Adult: In patients with inadequate glycaemic control on diet and exercise alone: As conventional tab: Initially, 2.5-5 mg daily, adjusted in increments of 2.5 mg daily at weekly intervals based on patient's response. Max: 20 mg daily. Doses >10 mg daily may be given in 2 divided doses. As micronised tab: Initially, 1.5-3 mg daily, increased in increments of 1.5 mg at weekly intervals based on patient's response. Max: 12 mg daily. Doses >6 mg daily may be given in 2 divided doses. Elderly: Initiate at a lower dose.
Should be taken with food. Take w/ breakfast or the 1st main meal of the day.
Hypersensitivity to glibenclamide, other sulfonylureas or sulfonamides. Type 1 diabetes mellitus, diabetic ketoacidosis, diabetic coma or pre-coma, porphyria; stress-related states (e.g. trauma, surgical procedures, severe infection). Severe renal and hepatic impairment. Concomitant use with bosentan.
Patient with G6PD deficiency, adrenal or pituitary insufficiency; conditions that increase the risk of developing hypoglycaemia (e.g. insufficient calorie intake, strenuous exercise, irregular mealtimes or missed meals); atherosclerotic CV disease. Debilitated and malnourished patients. Conventional tab are not bioequivalent to micronised tab; dosage adjustment may be necessary when switching between dosage forms. Mild to moderate renal and hepatic impairment. Elderly. Pregnancy and lactation.
Significant: Haemolytic anaemia (particularly in G6PD-deficient patients). Eye disorders: Temporary visual impairment. Gastrointestinal disorders: Nausea, vomiting, heartburn, anorexia, metallic taste, epigastric fullness, abdominal pain, dyspepsia, diarrhoea. Hepatobiliary disorders: Cholestatic jaundice, hepatic failure, hepatitis. Immune system disorders: Hypersensitivity (including dyspnoea and swelling of the lips, face, throat or tongue). Investigations: Increased serum transaminases, weight gain. Metabolism and nutrition disorders: Increased appetite. Very rarely, disulfiram-like reactions. Skin and subcutaneous tissue disorders: Rash, pruritus, erythema, photosensitivity. Potentially Fatal: Hypoglycaemia, increased risk for CV mortality; changes in the blood picture (e.g. thrombocytopenia [presenting as purpura], leucopenia, agranulocytosis, pancytopenia).
PO: C (manufacturer specific), B (manufacturer specific)
Patient Counseling Information
This drug may cause impaired alertness and reactions, if affected, do not drive or operate machinery.
Obtain urine glucose test, fasting blood glucose; HbA1c (at least twice yearly in patients with stable glycaemic control and are meeting treatment goals; quarterly in patients who do not meet treatment goals or with therapy change). Monitor for signs and symptoms of hypoglycaemia during treatment.
Symptoms: Hypoglycaemia. Management: Consider giving activated charcoal in acute poisoning. For mild hypoglycaemia without loss of consciousness or neurological findings, treat aggressively with oral glucose and adjust drug dosage and/or meal patterns. For severe hypoglycaemia with coma, administer glucose 50% solution via rapid IV inj, followed by continuous infusion of glucose 10% solution to maintain blood glucose levels above 100 mg/dL. Alternatively, may administer glucagon 1 mg via SC or IM inj to regain consciousness. Closely monitor the patient for several days.
Increased hypoglycaemic effect with anti-infective agents (e.g. chloramphenicol, fluconazole, miconazole, sulfonamides), anabolic steroids, anti-inflammatory or analgesic agents (e.g. phenylbutazone, salicylates), dicoumarin anticoagulants and heparin, lipid regulating agents (e.g. clofibrate), certain antidepressants (MAOIs, doxepin, nortriptyline), ACE-inhibitors (e.g. captopril, enalapril), H2-blockers (e.g. cimetidine, ranitidine), fenfluramine, methyldopa and sulfinpyrazone. Diminished hypoglycaemic effect with rifampicin, thiazide diuretics, β-blockers, furosemide, ethacrynic acid, phenothiazines, oral contraceptives containing estrogens and corticosteroids. Impaired glucose tolerance with Ca channel blockers and lithium. May either potentiate or weaken the effect of coumarin derivatives. May increase plasma concentration of ciclosporin. Concurrent use with colesevelam may decrease the plasma concentration of glibenclamide; administer glibenclamide at least 4 hours before colesevelam. Potentially Fatal: Increased risk of hepatotoxicity with bosentan.
May enhance hypoglycaemic effect or cause a rare disulfiram-like reactions with alcohol.
Description: Glibenclamide lowers blood glucose concentration by stimulating the secretion of insulin from the pancreatic β-cells. Additionally, it reduces glucose output from the liver and increases insulin sensitivity at the peripheral target sites.
Synonym: glyburide. Onset: Increase in serum insulin levels: 15-60 minutes. Duration: ≤24 hours. Pharmacokinetics: Absorption: Rapidly and nearly completely absorbed from the gastrointestinal tract. Time to peak plasma concentration: 2-4 hours. Distribution: Crosses the placenta. Plasma protein binding: 99% (extensive), mainly to albumin. Metabolism: Almost completely metabolised in the liver into weakly active metabolites. Excretion: Via urine (50%) and faeces (50%) as metabolites. Elimination half-life: Approx 10 hours (conventional tab); approx 4 hours (micronised tab).
A10BB01 - glibenclamide ; Belongs to the class of sulfonylureas. Used in the treatment of diabetes.
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