Glucophage XR

Reduction in risk or delay of type 2 DM onset in adults, overwt patients w/ impaired glucose tolerance & fasting glucose &/or increased HbA1c who are at high risk for developing overt type 2 DM & still progressing towards type 2 DM despite implementing intensive lifestyle change for 3-6 mth. Monotherapy or in combination w/ other oral antidiabetic agents or w/ insulin for type 2 DM in adults when dietary management & exercise alone results in inadequate glycaemic control. 500 & 750 mg: Reduction of diabetic complications in overwt type 2 diabetic patients treated w/ IR metformin as 1st-line therapy after diet failure.

Adult w/ normal renal function (GFR ≥90 mL/min) Initially 1 500-mg tab once daily, adjusted based on blood glucose measurements after 10-15 days. Dosage may be increased every 10-15 days up to max: 4 500-mg or 2 750-mg or 2 1,000-mg tab daily. Patient already treated w/ metformin Initially same daily dose of metformin IR tab. Transfer from another oral antidiabetic agent Discontinue the other agent & initiate as indicated. Combination w/ insulin 500 or 750 mg daily, adjust insulin dose based on blood glucose measurements. Renal impairment GFR 45-89 mL/min Max: 2,000 mg daily, GFR 30-44 mL/min Max: 1,000 mg daily.

Should be taken with food: Take w/ evening meal.

Hypersensitivity. Any type of acute metabolic acidosis eg, lactic acidosis, diabetic ketoacidosis. Diabetic pre-coma; acute conditions w/ potential to alter renal function eg, dehydration, severe infection, shock; disease causing tissue hypoxia eg, decompensated heart failure, resp failure, recent MI. Acute alcohol intoxication, alcoholism. Severely reduced renal function (GFR <30 mL/min), hepatic insufficiency.

Temporarily discontinue use if dehydration occurs; in presence of conditions altering renal function. Not recommended in patients w/ known mitochondrial diseases eg, mitochondrial encephalomyopathy w/ lactic acidosis & stroke-like episodes syndrome (MELAS) & maternal inherited diabetes & deafness (MIDD). Lactic acidosis. Patients w/ inadequately controlled diabetes, ketosis, prolonged fasting, conditions associated w/ hypoxia; stable chronic heart failure. May reduce vit B₁₂ serum levels. Assess renal function prior to initiation & regularly thereafter. Regularly monitor cardiac function; perform usual lab tests for diabetes monitoring. Overwt patients should continue energy-restricted diet. Discontinue prior to, during or 48 hr after use of intravascular iodinated contrast agents & surgery under general, spinal or epidural anaesth. Hypoglycaemia w/ insulin or other antidiabetics eg, sulfonylureas, meglitinides. Concomitant use w/ antihypertensives, diuretics, NSAIDs. Pregnancy. Not recommended during lactation. Not to be used in childn. Not recommended in elderly ≥75 yr.

GI disorders eg, nausea, vomiting, diarrhoea, abdominal pain, loss of appetite. Vit B₁₂ decrease/deficiency; taste disturbance.

Increased risk of lactic acidosis w/ alcohol intoxication; NSAIDs including selective COX-2 inhibitors, ACE inhibitors, AIIA, diuretics especially loop diuretics. Reduced efficacy w/ OCT1 inhibitors eg, verapamil. Increased GI absorption & efficacy w/ OCT1 inducers eg, rifampicin. Increased plasma conc w/ OCT2 inhibitors eg, cimetidine, dolutegravir, ranolazine, trimethoprim, vandetanib, isavuconazole. Altered efficacy & renal elimination w/ OCT1 & OCT2 inhibitors eg, crizotinib, olaparib. More frequent blood glucose monitoring in drugs w/ intrinsic hyperglycaemic activity eg, systemic & local glucocorticoids, sympathomimetics.

Antidiabetic Agents

A10BA02 - metformin ; Belongs to the class of biguanides. Used in the treatment of diabetes.

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