Identification

Name
Tolterodine
Accession Number
DB01036  (APRD00146)
Type
Small Molecule
Groups
Approved, Investigational
Description

Tolterodine 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
Product Ingredients
IngredientUNIICASInChI Key
Tolterodine Tartrate5T619TQR3R124937-52-6TWHNMSJGYKMTRB-KXYUELECSA-N
Product Images
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Ach-tolterodine Tartrate Extended ReleaseCapsule, extended release4 mgOralAccord Healthcare LimitedNot applicableNot applicableCanada
Ach-tolterodine Tartrate Extended ReleaseCapsule, extended release2 mgOralAccord Healthcare LimitedNot applicableNot applicableCanada
DetrolTablet, film coated2 mg/1OralStat Rx USA1998-03-25Not applicableUs
DetrolTablet, film coated1 mg/1OralPharmacia & Upjohn Inc1998-03-25Not applicableUs
DetrolTablet2 mgOralPfizer1998-11-23Not applicableCanada
DetrolTablet, film coated2 mg/1OralPharmacia & Upjohn Inc1998-03-25Not applicableUs
DetrolTablet1 mgOralPfizer1998-11-26Not applicableCanada
Detrol LACapsule, extended release4 mgOralPfizer2002-03-26Not applicableCanada
Detrol LACapsule, extended release4 mg/1OralLake Erie Medical &Surgical Supply Dba Quality Care Products Llc2012-02-282017-10-02Us
Detrol LACapsule, extended release4 mg/1OralPharmacia & Upjohn Inc2000-02-22Not applicableUs
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Apo-tolterodineTablet2 mgOralApotex Corporation2016-03-03Not applicableCanada
Apo-tolterodineTablet1 mgOralApotex Corporation2016-03-03Not applicableCanada
Tolterodine TartrateTablet, film coated2 mg/1OralMylan Pharmaceuticals2012-11-27Not applicableUs
Tolterodine TartrateCapsule, extended release4 mg/1OralMajor2015-08-11Not applicableUs
Tolterodine tartrateTablet, film coated1 mg/1OralMacleods Pharmaceuticals Limited2015-10-08Not applicableUs
Tolterodine TartrateCapsule, extended release2 mg/1OralAmerincan Health Packaging2017-07-15Not applicableUs
Tolterodine TartrateCapsule, extended release4 mg/1OralMylan Institutional2014-01-29Not applicableUs
Tolterodine TartrateTablet, film coated1 mg/1OralTeva2015-11-01Not applicableUs00093 0010 06 nlmimage10 784a3c11
Tolterodine TartrateCapsule, extended release4 mg/1OralAvera Mc Kennan Hospital2016-01-13Not applicableUs
Tolterodine TartrateCapsule, extended release2 mg/1OralMajor2015-08-11Not applicableUs
International/Other Brands
Detrusitol
Categories
UNII
WHE7A56U7K
CAS number
124937-51-5
Weight
Average: 325.4876
Monoisotopic: 325.240564619
Chemical Formula
C22H31NO
InChI Key
OOGJQPCLVADCPB-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

Indication

For the treatment of overactive bladder (with symptoms of urinary frequency, urgency, or urge incontinence).

Structured Indications
Pharmacodynamics

Tolterodine 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 action

Both 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.

TargetActionsOrganism
AMuscarinic acetylcholine receptor M3
antagonist
Human
AMuscarinic acetylcholine receptor M2
antagonist
Human
AMuscarinic acetylcholine receptor M5
antagonist
Human
AMuscarinic acetylcholine receptor M1
antagonist
Human
AMuscarinic acetylcholine receptor M4
antagonist
Human
Absorption
Not Available
Volume of distribution
  • 113 ± 26.7 L
Protein binding

Approximately 96.3%.

Metabolism
Route of elimination

Following 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 life

1.9-3.7 hours

Clearance
Not Available
Toxicity
Not Available
Affected organisms
  • Humans and other mammals
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Interacting Gene/EnzymeAllele nameGenotype(s)Defining Change(s)Type(s)DescriptionDetails
Cytochrome P450 2D6CYP2D6*3Not AvailableC alleleEffect InferredPoor drug metabolizer, greater QTc interval increase in poor metabolizers, but no association of drug with Torsade de Pointes.Details
Cytochrome P450 2D6CYP2D6*4Not AvailableC alleleEffect InferredPoor drug metabolizer, greater QTc interval increase in poor metabolizers, but no association of drug with Torsade de Pointes.Details
Cytochrome P450 2D6CYP2D6*5Not AvailableWhole-gene deletionEffect InferredPoor drug metabolizer, greater QTc interval increase in poor metabolizers, but no association of drug with Torsade de Pointes.Details
Cytochrome P450 2D6CYP2D6*6Not Available1707delTEffect InferredPoor drug metabolizer, greater QTc interval increase in poor metabolizers, but no association of drug with Torsade de Pointes.Details
Cytochrome P450 2D6CYP2D6*7Not Available2935A>CEffect InferredPoor drug metabolizer, greater QTc interval increase in poor metabolizers, but no association of drug with Torsade de Pointes.Details
Cytochrome P450 2D6CYP2D6*8Not Available1758G>TEffect InferredPoor drug metabolizer, greater QTc interval increase in poor metabolizers, but no association of drug with Torsade de Pointes.Details
Cytochrome P450 2D6CYP2D6*11Not Available883G>CEffect InferredPoor drug metabolizer, greater QTc interval increase in poor metabolizers, but no association of drug with Torsade de Pointes.Details
Cytochrome P450 2D6CYP2D6*12Not Available124G>AEffect InferredPoor drug metabolizer, greater QTc interval increase in poor metabolizers, but no association of drug with Torsade de Pointes.Details
Cytochrome P450 2D6CYP2D6*13Not AvailableCYP2D7/2D6 hybrid gene structureEffect InferredPoor drug metabolizer, greater QTc interval increase in poor metabolizers, but no association of drug with Torsade de Pointes.Details
Cytochrome P450 2D6CYP2D6*14ANot Available1758G>AEffect InferredPoor drug metabolizer, greater QTc interval increase in poor metabolizers, but no association of drug with Torsade de Pointes.Details
Cytochrome P450 2D6CYP2D6*15Not Available137insT, 137_138insTEffect InferredPoor drug metabolizer, greater QTc interval increase in poor metabolizers, but no association of drug with Torsade de Pointes.Details
Cytochrome P450 2D6CYP2D6*19Not Available2539_2542delAACTEffect InferredPoor drug metabolizer, greater QTc interval increase in poor metabolizers, but no association of drug with Torsade de Pointes.Details
Cytochrome P450 2D6CYP2D6*20Not Available1973_1974insGEffect InferredPoor drug metabolizer, greater QTc interval increase in poor metabolizers, but no association of drug with Torsade de Pointes.Details
Cytochrome P450 2D6CYP2D6*21Not Available2573insCEffect InferredPoor drug metabolizer, greater QTc interval increase in poor metabolizers, but no association of drug with Torsade de Pointes.Details
Cytochrome P450 2D6CYP2D6*31Not Available-1770G>A / -1584C>G  … show all Effect InferredPoor drug metabolizer, greater QTc interval increase in poor metabolizers, but no association of drug with Torsade de Pointes.Details
Cytochrome P450 2D6CYP2D6*36Not Available100C>T / -1426C>T  … show all Effect InferredPoor drug metabolizer, greater QTc interval increase in poor metabolizers, but no association of drug with Torsade de Pointes.Details
Cytochrome P450 2D6CYP2D6*38Not Available2587_2590delGACTEffect InferredPoor drug metabolizer, greater QTc interval increase in poor metabolizers, but no association of drug with Torsade de Pointes.Details
Cytochrome P450 2D6CYP2D6*40Not Available1863_1864ins(TTT CGC CCC)2Effect InferredPoor drug metabolizer, greater QTc interval increase in poor metabolizers, but no association of drug with Torsade de Pointes.Details
Cytochrome P450 2D6CYP2D6*42Not Available3259_3260insGTEffect InferredPoor drug metabolizer, greater QTc interval increase in poor metabolizers, but no association of drug with Torsade de Pointes.Details
Cytochrome P450 2D6CYP2D6*44Not Available2950G>CEffect InferredPoor drug metabolizer, greater QTc interval increase in poor metabolizers, but no association of drug with Torsade de Pointes.Details
Cytochrome P450 2D6CYP2D6*47Not Available100C>T / -1426C>T  … show all Effect InferredPoor drug metabolizer, greater QTc interval increase in poor metabolizers, but no association of drug with Torsade de Pointes.Details
Cytochrome P450 2D6CYP2D6*51Not Available-1584C>G / -1235A>G  … show all Effect InferredPoor drug metabolizer, greater QTc interval increase in poor metabolizers, but no association of drug with Torsade de Pointes.Details
Cytochrome P450 2D6CYP2D6*56Not Available3201C>TEffect InferredPoor drug metabolizer, greater QTc interval increase in poor metabolizers, but no association of drug with Torsade de Pointes.Details
Cytochrome P450 2D6CYP2D6*57Not Available100C>T / 310G>T  … show all Effect InferredPoor drug metabolizer, greater QTc interval increase in poor metabolizers, but no association of drug with Torsade de Pointes.Details
Cytochrome P450 2D6CYP2D6*62Not Available4044C>TEffect InferredPoor drug metabolizer, greater QTc interval increase in poor metabolizers, but no association of drug with Torsade de Pointes.Details
Cytochrome P450 2D6CYP2D6*68ANot Available-1426C>T / -1235A>G  … show all Effect InferredPoor drug metabolizer, greater QTc interval increase in poor metabolizers, but no association of drug with Torsade de Pointes.Details
Cytochrome P450 2D6CYP2D6*68BNot AvailableSimilar but not identical switch region compared to CYP2D6*68A. Found in tandem arrangement with CYP2D6*4.Effect InferredPoor drug metabolizer, greater QTc interval increase in poor metabolizers, but no association of drug with Torsade de Pointes.Details
Cytochrome P450 2D6CYP2D6*69Not Available2988G>A / -1426C>T  … show all Effect InferredPoor drug metabolizer, greater QTc interval increase in poor metabolizers, but no association of drug with Torsade de Pointes.Details
Cytochrome P450 2D6CYP2D6*92Not Available1995delCEffect InferredPoor drug metabolizer, greater QTc interval increase in poor metabolizers, but no association of drug with Torsade de Pointes.Details
Cytochrome P450 2D6CYP2D6*100Not Available-1426C>T / -1235A>G  … show all Effect InferredPoor drug metabolizer, greater QTc interval increase in poor metabolizers, but no association of drug with Torsade de Pointes.Details
Cytochrome P450 2D6CYP2D6*101Not Available-1426C>T / -1235A>G  … show all Effect InferredPoor drug metabolizer, greater QTc interval increase in poor metabolizers, but no association of drug with Torsade de Pointes.Details

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
AlcuroniumThe risk or severity of adverse effects can be increased when Tolterodine is combined with Alcuronium.Experimental
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
AlphaprodineThe risk or severity of adverse effects can be increased when Tolterodine is combined with Alphaprodine.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
AtracuriumThe risk or severity of adverse effects can be increased when Tolterodine is combined with Atracurium.Experimental, Investigational
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
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, Investigational
BoceprevirThe serum concentration of Tolterodine can be increased when it is combined with Boceprevir.Approved, Withdrawn
BornaprineThe risk or severity of adverse effects can be increased when Bornaprine is combined with Tolterodine.Experimental
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, Investigational, 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, Investigational
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
CrisaboroleThe metabolism of Tolterodine can be decreased when combined with Crisaborole.Approved
CrizotinibTolterodine may increase the QTc-prolonging activities of Crizotinib.Approved
CyclopenthiazideThe serum concentration of Cyclopenthiazide can be increased when it is combined with Tolterodine.Experimental
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
DexetimideThe risk or severity of adverse effects can be increased when Dexetimide is combined with Tolterodine.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, Investigational, Withdrawn
DezocineThe risk or severity of adverse effects can be increased when Tolterodine is combined with Dezocine.Approved, Investigational
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
DistigmineThe therapeutic efficacy of Tolterodine can be decreased when used in combination with Distigmine.Experimental
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
DosulepinThe metabolism of Tolterodine can be decreased when combined with Dosulepin.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 metabolism of Tolterodine can be decreased when combined with Efavirenz.Approved, Investigational
EliglustatTolterodine may increase the QTc-prolonging activities of Eliglustat.Approved
EluxadolineTolterodine may increase the constipating activities of Eluxadoline.Approved
EmeproniumThe risk or severity of adverse effects can be increased when Tolterodine is combined with Emepronium.Experimental
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 metabolism of Tolterodine can be decreased when combined with Eslicarbazepine acetate.Approved
EsomeprazoleThe metabolism of Tolterodine can be decreased when combined with Esomeprazole.Approved, Investigational
EtanautineThe risk or severity of adverse effects can be increased when Tolterodine is combined with Etanautine.Experimental
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 metabolism of Tolterodine can be decreased when combined with Etravirine.Approved
EtybenzatropineThe risk or severity of adverse effects can be increased when Tolterodine is combined with Etybenzatropine.Experimental
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
GallamineThe risk or severity of adverse effects can be increased when Tolterodine is combined with Gallamine.Experimental
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
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, Investigational
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, Investigational
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
IpidacrineThe therapeutic efficacy of Tolterodine can be decreased when used in combination with Ipidacrine.Experimental
Ipratropium bromideThe risk or severity of adverse effects can be increased when Ipratropium bromide is combined with 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, Investigational, 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, Investigational
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, Investigational
LevorphanolThe risk or severity of adverse effects can be increased when Tolterodine is combined with Levorphanol.Approved
LobeglitazoneThe metabolism of Tolterodine can be decreased when combined with Lobeglitazone.Approved, Investigational
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
ManidipineThe metabolism of Tolterodine can be decreased when combined with Manidipine.Approved, Investigational
MazaticolThe risk or severity of adverse effects can be increased when Tolterodine is combined with Mazaticol.Experimental
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
MeptazinolThe risk or severity of adverse effects can be increased when Tolterodine is combined with Meptazinol.Experimental
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, Investigational
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
Methylscopolamine bromideThe risk or severity of adverse effects can be increased when Tolterodine is combined with Methylscopolamine bromide.Approved
MetixeneThe risk or severity of adverse effects can be increased when Tolterodine is combined with Metixene.Approved
MetoclopramideThe therapeutic efficacy of Tolterodine can be decreased when used in combination with Metoclopramide.Approved, Investigational
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, Investigational
MidostaurinThe metabolism of Tolterodine can be decreased when combined with Midostaurin.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 metabolism of Tolterodine can be decreased when 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
NabiloneTolterodine may increase the tachycardic activities of Nabilone.Approved, Investigational
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
NicomorphineThe risk or severity of adverse effects can be increased when Tolterodine is combined with Nicomorphine.Experimental
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
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
OtiloniumThe risk or severity of adverse effects can be increased when Tolterodine is combined with Otilonium.Experimental, Investigational
OxitropiumThe risk or severity of adverse effects can be increased when Tolterodine is combined with Oxitropium.Investigational
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
ParaoxonThe therapeutic efficacy of Tolterodine can be decreased when used in combination with Paraoxon.Experimental
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
PhenazocineThe risk or severity of adverse effects can be increased when Tolterodine is combined with Phenazocine.Experimental
PhenglutarimideThe risk or severity of adverse effects can be increased when Phenglutarimide is combined with Tolterodine.Experimental
PhenobarbitalThe metabolism of Tolterodine can be increased when combined with Phenobarbital.Approved
PhenoperidineThe risk or severity of adverse effects can be increased when Tolterodine is combined with Phenoperidine.Experimental
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.Approved, 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, Investigational
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
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, Vet 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.Investigational, 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, Investigational
TacrineThe therapeutic efficacy of Tolterodine can be decreased when used in combination with Tacrine.Investigational, 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, Withdrawn
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, Withdrawn
TicagrelorThe metabolism of Tolterodine can be decreased when combined with Ticagrelor.Approved
TiclopidineThe metabolism of Tolterodine can be decreased when combined with Ticlopidine.Approved
TilidineThe risk or severity of adverse effects can be increased when Tolterodine is combined with Tilidine.Experimental
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
TopiroxostatThe metabolism of Tolterodine can be decreased when combined with Topiroxostat.Approved, Investigational
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, Investigational
TrimethoprimThe metabolism of Tolterodine can be decreased when combined with Trimethoprim.Approved, Vet Approved
TropatepineThe risk or severity of adverse effects can be increased when Tolterodine is combined with Tropatepine.Experimental
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
ZucapsaicinThe metabolism of Tolterodine can be decreased when combined with Zucapsaicin.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 References
Not Available
External Links
Human Metabolome Database
HMDB15170
KEGG Drug
D00646
KEGG Compound
C07750
PubChem Compound
443879
PubChem Substance
46508059
ChemSpider
391967
BindingDB
50165008
ChEBI
9622
ChEMBL
CHEMBL1382
Therapeutic Targets Database
DAP000376
PharmGKB
PA164746757
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Tolterodine
ATC Codes
G04BD07 — Tolterodine
AHFS Codes
  • 86:12.04 — Antimuscarinics
  • 86:12.00 — Genitourinary Smooth Muscle Relaxants
FDA label
Download (94.9 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
1CompletedNot AvailableOveractive Bladder1
1CompletedNot AvailableUrinary Bladder, Overactive1
1CompletedBasic ScienceGenotype Guided(HNF4a) / Healthy Volunteers1
1CompletedDiagnosticOveractive Bladder1
1CompletedTreatmentHealthy Volunteers1
1CompletedTreatmentIncontinence1
1CompletedTreatmentOveractive Bladder1
1TerminatedTreatmentOveractive Bladder / Overactive Urinary Bladder1
1, 2CompletedBasic SciencePain, Neuropathic1
2CompletedTreatmentHealth1
2CompletedTreatmentOveractive Bladder5
2CompletedTreatmentUreteral Stent Discomfort1
2CompletedTreatmentUrinary Bladder, Overactive2
2TerminatedTreatmentOveractive Bladder / Urinary Incontinence (UI)1
2, 3CompletedNot AvailableOveractive Bladder1
2, 3CompletedTreatmentDisorder of Urinary Stent1
2, 3CompletedTreatmentLower Urinary Tract Symptoms (LUTS) / Overactive Bladder1
3CompletedBasic ScienceLow Back Pain (LBP)1
3CompletedTreatmentOveractive Bladder4
3CompletedTreatmentPain1
3CompletedTreatmentUrinary Bladder, Overactive6
3CompletedTreatmentUrinary Incontinence (UI)1
3RecruitingTreatmentPelvic Organ Prolapse (POP)1
4Active Not RecruitingTreatmentUreteral Obstruction1
4CompletedNot AvailableHealthy Volunteers / Pharmacokinetics of Mirabegron and Tolterodine1
4CompletedTreatmentBenign Prostatic Hyperplasia (BPH)1
4CompletedTreatmentCognition / Memory1
4CompletedTreatmentHealthy Volunteers1
4CompletedTreatmentOveractive Bladder4
4CompletedTreatmentOveractive Bladder (OAB)3
4CompletedTreatmentUrinary Bladder, Overactive1
4CompletedTreatmentUrinary Incontinence (UI)1
4RecruitingTreatmentPain, Chronic2
4RecruitingTreatmentUrge Incontinence / Urinary Incontinence, Urge1
4TerminatedTreatmentOveractive Bladder1
4TerminatedTreatmentUrinary Incontinence (UI)1
4Unknown StatusTreatmentMixed Urinary Incontinence / Urinary Incontinence, Urge / Urinary Incontinence,Stress1
4Unknown StatusTreatmentOveractive Bladder1
Not AvailableCompletedNot AvailableOveractive Bladder1
Not AvailableCompletedNot AvailableOveractive Bladder / Urinary Bladder Diseases / Urinary Bladder Overactive / Urologic Diseases1
Not AvailableCompletedNot AvailableUrinary Bladder, Overactive1
Not AvailableCompletedTreatmentAntimuscarinic Drug1
Not AvailableCompletedTreatmentOveractive Bladder1
Not AvailableCompletedTreatmentUrgency-frequency Syndrome1
Not AvailableCompletedTreatmentUrinary Incontinence (UI)1
Not AvailableNot Yet RecruitingTreatmentOveractive Bladder / Spinal Vascular Disorder Nos1
Not AvailableRecruitingTreatmentUrinary Incontinence, Urge1
Not AvailableUnknown StatusDiagnosticBladder Dysfunction / Urinary Incontinence (UI)1
Not AvailableUnknown StatusTreatmentProstatitis1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Dosage forms
FormRouteStrength
TabletOral1 mg
TabletOral2 mg
Capsule, extended releaseOral2 mg
Capsule, extended releaseOral4 mg
Capsule, extended releaseOral4 mg/1
Capsule, extended releaseOral2 mg/1
Tablet, film coatedOral1 mg/1
Tablet, film coatedOral2 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)
US5382600No1995-03-252012-03-25Us
CA2311755No2010-03-232019-08-26Canada
CA1340223No1998-12-152015-12-15Canada
US6630162Yes2000-05-112020-05-11Us
US6770295Yes2000-02-262020-02-26Us
US6911217Yes2000-05-112020-05-11Us

Properties

State
Solid
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 FiveNoChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleNoChemAxon
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)

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSNot Available
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available
LC-MS/MS Spectrum - LC-ESI-qTof , PositiveLC-MS/MSNot Available
MS/MS Spectrum - , positiveLC-MS/MSsplash10-000t-2911000000-6586d7c95e03f623dbf4

Taxonomy

Description
This compound belongs to the class of organic compounds known as diphenylmethanes. These are compounds containing a diphenylmethane moiety, which consists of a methane wherein two hydrogen atoms are replaced by two phenyl groups.
Kingdom
Organic compounds
Super Class
Benzenoids
Class
Benzene and substituted derivatives
Sub Class
Diphenylmethanes
Direct Parent
Diphenylmethanes
Alternative Parents
Para cresols / Toluenes / Aralkylamines / 1-hydroxy-2-unsubstituted benzenoids / Trialkylamines / Organopnictogen compounds / Organooxygen compounds / Hydrocarbon derivatives
Substituents
Diphenylmethane / P-cresol / 1-hydroxy-2-unsubstituted benzenoid / Phenol / Aralkylamine / Toluene / Tertiary amine / Tertiary aliphatic amine / Amine / Hydrocarbon derivative
Molecular Framework
Aromatic homomonocyclic compounds
External Descriptors
tertiary amine (CHEBI:9622)

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...
Gene Name
CHRM3
Uniprot ID
P20309
Uniprot Name
Muscarinic acetylcholine receptor M3
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...
Gene Name
CHRM2
Uniprot ID
P08172
Uniprot Name
Muscarinic acetylcholine receptor M2
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...
Gene Name
CHRM5
Uniprot ID
P08912
Uniprot Name
Muscarinic acetylcholine receptor M5
Molecular Weight
60073.205 Da
References
  1. Maruyama S, Oki T, Otsuka A, Shinbo H, Ozono S, Kageyama S, Mikami Y, Araki I, Takeda M, Masuyama K, Yamada S: Human muscarinic receptor binding characteristics of antimuscarinic agents to treat overactive bladder. J Urol. 2006 Jan;175(1):365-9. [PubMed:16406943]
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Antagonist
General Function
Phosphatidylinositol phospholipase c activity
Specific Function
The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the...
Gene Name
CHRM1
Uniprot ID
P11229
Uniprot Name
Muscarinic acetylcholine receptor M1
Molecular Weight
51420.375 Da
References
  1. 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...
Gene Name
CHRM4
Uniprot ID
P08173
Uniprot Name
Muscarinic acetylcholine receptor M4
Molecular Weight
53048.65 Da
References
  1. Maruyama S, Oki T, Otsuka A, Shinbo H, Ozono S, Kageyama S, Mikami Y, Araki I, Takeda M, Masuyama K, Yamada S: Human muscarinic receptor binding characteristics of antimuscarinic agents to treat overactive bladder. J Urol. 2006 Jan;175(1):365-9. [PubMed:16406943]

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...
Gene Name
CYP2D6
Uniprot ID
P10635
Uniprot Name
Cytochrome P450 2D6
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 react...
Gene Name
CYP3A4
Uniprot ID
P08684
Uniprot Name
Cytochrome P450 3A4
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 un...
Gene Name
CYP2C9
Uniprot ID
P11712
Uniprot Name
Cytochrome P450 2C9
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 im...
Gene Name
CYP2C19
Uniprot ID
P33261
Uniprot Name
Cytochrome P450 2C19
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]

Drug created on June 13, 2005 07:24 / Updated on November 19, 2017 20:34