Icosapent ethyl

Icosapent ethyl is Antilipemic agents belonging to lipid-lowering agents.

Icosapent ethyl is used in the treatment Cardiovascular risk reduction with hypertriglyceridemia and Hypertriglyceridemia (adjunctive agent)

Icosapent ethyl is de-esterfied, converted into active EPA, and then absorbed in the small intestine. It reaches peak plasma concentration in 5 hours post-oral administration. Very little (<1%) is left circulating in the plasma as EPA incorporates into phospholipids, TG's, and cholesteryl esters.

Icosapent ethyl shows common side effects like Atrial fibrillation, atrial flutter, peripheral edema.

Icosapent ethyl is available in Capsules.

Icosapent ethyl is available in India, Germany, Canada, France, USA.

Reduction in the hepatic production of triglyceride-rich very low-density lipoproteins. Possible cellular mechanisms include inhibition of acyl CoA:1,2 diacylglycerol acyltransferase, increased hepatic mitochondrial and peroxisomal beta-oxidation, and a reduction in the hepatic synthesis of triglycerides. The mechanisms contributing to reduction of cardiovascular events are not completely understood but are likely multifactorial (eg, increased eicosapentaenoic acid [EPA] composition from carotid plaques, increased circulating EPA/arachidonic acid ratio, inhibition of platelet aggregation).

Icosapent ethyl is available in the form of Capsules.

Icosapent ethyl is used in the treatment Cardiovascular risk reduction with hypertriglyceridemia and Hypertriglyceridemia (adjunctive agent).

Icosapent ethyl or ethyl eicosapentaenoic acid is a synthetic derivative of the omega-3 fatty acid eicosapentaenoic acid (EPA). It is used as an adjunct therapy for severe hypertriglyceridemia (TG levels > 500 mg/dL) and to reduce the risk of cardiovascular events in certain patients with elevated triglycerides.

Icosapent ethyl is approved for use in the following clinical indications

• Cardiovascular risk reduction with hypertriglyceridemia: As an adjunct to maximally tolerated statin therapy to reduce the risk of myocardial infarction, stroke, coronary revascularization, and unstable angina requiring hospitalization in adult patients with triglyceride levels ≥150 mg/dL and either established cardiovascular disease or type 2 diabetes mellitus with ≥2 risk factors for cardiovascular disease.

• Hypertriglyceridemia: As an adjunct to diet to reduce triglyceride levels in adults with severe (≥500 mg/dL) hypertriglyceridemia.

• Cardiovascular risk reduction with hypertriglyceridemia (adjunctive agent):

Note: For patients whose triglycerides remain ≥150 mg/dL after general measures and optimal LDL lowering therapy who warrant additional ASCVD risk reduction (ie, those with established ASCVD or diabetes mellitus plus ≥2 risk factors for ASCVD), use icosapent ethyl over other triglyceride lowering therapies

Oral: 2 g twice daily with meals

• Hypertriglyceridemia (adjunctive agent):

Note: For patients whose triglycerides remain ≥500 mg/dL after general measures and optimal LDL lowering therapy who do not warrant additional ASCVD risk reduction, any prescription strength omega-3 fatty acid (including icosapent ethyl) or a fibrate (fenofibrate preferred) is reasonable

Oral: 2 g twice daily with meals.

Icosapent ethyl is available in the dosage strength of 0.5g, 1g.

Icosapent ethyl is available in the form of Capsules.

Take after eating and with a full glass of water to decrease gastric upset.

Icosapent ethyl is contraindicated in patients with:

Hypersensitivity (eg, anaphylactic reaction) to icosapent ethyl or any component of the formulation.

Concerns related to adverse effects:

• Bleeding: Bleeding, including serious events, has been reported; risk may be increased with concomitant anticoagulant/antiplatelet use. Prolongation of bleeding time not exceeding normal limits has also been observed; use with caution in patients with coagulopathy. Monitor for signs and symptoms of bleeding.

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

Disease related concerns:

• Atrial fibrillation: Atrial fibrillation (AF) or flutter requiring hospitalization may occur; risk increased in patients with a history of AF or flutter.

• Conditions associated with abnormal lipids: Manage concurrent conditions (eg, diabetes, hypothyroidism, excessive alcohol intake) that may contribute to lipid abnormalities.

Icosapent ethyl may cause liver problems, and using it with substantial quantities of ethanol may increase that risk.

Icosapent ethyl is used off label to enhance leflunomide elimination. Use of the enhanced elimination procedure is recommended in all females of reproductive potential upon discontinuation of leflunomide. Pregnancy should be avoided until undetectable serum concentrations (<0.02 mg/L) of leflunomide are verified.

• Common Adverse effects:

Atrial fibrillation, atrial flutter, peripheral edema

• Less Common Adverse effects:

Musculoskeletal pain, Increased serum triglycerides

• Rare Adverse effects

Abdominal distress, diarrhea, Limb pain

• Agents with Antiplatelet Properties (e.g., P2Y12 inhibitors, NSAIDs, SSRIs, etc.): Icosapent Ethyl may enhance the antiplatelet effect of Agents with Antiplatelet Properties. Risk C: Monitor therapy

• Anticoagulants: Icosapent Ethyl may enhance the anticoagulant effect of Anticoagulants. Risk C: Monitor therapy

• Ibrutinib: Icosapent Ethyl may enhance the antiplatelet effect of Ibrutinib. Risk C: Monitor therapy

The common side effects of Icosapent ethyl include the following :

Icosapent ethyl is generally well tolerated and adverse effects are unrelated to treatment.

• Pharmacodynamic

Reduction in the hepatic production of triglyceride-rich very low-density lipoproteins. Possible cellular mechanisms include inhibition of acyl CoA:1,2 diacylglycerol acyltransferase, increased hepatic mitochondrial and peroxisomal beta-oxidation, and a reduction in the hepatic synthesis of triglycerides. The mechanisms contributing to reduction of cardiovascular events are not completely understood but are likely multifactorial (eg, increased eicosapentaenoic acid [EPA] composition from carotid plaques, increased circulating EPA/arachidonic acid ratio, inhibition of platelet aggregation).

• Pharmacokinetics

Absorption: Icosapent ethyl is de-esterfied, converted into active EPA, and then absorbed in the small intestine. It reaches peak plasma concentration in 5 hours post-oral administration. Very little (<1%) is left circulating in the plasma as EPA incorporates into phospholipids, TG's, and cholesteryl esters.

1. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC1364710/
2. https://reference.medscape.com/drug/colestid-Icosapent ethyl -342452
3. https://go.drugbank.com/drugs/DB00375
4. https://www.sciencedirect.com/topics/medicine-and-dentistry/Icosapent ethyl
5. https://europepmc.org/article/med/6988203