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At least 217 records · Page 12Linked to original sources
PubMed1977

Oestrogenic activity of oestradiol-decanoate after oral administration to rodents.

Oestradiol-decanoate, dissolved in arachis oil and orally administered to rodents, produces oestrogenic effects. Compared on a molecular basis the ester has 0.1-1.0 times the activity of ethinyl oestradiol, dependent on the species and the parameter studied. The effects of oestradiol-decanoate are less or absent when the oil is omitted. It is likely that absorption of the steroid ester takes place via the intestinal lymphatics in conjunction with the oil.

Administration, Oral↗
PubMed1979

Plasma medroxyprogesterone acetate levels following intramuscular or oral administration in patients with endometrial adenocarcinoma.

The concentration of medroxyprogesterone acetate (MPA) in plasma samples taken 24 h after intramuscular or oral administration of 100 mg daily doses of the drug to patients with endometrial adenocarcinoma was measured by radioimmunoassay. In general, a plasma level of about 4 ng/ml was found 24 h after the dose, independent of the route of drug administration. However, in three of the patients to whom intramuscular MPA was given, considerably higher values were found. A maximal plasma level was achieved three hours after ingestion of 100 mg MPA. This was followed by a rapid decline to 20-25% of the peak value after about 12 h. A rather small day-to-day intraindividual variation was found in daily blood samples taken just before administration of the next dose. However, considerable differences were found between individuals and it is concluded that this variation in plasma levels may be reflected in the clinical efficacy of the treatment. Thus further studies in which plasma values and clinical effectiveness are correlated seem to be indicated.

Adenocarcinoma↗
PubMed1975

Microbiological hydroxylation of norethisterone.

Hydroxylation of norethisterone by a large number of fungi has been investigated. 1alpha-Hydroxy-, 6beta-hydroxy-, 10beta-hydroxy-, 10beta,11beta-dihydroxy-15alpha-and 15beta-hydroxy-derivatives were formed from norethisterone. The microbiological dehydrogenation of 10beta-hydroxy-norethisterone resulting in 10beta,17beta-dihydroxy-17-ethynyl-1,4-estradien-3-one was also observed. The structure of transformation products was established by chemical and spectroscopical methods.

Chemical Phenomena↗
PubMedDate not supplied

Radioimmunoassay of norethindrone (17 alpha-ethynyl-17 beta-hydroxy-4-estren-3-one) and ethynyl-estradiol (17 alpha-ethynyl-1,3,5, (10)-estratien-3, 17 beta-diol). Application to human plasma determination of norethindrone after oral administration of this steroid.

The experiment conditions for the evaluation of Norethindrone (17 alpha-Ethynyl-17 beta-hydroxy-4-estren-3-one, NET) and Ethynyl-estradiol (17 alpha-ethynyl-1, 3, 5 (10) estratrien-3, 17 beta-diol, EE) by radioimmunoassay are described. A minimal quantity of 25 pg of these two steroids could be evaluated using different reduced metabolites of NET, very little cross reaction is observed with 200 pg of these metabolites. No effect was observed with estradiol for the EE-antiserum. The NET-antiserum was used to evaluate this steroid and ethynodiol diacetate after oral administration to female volunteers. Maximal values in the plasma (2-3% of the administered dose) was found between 1-3 h after administration and at 24 h a concentration of 0.1-0.3% still remained in the plasma.

Administration, Oral↗
PubMed1981

Enzyme immunoassay for specific determination of the synthetic estrogen, ethynyl estradiol, in plasma.

In this enzyme immunoassay for ethynyl estradiol, a conjugate of the 3-(O-carboxymethyl)ether with horseradish peroxidase is used as the label and a conjugate of the 6-(O-carboxymethyl)oxime with bovine serum albumin as the immunogen. A solid-phase antibody procedure is used in separating antibody-bound and free steroid. The lower limit of sensitivity of the assay is 2 pg per assay tube. Interference by synthetic progestagens was minimized by extracting the sample with an anti-estrogen serum before assay. Results obtained with a comparison radioimmunoassay and this procedure agreed well (r greater than 0.98).

Contraceptives, Oral↗
PubMed1982

Sex hormone levels and intestinal absorption of estradiol and D-norgestrel in women following bypass surgery for morbid obesity.

A report of reduced serum levels of progestins, following oral administration after jejunoileal bypass, promoted the present investigation of the absorption of D-norgestrel and estradiol following different types of intestinal bypass surgery for morbid obesity. A group of non-operated obese patients served as control. Apart from significantly higher gonadotrophin levels, which could be attributed to periovulatory sampling in the non-operated group, there was no significant differences in basal levels of estradiol, estrone, conjugated estrone, androstendione, testosterone, and progesterone. The operation did not influence the pattern of the menstrual cycle. Following a single oral dose of 4 mg micronized estradiol and 125 microgram D-norgestrel, serum levels of estradiol and estrone were equal in the three groups. serum D-norgestrel was equal in the two operated groups, but was significantly higher in the bypass group with 1:3 jejunoileal ratio, compared with the non-operated group. Further, a significant negative correlation between peak levels and weight was found. It is suggested that one year following bypass surgery, obesity - but not intestinal bypass - might be associated with reduced serum levels of exogenous sex steroids following oral administration.

Adult↗