Icosapent ethyl

Oral
Cardiovascular risk reduction

Oral
Severe hypertriglyceridaemia

Should be taken with food. Swallow whole, do not break open/crush/dissolve/chew.

Patient with known allergy or sensitivity to fish and/or shellfish, coagulopathy, history of atrial fibrillation or flutter. Pregnancy and lactation.

Significant: Bleeding, atrial fibrillation or atrial flutter, hypersensitivity (in patients with fish allergy).
Gastrointestinal disorders: Constipation, eructation, diarrhoea, abdominal discomfort.
General disorders and admin site conditions: Peripheral oedema.
Investigations: Increased serum triglycerides.
Metabolism and nutrition disorders: Gout.
Musculoskeletal and connective tissue disorders: Musculoskeletal pain, limb pain, arthralgia.
Respiratory, thoracic and mediastinal disorders: Oropharyngeal pain.
Skin and subcutaneous tissue disorders: Rash.

Monitor triglycerides and other lipids at baseline and periodically; ALT and AST (in patients with hepatic impairment) periodically during treatment. Monitor for signs and symptoms of bleeding.

Increased risk of bleeding with anticoagulants and antiplatelets.

Description:
Mechanism of Action: Icosapent ethyl is a stable ethyl ester of eicosapentaenoic acid (EPA). Its mechanisms of action contributing to the reduction of CV events are not fully understood, but are likely multifactorial such as reduction of triglyceride-rich lipoprotein, inhibition of platelet aggregation, increasing EPA composition from carotid plaques, or increasing the circulating EPA/arachidonic acid ratio. Other possible cellular mechanisms include inhibition of acyl CoA:1,2-diacylglycerol acyltransferase, increased hepatic β-oxidation, and decreased hepatic synthesis of triglycerides.
Synonym: ethyl icosapentate; ethyl-eicosapentaenoic acid, ethyl-EPA.
Pharmacokinetics:
Absorption: De-esterified to an active metabolite (EPA), which is absorbed in the small intestine. Time to peak plasma concentration: Approx 5 hours.
Distribution: Volume of distribution: Approx 88 L. Plasma protein binding: >99%.
Metabolism: Metabolised mainly in the liver via β-oxidation (similar to dietary fatty acids).
Excretion: Elimination half-life: Approx 37-89 hours.

Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 9831415, Icosapent ethyl. https://pubchem.ncbi.nlm.nih.gov/compound/Icosapent-ethyl. Accessed Oct. 27, 2021.

Store below 30°C.

Dyslipidaemic Agents / Supplements & Adjuvant Therapy

Anon. Icosapent Ethyl. AHFS Clinical Drug Information [online]. Bethesda, MD. American Society of Health-System Pharmacists, Inc. https://www.ahfscdi.com. Accessed 15/10/2021.

Anon. Icosapent Ethyl. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 15/10/2021.

Buckingham R (ed). Omega-3 Fatty Acids. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 15/10/2021.

Epadel S900 (Catalent Japan K.K. Kakegawa Plant). MIMS Thailand. http://www.mims.com/thailand. Accessed 15/10/2021.

Vascepa (Amarin Pharma Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 15/10/2021.

Vazkepa 998 mg Soft Capsules (Amarin Pharmaceuticals Ireland Limited). MHRA. https://products.mhra.gov.uk. Accessed 15/10/2021.