1 tabl powl. contains 600 mg eprosartan as mesilate.
Action:
Angiotensin II receptor antagonist (AT type1). The pressure drop is maintained for more than 24 h, without orthostatic hypotension after the first dose. Discontinuation of treatment does not cause a rapid increase in blood pressure based on the "rebound effect". In hypertensive patients, eprosartan does not affect plasma fasting triglycerides, total cholesterol or LDL cholesterol. After oral administration, eprosartan is absorbed from the gastrointestinal tract to a limited extent (bioavailability is approximately 13%). The maximum concentration in the blood reaches after 1-2 h after taking on an empty stomach. About 98% is bound to plasma proteins. It is excreted in urine and faeces. T0,5 is 5-9 hours.
Contraindications:
Hypersensitivity to the components of the preparation. Severe hepatic failure. Significant hemodynamically bilateral renal artery stenosis or severe artery stenosis of the sole active kidney. Co-administration with aliskiren in patients with diabetes or renal impairment (GFR <60 ml / min / 1.73 m2). II and III trimester of pregnancy. Breastfeeding period.
Precautions:
Special care should be taken in patients with mild to moderate hepatic impairment as there is limited experience in this group of patients. In patients with severe hypovolaemia and / or salt deficiency (eg when using diuretics in high doses), symptomatic hypotension may occur - these conditions should be corrected before starting treatment. Caution is advised when used in patients with a creatinine clearance <30 ml / min or dialysis patients. In patients with renal function dependent on the activity of the renin-angiotensin system (patients with severe heart failure - NYHA class IV, bilateral renal artery stenosis or renal artery stenosis of the sole active kidney) may occur oliguria and / or progressive azotemia, rarely - acute kidney. Due to the risk of hypotension, syncope, hyperkalemia and renal dysfunction (including acute renal failure), dual RAA blocking is not recommended (eg, by the combined use of an angiotensin II receptor antagonist with an ACE inhibitor or aliskiren); if the use of the RAA double block is absolutely necessary, it should only be carried out under the supervision of a specialist. At the same time, angiotensin II receptor antagonists and ACE inhibitors should not be used in patients with diabetic nephropathy. Particularly cautiously used in patients with impaired renal function. Lack of experience in patients after recent kidney transplantation. Use in patients with primary hyperaldosteronism is not recommended. As with all vasodilators, eprosartan should be used with caution in patients with aortic or mitral stenosis or hypertrophic cardiomyopathy. Due to the lactose content, the preparation should not be used in patients with galactose intolerance, Lapp lactase deficiency or malabsorption of glucose-galactose. The efficacy and safety of the preparation in children and adolescents has not been established - it is not recommended to use in this group of patients.
Pregnancy and lactation:
Eprosartan is not recommended during the first trimester of pregnancy. The use of eprosartan in the second and third trimester of pregnancy is contraindicated. Drugs that directly affect the renin-angiotensin-aldosterone system can have a detrimental effect on pregnancy and the fetus or newborn (including deaths) and / or can cause serious birth defects if administered in the second and third trimester of pregnancy. Due to the lack of data on the use of eprosartan during breast-feeding, its use is not recommended.
Side effects:
Very common: headache. Common: dizziness, rhinitis, cutaneous allergic reactions (eg pruritus, rash), non-specific gastrointestinal complaints (eg, nausea, vomiting, diarrhea, weakness).Uncommon: hypersensitivity reactions, hypotension, angioneurotic edema. In addition, renal dysfunction (including renal failure) was observed in patients at risk (eg with renal artery stenosis).
Dosage:
Orally. Adults: the recommended dose is 600 mg once a day in the morning. For the majority of patients, maximum effectiveness may be achieved after 2-3 weeks of treatment. Eprosartan can be used alone or in combination with other blood pressure lowering medicines if a blood pressure-lowering effect is needed. It is recommended primarily for combination with thiazide diuretics (e.g. hydrochlorothiazide) or Calcium antagonists (e.g. nifedipine). In patients with moderate or severe renal insufficiency (creatinine clearance <60 ml / min) the maximum daily dose is 600 mg. There is limited experience in patients with hepatic impairment. The drug can be taken regardless of meals.