依普利酮(Eplerenone)的功效与作用

Eplerenone developed by Pfizer, as a new selective aldosterone receptor antagonist, has important value in the treatment of cardiovascular diseases.

Indications of Eplerenone

It was first approved for marketing in the United States in 2002 and is mainly used in two types of clinical situations:

1. To improve the survival rate of heart failure patients with reduced ejection fraction (HFrEF) after acute myocardial infarction (MI).

2. Treatment of hypertension in adults to lower blood pressure and reduce the risk of cardiovascular events.

The above content only reflects the scope of indications of eplerenone in overseas registration countries, does not represent the scope of approved use in mainland China, and cannot be used as any treatment decision.

The pictures come from public channels (such as the official website of the FDA, the official website of the original drug manufacturer, etc.) and are for reference only.

Efficacy and effects of Eplerenone

1. Using its high selectivity for aldosterone receptors and its antagonism to aldosterone, eplerenone can effectively reduce the effect of aldosterone, thereby achieving its therapeutic effect on hypertension.

2. By blocking the action of aldosterone, eplerenone can reduce sodium reabsorption, lower blood pressure, and has anti-fibrosis and anti-inflammatory effects.

3. In addition, it can also increase plasma renin and aldosterone levels, but this feedback increase does not weaken its therapeutic effect.

Clinical application and dosage regimen of Eplerenone

1. Heart failure after myocardial infarction

(1) Medication dosage

According to the patient's tolerance, the initial dose of 25 mg once a day can be gradually increased to 50 mg a day, with a cycle of 4 weeks, until a stable therapeutic effect is achieved.

(2) Dose adjustment

The drug dosage should be adjusted appropriately according to the patient's blood potassium level, and the treatment process should also be closely monitored to prevent adverse reactions caused by fluctuations in blood potassium.

2. Hypertension

(1) Starting dose

Based on the actual needs of the patient, it is usually recommended to start with a starting dose of 50 mg per day.

(2) Increase the dose

According to the control of blood pressure, the daily tablet dose can be increased from the original 80 mg once a day to 50 mg twice a day (i.e. the total daily dose is 100 mg).

Recommendations for the use of eplerenone in special populations

1. Elderly patients

Due to decreased renal function in elderly patients, the risk of hyperkalemia increases after using eplerenone, and they need to be used with caution and strengthened monitoring.

2. Pregnancy and lactation

Currently there is a lack of sufficient data on the use of eplerenone in pregnant women. Animal experiments have not found teratogenicity, but it should still be used after weighing the pros and cons. It is unknown whether it is excreted in breast milk and should be avoided by breastfeeding women.

3. Children and Adolescents

However, because its effect on hypertension in children is not obvious, it is not recommended for people under the age of 18.

4. Patients with hepatic insufficiency

Patients with moderate hepatic insufficiency need to use eplerenone with caution as it may increase drug exposure.