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Identification
NameRosiglitazone
Accession NumberDB00412  (APRD00403)
TypeSmall Molecule
GroupsApproved, Investigational
DescriptionRosiglitazone is an anti-diabetic drug in the thiazolidinedione class of drugs. It is marketed by the pharmaceutical company GlaxoSmithKline as a stand-alone drug (Avandia) and in combination with metformin (Avandamet) or with glimepiride (Avandaryl). Like other thiazolidinediones, the mechanism of action of rosiglitazone is by activation of the intracellular receptor class of the peroxisome proliferator-activated receptors (PPARs), specifically PPARγ. Rosiglitazone is a selective ligand of PPARγ, and has no PPARα-binding action. Apart from its effect on insulin resistance, it appears to have an anti-inflammatory effect: nuclear factor kappa-B (NFκB) levels fall and inhibitor (IκB) levels increase in patients on rosiglitazone. Recent research has suggested that rosiglitazone may also be of benefit to a subset of patients with Alzheimer's disease not expressing the ApoE4 allele. This is the subject of a clinical trial currently underway.
Structure
Thumb
Synonyms
(±)-5-[p-[2-(methyl-2-pyridylamino)ethoxy]benzyl]-2,4-thiazolidinedione
(RS)-5-{4-[2-(Methyl-2-pyridylamino)ethoxy]benzyl}-2,4-thiazolidinedion
Rosiglitazon
Rosiglitazona
Rosiglitazone
Rosiglitazonum
External Identifiers
  • BRL 49653 C
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
AvandiaTablet, film coated2 mg/1OralPhysicians Total Care, Inc.2005-05-13Not applicableUs
AvandiaTablet, film coated2 mg/1OralGlaxo Smith Kline Llc2011-05-252016-06-18Us
AvandiaTablet4 mgOralGlaxosmithkline Inc2000-03-21Not applicableCanada
AvandiaTablet, film coated4 mg/1OralCardinal Health1999-05-29Not applicableUs
AvandiaTablet, film coated8 mg/1OralGlaxo Smith Kline Llc2011-05-252016-04-03Us
AvandiaTablet8 mgOralGlaxosmithkline Inc2000-03-21Not applicableCanada
AvandiaTablet, film coated4 mg/1OralPhysicians Total Care, Inc.2006-02-07Not applicableUs
AvandiaTablet, film coated8 mg/1OralCardinal Health1999-05-28Not applicableUs
AvandiaTablet, film coated8 mg/1OralPhysicians Total Care, Inc.2001-05-09Not applicableUs
AvandiaTablet2 mgOralGlaxosmithkline Inc2000-03-21Not applicableCanada
Avandia 2mgTablet, film coated2 mg/1OralGlaxo Smith Kline Llc2011-05-25Not applicableUs
Avandia 4mgTablet, film coated4 mg/1OralGlaxo Smith Kline Llc2011-05-25Not applicableUs
Avandia 8mgTablet, film coated8 mg/1OralGlaxo Smith Kline Llc2011-05-252016-10-13Us
Dom-rosiglitazoneTablet2 mgOralDominion PharmacalNot applicableNot applicableCanada
Dom-rosiglitazoneTablet4 mgOralDominion PharmacalNot applicableNot applicableCanada
Dom-rosiglitazoneTablet8 mgOralDominion PharmacalNot applicableNot applicableCanada
Mylan-rosiglitazoneTablet4 mgOralMylan Pharmaceuticals UlcNot applicableNot applicableCanada
Mylan-rosiglitazoneTablet8 mgOralMylan Pharmaceuticals UlcNot applicableNot applicableCanada
Mylan-rosiglitazoneTablet2 mgOralMylan Pharmaceuticals UlcNot applicableNot applicableCanada
PHL-rosiglitazoneTablet2 mgOralPharmel IncNot applicableNot applicableCanada
PHL-rosiglitazoneTablet4 mgOralPharmel IncNot applicableNot applicableCanada
PHL-rosiglitazoneTablet8 mgOralPharmel IncNot applicableNot applicableCanada
PMS-rosiglitazoneTablet8 mgOralPharmascience IncNot applicableNot applicableCanada
PMS-rosiglitazoneTablet2 mgOralPharmascience IncNot applicableNot applicableCanada
PMS-rosiglitazoneTablet4 mgOralPharmascience IncNot applicableNot applicableCanada
Teva-rosiglitazoneTablet2 mgOralTeva Canada LimitedNot applicableNot applicableCanada
Teva-rosiglitazoneTablet4 mgOralTeva Canada LimitedNot applicableNot applicableCanada
Teva-rosiglitazoneTablet8 mgOralTeva Canada LimitedNot applicableNot applicableCanada
Approved Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Apo-rosiglitazoneTablet2.0 mgOralApotex IncNot applicableNot applicableCanada
Apo-rosiglitazoneTablet4.0 mgOralApotex IncNot applicableNot applicableCanada
Apo-rosiglitazoneTablet8.0 mgOralApotex IncNot applicableNot applicableCanada
Approved Over the Counter ProductsNot Available
Unapproved/Other Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
AvandiaTablet, film coated4 mgOralSmith Kline Beecham Plc2000-07-11Not applicableEu
AvandiaTablet, film coated2 mgOralSmith Kline Beecham Plc2000-07-11Not applicableEu
AvandiaTablet, film coated4 mgOralSmith Kline Beecham Plc2000-07-11Not applicableEu
AvandiaTablet, film coated2 mgOralSmith Kline Beecham Plc2000-07-11Not applicableEu
AvandiaTablet, film coated4 mgOralSmith Kline Beecham Plc2000-07-11Not applicableEu
AvandiaTablet, film coated8 mgOralSmith Kline Beecham Plc2000-07-11Not applicableEu
AvandiaTablet, film coated2 mgOralSmith Kline Beecham Plc2000-07-11Not applicableEu
AvandiaTablet, film coated8 mgOralSmith Kline Beecham Plc2000-07-11Not applicableEu
AvandiaTablet, film coated4 mgOralSmith Kline Beecham Plc2000-07-11Not applicableEu
AvandiaTablet, film coated4 mgOralSmith Kline Beecham Plc2000-07-11Not applicableEu
AvandiaTablet, film coated8 mgOralSmith Kline Beecham Plc2000-07-11Not applicableEu
AvandiaTablet, film coated2 mgOralSmith Kline Beecham Plc2000-07-11Not applicableEu
AvandiaTablet, film coated8 mgOralSmith Kline Beecham Plc2000-07-11Not applicableEu
AvandiaTablet, film coated4 mgOralSmith Kline Beecham Plc2000-07-11Not applicableEu
AvandiaTablet, film coated8 mgOralSmith Kline Beecham Plc2000-07-11Not applicableEu
AvandiaTablet, film coated4 mgOralSmith Kline Beecham Plc2000-07-11Not applicableEu
AvandiaTablet, film coated2 mgOralSmith Kline Beecham Plc2000-07-11Not applicableEu
International Brands
NameCompany
BlutabWerrick
DH-RosidiaHasan
DiabenElea
DiaglinexFarmindustria
GaudilCraveri
GliximinaDenver
NaidiHisun
RogelinTorrent
RoglitGedeon Richter
RomerolDrug International
RositDelta
RosixGarmisch
RossiniTrima
SensulinSquare
Sheng AoHengrui
Sheng MinShengJiTang Pharmaceutical
Brand mixtures
NameLabellerIngredients
AvaglimSmith Kline Beecham Ltd
AvandametGlaxo Smith Kline Llc
AvandarylGlaxo Smith Kline Llc
PMS-rosiglitazone-metforminPharmascience Inc
Salts
Name/CASStructureProperties
Rosiglitazone Maleate
155141-29-0
Thumb
  • InChI Key: SUFUKZSWUHZXAV-BTJKTKAUNA-N
  • Monoisotopic Mass: 473.125670795
  • Average Mass: 473.499
DBSALT000153
Categories
UNII05V02F2KDG
CAS number122320-73-4
WeightAverage: 357.427
Monoisotopic: 357.114712179
Chemical FormulaC18H19N3O3S
InChI KeyYASAKCUCGLMORW-UHFFFAOYNA-N
InChI
InChI=1/C18H19N3O3S/c1-21(16-4-2-3-9-19-16)10-11-24-14-7-5-13(6-8-14)12-15-17(22)20-18(23)25-15/h2-9,15H,10-12H2,1H3,(H,20,22,23)
IUPAC Name
5-[(4-{2-[methyl(pyridin-2-yl)amino]ethoxy}phenyl)methyl]-1,3-thiazolidine-2,4-dione
SMILES
CN(CCOC1=CC=C(CC2SC(=O)NC2=O)C=C1)C1=CC=CC=N1
Pharmacology
IndicationRosiglitazone is indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus.
Structured Indications
PharmacodynamicsWhen rosiglitazone is used as monotherapy, it is associated with increases in total cholesterol, LDL, and HDL. It is also associated with decreases in free fatty acids. Increases in LDL occurred primarily during the first 1 to 2 months of therapy with AVANDIA and LDL levels remained elevated above baseline throughout the trials. In contrast, HDL continued to rise over time. As a result, the LDL/HDL ratio peaked after 2 months of therapy and then appeared to decrease over time.
Mechanism of actionRosiglitazone acts as a highly selective and potent agonist at peroxisome proliferator activated receptors (PPAR) in target tissues for insulin action such as adipose tissue, skeletal muscle, and liver. Activation of PPAR-gamma receptors regulates the transcription of insulin-responsive genes involved in the control of glucose production, transport, and utilization. In this way, rosiglitazone enhances tissue sensitivity to insulin.
TargetKindPharmacological actionActionsOrganismUniProt ID
Peroxisome proliferator-activated receptor gammaProteinyes
agonist
HumanP37231 details
Long-chain-fatty-acid--CoA ligase 4Proteinunknown
inhibitor
HumanO60488 details
Related Articles
AbsorptionThe absolute bioavailability of rosiglitazone is 99%. Peak plasma concentrations are observed about 1 hour after dosing. Administration of rosiglitazone with food resulted in no change in overall exposure (AUC), but there was an approximately 28% decrease in Cmax and a delay in Tmax (1.75 hours). These changes are not likely to be clinically significant; therefore, rosiglitazone may be administered with or without food. Maximum plasma concentration (Cmax) and the area under the curve (AUC) of rosiglitazone increase in a dose-proportional manner over the therapeutic dose range.
Volume of distribution
  • 17.6 L [oral volume of distribution Vss/F]
  • 13.5 L [population mean, pediatric patients]
Protein binding99.8% bound to plasma proteins, primarily albumin.
Metabolism

Hepatic. Rosiglitazone is extensively metabolized in the liver to inactive metabolites via N-demethylation, hydroxylation, and conjugation with sulfate and glucuronic acid. In vitro data have shown that Cytochrome (CYP) P450 isoenzyme 2C8 (CYP2C8) and to a minor extent CYP2C9 are involved in the hepatic metabolism of rosiglitazone.

SubstrateEnzymesProduct
Rosiglitazone
N-DesmethylrosiglitazoneDetails
Rosiglitazone
para-HydroxyrosiglitazoneDetails
Rosiglitazone
ortho-HydroxyrosiglitazoneDetails
Rosiglitazone
Not Available
N-Despyridinyl rosiglitazoneDetails
N-Desmethylrosiglitazone
Not Available
N-Desmethyl-ortho-hydroxy rosiglitazoneDetails
ortho-Hydroxyrosiglitazone
Not Available
N-Desmethyl-ortho-hydroxy rosiglitazoneDetails
N-Desmethylrosiglitazone
Not Available
N-Desmethyl-para-hydroxy rosiglitazoneDetails
para-Hydroxyrosiglitazone
Not Available
N-Desmethyl-para-hydroxy rosiglitazoneDetails
N-Desmethyl-ortho-hydroxy rosiglitazone
Not Available
N-Desmethyl-ortho-O-sulfate rosiglitazoneDetails
ortho-Hydroxyrosiglitazone
Not Available
ortho-O-Glucuronide rosiglitazoneDetails
ortho-Hydroxyrosiglitazone
Not Available
ortho-O-Sulfate rosiglitazoneDetails
N-Desmethylrosiglitazone
Not Available
N-Desmethyl glucuronide rosiglitazoneDetails
para-Hydroxyrosiglitazone
Not Available
para-O-Glucuronide rosiglitazoneDetails
para-Hydroxyrosiglitazone
Not Available
para-O-Sulfate rosiglitazoneDetails
N-Desmethyl-para-hydroxy rosiglitazone
Not Available
N-Desmethyl para-O-sulfate rosiglitazoneDetails
Rosiglitazone
Not Available
Phenoxyacetic acid derivative of rosiglitazoneDetails
Route of eliminationFollowing oral or intravenous administration of [14C]rosiglitazone maleate, approximately 64% and 23% of the dose was eliminated in the urine and in the feces, respectively.
Half life3-4 hours (single oral dose, independent of dose)
Clearance
  • Oral clearance (CL) = 3.03 ± 0.87 L/hr [1 mg Fasting]
  • Oral CL = 2.89 ± 0.71 L/hr [2 mg Fasting]
  • Oral CL = 2.85 ± 0.69 L/hr [8 mg Fasting]
  • Oral CL = 2.97 ± 0.81 L/hr [8 mg Fed]
  • 3.15 L/hr [Population mean, Pediatric patients]
ToxicitySide effects include fluid retention, congestive heart failure (CHF), liver disease
Affected organisms
  • Humans and other mammals
Pathways
PathwayCategorySMPDB ID
Rosiglitazone Metabolism PathwayDrug metabolismSMP00653
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
Interactions
Drug Interactions
DrugInteractionDrug group
7,8-DICHLORO-1,2,3,4-TETRAHYDROISOQUINOLINE7,8-DICHLORO-1,2,3,4-TETRAHYDROISOQUINOLINE may increase the hypoglycemic activities of Rosiglitazone.Experimental
AbciximabRosiglitazone may increase the anticoagulant activities of Abciximab.Approved
AbirateroneThe serum concentration of Rosiglitazone can be increased when it is combined with Abiraterone.Approved
AcenocoumarolRosiglitazone may increase the anticoagulant activities of Acenocoumarol.Approved
AcetaminophenThe metabolism of Acetaminophen can be decreased when combined with Rosiglitazone.Approved
AcetohexamideRosiglitazone may increase the hypoglycemic activities of Acetohexamide.Withdrawn
Acetylsalicylic acidThe risk or severity of adverse effects can be increased when Acetylsalicylic acid is combined with Rosiglitazone.Approved, Vet Approved
AlmotriptanThe metabolism of Almotriptan can be decreased when combined with Rosiglitazone.Approved, Investigational
AlprostadilAlprostadil may increase the anticoagulant activities of Rosiglitazone.Approved, Investigational
AminophenazoneThe metabolism of Aminophenazone can be decreased when combined with Rosiglitazone.Approved, Withdrawn
Aminosalicylic AcidThe risk or severity of adverse effects can be increased when Aminosalicylic Acid is combined with Rosiglitazone.Approved
AmiodaroneThe metabolism of Rosiglitazone can be decreased when combined with Amiodarone.Approved, Investigational
AmitriptylineThe metabolism of Amitriptyline can be decreased when combined with Rosiglitazone.Approved
AmodiaquineThe serum concentration of Amodiaquine can be increased when it is combined with Rosiglitazone.Approved
AmprenavirThe metabolism of Amprenavir can be decreased when combined with Rosiglitazone.Approved
AnagrelideAnagrelide may increase the anticoagulant activities of Rosiglitazone.Approved
AncrodRosiglitazone may increase the anticoagulant activities of Ancrod.Investigational
AntipyrineThe metabolism of Antipyrine can be decreased when combined with Rosiglitazone.Approved
Antithrombin III humanRosiglitazone may increase the anticoagulant activities of Antithrombin III human.Approved
ApixabanRosiglitazone may increase the anticoagulant activities of Apixaban.Approved
AprepitantThe metabolism of Rosiglitazone can be increased when combined with Aprepitant.Approved, Investigational
AprotininThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Aprotinin.Approved, Withdrawn
ArdeparinRosiglitazone may increase the anticoagulant activities of Ardeparin.Approved, Withdrawn
ArgatrobanRosiglitazone may increase the anticoagulant activities of Argatroban.Approved, Investigational
AripiprazoleThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Aripiprazole.Approved, Investigational
Arsenic trioxideThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Arsenic trioxide.Approved, Investigational
ArtesunateThe serum concentration of the active metabolites of Artesunate can be reduced when Artesunate is used in combination with Rosiglitazone resulting in a loss in efficacy.Approved
ArticaineThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Articaine.Approved
AsenapineThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Asenapine.Approved
AtazanavirThe serum concentration of Rosiglitazone can be increased when it is combined with Atazanavir.Approved, Investigational
AtorvastatinThe metabolism of Atorvastatin can be decreased when combined with Rosiglitazone.Approved
AzelastineThe metabolism of Azelastine can be decreased when combined with Rosiglitazone.Approved
BalsalazideThe risk or severity of adverse effects can be increased when Balsalazide is combined with Rosiglitazone.Approved, Investigational
BecaplerminRosiglitazone may increase the anticoagulant activities of Becaplermin.Approved, Investigational
BendroflumethiazideThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Bendroflumethiazide.Approved
BenmoxinBenmoxin may increase the hypoglycemic activities of Rosiglitazone.Withdrawn
Benzyl alcoholThe metabolism of Benzyl alcohol can be decreased when combined with Rosiglitazone.Approved
BeraprostThe metabolism of Beraprost can be decreased when combined with Rosiglitazone.Investigational
BetamethasoneThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Betamethasone.Approved, Vet Approved
BivalirudinRosiglitazone may increase the anticoagulant activities of Bivalirudin.Approved, Investigational
BrexpiprazoleThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Brexpiprazole.Approved
BrompheniramineThe metabolism of Brompheniramine can be decreased when combined with Rosiglitazone.Approved
BumetanideThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Bumetanide.Approved
BuprenorphineThe metabolism of Buprenorphine can be decreased when combined with Rosiglitazone.Approved, Illicit, Investigational, Vet Approved
BupropionThe metabolism of Bupropion can be decreased when combined with Rosiglitazone.Approved
BuserelinThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Buserelin.Approved
ButylphthalideButylphthalide may increase the anticoagulant activities of Rosiglitazone.Investigational
CabazitaxelThe metabolism of Cabazitaxel can be decreased when combined with Rosiglitazone.Approved
CaffeineThe metabolism of Caffeine can be decreased when combined with Rosiglitazone.Approved
CangrelorCangrelor may increase the anticoagulant activities of Rosiglitazone.Approved
CapecitabineThe metabolism of Rosiglitazone can be decreased when combined with Capecitabine.Approved, Investigational
CarbamazepineThe metabolism of Rosiglitazone can be increased when combined with Carbamazepine.Approved, Investigational
CarbinoxamineThe metabolism of Carbinoxamine can be decreased when combined with Rosiglitazone.Approved
CaroxazoneCaroxazone may increase the hypoglycemic activities of Rosiglitazone.Withdrawn
CelecoxibThe metabolism of Rosiglitazone can be decreased when combined with Celecoxib.Approved, Investigational
CeritinibThe serum concentration of Rosiglitazone can be increased when it is combined with Ceritinib.Approved
CerivastatinThe metabolism of Cerivastatin can be decreased when combined with Rosiglitazone.Withdrawn
CertoparinRosiglitazone may increase the anticoagulant activities of Certoparin.Approved
ChloroquineThe metabolism of Chloroquine can be decreased when combined with Rosiglitazone.Approved, Vet Approved
ChlorothiazideThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Chlorothiazide.Approved, Vet Approved
ChlorpropamideRosiglitazone may increase the hypoglycemic activities of Chlorpropamide.Approved
ChlorthalidoneThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Chlorthalidone.Approved
CholecalciferolThe metabolism of Rosiglitazone can be decreased when combined with Cholecalciferol.Approved, Nutraceutical
CholestyramineThe serum concentration of Rosiglitazone can be decreased when it is combined with Cholestyramine.Approved
CilostazolThe serum concentration of Cilostazol can be increased when it is combined with Rosiglitazone.Approved
CinoxacinCinoxacin may increase the hypoglycemic activities of Rosiglitazone.Approved, Withdrawn
CiprofloxacinCiprofloxacin may increase the hypoglycemic activities of Rosiglitazone.Approved, Investigational
CisaprideThe metabolism of Cisapride can be decreased when combined with Rosiglitazone.Approved, Investigational, Withdrawn
CitalopramCitalopram may increase the hypoglycemic activities of Rosiglitazone.Approved
Citric AcidRosiglitazone may increase the anticoagulant activities of Citric Acid.Nutraceutical, Vet Approved
ClopidogrelThe metabolism of Rosiglitazone can be decreased when combined with Clopidogrel.Approved, Nutraceutical
ClotrimazoleThe metabolism of Rosiglitazone can be decreased when combined with Clotrimazole.Approved, Vet Approved
ClozapineThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Clozapine.Approved
CorticotropinThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Corticotropin.Approved, Vet Approved
Cortisone acetateThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Cortisone acetate.Approved
CyclophosphamideThe metabolism of Cyclophosphamide can be decreased when combined with Rosiglitazone.Approved, Investigational
CyclosporineThe metabolism of Rosiglitazone can be decreased when combined with Cyclosporine.Approved, Investigational, Vet Approved
Cyproterone acetateThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Cyproterone acetate.Approved, Investigational
Dabigatran etexilateRosiglitazone may increase the anticoagulant activities of Dabigatran etexilate.Approved
DabrafenibThe serum concentration of Rosiglitazone can be decreased when it is combined with Dabrafenib.Approved
DalteparinRosiglitazone may increase the anticoagulant activities of Dalteparin.Approved
DanaparoidRosiglitazone may increase the anticoagulant activities of Danaparoid.Approved, Withdrawn
DanazolThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Danazol.Approved
DapoxetineDapoxetine may increase the hypoglycemic activities of Rosiglitazone.Investigational
DapsoneThe metabolism of Dapsone can be decreased when combined with Rosiglitazone.Approved, Investigational
DarunavirThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Darunavir.Approved
DasabuvirThe metabolism of Dasabuvir can be decreased when combined with Rosiglitazone.Approved
DeferasiroxThe serum concentration of Rosiglitazone can be increased when it is combined with Deferasirox.Approved, Investigational
DefibrotideDefibrotide may increase the anticoagulant activities of Rosiglitazone.Approved, Investigational
DelavirdineThe metabolism of Rosiglitazone can be decreased when combined with Delavirdine.Approved
dersalazineThe risk or severity of adverse effects can be increased when dersalazine is combined with Rosiglitazone.Investigational
DesirudinRosiglitazone may increase the anticoagulant activities of Desirudin.Approved
DesogestrelThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Desogestrel.Approved
DesvenlafaxineDesvenlafaxine may increase the hypoglycemic activities of Rosiglitazone.Approved
DexamethasoneThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Dexamethasone.Approved, Investigational, Vet Approved
DextranRosiglitazone may increase the anticoagulant activities of Dextran.Approved, Vet Approved
Dextran 40Rosiglitazone may increase the anticoagulant activities of Dextran 40.Approved
Dextran 70Rosiglitazone may increase the anticoagulant activities of Dextran 70.Approved
Dextran 75Rosiglitazone may increase the anticoagulant activities of Dextran 75.Approved
DextromethorphanThe metabolism of Dextromethorphan can be decreased when combined with Rosiglitazone.Approved
DiazepamThe metabolism of Diazepam can be decreased when combined with Rosiglitazone.Approved, Illicit, Vet Approved
DiazoxideThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Diazoxide.Approved
DiclofenacThe metabolism of Diclofenac can be decreased when combined with Rosiglitazone.Approved, Vet Approved
DicoumarolRosiglitazone may increase the anticoagulant activities of Dicoumarol.Approved
DienogestThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Dienogest.Approved
DiflunisalThe risk or severity of adverse effects can be increased when Diflunisal is combined with Rosiglitazone.Approved
DihydrotestosteroneDihydrotestosterone may increase the hypoglycemic activities of Rosiglitazone.Illicit
DiltiazemThe metabolism of Diltiazem can be decreased when combined with Rosiglitazone.Approved
DipyridamoleDipyridamole may increase the anticoagulant activities of Rosiglitazone.Approved
DisopyramideRosiglitazone may increase the hypoglycemic activities of Disopyramide.Approved
DomperidoneThe metabolism of Domperidone can be decreased when combined with Rosiglitazone.Approved, Investigational, Vet Approved
DrospirenoneThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Drospirenone.Approved
DuloxetineDuloxetine may increase the hypoglycemic activities of Rosiglitazone.Approved
Edetic AcidRosiglitazone may increase the anticoagulant activities of Edetic Acid.Approved, Vet Approved
EdoxabanRosiglitazone may increase the anticoagulant activities of Edoxaban.Approved
EfavirenzThe metabolism of Rosiglitazone can be decreased when combined with Efavirenz.Approved, Investigational
EltrombopagThe metabolism of Eltrombopag can be decreased when combined with Rosiglitazone.Approved
EnoxacinEnoxacin may increase the hypoglycemic activities of Rosiglitazone.Approved
EnoxaparinRosiglitazone may increase the anticoagulant activities of Enoxaparin.Approved
EnzalutamideThe metabolism of Enzalutamide can be decreased when combined with Rosiglitazone.Approved
EpinastineEpinastine may increase the anticoagulant activities of Rosiglitazone.Approved, Investigational
EpinephrineThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Epinephrine.Approved, Vet Approved
eplivanserineeplivanserine may increase the anticoagulant activities of Rosiglitazone.Investigational
EpoprostenolEpoprostenol may increase the anticoagulant activities of Rosiglitazone.Approved
EptifibatideEptifibatide may increase the anticoagulant activities of Rosiglitazone.Approved, Investigational
ErlotinibThe metabolism of Erlotinib can be decreased when combined with Rosiglitazone.Approved, Investigational
Erythrityl TetranitrateThe risk or severity of adverse effects can be increased when Erythrityl Tetranitrate is combined with Rosiglitazone.Approved
EscitalopramEscitalopram may increase the hypoglycemic activities of Rosiglitazone.Approved, Investigational
EstradiolThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Estradiol.Approved, Investigational, Vet Approved
Estrone sulfateThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Estrone sulfate.Approved
EszopicloneThe metabolism of Eszopiclone can be decreased when combined with Rosiglitazone.Approved
Etacrynic acidThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Etacrynic acid.Approved
Ethinyl EstradiolThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Ethinyl Estradiol.Approved
Ethyl biscoumacetateRosiglitazone may increase the anticoagulant activities of Ethyl biscoumacetate.Withdrawn
Ethynodiol diacetateThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Ethynodiol diacetate.Approved
EtonogestrelThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Etonogestrel.Approved, Investigational
EtoperidoneEtoperidone may increase the hypoglycemic activities of Rosiglitazone.Approved
EtravirineThe metabolism of Rosiglitazone can be decreased when combined with Etravirine.Approved
EverolimusThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Everolimus.Approved
FelodipineThe metabolism of Rosiglitazone can be decreased when combined with Felodipine.Approved, Investigational
FesoterodineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Rosiglitazone.Approved
FleroxacinFleroxacin may increase the hypoglycemic activities of Rosiglitazone.Approved
FloxuridineThe metabolism of Rosiglitazone can be decreased when combined with Floxuridine.Approved
FluconazoleThe metabolism of Rosiglitazone can be decreased when combined with Fluconazole.Approved
FludrocortisoneThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Fludrocortisone.Approved
FluindioneRosiglitazone may increase the anticoagulant activities of Fluindione.Investigational
FlumequineFlumequine may increase the hypoglycemic activities of Rosiglitazone.Withdrawn
FluorouracilThe metabolism of Rosiglitazone can be decreased when combined with Fluorouracil.Approved
FluoxetineFluoxetine may increase the hypoglycemic activities of Rosiglitazone.Approved, Vet Approved
FluoxymesteroneFluoxymesterone may increase the hypoglycemic activities of Rosiglitazone.Approved, Illicit
FluvastatinThe metabolism of Rosiglitazone can be decreased when combined with Fluvastatin.Approved
FluvoxamineThe metabolism of Rosiglitazone can be decreased when combined with Fluvoxamine.Approved, Investigational
FondaparinuxRosiglitazone may increase the anticoagulant activities of Fondaparinux.Investigational
Fondaparinux sodiumRosiglitazone may increase the anticoagulant activities of Fondaparinux sodium.Approved, Investigational
FosamprenavirThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Fosamprenavir.Approved
FosphenytoinThe metabolism of Rosiglitazone can be increased when combined with Fosphenytoin.Approved
FurazolidoneFurazolidone may increase the hypoglycemic activities of Rosiglitazone.Approved, Vet Approved
FurosemideThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Furosemide.Approved, Vet Approved
GabexateRosiglitazone may increase the anticoagulant activities of Gabexate.Investigational
GarenoxacinGarenoxacin may increase the hypoglycemic activities of Rosiglitazone.Investigational
GatifloxacinGatifloxacin may increase the hypoglycemic activities of Rosiglitazone.Approved, Investigational
GemfibrozilThe metabolism of Rosiglitazone can be decreased when combined with Gemfibrozil.Approved
GemifloxacinGemifloxacin may increase the hypoglycemic activities of Rosiglitazone.Approved, Investigational
GlibornurideRosiglitazone may increase the hypoglycemic activities of Glibornuride.Withdrawn
GliclazideRosiglitazone may increase the hypoglycemic activities of Gliclazide.Approved
GlimepirideRosiglitazone may increase the hypoglycemic activities of Glimepiride.Approved
GlipizideRosiglitazone may increase the hypoglycemic activities of Glipizide.Approved
GliquidoneRosiglitazone may increase the hypoglycemic activities of Gliquidone.Approved
GlisoxepideRosiglitazone may increase the hypoglycemic activities of Glisoxepide.Approved
GlyburideRosiglitazone may increase the hypoglycemic activities of Glyburide.Approved
GoserelinThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Goserelin.Approved
GrepafloxacinGrepafloxacin may increase the hypoglycemic activities of Rosiglitazone.Withdrawn
HalofantrineThe metabolism of Halofantrine can be decreased when combined with Rosiglitazone.Approved
HeparinRosiglitazone may increase the anticoagulant activities of Heparin.Approved, Investigational
HirulogRosiglitazone may increase the anticoagulant activities of Hirulog.Experimental
HistrelinThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Histrelin.Approved
HydracarbazineHydracarbazine may increase the hypoglycemic activities of Rosiglitazone.Approved
HydrochlorothiazideThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Hydrochlorothiazide.Approved, Vet Approved
HydrocortisoneThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Hydrocortisone.Approved, Vet Approved
HydroflumethiazideThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Hydroflumethiazide.Approved
Hydroxyprogesterone caproateThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Hydroxyprogesterone caproate.Approved
IbudilastIbudilast may increase the anticoagulant activities of Rosiglitazone.Approved, Investigational
IbuprofenThe metabolism of Ibuprofen can be decreased when combined with Rosiglitazone.Approved
Icosapent ethylIcosapent ethyl may increase the anticoagulant activities of Rosiglitazone.Approved, Nutraceutical
idraparinuxRosiglitazone may increase the anticoagulant activities of idraparinux.Investigational
IfenprodilIfenprodil may increase the anticoagulant activities of Rosiglitazone.Approved, Withdrawn
IfosfamideThe metabolism of Ifosfamide can be decreased when combined with Rosiglitazone.Approved
IloperidoneThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Iloperidone.Approved
IloprostIloprost may increase the anticoagulant activities of Rosiglitazone.Approved, Investigational
IndalpineIndalpine may increase the hypoglycemic activities of Rosiglitazone.Investigational, Withdrawn
IndapamideThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Indapamide.Approved
IndinavirThe metabolism of Rosiglitazone can be decreased when combined with Indinavir.Approved
Insulin AspartRosiglitazone may increase the hypoglycemic activities of Insulin Aspart.Approved
Insulin DetemirRosiglitazone may increase the hypoglycemic activities of Insulin Detemir.Approved
Insulin GlargineRosiglitazone may increase the hypoglycemic activities of Insulin Glargine.Approved
Insulin GlulisineRosiglitazone may increase the hypoglycemic activities of Insulin Glulisine.Approved
Insulin HumanRosiglitazone may increase the hypoglycemic activities of Insulin Human.Approved, Investigational
Insulin LisproRosiglitazone may increase the hypoglycemic activities of Insulin Lispro.Approved
Insulin PorkThe risk or severity of adverse effects can be increased when Insulin Pork is combined with Rosiglitazone.Approved
IproclozideIproclozide may increase the hypoglycemic activities of Rosiglitazone.Withdrawn
IproniazidIproniazid may increase the hypoglycemic activities of Rosiglitazone.Withdrawn
IrbesartanThe metabolism of Rosiglitazone can be decreased when combined with Irbesartan.Approved, Investigational
IsocarboxazidIsocarboxazid may increase the hypoglycemic activities of Rosiglitazone.Approved
Isosorbide DinitrateThe risk or severity of adverse effects can be increased when Isosorbide Dinitrate is combined with Rosiglitazone.Approved
Isosorbide MononitrateThe risk or severity of adverse effects can be increased when Isosorbide Mononitrate is combined with Rosiglitazone.Approved
IxazomibThe metabolism of Ixazomib can be decreased when combined with Rosiglitazone.Approved
KetamineThe metabolism of Ketamine can be decreased when combined with Rosiglitazone.Approved, Vet Approved
KetanserinKetanserin may increase the anticoagulant activities of Rosiglitazone.Investigational
KetobemidoneThe metabolism of Ketobemidone can be decreased when combined with Rosiglitazone.Approved
KetoconazoleThe metabolism of Rosiglitazone can be decreased when combined with Ketoconazole.Approved, Investigational
LanreotideThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Lanreotide.Approved
LansoprazoleThe metabolism of Lansoprazole can be decreased when combined with Rosiglitazone.Approved, Investigational
LapatinibThe metabolism of Lapatinib can be decreased when combined with Rosiglitazone.Approved, Investigational
LeflunomideThe metabolism of Rosiglitazone can be decreased when combined with Leflunomide.Approved, Investigational
LepirudinRosiglitazone may increase the anticoagulant activities of Lepirudin.Approved
LeuprolideThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Leuprolide.Approved, Investigational
LevofloxacinLevofloxacin may increase the hypoglycemic activities of Rosiglitazone.Approved, Investigational
LevomilnacipranLevomilnacipran may increase the hypoglycemic activities of Rosiglitazone.Approved
LevonorgestrelThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Levonorgestrel.Approved, Investigational
LicofeloneThe metabolism of Licofelone can be decreased when combined with Rosiglitazone.Investigational
LidocaineThe metabolism of Lidocaine can be decreased when combined with Rosiglitazone.Approved, Vet Approved
LimaprostThe risk or severity of adverse effects can be increased when Limaprost is combined with Rosiglitazone.Approved
Lipoic AcidLipoic Acid may increase the hypoglycemic activities of Rosiglitazone.Approved, Nutraceutical
LomefloxacinLomefloxacin may increase the hypoglycemic activities of Rosiglitazone.Approved
LoperamideThe metabolism of Loperamide can be decreased when combined with Rosiglitazone.Approved
LopinavirThe metabolism of Rosiglitazone can be decreased when combined with Lopinavir.Approved
LoratadineThe metabolism of Loratadine can be decreased when combined with Rosiglitazone.Approved
LosartanThe metabolism of Rosiglitazone can be decreased when combined with Losartan.Approved
LovastatinThe metabolism of Rosiglitazone can be decreased when combined with Lovastatin.Approved, Investigational
LumacaftorThe serum concentration of Rosiglitazone can be increased when it is combined with Lumacaftor.Approved
LurasidoneThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Lurasidone.Approved
MebanazineMebanazine may increase the hypoglycemic activities of Rosiglitazone.Withdrawn
MecaserminRosiglitazone may increase the hypoglycemic activities of Mecasermin.Approved, Investigational
Medroxyprogesterone acetateThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Medroxyprogesterone acetate.Approved, Investigational
Mefenamic acidThe metabolism of Mefenamic acid can be decreased when combined with Rosiglitazone.Approved
Megestrol acetateThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Megestrol acetate.Approved, Vet Approved
MeloxicamThe metabolism of Meloxicam can be decreased when combined with Rosiglitazone.Approved, Vet Approved
MephenytoinThe metabolism of Mephenytoin can be decreased when combined with Rosiglitazone.Investigational, Withdrawn
MesalazineThe risk or severity of adverse effects can be increased when Mesalazine is combined with Rosiglitazone.Approved
MestranolThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Mestranol.Approved
MethadoneThe metabolism of Methadone can be decreased when combined with Rosiglitazone.Approved
MethotrimeprazineThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Methotrimeprazine.Approved
MethyclothiazideThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Methyclothiazide.Approved
Methylene blueMethylene blue may increase the hypoglycemic activities of Rosiglitazone.Investigational
MethylprednisoloneThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Methylprednisolone.Approved, Vet Approved
MethyltestosteroneMethyltestosterone may increase the hypoglycemic activities of Rosiglitazone.Approved
MetolazoneThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Metolazone.Approved
MetoprololThe serum concentration of Metoprolol can be increased when it is combined with Rosiglitazone.Approved, Investigational
MifepristoneThe serum concentration of Rosiglitazone can be increased when it is combined with Mifepristone.Approved, Investigational
MilnacipranMilnacipran may increase the hypoglycemic activities of Rosiglitazone.Approved
MilrinoneMilrinone may increase the anticoagulant activities of Rosiglitazone.Approved
MinaprineMinaprine may increase the hypoglycemic activities of Rosiglitazone.Approved
MirtazapineThe metabolism of Mirtazapine can be decreased when combined with Rosiglitazone.Approved
MoclobemideMoclobemide may increase the hypoglycemic activities of Rosiglitazone.Approved
MorphineThe metabolism of Morphine can be decreased when combined with Rosiglitazone.Approved, Investigational
MoxifloxacinMoxifloxacin may increase the hypoglycemic activities of Rosiglitazone.Approved, Investigational
muraglitazarThe metabolism of muraglitazar can be decreased when combined with Rosiglitazone.Investigational
Mycophenolate mofetilThe metabolism of Mycophenolate mofetil can be decreased when combined with Rosiglitazone.Approved, Investigational
NadroparinRosiglitazone may increase the anticoagulant activities of Nadroparin.Approved
NafamostatRosiglitazone may increase the anticoagulant activities of Nafamostat.Investigational
NaftopidilNaftopidil may increase the anticoagulant activities of Rosiglitazone.Investigational
Nalidixic AcidNalidixic Acid may increase the hypoglycemic activities of Rosiglitazone.Approved
NaloxoneThe metabolism of Naloxone can be decreased when combined with Rosiglitazone.Approved, Vet Approved
NaproxenThe metabolism of Naproxen can be decreased when combined with Rosiglitazone.Approved, Vet Approved
NateglinideRosiglitazone may increase the hypoglycemic activities of Nateglinide.Approved, Investigational
NCX 4016The risk or severity of adverse effects can be increased when NCX 4016 is combined with Rosiglitazone.Investigational
NefazodoneNefazodone may increase the hypoglycemic activities of Rosiglitazone.Approved, Withdrawn
NelfinavirThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Nelfinavir.Approved
NemonoxacinNemonoxacin may increase the hypoglycemic activities of Rosiglitazone.Investigational
NiacinThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Niacin.Approved, Investigational, Nutraceutical
NialamideNialamide may increase the hypoglycemic activities of Rosiglitazone.Withdrawn
NicardipineThe metabolism of Rosiglitazone can be decreased when combined with Nicardipine.Approved
NicotineThe metabolism of Nicotine can be decreased when combined with Rosiglitazone.Approved
NilotinibThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Nilotinib.Approved, Investigational
NimesulideNimesulide may increase the anticoagulant activities of Rosiglitazone.Approved, Withdrawn
NitroaspirinThe risk or severity of adverse effects can be increased when Nitroaspirin is combined with Rosiglitazone.Investigational
NitroglycerinThe risk or severity of adverse effects can be increased when Nitroglycerin is combined with Rosiglitazone.Approved, Investigational
NorethisteroneThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Norethisterone.Approved
NorfloxacinNorfloxacin may increase the hypoglycemic activities of Rosiglitazone.Approved
NorgestimateThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Norgestimate.Approved
OctamoxinOctamoxin may increase the hypoglycemic activities of Rosiglitazone.Withdrawn
OctreotideThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Octreotide.Approved, Investigational
OfloxacinOfloxacin may increase the hypoglycemic activities of Rosiglitazone.Approved
OlanzapineThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Olanzapine.Approved, Investigational
OlodaterolThe metabolism of Olodaterol can be decreased when combined with Rosiglitazone.Approved
OlsalazineThe risk or severity of adverse effects can be increased when Olsalazine is combined with Rosiglitazone.Approved
OmbitasvirThe metabolism of Ombitasvir can be decreased when combined with Rosiglitazone.Approved
OmeprazoleThe metabolism of Rosiglitazone can be decreased when combined with Omeprazole.Approved, Investigational, Vet Approved
OtamixabanRosiglitazone may increase the anticoagulant activities of Otamixaban.Investigational
OxandroloneOxandrolone may increase the hypoglycemic activities of Rosiglitazone.Approved, Investigational
OxymetholoneOxymetholone may increase the hypoglycemic activities of Rosiglitazone.Approved, Illicit
PaclitaxelThe metabolism of Paclitaxel can be decreased when combined with Rosiglitazone.Approved, Vet Approved
PaliperidoneThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Paliperidone.Approved
ParamethadioneThe metabolism of Paramethadione can be decreased when combined with Rosiglitazone.Approved
PargylinePargyline may increase the hypoglycemic activities of Rosiglitazone.Approved
ParoxetineParoxetine may increase the hypoglycemic activities of Rosiglitazone.Approved, Investigational
PasireotideThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Pasireotide.Approved
PazopanibThe metabolism of Pazopanib can be decreased when combined with Rosiglitazone.Approved
PazufloxacinPazufloxacin may increase the hypoglycemic activities of Rosiglitazone.Investigational
PefloxacinPefloxacin may increase the hypoglycemic activities of Rosiglitazone.Approved
PegvisomantPegvisomant may increase the hypoglycemic activities of Rosiglitazone.Approved
PentamidineThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Pentamidine.Approved
Pentosan PolysulfateRosiglitazone may increase the anticoagulant activities of Pentosan Polysulfate.Approved
PentoxifyllinePentoxifylline may increase the anticoagulant activities of Rosiglitazone.Approved, Investigational
PerphenazineThe metabolism of Perphenazine can be decreased when combined with Rosiglitazone.Approved
PhenelzinePhenelzine may increase the hypoglycemic activities of Rosiglitazone.Approved
PhenindioneRosiglitazone may increase the anticoagulant activities of Phenindione.Approved
PheniprazinePheniprazine may increase the hypoglycemic activities of Rosiglitazone.Withdrawn
PhenobarbitalThe metabolism of Rosiglitazone can be increased when combined with Phenobarbital.Approved
PhenoxypropazinePhenoxypropazine may increase the hypoglycemic activities of Rosiglitazone.Withdrawn
PhenprocoumonRosiglitazone may increase the anticoagulant activities of Phenprocoumon.Approved
PhenytoinThe metabolism of Rosiglitazone can be increased when combined with Phenytoin.Approved, Vet Approved
PioglitazoneThe metabolism of Pioglitazone can be decreased when combined with Rosiglitazone.Approved, Investigational
PiperazineThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Piperazine.Approved, Vet Approved
PipotiazineThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Pipotiazine.Approved
PirlindolePirlindole may increase the hypoglycemic activities of Rosiglitazone.Approved
PiroxicamThe metabolism of Piroxicam can be decreased when combined with Rosiglitazone.Approved, Investigational
PitavastatinThe metabolism of Pitavastatin can be decreased when combined with Rosiglitazone.Approved
PivhydrazinePivhydrazine may increase the hypoglycemic activities of Rosiglitazone.Withdrawn
PolythiazideThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Polythiazide.Approved
PonatinibThe metabolism of Ponatinib can be decreased when combined with Rosiglitazone.Approved
PrasugrelPrasugrel may increase the anticoagulant activities of Rosiglitazone.Approved
PrednisoloneThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Prednisolone.Approved, Vet Approved
PrednisoneThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Prednisone.Approved, Vet Approved
PregabalinPregabalin may increase the fluid retaining activities of Rosiglitazone.Approved, Illicit, Investigational
PrimidoneThe metabolism of Rosiglitazone can be increased when combined with Primidone.Approved, Vet Approved
ProgesteroneThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Progesterone.Approved, Vet Approved
PropofolThe metabolism of Propofol can be decreased when combined with Rosiglitazone.Approved, Investigational, Vet Approved
Protein CRosiglitazone may increase the anticoagulant activities of Protein C.Approved
Protein S humanRosiglitazone may increase the anticoagulant activities of Protein S human.Approved
ProtocatechualdehydeRosiglitazone may increase the anticoagulant activities of Protocatechualdehyde.Approved
PrulifloxacinPrulifloxacin may increase the hypoglycemic activities of Rosiglitazone.Investigational
PyrimethamineThe metabolism of Rosiglitazone can be decreased when combined with Pyrimethamine.Approved, Vet Approved
QuetiapineThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Quetiapine.Approved
QuinethazoneThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Quinethazone.Approved
QuinidineThe metabolism of Quinidine can be decreased when combined with Rosiglitazone.Approved
QuinineThe metabolism of Rosiglitazone can be decreased when combined with Quinine.Approved
RabeprazoleThe metabolism of Rosiglitazone can be decreased when combined with Rabeprazole.Approved, Investigational
RamatrobanRamatroban may increase the anticoagulant activities of Rosiglitazone.Investigational
RasagilineRasagiline may increase the hypoglycemic activities of Rosiglitazone.Approved
RepaglinideThe metabolism of Repaglinide can be decreased when combined with Rosiglitazone.Approved, Investigational
ResveratrolResveratrol may increase the anticoagulant activities of Rosiglitazone.Experimental, Investigational
ReviparinRosiglitazone may increase the anticoagulant activities of Reviparin.Approved
RidogrelRidogrel may increase the anticoagulant activities of Rosiglitazone.Approved
RifampicinThe metabolism of Rosiglitazone can be increased when combined with Rifampicin.Approved
RifapentineThe metabolism of Rosiglitazone can be increased when combined with Rifapentine.Approved
RiociguatThe metabolism of Riociguat can be decreased when combined with Rosiglitazone.Approved
RisperidoneThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Risperidone.Approved, Investigational
RitonavirThe metabolism of Rosiglitazone can be decreased when combined with Ritonavir.Approved, Investigational
RivaroxabanRosiglitazone may increase the anticoagulant activities of Rivaroxaban.Approved
RofecoxibThe metabolism of Rofecoxib can be decreased when combined with Rosiglitazone.Investigational, Withdrawn
RosoxacinRosoxacin may increase the hypoglycemic activities of Rosiglitazone.Approved
SafrazineSafrazine may increase the hypoglycemic activities of Rosiglitazone.Withdrawn
Salicylic acidThe risk or severity of adverse effects can be increased when Salicylic acid is combined with Rosiglitazone.Approved, Vet Approved
SaquinavirThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Saquinavir.Approved, Investigational
SCH-530348SCH-530348 may increase the anticoagulant activities of Rosiglitazone.Investigational
SecobarbitalThe metabolism of Rosiglitazone can be increased when combined with Secobarbital.Approved, Vet Approved
SelegilineSelegiline may increase the hypoglycemic activities of Rosiglitazone.Approved, Investigational, Vet Approved
SelexipagThe metabolism of Selexipag can be decreased when combined with Rosiglitazone.Approved
SeratrodastThe metabolism of Seratrodast can be decreased when combined with Rosiglitazone.Approved, Investigational
SertralineSertraline may increase the hypoglycemic activities of Rosiglitazone.Approved
SevofluraneSevoflurane may increase the anticoagulant activities of Rosiglitazone.Approved, Vet Approved
SildenafilThe metabolism of Rosiglitazone can be decreased when combined with Sildenafil.Approved, Investigational
SimvastatinThe metabolism of Simvastatin can be decreased when combined with Rosiglitazone.Approved
SirolimusThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Sirolimus.Approved, Investigational
SitagliptinThe metabolism of Sitagliptin can be decreased when combined with Rosiglitazone.Approved, Investigational
SorafenibThe metabolism of Rosiglitazone can be decreased when combined with Sorafenib.Approved, Investigational
SparfloxacinSparfloxacin may increase the hypoglycemic activities of Rosiglitazone.Approved
SRT501SRT501 may increase the anticoagulant activities of Rosiglitazone.Investigational
StanozololStanozolol may increase the hypoglycemic activities of Rosiglitazone.Approved, Vet Approved
StiripentolThe metabolism of Rosiglitazone can be decreased when combined with Stiripentol.Approved
SulfadiazineThe metabolism of Rosiglitazone can be decreased when combined with Sulfadiazine.Approved, Vet Approved
SulfamethoxazoleThe metabolism of Rosiglitazone can be decreased when combined with Sulfamethoxazole.Approved
SulfinpyrazoneThe metabolism of Sulfinpyrazone can be decreased when combined with Rosiglitazone.Approved
SulfisoxazoleThe metabolism of Rosiglitazone can be decreased when combined with Sulfisoxazole.Approved, Vet Approved
SulodexideRosiglitazone may increase the anticoagulant activities of Sulodexide.Approved, Investigational
SunitinibRosiglitazone may increase the hypoglycemic activities of Sunitinib.Approved, Investigational
TacrolimusThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Tacrolimus.Approved, Investigational
TamoxifenThe metabolism of Rosiglitazone can be decreased when combined with Tamoxifen.Approved
TazaroteneThe metabolism of Tazarotene can be decreased when combined with Rosiglitazone.Approved, Investigational
TemafloxacinTemafloxacin may increase the hypoglycemic activities of Rosiglitazone.Withdrawn
TemazepamThe metabolism of Temazepam can be decreased when combined with Rosiglitazone.Approved
TemsirolimusThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Temsirolimus.Approved
TerbinafineThe metabolism of Terbinafine can be decreased when combined with Rosiglitazone.Approved, Investigational, Vet Approved
TeriflunomideThe metabolism of Rosiglitazone can be decreased when combined with Teriflunomide.Approved
TesmilifeneTesmilifene may increase the anticoagulant activities of Rosiglitazone.Investigational
TestosteroneThe metabolism of Testosterone can be decreased when combined with Rosiglitazone.Approved, Investigational
TheophyllineThe metabolism of Theophylline can be decreased when combined with Rosiglitazone.Approved
ThioridazineThe serum concentration of Thioridazine can be increased when it is combined with Rosiglitazone.Approved
TicagrelorThe metabolism of Rosiglitazone can be decreased when combined with Ticagrelor.Approved
TiclopidineThe metabolism of Rosiglitazone can be decreased when combined with Ticlopidine.Approved
TipranavirThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Tipranavir.Approved, Investigational
TirofibanTirofiban may increase the anticoagulant activities of Rosiglitazone.Approved
TolazamideRosiglitazone may increase the hypoglycemic activities of Tolazamide.Approved
TolbutamideRosiglitazone may increase the hypoglycemic activities of Tolbutamide.Approved
ToloxatoneToloxatone may increase the hypoglycemic activities of Rosiglitazone.Approved
TorasemideThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Torasemide.Approved
TranilastTranilast may increase the anticoagulant activities of Rosiglitazone.Approved, Investigational
Trans-2-PhenylcyclopropylamineTrans-2-Phenylcyclopropylamine may increase the hypoglycemic activities of Rosiglitazone.Experimental
TranylcypromineTranylcypromine may increase the hypoglycemic activities of Rosiglitazone.Approved
TrapidilTrapidil may increase the anticoagulant activities of Rosiglitazone.Approved
TreprostinilThe risk or severity of adverse effects can be increased when Rosiglitazone is combined with Treprostinil.Approved, Investigational
TretinoinThe metabolism of Tretinoin can be decreased when combined with Rosiglitazone.Approved, Investigational, Nutraceutical
TriamcinoloneThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Triamcinolone.Approved, Vet Approved
TrichlormethiazideThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Trichlormethiazide.Approved, Vet Approved
TriflusalTriflusal may increase the anticoagulant activities of Rosiglitazone.Approved
TrimethadioneThe metabolism of Trimethadione can be decreased when combined with Rosiglitazone.Approved
TrimethoprimThe metabolism of Rosiglitazone can be decreased when combined with Trimethoprim.Approved, Vet Approved
TriptorelinThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Triptorelin.Approved, Vet Approved
TroglitazoneThe metabolism of Troglitazone can be decreased when combined with Rosiglitazone.Withdrawn
TrovafloxacinTrovafloxacin may increase the hypoglycemic activities of Rosiglitazone.Approved, Withdrawn
Valproic AcidThe metabolism of Rosiglitazone can be decreased when combined with Valproic Acid.Approved, Investigational
ValsartanThe metabolism of Rosiglitazone can be decreased when combined with Valsartan.Approved, Investigational
VenlafaxineVenlafaxine may increase the hypoglycemic activities of Rosiglitazone.Approved
VerapamilThe metabolism of Verapamil can be decreased when combined with Rosiglitazone.Approved
VorapaxarVorapaxar may increase the anticoagulant activities of Rosiglitazone.Approved
VoriconazoleThe metabolism of Rosiglitazone can be decreased when combined with Voriconazole.Approved, Investigational
VorinostatThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Vorinostat.Approved, Investigational
VortioxetineThe metabolism of Vortioxetine can be decreased when combined with Rosiglitazone.Approved
WarfarinRosiglitazone may increase the anticoagulant activities of Warfarin.Approved
XimelagatranRosiglitazone may increase the anticoagulant activities of Ximelagatran.Approved, Investigational, Withdrawn
Ym150Rosiglitazone may increase the anticoagulant activities of Ym150.Investigational
ZafirlukastThe metabolism of Rosiglitazone can be decreased when combined with Zafirlukast.Approved, Investigational
ZidovudineThe metabolism of Zidovudine can be decreased when combined with Rosiglitazone.Approved
ZimelidineZimelidine may increase the hypoglycemic activities of Rosiglitazone.Withdrawn
ZiprasidoneThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Ziprasidone.Approved
ZopicloneThe metabolism of Zopiclone can be decreased when combined with Rosiglitazone.Approved
Food InteractionsNot Available
References
Synthesis Reference

Manne Reddy, “Amorphous form of rosiglitazone maleate and process for preparation thereof.” U.S. Patent US20040242658, issued December 02, 2004.

US20040242658
General References
  1. Mohanty P, Aljada A, Ghanim H, Hofmeyer D, Tripathy D, Syed T, Al-Haddad W, Dhindsa S, Dandona P: Evidence for a potent antiinflammatory effect of rosiglitazone. J Clin Endocrinol Metab. 2004 Jun;89(6):2728-35. [PubMed:15181049 ]
  2. Kahn SE, Haffner SM, Heise MA, Herman WH, Holman RR, Jones NP, Kravitz BG, Lachin JM, O'Neill MC, Zinman B, Viberti G: Glycemic durability of rosiglitazone, metformin, or glyburide monotherapy. N Engl J Med. 2006 Dec 7;355(23):2427-43. Epub 2006 Dec 4. [PubMed:17145742 ]
External Links
ATC CodesA10BD03A10BG02A10BD04
AHFS Codes
  • 68:20.28
PDB EntriesNot Available
FDA labelDownload (86.2 KB)
MSDSDownload (30 KB)
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9861
Blood Brain Barrier+0.8994
Caco-2 permeable-0.5451
P-glycoprotein substrateSubstrate0.6535
P-glycoprotein inhibitor INon-inhibitor0.5274
P-glycoprotein inhibitor IINon-inhibitor0.6289
Renal organic cation transporterNon-inhibitor0.5203
CYP450 2C9 substrateNon-substrate0.7418
CYP450 2D6 substrateNon-substrate0.9116
CYP450 3A4 substrateSubstrate0.5744
CYP450 1A2 substrateInhibitor0.5391
CYP450 2C9 inhibitorInhibitor0.5783
CYP450 2D6 inhibitorNon-inhibitor0.846
CYP450 2C19 inhibitorInhibitor0.5884
CYP450 3A4 inhibitorNon-inhibitor0.8309
CYP450 inhibitory promiscuityHigh CYP Inhibitory Promiscuity0.7213
Ames testNon AMES toxic0.687
CarcinogenicityNon-carcinogens0.9465
BiodegradationNot ready biodegradable0.8635
Rat acute toxicity2.4515 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.8055
hERG inhibition (predictor II)Non-inhibitor0.7768
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
Manufacturers
  • Sb pharmco puerto rico inc
  • Glaxosmithkline
Packagers
Dosage forms
FormRouteStrength
TabletOral2.0 mg
TabletOral4.0 mg
TabletOral8.0 mg
TabletOral
Tablet, film coatedOral
TabletOral2 mg
TabletOral4 mg
TabletOral8 mg
Tablet, film coatedOral2 mg/1
Tablet, film coatedOral2 mg
Tablet, film coatedOral4 mg
Tablet, film coatedOral8 mg
Tablet, film coatedOral8 mg/1
Tablet, film coatedOral4 mg/1
Prices
Unit descriptionCostUnit
Avandia 8 mg tablet8.69USD tablet
Avandia 4 mg tablet4.72USD tablet
Avandia 2 mg tablet3.22USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
CA1328452 No1994-04-122011-04-12Canada
CA2143849 No2000-04-252013-09-01Canada
US5002953 No1994-09-172011-09-17Us
US5965584 No1996-06-192016-06-19Us
US6166042 No1996-06-192016-06-19Us
US6288095 Yes1997-08-112017-08-11Us
US7358366 Yes2000-10-192020-10-19Us
US8236345 No2002-10-072022-10-07Us
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point122-123 °CNot Available
logP2.4Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.038 mg/mLALOGPS
logP2.95ALOGPS
logP2.45ChemAxon
logS-4ALOGPS
pKa (Strongest Acidic)6.84ChemAxon
pKa (Strongest Basic)6.23ChemAxon
Physiological Charge-1ChemAxon
Hydrogen Acceptor Count5ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area71.53 Å2ChemAxon
Rotatable Bond Count7ChemAxon
Refractivity97.79 m3·mol-1ChemAxon
Polarizability37.8 Å3ChemAxon
Number of Rings3ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
Spectra
Spectrum TypeDescriptionSplash Key
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, NegativeNot Available
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as phenol ethers. These are aromatic compounds containing an ether group substituted with a benzene ring.
KingdomOrganic compounds
Super ClassBenzenoids
ClassBenzene and substituted derivatives
Sub ClassPhenol ethers
Direct ParentPhenol ethers
Alternative Parents
Substituents
  • Dialkylarylamine
  • Phenol ether
  • Thiazolidinedione
  • Aminopyridine
  • Alkyl aryl ether
  • Imidolactam
  • Pyridine
  • Heteroaromatic compound
  • Thiazolidine
  • Tertiary amine
  • Carboxamide group
  • Azacycle
  • Organoheterocyclic compound
  • Thioether
  • Ether
  • Carboxylic acid derivative
  • Hydrocarbon derivative
  • Organooxygen compound
  • Organonitrogen compound
  • Carbonyl group
  • Amine
  • Aromatic heteromonocyclic compound
Molecular FrameworkAromatic heteromonocyclic compounds
External DescriptorsNot Available

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
agonist
General Function:
Zinc ion binding
Specific Function:
Nuclear receptor that binds peroxisome proliferators such as hypolipidemic drugs and fatty acids. Once activated by a ligand, the nuclear receptor binds to DNA specific PPAR response elements (PPRE) and modulates the transcription of its target genes, such as acyl-CoA oxidase. It therefore controls the peroxisomal beta-oxidation pathway of fatty acids. Key regulator of adipocyte differentiation...
Gene Name:
PPARG
Uniprot ID:
P37231
Molecular Weight:
57619.58 Da
References
  1. Su JL, Winegar DA, Wisely GB, Sigel CS, Hull-Ryde EA: Use of a PPAR gamma-specific monoclonal antibody to demonstrate thiazolidinediones induce PPAR gamma receptor expression in vitro. Hybridoma. 1999 Jun;18(3):273-80. [PubMed:10475242 ]
  2. Rieusset J, Auwerx J, Vidal H: Regulation of gene expression by activation of the peroxisome proliferator-activated receptor gamma with rosiglitazone (BRL 49653) in human adipocytes. Biochem Biophys Res Commun. 1999 Nov;265(1):265-71. [PubMed:10548525 ]
  3. Kameda N, Okuya S, Oka Y: [Rosiglitazone (BRL-49653)]. Nihon Rinsho. 2000 Feb;58(2):401-4. [PubMed:10707565 ]
  4. Johnson BA, Wilson EM, Li Y, Moller DE, Smith RG, Zhou G: Ligand-induced stabilization of PPARgamma monitored by NMR spectroscopy: implications for nuclear receptor activation. J Mol Biol. 2000 Apr 28;298(2):187-94. [PubMed:10764590 ]
  5. Camp HS, Li O, Wise SC, Hong YH, Frankowski CL, Shen X, Vanbogelen R, Leff T: Differential activation of peroxisome proliferator-activated receptor-gamma by troglitazone and rosiglitazone. Diabetes. 2000 Apr;49(4):539-47. [PubMed:10871190 ]
  6. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Very long-chain fatty acid-coa ligase activity
Specific Function:
Activation of long-chain fatty acids for both synthesis of cellular lipids, and degradation via beta-oxidation. Preferentially uses arachidonate and eicosapentaenoate as substrates.
Gene Name:
ACSL4
Uniprot ID:
O60488
Molecular Weight:
79187.38 Da
References
  1. Askari B, Kanter JE, Sherrid AM, Golej DL, Bender AT, Liu J, Hsueh WA, Beavo JA, Coleman RA, Bornfeldt KE: Rosiglitazone inhibits acyl-CoA synthetase activity and fatty acid partitioning to diacylglycerol and triacylglycerol via a peroxisome proliferator-activated receptor-gamma-independent mechanism in human arterial smooth muscle cells and macrophages. Diabetes. 2007 Apr;56(4):1143-52. Epub 2007 Jan 26. [PubMed:17259370 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitor
General Function:
Steroid hydroxylase activity
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. In the epoxidation of arachidonic acid it generates only 14,15- and 11,12-cis-epoxyeicosatrienoic acids. It is the principal enzyme...
Gene Name:
CYP2C8
Uniprot ID:
P10632
Molecular Weight:
55824.275 Da
References
  1. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [PubMed:19515014 ]
  2. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitor
General Function:
Steroid hydroxylase activity
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. This enzyme contributes to the wide pharmacokinetics variability of the metabolism of drugs such as S-warfarin, diclofenac, phenyto...
Gene Name:
CYP2C9
Uniprot ID:
P11712
Molecular Weight:
55627.365 Da
References
  1. 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
substrate
General Function:
Prostaglandin-endoperoxide synthase activity
Specific Function:
Converts arachidonate to prostaglandin H2 (PGH2), a committed step in prostanoid synthesis. Involved in the constitutive production of prostanoids in particular in the stomach and platelets. In gastric epithelial cells, it is a key step in the generation of prostaglandins, such as prostaglandin E2 (PGE2), which plays an important role in cytoprotection. In platelets, it is involved in the gener...
Gene Name:
PTGS1
Uniprot ID:
P23219
Molecular Weight:
68685.82 Da
References
  1. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [PubMed:19515014 ]
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 unrelated compounds, including steroids, fatty acids, and xenobiotics. Most active in catalyzing 2-hydroxylation. Caffeine is metabolized primarily by cytochrome CYP1A2 in the liver through an initial N...
Gene Name:
CYP1A2
Uniprot ID:
P05177
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
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. Constitutes the major nicotine C-oxidase. Acts as a 1,4-cineole 2-exo-monooxygenase. Possesses low phenacetin O-deethylation activity.
Gene Name:
CYP2A6
Uniprot ID:
P11509
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:
Responsible for the metabolism of a number of therapeutic agents such as the anticonvulsant drug S-mephenytoin, omeprazole, proguanil, certain barbiturates, diazepam, propranolol, citalopram and imipramine.
Gene Name:
CYP2C19
Uniprot ID:
P33261
Molecular Weight:
55930.545 Da
References
  1. 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 antidepressants.
Gene Name:
CYP2D6
Uniprot ID:
P10635
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 ]

Carriers

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Toxic substance binding
Specific Function:
Serum albumin, the main protein of plasma, has a good binding capacity for water, Ca(2+), Na(+), K(+), fatty acids, hormones, bilirubin and drugs. Its main function is the regulation of the colloidal osmotic pressure of blood. Major zinc transporter in plasma, typically binds about 80% of all plasma zinc.
Gene Name:
ALB
Uniprot ID:
P02768
Molecular Weight:
69365.94 Da

Transporters

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Sodium-independent organic anion transmembrane transporter activity
Specific Function:
Mediates the Na(+)-independent uptake of organic anions such as pravastatin, taurocholate, methotrexate, dehydroepiandrosterone sulfate, 17-beta-glucuronosyl estradiol, estrone sulfate, prostaglandin E2, thromboxane B2, leukotriene C3, leukotriene E4, thyroxine and triiodothyronine. Involved in the clearance of bile acids and organic anions from the liver.
Gene Name:
SLCO1B1
Uniprot ID:
Q9Y6L6
Molecular Weight:
76447.99 Da
References
  1. Nozawa T, Sugiura S, Nakajima M, Goto A, Yokoi T, Nezu J, Tsuji A, Tamai I: Involvement of organic anion transporting polypeptides in the transport of troglitazone sulfate: implications for understanding troglitazone hepatotoxicity. Drug Metab Dispos. 2004 Mar;32(3):291-4. [PubMed:14977862 ]
Comments
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Drug created on June 13, 2005 07:24 / Updated on December 09, 2016 03:54