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Eplerenone
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Eplerenone is a prescription drug used to treat patients with congestive heart failure (CHF) and high blood pressure (hypertension).
It belongs to a family of drugs called aldosterone antagonists. Other members of this family are spironolactone and canrenone.
Eplerenone is marketed by Pfizer under the name "Inspra."
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Uses
Eplerenone is indicated for the treatment of congestive heart failure (CHF) in people after they have had a heart attack (acute myocardial infarction, or "MI").
Eplerenone is also indicated for the treatment of hypertension (high blood pressure).
How Eplerenone Is Taken
Inspra is available in 25 and 50 mg tablets, which are taken by mouth.
In congestive heart failure patients
Treatment is started at 25 mg once daily and then raised to 50 mg once daily over a course of 4 weeks.
In hypertension patients
The recommended starting dose is 50 mg once daily.
How It Works
Aldosterone is a hormone produced by the adrenal gland. Aldosterone acts to raise blood pressure levels by binding to a specific receptor in the adrenal gland, called the mineralocorticoid receptor.
Eplerenone works by blocking aldosterone from binding to this receptor, thereby reducing blood pressure.
How the body affects Eplerenone
Peak circulating levels of eplerenone are reached approximately 1.5 hours post-dosing.
Eplerenone metabolism is primarily mediated via the liver enzyme CYP3A4.
Approximately 32% of the original dose is excreted in the feces and approximately 67% is excreted in the urine in the form of metabolites.
Side Effects
The most common side effects attributable to Inspra use are:
- Hypercholesterolemia (high blood cholesterol levels)
- Hypertriglyceridemia (high blood lipid levels)
- Diarrhea
- Abdominal pain
- Albuminuria (increased levels of the blood protein albumin excreted in the urine)
- Coughing
- Dizziness
- Fatigue
- Flu-like symptoms
Risks and Precautions
Eplerenone can cause hyperkalemia (high blood potassium levels). Signs of hyperkalemia include:
- Malaise (feeling tired)
- Heart palpitations
- Muscle weakness
Drug Interactions
Because eplerenone metabolism is predominantly mediated via the liver enzyme CYP3A4, eplerenone is not to be used with drugs that are strong inhibitors of CYP3A4.
Patients with hypertension who are also taking moderate CYP3A4 inhibitors, the starting dose is lowered to 25 mg once daily.
Effectiveness
Eplerenone was studied in patients with congestive heart failure (CHF) after experiencing a heart attack (acute MI). Eplerenone resulted in a 15% reduction in death rates after one year.[1]
One study demonstrated significant reductions in blood pressure in patients treated with 50 mg eplerenone daily.[2]
References
- ↑ Pitt B, et al. The EPHESUS Trial: eplerenone in patients with heart failure (HF) due to systolic dysfunction complicating acute myocardial infarction. NEJM 2003.
- ↑ White WB, Carr AA, Krause S, Jordan R, Roniker B, Oigman W. Assessment of the novel selective aldosterone blocker eplerenone using ambulatory and clinical blood pressure in patients with systemic hypertension. Am J Cardiol. 2003;92:38–42.
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