Glucophage, with the active ingredient metformin hydrochloride, is a foundational oral antihyperglycemic agent classified as a biguanide. It is widely recognized as a first-line pharmacological intervention in the management of type 2 diabetes mellitus, both as monotherapy and in combination with other antidiabetic agents or insulin. Its primary mechanism of action involves decreasing hepatic glucose production, reducing intestinal absorption of glucose, and improving insulin sensitivity by increasing peripheral glucose uptake and utilization. By addressing core pathophysiological defects of the disease, Glucophage provides a robust and well-established approach to glycemic control.

Features

• Active Ingredient: Metformin Hydrochloride
• Drug Class: Biguanide antihyperglycemic
• Available Formulations: Immediate-release tablets (500 mg, 850 mg, 1000 mg) and extended-release tablets (500 mg, 750 mg)
• Primary Mechanism: Reduces hepatic gluconeogenesis and enhances peripheral insulin sensitivity
• Prescription Status: Available by prescription only

Benefits

• Achieves significant and sustained reductions in both fasting and postprandial plasma glucose levels.
• Lowers HbA1c (glycated hemoglobin) by an average of 1–2%, a key marker for long-term glycemic control.
• Is not associated with weight gain and may promote modest weight loss, a distinct advantage over many other antidiabetic therapies.
• Has a neutral or potentially beneficial effect on lipid profiles, often reducing triglycerides and LDL cholesterol.
• Carries a very low risk of hypoglycemia when used as monotherapy, as its action is glucose-dependent.
• May offer cardiovascular protective benefits, as evidenced by long-term outcome studies.

Common use

Glucophage (metformin) is indicated as an adjunct to diet and exercise to improve glycemic control in adults and pediatric patients 10 years of age and older with type 2 diabetes mellitus. It is the most commonly prescribed initial medication upon diagnosis. It is also used off-label for the management of polycystic ovary syndrome (PCOS) to address insulin resistance and support ovulation regulation.

Dosage and direction

Dosage must be individualized based on efficacy and tolerance, under the direction of a physician. The usual starting dose for adults is 500 mg twice daily or 850 mg once daily with meals. Dosage may be increased gradually, typically at weekly intervals, to minimize gastrointestinal side effects. The maximum recommended daily dose is 2550 mg administered in divided doses for the immediate-release formulation and 2000 mg for the extended-release formulation. The extended-release tablets must be swallowed whole and never crushed or chewed. It is crucial to take Glucophage with meals to reduce gastrointestinal upset.

Precautions

Prior to initiation, assess renal function through estimated glomerular filtration rate (eGFR). Avoid use in patients with an eGFR below 30 mL/min/1.73m². Use with caution in patients with an eGFR between 30-45 mL/min/1.73m². Withhold Glucophage for any condition associated with hypoxemia (e.g., CHF, sepsis), dehydration, or acute hemodynamic instability due to the increased risk of lactic acidosis. Temporarily discontinue before any surgical procedure or radiographic study involving intravascular iodinated contrast materials; therapy may be restarted 48 hours after the procedure upon confirmation of normal renal function. Monitor vitamin B12 levels annually or biannually, as long-term use can impair its absorption.

Contraindications

Glucophage is strictly contraindicated in patients with severe renal impairment (eGFR < 30 mL/min) or renal disease. It is also contraindicated in patients with known hypersensitivity to metformin or any ingredient in the formulation. Use is prohibited in patients with metabolic acidosis, including diabetic ketoacidosis, which should be treated with insulin. Acute or chronic disease states that may cause tissue hypoxia, such as congestive heart failure requiring pharmacologic management, hepatic disease, or alcohol abuse, are also contraindications.

Possible side effect

The most common adverse reactions are gastrointestinal in nature and often transient, including diarrhea, nausea, vomiting, abdominal bloating, flatulence, anorexia, and a metallic taste. These effects are frequently dose-related and may be mitigated by taking the medication with food and using a gradual dose titration schedule. A rare but serious side effect is lactic acidosis, presenting with symptoms like malaise, myalgia, respiratory distress, somnolence, and abdominal pain; this constitutes a medical emergency. Long-term use can lead to vitamin B12 deficiency, which may manifest as megaloblastic anemia.

Drug interaction

Concomitant administration of drugs that impair renal function (e.g., NSAIDs, certain antihypertensives) can increase metformin accumulation. Cationic drugs (e.g., amiloride, digoxin, morphine, procainamide, quinidine, quinine, ranitidine, trimethoprim, vancomycin) that are eliminated by renal tubular secretion may interact with metformin by competing for common renal tubular transport systems, potentially increasing the peak concentration of both drugs. Alcohol potentiates the effect of metformin on lactate metabolism and increases the risk of lactic acidosis; excessive alcohol intake is to be avoided. Glucophage may require dose adjustment when starting or stopping other hyperglycemic agents, including insulin, to maintain glycemic control and avoid hypoglycemia.

Missed dose

If a dose is missed, it should be taken as soon as remembered, unless it is almost time for the next scheduled dose. In that case, the missed dose should be skipped, and the regular dosing schedule resumed. Do not take a double dose to make up for a missed one.

Overdose

Hypoglycemia has not been reported with metformin overdose alone but may occur when Glucophage is taken in conjunction with other glucose-lowering agents. The primary risk of a significant metformin overdose is lactic acidosis, which is a medical emergency characterized by electrolyte imbalances and an elevated blood lactate level. Symptoms include severe nausea, vomiting, diarrhea, hyperventilation, malaise, and progressing to circulatory collapse. Management involves immediate hospitalization, supportive care, and hemodialysis, which is effective in correcting acidosis and removing accumulated metformin.

Storage

Store Glucophage tablets at controlled room temperature, 20°C to 25°C (68°F to 77°F), in a tightly closed container. Protect from moisture and light. Keep all medications out of the reach of children and pets. Do not flush medications down the toilet or pour them into a drain. Dispose of unused or expired medication through a medicine take-back program or according to local guidelines.

Disclaimer

This information is for educational purposes only and is not a substitute for professional medical advice, diagnosis, or treatment. Always seek the advice of your physician or other qualified health provider with any questions you may have regarding a medical condition or before starting any new treatment. Never disregard professional medical advice or delay in seeking it because of something you have read here.

Reviews

“Glucophage has been the cornerstone of my type 2 diabetes management for over a decade. Its efficacy in controlling my blood sugar without causing weight gain or significant hypoglycemic episodes has been remarkable. The initial gastrointestinal side effects subsided after the first few weeks.” – M.B., Patient

“As an endocrinologist, metformin remains my first-line go-to pharmacotherapy for new-onset type 2 diabetes. Its efficacy, safety profile, beneficial metabolic effects, and low cost make it an unparalleled choice. Managing the initial GI tolerance is key to long-term adherence.” – Dr. A.S., Endocrinologist

“After my diagnosis, my doctor started me on a low dose of Glucophage and gradually increased it. While I experienced some bloating at first, it resolved. My HbA1c dropped from 8.5% to 6.2% within six months, and I lost a modest amount of weight, which was a welcome bonus.” – R.T., Patient