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Eplerenone is a selective aldosterone receptor antagonist that inhibits sodium ion reabsorption and potassium ion excretion by blocking the binding of aldosterone to mineralocorticoid receptors, thereby reducing water and sodium retention, lowering blood pressure, and improving cardiac function.
1. Generic name : Eplerenone (Eplerenone)
2. Trade name : INSPRA®
3. Dosage form :Film-coated tablets
4. Main ingredients :Each tablet contains 25 mg, 50 mg or 100 mg of eplerenone (in the form of ethanesulfonate), and excipients include lactose, microcrystalline cellulose, croscarmellose sodium, hypromellose, etc.
Hypertension : For the treatment of hypertension in adults, it can be used alone or in combination with other antihypertensive drugs.
1. Specifications of : 25mg (yellow diamond-shaped tablets), 50mg (pink diamond-shaped tablets), 100mg (red diamond-shaped tablets).
2. Characteristics of :The tablet surface is printed with a logo (for example, a 25 mg tablet is marked with "PHA1710"), and the content is white to off-white powder.
1. Recommended dose of : The starting dose is 50 mg once a day. If the effect is insufficient after 4 weeks, it can be increased to 50 mg twice a day (maximum dose 100 mg/day).
2. Taking time: There is no need to consider before or after meals.
3. What to do if you miss a dose : There is no need to take the next dose as planned.
1. Hepatic insufficiency : No adjustment is required for mild to moderate (Child-PughA/B), and it is disabled for severe (Child-PughC).
2. Drug interaction : When combined with weak CYP3A4 inhibitors (such as erythromycin), the starting dose should be reduced to 25 mg once a day.
1. Risk of hyperkalemia : Avoid combined use of potassium supplements, potassium-sparing diuretics or strong CYP3A4 inhibitors (such as ketoconazole).
2. Monitoring requirements : Monitor serum potassium every 2 weeks at the beginning of treatment, and once a month after stabilization; check liver and kidney function regularly.
3. Dietary restrictions : Avoid high-potassium diet and potassium-containing salt substitutes.
1. Pregnant women : Contraindicated during pregnancy (animal experiments show fetal toxicity).
2. Lactation : Stop breastfeeding during treatment.
3. Children : Safety has not been established.
4. U200c for the elderly: No dose adjustment is required for those aged ≥65 years.
1. Common (≥1%) : Dizziness (3%), diarrhea (2%), abdominal pain (1%), hyperkalemia (1%).
2. Severe reactions : Hyperkalemia (serum potassium>5.5meq/L), abnormal liver function (ALT>3 times ULN).
1. Serum potassium>5.5meq/L;
2. Type 2 diabetes combined with microalbuminuria;
3. Severe renal insufficiency (Cr>2.0mg/dL for men, Cr>1.8mg/dL for women);
4. Combined use of strong CYP3A4 inhibitors or potassium-sparing diuretics.
1. CYP3A4 inhibitor (such as ketoconazole): increases the plasma concentration of eplerenone by 5.4 times and is prohibited from combined use;
2. ACEI/ARB antihypertensive drug :increases the risk of hyperkalemia and requires close monitoring;
3. NSAIDs :may weaken the antihypertensive effect and aggravate kidney damage.
Unopened tablets should be stored in a dark place below 25°C (77°F). Short-term storage at 15-30°C is allowed.
Note : If muscle weakness, arrhythmia, or persistent nausea and vomiting occur during treatment, you should seek medical attention immediately to evaluate blood potassium levels. Smoking may reduce the efficacy of the drug, so it is recommended to quit smoking.