依普利酮（Inspra）注意事项

Eplerenone (Inspra) lowers blood pressure by binding to aldosterone receptors and blocking aldosterone in the renin-angiotensin-aldosterone system (RAAS).

Eplerenone (Inspra) for the treatment of congestive heart failure after acute myocardial infarction: the recommended dose is 50 mg/time, once/day. The initial dose should be 25 mg/time, once/day, and within 4 weeks, the dose should be gradually increased to 50 mg/time, once/day as tolerated by the patient within 4 weeks. The average time to peak efficacy of eplerenone (Inspra) after oral administration is approximately 1.5 hours. Peak concentration (Cmax) and T area of ​​the curve (AUC) increase in proportion to the dose within the dose range of 25 to 100 mg. When the dose exceeds 100 mg, AUC becomes inversely proportional to the dose. The plasma protein binding rate of eplerenone (Inspra) is approximately 50%, and it binds mainly to α1, acid glycoprotein. In healthy volunteers and hypertensive patients, the apparent volume of distribution ranges from 43 to 90 L at steady state. Eplerenone (Inspra) is metabolized primarily by the CYP3A4 enzyme. No active metabolite can be detected in human serum, and about 5% of unmetabolized product can be detected in urine and feces.

Precautions for patients using eplerenone (Inspra):

(1) Eplerenone (Inspra) cannot be combined with potassium supplements, potassium-containing salts or contraindicated drugs (potassium-sparing diuretics, strong inhibitors of CYP450 liver enzymes). (2) Non-steroidal anti-inflammatory drugs and lithium can affect the blood concentration of this product and affect its efficacy. (3) Patients with high serum potassium, type 2 diabetes patients with microalbuminuria, patients with excessive serum creatinine levels, and patients with muscle intoxication clearance <50 mL/min should not take eplerenone (Inspra). (4) Pregnant women, children, and those with hepatic insufficiency, chronic cardiac insufficiency, and renal insufficiency should use with caution.