Metformin (INN) (met-fawr-min; originally sold as Glucophage) is an oral anti-diabetic drug in the biguanide class. It is the first-line drug of choice for the treatment of type 2 diabetes, in particular, in overweight and obese people and those with normal kidney function.
Evidence is also mounting for its efficacy in gestational diabetes, although safety concerns still preclude its widespread use in this setting. It is also used in the treatment of polycystic ovary syndrome and has been investigated for other diseases where insulin resistance may be an important factor.
When prescribed appropriately, metformin causes few adverse effects - the most common is gastrointestinal upset - and is associated with a low risk of hypoglycemia. Lactic acidosis (a buildup of lactate in the blood) can be a serious concern in overdose and when it is prescribed to people with contraindications, but otherwise, there is no significant risk.
Metformin helps reduce LDL cholesterol and triglyceride levels and is not associated with weight gain, and is the only anti-diabetic drug that has been conclusively shown to prevent the cardiovascular complications of diabetes.
Metformin is one of only two oral anti-diabetics in the World Health Organization Model List of Essential Medicines (the other being glibenclamide).
First synthesized and found to reduce blood sugar in the 1920s, metformin was forgotten for the next two decades as research shifted to insulin and other anti-diabetic drugs.
Interest in metformin was rekindled in the late 1940s after several reports that it could reduce blood sugar levels in people, and in 1957, French physician Jean Sterne published the first clinical trial of metformin as a treatment for diabetes.
It was introduced to the United Kingdom in 1958, Canada in 1972, and the United States in 1995.
Metformin is now believed to be the most widely prescribed anti-diabetic drug in the world; in the United States alone, more than 42 million prescriptions were filled in 2009 for its generic formulations.
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Last Updated: Feb 21, 2011