Kommersiellt obunden läkemedelsinformation riktad till läkare och sjukvårdspersonal

Eplerenon

Klassificering: A

Preparat: Eplerenon Accord, Eplerenon Actavis, Eplerenon Bluefish, Eplerenon Krka, Eplerenon Medical Valley, Eplerenon STADA, Eplerenone Sandoz, Eplerenone Teva, Inspra, Inspra®

ATC kod: C03DA04

Substanser: eplerenon

Sammanfattning

Eplerenon som tilläggsbehandling vid allvarlig hjärtsvikt minskar mortalitet och sjukhusinläggning på ett likvärdigt sätt hos kvinnor och män.

Eplerenon har färre hormonella biverkningar än spironolakton, men dessa kan förekomma vid långtidsbehandling.

Additional information

Pharmacokinetics and dosing

Following administration of single or multiple doses of eplerenone (12.5-100 mg) , no differences in pharmacokinetics parameters were found between men and women [1-4]. Black participants had 19% lower Cmax and 26% lower AUC than White participants at steady state [3, 4].

No sex differences in blood pressure reduction, regardless of dose regimens, have been found, and no sex differentiation in dosing is recommended [3].

Effects

In the major clinical trial of eplerenone in patients with acute myocardial infarction and left ventricular dysfunction, the EPHESUS trial (4714 men, 1918 women), mortality hazard ratios were similar for both sexes [5, 6].

The effects of eplerenone on clinical outcomes in patients with systolic heart failure and mild symptoms were investigated in the EMPHASIS-HF trial (2127 men, 610 women). Hazard ratios for hospitalization for heart failure or death from cardiovascular causes with eplerenone versus placebo were similar for men and women [7].

Adverse effects

Eplerenone is more specific than spironolactone in the effect on the mineralocorticoid receptor with minimal effects at other steroid receptors, thereby minimizing many of the hormonal adverse effects [6]. However, sex hormone-related adverse events that have been seen with eplerenone in clinical trials of hypertension. These are gynecomastia in men and abnormal vaginal bleeding in women. These adverse events increased marginally with longer duration of therapy [8].

In the EPHESUS trial mentioned above, adverse events occurred at a similar rate in both sexes [3, 5].

Reproductive health issues

Regarding teratogenic aspects, please consult the Drugs and Birth Defects Database (in Swedish, Janusmed fosterpåverkan).

Försäljning på recept

Fler män än kvinnor hämtade ut tabletter innehållande eplerenon (ATC-kod C03DA04) på recept i Sverige år 2015, totalt 5 412 män och 1 037 kvinnor. Det motsvarar 1,1 respektive 0,2 personer per tusen invånare. Andelen som hämtat ut läkemedel var högst i åldersgruppen 75-84 år hos båda könen. I genomsnitt var tabletter innehållande eplerenon 5,7 gånger vanligare hos män [7].

Uppdaterat: 2019-06-12

Litteratursökningsdatum: 2019-03-04

Referenser

  1. Croom KF, Perry CM. Eplerenone: a review of its use in essential hypertension. Am J Cardiovasc Drugs. 2005;5:51-69. PubMed
  2. Tolbert DS, Reid SE, Roniker B. Pharmacokinetics of eplerenone in special populations [abstract no 46]. Pharmacotherapy. 2002;22(1):1332.
  3. Inspra (eplerenone). DailyMed [www]. US National Library of Medicine. [updated 2018-06-20, cited 2019-03-04]. länk
  4. Inspra (eplerenon). Summary of Product Characteristics. Swedish Medical Products Agency [updated 2017-03-24, cited 2019-03-04].
  5. 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;348:1309-21. PubMed
  6. Seeland U, Regitz-Zagrosek V. Sex and gender differences in cardiovascular drug therapy. Handb Exp Pharmacol. 2012;214:211-36. PubMed
  7. Zannad F, McMurray JJ, Krum H, van Veldhuisen DJ, Swedberg K, Shi H et al. Eplerenone in patients with systolic heart failure and mild symptoms. N Engl J Med. 2011;364:11-21. PubMed
  8. Moore TD, Nawarskas JJ, Anderson JR. Eplerenone: a selective aldosterone receptor antagonist for hypertension and heart failure. Heart Dis. 2003;5:354-63. PubMed
  9. Läkemedelsstatistik. Stockholm: Socialstyrelsen. 2018 [cited 2019-03-08.] länk

Författare: Linnéa Karlsson Lind

Faktagranskat av: Mia von Euler

Godkänt av: Karin Schenck-Gustafsson