Treatment of hyperlipidemia

Treatment of elevated triglyceride levels

Fenofibrate

Fenofibrate (sold under the brand names Tricor, Fenobrat etc.), is an oral medication of the fibrate class used to treat abnormal blood lipid levels.[1] It is less commonly used compared than statins because it treats a different type of cholesterol abnormality to statins. While statins have strong evidence for reducing heart disease and death, there is evidence to suggest that fenofibrate also reduces to the risk of heart disease and death. However, this seems only to apply to specific populations of people with elevated triglyceride levels and reduced high-density lipoprotein (HDL) cholesterol.[1][2][3] See also [1].

In summary, enhanced catabolism of triglyceride-rich particles and reduced secretion of VLDL underlie the hypotriglyceridemic effect of fibrates, whereas their effect on HDL metabolism is associated with changes in HDL apolipoprotein expression.[4]

Fenofibrate is a fibrate derivative, a prodrug comprising fenofibric acid linked to an isopropyl ester. It lowers lipid levels by activating peroxisome proliferator-activated receptor alpha (PPARα). PPARα activates lipoprotein lipase and reduces apoprotein CIII, which increases lipolysis and elimination of triglyceride-rich particles from plasma.[4] See Peroxisome Proliferator-Activated Receptors and Lipoprotein Lipase (LPL) complexed with GPIHBP1.

PPARα also increases apoproteins AI and AII, reduces VLDL- and LDL-containing apoprotein B, and increases HDL-containing apoprotein AI and AII.

(6lx4).

. Water molecules are shown as red spheres.

Treatments:Hypercholeseterolemia

HMG-CoA Reductase Inhibitors (Statins)
Niemann-Pick C1-like 1 (NPC1L1) protein blocker

Fenofibrate

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ReferencesReferences

  1. 1.0 1.1 "Fenofibric Acid/Fenofibrate Monograph for Professionals". Drugs.com. American Society of Health-System Pharmacists. Retrieved 3 March 2019.
  2. Ginsberg HN, Elam MB, Lovato LC, Crouse JR 3rd, Leiter LA, Linz P, Friedewald WT, Buse JB, Gerstein HC, Probstfield J, Grimm RH, Ismail-Beigi F, Bigger JT, Goff DC Jr, Cushman WC, Simons-Morton DG, Byington RP. Effects of combination lipid therapy in type 2 diabetes mellitus. N Engl J Med. 2010 Apr 29;362(17):1563-74. PMID:20228404 doi:10.1056/NEJMoa1001282
  3. Kim NH, Han KH, Choi J, Lee J, Kim SG. Use of fenofibrate on cardiovascular outcomes in statin users with metabolic syndrome: propensity matched cohort study. BMJ. 2019 Sep 27;366:l5125. PMID:31562117 doi:10.1136/bmj.l5125
  4. 4.0 4.1 Staels B, Dallongeville J, Auwerx J, Schoonjans K, Leitersdorf E, Fruchart JC. Mechanism of action of fibrates on lipid and lipoprotein metabolism. Circulation. 1998 Nov 10;98(19):2088-93. PMID:9808609 doi:10.1161/01.cir.98.19.2088

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Alexander Berchansky