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Identification
NameRepaglinide
Accession NumberDB00912  (APRD00439)
TypeSmall Molecule
GroupsApproved, Investigational
DescriptionRepaglinide is an oral antihyperglycemic agent used for the treatment of non-insulin-dependent diabetes mellitus (NIDDM). It belongs to the meglitinide class of short-acting insulin secretagogues, which act by binding to β cells of the pancreas to stimulate insulin release. Repaglinide induces an early insulin response to meals decreasing postprandial blood glucose levels. It should only be taken with meals and meal-time doses should be skipped with any skipped meal. Approximately one month of therapy is required before a decrease in fasting blood glucose is seen. Meglitnides may have a neutral effect on weight or cause a slight increase in weight. The average weight gain caused by meglitinides appears to be lower than that caused by sulfonylureas and insulin and appears to occur only in those naïve to oral antidiabetic agents. Due to their mechanism of action, meglitinides may cause hypoglycemia although the risk is thought to be lower than that of sulfonylureas since their action is dependent on the presence of glucose. In addition to reducing postprandial and fasting blood glucose, meglitnides have been shown to decrease glycosylated hemoglobin (HbA1c) levels, which are reflective of the last 8-10 weeks of glucose control. Meglitinides appear to be more effective at lowering postprandial blood glucose than metformin, sulfonylureas and thiazolidinediones. Repaglinide is extensively metabolized in the liver and excreted in bile. Repaglinide metabolites do not possess appreciable hypoglycemic activity. Approximately 90% of a single orally administered dose is eliminated in feces and 8% in urine.
Structure
Thumb
Synonyms
AG-EE 388 ZW
AG-EE 623 ZW
Prandin
Repaglinida
Repaglinidum
Surepost
External Identifiers Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Act RepaglinideTablet0.5 mgOralActavis Pharma Company2010-10-18Not applicableCanada
Act RepaglinideTablet1 mgOralActavis Pharma Company2010-10-18Not applicableCanada
Act RepaglinideTablet2 mgOralActavis Pharma Company2010-10-18Not applicableCanada
Auro-repaglinideTablet0.5 mgOralAuro Pharma Inc2014-04-30Not applicableCanada
Auro-repaglinideTablet1 mgOralAuro Pharma Inc2014-04-30Not applicableCanada
Auro-repaglinideTablet2 mgOralAuro Pharma Inc2014-04-30Not applicableCanada
Gluconorm 0.5mgTablet0.5 mgOralNovo Nordisk Canada Inc1999-06-21Not applicableCanada
Gluconorm 1.0mgTablet1.0 mgOralNovo Nordisk Canada Inc1999-06-21Not applicableCanada
Gluconorm 2.0mgTablet2.0 mgOralNovo Nordisk Canada Inc1999-06-21Not applicableCanada
Mylan-repaglinideTablet2 mgOralMylan Pharmaceuticals UlcNot applicableNot applicableCanada
Mylan-repaglinideTablet0.5 mgOralMylan Pharmaceuticals UlcNot applicableNot applicableCanada
Mylan-repaglinideTablet1 mgOralMylan Pharmaceuticals UlcNot applicableNot applicableCanada
NovonormTablet2 mgOralNovo Nordisk A/s1998-08-17Not applicableEu
NovonormTablet1 mgOralNovo Nordisk A/s1998-08-17Not applicableEu
NovonormTablet0.5 mgOralNovo Nordisk A/s1998-08-17Not applicableEu
NovonormTablet2 mgOralNovo Nordisk A/s1998-08-17Not applicableEu
NovonormTablet2 mgOralNovo Nordisk A/s1998-08-17Not applicableEu
NovonormTablet1 mgOralNovo Nordisk A/s1998-08-17Not applicableEu
NovonormTablet0.5 mgOralNovo Nordisk A/s1998-08-17Not applicableEu
NovonormTablet2 mgOralNovo Nordisk A/s1998-08-17Not applicableEu
NovonormTablet0.5 mgOralNovo Nordisk A/s1998-08-17Not applicableEu
NovonormTablet1 mgOralNovo Nordisk A/s1998-08-17Not applicableEu
NovonormTablet0.5 mgOralNovo Nordisk A/s1998-08-17Not applicableEu
NovonormTablet2 mgOralNovo Nordisk A/s1998-08-17Not applicableEu
NovonormTablet1 mgOralNovo Nordisk A/s1998-08-17Not applicableEu
NovonormTablet1 mgOralNovo Nordisk A/s1998-08-17Not applicableEu
NovonormTablet0.5 mgOralNovo Nordisk A/s1998-08-17Not applicableEu
PMS-repaglinideTablet1.0 mgOralPharmascience Inc2010-10-20Not applicableCanada
PMS-repaglinideTablet2.0 mgOralPharmascience Inc2010-10-20Not applicableCanada
PMS-repaglinideTablet0.5 mgOralPharmascience Inc2010-10-20Not applicableCanada
PrandinTablet1 mg/1OralCardinal Health2000-01-03Not applicableUs
PrandinTablet2 mgOralNovo Nordisk A/s2001-01-29Not applicableEu
PrandinTablet.5 mg/1OralNovo Nordisk2000-01-03Not applicableUs
PrandinTablet1 mgOralNovo Nordisk A/s2001-01-29Not applicableEu
PrandinTablet0.5 mgOralNovo Nordisk A/s2001-01-29Not applicableEu
PrandinTablet.5 mg/1OralCarilion Materials Management2000-01-03Not applicableUs
PrandinTablet2 mg/1OralREMEDYREPACK INC.2011-10-042016-11-29Us
PrandinTablet2 mgOralNovo Nordisk A/s2001-01-29Not applicableEu
PrandinTablet2 mgOralNovo Nordisk A/s2001-01-29Not applicableEu
PrandinTablet1 mg/1OralNovo Nordisk2000-01-03Not applicableUs
PrandinTablet1 mgOralNovo Nordisk A/s2001-01-29Not applicableEu
PrandinTablet0.5 mgOralNovo Nordisk A/s2001-01-29Not applicableEu
PrandinTablet1 mg/1OralCarilion Materials Management2000-01-03Not applicableUs
PrandinTablet2 mg/1OralPhysicians Total Care, Inc.2000-01-03Not applicableUs
PrandinTablet2 mgOralNovo Nordisk A/s2001-01-29Not applicableEu
PrandinTablet1 mgOralNovo Nordisk A/s2001-01-29Not applicableEu
PrandinTablet2 mg/1OralNovo Nordisk2000-01-03Not applicableUs
PrandinTablet1 mgOralNovo Nordisk A/s2001-01-29Not applicableEu
PrandinTablet0.5 mgOralNovo Nordisk A/s2001-01-29Not applicableEu
PrandinTablet1 mg/1OralPhysicians Total Care, Inc.2000-01-03Not applicableUs
PrandinTablet2 mgOralNovo Nordisk A/s2001-01-29Not applicableEu
PrandinTablet0.5 mgOralNovo Nordisk A/s2001-01-29Not applicableEu
PrandinTablet.5 mg/1OralLake Erie Medical DBA Quality Care Products LLC2010-10-12Not applicableUs
PrandinTablet1 mgOralNovo Nordisk A/s2001-01-29Not applicableEu
PrandinTablet0.5 mgOralNovo Nordisk A/s2001-01-29Not applicableEu
RepaglinideTablet2.0 mgOralPro Doc Limitee2013-11-28Not applicableCanada
RepaglinideTablet0.5 mgOralPro Doc Limitee2013-11-28Not applicableCanada
RepaglinideTablet1.0 mgOralPro Doc Limitee2013-11-28Not applicableCanada
Sandoz RepaglinideTablet2 mgOralSandoz Canada Incorporated2011-02-17Not applicableCanada
Sandoz RepaglinideTablet0.5 mgOralSandoz Canada Incorporated2011-02-17Not applicableCanada
Sandoz RepaglinideTablet1 mgOralSandoz Canada Incorporated2011-02-17Not applicableCanada
Approved Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Apo-repaglinideTablet0.5 mgOralApotex Inc2012-10-16Not applicableCanada
Apo-repaglinideTablet1.0 mgOralApotex Inc2012-10-16Not applicableCanada
Apo-repaglinideTablet2.0 mgOralApotex Inc2012-10-16Not applicableCanada
EnyglidTablet0.5 mgOralKrka, D.D., Novo Mesto2009-10-14Not applicableEu
EnyglidTablet1 mgOralKrka, D.D., Novo Mesto2009-10-14Not applicableEu
EnyglidTablet2 mgOralKrka, D.D., Novo Mesto2009-10-14Not applicableEu
EnyglidTablet1 mgOralKrka, D.D., Novo Mesto2009-10-14Not applicableEu
EnyglidTablet0.5 mgOralKrka, D.D., Novo Mesto2009-10-14Not applicableEu
EnyglidTablet2 mgOralKrka, D.D., Novo Mesto2009-10-14Not applicableEu
EnyglidTablet0.5 mgOralKrka, D.D., Novo Mesto2009-10-14Not applicableEu
EnyglidTablet2 mgOralKrka, D.D., Novo Mesto2009-10-14Not applicableEu
EnyglidTablet2 mgOralKrka, D.D., Novo Mesto2009-10-14Not applicableEu
EnyglidTablet1 mgOralKrka, D.D., Novo Mesto2009-10-14Not applicableEu
EnyglidTablet0.5 mgOralKrka, D.D., Novo Mesto2009-10-14Not applicableEu
EnyglidTablet2 mgOralKrka, D.D., Novo Mesto2009-10-14Not applicableEu
EnyglidTablet1 mgOralKrka, D.D., Novo Mesto2009-10-14Not applicableEu
EnyglidTablet2 mgOralKrka, D.D., Novo Mesto2009-10-14Not applicableEu
EnyglidTablet1 mgOralKrka, D.D., Novo Mesto2009-10-14Not applicableEu
EnyglidTablet0.5 mgOralKrka, D.D., Novo Mesto2009-10-14Not applicableEu
EnyglidTablet0.5 mgOralKrka, D.D., Novo Mesto2009-10-14Not applicableEu
EnyglidTablet1 mgOralKrka, D.D., Novo Mesto2009-10-14Not applicableEu
EnyglidTablet0.5 mgOralKrka, D.D., Novo Mesto2009-10-14Not applicableEu
EnyglidTablet2 mgOralKrka, D.D., Novo Mesto2009-10-14Not applicableEu
EnyglidTablet1 mgOralKrka, D.D., Novo Mesto2009-10-14Not applicableEu
RepaglinideTablet.5 mg/1OralAurobindo Pharma Limited2014-01-22Not applicableUs
RepaglinideTablet1 mg/1OralSandoz Inc2014-01-22Not applicableUs
RepaglinideTablet1 mg/1OralBreckenridge Pharmaceutical, Inc.2015-05-01Not applicableUs
RepaglinideTablet.5 mg/1OralMylan Pharmaceuticals Inc.2013-08-27Not applicableUs
RepaglinideTablet.5 mg/1OralGolden State Medical Supply, Inc.2015-12-07Not applicableUs
RepaglinideTablet.5 mg/1OralMylan Institutional Inc.2013-11-21Not applicableUs
RepaglinideTablet2 mg/1OralAmerican Health Packaging2015-03-30Not applicableUs
RepaglinideTablet1 mg/1OralPaddock Laboratories, LLC2014-01-22Not applicableUs
RepaglinideTablet2 mg/1OralCitron Pharma LLC2014-01-22Not applicableUs
RepaglinideTablet1 mg/1OralAurobindo Pharma Limited2014-01-22Not applicableUs
RepaglinideTablet2 mg/1OralSandoz Inc2014-01-22Not applicableUs
RepaglinideTablet2 mg/1OralBreckenridge Pharmaceutical, Inc.2015-05-01Not applicableUs
RepaglinideTablet1 mg/1OralMylan Pharmaceuticals Inc.2014-01-22Not applicableUs
RepaglinideTablet1 mg/1OralGolden State Medical Supply, Inc.2015-12-17Not applicableUs
RepaglinideTablet1 mg/1OralMylan Institutional Inc.2014-02-27Not applicableUs
RepaglinideTablet2 mg/1OralPaddock Laboratories, LLC2014-01-22Not applicableUs
RepaglinideTablet1 mg/1OralSun Pharmaceutical Industries, Inc.2013-07-11Not applicableUs
RepaglinideTablet2 mg/1OralAurobindo Pharma Limited2014-01-22Not applicableUs
RepaglinideTablet1 mg/1OralAv Kare, Inc.2013-12-12Not applicableUs
RepaglinideTablet.5 mg/1OralCitron Pharma LLC2014-01-22Not applicableUs
RepaglinideTablet2 mg/1OralMylan Pharmaceuticals Inc.2014-01-22Not applicableUs
RepaglinideTablet2 mg/1OralGolden State Medical Supply, Inc.2015-12-17Not applicableUs
RepaglinideTablet2 mg/1OralMylan Institutional Inc.2014-02-24Not applicableUs
RepaglinideTablet2 mg/1OralSun Pharmaceutical Industries, Inc.2013-07-11Not applicableUs
RepaglinideTablet.5 mg/1OralSandoz Inc2013-12-27Not applicableUs
RepaglinideTablet1 mg/1OralAmerican Health Packaging2015-03-30Not applicableUs
RepaglinideTablet2 mg/1OralAv Kare, Inc.2013-12-12Not applicableUs
RepaglinideTablet.5 mg/1OralPaddock Laboratories, LLC2013-08-09Not applicableUs
RepaglinideTablet1 mg/1OralCitron Pharma LLC2014-01-22Not applicableUs
RepaglinideTablet.5 mg/1OralBreckenridge Pharmaceutical, Inc.2015-05-01Not applicableUs
Repaglinide AccordTablet2 mgOralAccord Healthcare Ltd2011-12-22Not applicableEu
Repaglinide AccordTablet1 mgOralAccord Healthcare Ltd2011-12-22Not applicableEu
Repaglinide AccordTablet0.5 mgOralAccord Healthcare Ltd2011-12-22Not applicableEu
Repaglinide AccordTablet2 mgOralAccord Healthcare Ltd2011-12-22Not applicableEu
Repaglinide AccordTablet2 mgOralAccord Healthcare Ltd2011-12-22Not applicableEu
Repaglinide AccordTablet2 mgOralAccord Healthcare Ltd2011-12-22Not applicableEu
Repaglinide AccordTablet1 mgOralAccord Healthcare Ltd2011-12-22Not applicableEu
Repaglinide AccordTablet0.5 mgOralAccord Healthcare Ltd2011-12-22Not applicableEu
Repaglinide AccordTablet2 mgOralAccord Healthcare Ltd2011-12-22Not applicableEu
Repaglinide AccordTablet0.5 mgOralAccord Healthcare Ltd2011-12-22Not applicableEu
Repaglinide AccordTablet0.5 mgOralAccord Healthcare Ltd2011-12-22Not applicableEu
Repaglinide AccordTablet1 mgOralAccord Healthcare Ltd2011-12-22Not applicableEu
Repaglinide AccordTablet0.5 mgOralAccord Healthcare Ltd2011-12-22Not applicableEu
Repaglinide AccordTablet2 mgOralAccord Healthcare Ltd2011-12-22Not applicableEu
Repaglinide AccordTablet0.5 mgOralAccord Healthcare Ltd2011-12-22Not applicableEu
Repaglinide AccordTablet1 mgOralAccord Healthcare Ltd2011-12-22Not applicableEu
Repaglinide AccordTablet1 mgOralAccord Healthcare Ltd2011-12-22Not applicableEu
Repaglinide AccordTablet1 mgOralAccord Healthcare Ltd2011-12-22Not applicableEu
Repaglinide KrkaTablet1 mgOralKrka, D.D., Novo Mesto2009-11-04Not applicableEu
Repaglinide KrkaTablet5 mgOralKrka, D.D., Novo Mesto2009-11-04Not applicableEu
Repaglinide KrkaTablet2 mgOralKrka, D.D., Novo Mesto2009-11-04Not applicableEu
Repaglinide KrkaTablet1 mgOralKrka, D.D., Novo Mesto2009-11-04Not applicableEu
Repaglinide KrkaTablet1 mgOralKrka, D.D., Novo Mesto2009-11-04Not applicableEu
Repaglinide KrkaTablet5 mgOralKrka, D.D., Novo Mesto2009-11-04Not applicableEu
Repaglinide KrkaTablet5 mgOralKrka, D.D., Novo Mesto2009-11-04Not applicableEu
Repaglinide KrkaTablet2 mgOralKrka, D.D., Novo Mesto2009-11-04Not applicableEu
Repaglinide KrkaTablet1 mgOralKrka, D.D., Novo Mesto2009-11-04Not applicableEu
Repaglinide KrkaTablet2 mgOralKrka, D.D., Novo Mesto2009-11-04Not applicableEu
Repaglinide KrkaTablet5 mgOralKrka, D.D., Novo Mesto2009-11-04Not applicableEu
Repaglinide KrkaTablet5 mgOralKrka, D.D., Novo Mesto2009-11-04Not applicableEu
Repaglinide KrkaTablet2 mgOralKrka, D.D., Novo Mesto2009-11-04Not applicableEu
Repaglinide KrkaTablet1 mgOralKrka, D.D., Novo Mesto2009-11-04Not applicableEu
Repaglinide KrkaTablet2 mgOralKrka, D.D., Novo Mesto2009-11-04Not applicableEu
Repaglinide KrkaTablet1 mgOralKrka, D.D., Novo Mesto2009-11-04Not applicableEu
Repaglinide KrkaTablet5 mgOralKrka, D.D., Novo Mesto2009-11-04Not applicableEu
Repaglinide KrkaTablet2 mgOralKrka, D.D., Novo Mesto2009-11-04Not applicableEu
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
GlucoNormNovo Nordisk
Brand mixtures
NameLabellerIngredients
PrandimetNovo Nordisk
Repaglinide and Metformin HydrochlorideLupin Pharmaceuticals, Inc.
SaltsNot Available
Categories
UNII668Z8C33LU
CAS number135062-02-1
WeightAverage: 452.5857
Monoisotopic: 452.26750765
Chemical FormulaC27H36N2O4
InChI KeyFAEKWTJYAYMJKF-QHCPKHFHSA-N
InChI
InChI=1S/C27H36N2O4/c1-4-33-25-17-20(12-13-22(25)27(31)32)18-26(30)28-23(16-19(2)3)21-10-6-7-11-24(21)29-14-8-5-9-15-29/h6-7,10-13,17,19,23H,4-5,8-9,14-16,18H2,1-3H3,(H,28,30)(H,31,32)/t23-/m0/s1
IUPAC Name
2-ethoxy-4-({[(1S)-3-methyl-1-[2-(piperidin-1-yl)phenyl]butyl]carbamoyl}methyl)benzoic acid
SMILES
CCOC1=C(C=CC(CC(=O)N[C@@H](CC(C)C)C2=CC=CC=C2N2CCCCC2)=C1)C(O)=O
Pharmacology
IndicationAs an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus.
Structured Indications
PharmacodynamicsInsulin secretion by pancreatic β cells is partly controlled by cellular membrane potential. Membrane potential is regulated through an inverse relationship between the activity of cell membrane ATP-sensitive potassium channels (ABCC8) and extracellular glucose concentrations. Extracellular glucose enters the cell via GLUT2 (SLC2A2) transporters. Once inside the cell, glucose is metabolized to produce ATP. High concentrations of ATP inhibit ATP-sensitive potassium channels causing membrane depolarization. When extracellular glucose concentrations are low, ATP-sensitive potassium channels open causing membrane repolarization. High glucose concentrations cause ATP-sensitive potassium channels to close resulting in membrane depolarization and opening of L-type calcium channels. The influx of calcium ions stimulates calcium-dependent exocytosis of insulin granules. Repaglinide increases insulin release by inhibiting ATP-sensitive potassium channels in a glucose-dependent manner.
Mechanism of actionRepaglinide activity is dependent on the presence functioning β cells and glucose. In contrast to sulfonylurea insulin secretatogogues, repaglinide has no effect on insulin release in the absence of glucose. Rather, it potentiates the effect of extracellular glucose on ATP-sensitive potassium channel and has little effect on insulin levels between meals and overnight. As such, repaglinide is more effective at reducing postprandial blood glucose levels than fasting blood glucose levels and requires a longer duration of therapy (approximately one month) before decreases in fasting blood glucose are observed. The insulinotropic effects of repaglinide are highest at intermediate glucose levels (3 to 10 mmol/L) and it does not increase insulin release already stimulated by high glucose concentrations (greater than 15 mmol/L). Repaglinide appears to be selective for pancreatic β cells and does not appear to affect skeletal or cardiac muscle or thyroid tissue.
TargetKindPharmacological actionActionsOrganismUniProt ID
ATP-binding cassette sub-family C member 8Proteinyes
inhibitor
HumanQ09428 details
Peroxisome proliferator-activated receptor gammaProteinunknown
agonist
HumanP37231 details
Related Articles
AbsorptionRapidly and completely absorbed following oral administration. Peak plasma concentrations are observed within 1 hour (range 0.5-1.4 hours). The absolute bioavailability is approximately 56%. Maximal biological effect is observed within 3-3.5 hours and plasma insulin levels remain elevated for 4-6 hours. When a single 2 mg dose of repaglinide is given to healthy subjects, the area under the curve (AUC) is 18.0 - 18.7 (ng/mL/h)^3.
Volume of distribution

31 L following IV administration in healthy individuals

Protein binding>98% (e.g. to to albumin and α1-acid glycoprotein)
Metabolism

Repaglinide is rapidly metabolized via oxidation and dealkylation by cytochrome P450 3A4 and 2C9 to form the major dicarboxylic acid derivative (M2). Further oxidation produces the aromatic amine derivative (M1). Glucuronidation of the carboxylic acid group of repaglinide yields an acyl glucuronide (M7). Several other unidentified metabolites have been detected. Repaglinide metabolites to not possess appreciable hypoglycemic activity.

SubstrateEnzymesProduct
Repaglinide
hydroxyrepaglinideDetails
Repaglinide
repaglinide aromatic amineDetails
Route of elimination90% eliminated in feces (<2% as unchanged drug), 8% in urine (0.1% as unchanged drug)
Half life1 hour
Clearance

33-38 L/hour following IV administration

ToxicityLD50 >1 g/kg (rat) (W. Grell)
Affected organisms
  • Humans and other mammals
Pathways
PathwayCategorySMPDB ID
Repaglinide Action PathwayDrug actionSMP00454
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 Repaglinide.Experimental
AbirateroneThe serum concentration of Repaglinide can be increased when it is combined with Abiraterone.Approved
AcarboseAcarbose may increase the hypoglycemic activities of Repaglinide.Approved, Investigational
AcetohexamideAcetohexamide may increase the hypoglycemic activities of Repaglinide.Withdrawn
Acetylsalicylic acidAcetylsalicylic acid may increase the hypoglycemic activities of Repaglinide.Approved, Vet Approved
AicarAicar may increase the hypoglycemic activities of Repaglinide.Experimental
AlogliptinAlogliptin may increase the hypoglycemic activities of Repaglinide.Approved
Aminosalicylic AcidAminosalicylic Acid may increase the hypoglycemic activities of Repaglinide.Approved
AmiodaroneThe serum concentration of Repaglinide can be increased when it is combined with Amiodarone.Approved, Investigational
AprepitantThe serum concentration of Repaglinide can be increased when it is combined with Aprepitant.Approved, Investigational
AripiprazoleThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Aripiprazole.Approved, Investigational
Arsenic trioxideThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Arsenic trioxide.Approved, Investigational
ArticaineThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Articaine.Approved
AsenapineThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Asenapine.Approved
AtazanavirThe serum concentration of Repaglinide can be increased when it is combined with Atazanavir.Approved, Investigational
AtomoxetineThe metabolism of Repaglinide can be decreased when combined with Atomoxetine.Approved
BalaglitazoneBalaglitazone may increase the hypoglycemic activities of Repaglinide.Investigational
BalsalazideBalsalazide may increase the hypoglycemic activities of Repaglinide.Approved, Investigational
BendroflumethiazideThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Bendroflumethiazide.Approved
BenmoxinBenmoxin may increase the hypoglycemic activities of Repaglinide.Withdrawn
BetamethasoneThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Betamethasone.Approved, Vet Approved
BexaroteneThe serum concentration of Repaglinide can be decreased when it is combined with Bexarotene.Approved, Investigational
BoceprevirThe serum concentration of Repaglinide can be increased when it is combined with Boceprevir.Approved
BortezomibThe metabolism of Repaglinide can be decreased when combined with Bortezomib.Approved, Investigational
BosentanThe serum concentration of Repaglinide can be decreased when it is combined with Bosentan.Approved, Investigational
BrexpiprazoleThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Brexpiprazole.Approved
BuforminBuformin may increase the hypoglycemic activities of Repaglinide.Withdrawn
BumetanideThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Bumetanide.Approved
BuserelinThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Buserelin.Approved
CanagliflozinCanagliflozin may increase the hypoglycemic activities of Repaglinide.Approved
CarbamazepineThe metabolism of Repaglinide can be increased when combined with Carbamazepine.Approved, Investigational
CarbomycinThe serum concentration of Repaglinide can be increased when it is combined with Carbomycin.Vet Approved
CaroxazoneCaroxazone may increase the hypoglycemic activities of Repaglinide.Withdrawn
CastanospermineCastanospermine may increase the hypoglycemic activities of Repaglinide.Experimental
CelecoxibThe metabolism of Repaglinide can be decreased when combined with Celecoxib.Approved, Investigational
CeritinibThe serum concentration of Repaglinide can be increased when it is combined with Ceritinib.Approved
ChlorothiazideThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Chlorothiazide.Approved, Vet Approved
ChlorpropamideChlorpropamide may increase the hypoglycemic activities of Repaglinide.Approved
ChlorthalidoneThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Chlorthalidone.Approved
CiglitazoneCiglitazone may increase the hypoglycemic activities of Repaglinide.Experimental
CinoxacinCinoxacin may increase the hypoglycemic activities of Repaglinide.Approved, Withdrawn
CiprofloxacinCiprofloxacin may increase the hypoglycemic activities of Repaglinide.Approved, Investigational
CitalopramCitalopram may increase the hypoglycemic activities of Repaglinide.Approved
ClarithromycinThe serum concentration of Repaglinide can be increased when it is combined with Clarithromycin.Approved
ClemastineThe metabolism of Repaglinide can be decreased when combined with Clemastine.Approved
ClopidogrelThe serum concentration of Repaglinide can be increased when it is combined with Clopidogrel.Approved, Nutraceutical
ClotrimazoleThe metabolism of Repaglinide can be decreased when combined with Clotrimazole.Approved, Vet Approved
ClozapineThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Clozapine.Approved
CobicistatThe serum concentration of Repaglinide can be increased when it is combined with Cobicistat.Approved
ConivaptanThe serum concentration of Repaglinide can be increased when it is combined with Conivaptan.Approved, Investigational
CorticotropinThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Corticotropin.Approved, Vet Approved
Cortisone acetateThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Cortisone acetate.Approved
CrizotinibThe metabolism of Repaglinide can be decreased when combined with Crizotinib.Approved
CyclosporineThe serum concentration of Repaglinide can be increased when it is combined with Cyclosporine.Approved, Investigational, Vet Approved
CyclosporineThe metabolism of Repaglinide can be decreased when combined with Cyclosporine.Approved, Investigational, Vet Approved
Cyproterone acetateThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Cyproterone acetate.Approved, Investigational
DabrafenibThe serum concentration of Repaglinide can be decreased when it is combined with Dabrafenib.Approved
DanazolThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Danazol.Approved
DapoxetineDapoxetine may increase the hypoglycemic activities of Repaglinide.Investigational
DarunavirThe serum concentration of Repaglinide can be increased when it is combined with Darunavir.Approved
DasatinibThe serum concentration of Repaglinide can be increased when it is combined with Dasatinib.Approved, Investigational
DeferasiroxThe serum concentration of Repaglinide can be increased when it is combined with Deferasirox.Approved, Investigational
DelavirdineThe metabolism of Repaglinide can be decreased when combined with Delavirdine.Approved
DeoxyspergualinDeoxyspergualin may increase the hypoglycemic activities of Repaglinide.Investigational
dersalazinedersalazine may increase the hypoglycemic activities of Repaglinide.Investigational
DesogestrelThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Desogestrel.Approved
DesvenlafaxineDesvenlafaxine may increase the hypoglycemic activities of Repaglinide.Approved
DexamethasoneThe serum concentration of Repaglinide can be decreased when it is combined with Dexamethasone.Approved, Investigational, Vet Approved
DiazoxideThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Diazoxide.Approved
DienogestThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Dienogest.Approved
DiflunisalDiflunisal may increase the hypoglycemic activities of Repaglinide.Approved
DihydroergotamineThe metabolism of Repaglinide can be decreased when combined with Dihydroergotamine.Approved
DihydrotestosteroneDihydrotestosterone may increase the hypoglycemic activities of Repaglinide.Illicit
DiltiazemThe metabolism of Repaglinide can be decreased when combined with Diltiazem.Approved
DisopyramideDisopyramide may increase the hypoglycemic activities of Repaglinide.Approved
DoxycyclineThe metabolism of Repaglinide can be decreased when combined with Doxycycline.Approved, Investigational, Vet Approved
DronedaroneThe metabolism of Repaglinide can be decreased when combined with Dronedarone.Approved
DrospirenoneThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Drospirenone.Approved
DulaglutideDulaglutide may increase the hypoglycemic activities of Repaglinide.Approved
DuloxetineDuloxetine may increase the hypoglycemic activities of Repaglinide.Approved
EfavirenzThe serum concentration of Repaglinide can be decreased when it is combined with Efavirenz.Approved, Investigational
EltrombopagThe serum concentration of Repaglinide can be increased when it is combined with Eltrombopag.Approved
EmpagliflozinEmpagliflozin may increase the hypoglycemic activities of Repaglinide.Approved
EnoxacinEnoxacin may increase the hypoglycemic activities of Repaglinide.Approved
EnzalutamideThe serum concentration of Repaglinide can be decreased when it is combined with Enzalutamide.Approved
EpinephrineThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Epinephrine.Approved, Vet Approved
ErythromycinThe serum concentration of Repaglinide can be increased when it is combined with Erythromycin.Approved, Vet Approved
EscitalopramEscitalopram may increase the hypoglycemic activities of Repaglinide.Approved, Investigational
Eslicarbazepine acetateThe serum concentration of Repaglinide can be decreased when it is combined with Eslicarbazepine acetate.Approved
EstradiolThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Estradiol.Approved, Investigational, Vet Approved
Estrone sulfateThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Estrone sulfate.Approved
Etacrynic acidThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Etacrynic acid.Approved
Ethinyl EstradiolThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Ethinyl Estradiol.Approved
Ethynodiol diacetateThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Ethynodiol diacetate.Approved
EtonogestrelThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Etonogestrel.Approved, Investigational
EtoperidoneEtoperidone may increase the hypoglycemic activities of Repaglinide.Approved
EtravirineThe serum concentration of Repaglinide can be decreased when it is combined with Etravirine.Approved
EverolimusThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Everolimus.Approved
ExenatideExenatide may increase the hypoglycemic activities of Repaglinide.Approved, Investigational
FelodipineThe metabolism of Repaglinide can be decreased when combined with Felodipine.Approved, Investigational
FleroxacinFleroxacin may increase the hypoglycemic activities of Repaglinide.Approved
FluconazoleThe metabolism of Repaglinide can be decreased when combined with Fluconazole.Approved
FludrocortisoneThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Fludrocortisone.Approved
FlumequineFlumequine may increase the hypoglycemic activities of Repaglinide.Withdrawn
FluoxetineFluoxetine may increase the hypoglycemic activities of Repaglinide.Approved, Vet Approved
FluoxymesteroneFluoxymesterone may increase the hypoglycemic activities of Repaglinide.Approved, Illicit
FluvoxamineThe metabolism of Repaglinide can be decreased when combined with Fluvoxamine.Approved, Investigational
FosamprenavirThe metabolism of Repaglinide can be decreased when combined with Fosamprenavir.Approved
FosaprepitantThe serum concentration of Repaglinide can be increased when it is combined with Fosaprepitant.Approved
FosphenytoinThe metabolism of Repaglinide can be increased when combined with Fosphenytoin.Approved
FurazolidoneFurazolidone may increase the hypoglycemic activities of Repaglinide.Approved, Vet Approved
FurosemideThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Furosemide.Approved, Vet Approved
Fusidic AcidThe serum concentration of Repaglinide can be increased when it is combined with Fusidic Acid.Approved
GarenoxacinGarenoxacin may increase the hypoglycemic activities of Repaglinide.Investigational
GatifloxacinGatifloxacin may increase the hypoglycemic activities of Repaglinide.Approved, Investigational
GemfibrozilThe serum concentration of Repaglinide can be increased when it is combined with Gemfibrozil.Approved
GemifloxacinGemifloxacin may increase the hypoglycemic activities of Repaglinide.Approved, Investigational
GlibornurideGlibornuride may increase the hypoglycemic activities of Repaglinide.Withdrawn
GliclazideRepaglinide may increase the hypoglycemic activities of Gliclazide.Approved
GlimepirideGlimepiride may increase the hypoglycemic activities of Repaglinide.Approved
GlipizideRepaglinide may increase the hypoglycemic activities of Glipizide.Approved
GliquidoneGliquidone may increase the hypoglycemic activities of Repaglinide.Approved
GlyburideRepaglinide may increase the hypoglycemic activities of Glyburide.Approved
GoserelinThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Goserelin.Approved
GrepafloxacinGrepafloxacin may increase the hypoglycemic activities of Repaglinide.Withdrawn
GusperimusGusperimus may increase the hypoglycemic activities of Repaglinide.Investigational
HistrelinThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Histrelin.Approved
HydracarbazineHydracarbazine may increase the hypoglycemic activities of Repaglinide.Approved
HydrochlorothiazideThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Hydrochlorothiazide.Approved, Vet Approved
HydrocortisoneThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Hydrocortisone.Approved, Vet Approved
HydroflumethiazideThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Hydroflumethiazide.Approved
Hydroxyprogesterone caproateThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Hydroxyprogesterone caproate.Approved
IdelalisibThe serum concentration of Repaglinide can be increased when it is combined with Idelalisib.Approved
IloperidoneThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Iloperidone.Approved
ImatinibThe metabolism of Repaglinide can be decreased when combined with Imatinib.Approved
IndalpineIndalpine may increase the hypoglycemic activities of Repaglinide.Investigational, Withdrawn
IndapamideThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Indapamide.Approved
IndinavirThe serum concentration of Repaglinide can be increased when it is combined with Indinavir.Approved
Insulin AspartRepaglinide may increase the hypoglycemic activities of Insulin Aspart.Approved
Insulin DetemirRepaglinide may increase the hypoglycemic activities of Insulin Detemir.Approved
Insulin GlargineInsulin Glargine may increase the hypoglycemic activities of Repaglinide.Approved
Insulin GlulisineRepaglinide may increase the hypoglycemic activities of Insulin Glulisine.Approved
Insulin HumanInsulin Human may increase the hypoglycemic activities of Repaglinide.Approved, Investigational
Insulin LisproInsulin Lispro may increase the hypoglycemic activities of Repaglinide.Approved
Insulin PorkInsulin Pork may increase the hypoglycemic activities of Repaglinide.Approved
IproclozideIproclozide may increase the hypoglycemic activities of Repaglinide.Withdrawn
IproniazidIproniazid may increase the hypoglycemic activities of Repaglinide.Withdrawn
IrbesartanThe metabolism of Repaglinide can be decreased when combined with Irbesartan.Approved, Investigational
IsavuconazoniumThe metabolism of Repaglinide can be decreased when combined with Isavuconazonium.Approved, Investigational
IsocarboxazidIsocarboxazid may increase the hypoglycemic activities of Repaglinide.Approved
IsradipineThe metabolism of Repaglinide can be decreased when combined with Isradipine.Approved
ItraconazoleThe serum concentration of Repaglinide can be increased when it is combined with Itraconazole.Approved, Investigational
IvacaftorThe serum concentration of Repaglinide can be increased when it is combined with Ivacaftor.Approved
JosamycinThe serum concentration of Repaglinide can be increased when it is combined with Josamycin.Approved
KetoconazoleThe serum concentration of Repaglinide can be increased when it is combined with Ketoconazole.Approved, Investigational
KitasamycinThe serum concentration of Repaglinide can be increased when it is combined with Kitasamycin.Experimental
LanreotideRepaglinide may increase the hypoglycemic activities of Lanreotide.Approved
LapatinibThe metabolism of Repaglinide can be decreased when combined with Lapatinib.Approved, Investigational
LeuprolideThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Leuprolide.Approved, Investigational
LevofloxacinLevofloxacin may increase the hypoglycemic activities of Repaglinide.Approved, Investigational
LevomilnacipranLevomilnacipran may increase the hypoglycemic activities of Repaglinide.Approved
LevonorgestrelThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Levonorgestrel.Approved, Investigational
LinagliptinLinagliptin may increase the hypoglycemic activities of Repaglinide.Approved
Lipoic AcidLipoic Acid may increase the hypoglycemic activities of Repaglinide.Approved, Nutraceutical
LiraglutideLiraglutide may increase the hypoglycemic activities of Repaglinide.Approved
LomefloxacinLomefloxacin may increase the hypoglycemic activities of Repaglinide.Approved
LopinavirThe serum concentration of Repaglinide can be increased when it is combined with Lopinavir.Approved
LosartanThe metabolism of Repaglinide can be decreased when combined with Losartan.Approved
LovastatinThe metabolism of Repaglinide can be decreased when combined with Lovastatin.Approved, Investigational
LuliconazoleThe serum concentration of Repaglinide can be increased when it is combined with Luliconazole.Approved
LumacaftorThe serum concentration of Repaglinide can be increased when it is combined with Lumacaftor.Approved
LurasidoneThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Lurasidone.Approved
MebanazineMebanazine may increase the hypoglycemic activities of Repaglinide.Withdrawn
MecaserminRepaglinide may increase the hypoglycemic activities of Mecasermin.Approved, Investigational
Medroxyprogesterone acetateThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Medroxyprogesterone acetate.Approved, Investigational
Megestrol acetateThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Megestrol acetate.Approved, Vet Approved
MesalazineMesalazine may increase the hypoglycemic activities of Repaglinide.Approved
MestranolThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Mestranol.Approved
MetforminMetformin may increase the hypoglycemic activities of Repaglinide.Approved
MethotrimeprazineThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Methotrimeprazine.Approved
MethyclothiazideThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Methyclothiazide.Approved
Methylene blueMethylene blue may increase the hypoglycemic activities of Repaglinide.Investigational
MethylprednisoloneThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Methylprednisolone.Approved, Vet Approved
MethyltestosteroneMethyltestosterone may increase the hypoglycemic activities of Repaglinide.Approved
MetolazoneThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Metolazone.Approved
MifepristoneThe serum concentration of Repaglinide can be increased when it is combined with Mifepristone.Approved, Investigational
MiglitolMiglitol may increase the hypoglycemic activities of Repaglinide.Approved
MiglustatMiglustat may increase the hypoglycemic activities of Repaglinide.Approved
MilnacipranMilnacipran may increase the hypoglycemic activities of Repaglinide.Approved
MinaprineMinaprine may increase the hypoglycemic activities of Repaglinide.Approved
MitiglinideMitiglinide may increase the hypoglycemic activities of Repaglinide.Approved, Investigational
MitotaneThe serum concentration of Repaglinide can be decreased when it is combined with Mitotane.Approved
MoclobemideMoclobemide may increase the hypoglycemic activities of Repaglinide.Approved
ModafinilThe serum concentration of Repaglinide can be decreased when it is combined with Modafinil.Approved, Investigational
MoxifloxacinMoxifloxacin may increase the hypoglycemic activities of Repaglinide.Approved, Investigational
NafcillinThe serum concentration of Repaglinide can be decreased when it is combined with Nafcillin.Approved
Nalidixic AcidNalidixic Acid may increase the hypoglycemic activities of Repaglinide.Approved
NateglinideNateglinide may increase the hypoglycemic activities of Repaglinide.Approved, Investigational
NCX 4016NCX 4016 may increase the hypoglycemic activities of Repaglinide.Investigational
NefazodoneThe serum concentration of Repaglinide can be increased when it is combined with Nefazodone.Approved, Withdrawn
NelfinavirThe serum concentration of Repaglinide can be increased when it is combined with Nelfinavir.Approved
NemonoxacinNemonoxacin may increase the hypoglycemic activities of Repaglinide.Investigational
NetupitantThe serum concentration of Repaglinide can be increased when it is combined with Netupitant.Approved
NevirapineThe metabolism of Repaglinide can be increased when combined with Nevirapine.Approved
NiacinThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Niacin.Approved, Investigational, Nutraceutical
NialamideNialamide may increase the hypoglycemic activities of Repaglinide.Withdrawn
NilotinibThe metabolism of Repaglinide can be decreased when combined with Nilotinib.Approved, Investigational
NitroaspirinNitroaspirin may increase the hypoglycemic activities of Repaglinide.Investigational
NorethisteroneThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Norethisterone.Approved
NorfloxacinNorfloxacin may increase the hypoglycemic activities of Repaglinide.Approved
NorgestimateThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Norgestimate.Approved
OctamoxinOctamoxin may increase the hypoglycemic activities of Repaglinide.Withdrawn
OctreotideOctreotide may increase the hypoglycemic activities of Repaglinide.Approved, Investigational
OfloxacinOfloxacin may increase the hypoglycemic activities of Repaglinide.Approved
OlanzapineThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Olanzapine.Approved, Investigational
OlaparibThe metabolism of Repaglinide can be decreased when combined with Olaparib.Approved
OleandomycinThe serum concentration of Repaglinide can be increased when it is combined with Oleandomycin.Vet Approved
OlsalazineOlsalazine may increase the hypoglycemic activities of Repaglinide.Approved
OsimertinibThe serum concentration of Repaglinide can be increased when it is combined with Osimertinib.Approved
OxandroloneOxandrolone may increase the hypoglycemic activities of Repaglinide.Approved, Investigational
OxymetholoneOxymetholone may increase the hypoglycemic activities of Repaglinide.Approved, Illicit
PalbociclibThe serum concentration of Repaglinide can be increased when it is combined with Palbociclib.Approved
PaliperidoneThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Paliperidone.Approved
PargylinePargyline may increase the hypoglycemic activities of Repaglinide.Approved
ParoxetineParoxetine may increase the hypoglycemic activities of Repaglinide.Approved, Investigational
PasireotideRepaglinide may increase the hypoglycemic activities of Pasireotide.Approved
PazufloxacinPazufloxacin may increase the hypoglycemic activities of Repaglinide.Investigational
PefloxacinPefloxacin may increase the hypoglycemic activities of Repaglinide.Approved
PegvisomantPegvisomant may increase the hypoglycemic activities of Repaglinide.Approved
PentamidinePentamidine may increase the hypoglycemic activities of Repaglinide.Approved
PentobarbitalThe metabolism of Repaglinide can be increased when combined with Pentobarbital.Approved, Vet Approved
PhenelzinePhenelzine may increase the hypoglycemic activities of Repaglinide.Approved
PhenforminPhenformin may increase the hypoglycemic activities of Repaglinide.Approved, Withdrawn
PheniprazinePheniprazine may increase the hypoglycemic activities of Repaglinide.Withdrawn
PhenobarbitalThe metabolism of Repaglinide can be increased when combined with Phenobarbital.Approved
PhenoxypropazinePhenoxypropazine may increase the hypoglycemic activities of Repaglinide.Withdrawn
PhenytoinThe metabolism of Repaglinide can be increased when combined with Phenytoin.Approved, Vet Approved
PioglitazoneThe metabolism of Repaglinide can be decreased when combined with Pioglitazone.Approved, Investigational
PiperazineThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Piperazine.Approved, Vet Approved
PipotiazineThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Pipotiazine.Approved
PirlindolePirlindole may increase the hypoglycemic activities of Repaglinide.Approved
PivhydrazinePivhydrazine may increase the hypoglycemic activities of Repaglinide.Withdrawn
PolythiazideThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Polythiazide.Approved
PosaconazoleThe serum concentration of Repaglinide can be increased when it is combined with Posaconazole.Approved, Investigational, Vet Approved
PramlintidePramlintide may increase the hypoglycemic activities of Repaglinide.Approved, Investigational
PrednisoloneThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Prednisolone.Approved, Vet Approved
PrednisoneThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Prednisone.Approved, Vet Approved
PrimidoneThe metabolism of Repaglinide can be increased when combined with Primidone.Approved, Vet Approved
ProgesteroneThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Progesterone.Approved, Vet Approved
PrulifloxacinPrulifloxacin may increase the hypoglycemic activities of Repaglinide.Investigational
QuetiapineThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Quetiapine.Approved
QuinethazoneThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Quinethazone.Approved
QuinineQuinine may increase the hypoglycemic activities of Repaglinide.Approved
RabeprazoleThe metabolism of Repaglinide can be decreased when combined with Rabeprazole.Approved, Investigational
RanolazineThe metabolism of Repaglinide can be decreased when combined with Ranolazine.Approved, Investigational
RasagilineRasagiline may increase the hypoglycemic activities of Repaglinide.Approved
RifabutinThe metabolism of Repaglinide can be increased when combined with Rifabutin.Approved
RifampicinThe serum concentration of Repaglinide can be decreased when it is combined with Rifampicin.Approved
RifapentineThe metabolism of Repaglinide can be increased when combined with Rifapentine.Approved
RisperidoneThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Risperidone.Approved, Investigational
RitonavirThe serum concentration of Repaglinide can be increased when it is combined with Ritonavir.Approved, Investigational
RosiglitazoneThe metabolism of Repaglinide can be decreased when combined with Rosiglitazone.Approved, Investigational
RosoxacinRosoxacin may increase the hypoglycemic activities of Repaglinide.Approved
SafrazineSafrazine may increase the hypoglycemic activities of Repaglinide.Withdrawn
Salicylic acidSalicylic acid may increase the hypoglycemic activities of Repaglinide.Approved, Vet Approved
SaquinavirThe serum concentration of Repaglinide can be increased when it is combined with Saquinavir.Approved, Investigational
SaxagliptinSaxagliptin may increase the hypoglycemic activities of Repaglinide.Approved
SecobarbitalThe metabolism of Repaglinide can be increased when combined with Secobarbital.Approved, Vet Approved
SelegilineSelegiline may increase the hypoglycemic activities of Repaglinide.Approved, Investigational, Vet Approved
SertralineSertraline may increase the hypoglycemic activities of Repaglinide.Approved
SildenafilThe metabolism of Repaglinide can be decreased when combined with Sildenafil.Approved, Investigational
SiltuximabThe serum concentration of Repaglinide can be decreased when it is combined with Siltuximab.Approved
SimeprevirThe serum concentration of Repaglinide can be increased when it is combined with Simeprevir.Approved
SirolimusThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Sirolimus.Approved, Investigational
SitagliptinSitagliptin may increase the hypoglycemic activities of Repaglinide.Approved, Investigational
SolithromycinThe serum concentration of Repaglinide can be increased when it is combined with Solithromycin.Investigational
SparfloxacinSparfloxacin may increase the hypoglycemic activities of Repaglinide.Approved
St. John's WortThe serum concentration of Repaglinide can be decreased when it is combined with St. John&#39;s Wort.Nutraceutical
StanozololStanozolol may increase the hypoglycemic activities of Repaglinide.Approved, Vet Approved
StiripentolThe serum concentration of Repaglinide can be increased when it is combined with Stiripentol.Approved
SulfadiazineSulfadiazine may increase the hypoglycemic activities of Repaglinide.Approved, Vet Approved
SulfamethoxazoleRepaglinide may increase the hypoglycemic activities of Sulfamethoxazole.Approved
SulfisoxazoleSulfisoxazole may increase the hypoglycemic activities of Repaglinide.Approved, Vet Approved
SulodexideSulodexide may increase the hypoglycemic activities of Repaglinide.Approved, Investigational
SunitinibRepaglinide may increase the hypoglycemic activities of Sunitinib.Approved, Investigational
TacrolimusThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Tacrolimus.Approved, Investigational
TamoxifenThe metabolism of Repaglinide can be decreased when combined with Tamoxifen.Approved
TelaprevirThe serum concentration of Repaglinide can be increased when it is combined with Telaprevir.Approved
TelithromycinThe serum concentration of Repaglinide can be increased when it is combined with Telithromycin.Approved
TemafloxacinTemafloxacin may increase the hypoglycemic activities of Repaglinide.Withdrawn
TemsirolimusThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Temsirolimus.Approved
TeriflunomideThe serum concentration of Repaglinide can be increased when it is combined with Teriflunomide.Approved
TestosteroneTestosterone may increase the hypoglycemic activities of Repaglinide.Approved, Investigational
ThiazolidinedioneThiazolidinedione may increase the hypoglycemic activities of Repaglinide.Investigational
TiclopidineThe metabolism of Repaglinide can be decreased when combined with Ticlopidine.Approved
TipranavirThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Tipranavir.Approved, Investigational
TocilizumabThe serum concentration of Repaglinide can be decreased when it is combined with Tocilizumab.Approved
TolazamideTolazamide may increase the hypoglycemic activities of Repaglinide.Approved
TolbutamideRepaglinide may increase the hypoglycemic activities of Tolbutamide.Approved
ToloxatoneToloxatone may increase the hypoglycemic activities of Repaglinide.Approved
TorasemideThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Torasemide.Approved
Trans-2-PhenylcyclopropylamineTrans-2-Phenylcyclopropylamine may increase the hypoglycemic activities of Repaglinide.Experimental
TranylcypromineTranylcypromine may increase the hypoglycemic activities of Repaglinide.Approved
TriamcinoloneThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Triamcinolone.Approved, Vet Approved
TrichlormethiazideThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Trichlormethiazide.Approved, Vet Approved
TrimethoprimThe metabolism of Repaglinide can be decreased when combined with Trimethoprim.Approved, Vet Approved
TriptorelinThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Triptorelin.Approved, Vet Approved
TroglitazoneTroglitazone may increase the hypoglycemic activities of Repaglinide.Withdrawn
TroleandomycinThe serum concentration of Repaglinide can be increased when it is combined with Troleandomycin.Approved
TrovafloxacinTrovafloxacin may increase the hypoglycemic activities of Repaglinide.Approved, Withdrawn
TylosinThe serum concentration of Repaglinide can be increased when it is combined with Tylosin.Vet Approved
VenlafaxineThe metabolism of Repaglinide can be decreased when combined with Venlafaxine.Approved
VerapamilThe metabolism of Repaglinide can be decreased when combined with Verapamil.Approved
VildagliptinVildagliptin may increase the hypoglycemic activities of Repaglinide.Approved, Investigational
VogliboseVoglibose may increase the hypoglycemic activities of Repaglinide.Approved, Investigational
VoriconazoleThe serum concentration of Repaglinide can be increased when it is combined with Voriconazole.Approved, Investigational
VorinostatThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Vorinostat.Approved, Investigational
ZimelidineZimelidine may increase the hypoglycemic activities of Repaglinide.Withdrawn
ZiprasidoneThe metabolism of Repaglinide can be decreased when combined with Ziprasidone.Approved
Food Interactions
  • Take up to 30 minutes before meals.
  • When taken with a high-fat meal, AUC and Cmax decreases.
References
Synthesis Reference

Manne Reddy, “Polymorphic forms of (S)-Repaglinide and the processes for preparation thereof.” U.S. Patent US20040102477, issued May 27, 2004.

US20040102477
General References
  1. Massi-Benedetti M, Damsbo P: Pharmacology and clinical experience with repaglinide. Expert Opin Investig Drugs. 2000 Apr;9(4):885-98. [PubMed:11060717 ]
External Links
ATC CodesA10BD14A10BX02
AHFS Codes
  • 68:20.16
PDB EntriesNot Available
FDA labelDownload (175 KB)
MSDSDownload (57.3 KB)
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9172
Blood Brain Barrier-0.7101
Caco-2 permeable-0.5891
P-glycoprotein substrateSubstrate0.8145
P-glycoprotein inhibitor IInhibitor0.6044
P-glycoprotein inhibitor IIInhibitor0.6868
Renal organic cation transporterNon-inhibitor0.849
CYP450 2C9 substrateNon-substrate0.8288
CYP450 2D6 substrateNon-substrate0.9117
CYP450 3A4 substrateSubstrate0.7019
CYP450 1A2 substrateNon-inhibitor0.9206
CYP450 2C9 inhibitorNon-inhibitor0.907
CYP450 2D6 inhibitorNon-inhibitor0.9231
CYP450 2C19 inhibitorNon-inhibitor0.9026
CYP450 3A4 inhibitorNon-inhibitor0.9264
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.8682
Ames testNon AMES toxic0.8136
CarcinogenicityNon-carcinogens0.8004
BiodegradationNot ready biodegradable0.919
Rat acute toxicity2.4497 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9605
hERG inhibition (predictor II)Non-inhibitor0.5272
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
Manufacturers
  • Novo nordisk inc
  • Novo Nordisk Inc.
Packagers
Dosage forms
FormRouteStrength
TabletOral1 mg
TabletOral2 mg
TabletOral0.5 mg
TabletOral1.0 mg
TabletOral2.0 mg
TabletOral
TabletOral.5 mg/1
TabletOral1 mg/1
TabletOral2 mg/1
TabletOral5 mg
Prices
Unit descriptionCostUnit
Prandin 1 mg tablet2.48USD tablet
Prandin 0.5 mg tablet2.47USD tablet
Prandin 2 mg tablet2.33USD tablet
Gluconorm 2 mg Tablet0.34USD tablet
Gluconorm 1 mg Tablet0.32USD tablet
Gluconorm 0.5 mg Tablet0.31USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
CA2111851 No2002-02-262011-06-21Canada
US6677358 No1998-06-122018-06-12Us
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point130-131 °CNot Available
logP5.9Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.00294 mg/mLALOGPS
logP5.05ALOGPS
logP3.95ChemAxon
logS-5.2ALOGPS
pKa (Strongest Acidic)3.68ChemAxon
pKa (Strongest Basic)4.82ChemAxon
Physiological Charge-1ChemAxon
Hydrogen Acceptor Count5ChemAxon
Hydrogen Donor Count2ChemAxon
Polar Surface Area78.87 Å2ChemAxon
Rotatable Bond Count10ChemAxon
Refractivity131.83 m3·mol-1ChemAxon
Polarizability51.49 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 phenylpiperidines. These are compounds containing a phenylpiperidine skeleton, which consists of a piperidine bound to a phenyl group.
KingdomOrganic compounds
Super ClassOrganoheterocyclic compounds
ClassPiperidines
Sub ClassPhenylpiperidines
Direct ParentPhenylpiperidines
Alternative Parents
Substituents
  • Phenylpiperidine
  • Phenylacetamide
  • Phenylpropylamine
  • Benzoic acid
  • Benzoic acid or derivatives
  • Substituted aniline
  • Dialkylarylamine
  • Phenol ether
  • Benzoyl
  • Aniline
  • Alkyl aryl ether
  • Benzenoid
  • Monocyclic benzene moiety
  • Tertiary amine
  • Secondary carboxylic acid amide
  • Carboxamide group
  • Azacycle
  • Monocarboxylic acid or derivatives
  • Ether
  • Carboxylic acid
  • Carboxylic acid derivative
  • Carboxylic acid amide
  • 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
inhibitor
General Function:
Sulfonylurea receptor activity
Specific Function:
Subunit of the beta-cell ATP-sensitive potassium channel (KATP). Regulator of ATP-sensitive K(+) channels and insulin release.
Gene Name:
ABCC8
Uniprot ID:
Q09428
Molecular Weight:
176990.36 Da
References
  1. Hu S, Wang S, Fanelli B, Bell PA, Dunning BE, Geisse S, Schmitz R, Boettcher BR: Pancreatic beta-cell K(ATP) channel activity and membrane-binding studies with nateglinide: A comparison with sulfonylureas and repaglinide. J Pharmacol Exp Ther. 2000 May;293(2):444-52. [PubMed:10773014 ]
  2. Sunaga Y, Gonoi T, Shibasaki T, Ichikawa K, Kusama H, Yano H, Seino S: The effects of mitiglinide (KAD-1229), a new anti-diabetic drug, on ATP-sensitive K+ channels and insulin secretion: comparison with the sulfonylureas and nateglinide. Eur J Pharmacol. 2001 Nov 9;431(1):119-25. [PubMed:11716850 ]
  3. Hansen AM, Christensen IT, Hansen JB, Carr RD, Ashcroft FM, Wahl P: Differential interactions of nateglinide and repaglinide on the human beta-cell sulphonylurea receptor 1. Diabetes. 2002 Sep;51(9):2789-95. [PubMed:12196472 ]
  4. Wangler B, Schneider S, Thews O, Schirrmacher E, Comagic S, Feilen P, Schwanstecher C, Schwanstecher M, Shiue CY, Alavi A, Hohnemann S, Piel M, Rosch F, Schirrmacher R: Synthesis and evaluation of (S)-2-(2-[18F]fluoroethoxy)-4-([3-methyl-1-(2-piperidin-1-yl-phenyl)-butyl-carbam oyl]-methyl)-benzoic acid ([18F]repaglinide): a promising radioligand for quantification of pancreatic beta-cell mass with positron emission tomography (PET). Nucl Med Biol. 2004 Jul;31(5):639-47. [PubMed:15219283 ]
  5. Wangler B, Beck C, Shiue CY, Schneider S, Schwanstecher C, Schwanstecher M, Feilen PJ, Alavi A, Rosch F, Schirrmacher R: Synthesis and in vitro evaluation of (S)-2-([11C]methoxy)-4-[3-methyl-1-(2-piperidine-1-yl-phenyl)-butyl-carbamoyl]-be nzoic acid ([11C]methoxy-repaglinide): a potential beta-cell imaging agent. Bioorg Med Chem Lett. 2004 Oct 18;14(20):5205-9. [PubMed:15380228 ]
  6. Dornhorst A: Insulinotropic meglitinide analogues. Lancet. 2001 Nov 17;358(9294):1709-16. [PubMed:11728565 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
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. Scarsi M, Podvinec M, Roth A, Hug H, Kersten S, Albrecht H, Schwede T, Meyer UA, Rucker C: Sulfonylureas and glinides exhibit peroxisome proliferator-activated receptor gamma activity: a combined virtual screening and biological assay approach. Mol Pharmacol. 2007 Feb;71(2):398-406. Epub 2006 Nov 2. [PubMed:17082235 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Steroid hydroxylase activity
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. 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 ]
  3. Bidstrup TB, Bjornsdottir I, Sidelmann UG, Thomsen MS, Hansen KT: CYP2C8 and CYP3A4 are the principal enzymes involved in the human in vitro biotransformation of the insulin secretagogue repaglinide. Br J Clin Pharmacol. 2003 Sep;56(3):305-14. [PubMed:12919179 ]
  4. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitor
General Function:
Vitamin d3 25-hydroxylase activity
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation reactions (e.g. caffeine 8-oxidation, omeprazole sulphoxidation, midazolam 1'-hydroxylation and midazolam 4-hydroxylation) of structurally unrelated compounds, including steroids, fatty acids, and xenobiot...
Gene Name:
CYP3A4
Uniprot ID:
P08684
Molecular Weight:
57342.67 Da
References
  1. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [PubMed:19515014 ]
  2. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
  3. Bidstrup TB, Bjornsdottir I, Sidelmann UG, Thomsen MS, Hansen KT: CYP2C8 and CYP3A4 are the principal enzymes involved in the human in vitro biotransformation of the insulin secretagogue repaglinide. Br J Clin Pharmacol. 2003 Sep;56(3):305-14. [PubMed:12919179 ]

Carriers

Kind
Protein
Organism
Human
Pharmacological action
unknown
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
substrate
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. He J, Qiu Z, Li N, Yu Y, Lu Y, Han D, Li T, Zhao D, Sun W, Fang F, Zheng J, Fan H, Chen X: Effects of SLCO1B1 polymorphisms on the pharmacokinetics and pharmacodynamics of repaglinide in healthy Chinese volunteers. Eur J Clin Pharmacol. 2011 Jul;67(7):701-7. doi: 10.1007/s00228-011-0994-7. Epub 2011 Feb 17. [PubMed:21327909 ]
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Drug created on June 13, 2005 07:24 / Updated on August 17, 2016 12:23