Home Medicines Bezafibrate: effect, areas of application, side effects

Bezafibrate: effect, areas of application, side effects

by Josephine Andrews
Published: Last Updated on 261 views

Bezafibrate is used to lower elevated blood fat levels. The active substance belongs to the class of fibrates. This class of active ingredients has been known and tested for a long time. Nevertheless, it is increasingly being replaced by statins because, unlike fibrates, they also have a life-prolonging effect. Here you can read everything you need to know about the effects and use of bezafibrate, side effects and interactions.

This is how bezafibrate works

Bezafibrate and other fibrates activate specific docking sites for the body’s own messenger substances in the liver cells, the so-called peroxisome proliferator-activated receptors (PPAR). The activity of genes involved in fat and carbohydrate metabolism is regulated via these receptors.

The blockage by bezafibrate is the signal for the liver cells to take up more LDL (low-density lipoprotein, lipoprotein; “bad fat “) and triglycerides (TG) from the blood and some more HDL (high-density lipoprotein, lipoprotein). high density; “good fat”).

Overall, taking bezafibrate primarily lowers triglycerides. At the same time, the LDL value is slightly reduced and the HDL value is slightly increased. Fibrates have also been shown to have a positive effect on diabetes, coagulation disorders and inflammation.

background

The blood contains so-called lipoproteins, which are required for the transport of fat-soluble substances in the watery blood. Fat-soluble substances include neutral fats (triglycerides), cholesterol (an important component of cell membranes and a precursor to some hormones and bile acids) and vitamins A, D, E and K.

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 transports them in the opposite direction.

High LDL cholesterol levels can therefore promote “hardening of the arteries” (arteriosclerosis), i.e. the “deposition” of fats in the blood vessels. Therefore, LDL cholesterol is also called “bad” cholesterol. Conversely, elevated HDL cholesterol levels are beneficial because HDL transports excess cholesterol from the tissues back to the liver where it can be converted into other substances.

However, triglycerides (TG) can also be elevated, either in isolation or in combination with other lipoproteins. This is particularly common in those who are severely overweight (obesity), alcoholism and type 2 diabetes .

In contrast to LDL and HDL, TG values ​​are significantly influenced by nutritional behavior. As a rule, increased TG levels can be reduced very well with the right diet (including little sugar and sweets, lots of plant-based foods), reducing alcohol consumption and, if necessary, good diabetes control.

The doctor will therefore first recommend a balanced, calorie-reduced diet, weight loss (if you are overweight) and physical activity. If these measures cannot (sufficiently) lower the elevated TG, fibrates such as bezafibrate are prescribed.

intake, degradation and excretion

After ingestion, the active ingredient enters the blood via the intestines, where it reaches its highest concentration after one to two hours. Bezafibrate is partially broken down at its site of action, the liver, and excreted in the urine via the kidneys.

When taking the delayed-release bezafibrate tablets (prolonged-release tablets), the blood levels halve again after about two to four hours.

When is bezafibrate used?

The areas of application (indications) for bezafibrate include:

  • severely elevated triglyceride levels with or without concomitantly decreased HDL levels
  • mixed hyperlipidemia (elevated triglycerides and LDL-cholesterol) when a statin is contraindicated or not tolerated

Treatment with bezafibrate should be combined with an appropriate diet and other non-drug measures. It can also take place in the longer term if non-drug measures alone do not improve the blood lipid levels sufficiently.

How bezafibrate is used

On the one hand, bezafibrate can be taken in the form of non-retarded tablets (immediate release of active ingredient). The usual dosage is 200 milligrams three times a day. On the other hand, slow-release tablets are also available, i.e. tablets with a delayed release of active ingredients. They are taken once a day (morning or evening) (dosage: 400 milligrams of bezafibrate).

The tablets should be taken with a glass of water before or after a meal. In patients with a sensitive stomach, treatment should be started with a low starting dose, which is then slowly increased. If the therapy is working well, the dosage can be reduced.

What are the side effects of bezafibrate?

The most common occurrence during treatment with bezafibrate is an increase in the level of creatinine in the blood. An excessive increase in this value can indicate that the kidneys are no longer working well enough – the dose must then be reduced or bezafibrate must be discontinued completely.

Occasionally, side effects in the form of hypersensitivity reactions, loss of appetite, headache, dizziness, feeling of fullness, nausea, bile stasis, itching, photosensitivity of the skin , skin bleeding, muscle weakness, pain and cramps as well as an increase in certain blood enzyme values ​​occur while taking bezafibrate.

Above all, discuss muscle pain and allergic reactions with your doctor.

What should be considered when taking bezafibrate?

Contraindications

Bezafibrate must not be taken in the following cases:

  • Hypersensitivity to the active substance or any of the other components of the drug
  • Liver disease (excluding fatty liver)
  • gallbladder disease
  • photoallergic reaction (rare form of sun allergy) in the past after taking fibrates
  • dialysis
  • Renal dysfunction (requiring dose reduction and possible discontinuation of bezafibrate)
  • in combination with statins if there are also diseases that increase the risk of muscle disease (myopathy), e.g. kidney dysfunction, severe infections, wounds

interactions

The cholesterol-lowering drug cholestyramine inhibits the absorption of bezafibrate in the intestine. The two active ingredients should therefore be taken at least two hours apart.

When bezafibrate is combined with coumarin-type anticoagulants (such as phenprocoumon , warfarin), coagulation levels should be closely monitored initially. In consultation with the doctor, the dose of the anticoagulant is usually reduced, since bezafibrate increases its effect.

The effect of blood sugar-lowering drugs (such as sulfonylureas, insulin ) in diabetics is enhanced by bezafibrate. The doctor may have to adjust the diabetes therapy.

Bezafibrate should not be taken with monoamine oxidase inhibitors (MAOIs). MAO inhibitors are used for depression and Parkinson’s disease .

age restriction

Nothing is known about the long-term safety or dosing of bezafibrate in children. The use in this age group must therefore be carefully considered by a doctor.

pregnancy and breast feeding period

Pregnant and breastfeeding women should not take bezafibrate because there is little data on this. If possible, use in these patient groups should be avoided.

How to get medication with bezafibrate

Drugs with the active ingredient bezafibrate are only available in pharmacies and require a prescription in Germany, Austria and Switzerland. Only the sustained-release tablets are commercially available in Switzerland.

Since when is bezafibrate known?

Fibrates have been known for over 80 years, although their mode of action could only be deciphered in the 1990s. Bezafibrate was approved as a drug in Germany in 1977.

Since the introduction of statins with fewer side effects in 1987, the use of preparations containing the active ingredient bezafibrate has steadily declined.

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