The pharmacokinetics and pharmacodynamics of agents proven to raise high-density lipoprotein cholesterol.
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.
Piepho
R W
RW
School of Pharmacy, University of Missouri-Kansas City, 64110-2499, USA.
D001682:Biological Availability; D002784:Cholesterol / Q000096:biosynthesis*; D008076:Cholesterol, HDL / Q000097:blood*; D003084:Colestipol / Q000494:pharmacology; D004347:Drug Interactions; D006801:Humans; D019161:Hydroxymethylglutaryl-CoA Reductase Inhibitors / Q000378:metabolism / Q000493:pharmacokinetics / Q000494:pharmacology*; D000960:Hypolipidemic Agents / Q000494:pharmacology; D008099:Liver / Q000187:drug effects* / Q000378:metabolism; D009525:Niacin / Q000378:metabolism / Q000493:pharmacokinetics / Q000494:pharmacology*
D008076:Cholesterol, HDL; D019161:Hydroxymethylglutaryl-CoA Reductase Inhibitors; D000960:Hypolipidemic Agents; D009525:Niacin; D002784:Cholesterol; D003084:Colestipol