Round, 8.0 mm in diameter, white uncoated tablet, flat faces, bevel-edged,
cross score embossed on one face.
Gliclazide 80 mg / tablet
ACTION & PHARMACOLOGY
Gliclazide, a sulphonylurea, acts by promoting release of insulin from
the beta cells of pancreatic islet tissue by an unknown process. Insulin
production is not increased. Hepatic glycogenolysis and gluconeogenesis are
decreased. Insulin sensitivity is increased at peripheral target sites.
Therefore, sulfonylureas are effective only in patients whose pancreas are
capable of producing insulin.
It is readily absorbed from the gastro-intestinal tract.
• Protein Binding
Gliclazide is very extensively bound to plasma proteins.
• Metabolic Reactions
It is extensively metabolized in the liver to metabolites without
significant hypoglycaemic activity.
Plasma half-life is about 10 to 12 hours.
Both unchanged drug and metabolites are excreted in the urine.
Gliclazide is indicated in non-insulin dependent diabetes mellitus.
• Except under special circumstances, this medication should not be used
when the following medical problems exist: Acidosis, burns, diabetic coma,
infection, ketoacidosis, ketosis, surgery and trauma.
• Risk-benefit should be considered when the following medical problems
exist: Adrenal insufficiency, pituitary insufficiency, fever, nausea,
vomiting, thyroid function impairment, debilitated physical condition,
hepatic function impairment, malnourishment, renal function impairment,
sensitivity to oral antidiabetic agents and patients with acute porphyria.
• Patients sensitive to one of the oral antidiabetic agents may be sensitive
to the others also.
• Oral antidiabetic agents must not be used during pregnancy. Abnormal blood
glucose levels have been associated with a higher incidence of congenital
abnormalities during early pregnancy, and with increased perinatal morbidity
and mortality later in pregnancy.
• It should not be used in
insulin-dependent diabetes mellitus.
• It should not be given in severe impairment of renal or hepatic function
because of an increased risk of hypoglycaemia or severe impairment of
• Its antidiuretic effect may cause problems in patients conditions
associated with fluid retention.
• It is not known whether gliclazide is excreted in breast milk. However
other sulphonylureas have been found in breast milk and there is no evidence
to suggest that gliclazide differs from the group in this respect.
• Geriatric patients and patients with renal insufficiency may be more
sensitive to the effects of this medication because of reduced metabolism
and excretion. Dosage should therefore be initiated at a lower level and
adjusted cautiously. In the elderly, hypoglycaemia may be more difficult to
recognize and may cause more neurological symptoms. These symptoms include
anxiety, confusion, difficulty in concentrating, drowsiness, nervousness or
• Dental: The leukopenic and thrombocytopenic effects of sulfonylureas may
result in an increased incidence of microbial infection, delayed healing and
gingival bleeding. If leukopenia or cytopenia occurs, dental work should be
deferred until blood counts have returned to normal. Patients should be
instructed in the proper oral hygiene required during this period. This
includes cautious use of regular toothbrushes, dental floss and toothpicks.
• Cross-sensitivity to other sulfonamide or thiazide-type medications may
PREGNANCY AND LACTATION
Not recommended in pregnancy and lactation.
MAIN SIDE/ADVERSE EFFECTS
• Gastro-intestinal disturbances such as nausea, vomiting, heart burn,
anorexia, diarrhoea and a metallic taste are usually mild and
• Skin rashes and pruritus.
• Severe, prolonged and sometimes fatal hypoglycaemia.
• Other severe effects may be manifestations of a hypersensitivity reaction
which includes cholestatic jaundice, leucopenia, thrombocytopenia, aplastic
anaemia, agranulocytosis, haemolytic anaemia, erythema multiforme or
Stevens-Johnson syndrome, exfoliative dermatitis and erythema nodosum.
• A syndrome of inappropriate secretion of antidiuretic hormone (SIADH)
characterized by water retention, hyponatraemia and central nervous effects
may infrequently be induced.
An odd interaction involves alcohol intolerance which is
similar to disulfiram-alcohol interaction. There is also an
increased risk of hypoglycaemia with alcohol.
• Compounds that may diminish the hypoglycaemic effect
and thus necessitate an increase in the dosage
requirement of the sulfonylurea include rifampicin and
thiazide diuretics, corticosteroids and estrogens.
• Compounds that may increase the hypoglycaemic effect
of sulfonylureas and necessitate a reduction in their
dosage requirement include anti-infective agents such as
chloramphenicol, guanetidine, monoamine oxidase
inhibitors, salicylates, sulfonamides, trimethoprim,
phenylbutazone, ketoconazole, miconazole, fluconazole,
sulphinpyrazone and azapropazone.
• A reversible decrease in thrombocyte count in patients
receiving ketotifen concomitantly with oral antidiabetic
agents has been observed in a few cases. Concurrent
administration of ketotifen should therefore be avoided.
• Beta-blockers may mask some of the symptoms of
hypoglycaemia. Also, beta-blockers may have
hypoglycaemic or hyperglycaemic actions of their own.
• The hypoglycaemic effect may be enhanced when
administered concurrently with insulin.
• If administered concurrently with anticoagulants,
increased plasma concentrations of both the
anticoagulant and sulfonylurea may occur initially; with
continued therapy, decreased anticoagulant plasma
concentrations and increased hepatic metabolism of the
sulphonylurea may occur; dosage adjustments of one or
both medications may be required.
Nausea and vomiting.
• Abdominal pain, (rarely) haematemesis and melaena.
• Drowsiness, coma, twitching, convulsions.
• Depressed limb reflexes with extensor plantar responses.
• Hyperapnoea, acute pulmonary oedema.
• Sinus tachycardia, hypotension, circulatory failure.
• Absence of sweating.
• Hypoglycaemia, hyperkalaemia, metabolic (lactic)
• Late complication cholestasis jaundice.
• Emesis or gastric lavage, if appropriate. Administration of
repeated doses of oral activated charcoal with
appropriate cathartic may also be used.
• Supportive measures.
• 50 ml of 50% glucose IV repeated as necessary and/or
glucagon 1 - 2 mg IV to correct hypoglycaemia, followed
by an IV infusion of 5 - 10% dextrose for 24 to 72 hours
• Treat mild hypoglycaemia with immediate ingestion of a source of sugar.
Oral, 40 to 80 mg daily, gradually increased, if necessary, up
to 320 mg daily. Doses of more than 160 mg daily should be
given in 2 divided doses.
Store below 30°C. Protect from moisture.
Blisters of 10 x 10's.