Cardiovascular disease, Heart failure, Myocardial infarction, Hypertension
potassium-sparing diuretic
Eplerenone is a blocker of aldosterone binding at the mineralocorticoid receptor. Eplerenone binds to the mineralocorticoid receptor and blocks the binding of aldosterone, a component of the renin-angiotensin-aldosterone-system (RAAS). Aldosterone synthesis, which occurs primarily in the adrenal gland, is modulated by multiple factors, including angiotensin II and non-RAAS mediators such as adrenocorticotropic hormone and potassium. Aldosterone binds to mineralocorticoid receptors in both epithelial (e.g. kidney) and nonepithelial (e.g. heart, blood vessels, and brain) tissues and increases blood pressure through induction of sodium reabsorption and possibly other mechanisms. Eplerenone has been shovvn to produce sustained increases in plasma renin and serum aldosterone, consistent with inhibition of the negative regulatory feedback of aldosterone on renin secretion. The resulting increased plasma renin activity and aldosterone circulating levels do not overcome the effects of Eplerenone.
Adjunct in stable patients with left ventricular ejection fraction 40%with evidence of heart failure, following myocardial infarction (start therapy within 3-14 days of event) | Adjunct in chronic mild heart failure with left ventricular ejection fraction 30% BY MOUTH Adult: Initially 25 mg daily, then increased to 50 mg daily, increased within 4 weeks of initial treatment.
May increase risk of hyperkalaemia with ACE inhibitors and/or angiotension receptor blocker, ciclosporin, tacrolimus, trimethoprim. May reduce antihypertensive effect with NSAIDs, glucocorticoids, tetracosactide. May enhance hypotensive effect of α1-blockers (e.g. alfuzosin, prazosin), TCAs, amifostine, baclofen, neuroleptics. May increase plasma level with mild to moderate CYP3A4 inhibitors (e.g. fluconazole, erythromycin, saquinavir, amiodarone, diltiazem, verapamil).
Common or very common Azotaemia . constipation . cough . diarrhoea . dizziness . hyperkalaemia . hypotension . muscle spasm . musculoskeletal pain . nausea . pruritus . rash . renal impairment . syncope Uncommon Arterial thrombosis . atrial fibrillation . back pain . cholecystitis . dehydration . dyslipidaemia . eosinophilia . epidermal growth factor receptor decreased . flatulence . gynaecomastia . headache . hyperglycaemia . hypoaesthesia . hyponatraemia . hypothyroidism . insomnia . malaise . pharyngitis . postural hypotension . pyelonephritis . sweating . tachycardia . vomiting Frequency not known Angioedema
PREGNANCY Manufacturer advises caution?no information available. BREAST FEEDING Manufacturer advises use only if potential benefit outweighs risk.
Eplerenone store below 30°C in a cool and dry place, protected from light and moisture. Keep out of children’s reach.
.png&w=384&q=75)