Drospirenone, a progestogen with antimineralocorticoid properties: a short review

@article{Oelkers2004DrospirenoneAP,
  title={Drospirenone, a progestogen with antimineralocorticoid properties: a short review},
  author={Wolfgang Oelkers},
  journal={Molecular and Cellular Endocrinology},
  year={2004},
  volume={217},
  pages={255-261}
}
  • W. Oelkers
  • Published 31 March 2004
  • Medicine, Biology
  • Molecular and Cellular Endocrinology

Drospirenone and its antialdosterone

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.

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.

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: an antihypertensive in waiting.

  • D. Sica
  • Medicine, Biology
    Hypertension
  • 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.

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.

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.
...

References

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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.

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.

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.

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

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  • 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.

Efficacy and tolerability of a monophasic oral contraceptive containing ethinylestradiol and drospirenone

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The combination of 30 g ethinylestradiol/3 mg drospirenone provides effective oral contraception, excellent cycle control, good tolerability and a level of weight loss that may have a significant beneficial effect on compliance in women with a tendency to weight gain due to water retention.

A new monophasic oral contraceptive containing drospirenone. Effect on premenstrual symptoms.

An oral contraceptive containing drospirenone/ethinyl estradiol may reduce the premenstrual symptoms of negative affect, water retention and increased appetite.

Evaluation of a unique oral contraceptive (Yasmin) in the management of premenstrual dysphoric disorder.

Preliminary results suggest the beneficial effect of DRSP/EE on PMDD and offer an alternative class of medication that also provides the range of benefits of oral contraception for women with PMDD.