Eplerenone oral
- Drugs List
- Therapeutic Indications
- Dosage
- Contraindications
- Precautions and Warnings
- Pregnancy and Lactation
- Side Effects
- Monograph
Presentation
Oral formulations of eplerenone
Drugs List
Therapeutic Indications
Uses
Cardiac failure secondary to recent M.I.: adjunctive treatment
Chronic cardiac failure (NYHA Class II) with LVEF <31% : adjunct
For addition to standard therapy (including beta-blockers), to reduce to risk of cardiovascular mortality and morbidity in stable patients with left ventricular dysfunction (LVEF equal to or less than 40%) and clinical evidence of heart failure after recent myocardial infarction.
For addition to standard optimal therapy, to reduce the risk of cardiovascular mortality and morbidity in adult patients with New York Heart Association (NYHA) class II (chronic) heart failure and left ventricular systolic dysfunction (LVEF less than or equal to 30%).
Dosage
Adults
Post-myocardial infarction cardiac failure
Initiate treatment at 25 mg once daily and titrate to the target maintenance dose of 50 mg once daily preferably within 4 weeks. Consider the serum potassium levels during titration.
Treatment should be initiated 3 to 14 days after an acute myocardial infarction.
NYHA class II (chronic) cardiac failure
Initiate treatment at 25 mg once daily and titrate to the target maintenance dose of 50 mg once daily preferably within 4 weeks. Consider the serum potassium levels during titration.
Patients with a serum potassium level of greater than 5 mmol/L should not be started on eplerenone. Measure serum potassium prior to therapy, within the first week and at one month after start of treatment or dose adjustment. Assess serum potassium periodically thereafter.
Once initiated, dosage should be based on the serum potassium level.
Serum potassium below 5 mmol/L:
Increase dose from 25 mg every other day to 25 mg once daily.
or
From 25 mg once daily increase to 50 mg once daily.
Serum potassium 5 to 5.4 mmol/L:
No dose adjustment required.
Serum potassium 5.5 to 5.9 mmol/L:
Decrease dose from
50 mg once daily to 25 mg once daily.
or
25 mg once daily to 25 mg every other day.
or
25 mg every other day to withdraw eplerenone therapy.
Serum potassium equal to or greater than 6 mmol/L:
Withdraw eplerenone therapy. This can be re-started once potassium levels fall below 5 mmol/L, at a dose of 25 mg every other day.
Elderly
(See Dosage; Adult).
However the risk of hyperkalaemia is increased in elderly patients, especially with mild to moderate hepatically impaired individuals. Periodic monitoring of serum potassium is recommended.
Patients with Renal Impairment
Moderate renal impairment (creatinine clearance 30 to 60 ml/minute)
Patients should be started at 25 mg every other day, and the dose should be adjusted based on the potassium level.
Monitor serum potassium levels periodically.
Post MI heart failure with creatinine clearance less than 50 ml/minute
Use with caution in these patients.
Doses above 25 mg once daily have not been studied.
The Renal Drug Handbook suggests the following doses for renal impairment:
Glomerular Filtration Rate (GFR)
GFR 20 to 50 ml/minute - Dose as in normal renal function.
GFR 10 to 20 ml/minute - Dose as in normal renal function.
GFR Less than 10 ml/minute - Dose as in normal renal function.
Additional Dosage Information
A maximum dose of 25 mg eplerenone daily may be given when taking concurrent amiodarone, diltiazem or verapamil.
Contraindications
Baseline serum potassium above 5 mmol/L
Children under 18 years
Breastfeeding
Galactosaemia
Renal impairment - eGFR below 30ml/minute/1.73m sq
Severe hepatic impairment
Precautions and Warnings
Elderly
Diabetes mellitus
Glucose-galactose malabsorption syndrome
Lactose intolerance
Mild hepatic impairment
Pregnancy
Renal impairment
Advise ability to drive/operate machinery may be affected by side effects
Contains lactose
Monitor serum potassium levels before treatment
Consider dose reduction if significant rise in serum potassium occurs
Monitor serum potassium regularly
Increased risk of hyperkalaemia with K+ suppl. and K+ sparing diuretic
Advise patient not to take NSAIDs unless advised by clinician
Advise patient not to take St John's wort concurrently
Advise on problems of salt substitutes/high intake of potassium-rich food
Advise patient grapefruit products may increase plasma level
Hyperkalaemia may occur. Monitor potassium levels in all patients at initiation of therapy, within the first week and at one month after the start of treatment or dose adjustment.
One study suggested that the concurrent use of hydrochlorothiazide may offset increases in serum potassium.
Eplerenone is not dialysable.
Monitor serum electrolytes in patients with hepatic impairment.
Pregnancy and Lactation
Pregnancy
Use eplerenone with caution in pregnancy.
Caution when prescribing eplerenone to pregnant women as there is no adequate data.
Animal studies did not indicate direct or indirect adverse effects with respect to pregnancy, embryofoetal development, parturition and post natal development.
The use of all medication in pregnancy should be avoided whenever possible; particularly in the first trimester. Non-drug treatments should also be considered. When essential, a medication with the best safety record over time should be chosen, employing the lowest effective dose for the shortest possible time. Polypharmacy should be avoided. Teratogens taken in the pre-embryonic period, often quoted as lasting until 14 to 17 days post-conception, are believed to have an all-or-nothing effect. Where drugs have a short half-life, and when the date of conception is certain, this may allow women to be reassured where drug exposure has occurred within this time frame. Further advice may be available from the UK National Teratology Information Service (NTIS) and through ToxBase, available via password on the internet ( www.toxbase.org ) or if this is unavailable at the backup site ( www.toxbasebackup.org ).
Lactation
Eplerenone is contraindicated in breastfeeding.
It is unknown if eplerenone is excreted in breast milk.
Because of the unknown potential for adverse effects on the breastfed infant, a decision should be made whether to discontinue the drug or discontinue breastfeeding taking into account the importance of the drug to the mother.
Neonates, infants born prematurely, those with low birth weight, those with an unstable gastrointestinal function or who have serious illnesses may require special consideration. For any infant, if a drug is prescribed to the nursing mother, it should be at the lowest practical dose and for the shortest time. When drug administration is unavoidable and breastfeeding is to continue, minimisation of exposure of the infant to the drug may sometimes be achieved by timing the maternal doses to just after a feeding episode. Infants exposed to drugs via breast milk should be monitored for unusual signs or symptoms. Interactions between the drug received by the infant from the mother's milk and medication prescribed for the infant should also be considered, for example, when the drug given to the infant may prevent metabolism of the drug received via breast milk.
Specialist advice is available from the UK Drugs in Lactation Advisory Service at https://www.midlandsmedicines.nhs.uk/content.asp?section=6&subsection=17&pageIdx=1
Side Effects
Angioedema
Arterial thrombosis
Asthenia
Atrial fibrillation
Azotaemia
Back pain
Blood urea increased
Cholecystitis
Constipation
Cough
Dehydration
Diarrhoea
Dizziness
Elevated blood glucose (transient)
Eosinophilia
Epidermal growth factor receptor decreased
Flatulence
Gynaecomastia
Headache
Hypercholesterolaemia
Hyperhidrosis
Hyperkalaemia
Hypertriglyceridaemia
Hypoaesthesia
Hyponatraemia
Hypotension
Hypothyroidism
Increase in creatinine
Infections
Insomnia
Left ventricular failure
Leg cramps
Malaise
Muscle spasm
Musculoskeletal pain
Myocardial infarction
Nausea
Pharyngitis
Postural hypotension
Pruritus
Pyelonephritis
Rash
Renal impairment
Syncope
Tachycardia
Vomiting
Overdosage
It is strongly recommended that the UK National Poisons Information Service be consulted on cases of suspected or actual overdose where there is doubt over the degree of risk or about appropriate management.
The following number will direct the caller to the relevant local centre (0844) 892 0111
Information may be obtained if you have access to ToxBase the primary clinical toxicology database of the National Poisons Information Service. This is available via password on the internet ( www.toxbase.org ) or if this is unavailable at the backup site ( www.toxbasebackup.org ).
Further Information
Last Full Review Date: August 2016
Reference Sources
Drugs During Pregnancy and Lactation: Treatment Options and Risk Assessment, 2nd edition (2007) ed. Schaefer, C., Peters, P. and Miller, R. Elsevier, London.
Joint Formulary Committee. British National Formulary(online) London: BMJ Group and Pharmaceutical Press Accessed on 17 August 2016.
Summary of Product Characteristics: Eplerenone 25mg/50mg film-coated tablets. Accord Healthcare Ltd. Revised August 2015.
Summary of Product Characteristics: Eplerenone 25mg film-coated tablets. Actavis UK Ltd. Revised March 2016.
Summary of Product Characteristics: Eplerenone 50mg film-coated tablets. Actavis UK Ltd. Revised March 2016.
Summary of Product Characteristics: Eplerenone 25mg film-coated tablets. Consilient Healthcare Ltd. Revised June 2015.
Summary of Product Characteristics: Eplerenone 50mg film-coated tablets. Consilient Healthcare Ltd. Revised June 2015.
Summary of Product Characteristics: Eplerenone 25mg film-coated tablets. Pfizer Ltd. Revised March 2016.
Summary of Product Characteristics: Eplerenone 50mg film-coated tablets. Pfizer Ltd. Revised March 2016.
Summary of Product Characteristics: Eplerenone 25mg film-coated tablets. Zentiva. Revised February 2016.
Summary of Product Characteristics: Eplerenone 50mg film-coated tablets. Zentiva. Revised February 2016.
Summary of Product Characteristics: Inspra 25mg film-coated tablets. Pfizer Ltd. Revised March 2016.
Summary of Product Characteristics: Inspra 50mg film-coated tablets. Pfizer Ltd. Revised March 2016.
The Renal Drug Handbook. Fourth Edition (2014) ed. Ashley, C and Dunleavy, A, Radcliffe Publishing Ltd, London.
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