💊 Thiazolidinediones, also known as glitazones, are a class of oral antidiabetic agents that improve insulin sensitivity in peripheral tissues. They primarily act on adipose tissue, muscle, and the liver to enhance glucose uptake and utilization, making them effective in treating type 2 diabetes mellitus.
▪️ TZDs (e.g., pioglitazone, rosiglitazone) work by activating PPAR-γ in adipose tissue, increasing insulin sensitivity in muscle and fat while reducing hepatic glucose output.
▪️ TZDs increase renal sodium reabsorption, leading to fluid retention (worsening heart failure risk). Weight gain is due to fat redistribution (subcutaneous, not visceral fat).
▪️ TZDs can cause fluid retention leading to or worsening heart failure, and are contraindicated in NYHA Class III or IV heart failure.
▪️ Pioglitazone improves lipid parameters—especially raising HDL and lowering triglycerides—beneficial for cardiovascular health.
▪️ Rosiglitazone was linked to higher risks of myocardial infarction and cardiovascular death, leading to restricted use (now lifted in some countries with caution).
▪️ TZDs act via gene transcription changes and take weeks to exert full effects, unlike rapid-acting agents like sulfonylureas.
▪️ TZDs decrease bone mineral density and increase the risk of fractures, especially in women.
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Chapters:
0:00 - thiazolidinediones (glitazones) pharmacology
0:21 - thiazolidinediones (glitazones) clinical pharmacology
0:28 - thiazolidinediones (glitazones) and fluid retention (edema)
0:51 - thiazolidinediones (glitazones) and weight gain
1:09 - thiazolidinediones (glitazones) and bone fracture risk
1:32 - thiazolidinediones (glitazones) and bladder cancer
1:51 - thiazolidinediones (glitazones) and hepatotoxicity
2:10 - thiazolidinediones (glitazones) clinical summary
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