Icosapent Ethyl

This medication may be prescribed for other uses; ask your doctor or pharmacist for more information.

Icosapent ethyl is a prescription medicine used to lower very high levels of triglycerides (TG) in adults. Icosapent ethyl is used along with a low-fat and low-cholesterol diet.

This medication may be prescribed for other uses. Ask your doctor or pharmacist for more information.

The most common side effect is joint pain.

This is not a complete list of icosapent ethyl side effects. For more information, ask your doctor or pharmacist.

Tell your doctor about any side effect that is bothersome or doesn't go away. You may report side effects to FDA at 1-800-FDA-1088.

Before receiving this medication, tell your doctor if you:

• have diabetes
• have a low thyroid problem (hypothyroidism)
• have liver disease
• have a pancreas problem
• are allergic to fish or shellfish. It is not known if people who are allergic to fish or shellfish are also allergic to icosapent ethyl.

Tell your doctor if you are pregnant or breastfeeding.

Tell your doctor about all the medicines you take, including prescription and non-prescription medicines, vitamins, and dietary or herbal supplements.

• Take icosapent ethyl exactly as prescribed by your doctor. Follow the directions on your prescription label carefully.
• Do not change your dose or stop taking icosapent ethyl without talking to your doctor.
• You should not take more than 4 capsules of icosapent ethyl each day. Do not take more capsules than what is prescribed by your doctor.
• Take icosapent ethyl capsules whole. Do not break, crush, dissolve, or chew icosapent ethyl capsules before swallowing.
• If you miss a dose of icosapent ethyl, take it as soon as you remember, unless it is almost time for your next dose. If you miss one day of icosapent ethyl, do not double your dose when you take it.
• Follow your doctor's recommendations for a diet that is low in saturated fat, cholesterol, carbohydrates, added sugars. Your doctor may recommend you start this diet before giving you icosapent ethyl. Stay on this diet while taking icosapent ethyl. Your healthcare provider may also recommend that you limit alcohol consumption to help lower your triglycerides.
• Your doctor may do blood tests to check your triglyceride and other lipid levels while you take icosapent ethyl.

Dyslipidemias

Adjunct to dietary therapy to reduce triglyceride concentrations in adults with severe hypertriglyceridemia (triglyceride concentration ≥500 mg/dL).1 Effect on risk of pancreatitis or on cardiovascular morbidity or mortality in these patients not established.1

Has been used to reduce residually high (200–499 mg/dL) triglyceride concentrations† in statin-treated adults at high risk for cardiovascular disease despite adequately controlled LDL-cholesterol concentrations (40–99 mg/dL).4 5

Reductions in triglyceride concentrations not associated with increases in LDL-cholesterol concentrations.1 3

CYP isoenzymes play a minor role in metabolism of EPA.1

Specific Drugs

Absorption

Bioavailability

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.1

EPA: Peak plasma concentrations achieved approximately 5 hours following oral administration of icosapent ethyl.1 Steady-state plasma concentrations reached in 7–10 days.5

Food

Icosapent ethyl was administered with or following a meal in clinical studies; no food effect studies performed.1 (See Oral Administration under Dosage and Administration.)

Special Populations

Gender: Plasma total EPA concentrations not substantially different between men and women.1

Pediatric patients: Pharmacokinetics not studied.1

Distribution

Extent

EPA: Majority circulating in plasma is incorporated in phospholipids, triglycerides, and cholesteryl esters; <1% present as unesterified fatty acid.1

Distributed into milk in rats.1 6 (See Lactation under Cautions.)

Plasma Protein Binding

Unesterified EPA: >99%.1

Elimination

Metabolism

EPA: Mainly metabolized in liver by β-oxidation similar to dietary fatty acids; β-oxidation splits long carbon chain into acetyl-coenzyme A, which is converted into energy via the Krebs cycle.1

EPA: CYP isoenzymes play a minor role in metabolism of EPA.1

Elimination Route

Icosapent ethyl: Not renally excreted.1

Half-life

EPA: Approximately 89 hours.1

Icosapent ethyl is used together with a proper diet to lower very high triglyceride (fat-like substance) levels in the blood.

icosapent ethyl is available only with your doctor's prescription.

In deciding to use a medicine, the risks of taking the medicine must be weighed against the good it will do. This is a decision you and your doctor will make. For icosapent ethyl, the following should be considered:

Allergies

Tell your doctor if you have ever had any unusual or allergic reaction to icosapent ethyl or any other medicines. Also tell your health care professional if you have any other types of allergies, such as to foods, dyes, preservatives, or animals. For non-prescription products, read the label or package ingredients carefully.

Pediatric

Appropriate studies have not been performed on the relationship of age to the effects of icosapent ethyl in the pediatric population. Safety and efficacy have not been established.

Geriatric

Appropriate studies performed to date have not demonstrated geriatric-specific problems that would limit the usefulness of icosapent ethyl in the elderly.

Pregnancy

Breast Feeding

There are no adequate studies in women for determining infant risk when using this medication during breastfeeding. Weigh the potential benefits against the potential risks before taking this medication while breastfeeding.

Interactions with Medicines

Although certain medicines should not be used together at all, in other cases two different medicines may be used together even if an interaction might occur. In these cases, your doctor may want to change the dose, or other precautions may be necessary. Tell your healthcare professional if you are taking any other prescription or nonprescription (over-the-counter [OTC]) medicine.

Interactions with Food/Tobacco/Alcohol

Certain medicines should not be used at or around the time of eating food or eating certain types of food since interactions may occur. Using alcohol or tobacco with certain medicines may also cause interactions to occur. Discuss with your healthcare professional the use of your medicine with food, alcohol, or tobacco.

Other Medical Problems

The presence of other medical problems may affect the use of icosapent ethyl. Make sure you tell your doctor if you have any other medical problems, especially:

• Allergy to fish or shellfish, history of—May have an increase risk of an allergic reaction to icosapent ethyl.

• Diabetes or
• Hypothyroidism (underactive thyroid)—Use with caution. Your doctor will tell you how to control these conditions that may cause lipid (fat) disorders.

• Liver problems—Your doctor may want to monitor you more closely for unwanted effects.