The clinical relevance of omega-3 fatty acids in the management of hypertriglyceridemia

Lipids in Health and Disease

Review

Julia Catini¹  Deborah Anzalone¹  James Backes²  Daniel Hilleman³ 

[1] AstraZeneca, Wilmington, DE, USA;Atherosclerosis and LDL-Apheresis Center, School of Pharmacy, University of Kansas, 3901 Rainbow Boulevard, 66160, Kansas City, KS, USA;Creighton University, Omaha, NE, USA;

关键词: Docosahexaenoic acid;    Docosapentaenoic acid;    Eicosapentaenoic acid;    Hypertriglyceridemia;    Omega-3 fatty acids;   

DOI  :  10.1186/s12944-016-0286-4

 received in 2016-03-05, accepted in 2016-07-08,  发布年份 2016

来源: Springer

【 摘 要 】

Hypertriglyceridemia (triglycerides > 150 mg/dL) affects ~25 % of the United States (US) population and is associated with increased cardiovascular risk. Severe hypertriglyceridemia (≥ 500 mg/dL) is also a risk factor for pancreatitis. Three omega-3 fatty acid (OM3FA) prescription formulations are approved in the US for the treatment of adults with severe hypertriglyceridemia: (1) OM3FA ethyl esters (OM3EE), a mixture of OM3FA ethyl esters, primarily eicosapentaenoic acid (EPA) and docosahexaenoic acid (DHA) (Lovaza®, Omtryg™, and generics); (2) icosapent ethyl (IPE), EPA ethyl esters (Vascepa®); and (3) omega-3 carboxylic acids (OM3CA), a mixture of OM3FAs in free fatty acid form, primarily EPA, DHA, and docosapentaenoic acid (Epanova®). At approved doses, all formulations substantially reduce triglyceride and very-low-density lipoprotein levels. DHA-containing formulations may also increase low-density lipoprotein cholesterol. However, this is not accompanied by increased non-high-density lipoprotein cholesterol, which is thought to provide a better indication of cardiovascular risk in this patient population. Proposed mechanisms of action of OM3FAs include inhibition of diacylglycerol acyltransferase, increased plasma lipoprotein lipase activity, decreased hepatic lipogenesis, and increased hepatic β-oxidation. OM3CA bioavailability (area under the plasma concentration-time curve from zero to the last measurable concentration) is up to 4-fold greater than that of OM3FA ethyl esters, and unlike ethyl esters, the absorption of OM3CA is not dependent on pancreatic lipase hydrolysis. All three formulations are well tolerated (the most common adverse events are gastrointestinal) and demonstrate a lack of drug-drug interactions with other lipid-lowering drugs, such as statins and fibrates. OM3FAs appear to be an effective treatment option for patients with severe hypertriglyceridemia.

【 授权许可】

CC BY   
© The Author(s). 2016