Fibraates: cholesterol medication for treating high cholesterol

Fibrates are a group of cholesterol-lowering medications that are primarily used to treat elevated triglycerides and low HDL cholesterol ("good" cholesterol). Although fibrates are not as well-known as statins, they are very important medications, especially for patients with mixed dyslipidemia or difficult-to-manage triglyceride levels. This article discusses how fibrates work, when they are used, their dosage, potential side effects, and their role in the prevention of cardiovascular diseases.

Fibrates are medications that specifically lower triglyceride levels in the blood and may also raise HDL cholesterol levels.They act by activating the peroxisome proliferator-activated receptor alpha (PPAR-α), which is an important regulator of fatty acid metabolism.

The mechanism of action of fibrates is complex and involves several processes:

•  Increased breakdown of triglycerides: Fibrates increase the activity of lipoprotein lipase, which accelerates the breakdown and removal of triglycerides from the bloodstream.

•  Reduction of VLDL particles: Fibrates reduce the production of very low-density lipoproteins (VLDL) in the liver, which lowers triglyceride levels.

•  Raising HDL cholesterol : Fibrates increase apolipoprotein A-I

  and A-II

  production, which leads to an increase in HDL cholesterol.

Fibrates are particularly beneficial for patients with high triglyceride levels and low HDL cholesterol levels. They are often used in the following situations:

•  Mixed dyslipidemia : In patients with simultaneously high triglycerides and low HDL cholesterol, fibrates may be the primary treatment, especially if statins are insufficient.

•  Hypertriglyceridemia : In patients with very high triglyceride levels (> 500 mg/dl), fibrates may reduce the risk of pancreatitis associated with these high levels.

•  In the context of diabetes : Diabetics often have high triglyceride levels and low HDL cholesterol, making fibrates a good choice for managing the lipids of these patients.

•  Primary dyslipidemia : In some cases, fibrates may be used in patients with genetically inherited dyslipidemia, especially if they cannot tolerate statins or do not achieve adequate response from statins alone.

There are several different fibrates on the market, the most common being gemfibrozil and fenofibrate. The dosage of these medications varies slightly, but both are used on the same principle.

Gemfibrozil: 

• The usual dose is 600 mg twice a day, typically 30 minutes before breakfast and dinner.

• Gemfibrozil is particularly effective in lowering triglycerides, but it has a higher risk of interactions with statins, which increases the risk of muscle side effects.

 Fenofibrate: 

• The usual dose is 145 mg once a day, typically taken with food.

• Fenofibrate is a more commonly used fibrate because it has fewer interactions with other medications.

The dosing of fibrates is based on the individual needs and health status of the patient, and the doctor adjusts the dose as necessary. It is important to strictly follow the instructions given by the doctor and to have regular blood tests to monitor lipid levels and any potential side effects.

Like all medications, fibrates can also cause side effects.Although most patients tolerate them well, it is important to be aware of the potential risks.

Common side effects: 

•  Gastrointestinal symptoms: Fibrates may cause stomach issues such as nausea, diarrhea, or abdominal pain.

•  Muscle pain: Muscle pain is possible, especially if fibrates are used in conjunction with statins. This can lead to more serious muscle damage, such as rhabdomyolysis, particularly with gemfibrozil.

•  Headache and dizziness: Headache and dizziness are possible, but usually mild and transient.

Rare but serious side effects: 

•  Changes in liver function tests: Fibrates can raise liver enzyme levels, which may be a sign of liver irritation or damage.

•  Gallstones: Long-term use of fibrates may increase the risk of gallstone formation, as the medication increases cholesterol secretion into bile.

If the patient experiences serious side effects such as severe muscle pain, jaundice, or extreme fatigue, they should contact a doctor immediately.

Fibrates may interact with other medications, which can affect their efficacy or increase the risk of side effects. In particular, the combination of fibrates and statins requires careful monitoring.

• Statins: The combination of fibrates and statins may increase the risk of muscle pain and rhabdomyolysis, especially with gemfibrozil.

•  Warfarin and other anticoagulants: Fibrates may enhance the effects of anticoagulants, increasing the risk of bleeding.

•  Cholesterol-binding agents (resins) : Resins, such as cholestyramine, can reduce the absorption of fibrates, which may diminish their effectiveness.

During fibrate therapy, it is important to regularly monitor lipid levels and liver function. The doctor may order blood tests to ensure that the medication is working as expected and that the liver is not overloaded. Particularly when using a combination of statin and fibrate therapy, muscle symptoms should be monitored regularly.

Although fibrates are effective cholesterol medications, they do not replace healthy lifestyles.A healthy diet, regular exercise, weight management, and quitting smoking are essential components in reducing the risk of cardiovascular diseases. Fibrate therapy should always be part of a comprehensive treatment plan that also includes these lifestyle changes.

Fibrates are an important class of medications, particularly for the treatment of elevated triglycerides and low HDL cholesterol. They work by activating the PPAR-α receptor, which leads to an increase in the breakdown of triglycerides and a rise in HDL cholesterol. Fibrates are especially used in patients with mixed dyslipidemia, hypertriglyceridemia, or those who cannot tolerate statins.

Adherence to a doctor's prescription, regular monitoring, and healthy lifestyles are key to the success of fibrate therapy.Together with other cholesterol-lowering treatments, fibrates can help patients achieve and maintain healthy lipid levels and reduce the risk of cardiovascular diseases in the long term.