Vasomotor symptoms are the most common symptoms of menopause, requiring treatment with estrogen and/or progestogen. Recent international guidelines recognize the need to use the lowest effective dose of hormone replacement therapy. Drospirenone (DR) in combination with 17β-estradiol (E2) is used as hormone therapy (HT) for relief the symptoms and prevention of postmenopausal osteoporosis.The review presents data of 2 large randomized controlled studies that evaluated the lowest effective dose combination DRSP/ E2, the safety of this dose for endometrium, identified features of its pharmacodynamics and pharmacokinetics, depending on various factors. The minimum effective dose for the relief of hot flushes without causing any significant impact on the endometrium is DRSP of 0,25 mg/E2 of 0,5 mg. According to the results of the pharmacokinetic study a correlation between effectiveness of low dose DRSP/E2 with DRSP and E2 exposure levels was showed, and smoking reduces the effectiveness of hormonal therapy. This drug not only copes with moderate to severe hot flushes, but also reduces the incidence of symptoms of vulvovaginal atrophy, improving quality of life.
Treatment with an orally bioavailable prodrug of 17β-estradiol alleviates hot flushes without hormonal effects in the periphery
