buformin

Buformin is an oral antidiabetic medication in the biguanide class that has been used to treat type 2 diabetes mellitus. It lowers hepatic glucose production and improves insulin sensitivity in peripheral tissues, with additional modest effects on intestinal glucose absorption. It is typically administered in divided doses with meals.

Buformin was developed in the mid-20th century and used in several countries, but its use declined after safety concerns emerged. The drug has been associated with lactic acidosis, a rare but serious condition, particularly in patients with renal impairment, liver disease, heart failure, or conditions causing hypoxia. In response to these risks, buformin was withdrawn from many markets in the late 20th century and is now not widely marketed, remaining available only in a limited number of jurisdictions or historical registries.

Pharmacokinetics and administration: Buformin is taken orally and is absorbed from the gastrointestinal tract. It is largely excreted unchanged by the kidneys, so renal function significantly influences clearance. Dose adjustments are typically required in renal impairment, and accumulation can occur if clearance is reduced.

Adverse effects and safety: The most common adverse effects are gastrointestinal, including nausea, diarrhea, and abdominal discomfort. The most serious risk is lactic acidosis, which necessitates careful monitoring of kidney function and other risk factors. Contraindications include significant renal impairment, hepatic disease, and conditions predisposing to lactic acidosis. Given its safety profile, buformin is now rarely used and is often considered a historical or restricted-treatment option compared with metformin.