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Eplerenone

 
Drug Info:

Eplerenone

Brand names: Inspra™

Chemical formula:



Eplerenone Oral tablet

What is this medicine?

EPLERENONE (e PLER en one) is used to treat high blood pressure. This medicine is also used to improve symptoms of heart failure.
 
This medicine may be used for other purposes; ask your health care provider or pharmacist if you have questions.

What should I tell my health care provider before I take this medicine?

They need to know if you have any of these conditions:
•diabetes
•high blood level of potassium
•if you are on a special diet, such as a low-salt diet and are using dietary salt substitutes
•kidney disease
•liver disease
•an unusual or allergic reaction to eplerenone, other medicines, foods, dyes, or preservatives
•pregnant or trying to get pregnant
•breast-feeding

How should I use this medicine?

Take this medicine by mouth with a glass of water. Follow the directions on the prescription label. You may take this medicine with or without food. Take your doses at regular intervals. Do not take your medicine more often than directed. Do not stop taking except on the advice of your doctor or health care professional.

Talk to your pediatrician regarding the use of this medicine in children. Special care may be needed.

Overdosage: If you think you have taken too much of this medicine contact a poison control center or emergency room at once.
NOTE: This medicine is only for you. Do not share this medicine with others.

What may interact with this medicine?

Do not take this medicine with any of the following medications:
•certain antibiotics like clarithromycin, erythromycin, troleandomycin
•conivaptan
•diuretics, especially amiloride, spironolactone or triamterene
•imatinib, STI-571
•medicines for fungal infections like itraconazole and ketoconazole
•nefazodone
•nelfinavir
•potassium salts or supplements
•ritonavir

This medicine may also interact with the following medications:
•fluconazole
•grapefruit juice
•lithium
•medicines for high blood pressure
•medicines for HIV infection
•NSAIDs, medicines for pain and inflammation, like ibuprofen or naproxen
•St. John's Wort

This list may not describe all possible interactions. Give your health care provider a list of all the medicines, herbs, non-prescription drugs, or dietary supplements you use. Also tell them if you smoke, drink alcohol, or use illegal drugs. Some items may interact with your medicine.

What should I watch for while using this medicine?

Visit your doctor or health care professional for regular checks on your progress. Check your blood pressure as directed. Ask your doctor or health care professional what your blood pressure should be and when you should contact him or her.

You may need to be on a special diet while taking this medicine. Ask your doctor. Also, ask how many glasses of fluid you need to drink each day. You must not get dehydrated.

You may get drowsy or dizzy. Do not drive, use machinery, or do anything that needs mental alertness until you know how this medicine affects you. Do not stand or sit up quickly, especially if you are an older patient. This reduces the risk of dizzy or fainting spells. Alcohol may interfere with the effect of this medicine. Avoid alcoholic drinks.

What side effects may I notice from receiving this medicine?

Side effects that you should report to your doctor or health care professional as soon as possible:
•allergic reactions like skin rash, itching or hives, swelling of the face, lips, or tongue
•chest pain
•confusion
•enlarged breasts or breast pain in males
•fast or irregular heartbeat, palpitations
•increased hair growth in females
•irregular menstrual periods
•sexual difficulty
•unusually weak or tired

Side effects that usually do not require medical attention (report to your doctor or health care professional if they continue or are bothersome):
•cough
•diarrhea
•fatigue
•headache
•stomach pain

This list may not describe all possible side effects. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

Where should I keep my medicine?

Keep out of the reach of children.

Store at room temperature between 15 and 30 degrees C (59 and 86 degrees F). Throw away any unused medicine after the expiration date.

Last updated: 10/4/2002 12:57:00 PM

Important Disclaimer: The drug information provided here is for educational purposes only. It is intended to supplement, not substitute for, the diagnosis, treatment and advice of a medical professional. This drug information does not cover all possible uses, precautions, side effects and interactions. It should not be construed to indicate that this or any drug is safe for you. Consult your medical professional for guidance before using any prescription or over the counter drugs.

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Wikipedia:

Eplerenone

Top
Eplerenone
Systematic (IUPAC) name
pregn-4-ene-7,21-dicarboxylic acid, 9,11-epoxy-17-hydroxy-3-oxo, γ-lactone, methyl ester (7α, 11α, 17α)
Identifiers
CAS number 107724-20-9
ATC code C03DA04
PubChem 5282131
DrugBank APRD00707
Chemical data
Formula C24H30O6 
Mol. mass 414.49
Pharmacokinetic data
Bioavailability 69%
Metabolism hepatic (CYP3A4)
Half life 3–5 hours
Excretion 67% renal
32% biliary
Therapeutic considerations
Pregnancy cat. B3 (Aust)
Legal status Schedule 4 (Aust), Rx only (US)
Routes oral
 Yes check.svgY(what is this?)  (verify)

Eplerenone (INN) (pronounced /ɛpˈlɛrənoʊn/) is an aldosterone antagonist used as an adjunct in the management of chronic heart failure. It is similar to the diuretic spironolactone, though it may be more specific for the mineralocorticoid receptor and is specifically marketed for reducing cardiovascular risk in patients following myocardial infarction. It is marketed by Pfizer under the trade name Inspra.

Contents

Clinical use

Indications

Eplerenone is specifically indicated for the reduction of risk of cardiovascular death in patients with heart failure and left ventricular dysfunction within 3–14 days of an acute myocardial infarction, in combination with standard therapies and as treatment against hypertension.

Contraindications

Eplerenone is contraindicated in patients with hyperkalaemia, severe renal impairment (creatinine Cl less than 30 ml/min), or severe hepatic impairment (Child-Pugh score C). The manufacturer of eplerenone also contraindicates ( relative C.I. ) concomitant treatment with ketoconazole, itraconazole or other potassium-sparing diuretics (though the manufacturer still considers taking these drugs to be absolute C.I.) Potential benefits should be weighted against possible risks.

Adverse effects

Common adverse drug reactions (ADRs) associated with the use of eplerenone include: hyperkalaemia, hypotension, dizziness, altered renal function, and increased creatinine concentration.[1]

Drug interactions

Eplerenone is primarily metabolised by the cytochrome P450 enzyme CYP3A4. Thus the potential exists for adverse drug interactions with other drugs that induce or inhibit CYP3A4. Specifically, the concomitant use of the CYP3A4 potent inhibitors ketoconazole and itraconazole is contraindicated. Other CYP3A4 inhibitors including erythromycin, saquinavir, and verapamil should be used with caution. Other drugs that increase potassium concentrations may increase the risk of hyperkalaemia associated with eplerenone therapy, including salt substitutes,[2] potassium supplements and other potassium-sparing diuretics.

General considerations

Due to the high risk of elevated potassium levels in individuals taking eplerenone, The United States FDA suggests routine checks on the individual's potassium level to screen for hyperkalemia.

See also

References

  1. ^ Rossi S, editor. Australian Medicines Handbook 2006. Adelaide: Australian Medicines Handbook; 2006
  2. ^ LoSalt Advisory Statement (PDF)

 
 
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Wikipedia. This article is licensed under the Creative Commons Attribution/Share-Alike License. It uses material from the Wikipedia article "Eplerenone" Read more