icosapent (Rx)

1-10%

Arthralgia (2.3%)

Frequency Not Defined

Oropharyngeal pain

Contraindications

Hypersensitivity to drug or any of its components

Cautions

Lipid levels should be assessed prior to initiating therapy

Identify other potential causes of hypertriglyceridemia (eg, hypothyroidism, diabetes mellitus, alcohol intake, medications) and provide appropriate treatment as necessary

Medications such as estrogens, beta blockers and thiazides have been shown to exacerbate hypertriglyceridemia; discontinue or change medications if possible, otherwise monitor carefully

Prior to therapy, patients must start on a healthy regimen that includes an appropriate lipid-lowering diet and exercise, and this must be continued during treatment

Effect on the risk for pancreatitis in patients with severe hypertriglyceridemia has not been determined

Effect on cardiovascular mortality and morbidity in patients with severe hypertriglyceridemia has not been determined

Monitor ALT and AST levels periodically in patients with hepatic impairment

Contains ethyl esters of the omega-3 fatty acid, eicosapentaenoic acid (EPA) obtained from fish oil; caution in patients with known hypersensitivity to fish and/or shellfish

Omega-3 fatty acids may cause prolongation of bleeding time; monitor patients receiving concomitant anticoagulants/ anti-platelet therapy periodically

Pregnancy Category: C

Lactation: Omega-3-acid ethyl esters excreted in human breast milk; effects unknown, exercise caution

Pregnancy Categories

A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

NA: Information not available.

Mechanism of Action

Ethyl ester of eicosapentaenoic acid (EPA); EPA has been shown to reduce hepatic very low-density lipoprotein triglycerides (VLDL-TG) synthesis and/or secretion; enhances triglyceride clearance from circulating VLDL particle; may also increase beta-oxidation, inhibits acyl-CoA:1,2-diacylglycerol acyltransferase (DGAT), decrease lipogenesis in liver, and increase plasma lipoprotein lipase activity

Absorption

De-esterified during absorption to active EPA that is absorbed in small intestine

Peak Plasma Time: 5 hr

Distribution

Protein Bound: >99% of unesterified EPA

Vd: 88 L

Metabolism

Mainly metabolized by the liver via beta-oxidation similar to dietary fatty acids; minor CYP450 mediated metabolism

Elimination

Half-life: 89 hr

Does not undergo renal excretion

Total plasma clearance: 684 mL/hr