Gliclazide (generic name of the drug Diamicron MR) is an hypoglycemic agent of the sulfonylurea group. Its hypoglycemic action is related to an improvement in insulin secretion from the functioning beta cells of the pancreas. It potentiates the insulin release and improves the dynamics of insulin.
Hemobiological properties of gliclazide have been observed in pharmacology studies. These are attributed to gliclazide action on the platelet behavior, prostaglandin equilibrium and fibrinolysis. At normal therapeutic doses diamicron mr has been shown in man to reduce abnormal platelet adhesiveness and aggregation.
Gliclazide is rapidly absorbed from the gastrointestinal tract and the plasma peak of gliclazide occurs between 4 and 6 hours. In man it is highly bound to plasma proteins, about 94%. The mean elimination half-life in man approximates 10.4 hours.
Following oral administration the unchanged gliclazide in plasma is extensively metabolized with little of the unchanged compound (<1%) appearing in the urine.
Gliclazide metabolites and conjugates have no hypoglycemic effect. They are primarily eliminated via kidneys 60 to 70% and about 10 to 20% via feces.
Some 5 principal metabolites have been identified in urine, essentially oxidized and hydroxylated derivatives, some as glucuronic acid conjugates.
Symptoms And Treatment Of Overdose
Symptoms: Overdosage with sulfonylureas may result in hypoglycemia but it should be noted that the dosage which causes such hypoglycemia varies widely and may be within the accepted therapeutic range in sensitive individuals.
The manifestations of hypoglycemia include sweating, flushing or pallor, numbness, chilliness, hunger, trembling, headache, dizziness, increased pulse rate, palpitations, increased blood pressure and apprehensiveness in mild cases. In more severe cases, coma appears.
However, symptoms of hypoglycemia are not necessarily as typical as those described above and sulfonylureas may cause insidious development of symptoms mimicking cerebrovascular insufficiency
Treatment: Discontinue medication and treat hypoglycemia by giving dextrose promptly and in sufficient quantity.
Some sulfonylurea-induced hypoglycemias may be refractory to treatment and susceptible to relapse especially in elderly or malnourished patients. Continuous dextrose infusions for hours or days have been necessary.
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