A review of the cardiovascular and breast actions of drospirenone in preclinical studies

  title={A review of the cardiovascular and breast actions of drospirenone in preclinical studies},
  author={Tommaso Simoncini and Andrea R Genazzani},
  pages={22 - 33}
Objective Hormone therapy is effective for the relief of menopausal symptoms. For women with a uterus, addition of a progestogen is required to protect the endometrium. However, synthetic progestins differ in certain pharmacological characteristics that may have implications for clinical practice. This literature-based review explores differences in the preclinical and clinical profiles of the progestins used in hormone therapy, focusing on their effects on the cardiovascular system and breast… 

Progestogens used in postmenopausal hormone therapy: differences in their pharmacological properties, intracellular actions, and clinical effects.

Differences in chemical structure, metabolism, pharmacokinetics, affinity, potency, and efficacy via steroid receptors, intracellular action, and biological and clinical effects confirm the absence of a class effect of progestogens.

Estradiol 1 mg and drospirenone 2 mg as hormone replacement therapy in postmenopausal Chinese women

  • S-Q LinL-Z Sun X. Dong
  • Medicine
    Climacteric : the journal of the International Menopause Society
  • 2011
Daily treatment of postmenopausal Chinese women with DRSP/E2 for 16 weeks significantly reduced the incidence of hot flushes and demonstrated advantages vs. placebo for other climacteric symptoms.

Why sex matters: the biological mechanisms of cardiovascular disease

The pathophysiology of CVD in women and its potential clinical implications are reviewed, with particular emphasis on biochemical markers and to indicators of cardiovascular dysfunction and damage.

Factors affecting the choice of drospirenone as the component of combined contraceptive pill in daily clinical practice: the results of nation-wide survey.

Drospirenone is frequently chosen progestogen component in CCP by Polish gynecologists due to its good tolerance, consistent regulation of the menstrual cycle and no spotting in patients opinion and was most frequently used in patients with irregular menstrual cycles and painful menstruation.

One-year randomized study of the endometrial safety and bleeding pattern of 0.25 mg drospirenone/0.5 mg 17β-estradiol in postmenopausal women

The low-dose, 0.25 mg DRSP/0.5 mg E2 dose combination met the criteria for endometrial safety and demonstrated a favorable risk/benefit profile in this 1-year, double-blind, randomized study of postmenopausal women.

Effects of hormone replacement therapy on plasma and tissue fibrinolytic activity in a rat model of surgically induced menopause.

HRT showed beneficial effects by decreasing fibrinolytic activity related to surgically-induced menopause and short-term HRT treatment was associated with a shift in the procoagULant-anticoagulant balance toward a procoAGulant state.

A randomized, double-blind, placebo-controlled study of the lowest effective dose of drospirenone with 17&bgr;-estradiol for moderate to severe vasomotor symptoms in postmenopausal women

Drospirenone 0.25 mg/17&bgr;-estradiol 0.5 mg is concluded to be the lowest dose with demonstrated efficacy in the treatment of postmenopausal women with moderate to severe vasomotor symptoms.

Latest reports on the cardiovascular safety of hormone replacement therapy

W pracy dokonano przeglądu najnowszych doniesień dotyczących powikłań zakrzepowo-zatorowych, zarówno tętniczych, jak i żylnych, związanych ze stosowaniem hormonalnej terapii zastępczej (hormone

MHT vs. veins: is there any reason to fear?

Żylna choroba zakrzepowo-zatorowa (venous thromboembolism – VTE) jest zarówno przeciwwskazaniem, jak i powikłaniem terapii hormonalnej okresu menopauzy (menopausal hormone therapy – MHT). W pracy



Comparative analysis of the uterine and mammary gland effects of drospirenone and medroxyprogesterone acetate.

It is hypothesize that the safety of combined hormone therapy in postmenopausal women may be associated with a dissociation between the uterine and mammary gland activities of the progestin component.

Pharmacology of different progestogens: the special case of drospirenone

  • R. Sitruk-Ware
  • Biology, Medicine
    Climacteric : the journal of the International Menopause Society
  • 2005
Drospirenone, which has pharmacodynamic properties very similar to those of progesterone, has been developed as a combined oral contraceptive and may counteract the negative effect of androgens on hair growth, lipid changes, insulin and, possibly, body composition in postmenopausal women.

Drospirenone, a progestogen with antimineralocorticoid properties: a short review

  • W. Oelkers
  • Medicine, Biology
    Molecular and Cellular Endocrinology
  • 2004

Drospirenone in combination with estrogens: for contraception and hormone replacement therapy

  • W. Oelkers
  • Medicine, Biology
    Climacteric : the journal of the International Menopause Society
  • 2005
Drospirenone is not only a safe option for women using oral contraceptives or HRT, but it may offer new medical benefits, via its antimineralocorticoid and antialdosterone effects and its potential to decrease water retention and blood pressure.

Drospirenone and its antialdosterone properties

The combined actions of drospirenone on sodium and water retention and cardiovascular parameters make it a more attractive therapeutic option as a component of hormone replacement therapy than other synthetic progestins.

Differential signal transduction of progesterone and medroxyprogesterone acetate in human endothelial cells.

Findings show significant differences in the signal transduction pathways recruited by P and MPA in endothelial cells, which may have relevant clinical implications.

Medroxyprogesterone acetate prevents the cardioprotective and anti-inflammatory effects of 17beta-estradiol in an in vivo model of myocardial ischemia and reperfusion.

  • E. BoothB. Lucchesi
  • Biology, Medicine
    American journal of physiology. Heart and circulatory physiology
  • 2007
The results suggest that MPA antagonizes the infarct-sparing effects of E(2), possibly through modulation of the immune response after ischemia and reperfusion.

Medroxyprogesterone Acetate But Not Drospirenone Ablates the Protective Function of 17β-Estradiol in Aldosterone Salt-Treated Rats

The hypothesis of complex interactions among estrogen, progesterone, glucocorticoid, androgen, and mineralocortICoid receptor signaling in cardiovascular injury and inflammation is supported.