Products
Bezafibrate is commercially available in the form of sustained-release tablets (Cedur retard). It has been approved in many countries since 1979.
Structure and properties
Bezafibrate (C19H20ClNO4, Mr = 361.8 g/mol) lies as a white crystalline powder that is practically insoluble in water.
Effects
Bezafibrate (ATC C10AB02) primarily lowers elevated blood triglyceride levels. It has a moderate effect on LDL cholesterol and slightly increases HDL. In recent years, the mechanism of action has been elucidated. Fibrates activate nuclear receptors from the PPAR (peroxisome proliferator-activated receptor) family, which regulate genes that play an important role in lipid and glucose metabolism. According to Tenenbaum et al. (2005), bezafibrate is a pan-agonist and activates all three known PPAR subtypes, alpha, gamma and beta/delta. Accordingly, it is similar to glitazars, which are dual PPAR-α/γ agonists.
Indications
Bezafibrate is used to treat primary and secondary hyperlipidemias.
Dosage
According to the drug label. Bezafibrate is usually taken once daily after or with a meal. Non-retarded dosage forms are also commercially available in Germany, which must be administered three times daily.
Contraindications
- Hypersensitivity
- Known photoallergy or photoallergic reactions to fibrates.
- Pregnancy and lactation
- Liver disease
- Gallbladder diseases
- Serum creatinine levels > 1.5 mg/100 ml or with a creatinine clearance ≤ 60 ml/min
- Dialysis patients
- Bezafibrate should not be co-administered with statins if predisposing factors for myopathy are present.
For complete precautions, see the drug label.
Interactions
Drug-drug interactions have been described with the following agents: Vitamin K antagonists, estrogens, cholestyramine, perhexiline hydrogen maleate, MAO inhibitors, immunosuppressants, sulfonylureas, insulins. Statins may potentially increase the risk of muscle disease (rhabdomyolysis).
Adverse effects
The most common adverse effect is decreased appetite. Occasionally, hypersensitivity reactions, dizziness, headache, indigestion, muscle weakness, muscle disorders, muscle pain, muscle cramps, skin reactions, cholestasis, acute renal failure, erectile dysfunction, and altered laboratory values may occur. Very rare are severe blood count changes, skin reactions, skeletal muscle disintegration (rhabdomyolysis), and gallstones.
