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About GLUCOPHAGE or GLUCOPHAGE XR (metformin)
Worldwide, tens of millions use metformin tablets to control their blood sugar levels, with few side-effects.
Now, researchers from Harvard Medical School show metformin can also tackle cancer, by seeking out
an destroyed the deadly cells which give birth to tumours and fuel their spread. [1]

The drug is metformin, available generically and under brand names such as Glucophage and Fortamet.
A growing body of evidence suggests that diabetes patients taking metformin are less likely to get
cancer, and have better outcomes if they do get cancer, than those not taking the drug. [2]

Kevin Struhl, PhD, a Harvard researcher, find that metformin can kill breast cancer stem cells, thought to
be the cells responsible for breast cancer spread and recurrence. Struhl says cancer stem cells are "far
more nasty" than regular cancer cells. [2]

In the study, metformin seemed to work independently of its ability to improve insulin sensitivity and lower
blood sugar and insulin levels, all of which are also associated with better breast cancer outcomes.  In
mice, pretreatment with metformin prevented the otherwise dramatic ability of human breast cancer stem
cells to form tumors. In other mice where tumors were allowed to take hold for 10 days, the dual therapy
of metformin and deoxorubicin also reduced tumor mass more quickly and prevented relapse for longer
than doxorubicin alone. [3]

Facts about Metformin

Description
GLUCOPHAGE® (metformin hydrochloride) Tablets and GLUCOPHAGE® XR (metformin hydrochloride)
Extended-Release Tablets are oral antihyperglycemic drugs used in the management of type 2 diabetes.
Metformin hydrochloride is freely soluble in water and is practically insoluble in acetone, ether, and
chloroform. The pKa of metformin is 12.4. The pH of a 1% aqueous solution of metformin hydrochloride
is 6.68.

GLUCOPHAGE tablets contain 500 mg, 850 mg, or 1000 mg of metformin hydrochloride. GLUCOPHAGE
XR contains 500 mg or 750 mg of metformin hydrochloride as the active ingredient.

Pharmacology and Pharmacokinetics
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.

The absolute bioavailability of a GLUCOPHAGE 500 mg tablet given under fasting conditions is
approximately 50% to 60%. Studies using single oral doses of GLUCOPHAGE 500 to 1500 mg, and 850
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. Although the extent of metformin absorption (as
measured by AUC) from the GLUCOPHAGE XR tablet increased by approximately 50% when given with
food, there was no effect of food on Cmax and Tmax of metformin. Both high and low fat meals had the
same effect on the pharmacokinetics of GLUCOPHAGE XR.

Metformin may cause serious side effect.
Lactic acidosis is a rare, but serious, metabolic complication that can occur due to metformin
accumulation during treatment with GLUCOPHAGE or GLUCOPHAGE XR; when it occurs, it is fatal in
approximately 50% of cases. The reported incidence of lactic acidosis in patients receiving metformin
hydrochloride is very low (approximately 0.03 cases/1000 patient-years.

In a US double-blind study of Glucophage in patients with type 2 diabetes, side effects reported in
greater than 5% of metformin (Glucophage) as follows: Diarrhea, nausea / vomiting, flatulence, asthenia,
indigestion, abdominal discomfort and headache. In worldwide clinical trials over 900 patients with type 2
diabetes have been treated with GLUCOPHAGE XR, the major side effects are diarrhea and
nausea/vomiting.

Overdose of metformin hydrochloride has occurred, including ingestion of amounts greater than 50
grams. Hypoglycemia was reported in approximately 10% of cases, but no causal association with
metformin hydrochloride has been established. Lactic acidosis has been reported in approximately 32%
of metformin overdose cases.

This article highlights only a few features about metformin. For detailed information, users
should discuss with their medical doctors.
[1] Diabetic medicine fights cancer by destroying deadly cells Mail Online 15th September 2009
[2]  Diabetes Drug Fights Breast Cancer Metformin Kills Breast Cancer Stem Cells, May Fight Many
Cancers WebMD Health News Sept. 14, 2009 [3]  Combo with anti-diabetes drug found effective against
cancer AFP Sept. 14, 2009