Eplerenone

Brand Polpharma

In stock 1103 Items

Available since: 2019-09-19

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Clinical Pharmacology

Potassium-sparing diuretic. Eplerenone has a high selectivity for mineralocorticoid receptors in humans, unlike glucocorticoid, 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 pathogenesis of cardiovascular diseases.

Eplerenone causes a persistent increase in plasma renin activity and serum aldosterone. Subsequently, renin secretion is suppressed by aldosterone via a feedback mechanism. However, an increase in renin activity or concentration of circulating aldosterone does not affect the effects of eplerenone. No significant effect of eplerenone on heart rate, duration of QRS, PR or QT intervals was found 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 chronic heart failure of the II functional class according to the NYHA classification with a reduced left ventricular ejection fraction (

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, iron dye yellow oxide (E172) - 0.18 mg).

10 pieces. - blisters (3) - packs cardboard.

Eplerenone is marketed under different brands and generic names, and comes in different dosage forms:

Brand name	Manufacturer	Country	Dosage form
Espiro	Polpharma	Poland	pills
Inspra	Pfizer	USA	pills

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Dosage and Administration

The drug is prescribed by mouth, regardless of the meal.

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 NYHA classification

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.

The maximum daily dose is 50 mg.

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

Serum potassium concentration should be determined before the appointment of Espiro, during the first week and 1 month after the start of therapy or when changing the dose of the drug. In the future, it is also necessary to periodically monitor the concentration of potassium in the serum.

Correction of the initial dose in elderly patients is not required. Due to the age-related decline in kidney function in elderly patients, the risk of hyperkalemia increases, especially in the presence of comorbidities that increase serum levels of eplerenone, in particular, in violation of liver function from mild to moderate severity. It is recommended to periodically determine the concentration of potassium in the serum (see Table 1).

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

In patients with chronic heart failure functional class II according to the NYHA classification and moderate renal dysfunction (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 serum potassium concentration ( see table 1).

The experience of the use of the drug Espiro in patients with heart failure after myocardial infarction and CC

In patients with QA

Adjusting the initial dose in patients with mild to moderate hepatic impairment is not required. Given the increasing concentration of eplerenone in these patients, it is recommended to regularly monitor the concentration of potassium in the blood serum, especially in elderly patients. The use of the drug Espiro in patients with severely impaired liver function is contraindicated.

Concomitant therapy

With 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 Espiro can be started with a dose of 25 mg 1 time / day.

Adverse reactions

The following undesirable effects are given in accordance with the following gradation of the frequency of their occurrence according to the classification of the World Health Organization: very often (≥10%); often (≥1%,

From the hemopoietic system: infrequently - eosinophilia.

On the part of the endocrine system: infrequently - hypothyroidism.

Metabolism and nutrition: often - hyperkalemia, hypercholesterolemia, hypertriglyceridemia, dehydration; infrequently - hyponatremia.

Mental disorders: infrequently - insomnia.

The nervous system: often - dizziness, fainting; infrequently - headache, hypesthesia.

Since the cardiovascular system: frequent - a pronounced decrease in blood pressure, myocardial infarction; infrequently - atrial fibrillation, left ventricular failure, tachycardia, orthostatic hypotension, thrombosis of the arteries of the lower extremities.

On the part of the respiratory system: often - cough; infrequently - pharyngitis.

On the part of the digestive system: often - diarrhea, nausea, constipation; rarely - flatulence, vomiting, cholecystitis.

On the part of the skin and subcutaneous tissues: often - itchy skin; infrequently - excessive sweating.

On the part of the musculoskeletal system: often - calf muscles, musculoskeletal pain; infrequently - back pain.

On the part of the urinary system: often - impaired renal function; infrequently - pyelonephritis.

Allergic reactions: rarely - 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.

Contraindications

- clinically significant hyperkalemia;

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

- moderate or severe renal failure (QC

- severe liver failure (more than 9 points on the Child-Pugh scale);

- simultaneous use of potassium-sparing diuretics, potassium preparations or powerful 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 up to 18 years of age (there is no experience of using the drug in patients of this age group);

- Hypersensitivity to eplerenone or other components of the drug.

Precautions should be prescribed the drug for type 2 diabetes and microalbuminuria; the simultaneous use of eplerenone, ACE inhibitors or angiotensin II receptor antagonists, drugs containing lithium, cyclosporine or tacrolimus, digoxin and warfarin in doses close to the maximum therapeutic; in violation of renal function (CC

Drug interactions

Pharmacodynamic interaction

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

Preparations containing lithium: the interaction of eplerenone with lithium preparations has not been studied. However, in patients who received lithium preparations in combination with diuretics and ACE inhibitors, cases of increased concentration and lithium intoxication 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 kidney 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 eplerenone treatment, it is recommended to regularly monitor serum potassium concentration and renal function.

NSAIDs: The treatment of NSAIDs can lead to acute renal failure due to direct suppression of glomerular filtration, especially in patients at risk (elderly patients and / or patients with dehydration). With the joint use of these funds before and during treatment, it is necessary to provide an adequate water regime and monitor kidney function.

Trimethoprim: the simultaneous use of trimethoprim with eplerenone increases the risk of hyperkalemia.It is recommended to monitor serum potassium concentration and renal function, especially in patients with renal insufficiency and in elderly patients.

ACE inhibitors and angiotensin II receptor antagonists: when using eplerenone with ACE inhibitors or angiotensin II receptor antagonists, the concentration of potassium in the blood serum should be regularly monitored. Such a combination may 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-adrenergic blockers (prazosin, alfuzosin): with simultaneous use of alpha1-adrenergic blockers with eplerenone, the antihypertensive effect may increase and / or the risk of orthostatic hypotension may increase, and therefore it is recommended to control blood pressure when the body position changes.

Tricyclic antidepressants, neuroleptics, 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, tetrakozaktid: the simultaneous use of these funds with eplerenone can lead to sodium and fluid retention.

Pharmacokinetic interaction

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

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

Warfarin: there was no clinically significant pharmacokinetic interaction with warfarin. Care must be taken if warfarin is applied in doses close to the maximum therapeutic.

CYP3A4 substrates: in special studies, signs of the pharmacokinetic interaction of eplerenone with CYP3A4 substrates, for example, midazolam and cisapride, have not been identified.

CYP3A4 inhibitors:

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

- mild and moderate inhibitors of CYP3A4: simultaneous use with erythromycin, saquinavir, amiodarone, diltiazem, verapamil and fluconazole was accompanied by significant pharmacokinetic interaction (the degree of AUC increase varied from 98% to 187%). With the simultaneous use of these funds with eplerenone dose of the latter should not exceed 25 mg.

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

Antacids: Based on a pharmacokinetic clinical trial, a significant interaction of antacids with eplerenone is not suggested with their simultaneous use.

Pregnancy and Lactation

Information about the use of the drug in pregnant women do not. When pregnancy drug Espiro should be prescribed with caution and only in cases where the expected benefit to the mother far exceeds the potential risk to the fetus / child.

Information about the allocation of eplerenone with breast milk after oral administration is not. The possible undesirable effects of eplerenone on breastfed infants are unknown, so it is advisable either to stop breastfeeding or to cancel the drug, depending on its importance to the mother.

Special instructions

Hyperkalemia

With espiro treatment, hyperkalemia may develop, which is due to its mechanism of action. At the beginning of treatment and when changing the dose of the drug in all patients should be monitored the concentration of potassium in the serum. In the future, periodic monitoring of the potassium content is recommended in patients with an increased risk of hyperkalemia, for example, in elderly patients, patients with renal insufficiency and diabetes. Given the increased risk of hyperkalemia, the prescription of potassium drugs after starting treatment with Espiro is not recommended. Reducing the dose of espiro drug leads to a decrease in serum potassium concentration. In one study, the addition of hydrochlorothiazide to eplerenone prevented an increase in serum potassium concentration.

Renal dysfunction

In patients with impaired renal function, incl. diabetic microalbuminuria, it is recommended to regularly monitor the concentration of potassium in the serum. The risk of developing hyperkalemia increases with a decrease in renal function. Although the number of patients with type 2 diabetes and microalbuminuria was limited in research, nevertheless, an increase in the frequency of hyperkalemia was noted in this small sample. Therefore, in such patients, treatment should be carried out with caution. Eplerenone is not removed by hemodialysis. Use of the drug Espiro is contraindicated in severe renal failure.

Liver dysfunction

In patients with mild or moderate liver dysfunction (5-6 and 7-9 points on the Child-Pugh scale), no increase in serum potassium levels greater than 5.5 mmol / l was detected. In such patients, the electrolyte content should be monitored. In patients with severely impaired liver function, eplerenone has not been studied, so its use is contraindicated.

Inductors CYP3A4

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

Cyclosporine, tacrolimus, preparations containing lithium

During treatment drug Espiro should avoid the appointment of these funds.

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.

Influence on ability to drive motor transport and control mechanisms

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

Overdosage

Cases of overdose of eplerenone in humans have not been described. The most likely manifestations of overdose can be excessive blood pressure reduction and hyperkalemia.

Treatment: with an excessive decrease in blood pressure, supportive treatment should be prescribed. In the case of the development of hyperkalemia, standard therapy is indicated. Eplerenone is not removed by hemodialysis. It is established that eplerenone is actively associated with activated carbon.

Brand name: Espiro
Active ingredient: Eplerenone
Dosage form: pills, film coated yellow, round, biconvex, with a risk on one side; on a break - from white to almost white.
Manufacturer: Polpharma
Country of Origin: Poland