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In pharmacology, the fibrates are a class of amphipathic carboxylic acids. They are used for a range of metabolic disorders, mainly hypercholesterolemia (high cholesterol), and are therefore hypolipidemic agents.
Additional recommended knowledge
Fibrates prescribed commonly are:
Although less effective in lowering LDL, fibrates improve HDL and triglyceride levels (i.e. increase HDL levels and decrease triglyceride levels), and seem to improve insulin resistance when the dyslipidemia is associated with other features of Syndrome X (hypertension and diabetes mellitus type 2).
Fibrates are agonists of the PPARalpha receptor in muscle, liver, and other tissues. Activation of PPARalpha signaling results in:
Most fibrates can cause mild stomach upset and myopathy (muscle pain with CPK elevations).
In combination with statin drugs, fibrates cause an increased risk of rhabdomyolysis (idiosyncratic destruction of muscle tissue, leading to renal failure). A powerful statin drug, cerivastatin (Lipobay®), was withdrawn because of this complication. The less lipophilic statins are less prone to cause this reaction, and are probably safer when combined with fibrates.
Although used clinically since the early 1970s, the mechanism of action of fibrates remained unelucidated until, in the 1990s, it was discovered that fibrates activate PPAR (peroxisome proliferator-activated receptors), especially PPARα. The PPARs are a class of intracellular receptors that modulate carbohydrate, fat metabolism and adipose tissue differentiation.
Activation of PPARs causes transcription of a number of genes on the DNA that facilitate lipid metabolism.
|This article is licensed under the GNU Free Documentation License. It uses material from the Wikipedia article "Fibrate". A list of authors is available in Wikipedia.|