Abstract
Unlike other currently available progestogens, drospirenone (DRSP) has a pharmacological
profile, which closely mimics that of endogenous progesterone, most notably potent
anti-aldosterone and anti-androgenic effects. Consequently, DRSP, when combined with
17β-estradiol (E2) as hormone replacement therapy (HRT), offsets E2-related water
and sodium retention by blocking the mineralocorticoid receptor. This review evaluates
the potential benefits offered by DRSP as the progestin component of HRT with respect
to its anti-aldosterone activity, which translates into positive effects on body weight
and blood pressure in clinical trials of continuous, combined E2/DRSP in post-menopausal
women. In a 1-year, large-scale, randomised, controlled trial, E2 1 mg/DRSP 2 mg significantly decreased mean body weight by 1.2 kg versus baseline (P < 0.001), whereas patients receiving E2 1 mg gained weight. E2 1 mg/DRSP 2 mg also significantly lowered mean systolic blood pressure (SBP) by 9.0 mmHg from baseline (P < 0.05) versus 3.7 mmHg in the E2 1 mg group (P = 0.220) in a sub-group of hypertensive women. In addition, E2/DRSP was not associated
with hyperkalaemia (potassium ≥5.5 meq/L) irrespective of concomitant use of ACE inhibitors, angiotensin II receptor
antagonists or non-steroidal anti-inflammatory drugs, and co-morbid diabetes mellitus.
In summary, as well as effectively treating climacteric symptoms, DRSP 2 mg combined with E2 1 mg has shown positive effects on body weight and blood pressure in clinical trials,
most likely due to DRSP's anti-aldosterone properties. This combination may therefore
offer an alternative therapeutic option with additional benefits beyond current HRT
agents for symptomatic post-menopausal women.
Keywords
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Article info
Publication history
Published online: August 14, 2006
Accepted:
July 22,
2006
Received:
July 19,
2006
Identification
Copyright
© 2006 Elsevier Ireland Ltd. Published by Elsevier Inc. All rights reserved.
