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At least 127 records · Page 7Linked to original sources
PubMed1989

Prevention of the transient adverse effects of a gonadotropin-releasing hormone analogue (buserelin) in metastatic prostatic carcinoma by administration of an antiandrogen (nilutamide).

Gonadotropin-releasing hormone (GnRH) analogues administered for the treatment of advanced prostatic cancer induce a transient increase in plasma testosterone levels during the first week of treatment, often with a secondary rise in plasma levels of prostatic acid phosphatase and a flareup of disease. To determine whether the antiandrogen nilutamide (Anandron) blocks these effects, we carried out a multicenter, placebo-controlled study of nilutamide in men with prostatic cancer treated with the GnRH analogue buserelin. Thirty-six men with disseminated prostatic cancer and elevated plasma levels of prostatic acid phosphatase were randomly assigned to two groups. Group 1 included 17 men who received buserelin (500 micrograms daily subcutaneously) and nilutamide (300 mg daily by mouth); group 2 included 19 men treated with buserelin and placebo. Symptoms were assessed, and plasma was collected before treatment, daily for 14 days, and on days 18, 22, and 29 after the initiation of treatment. Bone pain appeared or worsened in 5 of the 17 men in group 1 and in 12 of the 19 men in group 2 (P less than 0.05). Acute urinary obstruction occurred in one man in group 2. Despite similar changes in the plasma testosterone levels in both groups, the median concentration of plasma prostatic acid phosphatase decreased almost immediately in group 1, but increased transiently, then decreased on day 14 in group 2. Median levels of prostate-specific antigen decreased immediately in group 1 and decreased on day 8 in group 2. We conclude that nilutamide can prevent the adverse consequences of the buserelin-induced transient rise in plasma testosterone levels in men with advanced prostate cancer treated with a GnRH analogue.

Acid Phosphatase↗
PubMed1997

17-Hydroxyprogesterone responses to gonadotrophin-releasing hormone agonist buserelin and adrenocorticotrophin in polycystic ovary syndrome: investigation of adrenal and ovarian cytochrome P450c17alpha dysregulation.

Abnormal regulation of cytochrome P450c17alpha causes the exaggerated secretion of ovarian androgens in polycystic ovary syndrome (PCOS). This enzyme is active in both the ovaries and adrenal glands. We examined whether there is an abnormal regulation of cytochrome P450c17alpha in the adrenal gland by investigating the relationship of 17-hydroxyprogesterone (17-OH progesterone) hyperresponsiveness to the gonadotrophin releasing hormone (GnRH) agonist, buserelin, testing with 17-OH progesterone response to adrenocorticotrophic hormone (ACTH) in PCOS. In all, 68 women with PCOS and 24 normal women were included in the study. Ultrasound, clinical and hormonal parameters were used to define PCOS. 17-OH progesterone response to ACTH was measured in all the women. In 52 of the 68 women with PCOS, 17-OH progesterone response to buserelin was measured. The mean basal 17-OH progesterone concentrations were similar in both PCOS and control groups. PCOS women had significantly higher net increment in 17-OH progesterone after ACTH administration (P<0.02). No significant correlations were found between the peak 17-OH progesterone values, the net increments in 17-OH progesterone and the area under the 17-OH progesterone-response curves after ACTH stimulation and buserelin test. Although 17-OH progesterone response to ACTH was significantly higher in the patients with PCOS than in the control subjects, the lack of relationship between 17-OH progesterone response to GnRH agonist buserelin and 17-OH progesterone response to ACTH stimulation suggests that the dysregulation of the cytochrome P450c17alpha enzyme may not play a role in adrenal androgen excess seen in PCOS.

17-alpha-Hydroxyprogesterone↗
PubMed1990

An improved use of buserelin in ovarian stimulation for in-vitro fertilization.

In earlier IVF programmes, subcutaneous buserelin (Suprefact, Hoechst) was initially administered three times per day (200 micrograms x 3); then twice daily (300 micrograms x 2). We now suggest that a single administration of 600 micrograms daily may be equally effective. In a preliminary study, 20 patients were selected on the basis of tubal or idiopathic infertility and received 0.6 ml buserelin subcutaneously once a day, beginning on day 1 or 2 of the cycle. A sufficient pituitary desensitization was obtained on day 10 in 75% of patients and on day 16 for 100% and the ongoing pregnancy rate was 35% per treatment cycle. A randomized study comparing the effect of 600 micrograms of buserelin administered in one (n = 50) or two injections (n = 46), has been carried out and indicates that the results in terms of the ovarian suppression and pregnancy rates, were similar. Therefore, this protocol represents a simplification of the treatment with buserelin.

Adult↗
PubMed1995

Endocrinological and histological changes after treatment of uterine leiomyomas with danazol or buserelin.

The following results were obtained from our investigations performed to compare the effects of danazol (400 mg/day orally for 4 to 6 months, n = 164) with those of buserelin (900 micrograms/day intranasally for 4 to 6 months, n = 83) on patients with uterine myomas. The effectiveness of buserelin (76.1%) in shrinking uterine myomas was better than that of danazol (56.7%). The serum-estradiol and progesterone levels were lower in the buserelin group than in the danazol group. The estrogen and progesterone receptors in a hysterectomied uterus were positively stained even at the end of those therapies. The degree and frequency of hyaline degeneration were higher in the buserelin group than in the danazol group. Thus, the shrinking of uterine myomas and the degree of hyaline degeneration might be caused by the lowering of uterine-tissue hormones, particularly of estradiol levels.

Adult↗
PubMed1988

Short-term utilization of a gonadotropin-releasing hormone agonist (buserelin) for induction of ovulation in an in vitro fertilization program.

Benefits of the short-term utilization of a gonadotropin-releasing hormone (GnRH) agonist (Buserelin, Hoechst, AG, Frankfurt am Mein, FRG) for induction of ovulation in an in vitro fertilization program (IVF) program were assessed. Eighteen patients underwent consecutively an induction of ovulation by clomiphene citrate (CC) and human menopausal gonadotropin (hMG), then by hMG alone, and finally by Buserelin and hMG. The switchover from CC and hMG to hMG alone significantly increased the number of aspirated follicles and the oocyte recovery rate. The addition of Buserelin prevented the outcome of spontaneous luteinizing hormone (LH) surges. It reduced the preovulatory luteinization and increased the number of recovered oocytes as well as the number of embryos available for transfer. A 33% clinical pregnancy rate per ovum pick-up was achieved with the Buserelin-hMG treatment.

Buserelin↗
PubMed1994

Successful treatment of refractory pure red cell aplasia by buserelin acetate.

A 39-year-old female with autoimmune hemolytic anemia suffered from pure red cell aplasia. She received immunosuppressive agents including prednisolone, azathioprine, cyclophosphamide and methotrexate, resulting in a little improvement of the anemia for only short term. Consequently, she required multiple red cell transfusions for 3 years. She received buserelin acetate, a gonadotropin-releasing hormone analogue. Thereafter, the anemia dramatically improved. The direct effect of buserelin on hemopoietic progenitors was not detected in the in vitro culture study. It is most likely that buserelin enhanced erythropoiesis through the alteration of hormonal milieu. The usefulness of buserelin in the treatment of refractory pure red cell aplasia is discussed.

Adult↗
PubMed1990

Urinary excretion of [D-Ser(t-Bu)6,Des-Gly10]GnRH ethylamide (buserelin) during therapy of central precocious puberty: a multicentre study.

In order to compare the clinical effects of buserelin on central precocious puberty to its excretion in urine, as a parameter of metabolism or compliance, we have studied 52 patients treated either sc or intranasally. In girls with good control, urinary buserelin excretion represented 0.5 +/- 0.1% of the daily intranasal dose vs 12.5 +/- 2.3% of the daily sc dose. In boys, it represented 0.8 +/- 0.2 and 9.9 +/- 2.7%, respectively. In the sc treated group, 3 patients (2 girls and 1 boy) with poor control who exhibited excretion levels similar to those with good control were classified as resistant to therapy. Clinical control was poor in 4 intranasally treated girls: 2 had low excretion values suggesting poor compliance or failure of absorption by the nasal mucosa, and 2 appeared resistant to therapy, as urinary excretion levels of buserelin were similar to those of well-controlled patients. In addition, these data suggest that the small amount of buserelin absorbed by the nasal mucosa, as expressed by urinary excretion, is sufficient to desensitize the pituitary gonadotropes without any significant first-pass effect in the systemic circulation. This may explain the clinical effectiveness of the intranasal route for administration of small hormonal peptides acting on the pituitary gland.

Administration, Intranasal↗
PubMed1997

Lack of relationship between 17-hydroxyprogesterone response to buserelin testing and hyperinsulinemia in polycystic ovary syndrome.

OBJECTIVE: To determine whether hyperinsulinism affects cytochrome P450c17 alpha activity by investigating the correlation between 17-hydroxyprogesterone (17-OHP) hyper-responsiveness to the gonadotropin-releasing hormone (GnRH) agonist, buserelin, and the insulin response to oral glucose in polycystic ovary syndrome (PCOS). DESIGN: Ultrasound, clinical and hormonal parameters were used to define PCOS in this prospective clinical study. We investigated the correlation between the 17-OHP response to buserelin testing and the insulin response to oral glucose in PCOS. METHODS: Twenty-eight women with PCOS and eighteen normal women were included in the study. 17-OHP response to buserelin, and insulin and C-peptide responses to oral glucose were measured. RESULTS: Twenty-five women with PCOS had an increased 17-OHP response. The PCOS patients showed significantly higher mean post-glucose load insulin and C-peptide levels than controls (P < 0.05). No significant correlations were found between basal 17-OHP and fasting insulin or fasting C-peptide, between peak 17-OHP and fasting insulin, peak insulin or peak C-peptide, between 17-OHP area under the curve (AUC) and insulin AUC or C-peptide AUC, and between percent increment in 17-OHP and insulin AUC or C-peptide AUC (P > 0.05). CONCLUSIONS: Lack of a relationship between the 17-OHP response to the GnRH agonist buserelin and hyperinsulinism suggests that hyperinsulinism may not play a role in the dysregulation of the cytochrome P450c17 alpha enzyme seen in PCOS.

17-alpha-Hydroxyprogesterone↗
PubMed1985

Changes in pituitary responsiveness to LH-releasing hormone after acute buserelin treatment: a time-course and dose-response study.

The acute in-vivo effects of a potent LH-releasing hormone (LHRH) agonist, buserelin, on LH secretion and pituitary responsiveness to LHRH have been investigated in oestrous rats. Doses of 50, 100 and 250 ng buserelin stimulated LH release in a dose-dependent manner, the peak serum LH concentrations being measured 1 h after the treatment. Thereafter LH levels fell rapidly between 1 and 6 h and by 18 h serum LH concentrations were similar in all groups of animals. Pituitary responsiveness to a challenge with 100 ng LHRH was potentiated by 50 or 100 ng buserelin injected 1 or 2 h before the LHRH challenge. In contrast, 250 ng buserelin completely abolished the LH response to LHRH when tested 1, 2 and 4 h after treatment, but by 6 h a small but attenuated response was observed. Four hours after treatment there was no significant difference in the responses when compared with the saline-treated controls.

Animals↗
PubMed1992

Buserelin in premenstrual syndrome.

Buserelin, a luteinizing hormone releasing hormone agonist was administered nasally in doses of 900 micrograms daily to inhibit the ovarian cycle. Of 16 patients recruited, ten completed the treatment. Daily symptoms were measured on the Visual Analogue Scale and Trigg's trend analysis utilized for the analysis. The peak severity of symptoms (ESAmax) and the maximum global scores (Gmax) reduced on buserelin treatment. The minimum global scores (Gmin) and the minimum score for each symptom (ESAmin) increased, suggesting worsening of underlying symptoms. The difference between ESAmax and ESAmin (ESAdelta) and Gmax and Gmin (Gdelta) were calculated to determine the degree of symptom change. The delta scores for symptoms of depression, bloatedness and breast symptoms, and Gdelta were significantly reduced (p less than 0.05) on buserelin, whilst the latter significantly worsened in the follow-up months. Side-effects may limit the place of buserelin in the long-term treatment of premenstrual syndrome, although combination of additional hormonal treatment may facilitate long-term treatment.

Administration, Intranasal↗
PubMed1990

Effect of fertirelin acetate or buserelin on conception rate at first or second insemination in lactating dairy cows.

The objective of this study was to determine if fertirelin acetate and buserelin, two GnRH agonists, improve conception rate when administered at the time of first or second AI in lactating dairy cows. The study consisted of a common protocol conducted at 10 commercial dairy farms. Approximately 150 cows within each dairy were assigned randomly in replicates to receive intramuscularly either no injection or injection of 25, 50, 75, or 100 micrograms fertirelin acetate or 10 micrograms buserelin immediately after AI. Cows were subjected to the reproductive management practices normal for each location. Cows at each location were palpated for pregnancy status at 35 to 60 d postinjection. No improvement in conception rate was detected in response to either agonist (control = 48%, fertirelin acetate = 41.5%, buserelin = 39.7%). Conception rate was unaffected by either days postpartum at injection or overall fertility of the individual herds. These observations do not support the routine use of doses of 25 to 100 micrograms fertirelin acetate or 10 micrograms buserelin at the time of first or second AI as a means to improve conception rate in lactating dairy cows.

Analysis of Variance↗
PubMed1991

The use of the LHRH-analogue Buserelin in the treatment of prostatic cancer. A 10-year review on 1522 patients treated in 119 centres on 4 continents.

In the ten years from 1979-1988, a total of 1725 patients with advanced prostatic cancer were entered into 28 studies, in which Buserelin as a nasal spray was the main androgen deprivation therapy. Patients treated with orchiectomy or other anti-androgen agents used in comparative groups, were considered unsuitable for the purpose of this study, which pools the data of the 1522 patients who received Buserelin monotherapy. Patients with stages C, D1 or D2 prostatic cancer who received Buserelin as monotherapy and had a known treatment duration were eligible for efficacy analysis. The clinical evaluation was done in 91% by NPCP-criteria and in the remainder by criteria of the EORTC or ECOG. Seventy-five per cent of the patients received Buserelin nasal spray (3x daily 400 mcg), 20% received subcutaneous injections (2x daily 200 mcg) and 4% received 2 combinations of nasal spray, subcutaneous injections and depot, or depot alone. Compliance failures were found in 4.4% and 2.4% stopped treatment due to adverse reactions. Statistical analysis includes Kaplan-Meier estimates of time-to-progression and survival. Since 1985, after 2 patients died from possible fare reactions, anti-androgens have been recommended as additional therapy for the first few weeks. Features of this analysis of great interest are the national differences in progression-free survival and overall survival.

Buserelin↗
PubMedDate not supplied

Endometriosis-associated infertility: evaluation of preoperative use of danazol, gestrinone, and buserelin.

In order to assess adequately the effectiveness of danazol, Gestrinone, and Buserelin, a prospective nonrandomized study was initiated in 126 patients with laparoscopically confirmed ovarian endometriosis. After hormonal therapy, laparotomy with microsurgical resection of endometriotic cysts was carried out. Regression (greater than 25%) of ovarian endometriosis was noted in 30%, 34%, and 73% of cases after danazol, Gestrinone, and Buserelin, respectively. The pregnancy rate in moderate endometriosis (53%) differed significantly from the rate obtained in severe endometriosis (45%). The highest percentages were found after Buserelin therapy. In conclusion, Buserelin emerged superior to danazol or Gestrinone treatment. Nevertheless, hormonal treatment leads to an incomplete suppression of ovarian endometriotic implants and this suggests the necessity of surgically removing invasive ovarian endometriosis.

Adult↗
PubMed1990

Efficacy and safety of intranasal buserelin acetate in the treatment of endometriosis: a review of six clinical trials and comparison with danazol.

The efficacy and safety of buserelin acetate in the treatment of endometriosis was studied in 4 open non-comparative trials and 2 open randomized comparative trials with danazol. 444 women were enrolled in the buserelin group and 89 in the danazol group. Treatment was for 6-10 months using 900-1200/micrograms intranasal buserelin/day and 400-800/micrograms oral danazol/day; patients were followed up for 6-8 months. Endometriotic lesions improved or disappeared in most women; pain (dysmenorrhoea, dyspareunia and pelvic pain) subsided rapidly. Most women had no, or alleviated, symptoms throughout follow-up, although ovarian function resumed promptly. Nearly a quarter of infertile women with a desire for children became pregnant. No significant differences between treatments emerged. Buserelin treatment was characterized by menopausal-like symptoms in most women, as well as by headache and nausea. Danazol treatment, which also gave rise to these effects, was accompanied by weight gain, myalgia and acne in a considerable proportion of women, as well as other anabolic and androgenic side effects. Buserelin would thus appear to be a safe and effective alternative to the standard therapy, danazol, in the treatment of endometriosis.

Administration, Intranasal↗
PubMedDate not supplied

Treatment with the gonadotropin-releasinghormone agonist buserelin to protect spermatogenesis against cytotoxic treatment in young men.

We treated 20 young men, after giving informed consent, with buserelin during their tumor treatment period. 11 of them suffered from Hodgkins disease, 2 had a non-Hodgkin lymphoma, 6 had a seminoma and 1 patient had an embryonic carcinoma of the testis. 7 of these patients received cytostatic treatment with MOPP and/or ABVD, 9 patients had a radiation treatment, 3 received both treatments. One patient remained free of further treatment. Buserelin treatment was recommended to start at least 7 days prior to the tumor treatment, the interval ranged between 7 and 43 days. It ended on the same day as the tumor treatment or some days later, but this recommendation was followed only in 12 patients. 4 patients cessated buserelin treatment before end of the tumor therapy, and 4 other dropped out of the study. Testosterone plasma levels were measured before, during and after treatment with buserelin. 7 days after starting they were increased in most patients, while they were lower after 14 days and at the end of treatment period. Semen analysis showed sperm counts of 1 to 44 millions/ml with motility rates from 9 to 81%. In only ten patients we analysed a semen sample up to 6 months after cessation of treatment. In all but one we found azoospermia. Thus this treatment at now cannot be recommended in young men undergoing cytotoxic treatment to preserve fertility.

Adolescent↗
PubMed1988

Effect of LHRH agonist (buserelin) on pulsatile secretion of LHRH and LH.

The LHRH agonist buserelin was administered intranasally to eight patients with endometriosis in doses of 300, 600 or 900 micrograms/day for six months. In all patients buserelin clearly suppressed ovulation. In the patients treated with 900 micrograms/day, estradiol levels declined to less than 30pg/ml, and LH release in response to LHRH testing decreased markedly after 2 months of treatment. A mild decrease in LH release was noted in the premarin test at the end of the treatment. At the end of buserelin treatment baseline levels of plasma LHRH, LHRH pulse amplitude and frequency were not lowered. However, baseline levels of plasma LH and LH pulse amplitude decreased. These results indicate that buserelin may act to decrease pituitary response to LHRH.

Adult↗
PubMedDate not supplied

Disposition of the 3H-labeled gonadotropin-releasing hormone analog buserelin in rats.

The short-time disposition of 3H-labeled D-Ser(TBU)6-desGly10-GnRH-ethylamide ([3H]buserelin) was studied in rats after bolus intravenous and subcutaneous injections and killing the rats after 1 and 3 hr, respectively. When estimated as the percentage of the injected dose, 3H-activity within the whole blood rapidly declined from 25.5% at 2 min to 4.7% at 60 min after intravenous injection and remained nearly constant at 3.4% from 30 to 180 min after subcutaneous injection. More than 94% of the blood activity was confined to plasma. 3H-Activity was highly concentrated in the pituitary, as seen from the concentration ratio of activity tissue/plasma (ti/pl), being 12.6 and 8.0 at 60 and 180 min, respectively. A transient accumulation of activity was observed in kidney (ti/pl 9.5 and 2.2 at 60 and 180 min, respectively). All the other tissues studied (liver, spleen, adrenal, testis, epididymis, muscle, lung, fat, skin, heart, thyroid, stomach, and intestine) showed ratios ti/pl below 2.0, mostly below 1.0. The tissues within the blood-brain barrier cortex/thalamus and hypothalamus had the lowest ti/pl (0.08 at 60 min). Within 24 hr after intravenous injection of [3H]buserelin into rats, 58% of the administered 3H-dose was recovered in urine, 21.6% of the urinary radioactivity being identified as intact buserelin. Only 3.6% of the 3H-dose were found in the feces. It is concluded that buserelin is concentrated specifically only in its target organ pituitary, whereas kidney accumulates the peptide transiently due to glomerular filtration and presence of the peptide in the primary urine, part of the peptide being degraded to smaller peptides in the kidney tubuli before being excreted into urine.(ABSTRACT TRUNCATED AT 250 WORDS)

Amino Acid Sequence↗
PubMed1994

Preparation and properties of buserelin suspensions.

Obtaining and some properties of suspensions with buserelin-there were obtained buserelin suspensions with zinc ions with pH 7.2-7.5 and hormone: zinc molar ratio from 1:2.5 to 1:500. The obtained buserelin suspensions show moderated hormone release in vitro and prolonged action in vivo. The pulsating buserelin release from suspensions has been found in vitro and in vivo.

Animals↗