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Identification
NameGliclazide
Accession NumberDB01120  (APRD00460)
TypeSmall Molecule
GroupsApproved
DescriptionGliclazide is an oral antihyperglycemic agent used for the treatment of non-insulin-dependent diabetes mellitus (NIDDM). It belongs to the sulfonylurea class of insulin secretagogues, which act by stimulating β cells of the pancreas to release insulin. Sulfonylureas increase both basal insulin secretion and meal-stimulated insulin release. Medications in this class differ in their dose, rate of absorption, duration of action, route of elimination and binding site on their target pancreatic β cell receptor. Sulfonylureas also increase peripheral glucose utilization, decrease hepatic gluconeogenesis and may increase the number and sensitivity of insulin receptors. Sulfonylureas are associated with weight gain, though less so than insulin. Due to their mechanism of action, sulfonylureas may cause hypoglycemia and require consistent food intake to decrease this risk. The risk of hypoglycemia is increased in elderly, debilitated and malnourished individuals. Gliclazide has been shown to decrease fasting plasma glucose, postprandial blood glucose and glycosolated hemoglobin (HbA1c) levels (reflective of the last 8-10 weeks of glucose control). Gliclazide is extensively metabolized by the liver; its metabolites are excreted in both urine (60-70%) and feces (10-20%).
Structure
Thumb
Synonyms
1-(3-Azabicyclo(3.3.0)oct-3-yl)-3-(p-tolylsulfonyl)urea
1-(Hexahydrocyclopenta(c)pyrrol-2(1H)-yl)-3-(p-tolylsulfonyl)urea
Gliclazida
Gliclazidum
N-(4-Methylbenzenesulfonyl)-N'-(3-azabicyclo(3.3.0)oct-3-yl)urea
External Identifiers Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Act Gliclazide Mrtablet (extended-release)30 mgoralActavis Pharma Company2015-03-31Not applicableCanada
Act Gliclazide Mrtablet (extended-release)60 mgoralActavis Pharma CompanyNot applicableNot applicableCanada
Ava-gliclazidetablet80 mgoralAvanstra Inc2011-08-112014-08-21Canada
Diamicrontablet80 mgoralServier Canada Inc1990-12-31Not applicableCanada
Diamicron Mrtablet (extended-release)30 mgoralServier Canada Inc2001-04-04Not applicableCanada
Diamicron Mrtablet (extended-release)60 mgoralServier Canada Inc2010-12-09Not applicableCanada
Glictablet80 mgoralPrempharm Inc2003-10-022005-08-05Canada
Gliclazidetablet80 mgoralSanis Health Inc2010-02-25Not applicableCanada
Gliclazide -tab 80mgtablet80 mgoralProval Pharma Division Of Servier Canada Inc1997-08-132012-02-13Canada
Gliclazide-80tablet80 mgoralPro Doc Limitee2003-12-10Not applicableCanada
Mint-gliclazide Mrtablet (extended-release)60 mgoralMint Pharmaceuticals IncNot applicableNot applicableCanada
Mint-gliclazide Mrtablet (extended-release)30 mgoralMint Pharmaceuticals Inc2014-06-02Not applicableCanada
Mylan-gliclazidetablet80 mgoralMylan Pharmaceuticals Ulc1998-08-13Not applicableCanada
Mylan-gliclazide Mrtablet (extended-release)30 mgoralMylan Pharmaceuticals Ulc2015-08-07Not applicableCanada
Mylan-gliclazide Mrtablet (extended-release)60 mgoralMylan Pharmaceuticals UlcNot applicableNot applicableCanada
Nu-gliclazidetablet80 mgoralNu Pharm IncNot applicableNot applicableCanada
PMS-gliclazidetablet80 mgoralPharmascience Inc2007-12-18Not applicableCanada
Ran-gliclazide Mrtablet (extended-release)60 mgoralRanbaxy Pharmaceuticals Canada Inc.Not applicableNot applicableCanada
Sandoz Gliclazidetablet80 mgoralSandoz Canada Incorporated2004-08-092008-08-07Canada
Teva-gliclazidetablet80 mgoralTeva Canada Limited1998-06-08Not applicableCanada
Approved Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Apo-gliclazidetablet80 mgoralApotex Inc2002-07-02Not applicableCanada
Apo-gliclazide Mrtablet (extended-release)60 mgoralApotex Inc2015-04-14Not applicableCanada
Apo-gliclazide Mrtablet (extended-release)30 mgoralApotex Inc2008-06-04Not applicableCanada
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
DiamicronServier
GlimicronNot Available
NordialexNot Available
Brand mixturesNot Available
SaltsNot Available
Categories
UNIIG4PX8C4HKV
CAS number21187-98-4
WeightAverage: 323.411
Monoisotopic: 323.130362243
Chemical FormulaC15H21N3O3S
InChI KeyInChIKey=BOVGTQGAOIONJV-BETUJISGNA-N
InChI
InChI=1/C15H21N3O3S/c1-11-5-7-14(8-6-11)22(20,21)17-15(19)16-18-9-12-3-2-4-13(12)10-18/h5-8,12-13H,2-4,9-10H2,1H3,(H2,16,17,19)/t12-,13+
IUPAC Name
3-[(3aR,6aS)-octahydrocyclopenta[c]pyrrol-2-yl]-1-(4-methylbenzenesulfonyl)urea
SMILES
[H][C@@]12CCC[C@]1([H])CN(C2)NC(=O)NS(=O)(=O)C1=CC=C(C)C=C1
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as benzenesulfonamides. These are organic compounds containing a sulfonamide group that is S-linked to a benzene ring.
KingdomOrganic compounds
Super ClassBenzenoids
ClassBenzene and substituted derivatives
Sub ClassBenzenesulfonamides
Direct ParentBenzenesulfonamides
Alternative Parents
Substituents
  • Tosyl compound
  • Benzenesulfonamide
  • Toluene
  • Sulfonylurea
  • Aminosulfonyl compound
  • Sulfonyl
  • Sulfonic acid derivative
  • Sulfonamide
  • Semicarbazide
  • Pyrrolidine
  • Cyclic alcohol
  • Azacycle
  • Organoheterocyclic compound
  • Hydrocarbon derivative
  • Organosulfur compound
  • Organooxygen compound
  • Organonitrogen compound
  • Aromatic heteropolycyclic compound
Molecular FrameworkAromatic heteropolycyclic compounds
External DescriptorsNot Available
Pharmacology
IndicationFor the treatment of NIDDM in conjunction with diet and exercise.
PharmacodynamicsGliclazide is a second generation sulphonylurea which acts as a hypoglycemic agent. It stimulates β cells of the islet of Langerhans in the pancreas to release insulin. It also enhances peripheral insulin sensitivity. Overall, it potentiates insulin release and improves insulin dynamics.
Mechanism of actionGliclazide binds to the β cell sulfonyl urea receptor (SUR1). This binding subsequently blocks the ATP sensitive potassium channels. The binding results in closure of the channels and leads to a resulting decrease in potassium efflux leads to depolarization of the β cells. This opens voltage-dependent calcium channels in the β cell resulting in calmodulin activation, which in turn leads to exocytosis of insulin containing secretorty granules.
Related Articles
AbsorptionRapidly and well absorbed but may have wide inter- and intra-individual variability. Peak plasma concentrations occur within 4-6 hours of oral administration.
Volume of distributionNot Available
Protein binding94%, highly bound to plasma proteins
Metabolism

Extensively metabolized in the liver. Less than 1% of the orally administered dose appears unchanged in the urine. Metabolites include oxidized and hydroxylated derivates, as well as glucuronic acid conjugates.

SubstrateEnzymesProduct
Gliclazide
7-β-HydroxygliclazideDetails
Gliclazide
6-β-HydroxygliclazideDetails
Gliclazide
MethylhydroxygliclazideDetails
Methylhydroxygliclazide
Not Available
CarboxygliclazideDetails
Gliclazide
7-α-HydroxygliclazideDetails
Gliclazide
6-α-HydroxygliclazideDetails
Route of eliminationMetabolites and conjugates are eliminated primarily by the kidneys (60-70%) and also in the feces (10-20%).
Half life10.4 hours. Duration of action is 10-24 hours.
ClearanceNot Available
ToxicityLD50=3000 mg/kg (orally in mice). Gliclazide and its metabolites may accumulate in those with severe hepatic and/or renal dysfunction. Symptoms of hypoglycemia include: dizziness, lack of energy, drowsiness, headache and sweating.
Affected organisms
  • Humans and other mammals
Pathways
PathwayCategorySMPDB ID
Gliclazide Action PathwayDrug actionSMP00461
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9944
Blood Brain Barrier+0.8445
Caco-2 permeable-0.6543
P-glycoprotein substrateSubstrate0.6982
P-glycoprotein inhibitor INon-inhibitor0.8619
P-glycoprotein inhibitor IINon-inhibitor0.931
Renal organic cation transporterNon-inhibitor0.8178
CYP450 2C9 substrateSubstrate0.6226
CYP450 2D6 substrateNon-substrate0.9116
CYP450 3A4 substrateNon-substrate0.6925
CYP450 1A2 substrateNon-inhibitor0.9046
CYP450 2C9 inhibitorNon-inhibitor0.9071
CYP450 2D6 inhibitorNon-inhibitor0.9231
CYP450 2C19 inhibitorNon-inhibitor0.9025
CYP450 3A4 inhibitorNon-inhibitor0.9218
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.8751
Ames testNon AMES toxic0.8047
CarcinogenicityNon-carcinogens0.7944
BiodegradationNot ready biodegradable0.7997
Rat acute toxicity2.0016 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.5992
hERG inhibition (predictor II)Non-inhibitor0.8064
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
ManufacturersNot Available
PackagersNot Available
Dosage forms
FormRouteStrength
Tablet (extended-release)oral60 mg
Tablet (extended-release)oral30 mg
Tabletoral80 mg
Prices
Unit descriptionCostUnit
Diamicron 80 mg Tablet0.42USD tablet
Apo-Gliclazide 80 mg Tablet0.23USD tablet
Gliclazide 80 mg Tablet0.23USD tablet
Mylan-Gliclazide 80 mg Tablet0.23USD tablet
Novo-Gliclazide 80 mg Tablet0.23USD tablet
Pms-Gliclazide 80 mg Tablet0.23USD tablet
Diamicron Mr 30 mg Sustained-Release Tablet0.16USD tablet
Apo-Gliclazide Mr 30 mg Sustained-Release Tablet0.15USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
CA2273420 No2002-07-092019-05-27Canada
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point180-182U.S. Patent 3,501,495
logP2.6Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.19 mg/mLALOGPS
logP1.52ALOGPS
logP1.73ChemAxon
logS-3.2ALOGPS
pKa (Strongest Acidic)4.07ChemAxon
pKa (Strongest Basic)1.38ChemAxon
Physiological Charge-1ChemAxon
Hydrogen Acceptor Count4ChemAxon
Hydrogen Donor Count2ChemAxon
Polar Surface Area78.51 Å2ChemAxon
Rotatable Bond Count2ChemAxon
Refractivity83.88 m3·mol-1ChemAxon
Polarizability34.17 Å3ChemAxon
Number of Rings3ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
SpectraNot Available
References
Synthesis Reference

U.S. Patent 3,501,495

General ReferencesNot Available
External Links
ATC CodesA10BB09
AHFS Codes
  • 68:20.20
PDB EntriesNot Available
FDA labelNot Available
MSDSDownload (57.5 KB)
Interactions
Drug Interactions
Drug
7,8-DICHLORO-1,2,3,4-TETRAHYDROISOQUINOLINE7,8-DICHLORO-1,2,3,4-TETRAHYDROISOQUINOLINE may increase the hypoglycemic activities of Gliclazide.
AbirateroneThe metabolism of Gliclazide can be decreased when combined with Abiraterone.
AcarboseAcarbose may increase the hypoglycemic activities of Gliclazide.
AcebutololAcebutolol may increase the hypoglycemic activities of Gliclazide.
AcenocoumarolGliclazide may increase the anticoagulant activities of Acenocoumarol.
AcetohexamideAcetohexamide may increase the hypoglycemic activities of Gliclazide.
Acetylsalicylic acidAcetylsalicylic acid may increase the hypoglycemic activities of Gliclazide.
AicarAicar may increase the hypoglycemic activities of Gliclazide.
AlbiglutideAlbiglutide may increase the hypoglycemic activities of Gliclazide.
AlogliptinAlogliptin may increase the hypoglycemic activities of Gliclazide.
AlprenololAlprenolol may increase the hypoglycemic activities of Gliclazide.
Aminosalicylic AcidAminosalicylic Acid may increase the hypoglycemic activities of Gliclazide.
AmiodaroneThe metabolism of Gliclazide can be decreased when combined with Amiodarone.
AmoxapineAmoxapine may increase the hypoglycemic activities of Gliclazide.
AprepitantThe metabolism of Gliclazide can be increased when combined with Aprepitant.
AripiprazoleThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Aripiprazole.
ArmodafinilThe metabolism of Gliclazide can be decreased when combined with Armodafinil.
ArotinololArotinolol may increase the hypoglycemic activities of Gliclazide.
Arsenic trioxideThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Arsenic trioxide.
ArticaineThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Articaine.
AsenapineThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Asenapine.
AtazanavirThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Atazanavir.
AtenololAtenolol may increase the hypoglycemic activities of Gliclazide.
AtorvastatinAtorvastatin may increase the hypoglycemic activities of Gliclazide.
BefunololBefunolol may increase the hypoglycemic activities of Gliclazide.
BendroflumethiazideThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Bendroflumethiazide.
BenmoxinBenmoxin may increase the hypoglycemic activities of Gliclazide.
BetamethasoneThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Betamethasone.
BetaxololBetaxolol may increase the hypoglycemic activities of Gliclazide.
BevantololBevantolol may increase the hypoglycemic activities of Gliclazide.
BezafibrateBezafibrate may increase the hypoglycemic activities of Gliclazide.
BisoprololBisoprolol may increase the hypoglycemic activities of Gliclazide.
BopindololBopindolol may increase the hypoglycemic activities of Gliclazide.
BortezomibThe metabolism of Gliclazide can be decreased when combined with Bortezomib.
BrexpiprazoleThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Brexpiprazole.
BuforminBuformin may increase the hypoglycemic activities of Gliclazide.
BufuralolBufuralol may increase the hypoglycemic activities of Gliclazide.
BumetanideThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Bumetanide.
BupranololBupranolol may increase the hypoglycemic activities of Gliclazide.
BuserelinThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Buserelin.
CanagliflozinCanagliflozin may increase the hypoglycemic activities of Gliclazide.
CapecitabineThe metabolism of Gliclazide can be decreased when combined with Capecitabine.
CarbamazepineThe metabolism of Gliclazide can be increased when combined with Carbamazepine.
CarbocisteineThe risk or severity of adverse effects can be increased when Gliclazide is combined with Carbocisteine.
CaroxazoneCaroxazone may increase the hypoglycemic activities of Gliclazide.
CarteololCarteolol may increase the hypoglycemic activities of Gliclazide.
CarvedilolCarvedilol may increase the hypoglycemic activities of Gliclazide.
CastanospermineCastanospermine may increase the hypoglycemic activities of Gliclazide.
CeliprololCeliprolol may increase the hypoglycemic activities of Gliclazide.
CeritinibThe serum concentration of Gliclazide can be increased when it is combined with Ceritinib.
ChloramphenicolThe metabolism of Gliclazide can be decreased when combined with Chloramphenicol.
ChlorothiazideThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Chlorothiazide.
ChlorpropamideChlorpropamide may increase the hypoglycemic activities of Gliclazide.
ChlorthalidoneThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Chlorthalidone.
CholecalciferolThe metabolism of Gliclazide can be decreased when combined with Cholecalciferol.
CiglitazoneCiglitazone may increase the hypoglycemic activities of Gliclazide.
CilostazolThe serum concentration of Cilostazol can be increased when it is combined with Gliclazide.
CimetidineThe serum concentration of Gliclazide can be increased when it is combined with Cimetidine.
CiprofibrateCiprofibrate may increase the hypoglycemic activities of Gliclazide.
CitalopramCitalopram may increase the hypoglycemic activities of Gliclazide.
ClofibrateClofibrate may increase the hypoglycemic activities of Gliclazide.
ClomipramineClomipramine may increase the hypoglycemic activities of Gliclazide.
ClotrimazoleThe metabolism of Gliclazide can be decreased when combined with Clotrimazole.
ClozapineThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Clozapine.
CorticotropinThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Corticotropin.
Cortisone acetateThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Cortisone acetate.
CyclosporineThe metabolism of Gliclazide can be decreased when combined with Cyclosporine.
Cyproterone acetateThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Cyproterone acetate.
DabrafenibThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Dabrafenib.
DanazolThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Danazol.
DapoxetineDapoxetine may increase the hypoglycemic activities of Gliclazide.
DarunavirThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Darunavir.
DelavirdineThe metabolism of Gliclazide can be decreased when combined with Delavirdine.
DesogestrelThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Desogestrel.
DexamethasoneThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Dexamethasone.
DiazoxideThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Diazoxide.
DicoumarolGliclazide may increase the anticoagulant activities of Dicoumarol.
DienogestThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Dienogest.
DiflunisalDiflunisal may increase the hypoglycemic activities of Gliclazide.
DihydrotestosteroneDihydrotestosterone may increase the hypoglycemic activities of Gliclazide.
DisopyramideGliclazide may increase the hypoglycemic activities of Disopyramide.
DrospirenoneThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Drospirenone.
DulaglutideDulaglutide may increase the hypoglycemic activities of Gliclazide.
EfavirenzThe metabolism of Gliclazide can be decreased when combined with Efavirenz.
EmpagliflozinEmpagliflozin may increase the hypoglycemic activities of Gliclazide.
EpinephrineThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Epinephrine.
EscitalopramEscitalopram may increase the hypoglycemic activities of Gliclazide.
Eslicarbazepine acetateThe metabolism of Gliclazide can be decreased when combined with Eslicarbazepine acetate.
EsmololEsmolol may increase the hypoglycemic activities of Gliclazide.
EsomeprazoleThe metabolism of Gliclazide can be decreased when combined with Esomeprazole.
EstradiolThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Estradiol.
Estrone sulfateThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Estrone sulfate.
Etacrynic acidThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Etacrynic acid.
EthanolThe risk or severity of adverse effects can be increased when Gliclazide is combined with Ethanol.
Ethinyl EstradiolThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Ethinyl Estradiol.
Ethyl biscoumacetateGliclazide may increase the anticoagulant activities of Ethyl biscoumacetate.
Ethynodiol diacetateThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Ethynodiol diacetate.
EtofibrateEtofibrate may increase the hypoglycemic activities of Gliclazide.
EtonogestrelThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Etonogestrel.
EtoperidoneEtoperidone may increase the hypoglycemic activities of Gliclazide.
EtravirineThe metabolism of Gliclazide can be decreased when combined with Etravirine.
EverolimusThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Everolimus.
ExenatideExenatide may increase the hypoglycemic activities of Gliclazide.
FenfluramineFenfluramine may increase the hypoglycemic activities of Gliclazide.
FenofibrateFenofibrate may increase the hypoglycemic activities of Gliclazide.
FloxuridineThe metabolism of Gliclazide can be decreased when combined with Floxuridine.
FluconazoleThe metabolism of Gliclazide can be decreased when combined with Fluconazole.
FludrocortisoneThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Fludrocortisone.
FluorouracilThe metabolism of Gliclazide can be decreased when combined with Fluorouracil.
FluoxetineFluoxetine may increase the hypoglycemic activities of Gliclazide.
FluoxymesteroneFluoxymesterone may increase the hypoglycemic activities of Gliclazide.
FluvastatinThe metabolism of Gliclazide can be decreased when combined with Fluvastatin.
FluvoxamineFluvoxamine may increase the hypoglycemic activities of Gliclazide.
FosamprenavirThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Fosamprenavir.
FosphenytoinThe metabolism of Gliclazide can be increased when combined with Fosphenytoin.
FurazolidoneFurazolidone may increase the hypoglycemic activities of Gliclazide.
FurosemideThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Furosemide.
GemfibrozilGemfibrozil may increase the hypoglycemic activities of Gliclazide.
GlibornurideGlibornuride may increase the hypoglycemic activities of Gliclazide.
GlimepirideGlimepiride may increase the hypoglycemic activities of Gliclazide.
GlipizideGlipizide may increase the hypoglycemic activities of Gliclazide.
GliquidoneGliquidone may increase the hypoglycemic activities of Gliclazide.
GlyburideGlyburide may increase the hypoglycemic activities of Gliclazide.
GoserelinThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Goserelin.
HistrelinThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Histrelin.
HydracarbazineHydracarbazine may increase the hypoglycemic activities of Gliclazide.
HydrochlorothiazideThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Hydrochlorothiazide.
HydrocortisoneThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Hydrocortisone.
HydroflumethiazideThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Hydroflumethiazide.
Hydroxyprogesterone caproateThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Hydroxyprogesterone caproate.
IloperidoneThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Iloperidone.
IndalpineIndalpine may increase the hypoglycemic activities of Gliclazide.
IndapamideThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Indapamide.
IndenololIndenolol may increase the hypoglycemic activities of Gliclazide.
IndinavirThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Indinavir.
Insulin AspartGliclazide may increase the hypoglycemic activities of Insulin Aspart.
Insulin DetemirGliclazide may increase the hypoglycemic activities of Insulin Detemir.
Insulin GlargineInsulin Glargine may increase the hypoglycemic activities of Gliclazide.
Insulin GlulisineGliclazide may increase the hypoglycemic activities of Insulin Glulisine.
Insulin HumanGliclazide may increase the hypoglycemic activities of Insulin Human.
Insulin LisproInsulin Lispro may increase the hypoglycemic activities of Gliclazide.
Insulin PorkInsulin Pork may increase the hypoglycemic activities of Gliclazide.
IproclozideIproclozide may increase the hypoglycemic activities of Gliclazide.
IproniazidIproniazid may increase the hypoglycemic activities of Gliclazide.
IrbesartanThe metabolism of Gliclazide can be decreased when combined with Irbesartan.
IsocarboxazidIsocarboxazid may increase the hypoglycemic activities of Gliclazide.
IsoniazidThe metabolism of Gliclazide can be decreased when combined with Isoniazid.
KetoconazoleThe metabolism of Gliclazide can be decreased when combined with Ketoconazole.
LabetalolLabetalol may increase the hypoglycemic activities of Gliclazide.
LanreotideThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Lanreotide.
LanreotideGliclazide may increase the hypoglycemic activities of Lanreotide.
LeflunomideThe metabolism of Gliclazide can be decreased when combined with Leflunomide.
LeuprolideThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Leuprolide.
LevobunololLevobunolol may increase the hypoglycemic activities of Gliclazide.
LevomilnacipranLevomilnacipran may increase the hypoglycemic activities of Gliclazide.
LevonorgestrelThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Levonorgestrel.
LinagliptinLinagliptin may increase the hypoglycemic activities of Gliclazide.
Lipoic AcidLipoic Acid may increase the hypoglycemic activities of Gliclazide.
LiraglutideLiraglutide may increase the hypoglycemic activities of Gliclazide.
LopinavirThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Lopinavir.
LosartanThe metabolism of Gliclazide can be decreased when combined with Losartan.
LovastatinThe metabolism of Gliclazide can be decreased when combined with Lovastatin.
Lu AA21004Lu AA21004 may increase the hypoglycemic activities of Gliclazide.
LuliconazoleThe serum concentration of Gliclazide can be increased when it is combined with Luliconazole.
LumacaftorThe serum concentration of Gliclazide can be decreased when it is combined with Lumacaftor.
LurasidoneThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Lurasidone.
MebanazineMebanazine may increase the hypoglycemic activities of Gliclazide.
MecaserminGliclazide may increase the hypoglycemic activities of Mecasermin.
Medroxyprogesterone acetateThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Medroxyprogesterone acetate.
Megestrol acetateThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Megestrol acetate.
MesalazineMesalazine may increase the hypoglycemic activities of Gliclazide.
MestranolThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Mestranol.
MetforminMetformin may increase the hypoglycemic activities of Gliclazide.
MethotrimeprazineThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Methotrimeprazine.
MethyclothiazideThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Methyclothiazide.
Methylene blueMethylene blue may increase the hypoglycemic activities of Gliclazide.
MethylprednisoloneThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Methylprednisolone.
MethyltestosteroneMethyltestosterone may increase the hypoglycemic activities of Gliclazide.
MetipranololMetipranolol may increase the hypoglycemic activities of Gliclazide.
MetolazoneThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Metolazone.
MetoprololMetoprolol may increase the hypoglycemic activities of Gliclazide.
MetreleptinMetreleptin may increase the hypoglycemic activities of Gliclazide.
MiconazoleMiconazole may increase the hypoglycemic activities of Gliclazide.
MifepristoneGliclazide may increase the hypoglycemic activities of Mifepristone.
MiglitolMiglitol may increase the hypoglycemic activities of Gliclazide.
MiglustatMiglustat may increase the hypoglycemic activities of Gliclazide.
MilnacipranMilnacipran may increase the hypoglycemic activities of Gliclazide.
MinaprineMinaprine may increase the hypoglycemic activities of Gliclazide.
MitiglinideMitiglinide may increase the hypoglycemic activities of Gliclazide.
MoclobemideMoclobemide may increase the hypoglycemic activities of Gliclazide.
ModafinilThe metabolism of Gliclazide can be decreased when combined with Modafinil.
NadololNadolol may increase the hypoglycemic activities of Gliclazide.
NateglinideNateglinide may increase the hypoglycemic activities of Gliclazide.
NelfinavirThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Nelfinavir.
NiacinThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Niacin.
NialamideNialamide may increase the hypoglycemic activities of Gliclazide.
NicardipineThe metabolism of Gliclazide can be decreased when combined with Nicardipine.
NilotinibThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Nilotinib.
NorethisteroneThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Norethisterone.
NorgestimateThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Norgestimate.
OctamoxinOctamoxin may increase the hypoglycemic activities of Gliclazide.
OctreotideThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Octreotide.
OctreotideGliclazide may increase the hypoglycemic activities of Octreotide.
OlanzapineOlanzapine may increase the hypoglycemic activities of Gliclazide.
OmeprazoleThe metabolism of Gliclazide can be decreased when combined with Omeprazole.
OxandroloneOxandrolone may increase the hypoglycemic activities of Gliclazide.
OxprenololOxprenolol may increase the hypoglycemic activities of Gliclazide.
OxymetholoneOxymetholone may increase the hypoglycemic activities of Gliclazide.
PaliperidoneThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Paliperidone.
PantoprazoleThe metabolism of Gliclazide can be decreased when combined with Pantoprazole.
PargylinePargyline may increase the hypoglycemic activities of Gliclazide.
ParoxetineParoxetine may increase the hypoglycemic activities of Gliclazide.
PasireotideThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Pasireotide.
PasireotideGliclazide may increase the hypoglycemic activities of Pasireotide.
PegvisomantPegvisomant may increase the hypoglycemic activities of Gliclazide.
PenbutololPenbutolol may increase the hypoglycemic activities of Gliclazide.
PentamidineThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Pentamidine.
PentamidineGliclazide may increase the hypoglycemic activities of Pentamidine.
PhenelzinePhenelzine may increase the hypoglycemic activities of Gliclazide.
PhenforminPhenformin may increase the hypoglycemic activities of Gliclazide.
PhenindioneGliclazide may increase the anticoagulant activities of Phenindione.
PheniprazinePheniprazine may increase the hypoglycemic activities of Gliclazide.
PhenobarbitalThe metabolism of Gliclazide can be increased when combined with Phenobarbital.
PhenoxypropazinePhenoxypropazine may increase the hypoglycemic activities of Gliclazide.
PhenprocoumonGliclazide may increase the anticoagulant activities of Phenprocoumon.
PhenytoinThe metabolism of Gliclazide can be increased when combined with Phenytoin.
PindololPindolol may increase the hypoglycemic activities of Gliclazide.
PioglitazonePioglitazone may increase the hypoglycemic activities of Gliclazide.
PiperazineThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Piperazine.
PipotiazineThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Pipotiazine.
PirlindolePirlindole may increase the hypoglycemic activities of Gliclazide.
PivhydrazinePivhydrazine may increase the hypoglycemic activities of Gliclazide.
PolythiazideThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Polythiazide.
PractololPractolol may increase the hypoglycemic activities of Gliclazide.
PramlintidePramlintide may increase the hypoglycemic activities of Gliclazide.
PrednisoloneThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Prednisolone.
PrednisoneThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Prednisone.
PrimidoneThe metabolism of Gliclazide can be increased when combined with Primidone.
ProbenecidThe protein binding of Gliclazide can be decreased when combined with Probenecid.
ProgesteroneThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Progesterone.
PropranololPropranolol may increase the hypoglycemic activities of Gliclazide.
PyrimethamineThe metabolism of Gliclazide can be decreased when combined with Pyrimethamine.
QuetiapineThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Quetiapine.
QuinethazoneThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Quinethazone.
QuinineGliclazide may increase the hypoglycemic activities of Quinine.
RanitidineThe serum concentration of Gliclazide can be increased when it is combined with Ranitidine.
RasagilineRasagiline may increase the hypoglycemic activities of Gliclazide.
RepaglinideRepaglinide may increase the hypoglycemic activities of Gliclazide.
RifampicinThe serum concentration of Gliclazide can be decreased when it is combined with Rifampicin.
RifapentineThe metabolism of Gliclazide can be increased when combined with Rifapentine.
RisperidoneThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Risperidone.
RitonavirThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Ritonavir.
RosiglitazoneRosiglitazone may increase the hypoglycemic activities of Gliclazide.
SafrazineSafrazine may increase the hypoglycemic activities of Gliclazide.
Salicylic acidSalicylic acid may increase the hypoglycemic activities of Gliclazide.
SaquinavirThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Saquinavir.
SaxagliptinSaxagliptin may increase the hypoglycemic activities of Gliclazide.
SecobarbitalThe metabolism of Gliclazide can be increased when combined with Secobarbital.
SelegilineSelegiline may increase the hypoglycemic activities of Gliclazide.
SertralineSertraline may increase the hypoglycemic activities of Gliclazide.
SildenafilThe metabolism of Gliclazide can be decreased when combined with Sildenafil.
SirolimusThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Sirolimus.
SitagliptinSitagliptin may increase the hypoglycemic activities of Gliclazide.
SorafenibThe metabolism of Gliclazide can be decreased when combined with Sorafenib.
SotalolSotalol may increase the hypoglycemic activities of Gliclazide.
StanozololStanozolol may increase the hypoglycemic activities of Gliclazide.
StiripentolThe metabolism of Gliclazide can be decreased when combined with Stiripentol.
SulfadiazineSulfadiazine may increase the hypoglycemic activities of Gliclazide.
SulfamethoxazoleSulfamethoxazole may increase the hypoglycemic activities of Gliclazide.
SulfisoxazoleSulfisoxazole may increase the hypoglycemic activities of Gliclazide.
SulodexideSulodexide may increase the hypoglycemic activities of Gliclazide.
SunitinibGliclazide may increase the hypoglycemic activities of Sunitinib.
TacrolimusThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Tacrolimus.
TemsirolimusThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Temsirolimus.
TestosteroneTestosterone may increase the hypoglycemic activities of Gliclazide.
TicagrelorThe metabolism of Gliclazide can be decreased when combined with Ticagrelor.
TiclopidineThe metabolism of Gliclazide can be decreased when combined with Ticlopidine.
TimololTimolol may increase the hypoglycemic activities of Gliclazide.
TipranavirThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Tipranavir.
TolazamideTolazamide may increase the hypoglycemic activities of Gliclazide.
TolbutamideGliclazide may increase the hypoglycemic activities of Tolbutamide.
ToloxatoneToloxatone may increase the hypoglycemic activities of Gliclazide.
TopiramateThe metabolism of Gliclazide can be decreased when combined with Topiramate.
TorasemideThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Torasemide.
Trans-2-PhenylcyclopropylamineTrans-2-Phenylcyclopropylamine may increase the hypoglycemic activities of Gliclazide.
TranylcypromineTranylcypromine may increase the hypoglycemic activities of Gliclazide.
TrazodoneTrazodone may increase the hypoglycemic activities of Gliclazide.
TriamcinoloneThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Triamcinolone.
TrichlormethiazideThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Trichlormethiazide.
TrimethoprimThe metabolism of Gliclazide can be decreased when combined with Trimethoprim.
TriptorelinThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Triptorelin.
TroglitazoneTroglitazone may increase the hypoglycemic activities of Gliclazide.
Valproic AcidThe metabolism of Gliclazide can be decreased when combined with Valproic Acid.
ValsartanThe metabolism of Gliclazide can be decreased when combined with Valsartan.
VilazodoneVilazodone may increase the hypoglycemic activities of Gliclazide.
VildagliptinVildagliptin may increase the hypoglycemic activities of Gliclazide.
VogliboseVoglibose may increase the hypoglycemic activities of Gliclazide.
VoriconazoleThe serum concentration of Gliclazide can be increased when it is combined with Voriconazole.
VorinostatThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Vorinostat.
VortioxetineVortioxetine may increase the hypoglycemic activities of Gliclazide.
WarfarinGliclazide may increase the anticoagulant activities of Warfarin.
ZafirlukastThe metabolism of Gliclazide can be decreased when combined with Zafirlukast.
ZimelidineZimelidine may increase the hypoglycemic activities of Gliclazide.
ZiprasidoneThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Ziprasidone.
Food Interactions
  • Avoid alcohol.
  • Take without regard to meals. A consistent diet is recommended to reduce the risk of hypoglycemia.

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
binder
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. Gribble FM, Ashcroft FM: Sulfonylurea sensitivity of adenosine triphosphate-sensitive potassium channels from beta cells and extrapancreatic tissues. Metabolism. 2000 Oct;49(10 Suppl 2):3-6. [PubMed:11078468 ]
  2. Harrower A: Gliclazide modified release: from once-daily administration to 24-hour blood glucose control. Metabolism. 2000 Oct;49(10 Suppl 2):7-11. [PubMed:11078469 ]
  3. Lawrence CL, Proks P, Rodrigo GC, Jones P, Hayabuchi Y, Standen NB, Ashcroft FM: Gliclazide produces high-affinity block of KATP channels in mouse isolated pancreatic beta cells but not rat heart or arterial smooth muscle cells. Diabetologia. 2001 Aug;44(8):1019-25. [PubMed:11484080 ]
  4. Reimann F, Ashcroft FM, Gribble FM: Structural basis for the interference between nicorandil and sulfonylurea action. Diabetes. 2001 Oct;50(10):2253-9. [PubMed:11574406 ]
  5. Proks P, Reimann F, Green N, Gribble F, Ashcroft F: Sulfonylurea stimulation of insulin secretion. Diabetes. 2002 Dec;51 Suppl 3:S368-76. [PubMed:12475777 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
other/unknown
General Function:
Vascular endothelial growth factor receptor binding
Specific Function:
Growth factor active in angiogenesis, vasculogenesis and endothelial cell growth. Induces endothelial cell proliferation, promotes cell migration, inhibits apoptosis and induces permeabilization of blood vessels. Binds to the FLT1/VEGFR1 and KDR/VEGFR2 receptors, heparan sulfate and heparin. NRP1/Neuropilin-1 binds isoforms VEGF-165 and VEGF-145. Isoform VEGF165B binds to KDR but does not activ...
Gene Name:
VEGFA
Uniprot ID:
P15692
Molecular Weight:
27042.205 Da
References
  1. Mamputu JC, Renier G: Advanced glycation end products increase, through a protein kinase C-dependent pathway, vascular endothelial growth factor expression in retinal endothelial cells. Inhibitory effect of gliclazide. J Diabetes Complications. 2002 Jul-Aug;16(4):284-93. [PubMed:12126787 ]
  2. Mamputu JC, Renier G: Signalling pathways involved in retinal endothelial cell proliferation induced by advanced glycation end products: inhibitory effect of gliclazide. Diabetes Obes Metab. 2004 Mar;6(2):95-103. [PubMed:14746574 ]
  3. Li L, Renier G: Activation of nicotinamide adenine dinucleotide phosphate (reduced form) oxidase by advanced glycation end products links oxidative stress to altered retinal vascular endothelial growth factor expression. Metabolism. 2006 Nov;55(11):1516-23. [PubMed:17046555 ]
  4. Kimura T, Takagi H, Suzuma K, Kita M, Watanabe D, Yoshimura N: Comparisons between the beneficial effects of different sulphonylurea treatments on ischemia-induced retinal neovascularization. Free Radic Biol Med. 2007 Aug 1;43(3):454-61. Epub 2007 May 3. [PubMed:17602961 ]

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. 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. 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
substrateinhibitor
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. 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 ]

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
References
  1. Igaki A, Kobayashi K, Kimura M, Sakoguchi T, Matsuoka A: Influence of blood proteins on biomedical analysis. XII. Effects of glycation on gliclazide (oral hypoglycemic drug)-binding with serum albumin in diabetics. Chem Pharm Bull (Tokyo). 1992 Jan;40(1):255-7. [PubMed:1576681 ]
  2. Kobayashi K, Kimura M, Sakoguchi T, Hase A, Matsuoka A: Influence of blood proteins on biomedical analysis. V. Effect of ethyl alcohol on gliclazide-binding with bovine serum albumin. Chem Pharm Bull (Tokyo). 1982 Mar;30(3):1077-80. [PubMed:7094168 ]
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Drug created on June 13, 2005 07:24 / Updated on August 17, 2016 12:23