Espiro tablets coated. 50 mg 30 pcs. pack (eplerenon)

Latin name

ESPIRO

Release form

Tablets, film-coated yellow, round, biconvex, with a risk on one side on the kink - from white to almost white.

Pharmacological action

Potassium-sparing diuretic.

Eplerenone is highly selective for human mineralocorticoid receptors, unlike glucocorticoid receptors, progesterone and androgen receptors and prevents the binding of mineralocorticoid receptors to aldosterone, the key hormone PAAC, which is involved in the regulation of blood pressure and the pathogenesis of cardiovascular diseases.

Eplerenone causes a steady increase in plasma renin and serum aldosterone activity. Subsequently, renin secretion is suppressed by aldosterone via a feedback mechanism. Moreover, an increase in renin activity or in the concentration of circulating aldosterone does not affect the effects of eplerenone. Significant effects of eplerenone on heart rate, duration of QRS, PR or QT intervals were not detected in healthy volunteers.

Indications

- myocardial infarction: in addition to standard therapy to reduce the risk of cardiovascular mortality and morbidity in patients with stable left ventricular dysfunction (ejection fraction less than 40%) and clinical signs of heart failure after

myocardial infarction - chronic heart failure: in addition to standard therapy to reduce cardiovascular mortality and morbidity in patients with NYHA class II functional heart failure with a reduced left ventricular ejection fraction.

Contraindications

- clinically significant hyperkalemia

- potassium concentration in the blood serum at the beginning of treatment more than 5 mmol / l

- moderate or severe renal failure

- severe hepatic failure (more than 9 points on the Child-Pview scale) potassium-sparing diuretics, potassium preparations or potent CYP3A4 inhibitors, for example, itraconazole, ketoconazole, ritonavir, nelfinavir, clarithromycin, telithromycin and nefazodone

- plasma creatinine concentration> 2 mg / dl (or> 177 mmol / l) in men or> 1.8 mg / dl (or> 159 mmol / l) in women

- lactase deficiency, lactose intolerance, glucose-galactose malabsorption syndrome

- children and adolescents under 18 years of age (there is no experience with the drug in patients of this age group)

- hypersensitivity to eplerenone or other components of the drug.

Caution is advised to prescribe a drug for type 2 diabetes mellitus and microalbuminuria with the simultaneous use of eplerenone, ACE inhibitors or angiotensin II receptor antagonists, preparations containing lithium, cyclosporine or tacrolimus, digoxin and warfarin at doses close to the maximum therapeutic for impaired renal function (

Use during pregnancy and lactation

There is no information on the use of the drug in pregnant women. During pregnancy, Espiro should be prescribed with caution and only in cases where the expected benefit to the mother significantly exceeds the potential risk to the fetus / child.

There is no information on the excretion of eplerenone with breast milk after oral administration. The possible undesirable effects of eplerenone on breast-fed infants are unknown, so it is advisable to either stop breastfeeding or discontinue the drug, depending on its importance to the mother.

Special instructions

Hyperkalemia

When treated with Espiro, hyperkalemia may develop due to its mechanism of action. At the beginning of treatment and when changing the dose of the drug in all patients, the concentration of potassium in the blood serum should be monitored. In the future, periodic monitoring of potassium is recommended in patients with an increased risk of developing hyperkalemia, for example, elderly patients, patients with renal failure and diabetes. Given the increased risk of developing hyperkalemia, the appointment of potassium preparations after the start of treatment with Espiro is not recommended. Reducing the dose of Espiro leads to a decrease in the concentration of potassium in the blood serum. In one study, the addition of hydrochlorothiazide to eplerenone prevented an increase in serum potassium concentration.

Impaired renal function

In patients with impaired renal function, including diabetic microalbuminuria, it is recommended to regularly monitor the concentration of potassium in the blood serum. The risk of developing hyperkalemia increases with decreased kidney function. Although the number of patients with type 2 diabetes and microalbuminuria in the studies was limited, however, in this small sample, an increase in the incidence of hyperkalemia was noted. In this regard, in such patients, treatment should be carried out with caution. Eplerenone is not removed by hemodialysis. The use of Espiro is contraindicated in severe renal failure.

Impaired liver function

In patients with mild or moderate impaired liver function (5-6 and 7-9 points on the Child-Pugh scale), an increase in serum potassium concentration of more than 5.5 mmol / L was not detected. In such patients, electrolyte levels should be monitored. In patients with severely impaired liver function, eplerenone has not been studied, therefore its use is contraindicated.

Inducers of CYP3A4

The simultaneous use of Espiro with powerful inducers of CYP3A4 is not recommended.

cyclosporine, tacrolimus, drugs, containing lithium

During treatment with Espiro, the administration of these agents should be avoided.

Lactose

Tablets contain lactose, so they should not be prescribed to patients with rare hereditary diseases such as lactose intolerance, lactase deficiency and glucose-galactose malabsorption syndrome.

Effect on the ability to drive vehicles and control mechanisms

The effect of the drug Espiro on the ability to drive vehicles or use sophisticated equipment has not been studied. However, given the possibility of the drug causing dizziness and fainting, caution should be exercised when driving vehicles or using sophisticated equipment while taking Espiro.

Composition

1 tab.

eplerenone 50 mg.

Excipients: lactose monohydrate - 77.34 mg, microcrystalline cellulose - 30.76 mg, hypromellose 15cP - 2.5 mg, sodium lauryl sulfate - 1.7 mg, croscarmellose sodium - 6 mg, magnesium stearate - 1.7 mg.

Shell composition: Opadry II 33G32578 (yellow) - 8 mg (hypromellose 6cP (E464) - 3.2 mg, titanium dioxide (E171) - 1.82 mg, lactose monohydrate - 1.68 mg, macrogol 3350 - 0.64 mg, triacetin - 0.48 mg, dye iron oxide yellow (E172) - 0.18 mg).

10 pcs - blisters (3) - packs of cardboard.

Dosage and administration

The drug is administered orally, regardless of food intake.

Myocardial infarction

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

Chronic heart failure II functional class according to NYHA classification

Treatment should be started with a dose of 25 mg 1 time / day and increased to 50 mg 1 time / day after 4 weeks, taking into account the concentration of potassium in the blood serum. The maximum daily dose is 50 mg.

After temporarily stopping the use of Espiro due to an increase in serum potassium concentration to 6 mmol / l or more, Espiro therapy can be resumed at a dose of 25 mg every other day, when the serum potassium concentration is

The serum potassium concentration should be determine before the appointment of the drug Espiro, during the first 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.

Initial dose adjustment in elderly patients is not required. Due to the age-related decline in renal function in elderly patients, the risk of developing hyperkalemia is increased, especially in the presence of concomitant diseases that increase the concentration of eplerenone in the blood serum, in particular, with impaired liver function from mild to moderate severity. It is recommended to periodically determine the concentration of potassium in the blood serum (see table 1).

Initial dose adjustment in patients with mild renal impairment is not required. The degree of hyperkalemia increases with impaired renal function. It is recommended to periodically determine the concentration of potassium in the blood serum (see table 1). Eplerenone is not removed by hemodialysis. In patients with severe renal impairment (CC

) In patients with NYHA classification II functional class chronic heart failure and moderate renal impairment (CC 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).

Experience with Espiro in patients with heart failure after myocardial infarction and KK

In patients with KK

Correction of initial Mild to moderate hepatic impairment is not required in patients with mild to moderate hepatic impairment.According to the increase in eplerenone concentration in such patients, it is recommended that serum potassium concentration be regularly monitored, especially in elderly patients. The use of Espiro in patients with severe liver dysfunction is contraindicated.

Concomitant therapy

With the simultaneous use of drugs that have a weak or moderate inhibitory effect on CYP3A4, for example, erythromycin, saquinavir, amiodarone, diltiazem, verapamil and fluconazole, treatment with Espiro can be started with a dose of 25 mg 1 time / day.

Side effects

The following adverse effects are shown in accordance with the following gradation of frequency of occurrence according to the World Health Organization classification: very often (? 10%) often (? 1%).

From the hematopoietic system: infrequently - eosinophilia.

From the endocrine system: infrequently - hypothyroidism.

From the side of metabolism and nutrition: often - hyperkalemia, hypercholesterolemia, hypertriglyceridemia, dehydration infrequently - hyponatremia.

Mental disorders: infrequently - insomnia.

From the nervous system: often - dizziness, fainting infrequently - headache, hypesthesia.

From the cardiovascular system: frequent - marked decrease in blood pressure, myocardial infarction infrequently - atrial fibrillation, left ventricular failure, tachycardia, orthostatic hypotension, thrombosis of lower limb arteries.

From the respiratory system: often - cough infrequently - pharyngitis.

From the digestive system: often - diarrhea, nausea, constipation infrequently - flatulence, vomiting, cholecystitis.

From the skin and subcutaneous tissues: often - skin itching infrequently - excessive sweating.

From the musculoskeletal system: often - spasms of the calf muscles, musculoskeletal pain infrequently - back pain.

From the urinary system: often - impaired renal function infrequently - pyelonephritis.

Allergic reactions: infrequently - skin rash frequency is unknown - angioedema.

Other: infrequently - asthenia, malaise, gynecomastia.

Laboratory indicators: infrequently - an increase in the concentration of residual nitrogen of urea, creatinine, a decrease in the expression of the epidermal growth factor receptor, an increase in the concentration of glucose in the blood serum.

Drug Interactions

Pharmacodynamic Interactions

Potassium-sparing diuretics and potassium preparations: Given the increased risk of hyperkalemia, eplerenone should not be prescribed to patients receiving potassium-sparing diuretics and potassium preparations. Potassium-sparing diuretics can enhance the effects of antihypertensive drugs and other diuretics.

Lithium-containing preparations: The interaction of eplerenone with lithium preparations has not been studied. However, in patients receiving lithium preparations in combination with diuretics and ACE inhibitors, cases of increased concentration and intoxication with lithium have been described. If such a combination is necessary, it is advisable to control the concentration of lithium in the blood plasma.

Cyclosporine, tacrolimus: cyclosporine and tacrolimus can cause impaired renal function and increase the risk of hyperkalemia. The simultaneous use of eplerenone and cyclosporine or tacrolimus should be avoided. If cyclosporine or tacrolimus is required during treatment with eplerenone, it is recommended that serum potassium concentration and renal function be regularly monitored.

NSAIDs: NSAID treatment can lead to acute renal failure by directly suppressing glomerular filtration, especially in patients at risk (elderly patients and / or patients with dehydration). With the combined use of these funds before and during treatment, it is necessary to ensure an adequate water regime and monitor kidney function.

Trimethoprim: concomitant use of trimethoprim with eplerenone increases the risk of hyperkalemia. It is recommended that serum potassium concentration and kidney function be monitored, especially in patients with renal failure and elderly patients.

ACE inhibitors and angiotensin II receptor antagonists: when using eplerenone with ACE inhibitors or angiotensin II receptor antagonists, serum potassium concentration should be regularly monitored. Such a combination can lead to an increased risk of hyperkalemia, especially in patients with impaired renal function, including in elderly patients. Do not use a triple combination of an ACE inhibitor and APAII with eplerenone.

Alpha1-blockers (prazosin, alfuzosin): with the simultaneous use of alpha1-blockers with eplerenone, the antihypertensive effect may increase and / or the risk of orthostatic hypotension may increase, in connection with which it is recommended to control blood pressure with a change in body position.

Tricyclic antidepressants, antipsychotics, amifostine, baclofen: with the simultaneous use of these agents with eplerenone, the antihypertensive effect may increase or the risk of orthostatic hypotension may increase.

Glucocorticoids, tetracosactide: The simultaneous use of these agents with eplerenone can lead to a retention of sodium and fluid.

Pharmacokinetic interaction

In vitro studies indicate that eplerenone does not inhibit the isoenzymes CYP1A2, CYP2C19, CYP2C9, CYP2D6 and CYP3A4. Eplerenone is not a substrate or inhibitor of the glycoprotein P.

Digoxin: Digoxin AUC when used concomitantly with eplerenone increases by 16% (90% CI: 4-30%). Care must be taken if digoxin is used in doses close to the maximum therapeutic.

Warfarin: No clinically significant pharmacokinetic interaction with warfarin has been identified. Caution must be exercised if warfarin is used in doses close to the maximum therapeutic.

CYP3A4 substrates: no special signs of pharmacokinetic interaction of eplerenone with CYP3A4 substrates, for example, midazolam and cisapride, were detected.

CYP3A4 inhibitors:

are potent inhibitors of CYP3A4: when using eplerenone with CYP3A4 inhibitors, significant pharmacokinetic interaction is possible. A potent inhibitor of CYP3A4 (ketoconazole 200 mg 2 times / day) caused an increase in AUC of eplerenone by 441%. Concomitant use of eplerenone with potent CYP3A4 inhibitors such as ketoconazole, itraconazole, ritonavir, nelfinavir, clarithromycin, telithromycin, and nefazadone,

is contraindicated - mild and moderate CYP3A4 inhibitors: simultaneous use with erythromycin, saquinavir, amiodarone, diltiazem, verapamil and fluconazole is accompanied by an increase of 18%, with a significant increase of 98% (7%). With the simultaneous use of these funds with eplerenone, the dose of the latter should not exceed 25 mg.

Inducers CYP3A4: the simultaneous administration of drugs containing St. John's wort perforated (a powerful inducer of CYP3A4) with eplerenone caused a decrease in AUC of the latter by 30%. When using more powerful CYP3A4 inducers, such as rifampicin, a more pronounced decrease in AUC of eplerenone is possible. Given the possible decrease in the effectiveness of eplerenone, the simultaneous use of powerful inducers of CYP3A4 (rifampicin, carbamazepine, phenytoin, phenobarbital, drugs containing St. John's wort perforated) is not recommended.

Antacids: based on a pharmacokinetic clinical study, significant interaction of antacids with eplerenone with their simultaneous use is not expected.

Overdose

There have been no cases of eplerenone overdose in humans. The most likely manifestations of overdose may be an excessive decrease in blood pressure and hyperkalemia.

Treatment: in case of excessive decrease in blood pressure, it is necessary to appoint supportive treatment. In the case of hyperkalemia, standard therapy is indicated. Eplerenone is not removed during hemodialysis. Eplerenone has been found to bind actively to activated carbon.

Storage conditions

The product should be stored out of the reach of children at a temperature not exceeding 25 ° C.

Shelf life

3 years.

Deystvuyushtee substance

Эplerenon

dosage form

tablets

Possible product names

Espiro tablets coated film 50 mg 30 pcs.

Polpharma, Poland



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