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At least 19 recordsLinked to original sources

PubMed1989

Mesterolone and idiopathic male infertility: a double-blind study. World Health Organization Task Force on the Diagnosis and Treatment of Infertility.

A prospective randomized double-blind study was undertaken to assess the effect on male fertility of 6 months' treatment with the synthetic androgen mesterolone. The study was performed in seven centres and 248 infertile couples were recruited. All men and their partners were investigated according to the standardized WHO protocol--Investigation and Diagnosis of the Infertile Couple. Following this investigation, 157 couples were selected in whom the male diagnosis was primary idiopathic testicular failure or idiopathic low sperm motility; the female partner had no demonstrable cause for infertility or was under successful treatment for a minor endocrine problem. The remaining 91 couples admitted were either incompletely investigated or had some additional factor associated with infertility. Men received either 150 or 75 mg mesterolone daily or placebo. Response was assessed in terms of semen characteristics and the partner's pregnancy rate. The cumulative life table pregnancy rates among all couples 8 months after randomization were 9 +/- 3% (+/- standard error), 12 +/- 4% and 16 +/- 4% in the placebo, 75 and 150 mg mesterolone groups, respectively. The ratios of the pregnancy rates compared to placebo were 1.3 (0.5-3.2) and 1.8 (0.7-4.4) for the 75 and 150 mg mesterolone groups respectively. Among the subset of 157 couples satisfying the strict eligibility criteria, the pregnancy rates were 11 +/- 5%, 12 +/- 5% and 19 +/- 6% in the placebo, 75 and 150 mg mesterolone groups, respectively. The corresponding ratios of pregnancy rates to the placebo group were 1.2 (0.4-3.4) and 1.8 (0.6-5.3) for the 75 and 150 mg mesterolone groups respectively. There were no significant changes semen quality during the course of the study, apart from an increase in sperm concentration 3 months after the start of treatment. The increase was greatest among the placebo treated group, but did not differ significantly between treatment groups.

Adult↗

PubMed1991

Placebo-controlled trial of high-dose Mesterolone treatment of idiopathic male infertility.

The possible effect of Mesterolone (Schering N.V., Brussels, Belgium) (1 alpha-methyl-5-alpha-androstane-17 beta-ol-3-one) on semen quality and fertility of men with idiopathic oligoasthenospermia and/or teratozoospermia has been evaluated in a double-blind trial. The study included 52 patients who were treated during 12 months with either 150 mg/d of Mesterolone or placebo. The overall pregnancy rate was similar in the Mesterolone-treated cases (26%) and in the placebo control cases (48%), although a significant increase in motility and in the proportion of spermatozoa with normal morphology was recorded in the Mesterolone-treated cases. Because similar semen improvement also occurred in the placebo controls, our findings cast doubt on the possible usefulness of high-dose Mesterolone treatment of idiopathic male infertility.

Administration, Oral↗

PubMed1992

Studies on anabolic steroids--11. 18-hydroxylated metabolites of mesterolone, methenolone and stenbolone: new steroids isolated from human urine.

New metabolites of mesterolone, methenolone and stenbolone bearing a C18 hydroxyl group were isolated from the steroid glucuronide fraction of urine specimens collected after administration of single 50 mg doses of these steroids to human subjects. Mesterolone gave rise to four metabolites which were identified by gas chromatography/mass spectrometry as 18-hydroxy-1 alpha-methyl-5 alpha-androstan-3,17-dione 1, 3 alpha,18-dihydroxy-1 alpha-methyl-5 alpha-androstan-17-one 2, 3 beta,18-dihydroxy-1-alpha-methyl-5 alpha-androstan-17-one 3 and 3 alpha,6 xi,18-trihydroxy-1 alpha-methyl-5 alpha-androstan-17-one 4. These data suggest that mesterolone itself was not hydroxylated at C18, but rather 1 alpha-methyl-5 alpha-androstan-3,17-dione, an intermediate metabolite which results from oxidation of mesterolone 17-hydroxyl group. In addition to hydroxylation at C18, reduction of the 3-keto group and further hydroxylation at C6 were other reactions that led to the formation of these metabolites. It is of interest to note that in the case of both methenolone and stenbolone, only one 18-hydroxylated urinary metabolite namely 18-hydroxy-1-methyl-5 alpha-androst-1-ene-3,17-dione 5 and 18-hydroxy-1-methyl-5 alpha-androst-1-ene-3,17-dione 6 were both detected in post-administration urine specimens. These data indicate that the presence of a methyl group at the C1 or C2 positions in the steroids studied is a structural feature that seems to favor interaction of hepatic 18-hydroxylases with these steroids. These data provide further evidence that 18-hydroxylation of endogenous steroids can also occur in extra-adrenal sites in man.

Androstenols↗

PubMed1978

Mesterolone treatment of patients with pathospermia.

The response to Mesterolone, in doses of 25 mg/day, was examined in 42 pathospermic patients. Treatment lasted for 100 days. The pronounced response to the Mesterolone treatment was observed in hypozoo- and oligozoospermia with low initial fructose content in the ejaculate. Fructose content attained its normal range after the treatment. During the therapeutic period 11 wives became pregnant. The authors conclude that Mesterolone does not influence plasma FSH, LH and testosterone levels, it has only peripheral effects.

Adult↗

PubMed1990

Treatment of primary nocturnal enuresis by oral androgen mesterolone. A clinical and cystometric study.

A double-blind clinical study of 30 boys, six to ten years of age, with primary nocturnal enuresis was undertaken to assess the role of androgens in treating enuresis. The oral synthetic androgen mesterolone was selected because of its minimal potential toxic effects. Twenty boys were treated with mesterolone and 10 received placebo. Fourteen boys (70%) became dry during treatment (20 mg daily for 14 days), and 5 (25%) remained dry for a follow-up period of four months. Increased cystometric bladder capacity and disappearance of uninhibited detrusor contractions were noticed in a significant number of cases after treatment. No side effects were recorded. Mesterolone has probably modulated the autonomic innervation of the vesical musculature with correction of the defective neural mechanism which is believed to be implicated in the pathogenesis of nocturnal enuresis.

Child↗

PubMed1979

Mesterolone: thrombosis during treatment, and a study of its prothrombotic effects.

1. We describe a patient who developed deep vein thrombosis after commencing treatment with the synthetic androgen, mesterolone (Pro-Viron). 2. To investigate the potential thrombogenic action of this drug, a 21 day course of mesterolone (100 mg/day) was given to nine healthy male volunteers. 3. No significant change after treatment occurred in any of the blood tests performed (clotting times, Factor VIII coagulant activity, Factor VIII related antigen, antithrombin III activity, fibrinogen, fibrinogen-fibrin degradation products, plasminogen, euglobulin lysis time, urokinase sensitivity, platelet count, haematocrit, whole blood viscosity and plasma viscosity). 4. We conclude that in a conventional dose taken for 3 weeks mesterolone does not produce a consistent measurable prothrombotic state, nor does it enhance fibrinolysis.

Adult↗

PubMed1977

Testosterone levels and gonadotrophins in Klinefelter's patients treated with injections of mesterolone cipionate.

Hormone levels were measured in patients with Klinefelter's syndrome after treatment with 100 mg mesterolone cipionate (twice monthly). There was no difference in plasma testosterone and FSH levels in treated and untreated patients. The basal and maximum LH levels were lower, but remained raised. The urinary excretion of testosterone as measured by liquid gaschromatography was higher in treated patients after treatment was discontinued.-From these results it is concluded that in spite of reported decreases of plasma testosterone during therapy with mesterolone cipionate this drug does not lead to severe impairment of the endogenous hormone production after discontinuing treatment.

Adult↗

PubMed1992

The methyl-5 alpha-dihydrotestosterones mesterolone and drostanolone; gas chromatographic/mass spectrometric characterization of the urinary metabolites.

Before including the detection of the methyl-5 alpha-dihydrotestosterones mesterolone (1 alpha-methyl-17 beta-hydroxy-5 alpha-androstan-3-one) and drostanolone (2 alpha-methyl-17 beta-hydroxy-5 alpha-androstan-3-one) in doping control procedures, their urinary metabolites were characterized by gas chromatography/mass spectrometry. Several metabolites were found after enzymatic hydrolysis and conversion of the respective metabolites to their trimethylsilyl-enol-trimethylsilyl ether derivatives. The major metabolites of mesterolone and drostanolone were identified as 1 alpha-methyl-androsterone and 2 alpha-methyl-androsterone, respectively. The parent compounds and the intermediate 3 alpha,17 beta-dihydroxysteroid metabolites were detected as well. The reduction into the corresponding 3 beta-hydroxysteroids was a minor metabolic pathway. All metabolites were found to be conjugated to glucuronic acid.

Androstanols↗

PubMed1979

Plasma cholesterol, triglycerides, FSH and testosterone levels of normolipemic male patients with decreased fertility treated with mesterolone.

There were no changes in plasma cholesterol, triglycerides, FSH and testosterone levels of 24 healthy men treated with mesterolone for infertility during period of 6 months. The patients were normolipemic and the daily doses were 75 mg. No side-effects were noticed. Mesterolone seems to have too selective or too low androgenic effect with the doses used in order to have an influence on the lipid metabolism of men.

Adult↗

PubMed1975

[Androgenic treatment with depot mesterolone in dyspermia].

The clinical use of testosterone, and more recently of orally administered mesterolone in disorders of male fertility is of limited therapeutic efficacy, as shown by data found in the literature. On the basis of these considerations, the authors have tested mesterolone cyclopentylproprionate in 15 subjects suffering from sperm disorders. The drug, which is slowly released in the tissues has been parenterally administered at a total dose of 1,200 mg (100 mg per week). During the therapeutic trial the following aspects have been studied: spermiologic and hormonal patterns, general conditions, libido, principal organic functions and the possible side effects. Results are critically evaluated.

Adult↗

PubMed1976

[The effect of mesterolone in panmyelopathic anemia and anemia of renal failure].

A controlled randomized multicenter trial was carried out to examine the therapeutic value of the androgen mesterolone in aplastic anemia and anemia of renal failure. the drug was given in a dose of 2 mg/kg orally for 6 months. Control patients received no androgens but were otherwise similarily treated. 31 patients with aplastic anemia could be evaluated. No significant difference was found between androgen treated control cases in respect to bone marrow cellularity, improvement of peripheral blood cell counts or survival. In a group of 14 patients not being hemodialyzed with anemia from renal failure, 3 of the androgen treated and none of the control patients showed progressive and significant improvement of erythropoiesis; however, this was not a statistically significant difference when the both groups of patients were compared. The results do not suggest that the androgen mesterolone is of therapeutic value in the majority of adult patients with aplastic anemia. Possible reasons of the discrepancy to positive results reported in the literature are discussed.

Adolescent↗

PubMed1977

The hormone response to a synthetic androgen (mesterolone) in oligospermia.

Forty subfertile men with oligospermia were treated with a synthetic androgen (Mesterolone). The effect of the drug was evaluated by measuring serum testosterone, luteinizing hormone (LH), follicle stimulating hormone (FSH) and analysing the semen before and after treatment. The results demonstrated that in twenty-three patients treated for 6-9 months there was a significant decrease in serum testosterone (P less than 0.01); the means +/- SEM before and after treatment were 17.05 +/- 0.95 and 14.7 +/- 0.95 (nmol/l serum) respectively. There was a pronounced increase in serum LH (P less than 0.01), the values being 2.73 +/- 0.26 and 3.61 +/- 0.3 (u/l) respectively. However, no significant difference was found in serum FSH before and after treatment. The sperm concentration showed a variable response to treatment. In twenty-one patients there was either no change or worsening in the sperm concentration, whereas in nineteen patients an improvement was observed. The analysis of variance of sperm concentration and motility for the periods before and after treatment, for all the patients, showed no significant difference in the sperm concentration F1.145 = 2.82 (P=0.1).

Dihydrotestosterone↗

PubMedDate not supplied

The effects of mesterolone on the male accessory sex organs, on spermiogram, plasma testosterone and FSH.

42 subfertile male ambulatory patients were treated with Proviron. Moderate oligoastheno-teratozoospermia was the most common injury in sperm analysis. The treatment did not change the amount of plasma FSH, testosterone or prostate phosphatase. Acid phosphatase and citric acid of semen showed an increased activity with mesterolone treatment. The amount of fructose decreased, it is probably due to the increased number of spermatozoa, which need more fructose for their metabolism respectively. The sperm of 93% of the patients improved or stayed unchanged. 30% of the patients developed normozoospermia. 6 pregnancies were achieved.

Acid Phosphatase↗

PubMed1977

Combined mesterolon-clomiphene citrate therapy for treatment of oligospermia.

42 subfertile patients with normal levels of plasma testerone (26 subnormal, suffering from oligospermia) have been treated with a combination of clomiphene citrate (50 mg Clomid daily) and mesterolon (50 mg Proviron daily) over a period of at least 3-6 months. The treatment resulted in pregnancy in 6 cases and in a significant improvement of the sperm count in 16. In 7, however, whilst the sperm count improved the qualitative results were unsatisfactory as many sperms were immature. Restricted spermatogenesis and a sperm count below 5 million/ml must be considered unfavourable but does not constitute a counter-indication to the combined therapy. No hazardous complications were observed.

Cell Count↗

PubMed1989