Glucophage/Glucophage Forte/Glucophage XR

Type 2 DM particularly in overwt, when dietary management & exercise does not result in adequate glycemic control: 1st-line therapy in overwt type 2 diabetic adult patients. Prevention of type 2 DM in patients w/ prediabetes & at least 1 additional risk factor in whom lifestyle modifications alone have not reached adequate glycemic control. Glucophage Monotherapy or in combination w/ other oral antidiabetics or w/ insulin in adults. Monotherapy or in combination w/ insulin in childn from 10 yr & adolescent. Glucophage XR Ovulation stimulation to support conception in women w/ PCOS. Monotherapy or in combination w/ other treatment options.

Glucophage/Glucophage Forte Adult Monotherapy or in combination w/ other oral antidiabetic agents Initially 500 mg or 850 mg bid or tid. Max: 3 g daily as 3 divided doses. Monotherapy in prediabetes 1,000-1,700 mg/day divided in 2 doses given during or after meals. Combination w/ insulin Initially 500 mg or 850 mg bid or tid, while insulin dosage is adjusted on the basis of blood glucose measurements. Childn from 10 yr & adolescent Monotherapy or in combination w/ insulin 500 mg or 850 mg once daily. Max: 2 g daily as 2 or 3 divided doses. Glucophage XR Monotherapy or in combination w/ other oral antidiabetic agents Initially 500 mg or 750 mg once daily w/ the evening meal. Maintenance therapy: 1 g for patients already treated w/ metformin. Dose adjustment based on blood glucose measurements is recommended after 10-15 days. A slow increase of dose may improve GI tolerability. Max recommended dose for 500 mg: 4 tab daily. Recommended dose of 750 mg: 2 tab once daily. If glycemic control is still not achieved on 2 tab of 750 mg once daily, may be increased to a max dose of 3 tab daily. Max recommended dose of 1 g: 2 tab daily. Combination w/ insulin Initially 500 mg or 750 mg once daily, while insulin dosage is adjusted on the basis of blood glucose measurements. Monotherapy for prediabetes 1,000-1,500 mg once daily. Moderate renal impairment stage 3 CrCl 30-59 mL/min or eGFR 30-59 mL/min/1.73 m² Starting dose: 500 mg or 850 mg daily. Max daily dose: 1,000 mg. Ovulation stimulation to support conception in women w/ PCOS 1,500-2,000 mg once daily. Max: 2,000 mg once daily w/ evening meal. Glucophage XR should be considered for at least 6 mth.

Should be taken with food: XR tab: Swallow whole, do not chew/crush. Must be taken daily w/o interruption w/ evening meal.

Hypersensitivity. Any type of metabolic acidosis (eg, lactic acidosis, diabetic ketoacidosis). Diabetic pre-coma. Acute conditions w/ the potential to alter renal function eg, dehydration, severe infection or shock; acute or chronic disease which may cause tissue hypoxia eg, unstable CHF, resp failure, recent MI or shock. Severe renal failure (CrCl <30 mL/min or eGFR <30 mL/min/1.73 m²). Hepatic insufficiency, acute alcohol intoxication, alcoholism. Iodinated contrast materials in radiodiagnostic exam can lead to renal failure. Discontinue 48 hr before the test in patients w/ CrCl <45 mL/min or eGFR <45 mL/min/1.73 m² for IV administration or w/ CrCl <60 mL/min or eGFR <60 mL/min/1.73 m² for intra-arterial administration. Discontinue 48 hr prior to elective major surgical interventions & may not be reinstituted until 48 hr afterwards.

Caution to situations where renal function may be acutely impaired in case of dehydration (severe or prolonged diarrhea or vomiting), when initiating drugs (eg, antihypertensives, diuretics & NSAIDs). Report of lactic acidosis in diabetic patients w/ acute renal failure or acute worsening of renal function. Not recommended in patients w/ known mitochondrial diseases eg, mitochondrial encephalomyopathy w/ lactic acidosis & stroke-like episodes (MELAS) syndrome & maternal inherited diabetes & deafness (MIDD). Immediately w/draw treatment in case of signs & symptoms suggestive of MELAS syndrome or MIDD. Regular monitoring of cardiac & renal function in patients w/ stable chronic heart failure. Patient should continue following dietary advice. Regularly perform usual lab tests for diabetes monitoring. Periodic vit B₁₂ monitoring in patients w/ risk factor for vit B₁₂ deficiency. Caution in combination w/ insulin, sulphonylureas or meglitinides. Alert patients of the risk of hypoglycemia in combination w/ other antidiabetic agents when driving or using machines. Avoid consumption of alcohol & alcohol-containing medicinal products. Pregnancy. Breastfeeding is not recommended during treatment. Glucophage/Glucophage Forte Confirmation of diagnosis of type 2 DM before initiation of treatment in childn from 10 yr & adolescents. Careful follow-up in childn especially pre-pubescent childn. Glucophage XR May result in ovulation in anovulatory women leading to unintended pregnancy in premenopausal women. Advise patients that it is normal that tab shells may be present in feces, & not linked w/ a decrease in therapeutic activity. Not recommended for use in childn.

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

More frequent blood glucose monitoring may be required, especially at the beginning of treatment w/ medicinal products w/ intrinsic hyperglycemic activity [eg, glucocorticoids & tetracosactides (systemic & local routes), β₂ agonists, danazol, chlorpromazine at high dose (100 mg/day) & diuretics]. Increased risk of lactic acidosis w/ diuretics especially loop diuretics & in acute alcohol intoxication particularly in case of fasting or malnutrition or hepatic insufficiency. Reduced efficacy w/ OCT1 substrate/inhibitors (eg, verapamil). Increased GI absorption & efficacy w/ OCT1 inducers (eg, rifampicin). Decreased renal elimination & increased plasma conc w/ OCT2 substrates/inhibitors (eg, cimetidine, dolutegravir, crizotinib, olaparib, daclatasvir, vandetanib).

Antidiabetic Agents

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

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