Gliclazide is a sulfonylurea that has hypoglycemic and potentially useful haemovascular properties. It stimulates the influx of calcium ions into pancreatic β-cells and as a result increases insulin secretion. Moreover, in vivo studies have demonstrated changes in thrombin-induced platelet aggregation in NIDDM patients treated with Gliclazide.
Pharmacology: Pharmacodynamics: Gliclazide has pharmacological actions common to all sulfonylurea drugs. Their primary effect is to potentiate glucose-stimulated insulin release from functioning β-cells of pancreatic islets. The mechanism by which this occurs has been elucidated in recent years.
Pharmacokinetics: Gliclazide is well-absorbed. The mean plasma half-life is 10 h (6-14 h) and the volume of distribution is about 17-25 L (15-40% of body weight). About 95% (85-97%) of Gliclazide is bound to protein in plasma, mostly to Albumin. Gliclazide is extensively metabolized and less than 20% is excreted in the urine in unchanged form. The hydroxy metabolites can be subsequently glucuronidated. Gliclazide is oxidized in the body in both the azobicyclooctyl portion of the molecule, to produce either hydroxylated metabolites or N-oxygenated compounds, and in the P-tolyl grouping, to produce the corresponding alcohol and carboxylic acid.
Non-insulin dependent diabetes mellitus (type-II) when dietary modification has failed to provide adequate glycemic control.
Initially 40-80 mg daily, adjusted according to response; up to 160 mg as a single dose, with breakfast; higher doses divided, maximum 320 mg daily.
Gliclazide is contraindicated in children. Gliclazide, as other sulfonylurea, is contraindicated in pregnant women. The use of Gliclazide is also contraindicated in: Hypersensitivity to Gliclazide or other sulfonylureas or sulfonamides, or to any of the excipients;
insulin dependent, particularly juvenile diabetes, diabetes complicated by ketosis and acidosis, or diabetic pre-coma or coma;
severe hepatic or renal insufficiency; concomitant treatment with miconazole (see Interactions).
In general, concomitant administration with phenylbutazone, danazol and alcohol is not recommended.
All sulfonylureas should be used with caution in the elderly because of the greater likelihood of their missing meals and the more severe outcome of significant hypoglycemia.
Hypoglycemia may occur in some patients and may be severe and prolonged, requiring hospitalisation and blood sugar level monitoring for several days.
Careful monitoring of the dosage may be necessary for patients with adrenal insufficiency or hypopituarism, or are on beta-blockers.
Renal or hepatic insufficiency may alter the distribution of Gliclazide and increase the risk of hypoglycaemic reactions.
Blood and urine glucose levels should be monitored regularly.
The risk of hypoglycaemia, its symptoms and treatment, and the predisposing factors should be explained to the patient.
Neonates: The drug is not used in neonates.
Nursing mothers: The drug should not be used by nursing mothers.
Pregnancy: Gliclazide, as other sulfonylurea, is contraindicated in pregnant women.
Sulfonylureas are teratogenic in animals at high doses, and is not to be given during pregnancy. Change from oral treatment to insulin is recommended if pregnancy is planned.
Potentially life-threatening effects: All hypoglycemic agents have the potential to cause severe hypoglycemia and may cause severe brain damage or death. Gliclazide used in standard dose is less likely than Glyburide to cause hypoglycemia. Hypoglycemia may be precipitated by concurrent conditions such as hepatic and renal disease, malnutrition, anorexia, senility, alcohol intoxication or adrenal and pituitary insufficiency.
Severe or irreversible adverse effects: Approximately 2% of patients have been withdrawn from therapy because of adverse reactions, namely hypoglycemia (overdose effect), gastrointestinal disturbances and dermatological reactions.
Symptomatic adverse effects: Side effects of Gliclazide treatment are similar to those of other sulfonylureas. Headache, gastrointestinal upsets, nausea, and dizziness have been reported and skin reactions, including rash, pruritus, erythema and bullous eruptions may occur. Abnormalities of liver function (e.g. elevations of AST, ALT, and/or alkaline phosphatase) may occur. Hepatitis has been rarely reported. Treatment should be discontinued if cholestatic jaundice occurs.
Hematological effects including anemia, leucopenia, and thrombocytopenia have been reported.
Potentially hazardous interactions: These may be divided into those which will tend to increase the hypoglycemic effect and those tending to oppose it. In the first category come drugs which displace the sulfonylurea from protein binding, such as aspirin, non-steroidal anti-inflammatory drugs, phenylbutazone, clofibrate, sulfonamides and coumarin anticoagulants, or which inhibit hepatic microsomal enzymes, for example cimetidine, sulfonamides, imidazole antifungal agents and monoamine oxidase inhibitors (MAOI), which may increase the hypoglycemic effect of Gliclazide.
The hypoglycemic action of sulfonylureas may be opposed by the induction of hepatic enzymes, which metabolize the drug causing lower plasma concentrations and less hypoglycemic effect. Common inducers include rifampicin, barbiturates, phenytoin and alcohol, or by drugs that inhibit the release or action of insulin, e.g. thiazide diuretics, dizoxide, glucocorticoids, estrogens or sympathomimetic drugs. Early symptoms of hypoglycemia such as tremor, sweating and tachycardia may be masked by β-adrenoreceptor blocking drugs, such as propranolol allowing severe hypoglycemic episodes without preceding warning symptoms.
A10BB09 - gliclazide ; Belongs to the class of sulfonylureas. Used in the treatment of diabetes.
Diapro tab 80 mg
5 × 10's
Sign Out
