Glitab

Gliclazide.

Each modified-release tablet contains: Gliclazide 30 mg.

Pharmacology: Gliclazide is a second generation sulfonylurea which acts as a hypoglycemic agent. It stimulates beta 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. For the treatment of diabetes mellitus.
Pharmacodynamics: Mechanism of Action: Gliclazide binds to the β cell sulfonylurea 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 secretory granules.
Pharmacokinetics: Gliclazide is readily absorbed from the gastrointestinal tract. It is extensively bound to plasma proteins. The half-life is about 10 to 12 hours. Gliclazide is extensively metabolized in the liver to metabolites that have no significant hypoglycemic activity. Metabolites and a small amount of unchanged drug are excreted in the urine.

Used in the treatment of type 2 diabetes mellitus.

Initially, 40 mg daily; may increase up to 320 mg daily. Doses up to 160 mg daily given as a single doses. Doses greater than 160 mg should be taken in divided doses.

An overdose of sulfonylureas may cause hypoglycaemia. Moderate symptoms of hypoglycaemia, without any loss of consciousness or neurological signs, must be corrected by carbohydrate intake, dose adjustment and/or change of diet. Strict monitoring should be continued until the doctor is sure that the patient is out of danger.
Severe hypoglycaemic reactions, with coma, convulsions or other neurological disorders are possible and must be treated as a medical emergency, requiring immediate hospitalization.
If hypoglycaemic coma is diagnosed or suspected, the patient should be given a rapid IV injection of 50 mL of concentrated glucose solution (20 to 30%). This should be followed by continuous infusion of a more dilute glucose solution (10%) at a rate that will maintain blood glucose levels above 1 g/L. Patients should be monitored closely and, depending on the patient's condition after this time, the doctor will decide if further monitoring is necessary.
Dialysis is of no benefit to patients due to the strong binding of gliclazide to proteins.

Diabetes complicated with acidosis, ketosis or coma. Juvenile onset diabetes and unstable or brittle diabetes. Severe renal and liver disease. Hypersensitivity to sulfonylureas; lactation.

Hepatic and/or renal impairment: A small starting dose should be used with careful patient monitoring. As with other sulfonylureas, hypoglycemic may occur if patient's dietary intake is reduced or if they are receiving a larger dose of Gliclazide than is required.

Use in Pregnancy: There is no or limited amount of data (less than 300 pregnancy outcomes) from the use of gliclazide in pregnant women, even though there are few data with other sulfonylureas. In animal studies, gliclazide is not teratogenic. As a precautionary measure, it is preferable to avoid the use of Gliclazide during pregnancy. Control of diabetes should be obtained before the time of conception to reduce the risk of congenital abnormalities linked to uncontrolled diabetes.
Oral hypoglycemic agents are not suitable, insulin is the drug of first choice for treatment of diabetes during pregnancy. It is recommended that oral hypoglycemic therapy is changed to insulin before a pregnancy is attempted, or as soon as pregnancy is discovered.
Use in Lactation: It is unknown whether gliclazide or its metabolites are excreted in human milk. Given the risk of neonatal hypoglycaemia, the product is therefore contraindicated in breastfeeding mothers. A risk to the newborns/infants cannot be excluded.
Fertility: No effect on fertility or reproductive performance was noted in male and female rats.

Nausea, headache, rashes and gastrointestinal disturbances.
Seek medical attention immediately at the first sign of any adverse drug reaction.

Potentiation of the hypoglycemic action of the drug may occur with the concomitant administration of sulfonamides, salicylates, phenylbutazone, beta-adrenoreceptor-blocking agents, MAOIs, ketoconazole and miconazole. Diminution of hypoglycemic action of the drug may occur with the concomitant administration of thiazide diuretics, corticosteroids and estrogens. Adjustment of dosage of hypoglycemic agents may be required in patients suffering from intercurrent infections, traumas, shock of after anesthesia. When major surgery is to be performed, insulin therapy should be substituted for oral hypoglycemics.

Store at temperatures not exceeding 30°C.

Antidiabetic Agents

A10BB09 - gliclazide ; Belongs to the class of sulfonylureas. Used in the treatment of diabetes.

Rx