Skip to main content

Thank you for visiting nature.com. You are using a browser version with limited support for CSS. To obtain the best experience, we recommend you use a more up to date browser (or turn off compatibility mode in Internet Explorer). In the meantime, to ensure continued support, we are displaying the site without styles and JavaScript.

  • Commentary
  • Published:

Does eplerenone have a future in the management of hypertension in Europe?

Journal of Human Hypertension volume 20, pages 829–832 (2006)Cite this article

Eplerenone (Inspra, Pfizer, New York, USA), a 9,11-epoxy derivative of spironolactone, is the second aldosterone antagonist commercially available for the present time. In the USA, it received Food and Drug Administration approval in September 2002 for the treatment of hypertension, and in July 2003 for post-myocardial infarction congestive heart failure.

The medical profession has been looking forward to this new inhibitor of aldosterone receptors as it appears to present significantly fewer adverse effects than does spironolactone, owing to a more selective binding to the mineralocorticoid receptor.1 These effects, gynaecomastia and impotence, stem from a dose-dependent antiandrogen action owing to a nonspecific binding to various steroid receptors,2 which limits the utilization of spironolactone in men. With spironolactone 100 mg daily, the incidence of gynaecomastia in men is 11.5% at 10 months, 15% at 20 months and 29% at 25 months;3 however, this side effect increases to 52% with 150 mg daily or higher.4

This is a preview of subscription content, access via your institution

Relevant articles

Open Access articles citing this article.

Access options

Buy this article

  • Purchase on Springer Link
  • Instant access to full article PDF
Buy now

Prices may be subject to local taxes which are calculated during checkout

References

  1. Menard J . The 45-year story of the development of an anti-aldosterone more specific than spironolactone. Mol Cell Endocrinol 2004; 217: 45–52.

    Article  CAS  Google Scholar 

  2. Corvol P, Michaud A, Menard J, Freifeld M, Mahoudeau J . Antiandrogenic effect of spironolactone: mechanisms of action. Endocrinology 1975; 97: 52–58.

    Article  CAS  Google Scholar 

  3. Froment A, Milon H . Etude en double aveugle de l'adjonction de spironolactone au traitement antihypertenseur thiazidique. La fréquence de la gynécomastie aur cours des tratements prolongés. In: External Activity of Aldosterone and its Antagonists. Excerpta Medica: Paris, 1971, pp 64–69.

    Google Scholar 

  4. Jeunemaitre X, Chatellier G, Kreft-Jais C, Charru A, DeVries C, Plouin PF et al. Efficacy and tolerance of spironolactone in essential hypertension. Am J Cardiol 1987; 60: 820–825.

    Article  CAS  Google Scholar 

  5. Lim PO, Young WF, MacDonald TM . A review of the medical treatment of primary aldosteronism. J Hypertens 2001; 19: 353–361.

    Article  CAS  Google Scholar 

  6. Nishizaka MK, Zaman MA, Calhoun DA . Efficacy of low-dose spironolactone in subjects with resistant hypertension. Am J Hypertens 2003; 16: 925–930.

    Article  CAS  Google Scholar 

  7. Weinberger MH, White WB, Ruilope LM, MacDonald TM, Davidson RC, Roniker B et al. Effects of eplerenone versus losartan in patients with low-renin hypertension. Am Heart J 2005; 150: 426–433.

    Article  CAS  Google Scholar 

  8. Pitt B, Remme W, Zannad F, Neaton J, Martinez F, Roniker B et al. Eplerenone, a selective aldosterone blocker, in patients with left ventricular dysfunction after myocardial infarction. N Engl J Med 2003; 348: 1309–1321.

    Article  CAS  Google Scholar 

  9. Weinberger MH, Roniker B, Krause SL, Weiss RJ . Eplerenone, a selective aldosterone blocker, in mild-to-moderate hypertension. Am J Hypertens 2002; 15: 709–716.

    Article  CAS  Google Scholar 

  10. White WB, Duprez D, St Hillaire R, Krause S, Roniker B, Kuse-Hamilton J et al. Effects of the selective aldosterone blocker eplerenone versus the calcium antagonist amlodipine in systolic hypertension. Hypertension 2003; 41: 1021–1026.

    Article  CAS  Google Scholar 

  11. Flack JM, Oparil S, Pratt JH, Roniker B, Garthwaite S, Kleiman JH et al. Efficacy and tolerability of eplerenone and losartan in hypertensive black and white patients. J Am Coll Cardiol 2003; 41: 1148–1155.

    Article  CAS  Google Scholar 

  12. Williams GH, Burgess E, Kolloch RE, Ruilope LM, Niegowska J, Kipnes MS et al. Efficacy of eplerenone versus enalapril as monotherapy in systemic hypertension. Am J Cardiol 2004; 93: 990–996.

    Article  CAS  Google Scholar 

  13. Burgess ED, Lacourciere Y, Ruilope-Urioste LM, Oparil S, Kleiman JH, Krause S et al. Long-term safety and efficacy of the selective aldosterone blocker eplerenone in patients with essential hypertension. Clin Ther 2003; 25: 2388–2404.

    Article  CAS  Google Scholar 

  14. Pitt B, Reichek N, Willenbrock R, Zannad F, Phillips RA, Roniker B et al. Effects of eplerenone, enalapril, and eplerenone/enalapril in patients with essential hypertension and left ventricular hypertrophy: the 4E-left ventricular hypertrophy study. Circulation 2003; 108: 1831–1838.

    Article  CAS  Google Scholar 

  15. Prisant LM, Krum H, Roniker B, Krause SL, Fakouhi K, He W . Can renin status predict the antihypertensive efficacy of eplerenone add-on therapy? J Clin Pharmacol 2003; 43: 1203–1210.

    Article  CAS  Google Scholar 

  16. Pitt B, Zannad F, Remme WJ, Cody R, Castaigne A, Perez A et al. The effect of spironolactone on morbidity and mortality in patients with severe heart failure. Randomized Aldactone Evaluation Study Investigators. N Engl J Med 1999; 341: 709–717.

    Article  CAS  Google Scholar 

  17. Jessani S, Watson T, Cappuccio FP, Lip GY . Prevention of cardiovascular disease in clinical practice: The Joint British Societies' (JBS 2) guidelines. J Hum Hypertens 2006 (doi:10.1038/sj.jhh.1002058).

    Article  CAS  Google Scholar 

  18. Williams B, Poulter NR, Brown MJ, Davis M, McInnes GT, Potter JF, et al., British Hypertension Society. Guidelines for management of hypertension: report of the fourth working party of the British Hypertension Society, 2004-BHS IV. J Hum Hypertens 2004; 18 (3): 139–185.

    Article  CAS  Google Scholar 

Download references

Author information

Authors and Affiliations

  1. Cardiologie/Hypertension Artérielle, Hypertension Unit Hôpital Saint André, Bordeaux University, 1 rue Jean Burguet, CHU Bordeaux, Bordeaux, France

    P Gosse

  2. University Department of Medicine, City Hospital, Birmingham, UK

    R J Macfadyen

Authors
  1. P Gosse
    View author publications

    You can also search for this author in PubMed Google Scholar

  2. R J Macfadyen
    View author publications

    You can also search for this author in PubMed Google Scholar

Corresponding author

Correspondence to P Gosse.

Rights and permissions

Reprints and permissions

About this article

Cite this article

Gosse, P., Macfadyen, R. Does eplerenone have a future in the management of hypertension in Europe?. J Hum Hypertens 20, 829–832 (2006). https://doi.org/10.1038/sj.jhh.1002070

Download citation

  • Published:

  • Issue Date:

  • DOI: https://doi.org/10.1038/sj.jhh.1002070

This article is cited by

Search

Advanced search

Quick links