Gemfibrozil: Effects, Uses & Risks

Gemfibrozil is a medical agent that belongs to the so-called fibrates. As such, gemfibrozil is administered to treat diseases as well as disorders of lipid metabolism. It can also be taken for dietary purposes. Through this, weight loss can be achieved.

What is gemfibrozil?

Gemfibrozil is an orally taken fibrate. The term fibrate covers various agents in human medicine that are used to treat severely elevated levels of cholesterol and triglycerides in the blood (hyperlipoproteinemia, or HLP). Gemfibrozil is therefore indicated primarily for diseases and disorders of lipid metabolism. By administering it, cholesterol levels, vascular deposits and blood lipid levels can be significantly reduced. It is also possible to reduce the risk of vasoconstriction by taking gemfibrozil, as well as to slow down constriction that is already taking place. The drug is described in chemistry and pharmacology by the molecular formula C 15 – H 22 – O 3, which corresponds to a moral mass of 250.34 g/mol. The white, waxy and crystalline powder is processed into film-coated tablets, which the patient takes independently. These are marketed under the trade name Gevilon.

Pharmacological effects on the body and organs

Gemfibrozil achieves its efficacy through activity at the receptor level. Here, it interferes with lipid metabolism in the human body. This involves binding to the so-called peroxisome proliferator-activated receptor (PPARα for short). This binding causes a synthesis of lipoprotein lipases from triglycerides. Lipases are water-soluble enzymes that cause cleavage of ester bonds into neutral fat. Lipoprotein lipases are able to cleave lipoproteins found in the blood, which prepares them well for cellular uptake. Due to the synthesis of lipoprotein lipases and triglycerides caused by gemfibrozil, there is a decrease in triglyceride levels in the blood. In addition, VLDL, and LDL levels are also lowered. LDL cholesterol increases the risk of stroke and heart attack. Literature reports that gemfibrozil lowers LDL levels between 10% and 20%. Moderate levels of HDL, on the other hand, are reported to be able to increase between 5% and 20%.

Medical use and use for treatment and prevention.

Gemfibrozil is being shifted for adjunctive treatments of lipid metabolism diseases and disorders. Gemfibrozil forms the second leg of therapy along with diet or other measures such as exercise. However, according to current therapeutic practice, gemfibrozil represents ultima ratio. The drug is therefore not the first choice. In advance, attempts must or should be made to treat the lipid metabolism in other ways. These include a change in diet, sufficient exercise and weight reduction. In addition, it should be checked whether the patient can be successfully treated beforehand with drugs from the statin group. As described in the literature, it has been shown that taking gemfibrozil can reduce the risk of myocardial infarction and the likelihood of coronary artery disease. Currently, gemfibrozil is indicated primarily in cases of type III hyperlipidemia or type IV hypertriglyceridemia. Gemfibrozil is subject to pharmacy and prescription restrictions in Germany and other European Union countries. The active ingredient is therefore only available in pharmacies and may not be dispensed without a doctor’s certificate. When taking it, it is mandatory to follow the instructions of the attending physician.

Risks and side effects

Since gemfibrozil is an effective drug, taking it does not remain completely free of risks. Attention should be paid to contraindications as well as side effects. A contraindication is when taking gemfibrozil does not produce the desired effects from a medical point of view but leads to severe risks. This is also referred to as a contraindication. In these cases, it is imperative to refrain from taking or administering the drug. Gemfibrozil is contraindicated in cases of allergy or hypersensitivity to gemfibrozil or other members of the fibrate group. Gemfibrozil must also not be taken in cases of acute liver or kidney dysfunction. This also applies to pregnant women, as the effects on the unborn child have not yet been fully clarified.In addition, interactions with other medications must be taken into account. These can occur especially with blood sugar-lowering drugs such as repaglinide or statin. The treating physicians must be informed. Furthermore, undesirable side effects are possible in the course of treatment. However, this is not mandatory. So far, a connection between the intake of gemfibrozil and the formation of gallstones has been established. Other side effects include an increased risk of carcinoma, hypokalemia or rhabdomyolysis. The latter is most noticeable by severe, sudden muscle pain. In addition, the patient’s blood count and lipid levels must be monitored during the treatment period. An examination of liver values may also be necessary. In addition, gemfibrozil impairs the ability to drive. After taking it, do not participate in road traffic. The operation of heavy machinery or equipment must also be refrained from.