As a treatment added to standard treatment involving the use of β-blockers, to reduce the risk of cardiovascular morbidity and morbidity in patients with a left ventricular dysfunction (LVEF ≤40%) and clinical signs of heart failure after a recent myocardial infarction heart's. As a treatment added to standard treatment, to reduce the risk of cardiovascular morbidity and morbidity in adult patients with (chronic) heart failure (NYHA class II) and with left ventricular dysfunction (LVEF ≤30%).
Composition:
1 tabl powl. contains 25 mg or 50 mg eplerenone (and 35.7 mg and 71.4 mg lactose, respectively).
Action:
Aldosterone antagonist. Eplerenone has a relative selectivity of binding to recombinant human mineralocorticoid receptors compared to binding to recombinant human glucocorticoid, Progesterone and androgen receptors. It prevents the binding of aldosterone. It causes a permanent increase in plasma renin activity and aldosterone concentration in the blood, associated with a reduction of the inhibitory effect of aldosterone on renin secretion. The resulting increased plasma renin activity and increased circulating aldosterone levels do not reduce eplerenone. After oral administration, eplerenone achieves Cmax after approx. 2 h. Food has no effect on absorption. It binds approximately 50% of plasma proteins. It is metabolised by CYP3A4 and excreted in the urine (67%) and faeces (32%), mainly in the form of metabolites. T0,5 is 3-5 hours.
Contraindications:
Hypersensitivity to the active substance or to any of the excipients. Potassium levels before treatment> 5 mmol / l. Severe renal failure (GFR <30 ml / min / 1.73 m2). Severe hepatic impairment (Child-Pugh C). Concomitant use of potassium-sparing diuretics, potassium preparations or potent CYP3A4 inhibitors (such as Itraconazole, ketoconazole, ritonavir, nelfinavir, Clarithromycin, telithromycin and nefazodone). Concomitant use of a combination of angiotensin converting enzyme (ACE) inhibitor and angiotensin receptor antagonist (ARB).
Precautions:
In all patients, the level of potassium should be determined before starting treatment, then during the first week of treatment and one month after starting treatment or changing the dose. In the course of further treatment, it is recommended to periodically monitor the level of potassium in the blood, especially in patients at risk of hyperkalemia (with renal insufficiency, diabetes, and in the elderly). Use with caution in patients with type 2 diabetes and microalbuminuria. In patients with mild and moderate hepatic impairment, electrolytes in the blood should be monitored. Avoid using lithium, cyclosporine, tacrolimus, or CYP3A4-potent drugs during eplerenone therapy. Due to the lactose content, the preparation should not be used in patients with rare hereditary galactose intolerance, Lapp lactase deficiency or malabsorption of glucose-galactose.
Pregnancy and lactation:
Animal studies do not indicate harmful effects of eplerenone on pregnancy and delivery, fetal health and postnatal development - use with caution in pregnancy. It is not known whether eplerenone is excreted in human milk (eplerenone and / or its metabolites are present in animal milk) - due to the potential for side effects in breast-fed infants, a decision should be made to discontinue breast-feeding or discontinue the medicine.
Orally.Patients with heart failure after myocardial infarction: initially 25 mg once a day, then the dose should be gradually increased (within 4 weeks), controlling the level of potassium in the blood, up to a maintenance dose of 50 mg once a day; eplerenone should be started within 3-14 days after the diagnosis of acute myocardial infarction.Patients with (chronic) heart failure (NYHA class II): initially 25 mg once a day, then the dose should be gradually increased (within 4 weeks), controlling the level of potassium in the blood, up to a maintenance dose of 50 mg once a day.Dose adjustment. After initiation of therapy, the dose of eplerenone should be adjusted depending on the potassium concentration in the blood: <5 mmol / l - increase the dose from 25 mg every other day to 25 mg once a day, from 25 mg once a day to 50 mg once a day; 5-5,4 mmol / l - keep the dose used; 5.5-9.9 mmol / l - reduce the dose from 50 mg once a day to 25 mg once a day, from 25 mg once a day to 25 mg every other day, with 25 mg every other day to stay; ≥6 mmol / l - the drug should be discontinued. After discontinuation due to potassium levels, treatment can be restarted with eplerenone 25 mg every other day, when potassium levels decrease <5 mmol / l.Special groups of patients. When concomitant use of weak or moderate CYP3A4 inhibitors, the initial and maintenance dose is 25 mg eplerenone once daily. There is no need to adjust the starting dose in patients with mild renal impairment; in patients with moderate renal impairment (CCr 30-60 ml / min), the starting dose is 25 mg every other day and the dose should be adjusted based on the control of potassium in the blood; lack of experience in patients with CCr <50 ml / min with post-infarction heart failure - be careful; doses> 25 mg per day have not been studied in patients with creatinine clearance <50 ml / min; use of the drug in patients with CCr <30 ml / min is contraindicated. No adjustment of the initial dose is required in patients with mild to moderate hepatic impairment; use in patients with severe hepatic impairment is contraindicated. In patients with serum potassium> 5.0mmol / 1, eplerenone should not be initiated. There is no need to modify the initial dose in elderly patients. The safety and efficacy of eplerenone in children and adolescents has not been established and is not recommended.Way of giving. The tablets can be taken regardless of meals.
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