Finofibrate ( Antara, Triglide, Lofibra)
Mechanism Of Action:
Fibrates stimulate the activity of peroxisome proliferating activating receptors (PPAR alpha), a class of nuclear receptor. Activation of these receptors alters the transcription of a number of genes involved in triglyceride metabolism including lipoprotin lipase and apolipoprotein CIII. This increases the peripheral catabolism (breakdown) of VLDL and chylomicrons, resulting in a reduction in the plasma concentration of VLDL, most notably in triglycerides, moreover, fibrates also reduce the synthesis of cholesterol, which further reduce plasma triglycerides.
Clinical and therapeutic uses:
a) Fenofibrate can be used to treat hyperlipidemia of several etiologies, especially hypertriglyceridemia due to dysbetalipoproteinemia, a defect in apolipoprotein E that impairs clearance of chylomicron remnants and VLDL.
b) it is ineffective in primary chylomicronemia (caused by deficiency in lipoprotein lipase).
c) it has antidiuretic action in individuals with mild to moderate diabetes insipidus
Adverse effects:
1. cholelithiases
2. Cholecystitis
3. GI intolerance
4. Nausea
5. Diarhea
6. Myalgia
7. displace other albumin bound drugs esp. sulfonyl ureas and warfarin
8. should be used cautiously in hepatic and renal impairment.