Eprosartan


Thông tin thuốc gốc
Chỉ định và Liều dùng
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.
Suy thận
Moderate to severe (CrCl <60 mL/min): Max: 600 mg daily.
Cách dùng
May be taken with or without food.
Chống chỉ định
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.
Thận trọng
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.
Tác dụng không mong muốn
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.
Thông tin tư vấn bệnh nhân
This drug may cause dizziness or tiredness, if affected, do not drive or operate machinery.
Chỉ số theo dõi
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.
Quá liều
Symptom: Hypotension. Management: Supportive treatment.
Tương tác
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.
Ảnh hưởng đến kết quả xét nghiệm
May result in false-negative aldosterone/renin ratio (ARR).
Tác dụng
Description:
Mechanism of Action: 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.
Đặc tính

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.

Bảo quản
Store between 20-25°C.
Phân loại MIMS
Thuốc đối kháng thụ thể angiotensin II
Phân loại ATC
C09CA02 - eprosartan ; Belongs to the class of angiotensin II receptor blockers (ARBs). Used in the treatment of cardiovascular disease.
Tài liệu tham khảo
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.

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