Molecular mechanisms of steroid receptor-mediated actions by synthetic progestins used in HRT and contraception

@article{Africander2011MolecularMO,
  title={Molecular mechanisms of steroid receptor-mediated actions by synthetic progestins used in HRT and contraception},
  author={Donita Africander and Nicolette J.D. Verhoog and Janet P. Hapgood},
  journal={Steroids},
  year={2011},
  volume={76},
  pages={636-652}
}

Figures and Tables from this paper

Potency of progestogens used in hormonal therapy: Toward understanding differential actions

Fourth-Generation Progestins Inhibit 3β-Hydroxysteroid Dehydrogenase Type 2 and Modulate the Biosynthesis of Endogenous Steroids

The results suggest that newer, fourth-generation progestins may exert both positive and negative physiological effects via the modulation of endogenous steroid hormone biosynthesis.

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.

Reciprocal Modulation of Antiretroviral Drug and Steroid Receptor Function In Vitro

The ability of TDF and DPV to influence GR and PR activity suggests that their use may be associated with steroid receptor-mediated off-target effects, and raises concerns that reciprocal modulation may cause side effects in a cell- and donor-specific manner in vivo.
...

References

SHOWING 1-10 OF 232 REFERENCES

Disruption of androgen receptor signaling by synthetic progestins may increase risk of developing breast cancer

It is proposed that the observed excess of breast malignancies associated with combined HRT may be explained, in part, by synthetic progestins such as MPA acting as endocrine disruptors to negate the protective effects of androgen signaling in the breast.

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.

Pharmacology of estrogens and progestogens: influence of different routes of administration

  • H. Kuhl
  • Medicine, Biology
    Climacteric : the journal of the International Menopause Society
  • 2005
This review comprises the pharmacokinetics and pharmacodynamics of natural and synthetic estrogens and progestogens used in contraception and therapy, with special consideration of hormone

Progestins and cardiovascular risk markers

The progestational and androgenic properties of medroxyprogesterone acetate: gene regulatory overlap with dihydrotestosterone in breast cancer cells

Clinically, the complex pharmacology of MPA not only influences its side-effect profile; but it is also possible that the increased breast cancer risk and/or the therapeutic efficacy of M PA in cancer treatment is in part mediated by androgen receptor.

Mechanism of action of contraceptive synthetic progestins.

Comparative cardiovascular effects of different progestins in menopause.

  • G. RosanoM. Fini
  • Medicine, Biology
    International journal of fertility and women's medicine
  • 2001
This study has shown that the adjunctive clinical impact of different progestogens on the beneficial effect of estrogen replacement therapy is trivial and that a careful selection of the progestin to be added to estrogen is of capital importance to preserve, or even enhance the positive vascular effects of estrogens.

Conception and pharmacodynamic profile of drospirenone

Drospirenone: pharmacology and pharmacokinetics of a unique progestogen.

...