Identification

Name
Ketoconazole
Accession Number
DB01026  (APRD00401)
Type
Small Molecule
Groups
Approved, Investigational
Description

Broad spectrum antifungal agent used for long periods at high doses, especially in immunosuppressed patients. It is a racemate consisting of equimolar amounts of (2R,4S)- and (2S,4R)-ketoconazole with the chiral centers on the acetal ring.

Structure
Thumb
Synonyms
  • Ketoconazol
  • Ketoconazole
  • Ketoconazolum
  • Ketozole
Product Images
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
ExtinaAerosol, foam20 mg/gTopicalPrestium Pharma, Inc.2014-01-10Not applicableUs
KetoconazoleShampoo20 mg/mLTopicalPatriot Pharmaceuticals2005-07-01Not applicableUs
Ketoderm Cream 2%Cream2 %TopicalTaropharma, A Division Of Taro Pharmaceuticals Inc.2002-05-23Not applicableCanada
NizoralTablet200 mg/1OralJanssen Pharmaceuticals1981-06-122017-01-26Us
NizoralShampoo20 mg/mLTopicalA S Medication Solutions1990-08-312017-06-20Us
NizoralShampoo20 mg/mLTopicalJanssen Pharmaceuticals1990-08-31Not applicableUs
Nizoral Cream 2%Cream2 %TopicalMcneil Consumer Healthcare Division Of Johnson & Johnson Inc1988-12-312007-08-02Canada
Nizoral Oral Suspension 20mg/mlSuspension20 mgOralJanssen Pharmaceutica, Division Of Janssen Ortho Inc.1989-12-311998-02-06Canada
Nizoral Shp 2%Shampoo2 %TopicalJanssen Pharmaceutica, Division Of Janssen Ortho Inc.1990-12-311997-08-12Canada
Nizoral Tablets 200mgTablet200 mgOralMcneil Consumer Healthcare Division Of Johnson & Johnson Inc1984-12-312003-02-06Canada
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Apo-ketoconazoleTablet200 mgOralApotex Corporation1998-02-03Not applicableCanada
KetoconazoleCream20 mg/1TopicalRemedy Repack2013-04-152017-02-15Us
KetoconazoleTablet200 mg/1OralAvera Mc Kennan Hospital2015-11-05Not applicableUs
KetoconazoleTablet200 mg/1OralNucare Pharmaceuticals, Inc.1999-06-15Not applicableUs
KetoconazoleCream20 mg/gTopicalNu Care Pharmaceuticals,inc.2002-12-18Not applicableUs
KetoconazoleShampoo, suspension20.5 mg/mLTopicalSandoz2005-11-04Not applicableUs
KetoconazoleCream20 mg/gTopicalA S Medication Solutions2004-04-28Not applicableUs
KetoconazoleCream20 mg/gTopicalE. Fougera & CO., A division of Fougera Pharmaceuticals Inc.2004-04-28Not applicableUs
KetoconazoleCream20 mg/gTopicalTeva2000-04-272017-05-31Us
KetoconazoleTablet200 mg/1OralState of Florida DOH Central Pharmacy2013-01-01Not applicableUs
Over the Counter Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Nizoral - 2%Shampoo2 %TopicalJohnson & Johnson1990-12-30Not applicableCanada
Nizoral A-DShampoo10 mg/mLTopicalJohnson & Johnson Consumer Inc., Mc Neil Consumer Healthcare Division1999-04-01Not applicableUs
International/Other Brands
Extina / Fungarest (Janssen-Cilag) / Fungoral (Johnson & Johnson) / Ketoderm (Hessel) / Ketoisdin (Isdin) / Ketozole (Ranbaxy) / Nizoral / Nizoral a-D / Nizoral Cream (Ortho-McNeil) / Nizoral Shampoo (Ortho-McNeil) / Orifungal (Janssen) / Orifungal M (Janssen) / Panfungol (Esteve) / Xolegel
Categories
UNII
R9400W927I
CAS number
65277-42-1
Weight
Average: 531.431
Monoisotopic: 530.148760818
Chemical Formula
C26H28Cl2N4O4
InChI Key
XMAYWYJOQHXEEK-UHFFFAOYSA-N
InChI
InChI=1S/C26H28Cl2N4O4/c1-19(33)31-10-12-32(13-11-31)21-3-5-22(6-4-21)34-15-23-16-35-26(36-23,17-30-9-8-29-18-30)24-7-2-20(27)14-25(24)28/h2-9,14,18,23H,10-13,15-17H2,1H3
IUPAC Name
1-[4-(4-{[2-(2,4-dichlorophenyl)-2-(1H-imidazol-1-ylmethyl)-1,3-dioxolan-4-yl]methoxy}phenyl)piperazin-1-yl]ethan-1-one
SMILES
CC(=O)N1CCN(CC1)C1=CC=C(OCC2COC(CN3C=CN=C3)(O2)C2=CC=C(Cl)C=C2Cl)C=C1

Pharmacology

Indication

For the treatment of the following systemic fungal infections: candidiasis, chronic mucocutaneous candidiasis, oral thrush, candiduria, blastomycosis, coccidioidomycosis, histoplasmosis, chromomycosis, and paracoccidioidomycosis.

Structured Indications
Pharmacodynamics

Ketoconazole, like clotrimazole, fluconazole, itraconazole, and miconazole, is an imidazole antifungal agent.

Mechanism of action

Ketoconazole interacts with 14-α demethylase, a cytochrome P-450 enzyme necessary for the conversion of lanosterol to ergosterol. This results in inhibition of ergosterol synthesis and increased fungal cellular permeability. Other mechanisms may involve the inhibition of endogenous respiration, interaction with membrane phospholipids, inhibition of yeast transformation to mycelial forms, inhibition of purine uptake, and impairment of triglyceride and/or phospholipid biosynthesis. Ketoconazole can also inhibit the synthesis of thromboxane and sterols such as aldosterone, cortisol, and testosterone.

TargetActionsOrganism
ALanosterol 14-alpha demethylase
inhibitor
Yeast
UAndrogen receptor
binder
Human
U17-hydroxylaseNot AvailableHuman
USteroid 21-hydroxylaseNot AvailableHuman
U11-hydroxylaseNot AvailableHuman
UCytochrome P450 19A1Not AvailableHuman
UPotassium voltage-gated channel subfamily H member 2
inhibitor
Human
UNuclear receptor subfamily 1 group I member 2
antagonist
Human
UNuclear receptor subfamily 1 group I member 3Not AvailableHuman
Absorption

Moderate

Volume of distribution
Not Available
Protein binding

99% (in vitro, plasma protein binding)

Metabolism

Hepatic

Route of elimination
Not Available
Half life

2 hours

Clearance
Not Available
Toxicity

Hepatotoxicity, LD50=86 mg/kg (orally in rat)

Affected organisms
  • Fungi
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteractionDrug group
16-BromoepiandrosteroneThe serum concentration of 16-Bromoepiandrosterone can be increased when it is combined with Ketoconazole.Investigational
19-norandrostenedioneThe serum concentration of 19-norandrostenedione can be increased when it is combined with Ketoconazole.Experimental, Illicit
4-MethoxyamphetamineThe metabolism of 4-Methoxyamphetamine can be decreased when combined with Ketoconazole.Experimental, Illicit
5-androstenedioneThe serum concentration of 5-androstenedione can be increased when it is combined with Ketoconazole.Experimental, Illicit
AbemaciclibThe serum concentration of Abemaciclib can be increased when it is combined with Ketoconazole.Approved
AbirateroneThe metabolism of Abiraterone can be decreased when combined with Ketoconazole.Approved
AceclofenacThe metabolism of Aceclofenac can be decreased when combined with Ketoconazole.Approved, Investigational
AcenocoumarolThe serum concentration of Acenocoumarol can be increased when it is combined with Ketoconazole.Approved
AcetaminophenThe metabolism of Acetaminophen can be decreased when combined with Ketoconazole.Approved
AcetylcholineThe metabolism of Acetylcholine can be decreased when combined with Ketoconazole.Approved
Acetylsalicylic acidThe metabolism of Acetylsalicylic acid can be decreased when combined with Ketoconazole.Approved, Vet Approved
AdinazolamThe metabolism of Adinazolam can be decreased when combined with Ketoconazole.Approved
AfatinibThe serum concentration of Afatinib can be increased when it is combined with Ketoconazole.Approved
AjmalineThe metabolism of Ajmaline can be decreased when combined with Ketoconazole.Approved, Investigational
AlbendazoleThe metabolism of Albendazole can be decreased when combined with Ketoconazole.Approved, Vet Approved
AlclometasoneThe metabolism of Alclometasone can be decreased when combined with Ketoconazole.Approved
AldosteroneThe serum concentration of Aldosterone can be increased when it is combined with Ketoconazole.Experimental, Investigational
AlfentanilThe metabolism of Alfentanil can be decreased when combined with Ketoconazole.Approved, Illicit
AlfuzosinThe serum concentration of Alfuzosin can be increased when it is combined with Ketoconazole.Approved, Investigational
AliskirenThe serum concentration of Aliskiren can be increased when it is combined with Ketoconazole.Approved, Investigational
AllylestrenolThe metabolism of Allylestrenol can be decreased when combined with Ketoconazole.Approved
AlmasilateThe serum concentration of Ketoconazole can be decreased when it is combined with Almasilate.Approved, Experimental
AlmotriptanThe serum concentration of Almotriptan can be increased when it is combined with Ketoconazole.Approved, Investigational
AlogliptinThe metabolism of Alogliptin can be decreased when combined with Ketoconazole.Approved
AloglutamolThe serum concentration of Ketoconazole can be decreased when it is combined with Aloglutamol.Experimental
AlosetronThe serum concentration of Alosetron can be increased when it is combined with Ketoconazole.Approved, Withdrawn
AlprazolamThe serum concentration of Alprazolam can be increased when it is combined with Ketoconazole.Approved, Illicit, Investigational
AlprenololThe metabolism of Alprenolol can be decreased when combined with Ketoconazole.Approved, Withdrawn
AluminiumThe serum concentration of Ketoconazole can be decreased when it is combined with Aluminium.Approved
Aluminium acetoacetateThe serum concentration of Ketoconazole can be decreased when it is combined with Aluminium acetoacetate.Experimental
Aluminium glycinateThe serum concentration of Ketoconazole can be decreased when it is combined with Aluminium glycinate.Experimental
Aluminum hydroxideThe serum concentration of Ketoconazole can be decreased when it is combined with Aluminum hydroxide.Approved
AmbrisentanThe metabolism of Ambrisentan can be decreased when combined with Ketoconazole.Approved, Investigational
AmbroxolThe metabolism of Ambroxol can be decreased when combined with Ketoconazole.Approved, Investigational
AmcinonideThe serum concentration of Amcinonide can be increased when it is combined with Ketoconazole.Approved
AminophenazoneThe metabolism of Aminophenazone can be decreased when combined with Ketoconazole.Approved, Withdrawn
AminophyllineThe metabolism of Aminophylline can be decreased when combined with Ketoconazole.Approved
AmiodaroneThe metabolism of Amiodarone can be decreased when combined with Ketoconazole.Approved, Investigational
AmitriptylineThe metabolism of Amitriptyline can be decreased when combined with Ketoconazole.Approved
AmlodipineThe metabolism of Amlodipine can be decreased when combined with Ketoconazole.Approved
AmodiaquineThe serum concentration of Amodiaquine can be increased when it is combined with Ketoconazole.Approved, Investigational
AmoxapineThe metabolism of Amoxapine can be decreased when combined with Ketoconazole.Approved
AmoxicillinThe metabolism of Amoxicillin can be decreased when combined with Ketoconazole.Approved, Vet Approved
AmphetamineThe metabolism of Amphetamine can be decreased when combined with Ketoconazole.Approved, Illicit
Amphotericin BThe therapeutic efficacy of Amphotericin B can be decreased when used in combination with Ketoconazole.Approved, Investigational
AmprenavirThe metabolism of Amprenavir can be decreased when combined with Ketoconazole.Approved
AmrinoneThe risk or severity of adverse effects can be increased when Ketoconazole is combined with Amrinone.Approved
AmsacrineThe metabolism of Amsacrine can be decreased when combined with Ketoconazole.Approved
AnagrelideKetoconazole may increase the QTc-prolonging activities of Anagrelide.Approved
AndrostenedioneThe serum concentration of Androstenedione can be increased when it is combined with Ketoconazole.Experimental, Illicit
AnecortaveThe serum concentration of Anecortave can be increased when it is combined with Ketoconazole.Investigational
anecortave acetateThe serum concentration of anecortave acetate can be increased when it is combined with Ketoconazole.Investigational
AntipyrineThe metabolism of Antipyrine can be decreased when combined with Ketoconazole.Approved
ApixabanThe serum concentration of Apixaban can be increased when it is combined with Ketoconazole.Approved
ApremilastThe metabolism of Apremilast can be decreased when combined with Ketoconazole.Approved, Investigational
AprepitantThe serum concentration of Ketoconazole can be increased when it is combined with Aprepitant.Approved, Investigational
AprindineThe metabolism of Aprindine can be decreased when combined with Ketoconazole.Approved
Arachidonic AcidThe metabolism of Arachidonic Acid can be decreased when combined with Ketoconazole.Experimental
ArformoterolThe metabolism of Arformoterol can be decreased when combined with Ketoconazole.Approved, Investigational
ArgatrobanThe metabolism of Argatroban can be decreased when combined with Ketoconazole.Approved, Investigational
AripiprazoleThe serum concentration of Aripiprazole can be increased when it is combined with Ketoconazole.Approved, Investigational
Arsenic trioxideKetoconazole may increase the QTc-prolonging activities of Arsenic trioxide.Approved, Investigational
ArtemetherThe metabolism of Artemether can be decreased when combined with Ketoconazole.Approved
ArtesunateThe serum concentration of the active metabolites of Artesunate can be reduced when Artesunate is used in combination with Ketoconazole resulting in a loss in efficacy.Approved, Investigational
AsenapineThe serum concentration of Ketoconazole can be decreased when it is combined with Asenapine.Approved
AstemizoleKetoconazole may increase the QTc-prolonging activities of Astemizole.Approved, Withdrawn
AtamestaneThe serum concentration of Atamestane can be increased when it is combined with Ketoconazole.Investigational
AtazanavirThe metabolism of Atazanavir can be decreased when combined with Ketoconazole.Approved, Investigational
AtomoxetineThe metabolism of Ketoconazole can be decreased when combined with Atomoxetine.Approved
AtorvastatinThe risk or severity of adverse effects can be increased when Atorvastatin is combined with Ketoconazole.Approved
AvanafilThe serum concentration of Avanafil can be increased when it is combined with Ketoconazole.Approved
AxitinibThe serum concentration of Axitinib can be increased when it is combined with Ketoconazole.Approved, Investigational
AzelastineThe metabolism of Azelastine can be decreased when combined with Ketoconazole.Approved
AzelnidipineThe risk or severity of adverse effects can be increased when Ketoconazole is combined with Azelnidipine.Approved, Investigational
AzimilideThe risk or severity of adverse effects can be increased when Ketoconazole is combined with Azimilide.Investigational
AzithromycinThe metabolism of Azithromycin can be decreased when combined with Ketoconazole.Approved
BanoxantroneThe metabolism of Banoxantrone can be decreased when combined with Ketoconazole.Investigational
BarnidipineThe serum concentration of Barnidipine can be increased when it is combined with Ketoconazole.Approved
Beclomethasone dipropionateThe serum concentration of Beclomethasone dipropionate can be increased when it is combined with Ketoconazole.Approved, Investigational
BedaquilineThe serum concentration of Bedaquiline can be increased when it is combined with Ketoconazole.Approved
BencyclaneThe risk or severity of adverse effects can be increased when Ketoconazole is combined with Bencyclane.Experimental
BenidipineThe risk or severity of adverse effects can be increased when Ketoconazole is combined with Benidipine.Approved, Investigational
BenzatropineThe metabolism of Benzatropine can be decreased when combined with Ketoconazole.Approved
BenzphetamineThe metabolism of Benzphetamine can be decreased when combined with Ketoconazole.Approved, Illicit
Benzyl alcoholThe metabolism of Benzyl alcohol can be decreased when combined with Ketoconazole.Approved
BepridilThe risk or severity of adverse effects can be increased when Ketoconazole is combined with Bepridil.Approved, Withdrawn
BetamethasoneThe serum concentration of Betamethasone can be increased when it is combined with Ketoconazole.Approved, Vet Approved
BetaxololThe metabolism of Betaxolol can be decreased when combined with Ketoconazole.Approved
BexaroteneThe metabolism of Bexarotene can be decreased when combined with Ketoconazole.Approved, Investigational
BezafibrateThe metabolism of Bezafibrate can be decreased when combined with Ketoconazole.Approved
BicalutamideThe metabolism of Bicalutamide can be decreased when combined with Ketoconazole.Approved
Bismuth SubcitrateThe serum concentration of Ketoconazole can be decreased when it is combined with Bismuth Subcitrate.Approved
Bismuth subnitrateThe serum concentration of Ketoconazole can be decreased when it is combined with Bismuth subnitrate.Experimental
BisoprololThe metabolism of Bisoprolol can be decreased when combined with Ketoconazole.Approved
BoceprevirThe serum concentration of Boceprevir can be increased when it is combined with Ketoconazole.Approved, Withdrawn
BortezomibThe serum concentration of Bortezomib can be increased when it is combined with Ketoconazole.Approved, Investigational
BosentanThe serum concentration of Bosentan can be increased when it is combined with Ketoconazole.Approved, Investigational
BosutinibThe serum concentration of Bosutinib can be increased when it is combined with Ketoconazole.Approved
Brentuximab vedotinThe serum concentration of Brentuximab vedotin can be increased when it is combined with Ketoconazole.Approved
BrexpiprazoleThe serum concentration of Brexpiprazole can be increased when it is combined with Ketoconazole.Approved
BrinzolamideThe serum concentration of Brinzolamide can be increased when it is combined with Ketoconazole.Approved
BrivaracetamThe metabolism of Brivaracetam can be decreased when combined with Ketoconazole.Approved, Investigational
BromazepamThe metabolism of Bromazepam can be decreased when combined with Ketoconazole.Approved, Illicit
BromocriptineThe metabolism of Bromocriptine can be decreased when combined with Ketoconazole.Approved, Investigational
BrompheniramineThe metabolism of Brompheniramine can be decreased when combined with Ketoconazole.Approved
BudesonideThe serum concentration of Budesonide can be increased when it is combined with Ketoconazole.Approved
BufuralolThe metabolism of Bufuralol can be decreased when combined with Ketoconazole.Experimental, Investigational
BupivacaineThe metabolism of Bupivacaine can be decreased when combined with Ketoconazole.Approved, Investigational
BuprenorphineThe metabolism of Buprenorphine can be decreased when combined with Ketoconazole.Approved, Illicit, Investigational, Vet Approved
BupropionThe metabolism of Bupropion can be decreased when combined with Ketoconazole.Approved
BuspironeThe metabolism of Buspirone can be decreased when combined with Ketoconazole.Approved, Investigational
BusulfanThe serum concentration of Busulfan can be increased when it is combined with Ketoconazole.Approved, Investigational
CabazitaxelThe serum concentration of Cabazitaxel can be increased when it is combined with Ketoconazole.Approved
CabergolineThe metabolism of Cabergoline can be decreased when combined with Ketoconazole.Approved
CabozantinibThe serum concentration of Cabozantinib can be increased when it is combined with Ketoconazole.Approved
CaffeineThe metabolism of Caffeine can be decreased when combined with Ketoconazole.Approved
CalcitriolThe metabolism of Calcitriol can be decreased when combined with Ketoconazole.Approved, Nutraceutical
Calcium CarbonateThe serum concentration of Ketoconazole can be decreased when it is combined with Calcium Carbonate.Approved
Calcium silicateThe serum concentration of Ketoconazole can be decreased when it is combined with Calcium silicate.Experimental
CanagliflozinThe metabolism of Canagliflozin can be decreased when combined with Ketoconazole.Approved
CandesartanThe metabolism of Candesartan can be decreased when combined with Ketoconazole.Experimental
Candesartan cilexetilThe metabolism of Candesartan cilexetil can be decreased when combined with Ketoconazole.Approved
CaptoprilThe metabolism of Captopril can be decreased when combined with Ketoconazole.Approved
CarbamazepineThe metabolism of Ketoconazole can be increased when combined with Carbamazepine.Approved, Investigational
CarbinoxamineThe metabolism of Carbinoxamine can be decreased when combined with Ketoconazole.Approved
CarbocisteineThe risk or severity of adverse effects can be increased when Ketoconazole is combined with Carbocisteine.Approved, Investigational
CarboxyamidotriazoleThe risk or severity of adverse effects can be increased when Ketoconazole is combined with Carboxyamidotriazole.Investigational
CariprazineThe metabolism of Cariprazine can be decreased when combined with Ketoconazole.Approved
CarisoprodolThe metabolism of Carisoprodol can be decreased when combined with Ketoconazole.Approved
CaroverineThe risk or severity of adverse effects can be increased when Ketoconazole is combined with Caroverine.Experimental
CarteololThe metabolism of Carteolol can be decreased when combined with Ketoconazole.Approved
CarvedilolThe serum concentration of Carvedilol can be increased when it is combined with Ketoconazole.Approved, Investigational
CelecoxibThe metabolism of Celecoxib can be decreased when combined with Ketoconazole.Approved, Investigational
CeliprololThe metabolism of Celiprolol can be decreased when combined with Ketoconazole.Approved, Investigational
CephalexinThe metabolism of Cephalexin can be decreased when combined with Ketoconazole.Approved, Vet Approved
CeritinibThe serum concentration of Ketoconazole can be increased when it is combined with Ceritinib.Approved
CerivastatinThe metabolism of Cerivastatin can be decreased when combined with Ketoconazole.Withdrawn
CevimelineThe metabolism of Cevimeline can be decreased when combined with Ketoconazole.Approved
Chenodeoxycholic acidThe metabolism of Chenodeoxycholic acid can be decreased when combined with Ketoconazole.Approved
ChloramphenicolThe metabolism of Chloramphenicol can be decreased when combined with Ketoconazole.Approved, Vet Approved
ChlordiazepoxideThe metabolism of Chlordiazepoxide can be decreased when combined with Ketoconazole.Approved, Illicit
ChloroquineThe metabolism of Chloroquine can be decreased when combined with Ketoconazole.Approved, Vet Approved
ChlorphenamineThe metabolism of Chlorphenamine can be decreased when combined with Ketoconazole.Approved
ChlorpromazineThe metabolism of Chlorpromazine can be decreased when combined with Ketoconazole.Approved, Vet Approved
ChlorpropamideThe metabolism of Chlorpropamide can be decreased when combined with Ketoconazole.Approved
ChlorzoxazoneThe metabolism of Chlorzoxazone can be decreased when combined with Ketoconazole.Approved
CholecalciferolThe metabolism of Cholecalciferol can be decreased when combined with Ketoconazole.Approved, Nutraceutical
Cholic AcidKetoconazole may decrease the excretion rate of Cholic Acid which could result in a higher serum level.Approved
CiclesonideThe metabolism of Ciclesonide can be decreased when combined with Ketoconazole.Approved, Investigational
CilnidipineThe risk or severity of adverse effects can be increased when Ketoconazole is combined with Cilnidipine.Approved, Investigational
CilostazolThe serum concentration of Cilostazol can be increased when it is combined with Ketoconazole.Approved
CimetidineThe serum concentration of Ketoconazole can be decreased when it is combined with Cimetidine.Approved
CinacalcetThe metabolism of Cinacalcet can be decreased when combined with Ketoconazole.Approved
CinnarizineThe risk or severity of adverse effects can be increased when Ketoconazole is combined with Cinnarizine.Approved, Investigational
CiprofloxacinKetoconazole may increase the QTc-prolonging activities of Ciprofloxacin.Approved, Investigational
CisaprideThe serum concentration of Cisapride can be increased when it is combined with Ketoconazole.Approved, Investigational, Withdrawn
CitalopramThe serum concentration of Citalopram can be increased when it is combined with Ketoconazole.Approved
ClarithromycinThe metabolism of Clarithromycin can be decreased when combined with Ketoconazole.Approved
ClemastineThe metabolism of Ketoconazole can be decreased when combined with Clemastine.Approved
ClevidipineThe risk or severity of adverse effects can be increased when Ketoconazole is combined with Clevidipine.Approved
ClindamycinThe metabolism of Clindamycin can be decreased when combined with Ketoconazole.Approved, Vet Approved
ClobazamThe metabolism of Clobazam can be decreased when combined with Ketoconazole.Approved, Illicit
ClobetasolThe serum concentration of Clobetasol can be increased when it is combined with Ketoconazole.Investigational
Clobetasol propionateThe serum concentration of Clobetasol propionate can be increased when it is combined with Ketoconazole.Approved
ClobetasoneThe serum concentration of Clobetasone can be increased when it is combined with Ketoconazole.Approved
ClocortoloneThe serum concentration of Clocortolone can be increased when it is combined with Ketoconazole.Approved
ClofazimineThe metabolism of Clofazimine can be decreased when combined with Ketoconazole.Approved, Investigational
ClofibrateThe metabolism of Clofibrate can be decreased when combined with Ketoconazole.Approved, Investigational
clomethiazoleThe metabolism of clomethiazole can be decreased when combined with Ketoconazole.Investigational
ClomipramineThe metabolism of Clomipramine can be decreased when combined with Ketoconazole.Approved, Vet Approved
ClonazepamThe metabolism of Clonazepam can be decreased when combined with Ketoconazole.Approved, Illicit
ClonidineThe metabolism of Clonidine can be decreased when combined with Ketoconazole.Approved
ClopidogrelThe serum concentration of the active metabolites of Clopidogrel can be reduced when Clopidogrel is used in combination with Ketoconazole resulting in a loss in efficacy.Approved, Nutraceutical
ClorazepateThe metabolism of Clorazepate can be decreased when combined with Ketoconazole.Approved, Illicit
ClorindioneThe serum concentration of Clorindione can be increased when it is combined with Ketoconazole.Experimental
ClotiazepamThe metabolism of Clotiazepam can be decreased when combined with Ketoconazole.Approved, Illicit
ClotrimazoleThe metabolism of Ketoconazole can be decreased when combined with Clotrimazole.Approved, Vet Approved
ClozapineThe metabolism of Clozapine can be decreased when combined with Ketoconazole.Approved
CobicistatThe serum concentration of Cobicistat can be increased when it is combined with Ketoconazole.Approved
CobimetinibThe serum concentration of Cobimetinib can be increased when it is combined with Ketoconazole.Approved
CocaineThe metabolism of Cocaine can be decreased when combined with Ketoconazole.Approved, Illicit
CodeineThe therapeutic efficacy of Codeine can be decreased when used in combination with Ketoconazole.Approved, Illicit
ColchicineThe serum concentration of Colchicine can be increased when it is combined with Ketoconazole.Approved
ConivaptanThe serum concentration of Conivaptan can be increased when it is combined with Ketoconazole.Approved, Investigational
Conjugated estrogensThe metabolism of Conjugated estrogens can be decreased when combined with Ketoconazole.Approved
CopanlisibThe metabolism of Copanlisib can be decreased when combined with Ketoconazole.Approved
Cortexolone 17α-propionateThe serum concentration of Cortexolone 17α-propionate can be increased when it is combined with Ketoconazole.Investigational
CorticosteroneThe serum concentration of Corticosterone can be increased when it is combined with Ketoconazole.Experimental
Cortisone acetateThe metabolism of Cortisone acetate can be decreased when combined with Ketoconazole.Approved
CrizotinibThe serum concentration of Crizotinib can be increased when it is combined with Ketoconazole.Approved
CyclobenzaprineThe metabolism of Cyclobenzaprine can be decreased when combined with Ketoconazole.Approved
CyclophosphamideThe metabolism of Cyclophosphamide can be decreased when combined with Ketoconazole.Approved, Investigational
CyclosporineThe metabolism of Cyclosporine can be decreased when combined with Ketoconazole.Approved, Investigational, Vet Approved
CytarabineThe metabolism of Cytarabine can be decreased when combined with Ketoconazole.Approved, Investigational
Dabigatran etexilateThe serum concentration of Dabigatran etexilate can be increased when it is combined with Ketoconazole.Approved
DabrafenibThe serum concentration of Ketoconazole can be decreased when it is combined with Dabrafenib.Approved
DaclatasvirThe serum concentration of Daclatasvir can be increased when it is combined with Ketoconazole.Approved
DantroleneThe metabolism of Dantrolene can be decreased when combined with Ketoconazole.Approved
DapagliflozinThe metabolism of Dapagliflozin can be decreased when combined with Ketoconazole.Approved
DapoxetineThe serum concentration of Dapoxetine can be increased when it is combined with Ketoconazole.Investigational
DapsoneThe metabolism of Dapsone can be decreased when combined with Ketoconazole.Approved, Investigational
DarifenacinThe metabolism of Darifenacin can be decreased when combined with Ketoconazole.Approved, Investigational
DarodipineThe risk or severity of adverse effects can be increased when Ketoconazole is combined with Darodipine.Experimental
DarunavirThe serum concentration of Ketoconazole can be increased when it is combined with Darunavir.Approved
DasabuvirThe metabolism of Dasabuvir can be decreased when combined with Ketoconazole.Approved
DasatinibThe serum concentration of Dasatinib can be increased when it is combined with Ketoconazole.Approved, Investigational
DaunorubicinThe metabolism of Daunorubicin can be decreased when combined with Ketoconazole.Approved
DebrisoquinThe metabolism of Debrisoquin can be decreased when combined with Ketoconazole.Approved, Investigational
DeferasiroxThe serum concentration of Ketoconazole can be decreased when it is combined with Deferasirox.Approved, Investigational
DeflazacortThe metabolism of Deflazacort can be decreased when combined with Ketoconazole.Approved
DelavirdineThe metabolism of Delavirdine can be decreased when combined with Ketoconazole.Approved
DesipramineThe metabolism of Desipramine can be decreased when combined with Ketoconazole.Approved
DesonideThe serum concentration of Desonide can be increased when it is combined with Ketoconazole.Approved, Investigational
DesoximetasoneThe serum concentration of Desoximetasone can be increased when it is combined with Ketoconazole.Approved
Desoxycorticosterone acetateThe serum concentration of Desoxycorticosterone acetate can be increased when it is combined with Ketoconazole.Approved
Desoxycorticosterone PivalateThe serum concentration of Desoxycorticosterone Pivalate can be increased when it is combined with Ketoconazole.Experimental, Vet Approved
DesvenlafaxineThe metabolism of Desvenlafaxine can be decreased when combined with Ketoconazole.Approved
DeutetrabenazineThe metabolism of Deutetrabenazine can be decreased when combined with Ketoconazole.Approved, Investigational
DexamethasoneThe metabolism of Dexamethasone can be decreased when combined with Ketoconazole.Approved, Investigational, Vet Approved
Dexamethasone isonicotinateThe serum concentration of Dexamethasone isonicotinate can be increased when it is combined with Ketoconazole.Vet Approved
Dexchlorpheniramine maleateThe metabolism of Dexchlorpheniramine maleate can be decreased when combined with Ketoconazole.Approved
DexfenfluramineThe metabolism of Dexfenfluramine can be decreased when combined with Ketoconazole.Approved, Illicit, Investigational, Withdrawn
DexlansoprazoleThe serum concentration of Ketoconazole can be decreased when it is combined with Dexlansoprazole.Approved
DexmethylphenidateThe metabolism of Dexmethylphenidate can be decreased when combined with Ketoconazole.Approved
DexrabeprazoleThe serum concentration of Ketoconazole can be decreased when it is combined with Dexrabeprazole.Experimental
DextroamphetamineThe metabolism of Dextroamphetamine can be decreased when combined with Ketoconazole.Approved, Illicit
DextromethorphanThe metabolism of Dextromethorphan can be decreased when combined with Ketoconazole.Approved
DextropropoxypheneThe metabolism of Dextropropoxyphene can be decreased when combined with Ketoconazole.Approved, Illicit, Investigational, Withdrawn
DiazepamThe metabolism of Diazepam can be decreased when combined with Ketoconazole.Approved, Illicit, Vet Approved
DiclofenacThe metabolism of Diclofenac can be decreased when combined with Ketoconazole.Approved, Vet Approved
DicoumarolThe serum concentration of Dicoumarol can be increased when it is combined with Ketoconazole.Approved
DidanosineDidanosine can cause a decrease in the absorption of Ketoconazole resulting in a reduced serum concentration and potentially a decrease in efficacy.Approved
DienogestThe serum concentration of Dienogest can be increased when it is combined with Ketoconazole.Approved
DiflorasoneThe serum concentration of Diflorasone can be increased when it is combined with Ketoconazole.Approved
DifluocortoloneThe serum concentration of Difluocortolone can be increased when it is combined with Ketoconazole.Approved, Investigational
DifluprednateThe serum concentration of Difluprednate can be increased when it is combined with Ketoconazole.Approved
DigitoxinThe metabolism of Digitoxin can be decreased when combined with Ketoconazole.Approved, Investigational
DigoxinThe metabolism of Digoxin can be decreased when combined with Ketoconazole.Approved
DihydrocodeineThe metabolism of Dihydrocodeine can be decreased when combined with Ketoconazole.Approved, Illicit
DihydroergocornineThe risk or severity of adverse effects can be increased when Dihydroergocornine is combined with Ketoconazole.Approved
DihydroergocristineThe risk or severity of adverse effects can be increased when Dihydroergocristine is combined with Ketoconazole.Experimental
DihydroergocryptineThe risk or severity of adverse effects can be increased when Dihydroergocryptine is combined with Ketoconazole.Experimental
DihydroergotamineThe serum concentration of Dihydroergotamine can be increased when it is combined with Ketoconazole.Approved
DiltiazemThe metabolism of Diltiazem can be decreased when combined with Ketoconazole.Approved
DiphenadioneThe serum concentration of Diphenadione can be increased when it is combined with Ketoconazole.Experimental
DiphenhydramineThe metabolism of Diphenhydramine can be decreased when combined with Ketoconazole.Approved
DisopyramideThe serum concentration of Disopyramide can be increased when it is combined with Ketoconazole.Approved
DisulfiramThe metabolism of Disulfiram can be decreased when combined with Ketoconazole.Approved
DocetaxelThe metabolism of Docetaxel can be decreased when combined with Ketoconazole.Approved, Investigational
DoconexentThe metabolism of Doconexent can be decreased when combined with Ketoconazole.Approved, Investigational
DofetilideThe serum concentration of Dofetilide can be increased when it is combined with Ketoconazole.Approved
DolasetronThe metabolism of Dolasetron can be decreased when combined with Ketoconazole.Approved
DomperidoneThe serum concentration of Domperidone can be increased when it is combined with Ketoconazole.Approved, Investigational, Vet Approved
DonepezilThe metabolism of Donepezil can be decreased when combined with Ketoconazole.Approved
DopamineThe metabolism of Dopamine can be decreased when combined with Ketoconazole.Approved
DorzolamideThe metabolism of Dorzolamide can be decreased when combined with Ketoconazole.Approved
DotarizineThe risk or severity of adverse effects can be increased when Ketoconazole is combined with Dotarizine.Investigational
DoxazosinThe metabolism of Doxazosin can be decreased when combined with Ketoconazole.Approved
DoxepinThe serum concentration of Ketoconazole can be decreased when it is combined with Doxepin.Approved
DoxorubicinThe serum concentration of Doxorubicin can be increased when it is combined with Ketoconazole.Approved, Investigational
DoxorubicinThe metabolism of Doxorubicin can be decreased when combined with Ketoconazole.Approved, Investigational
DoxycyclineThe metabolism of Ketoconazole can be decreased when combined with Doxycycline.Approved, Investigational, Vet Approved
DronabinolThe serum concentration of Dronabinol can be increased when it is combined with Ketoconazole.Approved, Illicit
DronedaroneThe serum concentration of Dronedarone can be increased when it is combined with Ketoconazole.Approved
DroperidolKetoconazole may increase the QTc-prolonging activities of Droperidol.Approved, Vet Approved
DrospirenoneThe serum concentration of Drospirenone can be increased when it is combined with Ketoconazole.Approved
DuloxetineThe metabolism of Duloxetine can be decreased when combined with Ketoconazole.Approved
DutasterideThe serum concentration of Dutasteride can be increased when it is combined with Ketoconazole.Approved, Investigational
EdoxabanThe serum concentration of Edoxaban can be increased when it is combined with Ketoconazole.Approved
EfavirenzThe serum concentration of Ketoconazole can be decreased when it is combined with Efavirenz.Approved, Investigational
EfonidipineThe risk or severity of adverse effects can be increased when Ketoconazole is combined with Efonidipine.Approved, Investigational
ElbasvirThe metabolism of Elbasvir can be decreased when combined with Ketoconazole.Approved
EletriptanThe serum concentration of Eletriptan can be increased when it is combined with Ketoconazole.Approved, Investigational
EliglustatThe serum concentration of Eliglustat can be increased when it is combined with Ketoconazole.Approved
ElvitegravirThe serum concentration of Elvitegravir can be increased when it is combined with Ketoconazole.Approved
EnalaprilThe metabolism of Enalapril can be decreased when combined with Ketoconazole.Approved, Vet Approved
EnasidenibThe metabolism of Enasidenib can be decreased when combined with Ketoconazole.Approved
EncainideThe metabolism of Encainide can be decreased when combined with Ketoconazole.Approved, Investigational, Withdrawn
EnclomipheneThe metabolism of Enclomiphene can be decreased when combined with Ketoconazole.Investigational
EnfuvirtideThe metabolism of Enfuvirtide can be decreased when combined with Ketoconazole.Approved, Investigational
EnzalutamideThe serum concentration of Ketoconazole can be decreased when it is combined with Enzalutamide.Approved
EperisoneThe risk or severity of adverse effects can be increased when Ketoconazole is combined with Eperisone.Approved, Investigational
EpinastineThe serum concentration of Ketoconazole can be decreased when it is combined with Epinastine.Approved, Investigational
EplerenoneThe serum concentration of Eplerenone can be increased when it is combined with Ketoconazole.Approved
EpoprostenolThe metabolism of Epoprostenol can be decreased when combined with Ketoconazole.Approved
EquileninThe serum concentration of Equilenin can be increased when it is combined with Ketoconazole.Experimental
EquilinThe serum concentration of Equilin can be increased when it is combined with Ketoconazole.Approved
ErgocalciferolThe metabolism of Ergocalciferol can be decreased when combined with Ketoconazole.Approved, Nutraceutical
Ergoloid mesylateThe serum concentration of Ergoloid mesylate can be increased when it is combined with Ketoconazole.Approved
ErgonovineThe serum concentration of Ergonovine can be increased when it is combined with Ketoconazole.Approved
ErgotamineThe serum concentration of Ergotamine can be increased when it is combined with Ketoconazole.Approved
ErlotinibThe serum concentration of Erlotinib can be increased when it is combined with Ketoconazole.Approved, Investigational
ErythromycinThe metabolism of Erythromycin can be decreased when combined with Ketoconazole.Approved, Vet Approved
EscitalopramThe metabolism of Escitalopram can be decreased when combined with Ketoconazole.Approved, Investigational
EsmirtazapineThe metabolism of Esmirtazapine can be decreased when combined with Ketoconazole.Investigational
EsomeprazoleThe serum concentration of Ketoconazole can be decreased when it is combined with Esomeprazole.Approved, Investigational
EstazolamThe serum concentration of Estazolam can be increased when it is combined with Ketoconazole.Approved, Illicit
EstradiolThe metabolism of Estradiol can be decreased when combined with Ketoconazole.Approved, Investigational, Vet Approved
Estradiol valerate/DienogestThe metabolism of Estradiol valerate/Dienogest can be decreased when combined with Ketoconazole.Approved, Investigational
EstramustineThe metabolism of Estramustine can be decreased when combined with Ketoconazole.Approved
Estrogens, esterifiedThe metabolism of Estrogens, esterified can be decreased when combined with Ketoconazole.Approved
EstroneThe metabolism of Estrone can be decreased when combined with Ketoconazole.Approved
Estrone sulfateThe metabolism of Estrone sulfate can be decreased when combined with Ketoconazole.Approved
EszopicloneThe metabolism of Eszopiclone can be decreased when combined with Ketoconazole.Approved
EthanolThe risk or severity of adverse effects can be increased when Ketoconazole is combined with Ethanol.Approved
Ethinyl EstradiolThe metabolism of Ethinyl Estradiol can be decreased when combined with Ketoconazole.Approved
EthosuximideThe metabolism of Ethosuximide can be decreased when combined with Ketoconazole.Approved
Ethyl biscoumacetateThe serum concentration of Ethyl biscoumacetate can be increased when it is combined with Ketoconazole.Withdrawn
EthylmorphineThe metabolism of Ethylmorphine can be decreased when combined with Ketoconazole.Approved, Illicit
EtizolamThe serum concentration of Etizolam can be increased when it is combined with Ketoconazole.Approved
EtodolacThe metabolism of Etodolac can be decreased when combined with Ketoconazole.Approved, Investigational, Vet Approved
EtonogestrelThe metabolism of Etonogestrel can be decreased when combined with Ketoconazole.Approved, Investigational
EtoposideThe metabolism of Etoposide can be decreased when combined with Ketoconazole.Approved
EtoricoxibThe metabolism of Etoricoxib can be decreased when combined with Ketoconazole.Approved, Investigational
EtravirineThe serum concentration of Etravirine can be increased when it is combined with Ketoconazole.Approved
EverolimusThe serum concentration of Everolimus can be increased when it is combined with Ketoconazole.Approved
ExemestaneThe metabolism of Exemestane can be decreased when combined with Ketoconazole.Approved, Investigational
FamciclovirThe metabolism of Famciclovir can be decreased when combined with Ketoconazole.Approved
FamotidineThe serum concentration of Ketoconazole can be decreased when it is combined with Famotidine.Approved
FelbamateThe metabolism of Felbamate can be decreased when combined with Ketoconazole.Approved
FelodipineThe serum concentration of Felodipine can be increased when it is combined with Ketoconazole.Approved, Investigational
FendilineThe risk or severity of adverse effects can be increased when Ketoconazole is combined with Fendiline.Withdrawn
FenofibrateThe metabolism of Fenofibrate can be decreased when combined with Ketoconazole.Approved
FentanylThe serum concentration of Fentanyl can be increased when it is combined with Ketoconazole.Approved, Illicit, Investigational, Vet Approved
FesoterodineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Ketoconazole.Approved
FexofenadineThe serum concentration of Fexofenadine can be increased when it is combined with Ketoconazole.Approved
FimasartanThe serum concentration of Fimasartan can be increased when it is combined with Ketoconazole.Approved, Investigational
FinasterideThe metabolism of Finasteride can be decreased when combined with Ketoconazole.Approved
FingolimodThe serum concentration of the active metabolites of Fingolimod can be increased when Fingolimod is used in combination with Ketoconazole.Approved, Investigational
FlecainideKetoconazole may increase the QTc-prolonging activities of Flecainide.Approved, Withdrawn
FlibanserinThe serum concentration of Flibanserin can be increased when it is combined with Ketoconazole.Approved
fluasteroneThe serum concentration of fluasterone can be increased when it is combined with Ketoconazole.Investigational
FluconazoleThe metabolism of Ketoconazole can be decreased when combined with Fluconazole.Approved
FludrocortisoneThe serum concentration of Fludrocortisone can be increased when it is combined with Ketoconazole.Approved
FluindioneThe serum concentration of Fluindione can be increased when it is combined with Ketoconazole.Investigational
FlumethasoneThe serum concentration of Flumethasone can be increased when it is combined with Ketoconazole.Approved, Vet Approved
FlunarizineThe risk or severity of adverse effects can be increased when Ketoconazole is combined with Flunarizine.Approved
FlunisolideThe metabolism of Flunisolide can be decreased when combined with Ketoconazole.Approved, Investigational
FlunitrazepamThe metabolism of Flunitrazepam can be decreased when combined with Ketoconazole.Approved, Illicit
Fluocinolone AcetonideThe serum concentration of Fluocinolone Acetonide can be increased when it is combined with Ketoconazole.Approved, Investigational, Vet Approved
FluocinonideThe serum concentration of Fluocinonide can be increased when it is combined with Ketoconazole.Approved, Investigational
FluocortoloneThe serum concentration of Fluocortolone can be increased when it is combined with Ketoconazole.Approved, Withdrawn
FluorometholoneThe metabolism of Fluorometholone can be decreased when combined with Ketoconazole.Approved
FluoxetineThe metabolism of Fluoxetine can be decreased when combined with Ketoconazole.Approved, Vet Approved
FlupentixolKetoconazole may increase the QTc-prolonging activities of Flupentixol.Approved, Withdrawn
FluphenazineThe metabolism of Fluphenazine can be decreased when combined with Ketoconazole.Approved
FluprednideneThe serum concentration of Fluprednidene can be increased when it is combined with Ketoconazole.Approved, Withdrawn
FluprednisoloneThe serum concentration of Fluprednisolone can be increased when it is combined with Ketoconazole.Approved
FlurandrenolideThe serum concentration of Flurandrenolide can be increased when it is combined with Ketoconazole.Approved
FlurazepamThe metabolism of Flurazepam can be decreased when combined with Ketoconazole.Approved, Illicit
FlurbiprofenThe metabolism of Flurbiprofen can be decreased when combined with Ketoconazole.Approved, Investigational
FlutamideThe metabolism of Flutamide can be decreased when combined with Ketoconazole.Approved
Fluticasone furoateThe metabolism of Fluticasone furoate can be decreased when combined with Ketoconazole.Approved
Fluticasone propionateThe serum concentration of Fluticasone propionate can be increased when it is combined with Ketoconazole.Approved
FluvastatinThe metabolism of Fluvastatin can be decreased when combined with Ketoconazole.Approved
FluvoxamineThe metabolism of Ketoconazole can be decreased when combined with Fluvoxamine.Approved, Investigational
FormestaneThe serum concentration of Formestane can be increased when it is combined with Ketoconazole.Approved, Investigational, Withdrawn
FormoterolThe metabolism of Formoterol can be decreased when combined with Ketoconazole.Approved, Investigational
FosamprenavirThe serum concentration of the active metabolites of Fosamprenavir can be increased when Fosamprenavir is used in combination with Ketoconazole.Approved
FosaprepitantThe serum concentration of Ketoconazole can be increased when it is combined with Fosaprepitant.Approved
FosphenytoinThe serum concentration of Ketoconazole can be decreased when it is combined with Fosphenytoin.Approved
FulvestrantThe metabolism of Fulvestrant can be decreased when combined with Ketoconazole.Approved, Investigational
Fusidic AcidThe serum concentration of Ketoconazole can be increased when it is combined with Fusidic Acid.Approved
GabapentinThe risk or severity of adverse effects can be increased when Ketoconazole is combined with Gabapentin.Approved, Investigational
Gadobenic acidKetoconazole may increase the QTc-prolonging activities of Gadobenic acid.Approved
GalantamineThe metabolism of Galantamine can be decreased when combined with Ketoconazole.Approved
GallopamilThe risk or severity of adverse effects can be increased when Ketoconazole is combined with Gallopamil.Investigational
GavestinelThe metabolism of Gavestinel can be decreased when combined with Ketoconazole.Investigational
GefitinibThe metabolism of Gefitinib can be decreased when combined with Ketoconazole.Approved, Investigational
GemfibrozilThe metabolism of Gemfibrozil can be decreased when combined with Ketoconazole.Approved
GemifloxacinKetoconazole may increase the QTc-prolonging activities of Gemifloxacin.Approved, Investigational
GliclazideThe metabolism of Gliclazide can be decreased when combined with Ketoconazole.Approved
GlimepirideThe metabolism of Glimepiride can be decreased when combined with Ketoconazole.Approved
GlipizideThe metabolism of Glipizide can be decreased when combined with Ketoconazole.Approved
GlucosamineThe metabolism of Glucosamine can be decreased when combined with Ketoconazole.Approved
GlyburideThe metabolism of Glyburide can be decreased when combined with Ketoconazole.Approved
GoserelinKetoconazole may increase the QTc-prolonging activities of Goserelin.Approved
GranisetronThe metabolism of Granisetron can be decreased when combined with Ketoconazole.Approved, Investigational
GrazoprevirThe metabolism of Grazoprevir can be decreased when combined with Ketoconazole.Approved
GrepafloxacinThe metabolism of Grepafloxacin can be decreased when combined with Ketoconazole.Investigational, Withdrawn
GuanfacineThe serum concentration of Guanfacine can be increased when it is combined with Ketoconazole.Approved, Investigational
HalcinonideThe serum concentration of Halcinonide can be increased when it is combined with Ketoconazole.Approved, Investigational, Withdrawn
HalofantrineThe serum concentration of Halofantrine can be increased when it is combined with Ketoconazole.Approved
HaloperidolThe metabolism of Haloperidol can be decreased when combined with Ketoconazole.Approved
HalothaneThe metabolism of Halothane can be decreased when combined with Ketoconazole.Approved, Vet Approved
HE3286The serum concentration of HE3286 can be increased when it is combined with Ketoconazole.Investigational
HexobarbitalThe metabolism of Hexobarbital can be decreased when combined with Ketoconazole.Approved
HistamineThe metabolism of Histamine can be decreased when combined with Ketoconazole.Approved, Investigational
HydrocodoneThe serum concentration of Hydrocodone can be increased when it is combined with Ketoconazole.Approved, Illicit
HydrocortisoneThe metabolism of Hydrocortisone can be decreased when combined with Ketoconazole.Approved, Vet Approved
HydromorphoneThe metabolism of Hydromorphone can be decreased when combined with Ketoconazole.Approved, Illicit
HydrotalciteThe serum concentration of Ketoconazole can be decreased when it is combined with Hydrotalcite.Experimental, Investigational
Hydroxyprogesterone caproateThe metabolism of Hydroxyprogesterone caproate can be decreased when combined with Ketoconazole.Approved
IbrutinibThe serum concentration of Ibrutinib can be increased when it is combined with Ketoconazole.Approved
IbuprofenThe metabolism of Ibuprofen can be decreased when combined with Ketoconazole.Approved
IbutilideKetoconazole may increase the QTc-prolonging activities of Ibutilide.Approved
IcotinibThe metabolism of Icotinib can be decreased when combined with Ketoconazole.Approved, Investigational
IdarubicinThe metabolism of Idarubicin can be decreased when combined with Ketoconazole.Approved
IdelalisibThe serum concentration of Idelalisib can be increased when it is combined with Ketoconazole.Approved
IfosfamideThe serum concentration of the active metabolites of Ifosfamide can be reduced when Ifosfamide is used in combination with Ketoconazole resulting in a loss in efficacy.Approved
IloperidoneThe serum concentration of the active metabolites of Iloperidone can be increased when Iloperidone is used in combination with Ketoconazole.Approved
ImatinibThe serum concentration of Imatinib can be increased when it is combined with Ketoconazole.Approved
ImidafenacinThe serum concentration of Imidafenacin can be increased when it is combined with Ketoconazole.Approved, Investigational
ImipramineThe metabolism of Imipramine can be decreased when combined with Ketoconazole.Approved
ImiquimodThe metabolism of Imiquimod can be decreased when combined with Ketoconazole.Approved, Investigational
IndacaterolThe metabolism of Indacaterol can be decreased when combined with Ketoconazole.Approved
IndapamideThe metabolism of Indapamide can be decreased when combined with Ketoconazole.Approved
IndinavirThe serum concentration of Indinavir can be increased when it is combined with Ketoconazole.Approved
indisulamThe metabolism of indisulam can be decreased when combined with Ketoconazole.Investigational
IndomethacinThe metabolism of Indomethacin can be decreased when combined with Ketoconazole.Approved, Investigational
Ipratropium bromideThe metabolism of Ipratropium bromide can be decreased when combined with Ketoconazole.Approved
IrbesartanThe metabolism of Irbesartan can be decreased when combined with Ketoconazole.Approved, Investigational
IrinotecanThe serum concentration of Irinotecan can be increased when it is combined with Ketoconazole.Approved, Investigational
IsavuconazoniumThe serum concentration of the active metabolites of Isavuconazonium can be increased when Isavuconazonium is used in combination with Ketoconazole.Approved, Investigational
IsoniazidThe serum concentration of Ketoconazole can be decreased when it is combined with Isoniazid.Approved
Isosorbide DinitrateThe metabolism of Isosorbide Dinitrate can be decreased when combined with Ketoconazole.Approved
Isosorbide MononitrateThe metabolism of Isosorbide Mononitrate can be decreased when combined with Ketoconazole.Approved
IsradipineThe metabolism of Isradipine can be decreased when combined with Ketoconazole.Approved
IstaroximeThe serum concentration of Istaroxime can be increased when it is combined with Ketoconazole.Investigational
ItraconazoleThe metabolism of Itraconazole can be decreased when combined with Ketoconazole.Approved, Investigational
IvabradineThe serum concentration of Ivabradine can be increased when it is combined with Ketoconazole.Approved
IvacaftorThe serum concentration of Ivacaftor can be increased when it is combined with Ketoconazole.Approved
IvermectinThe metabolism of Ivermectin can be decreased when combined with Ketoconazole.Approved, Vet Approved
IxabepiloneThe serum concentration of Ixabepilone can be increased when it is combined with Ketoconazole.Approved, Investigational
IxazomibThe metabolism of Ixazomib can be decreased when combined with Ketoconazole.Approved
KetamineThe metabolism of Ketamine can be decreased when combined with Ketoconazole.Approved, Vet Approved
KetazolamThe metabolism of Ketazolam can be decreased when combined with Ketoconazole.Approved
KetobemidoneThe metabolism of Ketobemidone can be decreased when combined with Ketoconazole.Approved, Investigational
KetoprofenThe metabolism of Ketoprofen can be decreased when combined with Ketoconazole.Approved, Vet Approved
LabetalolThe metabolism of Labetalol can be decreased when combined with Ketoconazole.Approved
LacidipineThe risk or severity of adverse effects can be increased when Ketoconazole is combined with Lacidipine.Approved, Investigational
LacosamideThe serum concentration of Lacosamide can be increased when it is combined with Ketoconazole.Approved
LamotrigineThe risk or severity of adverse effects can be increased when Ketoconazole is combined with Lamotrigine.Approved, Investigational
LansoprazoleThe serum concentration of Ketoconazole can be decreased when it is combined with Lansoprazole.Approved, Investigational
LapatinibThe serum concentration of Lapatinib can be increased when it is combined with Ketoconazole.Approved, Investigational
LaquinimodThe metabolism of Laquinimod can be decreased when combined with Ketoconazole.Investigational
LedipasvirThe serum concentration of Ledipasvir can be increased when it is combined with Ketoconazole.Approved
LeflunomideThe metabolism of Leflunomide can be decreased when combined with Ketoconazole.Approved, Investigational
LenvatinibThe metabolism of Lenvatinib can be decreased when combined with Ketoconazole.Approved
LercanidipineThe serum concentration of Lercanidipine can be increased when it is combined with Ketoconazole.Approved, Investigational
LesinuradThe metabolism of Lesinurad can be decreased when combined with Ketoconazole.Approved
LetermovirThe metabolism of Letermovir can be decreased when combined with Ketoconazole.Approved
LetrozoleThe metabolism of Letrozole can be decreased when combined with Ketoconazole.Approved, Investigational
LeuprolideKetoconazole may increase the QTc-prolonging activities of Leuprolide.Approved, Investigational
LevobupivacaineThe serum concentration of Levobupivacaine can be increased when it is combined with Ketoconazole.Approved, Investigational
LevocetirizineThe metabolism of Levocetirizine can be decreased when combined with Ketoconazole.Approved
LevodopaThe metabolism of Levodopa can be decreased when combined with Ketoconazole.Approved
LevofloxacinKetoconazole may increase the QTc-prolonging activities of Levofloxacin.Approved, Investigational
Levomethadyl AcetateThe metabolism of Levomethadyl Acetate can be decreased when combined with Ketoconazole.Approved, Investigational
LevomilnacipranThe serum concentration of Levomilnacipran can be increased when it is combined with Ketoconazole.Approved
LevonorgestrelThe metabolism of Levonorgestrel can be decreased when combined with Ketoconazole.Approved, Investigational
LevothyroxineThe metabolism of Levothyroxine can be decreased when combined with Ketoconazole.Approved
LicofeloneThe metabolism of Licofelone can be decreased when combined with Ketoconazole.Investigational
LidocaineThe metabolism of Lidocaine can be decreased when combined with Ketoconazole.Approved, Vet Approved
LidoflazineThe risk or severity of adverse effects can be increased when Ketoconazole is combined with Lidoflazine.Experimental
LisurideThe metabolism of Lisuride can be decreased when combined with Ketoconazole.Approved, Investigational
LomitapideThe serum concentration of Lomitapide can be increased when it is combined with Ketoconazole.Approved
LomustineThe metabolism of Lomustine can be decreased when combined with Ketoconazole.Approved
LoperamideThe metabolism of Loperamide can be decreased when combined with Ketoconazole.Approved
LopinavirThe serum concentration of Lopinavir can be increased when it is combined with Ketoconazole.Approved
LoratadineThe metabolism of Loratadine can be decreased when combined with Ketoconazole.Approved
LorcaserinThe metabolism of Lorcaserin can be decreased when combined with Ketoconazole.Approved
LornoxicamThe metabolism of Lornoxicam can be decreased when combined with Ketoconazole.Approved, Investigational
LosartanThe metabolism of Losartan can be decreased when combined with Ketoconazole.Approved
LoteprednolThe serum concentration of Loteprednol can be increased when it is combined with Ketoconazole.Approved
LovastatinThe serum concentration of Lovastatin can be increased when it is combined with Ketoconazole.Approved, Investigational
LuliconazoleThe serum concentration of Ketoconazole can be increased when it is combined with Luliconazole.Approved
LumacaftorThe serum concentration of Ketoconazole can be decreased when it is combined with Lumacaftor.Approved
LumefantrineThe serum concentration of Lumefantrine can be increased when it is combined with Ketoconazole.Approved
LumiracoxibThe metabolism of Lumiracoxib can be decreased when combined with Ketoconazole.Approved, Investigational
LurasidoneThe serum concentration of Lurasidone can be increased when it is combined with Ketoconazole.Approved
Lysergic Acid DiethylamideThe risk or severity of adverse effects can be increased when Lysergic Acid Diethylamide is combined with Ketoconazole.Illicit, Investigational, Withdrawn
MacitentanThe serum concentration of Macitentan can be increased when it is combined with Ketoconazole.Approved
MagaldrateThe serum concentration of Ketoconazole can be decreased when it is combined with Magaldrate.Approved, Withdrawn
Magnesium HydroxideThe serum concentration of Ketoconazole can be decreased when it is combined with Magnesium Hydroxide.Approved
Magnesium oxideThe serum concentration of Ketoconazole can be decreased when it is combined with Magnesium oxide.Approved
Magnesium peroxideThe serum concentration of Ketoconazole can be decreased when it is combined with Magnesium peroxide.Experimental
Magnesium silicateThe serum concentration of Ketoconazole can be decreased when it is combined with Magnesium silicate.Approved, Experimental
Magnesium SulfateThe risk or severity of adverse effects can be increased when Ketoconazole is combined with Magnesium Sulfate.Approved, Vet Approved
Magnesium TrisilicateThe serum concentration of Ketoconazole can be decreased when it is combined with Magnesium Trisilicate.Approved
ManidipineThe risk or severity of adverse effects can be increased when Ketoconazole is combined with Manidipine.Approved, Investigational
MaprotilineThe metabolism of Maprotiline can be decreased when combined with Ketoconazole.Approved
MaravirocThe serum concentration of Maraviroc can be increased when it is combined with Ketoconazole.Approved, Investigational
ME-609The serum concentration of ME-609 can be increased when it is combined with Ketoconazole.Investigational
MebendazoleThe metabolism of Mebendazole can be decreased when combined with Ketoconazole.Approved, Vet Approved
Medroxyprogesterone acetateThe serum concentration of Medroxyprogesterone acetate can be increased when it is combined with Ketoconazole.Approved, Investigational
MedrysoneThe serum concentration of Medrysone can be increased when it is combined with Ketoconazole.Approved
Mefenamic acidThe metabolism of Mefenamic acid can be decreased when combined with Ketoconazole.Approved
MefloquineThe metabolism of Mefloquine can be decreased when combined with Ketoconazole.Approved
MelatoninThe metabolism of Melatonin can be decreased when combined with Ketoconazole.Approved, Nutraceutical, Vet Approved
MelengestrolThe serum concentration of Melengestrol can be increased when it is combined with Ketoconazole.Vet Approved
MeloxicamThe metabolism of Meloxicam can be decreased when combined with Ketoconazole.Approved, Vet Approved
MephenytoinThe metabolism of Mephenytoin can be decreased when combined with Ketoconazole.Investigational, Withdrawn
MeprobamateThe metabolism of Meprobamate can be decreased when combined with Ketoconazole.Approved, Illicit
MequitazineThe metabolism of Mequitazine can be decreased when combined with Ketoconazole.Approved
MesoridazineThe metabolism of Mesoridazine can be decreased when combined with Ketoconazole.Approved, Investigational
MestranolThe metabolism of Mestranol can be decreased when combined with Ketoconazole.Approved
MetergolineThe risk or severity of adverse effects can be increased when Metergoline is combined with Ketoconazole.Experimental
MethadoneThe serum concentration of Methadone can be increased when it is combined with Ketoconazole.Approved
MethamphetamineThe metabolism of Methamphetamine can be decreased when combined with Ketoconazole.Approved, Illicit
MethanthelineThe serum concentration of Ketoconazole can be decreased when it is combined with Methantheline.Approved, Investigational
MethaqualoneThe metabolism of Methaqualone can be decreased when combined with Ketoconazole.Illicit, Withdrawn
MethotrimeprazineThe metabolism of Methotrimeprazine can be decreased when combined with Ketoconazole.Approved
MethoxsalenThe metabolism of Methoxsalen can be decreased when combined with Ketoconazole.Approved
MethoxyfluraneThe metabolism of Methoxyflurane can be decreased when combined with Ketoconazole.Approved, Investigational, Vet Approved
MethsuximideThe metabolism of Methsuximide can be decreased when combined with Ketoconazole.Approved
MethylergometrineThe serum concentration of Methylergometrine can be increased when it is combined with Ketoconazole.Approved
MethylphenidateThe metabolism of Methylphenidate can be decreased when combined with Ketoconazole.Approved, Investigational
MethylphenobarbitalThe metabolism of Methylphenobarbital can be decreased when combined with Ketoconazole.Approved
MethylprednisoloneThe serum concentration of Methylprednisolone can be increased when it is combined with Ketoconazole.Approved, Vet Approved
MethyltestosteroneThe metabolism of Methyltestosterone can be decreased when combined with Ketoconazole.Approved
MethyprylonThe metabolism of Methyprylon can be decreased when combined with Ketoconazole.Approved, Illicit, Withdrawn
MethysergideThe risk or severity of adverse effects can be increased when Methysergide is combined with Ketoconazole.Approved
MetiamideThe serum concentration of Ketoconazole can be decreased when it is combined with Metiamide.Experimental
MetoclopramideThe metabolism of Metoclopramide can be decreased when combined with Ketoconazole.Approved, Investigational
MetoprololThe serum concentration of Metoprolol can be increased when it is combined with Ketoconazole.Approved, Investigational
MetronidazoleThe metabolism of Metronidazole can be decreased when combined with Ketoconazole.Approved
MevastatinThe serum concentration of Mevastatin can be increased when it is combined with Ketoconazole.Experimental
MexiletineThe metabolism of Mexiletine can be decreased when combined with Ketoconazole.Approved
MianserinThe metabolism of Mianserin can be decreased when combined with Ketoconazole.Approved, Investigational
MibefradilThe metabolism of Mibefradil can be decreased when combined with Ketoconazole.Investigational, Withdrawn
MiconazoleThe metabolism of Miconazole can be decreased when combined with Ketoconazole.Approved, Investigational, Vet Approved
MidazolamThe serum concentration of Midazolam can be increased when it is combined with Ketoconazole.Approved, Illicit
MidostaurinThe metabolism of Midostaurin can be decreased when combined with Ketoconazole.Approved
MifepristoneMifepristone may increase the QTc-prolonging activities of Ketoconazole.Approved, Investigational
MinaprineThe metabolism of Minaprine can be decreased when combined with Ketoconazole.Approved
MirabegronThe serum concentration of Mirabegron can be increased when it is combined with Ketoconazole.Approved
MirtazapineThe metabolism of Mirtazapine can be decreased when combined with Ketoconazole.Approved
MitotaneThe serum concentration of Ketoconazole can be decreased when it is combined with Mitotane.Approved
MoclobemideThe metabolism of Moclobemide can be decreased when combined with Ketoconazole.Approved
ModafinilThe metabolism of Modafinil can be decreased when combined with Ketoconazole.Approved, Investigational
MometasoneThe serum concentration of Mometasone can be increased when it is combined with Ketoconazole.Approved, Vet Approved
MontelukastThe metabolism of Montelukast can be decreased when combined with Ketoconazole.Approved
MorphineThe metabolism of Morphine can be decreased when combined with Ketoconazole.Approved, Investigational
MoxifloxacinKetoconazole may increase the QTc-prolonging activities of Moxifloxacin.Approved, Investigational
Mycophenolate mofetilThe metabolism of Mycophenolate mofetil can be decreased when combined with Ketoconazole.Approved, Investigational
NaftopidilThe risk or severity of adverse effects can be increased when Ketoconazole is combined with Naftopidil.Investigational
NaloxegolThe serum concentration of Naloxegol can be increased when it is combined with Ketoconazole.Approved
NaloxoneThe metabolism of Naloxone can be decreased when combined with Ketoconazole.Approved, Vet Approved
NaproxenThe metabolism of Naproxen can be decreased when combined with Ketoconazole.Approved, Vet Approved
NateglinideThe metabolism of Nateglinide can be decreased when combined with Ketoconazole.Approved, Investigational
NCX 1022The serum concentration of NCX 1022 can be increased when it is combined with Ketoconazole.Investigational
NebivololThe serum concentration of Nebivolol can be increased when it is combined with Ketoconazole.Approved, Investigational
NefazodoneThe metabolism of Nefazodone can be decreased when combined with Ketoconazole.Approved, Withdrawn
NelfinavirThe metabolism of Ketoconazole can be decreased when combined with Nelfinavir.Approved
NeratinibThe metabolism of Neratinib can be decreased when combined with Ketoconazole.Approved, Investigational
NetupitantThe serum concentration of Ketoconazole can be increased when it is combined with Netupitant.Approved
NevirapineThe serum concentration of Ketoconazole can be decreased when it is combined with Nevirapine.Approved
NicardipineThe metabolism of Nicardipine can be decreased when combined with Ketoconazole.Approved
NicergolineThe metabolism of Nicergoline can be decreased when combined with Ketoconazole.Approved, Investigational
NiclosamideThe metabolism of Niclosamide can be decreased when combined with Ketoconazole.Approved, Investigational, Vet Approved
NicotineThe metabolism of Nicotine can be decreased when combined with Ketoconazole.Approved
NifedipineThe metabolism of Nifedipine can be decreased when combined with Ketoconazole.Approved
NiguldipineThe risk or severity of adverse effects can be increased when Ketoconazole is combined with Niguldipine.Experimental
NilotinibThe serum concentration of Nilotinib can be increased when it is combined with Ketoconazole.Approved, Investigational
NiludipineThe risk or severity of adverse effects can be increased when Ketoconazole is combined with Niludipine.Experimental
NilutamideThe metabolism of Nilutamide can be decreased when combined with Ketoconazole.Approved
NilvadipineThe metabolism of Nilvadipine can be decreased when combined with Ketoconazole.Approved, Investigational
NimesulideThe risk or severity of adverse effects can be increased when Ketoconazole is combined with Nimesulide.Approved, Investigational, Withdrawn
NimodipineThe serum concentration of Nimodipine can be increased when it is combined with Ketoconazole.Approved
NintedanibThe serum concentration of Nintedanib can be increased when it is combined with Ketoconazole.Approved
NisoldipineThe serum concentration of Nisoldipine can be increased when it is combined with Ketoconazole.Approved
NitrazepamThe metabolism of Nitrazepam can be decreased when combined with Ketoconazole.Approved
NitrendipineThe metabolism of Nitrendipine can be decreased when combined with Ketoconazole.Approved, Investigational
NitrofuralThe metabolism of Nitrofural can be decreased when combined with Ketoconazole.Approved, Investigational, Vet Approved
NizatidineThe serum concentration of Ketoconazole can be decreased when it is combined with Nizatidine.Approved
NorethisteroneThe metabolism of Norethisterone can be decreased when combined with Ketoconazole.Approved
NorgestrelThe metabolism of Norgestrel can be decreased when combined with Ketoconazole.Approved
NortriptylineThe metabolism of Nortriptyline can be decreased when combined with Ketoconazole.Approved
OdanacatibThe metabolism of Odanacatib can be decreased when combined with Ketoconazole.Investigational
OfloxacinKetoconazole may increase the QTc-prolonging activities of Ofloxacin.Approved
OlanzapineThe serum concentration of Ketoconazole can be decreased when it is combined with Olanzapine.Approved, Investigational
OlaparibThe serum concentration of Olaparib can be increased when it is combined with Ketoconazole.Approved
Oleoyl-estroneThe serum concentration of Oleoyl-estrone can be increased when it is combined with Ketoconazole.Investigational
OlodaterolThe metabolism of Olodaterol can be decreased when combined with Ketoconazole.Approved
OlopatadineThe metabolism of Olopatadine can be decreased when combined with Ketoconazole.Approved
OmeprazoleThe serum concentration of Ketoconazole can be decreased when it is combined with Omeprazole.Approved, Investigational, Vet Approved
OndansetronThe metabolism of Ondansetron can be decreased when combined with Ketoconazole.Approved
OrphenadrineThe metabolism of Orphenadrine can be decreased when combined with Ketoconazole.Approved
OsimertinibThe serum concentration of Ketoconazole can be increased when it is combined with Osimertinib.Approved
OspemifeneThe serum concentration of Ospemifene can be increased when it is combined with Ketoconazole.Approved
OtiloniumThe risk or severity of adverse effects can be increased when Ketoconazole is combined with Otilonium.Experimental, Investigational
OxaprozinThe metabolism of Oxaprozin can be decreased when combined with Ketoconazole.Approved
OxazepamThe metabolism of Oxazepam can be decreased when combined with Ketoconazole.Approved
OxiconazoleThe metabolism of Oxiconazole can be decreased when combined with Ketoconazole.Approved
OxybutyninThe serum concentration of Oxybutynin can be increased when it is combined with Ketoconazole.Approved, Investigational
OxycodoneThe risk or severity of adverse effects can be increased when Ketoconazole is combined with Oxycodone.Approved, Illicit, Investigational
OxymorphoneThe metabolism of Oxymorphone can be decreased when combined with Ketoconazole.Approved, Investigational, Vet Approved
PaclitaxelThe metabolism of Paclitaxel can be decreased when combined with Ketoconazole.Approved, Vet Approved
PalbociclibThe serum concentration of Ketoconazole can be increased when it is combined with Palbociclib.Approved
PaliperidoneKetoconazole may increase the QTc-prolonging activities of Paliperidone.Approved
PalonosetronThe metabolism of Palonosetron can be decreased when combined with Ketoconazole.Approved, Investigational
PanobinostatThe serum concentration of Panobinostat can be increased when it is combined with Ketoconazole.Approved, Investigational
PantoprazoleThe serum concentration of Ketoconazole can be decreased when it is combined with Pantoprazole.Approved
ParamethadioneThe metabolism of Paramethadione can be decreased when combined with Ketoconazole.Approved
ParamethasoneThe metabolism of Paramethasone can be decreased when combined with Ketoconazole.Approved
ParecoxibThe serum concentration of Parecoxib can be increased when it is combined with Ketoconazole.Approved
ParicalcitolThe serum concentration of Paricalcitol can be increased when it is combined with Ketoconazole.Approved, Investigational
ParitaprevirThe metabolism of Paritaprevir can be decreased when combined with Ketoconazole.Approved
ParoxetineThe metabolism of Paroxetine can be decreased when combined with Ketoconazole.Approved, Investigational
PazopanibThe serum concentration of Pazopanib can be increased when it is combined with Ketoconazole.Approved
PentamidineThe metabolism of Pentamidine can be decreased when combined with Ketoconazole.Approved
PentobarbitalThe metabolism of Ketoconazole can be increased when combined with Pentobarbital.Approved, Vet Approved
PerampanelThe metabolism of Perampanel can be decreased when combined with Ketoconazole.Approved
PerflutrenKetoconazole may increase the QTc-prolonging activities of Perflutren.Approved
PergolideThe metabolism of Pergolide can be decreased when combined with Ketoconazole.Approved, Investigational, Vet Approved, Withdrawn
PerhexilineThe metabolism of Perhexiline can be decreased when combined with Ketoconazole.Approved, Investigational
PermethrinThe metabolism of Permethrin can be decreased when combined with Ketoconazole.Approved, Investigational
PerospironeThe metabolism of Perospirone can be decreased when combined with Ketoconazole.Approved
PerphenazineThe metabolism of Perphenazine can be decreased when combined with Ketoconazole.Approved
PethidineThe metabolism of Pethidine can be decreased when combined with Ketoconazole.Approved
PhenacetinThe metabolism of Phenacetin can be decreased when combined with Ketoconazole.Withdrawn
PhenforminThe metabolism of Phenformin can be decreased when combined with Ketoconazole.Approved, Investigational, Withdrawn
PhenindioneThe serum concentration of Phenindione can be increased when it is combined with Ketoconazole.Approved, Investigational
PhenobarbitalThe metabolism of Ketoconazole can be increased when combined with Phenobarbital.Approved
PhenoxybenzamineThe metabolism of Phenoxybenzamine can be decreased when combined with Ketoconazole.Approved
PhenprocoumonThe serum concentration of Phenprocoumon can be increased when it is combined with Ketoconazole.Approved, Investigational
PhenylbutazoneThe metabolism of Phenylbutazone can be decreased when combined with Ketoconazole.Approved, Vet Approved
PhenytoinThe serum concentration of Phenytoin can be increased when it is combined with Ketoconazole.Approved, Vet Approved
PilocarpineThe metabolism of Pilocarpine can be decreased when combined with Ketoconazole.Approved
PimecrolimusThe metabolism of Pimecrolimus can be decreased when combined with Ketoconazole.Approved, Investigational
PimozideKetoconazole may increase the arrhythmogenic activities of Pimozide.Approved
PinacidilThe metabolism of Pinacidil can be decreased when combined with Ketoconazole.Withdrawn
PinaveriumThe risk or severity of adverse effects can be increased when Ketoconazole is combined with Pinaverium.Approved
PindololThe metabolism of Pindolol can be decreased when combined with Ketoconazole.Approved
PioglitazoneThe metabolism of Pioglitazone can be decreased when combined with Ketoconazole.Approved, Investigational
PiperazineThe metabolism of Piperazine can be decreased when combined with Ketoconazole.Approved, Vet Approved
PipotiazineThe metabolism of Pipotiazine can be decreased when combined with Ketoconazole.Approved, Investigational
PiroxicamThe metabolism of Piroxicam can be decreased when combined with Ketoconazole.Approved, Investigational
PitavastatinThe metabolism of Pitavastatin can be decreased when combined with Ketoconazole.Approved
PodofiloxThe metabolism of Podofilox can be decreased when combined with Ketoconazole.Approved
PomalidomideThe metabolism of Pomalidomide can be decreased when combined with Ketoconazole.Approved
PonatinibThe serum concentration of Ponatinib can be increased when it is combined with Ketoconazole.Approved
PosaconazoleThe metabolism of Posaconazole can be decreased when combined with Ketoconazole.Approved, Investigational, Vet Approved
PranlukastThe serum concentration of Pranlukast can be increased when it is combined with Ketoconazole.Approved, Investigational
PrasteroneThe metabolism of Prasterone can be decreased when combined with Ketoconazole.Approved, Nutraceutical
Prasterone sulfateThe serum concentration of Prasterone sulfate can be increased when it is combined with Ketoconazole.Investigational
PrasugrelThe serum concentration of the active metabolites of Prasugrel can be reduced when Prasugrel is used in combination with Ketoconazole resulting in a loss in efficacy.Approved
PravastatinThe metabolism of Pravastatin can be decreased when combined with Ketoconazole.Approved
PrazepamThe metabolism of Prazepam can be decreased when combined with Ketoconazole.Approved, Illicit
PraziquantelThe serum concentration of Praziquantel can be increased when it is combined with Ketoconazole.Approved, Vet Approved
PrednicarbateThe serum concentration of Prednicarbate can be increased when it is combined with Ketoconazole.Approved
PrednisoloneThe serum concentration of Prednisolone can be increased when it is combined with Ketoconazole.Approved, Vet Approved
PrednisoneThe serum concentration of Prednisone can be increased when it is combined with Ketoconazole.Approved, Vet Approved
PregabalinThe risk or severity of adverse effects can be increased when Ketoconazole is combined with Pregabalin.Approved, Illicit, Investigational
PregnenoloneThe serum concentration of Pregnenolone can be increased when it is combined with Ketoconazole.Experimental, Investigational
PrenylamineThe risk or severity of adverse effects can be increased when Ketoconazole is combined with Prenylamine.Withdrawn
PrimaquineThe metabolism of Primaquine can be decreased when combined with Ketoconazole.Approved
PrimidoneThe metabolism of Ketoconazole can be increased when combined with Primidone.Approved, Vet Approved
ProcainamideKetoconazole may increase the QTc-prolonging activities of Procainamide.Approved
ProchlorperazineThe metabolism of Prochlorperazine can be decreased when combined with Ketoconazole.Approved, Vet Approved
ProgesteroneThe therapeutic efficacy of Progesterone can be decreased when used in combination with Ketoconazole.Approved, Vet Approved
ProguanilThe metabolism of Proguanil can be decreased when combined with Ketoconazole.Approved
PromazineThe metabolism of Promazine can be decreased when combined with Ketoconazole.Approved, Vet Approved
PromethazineThe serum concentration of Ketoconazole can be decreased when it is combined with Promethazine.Approved
PropafenoneThe serum concentration of Ketoconazole can be increased when it is combined with Propafenone.Approved
PropofolThe metabolism of Propofol can be decreased when combined with Ketoconazole.Approved, Investigational, Vet Approved
Propoxyphene napsylateThe metabolism of Propoxyphene napsylate can be decreased when combined with Ketoconazole.Approved
PropranololThe metabolism of Propranolol can be decreased when combined with Ketoconazole.Approved, Investigational
ProtriptylineThe metabolism of Protriptyline can be decreased when combined with Ketoconazole.Approved
PrucaloprideThe serum concentration of Prucalopride can be increased when it is combined with Ketoconazole.Approved
PseudoephedrineThe metabolism of Pseudoephedrine can be decreased when combined with Ketoconazole.Approved
PyrazinamideThe metabolism of Pyrazinamide can be decreased when combined with Ketoconazole.Approved
QuazepamThe metabolism of Quazepam can be decreased when combined with Ketoconazole.Approved, Illicit
QuetiapineThe serum concentration of Quetiapine can be increased when it is combined with Ketoconazole.Approved
QuinacrineThe metabolism of Quinacrine can be decreased when combined with Ketoconazole.Approved, Investigational
QuinidineThe metabolism of Quinidine can be decreased when combined with Ketoconazole.Approved
QuinineThe metabolism of Quinine can be decreased when combined with Ketoconazole.Approved
RabeprazoleThe serum concentration of Ketoconazole can be decreased when it is combined with Rabeprazole.Approved, Investigational
RaloxifeneThe metabolism of Raloxifene can be decreased when combined with Ketoconazole.Approved, Investigational
RamelteonThe serum concentration of Ramelteon can be increased when it is combined with Ketoconazole.Approved, Investigational
RanitidineThe serum concentration of Ketoconazole can be decreased when it is combined with Ranitidine.Approved
RanolazineThe serum concentration of Ranolazine can be increased when it is combined with Ketoconazole.Approved, Investigational
ReboxetineThe metabolism of Reboxetine can be decreased when combined with Ketoconazole.Approved, Investigational
RegorafenibThe serum concentration of Regorafenib can be increased when it is combined with Ketoconazole.Approved
RemoxiprideThe metabolism of Remoxipride can be decreased when combined with Ketoconazole.Approved, Withdrawn
RepaglinideThe serum concentration of Repaglinide can be increased when it is combined with Ketoconazole.Approved, Investigational
repinotanThe metabolism of repinotan can be decreased when combined with Ketoconazole.Investigational
RetapamulinThe serum concentration of Retapamulin can be increased when it is combined with Ketoconazole.Approved
RibociclibThe serum concentration of Ribociclib can be increased when it is combined with Ketoconazole.Approved
RifabutinThe metabolism of Ketoconazole can be increased when combined with Rifabutin.Approved
RifampicinThe metabolism of Ketoconazole can be increased when combined with Rifampicin.Approved
RifapentineThe metabolism of Ketoconazole can be increased when combined with Rifapentine.Approved
RifaximinThe serum concentration of Rifaximin can be increased when it is combined with Ketoconazole.Approved, Investigational
RilpivirineThe serum concentration of Rilpivirine can be increased when it is combined with Ketoconazole.Approved
RimexoloneThe serum concentration of Rimexolone can be increased when it is combined with Ketoconazole.Approved
RimonabantThe metabolism of Rimonabant can be decreased when combined with Ketoconazole.Approved, Investigational
RiociguatThe serum concentration of Riociguat can be increased when it is combined with Ketoconazole.Approved
RisedronateThe risk or severity of adverse effects can be increased when Ketoconazole is combined with Risedronate.Approved, Investigational
RisperidoneThe metabolism of Risperidone can be decreased when combined with Ketoconazole.Approved, Investigational
RitonavirThe serum concentration of Ketoconazole can be increased when it is combined with Ritonavir.Approved, Investigational
RivaroxabanThe metabolism of Rivaroxaban can be decreased when combined with Ketoconazole.Approved
RofecoxibThe metabolism of Rofecoxib can be decreased when combined with Ketoconazole.Investigational, Withdrawn
RolapitantThe metabolism of Rolapitant can be decreased when combined with Ketoconazole.Approved
RomidepsinThe serum concentration of Romidepsin can be increased when it is combined with Ketoconazole.Approved, Investigational
RopiniroleThe metabolism of Ropinirole can be decreased when combined with Ketoconazole.Approved, Investigational
RopivacaineThe metabolism of Ropivacaine can be decreased when combined with Ketoconazole.Approved
RosiglitazoneThe metabolism of Rosiglitazone can be decreased when combined with Ketoconazole.Approved, Investigational
RosuvastatinThe metabolism of Rosuvastatin can be decreased when combined with Ketoconazole.Approved
RotigotineThe metabolism of Rotigotine can be decreased when combined with Ketoconazole.Approved
Roxatidine acetateThe serum concentration of Ketoconazole can be decreased when it is combined with Roxatidine acetate.Approved, Investigational
RoxithromycinThe metabolism of Roxithromycin can be decreased when combined with Ketoconazole.Approved, Investigational, Withdrawn
RucaparibThe metabolism of Rucaparib can be decreased when combined with Ketoconazole.Approved, Investigational
RupatadineThe metabolism of Rupatadine can be decreased when combined with Ketoconazole.Approved
RuxolitinibThe serum concentration of Ruxolitinib can be increased when it is combined with Ketoconazole.Approved
SafinamideThe metabolism of Safinamide can be decreased when combined with Ketoconazole.Approved
Salicylic acidThe metabolism of Salicylic acid can be decreased when combined with Ketoconazole.Approved, Vet Approved
SalmeterolThe serum concentration of Salmeterol can be increased when it is combined with Ketoconazole.Approved
SaquinavirThe serum concentration of Ketoconazole can be increased when it is combined with Saquinavir.Approved, Investigational
SaxagliptinThe serum concentration of Saxagliptin can be increased when it is combined with Ketoconazole.Approved
SelegilineThe metabolism of Selegiline can be decreased when combined with Ketoconazole.Approved, Investigational, Vet Approved
SelexipagThe metabolism of Selexipag can be decreased when combined with Ketoconazole.Approved
SeratrodastThe metabolism of Seratrodast can be decreased when combined with Ketoconazole.Approved
SertindoleThe metabolism of Sertindole can be decreased when combined with Ketoconazole.Approved, Investigational, Withdrawn
SertralineThe metabolism of Sertraline can be decreased when combined with Ketoconazole.Approved
SevofluraneThe metabolism of Sevoflurane can be decreased when combined with Ketoconazole.Approved, Vet Approved
SibutramineThe metabolism of Sibutramine can be decreased when combined with Ketoconazole.Approved, Illicit, Investigational, Withdrawn
SildenafilThe serum concentration of Sildenafil can be increased when it is combined with Ketoconazole.Approved, Investigational
SilodosinThe serum concentration of Silodosin can be increased when it is combined with Ketoconazole.Approved
SiltuximabThe serum concentration of Ketoconazole can be decreased when it is combined with Siltuximab.Approved
SimeprevirThe serum concentration of Ketoconazole can be increased when it is combined with Simeprevir.Approved
SimvastatinThe serum concentration of Simvastatin can be increased when it is combined with Ketoconazole.Approved
SirolimusThe serum concentration of Sirolimus can be increased when it is combined with Ketoconazole.Approved, Investigational
SitagliptinThe metabolism of Sitagliptin can be decreased when combined with Ketoconazole.Approved, Investigational
SitaxentanThe metabolism of Sitaxentan can be decreased when combined with Ketoconazole.Approved, Investigational, Withdrawn
Sodium bicarbonateThe serum concentration of Ketoconazole can be decreased when it is combined with Sodium bicarbonate.Approved
SolifenacinThe metabolism of Solifenacin can be decreased when combined with Ketoconazole.Approved
SonidegibThe serum concentration of Sonidegib can be increased when it is combined with Ketoconazole.Approved, Investigational
SorafenibThe serum concentration of Sorafenib can be increased when it is combined with Ketoconazole.Approved, Investigational
SotalolKetoconazole may increase the QTc-prolonging activities of Sotalol.Approved
SparteineThe metabolism of Sparteine can be decreased when combined with Ketoconazole.Experimental
SpiramycinThe metabolism of Spiramycin can be decreased when combined with Ketoconazole.Approved
St. John's WortThe serum concentration of Ketoconazole can be decreased when it is combined with St. John's Wort.Investigational, Nutraceutical
StiripentolThe serum concentration of Ketoconazole can be increased when it is combined with Stiripentol.Approved
SucralfateSucralfate can cause a decrease in the absorption of Ketoconazole resulting in a reduced serum concentration and potentially a decrease in efficacy.Approved
SufentanilThe metabolism of Sufentanil can be decreased when combined with Ketoconazole.Approved, Investigational
SulfadiazineThe metabolism of Sulfadiazine can be decreased when combined with Ketoconazole.Approved, Vet Approved
SulfamethoxazoleThe metabolism of Sulfamethoxazole can be decreased when combined with Ketoconazole.Approved
SulfamoxoleThe metabolism of Sulfamoxole can be decreased when combined with Ketoconazole.Approved
SulfinpyrazoneThe metabolism of Sulfinpyrazone can be decreased when combined with Ketoconazole.Approved
SulfisoxazoleKetoconazole may increase the QTc-prolonging activities of Sulfisoxazole.Approved, Vet Approved
SunitinibThe metabolism of Sunitinib can be decreased when combined with Ketoconazole.Approved, Investigational
SuprofenThe metabolism of Suprofen can be decreased when combined with Ketoconazole.Approved, Withdrawn
SuvorexantThe serum concentration of Suvorexant can be increased when it is combined with Ketoconazole.Approved
Synthetic Conjugated Estrogens, AThe metabolism of Synthetic Conjugated Estrogens, A can be decreased when combined with Ketoconazole.Approved
Synthetic Conjugated Estrogens, BThe metabolism of Synthetic Conjugated Estrogens, B can be decreased when combined with Ketoconazole.Approved
TacrolimusThe serum concentration of Tacrolimus can be increased when it is combined with Ketoconazole.Approved, Investigational
TadalafilThe serum concentration of Tadalafil can be increased when it is combined with Ketoconazole.Approved, Investigational
TamoxifenThe serum concentration of the active metabolites of Tamoxifen can be reduced when Tamoxifen is used in combination with Ketoconazole resulting in a loss in efficacy.Approved
TamsulosinThe serum concentration of Tamsulosin can be increased when it is combined with Ketoconazole.Approved, Investigational
TapentadolThe metabolism of Tapentadol can be decreased when combined with Ketoconazole.Approved
TasimelteonThe serum concentration of Tasimelteon can be increased when it is combined with Ketoconazole.Approved
TasosartanThe metabolism of Tasosartan can be decreased when combined with Ketoconazole.Approved
Taurochenodeoxycholic acidThe metabolism of Taurochenodeoxycholic acid can be decreased when combined with Ketoconazole.Experimental
TegaserodThe metabolism of Tegaserod can be decreased when combined with Ketoconazole.Investigational, Withdrawn
TelaprevirThe serum concentration of Telaprevir can be increased when it is combined with Ketoconazole.Approved, Withdrawn
TelavancinKetoconazole may increase the QTc-prolonging activities of Telavancin.Approved
TelithromycinThe serum concentration of Telithromycin can be increased when it is combined with Ketoconazole.Approved
TemazepamThe metabolism of Temazepam can be decreased when combined with Ketoconazole.Approved
TemsirolimusThe serum concentration of the active metabolites of Temsirolimus can be increased when Temsirolimus is used in combination with Ketoconazole.Approved
TeniposideThe metabolism of Teniposide can be decreased when combined with Ketoconazole.Approved
TenoxicamThe metabolism of Tenoxicam can be decreased when combined with Ketoconazole.Approved
TerbinafineThe metabolism of Terbinafine can be decreased when combined with Ketoconazole.Approved, Investigational, Vet Approved
TerfenadineKetoconazole may increase the QTc-prolonging activities of Terfenadine.Withdrawn
TergurideThe risk or severity of adverse effects can be increased when Terguride is combined with Ketoconazole.Experimental
TerodilineThe risk or severity of adverse effects can be increased when Ketoconazole is combined with Terodiline.Experimental
TesmilifeneThe metabolism of Tesmilifene can be decreased when combined with Ketoconazole.Investigational
TestosteroneThe metabolism of Testosterone can be decreased when combined with Ketoconazole.Approved, Investigational
TetrabenazineKetoconazole may increase the QTc-prolonging activities of Tetrabenazine.Approved
TetracyclineThe metabolism of Tetracycline can be decreased when combined with Ketoconazole.Approved, Vet Approved
TetrahydropalmatineThe risk or severity of adverse effects can be increased when Ketoconazole is combined with Tetrahydropalmatine.Investigational
ThalidomideThe metabolism of Thalidomide can be decreased when combined with Ketoconazole.Approved, Investigational, Withdrawn
TheophyllineThe metabolism of Theophylline can be decreased when combined with Ketoconazole.Approved
ThiamylalThe metabolism of Thiamylal can be decreased when combined with Ketoconazole.Approved, Vet Approved
ThioridazineThe serum concentration of Thioridazine can be increased when it is combined with Ketoconazole.Approved, Withdrawn
ThiotepaThe metabolism of Thiotepa can be decreased when combined with Ketoconazole.Approved
TiagabineThe metabolism of Tiagabine can be decreased when combined with Ketoconazole.Approved
TicagrelorThe serum concentration of the active metabolites of Ticagrelor can be reduced when Ticagrelor is used in combination with Ketoconazole resulting in a loss in efficacy.Approved
TiclopidineThe metabolism of Ticlopidine can be decreased when combined with Ketoconazole.Approved
TimololThe metabolism of Timolol can be decreased when combined with Ketoconazole.Approved
TinidazoleThe metabolism of Tinidazole can be decreased when combined with Ketoconazole.Approved, Investigational
TioclomarolThe serum concentration of Tioclomarol can be increased when it is combined with Ketoconazole.Experimental
TiotropiumThe metabolism of Tiotropium can be decreased when combined with Ketoconazole.Approved
TipranavirThe serum concentration of Ketoconazole can be increased when it is combined with Tipranavir.Approved, Investigational
TixocortolThe serum concentration of Tixocortol can be increased when it is combined with Ketoconazole.Approved
TizanidineThe serum concentration of Tizanidine can be increased when it is combined with Ketoconazole.Approved
TocilizumabThe serum concentration of Ketoconazole can be decreased when it is combined with Tocilizumab.Approved
TofacitinibThe serum concentration of Tofacitinib can be increased when it is combined with Ketoconazole.Approved, Investigational
TolbutamideThe metabolism of Tolbutamide can be decreased when combined with Ketoconazole.Approved
Tolfenamic AcidThe risk or severity of adverse effects can be increased when Ketoconazole is combined with Tolfenamic Acid.Approved
TolterodineThe serum concentration of Tolterodine can be increased when it is combined with Ketoconazole.Approved, Investigational
TolvaptanThe serum concentration of Tolvaptan can be increased when it is combined with Ketoconazole.Approved
TopotecanThe serum concentration of Topotecan can be increased when it is combined with Ketoconazole.Approved, Investigational
TorasemideThe metabolism of Torasemide can be decreased when combined with Ketoconazole.Approved
ToremifeneThe risk or severity of adverse effects can be increased when Ketoconazole is combined with Toremifene.Approved, Investigational
TrabectedinThe serum concentration of Trabectedin can be increased when it is combined with Ketoconazole.Approved, Investigational
TramadolThe therapeutic efficacy of Tramadol can be decreased when used in combination with Ketoconazole.Approved, Investigational
TranilastThe risk or severity of adverse effects can be increased when Ketoconazole is combined with Tranilast.Approved, Investigational
Trastuzumab emtansineThe serum concentration of the active metabolites of Trastuzumab emtansine can be increased when Trastuzumab emtansine is used in combination with Ketoconazole.Approved
TrazodoneThe metabolism of Trazodone can be decreased when combined with Ketoconazole.Approved, Investigational
TreprostinilThe metabolism of Treprostinil can be decreased when combined with Ketoconazole.Approved, Investigational
TretinoinThe metabolism of Tretinoin can be decreased when combined with Ketoconazole.Approved, Investigational, Nutraceutical
TriamcinoloneThe metabolism of Triamcinolone can be decreased when combined with Ketoconazole.Approved, Vet Approved
TriazolamThe serum concentration of Triazolam can be increased when it is combined with Ketoconazole.Approved
TrimethadioneThe metabolism of Trimethadione can be decreased when combined with Ketoconazole.Approved
TrimethoprimThe metabolism of Trimethoprim can be decreased when combined with Ketoconazole.Approved, Vet Approved
TrimipramineThe metabolism of Trimipramine can be decreased when combined with Ketoconazole.Approved
TroglitazoneThe metabolism of Troglitazone can be decreased when combined with Ketoconazole.Investigational, Withdrawn
TroleandomycinThe metabolism of Troleandomycin can be decreased when combined with Ketoconazole.Approved
TromethamineThe serum concentration of Ketoconazole can be decreased when it is combined with Tromethamine.Approved
UbidecarenoneThe serum concentration of Ubidecarenone can be increased when it is combined with Ketoconazole.Approved, Experimental
UdenafilThe metabolism of Udenafil can be decreased when combined with Ketoconazole.Approved, Investigational
UlipristalThe serum concentration of Ulipristal can be increased when it is combined with Ketoconazole.Approved
UlobetasolThe serum concentration of Ulobetasol can be increased when it is combined with Ketoconazole.Approved
UmeclidiniumThe metabolism of Umeclidinium can be decreased when combined with Ketoconazole.Approved
ValbenazineThe metabolism of Valbenazine can be decreased when combined with Ketoconazole.Approved, Investigational
ValdecoxibThe metabolism of Valdecoxib can be decreased when combined with Ketoconazole.Investigational, Withdrawn
Valproic AcidThe metabolism of Valproic Acid can be decreased when combined with Ketoconazole.Approved, Investigational
ValsartanThe metabolism of Valsartan can be decreased when combined with Ketoconazole.Approved, Investigational
VandetanibThe metabolism of Vandetanib can be decreased when combined with Ketoconazole.Approved
VanoxerineThe metabolism of Vanoxerine can be decreased when combined with Ketoconazole.Investigational
VardenafilThe serum concentration of Vardenafil can be increased when it is combined with Ketoconazole.Approved
VelpatasvirThe metabolism of Velpatasvir can be decreased when combined with Ketoconazole.Approved
VenetoclaxThe metabolism of Venetoclax can be decreased when combined with Ketoconazole.Approved
VenlafaxineThe metabolism of Venlafaxine can be decreased when combined with Ketoconazole.Approved
VerapamilThe metabolism of Verapamil can be decreased when combined with Ketoconazole.Approved
VernakalantThe metabolism of Vernakalant can be decreased when combined with Ketoconazole.Approved, Investigational
VicrivirocThe metabolism of Vicriviroc can be decreased when combined with Ketoconazole.Investigational
VilanterolThe metabolism of Vilanterol can be decreased when combined with Ketoconazole.Approved
VilazodoneThe serum concentration of Vilazodone can be increased when it is combined with Ketoconazole.Approved
VinblastineThe metabolism of Vinblastine can be decreased when combined with Ketoconazole.Approved
VincristineThe serum concentration of Vincristine can be increased when it is combined with Ketoconazole.Approved, Investigational
VincristineThe metabolism of Vincristine can be decreased when combined with Ketoconazole.Approved, Investigational
VindesineThe serum concentration of Vindesine can be increased when it is combined with Ketoconazole.Approved, Investigational
VinorelbineThe metabolism of Vinorelbine can be decreased when combined with Ketoconazole.Approved, Investigational
VinpocetineThe risk or severity of adverse effects can be increased when Ketoconazole is combined with Vinpocetine.Investigational
VismodegibThe metabolism of Vismodegib can be decreased when combined with Ketoconazole.Approved
VorapaxarThe serum concentration of Vorapaxar can be increased when it is combined with Ketoconazole.Approved
VoriconazoleThe metabolism of Ketoconazole can be decreased when combined with Voriconazole.Approved, Investigational
VortioxetineThe metabolism of Vortioxetine can be decreased when combined with Ketoconazole.Approved
VoxilaprevirThe metabolism of Voxilaprevir can be decreased when combined with Ketoconazole.Approved
WarfarinThe serum concentration of Warfarin can be increased when it is combined with Ketoconazole.Approved
XimelagatranThe metabolism of Ximelagatran can be decreased when combined with Ketoconazole.Approved, Investigational, Withdrawn
XylometazolineThe risk or severity of adverse effects can be increased when Ketoconazole is combined with Xylometazoline.Approved
YohimbineThe metabolism of Yohimbine can be decreased when combined with Ketoconazole.Approved, Vet Approved
ZafirlukastThe metabolism of Zafirlukast can be decreased when combined with Ketoconazole.Approved, Investigational
ZalcitabineThe metabolism of Zalcitabine can be decreased when combined with Ketoconazole.Approved, Investigational
ZaleplonThe metabolism of Zaleplon can be decreased when combined with Ketoconazole.Approved, Illicit, Investigational
ZaltoprofenThe metabolism of Zaltoprofen can be decreased when combined with Ketoconazole.Approved, Investigational
ZiconotideThe risk or severity of adverse effects can be increased when Ketoconazole is combined with Ziconotide.Approved
ZidovudineThe metabolism of Zidovudine can be decreased when combined with Ketoconazole.Approved
ZileutonThe metabolism of Zileuton can be decreased when combined with Ketoconazole.Approved, Investigational, Withdrawn
ZiprasidoneThe metabolism of Ziprasidone can be decreased when combined with Ketoconazole.Approved
ZolpidemThe serum concentration of Zolpidem can be increased when it is combined with Ketoconazole.Approved
ZomepiracThe metabolism of Zomepirac can be decreased when combined with Ketoconazole.Withdrawn
ZonisamideThe metabolism of Zonisamide can be decreased when combined with Ketoconazole.Approved, Investigational
ZopicloneThe serum concentration of Zopiclone can be increased when it is combined with Ketoconazole.Approved
ZuclopenthixolThe serum concentration of Zuclopenthixol can be increased when it is combined with Ketoconazole.Approved, Investigational
Food Interactions
  • Avoid alcohol.
  • Avoid milk, calcium containing dairy products, iron, antacids, or aluminum salts 2 hours before or 6 hours after using antacids while on this medication.
  • Take with food.

References

Synthesis Reference

U.S. Patent 4,144,346.

General References
  1. Goeders NE, Peltier RL, Guerin GF: Ketoconazole reduces low dose cocaine self-administration in rats. Drug Alcohol Depend. 1998 Dec 1;53(1):67-77. [PubMed:10933341]
  2. Berwaerts J, Verhelst J, Mahler C, Abs R: Cushing's syndrome in pregnancy treated by ketoconazole: case report and review of the literature. Gynecol Endocrinol. 1999 Jun;13(3):175-82. [PubMed:10451809]
  3. Kazy Z, Puho E, Czeizel AE: Population-based case-control study of oral ketoconazole treatment for birth outcomes. Congenit Anom (Kyoto). 2005 Mar;45(1):5-8. [PubMed:15737124]
  4. Pierard-Franchimont C, Goffin V, Decroix J, Pierard GE: A multicenter randomized trial of ketoconazole 2% and zinc pyrithione 1% shampoos in severe dandruff and seborrheic dermatitis. Skin Pharmacol Appl Skin Physiol. 2002 Nov-Dec;15(6):434-41. [PubMed:12476017]
External Links
KEGG Drug
D00351
PubChem Compound
3823
PubChem Substance
46506746
ChemSpider
3691
BindingDB
31768
ChEBI
48339
ChEMBL
CHEMBL157101
Therapeutic Targets Database
DAP000630
PharmGKB
PA450146
HET
KTN
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
PDRhealth
PDRhealth Drug Page
Wikipedia
Ketoconazole
ATC Codes
G01AF11 — KetoconazoleD01AC08 — KetoconazoleG01AF20 — Combinations of imidazole derivativesJ02AB02 — Ketoconazole
AHFS Codes
  • 84:04.08.08 — Azoles
  • 08:14.08 — Azoles
FDA label
Download (222 KB)
MSDS
Download (73.3 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
0Active Not RecruitingOtherInsulin Resistance1
1CompletedNot AvailableAlzheimer's Disease (AD) / Huntington's Disease (HD)1
1CompletedNot AvailableDrug Interactions1
1CompletedNot AvailableDrug Interactions / Healthy Volunteers / Pharmacokinetics1
1CompletedNot AvailableHCV Infections1
1CompletedNot AvailableHealthy Adult Volunteers / Pharmacokinetics of Isavuconazole / Pharmacokinetics of Ketoconazole1
1CompletedNot AvailableHealthy Volunteers5
1CompletedNot AvailableHealthy Volunteers / Pharmacokinetics of Darexaban and Metabolites1
1CompletedNot AvailableHealthy Volunteers / Pharmacokinetics of YM1781
1CompletedNot AvailableHealthy Volunteers / Pharmacology, Clinical1
1CompletedNot AvailableHypertension,Essential1
1CompletedNot AvailableMalignancies, Hematologic / Malignant Lymphomas1
1CompletedBasic ScienceAsthma Bronchial / AUC / Cmax / Ketoconazole / Metabolites / Pharmacokinetics / Tmax / Λz1
1CompletedBasic ScienceAlzheimer's Disease (AD)1
1CompletedBasic ScienceAutoimmune Diseases / Healthy Volunteers1
1CompletedBasic ScienceBioavailability / Drug- Drug Interactions / Healthy Volunteers1
1CompletedBasic ScienceDrug Interactions1
1CompletedBasic ScienceEffect of Ketoconazole on the PK of NBI-98854 in Healthy Subjects1
1CompletedBasic ScienceEvaluation of Pharmacokinetics of Sativex in the Absence and Presence of a CYP2C19 Inhibitor / Evaluation of Pharmacokinetics of Sativex in the Absence and Presence of a Known Inducer of CYP3A4 / Evaluation of Pharmacokinetics of Sativex in the Absence and Presence of a Potent Inhibitor of CYP3A41
1CompletedBasic ScienceHealthy Volunteers6
1CompletedBasic ScienceHuman Volunteers1
1CompletedBasic ScienceNon-Hodgkin's Lymphoma (NHL)1
1CompletedBasic ScienceObstetric Labour, Premature1
1CompletedBasic SciencePharmacokinetics1
1CompletedBasic ScienceTumors, Solid1
1CompletedDiagnosticHealthy Volunteers / Schizophrenic Disorders1
1CompletedOtherAsthma Bronchial1
1CompletedOtherDisseminated Sclerosis1
1CompletedTreatmentAdult Solid Neoplasm1
1CompletedTreatmentCancer, Advanced1
1CompletedTreatmentCancers2
1CompletedTreatmentCarcinoma NOS / Hodgkins Disease (HD) / Lymphoma, Large-Cell, Anaplastic / Neoplasms / Non-Hodgkin's Lymphoma (NHL)1
1CompletedTreatmentChronic Lymphocytic Leukaemia (CLL) / Malignant Lymphomas / Tumors, Solid1
1CompletedTreatmentErectile Dysfunction (ED)1
1CompletedTreatmentGastroparesis / Healthy Volunteers1
1CompletedTreatmentHealthy Male Volunteers1
1CompletedTreatmentHealthy Volunteers18
1CompletedTreatmentHealthy Volunteers / Pulmonary Disease, Chronic Obstructive2
1CompletedTreatmentHealthy Volunteers / Prophylaxis of acute chemotherapy induced nausea and vomiting2
1CompletedTreatmentMalignant Lymphomas / Nonhematologic Malignancies1
1CompletedTreatmentNeuroblastomas1
1CompletedTreatmentPharmacokinetics1
1CompletedTreatmentType 2 Diabetes Mellitus2
1CompletedTreatmentUnspecified Adult Solid Tumor, Protocol Specific2
1RecruitingTreatmentNeuroblastomas / Recurrent Neuroblastoma1
1TerminatedTreatmentHealthy Volunteers1
1TerminatedTreatmentTumors1
1WithdrawnTreatmentMalignant Melanoma, Neoplasms1
1, 2Active Not RecruitingTreatmentCancer of the Ovary / Cancer, Ovarian / Ovary Neoplasms / Primary Peritoneal Carcinoma1
1, 2CompletedTreatmentNeoplasm Metastases1
1, 2TerminatedTreatmentAdenocarcinoma, Prostate / Recurrent Prostate Carcinoma / Stage III Prostate Cancer / Stage IV Prostate Cancer1
1, 2TerminatedTreatmentProstate Cancer1
1, 2Unknown StatusTreatmentUnspecified Adult Solid Tumor, Protocol Specific1
2Active Not RecruitingTreatmentProstate Cancer2
2CompletedTreatmentCancers / Hormonal Cycling / Prostate1
2CompletedTreatmentChronic Central Serous Chorioretinopathy1
2CompletedTreatmentFemur Head Necrosis / Hip Fractures / Osteoarthritis (OA)1
2CompletedTreatmentMetastatic Breast Cancer (MBC)1
2CompletedTreatmentProstate Cancer4
2CompletedTreatmentProstate Cancer / Thromboembolism1
2CompletedTreatmentTinea Pedis1
2CompletedTreatmentTumors, Solid1
2Not Yet RecruitingTreatmentPituitary gonadotropin hypofunction1
2RecruitingTreatmentCastration-Resistant Prostate Cancer (CRPC)1
2RecruitingTreatmentProstate Cancer1
2TerminatedTreatmentAdenocarcinoma of the Prostate / Bone Metastases / Recurrent Prostate Cancer / Stage IV Prostate Cancer1
2TerminatedTreatmentGranulosa Cell Tumour of the Ovary1
2TerminatedTreatmentProstate Cancer2
2TerminatedTreatmentProstatic Neoplasms2
2Unknown StatusTreatmentCancers / Prostate Neoplasms1
2Unknown StatusTreatmentPsoriasis Vulgaris1
2, 3CompletedTreatmentMinor burns1
2, 3RecruitingTreatmentMinor burns1
3CompletedTreatmentChronic Lung Diseases / Respiratory Distress Syndrome, Adult1
3CompletedTreatmentProstate Cancer4
3Not Yet RecruitingTreatmentPost - Adolescence Acne1
3Not Yet RecruitingTreatmentTinea Pedis1
3TerminatedTreatmentProstate Cancer1
3TerminatedTreatmentTinea Pedis1
3Unknown StatusTreatmentBacterial Vaginosis (BV) / Candidiasis infection1
3WithdrawnTreatmentTinea Pedis1
4CompletedTreatmentChronic Obstructive Pulmonary Disease (COPD)1
4CompletedTreatmentSeborrheic Dermatitis1
4Unknown StatusBasic ScienceTransplantation, Kidney1
Not AvailableAvailableNot AvailableNeuroblastomas / Recurrent Neuroblastoma1
Not AvailableCompletedHealth Services ResearchGonadal Disorders / Hypogonadism / Olfacto genital dysplasia1
Not AvailableCompletedTreatmentEsophageal Candidiasis / Human Immunodeficiency Virus (HIV) Infections1
Not AvailableCompletedTreatmentSeborrheic Dermatitis1
Not AvailableRecruitingNot AvailableHealthy Volunteers1
Not AvailableUnknown StatusTreatmentProstate Cancer1
Not AvailableWithdrawnTreatmentProstate Cancer1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Dosage forms
FormRouteStrength
Aerosol, foamTopical20 mg/g
Aerosol, foamTopical2 g/100g
CreamTopical20 mg/g
CreamTopical20 mg/1
Shampoo, suspensionTopical20 mg/mL
Shampoo, suspensionTopical20.5 mg/mL
TabletOral200 mg/1
Kit
CreamTopical2 %
ShampooTopical20 mg/mL
ShampooTopical2 %
ShampooTopical10 mg/mL
SuspensionOral20 mg
TabletOral200 mg
GelTopical2 %
GelTopical20 mg/g
Prices
Unit descriptionCostUnit
Extina 2% Foam 100 gm Can375.44USD can
Extina 2% Foam 50 gm Can201.53USD can
Nizoral 2% Shampoo 120ml Bottle49.43USD bottle
Ketoconazole 2% Cream 60 gm Tube44.72USD tube
Ketoconazole 2% Cream 30 gm Tube29.43USD tube
Ketoconazole 2% Shampoo 120ml Bottle27.98USD bottle
Ketoconazole 2% Cream 15 gm Tube19.99USD tube
Ketoconazole powder15.0USD g
Nizoral 200 mg tablet4.75USD tablet
Extina 2% foam3.61USD g
Ketoconazole 200 mg tablet3.21USD tablet
Kuric 2% cream1.54USD g
Apo-Ketoconazole 200 mg Tablet1.24USD tablet
Novo-Ketoconazole 200 mg Tablet1.24USD tablet
Nu-Ketocon 200 mg Tablet1.24USD tablet
Nizoral 2% cream1.22USD g
Ketoconazole 2% cream1.1USD g
Ketoderm 2 % Cream0.35USD g
Ketoconazole 2% shampoo0.23USD ml
Nizoral a-d 1% shampoo0.07USD ml
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US5456851No1994-04-072014-04-07Us
US7179475No1998-12-042018-12-04Us
US8232276No2000-11-242020-11-24Us
US8735393No1998-12-042018-12-04Us
US7553835No1998-10-192018-10-19Us
US8026238No1998-10-192018-10-19Us

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)146U.S. Patent 4,144,346.
water solubility0.0866 mg/LNot Available
logP4.35SANGSTER (1993)
Predicted Properties
PropertyValueSource
Water Solubility0.00931 mg/mLALOGPS
logP4.3ALOGPS
logP4.19ChemAxon
logS-4.8ALOGPS
pKa (Strongest Basic)6.75ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count6ChemAxon
Hydrogen Donor Count0ChemAxon
Polar Surface Area69.06 Å2ChemAxon
Rotatable Bond Count7ChemAxon
Refractivity138.07 m3·mol-1ChemAxon
Polarizability54.83 Å3ChemAxon
Number of Rings5ChemAxon
Bioavailability1ChemAxon
Rule of FiveNoChemAxon
Ghose FilterNoChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleYesChemAxon
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9156
Blood Brain Barrier+0.6704
Caco-2 permeable+0.8866
P-glycoprotein substrateSubstrate0.7293
P-glycoprotein inhibitor IInhibitor0.8389
P-glycoprotein inhibitor IIInhibitor0.8388
Renal organic cation transporterNon-inhibitor0.5644
CYP450 2C9 substrateNon-substrate0.7898
CYP450 2D6 substrateNon-substrate0.9115
CYP450 3A4 substrateSubstrate0.7409
CYP450 1A2 substrateInhibitor0.9106
CYP450 2C9 inhibitorInhibitor0.8949
CYP450 2D6 inhibitorInhibitor0.8931
CYP450 2C19 inhibitorInhibitor0.8994
CYP450 3A4 inhibitorInhibitor0.796
CYP450 inhibitory promiscuityHigh CYP Inhibitory Promiscuity0.9386
Ames testNon AMES toxic0.7003
CarcinogenicityNon-carcinogens0.8836
BiodegradationNot ready biodegradable1.0
Rat acute toxicity3.4739 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9258
hERG inhibition (predictor II)Inhibitor0.8403
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 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 phenylpiperazines. These are compounds containing a phenylpiperazine skeleton, which consists of a piperazine bound to a phenyl group.
Kingdom
Organic compounds
Super Class
Organoheterocyclic compounds
Class
Diazinanes
Sub Class
Piperazines
Direct Parent
Phenylpiperazines
Alternative Parents
N-arylpiperazines / Aminophenyl ethers / Phenoxy compounds / Aniline and substituted anilines / Dialkylarylamines / Dichlorobenzenes / Alkyl aryl ethers / Ketals / Aryl chlorides / N-substituted imidazoles
show 12 more
Substituents
Phenylpiperazine / N-arylpiperazine / Aminophenyl ether / 1,3-dichlorobenzene / Phenol ether / Tertiary aliphatic/aromatic amine / Phenoxy compound / Dialkylarylamine / Aniline or substituted anilines / Alkyl aryl ether
show 34 more
Molecular Framework
Aromatic heteromonocyclic compounds
External Descriptors
N-arylpiperazine, imidazoles, ether, dioxolane, dichlorobenzene, N-carbonylpiperazine (CHEBI:48339) / a small molecule (CPD-4503)

Targets

Kind
Protein
Organism
Yeast
Pharmacological action
Yes
Actions
Inhibitor
General Function
Sterol 14-demethylase activity
Specific Function
Catalyzes C14-demethylation of lanosterol which is critical for ergosterol biosynthesis. It transforms lanosterol into 4,4'-dimethyl cholesta-8,14,24-triene-3-beta-ol.
Gene Name
ERG11
Uniprot ID
P10613
Uniprot Name
Lanosterol 14-alpha demethylase
Molecular Weight
60674.965 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. Agut J, Palacin C, Sacristan A, Ortiz JA: Inhibition of ergosterol synthesis by sertaconazole in Candida albicans. Arzneimittelforschung. 1992 May;42(5A):718-20. [PubMed:1627190]
  4. Berman HM, Westbrook J, Feng Z, Gilliland G, Bhat TN, Weissig H, Shindyalov IN, Bourne PE: The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42. [PubMed:10592235]
  5. Agut J, Palacin C, Salgado J, Casas E, Sacristan A, Ortiz JA: Direct membrane-damaging effect of sertaconazole on Candida albicans as a mechanism of its fungicidal activity. Arzneimittelforschung. 1992 May;42(5A):721-4. [PubMed:1627191]
  6. Croxtall JD, Plosker GL: Sertaconazole: a review of its use in the management of superficial mycoses in dermatology and gynaecology. Drugs. 2009;69(3):339-59. doi: 10.2165/00003495-200969030-00009. [PubMed:19275277]
  7. Borgers M, Degreef H, Cauwenbergh G: Fungal infections of the skin: infection process and antimycotic therapy. Curr Drug Targets. 2005 Dec;6(8):849-62. [PubMed:16375669]
  8. Warrilow AG, Martel CM, Parker JE, Melo N, Lamb DC, Nes WD, Kelly DE, Kelly SL: Azole binding properties of Candida albicans sterol 14-alpha demethylase (CaCYP51). Antimicrob Agents Chemother. 2010 Oct;54(10):4235-45. doi: 10.1128/AAC.00587-10. Epub 2010 Jul 12. [PubMed:20625155]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Binder
General Function
Zinc ion binding
Specific Function
Steroid hormone receptors are ligand-activated transcription factors that regulate eukaryotic gene expression and affect cellular proliferation and differentiation in target tissues. Transcription ...
Gene Name
AR
Uniprot ID
P10275
Uniprot Name
Androgen receptor
Molecular Weight
98987.9 Da
References
  1. Eil C: Ketoconazole binds to the human androgen receptor. Horm Metab Res. 1992 Aug;24(8):367-70. [PubMed:1526623]
3. 17-hydroxylase
Kind
Protein
Organism
Human
Pharmacological action
Unknown
References
  1. Trachtenberg J, Zadra J: Steroid synthesis inhibition by ketoconazole: sites of action. Clin Invest Med. 1988 Feb;11(1):1-5. [PubMed:2966691]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
General Function
Steroid hydroxylase activity
Specific Function
Specifically catalyzes the 21-hydroxylation of steroids. Required for the adrenal synthesis of mineralocorticoids and glucocorticoids.
Gene Name
CYP21A2
Uniprot ID
P08686
Uniprot Name
Steroid 21-hydroxylase
Molecular Weight
55886.805 Da
References
  1. Trachtenberg J, Zadra J: Steroid synthesis inhibition by ketoconazole: sites of action. Clin Invest Med. 1988 Feb;11(1):1-5. [PubMed:2966691]
5. 11-hydroxylase
Kind
Protein
Organism
Human
Pharmacological action
Unknown
References
  1. Trachtenberg J, Zadra J: Steroid synthesis inhibition by ketoconazole: sites of action. Clin Invest Med. 1988 Feb;11(1):1-5. [PubMed:2966691]
  2. Loose DS, Kan PB, Hirst MA, Marcus RA, Feldman D: Ketoconazole blocks adrenal steroidogenesis by inhibiting cytochrome P450-dependent enzymes. J Clin Invest. 1983 May;71(5):1495-9. [PubMed:6304148]
Details
6. Cytochrome P450 19A1
Kind
Protein
Organism
Human
Pharmacological action
Unknown
General Function
Oxygen binding
Specific Function
Catalyzes the formation of aromatic C18 estrogens from C19 androgens.
Gene Name
CYP19A1
Uniprot ID
P11511
Uniprot Name
Aromatase
Molecular Weight
57882.48 Da
References
  1. Weber MM, Will A, Adelmann B, Engelhardt D: Effect of ketoconazole on human ovarian C17,20-desmolase and aromatase. J Steroid Biochem Mol Biol. 1991 Feb;38(2):213-8. [PubMed:2004042]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Voltage-gated potassium channel activity involved in ventricular cardiac muscle cell action potential repolarization
Specific Function
Pore-forming (alpha) subunit of voltage-gated inwardly rectifying potassium channel. Channel properties are modulated by cAMP and subunit assembly. Mediates the rapidly activating component of the ...
Gene Name
KCNH2
Uniprot ID
Q12809
Uniprot Name
Potassium voltage-gated channel subfamily H member 2
Molecular Weight
126653.52 Da
References
  1. Chiu PJ, Marcoe KF, Bounds SE, Lin CH, Feng JJ, Lin A, Cheng FC, Crumb WJ, Mitchell R: Validation of a [3H]astemizole binding assay in HEK293 cells expressing HERG K+ channels. J Pharmacol Sci. 2004 Jul;95(3):311-9. [PubMed:15272206]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Antagonist
General Function
Zinc ion binding
Specific Function
Nuclear receptor that binds and is activated by variety of endogenous and xenobiotic compounds. Transcription factor that activates the transcription of multiple genes involved in the metabolism an...
Gene Name
NR1I2
Uniprot ID
O75469
Uniprot Name
Nuclear receptor subfamily 1 group I member 2
Molecular Weight
49761.245 Da
References
  1. Svecova L, Vrzal R, Burysek L, Anzenbacherova E, Cerveny L, Grim J, Trejtnar F, Kunes J, Pour M, Staud F, Anzenbacher P, Dvorak Z, Pavek P: Azole antimycotics differentially affect rifampicin-induced pregnane X receptor-mediated CYP3A4 gene expression. Drug Metab Dispos. 2008 Feb;36(2):339-48. Epub 2007 Nov 12. [PubMed:17998298]
  2. Li H, Redinbo MR, Venkatesh M, Ekins S, Chaudhry A, Bloch N, Negassa A, Mukherjee P, Kalpana G, Mani S: Novel yeast-based strategy unveils antagonist binding regions on the nuclear xenobiotic receptor PXR. J Biol Chem. 2013 May 10;288(19):13655-68. doi: 10.1074/jbc.M113.455485. Epub 2013 Mar 22. [PubMed:23525103]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
General Function
Zinc ion binding
Specific Function
Binds and transactivates the retinoic acid response elements that control expression of the retinoic acid receptor beta 2 and alcohol dehydrogenase 3 genes. Transactivates both the phenobarbital re...
Gene Name
NR1I3
Uniprot ID
Q14994
Uniprot Name
Nuclear receptor subfamily 1 group I member 3
Molecular Weight
39942.145 Da
References
  1. Dring AM, Anderson LE, Qamar S, Stoner MA: Rational quantitative structure-activity relationship (RQSAR) screen for PXR and CAR isoform-specific nuclear receptor ligands. Chem Biol Interact. 2010 Dec 5;188(3):512-25. doi: 10.1016/j.cbi.2010.09.018. Epub 2010 Oct 20. [PubMed:20869355]

Enzymes

Details
1. Cytochrome P450 3A4
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
Inhibitor
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. Sakaeda T, Iwaki K, Kakumoto M, Nishikawa M, Niwa T, Jin JS, Nakamura T, Nishiguchi K, Okamura N, Okumura K: Effect of micafungin on cytochrome P450 3A4 and multidrug resistance protein 1 activities, and its comparison with azole antifungal drugs. J Pharm Pharmacol. 2005 Jun;57(6):759-64. [PubMed:15969931]
  2. Elsherbiny ME, El-Kadi AO, Brocks DR: The metabolism of amiodarone by various CYP isoenzymes of human and rat, and the inhibitory influence of ketoconazole. J Pharm Pharm Sci. 2008;11(1):147-59. [PubMed:18445370]
  3. 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]
  4. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Inhibitor
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. 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
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. 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
Inhibitor
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. 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]
  2. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Oxygen binding
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
CYP3A5
Uniprot ID
P20815
Uniprot Name
Cytochrome P450 3A5
Molecular Weight
57108.065 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]
  2. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Oxygen binding
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
CYP3A7
Uniprot ID
P24462
Uniprot Name
Cytochrome P450 3A7
Molecular Weight
57525.03 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]
  2. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Inhibitor
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
CYP2C8
Uniprot ID
P10632
Uniprot Name
Cytochrome P450 2C8
Molecular Weight
55824.275 Da
References
  1. Walsky RL, Gaman EA, Obach RS: Examination of 209 drugs for inhibition of cytochrome P450 2C8. J Clin Pharmacol. 2005 Jan;45(1):68-78. [PubMed:15601807]
  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
Inhibitor
General Function
Oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen
Specific Function
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
CYP1A2
Uniprot ID
P05177
Uniprot Name
Cytochrome P450 1A2
Molecular Weight
58293.76 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Inhibitor
Inducer
General Function
Vitamin d 24-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
CYP1A1
Uniprot ID
P04798
Uniprot Name
Cytochrome P450 1A1
Molecular Weight
58164.815 Da
References
  1. Elsherbiny ME, El-Kadi AO, Brocks DR: The metabolism of amiodarone by various CYP isoenzymes of human and rat, and the inhibitory influence of ketoconazole. J Pharm Pharm Sci. 2008;11(1):147-59. [PubMed:18445370]
  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
Inhibitor
General Function
Oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, nad(p)h as one donor, and incorporation of one atom of oxygen
Specific Function
Catalyzes the side-chain cleavage reaction of cholesterol to pregnenolone.
Gene Name
CYP11A1
Uniprot ID
P05108
Uniprot Name
Cholesterol side-chain cleavage enzyme, mitochondrial
Molecular Weight
60101.87 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Steroid 11-beta-monooxygenase activity
Specific Function
Has steroid 11-beta-hydroxylase activity. In addition to this activity, the 18 or 19-hydroxylation of steroids and the aromatization of androstendione to estrone have also been ascribed to cytochro...
Gene Name
CYP11B1
Uniprot ID
P15538
Uniprot Name
Cytochrome P450 11B1, mitochondrial
Molecular Weight
57572.44 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Oxygen binding
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
CYP1B1
Uniprot ID
Q16678
Uniprot Name
Cytochrome P450 1B1
Molecular Weight
60845.33 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Retinoic acid binding
Specific Function
Plays a key role in retinoic acid metabolism. Acts on retinoids, including all-trans-retinoic acid (RA) and its stereoisomer 9-cis-RA. Capable of both 4-hydroxylation and 18-hydroxylation. Responsi...
Gene Name
CYP26A1
Uniprot ID
O43174
Uniprot Name
Cytochrome P450 26A1
Molecular Weight
56198.11 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Steroid hydroxylase activity
Specific Function
Exhibits a high coumarin 7-hydroxylase activity. Can act in the hydroxylation of the anti-cancer drugs cyclophosphamide and ifosphamide. Competent in the metabolic activation of aflatoxin B1. Const...
Gene Name
CYP2A6
Uniprot ID
P11509
Uniprot Name
Cytochrome P450 2A6
Molecular Weight
56501.005 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Inhibitor
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
CYP2B6
Uniprot ID
P20813
Uniprot Name
Cytochrome P450 2B6
Molecular Weight
56277.81 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Sterol 14-demethylase activity
Specific Function
Catalyzes C14-demethylation of lanosterol; it transforms lanosterol into 4,4'-dimethyl cholesta-8,14,24-triene-3-beta-ol.
Gene Name
CYP51A1
Uniprot ID
Q16850
Uniprot Name
Lanosterol 14-alpha demethylase
Molecular Weight
56805.26 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]

Transporters

Details
1. Bile salt export pump
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Transporter activity
Specific Function
Involved in the ATP-dependent secretion of bile salts into the canaliculus of hepatocytes.
Gene Name
ABCB11
Uniprot ID
O95342
Uniprot Name
Bile salt export pump
Molecular Weight
146405.83 Da
References
  1. Wang EJ, Casciano CN, Clement RP, Johnson WW: Fluorescent substrates of sister-P-glycoprotein (BSEP) evaluated as markers of active transport and inhibition: evidence for contingent unequal binding sites. Pharm Res. 2003 Apr;20(4):537-44. [PubMed:12739759]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
Inhibitor
General Function
Xenobiotic-transporting atpase activity
Specific Function
Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
Gene Name
ABCB1
Uniprot ID
P08183
Uniprot Name
Multidrug resistance protein 1
Molecular Weight
141477.255 Da
References
  1. Choo EF, Leake B, Wandel C, Imamura H, Wood AJ, Wilkinson GR, Kim RB: Pharmacological inhibition of P-glycoprotein transport enhances the distribution of HIV-1 protease inhibitors into brain and testes. Drug Metab Dispos. 2000 Jun;28(6):655-60. [PubMed:10820137]
  2. Wang EJ, Casciano CN, Clement RP, Johnson WW: Active transport of fluorescent P-glycoprotein substrates: evaluation as markers and interaction with inhibitors. Biochem Biophys Res Commun. 2001 Nov 30;289(2):580-5. [PubMed:11716514]
  3. Wang EJ, Lew K, Casciano CN, Clement RP, Johnson WW: Interaction of common azole antifungals with P glycoprotein. Antimicrob Agents Chemother. 2002 Jan;46(1):160-5. [PubMed:11751127]
  4. Ekins S, Kim RB, Leake BF, Dantzig AH, Schuetz EG, Lan LB, Yasuda K, Shepard RL, Winter MA, Schuetz JD, Wikel JH, Wrighton SA: Three-dimensional quantitative structure-activity relationships of inhibitors of P-glycoprotein. Mol Pharmacol. 2002 May;61(5):964-73. [PubMed:11961113]
  5. Schwab D, Fischer H, Tabatabaei A, Poli S, Huwyler J: Comparison of in vitro P-glycoprotein screening assays: recommendations for their use in drug discovery. J Med Chem. 2003 Apr 24;46(9):1716-25. [PubMed:12699389]
  6. Nagy H, Goda K, Fenyvesi F, Bacso Z, Szilasi M, Kappelmayer J, Lustyik G, Cianfriglia M, Szabo G Jr: Distinct groups of multidrug resistance modulating agents are distinguished by competition of P-glycoprotein-specific antibodies. Biochem Biophys Res Commun. 2004 Mar 19;315(4):942-9. [PubMed:14985103]
  7. Yasuda K, Lan LB, Sanglard D, Furuya K, Schuetz JD, Schuetz EG: Interaction of cytochrome P450 3A inhibitors with P-glycoprotein. J Pharmacol Exp Ther. 2002 Oct;303(1):323-32. [PubMed:12235267]
  8. Dahan A, Sabit H, Amidon GL: The H2 receptor antagonist nizatidine is a P-glycoprotein substrate: characterization of its intestinal epithelial cell efflux transport. AAPS J. 2009 Jun;11(2):205-13. doi: 10.1208/s12248-009-9092-5. Epub 2009 Mar 25. [PubMed:19319690]
  9. Takano M, Hasegawa R, Fukuda T, Yumoto R, Nagai J, Murakami T: Interaction with P-glycoprotein and transport of erythromycin, midazolam and ketoconazole in Caco-2 cells. Eur J Pharmacol. 1998 Oct 9;358(3):289-94. [PubMed:9822896]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Sodium-independent organic anion transmembrane transporter activity
Specific Function
Mediates the Na(+)-independent transport of organic anions such as sulfobromophthalein (BSP) and conjugated (taurocholate) and unconjugated (cholate) bile acids (By similarity). Selectively inhibit...
Gene Name
SLCO1A2
Uniprot ID
P46721
Uniprot Name
Solute carrier organic anion transporter family member 1A2
Molecular Weight
74144.105 Da
References
  1. Cvetkovic M, Leake B, Fromm MF, Wilkinson GR, Kim RB: OATP and P-glycoprotein transporters mediate the cellular uptake and excretion of fexofenadine. Drug Metab Dispos. 1999 Aug;27(8):866-71. [PubMed:10421612]

Drug created on June 13, 2005 07:24 / Updated on November 22, 2017 12:33