6533b860fe1ef96bd12c37d7

RESEARCH PRODUCT

Fibratos: efectos farmacológicos

subject

description

Fibrates have demonstrated efficacy in modifying the various parameters of atherogenic dyslipidemia. The best known fibrate is fenofibrate, which is indicated for the treatment of hypertriglyceridemia with or without low high-density lipoprotein cholesterol (HDL-c) and the treatment of atherogenic dyslipidemia in patients with statin intolerance or contraindications. Fenofibrate is also indicated in association with statins in patients with high cardiovascular risk when HDL-c and triglyceride (TG) concentrations are poorly controlled. The lipid-lowering effects of fenofibrate are mediated by activation of the nuclear transcription factor PPARα, which leads to an increase of lipolysis and plasma clearance of atherogenic TG-rich particles. Fenofibrate favors beta-oxidation of fatty acids and inhibits their synthesis, thus reducing the substrate for TG synthesis. The maximum plasma concentration is reached between 2 and 4 hours after oral fenofibrate administration in nanoparticles. Plasma stability is achieved a few days later and is maintained throughout treatment. The pharmacological effects of the drug become apparent after the first 2 weeks of treatment. The half-life is 21.7 hours, and the drug is eliminated mainly through the urine. Therapeutic effectiveness is demonstrated by decreases in cholesterol of between 20% and 25%, reductions in TG of between 40% and 55% and increases in HDL-c of between 10% and 50%, depending on the lipid phenotype. In general, fenofibrate is well tolerated and the most frequent adverse effects (<10%) are gastrointestinal symptoms and an increase in transaminase levels.