when combined with Venlafaxine.Approved
VerapamilThe metabolism of Solifenacin can be decreased when combined with Verapamil.Approved
VoriconazoleThe metabolism of Solifenacin can be decreased when combined with Voriconazole.Approved, Investigational
ZiprasidoneSolifenacin may increase the QTc-prolonging activities of Ziprasidone.Approved
ZuclopenthixolSolifenacin may increase the QTc-prolonging activities of Zuclopenthixol.Approved, Investigational
Food InteractionsNot Available
References
Synthesis Reference

Katsumi Saito, Masataka Katsuma, “Solifenacin transdermal preparation and method for enhancing transdermal permeation thereof.” U.S. Patent US20050181031, issued August 18, 2005.

US20050181031
General ReferencesNot Available
External Links
ATC CodesG04BD08G04CA53
AHFS Codes
  • 86:12.00
PDB EntriesNot Available
FDA labelDownload (68.6 KB)
MSDSNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9706
Blood Brain Barrier+0.6159
Caco-2 permeable-0.6679
P-glycoprotein substrateSubstrate0.7801
P-glycoprotein inhibitor IInhibitor0.8572
P-glycoprotein inhibitor IIInhibitor0.8611
Renal organic cation transporterNon-inhibitor0.7498
CYP450 2C9 substrateNon-substrate0.8311
CYP450 2D6 substrateNon-substrate0.7264
CYP450 3A4 substrateSubstrate0.545
CYP450 1A2 substrateNon-inhibitor0.8445
CYP450 2C9 inhibitorNon-inhibitor0.8755
CYP450 2D6 inhibitorNon-inhibitor0.8593
CYP450 2C19 inhibitorNon-inhibitor0.7037
CYP450 3A4 inhibitorNon-inhibitor0.7027
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.8748
Ames testNon AMES toxic0.8871
CarcinogenicityNon-carcinogens0.9596
BiodegradationNot ready biodegradable0.9828
Rat acute toxicity2.3839 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.8115
hERG inhibition (predictor II)Inhibitor0.727
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
ManufacturersNot Available
Packagers
Dosage forms
FormRouteStrength
TabletOral10 mg
TabletOral5 mg
Tablet, film coatedOral10 mg/1
Tablet, film coatedOral5 mg/1
Prices
Unit descriptionCostUnit
Fer-In-Sol 75 (15 Fe)mg/ml Solution 50ml Bottle19.0USD bottle
Fergon 100 240 (27 Fe)mg tablet Bottle15.99USD bottle
Fortabs 50-325-40 mg tablet0.4USD tablet
Hemocyte tablet0.33USD tablet
Hemocyte-f tablet0.33USD tablet
Feosol 45 mg tablet0.31USD tablet
Slow fe 142 mg tablet0.27USD tablet
Ferrous fumarate 324 mg tablet0.21USD tablet
Fer-in-sol 15 mg/ml drops0.19USD ml
Feosol 65 mg tablet0.18USD tablet
Ferretts 325 mg tablet0.14USD tablet
Fergon 27 mg tablet0.05USD tablet
Ferretts ips liquid0.05USD ml
Ferrous gluc 246 mg (27 mg) tablet0.04USD tablet
Ferrous gluconate 27 mg tablet0.04USD tablet
Ferrous sulfate 28 mg tablet0.04USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
CA2208839 No2006-01-312015-12-27Canada
US6017927 No1998-11-192018-11-19Us
Properties
StateSolid
Experimental PropertiesNot Available
Predicted Properties
PropertyValueSource
Water Solubility0.0729 mg/mLALOGPS
logP3.9ALOGPS
logP3.96ChemAxon
logS-3.7ALOGPS
pKa (Strongest Basic)8.88ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count2ChemAxon
Hydrogen Donor Count0ChemAxon
Polar Surface Area32.78 Å2ChemAxon
Rotatable Bond Count3ChemAxon
Refractivity106.06 m3·mol-1ChemAxon
Polarizability40.13 Å3ChemAxon
Number of Rings5ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
SpectraNot Available
Taxonomy
ClassificationNot classified

Targets

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 action of G proteins. Primary transducing effect is Pi turnover.
Gene Name:
CHRM3
Uniprot ID:
P20309
Molecular Weight:
66127.445 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284 ]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423 ]
  3. Ito Y, Oyunzul L, Yoshida A, Fujino T, Noguchi Y, Yuyama H, Ohtake A, Suzuki M, Sasamata M, Matsui M, Yamada S: Comparison of muscarinic receptor selectivity of solifenacin and oxybutynin in the bladder and submandibular gland of muscarinic receptor knockout mice. Eur J Pharmacol. 2009 Aug 1;615(1-3):201-6. doi: 10.1016/j.ejphar.2009.04.068. Epub 2009 May 13. [PubMed:19446545 ]
  4. Sinha S, Gupta S, Malhotra S, Krishna NS, Meru AV, Babu V, Bansal V, Garg M, Kumar N, Chugh A, Ray A: AE9C90CB: a novel, bladder-selective muscarinic receptor antagonist for the treatment of overactive bladder. Br J Pharmacol. 2010 Jul;160(5):1119-27. doi: 10.1111/j.1476-5381.2010.00752.x. [PubMed:20590605 ]
  5. Mansfield KJ, Chandran JJ, Vaux KJ, Millard RJ, Christopoulos A, Mitchelson FJ, Burcher E: Comparison of receptor binding characteristics of commonly used muscarinic antagonists in human bladder detrusor and mucosa. J Pharmacol Exp Ther. 2009 Mar;328(3):893-9. doi: 10.1124/jpet.108.145508. Epub 2008 Nov 24. [PubMed:19029429 ]
  6. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
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 action of G proteins. Primary transducing effect is Pi turnover.
Gene Name:
CHRM1
Uniprot ID:
P11229
Molecular Weight:
51420.375 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284 ]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423 ]
  3. Sinha S, Gupta S, Malhotra S, Krishna NS, Meru AV, Babu V, Bansal V, Garg M, Kumar N, Chugh A, Ray A: AE9C90CB: a novel, bladder-selective muscarinic receptor antagonist for the treatment of overactive bladder. Br J Pharmacol. 2010 Jul;160(5):1119-27. doi: 10.1111/j.1476-5381.2010.00752.x. [PubMed:20590605 ]
  4. Mansfield KJ, Chandran JJ, Vaux KJ, Millard RJ, Christopoulos A, Mitchelson FJ, Burcher E: Comparison of receptor binding characteristics of commonly used muscarinic antagonists in human bladder detrusor and mucosa. J Pharmacol Exp Ther. 2009 Mar;328(3):893-9. doi: 10.1124/jpet.108.145508. Epub 2008 Nov 24. [PubMed:19029429 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
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 action of G proteins. Primary transducing effect is adenylate cyclase inhibition. Signaling promotes phospholipase C activity, leading to the release of inositol trisphosphate (IP3); this then trigge...
Gene Name:
CHRM2
Uniprot ID:
P08172
Molecular Weight:
51714.605 Da
References
  1. Sinha S, Gupta S, Malhotra S, Krishna NS, Meru AV, Babu V, Bansal V, Garg M, Kumar N, Chugh A, Ray A: AE9C90CB: a novel, bladder-selective muscarinic receptor antagonist for the treatment of overactive bladder. Br J Pharmacol. 2010 Jul;160(5):1119-27. doi: 10.1111/j.1476-5381.2010.00752.x. [PubMed:20590605 ]
  2. Mansfield KJ, Chandran JJ, Vaux KJ, Millard RJ, Christopoulos A, Mitchelson FJ, Burcher E: Comparison of receptor binding characteristics of commonly used muscarinic antagonists in human bladder detrusor and mucosa. J Pharmacol Exp Ther. 2009 Mar;328(3):893-9. doi: 10.1124/jpet.108.145508. Epub 2008 Nov 24. [PubMed:19029429 ]
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 action of G proteins. Primary transducing effect is inhibition of adenylate cyclase.
Gene Name:
CHRM4
Uniprot ID:
P08173
Molecular Weight:
53048.65 Da
References
  1. Mansfield KJ, Chandran JJ, Vaux KJ, Millard RJ, Christopoulos A, Mitchelson FJ, Burcher E: Comparison of receptor binding characteristics of commonly used muscarinic antagonists in human bladder detrusor and mucosa. J Pharmacol Exp Ther. 2009 Mar;328(3):893-9. doi: 10.1124/jpet.108.145508. Epub 2008 Nov 24. [PubMed:19029429 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
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 action of G proteins. Primary transducing effect is Pi turnover.
Gene Name:
CHRM5
Uniprot ID:
P08912
Molecular Weight:
60073.205 Da
References
  1. Mansfield KJ, Chandran JJ, Vaux KJ, Millard RJ, Christopoulos A, Mitchelson FJ, Burcher E: Comparison of receptor binding characteristics of commonly used muscarinic antagonists in human bladder detrusor and mucosa. J Pharmacol Exp Ther. 2009 Mar;328(3):893-9. doi: 10.1124/jpet.108.145508. Epub 2008 Nov 24. [PubMed:19029429 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
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 reactions (e.g. caffeine 8-oxidation, omeprazole sulphoxidation, midazolam 1'-hydroxylation and midazolam 4-hydroxylation) of structurally unrelated compounds, including steroids, fatty acids, and xenobiot...
Gene Name:
CYP3A4
Uniprot ID:
P08684
Molecular Weight:
57342.67 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
Comments
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Drug created on June 13, 2005 07:24 / Updated on December 08, 2016 11:48