Fibrates

They work by lowering the lipids present in the blood.

What are they

Fibrates are a group of molecules belonging to the same chemical class (amphipathic carboxylic acids) capable of influencing lipid metabolism, and in particular the concentration of triglycerides in the blood.

As such, they are part of the broad category of so-called lipid-lowering drugs.

Mechanism of action

Fibrates exert their lipid-lowering activity by acting at different levels: mainly on the metabolism of triglycerides and VLDL (Very Low Density Lipoprotein) lipoproteins that transport them, secondly on cholesterol metabolism. Let’s see how.

Metabolism of triglycerides and VLDL lipoproteins They accelerate its elimination from the blood and reduce synthesis in the liver
Cholesterol metabolism They increase its elimination through bile and reduce its production in the liver, while increasing HDL lipoprotein formation (High Density Lipoprotein) that convey cholesterol intended for removal (therefore called “good cholesterol”)

The essential mechanism through which fibrates produce these effects is the stimulation of specific nuclear receptors (Peroxisomal Proliferator Activated Receptor, PPAR), present in the cells of different tissues, which regulate the expression of genes involved in the synthesis and activation of some key enzymes of lipoprotein metabolism.

What are they?

The molecules belonging to the group of fibrates currently in use in Italy are: bezafibratefenofibrate and gemfibrozil.

Directions

According to the most recent indications of the European Medicines Agency (EMA), fibrates are to be considered first choice drugs only for patients with severe hypertriglyceridemia.

In the treatment of hypercholesterolemia or mixed hyperlipidemia they can be used later when other lipid-lowering drugs (statins) are contraindicated or not tolerated or combined with other lipid-lowering drugs (statins) in patients at risk if the use of the latter alone is not sufficient to keep blood lipid levels in the normal range.

Side effects and contraindications

Generally, fibrates are well tolerated. Side effects, recorded in 5-10% of patients, may consist of gastrointestinal disorders, rashes, hives, hair loss, fatigue and anemia.

Cases of abnormal liver function have been reported, with modest increases in liver transaminase levels and decreased alkaline phosphatase levels.

The use of fibrates as monotherapy is associated with the risk of forms of suffering of muscle tissue: myositis and rhabdomyolysis.

The risk of muscle toxicity increases further (up to fivefold) in combination with statins.

Fibrates can interact with other drugs that may be taken at the same time, in particular with oral anticoagulants, whose action they tend to potentiate.

The intake of fibrates is contraindicated in the presence of renal insufficiency and liver dysfunction, as well as in pregnancy and children.

Joycelyn Elders is the author and creator of EmpowerEssence, a health and wellness blog. Elders is a respected public health advocate and pediatrician dedicated to promoting general health and well-being.

The blog covers a wide range of topics related to health and wellness, with articles organized into several categories.

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