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PubMed1975

Metabolites of lynestrenol acetate in the bile of rats after intravenous administration; a comparison with lynestrenol.

Some aspects of the metabolism of lynestrenol acetate, an orally active contraceptive compound, were studied in female rats. Lynestrenol acetate is stable in gastric and intestinal juice in vitro. After intravenous administration of lynestrenol acetate and lynestrenol with a -14C label in the nucleus approximately 40% of the administered radioactivity was excreted in the bile within 90 min. After administration of lynestrenol acetate labelled in the ester group, 6% of the radioactivity was found in the bile. This means that the greater part of the lynestrenol acetate had lost its acetate group during the process of metabolism. There was an important difference between the autoradiograms of the thin layer patterns of post-hydrolysis extracts after administration of [4-14C]lynestrenol acetate and those after administration of [1'-14C]lynestrenol acetate and [4-14C]lynestrenol: the major metabolite of [4-14C]lynestrenol acetate did not appear on the autoradiograms of [1'--14C]lynestrenol acetate and [4-14C]lynestrenol. This indicates that lynestrenol acetate was altered in the nucleus in the presence of the acetate group. The acetate group itself was removed, either when the alterations took place, or after it had been completed. The results of IR, NMR and mass spectrometry analysis indicate the introduction of a 15alpha hydroxyl group. Results of gas-liquid chromatography and thin layer chromatography indicate that a second important metabolic is 19-nor-17alpha-pregn-20-yne-3alpha, 17beta-diol. The main conclusions are: 1. A part of the lynestrenol acetate is metabolized and excreted in the bile, the acetate group still being present. 2. Lynestrenol acetate is to some extent metabolized via another pathway than lynestrenol. This indicates that esterification of a steroid can lead to deviation from the metabolic pathway of the free original steroid.

Acetates↗

PubMed1980

Effects of low-dose gestagen (lynestrenol 0.5 mg) and combination-type oral contraception (lynestrenol 1 mg and ethinyloestradiol 0.05 mg) on blood glucose and serum insulin levels after a glucose load.

Forty 3-h oral glucose tolerance tests (OGTTs) were performed in 10 apparently healthy female volunteers aged 21--34 years, each serving four times as her own control. Each subject was taking either a low-dose gestagen contraceptive (lynestrenol 0.5 mg) or a combination-type pill (lynestrenol 1 mg + ethinyloestradiol 0.05 mg) alternatingly in four consecutive treatment cycles. Blood glucose and serum insulin did not differ significantly with either contraceptive (paired t-test).

Adult↗

PubMed1981

[Pharmacokinetics of norethindrone and lynestrenol studied by HPLC (author's transl)].

The concentration of norethindrone in plasma samples from subjects receiving norethindrone (norethisterone) and lynestrenol orally was measured by high pressure liquid chromatography (HPLC). Norethindrone is a synthetic gestagen widely used in contraceptive formulations, and lynestrenol is also a synthetic gestagen which is metabolized to norethindrone in humans. But the evaluation of plasma norethindrone levels in subjects receiving lynestrenol has not yet been reported. After the administration of norethindrone, the peak level of norethindrone in the plasma was obtained within 2h, and the peak concentration in the plasma was about 3.5 ng/ml/mg norethindrone. During a period of 2-6hs after the administration of norethindrone, the half life of norethindrone in the plasma was approximately 1.8h, and during the period of 6-24hs, half life was variable. On the other hand, after the administration of lynestrenol, the peak level of norethindrone in the plasma was obtained within 4h, and the peak concentration of norethindrone was about 1.9 ng/ml/mg lynestrenol. During a period of 4-12hs, the half life of norethindrone was about 2.5h. The peak of the norethindrone level after the administration of lynestrenol was lower and appeared later than that after the administration of the same dose of norethindrone. Norethindrone in plasma in subjects receiving lynestrenol could be measured for a longer period than in those receiving the same dose of norethindrone. These results suggest that lynestrenol is stored in fat tissue and is slowly metabolized to norethindrone.

Administration, Oral↗

PubMed1992

Double-blind trial of promegestone (R 5020) and lynestrenol in the treatment of benign breast disease.

One hundred thirty-two women between the ages of 19 and 50, with various forms of benign breast diseases received 1 mg promegestone, or 0.5 mg promegestone, or 10 mg lynestrenol daily (double-blind), for 15 days per cycle, during three cycles. The groups were identical before treatment, with the exception of a longer history of mastodynia and mastopathies in the 1 mg promegestone group than in the lynestrenol group (P = 0.04) and a greater proportion of mastosis zones in the lynestrenol group as compared to the 0.500 mg promegestone group (P = 0.05). The effectiveness of lynestrenol both in terms of symptomatology (evaluated as good or excellent in 66.6% of the cases) and of clinical observations (evaluated as good or excellent in 59% of the cases) is not significantly different statistically from that of promegestone at 1 mg, whose effectiveness on symptomatology was good or excellent in 65.9% and 57.1% of the cases, respectively, or from that of promegestone at 0.5 mg/day (with 65% and 51.3% effectiveness, respectively). Clinical tolerance was rated good or excellent for 73.9% of the women on 1 mg promegestone and for 59.5% of the women on 0.500 mg promegestone, compared to 66.7% of the women on lynestrenol. No statistically significant difference was observed, neither between lynestrenol and promegestone 1 mg nor between lynestrenol and promegestone 0.5 mg. This study shows a clear improvement in functional and physical signs in patients treated with promegestone. Promegestone's efficacy is close to that of lynestrenol, a nonsteroidal progestin.2+ off

Adult↗

PubMed1990

The effect of peroral lynestrenol on serum lipids and lipoproteins in therapeutic amenorrhea of mentally retarded women.

Serum concentrations of total cholesterol, high-density lipoprotein cholesterol (HDL-C), apolipoprotein A1 (Apo A1), apolipoprotein B (Apo B), and triglyceride (TG) were measured and that of low density lipoprotein cholesterol (LDL-C) calculated in blood samples obtained from mentally handicapped women undergoing therapeutic amenorrhea (TA) induced by 5-10 mg of peroral lynestrenol, some receiving, some not receiving simultaneous anticonvulsant therapy (phenytoin, carbamazepine or barbiturate, alone or in combination). In addition, these analyses were carried out in women receiving only anti-convulsants and in controls (mentally handicapped women not receiving any of the above-mentioned medications). Significantly lower HDL-C, Apo A1, TG and cholesterol concentrations were measured in TA patients receiving lynestrenol only, than in those receiving anticonvulsants only, or in controls (p less than 0.001). With regard to HDL-C and Apo A1, patients receiving both lynestrenol and anticonvulsants were intermediate between lynestrenol only patients and controls, but the HDL-C/LDL-C and Apo A1/Apo B ratios were similar to those observed in lynestrenol only patients. Addition of 8 or 12 mg of estriol succinate to the lynestrenol regimen was virtually without an effect. However, halving of the lynestrenol dose resulted in a significant increase in HDL-C and in the HDL-C/LDL-C and Apo A1/Apo B ratios (p less than 0.001 or p less than 0.01), respectively. The lynestrenol dose was thus the most important determinant of lipoprotein pattern and should be kept as small as possible in order to reduce cardiovascular risk.

Adult↗

PubMed1980

Lynestrenol: a progesteronelike agent with immunostimulatory properties.

Lynestrenol, a synthetic progesteronelike drug, was assessed for its influence upon human leukocyte tests in vitro and in vivo. Lynestrenol markedly enhanced the lymphocyte response to phytohemagglutinin, the mixed lymphocyte culture, the active T-rosette test, the autologous red cell rosettes, and the number of nonadherent cells in the leukocyte adherence inhibition test. All these results indicate a stimulatory effect upon human T-cell function. Lynestrenol also increased monocyte phagocytosis. Lynestrenol delayed the appearance of malignant tumors in hamsters. Finally, lynestrenol, given to lung cancer patients, increased their T-cell functions as evaluated by skin tests. T-cell rosettes, and phytohemagglutinin response. Lynestrenol does possess immunostimulatory properties.

Adjuvants, Immunologic↗

PubMed1984

Androgenic, anabolic, estrogenic and antiestrogenic effects of desogestrel and lynestrenol: effects on serum proteins and vaginal cytology.

Eight healthy (apart from pelvic endometriosis) women were given daily doses of 0.125, 0.250 and 0.500 mg of desogestrel or 5 mg of lynestrenol orally in a randomized order. Duration of each treatment was 6 weeks. Serum was analyzed for sex hormone binding globulin (SHBG), ceruloplasmin, cortisol binding globulin (CBG), thyroxine binding globulin (TBG) and prealbumin using an electroimmunoassay. Serum 17 beta-estradiol (E2) and testosterone (T) were analyzed by radioimmunoassay. Vaginal cytology was studied using the maturation value (MV). E2 levels were depressed by desogestrel and lynestrenol apart from values in two women after 0.125 mg desogestrel. T concentration was suppressed by desogestrel but not by lynestrenol. SHBG concentration and MV were dose-dependently suppressed indicating an antiestrogenic or possibly androgenic effect of desogestrel and lynestrenol. No androgenic or anabolic effects of desogestrel were however seen, e.g. suppression of TBG content or increase in prealbumin levels. For lynestrenol, however, a small but significant increase in prealbumin concentration indicated a weak androgenic/anabolic effect. No estrogenic effects were seen, e.g. increases in ceruloplasmin, CBG levels or in elevations of MV. A depressed SHBG production ability in the hepatocytes during treatment with 19-nortestosterone derivatives is postulated, possibly due to competitive receptor binding.

Adult↗

PubMed1984

Metabolism of lynestrenol: characterization of 3-hydroxylation using rabbit liver microsomes in vitro.

In spite of the absence of oxygen at C-3, lynestrenol (17 alpha-ethynyl-4-estren-17 beta-ol) has a marked progestational activity. It is known to be metabolized to norethindrone (17 alpha-ethynyl-4-estren-17 beta-ol-3-one) by 3 beta-hydroxylation and dehydrogenation. In the present study this conversion of lynesterol to norethindrone, via the formation of 3 alpha-hydroxylynestrenol, was investigated using rabbit liver microsomes in vitro. Two hydroxylated metabolites, 3 alpha-hydroxy-lynestrenol and 3 beta-hydroxy-lynestrenol were separated and identified by GLC and GC-MS analyses. In the course of incubation, the concentration of 3 alpha-hydroxy-lynestrenol was much higher than that of the 3 beta-hydroxy isomer suggesting that the metabolic pathway in the conversion to norethindrone proceeds predominantly via 3 alpha-hydroxylation of lynestrenol.

Animals↗

PubMed2000

Leuprorelin depot 3.75 mg versus lynestrenol in the preoperative treatment of symptomatic uterine myomas: a multicentre randomised trial.

OBJECTIVES: To compare the effect of the gonadotrophin-releasing hormone agonist leuprorelin and progestin lynestrenol, given prior to surgical treatment of symptomatic uterine myomas, on the pre-operative symptoms, tolerance, and operative blood loss. STUDY DESIGN: Fifty-six women were randomly selected to receive, during 16 weeks, either monthly subcutaneous injections of leuprorelin 3.75 mg sustained release (n=33) or lynestrenol 5 mg two tabs per day (5th to the 25th menstrual cycle) (n=23). RESULTS: Intent-to-treat analysis of the main efficacy criterion, namely ultrasonographic reduction of myoma(s) diameter, showed a significant difference in favour of leuprorelin (P=0.02) with a mean decrease of 26.5+/-4.5% (n=29) as opposed to 7.3+/-5% in the lynestrenol group (n=17). Clinical improvement was satisfactory in both groups. Hematocrit decrease between the preoperative value and the value measured 48 h postoperatively was significantly lower in the leuprorelin group than in the lynestrenol one (P=0.02) (for hemoglobin: P=0.07). CONCLUSION: Leuprorelin was more effective than lynestrenol because of its more intense antigonadotropic activity. The tolerance was good, reflecting each drug mechanism of action.

Adult↗

PubMed1988

Peroral lynestrenol and arterial disease in mentally retarded women. A case-control study based on autopsy findings.

Autopsy findings from 170 non-smoking and mentally retarded women aged 12-51 years were analysed for any epidemiological association between the use of peroral lynestrenol for inducing therapeutic amenorrhea (TA) and arterial disease. Eighty-six women had received lynestrenol continuously for an average of 81 months (range 2-220 months) and the other 84 had not. After exclusion of 6 cases with known risk factors (diabetes, hypertension) predisposing to arterial disease, pathological arterial changes were found in 16 patients, 10 of them belonging to the TA group and 5 to the non-lynestrenol group. The incidence of arterial disease at autopsy at the age of 35 or more was 8/19 in TA patients and 1/15 in non-lynestrenol patients (p = 0.078). The benefits of prolonged TA induced by lynestrenol in this group of patients must be weighed very carefully against the possible risks involved.

Adolescent↗

PubMed1980

Effects on sex hormone binding globulin of different oral contraceptives containing norethisterone and lynestrenol.

Six combined oral contraceptive drugs containing ethinyloestradiol or mestranol and norethisterone or lynestrenol were studied throughout six 21-day cycles in healthy female volunteers. There was always one menstrual cycle without treatment between every treatment cycle. Plasma levels of norethisterone were determined throughout treatment by use of a specific radioimmunoassay. Sex hormone binding globulin (SHBG) was measured by an ammonium sulphate precipitation method at the beginning and at the end of each treatment cycle. The results indicated an accumulation of norethisterone in plasma when 1 to 3 mg of norethisterone or lynestrenol was given. There was no obvious accumulation during treatment with 0.5 mg norethisterone. SHBG increased during treatment with all combinations studied. However, this increase was most pronounced with the 50 microgram ethinyloestradiol/l mg lynestrenol, 50 microgram mestranol/l mg norethisterone and 35 microgram ethinyloestradiol/0.5 mg norethisterone combinations. There was no statistically significant increase in SHBG with 50 microgram ethinyloestradiol/2.5 mg lynestrenol or 50 microgram ethinyloestradiol/3 mg norethisterone acetate combinations. The results indicated that the induction of SHBG by the synthetic oestrogens was antagonized by the progestogens in a dose-dependent manner. The effect on SHBG by a combind preparation could be one assessment of the oestrogenicity or androgenicity of the preparation.

Adult↗

PubMed1991

Serum lipids and lipoproteins during therapeutic amenorrhea induced by lynestrenol and depot-medroxyprogesterone acetate.

Serum concentrations of total cholesterol, low-density lipoprotein cholesterol (LDL-C), high-density lipoprotein cholesterol (HDL-C), triglyceride (TG), apolipoprotein A1 (Apo A1), and apolipoprotein B (Apo B) were determined in mentally handicapped subjects (n = 87). 33 women were on lynestrenol 5-10 mg for therapeutic amenorrhea (TA). 18 of them were randomly allocated to continue on lynestrenol and 15 were switched to intramuscular administration of medroxyprogesterone (DMPA). The switch to DMPA resulted in significant increases in HDL-C (33%), Apo A1 (12%), as well as in the HDL-C/LDL-C (48%) and Apo A1/Apo B (22%) ratios. The concentrations of HDL-C and Apo A1 were significantly greater in patients receiving DMPA, than in patients continuing with lynestrenol therapy. The amenorrhea incidence, however, did not differ between the two therapy groups. It is concluded that therapy with DMPA may be associated with smaller atherosclerosis risk than with peroral lynestrenol, because of its weaker effect on HDL-C and A1 levels.

Adult↗

PubMed1992

[Lynestrenol and allylestrenol in the therapy of postmenopausal hot flushes].

In a parallel randomized placebo controlled clinical trial the authors tested two synthetic gestagens--allylestrenol and lynestrenol--in the treatment of postmenopausal flushes. Both preparations were administered during a six-week period in rapidly declining doses. Allylestrenol was administered in initial doses of 30 mg/d, after five days the doses were reduced so that after 15 days a daily dose of 5 mg was reached. The initial dose of lynestrenol was 10 mg/d with a similar gradual decline to 1.25 mg per day. The trial comprised 42 women with menopausal flushes after a natural or artificial menopause (castration). Both preparations improved the subjective condition of the patients and reduced the gonadotropic production significantly better than placebo (p < 0.05). Subjective relief after lynestrenol was recorded after the second week of therapy, in allylestrenol only after the sixth week when the effects of the two preparations were equal and significantly better than after placebo. Suppression of gonadotropin production was similar after both preparation but with a more rapid onset after lynestrenol and a more prolonged effect after allylestrenol even after significant reduction of the doses. No serious undesirable effects were recorded, no changes in indicators of liver functions or serum lipids incl. the HDL/LDL ratio. Endometrial bleeding after administration of hormones was not more frequent than after placebo. In the discussion the authors analyze some aspect of treatment of the climacteric syndrome by means of these hormones. Allylestrenol in particular is an interesting gestagen due to its inherent oestrogenic effect in the absence of an androgenic effect.

Adult↗

PubMed2005

In vivo induction of sister chromatid exchanges (SCEs) and chromosomal aberrations (CAs) by lynestrenol.

Genotoxicity study of synthetic progestin lynestrenol, was carried out on mouse bone marrow cells using sister chromatid exchanges (SCEs) and chromosomal aberrations (CAs) as parameters. Lynestrenol was studied at three different doses (6.87, 13.75 and 27.50 mg/kg body wt.). SCE and CA increased significantly as compared to normal control when treated with lynestrenol at 13.75 and 27.50 mg/kg body wt. The present results suggest that lynestrenol has both a genotoxic and cytotoxic effects in mouse bone marrow cells.

Animals↗

PubMed1979

The effect of lynestrenol and norethindrone on the carbohydrate and lipid metabolism in subjects with gestational diabetes.

The aim of this study was to investigate the effect of two different low-dose progestogens--norethindrone 0.3 mg per day and lynestrenol 0.5 mg per day--on carbohydrate and lipid metabolism in women who have had gestational diabetes. Fifteen patients were treated with norethindrone and 17 with lynestrenol, over a period of one year. The control group consisted of 13 women using an IUD. In both treatment groups all the women had normal OGTT curves during the use of norethindrone or lynestrenol. A very slight deterioration in the glucose tolerance was observed in the norethindrone group. There was no deterioration in the glucose tolerance in the lynestrenol and the IUD groups. We could not find any significant changes in mean fasting plasma cholesterol and triglyceride values.

Adult↗

PubMed1985

Effects of desogestrel, levonorgestrel and lynestrenol on serum sex hormone binding globulin, cortisol binding globulin, ceruloplasmin and HDL-cholesterol.

The effects of 0.125 mg daily doses of the new progestagen, desogestrel, 0.125 mg of levonorgestrel or 5 mg of lynestrenol on serum sex hormone binding globulin (SHBG), cortisol binding globulin (CBG), ceruloplasmin and HDL-cholesterol were studied in 30 healthy female volunteers to compare the possible androgenic and oestrogenic effects of these contraceptive steroids in vivo. All the progestagens in the applied dosages decreased SHBG and HDL-cholesterol concentrations, suggesting some androgenicity. Lynestrenol increased ceruloplasmin and CBG concentrations, indicating weak oestrogenic effects of the steroid. During desogestrel treatments, CBG and ceruloplasmin concentrations remained unchanged. After 30 days treatment with levonorgestrel there was a slight decrease (P less than 0.05) in ceruloplasmin concentrations. Thirty days after finishing the progestagen treatments serum protein concentrations were normal. In conclusion, at the doses used and under the present test conditions the progestagens studied had a weak androgen-like effect and lynestrenol also showed weak oestrogenic activity, as determined by their effects on serum proteins.

Adolescent↗

PubMed1986

Effects of tibolone, lynestrenol, ethylestrenol, and desogestrel on autoimmune disorders in NZB/W mice.

The effects of two progestagens--lynestrenol, desogestrel--an anabolic steroid--ethylestrenol--and a compound with weak progestational, anabolic, androgenic, and estrogenic activities--tibolone--on the development of systemic lupus erythematosus and Sjögren's syndrome-like disorders were studied in the NZB/W mouse. All four compounds inhibited the expression of autoimmune disease. Tibolone was 10-40 times more potent--depending on the parameter used--in preventing symptoms of autoimmunity than the second most effective compound lynestrenol. Ethylestrenol was the third effective compound and desogestrel the least effective compound in this series. Combined with literature data, these results show that steroids with different endocrine profiles can prevent the development of autoimmunity in the NZB/W mice. Since the NZB/W mouse is a good animal model for human systemic lupus erythematosus and Sjögren's syndrome and since tibolone, lynestrenol, and ethylestrenol have endocrinological profiles which are not prohibitive for treatment of male and female patients, investigation whether these compounds have a value in the treatment of human autoimmune diseases seems warranted.

Anabolic Agents↗

PubMed1984

[Lipoprotein changes during hormonal treatment of endometriosis with lynestrenol and danazol].

The Lipoprotein profile of 24 patients with endometriosis was determined before, during and after the treatment with the two steroid hormones Lynestrenol (10 mg/day) and Danazol (600-800 mg/day). The total cholesterol triglycerides, beta-, prebeta-, and Alphalipo -protein bound to cholesterol were determined. Both hormones cause a marked lowering of the Alpha-Lp-cholesterin. In addition, the beta-LP-cholesterin was elevated and the beta-alpha-LP-ratio was elevated. In the dosage used by us, Lynestrenol showed less effect on the Lipoprotein profile. Danazol caused changed in the beta- and alpha-lipoprotein pattern of highly pathological atherogenic types. The total cholesterol was not influenced. Since women in the fertile age group will suffer a higher risk of arteriosclerosis from an elevation of the beta-LP-cholesterin, the treatment with Danazol calls for a sophisticated monitoring of the lipid metabolism and care in the indication for long term treatment with Danazol or with Lynestrenol.

Adult↗