Glucophage tablets contain 500 mg, 850 mg, or 1000 mg of metformin hydrochloride.
Each tablet contains the inactive ingredients povidone and magnesium
stearate. In addition, the coating for the 500 mg and 850 mg tablets
contains hypromellose and the coating for the 1000 mg tablet contains
hypromellose and polyethylene glycol.
Metformin
is an antihyperglycemic agent which improves glucose tolerance in
patients with type 2 diabetes, lowering both basal and postprandial
plasma glucose. Its pharmacologic mechanisms of action are different
from other classes of oral antihyperglycemic agents.
Metformin
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.
The absolute bioavailability of a metformin hydrochloride 500 mg tablet
given under fasting conditions is approximately 50-60%. Studies using
single oral doses of metformin hydrochloride tablets 500 mg to 1500 mg,
and 850 mg to 2550 mg, indicate that there is a lack of dose
proportionality with increasing doses, which is due to decreased
absorption rather than an alteration in elimination. Food decreases the
extent of and slightly delays the absorption of
metformin,
as shown by approximately a 40% lower mean peak plasma concentration
(Cmax), a 25% lower area under the plasma concentration versus time
curve (AUC), and a 35 minute prolongation of time to peak plasma
concentration (Tmax) following administration of a single 850-mg tablet
of
metformin with food, compared to the same tablet strength administered fasting. The clinical relevance of these decreases is unknown.
The apparent volume of distribution (V/F) of metformin following single oral doses of
metformin hydrochloride tablets 850 mg averaged 654 ± 358 L.
Metformin is negligibly bound to plasma proteins, in contrast to sulfonylureas, which are more than 90% protein bound.
Metformin
partitions into erythrocytes, most likely as a function of time. At
usual clinical doses and dosing schedules of metformin hydrochloride
tablets, steady state plasma concentrations of
metformin are reached within 24 to 48 hours and are generally <1 mcg/mL. During controlled clinical trials of
metformin hydrochloride tablets, maximum
metformin plasma levels did not exceed 5 mcg/mL, even at maximum doses.
SIDE EFFECTS:
Glucophage could cause a very rare - but potentially fatal -
side effect
known as lactic acidosis. It is caused by a buildup of lactic acid in
the blood. The problem is most likely to occur in people whose liver or
kidneys are not working well, and in those who have multiple medical
problems, take several medications, or have congestive heart failure.
The risk also is higher if you are an older adult or drink alcohol.
Lactic acidosis is a medical emergency that must be treated in a
hospital. Notify your doctor immediately if you experience any of the
following:
Symptoms of lactic acidosis may include:
Dizziness, extreme weakness or tiredness, light-headedness, low body
temperature, rapid breathing or trouble breathing, sleepiness, slow or
irregular heartbeat, unexpected or unusual stomach discomfort, unusual
muscle pain.