Inspra tablets 25 mg, No. 30

myocardial infarction - in addition to standard therapy, in order to reduce the risk of cardiovascular mortality and morbidity in patients with stable LV dysfunction (EF ? 40%) and clinical signs of heart failure after myocardial infarction;

chronic heart failure - in addition to standard therapy, in order to reduce the risk of cardiovascular mortality and morbidity in patients with chronic heart failure of FC II according to the NYHA classification, with LV dysfunction (EF ? 35%).

Inside. Food intake does not affect the absorption of InspraЃ.

For individual dose selection, dosages of 25 and 50 mg can be used.

THEM

Treatment should begin with a dose of 25 mg 1 time per day and increase it to 50 mg 1 time per day for 4 weeks, taking into account the concentration of potassium in the blood serum (see table 1). The recommended maintenance dose of the drug is 50 mg once a day.

CHF II FC according to NYHA classification

Treatment should begin with a dose of 25 mg 1 time per day and increase it to 50 mg 1 time per day for 4 weeks, taking into account the concentration of potassium in the blood serum (see table 1). The maximum daily dose is 50 mg. After a temporary discontinuation of the drug due to an increase in serum potassium concentration to or more than 6 mmol / L, drug therapy can be resumed at a dose of 25 mg every other day, when the serum potassium concentration is <5 mmol / L.

General recommendations

The concentration of potassium in the blood serum should be determined before the administration of InspraЃ, within 1 week and 1 month after the start of therapy or when the dose of the drug is changed. In the future, it is also necessary to periodically monitor the concentration of potassium in the blood serum.

Elderly patients. Correction of the starting dose is not required in elderly patients. Due to the age-related decrease in renal function in elderly patients, the risk of developing hyperkalemia increases, especially in the presence of concomitant diseases that contribute to an increase in serum eplerenone concentrations, in particular, in case of mild to moderate hepatic dysfunction. It is recommended to periodically determine the concentration of potassium in the blood serum (see table 1, as well as 'Special instructions' and 'Contraindications', With caution).

Impaired renal function. Correction of the initial dose in patients with mild renal impairment is not required. The degree of hyperkalemia increases with deteriorating renal function. It is recommended to periodically determine the content of potassium in the blood serum (see table 1, as well as 'Special instructions'). InspraЃ is not removed by hemodialysis. In patients with CHF II FC according to the NYHA classification and moderate renal dysfunction (Cl creatinine 30-60 ml / min), therapy should be started with a dose of 25 mg every other day, followed by dose adjustment depending on the concentration of potassium in the blood serum (see. table 1). In patients with severe insufficiency of night function (Cl creatinine <30 ml / min), the use of the drug is contraindicated (see 'Contraindications').There is no experience of using InspraЃ in patients with heart failure after MI and Cl creatinine <50 ml / min. InspraЃ should be used with caution in these patients (see 'Contraindications', With caution). In patients with Cl creatinine <50 ml / min, the use of InspraЃ at a dose higher than 25 mg 1 time per day has not been studied (see 'Special instructions').

Liver dysfunction. Correction of the initial dose in patients with mild to moderate hepatic dysfunction is not required. Given the increase in the concentration of eplerenone in such patients, it is recommended to regularly monitor the concentration of potassium in the blood serum, especially in elderly patients (see 'Special instructions'). The use of InspraЃ in patients with severe hepatic dysfunction is contraindicated.

Concomitant therapy. With the simultaneous use of drugs that have a weak or moderately pronounced inhibitory effect on CYP3A4, for example, erythromycin, saquinavir, amiodarone, diltiazem, verapamil and fluconazole, treatment with InspraЃ can be started with a dose of 25 mg once a day, while the dose of the latter should not exceed 25 mg once a day (see 'Interaction').

Table 1

Dose selection after starting treatment

hypersensitivity to eplerenone or other components of the drug;

clinically significant hyperkalemia;

the serum potassium content at the beginning of treatment is more than 5 mmol / l;

moderate or severe renal failure (Cl creatinine <30 ml / min) in patients with chronic heart failure II FC according to the NYHA classification;

severe hepatic impairment (more than 9 points according to the Child-Pugh classification);

rare hereditary diseases such as lactose intolerance, lactase deficiency and glucose-galactose malabsorption syndrome (see 'Special instructions');

concomitant use of potassium-sparing diuretics, potassium preparations, or strong CYP3A4 inhibitors, such as itraconazole, ketoconazole, ritonavir, nelfinavir, clarithromycin, telithromycin and nefazodone (see Interaction);

plasma creatinine concentration> 2 mg / dL (> 177 mmol / L) in men or> 1.8 mg / dL (> 159 mmol / L) in women;

there is no experience of using the drug in children under the age of 18, therefore, its appointment to patients of this age group is not recommended.

With care: type 2 diabetes mellitus and microalbuminuria (see 'Special instructions'); elderly age; impaired renal function (Cl creatinine less than 50 ml / min); simultaneous use of eplerenone and ACE inhibitors or angiotensin II receptor antagonists, strong inducers of the isoenzyme CYP3A4, preparations containing lithium, cyclosporine or tacrolimus, digoxin and warfarin in doses close to the maximum therapeutic (see 'Special instructions' and 'Interaction'). A triple combination of an ACE inhibitor and angiotensin II receptor antagonists with eplerenone should not be used.

Pharmacological action
Inspra is a potassium-sparing diuretic. The drug prevents the binding of the key hormone of the renin-angiotensin-aldosterone system - aldosterone, which is involved in the regulation of blood pressure, the pathophysiology of cardiovascular diseases.
Indications
Inspra is used as an adjunct to standard optimal treatment:
- to reduce the risk of complications, mortality in patients with stable left ventricular dysfunction (with left ventricular ejection fraction less than 40%), clinical signs of cardiac insufficiency after myocardial infarction;
- to reduce the risk of complications and mortality in adults with chronic heart failure
Contraindications
Inspra is not used:
- in case of allergy to eplerenone, intolerance to excipients;
- when the level of potassium in plasma is more than 5 mmol / l at the time of initiation of therapy;
- with severe renal failure (with an estimated glomerular filtration rate of less than 30 ml / minute / 1.73 m2);
- with insufficient liver function (class C on the Child-Pugh scale);
- while taking potassium preparations, potassium-sparing diuretics, powerful inhibitors of CYP 3A4 (ritonavir, itraconazole, ketoconazole, nelfinavir, telithromycin, clarithromycin, nefazodone).
Application during pregnancy and
breastfeeding Inspra is not used during breastfeeding. For the treatment of pregnant women, it is used with caution.
Method of administration and dosage
The drug can be taken with food or with or without food.
For patients after myocardial infarction with the development of heart failure, a maintenance dose of 50 mg once a day is recommended. Treatment begins with a dose of 25 mg / day, which is gradually (preferably over four weeks) increased to the target dose of 50 mg / day, taking into account the level of potassium in the plasma. As a rule, treatment begins 3-14 days after an acute heart attack.
Patients with chronic heart failure (NYHA II) start treatment with a dose of 25 mg once a day, gradually increasing it to the target of 50 mg / day.
The maximum dose is 50 mg / day.
Side effects
Pharyngitis, pyelonephritis, hypothyroidism, hyperkalemia, dehydration, hypercholesterolemia, hyponatremia, insomnia, dizziness, headache, fainting, hypoesthesia, thrombosis of limb arteries, left ventricular failure, atrial fibrillation, atrial fibrillation, tachycardia, arteriostatic hypotension, orthostatic hypotension hyperhidrosis, allergic reactions, angioedema, muscle spasms, back pain, pain in the musculoskeletal system, impaired renal function, cholecystitis, gynecomastia.
Overdose
Probable manifestations: hyperkalemia, arterial hypotension.
Treatment: the appointment of activated carbon, supportive therapy.