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Identification
NameGliclazide
Accession NumberDB01120  (APRD00460)
TypeSmall Molecule
GroupsApproved
Description

Gliclazide 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
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Act Gliclazide Mrtablet (extended-release)30 mgoralActavis Pharma Company2015-03-31Not applicableCanada 5f16b84899037e23705f146ff57e3794121879cb055f0954756d94bc690476b4
Act Gliclazide Mrtablet (extended-release)60 mgoralActavis Pharma CompanyNot applicableNot applicableCanada 5f16b84899037e23705f146ff57e3794121879cb055f0954756d94bc690476b4
Ava-gliclazidetablet80 mgoralAvanstra Inc2011-08-112014-08-21Canada 5f16b84899037e23705f146ff57e3794121879cb055f0954756d94bc690476b4
Diamicron Mrtablet (extended-release)30 mgoralServier Canada Inc2001-04-04Not applicableCanada 5f16b84899037e23705f146ff57e3794121879cb055f0954756d94bc690476b4
Diamicron Mrtablet (extended-release)60 mgoralServier Canada Inc2010-12-09Not applicableCanada 5f16b84899037e23705f146ff57e3794121879cb055f0954756d94bc690476b4
Diamicron Tab 80mgtablet80 mgoralServier Canada Inc1990-12-31Not applicableCanada 5f16b84899037e23705f146ff57e3794121879cb055f0954756d94bc690476b4
Glictablet80 mgoralPrempharm Inc2003-10-022005-08-05Canada 5f16b84899037e23705f146ff57e3794121879cb055f0954756d94bc690476b4
Gliclazidetablet80 mgoralSanis Health Inc2010-02-25Not applicableCanada 5f16b84899037e23705f146ff57e3794121879cb055f0954756d94bc690476b4
Gliclazide -tab 80mgtablet80 mgoralProval Pharma Division Of Servier Canada Inc1997-08-132012-02-13Canada 5f16b84899037e23705f146ff57e3794121879cb055f0954756d94bc690476b4
Gliclazide-80tablet80 mgoralPro Doc Limitee2003-12-10Not applicableCanada 5f16b84899037e23705f146ff57e3794121879cb055f0954756d94bc690476b4
Mint-gliclazide Mrtablet (extended-release)30 mgoralMint Pharmaceuticals Inc2014-06-02Not applicableCanada 5f16b84899037e23705f146ff57e3794121879cb055f0954756d94bc690476b4
Mint-gliclazide Mrtablet (extended-release)60 mgoralMint Pharmaceuticals IncNot applicableNot applicableCanada 5f16b84899037e23705f146ff57e3794121879cb055f0954756d94bc690476b4
Mylan-gliclazidetablet80 mgoralMylan Pharmaceuticals Ulc1998-08-13Not applicableCanada 5f16b84899037e23705f146ff57e3794121879cb055f0954756d94bc690476b4
Mylan-gliclazide Mrtablet (extended-release)30 mgoralMylan Pharmaceuticals Ulc2015-08-07Not applicableCanada 5f16b84899037e23705f146ff57e3794121879cb055f0954756d94bc690476b4
Nu-gliclazidetablet80 mgoralNu Pharm IncNot applicableNot applicableCanada 5f16b84899037e23705f146ff57e3794121879cb055f0954756d94bc690476b4
PMS-gliclazidetablet80 mgoralPharmascience Inc2007-12-18Not applicableCanada 5f16b84899037e23705f146ff57e3794121879cb055f0954756d94bc690476b4
Ran-gliclazide Mrtablet (extended-release)60 mgoralRanbaxy Pharmaceuticals Canada Inc.Not applicableNot applicableCanada 5f16b84899037e23705f146ff57e3794121879cb055f0954756d94bc690476b4
Sandoz Gliclazidetablet80 mgoralSandoz Canada Incorporated2004-08-092008-08-07Canada 5f16b84899037e23705f146ff57e3794121879cb055f0954756d94bc690476b4
Teva-gliclazidetablet80 mgoralTeva Canada Limited1998-06-08Not applicableCanada 5f16b84899037e23705f146ff57e3794121879cb055f0954756d94bc690476b4
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Apo-gliclazidetablet80 mgoralApotex Inc2002-07-02Not applicableCanada 5f16b84899037e23705f146ff57e3794121879cb055f0954756d94bc690476b4
Apo-gliclazide Mrtablet (extended-release)60 mgoralApotex Inc2015-04-14Not applicableCanada 5f16b84899037e23705f146ff57e3794121879cb055f0954756d94bc690476b4
Apo-gliclazide Mrtablet (extended-release)30 mgoralApotex Inc2008-06-04Not applicableCanada 5f16b84899037e23705f146ff57e3794121879cb055f0954756d94bc690476b4
Over the Counter ProductsNot 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.
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
PathwaysNot Available
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
CountryPatent NumberApprovedExpires (estimated)
Canada22734202002-07-092019-05-27
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
AcetohexamideAcetohexamide may increase the hypoglycemic activities of Gliclazide.
Acetylsalicylic acidAcetylsalicylic acid may increase the hypoglycemic activities of Gliclazide.
AlogliptinAlogliptin may increase the hypoglycemic activities of Gliclazide.
AmitriptylineAmitriptyline may increase the hypoglycemic activities of Gliclazide.
AripiprazoleThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Aripiprazole.
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.
BendroflumethiazideThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Bendroflumethiazide.
BetamethasoneThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Betamethasone.
BrexpiprazoleThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Brexpiprazole.
BumetanideThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Bumetanide.
BuserelinThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Buserelin.
CanagliflozinCanagliflozin may increase the hypoglycemic activities of Gliclazide.
CarbocisteineThe risk or severity of adverse effects can be increased when Gliclazide is combined with Carbocisteine.
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.
ChlorpropamideGliclazide may increase the hypoglycemic activities of Chlorpropamide.
ChlorthalidoneThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Chlorthalidone.
CimetidineThe serum concentration of Gliclazide can be increased when it is combined with Cimetidine.
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.
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.
DarunavirThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Darunavir.
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.
DexketoprofenThe risk or severity of adverse effects can be increased when Dexketoprofen is combined with Gliclazide.
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.
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.
EpinephrineThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Epinephrine.
ErythromycinGliclazide may increase the hypoglycemic activities of Erythromycin.
EstradiolThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Estradiol.
EstropipateThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Estropipate.
Ethacrynic acidThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Ethacrynic 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.
EthynodiolThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Ethynodiol.
EtonogestrelThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Etonogestrel.
EverolimusThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Everolimus.
ExenatideExenatide 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.
FosamprenavirThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Fosamprenavir.
FurosemideThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Furosemide.
GlimepirideGliclazide may increase the hypoglycemic activities of Glimepiride.
GlipizideGliclazide may increase the hypoglycemic activities of Glipizide.
GliquidoneGliquidone may increase the hypoglycemic activities of Gliclazide.
GlyburideGliclazide may increase the hypoglycemic activities of Glyburide.
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.
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.
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.
IndapamideThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Indapamide.
IndinavirThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Indinavir.
inhaled insulinGliclazide may increase the hypoglycemic activities of inhaled insulin.
Insulin AspartInsulin Aspart may increase the hypoglycemic activities of Gliclazide.
Insulin degludecGliclazide may increase the hypoglycemic activities of Insulin degludec.
Insulin DetemirInsulin Detemir may increase the hypoglycemic activities of Gliclazide.
Insulin GlargineGliclazide may increase the hypoglycemic activities of Insulin Glargine.
Insulin GlulisineInsulin Glulisine may increase the hypoglycemic activities of Gliclazide.
Insulin LisproGliclazide may increase the hypoglycemic activities of Insulin Lispro.
Insulin RegularGliclazide may increase the hypoglycemic activities of Insulin Regular.
Insulin, isophaneInsulin, isophane may increase the hypoglycemic activities of Gliclazide.
LanreotideGliclazide may increase the hypoglycemic activities of Lanreotide.
LeuprolideThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Leuprolide.
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.
LopinavirThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Lopinavir.
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.
MecamylamineThe risk or severity of adverse effects can be increased when Gliclazide is combined with Mecamylamine.
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.
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.
MethylprednisoloneThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Methylprednisolone.
MetolazoneThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Metolazone.
MetreleptinMetreleptin may increase the hypoglycemic activities of Gliclazide.
MiconazoleMiconazole may increase the hypoglycemic activities of Gliclazide.
MifepristoneThe serum concentration of Gliclazide can be increased when it is combined with Mifepristone.
NadololNadolol may increase the hypoglycemic activities of Gliclazide.
NateglinideGliclazide may increase the hypoglycemic activities of Nateglinide.
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.
NilotinibThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Nilotinib.
NorethindroneThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Norethindrone.
NorgestimateThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Norgestimate.
OctreotideGliclazide may increase the hypoglycemic activities of Octreotide.
OlanzapineThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Olanzapine.
OxandroloneOxandrolone may increase the hypoglycemic activities of Gliclazide.
PaliperidoneThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Paliperidone.
ParoxetineParoxetine may increase the hypoglycemic activities of Gliclazide.
PasireotideGliclazide may increase the hypoglycemic activities of Pasireotide.
PegvisomantPegvisomant may increase the hypoglycemic activities of Gliclazide.
PentamidineGliclazide may increase the hypoglycemic activities of Pentamidine.
PhenelzinePhenelzine may increase the hypoglycemic activities of Gliclazide.
PhenytoinThe metabolism of Gliclazide can be increased when combined with Phenytoin.
PipotiazineThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Pipotiazine.
PorfimerGliclazide may increase the photosensitizing activities of Porfimer.
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.
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.
QuetiapineThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Quetiapine.
QuinineGliclazide may increase the hypoglycemic activities of Quinine.
RanitidineThe serum concentration of Gliclazide can be increased when it is combined with Ranitidine.
RepaglinideGliclazide may increase the hypoglycemic activities of Repaglinide.
Repository corticotropinThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Repository corticotropin.
RifampicinThe serum concentration of Gliclazide can be decreased when it is combined with Rifampicin.
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.
Salicylate-sodiumSalicylate-sodium 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.
SirolimusThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Sirolimus.
SitagliptinSitagliptin may increase the hypoglycemic activities of Gliclazide.
SparfloxacinSparfloxacin may increase the hypoglycemic activities of Gliclazide.
SulfadiazineGliclazide may increase the hypoglycemic activities of Sulfadiazine.
SulfamethoxazoleGliclazide may increase the hypoglycemic activities of Sulfamethoxazole.
SulfisoxazoleGliclazide may increase the hypoglycemic activities of Sulfisoxazole.
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.
TipranavirThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Tipranavir.
TolazamideGliclazide may increase the hypoglycemic activities of Tolazamide.
TolbutamideTolbutamide may increase the hypoglycemic activities of Gliclazide.
TorasemideThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Torasemide.
TranylcypromineTranylcypromine 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.
TrimethoprimGliclazide may increase the hypoglycemic activities of Trimethoprim.
TriptorelinThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Triptorelin.
TroglitazoneTroglitazone may increase the hypoglycemic activities of Gliclazide.
VerteporfinGliclazide may increase the photosensitizing activities of Verteporfin.
VildagliptinVildagliptin 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.
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

1. ATP-binding cassette sub-family C member 8

Kind: Protein

Organism: Human

Pharmacological action: yes

Actions: binder

Components

Name UniProt ID Details
ATP-binding cassette sub-family C member 8 Q09428 Details

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
  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
  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
  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
  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

2. Vascular endothelial growth factor A

Kind: Protein

Organism: Human

Pharmacological action: unknown

Actions: other/unknown

Components

Name UniProt ID Details
Vascular endothelial growth factor A P15692 Details

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
  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
  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
  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

Enzymes

1. Cytochrome P450 2C9

Kind: Protein

Organism: Human

Pharmacological action: unknown

Actions: substrate

Components

Name UniProt ID Details
Cytochrome P450 2C9 P11712 Details

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

2. Cytochrome P450 2C19

Kind: Protein

Organism: Human

Pharmacological action: unknown

Actions: substrate inhibitor

Components

Name UniProt ID Details
Cytochrome P450 2C19 P33261 Details

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
  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. Epub 2009 Nov 24. Pubmed

Carriers

1. Serum albumin

Kind: Protein

Organism: Human

Pharmacological action: unknown

Components

Name UniProt ID Details
Serum albumin P02768 Details

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
  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

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Drug created on June 13, 2005 07:24 / Updated on April 25, 2014 11:40