Question

Which of these drugs stimulates PPAR-alpha? PPAR alpha-Peroxisome proliferator-activated receptor alpha:

• A. Gemfibrozil
• B. Ezetimibe
• C. Colestipol
• D. Simvastatin

Hint:

Fibrates like gemfibrozil are the primary class of drugs that activate PPAR-alpha, and they are effective in lowering triglyceride levels and improving HDL cholesterol.

Answer 1

The Correct Option is A

PPAR-alpha (Peroxisome proliferator-activated receptor alpha) is a nuclear receptor that plays a crucial role in the regulation of lipid metabolism. When activated, PPAR-alpha increases the oxidation of fatty acids and lowers triglyceride levels in the bloodstream.
Gemfibrozil: This is a fibric acid derivative (fibrate) that is a potent activator of PPAR-alpha. It works by increasing the activity of lipoprotein lipase and decreasing the synthesis of triglycerides, thereby reducing serum triglyceride levels and increasing HDL cholesterol. This is why it is used primarily in the treatment of hypertriglyceridemia and mixed dyslipidemia.
Ezetimibe: This drug works by inhibiting cholesterol absorption at the intestinal level but does not affect PPAR-alpha.
Colestipol: A bile acid sequestrant, colestipol works by binding to bile acids in the intestine and promoting their excretion, but it does not activate PPAR-alpha.
Simvastatin: A statin that inhibits HMG-CoA reductase, simvastatin lowers cholesterol levels by reducing cholesterol synthesis. While statins have other metabolic effects, they do not directly stimulate PPAR-alpha. Thus, the correct answer is Gemfibrozil, as it directly activates PPAR-alpha.