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Review

Exploring The Clinical Pharmacokinetics of Eplerenone: A Systematic Review of Published Studies

Mohammed Kanan1★, Rahaf Alshahrani2, Amal Alqahtani2, Nada Wazi3, Khawlah Alsaqiti2, Sana Alassaf3, Miad Alhomaidi4, Samar Abdulrahman5, Reem Jibril6, Haya Alanazi7, Jory Alothman8, Shahad Al Obaid8, Sara Yasin9, Moath Alomairi10, Danah Aljuhani11★ Corresponding author

  1. 1Department of Pharmaceutical Care, Rafha General Hospital, Rafha, 76511, Kingdom of Saudi Arabia.
  2. 2Department of pharmacy, Abha Intel. Private Hospital, Abha, Kingdom of Saudi Arabia.
  3. 3Department of pharmacy, College of pharmacy, King Khalid University, Abha, Kingdom of Saudi Arabia.
  4. 4Department of pharmacy, HNH, private hospital, Abha, Kingdom of Saudi Arabia.
  5. 5Department of pharmacy, King Fahad Medical City, Riyadh, Kingdom of Saudi Arabia.
  6. 6Department of Pharmacy, Jazan University, Jazan, KSA.
  7. 7Department of medicine, King Saud University, Riyadh, Saudi Arabia.
  8. 8Department of medicine, Imam Abdulrahman Bin Faisal University, Dhahran, Saudi Arabia.
  9. 9Department of medicine, Imam Abdulrahman Bin Faisal University, Dammam, Saudi Arabia.
  10. 10Department of medicine, Umm Al-Qura University, Makkah, Saudi Arabia.
  11. 11Department of medicine, Fakeeh College of Medical Sciences, Jeddah, Kingdom of Saudi Arabia.

CORRESPONDENCE

Mohammed Kanan

Department of Pharmaceutical Care, Rafha General Hospital, Rafha, 76511, Kingdom of Saudi Arabia.

Received: 24-05-2024; Accepted: 02-08-2024.

Volume 23, Issue 2 · pp. 3127 · PUBLISHED 2 June 2025 · DOI: 10.18549/PharmPract.2025.2.3127

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ABSTRACT

Eplerenone is the first selective aldosterone antagonist to manage hypertension and congestive heart failure. This comprehensive review aims to collate all the published pharmacokinetic (PK) data on eplerenone by scavenging the relevant articles following oral route of administration in human subjects (healthy & diseased). Five databases, Science Direct, Cochrane Library, EBSCO, Google Scholar, and PubMed, were used systematically to retrieve the relevant studies containing at least one reported PK parameter of eplerenone. A total of 983 articles were identified, in which 08 studies were included after applying the inclusion/exclusion criteria. Eplerenone shows the linear PK profile as the area under the plasma concentration-time curve (AUC) and maximum plasma concentration (Cmax) increase dose-dependently. The Cmax was found to be increased by 2-fold following the administration of multiple doses in healthy as well as in subjects with renal impairment in comparison with single dose. In dialysis subjects, the peak time (Tmax) was significantly shorter than that of the healthy population, 1.28 ± 0.47 hr vs. 2.22 ± 0.75 hr. A significant increase in oral clearance (CL/F) was observed in dialysis patients compared to normal subjects after giving multiple doses. Moreover, co-administration of ketoconazole with eplerenone showed a 1.7-fold increase in Cmax. The current systematic review summarizes all the available PK parameters of eplerenone from the possible accessible studies that can assist clinicians in dosage adjustments in patients with renal failure and avoiding drug-drug interactions.

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    Kanan, M., Alshahrani, R., Alqahtani, A., Wazi, N., Alsaqiti, K., Alassaf, S., Alhomaidi, M., Abdulrahman, S., Jibril, R., Alanazi, H., Alothman, J., Obaid, S. A., Yasin, S., Alomairi, M., & Aljuhani, D. (2025). Exploring The Clinical Pharmacokinetics of Eplerenone: A Systematic Review of Published Studies. Pharmacy Practice, 23(2), 3127. https://doi.org/10.18549/PharmPract.2025.2.3127