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Eplerenone (Eplerenonum)

Given the increased risk of hyperkalemia, eplerenone should not be prescribed to patients receiving potassium-sparing diuretics and potassium supplements. Potassium-sparing diuretics may enhance the effects of antihypertensive agents and other diuretics.

Cases of lithium toxicity have been described in patients receiving lithium in combination with diuretics and ACE inhibitors. Concomitant use of eplerenone and lithium should be avoided.

Cyclosporine and tacrolimus may cause renal dysfunction and increase the risk of hyperkalemia. Concomitant use of eplerenone and cyclosporine or tacrolimus should be avoided.

Treatment with 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). When using these drugs together, it is necessary to ensure adequate fluid intake and monitor renal function before and during treatment.

Concomitant use of trimethoprim with eplerenone increases the risk of developing hyperkalemia. It is recommended to monitor serum potassium concentrations and renal function, especially in patients with renal failure and in elderly patients.

Eplerenone should be used with caution with ACE inhibitors or angiotensin II receptor antagonists. This combination may lead to an increased risk of hyperkalemia, especially in patients with impaired renal function, including the elderly. It is recommended to carefully monitor renal function and serum potassium concentrations.

With simultaneous use of alpha1-blockers with eplerenone, the hypotensive effect may be enhanced and/or the risk of developing orthostatic hypotension may increase, and therefore it is recommended to monitor blood pressure when changing body position.

When used simultaneously with eplerenone, tricyclic antidepressants, neuroleptics, amifostine, baclofen may enhance the antihypertensive effect or increase the risk of developing orthostatic hypotension.

Concomitant use of glucocorticoids and tetracosactide with eplerenone may lead to a weakening of the antihypertensive effect (sodium and fluid retention).

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 P-glycoprotein.

The AUC of digoxin when used simultaneously with eplerenone increases by 16%. Caution must be exercised if digoxin is used in doses close to the maximum therapeutic dose.

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 dose.

When eplerenone is used with drugs that inhibit CYP3A4, significant pharmacokinetic interactions are possible. A strong CYP3A4 inhibitor (ketoconazole 200 mg twice daily) caused an increase in eplerenone AUC by 441%. Concomitant use of eplerenone with strong CYP3A4 inhibitors such as ketoconazole, itraconazole, ritonavir, nelfinavir, clarithromycin, telithromycin and nefazodone is contraindicated.

Concomitant use with erythromycin, saquinavir, amiodarone, diltiazem, verapamil and fluconazole was accompanied by significant pharmacokinetic interactions (the degree of increase in AUC ranged from 98% to 187%). When using these drugs simultaneously with eplerenone, the dose of the latter should not exceed 25 mg.

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

Ipleron tab. p.p.o. 25mg N30

Registration Certificate Holder

ESKO PHARMA (Russia)

Dosage form

Medicine - Ipleron® (Ipleron)

Description

Film-coated tablets

Light yellow to light brownish in color, round, biconvex, engraved with "E9RN" on one side and "25" on the other side.

1 tab.

eplerenone 25 mg

Excipients

: lactose monohydrate - 35.7 mg, microcrystalline cellulose - 6.38 mg, microcrystalline cellulose (extragranular) - 9 mg, croscarmellose sodium - 4.25 mg, hypromellose - 2.55 mg, magnesium stearate - 0.43 mg, sodium lauryl sulfate - 0.85 mg, talc - 0.85 mg.

Film shell composition:

opadry yellow 15B220000 (hypromellose - 2.44 mg, polysorbate 80 - 0.04 mg, macrogol - 0.31 mg, titanium dioxide - 0.94 mg, iron dye yellow oxide - 0.1 mg).

10 pieces. - blisters (3) - cardboard packs. 10 pieces. - blisters (6) - cardboard packs.

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 chronic heart failure with reduced left ventricular ejection fraction (<35%).

Contraindications for use

Clinically significant hyperkalemia; serum potassium concentration at the beginning of treatment is more than 5 mmol/l; moderate or severe renal failure (creatinine clearance <30 ml/min in patients with chronic heart failure functional class II according to the NYHA classification); severe liver failure (more than 9 points on the Child-Pugh scale); concomitant use of potassium-sparing diuretics, potassium supplements or strong 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; children and adolescents up to 18 years of age; hypersensitivity to eplerenone.

pharmachologic effect

Potassium-sparing diuretic. Eplerenone has relative selectivity for mineralocorticoid receptors in humans compared to glucocorticoid, progesterone and androgen receptors and prevents their binding to aldosterone, a key hormone of the RAAS, which is involved in the regulation of blood pressure and the pathogenesis of cardiovascular diseases.

Eplerenone causes a persistent increase in plasma renin and serum aldosterone levels. Subsequently, renin secretion is suppressed by aldosterone via a feedback mechanism. However, an increase in renin activity or circulating aldosterone levels does not affect the effects of eplerenone.

In patients with chronic heart failure of functional class II-IV according to the NYHA classification, the addition of eplerenone to standard therapy led to a predicted dose-dependent increase in aldosterone levels. A study examining cardiac and renal function in patients also found a significant increase in aldosterone levels as a result of eplerenone therapy. These data support blockade of mineralocorticoid receptors.

Drug interactions

Cases of lithium toxicity have been described in patients receiving lithium in combination with diuretics and ACE inhibitors. Concomitant use of eplerenone and lithium should be avoided.

Cyclosporine and tacrolimus may cause renal dysfunction and increase the risk of hyperkalemia. Concomitant use of eplerenone and cyclosporine or tacrolimus should be avoided.

Eplerenone should be used with caution with ALP inhibitors or angiotensin II receptor antagonists. Such a combination may lead to an increased risk of developing hyperkalemia, especially in patients with impaired renal function, incl. in older people. It is recommended to carefully monitor renal function and serum potassium concentrations.

Concomitant use of glucocorticoids and tetracosactide with eplerenone may lead to a weakening of the antihypertensive effect (sodium and fluid retention).

The AUC of digoxin when used concomitantly with eplerenone increases by 16%. Caution must be exercised if digoxin is used in doses close to the maximum therapeutic dose.

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 dose.

When eplerenone is used with drugs that inhibit CYP3A4, significant pharmacokinetic interactions are possible. A potent inhibitor of CYP3A4 (ketoconazole 200 mg 2 times / day) caused an increase in eplerenone AUC by 441%. Concomitant use of eplerenone with strong CYP3A4 inhibitors such as ketoconazole, itraconazole, ritonavir, nelfinavir, clarithromycin, telithromycin and nefazodone is contraindicated.

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

Dosage regimen

Taken orally. The initial dose is 25 mg 1 time/day. The dose is increased gradually under the control of potassium levels in the blood. The recommended maintenance dose is 50 mg 1 time/day.

With the simultaneous use of drugs that have a weak or moderate inhibitory effect on CYP3A4, for example, amiodarone, diltiazem and verapamil, fluconazole, erythromycin, saquinavir, the dose of eplerenone should not exceed 25 mg 1 time / day.

Side effect

From the side of metabolism:

often - hyperkalemia; uncommon - dehydration, hypercholesterolemia, hypertriglyceridemia, hyponatremia.

From the nervous system:

often - dizziness; infrequently - headache, insomnia.

From the cardiovascular system:

often - decreased blood pressure; uncommon - atrial fibrillation, myocardial infarction, left ventricular failure, orthostatic hypotension, thrombosis of the arteries of the lower extremities.

From the digestive system:

often - diarrhea, nausea; infrequent - flatulence, vomiting.

From the hematopoietic system:

infrequently - eosinophilia.

From the respiratory system:

infrequently - pharyngitis.

From the skin:

infrequently - increased sweating, itching.

From the musculoskeletal system:

infrequently - back pain, cramps in the calf muscles of the legs.

From the kidneys and urinary tract:

often - renal dysfunction;
infrequently - pyelonephritis. General reactions:
infrequently - asthenia, malaise.

Laboratory indicators:

infrequently - increased levels of residual urea nitrogen, creatinine.

special instructions

Use with caution in patients with type 2 diabetes mellitus and microalbuminuria; simultaneously with ACE inhibitors or angiotensin II receptor antagonists, digoxin and warfarin in doses close to the maximum therapeutic, with lithium, cyclosporine, tacrolimus; in patients with impaired renal function (creatinine clearance <50 ml/min); in elderly patients.

When treated with eplerenone, 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, the concentration of potassium in the blood serum should be monitored. In the future, periodic monitoring of potassium concentration is recommended for patients with an increased risk of developing hyperkalemia, for example, elderly patients with renal failure and diabetes mellitus. Given the increased risk of hyperkalemia, administration of potassium supplements after initiation of eplerenone treatment is not recommended. Reducing the dose of eplerenone leads to a decrease in serum potassium concentration.

In patients with impaired renal function, incl. diabetic microalbuminuria, it is recommended to regularly monitor the concentration of potassium in the blood serum. The risk of developing hyperkalemia increases with decreased renal function. Eplerenone is not removed by hemodialysis.

In patients with mild or moderate liver dysfunction (class A and B 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.

Concomitant use of eplerenone with strong CYP3A4 inducers is not recommended.

During treatment with eplerenone, the use of cyclosporine, tacrolimus, and drugs containing lithium should be avoided.
Effect on the ability to drive vehicles and operate machinery
Eplerenone does not cause drowsiness or impaired cognitive function, but the possibility of dizziness must be taken into account.

Use during pregnancy and breastfeeding

Restrictions during pregnancy - With caution. Restrictions when breastfeeding - Contraindicated.

There is no information on use during pregnancy.
Use with caution and only in cases where the expected benefit to the mother significantly outweighs the possible risk to the fetus/child. It is not known whether eplerenone is excreted into breast milk in humans. If use is necessary during lactation, breastfeeding should be discontinued.