You are using an unsupported browser. Please upgrade your browser to a newer version to get the best experience on DrugBank.
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 release30 mgOralActavis Pharma Company2015-03-31Not applicableCanada
Act Gliclazide MrTablet, extended release60 mgOralActavis Pharma CompanyNot applicableNot applicableCanada
Ava-gliclazideTablet80 mgOralAvanstra Inc2011-08-112014-08-21Canada
DiamicronTablet80 mgOralServier Canada Inc1990-12-31Not applicableCanada
Diamicron MrTablet, extended release60 mgOralServier Canada Inc2010-12-09Not applicableCanada
Diamicron MrTablet, extended release30 mgOralServier Canada Inc2001-04-04Not 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 release60 mgOralMint Pharmaceuticals Inc2016-11-14Not applicableCanada
Mint-gliclazide MrTablet, extended release30 mgOralMint Pharmaceuticals Inc2014-06-02Not applicableCanada
Mylan-gliclazideTablet80 mgOralMylan Pharmaceuticals Ulc1998-08-13Not applicableCanada
Mylan-gliclazide MrTablet, extended release30 mgOralMylan Pharmaceuticals Ulc2015-08-07Not applicableCanada
Mylan-gliclazide MrTablet, extended release60 mgOralMylan Pharmaceuticals UlcNot applicableNot applicableCanada
Nu-gliclazideTablet80 mgOralNu Pharm IncNot applicableNot applicableCanada
PMS-gliclazideTablet80 mgOralPharmascience Inc2007-12-18Not applicableCanada
Ran-gliclazide MrTablet, extended release60 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 release60 mgOralApotex Inc2015-04-14Not applicableCanada
Apo-gliclazide MrTablet, extended release30 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 KeyBOVGTQGAOIONJV-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
Pharmacology
IndicationFor the treatment of NIDDM in conjunction with diet and exercise.
Structured Indications
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.
TargetKindPharmacological actionActionsOrganismUniProt ID
ATP-binding cassette sub-family C member 8Proteinyes
binder
HumanQ09428 details
Vascular endothelial growth factor AProteinunknown
other/unknown
HumanP15692 details
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
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 Gliclazide.Experimental
AbirateroneThe metabolism of Gliclazide can be decreased when combined with Abiraterone.Approved
AcarboseAcarbose may increase the hypoglycemic activities of Gliclazide.Approved, Investigational
AcebutololAcebutolol may increase the hypoglycemic activities of Gliclazide.Approved
AcenocoumarolGliclazide may increase the anticoagulant activities of Acenocoumarol.Approved
AcetohexamideAcetohexamide may increase the hypoglycemic activities of Gliclazide.Withdrawn
Acetylsalicylic acidAcetylsalicylic acid may increase the hypoglycemic activities of Gliclazide.Approved, Vet Approved
AicarAicar may increase the hypoglycemic activities of Gliclazide.Experimental
AlbiglutideAlbiglutide may increase the hypoglycemic activities of Gliclazide.Approved
AlogliptinAlogliptin may increase the hypoglycemic activities of Gliclazide.Approved
AlprenololAlprenolol may increase the hypoglycemic activities of Gliclazide.Approved, Withdrawn
Aminosalicylic AcidAminosalicylic Acid may increase the hypoglycemic activities of Gliclazide.Approved
AmiodaroneThe metabolism of Gliclazide can be decreased when combined with Amiodarone.Approved, Investigational
Aop200704Aop200704 may increase the hypoglycemic activities of Gliclazide.Investigational
AprepitantThe metabolism of Gliclazide can be increased when combined with Aprepitant.Approved, Investigational
AripiprazoleThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Aripiprazole.Approved, Investigational
ArmodafinilThe metabolism of Gliclazide can be decreased when combined with Armodafinil.Approved, Investigational
ArotinololArotinolol may increase the hypoglycemic activities of Gliclazide.Approved
Arsenic trioxideThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Arsenic trioxide.Approved, Investigational
ArticaineThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Articaine.Approved
AsenapineThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Asenapine.Approved
AtazanavirThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Atazanavir.Approved, Investigational
AtenololAtenolol may increase the hypoglycemic activities of Gliclazide.Approved
AtorvastatinAtorvastatin may increase the hypoglycemic activities of Gliclazide.Approved
BalaglitazoneBalaglitazone may increase the hypoglycemic activities of Gliclazide.Investigational
BalsalazideBalsalazide may increase the hypoglycemic activities of Gliclazide.Approved, Investigational
BefunololBefunolol may increase the hypoglycemic activities of Gliclazide.Experimental
BendroflumethiazideThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Bendroflumethiazide.Approved
BenmoxinBenmoxin may increase the hypoglycemic activities of Gliclazide.Withdrawn
BetamethasoneThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Betamethasone.Approved, Vet Approved
BetaxololBetaxolol may increase the hypoglycemic activities of Gliclazide.Approved
BevantololBevantolol may increase the hypoglycemic activities of Gliclazide.Approved
BezafibrateBezafibrate may increase the hypoglycemic activities of Gliclazide.Approved
BisoprololBisoprolol may increase the hypoglycemic activities of Gliclazide.Approved
BopindololBopindolol may increase the hypoglycemic activities of Gliclazide.Approved
BortezomibThe metabolism of Gliclazide can be decreased when combined with Bortezomib.Approved, Investigational
BrexpiprazoleThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Brexpiprazole.Approved
BucindololBucindolol may increase the hypoglycemic activities of Gliclazide.Investigational
BuforminBuformin may increase the hypoglycemic activities of Gliclazide.Withdrawn
BufuralolBufuralol may increase the hypoglycemic activities of Gliclazide.Experimental, Investigational
BumetanideThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Bumetanide.Approved
BupranololBupranolol may increase the hypoglycemic activities of Gliclazide.Approved
BuserelinThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Buserelin.Approved
CanagliflozinCanagliflozin may increase the hypoglycemic activities of Gliclazide.Approved
CapecitabineThe metabolism of Gliclazide can be decreased when combined with Capecitabine.Approved, Investigational
CarbamazepineThe metabolism of Gliclazide can be increased when combined with Carbamazepine.Approved, Investigational
CarbocisteineThe risk or severity of adverse effects can be increased when Gliclazide is combined with Carbocisteine.Approved
CaroxazoneCaroxazone may increase the hypoglycemic activities of Gliclazide.Withdrawn
CarteololCarteolol may increase the hypoglycemic activities of Gliclazide.Approved
CarvedilolCarvedilol may increase the hypoglycemic activities of Gliclazide.Approved, Investigational
CastanospermineCastanospermine may increase the hypoglycemic activities of Gliclazide.Experimental
CeliprololCeliprolol may increase the hypoglycemic activities of Gliclazide.Approved, Investigational
CeritinibThe serum concentration of Gliclazide can be increased when it is combined with Ceritinib.Approved
ChloramphenicolThe metabolism of Gliclazide can be decreased when combined with Chloramphenicol.Approved, Vet Approved
ChlorothiazideThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Chlorothiazide.Approved, Vet Approved
ChlorpropamideChlorpropamide may increase the hypoglycemic activities of Gliclazide.Approved
ChlorthalidoneThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Chlorthalidone.Approved
CholecalciferolThe metabolism of Gliclazide can be decreased when combined with Cholecalciferol.Approved, Nutraceutical
CiglitazoneCiglitazone may increase the hypoglycemic activities of Gliclazide.Experimental
CilostazolThe serum concentration of Cilostazol can be increased when it is combined with Gliclazide.Approved
CimetidineThe serum concentration of Gliclazide can be increased when it is combined with Cimetidine.Approved
CinoxacinCinoxacin may increase the hypoglycemic activities of Gliclazide.Approved, Withdrawn
CiprofibrateCiprofibrate may increase the hypoglycemic activities of Gliclazide.Approved
CiprofloxacinCiprofloxacin may increase the hypoglycemic activities of Gliclazide.Approved, Investigational
CitalopramThe metabolism of Gliclazide can be decreased when combined with Citalopram.Approved
ClofibrateClofibrate may increase the hypoglycemic activities of Gliclazide.Approved
ClotrimazoleThe metabolism of Gliclazide can be decreased when combined with Clotrimazole.Approved, Vet Approved
ClozapineThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Clozapine.Approved
CorticotropinThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Corticotropin.Approved, Vet Approved
Cortisone acetateThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Cortisone acetate.Approved
CyclosporineThe metabolism of Gliclazide can be decreased when combined with Cyclosporine.Approved, Investigational, Vet Approved
Cyproterone acetateThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Cyproterone acetate.Approved, Investigational
DabrafenibThe serum concentration of Gliclazide can be decreased when it is combined with Dabrafenib.Approved
DanazolThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Danazol.Approved
DapoxetineDapoxetine may increase the hypoglycemic activities of Gliclazide.Investigational
DarunavirThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Darunavir.Approved
DelavirdineThe metabolism of Gliclazide can be decreased when combined with Delavirdine.Approved
DeoxyspergualinDeoxyspergualin may increase the hypoglycemic activities of Gliclazide.Investigational
dersalazinedersalazine may increase the hypoglycemic activities of Gliclazide.Investigational
DesogestrelThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Desogestrel.Approved
DesvenlafaxineDesvenlafaxine may increase the hypoglycemic activities of Gliclazide.Approved
DexamethasoneThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Dexamethasone.Approved, Investigational, Vet Approved
DiazoxideThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Diazoxide.Approved
DicoumarolGliclazide may increase the anticoagulant activities of Dicoumarol.Approved
DienogestThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Dienogest.Approved
DiflunisalDiflunisal may increase the hypoglycemic activities of Gliclazide.Approved
DihydrotestosteroneDihydrotestosterone may increase the hypoglycemic activities of Gliclazide.Illicit
DisopyramideDisopyramide may increase the hypoglycemic activities of Gliclazide.Approved
DrospirenoneThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Drospirenone.Approved
DulaglutideDulaglutide may increase the hypoglycemic activities of Gliclazide.Approved
DuloxetineDuloxetine may increase the hypoglycemic activities of Gliclazide.Approved
EfavirenzThe metabolism of Gliclazide can be decreased when combined with Efavirenz.Approved, Investigational
EmpagliflozinEmpagliflozin may increase the hypoglycemic activities of Gliclazide.Approved
EnoxacinEnoxacin may increase the hypoglycemic activities of Gliclazide.Approved
EpinephrineThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Epinephrine.Approved, Vet Approved
EscitalopramEscitalopram may increase the hypoglycemic activities of Gliclazide.Approved, Investigational
Eslicarbazepine acetateThe metabolism of Gliclazide can be decreased when combined with Eslicarbazepine acetate.Approved
EsmololEsmolol may increase the hypoglycemic activities of Gliclazide.Approved
EsomeprazoleThe metabolism of Gliclazide can be decreased when combined with Esomeprazole.Approved, Investigational
EstradiolThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Estradiol.Approved, Investigational, Vet Approved
Estrone sulfateThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Estrone sulfate.Approved
Etacrynic acidThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Etacrynic acid.Approved
EthanolThe risk or severity of adverse effects can be increased when Gliclazide is combined with Ethanol.Approved
Ethinyl EstradiolThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Ethinyl Estradiol.Approved
Ethyl biscoumacetateGliclazide may increase the anticoagulant activities of Ethyl biscoumacetate.Withdrawn
Ethynodiol diacetateThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Ethynodiol diacetate.Approved
EtofibrateEtofibrate may increase the hypoglycemic activities of Gliclazide.Approved
EtonogestrelThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Etonogestrel.Approved, Investigational
EtoperidoneEtoperidone may increase the hypoglycemic activities of Gliclazide.Approved
EtravirineThe metabolism of Gliclazide can be decreased when combined with Etravirine.Approved
EverolimusThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Everolimus.Approved
ExenatideExenatide may increase the hypoglycemic activities of Gliclazide.Approved, Investigational
FenofibrateFenofibrate may increase the hypoglycemic activities of Gliclazide.Approved
FleroxacinFleroxacin may increase the hypoglycemic activities of Gliclazide.Approved
FloxuridineThe metabolism of Gliclazide can be decreased when combined with Floxuridine.Approved
FluconazoleThe serum concentration of Gliclazide can be increased when it is combined with Fluconazole.Approved
FludrocortisoneThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Fludrocortisone.Approved
FluindioneGliclazide may increase the anticoagulant activities of Fluindione.Investigational
FlumequineFlumequine may increase the hypoglycemic activities of Gliclazide.Withdrawn
FluorouracilThe metabolism of Gliclazide can be decreased when combined with Fluorouracil.Approved
FluoxetineThe metabolism of Gliclazide can be decreased when combined with Fluoxetine.Approved, Vet Approved
FluoxymesteroneFluoxymesterone may increase the hypoglycemic activities of Gliclazide.Approved, Illicit
FluvastatinThe metabolism of Gliclazide can be decreased when combined with Fluvastatin.Approved
FluvoxamineThe metabolism of Gliclazide can be decreased when combined with Fluvoxamine.Approved, Investigational
FosamprenavirThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Fosamprenavir.Approved
FosphenytoinThe metabolism of Gliclazide can be increased when combined with Fosphenytoin.Approved
FurazolidoneFurazolidone may increase the hypoglycemic activities of Gliclazide.Approved, Vet Approved
FurosemideThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Furosemide.Approved, Vet Approved
GarenoxacinGarenoxacin may increase the hypoglycemic activities of Gliclazide.Investigational
GatifloxacinGatifloxacin may increase the hypoglycemic activities of Gliclazide.Approved, Investigational
GemfibrozilThe metabolism of Gliclazide can be decreased when combined with Gemfibrozil.Approved
GemifloxacinGemifloxacin may increase the hypoglycemic activities of Gliclazide.Approved, Investigational
GlibornurideGlibornuride may increase the hypoglycemic activities of Gliclazide.Withdrawn
GlimepirideGlimepiride may increase the hypoglycemic activities of Gliclazide.Approved
GlipizideGlipizide may increase the hypoglycemic activities of Gliclazide.Approved
GliquidoneGliquidone may increase the hypoglycemic activities of Gliclazide.Approved
GlyburideGlyburide may increase the hypoglycemic activities of Gliclazide.Approved
GoserelinThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Goserelin.Approved
GrepafloxacinGrepafloxacin may increase the hypoglycemic activities of Gliclazide.Withdrawn
GusperimusGusperimus may increase the hypoglycemic activities of Gliclazide.Investigational
HistrelinThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Histrelin.Approved
HydracarbazineHydracarbazine may increase the hypoglycemic activities of Gliclazide.Approved
HydrochlorothiazideThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Hydrochlorothiazide.Approved, Vet Approved
HydrocortisoneThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Hydrocortisone.Approved, Vet Approved
HydroflumethiazideThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Hydroflumethiazide.Approved
Hydroxyprogesterone caproateThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Hydroxyprogesterone caproate.Approved
IloperidoneThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Iloperidone.Approved
IndalpineIndalpine may increase the hypoglycemic activities of Gliclazide.Investigational, Withdrawn
IndapamideThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Indapamide.Approved
IndenololIndenolol may increase the hypoglycemic activities of Gliclazide.Withdrawn
IndinavirThe metabolism of Gliclazide can be decreased when combined with Indinavir.Approved
Insulin AspartGliclazide may increase the hypoglycemic activities of Insulin Aspart.Approved
Insulin DetemirGliclazide may increase the hypoglycemic activities of Insulin Detemir.Approved
Insulin GlargineInsulin Glargine may increase the hypoglycemic activities of Gliclazide.Approved
Insulin GlulisineGliclazide may increase the hypoglycemic activities of Insulin Glulisine.Approved
Insulin HumanInsulin Human may increase the hypoglycemic activities of Gliclazide.Approved, Investigational
Insulin LisproInsulin Lispro may increase the hypoglycemic activities of Gliclazide.Approved
Insulin PorkInsulin Pork may increase the hypoglycemic activities of Gliclazide.Approved
IproclozideIproclozide may increase the hypoglycemic activities of Gliclazide.Withdrawn
IproniazidIproniazid may increase the hypoglycemic activities of Gliclazide.Withdrawn
IrbesartanThe metabolism of Gliclazide can be decreased when combined with Irbesartan.Approved, Investigational
IsocarboxazidIsocarboxazid may increase the hypoglycemic activities of Gliclazide.Approved
IsoniazidThe metabolism of Gliclazide can be decreased when combined with Isoniazid.Approved
KetoconazoleThe metabolism of Gliclazide can be decreased when combined with Ketoconazole.Approved, Investigational
LabetalolLabetalol may increase the hypoglycemic activities of Gliclazide.Approved
LanreotideGliclazide may increase the hypoglycemic activities of Lanreotide.Approved
LeflunomideThe metabolism of Gliclazide can be decreased when combined with Leflunomide.Approved, Investigational
LeuprolideThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Leuprolide.Approved, Investigational
LevobunololLevobunolol may increase the hypoglycemic activities of Gliclazide.Approved
LevofloxacinLevofloxacin may increase the hypoglycemic activities of Gliclazide.Approved, Investigational
LevomilnacipranLevomilnacipran may increase the hypoglycemic activities of Gliclazide.Approved
LevonorgestrelThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Levonorgestrel.Approved, Investigational
LinagliptinLinagliptin may increase the hypoglycemic activities of Gliclazide.Approved
Lipoic AcidLipoic Acid may increase the hypoglycemic activities of Gliclazide.Approved, Nutraceutical
LiraglutideLiraglutide may increase the hypoglycemic activities of Gliclazide.Approved
LomefloxacinLomefloxacin may increase the hypoglycemic activities of Gliclazide.Approved
LopinavirThe metabolism of Gliclazide can be increased when combined with Lopinavir.Approved
LosartanThe metabolism of Gliclazide can be decreased when combined with Losartan.Approved
LovastatinThe metabolism of Gliclazide can be decreased when combined with Lovastatin.Approved, Investigational
LuliconazoleThe serum concentration of Gliclazide can be increased when it is combined with Luliconazole.Approved
LumacaftorThe serum concentration of Gliclazide can be decreased when it is combined with Lumacaftor.Approved
LurasidoneThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Lurasidone.Approved
MebanazineMebanazine may increase the hypoglycemic activities of Gliclazide.Withdrawn
MecaserminGliclazide may increase the hypoglycemic activities of Mecasermin.Approved, Investigational
Medroxyprogesterone acetateThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Medroxyprogesterone acetate.Approved, Investigational
Megestrol acetateThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Megestrol acetate.Approved, Vet Approved
MesalazineMesalazine may increase the hypoglycemic activities of Gliclazide.Approved
MestranolThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Mestranol.Approved
MetforminMetformin may increase the hypoglycemic activities of Gliclazide.Approved
MethotrimeprazineThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Methotrimeprazine.Approved
MethyclothiazideThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Methyclothiazide.Approved
Methylene blueMethylene blue may increase the hypoglycemic activities of Gliclazide.Investigational
MethylprednisoloneThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Methylprednisolone.Approved, Vet Approved
MethyltestosteroneMethyltestosterone may increase the hypoglycemic activities of Gliclazide.Approved
MetipranololMetipranolol may increase the hypoglycemic activities of Gliclazide.Approved
MetolazoneThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Metolazone.Approved
MetoprololMetoprolol may increase the hypoglycemic activities of Gliclazide.Approved, Investigational
MetreleptinMetreleptin may increase the hypoglycemic activities of Gliclazide.Approved
MiconazoleMiconazole may increase the hypoglycemic activities of Gliclazide.Approved, Investigational, Vet Approved
MifepristoneThe serum concentration of Gliclazide can be increased when it is combined with Mifepristone.Approved, Investigational
MiglitolMiglitol may increase the hypoglycemic activities of Gliclazide.Approved
MiglustatMiglustat may increase the hypoglycemic activities of Gliclazide.Approved
MilnacipranMilnacipran may increase the hypoglycemic activities of Gliclazide.Approved
MinaprineMinaprine may increase the hypoglycemic activities of Gliclazide.Approved
MitiglinideMitiglinide may increase the hypoglycemic activities of Gliclazide.Approved, Investigational
MoclobemideMoclobemide may increase the hypoglycemic activities of Gliclazide.Approved
ModafinilThe metabolism of Gliclazide can be decreased when combined with Modafinil.Approved, Investigational
MoxifloxacinMoxifloxacin may increase the hypoglycemic activities of Gliclazide.Approved, Investigational
NadololNadolol may increase the hypoglycemic activities of Gliclazide.Approved
Nalidixic AcidNalidixic Acid may increase the hypoglycemic activities of Gliclazide.Approved
NateglinideNateglinide may increase the hypoglycemic activities of Gliclazide.Approved, Investigational
NCX 4016NCX 4016 may increase the hypoglycemic activities of Gliclazide.Investigational
NefazodoneNefazodone may increase the hypoglycemic activities of Gliclazide.Approved, Withdrawn
NelfinavirThe metabolism of Gliclazide can be decreased when combined with Nelfinavir.Approved
NemonoxacinNemonoxacin may increase the hypoglycemic activities of Gliclazide.Investigational
NiacinThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Niacin.Approved, Investigational, Nutraceutical
NialamideNialamide may increase the hypoglycemic activities of Gliclazide.Withdrawn
NicardipineThe metabolism of Gliclazide can be decreased when combined with Nicardipine.Approved
NilotinibThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Nilotinib.Approved, Investigational
NitroaspirinNitroaspirin may increase the hypoglycemic activities of Gliclazide.Investigational
NorethisteroneThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Norethisterone.Approved
NorfloxacinNorfloxacin may increase the hypoglycemic activities of Gliclazide.Approved
NorgestimateThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Norgestimate.Approved
OctamoxinOctamoxin may increase the hypoglycemic activities of Gliclazide.Withdrawn
OctreotideOctreotide may increase the hypoglycemic activities of Gliclazide.Approved, Investigational
OfloxacinOfloxacin may increase the hypoglycemic activities of Gliclazide.Approved
OlanzapineThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Olanzapine.Approved, Investigational
OlsalazineOlsalazine may increase the hypoglycemic activities of Gliclazide.Approved
OmeprazoleThe metabolism of Gliclazide can be decreased when combined with Omeprazole.Approved, Investigational, Vet Approved
OxandroloneOxandrolone may increase the hypoglycemic activities of Gliclazide.Approved, Investigational
OxprenololOxprenolol may increase the hypoglycemic activities of Gliclazide.Approved
OxymetholoneOxymetholone may increase the hypoglycemic activities of Gliclazide.Approved, Illicit
PaliperidoneThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Paliperidone.Approved
PantoprazoleThe metabolism of Gliclazide can be decreased when combined with Pantoprazole.Approved
PargylinePargyline may increase the hypoglycemic activities of Gliclazide.Approved
ParoxetineParoxetine may increase the hypoglycemic activities of Gliclazide.Approved, Investigational
PasireotideGliclazide may increase the hypoglycemic activities of Pasireotide.Approved
PazufloxacinPazufloxacin may increase the hypoglycemic activities of Gliclazide.Investigational
PefloxacinPefloxacin may increase the hypoglycemic activities of Gliclazide.Approved
PegvisomantPegvisomant may increase the hypoglycemic activities of Gliclazide.Approved
PenbutololPenbutolol may increase the hypoglycemic activities of Gliclazide.Approved, Investigational
PentamidinePentamidine may increase the hypoglycemic activities of Gliclazide.Approved
PhenelzinePhenelzine may increase the hypoglycemic activities of Gliclazide.Approved
PhenforminPhenformin may increase the hypoglycemic activities of Gliclazide.Approved, Withdrawn
PhenindioneGliclazide may increase the anticoagulant activities of Phenindione.Approved
PheniprazinePheniprazine may increase the hypoglycemic activities of Gliclazide.Withdrawn
PhenobarbitalThe metabolism of Gliclazide can be increased when combined with Phenobarbital.Approved
PhenoxypropazinePhenoxypropazine may increase the hypoglycemic activities of Gliclazide.Withdrawn
PhenprocoumonGliclazide may increase the anticoagulant activities of Phenprocoumon.Approved
PhenytoinThe metabolism of Gliclazide can be increased when combined with Phenytoin.Approved, Vet Approved
PindololPindolol may increase the hypoglycemic activities of Gliclazide.Approved
PioglitazonePioglitazone may increase the hypoglycemic activities of Gliclazide.Approved, Investigational
PiperazineThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Piperazine.Approved, Vet Approved
PipotiazineThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Pipotiazine.Approved
PirlindolePirlindole may increase the hypoglycemic activities of Gliclazide.Approved
PivhydrazinePivhydrazine may increase the hypoglycemic activities of Gliclazide.Withdrawn
PolythiazideThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Polythiazide.Approved
PractololPractolol may increase the hypoglycemic activities of Gliclazide.Approved
PramlintidePramlintide may increase the hypoglycemic activities of Gliclazide.Approved, Investigational
PrednisoloneThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Prednisolone.Approved, Vet Approved
PrednisoneThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Prednisone.Approved, Vet Approved
PrimidoneThe metabolism of Gliclazide can be increased when combined with Primidone.Approved, Vet Approved
ProbenecidThe protein binding of Gliclazide can be decreased when combined with Probenecid.Approved
ProgesteroneThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Progesterone.Approved, Vet Approved
PropranololPropranolol may increase the hypoglycemic activities of Gliclazide.Approved, Investigational
PrulifloxacinPrulifloxacin may increase the hypoglycemic activities of Gliclazide.Investigational
PyrimethamineThe metabolism of Gliclazide can be decreased when combined with Pyrimethamine.Approved, Vet Approved
QuetiapineThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Quetiapine.Approved
QuinethazoneThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Quinethazone.Approved
QuinineQuinine may increase the hypoglycemic activities of Gliclazide.Approved
RanitidineThe serum concentration of Gliclazide can be increased when it is combined with Ranitidine.Approved
RasagilineRasagiline may increase the hypoglycemic activities of Gliclazide.Approved
RepaglinideRepaglinide may increase the hypoglycemic activities of Gliclazide.Approved, Investigational
RifampicinThe serum concentration of Gliclazide can be decreased when it is combined with Rifampicin.Approved
RifapentineThe metabolism of Gliclazide can be increased when combined with Rifapentine.Approved
RisperidoneThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Risperidone.Approved, Investigational
RitonavirThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Ritonavir.Approved, Investigational
RosiglitazoneRosiglitazone may increase the hypoglycemic activities of Gliclazide.Approved, Investigational
RosoxacinRosoxacin may increase the hypoglycemic activities of Gliclazide.Approved
SafrazineSafrazine may increase the hypoglycemic activities of Gliclazide.Withdrawn
Salicylic acidSalicylic acid may increase the hypoglycemic activities of Gliclazide.Approved, Vet Approved
SaquinavirThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Saquinavir.Approved, Investigational
SaxagliptinSaxagliptin may increase the hypoglycemic activities of Gliclazide.Approved
SecobarbitalThe metabolism of Gliclazide can be increased when combined with Secobarbital.Approved, Vet Approved
SelegilineSelegiline may increase the hypoglycemic activities of Gliclazide.Approved, Investigational, Vet Approved
SertralineThe metabolism of Gliclazide can be decreased when combined with Sertraline.Approved
SildenafilThe metabolism of Gliclazide can be decreased when combined with Sildenafil.Approved, Investigational
SirolimusThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Sirolimus.Approved, Investigational
SitagliptinSitagliptin may increase the hypoglycemic activities of Gliclazide.Approved, Investigational
SorafenibThe metabolism of Gliclazide can be decreased when combined with Sorafenib.Approved, Investigational
SotalolSotalol may increase the hypoglycemic activities of Gliclazide.Approved
SparfloxacinSparfloxacin may increase the hypoglycemic activities of Gliclazide.Approved
StanozololStanozolol may increase the hypoglycemic activities of Gliclazide.Approved, Vet Approved
StiripentolThe metabolism of Gliclazide can be decreased when combined with Stiripentol.Approved
SulfadiazineThe metabolism of Gliclazide can be decreased when combined with Sulfadiazine.Approved, Vet Approved
SulfamethoxazoleSulfamethoxazole may increase the hypoglycemic activities of Gliclazide.Approved
SulfisoxazoleThe metabolism of Gliclazide can be decreased when combined with Sulfisoxazole.Approved, Vet Approved
SulodexideSulodexide may increase the hypoglycemic activities of Gliclazide.Approved, Investigational
SunitinibGliclazide may increase the hypoglycemic activities of Sunitinib.Approved, Investigational
TacrolimusThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Tacrolimus.Approved, Investigational
TemafloxacinTemafloxacin may increase the hypoglycemic activities of Gliclazide.Withdrawn
TemsirolimusThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Temsirolimus.Approved
TestosteroneTestosterone may increase the hypoglycemic activities of Gliclazide.Approved, Investigational
ThiazolidinedioneThiazolidinedione may increase the hypoglycemic activities of Gliclazide.Investigational
TicagrelorThe metabolism of Gliclazide can be decreased when combined with Ticagrelor.Approved
TiclopidineThe metabolism of Gliclazide can be decreased when combined with Ticlopidine.Approved
TimololTimolol may increase the hypoglycemic activities of Gliclazide.Approved
TipranavirThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Tipranavir.Approved, Investigational
TolazamideTolazamide may increase the hypoglycemic activities of Gliclazide.Approved
TolbutamideThe metabolism of Gliclazide can be decreased when combined with Tolbutamide.Approved
ToloxatoneToloxatone may increase the hypoglycemic activities of Gliclazide.Approved
TopiramateThe metabolism of Gliclazide can be decreased when combined with Topiramate.Approved
TorasemideThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Torasemide.Approved
Trans-2-PhenylcyclopropylamineTrans-2-Phenylcyclopropylamine may increase the hypoglycemic activities of Gliclazide.Experimental
TranylcypromineTranylcypromine may increase the hypoglycemic activities of Gliclazide.Approved
TriamcinoloneThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Triamcinolone.Approved, Vet Approved
TrichlormethiazideThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Trichlormethiazide.Approved, Vet Approved
TrimethoprimThe metabolism of Gliclazide can be decreased when combined with Trimethoprim.Approved, Vet Approved
TriptorelinThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Triptorelin.Approved, Vet Approved
TroglitazoneTroglitazone may increase the hypoglycemic activities of Gliclazide.Withdrawn
TrovafloxacinTrovafloxacin may increase the hypoglycemic activities of Gliclazide.Approved, Withdrawn
Valproic AcidThe metabolism of Gliclazide can be decreased when combined with Valproic Acid.Approved, Investigational
ValsartanThe metabolism of Gliclazide can be decreased when combined with Valsartan.Approved, Investigational
VenlafaxineVenlafaxine may increase the hypoglycemic activities of Gliclazide.Approved
VildagliptinVildagliptin may increase the hypoglycemic activities of Gliclazide.Approved, Investigational
VogliboseVoglibose may increase the hypoglycemic activities of Gliclazide.Approved, Investigational
VoriconazoleThe serum concentration of Gliclazide can be increased when it is combined with Voriconazole.Approved, Investigational
VorinostatThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Vorinostat.Approved, Investigational
WarfarinGliclazide may increase the anticoagulant activities of Warfarin.Approved
ZafirlukastThe metabolism of Gliclazide can be decreased when combined with Zafirlukast.Approved, Investigational
ZimelidineZimelidine may increase the hypoglycemic activities of Gliclazide.Withdrawn
ZiprasidoneThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Ziprasidone.Approved
Food Interactions
  • Avoid alcohol.
  • Take without regard to meals. A consistent diet is recommended to reduce the risk of hypoglycemia.
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)
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 releaseOral60 mg
Tablet, extended releaseOral30 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
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

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 ]
Comments
comments powered by Disqus
Drug created on June 13, 2005 07:24 / Updated on August 17, 2016 12:23