Fenofibrate

Products

Fenofibrate is commercially available in the form of capsules (lipanthyl). It has been approved in many countries since 1977. In 2014, a fixed combination with simvastatin was registered (Cholib); see Fenofibrate Simvastatin.

Structure and properties

Fenofibrate (C20H21ClO4, Mr = 360.8 g/mol) exists as a white crystalline powder that is practically insoluble in water. It is a benzophenone derivative and a prodrug that is metabolized in the body to the active fenofibric acid. Today, micronized fenofibrate is mainly used. Some drugs also contain the active fenofibric acid in the form of the choline salt choline fenofibrate, a white to yellow powder that is highly soluble in water (Trilipix).

Effects

Fenofibrate (ATC C10AB11) has lipid-lowering properties. It lowers cholesterol, triglycerides, and increases HDL. The effects are due to activation of nuclear receptors PPARα (Peroxisome Proliferator Activated Receptors). PPAR regulate genes that play important roles in lipid and glucose metabolism.

Indications

For the treatment of severe hypercholesterolemia and mixed hyperlipidemia.

Dosage

According to the SmPC. Medicines are usually taken once daily with a meal. Food taken at the same time increases absorption into the body.

Contraindications

  • Hypersensitivity
  • Renal insufficiency
  • Hepatic insufficiency
  • Persistent liver dysfunction
  • Diseases of the gallbladder
  • Previous photoallergy or phototoxic reaction under fibrates or ketoprofen.
  • Pancreatitis

For complete precautions, see the drug label.

Interactions

Drug-drug interactions are possible with oral anticoagulants, ciclosporin, hepatotoxic agents, and MAO inhibitors. Fenofibrate is a weak to moderate inhibitor of CYP2C19, CYP2A6, and CYP2C9.

Adverse effects

The most common potential adverse effects include digestive symptoms such as abdominal pain, nausea, vomiting, diarrhea, and flatulence, as well as an increase in serum transaminases. Fenofibrate can make the skin sensitive to UV radiation and rarely cause serious side effects such as muscle disorders, liver inflammation, and pancreatic inflammation.