Each tablet contains gliclazide 80mg
Actions and Mode of Action
Gliclazide is a sulphonylurea hypoglycaemic agent which stimulates insulin
secretion by the pancreatic β cells and consequently are effective only
when some residual pancreatic β-cell activity is present. Its action on
insulin secretion is mainly due to the restoration of the early phase;
however, it is also effective in stimulating secretion of insulin throughout
a meal. In addition to this pancreatic action, it has been demonstrated that
gliclazide improves the metabolic utilization of glucose at a peripheral
level. This extrapancreatic action may be due to the potentiation of the
post-receptor pathways. Thus, gliclazide restores glycaemic control
throughout 24 hours. It normalizes fasting and postprandial blood sugar.
The hypoglycaemic effect of gliclazide appears to be initiated by drug
interaction with cell-surface receptors on the pancreatic β cells; this
results in reduced conductance of an ATP-sensitive K+ channel.
The drug thus resembles physiological secretagogues (eg., glucose, leucine),
which also lowers the conductance of this channel. Reduced K+ conductance
causes membrane depolarization and influx of Ca2+ through
voltage-sensitive Ca2+ channels.
Gliclazide has also been shown to reduce platelet hyperadhesiveness and
hyperaggregation, to increase fibrinolytic activity and to oppose adrenaline
vasoconstriction. These factors are thought to be contributors of the
long-term complication of diabetes mellitus.
Gliclazide is readily absorbed from the gastrointestinal tract and peak
plasma concentrations occur 2-4 hours after administration. It is
extensively bound to plasma proteins. (85%) Gliclazide is extensively
metabolized in the liver to metabolites without significant hypoglycaemic
activity. Metabolites and a small amount of unchanged drug are excreted in
the urine. 10-20 % of the dose is excreted in the faeces as metabolites. The
half-life is about 10 to 12 hours.
Melicron is indicated for the treatment of non-insulin-dependent Diabetes
Mellitus. It is used to supplement treatment by dietary modification when
such modification has proved insufficient.
In the majority of cases, 2 tablets daily (1 tablet with breakfast, 1 tablet
with dinner). Dosage can vary from 1-4 tablets daily, adjusted according to
the individual patient's severity of Diabetes. The usual initial dose is 40
to 80mg daily. Doses of more than 160mg should be given in 2 divided doses.
Maximum dose is 320mg daily.
Melicron should not be used alone in insulin-dependent diabetes;
juvenile-onset diabetes; diabetes complicated by ketosis and acidosis;
pregnancy; diabetics undergoing surgery, after severe trauma or during
infections; precoma or coma; insulin should be given together and specific
care needed. Melicron is contraindicated in patients hypersensitive to any
other sulphonylureas and related drugs and patients with severe renal or
hepatic insufficiency. When major surgery is to be performed, insulin
therapy should be substituted for oral hypoglycaemia.
As gliclazide is metabolized and excreted extensively in the liver and renal
respectively, caution is needed in the elderly and patients with hepatic and
/ or renal impairment and a small starting dose should be used with careful
patient monitoring. Hypoglycaemia will occur if the patients' dietary intake
is reduced or if they are receiving a larger dose of Melicron. Melicron
should be used with caution during lactation.
Potentiation of the hypoglycaemic action of Melicron may occur with the
concomitant administration of sulfonamides, chloramphenicol, co-trimoxazole,
salicylates, phenylbutazone, beta-blockers, monoamine oxidase inhibitors (MAOIs),
ketoconazole and miconazole. Clofibrates, eg. Gemfibrozil may improve
glucose tolerance and have an additive effect.
Diminution of hypoglycaemic action of the drug may occur with concomitant
administration of loop and thiazide diuretics, corticosteroides and estogens
or oral contraceptives.
Side Effects / Adverse Reactions
Melicron is generally well tolerated. Hypoglycaemia may occur with all
hypoglycaemic agents. Skin rashes and pruritus may occur and
photosensitivity has been reported. Gastrointestinal disturbances such as
nausea, vomiting, heartburn, anorexia, diarrhoea, and a metallic taste may
occur with sulphonylureas and are usually mild and dose-dependent. Other
severe effects of sulphonyureas may be manifestations of hypersensitivity
reactions. They include cholestatic jaundice, leucopenia, thrombocytopenia,
aplastic anaemia, agranulocytosis and hemolytic anaemia, erythema multiforme
or the Steven-Johnson Syndrome, exfoliative dermatitis, and erythema nodosum.
All these phenomenas are very rare.
Symptoms and Treatment for Overdosage
The symptom of overdose is hypoglycaemia. In acute poisoning the stomach
should be emptied by emesis or lavage. Hypoglycaemia should be treated with
urgency. The patient should be observed over several days in case
hypoglycaemia recurs until the effect of the drug has ceased.
3 years from the date of manufacture.
White round, 7.9mm diameter, flat-bevelled edge with a cross-line on one
side and plain on reverse.
Packing / Pack sizes
Blister pack of 60's and 100's.
Store at room temperature below 30°C
KEEP ALL MEDICINES OUT OF REACH OF CHILDREN