OMACOR
Clinical safety rating
cautionComprehensive clinical and safety monograph for OMACOR (OMACOR).
Comprehensive clinical and safety monograph for OMACOR (OMACOR).
FDA: Adjunct to diet for reduction of triglyceride levels in adult patients with severe hypertriglyceridemia (≥500 mg/dL).Off-label: Secondary prevention of cardiovascular events in patients with hypertriglyceridemia or high cardiovascular risk.
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. |
| Molecular Weight | 882.21 |
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 | Avoid unless benefit clearly outweighs risk; use only if essential for maternal triglyceride reduction. |
| 2nd trimester | Use only if necessary; limited data, potential for bleeding complications due to antiplatelet effect. |
| 3rd trimester | Use with caution; may increase risk of postpartum hemorrhage due to antithrombotic properties. |
Clinical note
Comprehensive clinical and safety monograph for OMACOR (OMACOR).
| Placental transfer | Omega-3 fatty acids cross the placenta; documented transfer in humans. |
| Breastfeeding | Omega-3-acid ethyl esters are excreted into human milk in low amounts; likely compatible with breastfeeding. Monitor infant for potential bleeding if high doses used. |
| Lactation Rating | L2 (Safer) |
| 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. |
| 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. |
■ FDA Black Box Warning
No FDA black box warning.
| Serious Effects |
Hypersensitivity to omega-3-acid ethyl esters or any componentExogenous hypertriglyceridemia (chylomicronemia syndrome)
| 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). |
| Food/Dietary | Avoid high-fat meals as they may increase triglyceride levels. No specific food interactions known, but consistency in timing with meals is recommended. |
| Clinical Pearls | Omacor (omega-3-acid ethyl esters) is indicated as an adjunct to diet for severe hypertriglyceridemia (≥500 mg/dL). Monitor LDL-C levels as they may increase during therapy; adjust statin dose if needed. Administer with meals to enhance absorption and reduce gastrointestinal side effects. Avoid use in patients with fish or shellfish allergy. May prolong bleeding time; monitor in patients on anticoagulants. |
| Patient Advice | Take with food to improve absorption and reduce burping or fishy taste. · Do not take if you have an allergy to fish or shellfish. · Report unusual bleeding or bruising, especially if you are on blood thinners. · Do not substitute with over-the-counter fish oil supplements as they are not equivalent. · Continue dietary modifications and exercise as part of your treatment plan. |
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