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Gemfibrozil

Brand names: Jezil®, Gevilon® and many more
German: Gemfibrozil

1 Definition

Gemfibrozil is a fibrate that is used in the treatment for diseases linked to the metabolism of lipids.

2 Indications

Gemfibrozil is used in the therapy of type III hyperlipidemia, and type IV hypertriglyceridema.

3 General information

In blood 95% of the substance is present bound to plasma proteins. It is hepatically metabolized via the cytochrom P450 system (CYP3A4) and subsequently mostly eliminated renally. A small portion is also eliminated through the feces. The biological half-life is approximately 1,5 hours.

4 Mechanism of action

Gemfibrozil influences the metabolism of lipids on a receptor level. It binds to the PPARα (peroxisome proliferator-activated receptor), where it activates the lipoprotein lipase synthesis from triglycerides. This his how the desired effect, a decrease of the triglyceride leves, is achieved. Also the levels of LDL, HDL and VLDL are lowered.

5 Adverse effects

  • There is a chance for development of rhabdomyolysis. Especially when taken in combination with statins (also have rhabdomyolysis as a possible side effect), and are therefore contraindicated.

It is noticed by a sudden and unexplainable onset of muscle pains.

6 Contraindications

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