依普利酮是一种什么药物？

What kind of drug is it? Eplerenone is a new type of selective aldosterone receptor antagonist. It was approved for clinical use by the State Food and Drug Administration in 2002. The pure product is white or off-white crystal. Its antagonistic effect on aldosterone is stronger than that of spironolactone. It has extremely low affinity for androgen and progesterone receptors and has few adverse reactions. It has definite efficacy in the treatment of hypertension, heart failure and myocardial infarction. It has fewer adverse reactions and good tolerance. It is a good alternative drug to spironolactone. 

In a study of systolic hypertension in the elderly, 269 patients were treated with eplerenone (50-200) mg daily and amlodipine (2.5-10) mg daily. The results showed that both drugs had the same effect in lowering systolic blood pressure, while amlodipine lowered diastolic blood pressure more significantly. In terms of target organ protection, both drugs improved carotid-femoral and carotid-radial pulse rates after 24 weeks of treatment. In terms of the incidence of adverse reactions, 19.9% ​​of the amlodipine group developed peripheral edema, while only 2.7% of the eplerenone group developed hyperkalemia. 0.4% of the amlodipine group developed hyperkalemia, and 0.9% of the eplerenone group developed hyperkalemia.

Things to note when taking eplerenone

Hyperkalemia: Hyperkalemia may occur; the risk of hyperkalemia is increased with renal impairment, proteinuria, diabetes mellitus, and in patients concurrently taking ACE (angiotensin-converting enzyme) inhibitors, angiotensin II inhibitors, NSAIDs, or moderate CYP3A inhibitors. Monitor closely for hyperkalemia; serum potassium increased dose-related during clinical trials. As hyperkalemia develops, dose reduction or treatment interruption may be necessary. If concomitant treatment with a moderate CYP3A4 inhibitor cannot be avoided, reduce the eplerenone dose. It is contraindicated in patients with potassium greater than 5.5 meq/L at the beginning of treatment. 

Diabetes: Use with caution in patients with diabetes and post-myocardial infarction heart failure (especially those with proteinuria); the risk of hyperkalemia is increased.

  Heart failure: When evaluating patients with heart failure to receive eplerenone treatment, eGFR (epidermal growth factor receptor) should be greater than 30ml/min/1.73m2 or creatinine should be less than or equal to 2.5mg/dL (men) or less than or equal to 2mg/dL (women) with no recent worsening, potassium less than 5meq/L and no history of severe hyperkalemia. If blood potassium levels are elevated, close monitoring and management are required. The manufacturer recommends that treatment should be discontinued if serum potassium is >6 meq/L. ACCF/AHA (American College of Cardiology Foundation) recommends that when serum potassium concentration is >5.5 meq/L or renal function worsens, discontinuation of the drug should be considered and the entire medical regimen should be carefully evaluated. Avoid conventional triple therapy and use a combination of ACE (angiotensin-converting enzyme) inhibitors, ARB (one of the first-line treatments for hypertension) and eplerenone. Instruct patients with heart failure to discontinue use during episodes of diarrhea or dehydration or when circulating diuretic therapy is interrupted. 

Hepatic Impairment: Use eplerenone with caution in patients with moderate to severe hepatic impairment. Kidney Impairment: As kidney function decreases, the risk of hyperkalemia increases. Use with caution in patients with mild renal impairment; it may be disabled depending on the indications and degree of damage.