Fibrate

Chemical structure of Fenofibrate

Fibrates are a class of amphipathic carboxylic acids used primarily as lipid-lowering agents. They are particularly effective in reducing triglyceride levels and are also used to increase high-density lipoprotein (HDL) cholesterol levels. Fibrates are often prescribed to patients with dyslipidemia, especially those with elevated triglycerides and low HDL cholesterol.

Mechanism of Action

Diagram of PPAR activation

Fibrates exert their effects by activating the peroxisome proliferator-activated receptor alpha (PPARα), a type of nuclear receptor. Activation of PPARα leads to increased expression of genes involved in fatty acid oxidation, lipoprotein metabolism, and apolipoprotein synthesis. This results in decreased triglyceride levels, increased HDL cholesterol, and a modest reduction in low-density lipoprotein (LDL) cholesterol.

Clinical Uses

Fibrates are primarily used to treat hypertriglyceridemia and mixed dyslipidemia. They are particularly beneficial in patients with metabolic syndrome or type 2 diabetes mellitus, where triglyceride levels are often elevated. Fibrates can be used alone or in combination with other lipid-lowering agents such as statins.

Common Fibrates

Fenofibrate

Fenofibrate is one of the most commonly prescribed fibrates. It is used to reduce cholesterol levels in patients at risk of cardiovascular disease.

Clofibrate

Chemical structure of Clofibrate

Clofibrate was one of the first fibrates developed but is less commonly used today due to concerns about its safety profile.

Bezafibrate

Chemical structure of Bezafibrate

Bezafibrate is used to treat hyperlipidemia and has a broad spectrum of action on lipid parameters.

Ciprofibrate

Chemical structure of Ciprofibrate

Ciprofibrate is another fibrate used to manage lipid disorders, particularly in patients with high triglyceride levels.

Choline Fenofibrate

Chemical structure of Choline Fenofibrate

Choline fenofibrate is a newer formulation designed to improve the bioavailability of fenofibrate.

Clinofibrate

Chemical structure of Clinofibrate

Clinofibrate is used in some countries for the treatment of hyperlipidemia.

Aluminium Clofibrate

Chemical structure of Aluminium Clofibrate

Aluminium clofibrate is a derivative of clofibrate, used in certain formulations.

Side Effects

Common side effects of fibrates include gastrointestinal disturbances, such as nausea and abdominal pain. Muscle pain and weakness can occur, particularly when fibrates are used in combination with statins. Rarely, fibrates can cause liver dysfunction and gallstones.

Related Pages

• Statin
• Cholesterol
• Triglyceride
• Lipoprotein
• Peroxisome proliferator-activated receptor