Eprosartan


Generic Medicine Info
Indications and Dosage
Oral
Essential hypertension
Adult: Monotherapy or in combination with other antihypertensive agents such as thiazide-type diuretics (e.g. hydrochlorothiazide), or Ca channel blockers (e.g. nifedipine): Initially, 600 mg once daily, may be increased up to Max of 800 mg once daily according to individual response.
Renal Impairment
Moderate to severe (CrCl <60 mL/min): Max: 600 mg daily.
Administration
May be taken with or without food.
Contraindications
Haemodynamically significant bilateral renovascular disease or severe stenosis of a solitary functioning kidney. Severe hepatic impairment. Pregnancy. Concomitant use with aliskiren in patients with diabetes mellitus or renal impairment (GFR <60 mL/min/1.73 m2). Concurrent use with ACE inhibitors in patients with diabetic nephropathy.
Special Precautions
Patient with aortic or mitral valve stenosis, hypertrophic cardiomyopathy, coronary heart disease, salt or volume depletion, primary hyperaldosteronism, idiopathic or hereditary angioedema, history of angioedema associated with ACE inhibitor therapy; diabetes mellitus, ascites due to cirrhosis or refractory ascites. Patient undergoing surgery. Black race. Renal and mild to moderate hepatic impairment. Elderly. Lactation.
Adverse Reactions
Significant: Hyperkalaemia, renal function deterioration, increased serum creatinine; symptomatic hypotension (particularly in patients with severe salt or volume depletion). Rarely, angioedema.
Cardiac disorders: Chest pain.
Gastrointestinal disorders: Diarrhoea, nausea, vomiting, abdominal pain, dyspepsia.
General disorders and administration site conditions: Fatigue, asthenia.
Infections and infestations: Viral infection.
Injury, poisoning and procedural complications: Injury.
Metabolism and nutrition disorders: Hypertriglyceridaemia, dependent oedema.
Musculoskeletal and connective tissue disorders: Arthralgia, myalgia.
Nervous system disorders: Dizziness, headache.
Psychiatric disorders: Depression.
Renal and urinary disorders: UTI.
Respiratory, thoracic and mediastinal disorders: Upper respiratory tract infection, pharyngitis, rhinitis, cough, sinusitis, bronchitis.
Skin and subcutaneous tissue disorders: Rash, pruritus.
Vascular disorders: Postural hypotension.
Patient Counseling Information
This drug may cause dizziness or tiredness, if affected, do not drive or operate machinery.
Monitoring Parameters
Monitor blood pressure regularly during therapy; BUN, eGFR, serum creatinine, and serum K levels prior to and after dose changes and at least annually thereafter. Assess for signs of angioedema.
Overdosage
Symptom: Hypotension. Management: Supportive treatment.
Drug Interactions
May increase K concentrations with K-sparing diuretics, K supplements, K-containing salt substitutes, or other drugs that may elevate K levels (e.g. heparin, trimethoprim). Enhanced blood pressure-lowering effect with other antihypertensive drugs. May increase the serum concentration and toxicity of lithium. May increase serum K levels and risk of worsened renal function (including acute renal failure) with NSAIDs.
Potentially Fatal: Increased risk of hypotension, hyperkalaemia, and reduced renal function (including acute renal failure) with aliskiren or ACE-inhibitors.
Lab Interference
May result in false-negative aldosterone/renin ratio (ARR).
Action
Description: Eprosartan is a potent non-biphenyl non-tetrazole angiotensin II receptor antagonist that selectively binds to the angiotensin II receptor type 1 (AT1 receptors). It blocks the vasoconstricting and aldosterone-secreting action of angiotensin II by selectively inhibiting the binding of angiotensin II to AT1 receptor in various tissues (e.g. vascular smooth muscle, adrenal gland).
Onset: Approx 1-2 hours.
Pharmacokinetics:
Absorption: Absorbed from the gastrointestinal tract. Absolute bioavailability: Approx 13% (300 mg dose). Time to peak plasma concentration: Approx 1-2 hours (fasted state).
Distribution: Volume of distribution: Approx 13 L. Plasma protein binding: Approx 98%.
Metabolism: Minimally metabolised in the liver.
Excretion: Via faeces (90%); urine (7%, mainly as unchanged drug and the remaining as acyl glucuronide). Terminal elimination half-life: Approx 5-9 hours.
Chemical Structure

Chemical Structure Image
Eprosartan

Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 5281037, Eprosartan. https://pubchem.ncbi.nlm.nih.gov/compound/5281037. Accessed July 27, 2022.

Storage
Store between 20-25°C.
MIMS Class
Angiotensin II Antagonists
ATC Classification
C09CA02 - eprosartan ; Belongs to the class of angiotensin II receptor blockers (ARBs). Used in the treatment of cardiovascular disease.
References
Anon. Eprosartan Mesylate. AHFS Clinical Drug Information [online]. Bethesda, MD. American Society of Health-System Pharmacists, Inc. https://www.ahfscdi.com. Accessed 09/06/2022.

Anon. Eprosartan. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 09/06/2022.

Buckingham R (ed). Eprosartan Mesilate. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 09/06/2022.

Eprosartan 300 mg Film-coated Tablets (Manx Healthcare Ltd). MHRA. https://products.mhra.gov.uk. Accessed 09/06/2022.

Eprosartan Mylan 400 mg Film-coated Tablets (Generics [UK] Limited t/a Mylan). MHRA. https://products.mhra.gov.uk. Accessed 09/06/2022.

Joint Formulary Committee. Eprosartan. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. Accessed 09/06/2022.

Disclaimer: This information is independently developed by MIMS based on Eprosartan from various references and is provided for your reference only. Therapeutic uses, prescribing information and product availability may vary between countries. Please refer to MIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, MIMS shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise. Copyright © 2023 MIMS. All rights reserved. Powered by MIMS.com
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