The use of newer progestins for contraception

Sitruk-Ware, Régine; Nath, Anita

doi:10.1016/j.contraception.2010.04.004

Cited by 145 publications

(85 citation statements)

References 69 publications

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“…Since the beginning of the 1980s, the third-generation pill relies on three major new progestins (NGM, desogestrel (DSG), and GSD) (10). Drospirenone (DRSP), an aldosterone antagonist, and cyproterone acetate (CPA) are molecules presenting high-anti-androgenic effects and are classified as other generation pills (11). There is no generally accepted way to classify COC.…”

Section: Oral Route Of Administrationmentioning

confidence: 99%

MECHANISMS IN ENDOCRINOLOGY: Epidemiology of hormonal contraceptives-related venous thromboembolism

Hugon-Rodin

Gompel

Plu‐Bureau

2014

European Journal of Endocrinology

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For many years, it has been well documented that combined hormonal contraceptives increase the risk of venous thromboembolism (VTE). The third-generation pill use (desogestrel or gestodene (GSD)) is associated with an increased VTE risk as compared with second-generation (levonorgestrel) pill use. Other progestins such as drospirenone or cyproterone acetate combined with ethinyl-estradiol (EE) have been investigated. Most studies have reported a significant increased VTE risk among users of these combined oral contraceptives (COCs) when compared with users of second-generation pills. Non-oral combined hormonal contraception, such as the transdermal patch and the vaginal ring, is also available. Current data support that these routes of administration are more thrombogenic than second-generation pills. These results are consistent with the biological evidence of coagulation activation. Overall, the estrogenic potency of each hormonal contraceptive depending on both EE doses and progestin molecule explains the level of thrombotic risk. Some studies have shown a similar increased VTE risk among users of COCs containing norgestimate (NGM) as compared with users of second-generation pill. However, for this combination, biological data, based on quantitative assessment of sex hormone-binding globulin or haemostasis parameters, are not in agreement with these epidemiological results. Similarly, the VTE risk associated with low doses of EE and GSD is not biologically plausible. In conclusion, newer generation formulations of hormonal contraceptives as well as non-oral hormonal contraceptives seem to be more thrombogenic than second-generation hormonal contraceptives. Further studies are needed to conclude on the combinations containing NGM or low doses of EE associated with GSD.

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Section: Oral Route Of Administrationmentioning

confidence: 99%

MECHANISMS IN ENDOCRINOLOGY: Epidemiology of hormonal contraceptives-related venous thromboembolism

Hugon-Rodin

Gompel

Plu‐Bureau

2014

European Journal of Endocrinology

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“…The 19-norpregnane derivatives like, for example, promegestone, trimegestone (TMG), nestorone, and nomogesterol acetate, are the most selective agonists of the PGR with very little or no activity for other steroid receptors (Sitruk-Ware & Nath 2010, Stanczyk et al 2013. On the other hand, it is quite common to find androgenic properties among progestins structurally related to testosterone like levonorgestrel (LNG), norethisterone (NET), and tibolone (TIB).…”

Section: Review S Giatti and Others Progestins In The Brainmentioning

confidence: 99%

The other side of progestins: effects in the brain

Giatti

Melcangi

Pesaresi

2016

Journal of Molecular Endocrinology

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Progestins are a broad class of progestational agents widely differing in their chemical structures and pharmacological properties. Despite emerging data suggest that progestins, besides their action as endometrial protection, can also have multiple nonreproductive functions, much remains to be discovered regarding the actions exerted by these molecules in the nervous system. Here, we report the role exerted by different progestins, currently used for contraception or in postmenopausal hormone replacement therapies, in regulating cognitive functions as well as social behavior and mood. We provide evidence that the effects and mechanisms underlying their actions are still confusing due to the use of different estrogens and progestins as well as different doses, duration of exposure, route of administration, baseline hormonal status and age of treated women. We also discuss the emerging issue concerning the relevant increase of these substances in the environment, able to deeply affect aquatic wildlife as well as to exert a possible influence in humans, which may be exposed to these compounds via contaminated drinking water and seafood. Finally, we report literature data showing the neurobiological action of progestins and in particular their importance during neurodegenerative events. This is extremely interesting, since some of the progestins currently used in clinical practice exert neuroprotective and anti-inflammatory effects in the nervous system, opening new promising opportunities for the use of these molecules as therapeutic agents for trauma and neurodegenerative disorders.

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“…In addition, based on earlier work it has been shown that chronic exposure to a mixture of PRG, LNG, DRO induce complex molecular changes both in brain, liver and serum of roach (Rutilus rutilus) [87]. Collectively in vertebrates, progestogens activate nuclear PRG receptors [88], but also may activate other steroid receptors, such as the androgen, estrogen, glucocorticoid and mineralocorticoid receptors, exerting combinations of progestogenic, (anti)androgenic, (anti) estrogenic, glucocorticoidogenic and anti-mineralocorticoidogenic effects [89].…”

Section: Progestogens As Neuroendocrine Disruptors: An Outlook On Thementioning

confidence: 99%

Pond Snail Reproduction as Model in the Environmental Risk Assessment: Reality and Doubts

Pirger¹,

Zrínyi²,

Maász³

et al. 2018

Biological Resources of Water

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In European limnetic systems, the most relevant endocrine-disrupting chemicals (EDCs) of steroid type are the natural and synthetic hormones, phytosterols, pesticides, biocides and other chemicals produced by the plastic industry. Their presence in aquatic ecosystems represents a potentially adverse environmental and public health impact. Furthermore, this is a warning signal that the current handling of pharmaceuticals needs to be further improved. Nowadays, it has become clear that EDCs have specific disturbing effects on the neuroendocrine system of invertebrate and vertebrate aquatic animals, particularly gastropods. Among a latter, pond snail (Lymnaea stagnalis) has been used as the first aquatic non-arthropod test organism in studying the effect of EDCs because they are sensitive to various anthropogenic steroids, like progestogens. Investigating a variety of reproductive endpoints of Lymnaea, such as fecundity, oocyte production, egg mass production, the quality of egg masses, the shell size in development and after egg-laying, the time window of cell division in the offspring, the metabolite content of single-cell zygotes and egg albumen has concluded that progestogen contaminations in water are detrimental for reproduction and early stage development of Lymnaea. This chapter is an attempt to show whether Lymnaea reproduction, despite many altering reproductive endpoints, is a suitable model for environmental risk assessment or not.

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The use of newer progestins for contraception

Cited by 145 publications

References 69 publications

MECHANISMS IN ENDOCRINOLOGY: Epidemiology of hormonal contraceptives-related venous thromboembolism

MECHANISMS IN ENDOCRINOLOGY: Epidemiology of hormonal contraceptives-related venous thromboembolism

The other side of progestins: effects in the brain

Pond Snail Reproduction as Model in the Environmental Risk Assessment: Reality and Doubts

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