Eplerenone

Uses	Hypertension, Edema
Therapy	Drugs For Congestive Heart Failure
Side Effects	Increased Potassium Levels, Sleeplessness, Dizziness, Headache

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Molecule Description

Eplerenone is used to reduce the risk of complications or death due to heart failure (impaired pumping efficiency of the heart). It belongs to a class of medicines called ‘aldosterone blocking agents.’

Uses

It is used to treat and prevent heart failure.

Contraindications

When should one not use Eplerenone

Allergy to Eplerenone or any components of the medicine
Medicines that increase potassium levels in the body (Spironolactone, Potassium supplements, etc.)
Severe kidney or liver disease
Medicines to treat infections (Clarithromycin, Telithromycin, Ketoconazole, Itraconazole, Nelfinavir, Ritonavir)
Nefazodone (treats depression)
If you are taking a certain class of blood pressure medications (ACE inhibitors - Ramipril, Lisinopril, Enalapril) with another particular type of medicines called angiotensin receptor blockers or ARBs (Losartan, Telmisartan, Valsartan, etc.)

Side effects

Common side effects of this drug are:

Elevated levels of potassium in the body (headache, nausea, muscle cramps or loose motions)
Feeling dizzy, fainting (low blood pressure)
High cholesterol levels
Difficulty in sleeping
Constipation
Weakness, muscle aches
Rashes, itching
Kidney problems (increased urea and creatinine levels)
Increase in certain types of white blood cells (eosinophilia), dehydration, infections, low sodium levels, gall bladder problems, blood clots in the leg, sore throat, increased sweating, male breasts, thyroid problems, raised blood glucose levels
Severe allergic reactions causing swelling of face, lips, throat causing difficulty in breathing and swallowing, with or without itching, rashes, skin blisters and peeling

Precautions and Warnings

Pregnancy

Eplerenone is not known to cause any harmful effects to the baby, but careful and close monitoring is recommended while using in pregnant women, due to lack of adequate data.

Breast Feeding

It is not known if Eplerenone is secreted in breast milk. But, because this medicine is used in severe conditions that may harm the mother, a careful decision has to be taken by the doctor about discontinuing the medication or even breastfeeding.

Driving

Eplerenone does not affect your ability to drive. But taking into account the condition of your heart and side effects such as dizziness, caution is advised.

Alcohol

Alcohol lowers blood pressure, causes drowsiness and is not suitable for your heart. Hence it is advised to avoid alcohol while taking Eplerenone.

Other General Warnings

Talk to your doctor if

You have kidney or liver diseases
You are taking:
Lithium (for extreme mood swings)
Cyclosporine or Tacrolimus (used to treat allergic skin reactions and suppress the immune system, especially after an organ transplant)

Mode of Action

How Does It Work?

Aldosterone is a hormone secreted by adrenal gland present above the kidney. The primary function of this substance is to prevent excretion of water by the kidneys. Eplerenone blocks the action of aldosterone and causes more fluid to excrete through the kidneys. Thus relieving high blood pressure and reducing the load on the heart, whose pumping ability is already impaired due to heart failure.

Interactions

Interactions with other medicines

Medicines to treat infections (Clarithromycin, Telithromycin, Ketoconazole, Itraconazole, Nelfinavir, Ritonavir)
Nefazodone (treats depression)
Do not take these two classes of blood pressure medications together while taking Eplerenone
ACE inhibitors (Ramipril, Lisinopril, Enalapril) with Angiotensin Receptor Blockers or ARBs (Losartan, Telmisartan, Valsartan, etc.)
Use with caution:
Medicines used to treat depression, mood disorders, psychosis (Lithium, Chlorpromazine, Haloperidol, Amitryptiline, Amoxapine)
Medicines used to suppress the immune system or immune response (Cyclosporine, Tacrolimus Hydrocortisone, Prednisone, Tetracosactide)
Medicines used to treat bacterial infections (Trimethoprim, Erythromycin, Rifampicin)
Amifostine (cancer treatment)
Baclofen (treats muscle tightness)
Digoxin and Amiodarone (used for irregular heart rhythms)
Certain blood pressure medications (Diltiazem, Verapamil)
Anti-seizure medications (Carbamazepine, Phenytoin, Phenobarbital)
Pain killers

Interactions with food items

Eplerenone can be taken with or without food.

Dosage

Overdose

Be careful while using Eplerenone. It is strictly recommended to avoid any overdose. Symptoms of overdosage may include slow heart rate, weak pulse, muscle weakness, dizziness or feeling like you might pass out or faint. Inform your doctor and seek medical attention without delay if you start feeling uncomfortable.

Missed a Dose

Take the missed dose as early as you remember. Ensure to have at least a 12-hour gap between two dosages. Skip the missed dose if your next dose is due in less than 12 hours and continue with the usual next dose. Do not take extra medicine or double dose to compensate for the missed dose.

Frequently Asked Questions (FAQs)

Eplerenone is usually given in combination with other medications. It is started on a low doseand then increased gradually.Eplerenone can elevate blood potassium levels and regular blood tests are required to monitorthis. Checking for potassium levels is necessary in the first week and after the first month ofstarting the treatment (before changing the dose). The correct dose needs to adjusted based onthe blood potassium levels.Dose adjustment may be required in kidney disease.Take this medicine with plenty of water.

Eplerenone is associated with good control of blood pressure, reduced death rates due toheart disease and improved survival rates.It has a better safety profile than the other medicine in its class (spironolactone).Eplerenone can increase blood potassium levels and cause irregular heartbeats or rhythms, butthese effects are not very severe.This medicine is specifically used when there are increased levels of the hormone aldosteronewhich causes decreased fluid excretion and increased levels in the body leading to high bloodpressure and load on the heart. Aldosterone also has harmful effects on the heart.Eplerenone blocks aldosterone and its actions and will prove beneficial for survival.

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References:

Webmd eplerenone[accessed on 24Aug2019] (Online) Available from:

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