Monograph
C03DA04 - Eplerenone |
Propably not porphyrinogenic |
PNP |
Rationale
Eplerenone is metabolised by CYP3A4 but does not inhibit or induce CYP 3A4 or 2C9. It is a selective aldosterone antagonist, with less than 1 % affinity for glucocorticoid, progesterone and androgen receptors.
Chemical description
Eplerenone is competitive mineralocorticoid (aldosterone) receptor antagonist.
Therapeutic characteristics
Eplerenone is given orally in the management of hypertension and heart failure. It is an aldosterone antagonist with properties similar to those of spironolactone, but with a higher selectivity for the aldosterone receptor. Eplerenone binds selectively to mineralocorticoid receptors and has low (less than 1%) affinity for glucocorticoid, progesterone, and androgen receptors. The steroid-related adverse effects (e.g., gynecomastia, impotence, menstrual abnormalities) occur less frequently with eplerenone than with spironolactone. Common adverse reactions of eplerenone that can be confused with an acute porphyric attack are diarrhoea, abdominal pain and nausea.
Metabolism and pharmacokinetics
Eplerenone metabolism is primarily mediated via CYP3A4. Eplerenone is not an inhibitor or inducer of the (CYP) isoenzymes 1A2, 3A4, 2C19, 2C9, or 2D6 (Cook, 2002; Muldowney III, 2009; Tolbert, 2002).
References
| # | Citation details | PMID |
|---|---|---|
| * | Scientific articles | |
| 1. | Involvement of CYP3A in the metabolism of eplerenone in humans and dogs: differential metabolism by CYP3A4 and CYP3A5.
Cook CS, Berry LM et al. Drug Metab Dispos. 2002;30(12):1344-51. |
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| 2. | The clinical pharmacology of eplerenone. Expert Opinion on Drug Metabolism and Toxicology 2009; 5(4):425-432.
Muldowney III JAS, Schoenhard JA, et al. |
19379127 |
| 3. | Pharmacokinetics of eplerenone coadministered with other medications [abstract 44]. Pharmacotherapy 2002;22(10):1331
Tolbert DS, Reid SE, et al. |
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| * | Drug reference publications | |
| 4. | McEvoy GK, editor.Eplerenone. The AHFS Drug Information 2008. Bethesda, MD: American Society of Health-System Pharmacists; 2009. Electronic version (08.07.10).
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| 5. | Sweetman SC, editor. Martindale: The complete drug reference.Eplerenone. Pharmaceutical Press 2009.
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| * | Summary of Product Characteristics | |
| 6. | The electronic Medicines Compendium (emc). Summary of Product Characteristics (SPC). Inspra.
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