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依普利酮要注意哪些事项呢?

Author: Medicalhalo
Release time: 2025-10-19 11:44:20

Binds to mineralocorticoid receptors, thereby blocking the binding of aldosterone, a component of the renin-angiotensin-aldosterone system (RAAS). Aldosterone synthesis occurs primarily in the adrenal gland and is regulated by multiple factors, including angiotensin II and non-RAAS mediators such as adrenocorticotropic hormone (ACTH) and potassium. Aldosterone binds to mineralocorticoid receptors in epithelial tissues (such as the kidneys) and non-epithelial tissues (such as the heart, blood vessels, and brain) and increases blood pressure by inducing sodium reabsorption and possibly other mechanisms.

What should I pay attention to 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.

Liver damage: Use with caution in patients with moderate to severe liver damage.

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.

Drug-Drug Interactions: Significant interactions may exist requiring dose or frequency adjustment, additional monitoring, and/or selection of alternative therapies.

Potassium Supplements: Avoid potassium supplements, potassium-containing salt substitutes, potassium-rich diets, or other medications that may cause hyperkalemia (e.g., other potassium-sparing diuretics, nonsteroidal anti-inflammatory drugs). Concomitant use of potassium supplements or potassium-sparing diuretics is contraindicated in the treatment of hypertension.

Pregnancy: Untreated hypertension and heart failure are both associated with adverse pregnancy outcomes. The use of mineralocorticoid receptor antagonists is not recommended for the treatment of chronic isolated hypertension in pregnant women and should generally be avoided in women of reproductive potential.

Storage: Store at 25°C (77°F); tolerance allowed 15°C to 30°C (59°F to 86°F).

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