Adult: Dosage is individualised based on patient’s blood glucose level. Conventional Conventional tab: Initially, 40-80 mg daily gradually increased to 320 mg daily if necessary. Doses >160 mg daily are given in 2 divided doses. Modified-release tab: Initially, 30 mg daily, may increase in increments of 30 mg up to max 120 mg daily if necessary. Interval between each dose increment must be at least 1 month. For non-respondent patients, dose may be increased after 2 weeks.
Should be taken with food.
Hypersensitivity to gliclazide, sulfonylureas or sulphonamides. Type 1 diabetes, diabetic pre-coma and coma, diabetic keto-acidosis. Severe renal and hepatic impairment. Concomitant use with miconazole Pregnancy and lactation.
Patient with risk factors of hypoglycaemia (e.g. malnourished, poorly compensated endocrine disorders, severe vascular disease), and with poor carbohydrate intake or imbalanced diet, stress-related states (e.g. trauma, infection, surgery), G6PD-deficiency. Mild to moderate hepatic and renal impairment.
Significant: Hypoglycaemia. Blood and lymphatic system disorders: Rarely, anaemia, leucopenia, thrombocytopenia, agranulocytosis, pancytopenia, haemolytic anaemia, erythrocytopenia. Endocrine disorders: Hyperglycaemia. Eye disorders: Rarely, visual disturbances. Gastrointestinal disorders: Abdominal pain, nausea, vomiting, dyspepsia, diarrhoea, constipation, gastrointestinal haemorrhage. General disorders and admin site conditions: Weakness. Hepatobiliary disorders: Rarely, cholestasis, jaundice, hepatitis. Infections and infestations: Viral infection. Investigations: Rarely, elevated hepatic enzyme levels, increased serum creatinine and BUN. Musculoskeletal and connective tissue disorders: Arthralgia, arthritis, back pain. Nervous system disorders: Headache, dizziness, signs of adrenergic counter-regulation including hyperhidrosis, clammy skin, anxiety, tachycardia, palpitations, angina pectoris, cardiac arrhythmia and hypertension. Renal and urinary disorders: UTI. Respiratory, thoracic and mediastinal disorders: Bronchitis, rhinitis, pharyngitis, upper respiratory tract infection, cough. Skin and subcutaneous tissue disorders: Rarely, rash, pruritus, urticaria, angioedema, erythema, maculopapular rashes, bullous reactions including Stevens-Johnson syndrome and toxic epidermal necrolysis, drug rash with eosinophilia and systemic symptoms.
Patient Counseling Information
This medicine may cause dizziness, drowsiness or loss of consciousness which may indicate a severe fall of blood sugar, if affected, do not drive or operate machinery. Adhere strictly to diabetic diet. Avoid severe or prolonged exercise.
Monitor fasting blood glucose, glycosylated Hb based on response, signs and symptoms of hypoglycaemia.
Symptoms: Hypoglycaemic reactions with or without coma, convulsions or other neurological disorders. Management: Consider carbohydrate intake, or modification of diet and dose adjustment. Administration of rapid IV injection of 50 mL (20-30%) concentrated glucose solution, followed by continuous infusion of 10% diluted glucose solution. Close monitoring is recommended.
Increased hypoglycaemic effect with phenylbutazone. May decrease metabolism with chloramphenicol. May enhance effect of anticoagulant agents (e.g. warfarin). May enhance hypoglycaemic effect with other antidiabetic agents (e.g. insulin, metformin, glucagon-like peptide-1 receptor agonists, acarbose, thiazolidinediones, dipeptidyl peptidase-4 inhibitors), ß-blockers, fluconazole, salicylates, ACE inhibitors (e.g. captopril, enalapril), H2-receptor blockers, MAOIs, sulfonamides, quinolone antibiotics, clarithromycin, and other NSAIDs. Increased blood glucose levels with chlorpromazine (at high doses), ß-agonists (e.g. salbutamol, ritodrine), tetracosactrin, glucocorticoids (with possible ketosis), and danazol. Potentially Fatal: Increased hypoglycaemic effect and possible onset of hypoglycaemia, or coma with miconazole.
May lead to onset of hypoglycaemic coma or increase of hypoglycaemic effect, and disulfiram-like reaction with alcohol. Decreased serum concentration with St. John’s Wort.
Description: Gliclazide is an antidiabetic sulphonylurea. It increases insulin sensitivity at peripheral target sites by stimulating insulin release from the pancreatic ß-cells and reducing insulin uptake and glucose output of the liver. It has haemovascular properties in which it decreases microthrombosis by restoring fibrinolysis with increase in tissue plasminogen activator (t-PA) activity, and by partial inhibition of platelet aggregation and adhesion. Duration: 24 hours (modified-release). Pharmacokinetics: Absorption: Conventional tab: Rapidly absorbed from the gastrointestinal tract. Modified release tab: Slow and complete. Bioavailability: 97% (modified-release). Bioavailability: 97% (modified-release). Time to peak plasma concentrations: 4-6 hours (immediate-release); approx 6 hours (modified-release). Distribution: Volume of distribution: 19 L (immediate-release); 30 L (modified-release). Plasma protein binding: Approx 94-95%. Metabolism: Hepatic by CYP2C9 and CYP2C19 to inactive metabolites. Excretion: Via urine (60-70% as metabolites; <1% as unchanged drug), faeces (10-20% as metabolites). Elimination half-life: 10-12 hours (immediate-release); 16 hours (modified-release).