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Results for “Norpregnatrienes”

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At least 19 recordsLinked to original sources

GLC determination of 17 alpha-ethynylestriol 3-cyclopentyl ether.

A rapid, sensitive, and accurate GLC method of analysis of a new estrogenic drug, 17 alpha-ethynylestriol 3-cyclopentyl ether, was developed. The drug and the internal standard, tetratriacontane, are dissolved in chloroform, and an aliquot is heated with N-trimethylsilylimidazole at 80 degrees for 30 min. The silylated sample is chromatographed using a column packed with 1% methyl vinyl silicone gum on Gas Chrom Q. Quantitation is achieved by computer calculation of the peak area ratios. The observed peak is the 16alpha,17beta-bistrimethylsilyl derivative of the new drug substance. The GLC method was applied to the quantitative determination of the estrogenic compound in a tablet formulation containing 25 mug/tablet.

Chromatography, Gas↗

High-pressure liquid chromatographic assay of quinestrol tablets.

A specific assay for quinestrol was developed using high-pressure liquid chromatography. The estrogen was separated from tablet excipients on a chemically bonded hydrocarbon column utilizing acetonitrile-water as the mobile phase. Linearity studies were carried out using peak height measurements, and the detector response to the concentration of the steroid was confirmed. This procedure was rapid, accurate precise, and specific for the assay of the synthetic estrogen in the presence of formulation excipients and structurally similar estrogens.

Chromatography, High Pressure Liquid↗

[Changes in carbohydrate tolerance in the puerperium by inhibition of lactation with bromocriptine and quinestrol (author's transl)].

In the present study the influence of bromocriptine on carbohydrate tolerance was examined and its effects compared with those of an estrogenic compound (Quinestrol). Sixteen patients were studied in each group. The controls consisted of 16 women who breastfed their children. No significant difference was found in the oGTT in patients who had Quinestrol compared with the controls. However blood sugar values in women receiving bromocriptine were significantly lowered when compared with values of individuals who had Quinestrol. The reduction of blood sugar values depends on the dosage of bromocriptine. Inhibition of lactation with bromocriptine may lead to false negative results in patients who are at risk to have a prediabetic condition.

Blood Glucose↗

[Treatment of endometriosis].

In a randomized study, the effect of gestrinone (2 x 2.5 mg/week) was compared with the effect of danazol (3 x 200 mg/day) in treating 30 patients with laparoscopically proven endometriotic implants for 6 months. Therapy was effective in 80%-90% of cases and pregnancy rates were similar, but the incidence of side effects was different in the groups. In addition, buserelin (900 micrograms/day intranasally) was investigated in a multinational, multicenter trial in 275 patients. In 80%, GnRH agonist treatment induced the disappearance or reduction of endometriotic implants. The main side effects were due to estrogenic suppression. Presently, various methods of hormonal treatment are under investigation, especially to determine recurrency rates of endometriosis and long-term side effects.

Adult↗

Action of midcycle contraceptive (R 2323) on the human endometrium.

Over 2,148 cycles of midcycle oral administration of R 2323 (50 mg. per day on Days 15,16, and 17), the authors recorded a drug-failure pregnancy rate of 5 per cent and an unusually regular cycle length of 28 +/- 2 days. During this trial, endometrial biopsies obtained in the luteal phase were examined by light and electron microscopy and compared to pretreatment biopsies. Light microscopy indicated a weakly secretory endometrium suggestive of some, albeit low, progesterone impregnation. Ultrastructural examination revealed deleterious changes in the development of the nucleolar channel system and giant mitochondria and a delay in the migration of glycogen granules. This low progesterone impregnation could be explained either by a direct effect of R 2323 on cell ultrastructure or by interference with progesterone availability. It would appear that R 2323 acts as a temporary substitute for progesterone at the receptor level but that it does not induce all the biological manifestations of this hormone, in particular, the endometrial changes required for implantation.

Biopsy↗

Treatment of endometriosis with gestrinone (R-2323), a synthetic antiestrogen, antiprogesterone.

Twenty patients with endometriosis diagnosed by laparoscopy were treated with the antiestrogen, antiprogesterone gestrinone (R-2323) for 6 to 8 months. The drug was administered in a dose of 5 mg twice weekly. According to the American Fertility Society's classification of endometriosis, five patients were classified as having mild (Stage I), eight as having moderate (Stage II), and seven as having severe endometriosis (Stage III). All patients became amenorrheic at the end of the second month of treatment, and symptomless at the end of the third month. Of nine women who had the potential and the desire to conceive, three conceived within 3 months after termination of treatment. Two more became pregnant within 1 year, and another, 14 months after termination of treatment. Five pregnancies progressed to term. One patient aborted. Two of the three women who did not conceive had subfertile husbands. Major side effects recorded were seborrhea and acne, which subsided after discontinuation of therapy. Treatment of endometriosis with gestrinone offers the advantage of effective clearing of lesions with relatively low dosage and frees the patient from the daily administration of drugs required by similar conservative hormonal therapies.

Acne Vulgaris↗

Long acting contraceptive implants. An analysis of menstrual bleeding patterns.

The menstrual patterns of women using subdermal implants of levonorgestrel and norgestrienone included in a double-blind clinical trial was evaluated by the method developed by the International Committee on Contraception Research. Women using Copper T200 randomly selected in the same clinics were used as controls. Both implant regimens were associated with a high frequency of reduced bleeding and norgestrel patients had also a high proportion of increased and irregular bleeding. Termination of use was associated to increased bleeding but not so much to reduced bleeding.

Adolescent↗

Release of contraceptive steroids from sustained release dosage forms and resulting plasma levels.

The correlations of plasma levels of levonorgestrel, megestrol acetate and norgestrienone with the doses delivered from subdermal implants and contraceptive rings have been examined. Differences in plasma levels as large as three-fold between different subjects receiving nearly identical doses were observed with all three steroids. The relative plasma levels seen from one subject to another showed high consistency over time. Part of the explanation may lie in differing levels of sex hormone binding globulin, but additional factors must be operative since megestrol acetate binds only weakly with this carrier.

Contraceptive Devices, Female↗