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.
Renal Impairment
Severe: Contraindicated.
Hepatic Impairment
Severe: Contraindicated.
Administration
Should be taken with food. Take w/ breakfast or the 1st main meal of the day.
Contraindications
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.
Special Precautions
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.
Adverse Reactions
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.
Monitoring Parameters
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.
Overdosage
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.
Drug Interactions
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.
Food Interaction
May enhance hypoglycaemic effect or cause a rare disulfiram-like reactions with alcohol.
Action
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).
Chemical Structure
Glibenclamide Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 3488, Glyburide. https://pubchem.ncbi.nlm.nih.gov/compound/Glyburide. Accessed Sept. 26, 2022.
A10BB01 - glibenclamide ; Belongs to the class of sulfonylureas. Used in the treatment of diabetes.
References
Anon. Glibenclamide (Glyburide). Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 07/07/2022.Anon. Glyburide. AHFS Clinical Drug Information [online]. Bethesda, MD. American Society of Health-System Pharmacists, Inc. https://www.ahfscdi.com. Accessed 07/07/2022.Buckingham R (ed). Glibenclamide. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 07/07/2022.Daonil (PT Aventis Pharma). National Pharmaceutical Regulatory Agency - Ministry of Health Malaysia. https://www.npra.gov.my. Accessed 07/07/2022.Glibenclamide 2.5 mg Tablets (Milpharm Limited). MHRA. https://products.mhra.gov.uk. Accessed 07/07/2022.Glyburide Tablets (Amneal Pharmaceuticals of New York LLC). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 07/07/2022.Glynase PresTab (Pharmacia and Upjohn Company LLC). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 07/07/2022.Sanofi-Aventis New Zealand Limited. Daonil 5 mg Tablets data sheet 25 August 2017. Medsafe. http://www.medsafe.govt.nz. Accessed 07/07/2022.
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