The effects of levonorgestrel on various sperm functions.
ABSTRACT Two doses of 750-microg levonorgestrel at 12 h apart is one of the regimens for emergency contraception. The mechanism of action of this regimen is not fully known. We investigated whether levonorgestrel influences sperm functions and thereby, exerts contraceptive activity. The motility, acrosome reaction, zona binding capacity, and oocyte fusion capacity of human spermatozoa treated with 1, 10, and 100 ng/mL levonorgestrel for 3 h were evaluated. Levonorgestrel decreased the curvilinear velocity of the treated spermatozoa in a dose-dependent manner. A significant decrease in straight-line velocity, average path velocity and linearity were also found with 100 ng/mL levonorgestrel treatment. This concentration of levonorgestrel, but not others, also marginally decreased (p = 0.045) the zona binding capacity of the treated spermatozoa. The steroid had no effect on acrosome reaction but had a dose-dependent inhibition on spermatozoa-oocyte fusion. These data show that levonorgestrel affects sperm function only at high concentration and the contribution of these effects to emergency contraception is unlikely to be significant.
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ABSTRACT: This review gives an overview of the mechanisms of action of oral emergency contraception pills (ECPs), focusing on the levonorgestrel (LNG) and ulipristal acetate (UPA) containing ECPs. In vivo and in vitro studies have addressed the effect of EC on various possible targets. Based on these studies as well as on clinical trials it is clear that the efficacy of ECPs to prevent an unintended pregnancy depends on their mechanism of action as well as on their use in relation to the fertile window. While the main effect of both available ECPs is to prevent or delay ovulation the window of action for UPA is wider than that of LNG. This provides the biological explanation for the difference observed in clinical trials and the higher efficacy of UPA. Neither LNG nor UPA impairs endometrial receptivity or embryo implantation. Correct knowledge on the mechanism of action of ECPs is important to avoid overestimating their effectiveness and to advise women on correct use.Gynecological Endocrinology 08/2014; · 1.14 Impact Factor
Article: Emergency contraception.[Show abstract] [Hide abstract]
ABSTRACT: This review summarises the development of emergency contraception (EC) methods, and provides an overview on the currently available options of EC which are effective and safe back-up methods in case of non-use or failure of the regular contraception. The copper intrauterine contraceptive device is currently the most effective method. In most countries, a single dose of levonorgestrel 1.5 mg is the first-line hormonal EC given within 72 h of unprotected intercourse. The oral anti-progestogens such as mifepristone and ulipristal acetate are promising alternatives with better efficacies and a wider treatment window of up to 120 h post coitus, probably resulting from more diverse ancillary mechanisms of actions. Education on EC should be part of any contraceptive counselling. Improving access to EC by providing it over the counter or in advance would not promote its abuse nor encourage risky sexual behaviours, but may further facilitate the timely use so as to achieve the best efficacy.Bailliè re s Best Practice and Research in Clinical Obstetrics and Gynaecology 05/2014; · 3.00 Impact Factor
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ABSTRACT: Human pharmaceuticals are commonly detected in the environment. Concern over these compounds in the environment center around the potential for pharmaceuticals to interfere with the endocrine system of aquatic organisms. The main focus of endocrine disruption research has centered on how estrogenic and androgenic compounds interact with the endocrine system to elicit reproductive effects. Other classes of compounds, such as progestins, have been overlooked. Recently, studies have investigated the potential for synthetic progestins to impair reproduction and growth in aquatic organisms. The present study utilizes the OECD 210 Early-life Stage (ELS) study to investigate the impacts levonorgestrel (LNG), a synthetic progestin, on fathead minnow (FHM) survival and growth. After 28 days post-hatch, survival of larval FHM was impacted at 462ng/L, while growth was significantly reduced at 86.9ng/L. Further analysis was conducted by measuring specific endocrine related mRNA transcript profiles in FHM larvae following the 28 day ELS exposure to LNG. Transcripts of 3β-HSD, 20β-HSD, CYP17, AR, ERα, and FSH were significantly down-regulated following 28d exposure to 16.3ng/L LNG, while exposure to 86.9ng/L significantly down-regulated 3β-HSD, 20β-HSD, CYP19A, and FSH. At 2392ng/L of LNG, a significant down-regulation occurred with CYP19A and ERβ transcripts, while mPRα and mPRβ profiles were significantly induced. No significant changes occurred in 11β-HSD, CYP11A, StAR, LHβ, and VTG mRNA expression following LNG exposure. An ex vivo steroidogenesis assay was conducted with sexually mature female FHM following a 7 day exposure 100ng/L LNG with significant reductions observed in pregnenolone, 17α,20β-dihydroxy-4-pregnen-3-one (17,20-DHP), testosterone, and 11-ketotestosterone. Together these data suggest LNG can negatively impact FHM larval survival and growth, with significant alterations in endocrine related responses.Aquatic toxicology (Amsterdam, Netherlands) 01/2014; 148C:152-161. · 3.12 Impact Factor