A number of oral contraceptive steroids undergo first-pass metabolism in the gastrointestinal mucosa. Ethinyl estradiol (mean systemic bioavailability 40% to 50%) is extensively metabolized, principally to a sulfate conjugate. In vivo studies that use portal vein catheterization and the administration of radiolabeled ethinyl estradiol have shown that the fraction of steroid metabolized in the gut wall is 0.44. In vitro studies with jejunal biopsy samples or larger pieces of jejunum or terminal ileum mounted in Ussing chambers have indicated that more than 30% of added ethinyl estradiol is sulfated. The progestogen desogestrel is a prodrug that is converted to the active metabolite 3-ketodesogestrel. Substantial first-pass metabolism of desogestrel occurs in the gut mucosa, with evidence from Ussing chamber studies for the formation of the active metabolite. Another progestogen, norgestimate, is also metabolized by the gut wall in vitro of which the principal metabolite is the deacetylated product, norgestrel oxime. It seems very likely that this will also occur in vivo. Drug interactions occurring in the gut wall have been reported with ascorbic acid (vitamin C) and paracetamol. 相似文献
Objective To assess the side effects and the continuation rate of combined oral contraceptive(COC) containing desogestrel(Marvelon) during 12 months. Methods This was a post-marketing surveillance study on Marvelon COC among 870 healthy rural women in 5 different counties of Jiangsu Province during 12 months. Results About 24.02% of the women who used Marvelon COC experienced side effects during 12 months. Gastrointestinal disorder,bleeding/spotting and chloasma were ranked the first three in the side ef... 相似文献
Objective: In contrast with combined hormonal contraception, progestin-only contraception is not associated with an increase in venous thromboembolism or stroke. Women with migraine are at increased risk of ischaemic stroke. Several studies have reported a reduction in migraine frequency and intensity with desogestrel 75 µg, a progestin-only pill. At present the quality of data is limited by retrospective study designs, lack of control groups and small sample sizes. We present the first prospective nonrandomised controlled trial.
Methods: A total of 150 women with migraine visiting our clinic for contraceptive counselling were screened. The intervention group comprised women who opted for contraception with desogestrel (n?=?98); the control group comprised women who continued their usual contraceptive (n?=?36). Participants completed daily diaries for 90 days before the intervention and 180 days after the intervention.
Results: In the intervention group, we found improvements in migraine frequency (p?<?.001), migraine intensity (p?<?.001) and the number of triptans used (p?<?.001). These improvements were already significant after 90 days of desogestrel use (p?<?.001). Disability scores also decreased significantly. No improvement was seen in the nonintervention group.
Conclusion: These data demonstrate for the first time in a prospective controlled setting that daily use of the progestin desogestrel is associated with a decrease in migraine frequency, migraine intensity and pain medication use in women with migraine, with and without aura, who had previously been experiencing at least three days of migraine per month.
Objective.?Recently, we found decreased levels of C-reactive protein (CRP) during use of the low-dosed contraceptive implant Implanon®. To further elucidate, whether this finding might be a sign for a lower inflammatory reaction and is associated with changes in levels of other cytokines, we investigated the effect of this implant on interleukin-6 (IL-6) and adiponectin. Plasma lipids and sex hormone levels have been shown to interact with the investigated parameters in vivo and in vitro. Therefore these parameters were measured as well.Design.?Prospective case–control study.Setting.?Family-planning centre, University hospital.Subjects.?Thirty-six non-smoking women with regular cycles.Interventions.?Blood samples for the measurements were taken in the early follicular phase of the cycle in both groups. A second sample was taken 12 weeks after Implanon insertion or in the controls during the early follicular phase of cycle 4.Results.?Implanon did not cause significant changes in IL-6, adiponectin or lipoprotein (Lp)(a). At baseline, there was a significant positive correlation between IL-6 and CRP and a negative correlation between adiponectin and CRP.Conclusion.?We did not observe a negative impact of Implanon on risk markers for atherosclerotic disease such as IL-6, adiponectin, and Lp(a). These data are reassuring for clinicians who prescribe progestagen-only preparations as first choice contraceptives in females with cardiovascular risk factors. 相似文献
In an open, randomized study in an outpatient clinic of a large teaching hospital, thirty-one female volunteers with regular cycles and established ovulation by ultrasonography were given one of two triphasic oral contraceptives containing ethinylestradiol combined with levonorgestrel or desogestrel during six cycles of treatment. The main outcome measures were transvaginal ultrasonography and serum E2 and P measurements in pill cycles 1, 3 and 6.
No ovarian activity was found in 10 subjects. Among the remaining 21 women who showed ovarian activity, most follicle-like structures developed in the pill-free week and decreased in size or disappeared in the first pill week. One women taking triphasic desogestrel had evidence of a luteinized unruptured follicle and one women taking triphasic levonorgestrel had a possible ovulation. The latter women also showed symptoms of lower abdominal pain. A statistically significant difference in ovarian activity between the two oral contraceptives could not be established. The two triphasic oral contraceptives suppressed ovarian activity to the same degree. A trend was seen towards increasing ovarian activity with duration of use in both treatment groups. 相似文献
A randomized, double-blind, group-comparative study was performedover a 6 month period to compare ovarian suppression and vaginalbleeding during the use of three oral contraceptives containingdoses of 30, 50 or 75 µg desogestrel. A total of 44 femalevolunteers with regular cycles and established ovulation byultrasonography were recruited from an out-patient clinic hia university hospital and asked to participate in the study.Ultrasonography and serum oestradiol and progesterone measurementswere performed during two assessment periods. The 75 µgdose showed complete suppression of ovulation and a more acceptablebleeding pattern than the lower doses. The 75 jig dose of desogestrelis the most promising dose for the development of a new progestogen-onlyoral contraceptive agent. 相似文献