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Information about Glucophage*
Metformin (Glucophage®) is an anti-diabetic drug from the
biguanide class (its other members are the withdrawn agents phenformin and
buformin).
Uses
The main use for metformin is for the treatment of diabetes mellitus, especially
when is concomitant obesity and insulin resistance. It is also being used
increasingly in polycystic ovary syndrome (PCOS) and non-alcoholic
steatohepatitis, two other diseases that feature insulin resistance.
Mode of action
Despite its therapeutic benefits, the actual mode of action of metformin is
uncertain. A report from 2001 (Zhou G et al) indicated that it acts by
activating AMP-activated protein kinase (AMPK) in liver cells, leading to
increased fatty acid oxidation and glucose uptake by cells and decreased
lipogenesis and hepatic glucose production. Its net effect is an improvement in
insulin resistance.
Side-effects
The most common side effect of Metformin HCl immediate-release is diarrhea. In a
clinical trial of 286 subjects, 53.2% of the 141 who were given Metformin IR (as
opposed to placebo) reported diarrhea, and 25.5% reported nausea/vomiting.
(source: Drug Facts & Comparisons 2005)
Phenformin was withdrawn because of an increased risk of lactic acidosis (up to
60 cases per million patient-years). In recent studies it was revealed that, as
long as it is not prescribed to patients who are at risk, metformin is much
safer, and the risk of lactic acidosis approximates that of people who are not
on the medication (Salpeter SR et al).
Contra-indications
Metformin should not be used in any condition that may increase the risk of
lactic acidosis. This includes heart failure, kidney disorders (creatinine over
150 µmol/l), lung disease and liver disease.
History
The class of biguanide originates from the French lilac (Galega officinalis), a
plant known for several centuries to improve the symptoms of diabetes mellitus.
The source of this article is
Wikipedia, the free encyclopedia. The text of this
article is licensed under the
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