Pharmacology: Pharmacodynamics: Omega-3 fatty acids (predominantly EPA and DHA) can reduce hepatic very-low density lipoprotein triglyceride (VLDL-TG) synthesis/secretion and enhances triglyceride clearance from circulating VLDL particles. They may equally accelerate chylomicron triglyceride clearance by promoting increased lipoprotein lipase activity. They also have anti-inflammatory, anti-thrombotic and immunomodulatory actions.
Pharmacokinetics: Eicosapentaenoic acid (EPA) and Docosahexaenoic acid (DHA)-laden triacylglycerols, following ingestion, undergo hydrolysis via lipases to form monoglycerides and free fatty acids. In the enterocytes, reacylation takes place reforming triacylglycerols, which are then assembled with phospholipids, cholesterol and apoproteins into chylomicrons. The chylomicrons are released into the lymphatics from whence they are transported to the systemic circulation. In the circulation, the chylomicrons are degraded by lipoprotein lipase, and EPA and DHA are transported by the circulation to various tissues of the body where they are used mainly for the synthesis of phospholipids. These phospholipids are incorporated into the cell membranes of the red blood cell, platelets and CNS cells among others. EPA and DHA are mainly found in the phospholipid components of the cell membranes. DHA is taken up by the brain in preference to other fatty acids. DHA can partially reconvert to DHA, which can partially retroconvert to EPA, and EPA may partially convert to DHA. Enteral absorption of EPA and DHA is at least as good from semi-synthetic ethyl esters as it is from the natural forms.