Fibrate

Fibrates ( Fibrinsäuren and derivatives thereof ) are a group of carboxylic acids, which are used in the medical field as a drug for the treatment of high blood lipid levels. The use of fibrates is indicated for hypercholesterolemia and hypertriglyceridemia.

Mechanism of action

Fibrates cause an increase in activity of fatty acid oxidation in peroxisomes by binding to the intracellular PPAR. This leads, similar to the mechanism of glucocorticoid receptors, the binding of fibrates to PPAR for the dimerization of the receptor, followed by binding to the DNA. This leads inter alia to an increase in degradation of the LDL cholesterol. In addition, the VLDL synthesis is reduced. The result is a decrease in LDL cholesterol by 10-20% and an increase in the " good" HDL cholesterol by 5-10%. The triglycerides are reduced by 20-40%.

The use of fibrates is controversial because they - have failed to demonstrate a prolongation of life - in contrast to the statins. In the treatment of CHD, they are considered lipid - lowering agents of second choice, especially if statins are not tolerated or hypertriglyceridemia dominated.

Interactions

Concomitant use of other drugs, there may be interactions. Thus, it may lead to increased anticoagulation with concurrent use of oral anticoagulants, and increase blood sugar when given concomitantly with oral antidiabetics and insulin. There is also an increased risk of myopathy with concomitant use of statins and nicotinic acid derivatives.

As a side effect is often a tendency for the formation of gallstones. Complaints of the gastrointestinal tract are equally observed.

Reduction

The fibrates are metabolized in the body to clofibric acid. This accumulates because of their high microbial persistence and low sorption in groundwater.

Representative

• Bezafibrate ( Cedur ®)
• Clofibrate (except trade )
• Etofibrate ( Lipo -Merz retard )
• Fenofibrate ( Lipidil ®, Liperial ® [ D]; Lipcor ® [ AT ]; Lipanthyl ® [ CH], numerous generics)
• Gemfibrozil ( Lopid ®)