allylestrenol and Prostatic-Hyperplasia

One hundred and twenty-nine patients with benign prostatic hypertrophy (BPH) were registered and treated with allylestrenol. Allylestrenol was administered at a dose of 50 mg/day given twice a day for 16 weeks. Out of 129 patients with a mean age of 67.8 years old, 92 cases completed the study and 48 cases with moderate symptoms were objectively evaluated with "Criteria for Treatment Efficacy in BPH" proposed by The Japanese Urological Association in 1997. Prostate volume was significantly decreased from 32.7 +/- 11.9 to 27.4 +/- 11.2 ml (mean +/- SD), and maximum flow rate was significantly increased from 8.4 +/- 3.4 to 10.8 +/- 5.0 ml/sec. Residual urine volume was significantly decreased from 62.4 +/- 57.4 to 37.0 +/- 38.7 ml. IPSS was significantly decreased from 15.3 +/- 4.9 to 9.9 +/- 4.0, and QOL index was significantly decreased from 4.4 +/- 0.8 to 2.7 +/- 1.2. The efficacy of allylestrenol was shown by its effects on prostate volume (anatomy), maximum urinary flow rate (function), and symptom scores (symptom) at the end of 16 weeks of treatment. The rates of improvement for symptoms, QOL, function, and anatomy are 68.7% (N = 48), 79.2% (N = 48), 50.0% (N = 48), and 61.0% (N = 41), respectively. Overall efficacy (Good and Fair) was 70.9% (N = 48). During this study, 5 patients (3.9%) complained of loss of libido and 2 patients dropped out. In conclusion, allylestrenol was demonstrated to be a quite effective and safe medical treatment for patients with symptomatic BPH based on the criteria for treatment efficacy in BPH.

Topics: Aged; Aged, 80 and over; Allylestrenol; Drug Administration Schedule; Humans; Male; Middle Aged; Practice Guidelines as Topic; Progesterone Congeners; Prostatic Hyperplasia; Quality of Life; Registries

A multicenter, clinical trial investigated the effects of an interruption of antiandrogen therapy on subjective and objective clinical parameters in patients with benign prostatic hypertrophy (BPH).. Patients were given antiandrogen therapy with allylestrenol (50 mg/day) for 16 weeks. The medication was then withheld and the patients were carefully monitored for an additional 16 weeks. There were 34 BPH patients ranging in age from 55 to 82 years (mean, 66.1 years). The efficacy of allylestrenol was evaluated by its effects on prostate volume, maximum urinary flow rate (MFR), and symptom scores at the end of 16 weeks of treatment and then again at 32 weeks (16 weeks after cessation of therapy).. Allylestrenol was effective in the treatment of BPH, and was still effective 16 weeks after the cessation of medication. The prostate volume did not change after treatment cessation nor did the total symptom score, but the MFR reversed to the pretreatment level. Serum testosterone (1.95 ng/mL), dihydrotestosterone, and gonadotropin levels decreased on therapy, but were completely reversed by the end of this study. A prostate needle biopsy revealed that after 16 weeks without therapy, some glands showed regressive glandular changes, while some glands showed slight hyperplastic changes of the secretory epithelium. Eight per cent of patients complained of loss of libido during this study.. Allylestrenol is an effective and safe medical treatment for patients with symptomatic BPH. Hormonal and histopathologic findings suggest that the prostate gland may regrow after discontinuation of medication.

Topics: Aged; Aged, 80 and over; Allylestrenol; Biopsy, Needle; Follow-Up Studies; Gonadal Steroid Hormones; Humans; Male; Middle Aged; Progesterone Congeners; Prostate-Specific Antigen; Prostatic Hyperplasia; Retrospective Studies; Safety; Treatment Outcome; Urodynamics

To determine whether transrectal ultrasonography (TRUS) can predict the clinical response of patients with benign prostatic hypertrophy (BPH) to alpha 1-blocker and anti-androgen therapy.. From April 1994 to July 1995, 128 patients with BPH were randomized to treatment for 6 months with either tamsulosin (a long-acting selective alpha 1-blocker) or allylestrenol (an anti-androgen), with 64 patients receiving tamsulosin (0.2 mg/day) and 64 receiving allylestrenol (50 mg/day). The results of TRUS, uroflowmetry and the American Urologic Association (AUA) symptom score were compared before and after treatment. TRUS was used to calculate the transition zone (TZ) volume, transition zone ratio (TZ ratio = TZ volume/total prostate volume), total prostate volume and prostate-specific antigen density (PSAD).. Both groups showed a statistically significant improvement in the AUA symptom score, quality-of-life (QOL) score and peak urinary flow rate (Qmax) at 6 months (P < 0.001). In the tamsulosin group, there was a significant negative correlation between the pretreatment PSAD and the percentage change in Qmax (r = -0.640, P < 0.001), while there was a positive correlation between PSAD and the percentage change in the AUA symptom score (r = 0.589, P < 0.001). On the other hand, the allylestrenol group showed a significant positive correlation between PSAD and the percentage change in Qmax (r = 0.397, P < 0.01) and a negative correlation between PSAD and the AUA symptom score (r = -0.313, P < 0.01).. Patients with a high pretreatment PSAD responded well to anti-androgen therapy, while those with a low PSAD responded better to alpha 1-blocker therapy.

Topics: Adrenergic alpha-Antagonists; Aged; Aged, 80 and over; Allylestrenol; Androgen Antagonists; Forecasting; Humans; Male; Middle Aged; Prostate-Specific Antigen; Prostatic Hyperplasia; Sulfonamides; Tamsulosin; Treatment Outcome; Urination Disorders; Urodynamics

Anti-androgenergic agents are usually used for patients with benign prostatic hypertrophy (BPH). However steroidal anti-androgenergic agents tend to suppress the sexual function. This side effect is very significant in middle-aged men. Therefore we studied the preventive effect of indeloxazine hydrochloride (INDX), which induces an increase of the dopamine level in the brain, on the sexual dysfunction induced by an anti-androgenergic agent (allylestrenol: ALE). Thirty-six patients with BPH were classified into two groups, one used ALE only, and the other ALE with INDX. For the subjective evaluation of the sexual function, a self assessment questionnaire method was employed before and after administration. We especially studied 3 questions, "morning erection", "erectile capacity" and "frequency of sex". For the objective evaluation of the sexual function, nocturnal penile tumescence (NPT) was measured using an erectometer. NPT occurs in healthy males as a physiological phenomenon and it shows the erectile capacity objectively. The levels of LH, total testosterone and free testosterone were also determined. In the ALE only group, sexual dysfunction was found subjectively and objectively, but in the ALE with INDX group, it was not found. Levels of LH, total testosterone and free testosterone were decreased in the both groups. There was no significant difference between the two groups. We hypothesized that the sexual dysfunction due to ALE is related with not only to the decrease of androgen, but also to suppression of the central nervous system; for example, the suppression of the area of the brain mediating sexual behavior.(ABSTRACT TRUNCATED AT 250 WORDS)

Topics: Aged; Allylestrenol; Androgen Antagonists; Humans; Male; Middle Aged; Morpholines; Prostatic Hyperplasia; Sexual Dysfunction, Physiological

A multicenter trial was carried out on 100 patients with benign prostatic hypertrophy to elucidate the efficacy of anti-androgen therapy with allylestrenol (AE). AE was administered at a daily dose of 50 mg for 16 weeks to the patients and its efficacy was evaluated with subjective symptom scores, residual urine volume and uroflow rates. The effects of AE on prostatic volume and morphology were evaluated using transrectal ultrasound. Of these patients 65 completed the protocol, and only three patients withdrew from the study owing to side effects. Very modest adverse effects on sexual performance were seen in one patient. In this study, significant beneficial effects of AE on symptom scores, residual urine, maximum flow rate, and prostate size were demonstrated. However, volumetric reduction was not associated with urodynamic improvement. Prostatic shape was not changed throughout the study. These findings suggest that allylestrenol can be used as an alternative to prostatectomy in patients who are at high risk for surgery.

Topics: Aged; Aged, 80 and over; Allylestrenol; Androgen Antagonists; Drug Evaluation; Humans; Male; Middle Aged; Prostate; Prostatic Hyperplasia; Ultrasonography; Urodynamics

Allylestrenol (ALE) and chlormadinone acetate (CMA) were administered to patients with prostatomegaly by the double-blind method, and the effects of these antiandrogens on their sexual function were objectively compared. Each agent was orally administered to 58 patients in a dosage of 50 mg/day for 12 consecutive weeks. For the objective evaluation of the sexual function, nocturnal penil tumescence (NPT) was measured using an erectometer. For the subjective evaluation the conventional interview method was employed. The levels of hormones relating to sexual function were also determined. A decrease in NPT was noted in both the ALE and CMA groups, but the degree of the decrease was significantly smaller in the ALE group than in the CMA group (p less than 0.001). The results of the interview, revealed a large between the two drug groups; in the CMA group, marked worsening for all items. In the determination of hormones, levels of luteinizing hormone, follicle stimulating hormone, testosterone and estradiol were decreased in both drug groups, while the prolactin level was increased in both groups. The changes in the testosterone, estradiol and prolactin levels in the CMA group were significantly dominant compared with those in the ALE group. In addition, drop-out cases due to a decrease in the sexual function numbered 7 (12.1%) in the CMA group, while there were no such drop-out cases in the ALE group; the difference in the drop-out rate was thus significant. In conclusion, ALE's effects on the sexual function were concluded to be smaller than those of CMA.

Topics: Aged; Allylestrenol; Chlormadinone Acetate; Clinical Trials as Topic; Double-Blind Method; Estrenes; Humans; Male; Middle Aged; Monitoring, Physiologic; Multicenter Studies as Topic; Penile Erection; Prostatic Hyperplasia; Sleep; Testosterone; Urination

Allylestrenol (ALE) and chlormadinone acetate (CMA) were administered to patients with prostatomegaly by the double-blind method, and a self-assessment questionnaire method developed by the authors was used to study the influence of these two antiandrogens on their sexual function. Each test drug was orally administered to 58 patients, in a daily dosage of 50 mg for 12 consecutive weeks. The questionnaires consisted of 6 categories each consisting of 5 questions, or 30 questions in total. The 6 categories were "sexual desire," "erectile capacity" and "ejaculation," which relate to the sexual function, and "living environment (including the frequency of sex)," "dysuria" and "dummy (personality)." Each question was graded into 0-10 points, and each patient was requested to circle the number which best described his status. The scores were compiled and statistically analyzed. Many patients were senile. Evaluable answers were obtained for 99 (85.3%) of the 116 patients. Factor analysis based on the preadministration scores confirmed the contents of the questionnaires to be appropriate for the objectives of the present study. Multiple regression analysis revealed a high correlation between the self-assessment scores and objective data (nocturnal penile tumescence values; NPT values) when dropout cases due to a decrease in the sexual function and non-replying cases were excluded. The self-assessment questionnaire method was concluded to be as useful an objective test method as the NPT measurement for examining the sexual function. Aggravation of the "frequency of urination during night" was conspicuous in the CMA group, and there was a significant difference (p less than 0.05) in this parameter between the two groups. Except for this parameter, dysuria was improved in both administration groups, and there was no significant difference in the efficacy of the two drugs. Both drugs tended to suppress overall sexual function, but the suppression was less severe in the ALE group. Especially the suppression was significantly (p less than 0.05) lower in the ALE group regarding the 3 parameters of "contact sexual arousal," "contact erection" and "morning erection", which are included in the category of "sexual desire" or "erectile capacity." Also, suppression of "frequency of sex" and "intensity of sexual desire" tended to be lower in the ALE group at a level of significance of p less than 0.1. Regarding questions in the category of "ejaculation," the incidence of non-

Topics: Adult; Aged; Allylestrenol; Chlormadinone Acetate; Clinical Trials as Topic; Double-Blind Method; Estrenes; Humans; Male; Middle Aged; Multicenter Studies as Topic; Prostatic Hyperplasia; Self-Assessment; Sex; Surveys and Questionnaires

A double blind comparative clinical trial was performed with allylestrenol (AE) and chlormadinone acetate (CMA) to investigate the clinical efficacy of AE on prostatic hypertrophy. Both drugs were administered orally for 12-16 weeks in a daily dose of 50 mg. With both drugs marked improvement of disorders of micturition and a slight decrease in the size of the hypertrophied prostatic node were observed. No significant difference was observed between the two drugs in the overall efficacy of the treatments. Significant improvement of practically all parameters used for evaluation of results was observed with both drugs following treatment. Ultrasonotomographic examination revealed diminution of the size of the prostatic node and x-ray examination of the ureter showed improvement in elevation of the fundus of the bladder. These improvements were better after CMA treatment than after AE treatment. With all other parameters used no significant difference was observed between the two drugs. Mild adverse effects such as loss of sexual desire and potency were observed in a few cases. The incidence of side-effects was lower following AE treatment, and the incidence of loss of sexual desire and potency was significantly lower after AE than after CMA. Taking into consideration efficacy and safety of the treatments, no significant difference was observed in usefulness between the two drugs, and we were able to confirm the usefulness of AE for the conservative treatment of prostatic hypertrophy.

Topics: Administration, Oral; Aged; Allylestrenol; Chlormadinone Acetate; Clinical Trials as Topic; Double-Blind Method; Estrenes; Humans; Male; Middle Aged; Prostatic Hyperplasia

Decrease in serum prostate specific antigen (PSA) concentration is inevitably associated with antiandrogen therapy for benign prostatic hyperplasia (BPH), and might mask the presence of prostate cancer or delay its diagnosis. To determine the appropriate timepoint for determination of correct PSA value, we sequentially measured serum PSA and testosterone levels after discontinuation of antiandrogen therapy for BPH. With informed consent, 12 patients (72.8 +/- 12.2* years old) with BPH were treated with allylestrenol 50 mg/day for 4 months. Serum testosterone and PSA concentrations were determined before and just after treatment, as well as every month after treatment up to 3 months. After treatment with allylestrenol for 4 months, mean serum testosterone and PSA levels were significantly decreased from 408 +/- 136* to 87.9 +/- 76.2* ng/dl, and from 2.81 +/- 0.87* to 2.04 +/- 0.82* ng/ml, respectively. The mean serum PSA level recovered to the pretreatment level within 2 months and mean serum testosterone concentration within one month after discontinuation of administration. In conclusion, during treatment of BPH with antiandrogen allylestrenol, a two-month washout is adequate for determination of correct PSA value (*: M +/- SD).

Topics: Allylestrenol; Androgen Antagonists; Humans; Male; Progesterone Congeners; Prostate-Specific Antigen; Prostatic Hyperplasia; Testosterone; Time Factors

We compared the prostate specific antigen (PSA) levels in benign prostatic hyperplasia (BPH) patients with antiandrogen chlormadinone acetate (CMA) or allylestrenol (AE) before and during the treatment. We also investigated the serial change of PSA levels before, during and after discontinuation of antiandrogen therapy. Fifty-one BPH patients with normal PSA levels were treated with CMA or AE for 16 weeks. The mean serum PSA level significantly decreased after the treatment from 1.9 +/- 1.0 ng/ml to 1.1 +/- 0.7 ng/ml (M +/- SD). We discontinued medication with informed consent and the patients were carefully monitored for another 16 weeks. Nineteen patients were followed for 32 weeks. The mean serum PSA level decreased significantly from 2.0 +/- 1.0 ng/ml to 1.1 +/- 0.5 ng/ml (M +/- SD) and recovered approximately to the pretreatment level (1.7 +/- 1.1 ng/ml) at the end of this study. We found only one patient whose PSA was slightly elevated to a subnormal range (4.3 ng/ml) after discontinuation of therapy. The other BPH patients with normal PSA levels showed no excessive increase in PSA levels beyond the normal limit after discontinuation of antiandrogen therapy compared with the pretreatment baseline. In conclusion, BPH patients with a marked increase in PSA after discontinuation of antiandrogen therapy should be checked for prostate cancer.

Topics: Aged; Aged, 80 and over; Allylestrenol; Androgen Antagonists; Chlormadinone Acetate; Drug Administration Schedule; Humans; Male; Middle Aged; Progesterone Congeners; Prostate-Specific Antigen; Prostatic Hyperplasia

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

Transurethral microwave thermotherapy (TUMT) has been shown to produce a clinical benefit in patients with symptomatic benign prostatic hyperplasia. In order to identify the features of the ideal candidate, a retrospective analysis was conducted in 32 patients who were followed for 2 mo or more. Good responders (GR) were defined as having their Siroky peak flow rate (PFR) standard deviation (SD) increase by < 0.5 or a decrease in the International Prostatic Symptom Score (I-PSS) of > 10 (22 patients). Poor responders (PR) were defined as having their PFR SD increase by < or = 0.5 and their I-PSS decrease by < or = 10 (10 patients). The prostate volume, pre-TUMT I-PSS and intravesical opening pressure were significantly greater in the GR group, while there were no significant differences between the 2 groups for the other baseline patient characteristics: age, prostate length, PFR, PFR SD, post-voiding residual volume and quality of life. Concerning the operational parameters, significantly more total energy was delivered to the prostate in the GR group (mean 131 kJ) than in the PR group (mean 101 kJ). Moreover, the 7 patients with anti-androgen therapy pre-TUMT received less total energy and 5 of the 7 were poor responders. These results suggest that patients with apparent obstructive symptoms and with moderate enlargement of prostate could benefit more from this less invasive therapy. Clinical response seems to be dose-dependent and patients with a history of recent anti-androgen treatment may have a less favorable response.(ABSTRACT TRUNCATED AT 250 WORDS)

Topics: Allylestrenol; Chlormadinone Acetate; Dose-Response Relationship, Radiation; Humans; Hyperthermia, Induced; Male; Microwaves; Pressure; Prostatic Hyperplasia; Treatment Outcome; Urination

The efficacy and safety of allylestrenol were studied in 22 patients with benign prostatic hypertrophy. A 25 mg allylestrenol tablet (Perselin tablet) was administered twice a day. A significant decrease in frequency of nocturnal urination was observed and improvement rates of subjective symptoms, such as sensation of residual urine, delay in start of urination, straining during urination and strength of urinary stream, were 59.1-68.2%. The rate of decrease of maximum area of transverse plane of prostate estimated by transrectal sonography was 13.2% and presumed circle area ratio (PCAR) improved significantly. The incidence of total side effects was 22.7%, whereas a decrease in sexual potency was observed in only 4.5% of the cases. The final global improvement rating of allylestrenol was 72.2% and the rate of usefulness was estimated in 63.6% of the patients. The present findings confirmed that allylestrenol is a useful and safe drug for the treatment of benign prostatic hypertrophy.

Topics: Administration, Oral; Aged; Aged, 80 and over; Allylestrenol; Drug Administration Schedule; Drug Evaluation; Humans; Male; Middle Aged; Prostatic Hyperplasia; Tablets

Various non-surgical therapeutic modalities such as balloon dilation of the prostatic urethra, hyperthermia of the prostate and medication with antiandrogens and/or adrenergic blockade have been attempted for the patients with benign prostatic hyperplasia (BPH) especially in an early stage or in a poor operative risk. The observation that androgen deprivation induces shrinkage of the hyperplastic prostate represents the basis for the treatment of BPH with antiandrogen. Although several antiandrogens are now in clinical use in our country, there still remain problems to be solved. We reviewed the mechanism of action and the clinical results of antiandrogens in the treatment of BPH. The improvement following antiandrogen therapy occurred among the patients with symptomatic BPH, in 50-80% subjectively and in 40-50% objectively. The therapy appeared to be more effective in an early stage of the disease. However, the limitation of the duration of the effects and unfavorable side effects should also be noticed. The progestational agents such as gestonorone caproate, chlormadinone acetate and allylestrenol suppress more or less sexual function by interference of the pituitary-gonadal axis. Besides, coincidental prostate cancer must be excluded since antiandrogen therapy might hinder the natural course of the cancer.

Topics: Administration, Oral; Allylestrenol; Androgen Antagonists; Chlormadinone Acetate; Drug Administration Schedule; Drug Evaluation; Gestonorone Caproate; Humans; Male; 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

Allylestrenol at the daily dose of 50 mg was administered to 45 patients with benign prostatic hypertrophy. The treatment was performed for more than 12 weeks in 40 patients, and improvements, marked and moderate, were observed in 22 patients (55%) in the overall judgement. As side effects of this drug, decrease of potency was observed in 3 cases, decrease of libido in 1 case, pigmentation on breasts in 2 cases, palpitation in 2 cases, short breath in 1 case, and gastrointestinal symptoms in 1 case. However, these side effects were not serious. Our trial suggests that the treatment of benign prostatic hypertrophy with allylestrenol can be useful in urological clinics.

Topics: Aged; Allylestrenol; Drug Evaluation; Estrenes; Humans; Male; Middle Aged; Organ Size; Prostate; Prostatic Hyperplasia; Urodynamics

Clinical effects of allylestrenol were studied on 26 patients with benign prostatic hypertrophy with urinary disturbances. Allylestrenol was administered at the dose of 50 mg/day given twice a day for more than 10 weeks. Evaluation of the drug efficacy was made based on urodynamic and ultrasonographic findings. One of the 26 cases dropped due to a side-effect (vertigo) and another due to defusal of treatment. The efficacy rate was 50%. Side-effects were observed in 2 cases (1 with decrease of potency and the other with vertigo) but were mild. It was concluded that allylestrenol is useful for treatment of urinary disturbances caused by prostatic hypertrophy.

Topics: Aged; Allylestrenol; Drug Evaluation; Estrenes; Humans; Male; Middle Aged; Organ Size; Prostate; Prostatic Hyperplasia; Urodynamics

Seventeen patients with benign prostatic hypertrophy were treated with 50 mg allylestrenol per day for a long period of time (mean: 37.7 weeks), and subjective and objective findings, transrectal ultrasonotomography, urodynamics, serum lipids and hormone levels were examined. Improvement rates of subjective and objective findings were 42.9-92.9%. A significant decrease in weight and diameter (antero-posterior, lateral) of the prostate was observed, but the difference in the height of the prostate was not significant. Increase in intravesical pressure was observed in 9 out of 14 cases (64.3%) and the decrease in area under the urethral pressure curve at functional profile length was observed in 6 out of 11 cases (54.5%). Slight increase of the serum lipid levels was observed in a few cases, but in many cases the fluctuation was within normal range. Although clear decrease in the testosterone levels was seen, decrease of libido and potency was observed in only one case (5.9%). No other side-effect was found. The overall efficacy rate was 58.8%, and clinical usefulness of Allylestrenol on benign prostatic hypertrophy was confirmed.

Topics: Aged; Allylestrenol; Estrenes; Follow-Up Studies; Humans; Male; Middle Aged; Prostatic Hyperplasia; Ultrasonography; Urodynamics

The anti-androgen activity of allylestrenol was studied in the rat, and it was found to have an activity which was equivalent to that of chlormadinone acetate. The direct anti-prostatic activity is the result of the following mechanism: inhibition of serum testosterone uptake into the prostate, inhibition of testosterone-5 alpha-reductase activity and inhibition of 5 alpha-DHT . receptor complex formation. Large doses of allylestrenol administered to normal mature rats, inhibit the hypothalamus-pituitary-gonadal axis, and atrophy of the prostate will be more marked due to an indirect effect as a result of the reduction in the serum testosterone level. Based on this finding, we performed a clinical trial with allylestrenol in patients with hypertrophy of the prostate and cancer of the prostate. We administered 45 mg a day allylestrenol to 19 patients with prostatic hypertrophy and obtained satisfactory clinical results in so far as improvement of micturition and reduction in prostate mass was concerned. We also administered 90 mg a day of allylestrenol to 4 patients with cancer of the prostate and obtained a cytostatic effect.

Topics: 5-alpha Reductase Inhibitors; Aged; Allylestrenol; Androgen Antagonists; Animals; Cytosol; Dihydrotestosterone; Drug Evaluation; Estrenes; Follicle Stimulating Hormone; Genitalia, Male; Humans; Luteinizing Hormone; Male; Middle Aged; Organ Size; Prostate; Prostatic Hyperplasia; Rats; Rats, Inbred Strains; Testosterone