Potency of progestogens used in hormonal therapy: Toward understanding differential actions
@article{Hapgood2014PotencyOP, title={Potency of progestogens used in hormonal therapy: Toward understanding differential actions}, author={Janet P. Hapgood and Donita Africander and Renate Louw and Ramesh M. Ray and Julia Rohwer}, journal={The Journal of Steroid Biochemistry and Molecular Biology}, year={2014}, volume={142}, pages={39-47} }
58 Citations
Pharmacokinetics, metabolism and serum concentrations of progestins used in contraception.
- Biology, MedicinePharmacology & therapeutics
- 2020
Differential metabolism of clinically-relevant progestogens in cell lines and tissue: Implications for biological mechanisms
- BiologyThe Journal of Steroid Biochemistry and Molecular Biology
- 2019
Progestogens as a component of menopausal hormone therapy: the right molecule makes the difference
- Medicine, BiologyDrugs in context
- 2020
Micronized progesterone and dydrogesterone appear to be the safest options, with lower associated cardiovascular, thromboembolic, and breast cancer risks compared with other progestogens, and are the first-choice options for use in ‘special situations,’ such as in women with high-density breast tissue, diabetes, obesity, smoking, and risk factors for venous throm boembolism.
Progestogens exhibit progestogen-, promoter- and isoform-specific effects via the progesterone receptor
- BiologySteroids
- 2022
It is revealed that progestogen responses via PR-A are significantly more potent and less efficacious than those observed viaPR-B, and that this is unlikely due to differences in PR protein levels.
Fourth-Generation Progestins Inhibit 3β-Hydroxysteroid Dehydrogenase Type 2 and Modulate the Biosynthesis of Endogenous Steroids
- Biology, ChemistryPloS one
- 2016
The results suggest that newer, fourth-generation progestins may exert both positive and negative physiological effects via the modulation of endogenous steroid hormone biosynthesis.
Progestogen safety and tolerance in hormonal replacement therapy
- Medicine, BiologyExpert opinion on drug safety
- 2016
Short-term clinical studies, observational, and in animal and in vitro studies indicate that both micronized progesterone and dydrogesterone are the safer progestogens with an acceptable metabolic profile.
Differential Glucocorticoid Receptor‐Mediated Effects on Immunomodulatory Gene Expression by Progestin Contraceptives: Implications for HIV‐1 Pathogenesis
- Biology, MedicineAmerican journal of reproductive immunology
- 2014
It is reported that MPA, unlike NET and progesterone, represses inflammatory genes in human PBMCs in a dose‐dependent manner, via the glucocorticoid receptor (GR), at concentrations within the physiologically relevant range.
A direct comparison of the transcriptional activities of progestins used in contraception and menopausal hormone therapy via the mineralocorticoid receptor.
- BiologyBiochemical and biophysical research communications
- 2020
Recent advances in structure of progestins and their binding to progesterone receptors
- BiologyJournal of enzyme inhibition and medicinal chemistry
- 2015
The aim of this review is to describe the basic structure of PR agonists and antagonists as well as the recent treatments for illness associated with the progesterone receptor.
Comparing the androgenic and estrogenic properties of progestins used in contraception and hormone therapy.
- BiologyBiochemical and biophysical research communications
- 2017
References
SHOWING 1-10 OF 62 REFERENCES
Molecular mechanisms of steroid receptor-mediated actions by synthetic progestins used in HRT and contraception
- Biology, MedicineSteroids
- 2011
Progestogens used in postmenopausal hormone therapy: differences in their pharmacological properties, intracellular actions, and clinical effects.
- Medicine, BiologyEndocrine reviews
- 2013
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.
Multiple nuclear receptor signaling pathways mediate the actions of synthetic progestins in target cells
- BiologyMolecular and Cellular Endocrinology
- 2012
Pharmacology of estrogens and progestogens: influence of different routes of administration
- Medicine, BiologyClimacteric : 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…
Drospirenone: pharmacology and pharmacokinetics of a unique progestogen.
- Biology, MedicineContraception
- 2000
Not all progestins are the same: implications for usage.
- BiologyTrends in pharmacological sciences
- 2004
The preclinical biology of a new potent and selective progestin: trimegestone
- Biology, MedicineSteroids
- 2003
The pharmacological profile of a novel norpregnance progestin (trimegestone).
- Biology, MedicineGynecological endocrinology : the official journal of the International Society of Gynecological Endocrinology
- 1999
Results show trimegestone to have a favorable pharmacological profile with potent progestomimetic activity, and to be not associated with any unwanted pharmacological effects.
Assessment of the potency of orally administered progestins in women.
- Medicine, BiologyFertility and sterility
- 1986