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    Active Ingredient
    Eplerenone 25 mg, 50 mg

    Status in Israel
    RX

    Presentation and Status in Health Basket

    Presentation Basket Yarpa Pharmasoft

    Film Coated Tablets

    28 X 25 mg

    partial basket chart 65824 9237

    Film Coated Tablets

    28 X 50 mg

    partial basket chart 65825 9238

    Related information


    Dosage

    For the individual adjustment of dose, the strengths of 25 mg and 50 mg are available. The maximum dose regimen is 50 mg daily.
    For post-MI heart failure patients:
    The recommended maintenance dose of eplerenone is 50 mg once daily (OD). Treatment should be initiated at 25 mg once daily and titrated to the target dose of 50 mg once daily preferably within 4 weeks, taking into account the serum potassium level. Eplerenone therapy should usually be started within 3-14 days after an acute MI.
    For patients with NYHA class II (chronic) heart failure:
    For chronic heart failure NYHA class II patients, treatment should be initiated at a dose of 25 mg once daily and titrated to the target dose of 50 mg once daily preferably within 4 weeks; taking into account the serum potassium levelPatients with a serum potassium of > 5.0 mmol/L should not be started on eplerenone. Serum potassium should be measured before initiating eplerenone therapy, within the first week and at one month after the start of treatment or dose adjustment. Serum potassium should be assessed as needed periodically thereafter. After initiation, the dose should be adjusted based on the serum potassium level.
    See prescribing information for full details.
    Patients with a serum potassium of > 5.0 mmol/L should not be started on eplerenone. Serum potassium should be measured before initiating eplerenone therapy, within the first week and at one month after the start of treatment or dose adjustment. Serum potassium should be assessed as needed periodically thereafter.
    See prescribing information for full details.
    Paediatric population: The safety and efficacy of eplerenone in children and adolescents have not been established.
    Elderly: No initial dose adjustment is required in the elderly. Due to an age-related decline in renal function, the risk of hyperkalaemia is increased in elderly patients. This risk may be further increased when co-morbidity associated with increased systemic exposure is also present, in particular mild-to-moderate hepatic impairment. Periodic monitoring of serum potassium is recommended.
    See prescribing information for full details.
    Renal impairment: No initial dose adjustment is required in patients with mild renal impairment. Periodic monitoring of serum potassium with dose adjustment is recommended. Patients with moderate renal impairment (CrCl 30-60 mL /min) should be started at 25 mg every other day, and dose should be adjusted based on the potassium level.
    See prescribing information for full details.
    Periodic monitoring of serum potassium is recommended. There is no experience in patients with CrCl <50 mL /min with post MI heart failure. The use of eplerenone in these patients should be done cautiously. Doses above 25 mg daily have not been studied in patients with CrCl <50 mL/min.
    See prescribing information for full details.


    Indications

    Eplerenone is indicated. In addition to standard therapy including beta-blockers, to reduce the risk of cardiovascular (CV) mortality and morbidity in stable patients with left ventricular dysfunction (LVEF ≤ 40 %) and clinical evidence of heart failure after recent myocardial infarction(MI). In addition to standard optimal therapy, to reduce the risk of CV mortality and morbidity in adult patients with New York Heart Association (NYHA) class II (chronic) heart failure and left ventricular systolic dysfunction (LVEF ≤30%).


    Contra-Indications

    Hypersensitivity to the active substance or to any of the excipients listed in section 6.1. Patients with clinically significant hyperkalemia or with conditions associated with hyperkalemia. Patients with serum potassium level > 5.0 mmol/L at initiation. Patients with severe renal insufficiency (eGFR <30 mL per minute per 1.73 m2). Patients with severe hepatic insufficiency (Child-Pugh Class C). Patients receiving potassium-sparing diuretics, potassium-supplements or strong inhibitors of CYP 3A4 (e.g., itraconazole, ketoconazole, ritonavir, nelfinavir, clarithromycin, telithromycin and nefazodone). The combination of an angiotensin converting enzyme (ACE) inhibitor and an angiotensin receptor blocker (ARB) with eplerenone.


    Special Precautions

    Hyperkalaemia: Consistent with its mechanism of action, hyperkalaemia may occur with eplerenone. Serum potassium levels should be monitored in all patients at initiation of treatment and with a change in dosage. Thereafter, periodic monitoring is recommended especially in patients at risk for the development of hyperkalaemia, such as elderly patients, patients with renal insufficiency and patients with diabetes. The use of potassium supplements after initiation of eplerenone therapy is not recommended, due to an increased risk of hyperkalaemia. Dose reduction of eplerenone has been shown to decrease serum potassium levels. In one study, the addition of hydrochlorothiazide to eplerenone therapy has been shown to offset increases in serum potassium. The risk of hyperkalaemia may increase when eplerenone is used in combination with an ACE inhibitor and/or an ARB. The combination of an ACE inhibitor and an ARB with eplerenone should not be used.
    Impaired renal function:
    Potassium levels should be monitored regularly in patients with impaired renal function, including diabetic microalbuminuria. The risk of hyperkalaemia increases with decreasing renal function. While the data from Eplerenone Post-acute Myocardial Infarction Heart failure Efficacy and Survival Study (EPHESUS) in patients with Type 2 diabetes and microalbuminuria is limited, an increased occurrence of hyperkalaemia was observed in this small number of patients. Therefore, these patients should be treated with caution. Eplerenone is not removed by haemodialysis.
    Impaired hepatic function: No elevations of serum potassium above 5.5 mmol/L were observed in patients with mild to moderate hepatic impairment (Child Pugh class A and B). Electrolyte levels should be monitored in patients with mild to moderate hepatic impairment. The use of eplerenone in patients with severe hepatic impairment has not been evaluated and its use is therefore contraindicated.
    CYP3A4 inducers: Coadministration of eplerenone with strong CYP3A4 inducers is not recommended.
    Lithium, cyclosporin, tacrolimus: should be avoided during treatment with eplerenone.
    Lactose: The tablets contain lactose and should not be administered in patients with rare hereditary problems of galactose intolerance, the Lapp lactase deficiency or glucose-galactose malabsorption.
    Information for Patients: Patients receiving eplerenone should be informed not to use potassium supplements, salt substitutes containing potassium, or contraindicated medications without consulting the prescribing physician.


    Side Effects

    Hyperkalaemia, hypercholesterolaemia, hyponatraemia, dehydration, hypertriglyceridaemia, insomnia, dizziness, syncope, headache, left ventricular failure, atrial fibrillation, rash, pruritus, muscle spasms, back pain, asthenia, blood urea increased, blood creatinine increased.
    See prescribing information for full details.


    Drug interactions

    Pharmacodynamic interactions
    Potassium-sparing diuretics and potassium supplements: Due to increased risk of hyperkalaemia, eplerenone should not be administered to patients receiving other potassium-sparing diuretics and potassium supplements. Potassium-sparing diuretics may also potentiate the effect of anti-hypertensive agents and other diuretics.
    ACE inhibitors, ARBsThe risk of hyperkalaemia may increase when eplerenone is used in combination with an ACE inhibitor and/or an ARB. A close monitoring of serum potassium and renal function is recommended, especially in patients at risk for impaired renal function, e.g., the elderly. The triple combination of an ACE inhibitor and an ARB with eplerenone should not be used.
    LithiumDrug interaction studies of eplerenone have not been conducted with lithium. However, lithium toxicity has been reported in patients receiving lithium concomitantly with diuretics and ACE inhibitors. Coadministration of eplerenone and lithium should be avoided. If this combination appears necessary, lithium plasma concentrations should be monitored.
    Cyclosporin, tacrolimus: Cyclosporin and tacrolimus may lead to impaired renal function and increase the risk of hyperkalaemia. The concomitant use of eplerenone and cyclosporin or tacrolimus should be avoided. If needed, close monitoring of serum potassium and renal function are recommended when cyclosporine and tacrolimus are to be administered during treatment with eplerenone.
    Non-steroidal anti-inflammatory drugs (NSAIDs)Treatment with NSAIDs may lead to acute renal failure by acting directly on glomerular filtration, especially in at-risk patients (elderly and/or dehydrated patients). Patients receiving eplerenone and NSAIDs should be adequately hydrated and be monitored for renal function prior to initiating treatment.
    TrimethoprimThe concomitant administration of trimethoprim with eplerenone increases the risk of hyperkalaemia. Monitoring of serum potassium and renal function should be made, particularly in patients with renal impairment and in the elderly.
    Alpha-1-blockers (e.g. prazosin, alfuzosine)When alpha-1-blockers are combined with eplerenone, there is the potential for increased hypotensive effect and/or postural hypotension. Clinical monitoring for postural hypotension is recommended during alpha-1-blocker co-administration.
    Tricyclic anti-depressants, neuroleptics, amifostine, baclofeneCo-administration of these drugs with eplerenone may potentially increase antihypertensive effects and risk of postural hypotension.
    Glucocorticoids, tetracosactide: Co-administration of these drugs with eplerenone may potentially decrease antihypertensive effects (sodium and fluid retention).
    Pharmacokinetic interactions
    Digoxin: Systemic exposure (AUC) to digoxin increases by 16% (90% CI: 4% – 30%) when co-administered with eplerenone. Caution is warranted when digoxin is dosed near the upper limit of therapeutic range. Mild to moderate CYP3A4 inhibitors: Co-administration with erythromycin, saquinavir, amiodarone, diltiazem, verapamil, and fluconazole have led to significant pharmacokinetic interactions with rank order increases in AUC ranging from 98% to 187%. Eplerenone dosing should therefore not exceed 25 mg when mild to moderate inhibitors of CYP3A4 are co-administered with eplerenone.
    See prescribing information for details.


    Pregnancy and Lactation

    Pregnancy: There are no adequate data on the use of eplerenone in pregnant women.
    Lactation: It is unknown if eplerenone is excreted in human breast milk after oral administration.
    See prescribing information for full details.


    Overdose

    No cases of adverse events associated with overdose of eplerenone in humans have been reported. The most likely manifestation of human overdose would be anticipated to be hypotension or hyperkalaemia. Eplerenone cannot be removed by haemodialysis. Eplerenone has been shown to bind extensively to charcoal. If symptomatic hypotension should occur, supportive treatment should be initiated. If hyperkalaemia develops, standard treatment should be initiated.


    Important notes

    Storage: Store below 25ºC.


    Manufacturer
    Fareva Amboise, Poce-sur-Cisse, France
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