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Lactic acidosis reported (rare); increased risk with increased age, diabetes mellitus (DM), renal dysfunction, CHF, and conditions with risk of hypoperfusion and hypoxemia. Avoid use in patients ≥80 yrs of age unless renal function is normal. Withhold therapy in the presence of any condition associated with hypoxemia, dehydration, or sepsis. Avoid with clinical or lab evidence of hepatic disease. Caution against excessive alcohol intake; may potentiate the effects of metformin on lactate metabolism. Temporarily d/c prior to any IV radiocontrast study or surgical procedures. D/C use and institute appropriate therapy if lactic acidosis occurs.








Adjunct to diet and exercise to improve glycemic control in type 2 DM.


Type 2 Diabetes Mellitus

Initial: 500mg bid or 850mg qd w/ meals
Titrate: Increase by 500mg/week or 850mg every 2 weeks, up to a total of 2000mg/day given in divided doses; may also titrate from 500mg bid to 850mg bid after 2 weeks
Max: 2550mg/day; doses >2000mg/day may be better tolerated given tid

Tab, Exntended-Release (ER):
Initial: 500mg qd w/ pm meal
Titrate: Increase by 500mg/week
Max: 2000mg/day; consider 1000mg bid if unable to achieve glycemic control on 2000mg qd


Type 2 Diabetes Mellitus

10-16 Years:
Initial: 500mg bid w/ meals
Titrate: Increase by 500mg/week
Max: 2000mg/day


Concomitant Medications
Insulin Therapy in Adults:
Initial: 500mg qd while continuing current insulin dose
Titrate: Increase by 500mg/week; decrease insulin dose by 10-25% when FPG <120mg/dL
Max: 2500mg/day (tab) and 2000mg/day (tab, extended-release [ER])

Oral Sulfonylurea Therapy in Adults:
Consider gradual addition of an oral sulfonylurea if unresponsive to 4 weeks of max dose of Glucophage or Glucophage XR monotherapy; if patients have not satisfactorily responded to 1-3 months of concomitant therapy, consider therapeutic alternatives (eg, switching to insulin w/ or w/o Glucophage or Glucophage XR)

Dose conservatively; do not titrate to max dose

Other Important Considerations
Transferring Patients from Chlorpropamide: Exercise care during the first 2 weeks because of the prolonged retention of chlorpropamide in the body
Debilitated/Malnourished: Do not titrate to max dose


Oral route

Give in divided doses w/ meals

Tab, ER
Give qd w/ the pm meal
Must be swallowed whole; do not crush or chew


Tab: (Glucophage) 500mg, 850mg, 1000mg; Tab, ER: (Glucophage XR) 500mg, 750mg


Renal disease/dysfunction (eg, SrCr ≥1.5mg/dL [males], ≥1.4mg/dL [females], or abnormal CrCl), acute or chronic metabolic acidosis, diabetic ketoacidosis with or without coma. D/C temporarily (48 hrs) for radiologic studies with intravascular iodinated contrast materials.


D/C therapy if conditions associated with lactic acidosis and characterized by hypoxemia states (eg, acute CHF, cardiovascular [CV] collapse, acute MI), or prerenal azotemia develop. D/C therapy if temporary loss of glycemic control occurs due to stress; temporarily give insulin and reinstitute after acute episode is resolved. May decrease serum vitamin B12 levels. Increased risk of hypoglycemia in elderly, debilitated/malnourished or with adrenal or pituitary insufficiency or alcohol intoxication. Consider therapeutic alternatives, including initiation of insulin, if secondary failure occurs. Caution in elderly.


Lactic acidosis, diarrhea, N/V, flatulence, asthenia, abdominal discomfort, hypoglycemia, dizziness, dyspnea, taste disorder, chest discomfort, flu syndrome, palpitations, indigestion.


See Boxed Warning and Contraindications. May increase levels with furosemide, nifedipine, cimetidine, cationic drugs (eg, digoxin, amiloride, procainamide, quinidine, quinine, ranitidine, trimethoprim, vancomycin, triamterene, morphine). Observe for loss of glycemic control with thiazides, other diuretics, corticosteroids, phenothiazines, thyroid products, estrogens, oral contraceptives, phenytoin, nicotinic acid, sympathomimetics, calcium channel blockers, and isoniazid. May interact with highly protein-bound drugs (eg, salicylates, sulfonamides, chloramphenicol, probenecid). May decrease furosemide or glyburide levels. Caution with drugs that may affect renal function or result in significant hemodynamic change or may interfere with the disposition of metformin. Hypoglycemia may occur with concomitant use of other glucose-lowering agents (eg, sulfonylureas, insulin). May overlap drug effects when transferred from chlorpropamide. Hypoglycemia may be difficult to recognize with β-adrenergic blocking drugs.


Category B, not for use in nursing.


Biguanide; decreases hepatic glucose production and intestinal absorption of glucose, and improves insulin sensitivity by increasing peripheral glucose uptake and utilization.


Absorption: (Tab) Absolute bioavailability (50-60%); (Tab, ER) Tmax=7 hrs. Administration of different doses resulted in different parameters. Distribution: (Tab) Vd=654L. Elimination: Urine (90%); T1/2=6.2 hrs (plasma), 17.6 hrs (blood).


Assess for renal/hepatic impairment, acute/chronic metabolic acidosis, presence of a hypoxic state (eg, acute CHF, acute MI, CV collapse), dehydration, sepsis, alcoholism, nutritional status, adrenal/pituitary insufficiency, pregnancy/nursing status, and for possible drug interactions. Assess baseline renal function, FPG, HbA1c, and hematological parameters (Hct, Hgb, RBC indices).


Monitor for lactic/metabolic acidosis, ketoacidosis, hypoglycemia, hypoxemia (eg, CV collapse, acute CHF, acute MI), prerenal azotemia, and for decreases in vitamin B12 levels. Monitor FPG, HbA1c, renal function (eg, SrCr, CrCl), and hematological parameters (eg, Hgb, Hct, RBC indices).


Inform of the potential risks and benefits of therapy. Inform about the importance of adherence to dietary instructions and a regular exercise program. Inform of the risk of developing lactic acidosis during therapy; advise to d/c therapy immediately and contact physician if unexplained hyperventilation, myalgia, malaise, unusual somnolence, or other nonspecific symptoms occur. Instruct to avoid excessive alcohol intake. Counsel to take tab with meals and ER tab with pm meal. Instruct that ER tab must be swallowed whole and not crushed or chewed.


20-25°C (68-77°F); excursions permitted to 15-30°C (59-86°F).


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