OMEGA-3FATTYACIDETHYLESTERS

Absorption

Omega-3-acid ethyl esters are rapidly hydrolysed to free fatty acids in the intestinal lumen which then become incorporated into phospholipids, cholesterol, and triglycerides so determination of bioavailability by serum concentration is not possible.

Toxicity

In rats, omega-3-acid ethyl esters are not mutagenic or clastogenic and do not lead to impairment of fertility.
Safety in human pregnancy have not been performed, however an embryocidal effect was seen in rats force fed 7 times the maximum recommended human dose. The risk and benefit of treatment during pregnancy should be weighed before deciding on treatment.
Animal studies in lactating rats have shown excretion of omega-3-acid ethyl esters at concentrations 6 to 14 times higher than in the serum of the mother, however the effects of this excretion on a mother or child have not been established.
Safety and effectiveness in pediatric patients has not been established.
There appear to be no differences in the safety and efficacy in patients above or below 60 years of age based on limited data.

Indications

Omega-3-Acid Ethyl Esters capsules, USP are indicated as an adjunct to diet to reduce triglyceride (TG) levels in adult patients with severe (≥500 mg/dL) hypertriglyceridemia (HTG).

Background

Omega-3-acid ethyl esters are prescription drugs that contain eicosapentaenoic acid-ethyl ester (EPA) and docosahexaenoic acid-ethyl ester (DHA) that are used in combination with changes in diet to lower triglyceride levels in adults with severe (≥ 500 mg/dL) hypertriglyceridemia. Omega-3-acid ethyl esters are currently marketed in the US, EU, and many other regions under the brand name Lovaza.

Pharmacokinetics

Omega-3-acid ethyl esters reduce triglyceride production, increase fatty acid metabolism, inhibit the release of fatty acids, increase triglyceride clearance, and decrease production of very low density lipoprotein cholesterol(VLDL-C).

Metabolism

Omega-3-acid ethyl esters are hydrolysed to free fatty acids in the intestinal lumen by pancreatic lipase. Once in enterocytes, the free fatty acids are packaged in chylomicrons which are released from cells into the circulation. Fatty acids then enter the liver where they can be incorporated into liver stores, incorporated into lipoprotein phospholipids, or oxidised for energy.