Epletor (eplerenone) coated tablets 25 mg. №30

Description

Epletor 25 mg. Composition
active substance: eplerenone;

1 tablet contains 25 mg or 50 mg of eplerenone (in terms of 100% anhydrous substance);

Epletor 25 mg excipients:

lactose monohydrate, microcrystalline cellulose, sodium croscarmellose, hypromellose, sodium lauryl sulfate, talc, magnesium stearate;

film coating: Opadry yellow 15 B220000 (hypromellose, polysorbate 80, macrogol (PEG 400), titanium dioxide (E 171), iron oxide yellow (E 172)).

Epletor 25 mg Dosage form.

Film-coated tablets.

Basic physical and chemical properties: film-coated tablets, light yellow, round, with a biconvex surface. The surface of the tablets contains the imprint “E9RN” on one side and “25” or “50” on the other side for tablets of 25 mg and 50 mg, respectively.

Pharmacotherapeutic group. Potassium-sparing diuretics. Aldosterone antagonists. Eplerenone. ATX code C03D A04.

Pharmacological properties

Pharmacodynamics.

Eplerenone is a relatively selective drug for binding to recombinant human mineralocorticoid receptors versus recombinant glucocorticoid, progesterone, and androgen receptors. Eplerenone prevents the binding of aldosterone, a key hormone of the renin-angiotensin-aldosterone system involved in the regulation of blood pressure and the development of cardiovascular diseases.

Eplerenone causes a long-term increase in plasma renin and aldosterone levels, which is associated with a negative feedback regulation of renin secretion by aldosterone. However, increased plasma renin activity and circulating aldosterone levels are not reflected in the effect of eplerenone on blood pressure.

In studies, eplerenone significantly reduced blood pressure (when measured while sitting) compared to placebo. The antihypertensive effect of the drug appeared after 2 weeks and reached a maximum after 4 weeks of use. The severity of the antihypertensive effect persisted for 8-24 weeks and did not depend on the age, gender or race of patients, from the simultaneous use with drugs such as ACE inhibitors, angiotensin II receptor antagonists, calcium channel blockers, hydrochlorothiazide and β-blockers.

Indications
Adjunct to standard therapy with β-blockers to reduce the risk of morbidity and mortality associated with cardiovascular disease in stable patients with left ventricular dysfunction (left ventricular ejection fraction ≤ 40%) and clinical signs of heart failure after recent myocardial infarction …
Adjunct to standard optimal therapy to reduce the risk of morbidity and mortality associated with cardiovascular disease in adults with NYHA class II (chronic) heart failure and left ventricular dysfunction (left ventricular ejection fraction ≤ 30%).

Contraindications
Hypersensitivity to eplerenone or another component of the drug;
clinically significant hyperkalemia or related conditions (serum potassium levels more than 5 mmol / l (meq / l)) at the start of treatment;
severe renal failure (estimated glomerular filtration rate <30 ml / min / 1.73 m2);
severe hepatic impairment (Child-Pugh class C);
simultaneous use with other potassium-sparing diuretics, potassium / potassium-containing supplements or such powerful CYP3A4 inhibitors as ketoconazole, itraconazole, ritonavir, nelfinavir, clarithromycin, telithromycin, nefazodone;
triple combination of ACE inhibitors, angiotensin receptor blockers (ARBs) and eplerenone.