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

  title={Drospirenone in combination with estrogens: for contraception and hormone replacement therapy},
  author={W Oelkers},
  pages={19 - 27}
  • W. Oelkers
  • Published 1 January 2005
  • Medicine, Biology
  • Climacteric
Progesterone has a high affinity for the mineralocorticoid receptor and is an antagonist of aldosterone. Almost all synthetic progestogens are devoid of an antimineralocorticoid effect, and are unable to antagonize the salt-retaining effect of estrogens. This property could be one cause of the weight gain and increase in blood pressure associated with the use of combined oral contraceptives and, in some susceptible women, with postmenopausal hormone replacement therapy (HRT). This review… 

Combination of Drospirenone and Estradiol: A New Hormone Therapy in Postmenopausal Women

  • J. Huber
  • Biology, Medicine
    Women's health
  • 2007
The problems that arise in connection with the menopause have been treated for many years with various hormone-replacement therapy formulations. The spironolactone derivative drospirenone is a novel

The use of newer progestins for contraception.

Drospirenone, a progestin with a unique cardiovascular profile, for safe contraception and treatment of menopausal symptoms

  • O. Ylikorkala
  • Medicine
    Climacteric : the journal of the International Menopause Society
  • 2005
A novel progestin is introduced, drospirenone, to be used in combination with ethinylestradiol for oral contraception or with estradiol with potentially harmful side-effects which are potentially harmful and reduce the tolerability of the contraceptive pill or HT.

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

Differences in pharmacological profile among progestins may translate to characteristic divergences in clinical profile, with potential implications for long-term health.

Drospirenone: an antihypertensive in waiting.

  • D. Sica
  • Medicine, Biology
  • 2006
DRSP pharmacokinetics are such that it has an oral bioavailability of &80%, a half-life of 30 to 35 hours, and is without active metabolites, a characteristic that distinguishes it from spironolactone.

Drospirenone: a novel progestin

Drospirenone-containing contraceptives have similar efficacy and safety profiles to other low-dose oral contraceptives, but seem to offer improved tolerability with regard to weight gain, mood changes, acne and treatment of a severe form of premenstrual syndrome called pre menstrual dysphoric disorder.

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.

Oral contraceptive progestins and angiotensin-dependent control of the renal circulation in humans

The results suggest that the OC progestin component is a significant influence on the degree of angiotensin-dependent control of the renal circulation, though these findings may not apply to women with diabetes.



Antimineralocorticoid activity of a novel oral contraceptive containing drospirenone, a unique progestogen resembling natural progesterone.

  • W. Oelkers
  • Biology, Medicine
    The European journal of contraception & reproductive health care : the official journal of the European Society of Contraception
  • 2002
Drospirenone is a new progestogen with antimineralocorticoid and antiandrogenic activity and, due to a lack of sodium retention, may counteract cyclical weight gain and other symptoms related to estrogen-induced fluid retention.

Drospirenone: a new cardiovascular-active progestin with antialdosterone and antiandrogenic properties.

  • A. Rübig
  • Biology, Medicine
    Climacteric : the journal of the International Menopause Society
  • 2003
Phase III studies with E2/DRSP show that DRSP does not antagonize the well-documented reductions of blood pressure associated with E1; rather, small DRSP dose-related reductions in systolic and diastolic blood pressures were observed, which should be beneficial for recipients, especially those who are mildly hypertensive.

Drospirenone: a Novel Progestogen with Antimineralocorticoid and Antiandrogenic Activity

Drospirenone exerts potent progestogenic and antigonadotropic activity which was studied in various animal species and efficiently promotes the maintenance of pregnancy in ovariectomized rats, inhibits ovulation in rats and mice and stimulates endometrial transformation in the rabbit.

Effects of a new oral contraceptive containing an antimineralocorticoid progestogen, drospirenone, on the renin-aldosterone system, body weight, blood pressure, glucose tolerance, and lipid metabolism.

To the authors' knowledge, this is the first report on a combined OC that leads to a small decrease in body weight and blood pressure and may be especially beneficial for women susceptible for a gain in weight and a rise in blood pressure.

Inhibition of ovulation by a novel progestogen (drospirenone) alone or in combination with ethinylestradiol

  • P. RosenbaumW. Schmidt R. Heithecker
  • Medicine
    The European journal of contraception & reproductive health care : the official journal of the European Society of Contraception
  • 2000
The combination of 3 mg drospirenone/30 μg ethinylestradiol (Yasmin ®, Schering AG) reliably inhibits ovulation, with a low frequency of follicular maturation, and provides a reasonable safety margin.

Effects of progesterone and four synthetic progestagens on sodium balance and the renin-aldosterone system in man.

The influence of treatment with progesterone and with 4 synthetic progestagens for 6 days on sodium balance and on different factors of the renin-aldosterone system was investigated in 20 young healthy men on a fixed sodium intake.

Dihydrospirorenone, a new progestogen with antimineralocorticoid activity: effects on ovulation, electrolyte excretion, and the renin-aldosterone system in normal women.

It is concluded that DHSP may be a suitable partner of ethinyl estradiol as a constituent of an oral contraceptive, since its progestogenic and antialdosterone profile is similar to that of progesterone.

Estradiol and drospirenone for climacteric symptoms in postmenopausal women: a double-blind, randomized, placebo-controlled study of the safety and efficacy of three dose regimens

It is demonstrated that the combinations of 1, 2, and 3’mg drospirenone with 1 mg estradiol are safe and effective for the treatment of climacteric symptoms.