Eplerenone

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Contents

[edit] BRAND NAMES

[edit] STRUCTURE

File:Eplerenone.jpg

[edit] MECHANISM OF ACTION

Eplerenone is a potassium sparing diuretic that acts by antagonism of aldosterone to the renal mineralocorticoid receptor in the distal renal tubules. The primary function of Aldosterone is to retain sodium and excrete potassium in the kidneys, therefore, Eplerenone causes increased amounts of sodium and water to be excreted, while potassium is retained.

Compared with spironolactone Eplerenone is much more selective, with minimal affinity for progesterone and androgenic receptors; therefore, there are very few reports of adverse sexual effects.

[edit] INDICATIONS

Eplerenone is indicated for:

  • Improving survival of stable patients with LV systolic dysfunction (LVEF ≤40%) and CHF after an acute myocardial infarction.
  • Hypertension, alone or combined with other agents.

Eplerenone is indicated for the treatment of hypertension, to lower blood pressure. Lowering blood pressure reduces the risk of fatal and nonfatal cardiovascular events, primarily strokes and myocardial infarctions.

[edit] DOSAGE

  • Congestive Heart Failure Post-Myocardial Infarction: Initiate treatment with 25 mg once daily. Titrate to maximum of 50 mg once daily within 4 weeks, as tolerated. Dose adjustments may be required based on potassium levels.
  • Hypertension: 50 mg once daily, alone or combined with other antihypertensive agents. For inadequate response, increase to 50 mg twice daily. Higher dosages are not recommended.

For all patients: Measure serum potassium before starting Eplerenone and periodically thereafter.

[edit] DOSAGE FORMS AND STRENGTHS

Tablets: 25 mg, 50 mg

[edit] CONTRAINDICATIONS

For all patients:

  • Serum potassium >5.5 mEq/L at initiation
  • Creatinine clearance ≤30 mL/min
  • Concomitant use with strong CYP3A4 inhibitors

For the treatment of hypertension:

  • Type 2 diabetes with microalbuminuria (4)
  • Serum creatinine >2.0 mg/dL in males, >1.8 mg/dL in females
  • Creatinine clearance <50 mL/min (4)
  • Concomitant use of potassium supplements or potassium-sparing diuretics

[edit] WARNINGS AND PRECAUTIONS

Hyperkalemia: Patients with decreased renal function and diabetics with proteinuria are at increased risk. Proper patient selection and monitoring and avoiding certain concomitant medications can minimize the risk.

[edit] INTERACTIONS

CYP3A4 Inhibitors: Reduce the starting dose for hypertension to 25 mg once daily when used with moderate CYP3A4 inhibitors (e.g., verapamil, erythromycin, saquinavir, fluconazole).

[edit] PREGNANCY AND LACTATION

  • Pregnancy Category B (US). Eplerenone should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.
  • Nursing Mothers: The concentration of eplerenone in human breast milk after oral administration is unknown. However, preclinical data show that eplerenone and/or metabolites are present in rat breast milk (0.85:1 [milk:plasma] AUC ratio) obtained after a single oral dose. Peak concentrations in plasma and milk were obtained from 0.5 to 1 hour after dosing. Rat pups exposed by this route developed normally. Because many drugs are excreted in human milk and because of the unknown potential for adverse effects on the nursing infant, a decision should be made whether to discontinue nursing or discontinue the drug, taking into account the importance of the drug to the mother.

[edit] SIDE EFFECTS

  • Congestive Heart Failure Post-Myocardial Infarction: Most common adverse reactions (>2% and more frequent than with placebo): hyperkalemia and increased creatinine.
  • Hypertension: Most common adverse reactions (≥2% and more frequent than with placebo): dizziness, diarrhea, coughing, fatigue and flu-like symptoms.

[edit] RELATED LINKS

[edit] REFERENCES

Antihypertensives
ACE inhibitors Benazepril (Lotensin)   Captopril (Capoten)   Cilazapril   Delapril   Enalapril (Renitec, Vasotec)   Fosinopril (Monopril)  Lisinopril (Prinivil, Zestril)   Moexipril (Univasc)  Perindopril (Aceon)  Quinapril (Accupril)  Ramipril (Altace, Triatec)   Trandolapril (Mavik)  Zofenopril (Bifril, Zopranol)
Angiotensin II receptor antagonist Azilsartan (Edarbi)   Candesartan (Atacand)   Eprosartan (Teveten)   Irbesartan (Aprovel, Avapro, Karvea)   Losartan (Cozaar)   Olmesartan (Benicar, Olmetec)   Telmisartan (Micadis)   Valsartan (Diovan, Tareg)
Renin inhibitors Aliskiren (Rasilez, Tekturna)
Alpha-1 blockers Doxazosin (Cardura)   Prazosin (Minipress)   Terazosin (Hytrin)
Alpha-2 agonists (centrally acting) Clonidine (Oral route)   Clonidine (Transdermal) (Catapresan)   Guanfacine (Tenex)   Methyldopa (Aldomet)
Calcium channel blockers Dihydropyridines‎ Amlodipine (Norvasc)   Barnidipine (Vasexten)   Felodipine (Plendil)   Isradipine (Dynacirc)   Lacidipine (Lacipil, Motens)   Lercanidipine (Zanidip)   Manidipine   Nicardipine   Nifedipine (Adalat)   Nisoldipine   Nitrendipine
Benzothiazepine‎ Diltiazem (Cardizem, Taztia XT, Tiazac, Tildiem)
Phenylalkylamine‎ Gallopamil   Verapamil (Calan)
Beta blockers Beta1 selective (cardioselective) Acebutolol (Sectral)   Atenolol (Tenormin)   Betaxolol (Kerlon)   Bisoprolol (Concor)   Celiprolol (Cordiax)   Metoprolol (Betaloc, Lopressor, Toprol-XL)   Nebivolol (Bystolic, Lobivon, Nebilox)
Nonselective (Beta1 and Beta2 blockers) Oxprenolol (Trasitensin)   Propranolol (Inderal)   Timolol (Blocadren)
Nonselective (Beta1, Beta2 and Alpha1 blockers) Carvedilol (Dilatrend)   Labetalol (Trandate)
Beta blocker with intrinsic sympathomimetic activity (ISA) Acebutolol (Sectral)   Celiprolol (Cordiax)
Lipophilic Beta blockers Propranolol (Inderal)   Metoprolol (Betaloc, Lopressor, Toprol-XL)   Oxprenolol (Trasitensin)
Diuretics Carbonic anhydrase inhibitors Acetazolamide (Diamox)
Loop diuretics Bumetanide   Etacrynic acid   Furosemide (Lasix)   Piretanide   Torasemide (Demadex)
Thiazide diuretics Chlorothiazide (Diuril)   Hydrochlorothiazide (Esidrex)
Thiazide-like diuretics Chlortalidone (Hygroton)   Indapamide (Lozol, Lozide)   Metolazone
Potassium-sparing diuretics Epithelial sodium channel blockers: Amiloride (Midamor)   Triamterene (Dyrenium)
Aldosterone receptor antagonists: Potassium canrenoate   Eplerenone (Inspra)   Spironolactone (Aldactone)
Osmotic diuretics Mannitol
Combination therapy Amiloride/Hydrochlorothiazide (Moduretic)   Spironolactone/Hydrochlorothiazide (Aldactazide)