依普利酮治疗期间要注意什么?
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 during treatment with eplerenone?
1. Hyperkalemia: Hyperkalemia may occur; the risk of hyperkalemia increases with renal impairment, proteinuria, diabetes, and patients taking concurrent ACE (angiotensin-converting enzyme) inhibitors, angiotensin II inhibitors, nonsteroidal anti-inflammatory drugs, 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.
2. Diabetes: Use with caution in patients with diabetes and heart failure after myocardial infarction (especially those with proteinuria); the risk of hyperkalemia is increased.
3. Heart failure: When evaluating patients with heart failure to receive eplerenone treatment, the eGFR (epidermal growth factor receptor) should be greater than 30ml/min/1.73m2 or the creatinine should be less than or equal to 2.5mg/dL (men) or less than or equal to 2mg/dL (women) with no recent deterioration, 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.
4. Liver damage: Patients with moderate to severe liver damage should use eplerenone with caution.
5. Kidney damage: As kidney function declines, 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.
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