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At least 19 recordsLinked to original sources
PubMed1976

[Blood coagulation and fibrinolysis in women receiving estrogen, gestagen and estrogen-gestagen-contraceptives (author's transl)].

Eight femal subjects received a contraceptive with a low estrogen content (Neogynon), the estrogen component (50 mug ethinylestradiol) and consecutively the gestagen component (250 mug D-Norgestrel) of the contraceptive. Each treatment cycle was followed by a control cycle. At various times of the control and therapy cycles several coagulation and fibrinolytic parameters were investigated. Statistical analyses were performed by multivariate two-factorial analysis of variance. Plasminogen exhibities a statistically significant increase during the treatment with ethinylestradiol and the combination of this steroid with D-norgestrel. No significant changes were found for all other parameters, including partial thromboplastin time, fibriogen, factors X, IX, VIII, factor VIII-related antigen, antithrombin III and fibrin(ogen)degradation products.

Adult↗
PubMed1992

Comparison of Yuzpe regimen, danazol, and mifepristone (RU486) in oral postcoital contraception.

OBJECTIVE: To compare the effectiveness and acceptability of three regimens of postcoital contraception. DESIGN: Randomised group comparison of ethinyloestradiol 100 micrograms plus levonorgestrel 500 micrograms repeated after 12 hours (Yuzpe method); danazol 600 mg repeated after 12 hours; and mifepristone 600 mg single dose. SETTING: Community family planning clinic. SUBJECTS: 616 consecutive women with regular cycles aged 16 to 45 years. MAIN OUTCOME MEASURES: Number of pregnancies, incidence of side effects, and timing of next period. RESULTS: The raw pregnancy rates (with 95% confidence intervals) for the Yuzpe, danazol, and mifepristone groups were 2.62% (0.86% to 6.00%), 4.66% (2.15% to 8.67%), and 0% (0% to 1.87%) respectively. Overall, these rates differed significantly (chi 2 = 8.988, df = 2; p = 0.011). The differences between the mifepristone and Yuzpe groups and between the mifepristone and danazol groups were also significant. Side effects were more common and more severe in the Yuzpe group (133 women (70%)) than in either the danazol group (58 (30%)) or the mifepristone group (72 (37%)). The Yuzpe regimen tended to induce bleeding early but mifepristone prolonged the cycle. Three women bled more than seven days late in the Yuzpe group compared with 49 in the mifepristone group. CONCLUSIONS: Mifepristone was effective in reducing expected pregnancy rates and the Yuzpe method also had a clinical effect. Danazol had little or no effect. A further multicentre trial is needed.

Adolescent↗
PubMed1992

A comparison study of lipid and androgen metabolism with triphasic oral contraceptive formulations containing norgestimate or levonorgestrel.

The effects of norgestimate triphasic (Ortho Tri-Cyclen, Tri-Ciles) and levonorgestrel triphasic (Triphasi) formulations on lipid and androgen metabolism were assessed in a study of 66 healthy women treated through six menstrual cycles. Levels of the following were measured: cholesterol and its subfractions, triglycerides, carrier lipoproteins, estradiol, testosterone, and sex hormone binding globulin (SHBG). Comparison of baseline values with values after 3 and 6 months of treatment indicated that both regimens influenced lipid and androgen metabolism. There was a statistically significant between-regimen difference in levels of high-density lipoprotein, which were favorably increased with norgestimate triphasic but reduced with levonorgestrel triphasic. Related data on SHBG showed that plasma levels of this marker of estrogen/androgen balance were increased significantly more in the norgestimate triphasic group, providing additional evidence of low androgenicity. Both regimens inhibited follicular growth to the same extent, as evidenced by low mean levels of estradiol in all on-therapy cycles; and both decreased free testosterone. Side effects in both groups were minor and characteristic of those observed with low-dose oral contraceptive agents. The results of the study support the reported safety and positive effects of norgestimate on lipid and androgen metabolism, in comparison with a levonorgestrel-containing combined oral contraceptive.

Adolescent↗
PubMed1976

[Histochemical and histological investigations on the human fallopian tube under different hormonal influences. I. Demonstration of ATPase with special reference to reactive ciliated cells (author's transl)].

The localization of the Mg++-activated adenosine triphosphatase (ATPase) in the human Fallopian tube has been studied by means of histochemical methods. The samples were obtained from 18 women in the age from 23--62 years. Some of them were treated by various steroid hormones. Endosalpinx ciliary ATPase-activity represents dynein and is therefore an indicator of ciliary motility. Estrogens and gestagens have a different influence on the ATPase-activity. All cilia of one ciliated cell react in the same manner and may be regarded as a reaction unit. The relation of negative to positive ciliary borders differs characteristically in the tubal isthmus, ampulls and infundibulum and coincides with commonly known phenomena of egg transport through the oviduct. Postovulatory, reaction units increase in ampulla and infundibulum compared with the proliferative phase. The oviducts of postmenopausal women possess but a scanty outfit of reaction units. Short-time treatment with estrogen in the early secretory phase results in a great number of reaction units in all tubal segments; a similar treatment in the proliferative phase diminishes the reaction units in the ampulla. Midcycle progesterone treatment activates the ciliary ATPase in the isthmus. Low doses of lynestrenol (minipill) in the proliferative phase leads to a decrease of reaction units in all tubal segments; the pattern of ciliary reaction under low doses of lynestrenol at the time of ovulation coincides with that of the proliferative phase. Treatment with a contraceptive steroid (0,05 mg ethinylestradiol and 0,25 d-norgestrel) causes a considerable activation of the ciliary ATPase in all portions of the oviduct.

Adenosine Triphosphatases↗
PubMed1977

d-Norgestrel concentrations in maternal plasma, milk, and child plasma during administration of oral contraceptives to nursing women.

In order to correlate plasma and milk concentrations of d-norgestrel (d-Ng) in lactating women, three oral contraceptives, containing different amounts of this synthetic gestagen, were given to 15 fully lactating women, starting two months post partum. Plasma and milk samples were collected according to a special schedule. d-Ng concentrations in plasma and milk were measured by radioimmunoassay. When d-Ng was measured in milk, extraction was performed with petroleum ether and in the radioimmunoassay an internal standard was used. This method is evaluated in the present paper. The plasma: milk ratio of d-Ng was found to be about 100:15 and the amounts of d-Ng transferred with 600 ml. of milk per day were calculated to be 0.3 an 0.15 microgram with daily intakes of 250 and 150 microgram of d-Ng, respectively, corresponding to about 0.1 per cent of the given dose. When the women received 30 microgram of d-Ng daily, no d-Ng could be detected in the milk. In three of the breast-fed children the d-Ng concentration in plasma was measured. This concentration was found to be in the same range as would be expected after oral d-Ng medication to adults, allowing for body weight differences, indicating that d-Ng is metabolized and is not accumulated in the baby.

Contraceptives, Oral↗
PubMed1991

Effect of the progestogens, gestodene, 3-keto desogestrel, levonorgestrel, norethisterone and norgestimate on the oxidation of ethinyloestradiol and other substrates by human liver microsomes.

A number of different progestogens, levonorgestrel (LNG), norethisterone (NET), gestodene (GSD), desogestrel (DG) and norgestimate (NORG) are used in combination with the oestrogen ethinyloestradiol (EE2) in oral contraceptive steroid preparations. All the progestogens are acetylenic steroids and previous studies have indicated the potential of acetylenic steroids to cause mechanism-based or "suicide" inactivation of cytochrome P-450. We have compared the effects of the different progestogens on EE2 2-hydroxylation (a reaction catalyzed by enzymes from the P-450IIC, P-450IIIA and P-450IIE gene families) and also the oxidative metabolism of other drug substrates (cyclosporin, diazepam, tolbutamide) by human liver microsomes. On coincubation with EE2 as substrate, GSD, 3-keto desogestrel (3-KD, the active metabolite of desogestrel) and LNG produced some concentration-dependent inhibition of EE2 2-hydroxylation (maximum 32% inhibition at 100 microM 3-keto desogestrel). Ki values determined for GSD and 3-KD were 98.5 +/- 12.3 and 93.2 +/- 10.3 microM (mean +/- SD; n = 4), respectively. Preincubation of progestogens in a small volume (50 microliters) incubation for 30 min in the presence of an NADPH-generating system enhanced the inhibitory potential of all the steroids (at 100 microM, inhibition was for GSD 39%, 3-KD 46%, LNG 46%, NET 51% and NORG 43%). Inhibitory effects were therefore comparable and also similar to the macrolide antibiotic troleandomycin. The most marked inhibition seen was of diazepam N-demethylation and hydroxylation by GSD (71 and 57%, respectively) and 3-KD (62 and 50%, respectively). In preincubation studies involving cyclosporin as the substrate, the order of inhibitory potency was GSD greater than 3-KD greater than NET greater than LNG for production of both metabolite M17 and M21. The results of the study indicate that all the progestogens in common use have the propensity to inhibit a number of oxidative pathways but there is little evidence for one progestogen being more markedly inhibitory than others.

Contraceptives, Oral↗
PubMed1976

The effect of D-norgestrel, 30 micrograms, on the oral glucose tolerance test, including insulin levels, in Thai women.

The effect of D-norgestrel, 30 mug, on the oral glucose tolerance test was studied in 49 Thai women. There was a significant elevation of the blood glucose level at 60 minutes during the test in women who had taken D-norgestrel for 6 and 12 months. Insulin levels in the blood were significantly elevated over control levels in both groups of women at 90, 120, 150, and 180 minutes during the test. There was no difference in the results obtained at 6 months and 12 months. There was also no significant difference in the fasting blood glucose or insulin levels in the three groups of women. The results indicate that D-norestrel at a daily dose of 30 mug has an effect on carbohydrate metabolism in Thai women.

Administration, Oral↗
PubMed1991

A neutrophilic reaction of Sweet's syndrome type associated with the oral contraceptive.

A case is presented of a Sweet's syndrome-like eruption in association with the oral contraceptive. A 46 year old caucasian woman developed recurrent episodes of erythematous tender plaques on her trunk six weeks after commencement of the oral contraceptive (OC). Her condition clinically and histologically resembled Sweet's dermatosis. On cessation of the OC there was complete resolution of her lesions and she remains well 12 months later. This is the first report, to our knowledge, of a neutrophilic reaction to the oral contraceptive, and we believe that drugs may be implicated in the aetiology of atypical neutrophilic reactions simulating Sweet's syndrome in patients who are otherwise well.

Contraceptives, Postcoital, Hormonal↗
PubMed1976

[Effect of an oral contraceptive (ethinylestradiol/D-norgestrel) on growth hormone and insulin secretion].

The growth hormone, insulin and blood glucose values were measured during a glucose tolerance test in 12 women before and after 3 months' use of a contraceptive of the sequential type (11 pills containing 0.05 mg D-norgestrel and 0.05 mg ethinylestradiol and 10 pills containing 0.125 mg D-norgestrel and 0.05 mg ethinylestradiol). Neither fasting blood glucose nor glucose tolerance are altered during administration of the contraceptive steroids. On the other hand, the reactive insulin level is significantly increased in comparison to the basal value, thus showing the signs of hyperinsulinemia. Both the gestagens and the estrogens appear to contribute to this disturbance of insulin secretion. Presumably the hyperinsulinemia is an expression of decreased sensitivity of the peripheral tissue to insulin. The growth hormone, a so-called insulin antagonist, is not responsible for the "insulin resistance" observed. The values measured by us after administration of the contraceptive do not significantly differ from the basal values.

Adult↗
PubMed1991

Ovulatory dysfunction during continuous administration of low-dose levonorgestrel by subdermal implants.

OBJECTIVE: To study the endocrinologic profile of regularly menstruating users of levonorgestrel subdermal implants. DESIGN: Observational, prospective, case-controlled comparative study. SETTING: The Family Planning Clinic of PROFAMILIA, in Santo Domingo, Dominican Republic. PATIENTS, PARTICIPANTS: Thirty one regularly cycling Norplant users and 12 nonhormonal contraceptors who volunteered to participate. INTERVENTIONS: Norplant contraceptive implants were inserted in 31 subjects between 13 and 77 months before this study. MAIN OUTCOME MEASURES: Follicle-stimulating hormone, luteinizing hormone, estradiol (E2), and progesterone (P) were serially assayed for one menstrual cycle. RESULTS: Almost half of the cycles among Norplant users were anovulatory; all the rest (55%) had some form of dysfunction: diminished gonadotropin surge, luteal phase insufficiency (low P levels and shortened luteal phase), and E2 profiles different from normal controls. CONCLUSIONS: Anovulation is clearly one of the main mechanisms of action of Norplant, but even in presumptive ovulatory cycles, the dysfunctions described possibly contribute to the high contraceptive effectiveness of Norplant.

Adult↗
PubMed1990

Modern trends in contraception.

Substantial improvements have been made in oral contraceptives, a new injectable contraceptive (Norplant), and the intrauterine device (IUD). Major risks with oral contraceptives have declined substantially, and a number of noncontraceptive health benefits have been discovered. Norplant is probably the first new contraceptive in recent years, and offers long-term contraception with high efficacy and modest risks. The IUD, by carefully selecting users, is a safe and efficacious contraceptive method. The major risk, pelvic inflammatory disease (PID), is far less common if one avoids use in the presence of risk factors for PID.

Contraceptive Agents, Female↗