Current Hypertension Reports

, 16:414

Converging Indications of Aldosterone Antagonists (Spironolactone and Eplerenone): A Narrative Review of Safety Profiles

  • Mohammed I Danjuma
  • Ipshita Mukherjee
  • Janine Makaronidis
  • Serge Osula
Antihypertensive Agents: Mechanisms of Drug Action (M Ernst, Section Editor)

DOI: 10.1007/s11906-013-0414-8

Cite this article as:
Danjuma, M.I., Mukherjee, I., Makaronidis, J. et al. Curr Hypertens Rep (2014) 16: 414. doi:10.1007/s11906-013-0414-8
Part of the following topical collections:
  1. Topical Collection on Antihypertensive Agents: Mechanisms of Drug Action

Abstract

The converging clinical effectiveness of mineralocorticoid receptor antagonists (MRAs) Spironolactone and Eplerenone has made their safety profiles/cost-effectiveness key determinants of “agents of choice” across a broad range of clinical indications. The clinical biology of the aldosterone molecule and its range of effects in varied organ systems have been well elucidated from recent mechanistic and systematic studies. Clinical experience with Spironolactone is well established, as is its adverse effects profile. The range of adverse effects experienced with Spironolactone subsequently led to its modification and synthesis of Eplerenone. Recent published reports have confirmed lower prevalence rates of sex-related adverse effects attributable to Eplerenone compared to Spironolactone. There is, however, not much to choose between these agents in regards to other adverse effects including hyperkalemia and kidney failure. As was the experience with Spironolactone, as more robust observational data on Eplerenone accrues, it is possible that the real-life experience of its adverse profile may be discordant with that reported by randomized controlled clinical trials (RCTs). In addition, its metabolism by the vulnerable and highly polymorphic cytochrome dependent pathway also makes it susceptible to various drug interactions. The potential implication of the latter (including morbidity and mortality) may take years to evolve.

Keywords

Aldosterone Spironolactone Eplerenone Mineralocorticoid receptor antagonists 

Abbreviations

MR

Mineralocorticoid receptor

MRA

Mineralocorticoid receptor antagonists

EMPHASIS-HF

Eplerenone in Mild Patients Hospitalization And Survival Study in Heart Failure study

CYP

Cytochrome

RCTs

Randomized controlled trials

EPHESUS

Eplerenone Post-Acute Myocardial Infarction Heart Failure Efficacy and Survival Study

RALES

Randomized aldactone evaluation study

ACEIs

Angiotensin converting enzyme inhibitors

ARB

Aldosterone Receptor Blockers

NSAIDS

Nonsteroidal ant-inflammatory drugs

CKD

Chronic kidney disease

ASCOT-BPLA

Anglo-Scandinavian Cardiac Outcomes Trial–Blood Pressure-Lowering Arm

LVH

Left ventricular hypertrophy

GFR

Glomerular filtrate rate

Copyright information

© Springer Science+Business Media New York 2014

Authors and Affiliations

  • Mohammed I Danjuma
    • 1
    • 3
    • 5
  • Ipshita Mukherjee
    • 2
  • Janine Makaronidis
    • 3
  • Serge Osula
    • 4
  1. 1.Consultant in Acute Medicine/ Clinical Pharmacology/Therapeutics and Honorary Clinical Lecturerthe University of LiverpoolLiverpoolUK
  2. 2.Greater Manchester West Mental Health NHS Foundation TrustManchesterUK
  3. 3.Stockport NHS Foundation TrustStepping Hill HospitalStockportUK
  4. 4.Warrington and Halton General HospitalWarringtonUK
  5. 5.Department of MedicineStockport NHS Foundation Trust, Stepping Hill HospitalStockportUK

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