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Identification
NameTolterodine
Accession NumberDB01036  (APRD00146)
TypeSmall Molecule
GroupsApproved, Investigational
DescriptionTolterodine is an antimuscarinic drug that is used to treat urinary incontinence. Tolterodine acts on M2 and M3 subtypes of muscarinic receptors.
Structure
Thumb
Synonyms
(+)-(R)-2-(alpha-(2-(Diisopropylamino)ethyl)benzyl)-p-cresol
(+)-Tolterodine
Tolterodina
Tolterodine
Tolterodinum
External Identifiers Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
DetrolTablet, film coated1 mg/1OralPharmacia and Upjohn Company1998-03-25Not applicableUs
DetrolTablet, film coated2 mg/1OralPharmacia and Upjohn Company1998-03-25Not applicableUs
DetrolTablet1 mgOralPfizer Canada Inc1998-11-26Not applicableCanada
DetrolTablet, film coated2 mg/1OralSTAT Rx USA LLC1998-03-25Not applicableUs
DetrolTablet2 mgOralPfizer Canada Inc1998-11-23Not applicableCanada
Detrol LACapsule, extended release4 mg/1OralLake Erie Medical & Surgical Supply DBA Quality Care Products LLC2012-02-28Not applicableUs
Detrol LACapsule, extended release2 mg/1OralCardinal Health2000-12-22Not applicableUs
Detrol LACapsule, extended release2 mgOralPfizer Canada Inc2002-03-26Not applicableCanada
Detrol LACapsule, extended release4 mg/1OralPhysicians Total Care, Inc.2004-09-03Not applicableUs
Detrol LACapsule, extended release4 mg/1OralPd Rx Pharmaceuticals, Inc.2000-02-22Not applicableUs
Detrol LACapsule, extended release4 mgOralPfizer Canada Inc2002-03-26Not applicableCanada
Detrol LACapsule, extended release2 mg/1OralPhysicians Total Care, Inc.2004-09-03Not applicableUs
Detrol LACapsule, extended release2 mg/1OralPharmacia and Upjohn Company2000-02-22Not applicableUs
Detrol LACapsule, extended release4 mg/1OralCardinal Health2000-12-22Not applicableUs
Detrol LACapsule, extended release4 mg/1OralPharmacia and Upjohn Company2000-02-22Not applicableUs
Gd-tolterodineTablet2 mgOralGenmed A Division Of Pfizer Canada IncNot applicableNot applicableCanada
Gd-tolterodineTablet1 mgOralGenmed A Division Of Pfizer Canada IncNot applicableNot applicableCanada
Gd-tolterodine LACapsule, extended release4 mgOralGenmed A Division Of Pfizer Canada IncNot applicableNot applicableCanada
Gd-tolterodine LACapsule, extended release2 mgOralGenmed A Division Of Pfizer Canada IncNot applicableNot applicableCanada
Mint-tolterodineTablet2 mgOralMint Pharmaceuticals Inc2015-12-16Not applicableCanada
Mint-tolterodineTablet1 mgOralMint Pharmaceuticals Inc2015-12-16Not applicableCanada
Mylan-tolterodine ERCapsule, extended release2 mgOralMylan Pharmaceuticals Ulc2015-10-23Not applicableCanada
Mylan-tolterodine ERCapsule, extended release4 mgOralMylan Pharmaceuticals Ulc2015-10-23Not applicableCanada
Ran-tolterodineTablet2 mgOralRanbaxy Pharmaceuticals Canada Inc.Not applicableNot applicableCanada
Ran-tolterodineTablet1 mgOralRanbaxy Pharmaceuticals Canada Inc.Not applicableNot applicableCanada
Sandoz Tolterodine LACapsule, extended release2 mgOralSandoz Canada Incorporated2015-12-16Not applicableCanada
Sandoz Tolterodine LACapsule, extended release4 mgOralSandoz Canada Incorporated2015-12-16Not applicableCanada
Teva-tolterodineTablet2 mgOralTeva Canada Limited2015-12-16Not applicableCanada
Teva-tolterodineTablet1 mgOralTeva Canada Limited2015-12-16Not applicableCanada
Teva-tolterodine LACapsule, extended release2 mgOralTeva Canada Limited2015-12-16Not applicableCanada
Teva-tolterodine LACapsule, extended release4 mgOralTeva Canada Limited2015-12-16Not applicableCanada
Tolterodine TartrateCapsule, extended release4 mg/1OralTeva Pharmaceuticals USA Inc2014-01-02Not applicableUs
Tolterodine TartrateTablet, film coated1 mg/1OralGreenstone LLC2014-01-21Not applicableUs
Tolterodine TartrateCapsule, extended release4 mg/1OralCarilion Materials Management2014-01-02Not applicableUs
Tolterodine TartrateTablet, film coated2 mg/1OralTeva Pharmaceuticals USA Inc2012-05-11Not applicableUs
Tolterodine TartrateCapsule, extended release2 mg/1OralTeva Pharmaceuticals USA Inc2014-01-02Not applicableUs
Tolterodine TartrateTablet, film coated2 mg/1OralGreenstone LLC2014-01-21Not applicableUs
Tolterodine TartrateTablet, film coated1 mg/1OralTeva Pharmaceuticals USA Inc2012-05-11Not applicableUs
Tolterodine TartrateTablet, film coated1 mg/1Oralbryant ranch prepack2012-05-11Not applicableUs
Tolterodine TartrateCapsule, extended release4 mg/1OralCarilion Materials Management2014-01-02Not applicableUs
Tolterodine Tartrate Extended ReleaseCapsule, extended release2 mg/1OralGreenstone LLC2000-02-22Not applicableUs
Tolterodine Tartrate Extended ReleaseCapsule, extended release4 mg/1OralGreenstone LLC2000-02-22Not applicableUs
Approved Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Apo-tolterodineTablet1 mgOralApotex Inc2016-03-03Not applicableCanada
Apo-tolterodineTablet2 mgOralApotex Inc2016-03-03Not applicableCanada
Tolterodine TartrateCapsule, extended release4 mg/1OralMylan Institutional Inc.2014-01-29Not applicableUs
Tolterodine TartrateTablet, film coated1 mg/1OralMylan Pharmaceuticals Inc.2012-11-27Not applicableUs
Tolterodine TartrateTablet, film coated1 mg/1OralTeva Pharmaceuticals USA Inc2015-11-01Not applicableUs
Tolterodine TartrateTablet, film coated1 mg/1OralMacleods Pharmaceuticals Limited2015-10-08Not applicableUs
Tolterodine TartrateTablet, film coated2 mg/1OralMylan Institutional Inc.2013-03-26Not applicableUs
Tolterodine TartrateTablet, film coated2 mg/1OralMylan Pharmaceuticals Inc.2012-11-27Not applicableUs
Tolterodine TartrateTablet, film coated2 mg/1OralTeva Pharmaceuticals USA Inc2015-11-01Not applicableUs
Tolterodine TartrateTablet, film coated2 mg/1OralMacleods Pharmaceuticals Limited2015-10-08Not applicableUs
Tolterodine TartrateTablet, film coated1 mg/1OralApotex Corp.2012-09-25Not applicableUs
Tolterodine TartrateCapsule, extended release2 mg/1OralMajor Pharmaceuticals2015-08-11Not applicableUs
Tolterodine TartrateCapsule, extended release2 mg/1OralTorrent Pharmaceuticals Limited2015-08-11Not applicableUs
Tolterodine TartrateCapsule, extended release2 mg/1OralMylan Pharmaceuticals Inc.2013-10-31Not applicableUs
Tolterodine TartrateCapsule, extended release2 mg/1OralMylan Institutional Inc.2014-01-28Not applicableUs
Tolterodine TartrateTablet, film coated2 mg/1OralApotex Corp.2012-09-25Not applicableUs
Tolterodine TartrateCapsule, extended release4 mg/1OralMajor Pharmaceuticals2015-08-11Not applicableUs
Tolterodine TartrateCapsule, extended release4 mg/1OralTorrent Pharmaceuticals Limited2015-08-11Not applicableUs
Tolterodine TartrateCapsule, extended release4 mg/1OralMylan Pharmaceuticals Inc.2013-10-31Not applicableUs
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
DetrusitolNot Available
Brand mixturesNot Available
Salts
Name/CASStructureProperties
Tolterodine Tartrate
124937-52-6
Thumb
  • InChI Key: TWHNMSJGYKMTRB-KXYUELECSA-N
  • Monoisotopic Mass: 475.257002543
  • Average Mass: 475.5745
DBSALT000467
Categories
UNIIWHE7A56U7K
CAS number124937-51-5
WeightAverage: 325.4876
Monoisotopic: 325.240564619
Chemical FormulaC22H31NO
InChI KeyOOGJQPCLVADCPB-HXUWFJFHSA-N
InChI
InChI=1S/C22H31NO/c1-16(2)23(17(3)4)14-13-20(19-9-7-6-8-10-19)21-15-18(5)11-12-22(21)24/h6-12,15-17,20,24H,13-14H2,1-5H3/t20-/m1/s1
IUPAC Name
2-[(1R)-3-[bis(propan-2-yl)amino]-1-phenylpropyl]-4-methylphenol
SMILES
CC(C)N(CC[[email protected]](C1=CC=CC=C1)C1=C(O)C=CC(C)=C1)C(C)C
Pharmacology
IndicationFor the treatment of overactive bladder (with symptoms of urinary frequency, urgency, or urge incontinence).
Structured Indications
PharmacodynamicsTolterodine is a competitive muscarinic receptor antagonist. Both urinary bladder contraction and salivation are mediated via cholinergic muscarinic receptors. After oral administration, tolterodine is metabolized in the liver, resulting in the formation of the 5-hydroxymethyl derivative, a major pharmacologically active metabolite. The 5-hydroxymethyl metabolite, which exhibits an antimuscarinic activity similar to that of tolterodine, contributes significantly to the therapeutic effect. Both tolterodine and the 5-hydroxymethyl metabolite exhibit a high specificity for muscarinic receptors, since both show negligible activity or affinity for other neurotransmitter receptors and other potential cellular targets, such as calcium channels. Tolterodine has a pronounced effect on bladder function. The main effects of tolterodine are an increase in residual urine, reflecting an incomplete emptying of the bladder, and a decrease in detrusor pressure, consistent with an antimuscarinic action on the lower urinary tract.
Mechanism of actionBoth tolterodine and its active metabolite, 5-hydroxymethyltolterodine, act as competitive antagonists at muscarinic receptors. This antagonism results in inhibition of bladder contraction, decrease in detrusor pressure, and an incomplete emptying of the bladder.
TargetKindPharmacological actionActionsOrganismUniProt ID
Muscarinic acetylcholine receptor M3Proteinyes
antagonist
HumanP20309 details
Muscarinic acetylcholine receptor M2Proteinyes
antagonist
HumanP08172 details
Muscarinic acetylcholine receptor M5Proteinyes
antagonist
HumanP08912 details
Muscarinic acetylcholine receptor M1Proteinyes
antagonist
HumanP11229 details
Muscarinic acetylcholine receptor M4Proteinyes
antagonist
HumanP08173 details
Related Articles
AbsorptionNot Available
Volume of distribution
  • 113 ± 26.7 L
Protein bindingApproximately 96.3%.
Metabolism
SubstrateEnzymesProduct
Tolterodine
N-Dealkylated tolterodineDetails
Tolterodine
5-Hydroxymethyl tolterodineDetails
N-Dealkylated tolterodine
Not Available
N-Dealkylated 5-hydroxymethyl tolterodineDetails
5-Hydroxymethyl tolterodine
Not Available
N-Dealkylated 5-hydroxymethyl tolterodineDetails
5-Hydroxymethyl tolterodine
Not Available
5-Carboxylic acid tolterodineDetails
Route of eliminationFollowing administration of a 5-mg oral dose of 14C-tolterodine solution to healthy volunteers, 77% of radioactivity was recovered in urine and 17% was recovered in feces in 7 days.
Half life1.9-3.7 hours
ClearanceNot Available
ToxicityNot Available
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 Tolterodine can be decreased when used in combination with 1,10-Phenanthroline.Experimental
AbirateroneThe serum concentration of Tolterodine can be increased when it is combined with Abiraterone.Approved
AclidiniumAclidinium may increase the anticholinergic activities of Tolterodine.Approved
AlfentanilThe risk or severity of adverse effects can be increased when Tolterodine is combined with Alfentanil.Approved, Illicit
AlphacetylmethadolThe risk or severity of adverse effects can be increased when Tolterodine is combined with Alphacetylmethadol.Experimental, Illicit
AmbenoniumThe therapeutic efficacy of Tolterodine can be decreased when used in combination with Ambenonium.Approved
AmiodaroneThe serum concentration of Tolterodine can be increased when it is combined with Amiodarone.Approved, Investigational
AnagrelideTolterodine may increase the QTc-prolonging activities of Anagrelide.Approved
Anisotropine MethylbromideThe risk or severity of adverse effects can be increased when Anisotropine Methylbromide is combined with Tolterodine.Approved
AprepitantThe serum concentration of Tolterodine can be increased when it is combined with Aprepitant.Approved, Investigational
ArmodafinilThe metabolism of Tolterodine can be decreased when combined with Armodafinil.Approved, Investigational
Arsenic trioxideTolterodine may increase the QTc-prolonging activities of Arsenic trioxide.Approved, Investigational
ArtemetherTolterodine may increase the QTc-prolonging activities of Artemether.Approved
AsenapineTolterodine may increase the QTc-prolonging activities of Asenapine.Approved
AtazanavirThe serum concentration of Tolterodine can be increased when it is combined with Atazanavir.Approved, Investigational
AtomoxetineThe metabolism of Tolterodine 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 Tolterodine.Approved
AtropineThe risk or severity of adverse effects can be increased when Atropine is combined with Tolterodine.Approved, Vet Approved
AzithromycinTolterodine may increase the QTc-prolonging activities of Azithromycin.Approved
BedaquilineTolterodine may increase the QTc-prolonging activities of Bedaquiline.Approved
BenactyzineThe risk or severity of adverse effects can be increased when Tolterodine is combined with Benactyzine.Withdrawn
BendroflumethiazideThe serum concentration of Bendroflumethiazide can be increased when it is combined with Tolterodine.Approved
BenzatropineThe risk or severity of adverse effects can be increased when Benzatropine is combined with Tolterodine.Approved
BetaxololThe metabolism of Tolterodine can be decreased when combined with Betaxolol.Approved
BexaroteneThe serum concentration of Tolterodine can be decreased when it is combined with Bexarotene.Approved, Investigational
BezitramideThe risk or severity of adverse effects can be increased when Tolterodine is combined with Bezitramide.Experimental, Illicit, Withdrawn
BiperidenThe risk or severity of adverse effects can be increased when Biperiden is combined with Tolterodine.Approved
BoceprevirThe serum concentration of Tolterodine can be increased when it is combined with Boceprevir.Approved
BortezomibThe metabolism of Tolterodine can be decreased when combined with Bortezomib.Approved, Investigational
BosentanThe serum concentration of Tolterodine can be decreased when it is combined with Bosentan.Approved, Investigational
Botulinum Toxin Type ATolterodine may increase the anticholinergic activities of Botulinum Toxin Type A.Approved, Investigational
Botulinum Toxin Type BTolterodine may increase the anticholinergic activities of Botulinum Toxin Type B.Approved
BuprenorphineThe risk or severity of adverse effects can be increased when Tolterodine is combined with Buprenorphine.Approved, Illicit, Investigational, Vet Approved
BupropionThe metabolism of Tolterodine can be decreased when combined with Bupropion.Approved
ButorphanolThe risk or severity of adverse effects can be increased when Tolterodine is combined with Butorphanol.Approved, Illicit, Vet Approved
CapecitabineThe metabolism of Tolterodine can be decreased when combined with Capecitabine.Approved, Investigational
CarbamazepineThe metabolism of Tolterodine can be increased when combined with Carbamazepine.Approved, Investigational
CarfentanilThe risk or severity of adverse effects can be increased when Tolterodine is combined with Carfentanil.Illicit, Vet Approved
CelecoxibThe metabolism of Tolterodine can be decreased when combined with Celecoxib.Approved, Investigational
CeritinibThe serum concentration of Tolterodine can be increased when it is combined with Ceritinib.Approved
ChloramphenicolThe metabolism of Tolterodine can be decreased when combined with Chloramphenicol.Approved, Vet Approved
ChloroquineTolterodine may increase the QTc-prolonging activities of Chloroquine.Approved, Vet Approved
ChlorothiazideThe serum concentration of Chlorothiazide can be increased when it is combined with Tolterodine.Approved, Vet Approved
ChlorphenoxamineThe risk or severity of adverse effects can be increased when Tolterodine is combined with Chlorphenoxamine.Withdrawn
ChlorpromazineTolterodine may increase the QTc-prolonging activities of Chlorpromazine.Approved, Vet Approved
ChlorthalidoneThe serum concentration of Chlorthalidone can be increased when it is combined with Tolterodine.Approved
CholecalciferolThe metabolism of Tolterodine can be decreased when combined with Cholecalciferol.Approved, Nutraceutical
CimetidineThe metabolism of Tolterodine can be decreased when combined with Cimetidine.Approved
CimetropiumTolterodine may increase the anticholinergic activities of Cimetropium.Experimental
CinacalcetThe metabolism of Tolterodine can be decreased when combined with Cinacalcet.Approved
CiprofloxacinTolterodine may increase the QTc-prolonging activities of Ciprofloxacin.Approved, Investigational
CisaprideTolterodine may increase the QTc-prolonging activities of Cisapride.Approved, Investigational, Withdrawn
CitalopramTolterodine may increase the QTc-prolonging activities of Citalopram.Approved
ClarithromycinThe serum concentration of Tolterodine can be increased when it is combined with Clarithromycin.Approved
ClemastineThe metabolism of Tolterodine can be decreased when combined with Clemastine.Approved
ClobazamThe metabolism of Tolterodine can be decreased when combined with Clobazam.Approved, Illicit
ClomipramineThe metabolism of Tolterodine can be decreased when combined with Clomipramine.Approved, Vet Approved
ClotrimazoleThe metabolism of Tolterodine can be decreased when combined with Clotrimazole.Approved, Vet Approved
ClozapineTolterodine may increase the QTc-prolonging activities of Clozapine.Approved
CobicistatThe serum concentration of Tolterodine can be increased when it is combined with Cobicistat.Approved
CocaineThe metabolism of Tolterodine can be decreased when combined with Cocaine.Approved, Illicit
CodeineThe risk or severity of adverse effects can be increased when Tolterodine is combined with Codeine.Approved, Illicit
ConivaptanThe serum concentration of Tolterodine can be increased when it is combined with Conivaptan.Approved, Investigational
CoumaphosThe therapeutic efficacy of Tolterodine can be decreased when used in combination with Coumaphos.Vet Approved
CrizotinibTolterodine may increase the QTc-prolonging activities of Crizotinib.Approved
CyclopentolateThe risk or severity of adverse effects can be increased when Cyclopentolate is combined with Tolterodine.Approved
CyclosporineThe metabolism of Tolterodine can be decreased when combined with Cyclosporine.Approved, Investigational, Vet Approved
DabrafenibThe serum concentration of Tolterodine 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 Tolterodine.Approved, Investigational
DarunavirThe serum concentration of Tolterodine can be increased when it is combined with Darunavir.Approved
DasatinibThe serum concentration of Tolterodine can be increased when it is combined with Dasatinib.Approved, Investigational
DecamethoniumThe therapeutic efficacy of Tolterodine can be decreased when used in combination with Decamethonium.Approved
DeferasiroxThe serum concentration of Tolterodine can be decreased when it is combined with Deferasirox.Approved, Investigational
DelavirdineThe metabolism of Tolterodine can be decreased when combined with Delavirdine.Approved
DemecariumThe therapeutic efficacy of Tolterodine can be decreased when used in combination with Demecarium.Approved
DesipramineThe metabolism of Tolterodine can be decreased when combined with Desipramine.Approved
DesloratadineThe risk or severity of adverse effects can be increased when Desloratadine is combined with Tolterodine.Approved, Investigational
DexamethasoneThe serum concentration of Tolterodine can be decreased when it is combined with Dexamethasone.Approved, Investigational, Vet Approved
DexetimideThe risk or severity of adverse effects can be increased when Tolterodine is combined with Dexetimide.Withdrawn
DextromoramideThe risk or severity of adverse effects can be increased when Tolterodine is combined with Dextromoramide.Experimental, Illicit
DextropropoxypheneThe risk or severity of adverse effects can be increased when Tolterodine is combined with Dextropropoxyphene.Approved, Illicit, Withdrawn
DezocineThe risk or severity of adverse effects can be increased when Tolterodine is combined with Dezocine.Approved
DichlorvosThe therapeutic efficacy of Tolterodine 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 Tolterodine.Approved
DihydrocodeineThe risk or severity of adverse effects can be increased when Tolterodine is combined with Dihydrocodeine.Approved, Illicit
DihydroergotamineThe metabolism of Tolterodine can be decreased when combined with Dihydroergotamine.Approved
DihydroetorphineThe risk or severity of adverse effects can be increased when Tolterodine is combined with Dihydroetorphine.Experimental, Illicit
DihydromorphineThe risk or severity of adverse effects can be increased when Tolterodine is combined with Dihydromorphine.Experimental, Illicit
DiltiazemThe metabolism of Tolterodine can be decreased when combined with Diltiazem.Approved
DiphenhydramineThe metabolism of Tolterodine can be decreased when combined with Diphenhydramine.Approved
DiphenoxylateThe risk or severity of adverse effects can be increased when Tolterodine is combined with Diphenoxylate.Approved, Illicit
DisopyramideTolterodine may increase the QTc-prolonging activities of Disopyramide.Approved
DofetilideTolterodine may increase the QTc-prolonging activities of Dofetilide.Approved
DolasetronTolterodine may increase the QTc-prolonging activities of Dolasetron.Approved
DomperidoneTolterodine may increase the QTc-prolonging activities of Domperidone.Approved, Investigational, Vet Approved
DonepezilThe therapeutic efficacy of Tolterodine can be decreased when used in combination with Donepezil.Approved
DoxycyclineThe metabolism of Tolterodine can be decreased when combined with Doxycycline.Approved, Investigational, Vet Approved
DPDPEThe risk or severity of adverse effects can be increased when Tolterodine is combined with DPDPE.Investigational
DronabinolTolterodine may increase the tachycardic activities of Dronabinol.Approved, Illicit
DronedaroneTolterodine may increase the QTc-prolonging activities of Dronedarone.Approved
DroperidolTolterodine may increase the QTc-prolonging activities of Droperidol.Approved, Vet Approved
DuloxetineThe metabolism of Tolterodine can be decreased when combined with Duloxetine.Approved
EchothiophateThe therapeutic efficacy of Tolterodine can be decreased when used in combination with Echothiophate.Approved
EdrophoniumThe therapeutic efficacy of Tolterodine can be decreased when used in combination with Edrophonium.Approved
EfavirenzThe serum concentration of Tolterodine can be decreased when it is combined with Efavirenz.Approved, Investigational
EliglustatTolterodine may increase the QTc-prolonging activities of Eliglustat.Approved
EluxadolineTolterodine may increase the constipating activities of Eluxadoline.Approved
EnzalutamideThe serum concentration of Tolterodine can be decreased when it is combined with Enzalutamide.Approved
ErythromycinTolterodine may increase the QTc-prolonging activities of Erythromycin.Approved, Vet Approved
EscitalopramTolterodine may increase the QTc-prolonging activities of Escitalopram.Approved, Investigational
Eslicarbazepine acetateThe serum concentration of Tolterodine can be decreased when it is combined with Eslicarbazepine acetate.Approved
EsomeprazoleThe metabolism of Tolterodine can be decreased when combined with Esomeprazole.Approved, Investigational
EthopropazineThe risk or severity of adverse effects can be increased when Ethopropazine is combined with Tolterodine.Approved
EthylmorphineThe risk or severity of adverse effects can be increased when Tolterodine is combined with Ethylmorphine.Approved, Illicit
EtorphineThe risk or severity of adverse effects can be increased when Tolterodine is combined with Etorphine.Illicit, Vet Approved
EtravirineThe serum concentration of Tolterodine can be decreased when it is combined with Etravirine.Approved
FentanylThe risk or severity of adverse effects can be increased when Tolterodine is combined with Fentanyl.Approved, Illicit, Investigational, Vet Approved
FenthionThe therapeutic efficacy of Tolterodine can be decreased when used in combination with Fenthion.Vet Approved
FesoterodineThe risk or severity of adverse effects can be increased when Tolterodine is combined with Fesoterodine.Approved
FlecainideTolterodine may increase the QTc-prolonging activities of Flecainide.Approved, Withdrawn
FloxuridineThe metabolism of Tolterodine can be decreased when combined with Floxuridine.Approved
FluconazoleThe metabolism of Tolterodine can be decreased when combined with Fluconazole.Approved
FluorouracilThe metabolism of Tolterodine can be decreased when combined with Fluorouracil.Approved
FluoxetineTolterodine may increase the QTc-prolonging activities of Fluoxetine.Approved, Vet Approved
FlupentixolTolterodine may increase the QTc-prolonging activities of Flupentixol.Approved, Withdrawn
FluvastatinThe metabolism of Tolterodine can be decreased when combined with Fluvastatin.Approved
FluvoxamineThe metabolism of Tolterodine can be decreased when combined with Fluvoxamine.Approved, Investigational
FosamprenavirThe metabolism of Tolterodine can be decreased when combined with Fosamprenavir.Approved
FosaprepitantThe serum concentration of Tolterodine can be increased when it is combined with Fosaprepitant.Approved
FosphenytoinThe metabolism of Tolterodine can be increased when combined with Fosphenytoin.Approved
Fusidic AcidThe serum concentration of Tolterodine can be increased when it is combined with Fusidic Acid.Approved
Gadobenic acidTolterodine may increase the QTc-prolonging activities of Gadobenic acid.Approved
GalantamineThe therapeutic efficacy of Tolterodine 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 Tolterodine.Approved
GemfibrozilThe metabolism of Tolterodine can be decreased when combined with Gemfibrozil.Approved
GemifloxacinTolterodine may increase the QTc-prolonging activities of Gemifloxacin.Approved, Investigational
Ginkgo bilobaThe therapeutic efficacy of Tolterodine can be decreased when used in combination with Ginkgo biloba.Approved, Nutraceutical
Glucagon recombinantThe risk or severity of adverse effects can be increased when Tolterodine is combined with Glucagon recombinant.Approved
GlycopyrroniumTolterodine may increase the anticholinergic activities of Glycopyrronium.Approved, Investigational, Vet Approved
GoserelinTolterodine may increase the QTc-prolonging activities of Goserelin.Approved
GranisetronTolterodine may increase the QTc-prolonging activities of Granisetron.Approved, Investigational
HaloperidolTolterodine may increase the QTc-prolonging activities of Haloperidol.Approved
HeroinThe risk or severity of adverse effects can be increased when Tolterodine is combined with Heroin.Approved, Illicit
HexamethoniumThe risk or severity of adverse effects can be increased when Tolterodine is combined with Hexamethonium.Experimental
HomatropineThe risk or severity of adverse effects can be increased when Tolterodine is combined with Homatropine.Approved
Huperzine AThe therapeutic efficacy of Tolterodine can be decreased when used in combination with Huperzine A.Investigational
HydrochlorothiazideThe serum concentration of Hydrochlorothiazide can be increased when it is combined with Tolterodine.Approved, Vet Approved
HydrocodoneThe risk or severity of adverse effects can be increased when Tolterodine is combined with Hydrocodone.Approved, Illicit
HydroflumethiazideThe serum concentration of Hydroflumethiazide can be increased when it is combined with Tolterodine.Approved
HydromorphoneThe risk or severity of adverse effects can be increased when Tolterodine is combined with Hydromorphone.Approved, Illicit
HyoscyamineThe risk or severity of adverse effects can be increased when Hyoscyamine is combined with Tolterodine.Approved
IbutilideTolterodine may increase the QTc-prolonging activities of Ibutilide.Approved
IdelalisibThe serum concentration of Tolterodine can be increased when it is combined with Idelalisib.Approved
IloperidoneTolterodine may increase the QTc-prolonging activities of Iloperidone.Approved
ImatinibThe metabolism of Tolterodine can be decreased when combined with Imatinib.Approved
ImipramineThe metabolism of Tolterodine can be decreased when combined with Imipramine.Approved
IndapamideThe serum concentration of Indapamide can be increased when it is combined with Tolterodine.Approved
IndinavirThe serum concentration of Tolterodine can be increased when it is combined with Indinavir.Approved
Ipratropium bromideThe risk or severity of adverse effects can be increased when Ipratropium bromide is combined with Tolterodine.Approved
IrbesartanThe metabolism of Tolterodine can be decreased when combined with Irbesartan.Approved, Investigational
IsavuconazoniumThe metabolism of Tolterodine can be decreased when combined with Isavuconazonium.Approved, Investigational
IsoflurophateThe therapeutic efficacy of Tolterodine can be decreased when used in combination with Isoflurophate.Approved, Withdrawn
IsoniazidThe metabolism of Tolterodine can be decreased when combined with Isoniazid.Approved
IsradipineThe metabolism of Tolterodine can be decreased when combined with Isradipine.Approved
ItoprideThe therapeutic efficacy of Itopride can be decreased when used in combination with Tolterodine.Investigational
ItraconazoleThe serum concentration of Tolterodine can be increased when it is combined with Itraconazole.Approved, Investigational
IvacaftorThe serum concentration of Tolterodine can be increased when it is combined with Ivacaftor.Approved
KetobemidoneThe risk or severity of adverse effects can be increased when Tolterodine is combined with Ketobemidone.Approved
KetoconazoleThe serum concentration of Tolterodine can be increased when it is combined with Ketoconazole.Approved, Investigational
LeflunomideThe metabolism of Tolterodine can be decreased when combined with Leflunomide.Approved, Investigational
LenvatinibTolterodine may increase the QTc-prolonging activities of Lenvatinib.Approved
LeuprolideTolterodine may increase the QTc-prolonging activities of Leuprolide.Approved, Investigational
LevofloxacinTolterodine may increase the QTc-prolonging activities of Levofloxacin.Approved, Investigational
Levomethadyl AcetateThe risk or severity of adverse effects can be increased when Tolterodine is combined with Levomethadyl Acetate.Approved
LevorphanolThe risk or severity of adverse effects can be increased when Tolterodine is combined with Levorphanol.Approved
LofentanilThe risk or severity of adverse effects can be increased when Tolterodine is combined with Lofentanil.Illicit
LopinavirThe serum concentration of Tolterodine can be increased when it is combined with Lopinavir.Approved
LorcaserinThe metabolism of Tolterodine can be decreased when combined with Lorcaserin.Approved
LosartanThe metabolism of Tolterodine can be decreased when combined with Losartan.Approved
LovastatinThe metabolism of Tolterodine can be decreased when combined with Lovastatin.Approved, Investigational
LuliconazoleThe serum concentration of Tolterodine can be increased when it is combined with Luliconazole.Approved
LumacaftorThe serum concentration of Tolterodine can be decreased when it is combined with Lumacaftor.Approved
LumefantrineTolterodine may increase the QTc-prolonging activities of Lumefantrine.Approved
MalathionThe therapeutic efficacy of Tolterodine 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 Tolterodine.Approved
MefloquineThe therapeutic efficacy of Tolterodine can be decreased when used in combination with Mefloquine.Approved
MemantineThe therapeutic efficacy of Tolterodine can be decreased when used in combination with Memantine.Approved, Investigational
MethadoneTolterodine may increase the QTc-prolonging activities of Methadone.Approved
Methadyl AcetateThe risk or severity of adverse effects can be increased when Tolterodine is combined with Methadyl Acetate.Approved, Illicit
Methanesulfonyl FluorideThe therapeutic efficacy of Tolterodine 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 Tolterodine.Approved
MethotrimeprazineThe metabolism of Tolterodine can be decreased when combined with Methotrimeprazine.Approved
MethyclothiazideThe serum concentration of Methyclothiazide can be increased when it is combined with Tolterodine.Approved
MetixeneThe risk or severity of adverse effects can be increased when Tolterodine is combined with Metixene.Approved
MetolazoneThe serum concentration of Metolazone can be increased when it is combined with Tolterodine.Approved
MetoprololThe metabolism of Tolterodine can be decreased when combined with Metoprolol.Approved, Investigational
MianserinMianserin may increase the anticholinergic activities of Tolterodine.Approved
MifepristoneThe serum concentration of Tolterodine can be increased when it is combined with Mifepristone.Approved, Investigational
MinaprineThe therapeutic efficacy of Tolterodine can be decreased when used in combination with Minaprine.Approved
MirabegronThe risk or severity of adverse effects can be increased when Tolterodine is combined with Mirabegron.Approved
MitotaneThe serum concentration of Tolterodine can be decreased when it is combined with Mitotane.Approved
MoclobemideThe metabolism of Tolterodine can be decreased when combined with Moclobemide.Approved
ModafinilThe serum concentration of Tolterodine can be decreased when it is combined with Modafinil.Approved, Investigational
MorphineThe risk or severity of adverse effects can be increased when Tolterodine is combined with Morphine.Approved, Investigational
MoxifloxacinTolterodine may increase the QTc-prolonging activities of Moxifloxacin.Approved, Investigational
N-butylscopolammonium bromideThe risk or severity of adverse effects can be increased when Tolterodine is combined with N-butylscopolammonium bromide.Vet Approved
NabiloneTolterodine may increase the tachycardic activities of Nabilone.Approved, Investigational
NafcillinThe serum concentration of Tolterodine can be decreased when it is combined with Nafcillin.Approved
NalbuphineThe risk or severity of adverse effects can be increased when Tolterodine is combined with Nalbuphine.Approved
NefazodoneThe serum concentration of Tolterodine can be increased when it is combined with Nefazodone.Approved, Withdrawn
NelfinavirThe serum concentration of Tolterodine can be increased when it is combined with Nelfinavir.Approved
NeostigmineThe therapeutic efficacy of Tolterodine can be decreased when used in combination with Neostigmine.Approved, Vet Approved
NetupitantThe serum concentration of Tolterodine can be increased when it is combined with Netupitant.Approved
NevirapineThe metabolism of Tolterodine can be increased when combined with Nevirapine.Approved
NicardipineThe metabolism of Tolterodine can be decreased when combined with Nicardipine.Approved
NilotinibTolterodine may increase the QTc-prolonging activities of Nilotinib.Approved, Investigational
NormethadoneThe risk or severity of adverse effects can be increased when Tolterodine is combined with Normethadone.Approved, Illicit
NVA237The risk or severity of adverse effects can be increased when Tolterodine is combined with NVA237.Investigational
OfloxacinTolterodine may increase the QTc-prolonging activities of Ofloxacin.Approved
OlaparibThe metabolism of Tolterodine can be decreased when combined with Olaparib.Approved
OmeprazoleThe metabolism of Tolterodine can be decreased when combined with Omeprazole.Approved, Investigational, Vet Approved
OndansetronTolterodine may increase the QTc-prolonging activities of Ondansetron.Approved
OpiumThe risk or severity of adverse effects can be increased when Tolterodine is combined with Opium.Approved, Illicit
OrphenadrineThe risk or severity of adverse effects can be increased when Tolterodine is combined with Orphenadrine.Approved
OsimertinibThe serum concentration of Tolterodine can be increased when it is combined with Osimertinib.Approved
OxybutyninThe risk or severity of adverse effects can be increased when Tolterodine is combined with Oxybutynin.Approved, Investigational
OxycodoneThe risk or severity of adverse effects can be increased when Tolterodine is combined with Oxycodone.Approved, Illicit, Investigational
OxymorphoneThe risk or severity of adverse effects can be increased when Tolterodine is combined with Oxymorphone.Approved, Investigational, Vet Approved
OxyphenoniumThe risk or severity of adverse effects can be increased when Oxyphenonium is combined with Tolterodine.Approved
PalbociclibThe serum concentration of Tolterodine can be increased when it is combined with Palbociclib.Approved
PaliperidoneTolterodine may increase the QTc-prolonging activities of Paliperidone.Approved
PancuroniumThe risk or severity of adverse effects can be increased when Tolterodine is combined with Pancuronium.Approved
PanobinostatThe serum concentration of Tolterodine can be increased when it is combined with Panobinostat.Approved, Investigational
PantoprazoleThe metabolism of Tolterodine can be decreased when combined with Pantoprazole.Approved
ParoxetineThe metabolism of Tolterodine can be decreased when combined with Paroxetine.Approved, Investigational
PazopanibTolterodine may increase the QTc-prolonging activities of Pazopanib.Approved
Peginterferon alfa-2bThe serum concentration of Tolterodine can be decreased when it is combined with Peginterferon alfa-2b.Approved
PentamidineTolterodine may increase the QTc-prolonging activities of Pentamidine.Approved
PentazocineThe risk or severity of adverse effects can be increased when Tolterodine is combined with Pentazocine.Approved, Vet Approved
PentobarbitalThe metabolism of Tolterodine can be increased when combined with Pentobarbital.Approved, Vet Approved
PentoliniumThe risk or severity of adverse effects can be increased when Tolterodine is combined with Pentolinium.Approved
PerflutrenTolterodine may increase the QTc-prolonging activities of Perflutren.Approved
PethidineThe risk or severity of adverse effects can be increased when Tolterodine is combined with Pethidine.Approved
PhenobarbitalThe metabolism of Tolterodine can be increased when combined with Phenobarbital.Approved
PhenytoinThe metabolism of Tolterodine can be increased when combined with Phenytoin.Approved, Vet Approved
PhysostigmineThe therapeutic efficacy of Tolterodine can be decreased when used in combination with Physostigmine.Approved
PimozideTolterodine may increase the QTc-prolonging activities of Pimozide.Approved
PipecuroniumThe risk or severity of adverse effects can be increased when Tolterodine is combined with Pipecuronium.Approved
PirenzepineThe risk or severity of adverse effects can be increased when Pirenzepine is combined with Tolterodine.Approved
PiritramideThe risk or severity of adverse effects can be increased when Tolterodine is combined with Piritramide.Investigational
PolythiazideThe serum concentration of Polythiazide can be increased when it is combined with Tolterodine.Approved
PosaconazoleThe serum concentration of Tolterodine can be increased when it is combined with Posaconazole.Approved, Investigational, Vet Approved
Potassium ChlorideTolterodine may increase the ulcerogenic activities of Potassium Chloride.Approved, Withdrawn
PramlintidePramlintide may increase the anticholinergic activities of Tolterodine.Approved, Investigational
PrimaquineTolterodine may increase the QTc-prolonging activities of Primaquine.Approved
PrimidoneThe metabolism of Tolterodine can be increased when combined with Primidone.Approved, Vet Approved
ProcainamideTolterodine may increase the QTc-prolonging activities of Procainamide.Approved
ProcyclidineThe risk or severity of adverse effects can be increased when Procyclidine is combined with Tolterodine.Approved
PromazineTolterodine may increase the QTc-prolonging activities of Promazine.Approved, Vet Approved
PropafenoneTolterodine may increase the QTc-prolonging activities of Propafenone.Approved
PropanthelineThe risk or severity of adverse effects can be increased when Propantheline is combined with Tolterodine.Approved
PropiverineThe risk or severity of adverse effects can be increased when Tolterodine is combined with Propiverine.Investigational
PyridostigmineThe therapeutic efficacy of Tolterodine can be decreased when used in combination with Pyridostigmine.Approved
PyrimethamineThe metabolism of Tolterodine can be decreased when combined with Pyrimethamine.Approved, Vet Approved
QuetiapineTolterodine may increase the QTc-prolonging activities of Quetiapine.Approved
QuinethazoneThe serum concentration of Quinethazone can be increased when it is combined with Tolterodine.Approved
QuinidineTolterodine may increase the QTc-prolonging activities of Quinidine.Approved
QuinineTolterodine may increase the QTc-prolonging activities of Quinine.Approved
RamosetronTolterodine may increase the constipating activities of Ramosetron.Approved
RanolazineThe metabolism of Tolterodine can be decreased when combined with Ranolazine.Approved, Investigational
RemifentanilThe risk or severity of adverse effects can be increased when Tolterodine is combined with Remifentanil.Approved
RifabutinThe metabolism of Tolterodine can be increased when combined with Rifabutin.Approved
RifampicinThe metabolism of Tolterodine can be increased when combined with Rifampicin.Approved
RifapentineThe metabolism of Tolterodine can be increased when combined with Rifapentine.Approved
RitonavirThe serum concentration of Tolterodine can be increased when it is combined with Ritonavir.Approved, Investigational
RivastigmineThe therapeutic efficacy of Tolterodine can be decreased when used in combination with Rivastigmine.Approved, Investigational
RolapitantThe metabolism of Tolterodine can be decreased when combined with Rolapitant.Approved
RopiniroleThe metabolism of Tolterodine can be decreased when combined with Ropinirole.Approved, Investigational
SaquinavirThe serum concentration of Tolterodine can be increased when it is combined with Saquinavir.Approved, Investigational
ScopolamineThe risk or severity of adverse effects can be increased when Scopolamine is combined with Tolterodine.Approved
Scopolamine butylbromideThe risk or severity of adverse effects can be increased when Tolterodine is combined with Scopolamine butylbromide.Approved
SecobarbitalThe metabolism of Tolterodine can be increased when combined with Secobarbital.Approved, Vet Approved
SecretinThe therapeutic efficacy of Secretin can be decreased when used in combination with Tolterodine.Approved, Investigational
SertralineThe metabolism of Tolterodine can be decreased when combined with Sertraline.Approved
SildenafilThe metabolism of Tolterodine can be decreased when combined with Sildenafil.Approved, Investigational
SiltuximabThe serum concentration of Tolterodine can be decreased when it is combined with Siltuximab.Approved
SimeprevirThe serum concentration of Tolterodine can be increased when it is combined with Simeprevir.Approved
SolifenacinThe risk or severity of adverse effects can be increased when Tolterodine is combined with Solifenacin.Approved
SorafenibThe metabolism of Tolterodine can be decreased when combined with Sorafenib.Approved, Investigational
SotalolTolterodine may increase the QTc-prolonging activities of Sotalol.Approved
St. John's WortThe serum concentration of Tolterodine can be decreased when it is combined with St. John's Wort.Nutraceutical
StiripentolThe serum concentration of Tolterodine can be increased when it is combined with Stiripentol.Approved
SufentanilThe risk or severity of adverse effects can be increased when Tolterodine is combined with Sufentanil.Approved, Investigational
SulfadiazineThe metabolism of Tolterodine can be decreased when combined with Sulfadiazine.Approved, Vet Approved
SulfamethoxazoleThe metabolism of Tolterodine can be decreased when combined with Sulfamethoxazole.Approved
SulfisoxazoleThe metabolism of Tolterodine can be decreased when combined with Sulfisoxazole.Approved, Vet Approved
SulpirideThe therapeutic efficacy of Sulpiride can be decreased when used in combination with Tolterodine.Approved
TacrineThe therapeutic efficacy of Tolterodine can be decreased when used in combination with Tacrine.Withdrawn
TapentadolThe risk or severity of adverse effects can be increased when Tolterodine is combined with Tapentadol.Approved
TelaprevirThe serum concentration of Tolterodine can be increased when it is combined with Telaprevir.Approved
TelavancinTolterodine may increase the QTc-prolonging activities of Telavancin.Approved
TelithromycinThe serum concentration of Tolterodine can be increased when it is combined with Telithromycin.Approved
TerbinafineThe metabolism of Tolterodine can be decreased when combined with Terbinafine.Approved, Investigational, Vet Approved
TetrabenazineTolterodine may increase the QTc-prolonging activities of Tetrabenazine.Approved
ThioridazineTolterodine may increase the QTc-prolonging activities of Thioridazine.Approved
TicagrelorThe metabolism of Tolterodine can be decreased when combined with Ticagrelor.Approved
TiclopidineThe metabolism of Tolterodine can be decreased when combined with Ticlopidine.Approved
TiotropiumTolterodine may increase the anticholinergic activities of Tiotropium.Approved
TipranavirThe metabolism of Tolterodine can be decreased when combined with Tipranavir.Approved, Investigational
TocilizumabThe serum concentration of Tolterodine can be decreased when it is combined with Tocilizumab.Approved
TolbutamideThe metabolism of Tolterodine can be decreased when combined with Tolbutamide.Approved
TopiramateThe risk or severity of adverse effects can be increased when Tolterodine is combined with Topiramate.Approved
ToremifeneTolterodine may increase the QTc-prolonging activities of Toremifene.Approved, Investigational
TramadolThe risk or severity of adverse effects can be increased when Tolterodine is combined with Tramadol.Approved, Investigational
TranylcypromineThe metabolism of Tolterodine can be decreased when combined with Tranylcypromine.Approved
TrichlorfonThe therapeutic efficacy of Tolterodine can be decreased when used in combination with Trichlorfon.Vet Approved
TrichlormethiazideThe serum concentration of Trichlormethiazide can be increased when it is combined with Tolterodine.Approved, Vet Approved
TrihexyphenidylThe risk or severity of adverse effects can be increased when Trihexyphenidyl is combined with Tolterodine.Approved
TrimethaphanThe risk or severity of adverse effects can be increased when Tolterodine is combined with Trimethaphan.Approved
TrimethoprimThe metabolism of Tolterodine can be decreased when combined with Trimethoprim.Approved, Vet Approved
TropicamideThe risk or severity of adverse effects can be increased when Tropicamide is combined with Tolterodine.Approved
TrospiumThe risk or severity of adverse effects can be increased when Trospium is combined with Tolterodine.Approved
TubocurarineThe risk or severity of adverse effects can be increased when Tolterodine is combined with Tubocurarine.Approved
UmeclidiniumUmeclidinium may increase the anticholinergic activities of Tolterodine.Approved
Valproic AcidThe metabolism of Tolterodine can be decreased when combined with Valproic Acid.Approved, Investigational
ValsartanThe metabolism of Tolterodine can be decreased when combined with Valsartan.Approved, Investigational
VandetanibTolterodine may increase the QTc-prolonging activities of Vandetanib.Approved
VecuroniumThe risk or severity of adverse effects can be increased when Tolterodine is combined with Vecuronium.Approved
VemurafenibTolterodine may increase the QTc-prolonging activities of Vemurafenib.Approved
VenlafaxineThe metabolism of Tolterodine can be decreased when combined with Venlafaxine.Approved
VerapamilThe metabolism of Tolterodine can be decreased when combined with Verapamil.Approved
VinblastineThe serum concentration of Tolterodine can be increased when it is combined with Vinblastine.Approved
VoriconazoleThe serum concentration of Tolterodine can be increased when it is combined with Voriconazole.Approved, Investigational
WarfarinTolterodine may increase the anticoagulant activities of Warfarin.Approved
ZafirlukastThe metabolism of Tolterodine can be decreased when combined with Zafirlukast.Approved, Investigational
ZiprasidoneTolterodine may increase the QTc-prolonging activities of Ziprasidone.Approved
ZuclopenthixolTolterodine may increase the QTc-prolonging activities of Zuclopenthixol.Approved, Investigational
Food Interactions
  • Take with food.
References
Synthesis Reference

Yatendra Kumar, “PROCESS FOR THE PREPARATION OF TOLTERODINE.” U.S. Patent US20040249211, issued December 09, 2004.

US20040249211
General ReferencesNot Available
External Links
ATC CodesG04BD07
AHFS Codes
  • 86:12.00
PDB EntriesNot Available
FDA labelDownload (94.9 KB)
MSDSNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.958
Blood Brain Barrier+0.9194
Caco-2 permeable+0.8286
P-glycoprotein substrateSubstrate0.5
P-glycoprotein inhibitor INon-inhibitor0.6727
P-glycoprotein inhibitor IINon-inhibitor0.8305
Renal organic cation transporterInhibitor0.6904
CYP450 2C9 substrateNon-substrate0.6235
CYP450 2D6 substrateSubstrate0.8918
CYP450 3A4 substrateSubstrate0.7408
CYP450 1A2 substrateInhibitor0.8139
CYP450 2C9 inhibitorNon-inhibitor0.6965
CYP450 2D6 inhibitorInhibitor0.7456
CYP450 2C19 inhibitorNon-inhibitor0.5853
CYP450 3A4 inhibitorNon-inhibitor0.8575
CYP450 inhibitory promiscuityHigh CYP Inhibitory Promiscuity0.5259
Ames testNon AMES toxic0.6658
CarcinogenicityNon-carcinogens0.7967
BiodegradationNot ready biodegradable0.9959
Rat acute toxicity2.5503 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.8014
hERG inhibition (predictor II)Inhibitor0.6875
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
ManufacturersNot Available
Packagers
Dosage forms
FormRouteStrength
TabletOral1 mg
TabletOral2 mg
Tablet, film coatedOral1 mg/1
Tablet, film coatedOral2 mg/1
Capsule, extended releaseOral2 mg
Capsule, extended releaseOral2 mg/1
Capsule, extended releaseOral4 mg
Capsule, extended releaseOral4 mg/1
Prices
Unit descriptionCostUnit
Detrol LA 2 mg 24 Hour Capsule5.01USD capsule
Detrol LA 4 mg 24 Hour Capsule4.84USD capsule
Detrol la 4 mg capsule4.82USD capsule
Detrol la 2 mg capsule4.81USD capsule
Detrol 2 mg tablet2.85USD tablet
Detrol 1 mg tablet2.77USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
CA1340223 No1998-12-152015-12-15Canada
CA2311755 No2010-03-232019-08-26Canada
US5382600 No1995-03-252012-03-25Us
US6630162 Yes2000-05-112020-05-11Us
US6770295 Yes2000-02-262020-02-26Us
US6911217 Yes2000-05-112020-05-11Us
Properties
StateSolid
Experimental Properties
PropertyValueSource
logP5.6Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.00534 mg/mLALOGPS
logP5.39ALOGPS
logP5.12ChemAxon
logS-4.8ALOGPS
pKa (Strongest Acidic)10.28ChemAxon
pKa (Strongest Basic)11.01ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count2ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area23.47 Å2ChemAxon
Rotatable Bond Count7ChemAxon
Refractivity103.96 m3·mol-1ChemAxon
Polarizability39.27 Å3ChemAxon
Number of Rings2ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
Spectra
Spectrum TypeDescriptionSplash Key
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, NegativeNot Available
Taxonomy
DescriptionThis 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.
KingdomOrganic compounds
Super ClassBenzenoids
ClassBenzene and substituted derivatives
Sub ClassDiphenylmethanes
Direct ParentDiphenylmethanes
Alternative Parents
Substituents
  • Diphenylmethane
  • Phenylpropylamine
  • P-cresol
  • Aralkylamine
  • Toluene
  • Phenol
  • Tertiary aliphatic amine
  • Tertiary amine
  • Hydrocarbon derivative
  • Organooxygen compound
  • Organonitrogen compound
  • Amine
  • Aromatic homomonocyclic compound
Molecular FrameworkAromatic homomonocyclic compounds
External Descriptors

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. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
  2. Schneider T, Fetscher C, Krege S, Michel MC: Signal transduction underlying carbachol-induced contraction of human urinary bladder. J Pharmacol Exp Ther. 2004 Jun;309(3):1148-53. Epub 2004 Feb 9. [PubMed:14769832 ]
  3. McNamara A, Pulido-Rios MT, Sweazey S, Obedencio GP, Thibodeaux H, Renner T, Armstrong SR, Steinfeld T, Hughes AD, Wilson RD, Jasper JR, Mammen M, Hegde SS: Pharmacological properties of TD-6301, a novel bladder selective muscarinic receptor antagonist. Eur J Pharmacol. 2009 Mar 1;605(1-3):145-52. doi: 10.1016/j.ejphar.2008.12.043. Epub 2009 Jan 10. [PubMed:19168050 ]
  4. Sellers DJ, Yamanishi T, Chapple CR, Couldwell C, Yasuda K, Chess-Williams R: M3 muscarinic receptors but not M2 mediate contraction of the porcine detrusor muscle in vitro. J Auton Pharmacol. 2000 Jun;20(3):171-6. [PubMed:11193006 ]
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 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. Nelson CP, Nahorski SR, Challiss RA: Constitutive activity and inverse agonism at the M2 muscarinic acetylcholine receptor. J Pharmacol Exp Ther. 2006 Jan;316(1):279-88. Epub 2005 Sep 27. [PubMed:16188951 ]
  2. Schneider T, Fetscher C, Krege S, Michel MC: Signal transduction underlying carbachol-induced contraction of human urinary bladder. J Pharmacol Exp Ther. 2004 Jun;309(3):1148-53. Epub 2004 Feb 9. [PubMed:14769832 ]
  3. McNamara A, Pulido-Rios MT, Sweazey S, Obedencio GP, Thibodeaux H, Renner T, Armstrong SR, Steinfeld T, Hughes AD, Wilson RD, Jasper JR, Mammen M, Hegde SS: Pharmacological properties of TD-6301, a novel bladder selective muscarinic receptor antagonist. Eur J Pharmacol. 2009 Mar 1;605(1-3):145-52. doi: 10.1016/j.ejphar.2008.12.043. Epub 2009 Jan 10. [PubMed:19168050 ]
  4. Sellers DJ, Yamanishi T, Chapple CR, Couldwell C, Yasuda K, Chess-Williams R: M3 muscarinic receptors but not M2 mediate contraction of the porcine detrusor muscle in vitro. J Auton Pharmacol. 2000 Jun;20(3):171-6. [PubMed:11193006 ]
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 action of G proteins. Primary transducing effect is Pi turnover.
Gene Name:
CHRM5
Uniprot ID:
P08912
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:
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. Schneider T, Fetscher C, Krege S, Michel MC: Signal transduction underlying carbachol-induced contraction of human urinary bladder. J Pharmacol Exp Ther. 2004 Jun;309(3):1148-53. Epub 2004 Feb 9. [PubMed:14769832 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
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. 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 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Steroid hydroxylase activity
Specific Function:
Responsible for the metabolism of many drugs and environmental chemicals that it oxidizes. It is involved in the metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic antidepressants.
Gene Name:
CYP2D6
Uniprot ID:
P10635
Molecular Weight:
55768.94 Da
References
  1. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [PubMed:19515014 ]
  2. 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 ]
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. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [PubMed:19515014 ]
  2. 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 ]
  3. Postlind H, DanielsonA, Lindgren A, Andersson SH: Tolterodine, a new muscarinic receptor antagonist, is metabolized by cytochromes P450 2D6 and 3A in human liver microsomes. Drug Metab Dispos. 1998 Apr;26(4):289-93. [PubMed:9531513 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Steroid 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 oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. This enzyme contributes to the wide pharmacokinetics variability of the metabolism of drugs such as S-warfarin, diclofenac, phenyto...
Gene Name:
CYP2C9
Uniprot ID:
P11712
Molecular Weight:
55627.365 Da
References
  1. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [PubMed:19515014 ]
  2. 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 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Steroid hydroxylase activity
Specific Function:
Responsible for the metabolism of a number of therapeutic agents such as the anticonvulsant drug S-mephenytoin, omeprazole, proguanil, certain barbiturates, diazepam, propranolol, citalopram and imipramine.
Gene Name:
CYP2C19
Uniprot ID:
P33261
Molecular Weight:
55930.545 Da
References
  1. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [PubMed:19515014 ]
  2. 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 ]
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Drug created on June 13, 2005 07:24 / Updated on December 10, 2016 03:55