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At least 271 records · Page 15Linked to original sources
PubMed1983

Long-acting contraceptive agents: structure activity relationships in a series of norethisterone and levonorgestrel esters.

A large number of esters of norethisterone (17 alpha-ethynyl-17 beta-hydroxyestr-4-en-3-one) and levonorgestrel (D-(-)-13 beta-ethyl-17 alpha-ethynyl-17 beta-hydroxygon-4-en-3-one) were synthesized and tested for biological activity. The test employed in these studies was the duration of estrus suppression in cycling mature rats. In the norethisterone series several esters exhibited duration of activity comparable to that of norethisterone enanthate. In the levonorgestrel series the butanoic, cyclobutylcarboxylic and cyclopropylcarboxylic esters were longer acting than medroxyprogesterone acetate (17 alpha-acetoxy-6 alpha-methylpregn-4-ene-3,20-dione) when prepared as aqueous microcrystalline suspensions.

Animals↗
PubMed1990

High progesterone receptor concentration in a variant of the ZR-75-1 human breast cancer cell line adapted to growth in oestrogen free conditions.

Culture of ZR-75-1 human breast cancer cells for 5 days in the absence of oestrogens (phenol red-free medium supplemented with dextran coated charcoal stripped 5% fetal calf serum) resulted in a slowing of growth rate and loss of progesterone receptors. Oestradiol at 10(-9) M markedly stimulated growth and progesterone receptor synthesis over a 5-day period. While medroxyprogesterone acetate (10(-10) to 10(-6) M) inhibited growth of ZR-75-1 cells growing in complete medium, in the short-term absence of oestrogens low concentrations were growth stimulatory. Cells deprived of oestrogens for 5 days retained sensitivity to growth inhibition by 4-hydroxy tamoxifen. ZR-75-1 cells were also adapted to growth in the absence of oestrogens over a 5-month period. These cells (ZR-PR-LT) failed to express binding sites characteristic of the type 1 oestrogen receptor but progesterone receptor expression was at a level normally associated with oestrogen induction. Adapted cells were growth inhibited by oestradiol, 4-hydroxy tamoxifen and medroxyprogesterone acetate, but despite elevated progesterone receptor expression the progestin was only marginally more inhibitory than in the parent line. Our data indicate a poor quantitative relationship between response to progestins in vitro and progesterone receptor concentration and support previous findings that acquisition of an oestrogen independent phenotype does not necessarily result in resistance to anti-oestrogens.

Antineoplastic Agents↗
PubMed1988

Pharmacokinetics of single and multiple doses of ethinyl estradiol and levonorgestrel in relation to smoking.

The effects of tobacco and oral contraceptive (OC) use (Ovral) on the pharmacokinetics of levonorgestrel (0.25 mg) and ethinyl estradiol (50 micrograms) were examined. Young women (n = 27) were grouped as follows: I: non-OC users/nonsmokers; II: OC users/nonsmokers; III: non-OC users/smokers; and IV: OC users/smokers. The apparent clearance of levonorgestrel in group I was 80.9 +/- 15.6 ml/hr/kg and the half-life was 19.3 hours. A significant decrease in levonorgestrel clearance was seen in the chronic OC users (groups II and IV). The apparent oral clearance of ethinyl estradiol was 1002 +/- 398 ml/hr/kg in group I and the half-life averaged 7.7 hours. Groups II and III showed decreased (not significant) clearance of ethinyl estradiol. Tobacco use had no effect on steroid pharmacokinetics in the non-OC users. Although chronic OC use did not affect ethinyl estradiol clearance, a joint effect of tobacco/OC use on enhancing clearance of ethinyl estradiol appeared to occur. A linear relationship was found between 24-hour trough serum concentrations and AUC values of both steroids that may facilitate population monitoring studies of OC exposure.

Adult↗
PubMed1989

Levels of the antiprogestin RU 486 and its metabolites in human blood and follicular fluid following oral administration of a single dose.

Using high-pressure liquid chromatography (HPLC) the antiprogestin RU 486 and two of its metabolites (N-monodemethyl RU 486 and propargyl RU 486) were measured in plasma and follicular fluid of 21 women requesting laparoscopic sterilization. Pretreatment of the women involved ovulation induction with clomiphene and HCG. RU 486 (100 mg) was administered orally and 1 h later blood samples were withdrawn. Thirty-four hours later, at laparoscopy, samples of both blood and follicular fluid were collected. During the 34-h period the average plasma level of RU 486 decreased from 1.93 mumol/l to 0.91 mumol/l, i.e. by -50%. The latter concentration of RU 486 was not significantly different from that found in follicular fluid (0.79 mumol/l). The monodemethyl metabolite exhibited significantly higher plasma levels (3.09 mumol/l) than RU 486 1 h after administration. Thirty-four hours later these levels had decreased to 0.92 mumol/l, i.e. by 70%. In follicular fluid, the levels of the monodemethyl metabolite (1.76 mumol/l) were significantly higher than those of RU 486 (0.79 mumol/l). Because of background noise, only approximate values were established for the propargyl metabolite. These were 0.67 and 0.40 mumol/l, respectively, in plasma and 0.42 mumol/l in follicular fluid. The results indicate that RU 486 and two of its major metabolites can readily cross the blood-follicle barrier of human pre-ovulatory follicles.

Abortifacient Agents↗
PubMed1983

Ethynyl estradiol content of cervical mucus after administration of oral contraceptive.

It was found by radioimmunoassay that the ethynyl estradiol concentration of the cervical mucus was 8.8 times higher than that of the serum in the first third of the cycle, 14 times higher in the second and 7.3 times higher in the third. The ethynyl estradiol content of the cervical mucus in the middle of the cycle showed a marked increase even when expressed as protein ratio. The accumulation of ethynyl estradiol in the cervical mucus is best demonstrated by the cervical mucus/serum ethynyl estradiol quotient of 9.7 found 12 h after oral administration of the contraceptive Bisecurin.

Adult↗
PubMed1983

Serum ferritin levels in pill and IUD users.

12 women using a low-dose combination oral contraceptive (OC) and 17 wearing a copper IUD were studied. Serum ferritin concentrations were measured before and 1, 3, and 6 months after commencing contraception. Ferritin levels in the iron-deficient range (below 50 mcg/l) were present in 5 (42%) and in 8 (47%) subjects, respectively, prior to the start of OCs or IUD insertion. The OC use induced only a temporary decrease in serum ferritin levels at the start of treatment, whereas 12 of 17 (71%) IUD users had reached iron-deficient levels by the end of the follow-up period. Thus, the use of OCs had no adverse effect on iron balance, but the monitoring of iron status and the administration of iron-replacement therapy seem to be indicated in the majority of women fitted with an IUD.

Biology↗
PubMed1977

Etiology, clinical features and prognosis in secondary amenorrhea.

A clinical investigation of 356 patients with secondary amenorrhea revealed that 95% of patients with postpill amenorrhea and 56% of patients with anorexia nervosa recovered in 6 years. The corresponding recovery rates for patients with psychogenic amenorrhea and amenorrhea following self-induced weight loss were 72% for both groups, and in patients with the amenorrhea-galactorrhea syndrome and idiophatic functional amenorrhea the recovery rates at 6 years were 64 and 61% respectively. Unlike the other groups with functional amenorrhea, patients with the amenorrhea-galactorrhea syndrome had impaired ovarian responsiveness to exogenous gonadotropins. Bromocriptine treatment resulted in disappearance of the galactorrhea and restoration of the menses and/or ovulation in nine of 18 patients; of these three became pregnant. The effect of bromocriptine did not persist for long after treatment ceased, and permanent recovery was recorded only in four patients. The group with functional amenorrhea included 34 patients who wished to become pregnant. Gonadotropin treatment was successful in 20 patients, clomiphene-hCG in two, tamoxifen in two, bromocriptine in two, and combined bromocriptine and clomiphene in one. Thus, the overall pregnancy rate in patients with functional amenorrhea was 79%. The groups with ovarian amenorrhea inclutients with assumed ovarian failure responded to large doses of exogenous gonadotropins by ovulation and three became pregnant. Ovarian wedge resection was ineffective in all five cases with polycystic ovaries, but two patients became pregnant after treatment with clomiphene and chorionic gonadotropin, and one with exogenous gonadotropins.

Amenorrhea↗
PubMed1982

[Cholestatic jaundice induced by D-penicillamine and oral steroid contraceptive in progressive systemic sclerosis (author's transl)].

A 25-year-old woman with progressive systemic sclerosis was treated with D-penicillamine. (DPA) 30 days after starting therapy cholestatic jaundice was observed. Moreover, for two years she has taken the pill. Both drugs were discontinued, the jaundice disappeared and the laboratory findings of liver became normal. A rechallenge of D-penicillamine after 9 months induced no reaction. An underlying chronic liver disease before cholestasis could be excluded by liver biopsy. Allergic cutantests and lymphocyte transformation test with D-penicillamine and penicillin gave normal results. The frequency of cholestatic jaundice caused by DPA-therapy is discussed and the possible pathomechanism analyzed.

Adult↗
PubMed1983

Desogestrel, a new progestational compound, and the liver.

The short- and long-term effects on the liver of oral contraceptive preparations containing the new progestational compound 13-ethyl-11-methylene-18,19-dinor-17 alpha-pregn-4-en-20-yn-17-ol (desogestrel) and ethinylestradiol (EE) were studied in multicentre efficacy trials. The following combinations (desogestrel/EE content per daily tablet in micrograms) were investigated: 150/30, 125/50, 100/50 and 75/50, to be taken once daily for 21 days, and a normophasic preparation containing 7 tablets with 50 micrograms EE and 15 tablets containing 125 micrograms desogestrel and 50 micrograms EE. Liver function parameters (SGOT, SGPT, alkaline phosphatase and total bilirubin) were monitored in the serum of 1856 women for periods of up to 36 treatment cycles. The incidence of values (single and combined) above the upper normal limits before treatment was 3.3%. A combination of values above upper normal limits before treatment was observed in 31 women (1.6%). In practically all cases values normalized during treatment; no deterioration was observed. During treatment a combination of values above the upper normal limits was observed in 30 women (having normal pretreatment values); they were distributed over the various preparations and unrelated to the period of contraceptive treatment. The values normalized in the majority of women during the course of treatment. This study shows that with oral contraceptive combinations containing desogestrel and EE (30 or 50 micrograms) liver function is not affected.

Contraceptives, Oral, Combined↗