Therapy added to standard therapy involving the use of β-blockers to reduce the risk of cardiovascular morbidity and morbidity in patients with a stable left ventricular dysfunction (left ventricular ejection fraction - LVEF ≤ 40%) and clinical symptoms of heart failure after a recent heart attack. Therapy added to standard therapy 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. The preparation contains lactose.
Action:
Aldosterone antagonist. Eplerenone has a relative binding specificity 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 sustained increase in plasma renin activity and aldosterone concentration in the blood, associated with a reduction of the feedback inhibitory effect of aldosterone on renin secretion. The resulting increase in 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. Eplerenone is not eliminated by hemodialysis. T0,5 is 3-5 hours.
Contraindications:
Hypersensitivity to the components of the preparation. 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). Dose reduction of eplerenone has been shown to reduce the amount of potassium in the blood. The addition of hydrochlorothiazide to eplerenone compensates for increases in potassium in the blood. Use with caution in patients with type 2 diabetes and microalbuminuria (increased risk of hyperkalemia). 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. The safety and efficacy of the preparation in children and adolescents has not yet been established.
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 (creatinine clearance 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 creatinine clearance <50 ml / min with post-infarction heart failure - use caution; doses> 25 mg per day have not been studied in patients with creatinine clearance <50 ml / min. No adjustment of the initial dose is required in patients with mild or moderate hepatic impairment. There is no need to modify the initial dose in elderly patients.Way of giving. The tablets can be taken regardless of meals.
(C)
