Bezafibrate: Effects, Uses & Risks

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

What is bezafibrate?

Bezafibrate (chemical name: 2-(4-{2-[(4-chlorobenzoyl)amino]ethyl}phenoxy)-2-methylpropionic acid), like clofibrate or fenofibrate, is a derivative of fibrates. Fibrates are drugs used to treat elevated blood lipids (hyperlipidemia). Bezafibrate is primarily used to lower high levels of triglycerides. However, the cholesterol-lowering effect in the blood is only slightly pronounced, which is why cholesterol lowering is primarily ensured by the drug group of statins. The cholesterol lowering effect of bezafibrate is only about 10 to 25 percent; accordingly, the greatest effect is more likely to be in the lowering of triglycerides (about 20 to 40 percent). Elevated triglycerides are a major problem because, on the one hand, they are difficult to treat and, on the other, they can cause severe cardiovascular disease. The consequences of elevated plasma levels of the fats range from atherosclerosis to heart attack and stroke. Statins are preferred here because they can greatly lower lipids and thus also reduce the risk of secondary diseases. In addition, fibrates are treated only as a second choice and are used if statin therapy is not effective, if statins are not tolerated, or if only those triglycerides are elevated whose lowering is the main effect of bezafibrate. Bezafibrate is given as a tablet or capsule containing a white and insoluble crystalline powder. Bezafibrate is broken down by being excreted in the urine after it is broken down to clofibric acid. Accordingly, the dose should be adjusted in renal insufficient patients.

Pharmacologic effects on body and organs

A reduction in the concentration of triglycerides is the most important effect of bezafibrate and other fibrates. However, exactly how this is achieved is not yet clear. Nevertheless, it is likely that bezafibrate drives a so-called PPARα or peroxisome proliferator-activated receptor. Some studies show that it also activates the PPARγ and PPARδ. The PPARα is a protein that binds to DNA and alters molecular processes there that are important for lipid metabolism. For example, it causes an increased reduction of LDL by 10 to 25 percent. This cholesterol is called bad because it is deposited in the walls of blood vessels and causes an inflammatory reaction there. Atherosclerosis is the result. Besides, bezafibrate causes an increase in HDL, which is also called good cholesterol. It is described as good because it helps to collect the cholesterol that has been deposited everywhere and transport it to the liver, through which it is subsequently excreted. In the liver, bezafibrate also causes a lower release of VLDL, which also contains cholesterol, but mainly triglycerides. Another effect is that bezafibrate activates lipoprotein lipase, a triglyceride-degrading enzyme. At the vessel walls, bezafibrate causes an anti-inflammatory process. Bezafibrate additionally acts at the gallbladder, where it increases the lithogenicity of bile, meaning that the risk of developing gallstones is increased.

Medical use and use for treatment and prevention.

Bezafibrate is used for elevated plasma levels of triglycerides. Elevated blood lipids can be congenital on the one hand, in which case there is usually a defect in an enzyme that is needed to break down triglycerides. This condition is also known as primary familial hypertriglyceridemia. On the other hand, elevated blood lipids may be acquired (secondary hypertriglyceridemia). The latter has various causes. For example, an elevated triglyceride level may be caused by the physician prescribing drugs that increase blood lipids (for example, 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 alter blood lipids. The metabolic syndrome (quartet of: Glucose intolerance, hypertension, impaired 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 and side effects

The adverse effects of bezafibrate are varied. For example, nonspecific effects include swelling, problems with breathing, and hives, which can be explained due to an allergic reaction of the body to bezafibrate. Other side effects include fever, a flu-like feeling, and also atypical effects such as headache, dizziness, alteration of consciousness, erection problems, and aching limbs. There are also gastrointestinal effects such as nausea, vomiting and diarrhea, as well as sudden weight gain. Loss of appetite is also frequently observed. Rather rarely, muscle breakdown or rhabdomyolysis is observed with bezafibrate. Patients suffer from pain, cramps and muscle weakness. Muscle breakdown can also be caused by statins, which is why these should not be given in combination with bezafibrate. A change in the blood count is also a rather rarely observed side effect. In addition, bezafibrate increases the lithogenicity of bile, which increases the risk of gallstones. Patients with liver disease or gallbladder disease, as well as renal insufficiency patients or pregnant women and nursing mothers, should not take bezafibrate.