PHAR 441 Lecture Notes - Lecture 10: Hmg-Coa Reductase, Low-Density Lipoprotein, Ezetimibe
10 Dec 2016
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Learning objectives: understand the moa of lipid lowering drugs, describe the most common adrs. 1st line tx for hypercholesterolemia most effective with fewer adrs. Effect: inhibition of intracellular cholesterol synthesis in the liver = ldl-r expression on hepatocytes = ldl extraction from plasma. In isoprenylated proteins that are known to activate rho (rho appears to be a common component for the pathogenesis of vascular disorders) Ldl-r also = uptake of vldl remnants (idl) Does not affect pts who lack genes necessary to make ldl-rs. Ldl by 18-55% rosuva and atorva have the most effect on. Rosuva, fluva = cyp2c9 interacts with 2c9 drugs = warfarin (fluva and rosuva warfarin monitor inr) Atorva, lova, simva cyp3a4 grapefruit juice (>1l/day) inhibits 3a4 = [statin] = adrs: oxidative stress = endothelial function, inflammatory response at plaque site, deg(cid:396)adatio(cid:374) of ecm = plaque stability, platelet aggregation = risk of thrombosis. Metabolized in the liver (except for prava is metabolized in the stomach, excreted renally)
