Gemfibrozil

Products

Gemfibrozil is commercially available in the form of film-coated tablets (Gevilon, Gevilon Uno). It has been approved in many countries since 1985.

Structure and properties

Gemfibrozil (C15H22O3, Mr = 250.3 g/mol) exists as a white powder that is practically insoluble in water.

Effects

Gemfibrozil (ATC C10AB04) has lipid-lowering properties. It lowers VLDL, triglycerides, total cholesterol, and LDL and increases HDL. The effects are due to activation of nuclear receptors of the PPAR (peroxisome proliferator-activated receptor) family, which regulate genes that play important roles in lipid and glucose metabolism.

Indications

  • Severe hypertriglyceridemia
  • Mixed hyperlipidemia (2nd choice agent).
  • Primary hypercholesterolemia (2nd choice agent).
  • For the prevention of cardiovascular disease (certain patient groups, 2nd choice agents).

Dosage

According to the professional information. The tablets are administered once daily with dinner.

Contraindications

  • Hypersensitivity
  • Impaired liver function
  • Gallbladder disease
  • Severe renal dysfunction
  • Photoallergic or phototoxic reactions among fibrates in patient history.
  • Pregnancy and lactation
  • Gemfibrozil must not be combined with repaglinide, a substrate of CYP2C8

For complete precautions, see the drug label.

Interactions

Gemfibrozil is an inhibitor of several CYP450 isozymes (CYP2C8, CYP2C9, CYP2C19, and CYP1A2) as well as UGTA1 and UGTA3. It should not be combined with other fibrates or statins. Other drug-drug interactions have been described with anticoagulants, antidiabetics, estrogens, ion-exchange resins, and bexarotene.

Adverse effects

The most common possible adverse effects include dyspepsia, abdominal pain, constipation, flatulence, loss of appetite, nausea, vomiting, diarrhea, rash, headache, dizziness, and fatigue. Fibrates may rarely cause muscle disease and very rarely rhabdomyolysis, and may cause liver dysfunction.