Estradiol in hormonal contraception: real evolution or just same old wine in a new bottle?

Grandi, Giovanni; Facchinetti, Fabio; Bitzer, Johannes

doi:10.1080/13625187.2017.1372571

Cited by 17 publications

(6 citation statements)

References 19 publications

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“…On the contrary, the most important limitation of this molecule is that it is still used in oral contraceptives only with synthetic estrogens such as EE, even at medium-high dosages (up to 35 µg). In the last years, the market of CHCs has been evolving toward a reduction of EE dose and more metabolically neutral estrogens such as E2 [29] and estetrol (E4) [70] and toward products that will be able to administer these weaker estrogens by non-oral ways of administration [30]. NGM would probably not be suitable for use in these formulations that require progestins with a more uterotropic effect (such as DNG, nomegestrol acetate or nestorone) [29], as NETA and DSG were not, mainly for the not satisfactory cycle control [71,72].…”

Section: Discussionmentioning

confidence: 99%

“…The acquired hypercoagulability seems to be independent of the route of administration of EE [26], but directly dependent on its dose [27,28]. Substitution of EE by oral E2, as performed in the last 10 years, may reduce but not abolish the coagulation stimulus of CHCs [29], though the transdermal/vaginal route of administration would be more neutral in comparison to the oral one [30].…”

Section: Effect Of the Estrogenic Componentmentioning

confidence: 99%

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The paradigm of norgestimate: a third-generation testosterone-derivative progestin with a peripheral anti-androgenic activity and the lowest risk of venous thromboembolism

Grandi

Savio

Facchinetti

2021

Expert Review of Clinical Pharmacology

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Introduction: Norgestimate (NGM) is a testosterone derivative with peculiar receptor activities.Areas covered: This is a narrative review of the available data on the pharmacotherapy of NGM in combined hormonal contraceptives (CHCs) in terms of contraceptive efficacy, venous thromboembolism (VTE) risk, safety, tolerability and bleeding patterns. A comprehensive literature review was conducted in August 2020 using PubMed with the keyword 'norgestimate'. Expert Opinion: NGM shows a mild estrogenic activity associated with anti-mineralocorticoid and antiandrogenic properties, largely responsible for the cardiovascular safety profile. The anti-androgenic property depends on the androgen receptor (AR) nuclear translocation (AR trafficking and its subnuclear distribution), the inhibition of 5α-reductase activity (it possesses higher activity compared to other available progestins), and the increase on sexual hormone binding globulin (SHBG) levels if combined with an estrogenic counterpart. NGM is one of the molecules that best modulates the power of ethinyl-estradiol on the thromboembolic risk, being associated with the lowest VTE risk between different CHCs. NGM has the advantage of retaining peripheral anti-androgenic activity, demonstrated by the impact on lipid and glucose metabolism, and it should be preferred if compared with other similar progestins of the same class of risk which are much more androgenic, such as levonorgestrel.

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Section: Discussionmentioning

confidence: 99%

Section: Effect Of the Estrogenic Componentmentioning

confidence: 99%

The paradigm of norgestimate: a third-generation testosterone-derivative progestin with a peripheral anti-androgenic activity and the lowest risk of venous thromboembolism

Grandi

Savio

Facchinetti

2021

Expert Review of Clinical Pharmacology

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“…L'estradiolo, venendo riconosciuto come estrogeno naturale, contrariamente all'etinilestradiolo, viene catabolizzato nel fegato a estrone (E1) ed estriolo (E3). Inoltre, ha un minor impatto sulla pressione arteriosa, dal momento che rispetto all'etinilestradiolo induce una minor sintesi epatica di angiotensinogeno [31].…”

Section: Composizione Dei Contraccettivi Ormonali: Componente Estroge...unclassified

Patologie mestruali e contraccezione: principi di personalizzazione della scelta terapeutica

et al. 2022

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SommarioLe patologie mestruali sono un problema di salute che affligge dal 5 all’80% delle donne, a seconda della specifica patologia considerata e dei diversi studi. Sono rappresentate da alterazioni del ciclo mestruale (alterazioni del ritmo, della quantità e della durata e dismenorrea) e disturbi extra-uterini correlati alla mestruazione, fra i quali rientrano anche le patologie infiammatorie e autoimmunitarie con esacerbazione catameniale. La contraccezione ormonale offre alle donne non solo un importante strumento per evitare gravidanze indesiderate, ma anche un’efficace opzione terapeutica nel trattamento delle patologie mestruali. I contraccettivi ormonali si dividono in metodi a breve durata d’azione (SARCs), quali contraccettivo orale estroprogestinico (COC), contraccettivo orale progestinico (POP), anello vaginale estroprogestinico e cerotto transdermico estroprogestinico, e metodi a lunga durata d’azione (LARCs), quali dispositivi intrauterini medicati al progesterone e impianto sottocutaneo. La combinazione dell’estrogeno e del progestinico in essi contenuto, nonché i differenti dosaggi e le vie di somministrazione, devono essere tenuti in considerazione nella personalizzazione del trattamento, sia al fine di fornire a ogni donna la terapia più adeguata alle sue necessità e ai suoi disturbi, sia in funzione delle specifiche controindicazioni. In questa rassegna analizziamo brevemente le diverse patologie mestruali, proponiamo una panoramica dei diversi contraccettivi ormonali a oggi disponibili sul mercato e riassumiamo le controindicazioni al loro utilizzo.

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“…Los más seguros son los que contienen LNG o norgestimato, sin que existan diferencias en función de la vía de administración 116 , 117 . Los nuevos preparados con estradiol, frente a los clásicos con etinilestradiol (EE), buscan la reducción del riesgo de TEV, sin significación estadística hasta ahora, y se necesitan series más grandes para sacar conclusiones 118 .…”

Section: Anticoncepciónunclassified

Actividades preventivas en la mujer. Actualización PAPPS 2022

et al. 2022

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Estradiol in hormonal contraception: real evolution or just same old wine in a new bottle?

Cited by 17 publications

References 19 publications

The paradigm of norgestimate: a third-generation testosterone-derivative progestin with a peripheral anti-androgenic activity and the lowest risk of venous thromboembolism

The paradigm of norgestimate: a third-generation testosterone-derivative progestin with a peripheral anti-androgenic activity and the lowest risk of venous thromboembolism

Patologie mestruali e contraccezione: principi di personalizzazione della scelta terapeutica

Actividades preventivas en la mujer. Actualización PAPPS 2022

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