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At least 19 recordsLinked to original sources
PubMed1975

[Androgen status of male diabetics. Total testosterone before and following stimulation with HCG, free testosterone, and testosterone binding capacity of patients with and without potency disorders].

In order to investigate the androgen status of diabetics we determined in 39 patients, 18-60 years old, 17 of which suffered from potency disturbances, the basal total plasma testosterone, the free testosterone fraction and the unbound plasma testosterone as well as the testosterone binding capacity. In 39 of these patients we proved the response of Leydig cells to HCG. Between normal persons and patients with and without potency disturbances basal total plasma testosterone did not differ significantly (p greater than 0.10). After a 3-day stimulation with HCG the increase of basal total plasma testosterone was significantly lower in the two diabetic groups in comparison with the normal persons (p less than 0.0005). The group with potency disturbances had significantly lower values for the free testosterone fraction (p less than 0.005) and unbound plasma testosterone (p less than 0.0025) than normal persons whereas diabetics without potency disturbances did not reveal any significant differences (p greater than 0.25 and p greater than 0.40). Further there were significant differences between the patients with and without potency disturbances (p less than 0.025) and (p less than 0.025). Testosterone binding capacity was significantly increased in the group with potency disturbances (p less than 0.0005) and also in the group without potency disturbances (p less than 0.01) as compared with controls. Moreover was it significantly higher in the group with potency disturbances than that without potency disturbances (p less than 0.01). For none of the parameters a functional correlation of age or diabetes duration could be demonstrated. The results are discussed with regard to the causes of potency disturbances in male diabetics.

Adolescent↗
PubMed1976

[Testosterone-binding capacity, free-plasma testosterone fraction, and free-plasma testosterone concentration in andrological patients (author's transl)].

Testosterone-binding capacity (TeBG), free-plasma testosterone fraction (%FT), and free-plasma testosterone concentration (AFT) were measured in 24 men with primary and 14 with secondary hypogonadism of various causes, as well as in eight with coital impotence. There was a highly significant correlation between TeBG and %FT (r = minus 0.891; P less than 0.0005). TeBG and %FT did not generally differ from normal in primary hypogonadism, while AFT was normal or decreased, depending on the corresponding whole testosterone concentrations. In secondary hypogonadism there was always an increased TeBG and decreased %FT. Depending on whole testosterone concentration, AFT was low or very low. In impotent subjects TeBG, %FT and AFT were generally normal. The role of AFT determination in andrological diagnosis is discussed.

Adolescent↗
PubMed1992

A biodegradable testosterone microcapsule formulation provides uniform eugonadal levels of testosterone for 10-11 weeks in hypogonadal men.

Limitations of presently available testosterone esters (enanthate and cypionate) include the fluctuating serum testosterone levels and the need for relatively frequent injections (every 10-21 days). These limitations of testosterone esters have prompted the development of more physiological and longer acting systems for androgen delivery. This paper reports pharmacokinetic and pharmacodynamic data with a second generation long-acting testosterone microcapsule formulation in hypogonadal men. This was a single dose, open label, nonrandomized study. Ten hypogonadal men with primary (n = 6) or secondary (n = 4) hypogonadism, otherwise in good health, received 630 mg microencapsulated testosterone in dextran solution (IM) on day 1. Serum total and free testosterone; LH; FSH; dihydrotesterone; estradiol; sex hormone-binding globulin; total cholesterol; high, low, and very low density lipoprotein cholesterol; triglycerides; and apoprotein-AII and -B were measured on multiple occasions during the 2-week control period and the 16-week treatment period. In addition, on days 0, 1, 28, 56, and 84, subjects were hospitalized for detailed hormone analyses over the 24-h period. Serum total and free testosterone levels rose quickly into the midnormal range and stayed uniformly in the eugonadal range for about 70-77 days, after which serum testosterone levels declined gradually into the hypogonadal range. Testosterone release from the microcapsule formulation over the first 10 weeks approximated zero order kinetics. Serum dihydrotestosterone levels rose into the normal range, and testosterone to dihydrotestosterone ratios remained in the physiological range. Serum estradiol levels rose and stayed in the midnormal male range. Serum sex hormone-binding globulin levels decreased significantly during treatment. Serum LH and FSH levels also significantly decreased in the six hypergonadotropic men. Total cholesterol low and very low density lipoprotein cholesterol and triglyceride levels did not change, but plasma high density lipoprotein cholesterol levels decreased significantly during treatment. These data indicate that testosterone microcapsule formulation provides uniform eugonadal levels of testosterone for about 10 weeks. The long duration and zero order kinetics make it an attractive alternative to existing methods of androgen replacement.

Adolescent↗
PubMed1979

Evaluation of various doses of testosterone on accessory reproductive organs and plasma testosterone in intact and gonadectomized rhesus monkeys (Macaca mulatta).

The effect of 10 days i.m. treatment of testosterone propionate (TP) on plasma testosterone and accessory reproductive organs were studied in adult (6 to 6 1/2 kg) male rhesus monkeys, housed under natural light conditions using six different dose levels. The study was scheduled in the month of September and October. To maintain the weight of accessory reproductive organs and testosterone levels in castrates, different dose levels of exogenous testosterone propionate were required: 3.2 mg/d for seminal vesicles, 4.8 mg/d for ventral prostate and 3.2 mg/d for plasma testosterone titer. The levels of so-called "physiological" doses of exogenous testosterone varied for various target organs under consideration. TP at a dose of 0.4 mg/d had a depressing effect on plasma testosterone in intact monkeys. For higher doses, plasma testosterone increased roughly similarly in both intact and castrated monkeys. It suggests that with otherwise "physiological" doses of testosterone propionate, there is an almost complete blockage of endogenous testosterone secretion.

Animals↗
PubMed1992

[Trimethylsilylation of testosterone, epi-testosterone and determination of their ratio in urine by GC-MS].

The trimethylsilylation of testosterone and epitestosterone was discussed in detail in this report. Both derivative conditions under which testosterone and epi-testosterone were prepared into TMS-derivatives in the presence of mercaptoethanol as an antioxidizing agent and method for the analysis of the ratio of testosterone to epi-testosterone in urine, based on GC-MS, had been established. The conditions of detection were: carrier gas was helium, derivatives were separated with SE-54 fused silica capillary column, using temperature program and detected by using multiple ion detection mode in which the ion of m/z 432 was the monitoring ion. The method is rapid, sensitive and specific. For the ratio of testosterone to epi-testosterone (testosterone: 20 ng/microliters), there is a linearity between ratio 1:1 and 10:1 (r = 0.998), the limit of detection for testosterone and epi-testosterone is 1 ng, and the minimum concentration of detection in urine is 8 ng/ml.

Antioxidants↗
PubMed1975

Plasma androgen levels in men after oral administration of testosterone or testosterone undecanoate.

Plasma testosterone and androstenedione levels in men were measured after oral administration of free testosterone and testosterone undecanoate. Both androgens were determined by simultaneous, specific radioimmunoassays after separation and isolation by thin layer chromatography. While free unesterified testosterone had no effect on plasma androgen levels, a striking increase of both testosterone and androstenedione levels was noted after administration of testosterone undecanoate, which is otherwise only achieved by parenteral testosterone application. This effect of testosterone undecanoate is probably due to absorption via the lymph rather than via the portal vessels so that peripheral circulation is reached before metabolism in the liver. Testosterone undecanoate promises to be an effective medication for oral androgen replacement.

Adolescent↗
PubMed1975

Relation between circulating levels of testosterone lh and fsh in intact and castrated, adult, male rats after testosterone administration.

Serum levels of LH, FSH and testosterone were measured by radioimmunoassay in intact and castrated, adult, male rats after testosterone was administered subcutaneously for seven days in doses ranging from 25 to 200 mug per 100 g body weight per day. Such treatment increased circulating testosterone both in intact and castrated rats, but its effects on serum gonadotrophins were different in these animal groups. All doses of testosterone suppressed serum LH and FSH in the normal rat. In the castrates, treatment with the lowest dose of testosterone resulted in serum LH levels significantly above the high castrate levels, while serum FSH tended to drop. Administration of the highest doses of testosterone did not depress serum LH and FSH in the castrates to those of intact, normal animals, though serum testosterone in these castrates was much higher than in normal, male rats. It is concluded, that the sensitivity of the hypothalamic-pituitary system for daily, subcutaneous testosterone administration during seven days is not the same in the intact and castrated, adult, male rat and that testicular factors different from testosterone may play a role in regulating production and/or secretion of gonadotrophins by the hypophysis in male animals.

Animals↗
PubMed1976

Distinct testicular 17-ketosteroid reductases, one in interstitial tissue and one in seminiferous tubules. Differential modulation by testosterone and metabolites of testosterone.

The final step in the biosynthesis of testosterone is the reduction of androstenedione, which is catalyzed by the microsomal enzyme 17-ketosteroid reductase. Evidence is presented which suggests that there are two distinct 17-ketosteroid reductases in rat testes, one in interstitial tissue and one in seminiferous tubules. The two enzymes have different pH optima, 5.6 for the one from interstitial tissue and 6.5 for the one from seminiferous tubules. At the optimum pH, a 70-fold difference in Km values was observed, 17 muM for the interstitial tissue enzyme and 0.25 muM for the enzyme from seminiferous tubules. Testosterone and metabolites of testosterone have very different effects of each of these enzyme activities. The interstitial tissue enzyme activity is inhibited by testosterone and several 5alpha-reduced metabolites of testosterone and by estrogens. The most potent inhibitor of the steroids investigated was 5alpha-androstane-3alpha, 17beta-diol, followed by 17beta-estradiol approximately equal to dihydrotestosterone greater than testosterone greater than estrone greater than estriol. 5alpha-Androstane-3alpha, 17beta-diol and 17beta-estradiol were shown to act by competitive inhibition with apparent Ki values of 2.2 and 3.7 muM, respectively. In contrast, it was demonstrated that among the above steroids, only dihydrotestosterone inhibits the 17-ketosteroid reductase activity of seminiferous tubules and this inhibition was only observed at very high concentrations of inhibitor. Testosterone stimulated the 17-ketosteroid reductase activity of seminiferous tubules. 5alpha-Androstane-3alpha, 17beta-diol at low concentrations stimulated the enzyme activity from seminiferous tubules, while it had no effect at high concentrations. The remainder of the steroids tested had no effect on the 17-ketosteroid reductase activity of seminiferous tubules. The difference in response of the two enzyme activities suggests a mechanism for local regulation of testosterone synthesis in each testicular compartment that does not involve directly pituitary gonadotropins.

17-Ketosteroids↗
PubMed1975

Radioimmunoassay of serum LH and testosterone in male rabbits actively immunized against testosterone.

Five male rabbits were actively immunized against testosterone to determine if this procedure could permanently inactivate circulating testosterone. To assess the response to immunization, serum LH, serum testosterone and antitestosterone titer (titer) were measured by radioimmunoassay at various times after immunization. All rabbits produced antisera to testosterone and developed serum LH levels similar to those measured in castrated males. The rise in serum LH was particularly pronounced after a booster immunization but these elevated levels were not maintained which suggests that biological neutralization was only transient. Serum testosterone rose dramatically after immunization and was directly correlated with titer. High serum testosterone concentrations were associated with both high and low serum LH. No correlation existed between titer ans serum LH. It is concluded that active immunization against testosterone does not necessarily result in a permanent neutralization of circulating testosterone and that titer alone is an inadequate criterion of neutralization.

Animals↗
PubMed1979

[Plasma testosterone, free testosterone fraction LH and FSH in males during the early stage of acute myocardial infarction (author's transl)].

In 18 males (age 49--79 yrs) without endocrine diseases, testosterone, free testosterone fraction, LH, FSH and cortisol (as indicator for stress) were determined in the early stage of an acute myocardia infarction. Blood was taken on admission as well as every 4 hours up to meanly 43 hours. The patients were separated in 2 groups for proving whether alterations of the parameters may depend on the severity of the myocardial infarction (group A=severe infarction; group B=not severe infarction). Testosterone showed a rapid decrease in the first 11 hours after admission, which continued less striking to the end of the investigation. Testosterone was significantly decreased in group A in comparison to group B. LH and FSH in both groups together were remarkably reduced during the whole time. Whereas group A demonstrated a tendency to decreased values in comparison to group B for LH, there were not any essential differences between the two groups for FSH. The free testosterone fraction was not altered. Cortisol in group A was twice as high as in group B during the entire investigation. The systolic pressure in group A was generally lower than in group B during the whole time. The results demonstrate an important reduction of the secretion of testosterone, LH and FSH during the early stage of the acute myocardial infarction. The testosterone suppression seems to be dependent on the severity of the myocardial infarction. These alterations may be caused by a general impaired perfusion as a consequence of myocardial infarction and a suppressive effect of increased cortisol values on testosterone levels.

Aged↗
PubMed1979

Separation and determination of testosterone and testosterone esters in selected pharmaceutical formulations.

A rapid quantitative procedure is presented for the separation of testosterone esters from their hydrolysis products through the use of the acetonitrile-infusorial earth column. The method was applied to testosterone cypionate, testosterone enanthate, and testosterone propionate. Recovery and replication of reference standard testosterone and its three esters through the proposed method ranged from 99.1 to 100.3%, and the percent relative standard deviation ranged from 0.6 to 1.0%. Two samples can be separated into testosterone and testosterone ester fractions in about 1.5 hr. The analyses of 20 injectable and one buccal tablet formulations made by 12 different manufacturers are reported.

Drug Stability↗
PubMed1978

Serum-testosterone during oral administration of testosterone in hypogonadal men and transsexual women.

Testosterone tablets of crystal size 2-5 micrometer were administered orally for 10 dags to 3 human subjects with low endogenous serum testosterone (se-T) levels. Fifty mg testosterone increased se-T slightly, while one daily dose of 200 mg maintained the se-T level within normal range for men for more than 12h. No cumulative effect was seen. Seven further subjects with low androgen production ingested 100 or 200 mg testosterone of crystal size 125-400 micrometer. Blood samples were taken frequently during the 24 h period following administration of the testosterone and se-T levels determined. Testosterone levels in serum increased in 6 patients and was maintained within the normal male range for 5-7 h. In one subject a slight but significant increase in se-T was observed although the level did not reach the normal male range. Although it has been shown that it is possible to use orally administered testosterone to maintain se-T levels in the normal male range, the convenience to the patient must be balanced against the cost and possible side effects of the large doses required.

Administration, Oral↗
PubMedDate not supplied

Testosterone-estradiol-binding globulin, unbound and total estradiol and testosterone, and total progesterone during the menstrual cycle in women with epilepsy taking antiepileptic drugs.

Total plasma estradiol, progesterone, testosterone, and the binding capacity of testosterone-estradiol-binding globulin (TeBG) were measured and plasma unbound estradiol and testosterone calculated, every second day during nine cycles in six patients with epilepsy. They all received phenytoin as one medication. Some had additionally, phenobarbital or ethosuximide. Plasma concentrations were compared with those of a group of healthy women without medication. Total plasma testosterone and TeBG binding capacity were significantly increased in the treated group, as compared to the control group. However, the unbound testosterone concentration was within the range of the controls. The percentage unbound testosterone of total plasma concentration was clearly below that of the control group. This indicates that there was a primarily increased TeBG binding capacity in patients taking antiepileptic drugs.

Adolescent↗
PubMed1978

Comparative studies of the ethynyl estrogens used in oral contraceptives: effects with and without progestational agents on plasma androstenedione, testosterone, and testosterone binding in humans, baboons, and beagles.

The effects of ethynylestradiol or mestranol given in cyclic fashion, with and without a progestational compound (norethindrone acetate, dl-norgestrel, or megestrol acetate), on plasma androgens and their binding were examined in adult women, female baboons, and beagles. The two estrogens are equivalent in their effect, and there were essentially no dose-related differences over the range examined. In human subjects, the estrogens increased total testosterone and testosterone binding, and decreased free testosterone. In baboons, estrogen produced a transient decrease in total testosterone and an increase in binding. The levels of progestational agents used did not affect total testosterone in humans, as is commonly observed with commercial agents, but did decrease it in baboons. Percentage binding was decreased in both species by the 19-nor compounds, but not by megestrol. Androstenedione levels were unaffected in human subjects, but effects of both estrogens and progestins were seen in baboons. Because of the very low levels of androgens in female beagles, this species did not lend itself well to a study of this kind. However, an increase in testosterone binding was induced by estrogen even in the absence of testosterone/estrogen-binding globulin.

Androstenedione↗
PubMed1979

Determination of plasma testosterone by mass fragmentography using testosterone-19-d3 as an internal standard. Comparison with radioimmunoassay.

Analytical procedures for the measurement of testosterone by mass fragmentography (MF) using trideuterated testosterone (testosterone-19,19,19-d3) are described. For the calculation of plasma testosterone, peak height ratios were measured by MF performed on the molecular ions of the TFA derivative of testosterone (m/e 480) and testosterone-19,19,19-d3 (m/e 483). The sensitivity of the method was judged from the lower limit of detection of the mass spectrometer which was at 10 pg. For the measurement of the precision, the inter- and intra-assay coefficients of variation (C.V.) were calculated by using a pooled plasma sample; they were 3.15% and 1.79%, respectively. The specificity was investigated by the use of 5 alpha-dihydrotestosterone and the MF method was found to afford a highly selective technique. These results obtained by MF have been compared with the results obtained by a radioimmunoassay method.

Gas Chromatography-Mass Spectrometry↗