Description
Generics: Eplerenone.
Dosage Form: Tablet.
Indications:
Hypertension, congestive heart failure after an acute myocardial infarction.
Pharmacology:
Eplerenone selectively binds to the mineralocorticoid receptor and blocks the binding of aldosterone, a key component in the renin-angiotensin-aldosterone-system, which is involved in the regulation of BP and pathophysiology of CV disease. Aldosterone binds to mineralocorticoid receptors in both epithelial (e.g. kidney, GI tract) and nonepithelial (e.g. heart, blood vessels, brain) tissues; causing increases in BP by inducing Na reabsorption, vascular remodelling, water retention, endothelial dysfunction and possibly other mechanisms.
Dosage guideline:
Once Daily.
Congestive Heart Failure after an acute Myocardial Infarction: The recommended dose of Eplerenone is 50 mg once daily. Treatment should be initiated at 25 mg once daily and titrated to the target dose of 50 mg once daily preferably within 4 weeks as tolerated by the patient. Eplerenone may be administered with or without food.
Hypertension:Â Eplerenone may be used alone or in combination with other antihypertensive agents. The recommended starting dose of Eplerenone is 50 mg administered once daily. For patients with an inadequate blood pressure response to 50 mg once daily the dosage of Eplerenone should be increased to 50 mg twice daily. Higher dosages of Eplerenone are not recommended either because they have no greater effect on blood pressure than 100 mg or because they are associated with an increased risk of hyperkalemia.
Route of administration: Orally.
Interaction:
ACE drugs and/or angiotension receptor blockers, ciclosporin, tacrolimus, and trimethoprim may raise the risk of hyperkalemia. NSAIDs, glucocorticoids, and tetracosactide may diminish the antihypertensive impact. TCAs, amifostine, baclofen, and neuroleptics may augment the hypotensive impact of 1-blockers (e.g. alfuzosin, prazosin), TCAs, amifostine, baclofen, and neuroleptics. Mild to moderate CYP3A4 inhibitors may cause an increase in plasma level.
Contraindications:
Eplerenone is contraindicated in-
- Hyperkalaemia
- Severe renal impairment (creatinine clearance less than 30 ml/min)
- Severe hepatic impairment
- Concomitant use with potent CYP3A4 inhibitors like Ketoconazole, Itraconazole, Nefazodone, Troleandomycin, Clarithromycin, Ritonavir, and Nelfinavir or other
- Potassium-sparing diuretics are also contraindicated.
Side Effects:
It is possible to get headaches, dizziness, diarrhea, stomach pain, nausea, cough, or flu-like symptoms. Rashes, itching, swelling, extreme dizziness, and problems breathing are all symptoms of a significant allergic reaction.
Pregnancy & Lactation:
Pregnancy: There are no satisfactory and well-controlled ponders in pregnant ladies. Eplerenone ought to be utilized amid pregnancy as it were in case the potential advantage legitimizes the potential hazard to the fetus.
Lactation: The concentration of Eplerenone in human breast drain after verbal organization is obscure. Since numerous drugs are excreted in human drain and since of the obscure potential for unfavorable impacts on the nursing newborn child, a choice ought to be made whether to cease nursing or cease the sedate, taking under consideration the significance of the sedate to the mother.
Precautions & Warnings:
In hyperkalemia, severe kidney disease, diabetic patients with congestive heart failure following an acute myocardial infarction, especially those with proteinuria, eplerenone should be taken with caution.
Therapeutic Class:
Potassium-sparing diuretics, Potassium-sparing diuretics, and Aldosterone antagonists are all potassium-sparing diuretics.
Storage Conditions:
Store at or below 30°C in a cool, dry location away from light and moisture. Keep out of reach of youngsters.
Manufactured by: UniMed UniHealth Pharmaceuticals Limited.
