Clofibrate

An article about the lipid-lowering agent Clofibrate

Clofibrate

Chemical structure of Clofibrate

Clofibrate is a fibrate class medication primarily used to lower cholesterol and triglyceride levels in the blood. It was one of the first drugs developed to treat hyperlipidemia, a condition characterized by elevated levels of lipids in the bloodstream.

Mechanism of Action

Clofibrate works by activating peroxisome proliferator-activated receptor alpha (PPAR_), a type of nuclear receptor that regulates the expression of genes involved in lipid metabolism. Activation of PPAR_ leads to increased oxidation of fatty acids in the liver and muscle tissues, thereby reducing the levels of triglycerides and low-density lipoprotein (LDL) cholesterol in the blood.

Clinical Use

Clofibrate was historically used to treat patients with hyperlipidemia and to prevent cardiovascular disease. However, its use has declined due to the development of newer fibrates and statins, which have more favorable safety profiles and efficacy.

Side Effects

Common side effects of clofibrate include gastrointestinal disturbances such as nausea and diarrhea. More serious adverse effects can include gallstone formation, myopathy, and liver dysfunction. Due to these potential risks, clofibrate is less commonly prescribed today.

History

Clofibrate was first introduced in the 1960s and was widely used for several decades. It was one of the first drugs to demonstrate the potential of pharmacological intervention in lipid disorders. However, subsequent studies raised concerns about its safety, particularly regarding its association with increased mortality in some patient populations.

Related pages

• Fibrate
• Hyperlipidemia
• Cholesterol
• Triglyceride
• Peroxisome proliferator-activated receptor