Source: Υπουργείο Υγείας (CY) Revision Year: 2017 Publisher: Remedica Ltd, Aharnon Street, Limassol Industrial Estate, 3056 Limassol, Cyprus
Pharmacotherapeutic group: Drugs used in diabetes; Blood glucose lowering drugs, excl. Insulins
ATC Code: A10BB09
Gliclazide is a hypoglycaemic sulphonylurea antidiabetic active substance differing from other related compounds by an N-conatining heterocyclic ring with an endocyclic bond.
Gliclazide reduces blood glucose levels by stimulating insulin secretion from the β-cells of the islets of Langerhans. Increase in postprandial insulin and C-peptide secretion persists after two years of treatment.
In addition to these metabolic properties, gliclazide has haemovascular properties.
In type 2 diabetics, gliclazide restores the first peak of insulin secretion in response to glucose and increases the second phase of insulin secretion. A significant increase in insulin response is seen in response to stimulation induced by a meal or glucose.
Gliclazide decreases microthrombosis by two mechanisms which may be involved in complications of diabetes:
Plasma levels increase reaching maximal concentrations between 2 and 6 hours.
Gliclazide is well absorbed. Food intake does not affect the rate or degree of absorption.
Plasma protein binding is approximately 95%. The volume of distribution is around 19 litres.
Gliclazide is mainly metabolised in the liver and excreted in the urine; less than 1% of the dose is excreted unchanged in the urine. No active metabolites have been detected in plasma.
The elimination half-life of gliclazide is between 10 and 12 hours.
The relationship between the dose administered between 40 and 400 mg and the mean plasma concentrations is linear.
No clinically significant changes in pharmacokinetic parameters have been observed in elderly patients.
Preclinical data reveal no special hazards for humans based on conventional studies of repeated dose toxicity and genotoxicity. Long term carcinogenicity studies have not been done. No teratogenic changes have been shown in animal studies, but lower fetal body weight was observed in animals receiving doses 9.4 fold higher than the maximum recommended dose in humans. Fertility and reproductive performance were unaffected after gliclazide administration in animal studies.
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