Eplepres (eplerenone) coated tablets 50 mg. №30

Description

Eplepres 50 mg. Storage
active substance: eplerenone;

1 tablet contains eplerenone 25 mg or 50 mg;

Eplepres 50 mg. excipients:

lactose monohydrate; microcrystalline cellulose; croscarmellose sodium; hypromellose (hydroxypropylmethylcellulose); sodium lauryl sulfate; talc; magnesium stearate;

shell: Opadry II Yellow 33G32799: hypromellose (hydroxypropylmethylcellulose); lactose monohydrate; polyethylene glycol; triacetin; titanium dioxide (E 171); iron oxide yellow (E 172).

Eplepres 50 mg. Dosage form
Film-coated tablets.

Main physical and chemical properties: round tablets with a biconvex surface, film-coated from light brownish-yellow to light yellow.

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

Pharmacological properties

Pharmacodynamics.

Eplerenone has relative selectivity for binding to recombinant human mineralocorticoid receptors compared to its interaction with recombinant human receptors for glucocorticoids, progesterone and androgens. Eplerenone prevents the binding of receptors to aldosterone, an important hormone in the renin-angiotensin-aldosterone system that is involved in regulating blood pressure and is involved in the pathophysiological mechanisms of cardiovascular disease.

Eplerenone leads to a sustained increase in plasma renin levels and serum aldosterone levels, which coincides with the suppression of the negative feedback pathway of aldosterone on renin secretion. At the same time increase in activity of renin in blood plasma and level of aldosterone in blood does not lead to suppression of action of eplerenone.

In chronic heart failure (New York Cardiac Association (NYHA) class II – IV), the addition of eplerenone to the standard treatment regimen resulted in the expected dose-dependent increase in aldosterone levels.

Indication
Addition to standard treatment with beta-blockers to reduce the risk of cardiovascular disease and mortality in stable patients with left ventricular dysfunction (left ventricular ejection fraction ≤ 40%) and clinical signs of heart failure after a recent transfer. myocardial infarction.

Addition to standard optimal therapy to reduce the risk of morbidity and mortality associated with cardiovascular disease in adult patients with class II heart failure (chronic) according to the NYHA classification and left ventricular dysfunction (left ventricular ejection fraction ≤ 30%) see section “Pharmacodynamics”).

Contraindication
Hypersensitivity to eplerenone or to any of the excipients.
Patients with serum potassium> 5 mmol / l at the start of treatment.
Patients with severe renal insufficiency (estimated glomerular filtration rate <30 ml / min / 1.73 m2).
Patients with severe hepatic impairment (Child-Pugh class C).
Patients taking potassium-sparing diuretics or potent CYP3A4 inhibitors (eg itraconazole, ketoconazole, ritonavir, nelfinavir, clarithromycin, telithromycin and nefazodone) (see Interaction with other medicinal products and other forms of interaction).
Concomitant use of eplerenone in a triple combination with an ACE inhibitor and an angiotensin receptor blocker.