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Icosapent Ethyl


General


Pronunciation

(eye KOE sa pent ETH il)


Brand Names: U.S.

  • Vascepa

Indications


Use: Labeled Indications

Adjunct to dietary therapy in the treatment of hypertriglyceridemia ( ≥500 mg/dL)


Contraindications


Hypersensitivity to icosapent ethyl or any component of the formulation


Dosing and Administration


Dosing: Adult

Hypertriglyceridemia: Oral: 2 g twice daily


Dosing: Geriatric

Refer to adult dosing.


Dosing: Renal Impairment

No dosage adjustment provided in manufacturers labeling (has not been studied); however, not renally eliminated.


Dosing: Hepatic Impairment

No dosage adjustment provided in manufacturers labeling (has not been studied); periodic monitoring of ALT and AST is recommended in patients with hepatic impairment.


Administration

Administer with food. Swallow whole; do not chew, crush, or divide.


Dietary Considerations

Take with food. Dietary modification is important in the control of severe hypertriglyceridemia. Maintain standard cholesterol-lowering diet during therapy.


Storage

Store at 20 ‚ °C to 25 ‚ °C (68 ‚ °F to 77 ‚ °F); excursions permitted to 15 ‚ °C to 30 ‚ °C (59 ‚ °F to 86 ‚ °F).


Dosage Forms/Strengths


Dosage Forms

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Capsule, Oral:

Vascepa: 1 g


Drug Interactions

Agents with Antiplatelet Properties (e.g., P2Y12 inhibitors, NSAIDs, SSRIs, etc.): Omega-3 Fatty Acids may enhance the antiplatelet effect of Agents with Antiplatelet Properties. Monitor therapy

Anticoagulants: Omega-3 Fatty Acids may enhance the anticoagulant effect of Anticoagulants. Monitor therapy


Monitoring Parameters

Triglycerides and other lipids (LDL-C) should be monitored at baseline and periodically. In patients with hepatic impairment, monitor ALT and AST periodically during treatment.


Adverse Reactions


1% to 10%: Neuromuscular & skeletal: Arthralgia (2%)

<1% (Limited to important or life-threatening): Oropharyngeal pain


Warnings/Precautions


Concerns related to adverse effects:

- Fish allergy: Use with caution in patients with known allergy or sensitivity to fish and/or shellfish.

- Prolongation of bleeding time: Prolongation of bleeding time not exceeding normal limits has been observed in some clinical studies of omega-3 fatty acids; clinically significant bleeding episodes did not occur. Use with caution in patients with coagulopathy or in those receiving therapeutic anticoagulation; monitor for changes in INR (with warfarin) or signs/symptoms of bleeding following initiation and dosage changes of icosapent ethyl and in patients receiving concomitant anticoagulant or antiplatelet therapy.

Disease related concerns:

- Hepatic impairment: Studies have not been conducted in patients with hepatic impairment; however, ALT/AST levels should be monitored periodically during therapy in hepatically impaired patients.

Concurrent drug therapy issues:

- Medications known to worsen hypertriglyceridemia (eg, beta-blockers, thiazides, estrogens) should be discontinued or changed prior to initiation of triglyceride-lowering therapy if possible.

Other warnings/precautions:

- Appropriate use: Should be used as an adjunct to diet therapy and exercise and only in those with very high triglyceride levels ( ≥500 mg/dL). Secondary causes of hyperlipidemia should be ruled out prior to therapy. The effect, if any, of icosapent ethyl on the risk of pancreatitis or cardiovascular mortality and morbidity in patients with severe hypertriglyceridemia is not known. Instruct patients to monitor ethanol use; may increase triglycerides.


Pregnancy Risk Factor

C


Pregnancy Considerations

Adverse events were observed in animal reproduction studies. Maternal dietary consumption of omega-3-fatty acids (containing eicosapentaenoic acid [EPA] and docosahexaenoic acid [DHA]) influences fetal concentrations (Coletta, 2010; Miles, 2011). Information specific to the therapeutic use of this product in pregnancy has not been located; however, the use of omega-3-fatty acids to manage elevated triglycerides in pregnancy has been described in case reports (Goldberg, 2012; Papadakis, 2011).


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Pharmacology

Icosapent ethyl, the ethyl ester of eicosapentaenoic acid (EPA), is an omega-3 fatty acid which aids in decreasing hepatic very low-density lipoprotein triglycerides (VLDL-TG) synthesis/secretion and increasing triglyceride clearance from VLDL particles. The mechanism has not been completely defined. Possible mechanisms include inhibition of acyl CoA: 1,2 diacylglycerol acyltransferase, increased hepatic beta-oxidation, a reduction in the hepatic synthesis of triglycerides, or an increase in plasma lipoprotein lipase activity.


Absorption

De-esterified to active metabolite (EPA) which is absorbed in the small intestine


Distribution

Vdss: EPA: ~88 L


Metabolism

Mainly hepatic via beta-oxidation; minor via CYP 450


Excretion

Not renally excreted


Time to Peak

EPA: ~5 hours


Half-Life Elimination

EPA: ~89 hours


Patient and Family Education


Patient Education

- Discuss specific use of drug and side effects with patient as it relates to treatment. (HCAHPS: During this hospital stay, were you given any medicine that you had not taken before? Before giving you any new medicine, how often did hospital staff tell you what the medicine was for? How often did hospital staff describe possible side effects in a way you could understand?)

- Have patient report immediately to prescriber significant dyspepsia, severe nausea, considerable arthralgia, or excessive weight gain (HCAHPS).

- Educate patient about signs of a significant reaction (eg, wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat). Note: This is not a comprehensive list of all side effects. Patient should consult prescriber for additional questions.

Intended Use and Disclaimer: Should not be printed and given to patients. This information is intended to serve as a concise initial reference for healthcare professionals to use when discussing medications with a patient. You must ultimately rely on your own discretion, experience and judgment in diagnosing, treating and advising patients.

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