A sulfonylurea oral hypoglycemic agent: Gliclazide

Description

Gliclazide, glimepiride, glipizide, and glyburide are second-generation sulfonylureas considered to be free of many of the troublesome side effects of first-generation sulfonylureas, particularly the disulfiram-like reaction. Gliclazide is commonly used in diabetic II treatment.

Hypoglycemic agent

Gliclazide is a second-generation, sulfonylurea oral hypoglycemic agent, with a pharmacology broadly similar to that of tolbutamide (also see Antidiabetic Agents) but is more potent, with a potency similar to that of glibenclamide. It has a long duration of action (up to 24 hours). Sulfonylureas increase the amount of insulin your pancreas makes. This lowers your blood sugar. Gliclazide stimulates insulin secretion through the beta cell sulphonylurea receptor, and possibly through a direct effect on intracellular calcium transport[1]. It specifically improves the abnormal first-phase insulin release in type 2 diabetes and also affects the second phase.

Antiplatelet and antioxidant activity

There is evidence that gliclazide has antiplatelet and antioxidant activity independent of its effects on glycemic control Jennings (2000). Mizuno et al. reported that gliclazide inhibits platelet functions, but its effective concentration is reported to be much higher in vitro than in vivo. Impedance aggregometry was found to be more sensitive than turbidimetry for detecting the inhibition of platelet aggregation and revealed significant inhibition at 1 × 10⁻⁴ M gliclazide. Gliclazide reduced the amount of prostaglandin I2 (PGI2) needed to inhibit ADP-induced platelet aggregation and the adhesiveness of platelets to a rabbit vessel wall after their preincubation with 1×10⁻³ M gliclazide for 10 min. These effects have been attributed to the azabicyclo ring, which is unique to gliclazide among the sulfonylureas. It remains to be seen in long-term, large-scale, randomized, controlled trials if these effects confer additional benefits on patients with type 2 diabetes, in terms of a reduction in diabetic complications and/or reduced mortality. Gliclazide reduces platelet adhesion, aggregation and hyperactivity and increases fibrinolysis. In particular, Gliclazide has been reported to inhibit the progression of diabetic retinopathy[2].

Contraindications

Gliclazide is not suitable for some people. To make sure it's safe for someone, tell their doctor before starting the medicine if they:

have ever had an allergic reaction to gliclazide or any other medicine

have ketone bodies and sugar in your urine (diabetic ketoacidosis)

have severe kidney or liver disease

have a rare condition called porphyria

are pregnant, trying to get pregnant, or breastfeeding

have a condition called G6PD deficiency

need to have surgery(research has explained that second-generation sulphonylureas should be discontinued 1 day before surgery)[3].

References

[1] Zhang, Z. H., and W. S. Pan. "Expert system for the development and formulation of push-pull osmotic pump tablets containing poorly water-soluble drugs." (2013).

[2] Campbell, D., and R. Lavielle. "The mode of action and clinical pharmacology of gliclazide: a review." Diabetes Res Clin Pract (1991).

[3] Marzio, Halegoua De, and V. J. Navarro. "Hepatotoxicity of Cardiovascular and Antidiabetic Drugs."Drug-Induced Liver Disease (Third Edition) (2013):519-540.