13.03.3 Fibric Acid Derivatives

The fibric acid derivates (fibrates) e.g. gemfibrozil, are used to increase HDL cholesterol especially in subjects who have low HDL cholesterol levels e.g. diabetics. The Peroxisome Proliferation-Activated Receptor (PPAR)a is a nuclear receptor that is stimulated by fatty acids from the diet or adipost tissue (Figure 13.14).  The receptor regulates gene expression, and stimulation of  PPARa leads to fatty acid oxidation to reduce the levels of triglycerides, stimulation lipoprotein lipase to clear triglycerides, and an increases HDL-cholesterol (Figure 13.14).  

Figure 13.14 Stimulation of PPARα (Copyright QUT, Sheila Doggrell)

As a result of these actions, the fibric acid derivatives, such as gemfibrozil, decrease levels of triglycerides, have variable small effects on LDL-cholesterol, but increase the levels of HDL-cholesterol.  The fibrates are used in subjects with high levels of triglycerides and low levels of HDL-cholesterol, which commonly occurs in the metabolic syndrome (obese, hypertensive, dyslipidemia) and diabetes.

Pharmacology InOneSemester,
Mar 24, 2015, 10:00 PM