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.
Moderate to severe (CrCl <60 mL/min): Max: 600 mg daily.
May be taken with or without food.
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.
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.
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.
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.
May result in false-negative aldosterone/renin ratio (ARR).
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.