Eplerenone

(e pler' en one)

PCaution when used during lactation / LCaution when used during lactation : Caution - pregnancy &  lactation (breast feeding)

Molecule Info

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Indication(s) 

Eplerenone is an aldosterone antagonist 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 tablets are 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.

Dosage & Administration

CHF Post-MI: 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 tablets and periodically thereafter.

May be taken with or without food.

Overdosage

No cases of human overdosage with eplerenone have been reported. Lethality was not observed in mice, rats, or dogs after single oral doses that provided C exposures at least 25 times higher than in humans receiving eplerenone 100 mg/day. Dogs showed emesis, salivation, and tremors at a C 41 times the human therapeutic C , progressing to sedation and convulsions at higher exposures. The most likely manifestation of human overdosage would be anticipated to be hypotension or hyperkalemia. Eplerenone cannot be removed by hemodialysis. Eplerenone has been shown to bind extensively to charcoal. If symptomatic hypotension should occur, supportive treatment should be instituted. If
hyperkalemia develops, standard treatment should be initiated.

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
  • Serum creatinine >2.0 mg/dL in males, >1.8 mg/dL in females
  • Creatinine clearance <50 mL/min
  • Concomitant use of potassium supplements or potassium-sparing diuretics

Warning & 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.

Eplerenone Tablets 50 mg contain FD&C Yellow No. 5 (tartrazine) which may cause allergic-type reactions (including bronchial asthma) in certain susceptible persons. Although the overall incidence of FD&C Yellow No. 5 (tartrazine) sensitivity in the general population is low, it is frequently seen in patients who also have aspirin hypersensitivity.

Adverse Drug Reaction(s)

Hyperkalaemia, hyponatraemia, dizziness, headache, abdominal pain, diarrhoea, cough, fatigue, influenza-like symptoms, abnormal vaginal bleeding, gynaecomastia, mastodynia, myocardial infarction, angina pectoris, hypercholesterolaemia, hypertriglyceridaemia, albuminuria, increased creatinine, elevated liver enzymes, increased uric acid, rash and angioneurotic oedema.

Drug Interactions

CYP3A4 Inhibitors
Because eplerenone metabolism is predominantly mediated via CYP3A4, do not use eplerenone with drugs that are strong inhibitors of CYP3A4. In patients with hypertension taking moderate CYP3A4 inhibitors, reduce the starting dose of eplerenone to 25 mg once daily.

ACE Inhibitors and Angiotens in II Receptor Antagonists
The risk of hyperkalaemia may increase when eplerenone is used in combination with an angiotensin converting enzyme (ACE) inhibitor and/or an angiotensin receptor blocker (ARB). A close monitoring of serum potassium and renal function is recommended, especially in patients at risk for impaired renal function, e.g., the elderly.

Congestive Heart Failure Post-Myocardial Infarction
In EPHESUS, 3,020 (91%) patients receiving eplerenone 25 mg to 50 mg also received ACE inhibitors or angiotensin II receptor antagonists (ACEI/ARB). Rates of patients with maximum potassium levels >5.5 mEq/L were similar regardless of the use of ACEI/ARB.

HYPERTENSION
In clinical studies of patients with hypertension, the addition of eplerenone 50 mg to 100 mg to ACE inhibitors and angiotensin II receptor antagonists increased mean serum potassium slightly (about 0.09mEq/L to 0.13 mEq/L). In a study in diabetics with microalbuminuria, eplerenone 200 mg combined with the ACE inhibitor enalapril 10 mg increased the frequency of hyperkalemia (serum potassium >5.5
mEq/L) from 17% on enalapril alone to 38%.

Lithium
A drug interaction study of eplerenone with lithium has not been conducted. Lithium toxicity has been reported in patients receiving lithium concomitantly with diuretics and ACE inhibitors. Serum lithium levels should be monitored frequently if eplerenone is administered concomitantly with lithium.

Nons teroidal Anti-Inflammatory Drugs (NSAIDs )
A drug interaction study of eplerenone with an NSAID has not been conducted. The administration of other potassium-sparing antihypertensives with NSAIDs has been shown to reduce the antihypertensive effect in some patients and result in severe hyperkalemia in patients with impaired renal function.

Therefore, when eplerenone and NSAIDs are used concomitantly, patients should be observed to determine whether the desired effect on blood pressure is obtained and monitored for changes in serum potassium levels.

Food Interaction

Avoid grapefruit juice as it may increase serum levels of Eplerenone. St.  Johns wort may decrease serum levels of Eplerenone.

Pregnancy Category (FDA)

Category B: Either animal-reproduction studies have not demonstrated a foetal risk but there are no controlled studies in pregnant women or animal-reproduction studies have shown an adverse effect that was not confirmed in controlled studies in women in the 1sttrimester.

Storage

Oral:  Store at 25°C; excursions permitted to 15-30°C.

Pharmacology

Aldosterone binds to mineralocorticoid receptors in both epithelial and nonepithelial tissues; causing increases in blood pressure by inducing sodium reabsorption, vascular remodeling, water retention and possibly other mechanisms.  Eplerenone is a relatively selective mineralocorticoid receptor antagonist, blocking binding of aldosterone and reducing blood pressure.  Eplerenone also appears to have cardioprotective effect in patients with congestive heart failure after myocardial infarction.

Absorption: Absolute bioavailability: About 69%. Mean Tmax: Approx 1.5 hr.Distribution: Protein binding: About 50%. Vd: About 43-90 L. Metabolism: Hepatic metabolism mainly via CYP3A4 to inactive metabolites.Excretion: About 67% is excreted in urine and 32% in faeces following a single Oral   dose.  <5% is excreted unchanged in urine and faeces.  Elimination half-life: About 4-6 hr.  Apparent plasma clearance: Approx 10 L/hr.

ATC Classification

C03DA04 - eplerenone; Belongs to the class of aldosterone antagonists.  Used as potassium-sparing diuretics.

 

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Brand/Product Info


Total Products : 1 
Brand Name Manufacturer/Marketer Composition Dosage Form Pack Size & Price
Epleron 25 Incepta Pharmaceuticals Limited Eplerenone INN 25 mg Tablet 4x5's:MRP 900 Tk

Gen. MedInfo

Why is Eplerenone prescribed?

Eplerenone is used alone or in combination with other medications to treat high blood pressure.  Eplerenone is in a class of medications called mineralocorticoid receptor antagonists.  It works by blocking the action of aldosterone, a natural substance in the body that raises blood pressure.

How should Eplerenone be used?

Eplerenone comes as a tablet to take by mouth.  It is usually taken once or twice a day, with or without food.  To help you remember to take eplerenone, take it around the same time every day.  Follow the directions on your prescription label carefully, and ask your Doctor to explain any part you do not understand.  Take eplerenone exactly as directed.  Do not take more or less of it or take it more often than prescribed by your doctor.

Your doctor may start you on a low dose of eplerenone and increase your dose after 4 weeks.

Eplerenone controls high blood pressure but does not cure it.  It may take 4 weeks or longer before you feel the full benefit of eplerenone.  Continue to take eplerenone even if you feel well.  Do not stop taking eplerenone without talking to your doctor.

Other uses of Eplerenone

Eplerenone may be prescribed for other uses; ask your Doctor for more information.

What special precautions to follow?

Before taking eplerenone,

  • tell your Doctor if you are allergic to eplerenone or any other medications.
  • do not take eplerenone if you are taking amiloride, amiloride and hydrochlorothiazide, itraconazole, ketoconazole, potassium supplements, spironolactone, spironolactone and hydrochlorothiazide, triamterene, or triamterene and hydrochlorothiazide.
  • tell your Doctor what other prescription and nonprescription medications, vitamins, and nutritional supplements you are taking.  Be sure to mention any of the following: angiotensin converting enzyme inhibitors such as benazepril, captopril, enalapril, fosinopril, lisinopril, and quinapril; angiotensin II receptor antagonists such as eprosartan, irbesartan, losartan, olmesartan, and valsartan; aspirin and other nonsteroidal anti-inflammatory drugs such as ibuprofen and naproxen; cimetidine; clarithromycin; danazol; delavirdine; diltiazem; erythromycin; fluconazole; fluoxetine; fluvoxamine; HIV protease inhibitors such as indinavir, ritonavir, and saquinavir; isoniazid; lithium; metronidazole; nefazodone; troleandomycin; verapamil; and zafirlukast.  Your doctor may need to change the doses of your medications or monitor you carefully for side effects.
  • tell your doctor what herbal products you are taking, especially St.  John's wort.
  • tell your doctor if you have or have ever had high blood levels of potassium, diabetes, gout, or liver or kidney disease.
  • tell your doctor if you are pregnant, plan to become pregnant, or are breast-feeding.  If you become pregnant while taking eplerenone, consult your doctor.

What special dietary instructions to follow?

Talk to your doctor about drinking grapefruit juice while taking Eplerenone.

Do not use salt substitutes containing potassium while you are taking eplerenone.  If your doctor prescribes a low-salt or low-sodium diet, follow these directions carefully.

What to do if I forget a dose?

Take the missed dose as soon as you remember it.  However, if it is almost time for the next dose, skip the missed dose and continue your regular dosing schedule.  Do not take a double dose to make up for a missed one.

What side effects can Eplerenone cause?

Eplerenone may cause side effects.  Tell your doctor if any of these symptoms are severe or do not go away:

  • headache
  • dizziness
  • diarrhea
  • stomach pain
  • cough
  • excessive tiredness
  • flu-like symptoms
  • breast enlargement or tenderness
  • abnormal vaginal bleeding
  • chest pain
  • tingling in arms and legs
  • loss of muscle tone
  • weakness or heaviness in legs
  • confusion
  • lack of energy
  • cold, gray skin
  • irregular heartbeat

Some side effects can be serious.  The following symptoms are uncommon, but if you experience any of them, consult your doctor immediately:

Eplerenone may cause other side effects.  Consult your doctor if you have any unusual problems while taking Eplerenone.

If you experience a serious side effect, you or your doctor may send a report to the Office of Directorate General, Drugs Administration.

What storage conditions are needed for Eplerenone?

Keep Eplerenone in the container it came in, tightly closed, and out of reach of children.  Store it at room temperature and away from excess heat and moisture.  Throw away any medication that is outdated or no longer needed.  Talk to your Doctor about the proper disposal of your medication.

In case of emergency/overdose

In case of overdose, consult your Doctor.  If the victim has collapsed or is not breathing, consult local medical emergency services..

Symptoms of overdose may include:

  • fainting
  • dizziness
  • blurred vision
  • upset stomach
  • tingling in arms and legs
  • loss of muscle tone
  • weakness or heaviness in legs
  • confusion
  • lack of energy
  • cold, gray skin
  • irregular or slow heartbeat

What other information to know?

Keep all appointments with your doctor and the laboratory.  Your doctor will check your blood pressure regularly and order certain lab tests to check your body's response to eplerenone.

Do not let anyone else take your medication.  

It is important for you to keep a written list of all of the prescription and nonprescription medicines you are taking, as well as any products such as vitamins, minerals, or other dietary supplements.  You should bring this list with you each time you visit a doctor or if you are admitted to a hospital.  It is also important information to carry with you in case of emergencies. 

Ref: U.S. Natl. Library of Medicine

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 This information is provided for reference only and not a replacement for and should only be used in conjunction with full consultation with a registered medical practitioner. It may not contain all the available information you require and cannot substitute professional medical care, nor does it take into account all individual circumstances. Although great effort has been made to ensure content accuracy, mph-bd shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise.

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