Eplerenone is a selective aldosterone receptor antagonist. It inhibits sodium ion reabsorption and potassium ion excretion by blocking the combination of aldosterone and mineralocorticoid receptor, thereby reducing water and sodium retention, lowering blood pressure, and improving cardiac function.

1、 Drug name and main ingredients

1. Common name: Eplerenone

2. Product Name: INSPRA ®

3. Dosage form: Film coated tablets

4. Main ingredients: Each tablet contains 25mg, 50mg, or 100mg of eplerenone (in the form of ethanesulfonate), and excipients include lactose, microcrystalline cellulose, cross-linked carboxymethyl cellulose sodium, hydroxypropyl methylcellulose, etc.

2、 Indications

Hypertension: Used for the treatment of adult hypertension, it can be used alone or in combination with other antihypertensive drugs.

3、 Specifications and characteristics

1. Specifications: 25mg (yellow diamond shaped tablet), 50mg (pink diamond shaped tablet), 100mg (red diamond shaped tablet).

2. Appearance: The surface of the tablet is marked with a label (such as "PHA1710" on a 25mg tablet), and the content is a white to off white powder.

4、 Usage and dosage

1. Recommended dosage: The initial dose is 50mg once daily, and if the therapeutic effect is insufficient after 4 weeks, it can be increased to 50mg twice daily (maximum dose is 100mg/day).

2. Dosage: No need to consider before or after meals.

3. Omission treatment: No need for replenishment, take the next dose according to the original plan.

5、 Dose adjustment

1. Liver dysfunction: Mild to moderate (Child Pugh A/B) does not require adjustment, severe (Child Pugh C) is contraindicated.

2. Drug interactions: When combined with weak CYP3A4 inhibitors (such as erythromycin), the initial dose should be reduced to 25mg once daily.

6、 Medication precautions

1. Risk of hyperkalemia: Avoid using potassium supplements, potassium sparing diuretics, or strong CYP3A4 inhibitors (such as ketoconazole) in combination.

2. Monitoring requirements: Blood potassium should be monitored every 2 weeks during the initial stage of treatment, and once a month after stabilization; Regularly check liver and kidney function.

3. Dietary restrictions: Avoid high potassium diets and potassium substitutes.

7、 Medication for special populations

1. Pregnant women: Prohibited during pregnancy (animal experiments show fetal toxicity).

2. Breastfeeding period: Stop breastfeeding during the treatment period.

3. Children: Safety has not been established.

4. Elderly individuals aged 65 and above do not need to adjust their dosage.

8、 Adverse reactions

1. Common (≥ 1%): Dizziness (3%), Diarrhea (2%), Abdominal Pain (1%), Hyperkalemia (1%).

2. Serious reactions: Hyperkalemia (serum potassium>5.5 meq/L), abnormal liver function (ALT>3 times ULN).

9、 Contraindications

1. Serum potassium>5.5 meq/L;

2. Type 2 diabetes with microalbuminuria;

3. Severe renal insufficiency (male Cr>2.0mg/dL, female Cr>1.8mg/dL);

4. Combination use of strong CYP3A4 inhibitors or potassium sparing diuretics.

10、 Drug interactions

1. CYP3A4 inhibitors (such as ketoconazole): increase the blood concentration of eplerenone by 5.4 times and prohibit combination use;

2. ACEI/ARB antihypertensive drugs: increase the risk of hyperkalemia and require close monitoring;

3. NSAIDs: May weaken blood pressure lowering effects and worsen kidney damage.

11、 Storage method

Unopened tablets should be stored in the dark below 25 ° C (77 ° F), and short-term storage at 15-30 ° C is allowed.

Note: If muscle weakness, arrhythmia, or persistent nausea and vomiting occur during treatment, immediate medical attention should be sought to assess blood potassium levels. Smoking may reduce the effectiveness of medication, it is recommended to quit smoking.

Eplerenoneinformation