Inspra coated tablets 25 mg. №30

Description

Inspra №30 Composition
active substance: eplerenone;

1 tablet contains 25 mg of eplerenone;

excipients: lactose, monohydrate, microcrystalline cellulose croscarmellose sodium; hypromellose; sodium lauryl sulfate; talc magnesium stearate Opadry yellow YS-1-12524-A.

Inspra №30 Dosage form
Film-coated tablets.

Basic physical and chemical properties: film-coated tablets, yellow, diamond-shaped, with stylized engraving “Pfizer” on one side of the tablet and “NSR” above “25” or “50” – on the other side tablets for 25 mg tablets and 50 mg, respectively.

Inspra №30 Pharmacotherapeutic group
Potassium-sparing diuretics. Aldosterone antagonists. Eplerenone. ATX code C03D A04.

Pharmacodynamics
Mechanism of action.

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 interferes with the binding of receptors to aldosterone, an important hormone of the renin-angiotensin-aldosterone system that is involved in the regulation of blood pressure and is involved in the pathophysiological mechanisms of the development of cardiovascular diseases.

Pharmacodynamic effects.

It has been demonstrated that eplerenone leads to a sustained increase in plasma renin and plasma aldosterone levels, which coincides with inhibition of the negative feedback pathway of aldosterone on renin secretion. At the same time, an increase in the activity of renin in the blood plasma and the level of aldosterone in the blood does not lead to the suppression of the action of eplerenone. In a dose range study for chronic heart failure (NYHA grades II – IV), the addition of eplerenone to the standard regimen resulted in the expected dose-dependent increase in aldosterone levels. Likewise, in the EPHESUS cardiac nephrology study (a study of the efficacy and lethality of eplerenone in patients with acute myocardial infarction, complicated left ventricular dysfunction and heart failure), treatment with eplerenone resulted in a significant increase in aldosterone levels.

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 …
An 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%) (see below). section “Pharmacological”).

Contraindications
Hypersensitivity to the active substance or to any of the excipients listed in the “Composition” section.
Patients with serum potassium levels> 5 mmol / L at the time of initiation of treatment.
Patients with severe renal failure (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 CYP 3A4 inhibitors (eg, itraconazole, ketoconazole, ritonavir, nelfinavir, clarithromycin, telithromycin, and nefazodone) (see Section “Interaction with other medicinal products and other forms of interaction”).
Simultaneous use of eplerenone in a triple combination together with an ACE inhibitor and angiotensin receptor blockers.