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At least 19 recordsLinked to original sources

PubMed1988

A case-control study to evaluate the risk of congenital anomalies as a result of allylestrenol therapy during pregnancy.

The 1980-1984 data base of the Hungarian Case Control Surveillance System for Congenital Anomalies was used to evaluate possible teratogenicity of allylestrenol therapy during pregnancy. In an initial global analysis, three of the 24 congenital anomaly groups studied (ie, clubfoot, multiple anomalies, and hypospadias) had a significantly higher incidence of allylestrenol use. A case control analysis, however, excluded a pathogenetic role for allylestrenol in the etiology of clubfoot and multiple congenital anomalies. A greater use of allylestrenol in the first global evaluation was explained by a higher incidence in these groups of impending miscarriage and preterm labor, which are indications for allylestrenol therapy. The case control analysis did indicate a greater use of allylestrenol in the hypospadias group, but this difference was not statistically significant in the critical period for induction of hypospadias (ie, the third and fourth months of gestation). The causal role of subfertility in the etiology of hypospadias was an indirect factor, explaining the greater use of allylestrenol during pregnancy in this group; in Hungary, women with a history of infertility frequently receive hormonal support in the first trimester. The authors conclude that the data analyzed do not indicate any teratogenic effects of the use of allylestrenol during pregnancy.

Abnormalities, Drug-Induced↗

PubMed1985

Receptor binding of allylestrenol, a progestagen of the 19-nortestosterone series without androgenic properties.

Allylestrenol (17 alpha-allyl-17 beta-hydroxy-4-estren) is an orally active progestagen of the 19-nortestosterone series resembling progesterone since it has no detectable androgenic activity in animal studies and in the human. In the present study, the affinity of its 3-keto metabolite for the transformed progesterone receptor in intact MCF-7 cells was about twice that of progesterone and cyproterone acetate and about 2-3 times less than that of medroxyprogesterone acetate and norethisterone, reflecting the known progestational activity of allylestrenol. The affinity of 3-ketoallylestrenol for the transformed androgen receptor in intact MCF-7 cells was weak (like other progestagens lacking androgenic activity or possessing anti-androgenic activity) and lower than that of weakly androgenic progestagens. On the other hand, the relatively high affinity of 3-keto-allylestrenol for the non-transformed androgen receptor at 4 degrees C in the cytosol fraction did not reflect the known lack of androgenic activity of allylestrenol. Thus competitive studies carried out with transformed receptor complexes in intact cells at 37 degrees C and non-transformed complexes in cytosol distinguish progestagen with weak androgenic activity (e.g. norethisterone) from those displaying no androgenic activity or possessing anti-androgenic activity (e.g. 3-keto-allylestrenol, progesterone, cyproterone acetate and spironolactone).

Allylestrenol↗

PubMed1987

The effect of estradiol valerate and allylestrenol on endometrial transformation in hypergonadotropic hypogonadic women.

The effect of estradiol valerate and allylestrenol on the endometrial transformation of five hypergonadotropic hypogonadic women was evaluated. Estradiol valerate was administered throughout the whole induced cycle (28 days), while allylestrenol was added during the second half of the cycle. Endometrial biopsies were performed during allylestrenol treatment and were evaluated histologically. Samples of endometrium were also subjected to one-dimensional SDS electrophoresis. Of ten biopsies performed, only one was interpreted to be in-phase, while the others were dated proliferative (4 biopsies) or showed abortive or out-of-phase secretory transformation. The highest mean serum progesterone level, detected under allylestrenol treatment, was 1.5 ng/ml. Protein electrophoresis demonstrated relative sequential changes in the protein patterns of the 115 kDa and 150 kDa protein bands. It is concluded that allylestrenol, although having gestagen properties, may not be efficient for the induction of an adequate secretory transformation of human endometrium in the absence of ovaries.

Adult↗

PubMed1995

Effect of neonatal allylestrenol treatment (hormonal imprinting) on the serum testosterone and progesterone concentration in adult rat.

Serum testosterone concentration was significantly elevated in adult male rats by a single perinatal allylestrenol administration. One week after a second allylestrenol treatment in adulthood the hormone concentration dropped below the control values. Serum progesterone concentration was significantly lowered in adult female rats by a single perinatal allylestrenol administration. Following a second allylestrenol treatment in adulthood the hormone concentration reached the control values. These experiments demonstrate that the hormonal imprinting caused by allylestrenol (a steroid used in the treatment of endangered pregnancy) not only acts at receptor level and produces changes in sexual behaviour, but also induces modifications in serum hormone concentrations.

Aging↗

PubMed1997

Effects of steroid 5alpha-reductase inhibitor ONO-9302 and anti-androgen allylestrenol on the prostatic growth, and plasma and prostatic hormone levels in rats.

ONO-9302 [epristeride; (-)-17beta-(tert-butylcarbamoyl)androsta-3,5-diene-3-carboxy lic acid] is a novel inhibitor of steroid 5alpha-reductase. We studied in vitro and in vivo effects of ONO-9302 on the rat prostatic tissue in comparison with those of the anti-androgen allylestrenol. ONO-9302 inhibited the rat prostatic enzyme with an IC50 value of 11 nM, whereas allylestrenol was about 80,000-fold less potent. The growth of ventral prostate, which was induced by the subcutaneous injection of testosterone propionate in the castrated rats, was significantly reduced by ONO-9302 at oral doses of 1-100 mg/kg/day. Allylestrenol showed a significant effect only at a dose of 100 mg/kg/day. In mature male rats, ONO-9302 significantly reduced the ventral prostate weight at doses of 10-100 mg/kg/day and decreased prostatic 5alpha-dihydrotestosterone (DHT) content associated with a rise in testosterone (T) content at doses of 0.1-100 mg/kg/day. Plasma hormone levels (i.e., T, DHT, luteinizing hormone (LH) and follicle stimulating hormone (FSH)) were not altered significantly. Allylestrenol significantly reduced the ventral prostate weight at doses of 10-100 mg/kg/day. However, unlike ONO-9302, allylestrenol reduced both the prostatic DHT and T contents and also lowered plasma T, DHT, LH and FSH levels at a dose of 30 mg/kg/day. These results suggest that ONO-9302 reduces the prostatic growth by inhibiting the conversion of T to DHT in the prostate without lowering blood T level unlike anti-androgen drugs.

5-alpha Reductase Inhibitors↗

PubMed1992

Impact of single neonatal allylestrenol treatment on the estrus cycle of rats treated with FSH+LH or TSH.

Neonatal allylestrenol treatment administered to female rats significantly increases the duration of estrus phase in the sexual cycle. Treatment with follicle stimulating hormone (FSH) + luteinizing hormone (LH) in adulthood prolongs the duration of estrus even on its own; the effect, however, is more pronounced in those animals who were treated (imprinted) with allylestrenol neonatally. When administered to the control animals, the chemically related thyreotrop hormone (TSH) is either indifferent or it even decreases the estrus index. In animals having received neonatal allylestrenol treatment, however, TSH administration increases significantly the duration of the estrus phase. Either with or without FSH+LH treatment, the ratio of estrogenic to gestagenic phase increases following neonatal allylestrenol treatment. The experiments call attention to the potential functional risks inherent in neonatal allylestrenol treatment. The actual risks, however, seem to be smaller than the effects seen at the receptor level.

Allylestrenol↗

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↗

PubMed1983

[Fundamental and clinical study of the anti-prostatic effect of allylestrenol].

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.

5-alpha Reductase Inhibitors↗

PubMed1980

Allylestrenol: three years of experience with Gestanon in threatened abortion and premature labor.

Allylestrenol was used to treat 375 women with threatened pregnancies. Results show that this drug is capable of maintaining pregnancy in a large series of ambulant patients and is safe for both mother and child. Allylestrenol does not maintain pregnancy if placental dysfunction is present, however. Newborns whose mothers are treated with allylestrenol have slightly higher birth weights than controls. The possible role of allylestrenol in this process is discussed. At high doses, allylestrenol effectively stops premature labor, suggesting a selective action on the myometrium.

Abortion, Threatened↗

PubMed1998

Clinical significance of interruption of therapy with allylestrenol in patients with benign prostatic hypertrophy.

BACKGROUND: 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). METHODS: 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). RESULTS: 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. CONCLUSIONS: 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.

Aged↗

PubMed2002

[Clinical effects of allylestrenol on patients with benign prostatic hyperplasia (BPH) evaluated with criteria for treatment efficacy in BPH].

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.

Aged↗

PubMed1993

[Clinical study of allylestrenol (Perselin) on patients with prostatic hypertrophy].

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.

Administration, Oral↗

PubMed1976

[Influence of allylestrenol on hpl serum levels in high-risk pregnancies (author's transl)].

32 patients with high-risk pregnancies were treated with 3 X 5 mg of 17alpha-ally1-17beta-hydroxy-estr-4-ene (allylestrenol, Gestanon) daily. Only those patients entered this study, who had pathological HPL serum levels during two successive control investigations. In addition, cytological analyses of vaginal smears were performed before treatment was started. The patients were treated with allylestrenol until normal HPL levels were recorded, but at least during 14 days. HPL serum levels were estimated every second day through 14 days. Thereafter HPL assays were performed in weekly intervals. Determinations of HPL were done by radioimmunoassay. Analyses of vaginal smears were done weekly. Statistical analysis of HPL serum levels were performed by Student's-t-test. A statistical significant increase of HPL serum levels were registered during allylestrenol therapy. These results suggest that the pregnancy maintaining effect of allylestrenol is at least partly due to a stimulation of placental function. Analyses of vaginal smears indicate a progestational effect of the norsteroid.

Allylestrenol↗

PubMed1995

Effect of prenatal allylestrenol treatment (hormonal imprinting) on the serum testosterone and progesterone level in adult rats.

1. Female rats were treated with allylestrenol on the 15th, 17th and 19th days of their pregnancy. 2. Serum testosterone and progesterone level of their three months old offspring were higher than control in males and females, respectively. 3. Serum progesterone levels of females, treated both prenatally and in adulthood, does not differ from control values. Serum testosterone level of males, treated prenatally and in adulthood, is lower than control. 4. One single allylestrenol treatment in adulthood does not make changes in testosterone concentration in males, but progesterone level is elevated in females. 5. Our experiments draw attention to the dangers of prenatal allylestrenol treatments (administered in case of endangered pregnancies) which may have long lasting effects on sexual steroid hormone levels.

Aging↗

PubMed1999

Effect of perinatal synthetic steroid hormone (allylestrenol, diethylstilbestrol) treatment (hormonal imprinting) on the bone mineralization of the adult male and female rat.

Neonatal treatment with allylestrenol or diethylstilbestrol (DES) reduced the bone mineral content (BMC/bw) of the adult (four months old) female rats, without influencing bone mineral density (BMD/bw). In males these neonatal treatments elevated BMC and BMD alike. Ovariectomy alone decreased BMC and BMD alike; however the neonatal hormone treatments did not influence this reduced value. Ovariectomy of two months old animals increased body weight without the influence of neonatal hormone treatments. In adult males, the body weight was reduced significantly by neonatal DES and non-significantly by neonatal allylestrenol treatment. The experiments call attention to the possible human bone-effects of allylestrenol, which was used in the last decades as medication protecting endangered pregnancies.

Absorptiometry, Photon↗

PubMed2006

Recovery of serum prostate specific antigen value after interruption of antiandrogen therapy with allylestrenol for benign 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).

Allylestrenol↗

PubMed1986

[Clinical effects of allylestrenol on prostatic hypertrophy].

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.

Aged↗

PubMed1994

Effects of benzpyrene and allylestrenol administered during pregnancy on the sexual behaviour of castrated and hormone treated adult rats.

Treatments with benzpyrene on the 15th, 17th and 19th day of the pregnancy result in sexually significantly less active offspring females following castration and treatments with sexual hormones in adulthood. The receptivity of animals treated with allylestrenol in embryonic period is also decreased but was not significant. Treatments with allylestrenol or benzpyrene of newborns did not alter the hormone-induced sexual behaviour. Comparing with our previous experiments it seems that the effect of benzpyrene--which is structurally more distinct however it binds to the steroid receptor--is more pronounced on the sexual behaviour than allylestrenol.

Allylestrenol↗