Diolin (Glibenclamide BP 5mg)
Oral Anti-diabetic agents (Sulfonamides). Glibenclamide is a sulfonylurea which lowers the blood glucose concentrations by increasing sensitivity of pancreatic beta cells to glucose, resulting in stimulation of insulin release.
Glibenclamide is rapidly absorbed and is extensively plasma protein bound, not readily displaced by acidic drugs. Extensively metabolized in liver & excreted as metabolites in urine & bile.
Glibenclamide tablet is indicated for treatment of non-insulin dependent diabetes in patients who respond inadequately to dietary measures alone.
In patients with known hypersensitivity to glibenclamide or any of the excipients, diabetic ketoacidosis or diabetic coma/precoma, insulin dependent diabetes mellitus, severe impairment of renal, hepatic, thyroid or adrenocortical function, unusual stress circumstances.
Special precautions and warning
patients with rare hereditary problems of galactose intolerance, Lapp lactase deficiency or glucose galactose malabsorption. Discontinue if clinical jaundice occurs.
Use with caution in elderly, during pregnancy & lactation, adrenal or pituitary insufficiency, debilitated or malnourished patients, particularly susceptible to hypoglycaemia.
Dosage and administration
Previously untreated diabetes: stabilize with Glibenclamide 5mg daily immediately after first meal with increments of 2.5mg weekly. No additional effects on dosage above 15mg/day
In debilitated patients or aged/patients: Initiate with one 2.5mg/daily.
Changeover from other sulphonylureas: initiate with equivalent dose of glibenclamide without exceeding initial dose of 10mg which can be raised step wise, to 15mg daily. Glibenclamide, 5mg is approximately equivalent to 1g tolbutamine or glymidine, 250mg chlorpropamide or tolazamide, 500mg acetohexamide, 25mg glibomuride or 5mg glipizide.
Changeover from biguanides: Withdraw biguanide and start glibenclamide with 2.5mg with increments of 2.5mg to achieve control. Control may be established by combined administration of glibenclamide & biguanide derivative. Glibenclamide is not recommended for use in children.
Hypoglycaemia, headache, ravenous hunger, nausea, vomiting, lassitude, sleepiness, disordered sleep, restlessness, aggressiveness, impaired concentration, alertness and reactions, depression, confusion, speech disorders, aphasia, visual disorders tremor, pareses, sensory disturbances, dizziness, helplessness, loss of self-control, delirium, cerebral convulsions, somnolence and loss of consciousness up to and including coma, shallow respiration and bradycardia.
Rarely, thrombocytopenia, leucopenia, agranulocytosis, pancytopenia, haemolytic anaemia, erythrrocytopenia, granulocytopenia, hypersensitivity, temporary visual impairment, abdominal pain, diarrhea, elevation of liver enzyme.
Elevation of liver enzymes in patients receiving glibenclamide wit bosentan.
Hypoglycaemia may be increased by antiinfective agents (chloramphenicol, fluconazole, miconazole, sulphonamides co-trimoxazole), anti-inflammatory/analgesic agents (phenylbutazone, salicylates), dicoumarin anticoagulants and heparin, lipid regulating agents (clofibrate), antidepressants (MAO inhibitors, doxepin, nortriptyline), ACE-inhibitors; captopril, enalapril, H2-blockers; cimetidine, ranitidine, fenfluramine, methyldopa and sulphinpyrazone.
Hypogycaemia may be diminished by rifampicin, thiazide diuretics & ß-blockers.
Alcohol may interact, provoking facial flushing, with variable effect on blood sugar levels. Glibenclamide alters effect of coumarin derivatives & raises plasma levels of ciclosporin.