Synthetic statins

Apr 8th, 2015
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Study guide on synthetic statins

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SYNTHETICSTATINS.These statins are the most effective and best-toleratedagentsfor treating dyslipidemia.SYNTHETICSTATINS. They are competitive inhibitors of 3-hydroxy-3A.K.A TYPE TWO STATINS.methylglutaryl coenzyme A (HMG-CoA) reductase.EXAMPLES OF SYTHETIC STATINS.AtorvastatinRosuvastatinFluvastatinCeruvastatinThis are structurally distinct synthetic compounds,fluvastatin, atorvastatin, rosuvastatin are fluorinecontaining congeners that are active as they are givenPHARMACOKINETICS.Absorption, Distribution, Metabolism, and Excretion ABSORPTION: After oral administration, intestinalabsorption of the statins varies between 30% and 85%.with the exception of fluvastatin, which is almostcompletely absorbed DISTRIBUTION: Due to extensive first-pass hepaticuptake, systemic bioavailability of the statins and theirhepatic metabolites varies between 5% and 30% ofadministered doses In the plasma, >95% of synthetic statins and theirmetabolites are protein bound After oral dosing, plasma concentrations of statins peak in14 hours. Plasma half-lives of these drugs range from 1 hour to 3hours except for atorvastatin, which has a half-life of 14hours, and rosuvastatin, 19 hours which may contributeto their greater cholesterol-lowering efficacyPHARMACOKINETICS.Absorption, Distribution, Metabolism, and Excretion METABOLISM: The catabolism of atorvastatinproceeds chiefly through CYP3A4, whereas that offlu

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