Clofibrate

What it is and how it works

Clofibrate activates peroxisome proliferator-activated receptor alpha (PPAR-alpha), increasing lipoprotein lipase activity and fatty-acid oxidation and reducing hepatic VLDL production. This lowers serum triglycerides markedly, with a smaller effect on LDL cholesterol.

Indications

Historically used for hypertriglyceridaemia and type III hyperlipoproteinaemia not responding to diet; now largely superseded by other fibrates and statins because of an unfavourable safety profile.

Dosage and administration (summary)

Oral (adults): historically 1.5–2 g daily in two to three divided doses with meals.

Contraindications

Severe hepatic or renal impairment; primary biliary cirrhosis; gallbladder disease or gallstones; pregnancy and breast-feeding; hypersensitivity.

Warnings and precautions

Long-term use was associated with increased incidence of cholelithiasis and cholecystitis and, in a WHO trial, with increased non-cardiovascular mortality. Myositis and rhabdomyolysis may occur, particularly in renal impairment or with statins. Potentiates oral anticoagulants (reduce warfarin dose and monitor INR) and may cause hepatic dysfunction.

Pregnancy

Contraindicated in pregnancy.

Storage and supply

Store below 25 °C, protected from light.

Source: reference summary prepared from the EU SmPC/EPAR, BNF and WHO Model Formulary. The approved product information in Iran governs.