Drospirenone for Oral Contraception and Hormone Replacement Therapy

@article{Motivala2012DrospirenoneFO,
  title={Drospirenone for Oral Contraception and Hormone Replacement Therapy},
  author={Apurva A. Motivala and Bertram Pitt},
  journal={Drugs},
  year={2012},
  volume={67},
  pages={647-655}
}
The use of combined estrogen/progesterone has been shown to result in an increased cardiovascular risk in randomised double-blinded trials. However, these studies used oral progestogen (progestin) preparations, which lack anti-mineralocorticoid activity and have suboptimal anti-androgenic activity compared with progesterone. Drospirenone is a unique progestogen that has clinically been shown to have anti-mineralocorticoid/anti-androgenic effects. Drospirenone in combination with estrogen is… 

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References

SHOWING 1-10 OF 94 REFERENCES

New progestogens in oral contraception.

Advances in oral hormonal contraception.

Researchers continue to search for newer oral contraceptive formulations that retain the pill's beneficial effects while minimizing side effects, and the identification of selective gonane progestins that do not have the same atherogenetic impact as their predecessors.

Effects of a New Hormone Therapy, Drospirenone and 17-&bgr;-Estradiol, in Postmenopausal Women With Hypertension

Data show that DRSP combined with E2 significantly reduces BP in postmenopausal women with hypertension and did not induce significant increases in serum potassium, which may lead to a new benefit for this novel hormone therapy in postwomen's hypertension.

Antihypertensive Effects of Drospirenone With 17&bgr;-Estradiol, a Novel Hormone Treatment in Postmenopausal Women With Stage 1 Hypertension

Combination therapy with DRSP/E2 significantly lowered both clinic and 24-hour systolic BP in postmenopausal women with stage 1 systolics hypertension, which may lead to benefit for cardiovascular risk reduction in this population of women.

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.
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