OMACOR
Clinical safety rating: caution
Comprehensive clinical and safety monograph for OMACOR (OMACOR).
Omega-3-acid ethyl esters (EPA and DHA) reduce hepatic triglyceride synthesis by inhibiting acyl-CoA:1,2-diacylglycerol acyltransferase and increasing beta-oxidation. They also decrease very-low-density lipoprotein (VLDL) secretion and enhance triglyceride clearance from circulating VLDL particles.
| Metabolism | Omega-3-acid ethyl esters are primarily hydrolyzed by pancreatic lipase to free fatty acids (EPA and DHA), which are then absorbed and incorporated into chylomicrons. They undergo hepatic metabolism via beta-oxidation. CYP450 involvement is minimal. |
| Excretion | Primarily fecal as unchanged drug and metabolites; <5% renal. Biliary excretion accounts for ~90% of elimination via feces, with minimal urinary excretion (0.5–2%). |
| Half-life | Terminal elimination half-life: ~55–75 hours for EPA and DHA (beta-phase). Clinical context: steady-state achieved after 4–8 weeks; half-life supports once-daily dosing. |
| Protein binding | Highly protein-bound (>99%) primarily to albumin. |
| Volume of Distribution | Vd: ~0.2–0.3 L/kg (EPA), ~2–3 L/kg (DHA). Clinical meaning: extensive tissue distribution, especially in adipose and cardiac tissues. |
| Bioavailability | Oral: 50–100% (enhanced with fatty meal; absolute bioavailability not determined). |
| Onset of Action | Oral: clinical effect (triglyceride reduction) observed after 2–4 weeks; maximal effect by 8–12 weeks. |
| Duration of Action | Duration: Up to 12 weeks after discontinuation for triglyceride-lowering effect to revert to baseline. Clinical note: effects persist proportional to plasma omega-3 levels. |
4 g orally once daily or 2 g orally twice daily, taken with meals. Each capsule contains 1 g of omega-3-acid ethyl esters (approximately 465 mg eicosapentaenoic acid and 375 mg docosahexaenoic acid).
| Dosage form | CAPSULE |
| Renal impairment | No dose adjustment required for any degree of renal impairment. Use caution in patients with renal disease due to potential for increased bleeding risk. |
| Liver impairment | Contraindicated in patients with Child-Pugh class C (severe) hepatic impairment. For Child-Pugh A or B, no dose adjustment is recommended, but monitor liver function tests periodically. |
| Pediatric use | Safety and efficacy not established in pediatric patients. Not recommended for use in children. |
| Geriatric use | No specific dose adjustment recommended. Monitor for potential drug interactions, especially with anticoagulants, due to increased bleeding risk. Start at lower end of dosing range if elderly patient has significant comorbidity or polypharmacy. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for OMACOR (OMACOR).
| Breastfeeding | Not recommended during breastfeeding. Omega-3 fatty acids are excreted in human milk; M/P ratio not established. Potential for adverse effects in nursing infant. Consider alternative treatment or discontinue nursing. |
| Teratogenic Risk | FDA Pregnancy Category C. No evidence of teratogenicity in animal studies at doses up to 10 times the human dose. There are no adequate and well-controlled studies in pregnant women. Use only if potential benefit justifies potential risk to fetus. Omega-3-acid ethyl esters may inhibit prostaglandin synthesis and delay labor. Third trimester use may increase risk of bleeding in mother and neonate. |
■ FDA Black Box Warning
No FDA black box warning.
| Serious Effects |
["Hypersensitivity to omega-3-acid ethyl esters or any component.","Acute pancreatitis with marked hypertriglyceridemia (consider if triglycerides >500 mg/dL and chylomicronemia)."]
| Precautions | ["Increased bleeding risk (monitor patients on anticoagulants).","Atrial fibrillation in patients with prior history or at high risk.","Persistent elevations of ALT or AST, especially with other hepatotoxic drugs.","Hypersensitivity reactions including anaphylaxis.","Fish allergy (capsules contain fish oil)."] |
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| Fetal Monitoring | Monitor serum triglycerides periodically. Assess coagulation parameters if concomitant anticoagulant use. Monitor for bleeding signs, especially in high doses. Fetal surveillance as clinically indicated. |
| Fertility Effects | No known effect on human fertility. Animal studies showed no impairment of fertility at doses up to 10 times human dose. |