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Lipid Metabolism
Lipid Triad-Role of PPARα Activation in Lipid Metabolism
Lipid Metabolism (1)
TriCor® ( fenofibrate tablets) Mechanism of Action (2)
- Fenofibric acid, the metabolite of fenofibrate, activates
peroxisome proliferator-activated receptor α (PPARα).
- Fenofibrate increases lipolysis and elimination of TG-rich
particles from plasma by activating lipoprotein lipase and reducing
production of apoprotein C-III (an inhibitor of lipoprotein lipase
activity).*
- The resulting fall in TG produces an alteration in the size
and composition of LDL from small dense particles (which are thought
to be atherogenic due to their susceptibility to oxidation) to large
buoyant particles. Large buoyant particles have a greater affinity
for cholesterol receptors and are catabolized rapidly.*
- In types IIa and IIb hyperlipidemia, LDL-C decreases; in
type IV hyperlipidemia, LDL-C often increases
- Activation of PPARα also induces an increase in the
synthesis of apoproteins A-I and A-II, and
HDL-C.*
- Fenofibrate also reduces serum uric acid levels in
hyperuricemic and normal individuals by increasing the urinary
excretion of uric acid.
*Based on in vitro data and in vivo animal studies.
References
- Adapted from Witztum JL. In: Hardman JG, Limbird LE,
Monlinoff PB, Ruddon RW, Gilman AG, eds. Goodman & Gilman's The
Pharmacological Basis of Therapeutics. 9th ed. New York, NY:
McGraw-Hill; 1996:876-878.
- TriCor tablets package insert, Abbott Laboratories.
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