Metformin
Metformin, sold under the brand name Glucophage, among others, is the main first-line medication for the treatment of type 2 diabetes, particularly in people who are overweight. It is also used in the treatment of polycystic ovary syndrome. It is sometimes used as an off-label adjunct to lessen the risk of metabolic syndrome in people who take antipsychotics. Metformin is not associated with weight gain and is taken by mouth.
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| Pronunciation | /mɛtˈfɔːrmɪn/, met-FOR-min |
| Trade names | Fortamet, Glucophage, Glumetza, others |
| Other names | N,N-dimethylbiguanide |
| AHFS/Drugs.com | Monograph |
| MedlinePlus | a696005 |
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| Routes of administration | By mouth |
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| Bioavailability | 50–60% |
| Protein binding | Minimal |
| Metabolism | Not by liver |
| Elimination half-life | 4–8.7 hours |
| Excretion | Urine (90%) |
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| ECHA InfoCard | 100.010.472 |
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| Formula | C4H11N5 |
| Molar mass | 129.167 g·mol−1 |
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| Density | 1.3±0.1 g/cm3 |
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Metformin is generally well tolerated. Common adverse effects include diarrhea, nausea, and abdominal pain. It has a small risk of causing low blood sugar. High blood lactic acid level (acidosis) is a concern if the medication is used in overly large doses or prescribed in people with severe kidney problems.
Metformin is a biguanide anti-hyperglycemic agent. It works by decreasing glucose production in the liver, increasing the insulin sensitivity of body tissues, and increasing GDF15 secretion, which reduces appetite and caloric intake.
Metformin was first described in scientific literature in 1922 by Emil Werner and James Bell. French physician Jean Sterne began the study in humans in the 1950s. It was introduced as a medication in France in 1957 and the United States in 1995. Metformin is on the World Health Organization's List of Essential Medicines, and is the most widely used medication for diabetes taken by mouth. It is available as a generic medication. In 2021, it was the second most commonly prescribed medication in the United States, with more than 91 million prescriptions.