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PubMed1996

[Effects of gonadotropin-releasing hormone and its analogue (buserelin) on aromatase in cultured human granulosa cells].

We studied the direct effects of gonadotropin-releasing hormone (GnRH) and its analogue (buserelin) on aromatase activity and the aromatase cytochrome P-450 (P-450arom) concentration in cultured human granulosa cells which were obtained during oocyte retrieval for in vitro fertilization. Aromatase activity was assessed by radioassay with [1beta-3H]androstenedione as the substrate. The P-450arom concentration was determined by an enzyme-linked immunosorbent assay with specific antibodies to P-450arom. Buserelin stimulated aromatase activity and P-450arom at low concentrations (10(-13) - 10(-9)M), but it suppressed these parameters at high concentrations (10(-8) - 10(-7)M). The stimulatory effect increased with time during 12- to 48-h culture and disappeared after 72-h culture. Follicle-stimulating hormone (FSH) (100 ng/ml) stimulated aromatase activity and the P-450arom concentration but, FSH stimulation was suppressed by co-administration of low or high concentrations of buserelin. In contrast GnRH suppressed aromatase activity and P-450arom at all concentrations (10(-12) - 10(-6)M). GnRH also suppressed FSH stimulation of aromatase. Aromatase activity was correlated with the P-450arom concentration. These results suggest that in human preovulatory granulosa cells, buserelin and GnRH modulate aromatase activity by changing the P-450arom concentration.

Aromatase↗
PubMed1988

A comparison of diethylstilbestrol or orchiectomy with buserelin and with methotrexate plus diethylstilbestrol or orchiectomy in newly diagnosed patients with clinical stage D2 cancer of the prostate.

From April 1983 to March 1985, 265 patients with newly diagnosed metastatic prostate cancer were randomized to one of three treatment protocols: (1) diethylstilbestrol (DES) or bilateral orchiectomy, (2) the leutinizing hormone-releasing hormone (LHRH) analog buserelin, or (3) methotrexate plus DES or orchiectomy. In 261 evaluable patients there was no significant difference in survival between the three groups. However, progression-free survival (PFS) was significantly different (P less than 0.0005, log-rank test). Of the possible pairwise comparisons for PFS, two showed significance; buserelin was inferior to DES/orchiectomy (P less than 0.05) and buserelin was inferior to methotrexate plus DES/orchiectomy (P less than 0.0001).

Antineoplastic Combined Chemotherapy Protocols↗
PubMed1993

Combined treatment with buserelin and cyproterone acetate in metastatic male breast cancer.

BACKGROUND: Male breast cancer (MBC) is considered an androgen-dependent tumor, and as in prostatic cancer, responses have been reported with use of antiandrogens or gonadotropin-releasing hormone analogs. Thus, it is reasonable to postulate that better results could be achieved by combining these two agents. METHODS: Eleven men with recurrent or progressive carcinoma of the breast have been treated with buserelin 1500 micrograms subcutaneously daily in the first week and 600 micrograms daily subsequently and cyproterone acetate (CPA) 100 mg twice a day orally starting 24 hours before the first dose of buserelin. RESULTS: Objective responses have been observed in seven patients with a median duration of 11.5 months (range, 9-24+ months). Responses were not correlated to the dominant site of disease. Three patients had stable disease lasting 5 months. Median survival was 18.5 months. Side effects primarily were decrease or loss of libido, impotence, and hot flushes. CONCLUSIONS: Total androgen blockade with buserelin and CPA seems effective in the treatment of patients with advanced cancer of the male breast, but its superiority over standard androgen suppression remains to be demonstrated.

Aged↗
PubMed1987

Treatment of cryptorchidism with low doses of buserelin over a 6-months period.

In a collaborative study, 48 prepubertal boys with undescended testes ranging in age from 15 months to 11 years were treated with low-dose intranasal buserelin following an every-other-day programme for a period of 6 months. Urinary LH, FSH, and testosterone were not altered during the treatment period. Boys over 7 years of age experienced a slight but significant rise in testosterone at the end of treatment. Testicular descent was achieved in only 17% of boys. In the remainder, bilateral testicular biopsies were obtained during orchiopexy. Grouped analysis showed a significant increase in the number of germ cells per tubule in both unilateral and bilateral cryptorchid boys, suggesting that buserelin treatment of the testis in a cryptorchid position is capable of improving fertility potential. If time-matched controls are compared to treated boys of the same age, again a significant difference is observed indicating that buserelin treatment does increase the germ cell count.

Administration, Intranasal↗
PubMed1989

LH-RH agonist (buserelin): treatment of endometriosis. Clinical, laparoscopic, endocrine and metabolic evaluation.

To investigate the effects of the LH-RH agonist Buserelin [D-Ser (But)6 des-Gly10-LHRH ethylamide] on endometriosis, 64 patients were treated with 900 micrograms/d Buserelin intranasally over 6 months after histological verification of the disease. As shown by the follow-up operation at the end of treatment, 73% of cases showed regression of implants, whereas adhesions seemed to be unaffected. The uncorrected pregnancy rate of the 45 patients with a history of infertility was 40%, while the overall recurrence rate--confirmed by histological examination--was 9.4%. The endocrine parameters demonstrated a highly significant suppression of estradiol (E2) and a sharp decline of progesterone (Prog), indicating anovulatory cycles. Follicle-stimulating hormone (FSH) was unchanged, while luteinizing hormone (LH) and prolactin (Prl) decreased significantly. The androgenic parameters testosterone (T), dehydroepiandrosterone sulfate (DHEA-S), and sex-hormone-binding globulin (SHBG) revealed no relevant changes. Influence on bone metabolism could not be detected by measuring calcitonin and parathyroid hormone fragments (PTH-C and PTH-MM). Negative metabolic effects were absent in terms of hematology, clotting system, liver enzymes, renal parameters and lipid metabolism. Remarkable was a significant increase of high-density-lipoprotein cholesterol (HDL). Subjective complaints were mostly attributed to the therapy-induced hypoestrogenism. We consider Buserelin to be an effective drug in the treatment of endometriosis, with a low incidence of relevant side effects.

Buserelin↗
PubMed1989

Buserelin treatment of advanced prostatic cancer: a phase II study.

From August 1986 to September 1988, 76 eligible patients with advanced prostatic carcinoma, measurable or evaluable disease, no previous hormonal treatment, were treated with Buserelin at a dosage of 500 micrograms every 8 h for 7 days, followed by 400 micrograms intranasally three times a day. No concomitant antiandrogens were administered. In the 63 evaluable patients (11 patients not yet evaluable because of short treatment time, two lost to follow-up), three complete remissions, 28 partial remissions, 30 stable disease and two progressions were obtained (National Prostatic Cancer Project criteria). Median duration of response was 55+ weeks. Side effects were modest, mostly related to the endocrinological effects of Buserelin. Transient increase in serum testosterone levels was found in 37% of the evaluable patients, but transitory 'flare-up' was present in seven patients only. With a median follow-up time of 11.5 months, median survival has not been reached. In conclusion, this study confirmed the activity of Buserelin and the feasibility of its middle-term administration.

Aged↗
PubMed1986

Combined effects of buserelin, estradiol and tamoxifen on the growth of MCF-7 human breast cancer cells in vitro.

The growth-stimulation of MCF-7 human breast cancer cells in vitro induced by 30 pM estradiol was inhibited both by the LHRH-agonist Buserelin and the anti-estrogen Tamoxifen used as single agents. Combined administration of both drugs was less effective in this respect. In the presence of estradiol Buserelin had no effect on the pattern of [35S]methionine labelled secretory proteins when examined with one-dimensional gel electrophoresis, whereas the estrogen-induced progesterone receptor synthesis was inhibited. Thus with estradiol concentrations comparable to plasma values in medically castrated patients, the LHRH-agonist Buserelin can directly inhibit breast cancer cell growth in vitro.

Breast Neoplasms↗
PubMed1994

Influence of the ovary on parameters of LH secretion during the recovery from buserelin-induced desensitization.

This study examined the effect of the ovary on LH pulsatility and on the secretory performance of gonadotrophs during the phase of recovery after treatment with buserelin, a GnRH analogue. We included 12 patients, who received buserelin (1.2 mg/day, intranasally for 3 months) as a reductive therapy for uterine leiomyomatosis prior to hysterectomy. Six patients were oophorectomized and the other 6 patients had their ovaries preserved. LH was measured in samples taken basally up to 36 days after suppression of buserelin. LH pulsatility was studied on day 9 along a 24-h cycle, and the response of the hormone to a double-stimulus GnRH test on days 0, 9, 20, and 34. The concentration of LH reached normal premenopausal levels after an average of 2 weeks in women with ovaries but increased until 4-5 weeks in oophorectomized patients. The pulsatility of LH on day 9 was similar for both groups, but parameters related to LH amplitude or to baseline secretory activity of gonadotrophs were higher in the oophorectomized women. The response of LH to the GnRH tests was also significantly higher in the oophorectomized group from day 9. The conclusions are as follows. (1) At the early stage of recovery from desensitization, as represented by day 9, LH pulsatility was not substantially influenced by the presence or absence of the ovary. (2) There was an increase in parameters related to the amplitude of the LH bursts in the oophorectomized women. Although a higher amplitude of the endogenous GnRH pulses cannot be discarded, most probably that difference is due to a higher sensitivity at a pituitary level, as reflected by the GnRH stimulation tests.

Administration, Intranasal↗
PubMed1991

Changes in thromboxane A2 generation and plasma lipid pattern in pseudomenopause induced by gonadotropin releasing hormone (GnRH) analogue buserelin.

An increased risk of cardiovascular disease has been found in postmenopausal women in comparison to premenopausal women. The aim of this study was to investigate platelet function, blood clotting and plasma lipid levels in 12 women with a condition of hypoestrogenism, similar to the postmenopausal status induced by treatment with the GnRH analogue buserelin for uterine leiomyoma. Platelet aggregation in whole blood and platelet-rich plasma (PRP), serum thromboxane (TX) B2 production, fibrinopeptide A (FPA) plasma levels and plasma lipid pattern were measured before and after 13 weeks of buserelin treatment. No changes of platelet aggregability were found either in whole blood or PRP. Serum TXB2 generation increased significantly after 13 weeks of therapy (p less than 0.001). No signs of increased thrombin generation were found, as indicated by unchanged FPA plasma levels. Total cholesterol plasma levels were found increased after 13 weeks, LDL cholesterol levels showed a tendency to increase although not significantly. HDL cholesterol and triglyceride concentrations were unaffected. The changes of arachidonic acid metabolism and lipid pattern suggest that buserelin treatment may induce a condition of increased thrombotic risk even if the lack of enhanced thrombin generation and increased platelet aggregability indicates that no blood clotting activation occurs.

Adult↗
PubMedDate not supplied

Effects of treatment with buserelin on plasma concentrations of oestradiol and progesterone and cycle length in the cow.

Treatment of cows with 10 micrograms of the gonadotrophin releasing hormone (GnRH) analogue, Buserelin (Receptal; Hoechst) 12 days after mating results in a 12% improvement in conception rate (Drew & Peters, 1991). We have now investigated the endocrine effects and possible mechanism of action underlying this effect. Treatment of cyclic cows (n = 5) with Buserelin on days 11 and 13 did not affect cycle length or plasma concentration of progesterone, but did significantly (P < 0.05) reduce plasma oestradiol concentration from day 12-16. We conclude that the Buserelin treatment acts by causing a fall in plasma oestradiol which results in a reduction in the strength of the luteolytic drive, improving the chance of an embryo being able to prevent luteal regression.

Animals↗
PubMed1997

Effects of oral buserelin on urinary LH secretion in male infants.

In recent years, several potent gonadotropin-releasing hormone (GnRH) analogues have become available for female contraception and one of them (buserelin) has been tested in lactating women. However, the possible effects on infants due to the transference of the analogue through breast milk have not been studied. The present work evaluated the effect of oral buserelin on urinary LH secretion in male infants. A total of 19 healthy full-term boys (aged 2-4 months) were included in the study. Infants received orally a single dose of a GnRH agonist mixed with breast milk. Urine samples were collected prior to, and 4-6 and 24 h after treatment for LH measurement. The results disclosed a significant increase in LH urine level in the sample taken 4-6 h after buserelin administration. Twenty-four hours after GnRH agonist ingestion, the LH level returned to baseline level. The present study demonstrated that GnRH analogue administered orally to infants escapes from gastrointestinal inactivation and induces a significant rise in LH levels 4-6 h after treatment.

Breast Feeding↗
PubMed1991

A controlled study of gonadotropin-releasing hormone agonist (buserelin acetate) for folliculogenesis in routine in vitro fertilization patients.

STUDY OBJECTIVE: To determine if gonadotropin-releasing hormone agonist (GnRH-a) and gonadotropin therapy could improve folliculogenesis and pregnancy rates (PRs) in women with a previously satisfactory response to clomiphene citrate and human menopausal gonadotropin (hMG). DESIGN: Randomized prospective study. SETTING: Assisted reproduction clinic. PATIENTS: One hundred fifty-seven women were randomized to receive either hMG alone or the GnRH-a buserelin acetate 600 microgram/d or buserelin acetate 1,200 microgram/d plus hMG. RESULTS: Compared with hMG alone, pretreatment with buserelin acetate significantly increased the PR per cycle started by preventing a premature luteinizing hormone rise and thereby reducing the number of abandoned cycles. There was, however, no difference between the number of follicles aspirated, oocytes obtained, or fertilization rates between groups. Furthermore, agonist therapy significantly increased both the dose of hMG required and the duration of stimulation. CONCLUSION: The routine use of GnRH-a in in vitro fertilization programs must be questioned.

Buserelin↗
PubMed2002

Peroral delivery systems based on superporous hydrogel polymers: release characteristics for the peptide drugs buserelin, octreotide and insulin.

Novel peroral peptide drug delivery systems based on superporous hydrogel (SPH) and SPH composite (SPHC) have recently been developed in our laboratory. In this report the following issues were studied: release of the peptide drugs buserelin, octreotide and insulin from SPH and SPHC polymers and the developed delivery systems, stability of these peptides during the release and the integrity of insulin in the polymeric matrix of SPHC. Release studies from SPH and SPHC polymers revealed that buserelin, octreotide and insulin were released almost completely from the polymers. Peptide release rates from SPH were faster than from SPHC, due to the more porous structure of SPH polymer. All peptides studied in contact with SPHC polymer were stable under different environmental conditions (ambient temperature, 37 degrees C, light and darkness and at pH values 3.2 and 7.2). FTIR studies demonstrated that no covalent binding occurred between insulin and the polymeric SPHC matrix. Release profiles of all peptides from the developed delivery systems showed a time-controlled release profile: after a short lag time of 10-15 min, a burst release of peptides occurred during which more than 80% of peptide was released within 30-45 min. In conclusion, the present delivery systems based on SPH and SPHC show appropriate in vitro properties for application in peroral peptide drug delivery of buserelin, octreotide and insulin, and are therefore promising for further in vivo evaluation.

Buserelin↗
PubMed1996

In vivo buccal delivery of the peptide drug buserelin with glycodeoxycholate as an absorption enhancer in pigs.

PURPOSE: To study the potential of buccal delivery of the peptide drug in pigs. METHODS: Intravenous administration and buccal delivery without and with 10 mM sodium glycodeoxycholate (GDC) as absorption enhancer were investigated as a randomised cross-over study in six pigs. The buccal delivery device consisted of an application chamber with a solution of buserelin and was attached to the buccal mucosa for 4 hours using an adhesive patch. RESULTS: Buccal administration of buserelin resulted in rapidly reached steady state plasma levels. The absolute bioavailability of the peptide after buccal delivery for 4 hours could be increased from 1.0 +/- 0.3 to 5.3 +/- 1.1% (mean +/- SD.) by co-administration of 10 mM GDC (0.45% w/v)). CONCLUSIONS: The results of this study demonstrate that buccal administration with the use of absorption enhancers is a useful approach for the delivery of peptide drugs such as buserelin.

Administration, Oral↗
PubMed1991

[Androgens and other hormones in buserelin therapy].

23 women of reproductive age were treated with Buserelin nose-spray for endometriosis, which had been diagnosed by laparoscopic and bioptic methods. The treatment period was 6 months. Various hormones in serum were determined after 2, 4, 8, 12, 16, 20 and 24 weeks during treatment. LH, E2, prolactin, progesterone, and testosterone concentrations were significantly decreased under Buserelin therapy, whereas there was only a slight decrease in FSH, free testosterone and androstendion. No changes were observed in the concentrations of DHEAS and SHEBG. Buserelin had no androgenic effect. There was a significant decrease of endometriosis as judged by the implantation score.

Administration, Intranasal↗
PubMed2000

Dynamic assays of inhibin B and oestradiol following buserelin acetate administration as predictors of ovarian response in IVF.

The study was designed to examine whether dynamic measurements of inhibin B and oestradiol following single administration of buserelin acetate were correlated with the ovarian response to stimulation in IVF. A total of 37 patients undergoing IVF treatment was studied when the long protocol was started in the early follicular phase. Blood samples were taken twice: on day 2 of the menstrual cycle, before the first s.c. administration of buserelin acetate 0.5 mg and on day 3, 24 h later. Inhibin B and oestradiol concentrations were compared with the ovarian response to stimulation. The ovarian response was defined in two ways: 'number of oocytes/total recombinant (r) follicle stimulating hormone (FSH) dose'; and 'square-root (number of follicles/total rFSH dose)'. The following measurements were highly correlated with the ovarian response to stimulation: increase in oestradiol (day 3-day 2 oestradiol concentration) [correlation coefficient (r) = 0.68, P: < 0.0001] and sum of inhibin B (day 2 + day 3 inhibin B concentrations) (r = 0.6, P: < 0.0001). Age and basal concentrations of FSH and inhibin B were inferior to the above measurements in terms of correlation with the ovarian response. In conclusion, dynamic measurements of inhibin B and oestradiol following single administration of buserelin acetate were highly correlated with the ovarian response to stimulation for IVF treatment.

Adult↗
PubMed1991

Long term follow-up of patients with advanced prostatic cancer treated with nasal buserelin.

Sixty one men, with advanced prostatic cancer, were entered on a trial using a nasally administered gonadotropin-releasing hormone analogue agonist, buserelin, as first line treatment. This is the first trial to use intranasal buserelin without primary injections and without antiandrogens. No 'flare' phenomenon was observed. The only side effects were hot flashes (69%) and decreased libido (25%). The response rate of 82%, with a median response duration of 16 months, compares favourably to responses reported with orchidectomy or estrogens. Serum testosterone, FSH and LH were monitored at regular intervals. Mean serum testosterone baseline values of 15 nmol/L decreased to castrate levels, and remained low while patients were on study. It is concluded that intranasal buserelin is an effective, simple and safe method to achieve androgen deprivation and is an alternative to orchidectomy in the treatment of advanced prostatic cancer.

Administration, Intranasal↗
PubMed1992

Cyclophosphamide, doxorubicin and fluorouracil (CAF) plus depo-buserelin in the treatment of premenopausal women with metastatic breast cancer.

A phase II study was undertaken to assess the effect of CAF plus depo-buserelin, as first-line treatment, in premenopausal women with breast cancer. Of 66 patients entered 60 are eligible and evaluable; their median age was 45, estrogen receptor (ER) was positive in 9, negative in 11 and unknown in 40. The median disease free interval (DFI) was 11 months. Metastatic sites were visceral in 14, bone in 34 and soft tissue in 37. Twenty-nine patients had metastatic disease of one site, while 31 had 2-4 sites. An objective response of 82% was documented (29 complete responders and 20 partial responders). Median time to treatment failure was 11.5 months and median survival 37 months. Most commonly encountered side effects attributable to CAF were alopecia, nausea and vomiting, leucopenia and thrombocytopenia. Side effects attributable to buserelin were hot flashes. After one cycle baseline mean serum estradiol fell from premenopausal levels to postmenopausal levels. This study showed that CAF plus buserelin is well tolerated, with a very high response rate in selected premenopausal patients with advanced breast cancer.

Adult↗