Glibenclamide + Metformin

Generic Medicine Info
Indications and Dosage
Type 2 diabetes mellitus
Adult: Each tab contains glibenclamide (mg) and metformin (mg): 1.25/250, 2.5/500, 5/500: Patients inadequately controlled on diet and exercise: Initially, 1.25 mg/250 mg 1-2 times daily. Patients w/ HbA1c >9% or fasting plasma glucose (FPG) >200 mg/dL: Initially, 1.25 mg/250 mg bid. May adjust daily dose in increments of 1.25 mg/250 mg at intervals of not less than 2 wk. Max: Glibenclamide 10 mg and metformin 2,000 mg daily. Patients inadequately controlled on sulfonylurea and/or metformin: Initially, 2.5 mg/500 mg or 5 mg/500 mg bid. May adjust daily dose in increments not more than 5 mg/500 mg. Max: Glibenclamide 20 mg and metformin 2,000 mg daily.
Renal Impairment
CrCl (mL/min) Dosage
<60 Contraindicated.
Hepatic Impairment
Should be taken with food.
Diabetic ketoacidosis or diabetic pre-coma; acute conditions which may alter renal function (e.g. dehydration, severe infection, shock); acute or chronic disease which may cause tissue hypoxia (e.g. cardiac or resp failure, recent MI, acute significant blood loss, sepsis, gangrene); major surgery, porphyria. Acute alcohol intoxication/alcoholism. Renal (CrCl <60 mL/min) or hepatic impairment. Lactation. Concomitant use w/ bosentan, miconazole and intravascular admin of iodinated contrast materials.
Special Precautions
Patient w/ impaired adrenal and/or pituitary function, G6PD deficiency, heart failure. Pregnancy.
Adverse Reactions
Hypoglycaemia, haemolytic anaemia, wt gain, upper resp infection, diarrhoea, headache, nausea and vomiting, abdominal pain, dizziness.
Potentially Fatal: Lactic acidosis.
Patient Counseling Information
May impair ability to drive or operate machinery.
Monitoring Parameters
Monitor urine for glucose and ketones, FPG, HbA1c, and fructosamine; haematologic parameters, renal and hepatic function; vit B12 and folate levels (if anaemia is suspected); signs and symptoms of hypoglycaemia.
Symptoms: Mild to severe hypoglycaemia which may lead to hypoglycaemic coma (glibenclamide); lactic acidosis (metformin). Management: Mild hypoglycaemia w/o loss of consciousness may be treated w/ oral glucose. Severe hypoglycaemic reactions w/ coma, seizure or other neurological impairment require immediate hospitalisation. Admin rapid IV inj of glucose 50% soln in case of hypoglycaemic coma. Haemodialysis may be useful for removal of accumulated drugs in metformin overdose.
Drug Interactions
Decreased hypoglycaemic effect w/ thiazides and other diuretics, corticosteroids, phenothiazines, thyroid products, oestrogen, OC, phenytoin, nicotinic acid, sympathomimetics, Ca channel blockers, isoniazid. Glibenclamide: Increased hypoglycaemic effect w/ NSAIDs and other highly protein bound drugs, salicylates, sulfonamides, chloramphenicol, probenecid, coumarins, MAOIs, β-blockers. Decreased plasma concentration w/ colesevelam. Metformin: Increased plasma concentration w/ furosemide, nifedipine and cimetidine.
Potentially Fatal: Increased risk of hepatotoxicity w/ bosentan. Risk of severe hypoglycaemia w/ miconazole (systemic route, oromucosal gel). Alteration of renal function w/ iodinated contrast materials.
Food Interaction
Alcohol may potentiate the risk of lactic acidosis, avoid use.
Description: Glibenclamide stimulates insulin secretion from pancreatic β-cells, reduces glucose output from the liver and increases insulin sensitivity at peripheral target sites. Metformin reduces hepatic glucose production by inhibiting gluconeogenesis, delays intestinal glucose absorption and improves insulin sensitivity by increasing peripheral glucose uptake and utilisation.
Absorption: Glibenclamide: Readily absorbed from the GI tract. Time to peak plasma concentration: W/in 2-4 hr. Metformin: Slowly and incompletely absorbed from the GI tract. Bioavailability: Approx 50-60%. Time to peak plasma concentration: 2.5 hr.
Distribution: Glibenclamide: Plasma protein binding: Extensively bound (99%). Metformin: Crosses the placenta and enters breast milk (small amounts).
Metabolism: Glibenclamide: Almost completely metabolised in the liver. Metformin: Not metabolised in the liver.
Excretion: Glibenclamide: Via urine (approx 50%) and bile (50%) into the faeces. Metformin: Via urine, as unchanged drug. Elimination half-life: Approx 2-6 hr.
Chemical Structure

Chemical Structure Image

Source: National Center for Biotechnology Information. PubChem Database. Glyburide, CID=3488, (accessed on Jan. 22, 2020)

Chemical Structure Image

Source: National Center for Biotechnology Information. PubChem Database. Metformin, CID=4091, (accessed on Jan. 20, 2020)

Store at or below 25°C. Protect from light.
MIMS Class
Anon. Glyburide and Metformin. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. Accessed 21/10/2015.

Buckingham R (ed). Glibenclamide. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. Accessed 21/10/2015.

Buckingham R (ed). Metformin Hydrochloride. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. Accessed 21/10/2015.

Glyburide and Metformin Hydrochloride Tablet, Film Coated (Teva Pharmaceuticals USA Inc). DailyMed. Source: U.S. National Library of Medicine. Accessed 21/10/2015.

Disclaimer: This information is independently developed by MIMS based on Glibenclamide + Metformin from various references and is provided for your reference only. Therapeutic uses, prescribing information and product availability may vary between countries. Please refer to MIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, MIMS shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise. Copyright © 2021 MIMS. All rights reserved. Powered by
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