依普利酮(Eplerenone)的不良反应及禁忌症

Eplerenone, trade name: INSPRA. It is mainly used to treat heart failure after acute myocardial infarction and hypertension in adults. There are also certain adverse reactions and strict contraindications during use. It should be used rationally under the guidance of a doctor.

Main adverse reactions of Eplerenone

1. Hyperkalemia

(1) Hyperkalemia is the most common adverse reaction of Eplerenone and requires great attention. Especially among high-risk groups, such as patients with renal insufficiency and diabetes.

(2), or patients who concurrently use angiotensin-converting enzyme inhibitors, angiotensin II receptor antagonists, nonsteroidal anti-inflammatory drugs, or moderate CYP3A inhibitors, the risk of hyperkalemia is further increased.

2. Increased creatinine

Some patients may experience an increase in serum creatinine levels after taking eplerenone.

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.

Other common adverse reactions of Eplerenone

Other common adverse reactions

(1) In patients with heart failure after myocardial infarction, except for hyperkalemia and increased creatinine, the overall incidence of adverse reactions is similar to that of placebo.

(2). The rate of discontinuation due to adverse reactions is low. Common reasons include hyperkalemia and abnormal renal function.

(3) In patients with hypertension, the adverse reactions of eplerenone are relatively rare.

(4) Adverse reactions that may lead to discontinuation include headache, dizziness, angina or myocardial infarction, and elevated gamma-glutamyl transferase (GGT).

Rare adverse reactions of Eplerenone

1. Angioedema and rash

(1). According to post-marketing surveillance, a very small number of patients may develop angioedema and rash.

(2). Since these reactions are reported voluntarily and the size of the population is uncertain, their specific frequency of occurrence is not yet clear.

2. Gender-related adverse reactions

Long-term use of eplerenone may cause gynecomastia and abnormal vaginal bleeding in women, and the incidence increases with the duration of medication.

Contraindications of Eplerenone

The use of Eplerenone is prohibited under the following circumstances:

1. The serum potassium level at the beginning of treatment is higher than 5.5mEq/L.

2. Creatinine clearance ≤30mL/min.

3. Use strong CYP3A inhibitors at the same time, such as ketoconazole, itraconazole, nefazodone, troleandomycin, clarithromycin, ritonavir or nelfinavir.

Additional contraindications for patients with hypertension

For patients with hypertension, the following conditions are also contraindications:

1. People with type 2 diabetes and microalbuminuria.

2. Serum creatinine in men is >2.0mg/dL or in women is >1.8mg/dL.

3. Creatinine clearance rate <50mL/min.

4. Use potassium supplements or potassium-sparing diuretics at the same time, such as amiloride, spironolactone or triamterene.

Eplerenone is an effective cardiovascular treatment drug. During its use, the contraindications must be strictly followed, and serum potassium and renal function must be regularly monitored during the medication. Particularly, caution should be exercised in high-risk patients. Patients should not take potassium supplements or potassium-containing salt substitutes on their own, and should seek immediate medical attention if they experience any symptoms.