Pharmacological properties : תכונות פרמקולוגיות

Pharmacodynamic Properties

5.1 Pharmacodynamic properties

Pharmakotherapeutic group: lipid-lowering agent, ATC Code: C10A B02
Bezafibrate lowers elevated blood fat levels (triglycerides and cholesterol). It lowers elevated VLDL and LDL concentrations and increases HDL levels. The activity of the triglyceride lipases involved in the breakdown of triglyceride-rich lipoproteins (lipoprotein lipase and hepatic lipoprotein lipase) is increased by the action of bezafibrate. HDL precursors develop during the accelerated breakdown of triglyceride- rich lipoproteins (chylomicrons, VLDL), which explains the increase in HDL levels. Bezafibrate also reduces cholesterol biosynthesis, in parallel to which, it stimulates the LDL receptor-mediated lipoprotein breakdown.

Bezafibrate also acts on thrombogenic factors: besides a decrease in platelet aggregation, it also achieves a significant lowering of elevated fibrinogen levels and blood viscosity.


The consensus conference of the European Atherosclerosis Society in Naples in June 1986 undertook to establish limits for disorders of fat metabolism that are to be used as guidelines for diagnosis and treatment:

In all adults, cholesterol and triglyceride levels warrant medical attention if they exceed 200 mg/dl.

The overall risk for coronary heart disease, taking into account family history, smoking habits, hypertension, diabetes mellitus, male sex, younger age and lower HDL cholesterol levels below 35 mg/dl, is estimated to be with cholesterol levels of between 200 and 300 mg/dl. (HDL = higher density lipoproteins, half of which consist of protein [apolipoprotein]. They play a role in the breakdown of triglyceride-rich lipoproteins [chylomicrons and VLDL] and in the removal of cholesterol from the arteries' endothelial cells.)

The following is recommended in patients with HDL cholesterol levels below 35 mg/dl and/or with other risk factors present:

For most people with cholesterol levels between 200 and 250 mg/dl, dietary advice and the treatment of the other risk factors present are recommended. For people with severe hypercholesterolaemia (250 - 300 mg/dl) intensive dietary treatment and, where necessary, drug therapy with regular monitoring of effects are recommended.

In isolated cases exhibiting increased triglyceride levels (200 - 500 mg/dl) the cause of the hypertriglyceridaemia should be investigated.

Cases of extreme hyperlipidaemia (cholesterol exceeding 300 mg/dl, triglycerides exceeding 500 mg/dl) require a secondary diagnosis from specialists in fat metabolism.

Drug therapy is only indicated if hyperlipoproteinaemia cannot be rectified despite adopting consistent non-drug measures, or by treating an existing primary disease such as diabetes mellitus, gout or other disease.

In diabetics, decreased glucose blood levels as a result of improved glucose tolerance have been reported. In these patients, both fasting and postprandial free fatty acid concentrations were reduced.

Pharmacokinetic Properties