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W Carol

Publications and source records attributed to W Carol.

At least 19 recordsLinked to original sources
PubMed1997

[Effect of ethinyl estradiol-dienogest combination on serum androgen concentrations].

Antiandrogens or progestins with an antiandrogenic component usually have only a weak antigonadotropic activity. It is thus possible that the antiandrogenic effect on the cellular level is cancelled or at least reduced by an increased ovarian androgen production. The aim of the four submitted clinical studies of the progestin and antiandrogen dienogest alone (0.5-2 mg/day) or of a combined regimen of ethinylestradiol (0.03 mg) plus dienogest (2 mg) (EE/DNG) was to examine the influence on the serum androgen and SHBG concentrations as well as on the serum FSH, LH, progesterone and 17 beta-estradiol concentrations in young women. Like the progesterone derivatives, dienogest has a relatively low antigonadotropic activity. Inhibition of ovulation is mainly produced by peripheral mechanisms such as the reduction of preovulatory 17 beta-estradiol secretion. Dienogest alone has no significant effects on the serum SHBG and androgen concentrations. Unlike this, the combination of EE plus DNG markedly increases SHBG concentrations (to 2.1-3.7 fold the basal levels). The decrease in serum androgens with total testosterone (by 17 and 40%), free testosterone (by 48 and 54%) and dehydroepiandrosterone sulfate (by 51%) corresponds to the values shown in the literature for other oral contraceptives with modern progestins. EE/DNG does not affect the serum concentrations of 5 alpha-dihydrotestosterone (DHT), although the marker of the peripheral transformation from T to DHT, androstanediol glucuronide, is distinctly reduced (by 38%). In a double-blind comparison no differences are found between EE/DNG and a regimen combining 0.02 mg of ethinylestradiol and 0.150 mg of desogestrel. Solely the SHBG concentrations, with EE/DNG, as expected, are significantly higher. In a sequential regimen, dienogest, chlormadinone acetate and desogestrel (progestins without binding to SHBG) enhance the inhibitory effect of ethinylestradiol sulfonate on free testosterone, whereas norethindrone acetate and levonorgestrel (progestins with a strong binding to SHBG) reduce this effect of the estrogen significantly. These results exclude the possibility that the very distinct antiandrogenic effect of dienogest on a cellular level is neutralised or reduced by an increased systemic supply of androgen.

Adolescent↗
PubMed1992

Pharmacokinetics of ethinylestradiol and levonorgestrel after administration of two oral contraceptive preparations.

Serum concentration profiles and pharmacokinetic parameters (cmax, tmax, AUC24, AUC0-00, MRT) of ethinylestradiol (EE2) and levonorgestrel (LNG) were obtained following administration of two combined oral contraceptives. The constituents of the preparations were as follows: Gravistat (0.05 mg EE2, 0.125 mg LNG); Minisiston (0.03 mg EE2, 0.125 mg LNG). In 20 of the volunteers blood samples were taken before and up to 36 hours following the intake of a single table. In 11 women the investigation was carried out at day 21 of a treatment cycle (steady-state condition). In spite of pronounced interindividual variations of the pharmacokinetic data, a clear dependency of EE2 concentration curves on the estrogen dose of the respective preparation could be demonstrated. Under the condition of steady-state (21st day of administration) there was a slight but significant rise of the EE2 peak serum concentrations and a pronounced increase of the LNG levels, closely reflected by elevation of the AUC values. SHBG serum concentration was significantly increased by the 10th day of treatment in all subjects receiving Gravistat, whereas the mean value in the Minisiston-group did not remarkably change. Although LNG is known to be bound to SHBG with high affinity, the missing parallelism between LNG- and SHBG-concentrations suggests other (additional?) mechanisms for the elevated LNG-binding capacity in women taking combined EE2-LNG preparations.

Administration, Oral↗
PubMed1992

[The diagnostic value of serum hormone parameters in hirsutism].

In 46 patients showing mild or moderate hirsutism, and 49 age-matched regularly menstruating women without symptoms the following hormone and protein serum levels were measured: Total testosterone (T), free testosterone (fT), dehydroepiandrosterone sulfate (DHEAS), androstendione (ASN), sex hormone binding globulin (SHBG), free androgen index (FAI) as expressed by the T/SHBG ratio, cortisol, Prolactin (PRL), LH/FSH ratio, 3 alpha-androstanediol glucuronide (ALG), basal and poststimulated 17-hydroxyprogesteron (17OH-P) and (in some cases) basal and poststimulated 11-deoxycortisol (S). The study was designed for exploring the diagnostic significance of these parameters and evaluating the extent to which they contribute in establishing the source of hyperandrogenism. The mean values of all but one (PRL) of the hormone and protein levels varied significantly from the controls, T, DHEAS, FAI and ALG showing the greatest differences. Most frequently elevations of T, DHEAS, and FAI values were established, the levels of which exhibited a highly significant correlation. In 96% of the hirsute women the elevation of 1 to 3 of these parameters was demonstrated. FAI was shown to be associated with a higher diagnostic accuracy than did SHBG or fT. In 9/43 patients increased values of ALG were found, which as an important metabolite of dihydrotestosterone reflects peripheral androgen activity, particularly of the skin. In every case these abnormal values were combined with elevated levels of other androgens (T, DHEAS, ASN). It is concluded from these limited data that an isolated elevation of ALG due to primary accentuation in 5 alpha-reductase is a rare or even non-existing occurrence.(ABSTRACT TRUNCATED AT 250 WORDS)

Adrenal Hyperplasia, Congenital↗
PubMed1991

Hormone analytical and carrier protein alternations following administration of mifepristone (RU 486) for termination of early pregnancy.

Outpatient terminations were performed on 50 biochemically confirmed pregnancies of 33 to 43 days amenorrhea with a single oral dose of 600 mg of mifepristone (RU 486). 37 women were randomly assigned to an additional endocrine investigation, comprising serum levels of beta hCG, progesterone (P), estradiol (E2), cortisol (C), sexual hormone binding globulin (SHBG), and cortisol binding globulin (CBG) on days 0 and 7 prior to and following the drug administration. Of these 37 patients, 30 experienced a complete expulsion of the uterine contents, 28 until day 7, 2 subjects on day 9 and 10, respectively. The remaining 7 women either showed an unaffected pregnancy or the symptoms of incomplete abortion, which made a surgical intervention necessary. In the successfully treated cases the levels of beta hCG, P and E2 decreased significantly, the nonresponders showed unchanged or even increasing hormone values. No significant changes of cortisol concentrations were found in the group of nonresponders, while the successful cases exhibited a slight elevation probably due to the abortion-associated processes. No considerable therapy-dependent differences were observed in the levels of SHBG. A small but significant decrease in the mean CBG value could be calculated in the group of responders.

Abortion, Spontaneous↗
PubMed1991

[The effect of physical training on the pharmacokinetics of steroidal contraceptives].

In 8 female sports students (runners) aged 20 and 21 years and 10 women between 20 and 40 years of age, who regularly underwent body building training, serum levels of ethinylestradiol (EE2) and levonorgestrel (LNG) have been determined under conditions of exercise as well as in rest, prior to and following the intake of 1 tablet of Gravistat (0.05 mg EE2, 0.125 mg LNG). Blood samples were obtained at points 0, 2, 6 and 24 hours. Exercise (5000 meter running and intensive body building training of one hour duration, respectively) was started immediately after intake of the steroid combination. There were no significant differences in the serum concentration levels obtained during exercise and rest. But exercise consistently resulted in a slight decrease of EE2 and LNG serum concentrations and the area under curve values.

Adult↗
PubMed1991

[Pharmacokinetics of contraceptive steroids with reference to long-term administration].

Pharmacokinetic investigations (c0h, c2h, c6h, c24h, AUC24) were carried out both in the first and last four days of a treatment cycle in patients of different ages, who used oral contraceptives at least for 12 months. 57 women took the preparation Trisiston (three-step-formulation with the components 0.03 mg ethinylestradiol (EE2) + 0.05 mg levonorgestrel (LNG), 0.04 mg EE2 + 0.075 mg LNG, 0.03 mg EE2 + 0.125 mg LNG), 23 subjects used Gravistat (0.05 mg EE2 + 0.125 mg LNG) and 17 patients were under Certostat, a preparation still in clinical evaluation (0.05 mg EE2 + 2.0 mg Dienogest (DNG)). The levels of EE2, LNG and DNG were measured by means of radioimmunoassays. Between the concentrations obtained after administration of a first and single tablet (earlier investigations) and those determined in long-time users during the first 4 days following the tablet-free interval no qualitative and quantitative differences were observed. Between the levels of EE2 and LNG determined in the first and last days of the treatment cycle, marked differences were found in patients under the formulations Trisiston and Gravistat, but not in those taking Certostat. It is concluded that a cyclic and reversible cumulating effect emerges under the influence of LNG-containing contraceptives, the mechanism of which cannot be explained solely by the increase of carrier protein capacity. It seems possibly due to an alteration of steroid metabolism resulting from the interaction between both components.

Adolescent↗
PubMed1991

[Inter- and intra-individual variability of pharmacokinetic parameters for contraceptive steroids].

Serum levels of ethinylestradiol (E2) and levonorgestrel (LNG) have been determined in 10 volunteers of similar age after administration of 1 tablet of the oral contraceptives Gravistat and Ediwal, respectively, each containing 0.05 mg E2 and 0.125 mg LNG, using a cross over design. The studies were carried out at intervals of 4 weeks, within the follicular phase of the menstrual cycle and under standardized conditions. Wide variations were observed between the women in the calculated pharmacokinetic parameters, while there was a relatively close correspondence between the intra-individually obtained values, except for one case.

Adult↗
PubMed1990

[The action of Sequostat in comparison to Sequence Ovosiston on selected metabolic parameters].

The effects of two sequential oral contraceptive preparations, Sequostat (6 days ethinylestradiol 0.05 mg, 15 days ethinylestradiol 0.05 mg + norethisterone acetate 1.0 mg) and Sequence-Ovosiston (9 days mestranol 0.1 mg, 12 days mestranol 0.08 mg + chlormadinone acetate 2.0 mg) on triglycerides, total cholesterol, HDL- and LDL-Cholesterol, glucose tolerance, total plasma proteins, plasma protein fractions, plasma transaminases, gamma-glutamyl-transferase, alkaline phosphatase and antithrombin III were studied in two groups of 46 and 29 young women respectively. Investigations were performed prior to the hormonal intake and after treatment for 3, 6 and 12 months. In nearly all parameters studied significant but minimal changes could be demonstrated which in most cases showed a minor degree in the Sequostat-group, while Sequence-Ovosiston exerted a less effect on glucose tolerance. A significant increase of HDL-cholesterol and a reduction of LDL/HDL-cholesterol relation could be demonstrated at least in the first six months, resulting from the estrogen dominance of the contraceptives.

Adolescent↗
PubMed1990

[Pharmacokinetics of ethinyl estradiol following the administration of combination contraceptive preparations].

A radioimmunoassay for ethinylestradiol (EE2) which was developed in the pharmacological department of VEB Jenapharm has been modified and fully validated. It was the purpose of the present study to extend the still limited data concerning EE2-serum levels after a single and repeated ingestion of combination pills with different doses of EE2. 10 volunteers aged 17-25 years with normal body weight and length received a single tablet of either Gravistat (0.05 mg ethinylestradiol + 0.125 mg levonorgestrel) or Minisiston (0.03 mg ethinylestradiol + 0.125 mg levonorgestrel). 11 other women were involved into the study after ingestion of the 21st tablet of a contraceptive cycle. Peak serum levels which were significantly higher in the Gravistat- than in the Minisiston-group were observed 90 to 120 minutes after the oral administration. Detectable EE2 levels were determined in all volunteers after 24 hours. Pharmacokinetic data showed pronounced interindividual variations. Whereas the mean 24 hours levels of EE2 increased progressively during the treatment cycles, kinetic values obtained at the end of the cycle exhibited a significantly higher level than those after ingestion of a single dose. Area under curve (AUC) was calculated by the trapezoidal rule with the aid of a compartment free model.

Adolescent↗
PubMed1990

[Chlamydia infection in gynecology].

The frequency of chlamydial infections was investigated by means of the McCoy culture technique and a serological procedure using the microimmunofluorescence test in female outpatients showing suspect symptoms; in patients suffering from acute salpingitis, and in women with involuntary infertility. In 18.6% of 290 subjects of the first group, chlamydiae were isolated from cultures. Of 26 patients with acute salpingitis, Chlamydia trachomatis could be detected in 10. The high frequency of positive serological tests suggests chlamydial infection to constitute an important etiological factor in female infertility and extrauterine pregnancies.

Adolescent↗
PubMed1989

[Experiences with the antigestagen mifepristone (RU 486) in the interruption of early pregnancy].

50 healthy women (mean age 29.9 +/- 6.4 years) with early unwanted pregnancy (mean duration 39.3 +/- 2.9 days post menstruationem) received a single oral dose of 600 mg of Mifepristone. Uterine bleedings occurred in all patients within 8 to 110 hours (43 +/- 23.3 hours) after the application, but its duration was very different and correlated with the results of treatment. 39 patients reported on an amount of bleeding exceeding by far the menstrual strength. But in most cases this heavy bleeding lasted only 1-3 days. Frequency of complete abortion was 80% (40 women). 4 patients had an incomplete abortion, and in 6 women the pregnancy was unaffected by the treatment. "Medical abortion" provides a novel alternative to the surgical procedure and is fairly accepted by the patients. Its efficacy, however, should be improved by focusing on early pregnancies not exceeding 10 days after the expected menstrual period and, perhaps, the additional usage of low doses of prostaglandin E derivatives.

Abortion, Induced↗
PubMed1989

[The behavior of cytoplasmic progesterone receptors in the cycling endometrium and the effect of hormonal contraceptives].

Concentration of cytosolic progesterone receptor (PR) was measured by means of an exchange procedure in the endometria of 80 women. Investigations carried out in 35 normal menstruating females showed a gradual increase of PR during the preovulatory and immediate postovulatory phases, decreasing to the lowest level at the end of the cycle. Measurements in endometrial samples obtained from women on combined hormonal contraceptives demonstrated a significant decline of PR concentration in the periovulatory phase resulting in a flattening of the sinusoid PR concentration curve. The stronger down regulation effect of the preparation containing 1.5 mg of dienogest is due to the higher progestogenic efficacy of dienogest in the respective dosage. We consider the down regulation phenomenon a useful means among others to characterize the progestogenic potency of a steroid.

Adult↗
PubMed1988

[Therapeutic use of gonadotropin-releasing hormone and its analogs].

The discovery of the structure of Gn-RH in 1971 has opened new ways of investigation and treatment. The anterior pituitary gland requires episodic Gn-RH stimulation in order to secrete the gonadotropins in a physiologic manner. Deficiency of Gn-RH leads in both sexes to functional disturbances which in females may produce chronic anovulation and amenorrhea. Replacement therapy with the administration of Gn-RH in a pulsatile rhythm corrects the deficiency of endogenous Gn-RH secretion and stimulates via gonadotropins the function of peripheral target organs. If given continuously, Gn-RH leads to desensitization of pituitary Gn-RH receptors and inhibition of LH and FSH secretion. Potent and long-acting agonistic Gn-RH analogs have been synthesized which are capable of producing a selective "medical castration". Indications and preliminary results of the administration of Gn-RH and its long-acting agonists in humans are reviewed.

Contraception↗
PubMed1988

[Prolactin stimulation using the metoclopramide test in females taking oral contraceptives].

In 31 patients taking oral contraceptives (o.c.) for a period between 1 year to more than 3 years, basal serum prolactin levels and metoclopramide induced prolactin values were determined 30 and 60 minutes following an i.v. injection of 10 mg of metoclopramide. The basal prolactin levels were elevated in 7 women to more than 1,000 mU l. The 3 groups of patients taking o.c. with different estrogen doses showed higher drug induced increase of their prolactin levels than the controls. These differences were statistically significant between groups I and III and the control group. No differences could be found between the challenged values of the users groups. The prolactin increase challenged with 200 micrograms TRH in 5 women under o.c. was considerably smaller than that observed in the metoclopramide groups, but exceeded the TRH induced levels found in the controls. The significance of these findings is discussed with special reference to the promotion of prolactinomas.

Adult↗