Grapefruit juice may increase the serum levels of eplerenone by 25% by inhibiting CYP3A4. Activation of the RAAS is associated with an increased risk of ischemic cardiovascular events, independent of effects on blood pressure, 1 whereas interruption of the RAAS by angiotensin-converting enzyme (ACE) inhibition or angiotensin type 1 receptor (AT 1 R) blockade reduces cardiovascular mortality 2,3 and slows the progression of renal dise. The more specific aldosterone blocker, eplerenone, does not induce the side effects seen with spironolactone. 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. Monitor therapy, Benperidol: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Monitor therapy, Voriconazole: May increase the serum concentration of Eplerenone. Hospital data paints a somewhat bleak picture for people with metabolic syndrome, cardiovascular disease and type 2 diabetes who develop COVID-19. Eplerenone has been shown to bind extensively to charcoal. It works by blocking the action of aldosterone, a natural substance in the body that raises blood pressure. It's FDA-approved to treat the following in males:* . There are no human data available on whether Eplerenone is present in human milk, or has effects on breastfed infants or on milk production. J Am Coll Cardiol. Eplerenone may decrease the excretion rate of Acetyldigitoxin which could result in a higher serum level. Disease-associated maternal and/or embryo/fetal risk. The average time to enrollment was 7 days post-MI. 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. The Eplerenone post-acute myocardial infarction heart failure efficacy and survival study (EPHESUS) was a multinational, multicenter, double-blind, randomized, placebo-controlled study in patients clinically stable 3 to 14 days after an acute MI with LV dysfunction (as measured by left ventricular ejection fraction [LVEF] 40%) and either diabetes or clinical evidence of HF (pulmonary congestion by exam or chest x-ray or S3). Dosage was reduced or suspended anytime during the study if serum potassium levels were 5.5 mEq/L [see Dosage and Administration (2.1)]. Hyperkalemia: Hyperkalemia may occur; risk of hyperkalemia is increased with renal impairment, proteinuria, diabetes, and patients taking concomitant angiotensin-converting enzyme (ACE) inhibitors, angiotensin-II receptor blockers (ARBs), nonsteroidal anti-inflammatory drugs (NSAIDs), and/or moderate CYP3A inhibitors. Treasure Island (FL): StatPearls Publishing; 2023 Jan. Would you like email updates of new search results? Hydrochlorothiazide acts on the distal convoluted tubules and inhibits the sodium chloride co-transporter system. Monitor therapy, Fluconazole: May increase the serum concentration of Eplerenone. government site. Monitor therapy, Nonsteroidal Anti-Inflammatory Agents: May diminish the antihypertensive effect of Eplerenone. Dogs showed emesis, salivation, and tremors at a Cmax 41 times the human therapeutic Cmax, progressing to sedation and convulsions at higher exposures. The safety and efficacy of Eplerenone tablets have been evaluated alone and in combination with other antihypertensive agents in clinical studies of 3091 hypertensive patients. In these two studies, 611 patients were randomized to Eplerenone tablets and 140 patients to placebo. The Mediterranean diet is a healthy way of eating that has been associated with many health benefits. and E. Coli), in vitro mammalian cell mutagenesis (mouse lymphoma cells), in vitro chromosomal aberration (Chinese hamster ovary cells), in vivo rat bone marrow micronucleus formation, and in vivo/ex vivo unscheduled DNA synthesis in rat liver. Blood pressure lowering was apparent within 2 weeks from the start of therapy with Eplerenone tablets, with maximal antihypertensive effects achieved within 4 weeks. Monitor therapy, Heparins (Low Molecular Weight): May enhance the hyperkalemic effect of Eplerenone. Potassium-Sparing Diuretics may increase the serum concentration of Cardiac Glycosides. This activity outlines the indications, action, and contraindications for eplerenone as a valuable agent in managing heart failure and hypertension. Consider therapy modification, Potassium-Sparing Diuretics: Eplerenone may enhance the hyperkalemic effect of Potassium-Sparing Diuretics. The most common reasons for discontinuation of Eplerenone tablets were headache, dizziness, angina pectoris/MI, and increased GGT. No significant changes in Eplerenone pharmacokinetics were observed when Eplerenone was administered with aluminum- and magnesium-containing antacids. Monitor therapy, CYP3A4 Inducers (Strong): May increase the metabolism of CYP3A4 Substrates (High risk with Inducers). Patients greater than 75 years did not appear to benefit from the use of Eplerenone [see Clinical Studies (14.1)]. The risk of birth defects, low birth weight, premature delivery, stillbirth, and neonatal death may be increased with chronic hypertension in pregnancy. Review our medical disclaimer. In: StatPearls [Internet]. You must talk with the healthcare provider for complete information about the risks and benefits of using this medicine. The full therapeutic effect of Eplerenone tablets is apparent within 4 weeks. Monitor therapy, Nicorandil: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Eplerenone has not been studied in pediatric patients with heart failure. Closely monitor pregnant patients for destabilization of their heart failure. Monitor therapy, Angiotensin-Converting Enzyme Inhibitors: Eplerenone may enhance the hyperkalemic effect of Angiotensin-Converting Enzyme Inhibitors. Dosage form: tablet, film coated Monitor therapy, Simeprevir: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Mechanism of action. Data from a randomized, double-blind, placebo-controlled trial of patients with heart failure with reduced ejection fraction plus New York Heart Association (NYHA) class II symptoms suggest that eplerenone is effective at reducing cardiovascular death and hospitalization in this population Zannad 2011. [8] Consult appropriate manufacturer labeling. This material is provided for educational purposes only and is not intended for medical advice, diagnosis, or treatment. Eplerenone may increase the hypotensive activities of Acebutolol. 2017 ACC/AHA/AAPA/ABC/ACPM/AGS/APhA/ASH/ASPC/NMA/PCNA Guideline for the Prevention, Detection, Evaluation, and Management of High Blood Pressure in Adults: A Report of the American College of Cardiology/American Heart Association Task Force on Clinical Practice Guidelines. In post-MI HFrEF patients taking a moderate CYP3A inhibitor, do not exceed 25 mg once daily. In: StatPearls [Internet]. 12.1 Mechanism of Action Eplerenone binds to the mineralocorticoid receptor and blocks the binding of aldosterone, a component of the renin-angiotensin-aldosterone-system (RAAS). Monitor therapy, Dexmethylphenidate: May diminish the therapeutic effect of Antihypertensive Agents. Treasure Island (FL): StatPearls Publishing; 2023 Jan. The easiest way to lookup drug information, identify pills, check interactions and set up your own personal medication records. In post-MI HFrEF patients receiving a moderate CYP3A inhibitor (e.g., erythromycin, saquinavir, verapamil, and fluconazole), do not exceed 25 mg once daily. Monitor therapy. The risk of hyperkalaemia increase when Eplerenone is used in combination with an ACE inhibitor and/or an ARB. This article will discuss uses, common brand names, and safety information of potassium-sparing diuretics. The most likely manifestation of human overdosage would be anticipated to be hypotension or hyperkalemia. [24][21] Eplerenone is currently approved for sale in Canada, the US, EU, Netherlands and Japan. Decreased pup weights were observed beginning at birth at 1000 mg/kg/day. Monitor therapy, Barbiturates: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Date of revision of the text Eplerenone is not removed by hemodialysis [see Warnings and Precautions (5.1)]. Eplerenone is an antimineralocorticoid, or an antagonist of the mineralocorticoid receptor (MR). N Engl J Med. In mature rats, male fertility was decreased with Eplerenone exposure at 17 times the 100 mg/day human therapeutic dose. Pharmacological properties 6. Consider therapy modification, Stiripentol: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Adverse events occurred at a similar rate regardless of age, gender, or race. 1. Monitor therapy, Amifostine: Blood Pressure Lowering Agents may enhance the hypotensive effect of Amifostine. -, Krasiska B, Cofta S, Szczepaniak-Chiche L, Rzymski P, Trafas T, Paluszkiewicz L, Tykarski A, Krasiski Z. Monitor therapy, Naftopidil: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Monitor therapy, Pholcodine: Blood Pressure Lowering Agents may enhance the hypotensive effect of Pholcodine. Excipient information presented when available (limited, particularly for generics); consult specific product labeling. Opioid Agonists may diminish the therapeutic effect of Diuretics. In patients with hypertension taking a moderate CYP3A inhibitor, initiate at 25 mg once daily. 2022 Jun 22. When a drug is present in animal milk, it is likely that the drug will be present in human milk. Eplerenone Tablets Dose Response Trough Cuff DBP. Any CYP3A4 substrate used with stiripentol requires closer monitoring. There was no drug-related tumor response in heterozygous P53 deficient mice when tested for 6 months at dosages up to 1000 mg/kg/day (systemic AUC exposures up to 9 times the exposure in humans receiving the 100 mg/day therapeutic dose). Specifically, the risk of acute phosphate nephropathy may be enhanced. Following a single dose of Eplerenone 100 mg and CYP3A inhibitor ketoconazole 200 mg twice a day, Eplerenones Cmax was 1.7-fold and AUC was 5.4-fold compared with Eplerenone alone. The mean age was 64 years (range, 22 to 94 years). 1 For information on medical conditions and factors associated with increased risk for progression to severe COVID-19, see the Centers for Disease Control and Prevention (CDC) website: https://www.cdc.gov/coronavirus/2019-ncov/hcp/clinical-care/underlyingconditions.html. The mean placebo-subtracted reductions in trough cuff blood pressure achieved by Eplerenone tablets in these studies at doses up to 200 mg are shown in Figures 3 and 4. Eplerenone was non-genotoxic in a battery of assays including in vitro bacterial mutagenesis (Ames test in Salmonella spp. 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). Steady state is reached within 2 days. The UK is the first country to allow OTC access to Sanofi's tadalafil-based erectile dysfunction drug Cialis following a successful switch. Cmax and AUC increased 3.6% and 42%, respectively, in moderate hepatic impairment. 8600 Rockville Pike Heart Dis. Patients who develop hyperkalemia (5.5-5.9 mEq/L) may continue Eplerenone therapy with proper dose adjustment. Absorption is not affected by food. [3] Blocking the action of aldosterone decreases blood volume and lowers blood pressure. It is very slightly soluble in water, with its solubility essential pH-independent. Cialis is a brand-name prescription medication. See full drug interaction monograph for details. Eplerenone is an aldosterone receptor antagonist used to improve survival of patients with symptomatic heart failure and to reduce blood pressure. The combined endpoints, including combined all-cause hospitalization and mortality were driven primarily by CV mortality. Monitor therapy, Herbs (Hypotensive Properties): May enhance the hypotensive effect of Blood Pressure Lowering Agents. Monitor therapy, Conivaptan: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Erectile Dysfunction and Benign Prostatic Hyperplasia Cialis is indicated for the treatment of ED and the signs and symptoms of BPH (ED/BPH). 2011 Jan 06;364(1):11-21. Avoid combination, Potassium Salts: Eplerenone may enhance the hyperkalemic effect of Potassium Salts. Heart failure with preserved ejection fraction (off-label use): Note: May be considered for use in patients with symptomatic heart failure with preserved ejection fraction (45%) who have an elevated serum natriuretic peptide level or have been hospitalized for heart failure in the last 12 months (ACC/AHA/HFSA [Yancy 2017]). The prostate atrophy was reversible after daily treatment for 1 year at 100 mg/kg/day. For specific advice on goals and management, see published guidelines, such as those of the National High Blood Pressure Education Programs Joint National Committee on Prevention, Detection, Evaluation, and Treatment of High Blood Pressure (JNC). Heart failure with preserved ejection fractionyes. Unauthorized use of these marks is strictly prohibited. Disclaimer. PMC Eplerenone is in a class of medications called mineralocorticoid receptor antagonists. J Clin Med. Monitor therapy, Hypotension-Associated Agents: Blood Pressure Lowering Agents may enhance the hypotensive effect of Hypotension-Associated Agents. Monitor therapy, Sarilumab: May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). For improvement of survival of stable patients with left ventricular systolic dysfunction (ejection fraction <40%) and clinical evidence of congestive heart failure after an acute myocardial infarction. Avoid combination, CycloSPORINE (Systemic): Eplerenone may enhance the hyperkalemic effect of CycloSPORINE (Systemic). Matthews, NC 28105, amlodipine, lisinopril, metoprolol, losartan, furosemide, carvedilol, hydrochlorothiazide, spironolactone. Easily compare up to 40 drugs with our drug interaction checker. Heart failure: Serum potassium and renal 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. Eplerenone selectively binds to human mineralocorticoid receptors relative to its binding to recombinant human glucocorticoid, progesterone, and androgen receptors. Drugs with mechanism of action that involves Tubulin-binding leading to loss of function of the structural protein include: 1. cyclosporine 2. neostigmine 3. colchicine 4. glibenclamide 5. metformin 3 What type of protein primarily targeted by digitalis glycosides when they exert their effect on the heart: Transporters Monitor therapy, DULoxetine: Blood Pressure Lowering Agents may enhance the hypotensive effect of DULoxetine. The metabolism of Eplerenone can be decreased when combined with Acalabrutinib. Note: Not recommended for the initial treatment of hypertension (ACC/AHA [Whelton 2018]). [4] [8] It is unclear if it is effective for treating sexual dysfunction in women. Once treatment with Eplerenone tablets has begun, adjust the dose based on the serum potassium level as shown in Table 1. Eplerenone tablets contain Eplerenone, a blocker of aldosterone binding at the mineralocorticoid receptor. Eplerenone has been evaluated for safety in 3091 patients treated for hypertension. [16], methyl (4aS,4bR,5aR,6aS,7R,9aS,9bR,10R)-4a,6a-dimethyl-2,5'-dioxo-2,4,4',4a,5',5a,6,6a,8,9,9a,9b,10,11-tetradecahydro-3H,3'H-spiro[cyclopenta[7,8]phenanthro[4b,5-b]oxirene-7,2'-furan]-10-carboxylate, COC(=O)[C@@H]4C\C1=C\C(=O)CC[C@]1(C)[C@@]65O[C@@H]6C[C@@]3(C)[C@@H](CC[C@]23CCC(=O)O2)[C@H]45, InChI=1S/C24H30O6/c1-21-7-4-14(25)10-13(21)11-15(20(27)28-3)19-16-5-8-23(9-6-18(26)30-23)22(16,2)12-17-24(19,21)29-17/h10,15-17,19H,4-9,11-12H2,1-3H3/t15-,16+,17-,19+,21+,22+,23-,24-/m1/s1, Last edited on 13 February 2023, at 13:44, selective aldosterone receptor antagonist, "A comparison of the aldosterone-blocking agents eplerenone and spironolactone", "Eplerenone: a selective aldosterone receptor antagonist (SARA)", "Effect of Mineralocorticoid Receptor Blockade on Arterial Stiffness and Endothelial Function: A Meta-Analysis of Randomized Trials", "The Effects of Aldosterone Antagonists in Patients With Resistant Hypertension: A Meta-Analysis of Randomized and Nonrandomized Studies", "Eplerenone does not improve vision in people with central serous chorioretinopathy", "Eplerenone for chronic central serous chorioretinopathy in patients with active, previously untreated disease for more than 4 months (VICI): a randomised, double-blind, placebo-controlled trial", "Eplerenone (Inspra), a new aldosterone antagonist for the treatment of systemic hypertension and heart failure", "Mineralocorticoid receptor antagonists: the evolution of utility and pharmacology", https://en.wikipedia.org/w/index.php?title=Eplerenone&oldid=1139122219, SC-66110; CGP-30083; 9-11-Epoxymexrenone; 9,11-Epoxy-7-methoxycarbonyl-3-oxo-17-pregn-4-ene-21,17-carbolactone, This page was last edited on 13 February 2023, at 13:44. The .gov means its official. [8] It is taken by mouth or by injection into a vein. Minimize the risk of hyperkalemia with proper patient selection and monitoring [see Dosage and Administration (2.1), Contraindications (4), Adverse Reactions (6.2), and Drug Interactions (7)]. In patients with hypertension receiving a moderate CYP3A inhibitor, initiate at 25 mg once daily. For patients with an inadequate blood pressure response to 50 mg once daily increase the dosage of Eplerenone tablets to 50 mg twice daily. Disclosure: Jonathan Hughes declares no relevant financial relationships with ineligible companies. Cmax and AUC increased 22% and 45%, respectively. For inadequate blood pressure response, dosing may be increased to a maximum of 25 mg twice daily [see Drug Interactions (7.1)]. Primary aldosteronism (alternative agent) (off-label use): Note: Alternative to spironolactone (ES [Funder 2016]). This was a 15% reduction in relative risk. The ascertainment rate for vital status was 99.7%. Note: When initiating therapy for any of the heart failure indications below, 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. Please enable it to take advantage of the complete set of features! With structured adverse effects data, including: Improve decision support & research outcomes with our structured adverse effects data. N Engl J Med. Eplerenone 6 Spironolactone 5; Mechanism of Action: Binds to the mineralocorticoid receptor and blocks the binding of aldosterone Eplerenone is a second-generation MRA that has less affinity than spironolactone for progesterone and androgen receptors 11: Binds to the mineralocorticoid receptor and blocks the binding of aldosterone [3] Eplerenone differs from spironolactone in its extensive metabolism, with a short half-life and inactive metabolites. 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