Bezafibrate

Bezafibrate belongs to the group of fibrates. Bezafibrate is a lipid-lowering drug and, in addition to statins and nicotinic acid, is an important therapeutic option for the treatment of high triglycerides in particular, but also, in some cases, high cholesterol.

What is bezafibrate?

Bezafibrate (chemical name: 2- (4- {2 - [(4-chlorobenzoyl) amino] ethyl} phenoxy) -2-methylpropionic acid) is, like clofibrate or fenofibrate, a derivative of fibrates. Fibrates are medicines that are used to treat high blood lipids (hyperlipidemia). Bezafibrate is primarily used to lower too high a level of triglycerides.

The cholesterol-lowering effect in the blood is, however, only slightly pronounced, which is why the cholesterol lowering is primarily ensured by the medicinal group of statins. The cholesterol lowering through bezafibrate is only approx. 10 to 25 percent, the greatest effect is accordingly more in the lowering of triglycerides (approx. 20 to 40 percent).

Elevated triglycerides are a major problem because they are difficult to treat and can cause severe cardiovascular disease. The consequences of an increased plasma level of fats range from atherosclerosis to heart attacks and strokes.

Statins are preferred because they can greatly reduce lipids and thus also reduce the risk of secondary diseases. In addition, fibrates are only treated as a second choice and are used when therapy with statins does not work, these are not tolerated or when only those triglycerides are increased, the lowering of which is the main effect of bezafibrate.

Bezafibrate is given as a tablet or capsule, which contains a white and insoluble crystalline powder. Bezafibrate is broken down by excreting it in the urine after it is broken down into clofibric acid. The dose should be adjusted accordingly in patients with renal insufficiency.

Pharmacological effect on the body and organs

Lowering the concentration of triglycerides is the main effect of bezafibrate and other fibrates. How this is achieved, however, is not yet fully understood. Nevertheless, it is likely that bezafibrate drives a so-called PPARα or peroxisome proliferator activated receptor. Some studies show that it also activates PPARγ and PPARδ. PPARα is a protein that binds to DNA and changes molecular processes there that are important for lipid metabolism. For example, it causes an increased reduction in LDL by 10 to 25 percent. This cholesterol is called bad because it is deposited in the vessel walls and causes an inflammatory reaction there. Atherosclerosis is the result.

In addition, bezafibrate causes an increase in HDL, which is also known as good cholesterol. It is described as good because it helps to collect the cholesterol that has built up everywhere and transport it to the liver, where it is then excreted. In the liver, bezafibrate also reduces the release of VLDL, which also contains cholesterol, but mainly triglycerides.

Another effect is that bezafibrate activates lipoprotein lipase, a triglyceride-breaking enzyme. Bezafibrate causes an anti-inflammatory process on the vessel walls. Bezafibrate also acts on the gallbladder, where it increases the lithogenicity of the bile, which means that the risk of developing gallstones is increased.

Medical application & use for treatment & prevention

Bezafibrate is used when the plasma level of triglycerides is increased. On the one hand, elevated blood lipids can be congenital, and an enzyme that is required to break down triglycerides is usually defective. This condition is also known as primary familial hypertriglyceridemia. On the other hand, elevated blood lipids can be acquired (secondary hypertriglyceridemia). The latter has various causes. An increased triglyceride level can be caused by the doctor who prescribes drugs that increase blood lipids (e.g. beta blockers, glucocorticoids, hormones). But an incorrect, high-fat diet can also lead to an increase in triglycerides.

The metabolic disorder diabetes can also negatively affect blood lipids. The metabolic syndrome (quartet of: glucose intolerance, hypertension, disturbed lipid metabolism and obesity) is also a possible application of bezafibrate.

Bezafibrate has a half-life of 2 hours and is taken in the form of tablets or capsules of 200 mg three times a day.

Risks & side effects

The undesirable effects of bezafibrate are many. Non-specific effects include swelling, breathing problems and nettle formation, which can be explained by the body's allergic reaction to bezafibrate.

Other side effects are fever, a flu-like feeling and also atypical effects such as headache, dizziness, changes in consciousness, erection problems and body aches. In addition, there are effects on the gastrointestinal area such as nausea, vomiting and diarrhea, as well as sudden weight gain. Loss of appetite is just as common.

Muscle breakdown or rhabdomyolysis is rarely observed with bezafibrate. Patients suffer from pain, cramps and muscle weakness. Muscle breakdown can also be caused by statins, which is why they should not be given in combination with bezafibrate. A change in the blood count is also a rarely observed side effect. Bezafibrate also increases the lithogenicity of the bile, which increases the risk of developing gallstones. Patients with liver disease or gallbladder disease, kidney insufficiency, pregnant women and nursing mothers should not take bezafibrate.