Gestodene: A review of its pharmacology, potency and tolerability in combined contraceptive preparations

Stanczyk, Frank Z.; Archer, David F.

doi:10.1016/j.contraception.2013.12.003

Cited by 29 publications

(8 citation statements)

References 86 publications

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“…NGMN must contribute significantly to the biological activity of NGM in target tissues. NGM-COC provides a pharmacological profile which is probably different from that of LNG-COC (16).…”

Section: Pharmacological Profile Of Progestins Used In Hormonal Contrmentioning

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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“…NGMN must contribute significantly to the biological activity of NGM in target tissues. NGM-COC provides a pharmacological profile which is probably different from that of LNG-COC (16).…”

Section: Pharmacological Profile Of Progestins Used In Hormonal Contrmentioning

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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“…Interest in the 24/4 regimen options was low overall despite their associated benefits such as enhanced ovarian suppression and reduction of menstrual blood loss and cycle-related symptoms [ 4 ], suggesting once again that stronger communication of the specific therapeutic advantages of various OC formulations is necessary. Although all modern OCs provide the universal basic needs of OCs and share many non-contraceptive benefits in common [ 35 ], compositional differences mean that some formulations may be especially well suited for use in certain situations; for example, 2 mg chlormadinone + 0.03 mg ethinylestradiol to improve skin appearance and strengthen hair and nails [ 10 – 18 ]; 3 mg drospirenone + 0.02 mg ethinylestradiol 24+4 tablets to relieve cycle-related symptoms and reduce symptoms of PMS [ 19 – 22 ]; 0.075 mg gestodene + 0.02 mg ethinylestradiol in cases where low-dose estrogen is preferred [ 23 – 25 ]; 0.06 mg gestodene + 0.015 mg ethinylestradiol 24+4 tablets in case where an ultra-low-dose contraceptive is preferred [ 26 – 28 ]; 3 mg drospirenone + 0.03 mg ethinylestradiol to provide good cycle control with negligible effect on body weight [ 29 – 34 ].…”

Section: Discussionmentioning

confidence: 99%

Needs and preferences of women users of oral contraceptives in selected countries in Central and Eastern Europe

Fait¹,

Buryak²,

Cirstoiu³

et al. 2018

DIC

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BackgroundThe availability of various oral contraceptive (OC) pill formulations with different hormone compositions suggests that there is potential to align a particular product with an individual user’s needs and preferences. To explore this concept further, a survey was conducted of current users of OCs to define and confirm areas of specific needs, and to gain insight into their views and preferences for OC formulations.MethodsDuring November and December 2015, women users (n=615) of OCs in five Central and Eastern European countries were surveyed in face-to-face interviews conducted by experienced interviewers. The survey questionnaire comprised 34 questions about the use of and specific needs for OCs.ResultsFour basic needs of women taking OCs were identified: reliable contraception, reversibility of contraception, no effect on body weight and safety. Overall, 85% of surveyed women indicated that prevention of pregnancy was the main reason for taking OCs. Weight gain was the side effect of greatest concern with OC use (46% spontaneous answer; 65% aided answer). Independent behavioural segmentation analysis identified four groups – Solved Cycle Problems (46% of participants), Low Hormone Content (22%), Lifestyle (17%) and Beauty (14%) – which characterised the women according to needs and preferences beyond the basic needs of OCs. Each group had unique features and distinct preferences for different formulations of OCs.ConclusionsAligning product advantages with specific individual needs may enhance users’ overall experience with OCs as a contraceptive option.

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“…In addition to low androgenic activity, desogestrel exhibits high antigonadotropic activity 147 . Gestodene has inherent progestational activity, slight mineralocorticoid activity and high anti-estrogenic activity 148 . Gestodene is characterized by prolonged half-life and 100% oral bioavailability 147 .…”

Section: Testosterone Derivativesmentioning

confidence: 99%

Contraceptive use and the risk of ovarian cancer among women with a BRCA1 or BRCA2 mutation

Xia

Gronwald

Karlan

et al. 2022

Gynecologic Oncology

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BRCA mutation carriers face a high lifetime risk of developing ovarian cancer. Oral contraceptives are protective in this high-risk population; however, the impact of other types of contraception (e.g. intrauterine devices (IUDs), implants, injections) is unknown. This study evaluated the relationships between type of contraception and risk of developing ovarian cancer among women with a BRCA mutation. Ever use of any contraceptive was significantly associated with reduced risk of ovarian cancer, which was driven by significant inverse associations with oral contraceptives and implants. We observed a similar albeit non-significant effect with use of injections and IUDs. No significant associations were observed between patterns of IUD use and risk of ovarian cancer. These findings support a protective effect of oral contraceptives and implants on risk of ovarian cancer among women with a BRCA1 or BRCA2 mutation. The possible reduced risk with use of injections and IUDs requires further evaluation.

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Gestodene: A review of its pharmacology, potency and tolerability in combined contraceptive preparations

Cited by 29 publications

References 86 publications

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

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

Needs and preferences of women users of oral contraceptives in selected countries in Central and Eastern Europe

Contraceptive use and the risk of ovarian cancer among women with a BRCA1 or BRCA2 mutation

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