| name | Eplerenone |
| classification | Mineralocorticoid Receptor Antagonist |
| pharmacokinetics | | absorption | Well absorbed after oral administration, but bioavailability is variable and can be affected by food. | | distribution | Distributed throughout the body, with concentrations varying among tissues. High levels in the kidney. | | metabolism | Primary metabolism occurs via CYP3A4, therefore drug interactions are possible. | | excretion | Excreted primarily in the urine as metabolites. |
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| suggested dosage | | initial dosage | 50 mg once daily. | | adjustments | The dosage can be increased up to 100 mg once daily, or less frequently. Dosage needs to be individualized based on patient response, tolerability, and renal function. | | comments | Adjust according to patient response and blood pressure, kidney function, and electrolytes. |
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| indications | | 1 | Management of essential hypertension | | 2 | Reduction of cardiovascular events in patients with left ventricular dysfunction after a myocardial infarction. | | 3 | Treatment of primary aldosteronism (Conn's syndrome). |
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| safety in pregnancy | | status | Category C. Should be used only if potential benefits outweigh potential risks. No adequate and well-controlled studies in pregnant women. | | comments | Eplerenone should be used with caution in pregnant women. If used during pregnancy, close monitoring is important. |
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| safety in breastfeeding | | status | Limited data available. Potential for excretion in breast milk. Should be used with caution. | | comments | Caution is advised if breastfeeding. It is best to consult with a healthcare professional for risk assessment. |
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| side effects | | 1 | Hyperkalemia (high potassium levels) | | 2 | Gynecomastia (breast enlargement in males) | | 3 | Fatigue | | 4 | Dizziness | | 5 | Headache | | 6 | Drowsiness | | 7 | Renal impairment | | 8 | Gastrointestinal issues (e.g., nausea, vomiting) | | 9 | Hypotension | | 10 | Cardiac arrhythmias |
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| alternatives | |
| contraindications | | 1 | Severe renal impairment | | 2 | Hyperkalemia (high potassium levels) | | 3 | Known hypersensitivity to eplerenone or related drugs | | 4 | Severe liver dysfunction | | 5 | Concurrent use of potassium-sparing diuretics or potassium supplements |
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| interactions | | 1 | Potassium-sparing diuretics (e.g., amiloride) | | 2 | Potassium supplements | | 3 | ACE inhibitors, ARBs, NSAIDs (potentially increased risk of hyperkalemia) | | 4 | CYP3A4 inhibitors (e.g., ketoconazole, erythromycin) | | 5 | CYP3A4 inducers (e.g. rifampin, St. John's Wort - potentially decreased eplerenone levels) | | 6 | Lithium | | 7 | Other drugs that affect potassium levels |
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| warnings and precautions | | 1 | Regular monitoring of potassium levels is essential, especially during initiation and titration of the dosage. | | 2 | Careful monitoring of renal function is needed | | 3 | Patients with pre-existing kidney disease should be closely monitored | | 4 | Avoid use with concomitant potassium-sparing diuretics and potassium supplements | | 5 | Caution in patients with liver impairment | | 6 | Hypotension may occur | | 7 | Assess baseline electrolytes and renal function before starting therapy. |
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| additional informations | | patient specific considerations | In a 25-year-old male weighing 70 kg, the dosage should be initiated at 50mg and titrated based on response, blood pressure, and electrolytes. Close monitoring of potassium levels is mandatory. | | patient education | The patient should be educated on the importance of following prescribed medication dosage, potential side effects, and the need for regular check-ups, particularly for monitoring potassium levels and kidney function. |
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