Eplerenone (Inspra) is an aldosterone antagonist that was first approved for marketing in the United States in 2002. As a selective mineralocorticoid receptor blocker, this drug holds an important position in the field of cardiovascular disease treatment.

What are the indications for Eplerenone (Inspra)?

Treatment of Heart Failure after Myocardial Infarction

Eplerenone is indicated to improve survival in adult patients with symptomatic heart failure with reduced ejection fraction (HFrEF, ≤40%) following myocardial infarction.

Treatment of Hypertension

(1) The drug is also approved for the treatment of hypertension in adults, and can be used alone or in combination with other antihypertensive drugs.

(2) By lowering blood pressure, it can effectively reduce the risk of fatal and non-fatal cardiovascular events, especially stroke and myocardial infarction.

Contraindications

(1) Patients with type 2 diabetes mellitus complicated with microalbuminuria.

(2) Patients with serum creatinine levels >2.0 mg/dL in males or >1.8 mg/dL in females.

(3) Patients with creatinine clearance <50 mL/min.

(4) Patients taking potassium supplements or potassium-sparing diuretics.

Specifications and Properties of Eplerenone (Inspra)

Drug Specifications

(1) The 25mg tablet is a yellow diamond-shaped biconvex film-coated tablet, engraved with "VLE" on one side and "NSR" over "25" on the other side.

(2) The 50mg tablet is also a yellow diamond-shaped biconvex film-coated tablet, engraved with "VLE" on one side and "NSR" over "50" on the other side.

Physicochemical Properties

(1) The chemical name of eplerenone is Pregn-4-ene-7,21-dicarboxylicacid,9,11-epoxy-17-hydroxy-3-oxo-,γ-lactone,methylester,(7α,11α,17α)-.

(2) Its molecular formula is C₂₄H₃₀O₆ with a molecular weight of 414.50.(3) The substance is an odorless, white to off-white crystalline powder, slightly soluble in water, and its solubility is basically not affected by pH value. At pH 7.0, the octanol/water partition coefficient of eplerenone is approximately 7.1.

Formulation Composition

In addition to the active ingredient eplerenone, eplerenone tablets also contain the following excipients: croscarmellose sodium, hypromellose, lactose monohydrate, magnesium stearate, microcrystalline cellulose, polyethylene glycol, polysorbate 80, red iron oxide, sodium lauryl sulfate, talc, titanium dioxide, and yellow iron oxide.

Storage Methods for Eplerenone (Inspra)

Storage Conditions

(1) Eplerenone tablets should be stored at 25°C (77°F), with allowable fluctuations in the range of 15-30°C (59-86°F).

(2) The medicine must be kept in its original packaging to avoid moisture and light exposure.

Special Requirements

(1) During storage, the medicine should be protected from freezing and high-temperature environments.

(2) The medicine is packaged in bottles of 30 tablets, with NDC codes 58151-142-93 (25mg) and 58151-143-93 (50mg) respectively.

Stability

(1) Proper storage conditions can ensure the stability and efficacy of the medicine throughout its validity period.

(2) Patients should keep the medicine out of the reach of children.

Pre-use Inspection

(1) Before using eplerenone, the appearance of the tablets should be carefully inspected.

(2) A normal 25mg tablet should be yellow and diamond-shaped with corresponding markings.

(3) A normal 50mg tablet should also be yellow and diamond-shaped with corresponding markings.