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At least 127 records · Page 7Linked to original sources
PubMed1997

Comparative serum estradiol profiles from a new once-a-week transdermal estradiol patch and a twice-a-week transdermal estradiol patch.

Two identical open-label, randomized crossover studies were conducted to compare serum estradiol profiles from the new 12.5- and 25-cm2 once-a-week adhesive patches with those from the 10- and 20-cm2 commercially available twice-a-week Estraderm patches when applied as directed during a 1-week patch-wear period. Both studies were conducted in healthy postmenopausal women; serum estradiol levels were determined by gas chromatography/mass spectroscopy (GC/MS). Although both sizes of both patch treatments produced mean serum estradiol levels in the therapeutic range, the once-a-week patch provided more constant mean levels, avoiding large peak-to-trough fluctuations. As expected, the differences in mean serum estradiol concentrations between the two patch treatments occurred during the second application of the twice-a-week patch. Based on these results, the once-a-week drug in adhesive patch appears to be an acceptable means of hormone replacement therapy.

Administration, Cutaneous↗
PubMed2003

The isolated normothermic hemoperfused porcine forelimb as a test system for transdermal absorption studies.

For transdermal absorption studies, a porcine skin model that maintains the characteristics of the skin as close to physiological conditions as possible should be established because of the close similarity of porcine and human skin. Perfusion flow, glucose concentration, and oxygen supply were varied and organ resistance and lactate concentration were measured as parameters for organ performance. Transdermal absorption studies were performed using nitroglycerin or estradiol as test solutes. By the use of a standardized perfusion apparatus, limbs were perfused with a normothermic blood/electrolyte mix over a 6-h period. Organ resistance and lactate concentration were lower in limbs perfused with high flow as compared to perfusion with low flow. However, high perfusion flow caused an initial increase of hemolysis in the venous perfusate resulting in a higher concentration of free hemoglobin compared to low perfusion flow conditions. Glucose level in the perfusate was maintained within the porcine physiological range. By applying optimized conditions, the transdermal absorption of nitroglycerin or estradiol released from transdermal therapeutic systems was investigated. A time-dependent accumulation of the substances in the perfusion medium was observed, indicating the continuous uptake via the skin. After 6 h (nitroglycerin) or 5 h (estradiol) of perfusion, test substances accumulated to concentrations comparable to those described in humans. In conclusion the perfused porcine limb may serve as a reliable test system for transdermal absorption studies. The model is suited to the replacement of animal testing and has a higher predictive potential because of the similarities of porcine and human skin.

Animals↗
PubMedDate not supplied

Ethinyl estradiol and medroxyprogesterone treatment in advanced breast cancer: a pilot study.

Twenty patients with disseminated breast cancer unresponsive to conventional chemotherapy and chemohormonotherapy were treated with an alternating sequential schedule of ethinyl estradiol and medroxyprogesterone on the basis of correlations between hormones and estrogen and progestin receptors. Of 19 evaluable patients, six underwent partial or complete remission, while five others showed minor responses.

Breast Neoplasms↗
PubMed2006

Comparison of reproductive effects of levetiracetam and valproate studied in prepubertal porcine ovarian follicular cells.

PURPOSE: Long-term valproate (VPA) treatment has been associated with reproductive endocrine disorders characterized by hyperandrogenism and polycystic changes in the ovaries in women with epilepsy. Levetiracetam (LEV) is a promising, new antiepileptic drug that may represent an alternative to VPA for many patients. Here the effect of LEV and VPA on basal and gonadotropin-stimulated steroid secretion from prepubertal porcine ovarian follicular cells was compared and the conversion of testosterone to estradiol is measured. METHODS: Ovarian follicles were obtained from prepubertal pigs. Follicular theca and granulosa cells were cocultured and different concentrations of LEV or VPA added to the control or gonadotropin-stimulated cultures. RESULTS: VPA, but not LEV, caused a significant increase of LH-stimulated testosterone secretion and decreased FSH-stimulated estradiol secretion. VPA decreased conversion of testosterone to estradiol in both basal and FSH-stimulated cultures, while LEV only decreased testosterone to estradiol conversion after FSH stimulation and only at the highest, nontherapeutic drug concentration. Both drugs increased basal testosterone secretion at therapeutic drug levels. VPA also reduced basal estradiol secretion, while LEV decreased basal estradiol secretion only at nontherapeutic drug levels. CONCLUSION: Both LEV and VPA affect endocrine function in the prepubertal ovary. But while VPA alters both basal and gonadotropin-stimulated testosterone and estradiol secretion at therapeutic drug concentrations, LEV only affects basal hormone secretion at this concentration level. The possibility that LEV could be an alternative treatment to VPA if reproductive endocrine problems emerge in adult women, is discussed. However, extrapolation to the clinical situation is problematic and particular emphasis is placed on the need for further studies.

Animals↗
PubMed1991

Analytic variability and clinical significance of different assays for serum estradiol.

Recent reports in the clinical laboratory literature have raised questions about the accuracy of different methods of measuring serum estradiol. To determine whether between-method variability was clinically significant, we used five different commercial radioimmunoassay methods to measure the concentration of estradiol in sera from nine patients undergoing induction of ovulation for gamete intrafallopian transfer. There were large differences between the estradiol concentrations measured in the same samples by the different methods. Furthermore, apparent changes in concentration that would be regarded as clinically significant may reflect nothing more than the imprecision of the assay. Physicians using serum estradiol measurements to support therapeutic decisions should be aware that an excessive reliance on those measurements may be misleading.

Adult↗
PubMed1988

Sex hormones modulate the response of pulmonary perivascular inflammation to cyclophosphamide therapy in MRL/MpJ-lpr/lpr mice.

Responses of pulmonary perivascular infiltrates to immunosuppressive therapy with cyclophosphamide (CY) were evaluated in the MRL/MpJ-lpr/lpr (MRL/1) mouse, a model for the study of systemic lupus erythematosus. Male and female mice were divided into the following groups: controls injected with saline; intact mice receiving CY; castrated CY-treated mice; castrated, hormone implanted, CY-treated mice. CY treatment began at 30 days of age and animals were killed at 60 days of age. Lungs were fixed-inflated to 26 cm H2O pressure with glutaraldehyde-formaldehyde fixative. The pulmonary perivascular response to immunosuppressive therapy was graded depending on the extent of infiltrates surrounding 15 pulmonary vessels per animal. Intact males treated with CY alone had almost complete clearing of perivascular infiltrates, whereas intact females did not respond to therapy. Castrated CY-treated males showed a decreased response to CY compared to intact CY-treated males. Castrated, estradiol-implanted males had no response to CY therapy. Estradiol interfered with the therapeutic response to CY in male MRL/1 mice.

Animals↗
PubMed2003

Clinical evidence of the endocrinological influence of a triphasic oral contraceptive containing norgestimate and ethinyl estradiol in treating women with acne vulgaris. A pilot study.

BACKGROUND AND OBJECTIVE: The aim of this study was to evaluate the efficacy of a triphasic combination oral contraceptive (OC) containing norgestimate and ethinyl estradiol in the treatment of women with acne vulgaris. METHODS: 12 female patients were included and 10 completed the trial. Over a period of 6 months, efficacy was assessed by means of facial acne lesion counts, by an investigator's global assessment, by patients' self-assessments and by measuring epidermal moisture and skin surface lipids. In addition, a photo documentation was compiled and hormone levels were measured. RESULTS: After 6 months of therapy, the number of acne counts improved. The success of treatment was rated positively both by the investigator and by all patients but one who did not report any changes. Skin surface lipids were significantly reduced while skin hydration showed no significant change. Testosterone and progesterone decreased, and sex-hormone-binding globulin increased, significantly. CONCLUSION: Our data show that an OC containing norgestimate and ethinyl estradiol is a good therapeutic option for women of fertile age suffering from mild to moderate acne vulgaris.

Acne Vulgaris↗
PubMed1978

[Rebound regression after additional hormonal treatment with ethinyl oestradiol of metastasising carcinoma of the breast in females: frequency and clinical significance (author's transl)].

Rebound regression occurred in 13 of 42 females (30.9% with metastasising carcinoma of the breast in the postmenopausal period in whom additional hormonal treatment with ethinyl oestradiol had brought about a remission. Duration of the rebound response ranged from 3 to 44 months (average 11.2 months; mean 8 months). There was a significantly longer duration of remission (18.7 months compared with 12.0 months; P = 0.01) in patients with than those without a rebound response. There was also a significant correlation between the duration of the preceding remission under additional hormonal treatment and the duration of the subsequent rebound response (P less than 0.01). On the other hand, there was a negative but not significant correlation between the free interval duration which preceded the metastasisation and the duration of the rebound regression.

Breast Neoplasms↗
PubMed1975

Inhibition of cyclic gonadotropin secretion by endogenous human prolactin.

The resumption of cyclic uterine bleeding reportedly accompanies the use of human prolactin (HPRL)-suppressing agents in postpill galactorrhea-amenorrhea. In this laboratory, HPRL suppression with L-dopa was variable and short lived. Basal plasma HPRL levels were elevated before and after as much as five months of therapy. Galactorrhea persisted and mean gonadotropin concentrations were subnormal. An immediate and sustained attenuation of HPRL secretion ( less than 200 per cent) followed the use of 2-Br-alpha-ergocryptine (CB-154). Cyclic gonadotropin secretion resumed and was accompanied by ovulation and, in one instance, pregnancy. The cessation of galactorrhea was positively correlated with the rise in the daily concentration of 17 beta-estradiol. Cyclic postovulatory menstruation continued after the cessation of CB-154 treatment. HPRL levels remained normal. The daily patterns of human follicle-stimulating hormone (HFSH) and human tuteinizing hormone (HLH) secretion created by the suppression of HPRL displayed an inherent rhythmicity identical to that observed at the time of menarche. The inhibitory effects of HPRL appeared directed at cyclic rather than tonic gonadotropin secretion. At the same time, diminished ovarian estrogen production seemed to increase mammary gland sensitivity to HPRL, leading to lactation. One may postulate, therefore, that the ingestion of sex steroids is associated with an over-all suppression of endogenous cyclic and, to a lesser extent, tonic gonadotropin secretion secondary to which ovarian function is attenuated. Without physiologic concentration of circulating estrogen, HPRL induces mammary alveolar function with the production of a milklike secretion.

Amenorrhea↗