The drug "Decriz" is used as:
adjunct to standard beta-blocker therapy to reduce the risk of cardiovascular morbidity and mortality in stable patients with left ventricular dysfunction (left ventricular ejection fraction ≤ 40%) and clinical signs of heart failure after a recent myocardial infarction; adjunct to standard optimal therapy to reduce the risk of cardiovascular morbidity and mortality in adult patients with NYHA class II (chronic) heart failure and left ventricular dysfunction (left ventricular ejection fraction ≤ 30%).
Composition
1 tablet contains 50 mg of eplerenone (active ingredient).
Excipients: lactose monohydrate, microcrystalline cellulose, croscarmellose sodium, hypromellose, sodium lauryl sulfate, talc, magnesium stearate.
Tablet coating: hypromellose, macrogol 400, polysorbate 80, titanium dioxide (E 171), iron oxide yellow (E 172), iron oxide red (E 172).
Contraindication
Hypersensitivity to eplerenone or to any of the excipients.
Serum potassium level > 5 mmol/L at the time of initiation of treatment.
Severe renal insufficiency (estimated glomerular filtration rate < 30 ml/min/1.73 m2).
Severe hepatic impairment (Child-Pugh class C).
Concomitant use of potassium-sparing diuretics, potassium supplements or strong CYP3A4 inhibitors (e.g. itraconazole, ketoconazole, ritonavir, nelfinavir, clarithromycin, telithromycin and nefazodone) (see section "Interaction with other medicinal products and other types of interactions").
Concomitant use of eplerenone in a triple combination with an ACE inhibitor and an angiotensin receptor blocker.
Method of administration and doses
The tablets of the drug contain doses of 25 mg or 50 mg. The maximum daily dose of the drug is 50 mg per day.
Eplerenone can be taken with or without food (see Pharmacokinetics).
Patients with heart failure after myocardial infarction. The recommended maintenance dose of eplerenone is 50 mg once daily. Treatment should be initiated at 25 mg once daily and titrated to a target dose of 50 mg once daily. This dose level should be achieved within 4 weeks, taking into account serum potassium levels (see table below). Treatment with eplerenone should usually be initiated 3 to 14 days after acute myocardial infarction.
Patients with NYHA class II (chronic) heart failure.
Treatment of patients with chronic heart failure class II according to the NYHA classification should be initiated at a dose of 25 mg once daily and gradually increased to a target dose of 50 mg once daily. It is advisable to reach this dose level within 4 weeks, taking into account the level of potassium in the blood serum (see table below and section "Special instructions").
Patients with serum potassium levels greater than 5 mmol/L should not initiate treatment with eplerenone (see section 4.3).
Serum potassium levels should be measured prior to initiation of eplerenone therapy, during the first week of treatment, and one month after initiation of treatment or dose adjustment. Serum potassium levels should be measured periodically throughout treatment as necessary.
After initiation of treatment, the dose should be adjusted based on serum potassium levels as shown in the table below.
Dose adjustment after initiation of treatment.
Serum potassium concentration (mmol/L) | Action | Dose adjustment |
< 5.0 | Increase | From 25 mg every 2 days to 25 mg once a day From 25 mg once daily to 50 mg once daily |
5.0-5.4 | No changes | The dose is not changed. |
5.5-5.9 | Decrease | From 50 mg once daily to 25 mg once daily From 25 mg once daily to 25 mg once every 2 days From 25 mg once every 2 days until temporary discontinuation |
≥ 6.0 | Temporary cancellation | - |
After temporary discontinuation of eplerenone due to an increase in potassium levels to ≥ 6 mmol/L, treatment can be resumed at a dose of 25 mg every 2 days after the potassium concentration decreases to below 5 mmol/L.
Application features
Pregnant women
There are no adequate data from the use of eplerenone in pregnant women. Animal studies do not indicate direct or indirect harmful effects with respect to pregnancy, embryonal/fetal development, parturition or postnatal development. Eplerenone should be administered with caution to pregnant women.
Breastfeeding. It is not known whether eplerenone is excreted in human milk after oral administration. However, nonclinical data indicate that eplerenone and/or its metabolites are present in the milk of rats and that the offspring of these exposed rats developed normally. Because the potential for adverse reactions in breastfed infants has not been studied, a clinical decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother.
There is no information to recommend the use of eplerenone in children. Therefore, the use of the drug in this age group of patients is not recommended.
Drivers
Studies on the effects of eplerenone on the ability to drive or use machines have not been conducted. Eplerenone does not cause drowsiness or cognitive impairment, but when driving or operating machinery, the possibility of dizziness should be taken into account.
Overdose
There have been no reports of adverse reactions associated with eplerenone overdose in humans. The most likely manifestations of overdose in humans are expected to be hypotension or hyperkalemia. Eplerenone is not removed by hemodialysis. Eplerenone has been shown to bind effectively to activated charcoal. In cases of hypotension, supportive treatment should be initiated. In cases of hyperkalemia, treatment should be initiated according to standards.
Adverse reactions
The following are adverse reactions that are possibly related to the use of eplerenone and that occurred during treatment more often than during placebo, or serious adverse reactions that occurred during treatment more often than during placebo, or those that were described during post-marketing surveillance.
Adverse reactions are classified by organ system and absolute frequency: very common (≥ 1/10), common (≥ 1/100 - < 1/10), uncommon (≥ 1/1000 - < 1/100), rare (≥ 1/10000 - < 1/1000), very rare (< 1/10000), unknown (cannot be determined based on available information).
Infections and infestations: uncommon – infection, pyelonephritis, pharyngitis.
From the blood and lymphatic system: infrequently - eosinophilia.
On the part of the endocrine system: infrequently - hypothyroidism.
Metabolism and digestion: often - hyperkalemia (see sections "Contraindications" and "Features of use"), hypercholesterolemia; infrequently - hyponatremia, dehydration, hypertriglyceridemia.
On the part of the psyche: often - insomnia.
From the nervous system: often - dizziness, syncope, headache; infrequently - hypoesthesia.
Cardiac disorders: often – left ventricular failure, atrial fibrillation; infrequently – tachycardia.
Vascular disorders: often - hypotension; infrequently - thrombosis of the arteries of the extremities, orthostatic hypotension.
From the respiratory system, thoracic organs, mediastinum: often - cough.
From the gastrointestinal tract: often - dyspepsia; infrequently - bloating.
Skin and subcutaneous tissue disorders: common: allergic reactions; uncommon: hyperhidrosis, angioedema.
Musculoskeletal and connective tissue disorders: common: muscle spasms, back pain; uncommon: musculoskeletal pain.
On the part of the kidneys and urinary tract: often - impaired renal function (see sections "Special instructions for use" and "Interaction with other medicinal products and other types of interactions").
Hepatobiliary disorders: uncommon – cholecystitis.
Reproductive system and breast disorders: uncommon – gynecomastia.
General disorders and administration site conditions: common: asthenia; uncommon: malaise.
Laboratory tests: often - increased blood urea; infrequently - increased creatinine; infrequently - decreased epidermal growth factor receptor number, increased blood glucose level.
In the EPHESUS study, an increased incidence of stroke was observed in elderly patients (≥ 75 years). However, there was no statistically significant difference between the incidence of stroke in the eplerenone group and the placebo group.
Storage conditions.
Store in the original packaging at a temperature not exceeding 25 °C.
Keep out of reach of children.
Shelf life - 3 years.
