Restovar--new low-dose, combined, oral contraceptive. Effects on serum proteins, free testosterone and clinical efficacy.
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Acne Vulgaris↗
Biomedical subjects
G Cullberg
Publications and source records attributed to G Cullberg.
Effects of a continuous estrogen-progestogen therapy for climacteric symptoms on circulating sex steroids and gonadotrophins.
Twenty-six peri- and postmenopausal women with climacteric symptoms were given each day for 1 year a tablet containing 2 mg 17-beta-estradiol, 1 mg estriol and 1 mg norethisterone acetate. Blood samples were collected before, after 3 months and after 12 months of treatment and were analysed for their gonadotrophins, estradiol, estrone, testosterone, androstenedione content and for their SHBG binding capacity. Serum levels of estrone and androstenedione before treatment were found to be higher in the perimenopausal than in the postmenopausal group. An increase of serum estrogens concomitant with a decrease of gonadotrophins was noted. The estrone/estradiol ratios after 3 and 12 months of treatment were 5.3 and 4.7, respectively. A decrease in the serum concentration of testosterone and androstenedione was recorded during treatment. The reduction of gonadotrophins, especially LH, might have been responsible for the reduction in circulating androgens. The reduction of serum levels of androgens during the present long-term replacement therapy could be of metabolic importance.
Adult↗
Ethinylestradiol administered by oral and sublingual routes: a comparative study in ovariectomized women.
Eight ovariectomized women with an intact uterus received 12.5 micrograms ethinylestradiol for 14 days, in a cross over fashion. Ethinylestradiol was administered as a paper disc for sublingual application or as a tablet for oral administration. The parameters studied were FSH secretion, plasma protein synthesis, endometrial morphology, cervical mucus properties and the karyopyknotic index. Both types of treatment resulted in estrogenic effects with a more pronounced effect on sperm penetration and the Spinnbarkeit test after paper disc treatment than after conventional tablet treatment. The post-treatment FSH concentration 20 h after ethinylestradiol administration was significantly lower than the pretreatment value only in the case of the paper disc treatment. There was no evidence of any difference in effects on protein synthesis. The results indicate that the availability of ethinylestradiol for peripheral tissues may be increased by sublingual administration compared to oral tablet administration, whereas the effects on liver protein synthesis may remain unchanged.
Administration, Oral↗
Vaginal absorption of two estriol preparations. A comparative study in postmenopausal women.
In a comparative randomized cross-over study the absorption of a single dose of 0.5 mg estriol from a vaginal cream or a vaginal suppository (OvestinR, Organon, The Netherlands) was studied. Eight healthy postmenopausal women participated and the preparations were given with an interval of 14 days. Blood sampling was performed twice before application and then after 1/4, 1/2, 1, 2, 4, 6, 8, 24 and 48 hours. Serum was analysed for unconjugated and conjugated estriol (E3), FSH and LH by radio-immunoassay. Considerable interindividual variations in serum levels of unconjugated E3 were found but mean values were about equal throughout the study for the two preparations. Peak levels of 0.5-0.6 nmol/l were achieved 1-2 hours after application of the preparations and after 24 hours no unconjugated E3 was measurable. Conjugated E3 rose rapidly but within 48 hours serum concentrations reached baseline levels. A maximum decrease in serum LH levels of about 40% was obtained with both preparations after 6 hours and the return to baseline within 24 hours indicates a relationship to unconjugated E3. FSH in serum was maximally suppressed 6-12%. Estriol is thus readily absorbed by the vaginal route and peak levels of unconjugated E3 after insertion of 0.5 mg estriol seem to be comparable to those obtained after 8-12 mg estriol given orally.
Absorption↗
A clinical evaluation of treatment with estriol vaginal cream versus suppository in postmenopausal women.
Thirty postmenopausal women with vaginal atrophy were treated with a vaginal cream or vaginal suppositories containing 0.5 mg estriol (OvestinR, Organon, The Netherlands). The preparations were given daily for 14 days and then during the next 6 weeks a maintenance dose was applied twice a week. Cervical mucus, vaginal cytology and the endometrium were studied. Blood samples were analysed for unconjugated and conjugated estriol, FSH, LH, prolactin and sex hormone binding globulin capacity, before and after 2 weeks of treatment. Subjective relief of vaginal symptoms was reported by all patients. Restoration of vaginal mucosa was confirmed by colposcopy. Some women noted a feeling of transient "vaginal heat" during the first days of treatment; otherwise no side effects were reported. Higher values for Spinnbarkeit, ferning and karyopyknotic index were found for the cream group on day 14. No endometrial stimulation was detected as judged by light microscopy in any of the samples. No significant differences between the preparations were found for any of the hormone variables, or sex hormone binding globulin capacity, except for prolactin levels after 2 weeks of treatment. Possible reasons for the disparity between the two preparations regarding peripheral variables are discussed.
Aged↗
Two oral contraceptives, efficacy, serum proteins, and lipid metabolism. A comparative multicentre study on a triphasic and a fixed dose combination.
A triphasic, combined oral contraceptive containing 30 - 40 - 30 micrograms ethinyloestradiol (EE), and 50 - 75 - 125 micrograms levonorgestrel was compared with a fixed dose combination containing 30 micrograms EE and 150 micrograms desogestrel in a randomized multicentre trial in 193/199 women and 1 063/1 073 cycles, respectively. The duration of the trial was six months. Eleven centres in Denmark, Sweden, and Norway participated. Contraceptive reliability, bleeding control and side effects were evaluated. Influence on serum sex hormone binding globulin (SHBG) and transcortin was assayed as well as lipid metabolism. Three pregnancies occurred in the group using the triphasic regimen but none in the fixed dose regimen. Two of the three pregnancies were considered drug failures and the third a possible interaction. Possible reasons for the triphasic contraceptive failure are discussed with special reference to a British report on eight pregnancies. Bleeding control appeared to be equally good for the two preparations. However, the number of cycles with spotting, breakthrough bleeding and missed withdrawal bleeding were above the levels reported earlier on the triphasic regimen. About 80 per cent of the women completed the planned six months on either combination. Side effects were generally mild and in accordance with earlier reports on low dose oral contraceptives. Metabolically the triphasic levonorgestrel combination increased SHBG 100 per cent versus 200 per cent for the fixed desogestrel combination. Transcortin rose about 98 and 110 per cent, respectively. Both preparations induced similar changes in the levels of lipids and lipoproteins with the exception of a significant increase in the arachidonic content of cholesterol during treatment with the desogestrel-containing preparation.
Adolescent↗
Evaluation of a continuous oestrogen-progestogen regimen for climacteric complaints.
Subjective complaints, endometrial histopathology, vaginal cytology and bleeding patterns were recorded in 26 patients treated with a continuous oestrogen-progestogen regimen for 12 mth. A marked reduction of hot flushes and sweats were noted and the evaluation of endometrial specimens revealed that the mucosae were mostly inactive-atrophic. The karyopyknotic index proved to be a poor indicator of oestrogenic activity. The number of recorded bleedings in the peri-menopausal women differed markedly from the post-menopausal women during treatment; they were very slight in the latter group. Even in those cases where bleeding occurred, the endometrial samples were found to be atrophic. Vaginal bleeding seemed to be an unreliable indicator of endometrial histopathology. The present combination of hormones used in a continuous regimen is a good alternative for post-menopausal women in need of hormonal therapy.
Climacteric↗
Influence of esterified estrogens and medroxyprogesterone on lipid metabolism and sex steroids. A study in oophorectomized women.
Eight oophorectomized women were given 1.25 mg esterified estrogens (EE) daily for 21 days and 5 mg medroxyprogesteroneacetate (MPA) daily for 5 days in a sequence combination. The effects on sex steroids, gonadotrophins, lipids and lipoproteins as well as the relative fatty acid composition of lecithin and cholesterol ester induced by treatment were studied. Esterified estrogens were readily absorbed with estrogen levels corresponding to those of a normal luteal phase. A favourable estrone/estradiol ratio was found during treatment. After two days without EE no estrogens could be detected. Androstenedione was significantly depressed after the MPA period, otherwise it remained unchanged. Minor changes were induced in serum lipids and lipoproteins. A decrease in cholesterol ester of 12 and 23 per cent was found for palmitic and stearic acid concomitant with an increase of arachidonic acid of about 20 per cent after three weeks of estrogen treatment. After the MPA period increases in free cholesterol, total cholesterol and phospholipids in HDL were assessed. It was concluded that MPA in this experiment from a lipid metabolic point of view seemed to be a favourable progestogen complement.
Adult↗
Administration of dehydroepiandrosterone enanthate to oophorectomized women--effects on sex hormones and lipid metabolism.
Eight bilaterally oophorectomized women were given a depot injection of 200 mg DHEA-enanthate to study the effect on endocrine and lipid metabolism. A decrease in sex-hormone binding globulin (SHBG) and an increase in androstenedione was found 14 and 30 days after the injection. No changes could be detected in LH, FSH, oestrone, oestradiol or oestriol. Testosterone showed a tendency towards an increase. As compared to pre-treatment values, plasma lipids were unaltered after 30 days. A decrease in high density lipoproteins (HDL), cholesterol and in very low density lipoproteins (VLDL), free cholesterol, total cholesterol and phospholipids were seen in the lipid composition of the lipoproteins on day 30. These findings are in agreement with previous data reported after the administration of drugs with androgen-like effects. The relative fatty acid composition of plasma lecithin revealed only minor changes while the fatty acid composition of cholesterol esters indicated a decreased portion of essential fatty acids. These results suggest, in agreement with previous studies, an impaired endogenous cholesterol formation in the liver. The results from the analysis of the fatty acid composition of lecithin and cholesterol esters might indicate a decreased percentage of exogenous (dietary) cholesterol ester in plasma.
Adult↗
Some adverse effects of copper-IUD.
Perforations and extraction problems in some 30 700 women wearing a copper intrauterine device (Cu-IUD), either a Cu-7 or Cu-T have been studied. Perforations were very rare. Judging from the literature and the present investigation, in cases of perforation the Cu-7-IUD has a tendency to penetrate the uterine wall and the Cu-T-IUD the cervical wall. Retracted and detached strings were observed somewhat more often in women wearing Cu-7-IUD's. The number of such cases was, however, not large enough to warrant a statistical comparison. The cause of retention, investigative procedures and recommendations in the removal of lodged Cu-IUD's are discussed.
Cervix Uteri↗
Intraabdominal pneumococcal abscess.
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Abdomen↗
What is "normal" prolactin concentration in amenorrhoea.
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Adult↗
[Delivery at a general hospital: 2 rare complications].
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Adult↗
Flavonoids in grapefruit juice inhibit the in vitro hepatic metabolism of 17 beta-estradiol.
Naringenin, quercetin and kaempferol, which may be found in glycoside form in natural compounds such as grapefruit, are potent inhibitors of cytochrome P-450 metabolism. The influence of these flavonoids on the metabolism of 17 beta-estradiol was investigated in a microsome preparation from human liver. The flavonoids were added in concentrations of 10, 50, 100, 250 and 500 mumol/l to the microsome preparation. The metabolism of 17 beta-estradiol was concentration dependently inhibited by all the flavonoids tested. Addition of the flavonoids to the microsome preparation did not influence estrone formation, while a potent inhibition of estriol formation was observed. At the highest concentrations tested of the respective flavonoid, there was approximately 75-85% inhibition of estriol formation. However, naringenin was a less potent inhibitor of 17 beta-estradiol metabolism as compared to quercetin and kaempferol. The most likely mechanism of action of the flavonoids on 17 beta-estradiol metabolism is inhibition of the cytochrome P-450 IIIA4 enzyme, which catalyzes the reversible hydroxylation of 17 beta-estradiol into estrone and further into estriol. These hydroxylation processes represent the predominant steps of the hepatic metabolic conversion of endogenous as well as exogenous 17 beta-estradiol. This interaction would be expected to inhibit the first-pass metabolism of 17 beta-estradiol, and this has recently been demonstrated after oral administration of 17 beta-estradiol to women.
Adult↗