Drug information of eplerenone

eplerenone

Drug group:

Eplerenone is used for Treating high blood pressure alone or along with other medicines. It is also used to improve survival in patients who have certain heart problems (left ventricular systolic dysfunction and congestive heart failure) following a heart attack. It may also be used for other conditions as determined by your doctor.

Mechanism of effect

Eplerenone is an aldosterone blocker. It works by blocking the hormone aldosterone, which lowers the amount of sodium and water the body retains. This helps to lower blood pressure to help prevent strokes, heart attacks, and kidney problems.

Pharmacodynamic

Selective aldosterone receptor antagonist; blocks aldosterone binding at the mineralocorticoid receptor

Pharmacokinetics

  • Half-Life: 3.5-6 hr
  • Peak Plasma Time: 1-2 hr
  • Bioavailability: 69%
  • Protein Bound: 50%
  • Metabolism: primarily hepatic CYP3A4
  • Metabolite: no active mets identified
  • Total Body Clearance: 10 L/hr
  • Excretion: feces (32%) and urine (67%)

Dosage

Hypertension (HTN): Initial 50 mg PO qDay; may increase to 50 mg PO q12hr; may take up to four weeks for full therapeutic response; hyperkelemia may occur with doses >100 mg/day

Heart Failure Post MI: Initial 25 mg PO qDay; may titrate to maximum of 50 mg once daily within 4 weeks as tolerated

Alerts

Eplerenone may cause dizziness. This effect may be worse if you take it with alcohol or certain medicines. Use eplerenone with caution. Do not drive or perform other possibly unsafe tasks until you know how you react to it.

Lab tests, including blood potassium levels, blood pressure measurements, and kidney function, may be performed while you use eplerenone. These tests may be used to monitor your condition or check for side effects. Be sure to keep all doctor and lab appointments.

Use eplerenone with caution in the ELDERLY; they may be more sensitive to its effects, especially high blood potassium levels.

Eplerenone should be used with extreme caution in CHILDREN younger than 4 years old; safety and effectiveness in these children have not been confirmed.

It is not known if this medicine is found in breast milk. Do not breast-feed while taking eplerenone.

Points of recommendation

It may take up to 4 weeks to see the full benefit of eplerenone on your blood pressure. Do not stop taking eplerenone without checking with your doctor.

Do not exceed the recommended dose of eplerenone. Doing so will not improve your condition faster and may lead to side effects.

Do not use a salt substitute or a potassium supplement without checking with your doctor.

Tell your doctor or dentist that you take eplerenone before you receive any medical or dental care, emergency care, or surgery.

Patients who take medicine for high blood pressure often feel tired or rundown for a few weeks after starting treatment. Be sure to take your medicine even if you may not feel quite "normal." Tell your doctor if you develop any new symptoms.

Pregnancy level

B


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