Inspra是什么？

It 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. It has stronger aldosterone antagonism than spironolactone and has extremely low affinity for androgen and progesterone receptors. It 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. 

Inspra side effects

>10%: Endocrine and Metabolic: Hyperkalemia (2-10%), presence of renal dysfunction leading to increased risk of hyperkalemia, hypertension, >5.5 meq/L: 400 mg: 9%; dose ≤200 mg: ≤1%, hypertriglyceridemia (1%-15%; dose related); 1%-10% : Central nervous system: dizziness, fatigue, endocrinology and metabolism: hyponatremia (2%; dose-related), proteinuria, gynecomastia, hypercholesterolemia, gastrointestinal tract: diarrhea, abdominal pain, genitourinary system: abnormal vaginal bleeding (≤2%), mastalgia (men: ≤1%), renal: increased serum creatinine (heart failure, post-myocardial infarction: 6%), respiratory system: cough, flu-like symptoms.

<1%: Post-marketing or case reports: angioedema, increased blood urea nitrogen, increased liver enzymes, increased uric acid, rash, etc.

Notes on Inspra

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 Inspra 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 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, ARBs (one of the first-line treatments for hypertension), and Inspra. 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 Inspra with caution. 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.