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The pharmacokinetics and pharmacodynamics of agents proven to raise high-density lipoprotein cholesterol

  • Robert W Piepho
    Correspondence
    Address for reprints: Robert W. Piepho, PhD, University of Missouri-Kansas City School of Pharmacy, 5005 Rockhill Road, KPB, Room 101, Kansas City, Missouri 64110-2499
    Affiliations
    School of Pharmacy, University of Missouri-Kansas City, Kansas City, Missouri, USA
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      Abstract

      Bile acid sequestrants, fibric acid derivatives (fibrates), hydroxy-methylglutaryl coenzyme A (HMG CoA) reductase inhibitors (“statins”), and niacin are able to increase HDL-C serum concentrations to varying degrees. Bile acid sequestrants are the least effective, whereas niacin is the most powerful agent for increasing HDL-C levels. Because of 2 alternate metabolic pathways of niacin breakdown, flushing or hepatotoxicity can occur in patients taking niacin. These effects can be mediated in a carefully designed formulation of niacin that releases the drug at a predictable rate. Niacin has few drug interactions and is a relatively inexpensive means of increasing HDL-C. A combination formulation that combines niacin plus a statin has shown promise in ongoing clinical trials.
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