How bezafibrate works
Bezafibrate and other fibrates activate certain docking sites for endogenous messenger substances in liver cells, the so-called peroxisome proliferator-activated receptors (PPAR). These receptors regulate the activity of genes involved in fat and carbohydrate metabolism.
Overall, the intake of bezafibrate primarily lowers triglycerides. At the same time, the LDL value is slightly lowered and the HDL value slightly increased. In addition, fibrates have been shown to have a positive effect on diabetes, coagulation disorders and inflammation.
Background
There are different groups of lipoproteins. The best known are LDL and HDL. LDL transports cholesterol and other fat-soluble substances from the liver to other tissues, while HDL does the transport in the opposite direction.
But triglycerides (TG) can also be elevated, either in isolation or in combination with other lipoproteins. This is particularly common in cases of severe overweight (obesity), alcoholism and type 2 diabetes.
Consequently, the physician will first recommend a balanced, calorie-reduced diet, weight loss (if overweight), and exercise. If these measures cannot (sufficiently) lower the elevated TG, fibrates such as bezafibrate are prescribed.
Absorption, degradation and excretion
When taking Bezafibrate delayed-release tablets (sustained-release tablets), blood levels are halved again after about two to four hours.
When is bezafibrate used?
The indications for use (indications) of bezafibrate include:
- severely elevated triglyceride levels with or without concomitant lowered HDL levels
- Mixed hyperlipidemia (elevated levels of triglycerides and LDL cholesterol), when a statin is contraindicated or not tolerated
How Bezafibrate is used
Bezafibrate can be taken in the form of non-retarded tablets (immediate release). The usual dosage is 200 milligrams three times a day. On the other hand, sustained-release tablets are also available. They are taken once daily (in the morning or evening) (dosage: 400 milligrams of bezafibrate).
What are the side effects of bezafibrate?
The most common side effect of treatment with bezafibrate is an elevated creatinine level in the blood. An excessive increase in this value may indicate that the kidneys are no longer working sufficiently well – the dose must then be reduced or bezafibrate discontinued completely.
Discuss especially muscle pain and allergic reactions with your treating physician.
What should be considered when taking bezafibrate?
Contraindications
Bezafibrate should not be taken in the following cases:
- hypersensitivity to the active substance or to any of the other components of the drug
- liver disease (except fatty liver)
- gallbladder disease
- photoallergic reaction (rare form of sun allergy) in the past after taking fibrates
- Renal dysfunction (necessitating dose reduction and, if necessary, discontinuation of bezafibrate).
- in combination with statins if there are concomitant conditions that increase the risk of muscle disease (myopathy), e.g., renal dysfunction, severe infection, wounds
Interactions
The cholesterol-lowering drug colestyramine inhibits the absorption of bezafibrate in the intestine. The two active ingredients should therefore be taken at least two hours apart.
The effect of blood sugar-lowering drugs (such as sulfonylureas, insulin) in diabetics is also enhanced by bezafibrate. The physician may therefore have to adjust the diabetes therapy.
Bezafibrate should not be taken together with monoaminooxidase inhibitors (MAO inhibitors). MAO inhibitors are used for depression and Parkinson’s disease.
Age Limitation
Pregnancy and lactation
Pregnant and lactating women should not take bezafibrate because of limited data. If possible, avoid use in these patient groups.
How to obtain medicines containing bezafibrate
Medicines containing the active ingredient bezafibrate are available only on prescription in Germany, Austria and Switzerland. In Switzerland, only the retard tablets are on the market.
Since when is bezafibrate known?
Since the introduction of statins, which have fewer side effects, in 1987, the use of preparations containing the active ingredient bezafibrate has declined steadily.
