Metformin

An oral diabetes medication

Metformin
INN
Drug class
Routes of administration
Pregnancy category
Bioavailability
Metabolism
Elimination half-life
Excretion
Legal status
CAS Number
PubChem
DrugBank
ChemSpider
KEGG

Metformin is a medication primarily used for the treatment of type 2 diabetes. It is considered the first-line medication for the management of this condition, particularly in people who are overweight. Metformin is also used in the treatment of polycystic ovary syndrome (PCOS) and has been investigated for other uses, including the treatment of gestational diabetes and prediabetes.

History

Galega officinalis, a plant from which metformin was originally derived

The use of metformin can be traced back to the traditional use of the plant Galega officinalis (French lilac) for the treatment of diabetes. The active ingredient, guanidine, was identified in the early 20th century, but it was not until the 1950s that metformin was synthesized and introduced as a diabetes medication. It was first marketed in France in 1957 and became available in the United States in 1995.

Mechanism of Action

Metformin works by decreasing hepatic glucose production, decreasing intestinal absorption of glucose, and improving insulin sensitivity by increasing peripheral glucose uptake and utilization. Unlike other antidiabetic drugs, metformin does not cause hypoglycemia when used alone.

Medical Uses

Metformin is primarily used to treat type 2 diabetes. It is effective in lowering blood sugar levels and is often used in combination with other medications. Metformin is also used to treat polycystic ovary syndrome (PCOS) and has been shown to improve insulin sensitivity and reduce insulin levels in women with PCOS.

Side Effects

Common side effects of metformin include gastrointestinal issues such as diarrhea, nausea, and abdominal pain. These side effects are often transient and can be minimized by starting with a low dose and gradually increasing it. A rare but serious side effect is lactic acidosis, which can occur in people with significant kidney impairment or other risk factors.

Synthesis

Chemical synthesis of metformin

Metformin is synthesized from dimethylamine hydrochloride and 2-cyanoguanidine. The reaction involves the formation of a biguanide structure, which is the active component of metformin.

Formulations

Metformin is available in several formulations, including immediate-release and extended-release tablets. The extended-release formulation is designed to reduce gastrointestinal side effects and improve patient compliance.

Pharmacokinetics

Metformin is absorbed primarily from the small intestine and is excreted unchanged in the urine. It has a half-life of approximately 4 to 8.7 hours, and its bioavailability is about 50-60% under fasting conditions.

Related Pages

• Type 2 diabetes
• Polycystic ovary syndrome
• Hypoglycemia
• Lactic acidosis