Inspra®
GoodRxEplerenone · oral tablet
Misc.
OFF-LABELNot in the FDA label for this product
Chronic central serous chorioretinopathy
25 mg orally once daily for 1 week, then 50 mg once daily, in the trial regimen
RCT · n=114 · no benefit
VICI randomised 114 patients with treatment-naive chronic CSCR of 4 months or more to eplerenone or placebo for up to 12 months. Mean best-corrected visual acuity at 12 months was 80.4 letters on eplerenone against 79.5 on placebo, a difference of 1.73 letters (95% CI -1.12 to 4.57, p=0.24). The authors concluded that ophthalmologists who currently prescribe eplerenone for chronic CSCR should discontinue this practice. Hyperkalaemia occurred in 8 patients (14%) in each group.
Chronic central serous chorioretinopathy, compared with photodynamic therapy
Oral eplerenone for 12 weeks, against a single indocyanine green-guided half-dose PDT session
RCT · n=107 · PDT clears more
SPECTRA randomised 107 patients to half-dose PDT or oral eplerenone in an open-label trial, eplerenone given for 12 weeks. At 3 months, subretinal fluid had resolved completely in 78% of the PDT group against 17% of the eplerenone group (p<0.001). Visual acuity did not differ (83.7 letters against 82.8, p=0.555), though retinal sensitivity on microperimetry modestly favoured PDT (25.4 against 23.9 dB, p=0.041). Adverse events occurred in 3 patients (6%) on PDT and 18 (33%) on eplerenone.
Contraindications
- Serum potassium >5.5 mEq/L at initiation
- Creatinine clearance ≤30 mL/min
- Concomitant administration of strong CYP3A inhibitors (e.g., ketoconazole, itraconazole, nefazodone, troleandomycin, clarithromycin, ritonavir, and nelfinavir)
Available Forms25 mg, 50 mg
Mechanism of ActionEplerenone binds to the mineralocorticoid receptor and blocks the binding of aldosterone, a component of the renin-angiotensin-aldosterone-system (RAAS). Aldosterone synthesis, which occurs primarily in the adrenal gland, is modulated by multiple factors, including angiotensin II and non-RAAS mediators such as adrenocorticotropic hormone (ACTH) and potassium. Aldosterone binds to mineralocorticoid receptors in both epithelial (e.g., kidney) and nonepithelial (e.g., heart, blood vessels, and brain) tissues and increases blood pressure through induction of sodium reabsorption and possibly other mechanisms.
Warnings & Precautions
Hyperkalemia: Patients with decreased renal function, diabetes, proteinuria or patients who are taking ACEs and ARBs, NSAIDs or moderate CYP3A inhibitors are at increased risk. Monitor serum potassium levels and adjust dose as needed.
Common Side Effects
The most common reasons for discontinuation of INSPRA were headache, dizziness, angina pectoris/MI, and increased GGT.
Pregnancy & LactationPregnancy: The available data from published case reports on eplerenone use during pregnancy are insufficient to establish a drug-associated risk of major birth defects, miscarriage, adverse maternal or fetal outcomes .
Lactation: There are no human data available on whether eplerenone is present in human milk, or has effects on breastfed infants or on milk production. Eplerenone was present in the milk of lactating rats.
Pediatric UseThe safety and effectiveness of INSPRA for treatment of hypertension have not been established in pediatric patients. In a 10-week study of 304 hypertensive pediatric patients ages 4 to 16 years treated with INSPRA up to 100 mg per day, doses that produced exposure similar to that in adults, INSPRA did not lower blood pressure.