Effect on biochemical vasoactive markers during postmenopausal hormone replacement therapy: estradiol versus estradiol/dienogest

Mueck, Alfred O.; Seeger, Harald; Lüdtke, Rainer; Gräser, T; Wallwiener, D.

doi:10.1016/s0378-5122(01)00169-4

Cited by 29 publications

(17 citation statements)

References 23 publications

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“…Average control values for all experiments were pregnancy (Rupnow et al 2002). In contrast, the decreased urine PGI2 metabolite observed after menopause is reversed in women receiving estrogen replacement therapy (Mueck et al 2001).…”

Section: Discussionmentioning

confidence: 92%

“…estrogen therapy (Henriksson et al 1996). Moreover, the ratio of in vivo PGI2 to TXA2 formation increased twofold during estrogen replacement therapy (Mueck et al 2001). Nevertheless, it has also been documented that estrogen increases platelet activation with the liberation of TXA2 in women treated with hormone replacement therapy (Oliveira et al 2005), and that estrogen enhances the constrictor prostanoid function in female rat aorta (Li et al 2008).…”

Section: Discussionmentioning

confidence: 99%

See 1 more Smart Citation

Estradiol selectively stimulates endothelial prostacyclin production through estrogen receptor-α

Sobrino¹,

Oviedo²,

Novella³

et al. 2010

Journal of Molecular Endocrinology

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Estradiol (E 2 ) acts on the endothelium to promote vasodilatation through the release of several compounds, including prostanoids, which are products of arachidonic acid metabolism. Among these, prostacyclin (PGI2) and thromboxane A2 (TXA2) exert opposite effects on vascular tone. The role of different estrogen receptors (ERs) in the PGI2/TXA2 balance, however, has not been fully elucidated. Our study sought to uncover whether E 2 enhances basal production of PGI2 or TXA2 in cultured human umbilical vein endothelial cells (HUVECs), to analyze the enzymatic mechanisms involved, and to evaluate the different roles of both types of ERs (ERa and ERb). HUVECs were exposed to E 2 , selective ERa (1,3,5-tris(4-hydroxyphenyl)-4-propyl-1h-pyrazole, PPT) or ERb (diarylpropionitrile, DPN) agonists and antagonists (unspecific: ICI 182 780; specific for ERa: methyl-piperidino-pyrazole, MPP). PGI2 and TXA2 production was measured by ELISA. Expression of phospholipases, cyclooxygenases (COX-1 and COX-2), PGI2 synthase (PGIS), and thromboxane synthase (TXAS) was analyzed by western blot and quantitative RT-PCR. E 2 (1-100 nM) dose dependently increased PGI2 production (up to 50%), without affecting TXA2 production. COX-1 and PGIS protein and gene expressions were increased, whereas COX-2, phospholipases, and TXAS expression remained unaltered. All these effects were mediated through ERa, since they were produced not only in the presence of E 2 , but also in that of PPT, while they were abolished in the presence of MPP. In conclusion, E 2 , acting through ERa, up-regulates COX-1 and PGIS expression, thus directing prostanoid balance toward increased PGI2 production.

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Section: Discussionmentioning

confidence: 92%

Section: Discussionmentioning

confidence: 99%

Estradiol selectively stimulates endothelial prostacyclin production through estrogen receptor-α

Sobrino¹,

Oviedo²,

Novella³

et al. 2010

Journal of Molecular Endocrinology

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“…69 Changes seen in vasoactive marker with E 2 V/DNG use suggests a possible estrogenic vasorelaxant effect, but the clinical relevance of those changes has not been identified. 70 The impacts of E 2 V/DNG pills on lipids were also studied extensively. In a randomized, open-label 7-cycle study, that pill was compared to a triphasic LNG pill.…”

Section: Hemostatic and Metabolic Effectsmentioning

confidence: 99%

New developments in oral contraception: clinical utility of estradiol valerate/dienogest (Natazia®) for contraception and for treatment of heavy menstrual bleeding: patient considerations

Nelson¹

2012

OAJC

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Natazia ® is a new oral contraceptive with estradiol valerate and dienogest in a unique multiphasic formulation that includes a shortened hormone-free interval. This new formulation has been approved for both contraception and also as a treatment for heavy menstrual bleeding in women who desire to use oral contraceptives as their method of birth control. It is marketed in the US as Natazia ® and elsewhere as Qlaira ® . This article will review the properties of each of the major new features of this pill: estradiol used in place of ethinyl estradiol, dienogest as the progestin, and the unique dosing pattern of this product. It will also summarize the results of the pivotal clinical trials of contraceptive effectiveness, bleeding patterns, safety and tolerability. The lessons learned from the clinical trials about the effectiveness of this formulation in the treatment of excessive menstrual bleeding will be summarized. Also, results of trials comparing this new pill to other popular formulations for "menstrually-related" symptoms and for potential female sexual dysfunction related to use of oral contraceptives will be presented. This review will suggest how all this information might be used to counsel women about how to use this pill most successfully.

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“…In men, there is a decrease in the formation of thromboxane A 2 after the use of high dosage intra-muscular estrogen therapy (Henriksson et al, 1996). Moreover, the ratio of in vivo prostacyclin to thromboxane A 2 formation increases 2-fold during estrogen replacement therapy (Mueck et al, 2001). Nevertheless, it has also been documented that estrogen increases platelet activation with the liberation of thromboxane A 2 in women treated with hormone replacement therapy (Oliveira et al, 2005) and that estrogen enhances the constrictor prostanoid function in female rat aorta (Li et al, 2008).…”

Section: Delayed (Genomic) Effects Of Estrogens On Prostanoids Vasculmentioning

confidence: 99%

Estradiol Regulation of Prostanoids Production in Endothelium

Novella¹,

Hermenegildo²

2011

Basic and Clinical Endocrinology Up-to-Date

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Effect on biochemical vasoactive markers during postmenopausal hormone replacement therapy: estradiol versus estradiol/dienogest

Cited by 29 publications

References 23 publications

Estradiol selectively stimulates endothelial prostacyclin production through estrogen receptor-α

Estradiol selectively stimulates endothelial prostacyclin production through estrogen receptor-α

New developments in oral contraception: clinical utility of estradiol valerate/dienogest (Natazia®) for contraception and for treatment of heavy menstrual bleeding: patient considerations

Estradiol Regulation of Prostanoids Production in Endothelium

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Effect on biochemical vasoactive markers during postmenopausal hormone replacement therapy: estradiol versus estradiol/dienogest

Cited by 29 publications

References 23 publications

Estradiol selectively stimulates endothelial prostacyclin production through estrogen receptor-α

Estradiol selectively stimulates endothelial prostacyclin production through estrogen receptor-α

New developments in oral contraception: clinical utility of estradiol valerate/dienogest (Natazia&reg;) for contraception and for treatment of heavy menstrual bleeding: patient considerations

Estradiol Regulation of Prostanoids Production in Endothelium

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Product

Resources

About

New developments in oral contraception: clinical utility of estradiol valerate/dienogest (Natazia®) for contraception and for treatment of heavy menstrual bleeding: patient considerations