COMPOSITION: Each tablet contains 80 mg gliclazide
PHARMACOLOGICAL CLASSIFICATION: A 21.2 Oral hypoglycaemics
PHARMACOLOGICAL ACTION: Gliclazide is a sulphonylurea hypoglycaemic agent which causes hypoglycaemia by stimulating the release of insulin from the pancreatic ß cells and by increasing the sensitivity of the peripheral tissues to insulin. The predominant effect is on insulin secretion.
In studies involving experimental animals it has been suggested that gliclazide may reduce platelet adhesiveness and may prevent abnormal fibrin deposition on microsomal wall.
Gliclazide is well absorbed from the gastro-intestinal tract and it is extensively bound to plasma proteins.
The elimination half life is about 10 to 12 hours with peak plasma concentrations occuring 2 to 8 hours after administration.
Gliclazide is metabolised in the liver to metabolites without significant hypoglycaemic activity. Both unchanged medicine and metabolites are excreted in the urine.
INDICATIONS: To control hyperglycaemia in TYPE-II diabetics(non-insulin dependent or maturity onset diabetes mellitus) who cannot achieve appropriate control with dietary management alone.
CONTRA-INDICATIONS: Hypersensitivity to gliclazide or sulphonylureas. Contra-indicated in TYPE-I diabetes(insulin-dependent or juvenile diabetes), pregnancy, lactation and significant hepatic or renal insufficiency in which insulin is preferrably used.
Patients with ketoacidosis and in those with severe infection, stress, trauma, or other severe conditions where gliclazide is unlikely to control the hyperglycaemia; insulin should be administered in such situations.
Do not use in patients with severe impairment of thyroid function.
Considered unsafe in patients with acute porphyria.
WARNING: The administation of sulphonylureas may be associated with an increase in cardiovascular mortality as compared to treatment with diet alone or diet with insulin.
DOSAGE AND DIRECTIONS FOR USE: Treatment with gliclazide must be guided by the individual patient's response and this should be monitored frequently.
Gliclazide is used to supplement treatment by diet modification when such modification has not proved effective on it's own.
A reduction in dosage may be necessary in patients with renal dysfunction.
The usual initial oral dose of gliclazide is 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 two divided doses, morning and evening.
Combinations of insulin and gliclazide have been used in some patients with insulin dependent diabetes but because of the possibility of hypoglycaemia the blood sugar levels should be checked regularly.
In combined therapy with a biguanide there may be a greater risk of cardiovascular mortality than with the use of gliclazide alone.
SIDE EFFECTS AND SPECIAL PRECAUTIONS: Gastro-intestinal disturbances such as nausea, vomiting, heartburn, anorexia, diarrhoea and a metallic taste may occur, also increased appetite and weight gain may occur.
Manifestations of hypersensitivity reactions may include the following severe effects: rashes, cholestatic jaundice, leucopenia, thrombocytopenia, aplastic anaemia, agranulocytosis, haemolytic anaemia, erythema multiforme or Steven-Johnson Syndrome, exfoliative dermatitis, and erythema nodosum.
Care should be taken in the elderly, debilitated and malnourished patients; patients with adrenal or pituitary insufficiency; also those with impaired hepatic or renal function, as all are susceptible to the hypoglycaemic effects of sulphonylureas. During excessive exercise care should be taken as not to provoke hypoglycaemia.
Compounds that may diminish the hypoglycaemic effect of gliclazide include rifampicin, thiazide diuretics, adrenalin, chlorpromazine, corticosteroids, cyclophosphamide, diazoxide, gemfibrozil, isoniazid, oestrogens, oral contraceptives, phenytoin and thyroid hormones.
Compounds that may increase the hypoglycaemic effect of gliclazide include chloramphenicol, fluconazole, miconazole, sulphonamides, azapropazone, phenylbutazone, salicylates, coumarin, anticoagulants, heparin, cimetidine, ranitidine, clofibrate, mono-amine oxidase inhibitors and beta - adrenoreceptor blocking agents.
Ethanol may enhance the action of gliclazide by causing hypoglycaemia.
Beta blockers may mask some of the symptoms of hypoglycaemia.
About 10 to 15% of patients who receive sulphonylureas may develop an alcohol-induced flush.
In patients suffering from infections, traumas, shock or after anaesthesia, the dosage of gliclazide may have to be adjusted. Before major surgery, insulin therapy may be substituted for gliclazide.
KNOWN SYMPTOMS OF OVERDOSAGE AND PARTICULARS OF IT'S TREATMENT: In acute poisoning, the stomach should be emptied by emesis or lavage and hypoglycaemia should be treated with urgency.
The patient should be observed over several days in case hypoglycaemia recurs.
Further treatment is symptomatic and supportive.
IDENTIFICATION: A white, round, flat, bevelled tablet, bisected and imprinted with "G1" on one side and imprinted with a mortar and pestle on the other side.
PRESENTATION: Securitainers of 60 and 500 tablets.
STORAGE INSTRUCTIONS: Store in airtight containers below 25°C and protect from light. KEEP OUT OF THE REACH OF CHILDREN
REGISTRATION NUMBER: 31/21.2/0311
NAME AND ADDRESS OF APPLICANT: Pharmacare Limited
7 Fairclough Road
DATE OF PUBLICATION: 17 January 1997
New addition to this site:April 2005
Source: Hospital Pharmacy