Vascepa (icosapent ethyl)
Antihyperlipidemic-eicosapentaenoic acid (EPA) derivatives Oral Capsule
Last reviewed · Source: First Databank (FDB) drug data
Overview
Icosapent ethyl, an ethyl ester of the omega-3 fatty acid eicosapentaenoic acid (EPA), is an antilipemic agent.
Icosapent ethyl is a purified preparation of eicosapentaenoic acid (EPA), an omega-3 fatty acid. EPA is a long-chain, polyunsaturated fatty acid (PUFA) that is obtained mainly from marine sources such as fatty fish (e.g., herring, mackerel, salmon, sardines, tuna). Icosapent ethyl is commercially available in the US as a prescription drug.
Each 1-g capsule of icosapent ethyl contains 1 g of a highly purified (at least 96%), esterified form of the omega-3 fatty acid EPA; icosapent ethyl does not contain docosahexaenoic acid (DHA).
The mechanism by which EPA and other omega-3 fatty acids reduce triglyceride concentrations is not completely understood; however, studies suggest that EPA reduces hepatic synthesis and/or secretion of very low-density lipoprotein (VLDL)-triglycerides and enhances triglyceride clearance from circulating VLDL particles. Omega-3 fatty acids may reduce the synthesis of VLDL-triglycerides or triglycerides by reducing the amount of substrate (fatty acids) available for triglyceride formation (i.e., by increasing beta-oxidation, decreasing delivery of free fatty acid to the liver, decreasing hepatic lipogenesis, increasing phospholipid synthesis, and/or inhibiting hormone-sensitive lipase in adipose tissue). In addition to reducing the amount of substrate available for triglyceride formation, omega-3 fatty acids may reduce triglyceride synthesis by limiting activity of key triglyceride-synthesizing enzymes (e.g., diacylglycerol O-acyltransferase, phosphatidate phosphatase).
Omega-3 fatty acids may enhance activity of lipoprotein lipase in peripheral adipose tissue, resulting in increased peripheral conversion of VLDL particles to LDL particles.
The mechanism of action of icosapent ethyl in reducing the risk of atherosclerotic cardiovascular disease (ASCVD) is not clear, but is likely to be multifactorial. The relatively modest effects of the drug on triglyceride concentrations and other atherogenic lipoproteins observed in clinical studies suggest that the cardiovascular benefits are attributed in part to other potential mechanisms (e.g., membrane stabilizing effects; anti-inflammatory, antithrombotic, or antiarrhythmic effects; reduction in coronary plaque progression).
Following oral administration, icosapent ethyl is de-esterified during absorption; the active metabolite, EPA, is absorbed in the small intestine and enters systemic circulation mainly by the thoracic duct lymphatic system. The majority of EPA circulating in plasma is incorporated in phospholipids, triglycerides, and cholesteryl esters, and less than 1% is present as the unesterified fatty acid. EPA is mainly metabolized in the liver by beta-oxidation similar to dietary fatty acids.
Cytochrome P-450 (CYP) isoenzymes play a minor role in the metabolism of EPA. The plasma elimination half-life of EPA is approximately 89 hours. Icosapent ethyl is not renally excreted.
USES: Icosapent ethyl is used along with certain other cholesterol medications ("statins" such as atorvastatin, simvastatin) to reduce the risk of heart attack, stroke, and certain types of heart problems that require treatment in a hospital. It is also used along with a proper diet to help lower fats (triglycerides) in the blood. Icosapent ethyl is a type of omega-3 fatty acid, a fat found in fish oil.
It is thought to work by decreasing the amount of triglycerides made by the body. In addition to eating a proper diet (such as a low-cholesterol/low-fat diet), other lifestyle changes that may help this medication work better include exercising, losing weight if overweight, and stopping smoking. Consult your doctor for more details.
Generic name: icosapent ethyl
Pronunciation: (eye-KOE-sa-pent ETH-il)
Drug class: Antihyperlipidemic-eicosapentaenoic acid (EPA) derivatives
Therapeutic class: Cardiovascular Therapy Agents
Reference product & biosimilars
No reference, biosimilar or interchangeable associated with this drug.
Today’s intelligence on Vascepa
Indications
The following indications are listed for Vascepa:
- Hypertriglyceridemia
Also known as: Abnormally Increased Triglycerides In The Blood, Elevated Triglyceride Level, Increased Triglyceride Levels.
Dosing
No dosing information is available for this tab.
Icosapent ethyl is administered orally twice daily with food. In clinical studies, icosapent ethyl was administered with or following a meal; food effect studies have not been performed.
Icosapent ethyl capsules should be swallowed whole and should not be broken, crushed, dissolved, or chewed.
| Drug label | Dosing type | Instructions |
|---|---|---|
| Vascepa 1 Gm Capsule | Maintenance | Take 2 capsules (2 gram) by oral route 2 times per day with food swallowing whole. Do not chew, open, dissolve and/or crush. |
| Vascepa 0.5 Gm Capsule | Maintenance | Take 4 capsules (2 gram) by oral route 2 times per day with food swallowing whole. Do not chew, open, dissolve and/or crush. |
| Vascepa 1 Gram Capsule | Maintenance | Take 2 capsules (2 gram) by oral route 2 times per day with food swallowing whole. Do not chew, open, dissolve and/or crush. |
| Drug label | Dosing type | Instructions |
|---|---|---|
| Icosapent Ethyl 1 Gram Capsule | Maintenance | Take 2 capsules (2 gram) by oral route 2 times per day with food swallowing whole. Do not chew, open, dissolve and/or crush. |
| Icosapent Ethyl 0.5 Gm Capsule | Maintenance | Take 4 capsules (2 gram) by oral route 2 times per day with food swallowing whole. Do not chew, open, dissolve and/or crush. |
| Icosapent Ethyl 500 Mg Capsule | Maintenance | Take 4 capsules (2 gram) by oral route 2 times per day with food swallowing whole. Do not chew, open, dissolve and/or crush. |
Drug interactions
Cytochrome P-450 (CYP) isoenzymes play a minor role in the metabolism of eicosapentaenoic acid (EPA).
There are no contraindication interactions for this drug.
There are no severe interactions for this drug.
Moderate Interaction: Assess the risk to the patient and take action as needed.
Icosapent Ethyl/Anticoagulant;Antiplatelet;Thrombolytic
SEVERITY LEVEL: 3-Moderate Interaction: Assess the risk to the patient and take action as needed.
MECHANISM OF ACTION: In vitro data suggests that fish oils can competitively inhibit cyclooxygenase which decreases synthesis of thromboxane A1 leading to a decrease in platelet aggregation.(1)
CLINICAL EFFECTS: Concurrent use of anticoagulant, antiplatelet, or thrombolytic agents increase bleeding risks.
PREDISPOSING FACTORS: The risk for bleeding episodes may be greater in patients with disease-associated factors (e.g. thrombocytopenia). Drug associated risk factors include concurrent use of multiple drugs which inhibit anticoagulant/antiplatelet metabolism and/or have an inherent risk for bleeding (e.g. NSAIDs).
PATIENT MANAGEMENT: If concurrent therapy is deemed medically necessary, monitor patients receiving concurrent therapy for signs of blood loss, including decreased hemoglobin, hematocrit, fecal occult blood, and/or decreased blood pressure and promptly evaluate patients with any symptoms. When applicable, perform agent-specific laboratory tests (e.g. INR, aPTT) to monitor efficacy and safety of anticoagulation. Discontinue anticoagulation in patients with active pathologic bleeding. Instruct patients to report any signs and symptoms of bleeding, such as unusual bleeding from the gums or nose; unusual bruising; red or black, tarry stools; red, pink or dark brown urine; acute abdominal or joint pain and/or swelling. The time of highest risk for a coumarin-type drug interaction is when the precipitant drug is initiated or discontinued. Contact the prescriber before initiating, altering the dose or discontinuing either drug.
DISCUSSION: Specific studies with icosapent ethyl and affects on bleeding risk have not been conducted. Concurrent use of anticoagulant, antiplatelet, or thrombolytic agents may increase bleeding risks by impairing platelet function and prolonging bleeding time.(1) Several case reports have shown increased bleeding time and an increased risk of adverse effects from concurrent therapy.(2,3,4) A randomized placebo controlled study of 40 people taking omega-3 fatty acids and oral anticoagulants showed a significant prolongation in bleeding time.(5)
Contraindications
*Known hypersensitivity (e.g., anaphylactic reaction) to icosapent ethyl or any ingredient in the formulation.
There are no contraindication contraindications for this drug.
- Atrial fibrillation
- Increased risk of bleeding
- Disease of liver
Adverse reactions
Adverse effects reported in patients receiving icosapent ethyl and occurring more frequently than with placebo in hypertriglyceridemia trials include arthralgia and oropharyngeal pain.
Adverse effects reported in >=3% of patients receiving icosapent ethyl and occurring more frequently than with placebo in the cardiovascular outcomes trial (REDUCE-IT) include musculoskeletal pain, peripheral edema, constipation, gout, and atrial fibrillation.
More Frequent
- Atrial fibrillation
- Gout
Less Frequent
- Hemorrhage
Rare or Very Rare
- Atrial flutter
More Frequent
- Musculoskeletal pain
- Pain in oropharynx
- Peripheral edema
Less Frequent
- Arthralgia
Rare or Very Rare
- Acute abdominal pain
- Diarrhea
- Pain
Precautions
No enhanced messaging available.
Safety and efficacy of icosapent ethyl have not been established in pediatric patients.
Available data are insufficient to identify a drug-associated risk of major birth defects, miscarriage or adverse maternal or fetal outcomes with the use of icosapent ethyl in pregnant women.
In animal reproduction studies in pregnant rats, minor developmental findings were observed following oral administration of icosapent ethyl during organogenesis at exposures equivalent to that in humans at a dosage of 4 g daily. No clinically relevant adverse developmental effects were observed when icosapent ethyl was administered orally to pregnant rabbits at exposures 5 times the human exposure at the maximum dosage of 4 g daily.
Omega-3 fatty acids, including EPA, have been detected in human milk. Higher levels of omega-3 fatty acids have been observed in the milk of lactating women receiving omega-3 fatty acid supplementation. There are no data on the effects of omega-3 fatty acid ethyl esters on the breast-fed infant or on milk production.
Consider the developmental and health benefits of breast-feeding along with the mother's clinical need for icosapent ethyl and any potential adverse effects on the breast-fed child from icosapent ethyl or from the underlying maternal condition.
In clinical studies of icosapent ethyl, approximately 45% of patients were >=65 years of age. No overall differences in safety or efficacy were observed between geriatric and younger adults, and other reported clinical experience has not revealed age-related differences in response.
ICD codes
| Code | Type | Description |
|---|---|---|
| Hypertriglyceridemia | ||
| E78.1 | ICD10CM | Pure hyperglyceridemia |
| E78.2 | ICD10CM | Mixed hyperlipidemia |
ICD code information from First Databank (FDB).
Formulary status
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Last reviewed · Source: First Databank (FDB) drug data
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