Fibrates are carboxylic acids and belong to the organic compounds. Various representatives such as clofibrate, gemfibrozil and etofibrate are known on the market. Fibrates bind to specific receptors in cell organelles, causing a reduction in blood lipid levels. They are therefore used to treat lipid disorders such as high cholesterol or triglyceride levels. Fibrates should not be prescribed in cases of known liver disease. The drug may cause side effects such as nausea, bloating, vomiting, abdominal pain, and headache.
What are fibrates?
Fibrates and fibrinic acids belong to the group of carboxylic acids. These acids carry at least one carboxy group and belong to the chemical class of organic compounds. This means that their molecular compounds contain water and carbon. Fibrates are available on the market under various trade names. Representatives of this group include fenofibrate, clofibrate, bezafibrate, etofibrate, and gemfibrozil.
Pharmacologic effects on the body and organs
Fibric acid, fibrates, and their derivatives accelerate the breakdown of fatty acids in the peroxisome. Peroxisomes are cell organelles found in eukaryotes. They are surrounded by a cell membrane and are one of the detoxification apparatuses in the human organism. Fibrates bind to the so-called peroxisome proliferator-activated receptors. These receptors are called PPARs for short. They are located in the cells and can be activated by both physiological and pharmacological ligands. They then serve as transcription factors and regulate the expression of various genes. When fibrates bind to the PPARs, there is a sizing of the receptor and subsequent binding to deoxyribonucleic acid, or DNA. As a result, there is increased degradation of LDL cholesterol. This can reduce LDL levels, the “bad” cholesterol, by ten to twenty percent. At the same time, this promotes an increase in “good” cholesterol, or HDL, by five to ten percent. Furthermore, the triglyceride level can be reduced by twenty to forty percent. At the same time, fibrate promotes the secretion of two enzymes. As a result, more cholesterol is secreted into the bile. This results in a slightly increased risk of developing cholestrol-containing gallstones.
Medical use and application for treatment and prevention.
Fibrates are used in medicine to treat high blood lipid levels. Blood lipids are different lipids in the blood. In addition to cholesterol, they include triglycerides and fat-soluble vitamins. Fibrates are used to treat various disorders of lipid levels, while the so-called statins are prescribed almost exclusively for the treatment of hypercholesterolemia. In addition to disorders of blood lipid levels, so-called hypertriglyceridemia is a clinical picture that is treated with fibrates. The main goal of treatment with fibrates is prevention of arteriosclerosis. Arteriosclerosis is a calcification of the blood vessels that can lead to fatal secondary diseases such as stroke or heart attack. Contraindications for these drugs include liver disease, gallbladder disease and known photosensitivity of the skin. Furthermore, dialysis patients and patients allergic to fibric acid must not be treated with the drug. The intake and dosage of the drug should be individually tailored to the patient and their disease severity. Fibrates are usually not administered as monotherapy. Elevated blood lipid levels can also be positively influenced by adequate exercise and nutritional intervention. Thus, the drug is usually part of a multi-column therapy. Pregnant women and nursing mothers should always consult their attending physician before taking the drug. With regard to dosage in children, there are as yet no conclusive figures. Fibrates usually have to be administered over a longer period of time. Patients should take the medication regularly and act as prescribed by their treating physician. If the dosage is suspected to be too weak or too strong, the physician should be contacted immediately. Furthermore, it is necessary to check blood lipid levels regularly to verify the effectiveness of the therapy and modify it if necessary.
Risks and side effects
Taking fibrates may cause risks and side effects.However, when used correctly, most of the listed side effects are only temporary. Discontinuation of the drug is not always mandatory when undesirable side effects occur and should never be done on one’s own but always in consultation with the treating physician. Common adverse effects include abdominal pain, bloating, constipation, loss of appetite, nausea, dizziness, skin rash, headache, fatigue, diarrhea, and dyspepsia. The latter is characterized by indigestion in the upper abdomen. It is characterized by malaise, burning of the stomach, and an early feeling of satiety. Rather rarely, fibrates can lead to muscle disorders. In isolated cases, ingestion can lead to liver dysfunction. Very rarely, so-called rhabdomyolysis can occur. This is a life-threatening dissolution of the striated skeletal muscles. Symptoms of this disease include fever, vomiting, muscle weakness, muscle pain and acute renal failure. As mentioned in the paragraph above, fibrates may increase the risk of developing cholesterol-containing gallstones. Interactions with other medications such as antidiabetics or anticoagulants are possible. Therefore, it is important to ask about the use of other medications when discontinuing the drug.