Peringatan Keamanan

LD50=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.

Gliclazide

DB01120

small molecule approved

Deskripsi

Gliclazide is an oral antihyperglycemic agent used for the treatment of non-insulin-dependent diabetes mellitus (NIDDM). It has been classified differently according to its drug properties in which based on its chemical structure, gliclazide is considered a first-generation sulfonylurea due to the structural presence of a sulfonamide group able to release a proton and the presence of one aromatic group.A39546 On the other hand, based on the pharmacological efficacy, gliclazide is considered a second-generation sulfonylurea which presents a higher potency and a shorter half-life.T238, T360 Gliclazide 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%).

Struktur Molekul 2D

Berat 323.41
Wujud solid

Peta Jejaring Molekuler
Legenda: ObatTargetGenEnzim(Panah → menunjukkan arah efek / relasi)TransporterCarrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) 10.4 hours. Duration of action is 10-24 hours.
Volume Distribusi -
Klirens (Clearance) -

Absorpsi

Rapidly and well absorbed but may have wide inter- and intra-individual variability. Peak plasma concentrations occur within 4-6 hours of oral administration.

Metabolisme

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.

Rute Eliminasi

Metabolites and conjugates are eliminated primarily by the kidneys (60-70%) and also in the feces (10-20%).

Farmakogenomik

2 Varian
CYP2C19 (rs4244285)

The presence of this polymorphism in CYP2C19 is associated with reduction in gliclazide metabolism.

CYP2C19 (rs4986893)

The presence of this polymorphism in CYP2C19 is associated with reduction in gliclazide metabolism.

Interaksi Makanan

2 Data
  • 1. Avoid alcohol.
  • 2. Take with or without food. Consistent food intake reduces the risk of hypoglycemia.

Interaksi Obat

1090 Data
Pegvisomant The risk or severity of hypoglycemia can be increased when Pegvisomant is combined with Gliclazide.
Dabrafenib The serum concentration of Gliclazide can be decreased when it is combined with Dabrafenib.
Luliconazole The serum concentration of Gliclazide can be increased when it is combined with Luliconazole.
Carbocisteine The risk or severity of adverse effects can be increased when Gliclazide is combined with Carbocisteine.
Chloramphenicol The metabolism of Gliclazide can be decreased when combined with Chloramphenicol.
Cimetidine The serum concentration of Gliclazide can be increased when it is combined with Cimetidine.
Fluconazole The serum concentration of Gliclazide can be increased when it is combined with Fluconazole.
Metreleptin Metreleptin may increase the hypoglycemic activities of Gliclazide.
Probenecid The protein binding of Gliclazide can be decreased when combined with Probenecid.
Ranitidine The serum concentration of Gliclazide can be increased when it is combined with Ranitidine.
Voriconazole The serum concentration of Gliclazide can be increased when it is combined with Voriconazole.
Clarithromycin The serum concentration of Gliclazide can be increased when it is combined with Clarithromycin.
Lipoic acid The risk or severity of hypoglycemia can be increased when Lipoic acid is combined with Gliclazide.
Rifampin The serum concentration of Gliclazide can be decreased when it is combined with Rifampicin.
Moxifloxacin The therapeutic efficacy of Gliclazide can be increased when used in combination with Moxifloxacin.
Grepafloxacin The therapeutic efficacy of Gliclazide can be increased when used in combination with Grepafloxacin.
Enoxacin The therapeutic efficacy of Gliclazide can be increased when used in combination with Enoxacin.
Pefloxacin The therapeutic efficacy of Gliclazide can be increased when used in combination with Pefloxacin.
Ciprofloxacin The therapeutic efficacy of Gliclazide can be increased when used in combination with Ciprofloxacin.
Trovafloxacin The therapeutic efficacy of Gliclazide can be increased when used in combination with Trovafloxacin.
Nalidixic acid The therapeutic efficacy of Gliclazide can be increased when used in combination with Nalidixic acid.
Rosoxacin The therapeutic efficacy of Gliclazide can be increased when used in combination with Rosoxacin.
Cinoxacin The therapeutic efficacy of Gliclazide can be increased when used in combination with Cinoxacin.
Lomefloxacin The therapeutic efficacy of Gliclazide can be increased when used in combination with Lomefloxacin.
Gatifloxacin The therapeutic efficacy of Gliclazide can be increased when used in combination with Gatifloxacin.
Norfloxacin The therapeutic efficacy of Gliclazide can be increased when used in combination with Norfloxacin.
Levofloxacin The therapeutic efficacy of Gliclazide can be increased when used in combination with Levofloxacin.
Gemifloxacin The therapeutic efficacy of Gliclazide can be increased when used in combination with Gemifloxacin.
Ofloxacin The therapeutic efficacy of Gliclazide can be increased when used in combination with Ofloxacin.
Sparfloxacin The therapeutic efficacy of Gliclazide can be increased when used in combination with Sparfloxacin.
Temafloxacin The therapeutic efficacy of Gliclazide can be increased when used in combination with Temafloxacin.
Fleroxacin The therapeutic efficacy of Gliclazide can be increased when used in combination with Fleroxacin.
Technetium Tc-99m ciprofloxacin The therapeutic efficacy of Gliclazide can be increased when used in combination with Technetium Tc-99m ciprofloxacin.
Garenoxacin The therapeutic efficacy of Gliclazide can be increased when used in combination with Garenoxacin.
Nemonoxacin The therapeutic efficacy of Gliclazide can be increased when used in combination with Nemonoxacin.
Flumequine The therapeutic efficacy of Gliclazide can be increased when used in combination with Flumequine.
Enrofloxacin The therapeutic efficacy of Gliclazide can be increased when used in combination with Enrofloxacin.
Orbifloxacin The therapeutic efficacy of Gliclazide can be increased when used in combination with Orbifloxacin.
Sarafloxacin The therapeutic efficacy of Gliclazide can be increased when used in combination with Sarafloxacin.
Difloxacin The therapeutic efficacy of Gliclazide can be increased when used in combination with Difloxacin.
Pazufloxacin The therapeutic efficacy of Gliclazide can be increased when used in combination with Pazufloxacin.
Prulifloxacin The therapeutic efficacy of Gliclazide can be increased when used in combination with Prulifloxacin.
Delafloxacin The therapeutic efficacy of Gliclazide can be increased when used in combination with Delafloxacin.
Sitafloxacin The therapeutic efficacy of Gliclazide can be increased when used in combination with Sitafloxacin.
Oxolinic acid The therapeutic efficacy of Gliclazide can be increased when used in combination with Oxolinic acid.
Rufloxacin The therapeutic efficacy of Gliclazide can be increased when used in combination with Rufloxacin.
Pipemidic acid The therapeutic efficacy of Gliclazide can be increased when used in combination with Pipemidic acid.
Methyclothiazide The therapeutic efficacy of Gliclazide can be decreased when used in combination with Methyclothiazide.
Chlorthalidone The therapeutic efficacy of Gliclazide can be decreased when used in combination with Chlorthalidone.
Bendroflumethiazide The therapeutic efficacy of Gliclazide can be decreased when used in combination with Bendroflumethiazide.
Metolazone The therapeutic efficacy of Gliclazide can be decreased when used in combination with Metolazone.
Benzthiazide The therapeutic efficacy of Gliclazide can be decreased when used in combination with Benzthiazide.
Hydroflumethiazide The therapeutic efficacy of Gliclazide can be decreased when used in combination with Hydroflumethiazide.
Indapamide The therapeutic efficacy of Gliclazide can be decreased when used in combination with Indapamide.
Chlorothiazide The therapeutic efficacy of Gliclazide can be decreased when used in combination with Chlorothiazide.
Hydrochlorothiazide The therapeutic efficacy of Gliclazide can be decreased when used in combination with Hydrochlorothiazide.
Trichlormethiazide The therapeutic efficacy of Gliclazide can be decreased when used in combination with Trichlormethiazide.
Polythiazide The therapeutic efficacy of Gliclazide can be decreased when used in combination with Polythiazide.
Quinethazone The therapeutic efficacy of Gliclazide can be decreased when used in combination with Quinethazone.
Cyclopenthiazide The therapeutic efficacy of Gliclazide can be decreased when used in combination with Cyclopenthiazide.
Epitizide The therapeutic efficacy of Gliclazide can be decreased when used in combination with Epitizide.
Esmolol Esmolol may increase the hypoglycemic activities of Gliclazide.
Landiolol Landiolol may increase the hypoglycemic activities of Gliclazide.
Lumacaftor The serum concentration of Gliclazide can be decreased when it is combined with Lumacaftor.
Ethanol The risk or severity of adverse effects can be increased when Gliclazide is combined with Ethanol.
Protriptyline Protriptyline may decrease the hypoglycemic activities of Gliclazide.
Nortriptyline Nortriptyline may decrease the hypoglycemic activities of Gliclazide.
Amoxapine Amoxapine may decrease the hypoglycemic activities of Gliclazide.
Desipramine Desipramine may decrease the hypoglycemic activities of Gliclazide.
Amineptine Amineptine may decrease the hypoglycemic activities of Gliclazide.
Dimetacrine Dimetacrine may decrease the hypoglycemic activities of Gliclazide.
Butriptyline Butriptyline may decrease the hypoglycemic activities of Gliclazide.
Dosulepin Dosulepin may decrease the hypoglycemic activities of Gliclazide.
Tianeptine Tianeptine may decrease the hypoglycemic activities of Gliclazide.
Oxaprotiline Oxaprotiline may decrease the hypoglycemic activities of Gliclazide.
Opipramol Opipramol may decrease the hypoglycemic activities of Gliclazide.
Amitriptylinoxide Amitriptylinoxide may decrease the hypoglycemic activities of Gliclazide.
Dibenzepin Dibenzepin may decrease the hypoglycemic activities of Gliclazide.
Quinupramine Quinupramine may decrease the hypoglycemic activities of Gliclazide.
Melitracen Melitracen may decrease the hypoglycemic activities of Gliclazide.
Lofepramine Lofepramine may decrease the hypoglycemic activities of Gliclazide.
Iprindole Iprindole may decrease the hypoglycemic activities of Gliclazide.
Imipramine oxide Imipramine oxide may decrease the hypoglycemic activities of Gliclazide.
Amitriptyline Amitriptyline may decrease the hypoglycemic activities of Gliclazide.
Doxepin Doxepin may decrease the hypoglycemic activities of Gliclazide.
Clofibrate The risk or severity of hypoglycemia can be increased when Clofibrate is combined with Gliclazide.
Fenofibrate The risk or severity of hypoglycemia can be increased when Fenofibrate is combined with Gliclazide.
Bezafibrate The risk or severity of hypoglycemia can be increased when Bezafibrate is combined with Gliclazide.
Etofibrate The risk or severity of hypoglycemia can be increased when Etofibrate is combined with Gliclazide.
Ciprofibrate The risk or severity of hypoglycemia can be increased when Ciprofibrate is combined with Gliclazide.
Simfibrate The risk or severity of hypoglycemia can be increased when Simfibrate is combined with Gliclazide.
Ronifibrate The risk or severity of hypoglycemia can be increased when Ronifibrate is combined with Gliclazide.
Aluminium clofibrate The risk or severity of hypoglycemia can be increased when Aluminium clofibrate is combined with Gliclazide.
Clofibride The risk or severity of hypoglycemia can be increased when Clofibride is combined with Gliclazide.
Fenofibric acid The risk or severity of hypoglycemia can be increased when Fenofibric acid is combined with Gliclazide.
Miconazole The serum concentration of Gliclazide can be increased when it is combined with Miconazole.
Phenindione Gliclazide may increase the anticoagulant activities of Phenindione.
Coumarin Gliclazide may increase the anticoagulant activities of Coumarin.
Clorindione Gliclazide may increase the anticoagulant activities of Clorindione.
Diphenadione Gliclazide may increase the anticoagulant activities of Diphenadione.

Target Protein

ATP-binding cassette sub-family C member 8 ABCC8
Vascular endothelial growth factor A, long form VEGFA

Referensi & Sumber

Synthesis reference: U.S. Patent 3,501,495
Artikel (PubMed)
  • PMID: 2106423
    Ballagi-Pordany G, Koszeghy A, Koltai MZ, Aranyi Z, Pogatsa G: Divergent cardiac effects of the first and second generation hypoglycemic sulfonylurea compounds. Diabetes Res Clin Pract. 1990 Jan;8(2):109-14.
Textbook
  • Scholar E. (2007). XPharm: The comprehensive Pharmacology Reference. Elsevier.
  • Ghosh S. and Collier A. (2012). Churchill's pocketbook of diabetes (2nd ed.). Elsevier.

Contoh Produk & Brand

Produk: 30 • International brands: 2
Produk
  • Ag-gliclazide Mr
    Tablet, extended release • 30 mg • Oral • Canada • Generic • Approved
  • Ag-gliclazide Mr
    Tablet, extended release • 60 mg • Oral • Canada • Generic • Approved
  • Apo-gliclazide
    Tablet • 80 mg • Oral • Canada • Generic • Approved
  • Apo-gliclazide Mr
    Tablet, extended release • 60 mg • Oral • Canada • Generic • Approved
  • Apo-gliclazide Mr
    Tablet, extended release • 30 mg • Oral • Canada • Generic • Approved
  • Ava-gliclazide
    Tablet • 80 mg • Oral • Canada • Generic • Approved
  • Diamicron
    Tablet • 80 mg • Oral • Canada • Approved
  • Diamicron Mr
    Tablet, extended release • 60 mg • Oral • Canada • Approved
Menampilkan 8 dari 30 produk.
International Brands
  • Glimicron
  • Nordialex

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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