Gliclazide:an oral hypoglycemic

Gliclazide is an oral hypoglycemic (anti-diabetic drug) and is classified as a sulfonylurea.

1. Uses

Gliclazide is used to treat type 2 diabetes mellitus.

It is one of a group of medicines known as sulfonylureas.

It is used to reduce blood sugar levels.

In general this drug is used in the treatment of diabetes mellitus when insulin is not necessary and when diet, exercise and weight loss fail to lower blood glucose (sugar).

Benefits of being on this drug can include control of type 2 diabetes mellitus.

2. Adverse effects

*Hypoglycemia - while it was proven to have the same efficacy as glimepiride, one of the newer sulfonylureas, the European GUIDE study has shown that it has approximately 50% fewer confirmed hypoglycaemic episodes in comparison with glimepiride.

*Gastrointestinal disturbance

*Skin reactions (rare)

*Hematological disorders (rare)

*Hepatic enzyme rises (exceptional)

2. Mode 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 the K+ ion channels. This decreases the efflux of potassium from the cell which leads to the depolarization of the cell. This causes voltage dependent Ca++ ion channels to open increasing the Ca++ influx. The calcium can then bind to and activate calmodulin which in turn leads to exocystosis of insulin vesicles leading to insulin release.

3. Dosage

The dosage for the 80 mg formulation is 40 to 320 mg daily in two divided doses, while the 30 mg and 60 mg modified release formulation may be given at a dose of 30 to 120 mg once daily at breakfast.

4. Missed Dose

If you miss a dose, take it as soon as you remember. If it is near the time of the next dose, skip the missed dose and resume your usual dosing schedule. Do not double the dose to catch up.

5. Storage

Keep out of the reach and sight of children.

6. Warning

Gliclazide should be used with caution in: the elderly, those with mild to moderate liver or kidney disease, pregnancy, people with glucose-6-phosphate-dehydrogenase deficiency, people at risk of hypoglycaemia (e.g. those on a low-calorie diet, malnourished, fasting, skipping meals, eating at irregular intervals, exercising excessively).