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Bioavailability of oral micronized progesterone.

Progesterone (P) has not been administered orally because of reportedly poor bioavailability and a rapid clearance rate. Unfortunately, the synthetic derivatives, although orally active, have a number of disadvantages and fail to mimic natural P completely. To investigate the bioavailability and short-term toxicity of oral micronized P, a standardized dose of 200 mg of micronized P was administered to nine healthy postmenopausal women and one male subject. Serial determinations of serum P concentrations demonstrated rapid absorption of P. Peak concentrations of P rose from a negligible baseline level to 17.0 +/- 4.9 ng/ml at an average of 2.8 +/- 0.35 hours after administration. The peak concentrations of P were equivalent to those observed in the midluteal phase in normal control cycles (14.1 +/- 2.7 ng/ml). All subjects exhibited significant elevation of P over baseline levels that persisted for at least 6 hours after the single oral dose and returned to initial levels by 24 hours. There was no significant change in estradiol, follicle-stimulating hormone, luteinizing hormone, cortisol, aldosterone, lipids, or hepatic enzymes during the 24-hour study interval.

Administration, Oral↗

[Estrogen dependance of the progesterone "receptor" in human tissues (author's transl)].

The concentration of specific progesterone receptor (RP) has been measured in the endometrium of 31 normal menstruating women during the two phases of their menstrual cycle, and compared with the plasma oestradiol-17 beta (E2) concentrations. There was no relationship between RP and plasma E2 when the two phases of the cycle were considered, however a correlation was observed when the follicular phase was only considered. The relationship between oestrogen and RP was then more directly studied in a breast cancer cell line in tissue culture (MCF-7). RP induction by E2 as well as oestriol was demonstrated, but oestrone was ineffective.

Endometrium↗

[Sex hormone regulation of progesterone and estradiol receptors in the cytosol of human endometrium in normal and pathologic pregnancy].

Hormonal control of progesterone and estradiol receptors was studied in the cytozol of short-lived culture of human endometrium in normal and undeveloping pregnancy. Endometrium was cultivated in the presence of estradiol or progesterone for 16 hours. In cultivation of normal endometrium with estradiol the content of estradiol receptors increased 4-fold in comparison with unstimulated tissue, and of progesteron receptors--3-fold. In cultivation of normal endometrium with progesterone the content of estradiol receptors rose 4--5-fold, and of progesterone receptors--3-fold. In cultivation of pathological endometrium with estradiol or progesterone the number of estradiol receptors was only doubled, and of progesterone receptors--increased only 1 1/2 times, this pointing to a diminished sensitivity of pathological endometrium to the regulating action of sex hormones.

Cells, Cultured↗

[Changes in serum beta-thromboglobulin levels during oral contraception, cardiac valve disease and pulmonary embolism (author's transl)].

beta-thromboglobulin (beta TG), a platelet-specific protein, was measured in the plasma of 53 healthy subjects (20 men and 33 women), 53 women using estrogen-progestogen contraceptives, 31 patients with cardiac valve disease (including 19 with prosthesis) and 71 patients about to undergo scintigraphy for suspected pulmonary embolism. Compared with levels in healthy subjects, beta TG levels were significantly increased in oral contraceptive users and in cardiac patients with or without prosthesis. High beta TG levels were also found in 20 out of 28 patients with pulmonary embolism confirmed by scintigraphy, but also in some of the .9 lung patients with chronic bronchopulmonary disease. Cardiac patients treated with heparin had higher beta TG levels than non heparin-treated patients, which raises queries about a possible influence of heparin on this particular blood protein.

Adult↗

Long-term intranasal luteinizing hormone-releasing hormone agonist treatment for contraception in women.

Fifty-one female volunteers used a superactive stimulatory luteinizing hormone-releasing hormone (LH-RH) analog for suppression of ovulation for 3 to 12 months. The potent LH-RH agonist D-Ser(TBU)6-EA10-LH-RH was administered intranasally once daily in a dose of 400 or 600 micrograms. No pregnancies occurred during the 283 treatment months. Severe bleeding disturbances were not observed during the long-term treatment. No signs of hyperplastic changes were found in endometrial biopsies. There were no serious side effects. Ovulation promptly returned after cessation of treatment even in women with amenorrhea during treatment periods of 1 year or more. Thus, long-term LH-RH agonist treatment proved to be a safe, effective, and rapidly reversible new method for peptide contraception.

Administration, Intranasal↗

Single midluteal progesterone assay in the management of ovulatory infertility.

A midluteal (five to ten days before the onset of the next period) single serum progesterone measurement, used routinely to assess luteal function, revealed, in 48 infertile women, values lower than 10 to 15 ng/ml. Clomid alone or with human chorionic gonadotropin (HGC) was used in their treatment. Twenty-six (58%) women successfully conceived on Clomid or Clomid and HCG. Progesterone measurements before and during treatment showed that values of midluteal progesterone increased from a pretreatment mean of +/- SD of 9.0 +/- 5.9 to 27.3 +/- 10.3 ng/ml during conception cycles. The single progesterone measurement at midluteal phase is a useful guide in the management of ovulatory infertility.

Body Temperature↗