Heart failure:
Note: When initiating therapy, verify the following: serum potassium <5 mEq/L and either serum creatinine ≤2.5 mg/dL in men and ≤2 mg/dL in women or eGFR >30 mL/minute/1.73 m2. If patient develops hyperkalemia or kidney function worsens, reduce the dose, change to every-other-day dosing, or discontinue therapy; assess for other causes of hyperkalemia before permanent discontinuation. If serum potassium cannot be maintained <5.5 mEq/L, discontinue therapy (ACC [Maddox 2021]; AHA/ACC/HFSA [Heidenreich 2022]).
Heart failure with preserved ejection fraction (off-label use):
Note: For use in patients with symptomatic heart failure with preserved ejection fraction (HFpEF) (≥50%) who have an elevated serum natriuretic peptide level or have been hospitalized for heart failure in the last 12 months (AHA/ACC/HFSA [Heidenreich 2022]). Some experts are more conservative regarding serum potassium for patients with HFpEF. They recommend initiating therapy or up-titrating the dose only if serum potassium is ≤4.7 mEq/L and eGFR is ≥30 mL/minute/1.73 m2. They recommend dose reduction or discontinuation if serum potassium is >5 mEq/L (Borlaug 2022).
Oral: Initial: 25 mg once daily; may double the dose after 4 weeks if serum potassium and kidney function are stable, to a maximum target dose of 50 mg once daily (AHA/ACC/HFSA [Heidenreich 2022]; Borlaug 2022).
Heart failure with reduced ejection fraction (off-label use):
Note: Should be considered for use in patients with symptomatic (New York Heart Association class II to IV) heart failure with reduced ejection fraction (HFrEF) (≤40%) as part of an optimal medical regimen for HFrEF (AHA/ACC/HFSA [Heidenreich 2022]).
Oral: Initial: 25 mg once daily; may double the dose after 4 weeks if serum potassium and kidney function are stable, to a maximum target dose of 50 mg once daily (AHA/ACC/HFSA [Heidenreich 2022]; Zannad 2011).
Post myocardial infarction, complicated by reduced ejection fraction:
Note: Should be considered for use following acute myocardial infarction in patients with left ventricular ejection fraction ≤40% plus symptoms of heart failure or diabetes. Use in addition to other pharmacologic therapies (AHA/ACC/HFSA [Heidenreich 2022]).
Oral: Initial: 25 mg once daily; may double the dose after 4 weeks if serum potassium and kidney function are stable, up to a maximum target dose of 50 mg once daily.
Hypertension, chronic (alternative agent):
Note: Not recommended for initial management but may be considered as additional therapy for resistant hypertension in patients who do not respond adequately to combination therapy with preferred agents (ACC/AHA [Whelton 2018]; Bazoukis 2018).
Oral: Initial: 50 mg once daily; evaluate response after ~2 to 4 weeks and titrate dose, as needed, to a maximum of 50 mg twice daily. Twice daily dosing is usually required for adequate BP lowering. Patients with severe asymptomatic hypertension and no signs of acute end organ damage should be evaluated for medication titration within 1 week (ACC/AHA [Whelton 2018]; Bazoukis 2018; Mann 2021).
Primary aldosteronism (alternative agent) (off-label use):
Note: Alternative to spironolactone (ES [Funder 2016]).
Oral: Initial: 25 mg twice daily; gradually titrate to the lowest effective dose; usual maximum dose: 300 mg/day. For surgical candidates, the last dose should be administered the day of surgery; discontinue eplerenone on postoperative day one (ES [Funder 2016]; Parthasarathy 2011).
Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.
Heart failure:
eGFR ≥50 mL/minute/1.73 m2: No initial dose adjustment necessary.
eGFR 31 to 49 mL/minute/1.73 m2: Initial: 25 mg every other day; may double the dose after 4 weeks if serum potassium and kidney function are stable, up to a maximum target dose of 25 mg once daily (ACCF/AHA [Yancy 2013]).
eGFR ≤30 mL/minute/1.73 m2: Not recommended (ACCF/AHA [Yancy 2013]).
Hemodialysis: Not removed by hemodialysis.
Hypertension, chronic (alternative agent):
CrCl ≥50 mL/minute: There are no dosage adjustments provided in the manufacturer's labeling.
CrCl <50 mL/minute or serum creatinine >2 mg/dL (males) or >1.8 mg/dL (females): Use is contraindicated.
There are no dosage adjustments provided in the manufacturer's labeling. Systemic exposure is increased in moderate hepatic impairment (Child-Pugh class B).
Refer to adult dosing.
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Tablet, Oral:
Inspra: 25 mg, 50 mg
Generic: 25 mg, 50 mg
Yes
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Tablet, Oral:
Inspra: 25 mg, 50 mg [contains polysorbate 80]
Generic: 25 mg, 50 mg
Oral: Administer with or without food.
Hypertension, chronic: Management of hypertension. Note: Not recommended for the initial treatment of hypertension (ACC/AHA [Whelton 2018]).
Post myocardial infarction, complicated by heart failure with reduced ejection fraction: To improve survival of stable patients with symptomatic heart failure (left ventricular ejection fraction ≤40%) following acute myocardial infarction.
Heart failure with preserved ejection fraction; Heart failure with reduced ejection fraction; Primary aldosteronism
Beers Criteria: Diuretics (eplerenone) are identified in the Beers Criteria as potentially inappropriate medications to be used with caution in patients 65 years and older due to the potential to cause or exacerbate syndrome of inappropriate antidiuretic hormone secretion (SIADH) or hyponatremia; monitor sodium concentration closely when initiating or adjusting the dose in older adults (Beers Criteria [AGS 2019]).
Inspra may be confused with Spiriva
Eplerenone can cause reversible hyperkalemia; however, if potassium is monitored periodically and with suspected changes in electrolytes (vomiting, diarrhea), the risk does not appear to translate into a higher risk of hospitalization or death (Ref).
Mechanism: Dose-related; related to the pharmacologic action. Competes with aldosterone for binding to the mineralocorticoid receptor, thereby inhibiting the exchange of sodium for potassium in the distal convoluted renal tubule and preventing potassium excretion (Ref).
Onset: Intermediate; usually occurs within 4 weeks of initiation or dose titration (Ref).
Risk factors:
• Doses >100 mg daily (Ref)
• Older patients (≥75 years of age) (Ref)
• Diabetes (Ref)
• Kidney impairment (Ref)
• Excessive potassium intake (eg, potassium supplements, potassium-containing salt substitutes)
• Concomitant use of certain medications (eg, angiotensin-converting enzyme inhibitors, angiotensin-receptor blockers, sacubitril/valsartan, nonsteroidal anti-inflammatory drugs, moderate CYP3A inhibitors)
• Baseline serum potassium >4.3 mEq/L (Ref)
• Prior use of antiarrhythmic agents (Ref)
• Proteinuria
The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified.
>10%: Endocrine & metabolic: Hyperkalemia (cardiac failure, post-myocardial infarction: 3%; >5.5 mEq/L: 16%; ≥6 mEq/L: 6%) (table 1)
|
Drug (Eplerenone) |
Placebo |
Indication |
Number of Patients (Eplerenone) |
Number of Patients (Placebo) |
Comments |
|---|---|---|---|---|---|
|
16% |
11% |
Cardiac failure, post-myocardial infarction |
3251 |
3237 |
>5.5 mEq/L |
|
6% |
4% |
Cardiac failure, post-myocardial infarction |
3251 |
3237 |
≥6 mEq/L |
|
3% |
2% |
Cardiac failure, post-myocardial infarction |
3307 |
3301 |
N/A |
1% to 10%: Renal: Increased serum creatinine (cardiac failure, post-myocardial infarction: 2% to 7%)
Frequency not defined:
Cardiovascular: Acute myocardial infarction, angina pectoris
Endocrine & metabolic: Gynecomastia, increased gamma-glutamyl transferase
Genitourinary: Abnormal vaginal hemorrhage
Nervous system: Dizziness, headache
Renal: Renal insufficiency
Postmarketing:
Dermatologic: Skin rash
Hypersensitivity: Angioedema
Serum potassium >5.5 mEq/L at initiation; CrCl ≤30 mL/minute; concomitant use of strong CYP3A4 inhibitors (eg, ketoconazole, itraconazole, nefazodone, troleandomycin, clarithromycin, ritonavir, nelfinavir).
The following additional contraindications apply to patients with hypertension: Type 2 diabetes mellitus (noninsulin dependent, NIDDM) with microalbuminuria; serum creatinine >2.0 mg/dL in males or >1.8 mg/dL in females; CrCl <50 mL/minute; concomitant use with potassium supplements or potassium-sparing diuretics (eg, amiloride, spironolactone, triamterene).
Per the Endocrine Society clinical practice guidelines, use in patients with Addison disease is contraindicated (Endocrine Society [Bornstein 2016])
Canadian labeling: Additional contraindications (not in US labeling): Hypersensitivity to eplerenone or any component of the formulation; serum potassium >5 mEq/L at initiation; severe hepatic impairment (Child-Pugh class C); clinically significant hyperkalemia; concomitant use with potassium supplements or potassium-sparing diuretics
The following additional contraindications apply to patients with hypertension: Serum creatinine >1.5 mg/dL [132 micromole/L] in males or >1.3 mg/dL [115 micromole/L] in females
Disease-related concerns:
• Heart failure: When evaluating a heart failure patient for eplerenone treatment, eGFR should be >30 mL/minute/1.73 m2 or creatinine should be ≤2.5 mg/dL (men) or ≤2 mg/dL (women) with no recent worsening and potassium should be <5 mEq/L with no history of severe hyperkalemia. Discontinue therapy if serum potassium cannot be maintained <5.5 mEq/L or if kidney function worsens. Consider the entire medical regimen and other potential causes of hyperkalemia AHA/ACC/HFSA [Heidenreich 2022]).
• Hepatic impairment: Use with caution in patients with moderate to severe hepatic impairment.
• Kidney impairment: Use with caution in patients with mild kidney impairment; based on indication and degree of impairment, use may be contraindicated (refer to "Contraindications").
Substrate of CYP3A4 (major); Note: Assignment of Major/Minor substrate status based on clinically relevant drug interaction potential
Note: Interacting drugs may not be individually listed below if they are part of a group interaction (eg, individual drugs within “CYP3A4 Inducers [Strong]” are NOT listed). For a complete list of drug interactions by individual drug name and detailed management recommendations, use the Lexicomp drug interactions program by clicking on the “Launch drug interactions program” link above.
Alfuzosin: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Risk C: Monitor therapy
Amifostine: Blood Pressure Lowering Agents may enhance the hypotensive effect of Amifostine. Management: When used at chemotherapy doses, hold blood pressure lowering medications for 24 hours before amifostine administration. If blood pressure lowering therapy cannot be held, do not administer amifostine. Use caution with radiotherapy doses of amifostine. Risk D: Consider therapy modification
Ammonium Chloride: Potassium-Sparing Diuretics may enhance the adverse/toxic effect of Ammonium Chloride. Specifically the risk of systemic acidosis. Risk C: Monitor therapy
Amphetamines: May diminish the antihypertensive effect of Antihypertensive Agents. Risk C: Monitor therapy
Angiotensin II Receptor Blockers: Eplerenone may enhance the hyperkalemic effect of Angiotensin II Receptor Blockers. Risk C: Monitor therapy
Angiotensin-Converting Enzyme Inhibitors: Eplerenone may enhance the hyperkalemic effect of Angiotensin-Converting Enzyme Inhibitors. Risk C: Monitor therapy
Antipsychotic Agents (Second Generation [Atypical]): Blood Pressure Lowering Agents may enhance the hypotensive effect of Antipsychotic Agents (Second Generation [Atypical]). Risk C: Monitor therapy
Barbiturates: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Risk C: Monitor therapy
Benperidol: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Risk C: Monitor therapy
Brigatinib: May diminish the antihypertensive effect of Antihypertensive Agents. Brigatinib may enhance the bradycardic effect of Antihypertensive Agents. Risk C: Monitor therapy
Brimonidine (Topical): May enhance the hypotensive effect of Blood Pressure Lowering Agents. Risk C: Monitor therapy
Bromperidol: May diminish the hypotensive effect of Blood Pressure Lowering Agents. Blood Pressure Lowering Agents may enhance the hypotensive effect of Bromperidol. Risk X: Avoid combination
Cardiac Glycosides: Potassium-Sparing Diuretics may diminish the therapeutic effect of Cardiac Glycosides. In particular, the inotropic effects of digoxin appear to be diminished. Potassium-Sparing Diuretics may increase the serum concentration of Cardiac Glycosides. This particular effect may be unique to Spironolactone. Risk C: Monitor therapy
Clofazimine: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Risk C: Monitor therapy
CycloSPORINE (Systemic): Eplerenone may enhance the hyperkalemic effect of CycloSPORINE (Systemic). Risk X: Avoid combination
CYP3A4 Inducers (Strong): May decrease the serum concentration of Eplerenone. Risk C: Monitor therapy
CYP3A4 Inhibitors (Moderate): May increase the serum concentration of Eplerenone. Management: If coadministered with moderate CYP3A4 inhibitors, the max dose of eplerenone is 25 mg daily if used for heart failure; if used for hypertension initiate eplerenone 25 mg daily, titrate to max 25 mg twice daily. Risk D: Consider therapy modification
CYP3A4 Inhibitors (Strong): May increase the serum concentration of Eplerenone. Risk X: Avoid combination
Desmopressin: Hyponatremia-Associated Agents may enhance the hyponatremic effect of Desmopressin. Risk C: Monitor therapy
Dexmethylphenidate: May diminish the therapeutic effect of Antihypertensive Agents. Risk C: Monitor therapy
Diacerein: May enhance the therapeutic effect of Diuretics. Specifically, the risk for dehydration or hypokalemia may be increased. Risk C: Monitor therapy
Diazoxide: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Risk C: Monitor therapy
Drospirenone-Containing Products: May enhance the hyperkalemic effect of Potassium-Sparing Diuretics. Risk C: Monitor therapy
DULoxetine: Blood Pressure Lowering Agents may enhance the hypotensive effect of DULoxetine. Risk C: Monitor therapy
Fexinidazole: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Risk X: Avoid combination
Finerenone: Potassium-Sparing Diuretics may enhance the hyperkalemic effect of Finerenone. Risk C: Monitor therapy
Fludrocortisone: May diminish the therapeutic effect of Mineralocorticoid (Aldosterone) Receptor Antagonists. Mineralocorticoid (Aldosterone) Receptor Antagonists may diminish the therapeutic effect of Fludrocortisone. Risk C: Monitor therapy
Flunarizine: May enhance the therapeutic effect of Antihypertensive Agents. Risk C: Monitor therapy
Fusidic Acid (Systemic): May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Risk X: Avoid combination
Heparin: May enhance the hyperkalemic effect of Eplerenone. Risk C: Monitor therapy
Heparins (Low Molecular Weight): May enhance the hyperkalemic effect of Eplerenone. Risk C: Monitor therapy
Herbal Products with Blood Pressure Increasing Effects: May diminish the antihypertensive effect of Antihypertensive Agents. Risk C: Monitor therapy
Herbal Products with Blood Pressure Lowering Effects: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Risk C: Monitor therapy
Hypotension-Associated Agents: Blood Pressure Lowering Agents may enhance the hypotensive effect of Hypotension-Associated Agents. Risk C: Monitor therapy
Levodopa-Containing Products: Blood Pressure Lowering Agents may enhance the hypotensive effect of Levodopa-Containing Products. Risk C: Monitor therapy
Lithium: Eplerenone may increase the serum concentration of Lithium. Risk C: Monitor therapy
Loop Diuretics: May enhance the hypotensive effect of Antihypertensive Agents. Risk C: Monitor therapy
Lormetazepam: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Risk C: Monitor therapy
Methylphenidate: May diminish the antihypertensive effect of Antihypertensive Agents. Risk C: Monitor therapy
Molsidomine: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Risk C: Monitor therapy
Naftopidil: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Risk C: Monitor therapy
Nicergoline: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Risk C: Monitor therapy
Nicorandil: May enhance the hyperkalemic effect of Potassium-Sparing Diuretics. Risk C: Monitor therapy
Nicorandil: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Risk C: Monitor therapy
Nitrofurantoin: May enhance the hyperkalemic effect of Eplerenone. Risk C: Monitor therapy
Nitroprusside: Blood Pressure Lowering Agents may enhance the hypotensive effect of Nitroprusside. Risk C: Monitor therapy
Nonsteroidal Anti-Inflammatory Agents: May diminish the antihypertensive effect of Eplerenone. Nonsteroidal Anti-Inflammatory Agents may enhance the hyperkalemic effect of Eplerenone. Risk C: Monitor therapy
Obinutuzumab: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Management: Consider temporarily withholding blood pressure lowering medications beginning 12 hours prior to obinutuzumab infusion and continuing until 1 hour after the end of the infusion. Risk D: Consider therapy modification
Opioid Agonists: May enhance the adverse/toxic effect of Diuretics. Opioid Agonists may diminish the therapeutic effect of Diuretics. Risk C: Monitor therapy
Pentoxifylline: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Risk C: Monitor therapy
Pholcodine: Blood Pressure Lowering Agents may enhance the hypotensive effect of Pholcodine. Risk C: Monitor therapy
Phosphodiesterase 5 Inhibitors: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Risk C: Monitor therapy
Potassium Salts: Eplerenone may enhance the hyperkalemic effect of Potassium Salts. Management: This combination is contraindicated in patients receiving eplerenone for treatment of hypertension. Potassium supplements may be needed to treat/prevent hypokalemia in selected patients with heart failure receiving eplerenone and high dose loop diuretics. Risk D: Consider therapy modification
Potassium-Sparing Diuretics: Eplerenone may enhance the hyperkalemic effect of Potassium-Sparing Diuretics. Management: This combination is contraindicated in patients receiving eplerenone for treatment of hypertension. Potassium supplements may be needed to treat/prevent hypokalemia in selected patients with heart failure receiving eplerenone and high dose loop diuretics. Risk D: Consider therapy modification
Prostacyclin Analogues: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Risk C: Monitor therapy
Quinagolide: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Risk C: Monitor therapy
QuiNIDine: Potassium-Sparing Diuretics may diminish the therapeutic effect of QuiNIDine. Risk C: Monitor therapy
Sodium Phosphates: Diuretics may enhance the nephrotoxic effect of Sodium Phosphates. Specifically, the risk of acute phosphate nephropathy may be enhanced. Risk C: Monitor therapy
Spironolactone: May enhance the hyperkalemic effect of Eplerenone. Risk X: Avoid combination
Tacrolimus (Systemic): Eplerenone may enhance the hyperkalemic effect of Tacrolimus (Systemic). Risk X: Avoid combination
Tolvaptan: May enhance the hyperkalemic effect of Potassium-Sparing Diuretics. Risk C: Monitor therapy
Trimethoprim: May enhance the hyperkalemic effect of Eplerenone. Risk C: Monitor therapy
Grapefruit juice increases eplerenone AUC ~25%. Management: Dosage adjustments of eplerenone may be needed.
Eplerenone may be preferred for the treatment of primary aldosteronism (PA) in patients who are planning to become pregnant and require treatment with a mineralocorticoid receptor antagonist (Forestiero 2022; Riester 2015). Use of eplerenone may be considered for patients experiencing menstrual irregularities or erectile dysfunction with other mineralocorticoid receptor antagonists during treatment for PA or resistant hypertension (AHA [Carey 2018]; ES [Funder 2016]; Kallistratos 2018).
Patients with heart failure who are planning to become pregnant should discontinue mineralocorticoid receptor antagonists prior to conception (AHA/ACC/HFSA [Heidenreich 2022]).
Eplerenone crosses the placenta (Saito 2021).
Data related to eplerenone use in pregnancy are limited (Cabassi 2012; Gehlert 2021; Gunganah 2015; Hutter 2006; Morton 2011; Morton 2017).
Chronic maternal hypertension is associated with adverse events in the fetus/infant. The risk of birth defects, low birth weight, premature delivery, stillbirth, and neonatal death may be increased with chronic hypertension in pregnancy. Actual risks may be related to duration and severity of maternal hypertension. The use of mineralocorticoid receptor antagonists for the treatment of hypertension in pregnancy is generally not recommended (ACOG 203 2019).
The treatment of edema associated with chronic heart failure during pregnancy is similar to that of nonpregnant patients. However, the use of mineralocorticoid receptor antagonists is not recommended. Patients diagnosed after delivery can be treated according to heart failure guidelines (AHA/ACC/HFSA [Heidenreich 2022]; ESC [Bauersachs 2016]; ESC [Regitz-Zagrosek 2018]).
Data specific to the treatment of primary aldosteronism (PA) in pregnancy are limited. Patients with PA should stop eplerenone before conception if possible. If treatment is stopped and PA is not controlled, eplerenone can be restarted in the second or third trimester (ES [Funder 2016]; Forestiero 2022; Riester 2015; Sanga 2022).
Case reports describe the use of potassium sparing diuretics such as eplerenone for the adjunctive treatment of Gitleman syndrome during pregnancy (Calò 2012; Moustakakis 2012; Shahzad 2019).
Eplerenone is present in breast milk.
Data related to the presence of eplerenone in breast milk are available from a case report. Eplerenone 50 mg once daily was initiated during pregnancy and continued postpartum. Multiple breast milk samples were obtained on postpartum days 7 and 35. The highest breast milk concentration observed was 161.2 ng/mL, obtained 4 hours after the dose on postpartum day 35. Using a milk concentration of 161.2 ng/mL, authors of the study calculated the estimated daily infant dose via breast milk to be 0.024 mg/kg/day, providing a relative infant dose of 3% based on the weight adjusted maternal dose. The infant was partially breastfed (over 50%); no adverse reactions were reported, and normal development was observed at 1 and 3 months (Saito 2021).
Do not use salt substitutes containing potassium.
BP; serum potassium (prior to therapy, within the first week, 1 month after start of treatment or dose adjustment, then periodically as clinically indicated); serum potassium and serum creatinine within 3 to 7 days after initiating concurrent therapy with a moderate CYP3A inhibitor, angiotensin-converting enzyme (ACE) inhibitor, angiotensin-II receptor blocker (ARB), or nonsteroidal anti-inflammatory drug.
Heart failure: Serum potassium and kidney function should be checked in 3 days after initiation, at 1 week after initiation, at least monthly for the first 3 months of therapy, and every 3 months thereafter. If adding or increasing the dose of concomitant ACE inhibitors or ARBs, a new cycle of monitoring should be done. If serum potassium increases to >5.5 mEq/L or kidney function worsens, hold doses until potassium is <5 mEq/L and consider restarting with a reduced dose after confirming resolution of hyperkalemia/kidney insufficiency for at least 72 hours. If serum potassium cannot be maintained <5.5 mEq/L, discontinue therapy (ACC [Maddox 2021]; AHA/ACC/HFSA [Heidenreich 2022]).
Aldosterone, a mineralocorticoid, increases blood pressure primarily by inducing sodium and water retention. Overexpression of aldosterone is thought to contribute to myocardial fibrosis (especially following myocardial infarction) and vascular fibrosis. Mineralocorticoid receptors are located in the kidney, heart, blood vessels, and brain. Eplerenone selectively blocks mineralocorticoid receptors reducing blood pressure in a dose-dependent manner and appears to prevent myocardial and vascular fibrosis.
Distribution: Vd: 42 to 90 L
Protein binding: ~50%; primarily to alpha1-acid glycoproteins
Metabolism: Primarily hepatic via CYP3A4; metabolites inactive
Bioavailability: 69%
Half-life elimination: ~3 to 6 hours
Time to peak, plasma: ~1.5 to 2 hours; may take up to 4 weeks for full antihypertensive effect
Excretion: Urine (~67%); feces (~32%); <5% as unchanged drug in urine and feces
Altered kidney function: AUC and Cmax increased 38% and 24%, respectively, in severe kidney impairment and decreased by 26% and 3%, respectively, in hemodialysis.
Hepatic function impairment: Cmax and AUC increased 3.6% and 42%, respectively, in moderate hepatic impairment.
Older adult: Cmax and AUC increased 22% and 45%, respectively.
Race/ethnicity: Cmax and AUC decreased 19% and 25%, respectively, in black patients.
Tablets (Eplerenone Oral)
25 mg (per each): $4.17 - $4.34
50 mg (per each): $4.17 - $4.34
Tablets (Inspra Oral)
25 mg (per each): $15.79
50 mg (per each): $15.79
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