Each Extended-Release Tablet contains: Metformin hydrochloride 750 mg.
Chemical name: N,N-dimethylimidodicarbonimidic diamide hydrochloride.
Chemical formula: C4H11N5•HCl.
Molecular weight: 165.6.
Pharmacology: Pharmacodynamics: Mechanism of Action: Metformin hydrochloride is an oral antihyperglycemic agent which improves glucose tolerance in patients with type 2 diabetes mellitus, lowering both basal and postprandial plasma glucose. Metformin (as hydrochloride) decreases hepatic glucose production, decreases intestinal absorption of glucose, and improves insulin sensitivity by increasing peripheral glucose uptake and utilization. Unlike sulfonylureas, metformin does not produce hypoglycemia in either patients with type 2 diabetes or normal subjects and does not cause hyperinsulinemia. With metformin therapy, insulin secretion remains unchanged while fasting insulin levels and day-long plasma insulin response may actually decrease.
Pharmacokinetics: Gastrointestinal absorption of Metformin hydrochloride is slow and incomplete. Absolute bioavailability of a single 500-mg dose is reported to be about 50 to 60% which may be decreased or slightly delayed by food. Protein binding in plasma is negligible once the drug is absorbed; it is excreted unchanged in the urine. The plasma elimination half-life ranges from about 2 to 6 hours after oral doses. Small amounts are distributed in breast milk.
Metformin hydrochloride is used for the management of type 2 diabetes mellitus as monotherapy, and as an adjunct to diet and exercise to improve glycemic control.
Immediate Release Tablet: Adult dose: The usual starting dose is 500 mg twice daily or 850 mg once a day given with meals. Make dosage increases in increments of 500 mg per week or 850 mg every 2 weeks, up to a total of 2000 mg per day given in divided doses. Patients can be titrated from 500 mg twice a day to 850 mg twice a day after 2 weeks. For those patients requiring additional glycemic control, it may be given to a maximum daily dose of 2550 mg per day. Doses >2000 mg may be better tolerated given 3 times a day with meals.
Pediatric dose: The usual starting dose is 500 mg twice a day given with meals. Make dosage increases in increments of 500 mg per week up to a maximum of 2000 mg per day given in divided doses.
Extended-Release Tablet: Adult Dose: Monotherapy and combination with other oral hypoglycemic agents.
The usual starting dose is 750 mg given with evening meals. Maximum dose of up to 1500 mg given with evening meals.
After 10 to 15 days, it is recommended to check if the dose given to the patient is adequate on the basis of blood glucose measurement.
Combination with Insulin: For patients treated with combination therapy of metformin and insulin, metformin dose 750 mg with evening meals, up to a maximum dose of 1500 mg given with evening meals. Insulin dosage is adjusted on the basis of blood glucose measurement of the patient.
Lactic acidosis is a common manifestation of overdosage. Metformin is dialyzable with a clearance of up to 170 mL/min under good hemodynamic conditions. Therefore, hemodialysis may be useful for removal of accumulated drug from patients in whom metformin overdosage is suspected.
Known hypersensitivity to metformin hydrochloride.
Renal disease or dysfunction which may also result from conditions such as cardiovascular collapse (shock), acute myocardial infarction or septicemia.
Patients undergoing radiologic studies involving intravascular administration of iodinated contrast media. Use of such products may result in acute alteration of renal function.
Acute or chronic metabolic acidosis, including diabetic ketoacidosis, with or without coma.
Acute hemodynamic compromise of hypoxic states.
Congestive heart failure.
Abnormal hepatic function.
Dehydration.
Lactation.
Lactic acidosis is a rare, but serious, metabolic complication that can occur due to metformin accumulation during treatment: occurrence is fatal in approximately 50% of cases.
Monitor renal function regularly in elderly patients particularly those >80 years of age.
Cardiovascular collapse (shock); acute congestive heart failure, myocardial infarction and other conditions characterized by hypoxemia.
Temporarily suspend therapy for any surgical procedure (except minor procedures not associated with restricted intake of food and fluids).
Excessive alcohol intake since it is known to potentiate the effect of metformin on lactate metabolism.
Patients with impaired hepatic function.
Annually measure hematologic parameters. Any apparent abnormalities should be appropriately investigated and managed.
Hypoglycemia may occur when caloric intake is deficient, when strenuous exercise is not compensated by caloric supplementation, or during concomitant use with other glucose-lowering agents (such as sulfonylureas and insulin) or ethanol.
Elderly, debilitated, or malnourished patients, those with adrenal insufficiency, and in people who are taking adrenergic blocking agents.
Exposure to stress such as fever, trauma, infection, or surgery may cause temporary loss of glycemic control.
There are no adequate and well-controlled studies in pregnant women with metformin. Generally not recommended for the routine management of gestational diabetes mellitus, type 2 diabetes in pregnant women or polycystic ovary syndrome.
Diarrhea, abnormal stools, hypoglycemia, myalgia, lightheaded, dyspnea, nail disorder, rash, sweating increased, taste disorder, chest discomfort, chills, flu syndrome, flushing, and palpitation.
Nifedipine appears to enhance the absorption of Metformin.
Cationic drugs (e.g., amiloride, digoxin, morphine, procainamide, quinidine, quinine, ranitidine, triamterene, trimethoprim, or vancomycin) could potentially interact with metformin by competing for common renal tubular transport systems.
Cimetidine increases peak plasma concentration of metformin and whole blood concentrations.
Certain drugs such as thiazides and other diuretics, corticosteroids, phenothiazines, thyroid products, estrogens, oral contraceptives, phenytoin, nicotinic acid, sympathomimetics, calcium channel blocking drugs, and isoniazid, tend to produce hyperglycemia and may lead to loss of glycemic control. Monitor closely for loss of blood glucose control in patients taking these drugs. When such drugs are withdrawn from a patient receiving metformin, the patient should be closely observed for hypoglycemia.
Store at temperatures not exceeding 30°C.
A10BA02 - metformin ; Belongs to the class of biguanides. Used in the treatment of diabetes.
Metfor XR tab 750 mg
30's (P235.2/box)
Sign Out
