Gliclazide

Gliclazide

Cat. No.: PI21187984

Description: Gliclazide is a sulfonylurea used to treat hyperglycemia in patients with type 2 diabetes mellitus.

Product Details
CAS 21187-98-4
Synonyms S1702; SE1702
Molecular Formula C15H21N3O3S
Molecular Weight 323.41
Therapeutic Category Antidiabetic
Available DMF/CEP/GMP CEP, JDMF, CADIFA, Canada, India
Uses Gliclazide is used for control of hyperglycemia in gliclazide-responsive diabetes mellitus of stable, mild, non-ketosis prone, type 2 diabetes. It is used when diabetes cannot be controlled by proper dietary management and exercise and when metformin has already been tried.
Mechanism Of Action Gliclazide selectively binds to sulfonylurea receptors (SUR-1) on the surface of the pancreatic beta-cells. It was shown to provide cardiovascular protection as it does not bind to sulfonylurea receptors (SUR-2A) in the heart. This binding effectively closes these K+ ion channels. This decreases the efflux of potassium from the cell which leads to the depolarization of the cell. This causes voltage dependent Ca2+ ion channels to open increasing the Ca2+ influx. The calcium can then bind to and activate calmodulin which in turn leads to exocytosis of insulin vesicles leading to insulin release.
Case Study

Gliclazide for the Preparation of Gliclazide-Loaded Galactomannan Hydrogel Microspheres (GHM)

Locust bean gum glutarate nanocomposite hydrogel microspheres of gliclazide: Optimization by Box-Behnken design and preclinical evaluation of anti-diabetic efficacy Yadav H, et al. International Journal of Biological Macromolecules, 2024, 283, 136963.

A specified amount of sodium carboxymethyl galactomannan was dissolved in 10 mL of a 0.1% (w/v) nanodispersed aluminum silicate (approximately 270 nm) aqueous solution, achieving a final concentration of 1-3% (w/v). Subsequently, gliclazide was added at 20% (w/w) of the total formulation, and the mixture was homogenized at 5000 rpm. The resulting drug-loaded polymer solution was transferred into a 10 mL glass syringe and dropped through a 21-gauge blunt needle into 50 mL of 1% (w/v) aluminum chloride aqueous solution. The solution was allowed to gel for 15 minutes in the gelling medium. The resulting hydrogel microspheres were then collected by filtration through a fine mesh cloth and washed with distilled water (3 × 50 mL). The microspheres were subsequently transferred to a succinic anhydride aqueous solution (0.15-0.45%, w/v), heated to 60°C, and incubated for 15-45 minutes. After filtration, the microspheres were washed with Milli-Q water and dried until the weight of each sample remained constant after three consecutive measurements.

Gliclazide in the Treatment of Obesity-Induced Polycystic Ovary Syndrome: A Combination Therapy with Metformin

A combination of gliclazide and metformin attenuates obesity-induced polycystic ovary syndrome in female Wistar rats Moazzam A, et al. Heliyon, 2024, 10(7), e29015.

Recent studies have extended its therapeutic potential, exploring its combined application with metformin in the management of obesity-induced polycystic ovary syndrome (PCOS). In a study conducted on female Wistar rats, a high-fat diet was used to induce obesity and subsequent PCOS, with estradiol valerate administered to enhance the syndrome's progression. The rats were then treated with gliclazide (5, 10 mg/kg) and metformin (100, 300 mg/kg), either alone or in combination, over a period of 28 days.
The results demonstrated significant improvements across several parameters in the treated groups compared to the disease control group (DCG). Notably, a marked reduction in body weight and blood glucose levels was observed, along with decreased hemoglobin A1c, serum insulin, cholesterol, triglycerides, and testosterone. In contrast, key reproductive hormones, including progesterone, estradiol, luteinizing hormone (LH), and follicle-stimulating hormone (FSH), were significantly elevated in the treatment groups. Furthermore, the combination therapy of metformin and gliclazide (M100+G10 mg/kg) was particularly effective in restoring ovarian antioxidant levels, evidenced by increased superoxide dismutase (SOD), catalase (CAT), and glutathione (GSH), alongside reduced oxidative stress markers like malondialdehyde (MDA) and nitric oxide (NO).
Histological examination of ovarian tissues corroborated these biochemical findings, showing marked improvements in tissue integrity. Moreover, treatment with gliclazide and metformin significantly modulated inflammatory markers, including interleukin-6 (IL-6), Nrf2, and NF-κB, underscoring the potential of this combination therapy in addressing the multifaceted pathophysiology of obesity-induced PCOS.

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