title: Gemfibrozil in Combination with Statins-Is It Really Contraindicated?
abstract: Gemfibrozil is a lipid-modifying agent that belongs to the fibric acid derivative class. Fibric acid derivatives activate peroxisome proliferator activated receptor α (PPAR-α). The primary role of these agents in clinical practice is for the management of hypertriglyceridemia. Triglycerides may be reduced by as much as 74 % in some patients. In addition to lowering triglycerides, these agents can also decrease very low-density lipoprotein cholesterol (VLDL-C) and low-density lipoprotein cholesterol (LDL-C) as well as raise high-density lipoprotein cholesterol (HDL-C). Based on the 2013 ACC/AHA Guideline on the Treatment of Blood Cholesterol to Reduce Atherosclerotic Cardiovascular Risk in Adults and the National Lipid Association, pharmacologic therapy to reduce triglycerides should be considered when triglyceride levels are ≥500 mg/dL. While the use of gemfibrozil has decreased over the years for a variety of reasons, muscle-associated adverse effects is the predominant reason and the one that is most clinically relevant. However, despite these concerns, there are situations in which the use of gemfibrozil in combination with a statin may be necessary. Understanding the metabolism of gemfibrozil and the degree of interaction with the various statins will assist health-care providers to optimize safety when this combination is clinically indicated.
authors.affiliation: Department of Pharmacy Services, Medical University of South Carolina, 25 Courtenay Drive, MSC 584, Charleston, SC, USA. wiggib@musc.edu.
authors.forename: Barbara S
authors.initials: BS
authors.lastname: Wiggins
authors.affiliation: Skaggs School of Pharmacy and Pharmaceutical Sciences, Department of Clinical Pharmacy, University of Colorado Anschutz Medical Campus, Aurora, CO, USA.|School of Medicine, Department of Family Medicine, University of Colorado Anschutz Medical Campus, Aurora, CO, USA.
authors.forename: Joseph J
authors.initials: JJ
authors.lastname: Saseen
authors.affiliation: School of Medicine, Department of Medicine Charleston, Medical University of South Carolina, Charleston, SC, USA.
authors.forename: Pamela B
authors.initials: PB
authors.lastname: Morris
mesh_terms: D002318:Cardiovascular Diseases / Q000188:drug therapy; D004338:Drug Combinations; D015248:Gemfibrozil / Q000627:therapeutic use*; D006801:Humans; D019161:Hydroxymethylglutaryl-CoA Reductase Inhibitors / Q000627:therapeutic use*; D000960:Hypolipidemic Agents / Q000627:therapeutic use*; D012307:Risk Factors
chemical_list: D004338:Drug Combinations; D019161:Hydroxymethylglutaryl-CoA Reductase Inhibitors; D000960:Hypolipidemic Agents; D015248:Gemfibrozil
keywords: Gemfibrozil; Muscle toxicity; Organic anion-transporting polypeptide; PPAR alpha; Statins