Eplerenone (Oral)

As a receptor blocker, Eplerenone works to limit the amount of aldosterone being absorbed in the body. This medication is used to decrease blood pressure and control potential effects of high blood pressure on the heart.

OVERVIEW

Oral Eplerenone, or Inspra, helps patients take control of their blood pressure. It may be used as a preventative to treat high blood pressure before damage to the heart occurs. It may also be used after a heart associated event such as congestive heart failure to prevent further damage to the tissue of the heart. Oral Eplerenone has proven to increase the survival rate of patients who are stabilized with left ventricular systolic dysfunction as well as treat congestive heart failure after acute myocardial infarction.

It is common for patients who suffer from hypertension to require more than one medication to reach blood pressure goals. Other factors to take into consideration are:

  • Lipid control
  • Diabetes management
  • Antithrombotic therapy
  • Smoking cessation
  • Exercise
  • Limited sodium intake

For more information on hypertension, you can visit the American Heart Association online at www.heart.org.

The process of regulating blood pressure is the responsibility of a variety of systems in the body. Each type of regulating medication works in tandem with a target system, or systems, depending on the patient's needs. Oral Eplerenone works against mineralocorticoid receptors to inhibit the amount of aldosterone being absorbed by the body. Eplerenone works by binding to the mineralocorticoid receptor and blocking the binding of the aldosterone. Aldosterone is a steroid hormone responsible for regulating salt and water in the body. These levels affect blood pressure regulation thus working to relieve hypertension.

CONDITIONS TREATED

  • High Blood Pressure
  • Congestive Heart Failure
  • May Prevent Heart Disease

TYPE OF MEDICINE

  • Mineralocorticoid Receptor Antagonists

SIDE EFFECTS

As with any medication, any user should seek emergency medical help if they are experiencing any signs of allergic reaction such as hives, swelling of the face/tongue/lips, dizziness, trouble breathing or abdominal pain. Although allergic reactions are not common with this medication, anyone may be allergic to the substance.

One possible serious side effect is high potassium that would result in a slowed heart rate, tingly feelings, weak pulse or muscle weakness. This medication may also cause low potassium that would cause confusion, increased urination, muscle weakness or limp feelings, extreme thirst and uneven heart rate.

Hyperkalemia is a potential side effect for anyone receiving over 100mg of Oral Eplerenone a day. Hyperkalemia occurs when an excess of potassium is in the blood. Hyperkalemia has the potential to cause threatening heart arrhythmias. The risk of hyperkalemia is more prevalent in patients with impaired renal function, proteinuria and diabetes.

Some less serious side effects may be diarrhea, cough, dizziness, lethargy, vaginal bleeding, breast swelling or tenderness in males, fever, chills, body aches and stomach pain.

This is not an exhaustive list of all side effects. If you are experiencing any side effects not listed it is important to call your doctor or pharmacist. You can also report your effects to the FDA at 1-800-FDA-1088.

DOSAGE

Any prescribed medication should be taken as prescribed by a doctor. Taking more than prescribed will not enhance its ability to treat the patient. Altering the dosage of medication can change the function of the medication in the body altogether causing serious side-effects, or ineffectiveness. Some doses currently being prescribed are as follows.

50mg by mouth per day is commonly used to treat Hypertension
25mg by mouth per day is used to treat Heart Failure post MI. However this medication will require monitoring by a doctor to ensure potassium levels remain in safe ranges.

For renal impairment, serum creatinine >2mg/dl in males or >18mg/dL in females or CrCl <50 mL/min is used.

For patients with an insufficient response to the 50mg dose, the dose may be raised to twice a day.

Doses higher than 100mg are not advised as they do not have any greater effect on blood pressure

Doses higher than 100mg have an increased risk of hyperkalemia

Some dosing considerations are in order for post-MI CHF patients who take a moderate CYP3A inhibitor should not exceed 25mg in one day.

Doctors may start a patient on 25mg and increase after 4 weeks when the full benefit has been realized. This medication may be taken with or without food. To make it easy to remember to take a patient may consider taking it at the same time of day each day. If a dose of medication is missed, call a pharmacists for instructions on how to proceed. It is important not to ever double up on this medication to compensate for the missed dose. Do not share this medication with others. Currently, Eplerenone doses can be found in 25mg and 50mg tablets that are yellow and diamond shaped with a film coating.

Clinical studies of this medication have found that short-term therapy of oral eplerenone have proven beneficial in children and well tolerated. Pediatric children younger than 4 years old have not had sufficient clinical trials for dosing. Seniors older than 75 years of age, aldosterone antagonists such as oral eplerenone were not as effective.

An overdose of this medication will cause weak pulse, slow heart rate, muscle weakness, dizziness or near fainting. If you suspect an overdose has occurred call Poison Help Line at 1-800-222-1222.

INTERACTIONS

Drug interactions will increase risk for serious side effects and may change the way this medication works in the body. This does not list all possible drug interactions. It is imperative to let your doctor or pharmacists know all other medications you are taking whether over-the-counter, herbal or topical. Do not start, stop or change any doses without doctor approval for your safety.

Medications that may later the amount of potassium in your blood are at risk for interaction, including: birth control pills and water pillsĀ like amiloride/triamterene/spironolactone

Some psychotropic medications may interact with Oral Eplerenone such as lithium

Other medications may affect the bodies process of eplerenone removal which may change the way the medication works for you. Examples of these types of medications are:

Certain azole antifungals (like itraconazole or ketoconazole)

  • Boceprecir
  • Cobicistat
  • Clarithromycin
  • Some HIC protease inhibitors (nelfinavir, ritonavir)
  • St Johns Wort
  • Telithromycin
  • Telaprevir and others.
  • Some medications may raise blood pressure, or worsen heart failure. Be sure to speak to a pharmacists if you are using over-the-counter medications such as:
  • Cough-and-cold medications
  • NSAIDS like ibuprophen or naproxen
  • Diet aids.

Antibiotics like Biaxin or erythromicin, ACE inhibitors like benazepril, captopril, enalapril, lisinopril, moexipril, perindopril, quinapril, ramipril or trandolapril may also cause serious interactions with this medication and should be reviewed by a professional before being used.

Some antidepressants have caused interactions with this medication such as SSRIs such as:

  • Prozac
  • Luvox
  • Sinequan
  • Silenor
  • Pamelor
  • Other medications that may interact with oral eplerenone are:
  • Amiloride
  • Boceprevir
  • Clarithromycin
  • Cobicistat
  • Conivaptan
  • Idelalisib
  • Indinavir
  • Itraconazole
  • Ketoconazole
  • Lopinavir
  • Nefazodone
  • Nelfinavir
  • Posaconaz
  • Potassium
  • Ritonavir
  • Saquinavir
  • Spironolactone
  • Telaprevir
  • Telithromycin
  • Triamterene
  • Voriconazole

Using Eplerenone with these medications is not usually recommended. However it may be required for some patients. Discuss risks and benefits with your doctor before using eplerenone with any of the following.

  • Aceclofenac
  • Acemetacin
  • Alacepril
  • Amtolmetin Guacil
  • Aprepitant
  • Arsenic Trioxide
  • Aspirin
  • Atazanavir
  • Benazepril
  • Bromfenac
  • Bufexamac
  • Captopril
  • Celecoxib
  • Ceritinib
  • Choline Salicylate
  • Cilazapril
  • Clonixin
  • Delapril
  • Dexibuprofen
  • Dexketprofen
  • Diclofenac
  • Diflunisal
  • Diltiazem
  • Dipyrone
  • Dronedarone
  • Droxicam
  • Enalaprilat
  • Enalapril Maleate
  • Erythromycin
  • Etodolac
  • Etofenamate
  • Felbinac
  • Fenoprofen
  • Fepradinol
  • Feprazone
  • Floctafenine
  • Fluconazone
  • Flufenamic Acid
  • Flurbiprofen
  • Sodium Salicylate
  • Spirapril
  • Sulindac
  • Temocapril
  • Tenoxicam
  • Tiaprofenic Acid
  • Tolfenamic Acid
  • Tolmetin
  • Trandolapril
  • Trimethoprim
  • Valdecoxib
  • Zofenopril
  • Please note, that these lists are not exhaustive and should not be used to determine safety of medication without a doctor's approval.

WARNINGS

As with any medication it is important to know before taking if you are allergic to any ingredients in Eplerenone. You can get a list of ingredients from your pharmacist. It is also important to tell your doctor if you have ever had a history of high or low potassium levels in the past, as this medication may alter potassium levels.

While the FDA has categorized this medication as a B. This medication is not expected to be a harm to an unborn child, however, if you are pregnant/intend to become pregnant this needs to be discussed with your doctor. While it is still unknown if breastfeeding while on this medication may harm a nursing baby, consult your doctor. If it is possible you may become pregnant while taking Eplerenone, call your doctor to discuss risks of the medication.

Some dietary instructions are required while taking this medication. Discuss with your doctor whether it is safe for you to continue drinking grapefruit juice while on this medications, as it is known to deactivate certain ingredients. Do not use salt substitutes containing potassium while on this medication to ensure balanced potassium levels in the body. Seniors may be more at risk of high potassium levels than younger patients.

It is imperative to discuss previous health problems with your doctor. Especially if you have type 2 diabetes with protein in your urine, kidney disease, liver disease, high cholesterol or triglycerides. Discuss this with your doctor to balance risks/advantages of medication.

Doses of Oral Eplerenone over 100mg are linked with an increased risk of hyperkalemia. Hyperkalemia is an elevated level of potassium in the blood. Hyperkalemia may not have any side-effects, but severe hyperkalemia may lead to potentially fatal heart arrhythmias. For a patient with a weakened heart or heart tissue this is an unnecessary risk.

It is advisable that patients taking oral eplerenone check their serum potassium and serum creatinine within 3-7 days of taking this medication. Follow up with your doctor to ensure all levels are within normal range. These levels may be checked by scheduling blood work at your family physicians office. Creatinine is a waste product that comes from muscle activity and is typically cleansed from blood by the kidneys. High levels of creatinine in the blood can indicate poor kidney functioning. Potassium is a mineral found in the blood that is used by muscles in order to function properly. If potassium levels are too low, or high, it can impair all muscle function. Including muscles in the heart.

STORAGE

All medications should be kept in the bottle in which it is prescribed with the prescription label intact. Oral Eplerenone should be stored away from heat at room temperature. Freezing temperatures need to be avoided at all times. This medication should also be kept from direct sunlight. Best storage for this medication is enclosed in a cupboard or cabinet and kept safely away from the access of children.

When this medication is no longer being used, Oral Eplerenone needs to be disposed of properly. Flushing medication down the toilet or throwing it in the garbage can lead to chemicals seeping into the groundwater and wildlife. Appropriate steps for disposal of this medication, and others can be taken at local police departments, hospitals, clinics, fire stations, pharmacys or doctor's offices. Using medication past the expiration date is dangerous as the chemicals used to create these medications may change causing the medications to respond dangerously in the body.

SUMMARY

Oral Eplerenone has proven to lower blood pressure to within safe ranges. Uncontrolled high blood pressure can cause heart attacks, strokes, aneurysm, heart failure, weakened or narrowed blood vessels in the eyes, metabolic syndrome, trouble with memory and confusion in patients of all ages. Eplerenone has the potential of risks and side effects especially for those who do not clearly communicate with their physician about their medical histories, and other medications they are currently taking. Over-the-counter medications, herbal supplements, and vitamins need to be disclosed as well as other prescription medications.

Potassium and creatinine in the patients blood-stream need to be monitored while on this medication as oral eplerenone may alter blood levels. It is the responsibility of the doctor, patient and pharmacist to discuss the pros and cons of taking this medication and determine whether the risks outweigh the benefit on a case-by-case basis. This medication should be stored in its original container and at room temperature. Direct sunlight should be avoided and the medication should be disposed of properly after use has ended, or the medication has expired.

Hyperkalemia is a possible serious side-effect of this medication. Hyperkalemia is caused by high levels of potassium in the bloodstream. This side-effect may cause life threatening heart arrhythmias. High potassium in the blood may cause dizziness, muscle weakness, irregular heartbeat and abdominal pain. Hyperkalemia may also present no symptoms and can go unnoticed. Frequent check-ups are vital to ensuring appropriate eplerenone dosage.

When taken correctly, this medication may prolong the life of the soft tissues in and around the heart by preventing damage caused by high blood-pressure. If a dose is missed, it is important to consult with a doctor or pharmacist as to how to proceed and never double a dose to catch up. There are alternative treatments to lowering high blood pressure including lifestyle changed such as exercise and diet that may prevent the need for medications such as oral eplerenone. For patients that are unable to control high blood pressure with lifestyle changes this medication may offer some much-needed relief. High blood pressure can also be caused by high salt intake, salt sensitivity, genetic predisposition, or abnormality of the arteries. It is good practice to measure your heart rate regularly while taking this medication. An individual's heart rate may vary slightly depending on health, size and age but healthy blood pressure should range around 120/80. Blood pressure at 130/80 is considered high and should be discussed with a doctor.