Identification

Name
Darifenacin
Accession Number
DB00496  (APRD00903)
Type
Small Molecule
Groups
Approved, Investigational
Description

Darifenacin (Enablex®, Novartis) is a medication used to treat urinary incontinence.

Darifenacin works by blocking the M3 muscarinic acetylcholine receptor, which is primarily responsible for bladder muscle contractions. It thereby decreases the urgency to urinate. It should not be used in people with urinary retention.

It is not known whether this selectivity for the M3 receptor translates into any clinical advantage when treating symptoms of overactive bladder syndrome.

Structure
Thumb
Synonyms
  • (S)-1-(2-(2,3-dihydro-5-Benzofuranyl)ethyl)-alpha,alpha-diphenyl-3-pyrrolidineacetamide
  • Darifenacin
  • Darifenacina
  • Darifénacine
  • Darifenacinum
External IDs
UK 88525 / UK 88525-04
Product Ingredients
IngredientUNIICASInChI Key
Darifenacin HydrobromideCR02EYQ8GV133099-07-7UQAVIASOPREUIT-VQIWEWKSSA-N
Product Images
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
DarifenacinTablet, extended release15 mg/1OralActavis Pharma Company2016-03-15Not applicableUs
DarifenacinTablet, extended release7.5 mg/1OralActavis Pharma Company2016-03-15Not applicableUs
EnablexTablet, extended release15 mg/1OralLake Erie Medical &Surgical Supply Dba Quality Care Products Llc2012-03-052017-09-22Us
EnablexTablet, extended release7.5 mgOralMerus Labs Luxco S. A R.L.2006-04-06Not applicableCanada
EnablexTablet, extended release15 mg/1OralWarner Chilcott2004-12-22Not applicableUs00430 0171 15 nlmimage10 153a0af0
EnablexTablet, extended release15 mg/1OralPhysicians Total Care, Inc.2005-07-20Not applicableUs
EnablexTablet, extended release15 mgOralMerus Labs Luxco S. A R.L.2006-04-06Not applicableCanada
EnablexTablet, extended release7.5 mg/1OralPhysicians Total Care, Inc.2006-11-06Not applicableUs
EnablexTablet, extended release7.5 mg/1OralWarner Chilcott2004-12-22Not applicableUs00430 0170 15 nlmimage10 993acca6
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Apo-darifenacinTablet, extended release7.5 mgOralApotex CorporationNot applicableNot applicableCanada
Apo-darifenacinTablet, extended release15 mgOralApotex CorporationNot applicableNot applicableCanada
DarifenacinTablet, extended release7.5 mg/1OralMacleods Pharmaceuticals Limited2017-07-29Not applicableUs
DarifenacinTablet, extended release15 mg/1OralJubilant Cadista Pharmaceuticals Inc.2016-10-12Not applicableUs
DarifenacinTablet, extended release7.5 mg/1OralCipla Limited2016-09-01Not applicableUs
DarifenacinTablet, extended release15 mg/1OralMacleods Pharmaceuticals Limited2017-07-29Not applicableUs
DarifenacinTablet, film coated, extended release7.5 mg/1OralAurobindo Pharma2016-09-19Not applicableUs
DarifenacinTablet, extended release7.5 mg/1OralTorrent Pharmaceuticals Limited2016-11-18Not applicableUs
DarifenacinTablet, extended release15 mg/1OralCipla Limited2016-09-01Not applicableUs
DarifenacinTablet, extended release7.5 mg/1OralJubilant Cadista Pharmaceuticals Inc.2016-10-12Not applicableUs
International/Other Brands
Emselex (Novartis) / Xelena (Dr. Reddy's)
Categories
UNII
APG9819VLM
CAS number
133099-04-4
Weight
Average: 426.55
Monoisotopic: 426.230728214
Chemical Formula
C28H30N2O2
InChI Key
HXGBXQDTNZMWGS-RUZDIDTESA-N
InChI
InChI=1S/C28H30N2O2/c29-27(31)28(23-7-3-1-4-8-23,24-9-5-2-6-10-24)25-14-17-30(20-25)16-13-21-11-12-26-22(19-21)15-18-32-26/h1-12,19,25H,13-18,20H2,(H2,29,31)/t25-/m1/s1
IUPAC Name
2-[(3S)-1-[2-(2,3-dihydro-1-benzofuran-5-yl)ethyl]pyrrolidin-3-yl]-2,2-diphenylacetamide
SMILES
NC(=O)C([[email protected]@H]1CCN(CCC2=CC3=C(OCC3)C=C2)C1)(C1=CC=CC=C1)C1=CC=CC=C1

Pharmacology

Indication

For the treatment of overactive bladder with symptoms of urge urinary incontinence, urgency and frequency.

Structured Indications
Pharmacodynamics

Darifenacin is a competitive muscarinic receptor antagonist. In vitro studies using human recombinant muscarinic receptor subtypes show that darifenacin has greater affinity for the M3 receptor than for the other known muscarinic receptors (9 and 12-fold greater affinity for M3 compared to M1 and M5, respectively, and 59-fold greater affinity for M3 compared to both M2 and M4). Muscarinic receptors play an important role in several major cholinergically mediated functions, including contractions of the urinary bladder smooth muscle and stimulation of salivary secretion. Adverse drug effects such as dry mouth, constipation and abnormal vision may be mediated through effects on M3 receptors in these organs.

Mechanism of action

Darifenacin selectively antagonizes the muscarinic M3 receptor. M3 receptors are involved in contraction of human bladder and gastrointestinal smooth muscle, saliva production, and iris sphincter function.

TargetActionsOrganism
AMuscarinic acetylcholine receptor M3
antagonist
Human
UMuscarinic acetylcholine receptor M1
antagonist
Human
UMuscarinic acetylcholine receptor M2
antagonist
Human
UMuscarinic acetylcholine receptor M4
antagonist
Human
UMuscarinic acetylcholine receptor M5
antagonist
Human
Absorption

The mean oral bioavailability at steady state is estimated to be 15% and 19% for 7.5 mg and 15 mg tablets, respectively.

Volume of distribution
  • 163 L
Protein binding

Darifenacin is approximately 98% bound to plasma proteins (primarily to alpha-1-acid-glycoprotein).

Metabolism

Hepatic. Primarily mediated by the cytochrome P450 enzymes CYP2D6 and CYP3A4.

Route of elimination
Not Available
Half life

The elimination half-life of darifenacin following chronic dosing is approximately 13-19 hours.

Clearance
  • 40 L/h [extensive metabolizers]
  • 32 L/h [poor metabolizers]
Toxicity

Overdosage can potentially result in severe central anticholinergic effects.

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.Details
Cytochrome P450 2D6CYP2D6*4Not AvailableC alleleEffect InferredPoor drug metabolizer.Details
Cytochrome P450 2D6CYP2D6*5Not AvailableWhole-gene deletionEffect InferredPoor drug metabolizer.Details
Cytochrome P450 2D6CYP2D6*6Not Available1707delTEffect InferredPoor drug metabolizer.Details
Cytochrome P450 2D6CYP2D6*7Not Available2935A>CEffect InferredPoor drug metabolizer.Details
Cytochrome P450 2D6CYP2D6*8Not Available1758G>TEffect InferredPoor drug metabolizer.Details
Cytochrome P450 2D6CYP2D6*11Not Available883G>CEffect InferredPoor drug metabolizer.Details
Cytochrome P450 2D6CYP2D6*12Not Available124G>AEffect InferredPoor drug metabolizer.Details
Cytochrome P450 2D6CYP2D6*13Not AvailableCYP2D7/2D6 hybrid gene structureEffect InferredPoor drug metabolizer.Details
Cytochrome P450 2D6CYP2D6*14ANot Available1758G>AEffect InferredPoor drug metabolizer.Details
Cytochrome P450 2D6CYP2D6*15Not Available137insT, 137_138insTEffect InferredPoor drug metabolizer.Details
Cytochrome P450 2D6CYP2D6*19Not Available2539_2542delAACTEffect InferredPoor drug metabolizer.Details
Cytochrome P450 2D6CYP2D6*20Not Available1973_1974insGEffect InferredPoor drug metabolizer.Details
Cytochrome P450 2D6CYP2D6*21Not Available2573insCEffect InferredPoor drug metabolizer.Details
Cytochrome P450 2D6CYP2D6*31Not Available-1770G>A / -1584C>G  … show all Effect InferredPoor drug metabolizer.Details
Cytochrome P450 2D6CYP2D6*36Not Available100C>T / -1426C>T  … show all Effect InferredPoor drug metabolizer.Details
Cytochrome P450 2D6CYP2D6*38Not Available2587_2590delGACTEffect InferredPoor drug metabolizer.Details
Cytochrome P450 2D6CYP2D6*40Not Available1863_1864ins(TTT CGC CCC)2Effect InferredPoor drug metabolizer.Details
Cytochrome P450 2D6CYP2D6*42Not Available3259_3260insGTEffect InferredPoor drug metabolizer.Details
Cytochrome P450 2D6CYP2D6*44Not Available2950G>CEffect InferredPoor drug metabolizer.Details
Cytochrome P450 2D6CYP2D6*47Not Available100C>T / -1426C>T  … show all Effect InferredPoor drug metabolizer.Details
Cytochrome P450 2D6CYP2D6*51Not Available-1584C>G / -1235A>G  … show all Effect InferredPoor drug metabolizer.Details
Cytochrome P450 2D6CYP2D6*56Not Available3201C>TEffect InferredPoor drug metabolizer.Details
Cytochrome P450 2D6CYP2D6*57Not Available100C>T / 310G>T  … show all Effect InferredPoor drug metabolizer.Details
Cytochrome P450 2D6CYP2D6*62Not Available4044C>TEffect InferredPoor drug metabolizer.Details
Cytochrome P450 2D6CYP2D6*68ANot Available-1426C>T / -1235A>G  … show all Effect InferredPoor drug metabolizer.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.Details
Cytochrome P450 2D6CYP2D6*69Not Available2988G>A / -1426C>T  … show all Effect InferredPoor drug metabolizer.Details
Cytochrome P450 2D6CYP2D6*92Not Available1995delCEffect InferredPoor drug metabolizer.Details
Cytochrome P450 2D6CYP2D6*100Not Available-1426C>T / -1235A>G  … show all Effect InferredPoor drug metabolizer.Details
Cytochrome P450 2D6CYP2D6*101Not Available-1426C>T / -1235A>G  … show all Effect InferredPoor drug metabolizer.Details
Cytochrome P450 3A4CYP3A4*20Not Available1461_1462insAEffect InferredPoor drug metabolizer.Details
Cytochrome P450 3A4CYP3A4*26Not Available802C>TEffect InferredPoor drug metabolizer.Details

Interactions

Drug Interactions
DrugInteractionDrug group
1,10-PhenanthrolineThe therapeutic efficacy of Darifenacin can be decreased when used in combination with 1,10-Phenanthroline.Experimental
4-MethoxyamphetamineThe metabolism of 4-Methoxyamphetamine can be decreased when combined with Darifenacin.Experimental, Illicit
AbirateroneThe serum concentration of Darifenacin can be increased when it is combined with Abiraterone.Approved
AcetaminophenThe metabolism of Acetaminophen can be decreased when combined with Darifenacin.Approved
AcetylcholineThe metabolism of Acetylcholine can be decreased when combined with Darifenacin.Approved
AclidiniumAclidinium may increase the anticholinergic activities of Darifenacin.Approved
AjmalineThe metabolism of Ajmaline can be decreased when combined with Darifenacin.Approved, Investigational
AlcuroniumThe risk or severity of adverse effects can be increased when Darifenacin is combined with Alcuronium.Experimental
AlfentanilThe risk or severity of adverse effects can be increased when Darifenacin is combined with Alfentanil.Approved, Illicit
AlmotriptanThe metabolism of Almotriptan can be decreased when combined with Darifenacin.Approved, Investigational
AlogliptinThe metabolism of Alogliptin can be decreased when combined with Darifenacin.Approved
AlphacetylmethadolThe risk or severity of adverse effects can be increased when Darifenacin is combined with Alphacetylmethadol.Experimental, Illicit
AlphaprodineThe risk or severity of adverse effects can be increased when Darifenacin is combined with Alphaprodine.Illicit
AlprenololThe metabolism of Alprenolol can be decreased when combined with Darifenacin.Approved, Withdrawn
AmbenoniumThe therapeutic efficacy of Darifenacin can be decreased when used in combination with Ambenonium.Approved
AminophenazoneThe metabolism of Aminophenazone can be decreased when combined with Darifenacin.Approved, Withdrawn
AmiodaroneThe metabolism of Darifenacin can be decreased when combined with Amiodarone.Approved, Investigational
AmitriptylineThe metabolism of Amitriptyline can be decreased when combined with Darifenacin.Approved
AmoxapineThe metabolism of Amoxapine can be decreased when combined with Darifenacin.Approved
AmphetamineThe metabolism of Amphetamine can be decreased when combined with Darifenacin.Approved, Illicit
AmprenavirThe metabolism of Amprenavir can be decreased when combined with Darifenacin.Approved
AmsacrineThe metabolism of Amsacrine can be decreased when combined with Darifenacin.Approved
Anisotropine MethylbromideThe risk or severity of adverse effects can be increased when Darifenacin is combined with Anisotropine Methylbromide.Approved
AntipyrineThe metabolism of Antipyrine can be decreased when combined with Darifenacin.Approved
AprepitantThe serum concentration of Darifenacin can be increased when it is combined with Aprepitant.Approved, Investigational
AprindineThe metabolism of Aprindine can be decreased when combined with Darifenacin.Approved
ArformoterolThe metabolism of Arformoterol can be decreased when combined with Darifenacin.Approved, Investigational
AripiprazoleThe serum concentration of Aripiprazole can be increased when it is combined with Darifenacin.Approved, Investigational
ArtemetherThe metabolism of Artemether can be decreased when combined with Darifenacin.Approved
AstemizoleThe metabolism of Astemizole can be decreased when combined with Darifenacin.Approved, Withdrawn
AtazanavirThe metabolism of Darifenacin can be decreased when combined with Atazanavir.Approved, Investigational
AtomoxetineThe metabolism of Darifenacin can be decreased when combined with Atomoxetine.Approved
AtracuriumThe risk or severity of adverse effects can be increased when Darifenacin is combined with Atracurium.Experimental, Investigational
Atracurium besylateThe risk or severity of adverse effects can be increased when Darifenacin is combined with Atracurium besylate.Approved
AtropineThe risk or severity of adverse effects can be increased when Atropine is combined with Darifenacin.Approved, Vet Approved
AzelastineThe metabolism of Azelastine can be decreased when combined with Darifenacin.Approved
BenactyzineThe risk or severity of adverse effects can be increased when Darifenacin is combined with Benactyzine.Withdrawn
BendroflumethiazideThe serum concentration of Bendroflumethiazide can be increased when it is combined with Darifenacin.Approved
BenzatropineThe risk or severity of adverse effects can be increased when Benzatropine is combined with Darifenacin.Approved
Benzyl alcoholThe metabolism of Benzyl alcohol can be decreased when combined with Darifenacin.Approved
BepridilThe metabolism of Bepridil can be decreased when combined with Darifenacin.Approved, Withdrawn
BetaxololThe metabolism of Betaxolol can be decreased when combined with Darifenacin.Approved
BezitramideThe risk or severity of adverse effects can be increased when Darifenacin is combined with Bezitramide.Experimental, Illicit, Withdrawn
BiperidenThe risk or severity of adverse effects can be increased when Biperiden is combined with Darifenacin.Approved, Investigational
BisoprololThe metabolism of Bisoprolol can be decreased when combined with Darifenacin.Approved
BoceprevirThe metabolism of Darifenacin can be decreased when combined with Boceprevir.Approved, Withdrawn
BornaprineThe risk or severity of adverse effects can be increased when Bornaprine is combined with Darifenacin.Experimental
BortezomibThe metabolism of Darifenacin can be decreased when combined with Bortezomib.Approved, Investigational
BosentanThe serum concentration of Darifenacin can be decreased when it is combined with Bosentan.Approved, Investigational
Botulinum Toxin Type ADarifenacin may increase the anticholinergic activities of Botulinum Toxin Type A.Approved, Investigational
Botulinum Toxin Type BDarifenacin may increase the anticholinergic activities of Botulinum Toxin Type B.Approved
BrexpiprazoleThe serum concentration of Brexpiprazole can be increased when it is combined with Darifenacin.Approved
BrompheniramineThe metabolism of Brompheniramine can be decreased when combined with Darifenacin.Approved
BufuralolThe metabolism of Bufuralol can be decreased when combined with Darifenacin.Experimental, Investigational
BupivacaineThe metabolism of Bupivacaine can be decreased when combined with Darifenacin.Approved, Investigational
BuprenorphineThe metabolism of Buprenorphine can be decreased when combined with Darifenacin.Approved, Illicit, Investigational, Vet Approved
BupropionThe metabolism of Darifenacin can be decreased when combined with Bupropion.Approved
BuspironeThe metabolism of Buspirone can be decreased when combined with Darifenacin.Approved, Investigational
ButorphanolThe risk or severity of adverse effects can be increased when Darifenacin is combined with Butorphanol.Approved, Illicit, Vet Approved
CaffeineThe metabolism of Caffeine can be decreased when combined with Darifenacin.Approved
CaptoprilThe metabolism of Captopril can be decreased when combined with Darifenacin.Approved
CarbamazepineThe metabolism of Darifenacin can be increased when combined with Carbamazepine.Approved, Investigational
CarfentanilThe risk or severity of adverse effects can be increased when Darifenacin is combined with Carfentanil.Illicit, Investigational, Vet Approved
CariprazineThe metabolism of Cariprazine can be decreased when combined with Darifenacin.Approved
CarteololThe metabolism of Carteolol can be decreased when combined with Darifenacin.Approved
CarvedilolThe metabolism of Carvedilol can be decreased when combined with Darifenacin.Approved, Investigational
CelecoxibThe metabolism of Darifenacin can be decreased when combined with Celecoxib.Approved, Investigational
CephalexinThe metabolism of Cephalexin can be decreased when combined with Darifenacin.Approved, Vet Approved
CeritinibThe serum concentration of Darifenacin can be increased when it is combined with Ceritinib.Approved
CevimelineThe metabolism of Cevimeline can be decreased when combined with Darifenacin.Approved
ChlordiazepoxideThe metabolism of Chlordiazepoxide can be decreased when combined with Darifenacin.Approved, Illicit
ChloroquineThe metabolism of Chloroquine can be decreased when combined with Darifenacin.Approved, Vet Approved
ChlorothiazideThe serum concentration of Chlorothiazide can be increased when it is combined with Darifenacin.Approved, Vet Approved
ChlorphenamineThe metabolism of Chlorphenamine can be decreased when combined with Darifenacin.Approved
ChlorphenoxamineThe risk or severity of adverse effects can be increased when Darifenacin is combined with Chlorphenoxamine.Withdrawn
ChlorpromazineThe metabolism of Darifenacin can be decreased when combined with Chlorpromazine.Approved, Vet Approved
ChlorthalidoneThe serum concentration of Chlorthalidone can be increased when it is combined with Darifenacin.Approved
ChlorzoxazoneThe metabolism of Chlorzoxazone can be decreased when combined with Darifenacin.Approved
CholecalciferolThe metabolism of Darifenacin can be decreased when combined with Cholecalciferol.Approved, Nutraceutical
CilostazolThe metabolism of Cilostazol can be decreased when combined with Darifenacin.Approved
CimetidineThe metabolism of Darifenacin can be decreased when combined with Cimetidine.Approved
CimetropiumDarifenacin may increase the anticholinergic activities of Cimetropium.Experimental, Investigational
CinacalcetThe metabolism of Darifenacin can be decreased when combined with Cinacalcet.Approved
CinnarizineThe metabolism of Cinnarizine can be decreased when combined with Darifenacin.Approved, Investigational
CitalopramThe metabolism of Citalopram can be decreased when combined with Darifenacin.Approved
ClarithromycinThe metabolism of Darifenacin can be decreased when combined with Clarithromycin.Approved
ClemastineThe metabolism of Darifenacin can be decreased when combined with Clemastine.Approved
ClevidipineThe metabolism of Clevidipine can be decreased when combined with Darifenacin.Approved
ClobazamThe metabolism of Darifenacin can be decreased when combined with Clobazam.Approved, Illicit
ClomipramineThe metabolism of Clomipramine can be decreased when combined with Darifenacin.Approved, Vet Approved
ClonidineThe metabolism of Clonidine can be decreased when combined with Darifenacin.Approved
ClotrimazoleThe metabolism of Darifenacin can be decreased when combined with Clotrimazole.Approved, Vet Approved
ClozapineThe metabolism of Clozapine can be decreased when combined with Darifenacin.Approved
CobicistatThe serum concentration of Darifenacin can be increased when it is combined with Cobicistat.Approved
CocaineThe metabolism of Darifenacin can be decreased when combined with Cocaine.Approved, Illicit
CodeineThe therapeutic efficacy of Codeine can be decreased when used in combination with Darifenacin.Approved, Illicit
ConivaptanThe serum concentration of Darifenacin can be increased when it is combined with Conivaptan.Approved, Investigational
CoumaphosThe therapeutic efficacy of Darifenacin can be decreased when used in combination with Coumaphos.Vet Approved
CrizotinibThe metabolism of Darifenacin can be decreased when combined with Crizotinib.Approved
CyclobenzaprineThe metabolism of Cyclobenzaprine can be decreased when combined with Darifenacin.Approved
CyclopenthiazideThe serum concentration of Cyclopenthiazide can be increased when it is combined with Darifenacin.Experimental
CyclopentolateThe risk or severity of adverse effects can be increased when Cyclopentolate is combined with Darifenacin.Approved
CyclophosphamideThe metabolism of Cyclophosphamide can be decreased when combined with Darifenacin.Approved, Investigational
CyclosporineThe metabolism of Darifenacin can be decreased when combined with Cyclosporine.Approved, Investigational, Vet Approved
DabrafenibThe serum concentration of Darifenacin can be decreased when it is combined with Dabrafenib.Approved
DapagliflozinThe metabolism of Dapagliflozin can be decreased when combined with Darifenacin.Approved
DarunavirThe serum concentration of Darifenacin can be increased when it is combined with Darunavir.Approved
DasabuvirThe metabolism of Dasabuvir can be decreased when combined with Darifenacin.Approved
DasatinibThe serum concentration of Darifenacin can be increased when it is combined with Dasatinib.Approved, Investigational
DebrisoquinThe metabolism of Debrisoquin can be decreased when combined with Darifenacin.Approved, Investigational
DecamethoniumThe therapeutic efficacy of Darifenacin can be decreased when used in combination with Decamethonium.Approved
DeferasiroxThe serum concentration of Darifenacin can be decreased when it is combined with Deferasirox.Approved, Investigational
DelavirdineThe metabolism of Darifenacin can be decreased when combined with Delavirdine.Approved
DemecariumThe therapeutic efficacy of Darifenacin can be decreased when used in combination with Demecarium.Approved
DesipramineThe metabolism of Desipramine can be decreased when combined with Darifenacin.Approved
DesloratadineThe risk or severity of adverse effects can be increased when Darifenacin is combined with Desloratadine.Approved, Investigational
DeutetrabenazineThe metabolism of Deutetrabenazine can be decreased when combined with Darifenacin.Approved, Investigational
Dexchlorpheniramine maleateThe metabolism of Dexchlorpheniramine maleate can be decreased when combined with Darifenacin.Approved
DexetimideThe risk or severity of adverse effects can be increased when Dexetimide is combined with Darifenacin.Withdrawn
DexfenfluramineThe metabolism of Dexfenfluramine can be decreased when combined with Darifenacin.Approved, Illicit, Investigational, Withdrawn
DexmethylphenidateThe metabolism of Dexmethylphenidate can be decreased when combined with Darifenacin.Approved
DextroamphetamineThe metabolism of Dextroamphetamine can be decreased when combined with Darifenacin.Approved, Illicit
DextromethorphanThe metabolism of Dextromethorphan can be decreased when combined with Darifenacin.Approved
DextromoramideThe risk or severity of adverse effects can be increased when Darifenacin is combined with Dextromoramide.Experimental, Illicit
DextropropoxypheneThe risk or severity of adverse effects can be increased when Darifenacin is combined with Dextropropoxyphene.Approved, Illicit, Investigational, Withdrawn
DezocineThe risk or severity of adverse effects can be increased when Darifenacin is combined with Dezocine.Approved, Investigational
DichlorvosThe therapeutic efficacy of Darifenacin 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 Darifenacin.Approved
DihydrocodeineThe metabolism of Dihydrocodeine can be decreased when combined with Darifenacin.Approved, Illicit
DihydroergotamineThe metabolism of Darifenacin can be decreased when combined with Dihydroergotamine.Approved
DihydroetorphineThe risk or severity of adverse effects can be increased when Darifenacin is combined with Dihydroetorphine.Experimental, Illicit
DihydromorphineThe risk or severity of adverse effects can be increased when Darifenacin is combined with Dihydromorphine.Experimental, Illicit
DiltiazemThe metabolism of Darifenacin can be decreased when combined with Diltiazem.Approved
DiphenhydramineThe metabolism of Diphenhydramine can be decreased when combined with Darifenacin.Approved
DiphenoxylateThe risk or severity of adverse effects can be increased when Darifenacin is combined with Diphenoxylate.Approved, Illicit
DistigmineThe therapeutic efficacy of Darifenacin can be decreased when used in combination with Distigmine.Experimental
DolasetronThe metabolism of Dolasetron can be decreased when combined with Darifenacin.Approved
DomperidoneThe metabolism of Domperidone can be decreased when combined with Darifenacin.Approved, Investigational, Vet Approved
DonepezilThe therapeutic efficacy of Darifenacin can be decreased when used in combination with Donepezil.Approved
DopamineThe metabolism of Dopamine can be decreased when combined with Darifenacin.Approved
DosulepinThe metabolism of Darifenacin can be decreased when combined with Dosulepin.Approved
DoxazosinThe metabolism of Doxazosin can be decreased when combined with Darifenacin.Approved
DoxepinThe metabolism of Doxepin can be decreased when combined with Darifenacin.Approved
DoxorubicinThe serum concentration of Doxorubicin can be increased when it is combined with Darifenacin.Approved, Investigational
DoxorubicinThe metabolism of Doxorubicin can be decreased when combined with Darifenacin.Approved, Investigational
DoxycyclineThe metabolism of Darifenacin can be decreased when combined with Doxycycline.Approved, Investigational, Vet Approved
DPDPEThe risk or severity of adverse effects can be increased when Darifenacin is combined with DPDPE.Investigational
DronabinolDarifenacin may increase the tachycardic activities of Dronabinol.Approved, Illicit
DronedaroneThe metabolism of Darifenacin can be decreased when combined with Dronedarone.Approved
DuloxetineThe metabolism of Darifenacin can be decreased when combined with Duloxetine.Approved
EchothiophateThe therapeutic efficacy of Darifenacin can be decreased when used in combination with Echothiophate.Approved
EdrophoniumThe therapeutic efficacy of Darifenacin can be decreased when used in combination with Edrophonium.Approved
EletriptanThe metabolism of Eletriptan can be decreased when combined with Darifenacin.Approved, Investigational
EliglustatThe serum concentration of Eliglustat can be increased when it is combined with Darifenacin.Approved
EluxadolineDarifenacin may increase the constipating activities of Eluxadoline.Approved
EmeproniumThe risk or severity of adverse effects can be increased when Darifenacin is combined with Emepronium.Experimental
EnasidenibThe metabolism of Enasidenib can be decreased when combined with Darifenacin.Approved
EncainideThe metabolism of Encainide can be decreased when combined with Darifenacin.Approved, Investigational, Withdrawn
EnclomipheneThe metabolism of Enclomiphene can be decreased when combined with Darifenacin.Investigational
EnzalutamideThe serum concentration of Darifenacin can be decreased when it is combined with Enzalutamide.Approved
EpinastineThe metabolism of Epinastine can be decreased when combined with Darifenacin.Approved, Investigational
ErlotinibThe metabolism of Erlotinib can be decreased when combined with Darifenacin.Approved, Investigational
ErythromycinThe metabolism of Darifenacin can be decreased when combined with Erythromycin.Approved, Vet Approved
EscitalopramThe metabolism of Escitalopram can be decreased when combined with Darifenacin.Approved, Investigational
EsmirtazapineThe metabolism of Esmirtazapine can be decreased when combined with Darifenacin.Investigational
EtanautineThe risk or severity of adverse effects can be increased when Darifenacin is combined with Etanautine.Experimental
EthopropazineThe risk or severity of adverse effects can be increased when Ethopropazine is combined with Darifenacin.Approved
EthylmorphineThe metabolism of Ethylmorphine can be decreased when combined with Darifenacin.Approved, Illicit
EtoricoxibThe metabolism of Etoricoxib can be decreased when combined with Darifenacin.Approved, Investigational
EtorphineThe risk or severity of adverse effects can be increased when Darifenacin is combined with Etorphine.Illicit, Vet Approved
EtybenzatropineThe risk or severity of adverse effects can be increased when Darifenacin is combined with Etybenzatropine.Experimental
FentanylThe risk or severity of adverse effects can be increased when Darifenacin is combined with Fentanyl.Approved, Illicit, Investigational, Vet Approved
FenthionThe therapeutic efficacy of Darifenacin can be decreased when used in combination with Fenthion.Vet Approved
FesoterodineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Darifenacin.Approved
FingolimodThe metabolism of Fingolimod can be decreased when combined with Darifenacin.Approved, Investigational
FlecainideThe metabolism of Flecainide can be decreased when combined with Darifenacin.Approved, Withdrawn
FluconazoleThe metabolism of Darifenacin can be decreased when combined with Fluconazole.Approved
FlunarizineThe metabolism of Flunarizine can be decreased when combined with Darifenacin.Approved
FluoxetineThe metabolism of Darifenacin can be decreased when combined with Fluoxetine.Approved, Vet Approved
FluphenazineThe metabolism of Fluphenazine can be decreased when combined with Darifenacin.Approved
FluvastatinThe metabolism of Fluvastatin can be decreased when combined with Darifenacin.Approved
FluvoxamineThe metabolism of Darifenacin can be decreased when combined with Fluvoxamine.Approved, Investigational
FormoterolThe metabolism of Formoterol can be decreased when combined with Darifenacin.Approved, Investigational
FosamprenavirThe metabolism of Darifenacin can be decreased when combined with Fosamprenavir.Approved
FosaprepitantThe serum concentration of Darifenacin can be increased when it is combined with Fosaprepitant.Approved
FosphenytoinThe metabolism of Darifenacin can be increased when combined with Fosphenytoin.Approved
Fusidic AcidThe serum concentration of Darifenacin can be increased when it is combined with Fusidic Acid.Approved
GalantamineThe therapeutic efficacy of Darifenacin can be decreased when used in combination with Galantamine.Approved
GallamineThe risk or severity of adverse effects can be increased when Darifenacin is combined with Gallamine.Experimental
Gallamine TriethiodideThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Darifenacin.Approved
GefitinibThe metabolism of Gefitinib can be decreased when combined with Darifenacin.Approved, Investigational
Glucagon recombinantThe risk or severity of adverse effects can be increased when Darifenacin is combined with Glucagon recombinant.Approved
GlycopyrroniumDarifenacin may increase the anticholinergic activities of Glycopyrronium.Approved, Investigational, Vet Approved
GranisetronThe metabolism of Granisetron can be decreased when combined with Darifenacin.Approved, Investigational
HalofantrineThe metabolism of Halofantrine can be decreased when combined with Darifenacin.Approved
HaloperidolThe metabolism of Haloperidol can be decreased when combined with Darifenacin.Approved
HalothaneThe metabolism of Halothane can be decreased when combined with Darifenacin.Approved, Vet Approved
HeroinThe risk or severity of adverse effects can be increased when Darifenacin is combined with Heroin.Approved, Illicit, Investigational
HexamethoniumThe risk or severity of adverse effects can be increased when Darifenacin is combined with Hexamethonium.Experimental
HomatropineThe risk or severity of adverse effects can be increased when Darifenacin is combined with Homatropine.Approved
Huperzine AThe therapeutic efficacy of Darifenacin can be decreased when used in combination with Huperzine A.Investigational
HydrochlorothiazideThe serum concentration of Hydrochlorothiazide can be increased when it is combined with Darifenacin.Approved, Vet Approved
HydrocodoneThe metabolism of Hydrocodone can be decreased when combined with Darifenacin.Approved, Illicit
HydroflumethiazideThe serum concentration of Hydroflumethiazide can be increased when it is combined with Darifenacin.Approved, Investigational
HydromorphoneThe metabolism of Hydromorphone can be decreased when combined with Darifenacin.Approved, Illicit
HyoscyamineThe risk or severity of adverse effects can be increased when Hyoscyamine is combined with Darifenacin.Approved
IbrutinibThe metabolism of Ibrutinib can be decreased when combined with Darifenacin.Approved
IdarubicinThe metabolism of Idarubicin can be decreased when combined with Darifenacin.Approved
IdelalisibThe serum concentration of Darifenacin can be increased when it is combined with Idelalisib.Approved
IloperidoneThe metabolism of Iloperidone can be decreased when combined with Darifenacin.Approved
ImatinibThe metabolism of Darifenacin can be decreased when combined with Imatinib.Approved
ImipramineThe metabolism of Imipramine can be decreased when combined with Darifenacin.Approved
IndapamideThe serum concentration of Indapamide can be increased when it is combined with Darifenacin.Approved
IndinavirThe metabolism of Darifenacin can be decreased when combined with Indinavir.Approved
IpidacrineThe therapeutic efficacy of Darifenacin 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 Darifenacin.Approved
IsavuconazoniumThe metabolism of Darifenacin can be decreased when combined with Isavuconazonium.Approved, Investigational
IsoflurophateThe therapeutic efficacy of Darifenacin can be decreased when used in combination with Isoflurophate.Approved, Investigational, Withdrawn
IsoniazidThe metabolism of Darifenacin can be decreased when combined with Isoniazid.Approved
IsradipineThe metabolism of Darifenacin can be decreased when combined with Isradipine.Approved
ItoprideThe therapeutic efficacy of Itopride can be decreased when used in combination with Darifenacin.Investigational
ItraconazoleThe metabolism of Darifenacin can be decreased when combined with Itraconazole.Approved, Investigational
IvacaftorThe serum concentration of Darifenacin can be increased when it is combined with Ivacaftor.Approved
IxazomibThe metabolism of Ixazomib can be decreased when combined with Darifenacin.Approved
KetobemidoneThe risk or severity of adverse effects can be increased when Darifenacin is combined with Ketobemidone.Approved, Investigational
KetoconazoleThe metabolism of Darifenacin can be decreased when combined with Ketoconazole.Approved, Investigational
LabetalolThe metabolism of Labetalol can be decreased when combined with Darifenacin.Approved
LetermovirThe metabolism of Letermovir can be decreased when combined with Darifenacin.Approved
LevodopaThe metabolism of Levodopa can be decreased when combined with Darifenacin.Approved
Levomethadyl AcetateThe risk or severity of adverse effects can be increased when Darifenacin is combined with Levomethadyl Acetate.Approved, Investigational
LevomilnacipranThe metabolism of Levomilnacipran can be decreased when combined with Darifenacin.Approved
LevorphanolThe risk or severity of adverse effects can be increased when Darifenacin is combined with Levorphanol.Approved
LidocaineThe metabolism of Lidocaine can be decreased when combined with Darifenacin.Approved, Vet Approved
LisurideThe metabolism of Lisuride can be decreased when combined with Darifenacin.Approved, Investigational
LofentanilThe risk or severity of adverse effects can be increased when Darifenacin is combined with Lofentanil.Illicit
LomustineThe metabolism of Lomustine can be decreased when combined with Darifenacin.Approved
LoperamideThe metabolism of Loperamide can be decreased when combined with Darifenacin.Approved
LopinavirThe metabolism of Darifenacin can be decreased when combined with Lopinavir.Approved
LoratadineThe metabolism of Loratadine can be decreased when combined with Darifenacin.Approved
LorcaserinThe metabolism of Lorcaserin can be decreased when combined with Darifenacin.Approved
LovastatinThe metabolism of Darifenacin can be decreased when combined with Lovastatin.Approved, Investigational
LuliconazoleThe serum concentration of Darifenacin can be increased when it is combined with Luliconazole.Approved
LumacaftorThe metabolism of Darifenacin can be increased when combined with Lumacaftor.Approved
LumefantrineThe metabolism of Darifenacin can be decreased when combined with Lumefantrine.Approved
MalathionThe therapeutic efficacy of Darifenacin can be decreased when used in combination with Malathion.Approved, Investigational
ManidipineThe metabolism of Darifenacin can be decreased when combined with Manidipine.Approved, Investigational
MaprotilineThe metabolism of Maprotiline can be decreased when combined with Darifenacin.Approved
MazaticolThe risk or severity of adverse effects can be increased when Darifenacin is combined with Mazaticol.Experimental
MecamylamineThe risk or severity of adverse effects can be increased when Darifenacin is combined with Mecamylamine.Approved
MefloquineThe therapeutic efficacy of Darifenacin can be decreased when used in combination with Mefloquine.Approved
MemantineThe therapeutic efficacy of Darifenacin can be decreased when used in combination with Memantine.Approved, Investigational
MephenytoinThe metabolism of Mephenytoin can be decreased when combined with Darifenacin.Investigational, Withdrawn
MeptazinolThe risk or severity of adverse effects can be increased when Darifenacin is combined with Meptazinol.Experimental
MequitazineThe metabolism of Mequitazine can be decreased when combined with Darifenacin.Approved
MesoridazineThe metabolism of Mesoridazine can be decreased when combined with Darifenacin.Approved, Investigational
MethadoneThe metabolism of Methadone can be decreased when combined with Darifenacin.Approved
Methadyl AcetateThe risk or severity of adverse effects can be increased when Darifenacin is combined with Methadyl Acetate.Approved, Illicit
MethamphetamineThe metabolism of Methamphetamine can be decreased when combined with Darifenacin.Approved, Illicit
Methanesulfonyl FluorideThe therapeutic efficacy of Darifenacin can be decreased when used in combination with Methanesulfonyl Fluoride.Investigational
MethanthelineThe risk or severity of adverse effects can be increased when Darifenacin is combined with Methantheline.Approved, Investigational
MethotrimeprazineThe metabolism of Darifenacin can be decreased when combined with Methotrimeprazine.Approved
MethoxyfluraneThe metabolism of Methoxyflurane can be decreased when combined with Darifenacin.Approved, Investigational, Vet Approved
MethyclothiazideThe serum concentration of Methyclothiazide can be increased when it is combined with Darifenacin.Approved
MethylphenidateThe metabolism of Methylphenidate can be decreased when combined with Darifenacin.Approved, Investigational
Methylscopolamine bromideThe risk or severity of adverse effects can be increased when Darifenacin is combined with Methylscopolamine bromide.Approved
MethyprylonThe metabolism of Methyprylon can be decreased when combined with Darifenacin.Approved, Illicit, Withdrawn
MetixeneThe risk or severity of adverse effects can be increased when Darifenacin is combined with Metixene.Approved
MetoclopramideThe metabolism of Metoclopramide can be decreased when combined with Darifenacin.Approved, Investigational
MetolazoneThe serum concentration of Metolazone can be increased when it is combined with Darifenacin.Approved
MetoprololThe serum concentration of Metoprolol can be increased when it is combined with Darifenacin.Approved, Investigational
MexiletineThe metabolism of Mexiletine can be decreased when combined with Darifenacin.Approved
MianserinMianserin may increase the anticholinergic activities of Darifenacin.Approved, Investigational
MidostaurinThe metabolism of Darifenacin can be decreased when combined with Midostaurin.Approved
MifepristoneThe serum concentration of Darifenacin can be increased when it is combined with Mifepristone.Approved, Investigational
MinaprineThe therapeutic efficacy of Darifenacin can be decreased when used in combination with Minaprine.Approved
MirabegronThe risk or severity of adverse effects can be increased when Darifenacin is combined with Mirabegron.Approved
MirtazapineThe metabolism of Mirtazapine can be decreased when combined with Darifenacin.Approved
MitotaneThe serum concentration of Darifenacin can be decreased when it is combined with Mitotane.Approved
MoclobemideThe metabolism of Moclobemide can be decreased when combined with Darifenacin.Approved
MorphineThe metabolism of Morphine can be decreased when combined with Darifenacin.Approved, Investigational
NabiloneDarifenacin may increase the tachycardic activities of Nabilone.Approved, Investigational
NalbuphineThe risk or severity of adverse effects can be increased when Darifenacin is combined with Nalbuphine.Approved
NateglinideThe metabolism of Nateglinide can be decreased when combined with Darifenacin.Approved, Investigational
NebivololThe serum concentration of Nebivolol can be increased when it is combined with Darifenacin.Approved, Investigational
NefazodoneThe metabolism of Darifenacin can be decreased when combined with Nefazodone.Approved, Withdrawn
NelfinavirThe metabolism of Darifenacin can be decreased when combined with Nelfinavir.Approved
NeostigmineThe therapeutic efficacy of Darifenacin can be decreased when used in combination with Neostigmine.Approved, Vet Approved
NetupitantThe serum concentration of Darifenacin can be increased when it is combined with Netupitant.Approved
NevirapineThe metabolism of Darifenacin can be increased when combined with Nevirapine.Approved
NicardipineThe metabolism of Nicardipine can be decreased when combined with Darifenacin.Approved
NicergolineThe metabolism of Nicergoline can be decreased when combined with Darifenacin.Approved, Investigational
NicomorphineThe risk or severity of adverse effects can be increased when Darifenacin is combined with Nicomorphine.Experimental
NicotineThe metabolism of Nicotine can be decreased when combined with Darifenacin.Approved
NifedipineThe metabolism of Nifedipine can be decreased when combined with Darifenacin.Approved
NilotinibThe metabolism of Darifenacin can be decreased when combined with Nilotinib.Approved, Investigational
NitrofuralThe metabolism of Nitrofural can be decreased when combined with Darifenacin.Approved, Investigational, Vet Approved
NormethadoneThe risk or severity of adverse effects can be increased when Darifenacin is combined with Normethadone.Approved, Illicit
NortriptylineThe metabolism of Nortriptyline can be decreased when combined with Darifenacin.Approved
OlanzapineThe metabolism of Olanzapine can be decreased when combined with Darifenacin.Approved, Investigational
OlaparibThe metabolism of Darifenacin can be decreased when combined with Olaparib.Approved
OndansetronThe metabolism of Ondansetron can be decreased when combined with Darifenacin.Approved
OpiumThe risk or severity of adverse effects can be increased when Darifenacin is combined with Opium.Approved, Illicit
OrphenadrineThe risk or severity of adverse effects can be increased when Darifenacin is combined with Orphenadrine.Approved
OsimertinibThe serum concentration of Darifenacin can be increased when it is combined with Osimertinib.Approved
OtiloniumThe risk or severity of adverse effects can be increased when Darifenacin is combined with Otilonium.Experimental, Investigational
OxitropiumThe risk or severity of adverse effects can be increased when Darifenacin is combined with Oxitropium.Investigational
OxybutyninThe risk or severity of adverse effects can be increased when Darifenacin is combined with Oxybutynin.Approved, Investigational
OxycodoneThe metabolism of Oxycodone can be decreased when combined with Darifenacin.Approved, Illicit, Investigational
OxymorphoneThe metabolism of Oxymorphone can be decreased when combined with Darifenacin.Approved, Investigational, Vet Approved
OxyphenoniumThe risk or severity of adverse effects can be increased when Oxyphenonium is combined with Darifenacin.Approved
PalbociclibThe serum concentration of Darifenacin can be increased when it is combined with Palbociclib.Approved
PalonosetronThe metabolism of Palonosetron can be decreased when combined with Darifenacin.Approved, Investigational
PancuroniumThe risk or severity of adverse effects can be increased when Darifenacin is combined with Pancuronium.Approved
PanobinostatThe serum concentration of Darifenacin can be increased when it is combined with Panobinostat.Approved, Investigational
ParaoxonThe therapeutic efficacy of Darifenacin can be decreased when used in combination with Paraoxon.Experimental
ParoxetineThe metabolism of Darifenacin can be decreased when combined with Paroxetine.Approved, Investigational
PazopanibThe metabolism of Pazopanib can be decreased when combined with Darifenacin.Approved
Peginterferon alfa-2bThe serum concentration of Darifenacin can be decreased when it is combined with Peginterferon alfa-2b.Approved
PentamidineThe metabolism of Pentamidine can be decreased when combined with Darifenacin.Approved
PentazocineThe risk or severity of adverse effects can be increased when Darifenacin is combined with Pentazocine.Approved, Vet Approved
PentobarbitalThe metabolism of Darifenacin can be increased when combined with Pentobarbital.Approved, Vet Approved
PentoliniumThe risk or severity of adverse effects can be increased when Darifenacin is combined with Pentolinium.Approved
PerhexilineThe metabolism of Perhexiline can be decreased when combined with Darifenacin.Approved, Investigational
PerospironeThe metabolism of Perospirone can be decreased when combined with Darifenacin.Approved
PerphenazineThe metabolism of Perphenazine can be decreased when combined with Darifenacin.Approved
PethidineThe metabolism of Pethidine can be decreased when combined with Darifenacin.Approved
PhenacetinThe metabolism of Phenacetin can be decreased when combined with Darifenacin.Withdrawn
PhenazocineThe risk or severity of adverse effects can be increased when Darifenacin is combined with Phenazocine.Experimental
PhenforminThe metabolism of Phenformin can be decreased when combined with Darifenacin.Approved, Investigational, Withdrawn
PhenglutarimideThe risk or severity of adverse effects can be increased when Phenglutarimide is combined with Darifenacin.Experimental
PhenobarbitalThe metabolism of Darifenacin can be increased when combined with Phenobarbital.Approved
PhenoperidineThe risk or severity of adverse effects can be increased when Darifenacin is combined with Phenoperidine.Experimental
PhenytoinThe metabolism of Darifenacin can be increased when combined with Phenytoin.Approved, Vet Approved
PhysostigmineThe therapeutic efficacy of Darifenacin can be decreased when used in combination with Physostigmine.Approved
PindololThe metabolism of Pindolol can be decreased when combined with Darifenacin.Approved
PipecuroniumThe risk or severity of adverse effects can be increased when Darifenacin is combined with Pipecuronium.Approved
PiperazineThe metabolism of Piperazine can be decreased when combined with Darifenacin.Approved, Vet Approved
PipotiazineThe metabolism of Pipotiazine can be decreased when combined with Darifenacin.Approved, Investigational
PirenzepineThe risk or severity of adverse effects can be increased when Darifenacin is combined with Pirenzepine.Approved
PiritramideThe risk or severity of adverse effects can be increased when Darifenacin is combined with Piritramide.Investigational
PolythiazideThe serum concentration of Polythiazide can be increased when it is combined with Darifenacin.Approved
PonatinibThe metabolism of Ponatinib can be decreased when combined with Darifenacin.Approved
PosaconazoleThe metabolism of Darifenacin can be decreased when combined with Posaconazole.Approved, Investigational, Vet Approved
Potassium ChlorideDarifenacin may increase the ulcerogenic activities of Potassium Chloride.Approved, Withdrawn
PramlintidePramlintide may increase the anticholinergic activities of Darifenacin.Approved, Investigational
PrimidoneThe metabolism of Darifenacin can be increased when combined with Primidone.Approved, Vet Approved
ProcainamideThe metabolism of Procainamide can be decreased when combined with Darifenacin.Approved
ProchlorperazineThe metabolism of Prochlorperazine can be decreased when combined with Darifenacin.Approved, Vet Approved
ProcyclidineThe risk or severity of adverse effects can be increased when Procyclidine is combined with Darifenacin.Approved
ProgesteroneThe metabolism of Progesterone can be decreased when combined with Darifenacin.Approved, Vet Approved
PromazineThe metabolism of Darifenacin can be decreased when combined with Promazine.Approved, Vet Approved
PromethazineThe metabolism of Promethazine can be decreased when combined with Darifenacin.Approved
PropafenoneThe serum concentration of Darifenacin can be increased when it is combined with Propafenone.Approved
PropanthelineThe risk or severity of adverse effects can be increased when Propantheline is combined with Darifenacin.Approved
PropiverineThe risk or severity of adverse effects can be increased when Darifenacin is combined with Propiverine.Approved, Investigational
PropofolThe metabolism of Propofol can be decreased when combined with Darifenacin.Approved, Investigational, Vet Approved
PropranololThe metabolism of Propranolol can be decreased when combined with Darifenacin.Approved, Investigational
ProtriptylineThe metabolism of Protriptyline can be decreased when combined with Darifenacin.Approved
PseudoephedrineThe metabolism of Pseudoephedrine can be decreased when combined with Darifenacin.Approved
PyridostigmineThe therapeutic efficacy of Darifenacin can be decreased when used in combination with Pyridostigmine.Approved
QuetiapineThe metabolism of Quetiapine can be decreased when combined with Darifenacin.Approved
QuinethazoneThe serum concentration of Quinethazone can be increased when it is combined with Darifenacin.Approved
QuinidineThe metabolism of Darifenacin can be decreased when combined with Quinidine.Approved
QuinineThe metabolism of Quinine can be decreased when combined with Darifenacin.Approved
RamosetronDarifenacin may increase the constipating activities of Ramosetron.Approved, Investigational
RanitidineThe metabolism of Ranitidine can be decreased when combined with Darifenacin.Approved
RanolazineThe metabolism of Darifenacin can be decreased when combined with Ranolazine.Approved, Investigational
RemifentanilThe risk or severity of adverse effects can be increased when Darifenacin is combined with Remifentanil.Approved
RemoxiprideThe metabolism of Remoxipride can be decreased when combined with Darifenacin.Approved, Withdrawn
repinotanThe metabolism of repinotan can be decreased when combined with Darifenacin.Investigational
RibociclibThe serum concentration of Darifenacin can be increased when it is combined with Ribociclib.Approved
RifabutinThe metabolism of Darifenacin can be increased when combined with Rifabutin.Approved
RifampicinThe metabolism of Darifenacin can be increased when combined with Rifampicin.Approved
RifapentineThe metabolism of Darifenacin can be increased when combined with Rifapentine.Approved
RisperidoneThe metabolism of Risperidone can be decreased when combined with Darifenacin.Approved, Investigational
RitonavirThe metabolism of Darifenacin can be decreased when combined with Ritonavir.Approved, Investigational
RivastigmineThe therapeutic efficacy of Darifenacin can be decreased when used in combination with Rivastigmine.Approved, Investigational
RolapitantThe metabolism of Darifenacin can be decreased when combined with Rolapitant.Approved
RopiniroleThe metabolism of Darifenacin can be decreased when combined with Ropinirole.Approved, Investigational
RopivacaineThe metabolism of Ropivacaine can be decreased when combined with Darifenacin.Approved
RotigotineThe metabolism of Rotigotine can be decreased when combined with Darifenacin.Approved
RucaparibThe metabolism of Rucaparib can be decreased when combined with Darifenacin.Approved, Investigational
RupatadineThe metabolism of Rupatadine can be decreased when combined with Darifenacin.Approved
SaquinavirThe metabolism of Darifenacin can be decreased when combined with Saquinavir.Approved, Investigational
ScopolamineThe risk or severity of adverse effects can be increased when Scopolamine is combined with Darifenacin.Approved
Scopolamine butylbromideThe risk or severity of adverse effects can be increased when Darifenacin is combined with Scopolamine butylbromide.Approved, Vet Approved
SecretinThe therapeutic efficacy of Secretin can be decreased when used in combination with Darifenacin.Approved, Investigational
SertindoleThe metabolism of Sertindole can be decreased when combined with Darifenacin.Approved, Investigational, Withdrawn
SertralineThe metabolism of Sertraline can be decreased when combined with Darifenacin.Approved
SildenafilThe metabolism of Darifenacin can be decreased when combined with Sildenafil.Approved, Investigational
SiltuximabThe serum concentration of Darifenacin can be decreased when it is combined with Siltuximab.Approved
SimeprevirThe serum concentration of Darifenacin can be increased when it is combined with Simeprevir.Approved
SimvastatinThe metabolism of Simvastatin can be decreased when combined with Darifenacin.Approved
SolifenacinThe risk or severity of adverse effects can be increased when Darifenacin is combined with Solifenacin.Approved
SparteineThe metabolism of Sparteine can be decreased when combined with Darifenacin.Experimental
St. John's WortThe serum concentration of Darifenacin can be decreased when it is combined with St. John's Wort.Investigational, Nutraceutical
StiripentolThe serum concentration of Darifenacin can be increased when it is combined with Stiripentol.Approved
SufentanilThe risk or severity of adverse effects can be increased when Darifenacin is combined with Sufentanil.Approved, Investigational
SulfisoxazoleThe metabolism of Darifenacin can be decreased when combined with Sulfisoxazole.Approved, Vet Approved
SulpirideThe therapeutic efficacy of Sulpiride can be decreased when used in combination with Darifenacin.Approved, Investigational
TacrineThe therapeutic efficacy of Darifenacin can be decreased when used in combination with Tacrine.Investigational, Withdrawn
TamoxifenThe serum concentration of the active metabolites of Tamoxifen can be reduced when Tamoxifen is used in combination with Darifenacin resulting in a loss in efficacy.Approved
TamsulosinThe metabolism of Tamsulosin can be decreased when combined with Darifenacin.Approved, Investigational
TapentadolThe metabolism of Tapentadol can be decreased when combined with Darifenacin.Approved
TegaserodThe metabolism of Tegaserod can be decreased when combined with Darifenacin.Investigational, Withdrawn
TelaprevirThe metabolism of Darifenacin can be decreased when combined with Telaprevir.Approved, Withdrawn
TelithromycinThe metabolism of Darifenacin can be decreased when combined with Telithromycin.Approved
TerbinafineThe metabolism of Darifenacin can be decreased when combined with Terbinafine.Approved, Investigational, Vet Approved
TerfenadineThe metabolism of Terfenadine can be decreased when combined with Darifenacin.Withdrawn
TesmilifeneThe metabolism of Tesmilifene can be decreased when combined with Darifenacin.Investigational
TetrabenazineThe metabolism of Tetrabenazine can be decreased when combined with Darifenacin.Approved
TheophyllineThe metabolism of Theophylline can be decreased when combined with Darifenacin.Approved
ThioridazineThe serum concentration of Thioridazine can be increased when it is combined with Darifenacin.Approved, Withdrawn
TiclopidineThe metabolism of Darifenacin can be decreased when combined with Ticlopidine.Approved
TilidineThe risk or severity of adverse effects can be increased when Darifenacin is combined with Tilidine.Experimental
TimololThe metabolism of Timolol can be decreased when combined with Darifenacin.Approved
TiotropiumDarifenacin may increase the anticholinergic activities of Tiotropium.Approved
TipranavirThe metabolism of Darifenacin can be decreased when combined with Tipranavir.Approved, Investigational
TocilizumabThe serum concentration of Darifenacin can be decreased when it is combined with Tocilizumab.Approved
TolterodineThe risk or severity of adverse effects can be increased when Darifenacin is combined with Tolterodine.Approved, Investigational
TopiramateThe risk or severity of adverse effects can be increased when Darifenacin is combined with Topiramate.Approved
TrabectedinThe metabolism of Trabectedin can be decreased when combined with Darifenacin.Approved, Investigational
TramadolThe therapeutic efficacy of Tramadol can be decreased when used in combination with Darifenacin.Approved, Investigational
TranylcypromineThe metabolism of Darifenacin can be decreased when combined with Tranylcypromine.Approved
TrazodoneThe metabolism of Trazodone can be decreased when combined with Darifenacin.Approved, Investigational
TrichlorfonThe therapeutic efficacy of Darifenacin can be decreased when used in combination with Trichlorfon.Vet Approved
TrichlormethiazideThe serum concentration of Trichlormethiazide can be increased when it is combined with Darifenacin.Approved, Vet Approved
TrihexyphenidylThe risk or severity of adverse effects can be increased when Trihexyphenidyl is combined with Darifenacin.Approved
TrimethaphanThe risk or severity of adverse effects can be increased when Darifenacin is combined with Trimethaphan.Approved, Investigational
TrimipramineThe metabolism of Trimipramine can be decreased when combined with Darifenacin.Approved
TropatepineThe risk or severity of adverse effects can be increased when Darifenacin is combined with Tropatepine.Experimental
TropicamideThe risk or severity of adverse effects can be increased when Tropicamide is combined with Darifenacin.Approved
TrospiumThe risk or severity of adverse effects can be increased when Trospium is combined with Darifenacin.Approved
TubocurarineThe risk or severity of adverse effects can be increased when Darifenacin is combined with Tubocurarine.Approved
UmeclidiniumUmeclidinium may increase the anticholinergic activities of Darifenacin.Approved
ValbenazineThe metabolism of Valbenazine can be decreased when combined with Darifenacin.Approved, Investigational
VecuroniumThe risk or severity of adverse effects can be increased when Darifenacin is combined with Vecuronium.Approved
VenlafaxineThe metabolism of Darifenacin can be decreased when combined with Venlafaxine.Approved
VerapamilThe metabolism of Darifenacin can be decreased when combined with Verapamil.Approved
VernakalantThe metabolism of Vernakalant can be decreased when combined with Darifenacin.Approved, Investigational
VilazodoneThe metabolism of Vilazodone can be decreased when combined with Darifenacin.Approved
VinblastineThe metabolism of Vinblastine can be decreased when combined with Darifenacin.Approved
VinorelbineThe metabolism of Vinorelbine can be decreased when combined with Darifenacin.Approved, Investigational
VoriconazoleThe metabolism of Darifenacin can be decreased when combined with Voriconazole.Approved, Investigational
VortioxetineThe metabolism of Vortioxetine can be decreased when combined with Darifenacin.Approved
YohimbineThe metabolism of Yohimbine can be decreased when combined with Darifenacin.Approved, Vet Approved
ZalcitabineThe metabolism of Zalcitabine can be decreased when combined with Darifenacin.Approved, Investigational
ZiprasidoneThe metabolism of Darifenacin can be decreased when combined with Ziprasidone.Approved
ZolpidemThe metabolism of Zolpidem can be decreased when combined with Darifenacin.Approved
ZuclopenthixolThe metabolism of Zuclopenthixol can be decreased when combined with Darifenacin.Approved, Investigational
Food Interactions
  • Take without regard to meals.

References

Synthesis Reference

Valeriano Merli, Augusto Canavesi, Paola Daverio, "Processes for preparing darifenacin hydrobromide." U.S. Patent US20070197631, issued August 23, 2007.

US20070197631
General References
Not Available
External Links
Human Metabolome Database
HMDB14639
KEGG Drug
D01699
PubChem Compound
444031
PubChem Substance
46508104
ChemSpider
392054
BindingDB
50109647
ChEBI
391960
ChEMBL
CHEMBL1346
Therapeutic Targets Database
DAP001131
PharmGKB
PA164774901
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Darifenacin
ATC Codes
G04BD10 — Darifenacin
AHFS Codes
  • 86:12.04 — Antimuscarinics
FDA label
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Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
1CompletedTreatmentHealthy Volunteers2
1Unknown StatusNot AvailableBioequivalency2
2CompletedTreatmentHealthy Volunteers1
2SuspendedTreatmentNeurogenic Detrusor Overactivity1
2TerminatedTreatmentDisseminated Sclerosis / Overactive Detrusor1
3CompletedTreatmentOveractive Bladder1
3CompletedTreatmentOveractive Bladder Syndrome2
4CompletedNot AvailableOveractive Bladder1
4CompletedNot AvailableUrinary Incontinence (UI)1
4CompletedTreatmentHealthy Volunteers1
4CompletedTreatmentNeurogenic Detrusor Overactivity / Spinal Cord Injuries (SCI)1
4CompletedTreatmentOveractive Bladder1
4CompletedTreatmentOveractive Bladder (OAB)1
4WithdrawnNot AvailableNocturia1
Not AvailableCompletedNot AvailableOveractive Bladder1
Not AvailableCompletedNot AvailableOveractive Bladder / Urinary Bladder Diseases / Urinary Bladder Overactive / Urologic Diseases1
Not AvailableCompletedTreatmentOveractive Bladder / Parkinson's Disease (PD)1
Not AvailableTerminatedTreatmentBladder Spasms / Overactive Bladder / Postoperative / Postoperative pain / Renal Colic / Ureteral Stent Pain1

Pharmacoeconomics

Manufacturers
  • Novartis pharmaceuticals corp
Packagers
Dosage forms
FormRouteStrength
Tablet, film coated, extended releaseOral15 mg/1
Tablet, film coated, extended releaseOral7.5 mg/1
Tablet, extended releaseOral15 mg/1
Tablet, extended releaseOral15 mg
Tablet, extended releaseOral7.5 mg/1
Tablet, extended releaseOral7.5 mg
Prices
Unit descriptionCostUnit
Enablex 15 mg 24 Hour tablet5.22USD tablet
Enablex 7.5 mg 24 Hour tablet5.22USD tablet
Enablex 15 mg tablet5.02USD tablet
Enablex 7.5 mg tablet5.02USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US5096890No1995-03-132015-03-13Us
CA2469702No2010-07-062022-03-05Canada
CA2230314No2003-06-242016-08-21Canada
US6106864No1996-08-212016-08-21Us

Properties

State
Solid
Experimental Properties
PropertyValueSource
logP4.5Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.000298 mg/mLALOGPS
logP4.35ALOGPS
logP4.54ChemAxon
logS-6.2ALOGPS
pKa (Strongest Acidic)16.21ChemAxon
pKa (Strongest Basic)10.11ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count3ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area55.56 Å2ChemAxon
Rotatable Bond Count7ChemAxon
Refractivity128.37 m3·mol-1ChemAxon
Polarizability48.54 Å3ChemAxon
Number of Rings5ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleYesChemAxon
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9966
Blood Brain Barrier+0.9989
Caco-2 permeable-0.5256
P-glycoprotein substrateSubstrate0.6385
P-glycoprotein inhibitor INon-inhibitor0.6329
P-glycoprotein inhibitor IIInhibitor0.5374
Renal organic cation transporterInhibitor0.6441
CYP450 2C9 substrateNon-substrate0.8774
CYP450 2D6 substrateNon-substrate0.5946
CYP450 3A4 substrateSubstrate0.6046
CYP450 1A2 substrateNon-inhibitor0.696
CYP450 2C9 inhibitorNon-inhibitor0.8253
CYP450 2D6 inhibitorInhibitor0.5816
CYP450 2C19 inhibitorInhibitor0.5399
CYP450 3A4 inhibitorInhibitor0.5
CYP450 inhibitory promiscuityHigh CYP Inhibitory Promiscuity0.6168
Ames testNon AMES toxic0.7145
CarcinogenicityNon-carcinogens0.8847
BiodegradationNot ready biodegradable0.9599
Rat acute toxicity3.0008 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.907
hERG inhibition (predictor II)Inhibitor0.6703
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

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
Phenylacetamides / Phenethylamines / Coumarans / Aralkylamines / Alkyl aryl ethers / N-alkylpyrrolidines / Trialkylamines / Primary carboxylic acid amides / Amino acids and derivatives / Oxacyclic compounds
show 5 more
Substituents
Diphenylmethane / Phenylacetamide / Phenethylamine / Coumaran / Alkyl aryl ether / Aralkylamine / N-alkylpyrrolidine / Pyrrolidine / Amino acid or derivatives / Carboxamide group
show 18 more
Molecular Framework
Aromatic heteropolycyclic compounds
External Descriptors
monocarboxylic acid amide, 1-benzofurans, pyrrolidines (CHEBI:391960)

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. Bharucha AE, Ravi K, Zinsmeister AR: Comparison of selective M3 and nonselective muscarinic receptor antagonists on gastrointestinal transit and bowel habits in humans. Am J Physiol Gastrointest Liver Physiol. 2010 Jul;299(1):G215-9. doi: 10.1152/ajpgi.00072.2010. Epub 2010 Apr 15. [PubMed:20395537]
  2. Bozkurt TE, Sahin-Erdemli I: M(1) and M(3) muscarinic receptors are involved in the release of urinary bladder-derived relaxant factor. Pharmacol Res. 2009 May;59(5):300-5. doi: 10.1016/j.phrs.2009.01.013. Epub 2009 Feb 5. [PubMed:19416629]
  3. Jha S, Parsons M: Treatment of overactive bladder in the aging population: focus on darifenacin. Clin Interv Aging. 2006;1(4):309-16. [PubMed:18046909]
  4. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Antagonist
General Function
Phosphatidylinositol phospholipase c activity
Specific Function
The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the...
Gene Name
CHRM1
Uniprot ID
P11229
Uniprot Name
Muscarinic acetylcholine receptor M1
Molecular Weight
51420.375 Da
References
  1. Jha S, Parsons M: Treatment of overactive bladder in the aging population: focus on darifenacin. Clin Interv Aging. 2006;1(4):309-16. [PubMed:18046909]
  2. Moriya H, Takagi Y, Nakanishi T, Hayashi M, Tani T, Hirotsu I: Affinity profiles of various muscarinic antagonists for cloned human muscarinic acetylcholine receptor (mAChR) subtypes and mAChRs in rat heart and submandibular gland. Life Sci. 1999;64(25):2351-8. [PubMed:10374898]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Antagonist
General Function
G-protein coupled acetylcholine receptor activity
Specific Function
The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the...
Gene Name
CHRM2
Uniprot ID
P08172
Uniprot Name
Muscarinic acetylcholine receptor M2
Molecular Weight
51714.605 Da
References
  1. Jha S, Parsons M: Treatment of overactive bladder in the aging population: focus on darifenacin. Clin Interv Aging. 2006;1(4):309-16. [PubMed:18046909]
  2. Moriya H, Takagi Y, Nakanishi T, Hayashi M, Tani T, Hirotsu I: Affinity profiles of various muscarinic antagonists for cloned human muscarinic acetylcholine receptor (mAChR) subtypes and mAChRs in rat heart and submandibular gland. Life Sci. 1999;64(25):2351-8. [PubMed:10374898]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Antagonist
General Function
Guanyl-nucleotide exchange factor activity
Specific Function
The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the...
Gene Name
CHRM4
Uniprot ID
P08173
Uniprot Name
Muscarinic acetylcholine receptor M4
Molecular Weight
53048.65 Da
References
  1. Jha S, Parsons M: Treatment of overactive bladder in the aging population: focus on darifenacin. Clin Interv Aging. 2006;1(4):309-16. [PubMed:18046909]
  2. Moriya H, Takagi Y, Nakanishi T, Hayashi M, Tani T, Hirotsu I: Affinity profiles of various muscarinic antagonists for cloned human muscarinic acetylcholine receptor (mAChR) subtypes and mAChRs in rat heart and submandibular gland. Life Sci. 1999;64(25):2351-8. [PubMed:10374898]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Antagonist
General Function
Phosphatidylinositol phospholipase c activity
Specific Function
The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the...
Gene Name
CHRM5
Uniprot ID
P08912
Uniprot Name
Muscarinic acetylcholine receptor M5
Molecular Weight
60073.205 Da
References
  1. Moriya H, Takagi Y, Nakanishi T, Hayashi M, Tani T, Hirotsu I: Affinity profiles of various muscarinic antagonists for cloned human muscarinic acetylcholine receptor (mAChR) subtypes and mAChRs in rat heart and submandibular gland. Life Sci. 1999;64(25):2351-8. [PubMed:10374898]
  2. Jha S, Parsons M: Treatment of overactive bladder in the aging population: focus on darifenacin. Clin Interv Aging. 2006;1(4):309-16. [PubMed:18046909]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Vitamin d3 25-hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation react...
Gene Name
CYP3A4
Uniprot ID
P08684
Uniprot Name
Cytochrome P450 3A4
Molecular Weight
57342.67 Da
References
  1. Skerjanec A: The clinical pharmacokinetics of darifenacin. Clin Pharmacokinet. 2006;45(4):325-50. [PubMed:16584282]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
Inhibitor
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. Skerjanec A: The clinical pharmacokinetics of darifenacin. Clin Pharmacokinet. 2006;45(4):325-50. [PubMed:16584282]

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