oxendolone and Prostatic-Hyperplasia

In a randomized triple-blind multicentre study, injections with the anti-androgenic agent oxendolone were compared with placebo in the treatment of benign prostatic hyperplasia. Thirty patients were treated with weekly injections of oxendolone 200 mg during a 3 months' period, and 30 patients were allocated to placebo treatment. During oxendolone treatment the maximum urinary flow rate increased statistically significantly (from 6.8 ml/s to 8.2 ml/s). However compared to placebo, the oxendolone effect was statistically insignificant. A slight but statistically significant improvement of the symptoms "sensation of retention", "urgency" and "frequency", was observed following oxendolone treatment, but an almost identical effect was seen in the placebo group. Following either treatment no change was observed in the residual urine volumes, in prostatic volume as measured by transrectal ultrasonotomography, or in any other therapeutic parameters. Conservative treatment of benign prostatic hyperplasia with the antiandrogen oxendolone in a dose of 200 mg a week cannot be recommended for clinical use.

Topics: Aged; Androgen Antagonists; Double-Blind Method; Humans; Male; Multicenter Studies as Topic; Nandrolone; Prospective Studies; Prostatic Hyperplasia; Random Allocation; Urination

Antiandrogen and alpha-adrenergic blockers have recently been tried in the medical treatment for benign prostatic hypertrophy and bladder neck contracture. We herein report our results of a randomized comparative study on the clinical efficacy of oxendolone, bunazosin hydrochloride (bunazosin) and their combination for the treatment of benign prostatic hypertrophy and bladder neck contracture. The attending doctors evaluated at twelve weeks the improvement rate for three treatment regimens, 400 mg/day oxendolone, 3 mg/day bunazosin and a combination of both. Oxendolone + bunazosin showed the highest improvement rate in the evaluation of each subjective symptom and objective finding and of both. Oxendolone + bunazosin tended to show a better clinical efficacy than the other of these regimens, when the improvement was defined as that with more than one degree in the severity of retarded voiding, prolonged voiding, urinary stream condition, abdominal pressure on voiding and residual urine sensation. The improvement of such subjective symptoms seemed to occur earlier with oxendolone + bunazosin or bunazosin than with oxendolone. A significant difference was shown among the three treatment regimens in the general improvement rate on four subjective symptoms, with oxendolone + bunazosin being the highest followed by bunazosin and oxendolone in this order. The improvement rates of maximum and mean flow rate which are most important parameters to evaluate the voiding condition, at twelve weeks were significantly higher with oxendolone + bunazosin. No serious side effects were observed in this study, although treatment regimens containing bunazosin caused some minor side effects. These side effects could be prevented by the use of initial low doses of bunazosin with a subsequent gradual increment up to 3 mg/day. Taking the differences in the mechanism of oxendolone and bunazosin and the results of our study into consideration, we believe that the combination of oxendolone and bunazosin would be more useful in a clinical situation.

Topics: Adrenergic alpha-Antagonists; Aged; Aged, 80 and over; Androgen Antagonists; Drug Evaluation; Drug Therapy, Combination; Female; Humans; Male; Middle Aged; Nandrolone; Prostatic Hyperplasia; Quinazolines; Urinary Bladder Neck Obstruction; Urination

Antiandrogen therapy has an important role in the treatment of patients with benign prostatic hypertrophy who lack indication for surgery. Herein, the effects on lipid metabolism of administration of antiandrogen agents for benign prostatic hypertrophy are reported. Eighty patients with benign prostatic hypertrophy were each treated with the antiandrogen agents, chlormadinone acetate, allylestrenol, gestonolone caproate and oxendolone for 12 months. The levels of total cholesterol (TC), triglyceride (TG), high density lipoprotein (HDL), low density lipoprotein (LDL), alpha-lipoprotein, apoprotein, and maronediardehyde (MDA) were measured every 4 weeks after initiation of antiandrogen treatment. In the chlormadinone acetate group, the TG level was significantly decreased between 3 and 6 months after treatment (p < 0.05). In the oxendolone group, the alpha-lipoprotein level was also elevated between 3 and 6 months and between 6 to 12 months after treatment (p < 0.05). The MDA level was also significantly elevated 6 and 12 months after treatment. However, the levels of the other lipids were within the normal range. In conclusion, the changes in the levels of plasma lipoprotein, apoprotein and MDA resulting from antiandrogen therapy were unlikely to be a cause of ischemic coronary disease.

Topics: Aged; Aged, 80 and over; Allylestrenol; Androgen Antagonists; Chlormadinone Acetate; Gestonorone Caproate; Humans; Lipid Metabolism; Lipids; Lipoproteins, HDL; Male; Malondialdehyde; Middle Aged; Nandrolone; Prostatic Hyperplasia

We evaluated the effect of anti-androgen therapy for benign prostatic hypertrophy. Patients showed a significant reduction in the prostatic weight measured by means of transrectal ultrasonography after 3 to 4 months of treatment. However, there were no patients who showed any symptomatic improvement despite a reduction in the prostatic weight. They had prostatic stones more frequently than the group who showed symptomatic improvement properly. We summarized some problems of anti-androgen therapy for benign prostatic hypertrophy.

Topics: Administration, Oral; Aged; Allylestrenol; Androgen Antagonists; Chlormadinone Acetate; Humans; Injections, Intramuscular; Male; Nandrolone; Prostatic Hyperplasia

We evaluated the effect of anti-androgen therapy for benign prostatic hypertrophy on 33 patients who had undergone transrectal prostatic ultrasonography both before and after administration of anti-androgenic drugs in our clinic. Patients treated with chlormadinone acetate (CMA) orally, or TSAA-291 intramuscularly showed a significant reduction in the prostatic weight. However, this reduction was not correlated with the degree of symptomatic improvement. In addition, patients who showed no symptomatic improvement despite a reduction in the prostatic weight often had prostatic stones or small inflammatory cell infiltrations in their prostatic tissue. Therefore, the coexistence of prostatitis or bladder neck obstruction with prostatic hypertrophy may contribute to the lack of symptomatic improvement in such patients.

Topics: Administration, Oral; Androgen Antagonists; Chlormadinone Acetate; Humans; Injections, Intramuscular; Male; Nandrolone; Prostate; Prostatic Hyperplasia; Ultrasonography

To investigate the effect of anti-androgens on BPH, Oxendolone (OXD), a pure anti-androgen, was tested in experimentally induced BPH in 17 beagle dogs, alone or in combination with medroxyprogesterone acetate (MPA) which displays both anti-androgenic and anti-estrogenic activity. The relatively early stage of canine BPH was induced by administration of 3 alpha-androstanediol (3 alpha-A) plus estradiol (E2) for 6 months and followed by testosterone propionate (TP) plus E2 for another 6 months during the anti-androgenic treatment. By the manipulation with T, a decrease in volume of glandular component associated with a relative increase in stromal tissue was achieved, which mimics human BPH histology. The prostate substituted with T and E2, however, gradually decreased in size. Therefore the effect of OXD or OXD + MPA was not significant against the untreated controls (T-E control). The weight of the prostate in these OXD +/- MPA groups was however significantly reduced as compared to that of BPH controls which received 3 alpha-A and E2 throughout the experimental period. On histological examination, atrophic changes were observed in the hormone-treated groups compared to the T-E control. The finding was the most striking in the OXD + MPA group with small non-involuted acini scattered in the abundant stomal tissue. This was almost identical to the appearances of castrated control groups. Atrophy may be due not only to the anti-androgenic but also to the anti-estrogenic property of MPA. A report on the hormonal background of this experiment will appear in the second article.

Topics: Androstane-3,17-diol; Animals; Dogs; Estradiol; Male; Medroxyprogesterone; Medroxyprogesterone Acetate; Nandrolone; Prostate; Prostatic Hyperplasia; Testosterone

The results of hormonal investigation of effects of an antiandrogen, Oxendolone (OXD), alone or in combination with medroxyprogesterone acetate (MPA), on experimentally induced canine BPH are reported. Seventeen beagle dogs were divided into 5 groups: 2 castrate controls for Group 0, 3 BPH controls for Group 1 which received 3 alpha-androstanediol (3 alpha-A) and estradiol (E2) for one year, and 12 dogs consisting of 3 groups which received 3 alpha-A and E2 for 6 months followed by testosterone propionate (TP) and E2 for another 6 months. The last 3 groups were treated with either 200 mg/week of OXD (Group 3) or OXD + 30 mg/week of MPA (Group 4), and otherwise untreated with these hormones (Group 2, T-E controls). On the blood hormone analysis, both T and 5 alpha-dihydrotestosterone (DHT) were generally lowered in the T-E administered groups (Group 2, 3 and 4) compared to those in Group 1. While MPA significantly decreased these androgen levels, OXD did not influence at all. The concentrations of E2 were similar. Although T content in the prostate did not differ significantly within the experimental groups, DHT was the highest in Group 1 and the lowest in Group 4 and was nearly the same level to Group 0. MPA reduced tissue DHT content but OXD did not. In the receptor assay study, nuclear androgen receptor (AR) content in Group 3 and 4 was significantly lower than that in Group 1. No obvious decrease in nuclear AR content could be seen among the other groups.(ABSTRACT TRUNCATED AT 250 WORDS)

Topics: Animals; Dihydrotestosterone; Dogs; Estradiol; Male; Medroxyprogesterone; Medroxyprogesterone Acetate; Nandrolone; Prostatic Hyperplasia; Receptors, Androgen; Receptors, Estrogen; Testosterone

The effect of a synthetic steroidal compound TSAA-291 (16 beta-ethyl-17 beta-hydroxy-4-estren-3-one) on the binding of methyltrienolone (R1881) and promegestone (R5020) to hyperplastic and neoplastic human prostate was investigated. TSAA-291 inhibits both androgen and progestogen binding to hyperplastic and neoplastic human prostate. Glycerol density gradient analysis revealed that the inhibition of promegestone (R5020) binding by TSAA-291 was significantly greater than that of methyltrienolone (R1881) in both hyperplastic and neoplastic human prostate. The nature of the inhibition was competitive as determined by Scatchard analysis and double reciprocal plots. Comparison of the Ki values for the inhibition by TSAA-291 of R1881 binding (3.2 X 10(-7) M) and of R5020 binding (2.0 X 10(-8) M) suggests that TSAA-291 binds to progesterone receptor with a greater affinity than to androgen receptor. Our results suggest that the effectiveness of the drug in the treatment of benign hyperplasia might be due not only to its anti-androgenic properties but also due to its ability to inhibit progesterone receptor.

Topics: Binding, Competitive; Centrifugation, Density Gradient; Cyproterone; Cyproterone Acetate; Dihydrotestosterone; Estrenes; Humans; Male; Mathematics; Metribolone; Nandrolone; Norpregnadienes; Promegestone; Prostatic Hyperplasia

Forty-three patients with benign prostatic hyperplasia were treated with weekly i.m. injections of 400 mg oxendolone for 12 weeks. The subjective symptoms were improved in 83% of these patients. Residual urine was decreased significantly and Qmax was increased by this treatment. Serum VLDL level was suppressed significantly, whereas the levels of LDL, total cholesterol, HDL-cholesterol and triglycerides were changed little. Atherosclerotic index and the ratio of (total cholesterol--HDL-cholesterol) to (HDL-cholesterol), was not influenced by the treatment. No severe side-effect was found. These findings suggest that oxendolone is the drug of choice for non-surgical treatment of benign prostatic hyperplasia.

Topics: Aged; Androgen Antagonists; Drug Evaluation; Humans; Lipids; Lipoproteins; Male; Middle Aged; Nandrolone; Prostatic Hyperplasia