Troglitazone

Products

Troglitazone (Rezulin, tablets) is not commercially available in many countries. It was approved in 1997 and withdrawn from the market in 2000 because of its liver-toxic properties.

Structure and properties

Troglitazone (C24H27NO5S, Mr = 441.5 g/mol) belongs structurally to the thiazolidinediones.

Effects

Troglitazone (ATC A10BG01) is antidiabetic. Effects are due to agonism at the PPAR-γ receptor, which controls the regulation of genes involved in glucose and lipid metabolism. The effects are primarily due to increased sensitivity of adipose tissue, muscle, and liver to insulin, thus decreasing insulin resistance and increasing uptake of blood glucose into tissues.

Indications

For the treatment of type 2 diabetes mellitus.

Adverse effects

Troglitazone may cause hepatotoxic side effects and is therefore no longer commercially available. It appears to cause liver injury comparatively frequently.