Etofibrate

Etofibrate Like clofibrate, it is a derivative of clofibric acid just like statins and nicotinic acids. They belong to the active ingredient group of lipid lowering agents. Etofibrate mainly works with an increased concentration of triglycerides. The lowering of cholesterol is less pronounced.

What is Etofibrate?

Etofibrate (chemical name: 2-hydroxymethylnicotinate) is, as the name suggests, a fibrate, which forms a group of drugs that are primarily used to treat hyperlipidemia (increased blood lipids). Fibrates are mainly used to reduce excessive levels of triglycerides, in contrast to statins, which are mainly used to treat high cholesterol levels. However, etofibrate also lowers the cholesterol level a little, the main effect is still with the triglycerides.

Etofibrate is one of the most important drugs for treating a disturbed metabolism of blood lipids and thus also for treating cardiovascular diseases. Etofibrate is only a second choice with other fibrates, since statins are the lipid-lowering drugs of choice. Therefore, they should be used especially when statins are not tolerated or when the triglycerides are increased.

Etofibrate is a white, crystalline, and insoluble powder and is given daily as a tablet or capsule. After ingestion, etofibrate is converted back into clofibric acid and again excreted via the kidneys. The dose should therefore be adjusted in case of renal insufficiency.

Pharmacological effect on the body and organs

Etofibrate lowers the concentration of triglycerides. How exactly is not yet adequately described. However, it is considered likely that etofibrate is responsible for the activation of PPARα, the peroxisome proliferator activated receptor. This is a protein that, when activated, binds to cellular DNA and influences the formation of some proteins involved in lipid metabolism. This also includes an increased breakdown of LDL by 10 to 25 percent, as well as an increase in HDL by around 10 percent.

LDL is the cholesterol that accumulates in the vessel walls and calcifies the vessels, which leads to atherosclerosis. In contrast, there is HDL, which is the cholesterol that is transported from the periphery to the liver in order to be broken down there. In addition, etofibrate works in the liver by releasing less of the VLDL, which is also a form of transport for cholesterol, but which consists more of triglycerides. This happens due to the impaired formation of cholesterol in the liver. Etofibrate also increases the activation of the enzyme lipoprotein lipase, which is essential for breaking down triglycerides in the blood.

In addition to the effects on blood lipids, etofibrate also affects other target structures, which is known as pleiotropic. These are, for example, an improved function of the vascular wall, an anti-inflammatory effect, and a reduced formation of cytokines, which cause inflammatory processes. However, etofibrate also increases the lithogenicity of bile, which means that the bile is at increased risk of forming cholesterol-containing gallstones.

Medical application & use for treatment & prevention

Etofibrate has a wide range of uses: it is mainly used in primary familial hypertriglyceridemia, a congenital metabolic disorder in which high levels of triglycerides in the blood occur. The most common cause is an enzyme defect, which leads to the breakdown of triglycerides.

In addition to the primary form of hypertriglyceridemia, etofibrate is also used in the secondary form, i.e. the acquired form. In addition to a high-fat diet, which can lead to obesity, the causes here are also some metabolic disorders such as diabetes or kidney failure or inflammatory diseases of the kidneys. Elevated blood lipids can also be caused by therapeutic measures when drugs are used that increase the plasma level of blood lipids. Examples are some hormones, beta blockers or glucocorticoids.

Etofibrate is also used in Metabolic Syndrome (also: "Syndrome X"), a severe metabolic disorder that involves various components. This disease is also called the "fatal quartet" because it has the four elements of a disturbed carbohydrate metabolism, increased blood pressure, severe obesity and a disturbed lipid metabolism with increased levels of triglycerides and decreased levels of HDL. Etofibrate is taken several times a day and is prescribed in the form of tablets or capsules.

Risks & side effects

Etofibrate, like other fibrates, has a wide profile of side effects. These include some non-specific side effects, including an allergic reaction to etofibrate. Like other allergic reactions, it is characterized by swelling, shortness of breath and wheals.

Etofibrate can also cause fever, chills, a flu-like feeling, as well as impotence, joint pain, headache and stomach ache, swelling of the legs and ankles, dizziness and drowsiness. Discomfort of the gastrointestinal tract can also occur. These include general symptoms such as nausea, vomiting, diarrhea and any weight gain.

Rhabdomyolysis (muscle breakdown), which is characterized by muscle cramps, pain and weakness, is typical, but rarely the case, for therapy with etofibrate. Statins also cause rhabdomyolysis, so a combination with etofibrate should be used with caution.

Furthermore, etofibrate also increases the lithogenicity of the bile, which is why there is an increased risk of developing gallstones. Etofibrate should not be taken if you have liver, gallbladder or kidney disease. Pregnancy and breastfeeding are also contraindicated.