Icosapent Ethyl 1gm Capsules

Contents

After oral administration, icosapent ethyl is de-esterified during the absorption process and the active metabolite EPA is absorbed in the small intestine and enters the systemic circulation mainly via the thoracic duct lymphatic system. Peak plasma concentrations of EPA were reached approximately 5 hours following oral doses of icosapent ethyl.

Icosapent Ethyl Capsules Prescribing Information

Medically reviewed by Drugs.com. Last updated on Oct 1, 2022.

Indications and Usage
Dosage and Administration
Dosage Forms and Strengths
Contraindications
Warnings and Precautions
Adverse Reactions/Side Effects
Drug Interactions
Use In Specific Populations
Description
Clinical Pharmacology
Nonclinical Toxicology
Clinical Studies
How Supplied/Storage and Handling
Patient Counseling Information

Indications and Usage for Icosapent Ethyl Capsules

Icosapent ethyl is indicated:

• as an adjunct to diet to reduce triglyceride (TG) levels in adult patients with severe (≥500 mg/dL) hypertriglyceridemia.

Limitations of Use

The effect of icosapent ethyl on the risk for pancreatitis in patients with severe hypertriglyceridemia has not been determined.

Icosapent Ethyl Capsules Dosage and Administration

Prior to Initiation of Icosapent Ethyl

• Assess lipid levels before initiating therapy. Identify other causes (e.g., diabetes mellitus, hypothyroidism, or medications) of high triglyceride levels and manage as appropriate. • Patients should engage in appropriate nutritional intake and physical activity before receiving icosapent ethyl, which should continue during treatment with icosapent ethyl.

Dosage and Administration

• The daily dose of icosapent ethyl is 4 grams per day taken as: o two 1 gram capsules twice daily with food. • Advise patients to swallow Icosapent Ethyl Capsules whole. Do not break open, crush, dissolve, or chew Icosapent Ethyl Capsules.

Dosage Forms and Strengths

Icosapent Ethyl Capsules are supplied as a 1 gram, clear, oblong capsule with product identification “54 648” on one side.

Related/similar drugs

Contraindications

Icosapent ethyl is contraindicated in patients with known hypersensitivity (e.g., anaphylactic reaction) to icosapent ethyl or any of its components.

Warnings and Precautions

Atrial Fibrillation/Flutter

Icosapent ethyl is associated with an increased risk of atrial fibrillation or atrial flutter requiring hospitalization. In a double-blind, placebo-controlled trial of 8,179 subjects, adjudicated atrial fibrillation or atrial flutter requiring hospitalization for 24 or more hours occurred in 127 (3%) patients treated with icosapent ethyl compared to 84 (2%) patients receiving placebo [HR= 1.5 (95% CI 1.14, 1.98)]. The incidence of atrial fibrillation was greater in patients with a previous history of atrial fibrillation or atrial flutter.

Potential for Allergic Reactions in Patients with Fish Allergy

Icosapent ethyl contains ethyl esters of the omega-3 fatty acid, eicosapentaenoic acid (EPA), obtained from the oil of fish. It is not known whether patients with allergies to fish and/or shellfish are at increased risk of an allergic reaction to icosapent ethyl. Inform patients with known hypersensitivity to fish and/or shellfish about the potential for allergic reactions to icosapent ethyl and advise them to discontinue icosapent ethyl and seek medical attention if any reactions occur.

Bleeding

Icosapent ethyl is associated with an increased risk of bleeding. In a double-blind, placebo-controlled trial of 8,179 patients, 482 (12%) patients receiving icosapent ethyl experienced a bleeding event compared to 404 (10%) patients receiving placebo. Serious bleeding events occurred in 111 (3%) of patients on icosapent ethyl vs. 85 (2%) of patients receiving placebo. The incidence of bleeding was greater in patients receiving concomitant antithrombotic medications, such as aspirin, clopidogrel, or warfarin.

Adverse Reactions

The following important adverse reactions are described below and elsewhere in the labeling:

• Atrial Fibrillation or Atrial Flutter [see Warnings and Precautions (5.1)] • Potential for Allergic Reactions in Patients with Fish Allergy [see Warnings and Precautions (5.2)] • Bleeding [see Warnings and Precautions (5.3)]

Clinical Trials Experience

Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice.

Common adverse reactions (incidence ≥3% on icosapent ethyl and ≥1% more frequent than placebo) included musculoskeletal pain, peripheral edema, constipation, gout, and atrial fibrillation.

In two randomized, double-blind, placebo-controlled trials in patients with triglyceride levels between 200 and
2000 mg/dL treated for 12 weeks, adverse reactions reported with icosapent ethyl at an incidence ≥1% more frequent than placebo based on pooled data included arthralgia and oropharyngeal pain.

Postmarketing Experience

Additional adverse reactions have been identified during post-approval use of icosapent ethyl. Because these reactions are reported voluntarily from a population of uncertain size, it is generally not possible to reliably estimate their frequency or establish a causal relationship to drug exposure.

• Diarrhea • Blood triglycerides increased • Abdominal discomfort • Pain in the extremities

Drug Interactions

Increased Bleeding Risk with Anticoagulants and Antiplatelet Agents

Some published studies with omega-3 fatty acids have demonstrated prolongation of bleeding time. The prolongation of bleeding time reported in those studies has not exceeded normal limits and did not produce clinically significant bleeding episodes. Monitor patients receiving icosapent ethyl and concomitant anticoagulants and/or antiplatelet agents for bleeding.

USE IN SPECIFIC POPULATIONS

Pregnancy

The available data from published case reports and the pharmacovigilance database on the use of icosapent ethyl in pregnant women are insufficient to identify a drug-associated risk for major birth defects, miscarriage or adverse maternal or fetal outcomes. In animal reproduction studies in pregnant rats, non-dose-related imbalances for some minor developmental findings were observed with oral administration of icosapent ethyl during organogenesis at exposures that were equivalent to the clinical exposure at the human dose of 4 g/day, based on body surface area comparisons. In a study in pregnant rabbits orally administered icosapent ethyl during organogenesis, there were no clinically relevant adverse developmental effects at exposures that were 5 times the clinical exposure, based on body surface area comparisons (see Data).

The estimated background risk of major birth defects and miscarriage for the indicated population is unknown. All pregnancies have a background risk of birth defect, loss, or other adverse outcomes. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2-4% and 15-20%, respectively.

Lactation

Published studies have detected omega-3 fatty acids, including EPA, in human milk. Lactating women receiving oral omega-3 fatty acids for supplementation have resulted in higher levels of omega-3 fatty acids in human milk. There are no data on the effects of omega-3 fatty acid ethyl esters on the breastfed infant or on milk production. The developmental and health benefits of breastfeeding should be considered along with the mother’s clinical need for icosapent ethyl and any potential adverse effects on the breastfed child from icosapent ethyl or from the underlying maternal condition.

Pediatric Use

Safety and effectiveness in pediatric patients have not been established.

Geriatric Use

Of the total number of patients in well-controlled clinical studies of icosapent ethyl, 45% were 65 years of age and over. No overall differences in safety or effectiveness were observed between these patients and younger groups. Other reported clinical experience has not identified differences in responses between the elderly and younger patients.

Hepatic Impairment

In patients with hepatic impairment, alanine aminotransferase (ALT) and aspartate aminotransferase (AST) levels should be monitored periodically during therapy with icosapent ethyl.

Icosapent Ethyl Capsules Description

Icosapent ethyl, a lipid-regulating agent, is supplied as a 1 gram, liquid-filled soft gelatin capsule for oral administration.

Icosapent ethyl is an ethyl ester of the omega-3 fatty acid eicosapentaenoic acid (EPA). The empirical formula of icosapent ethyl is C 22 H 34 O 2 and the molecular weight is 330.51. The chemical name for icosapent ethyl is ethyl all-cis-5,8,11,14,17-icosapentaenoate with the following chemical structure:

Each capsule contains the following inactive ingredients: gelatin, glycerin, purified water, sorbitol, sorbitan and tocopherol. The monogramming ink ingredients contain: ammonium hydroxide, iron oxide black, isopropyl alcohol, macrogol, polyvinyl acetate phthalate, propylene glycol, purified water and SDA alcohol (ethanol and ethyl acetate).

Icosapent Ethyl Capsules – Clinical Pharmacology

Mechanism of Action

Studies suggest that EPA reduces hepatic very low-density lipoprotein triglycerides (VLDL-TG) synthesis and/or secretion and enhances TG clearance from circulating VLDL particles. Potential mechanisms of action include increased β-oxidation; inhibition of acyl-CoA:1,2-diacylglycerol acyltransferase (DGAT); decreased lipogenesis in the liver; and increased plasma lipoprotein lipase activity.

Pharmacodynamics

In a 12-week, dose-ranging study in patients with severe hypertriglyceridemia, icosapent ethyl 4 grams per day reduced median TG from baseline relative to placebo [see Clinical Studies (14)] .

Pharmacokinetics

After oral administration, icosapent ethyl is de-esterified during the absorption process and the active metabolite EPA is absorbed in the small intestine and enters the systemic circulation mainly via the thoracic duct lymphatic system. Peak plasma concentrations of EPA were reached approximately 5 hours following oral doses of icosapent ethyl.

Icosapent ethyl was administered with or following a meal in all clinical studies; no food effect studies were performed. Take icosapent ethyl with or following a meal.

The mean volume of distribution at steady state of EPA is approximately 88 liters. The majority of EPA circulating in plasma is incorporated in phospholipids, triglycerides and cholesteryl esters, and

EPA is mainly metabolized by the liver via beta-oxidation similar to dietary fatty acids. Beta oxidation splits the long carbon chain of EPA into acetyl Coenzyme A, which is converted into energy via the Krebs cycle. Cytochrome P450-mediated metabolism is a minor pathway of elimination of EPA.

The total plasma clearance of EPA at steady state is 684 mL/hr. The plasma elimination half-life (t 1/2 ) of EPA is approximately 89 hours. Icosapent ethyl does not undergo renal excretion.

When administered icosapent ethyl in clinical trials, plasma total EPA concentrations did not differ significantly between men and women.

The pharmacokinetics of icosapent ethyl has not been studied in pediatric patients.

Hepatic or Renal Impairment

Icosapent ethyl has not been studied in patients with renal or hepatic impairment.

Drug Interaction Studies

Omeprazole: In a drug-drug interaction study with 28 healthy adult subjects, icosapent ethyl 4 g/day at steady-state did not significantly change the steady-state AUC τ or C max of omeprazole when co-administered at 40 mg/day to steady-state.

Rosiglitazone: In a drug-drug interaction study with 28 healthy adult subjects, icosapent ethyl 4 g/day at steady-state did not significantly change the single dose AUC or C max of rosiglitazone at 8 mg.

Warfarin: In a drug-drug interaction study with 25 healthy adult subjects, icosapent ethyl 4 g/day at steady-state did not significantly change the single dose AUC or C max of R – and S -warfarin or the anti-coagulation pharmacodynamics of warfarin when co-administered as racemic warfarin at 25 mg.

Atorvastatin: In a drug-drug interaction study of 26 healthy adult subjects, icosapent ethyl 4 g/day at steady-state did not significantly change the steady-state AUC τ or C max of atorvastatin, 2-hydroxyatorvastatin, or 4-hydroxyatorvastatin when co-administered with atorvastatin 80 mg/day at steady-state.

Nonclinical Toxicology

Carcinogenesis, Mutagenesis, Impairment of Fertility

In a 2-year rat carcinogenicity study with oral gavage doses of 0.09, 0.27, and 0.91 g/kg/day icosapent ethyl, respectively, males did not exhibit drug-related neoplasms. Hemangiomas and hemangiosarcomas of the mesenteric lymph node, the site of drug absorption, were observed in females at clinically relevant exposures based on body surface area comparisons across species relative to the maximum clinical dose of 4 g/day. Overall incidence of hemangiomas and hemangiosarcomas in all vascular tissues did not increase with treatment.

In a 6-month carcinogenicity study in Tg.rasH2 transgenic mice with oral gavage doses of 0.5, 1, 2, and 4.6 g/kg/day icosapent ethyl, drug-related incidences of benign squamous cell papilloma in the skin and subcutis of the tail was observed in high dose male mice. The papillomas were considered to develop secondary to chronic irritation of the proximal tail associated with fecal excretion of oil and therefore not clinically relevant. Drug-related neoplasms were not observed in female mice.

Icosapent ethyl was not mutagenic with or without metabolic activation in the bacterial mutagenesis (Ames) assay or in the in vivo mouse micronucleus assay. A chromosomal aberration assay in Chinese Hamster Ovary (CHO) cells was positive for clastogenicity with and without metabolic activation.

In an oral gavage rat fertility study, ethyl-EPA, administered at doses of 0.3, 1, and 3 g/kg/day to male rats for 9 weeks before mating and to female rats for 14 days before mating through day 7 of gestation, increased anogenital distance in female pups and increased cervical ribs were observed at 3 g/kg/day (7 times human systemic exposure with 4 g/day clinical dose based on a body surface area comparison).

Clinical Studies

Severe Hypertriglyceridemia

The effects of icosapent ethyl 4 grams per day were assessed in a randomized, placebo-controlled, double-blind, parallel-group study of adult patients (76 on icosapent ethyl, 75 on placebo) with severe hypertriglyceridemia. Patients whose baseline TG levels were between 500 and 2,000 mg/dL were enrolled in this study for 12 weeks. The median baseline TG and LDL-C levels in these patients were 684 mg/dL and 86 mg/dL, respectively. Median baseline HDL-C level was 27 mg/dL. The randomized population in this study was mostly Caucasian (88%) and male (76%). The mean age was 53 years and the mean body mass index was 31 kg/m 2 . Twenty-five percent of patients were on concomitant statin therapy, 28% were diabetics, and 39% of the patients had TG levels >750 mg/dL.

The changes in the major lipoprotein lipid parameters for the groups receiving icosapent ethyl or placebo are shown in Table 2.

Table 2. Median Baseline and Percent Change from Baseline in Lipid Parameters in Patients with Severe Hypertriglyceridemia (≥500 mg/dL)

Icosapent Ethyl 4 g/day

Icosapent Ethyl Capsules

Medically reviewed by Drugs.com. Last updated on Aug 28, 2022.

Uses of Icosapent Ethyl Capsules:

It is used to lower triglycerides.
It is used with other cholesterol drugs to lower the risk of heart attack, stroke, some heart procedures, and a type of chest pain (unstable angina).
It may be given to you for other reasons. Talk with the doctor.

What do I need to tell my doctor BEFORE I take Icosapent Ethyl Capsules?

If you are allergic to this medicine (icosapent ethyl capsules); any part of this medicine (icosapent ethyl capsules); or any other drugs, foods, or substances. Tell your doctor about the allergy and what signs you had.

This medicine may interact with other drugs or health problems.

Tell your doctor and pharmacist about all of your drugs (prescription or OTC, natural products, vitamins) and health problems. You must check to make sure that it is safe for you to take this medicine (icosapent ethyl capsules) with all of your drugs and health problems. Do not start, stop, or change the dose of any drug without checking with your doctor.

What are some things I need to know or do while I take Icosapent Ethyl Capsules?

Tell all of your health care providers that you take this medicine (icosapent ethyl capsules). This includes your doctors, nurses, pharmacists, and dentists.
If you are allergic to fish, fish oil, or shellfish, talk with your doctor.
Have blood work checked as you have been told by the doctor. Talk with the doctor.
Follow the diet and workout plan that your doctor told you about.
Talk with your doctor before you drink alcohol.
Certain types of abnormal heartbeats (atrial fibrillation or atrial flutter) have happened with this medicine (icosapent ethyl capsules). These abnormal heartbeats can be severe. The risk is raised in people who have had these abnormal heartbeats in the past.
Tell your doctor if you are pregnant, plan on getting pregnant, or are breast-feeding. You will need to talk about the benefits and risks to you and the baby.

How is this medicine (Icosapent Ethyl Capsules) best taken?

Use this medicine (icosapent ethyl capsules) as ordered by your doctor. Read all information given to you. Follow all instructions closely.

Take this medicine (icosapent ethyl capsules) with food.
Swallow whole. Do not chew, break, open, or dissolve.
If you have trouble swallowing, talk with your doctor.
Keep taking this medicine (icosapent ethyl capsules) as you have been told by your doctor or other health care provider, even if you feel well.

What do I do if I miss a dose?

Take a missed dose as soon as you think about it.
If it is close to the time for your next dose, skip the missed dose and go back to your normal time.
Do not take 2 doses at the same time or extra doses.

What are some side effects that I need to call my doctor about right away?

WARNING/CAUTION: Even though it may be rare, some people may have very bad and sometimes deadly side effects when taking a drug. Tell your doctor or get medical help right away if you have any of the following signs or symptoms that may be related to a very bad side effect:

Signs of an allergic reaction, like rash; hives; itching; red, swollen, blistered, or peeling skin with or without fever; wheezing; tightness in the chest or throat; trouble breathing, swallowing, or talking; unusual hoarseness; or swelling of the mouth, face, lips, tongue, or throat.
Fast or abnormal heartbeat.
Dizziness or passing out.
Shortness of breath.
Chest pain.
Any unexplained bruising or bleeding.
Swelling in the arms or legs.

What are some other side effects of Icosapent Ethyl Capsules?

All drugs may cause side effects. However, many people have no side effects or only have minor side effects. Call your doctor or get medical help if any of these side effects or any other side effects bother you or do not go away:

Muscle or joint pain.
Constipation.
Throat pain.

These are not all of the side effects that may occur. If you have questions about side effects, call your doctor. Call your doctor for medical advice about side effects.

You may report side effects to the FDA at 1-800-332-1088. You may also report side effects at https://www.fda.gov/medwatch.

If OVERDOSE is suspected:

If you think there has been an overdose, call your poison control center or get medical care right away. Be ready to tell or show what was taken, how much, and when it happened.

How do I store and/or throw out Icosapent Ethyl Capsules?

Store at room temperature in a dry place. Do not store in a bathroom.
Keep all drugs in a safe place. Keep all drugs out of the reach of children and pets.
Throw away unused or expired drugs. Do not flush down a toilet or pour down a drain unless you are told to do so. Check with your pharmacist if you have questions about the best way to throw out drugs. There may be drug take-back programs in your area.

Consumer Information Use and Disclaimer

If your symptoms or health problems do not get better or if they become worse, call your doctor.
Do not share your drugs with others and do not take anyone else’s drugs.
Some drugs may have another patient information leaflet. Check with your pharmacist. If you have any questions about this medicine (icosapent ethyl capsules), please talk with your doctor, nurse, pharmacist, or other health care provider.
If you think there has been an overdose, call your poison control center or get medical care right away. Be ready to tell or show what was taken, how much, and when it happened.

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