Adult: Glimepiride 1 mg and metformin 500 mg sustained-release tab
Glimepiride 2 mg and metformin 500 mg sustained-release tab
Glimepiride 2 mg and metformin 1,000 mg sustained-release tab
As an adjunct to diet and exercise: 1 tab once daily. Dose must be individualised according to patient's response and tolerability. Max: 8 mg glimepiride/2,000 mg metformin daily. Dosage and available fixed-dose combinations may vary between countries (refer to detailed product guidelines).
What are the brands available for Glimepiride + Metformin in Indonesia?
Should be taken with food. Take w/ meals to reduce GI discomfort. ER Tab: Swallow whole & do not break/crush.
Contraindications
Hypersensitivity to glimepiride, metformin, other sulfonylureas or sulfonamides. Type 1 diabetes mellitus; acute or chronic metabolic acidosis, including diabetic pre-coma/coma and diabetic ketoacidosis; acute conditions that may alter renal function (e.g. dehydration, shock); acute or chronic diseases associated with hypoxia (e.g. heart failure, acute or recent MI, respiratory failure); acute alcohol intoxication or alcoholism. Hepatic and severe renal impairment. Pregnancy. Concomitant intravascular administration of iodinated contrast agents. Contraindications may vary among countries and between individual products (refer to specific product guidelines).
Special Precautions
Patient with G6PD deficiency, stable heart failure; stress-related states (e.g. fever, trauma, infection), risk factors for hypoglycaemia (e.g. deficient caloric intake, malnutrition, impaired adrenal or pituitary function, after prolonged exercise). Withhold treatment at the time of surgical procedures; may restart treatment once renal function is stable. Mild to moderate renal impairment. Elderly. Lactation.
Adverse Reactions
Significant: Hypoglycaemia; increased risk of sulfonylurea-induced haemolytic anaemia (particularly in patients with G6PD deficiency); vitamin B12 deficiency (prolonged use). Blood and lymphatic system disorders: Rarely, thrombocytopenia, leucopenia. Eye disorders: Visual impairment. Gastrointestinal disorders: Nausea, vomiting, abdominal pain, diarrhoea, sensation of fullness in epigastrium. Hepatobiliary disorders: Cholestasis, jaundice, hepatitis. Investigations: Increased liver enzymes, decreased serum Na level. Skin and subcutaneous tissue disorders: Photosensitivity, skin rash, urticaria, pruritus. Potentially Fatal: Lactic acidosis.
Patient Counseling Information
This drug may impair the ability to react due to hypoglycaemia, if affected, do not drive or operate machinery.
Monitoring Parameters
Obtain plasma glucose (frequency depends on individual treatment regimen, hypoglycaemia risk and other patient-specific factors); HbA1c (twice yearly for those with stable glycaemic control; quarterly in patients not meeting treatment goals or with changes in treatment). Monitor renal function (before initiation and annually during treatment), haematologic parameters such as Hb/haematocrit, RBC indices (annually), volume status (e.g. blood pressure, electrolytes, haematocrit), and vitamin B12 serum concentrations (in patients on long-term therapy).
Overdosage
Symptoms: Hypoglycaemia which may be mild or severe; severe hypoglycaemia may be accompanied by convulsions/other neurological disorders and coma. Metformin: Lactic acidosis. Management: Administer oral glucose and adjust the dose and/or meal patterns for mild hypoglycaemia without loss of consciousness or neurological findings. In case of suspected or diagnosed hypoglycaemic coma, give rapid IV inj of concentrated (50%) glucose solution, followed by continuous infusion of a more dilute (10%) glucose solution at a rate that will maintain >100 mg/dL blood glucose levels. Haemodialysis may be considered to remove accumulated metformin.
Drug Interactions
Increased risk of hypoglycaemia with insulin or other oral antidiabetic agents. Diminished hypoglycaemic effect with thiazides and corticosteroids.
Glimepiride: Increased risk of hypoglycaemia with ACE inhibitors, β-blockers, guanethidine, chloramphenicol, tetracyclines, quinolones, sulfonamides, miconazole, coumarin derivatives, cyclophosphamide, disopyramide, fibrates, fluoxetine, MAOIs, phenylbutazone, probenecid, pentoxifylline (high dose), allopurinol, anabolic steroids, and male sex hormones. May result in hyperglycaemia with barbiturates, acetazolamide, diazoxide, epinephrine or other sympathomimetics, glucagon, laxative (after prolonged use), nicotinic acid (high doses), phenothiazines, estrogens, progestogen, phenytoin, and rifampicin. May potentiate or weaken the blood glucose lowering effect with histamine (H2) antagonists, clonidine, and reserpine.
Metformin: Increased risk of lactic acidosis with carbonic anhydrase inhibitors (e.g. topiramate), diuretics, antihypertensive agents, and NSAIDs. May increase serum concentration with cimetidine. Potentially Fatal: Metformin: Concomitant administration of iodinated contrast media may result in renal dysfunction which may increase the risk of metformin-associated lactic acidosis.
Food Interaction
Increased risk of hypoglycaemia and lactic acidosis with alcohol.
Action
Description: Mechanism of Action: Glimepiride, a sulfonylurea, reduces blood glucose levels by stimulating insulin release from pancreatic β-cells. It also decreases glucose output from the liver and increases insulin sensitivity at peripheral target sites.
Metformin, a biguanide antihyperglycaemic agent, improves glucose tolerance by lowering both basal and postprandial plasma glucose levels. It reduces hepatic glucose production, decreases intestinal glucose absorption, and improves insulin sensitivity by increasing peripheral glucose uptake and utilisation. Onset: Metformin: Within days. Duration: Glimepiride: 24 hours. Pharmacokinetics: Absorption: Glimepiride: Completely absorbed from the gastrointestinal tract. Time to peak plasma concentration: 2-3 hours.
Metformin: Slowly and incompletely absorbed from the gastrointestinal tract. Absolute bioavailability: 50-60%. Time to peak plasma concentration: 7 hours (range: 4-8 hours). Distribution: Glimepiride: Volume of distribution: 8.8 L. Plasma protein binding: >99.5%.
Metformin: Partitions into erythrocytes; concentrates in the liver, kidney, salivary gland, and gastrointestinal tract. Crosses the placenta; enters breast milk (small amounts). Volume of distribution: 654 ± 358 L. Metabolism: Glimepiride: Extensively metabolised in the liver via oxidation by CYP2C9 into M1 metabolite, then undergoes further oxidative metabolism by cytosolic enzymes into inactive M2 metabolite.
Metformin: Not metabolised. Excretion: Glimepiride: Via urine (60%; 80-90% as M1 and M2 metabolites); faeces (40%; 70% as M1 and M2 metabolites). Elimination half-life: 5-9 hours.
Metformin: Via urine (90% as unchanged drug). Elimination half-life: 4-9 hours (plasma); approx 17.6 hours (blood).
Chemical Structure
Glimepiride Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 3476, Glimepiride. https://pubchem.ncbi.nlm.nih.gov/compound/Glimepiride. Accessed Apr. 29, 2025.
Metformin Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 4091, Metformin. https://pubchem.ncbi.nlm.nih.gov/compound/Metformin. Accessed Apr. 29, 2025.
Storage
Store below 30°C. Protect from light and moisture.
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