A drospirenone-containing oral contraceptive improved bleeding pattern and personal satisfaction in 914 women from Jordan, Lebanon and Syria

Aim: We assessed bleeding pattern, tolerance and patient satisfaction of an oral contraceptive containing 3 mg drospirenone and 30 mcg ethinyl estradiol (DRSP/EE) under real-life conditions. Study Design: We performed a multicenter, prospective, 6-cycle, observational study in Canada, Europe and the Middle East. Detailed analyses of the three Middle East countries, Jordan, Lebanon andSyriawere presented here. The efficacy variables included an assessment of bleeding patterns, premenstrual symptoms of water retention and patient satisfaction, as determined by a visual analogue scale. Results: A total of 914 women were enrolled. The percentage of women with intermenstrual bleeding decreased from 37.4%, 48.7% and 32.2% at baseline to 9.7%, 6.1% and 10.9% at the end of cycle6 inJordan, Lebanon and Syria, respectively (creased sharply in all three countries (p Amenorrhea decreased significantly in Lebanon and Syria (p < 0.005). In addition, signs of water retention like abdominal bloating, breast tenderness and swelling of extremities decreased significantly over the course of 6 treatment cycles (p < 0.001). Patient satisfaction increased for all investigated items. Upon completion of the study, 82.7% of women answered “Yes” to continue treatment with this oral contraceptive. Conclusion: The oral contraceptive containing 3 mg drospirenone and 30 mcg ethinyl estradiol has beneficial effects on bleeding pattern, symptoms of water retention and patient satisfaction.

Effect of tibolone as well as Estradiol and Drospirenone replacement therapy on the neurohumoral indexes and immune function in perimenopausal women

Objective: To explore the effect of tibolone as well as Estradiol and Drospirenone replacement therapy on the neurohumoral indexes and immune function in perimenopausal women. Methods: A total of 180 perimenopausal women who were treated in our hospital between December 2014 and December 2016 were collected and divided into the tibolone group (n=90) as well as Estradiol and Drospirenone group (n=90) by random number table, they received tibolone as well as Estradiol and Drospirenone replacement therapy respectively, and both therapies lasted for 6 months. The differences in serum levels of neurohumoral indexes and immune function indexes were compared between the two groups. Results:Before treatment, differences in serum levels of neurohumoral indexes and immune function indexes were not statistically significant between the two groups. After 6 months of treatment, serum E2, IL-4 and IL-13 levels of both groups of patients were significantly higher than those before treatment while P, T, FSH, LH, PRL, IFN-γ and IL-2 levels were significantly lower than those before treatment, and serum E2, IL-4 and IL-13 levels of observation group were significantly higher than those of control group while P, T, FSH, LH, PRL, IFN-γ and IL-2 levels were significantly lower than those of control group. Conclusion: Both tibolone and Estradiol and Drospirenone can be used in the treatment of women with perimenopausal syndrome, but tibolone is more effective in optimizing hormone levels and equalizing immune function.

Comparison of Drospirenone-with Cyproterone Acetate-Containing Oral Contraceptives, Combined with Metformin and Lifestyle Modifications in Women with Polycystic Ovary Syndrome and Metabolic Disorders： A Prospective Randomized Control Trial

Background：While combined oral contraceptives （COCs） are commonly used to treat polycystic ovary syndrome （PCOS）,comparative data regarding metabolic effects of different progestogens on this patient population are missing.This study aimed to compare the different effects of drospirenone （DRP）-containing COCs with cyproterone acetate （CPA）-containing COCs,combined with metformin and lifestyle modifications in women with PCOS and metabolic disorders.Methods：Ninety-nine women with PCOS and a metabolic disorder between January 2011 and January 2013 were enrolled into this prospective randomized clinical trial.Participants were randomized into two groups such as DRP-containing COCs,and CPA-containing COCs.Participants took COCs cyclically for 6 months,combined with metformin administration （1.5 g/d） and lifestyle modifications （diet and exercise）.Clinical measures and biochemical and hormone profiles were compared.Comparisons for continuous variables were evaluated with paired and unpaired Student＆#39;s t-tests.The Wilcoxon signed rank test was used when the data were not normally distributed.Analysis of covariance was used to control for age,body mass index （BMI）,and baseline data of each analyzed parameter when compared between the two groups.Results：A total of 68 patients have completed the study.The combination regimen of COCs,metformin,and lifestyle modifications in these patients resulted in a significant decrease in BMI,acne,and hirsutism scores when compared to baseline levels in both groups （P 〈 0.05）.Blood pressure （BP） was significantly different in the CPA group when compared to baseline （75.14 ± 6.77 mmHg vs.80.70 ± 5.60 mmHg,P 〈 0.01）,and after 6 months of treatment,only the change in systolic BP was significantly different between the two groups （4.00 [-6.00,13.00] mmHg vs.-3.50 [-13.00,9.00] mmHg,P =0.009）.Fasting glucose,fasting insulin,and homeostasis model assessment-insulin resistance decreased significantly in the DRP group （5.40 ± 0.41 mmol/L vs.5.21 ± 0.32 mmol/L,P =0.041;13.90 [10.50,18.40] μU/ml vs.10.75 [8.60,13.50] μU/ml,P =0.020;3.74 [2.85,4.23] vs.2.55 [1.92,3.40],P =0.008） but did not differ between the two groups.While individual lipid profiles increased in both groups,no statistically significant difference was observed.Conclusions：DRP-containing COCs combined with metformin and lifestyle modifications could better control BP and correct carbohydrate metabolism in women with PCOS and metabolic disorders compared with CPA-containing COCs.

Stereospecific Synthesis of Drospirenone

A procedure for the stereospecific synthesis of drospirenone has been developed. The key steps included the stereospecific reduction of the C7-tertiary alcohol with ZnI2/Et3SiH, a novel mild and stereospecific tertiary alcohol reduction system, and the tandem oxidation/cyclopropanation reactions.

Comparison of Risks of Thromboembolism of Drospirenone-Containing and Nondrospirenone -Containing Combined Oral Contraceptive Use: A Meta-Analysis

This study aimed to estimate the risk of venous thromboembolism(VTE),arterial thromboembolism(ATE),and other side effects following the use of drospirenone(DRSP)-containing combined oral contraceptives(COCs).When compared with non-DRSP-containing COCs,DRSP-containing COCs decreased the risk of VTE by 15%in the overall study population,although this was not statistically significant(adjusted hazard ratio/risk ratio[95%confidence interval]0.85[0.69,1.04]).DRSP-containing COCs also showed significant benefits in terms of ATE risk.The body mass index of the subjects significantly decreased by 0.64 kg/m^(2) after taking the DRSP-containing COCs for 6 months.We concluded that DRSP-containing COCs were safe for use and could be broadly recommended.

Advanced therapy of overweight or obese polycystic ovary syndrome:a prospective study

Objective:To investigate the effects of orlistat combined with drospirenone/ethinylestradiol tablets(DRSP/EE)on anthropometric indices,sexual hormones,hepatorenal function parameters of overweight or obese patients with polycystic ovary syndrome(PCOS).Methods:75 overweight or obese PCOS patients[body mass index(BMI)>24 kg/m^(2)]were recruited within the Department of Gynecological Endocrinology,Beying Obstetrics and Gynecology Hospital,Capital Medical University,from April 2019 to January 2020,for a prospective,randomized,open-labelled comparing study.They were numbered one by one according to the order of recruitement and randomly divided into two groups,group 1 included 50 patients,orlistat plus DRSP/EE;group 2 included 25 patients treated with DRSP/EE alone.Both groups got the same comprehensive intervention in terms of individualized,standardized managment and monitoring of life-style like diet and exercise.The changes of anthropometric indices,sexual hormones,hepatorenal function parameters before and after three months of treatment in the two groups were compared.Results:After three months of treatment,body weight,waist circumference(WC),hip circumference(HC)and BMI of both groups were significantly decreased(P<0.05).The decrease of body weight,WC,HC and BMI in group 1 was significantly greater than those in group 2(P<0.05).Free testosterone and sex hormone-binding globulin in both groups were significantly changed(P<0.05).There was no significant difference in the hepatorenal function parameters between the two groups after three months treatment(P>0.05).Conclusion:To our knowledge our study is the first to investigate the effects of orlistat combined with DRSP/EE in overweight or obese PCOS patients comparing with the effect of using DRSP/EE alone.Orlistat combined with DRSP/EE was better than use DRSP/EE alone in getting weight loss,which provides an evidence for the choice of rational drug use in clinical practice.

Abiotic transformation of synthetic progestins in representative soil mineral suspensions

Altrenogest(ALT),drospirenone(DRO),and melengestrol acetate(MLA)are three highly potent synthetic progestins that can be released into agricultural soils,while their fate in soil minerals remains unclear.This study explored the transformation of these progestins in MnO_(2),SiO_(2),and ferrihydrite suspensions and identified their transformation products(TPs)via high resolution mass spectrometry and density functional theory calculations.Transformations were only observed for DRO and MLA in SiO_(2) suspension and ALT in MnO_(2) suspension(half-lives=0.86 min–9.90 day).ALT transformation was facilitated at higher MnO_(2) loadings,while DRO and MLA transformations were inhibited at higher SiO_(2) loadings.These data indicated that hydrophobic partitioning interactionwas dominant at higher SiO_(2) loadings rather than specific interaction,which limited subsequent surface-catalyzed transformation.ALT transformation rate decreased with increasing pH because MnO_(2) reduction requires proton participation.In contrast,relatively high pH facilitated MLA and DRO transformation,indicating that base-catalyzed hydrolysis occurred in SiO_(2) suspension.The clustermap demonstrated the formation of abundant TPs.Lactone ring and acetoxy group hydrolysis was the major transformation pathway for DRO and MLA,with estimated yields of 57.7%and 173.2%at 6 day,respectively.ALT experienced C12 hydroxylation and formed the major TP 326g(yield of 15.4%at 8 hr).ALT also experienced allyl group oxidation and subsequent C5 hydroxylation,forming the major TP 344a(yield of 14.1%at 8 hr).This study demonstrates that TPs ofmetastable progestins are likely the main species in soils and that TP identification is a particular priority for risk assessment.