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https://www.readbyqxmd.com/read/27731811/preparation-and-in-vitro-in-vivo-evaluation-of-gestodene-gest-intravaginal-ring
#1
Chunxiao Li, Meiying Ning, Xiaodong Yao, Yankun Wang, Ying Liu
Preparation and in vitro/in vivo evaluation of gestodene (GEST) intravaginal ring (IVR) formulations which can release a constant dose of GEST during 3 weeks were investigated. In present study a reservoir gestodene intravaginal ring, including a gestodene silicone elastomer core and the non-active silicone layer, was reported, which was manufactured by reaction injection moulding at 80°C for 20 min. The raw materials compatibility experiments showed that the silicone elastomer core carrier wouldn't interact with drugs...
September 2016: Pakistan Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/27164970/low-dose-oestrogen-combined-oral-contraception-and-risk-of-pulmonary-embolism-stroke-and-myocardial-infarction-in-five-million-french-women-cohort-study
#2
Alain Weill, Marie Dalichampt, Fanny Raguideau, Philippe Ricordeau, Pierre-Olivier Blotière, Jérémie Rudant, François Alla, Mahmoud Zureik
OBJECTIVE:  To assess the risk of pulmonary embolism, ischaemic stroke, and myocardial infarction associated with combined oral contraceptives according to dose of oestrogen (ethinylestradiol) and progestogen. DESIGN:  Observational cohort study. SETTING:  Data from the French national health insurance database linked with data from the French national hospital discharge database. PARTICIPANTS:  4 945 088 women aged 15-49 years, living in France, with at least one reimbursement for oral contraceptives and no previous hospital admission for cancer, pulmonary embolism, ischaemic stroke, or myocardial infarction, between July 2010 and September 2012...
2016: BMJ: British Medical Journal
https://www.readbyqxmd.com/read/27136904/pharmacokinetics-and-adhesion-of-a-transdermal-patch-containing-ethinyl-estradiol-and-gestodene-under-conditions-of-heat-humidity-and-exercise-a-single-center-open-label-randomized-crossover-study
#3
Christian Zurth, Barbara Schuett, Manuela Casjens, Matthias Ludwig, Katrin Waellnitz
In this open-label, randomized study, 36 women (18-45 years) applied an ethinyl estradiol/gestodene contraceptive patch once-weekly for 3 weeks followed by a 1-week, patch-free interval, in 3 treatment periods. The primary objective was to evaluate the pharmacokinetics of ethinyl estradiol and gestodene under conditions of heat, humidity, and exercise. The secondary objective was to evaluate patch adhesion under the same conditions. Weeks 1 and 2 of each period comprised "standardized normal activity" (SNA); in week 3, SNA continued or women used a sauna, whirlpool, swimming pool, or performed an exercise combination...
July 2015: Clinical Pharmacology in Drug Development
https://www.readbyqxmd.com/read/27134544/permeation-measurement-of-gestodene-for-some-biodegradable-materials-using-franz-diffusion-cells
#4
Danhua Liu, Chong Zhang, Xiaowei Zhang, Zhu Zhen, Ping Wang, Jianxin Li, Dongxu Yi, Ying Jin, Dan Yang
Biodegradable poly(d,l-lactide) (PDLLA), Poly(trimethylene carbonate) (PTMC), polycaprolactone (PCL), poly(caprolactone-co-d,l-lactide) (PCDLLA) and poly(trimethylene carbonate-co-caprolactone) (PTCL) are recently used for clinical drug delivery system such as subcutaneous contraceptive implant capsule due to their biodegradable properties that they could possess long-term stable performance in vivo without removal, however their permeation rate is unknown. In the work, biodegradable material membranes were prepared by solvent evaporation using chloroform, and commercial silicone rubber membrane served as a control...
September 2015: Saudi Pharmaceutical Journal: SPJ: the Official Publication of the Saudi Pharmaceutical Society
https://www.readbyqxmd.com/read/27129041/exposure-to-the-contraceptive-progestin-gestodene-alters-reproductive-behavior-arrests-egg-deposition-and-masculinizes-development-in-the-fathead-minnow-pimephales-promelas
#5
Tyler E Frankel, Michael T Meyer, Dana W Kolpin, Amanda B Gillis, David A Alvarez, Edward F Orlando
Endogenous progestogens and pharmaceutical progestins enter the environment through wastewater treatment plant effluent and agricultural field runoff. Lab studies demonstrate strong, negative exposure effects of these chemicals on aquatic vertebrate reproduction. Behavior can be a sensitive, early indicator of exposure to environmental contaminants associated with altered reproduction yet is rarely examined in ecotoxicology studies. Gestodene is a human contraceptive progestin and a potent activator of fish androgen receptors...
June 7, 2016: Environmental Science & Technology
https://www.readbyqxmd.com/read/26942251/gestodene-ethinvlestradiol-apleek%C3%A2-no-place-for-a-patch-containing-a-third-generation-progestin
#6
(no author information available yet)
No abstract text is available yet for this article.
January 2016: Prescrire International
https://www.readbyqxmd.com/read/26013557/use-of-combined-oral-contraceptives-and-risk-of-venous-thromboembolism-nested-case-control-studies-using-the-qresearch-and-cprd-databases
#7
Yana Vinogradova, Carol Coupland, Julia Hippisley-Cox
OBJECTIVE: To investigate the association between use of combined oral contraceptives and risk of venous thromboembolism, taking the type of progestogen into account. DESIGN: Two nested case-control studies. SETTING: General practices in the United Kingdom contributing to the Clinical Practice Research Datalink (CPRD; 618 practices) and QResearch primary care database (722 practices). PARTICIPANTS: Women aged 15-49 years with a first diagnosis of venous thromboembolism in 2001-13, each matched with up to five controls by age, practice, and calendar year...
May 26, 2015: BMJ: British Medical Journal
https://www.readbyqxmd.com/read/25611781/the-challenge-presented-by-progestins-in-ecotoxicological-research-a-critical-review
#8
REVIEW
Vimal Kumar, Andrew C Johnson, Achim Trubiroha, Jitka Tumová, Masaru Ihara, Roman Grabic, Werner Kloas, Hiroaki Tanaka, Hana Kocour Kroupová
Around 20 progestins (also called gestagens, progestogens, or progestagens) are used today in assisting a range of medical conditions from endometrial cancer to uterine bleeding and as an important component of oral contraception. These progestins can bind to a wide range of receptors including progestin, estrogen, androgen, glucocorticoid, and mineralocorticoid receptor, as well as sex hormone and corticosteroid binding globulins. It appears that only five of these (four synthetic and one natural) progestins have so far been studied in sewage effluent and surface waters...
March 3, 2015: Environmental Science & Technology
https://www.readbyqxmd.com/read/25539793/cardiovascular-risk-in-egyptian-healthy-consumers-of-different-types-of-combined-oral-contraceptives-pills-a-comparative-study
#9
Sahar M El-Haggar, Tarek M Mostafa
This study aimed to evaluate the associated cardiovascular risk in Egyptian healthy consumers of different types of combined oral contraceptives pills (COCPs) via determination of lipids profiles, Castelli index I, leptin, adiponectin, and resistin concentrations as cardiovascular risk factors. In this cross-sectional study, the study groups consisted of control group that represented by 30 healthy married women who were not on any contraceptive mean or any hormonal therapy and had normal menstrual cycles, group two consisted of 30 women who were users of Levonorgesterl 0...
August 2015: Endocrine
https://www.readbyqxmd.com/read/25525393/the-effect-of-pycnogenol-on-patients-with-dysmenorrhea-using-low-dose-oral-contraceptives
#10
Hugo Maia, Clarice Haddad, Julio Casoy
OBJECTIVE: Menstrual symptoms such as dysmenorrhea usually occur during the hormone-free interval in oral contraceptive users. Progestin withdrawal activates NF-κB transcription factor, which upregulates both vascular endothelial growth factor (VEGF) and Cox-2 expression in the endometrium. The use of natural NF-κB inhibitors such as pycnogenol may block this response, improving dysmenorrhea. PATIENTS AND METHODS: Twenty-four patients with severe dysmenorrhea were allocated to one of two treatment groups...
2014: International Journal of Women's Health
https://www.readbyqxmd.com/read/25453585/bleeding-pattern-and-cycle-control-of-a-low-dose-transdermal-contraceptive-patch-compared-with-a-combined-oral-contraceptive-a-randomized-study
#11
RANDOMIZED CONTROLLED TRIAL
M Merz, R Kroll, R Lynen, K Bangerter
OBJECTIVE(S): The aim of this study was to investigate the bleeding pattern and cycle control of a contraceptive patch containing 0.55 mg ethinyl estradiol (EE) and 2.1 mg gestodene (GSD) compared with a combined oral contraceptive (COC) containing 0.02 mg EE and 0.1 mg levonorgestrel (LNG). STUDY DESIGN: In this phase III, randomized, controlled, double-blind, double-dummy, multicenter trial, healthy women aged 18-45 years (smokers aged 18-35 years) received either the EE/GSD patch and a placebo tablet (n=171), or a placebo patch and the COC (n=175) for seven 28-day cycles...
February 2015: Contraception
https://www.readbyqxmd.com/read/25453582/a-comparison-of-bleeding-patterns-and-cycle-control-using-two-transdermal-contraceptive-systems-a-multicenter-open-label-randomized-study
#12
RANDOMIZED CONTROLLED TRIAL
D Gruber, A Skřivánek, M Serrani, V Lanius, M Merz
OBJECTIVE(S): To investigate the bleeding pattern and cycle control parameters of a contraceptive patch containing 0.55 mg ethinyl estradiol (EE) and 2.1 mg gestodene (GSD) compared with a patch containing 0.6 mg EE and 6 mg norelgestromin (NGMN). STUDY DESIGN: In this phase III, open-label, randomized, parallel-group trial, healthy women aged 18-35 years (smokers aged 18-30 years) received either the EE/GSD patch (n=200) or the EE/NGMN patch (n=198). Treatment consisted of one patch per week for 3 weeks followed by a 7-day, patch-free interval for seven cycles...
February 2015: Contraception
https://www.readbyqxmd.com/read/25420716/cycle-related-changes-in-mood-sexual-desire-and-sexual-activity-in-oral-contraception-using-and-nonhormonal-contraception-using-couples
#13
Els Elaut, Ann Buysse, Petra De Sutter, Jan Gerris, Griet De Cuypere, Guy T'Sjoen
Findings on women's sexuality across the menstrual cycle are inconsistent. One relatively consistent finding is a midcycle and premenstrual peak in sexual desire in freely cycling women. Results on the cycle-related effects on sexual behavior are less clear. Large proportions of reproductive-aged women use combined oral contraception (COC), but studies on potential cycle-related shifts in sexual desire and behavior are sparse. A prospective diary study assessed sexual desire, sexual behavior, and mood in 89 heterosexual couples...
2016: Journal of Sex Research
https://www.readbyqxmd.com/read/25295716/pharmacokinetic-overview-of-ethinyl-estradiol-dose-and-bioavailability-using-two-transdermal-contraceptive-systems-and-a-standard-combined-oral-contraceptive
#14
RANDOMIZED CONTROLLED TRIAL
Birte Hofmann, Isabel Reinecke, Barbara Schuett, Martin Merz, Christian Zurth
OBJECTIVE: To determine the relative bioavailability of ethinyl estradiol (EE) and gestodene (GSD) after application of a novel transdermal contraceptive patch vs. a standard combined oral contraceptive (COC) pill (study 1), and to evaluate the pharmacokinetics (PK) of EE after application of the EE/GSD patch compared with an EE/norelgestromin (NGMN) patch (study 2). MATERIALS: Participants were healthy, nonobese women aged 18 - 45 years (study 1) or 18 - 35 years (study 2)...
December 2014: International Journal of Clinical Pharmacology and Therapeutics
https://www.readbyqxmd.com/read/25227335/hormonal-contraception-thrombosis-and-age
#15
REVIEW
Øjvind Lidegaard
INTRODUCTION: This paper reviews the risk of thrombosis with use of different types of hormonal contraception in women of different ages. AREAS COVERED: Combined hormonal contraceptives with desogestrel, gestodene, drospirenone or cyproterone acetate (high-risk products) confer a sixfold increased risk of venous thromboembolism as compared with nonusers, and about twice the risk as compared with users of products with norethisterone, levonorgestrel or norgestimate (low-risk products)...
October 2014: Expert Opinion on Drug Safety
https://www.readbyqxmd.com/read/25138681/implications-of-different-application-sites-on-the-bioavailability-of-a-transdermal-contraceptive-patch-containing-ethinyl-estradiol-and-gestodene-an-open-label-randomized-crossover-study
#16
RANDOMIZED CONTROLLED TRIAL
Joachim Höchel, Barbara Schuett, Matthias Ludwig, Christian Zurth
OBJECTIVES: A novel once-a-week contraceptive patch delivers the same systemic exposure seen with a combined oral contraceptive pill containing 0.02 mg ethinyl estradiol (EE) and 0.06 mg gestodene (GSD). This study evaluated the relative bioavailability of EE and GSD after application of this patch to three different sites. METHODS: In this phase I, open-label, randomized, intra-individual comparison, crossover study, 43 women (aged 18 - 45 years) were randomized to one of six treatment sequences...
October 2014: International Journal of Clinical Pharmacology and Therapeutics
https://www.readbyqxmd.com/read/25012200/epidemiology-of-hormonal-contraceptives-related-venous-thromboembolism
#17
REVIEW
Justine Hugon-Rodin, Anne Gompel, Geneviève Plu-Bureau
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...
December 2014: European Journal of Endocrinology
https://www.readbyqxmd.com/read/24997757/pharmacokinetic-drug-drug-interaction-between-ethinyl-estradiol-and-gestodene-administered-as-a-transdermal-fertility-control-patch-and-two-cyp3a4-inhibitors-and-a-cyp3a4-substrate
#18
RANDOMIZED CONTROLLED TRIAL
Julia Winkler, Mark Goldammer, Matthias Ludwig, Beate Rohde, Christian Zurth
Pharmacokinetic (PK) interactions between the cytochrome P450 3A4 (CYP3A4) pathway and transdermally administered ethinyl estradiol (EE) and gestodene (GSD) were investigated. This paper reports the findings of three open-label, intra-individual, one-way crossover, Phase I trials. In two studies, women used a novel contraceptive patch for 3 weeks during two 4-week study periods; in the second period, the CYP3A4 inhibitors erythromycin (Study 1) or ketoconazole (Study 2) were administered concurrently. In a third study, women received single doses of the CYP3A4 model substrate midazolam, alone and after 3 weeks of concurrent patch application...
December 2015: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/24969733/impact-of-body-mass-index-on-suppression-of-follicular-development-and-ovulation-using-a-transdermal-patch-containing-0-55-mg-ethinyl-estradiol-2-1-mg-gestodene-a-multicenter-open-label-uncontrolled-study-over-three-treatment-cycles
#19
MULTICENTER STUDY
Carolyn L Westhoff, Isabel Reinecke, Keith Bangerter, Martin Merz
BACKGROUND: Body mass index (BMI) may influence ovulation inhibition resulting from transdermal hormone delivery. Investigation of this effect is important given the high prevalence of obesity in the US. STUDY DESIGN: This open-label, uncontrolled, Phase 2b trial stratified 173 women (18-35 years) according to three BMI groups (Group 1, n = 56, ≤ 30 kg/m²; Group 2, n = 55, > 30 kg/m² and ≤ 35 kg/m²; and Group 3, n = 47, > 35 kg/m²). Women used a contraceptive patch containing 0...
September 2014: Contraception
https://www.readbyqxmd.com/read/24961114/-preparation-and-release-mechanism-of-gestodene-reservoir-type-intravaginal-rings
#20
Chun-Xiao Li, Yan-Kun Wang, Mei-Ying Ning
This study taking gestodene (GEST) as a model, investigated the factors affecting reservoir-type intravaginal ring (IVR)'s drug release. This paper reported a gestodene intravaginal ring of reservoir design, comprising a gestodene silicone elastomer core encased in a non-medicated silicone sheath, separately manufactured by reaction injection moulding at 80 degrees C and heating vulcanization at 130 degrees C is reported. The test investigated the factors affecting drug release through a single variable method, taking the drug release rates of 21 days as standards...
March 2014: Yao Xue Xue Bao, Acta Pharmaceutica Sinica
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