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PubMed1996

Intranasal nafarelin versus buserelin (short protocol) for controlled ovarian hyperstimulation before in vitro fertilization: a prospective clinical trial.

The aim of this study was to compare the effect of nafarelin acetate with that of buserelin acetate nasal spray, when administered in a 'short' protocol, as an adjunct to human menopausal gonadotropin (hMG) for controlled ovarian hyperstimulation before in vitro fertilization (IVF). Twenty-two IVF subjects were randomly recruited. Each underwent two consecutive treatment cycles; one with buserelin (900 micrograms/day) and another with nafarelin (400 micrograms/day). The treatment protocol included transnasal gonadotropin-releasing hormone (GnRH) analog from the second cycle day and hMG from the fourth day of the cycle. The buserelin and nafarelin cycles did not differ significantly in the following parameters: baseline hormone profile, duration of GnRH analog treatment, mean hMG dose required, peak estradiol levels, number of preovulatory follicles, number of aspirated oocytes, fertilization rate and number of transferred or frozen embryos. No side-effects or cancellations of treatment were recorded. The average dose required was lower for nafarelin and, because this analog was given only twice a day, it was more convenient to administer. These findings suggest that nafarelin is as effective as buserelin (when administered in a "short' protocol) in achieving controlled ovarian hyperstimulation. It even offers advantages over buserelin with respect to the total dose required (which probably reflects its relatively high potency) and the subjects' compliance.

Administration, Intranasal↗
PubMed1990

[Treatment of endometriosis. Evaluation of preoperative therapy with danazol, gestrinone and buserelin (nasal spray and implant)].

In order to adequately assess the effectiveness of danazol, gestrinone, buserelin-nasal spray (IN) and buserelin-implant (SC), a prospective non randomized study was initiated in 178 patients with laparoscopically confirmed ovarian endometriosis. After hormonal therapy, laparotomy with microsurgical resection of endometriotic cysts or laparoscopy laser was carried out. Regression (greater than 25%) of ovarian endometriosis was noted in 30, 34, 73 and 91% of cases after danazol, gestrinone and buserelin IN and buserelin SC respectively. Histological study proves that hormonal treatment leads to an incomplete suppression of ovarian endometriotic implants and this suggests the necessity to remove surgically invasive ovarian endometriosis. The pregnancy rate in moderate endometriosis (55%) differed significantly from the rate obtained in severe endometriosis (44%). The highest percentages were found after buserelin therapy. In conclusion, preoperative use of a potent GnRH agonist, administered subcutaneously, seems to be the best therapeutic approach when associated to surgery (CO2 laser or microsurgery).

Administration, Intranasal↗
PubMed1987

Comparison of the actions of the antiprogestin mifepristone (RU486), the progestin megestrol acetate, the LHRH analog buserelin, and ovariectomy in treatment of rat mammary tumors.

The effects of the synthetic antiprogestin mifepristone (RU486) on growth of dimethylbenzanthracene (DMBA)-induced mammary tumors in female rats were investigated. Prophylactic treatment with mifepristone (10 mg/kg/day) for 3 weeks starting from the day of first DMBA injection resulted in a doubling of the average tumor latency period (81 +/- 16 days, n = 17 treated, versus 39 +/- 5 days, n = 75 controls; P less than 0.005) and was accompanied by a significant growth retardation as shown by lower body weight increments. A 3-week therapeutic treatment of rats bearing mammary tumors was performed by administration of different dosages of mifepristone (2.5, 10, or 40 mg/kg/day) or megestrol acetate (2.5 or 10 mg/kg/day), with the luteinizing hormone-releasing hormone agonist buserelin (40 micrograms/kg/day), buserelin plus mifepristone (10 mg/kg/day), or by ovariectomy. The effects of treatment on tumor load, pituitary, adrenal and reproductive organ weights, steroid receptor contents of mammary tumors, and blood plasma hormone concentrations were investigated. Mifepristone and megestrol acetate treatment gave rise to inhibition of mammary tumor growth with all dosages studied, in which mifepristone was more potent than megestrol acetate (80%-90% vs 40% inhibition, P less than 0.01). In contrast, buserelin treatment and ovariectomy resulted not only in inhibition, but in tumor remission by about 50%. Combined treatment with buserelin and mifepristone gave the same tumor remission as resulted from ovariectomy or single treatment with buserelin. Estradiol-stimulated growth of the human mammary cancer MCF-7 cells in culture was fully abolished by mifepristone (3.6 X 10(-8) M) or tamoxifen (4 X 10(-8) M), whereas growth of MCF-7 cells under control incubation was not affected by either agent. Therefore, a direct inhibition of the growth of rat mammary tumor cells by mifepristone appears likely. Based on the effects of mifepristone on plasma hormone levels (increased: luteinizing hormone, estradiol, progesterone; unchanged: follicle-stimulating hormone, adrenocorticotropic hormone, corticosterone), organ weights (increased: pituitary, ovaries, uterus; unchanged: adrenals) and steroid receptor contents of mammary tumors (decreased: estrogen receptor and progesterone receptor contents), the main mechanism of action is probably a direct antiprogestational effect at the level of the mammary tumor cells through occupancy of the progesterone receptor.

Animals↗
PubMed1988

Efficacy of buserelin in advanced prostate cancer and comparison with historical controls.

Buserelin (B) is a synthetic nonapeptide analogue of native LHRH. Upon continued administration it reliably lowers the serum testosterone level to less than 100 ng/dl. It has been used in a clinical trial for the treatment of patients with stage C, D1, and D2 prostate cancer. Analysis of efficacy of testosterone suppression and toxicity included all 207 buserelin-treated patients. A comparison with historical controls from two National Prostate Cancer Project (NPCP) studies considered only the 147 evaluable patients with distant metastases (stage D2). All patients received buserelin, 500 micrograms q 8 hours subcutaneously (s.c.) for the first 7 days and then elected to take 200 micrograms s.c. daily or 400 micrograms q 8 hours by the intranasal (i.n.) route. Seventy-three percent elected s.c. administration. Only 2% changed the route of administration. The serum testosterone (T) level increased during week 1 in both the s.c. (426 ng/dl) and the i.n. (521 ng/dl) group but reached castrate (less than 100 mg/dl) levels by 4 weeks in 90% of patients. Subsequently, the likelihood of having a T level greater than 100 was higher for those treated by the i.n. than the s.c. route. The mean T level 4 and 12 months after therapy for the s.c. treated patients was 29 and 28. These values were 61 and 53 for those taking i.n. buserelin. This difference may in part be due to poor compliance. Toxicity was minor. Twelve percent of 151 s.c. treated patients had at least one episode of reaction at the injection site. None required discontinuation of the agent. Seventy-two percent experienced hot flushes; this was the same for both the s.c. and i.n. groups. Only 2 of 207 patients had a severe exacerbation of symptoms (spinal cord compression) during the first week of therapy. The criteria for response to therapy were those of the NPCP. There was no significant difference in the percentage of patients achieving a response when comparing the B-treated D2 patients to the NPCP D2 patients treated with DES, 3 mg daily, or orchiectomy. More of the B-treated patients entered with pain, a poor performance status, and weight loss than the DES/orchiectomy group. Nonetheless, the progression-free survival did not differ among the treatments. In summary, buserelin reliably lowers the serum T level by week 4 in 95% of men. Treatment efficacy is equivalent to a historical group treated with either DES or orchiectomy.

Buserelin↗
PubMed1995

The effects of buserelin microparticles on ovarian function in healthy women.

OBJECTIVE: To investigate the tolerance, pharmacokinetics and pharmacodynamics of the microparticle formulation of buserelin, when it was administered subcutaneously. DESIGN: A single-blind, randomised, parallel-group design was used to investigate the duration of suppression of ovarian function associated with doses of 1.8 3.6 and 7.2 mg buserelin administered subcutaneously as microparticles. SETTING: The study was carried out at the Hoechst Research Centre for Clinical Pharmacology, Department of Pharmacology, University of the Orange Free State, Bloemfontein. PATIENTS: Thirty-two health premenopausal female volunteers aged between 19 and 39 years and weighing between 52 and 85 kg completed the study. OUTCOME MEASURES: Serum progesterone and oestradiol concentrations were measured twice weekly until normal ovarian function resumed, i.e. when serum progesterone concentrations increased to at least 8 nmol/l (a sign of ovulation) and oestradiol concentrations increased to values above 300 pmol/l. Serum and urinary concentrations of buserelin were measured at the same times as those of progesterone and oestradiol. RESULTS: Doses of 1.8 3.6 and 7.2 mg elicited anovulation for mean periods of 52, 77 and 113 days and suppressed ovarian production of oestrogen for 19, 38 and 69 days. Resumption of normal ovarian function occurred when serum buserelin concentrations decreased to between 0.03 and 0.05 microgram/ml. The correlation coefficient between dose and duration of anovulation was 0.75; the correlation coefficient between dose and duration of suppression of oestrogen production was 0.76. CONCLUSION: Apart from minor side-effects such as hot flushes, vaginal spotting and acne, the compound was tolerated well. We conclude that a good relationship exists between dose and duration of suppression of ovarian function. Doses of 3.6 - 7.2 mg buserelin should suppress oestrogen production for approximately 6 - 9 weeks and ovulation for 11 - 16 weeks.

Adolescent↗
PubMed1998

Comparison of buserelin and nafarelin in IVF cycles and in subsequent frozen-thawed embryo transfer cycles.

OBJECTIVE: To compare two gonadotropin-releasing hormone agonists for down-regulation prior to superovulation in in vitro fertilization/embryo transfer treatment. METHODS: Infertility patients (n=181) were randomized to receive buserelin (1200 microg/day, n=90) or nafarelin (800 microg/day, n=91) intranasally starting in the luteal phase. Serum levels of LH, estradiol and progesterone were measured during the treatment. The cycles were compared with regard to number of oocytes, fertilization and implantation rates and achieved pregnancies. RESULTS: Serum LH was lower after two weeks on buserelin: 1.8 (1.3-2.4) IU/L (median, with lower and upper quartile in parenthesis), than after nafarelin: 2.6 (1.8-4.0) IU/L, (p=0.0001). No other differences in serum hormone levels could be detected. More oocytes were recovered in the buserelin group: 13.0 (8.0-19.0) vs 11.0 (6.8-15.0), (p=0.046), but the fertilization rate was higher in the nafarelin group (49.9%, vs 45.1%, p=0.023). Implantation rate was higher in the nafarelin group (26.28% vs 15.5%, p=0.030), but there were an equal number of deliveries in both groups (20.9% vs 15.6% per started stimulation, p=0.420). In the subsequent frozen-thawed embryo transfer cycles the implantation rate was 21.1% (nafarelin group) and 10.6% (buserelin group, p=0.067), the pregnancy rate/ET was 31.7% and 17.0% (p=0.107) and the delivery rate was 22.0% and 10.6% (p=0.148), respectively. CONCLUSIONS: Differences exist in IVF-cycles down-regulated with buserelin or nafarelin which might affect embryo quality and treatment outcome.

Adult↗
PubMed1988

Advanced male breast cancer treatment with the LH-RH analogue buserelin alone or in combination with the antiandrogen flutamide.

Ten men with advanced breast cancer were evaluated for response to treatment with the luteinizing hormone-releasing hormone (LH-RH) analogue, buserelin, alone or in combination with the antiandrogen, flutamide. One of five patients receiving buserelin as a single agent had a partial remission lasting 12 months, and with the addition of flutamide, this lasted over 24 additional months. Three patients had stable disease with a median duration of 6 months (range, two to 14). One patient had progressive disease. Of five patients receiving the combination of buserelin and flutamide from the beginning of therapy, four patients had a partial remission with a median duration of over 15 months (range, over five to 16). One patient's disease remained stable for 12 months. Major side effects were hot flushes, loss of libido, and impotence. Buserelin initiates a castration-like endocrine response and has potential in the treatment of men with disseminated breast cancer when used either alone or in combination with flutamide.

Aged↗
PubMed1986

The first clinical use of depot buserelin for advanced prostatic carcinoma.

The agonist analogues of the gonadotrophin-releasing hormone now provide an alternate medical treatment of prostatic cancer. For effect repeated administration is required, either by five or six times daily intranasal or once daily subcutaneous treatment. There is an obvious disadvantage to such regimens in elderly patients who may have difficulty complying with therapy. In order to circumvent these difficulties, sustained release formulations of the agonist analogues have been synthesized. We report the first clinical use of a long-acting formulation of D-Ser (TBU)6-LHRH Ethylamide (buserelin) using a novel polymer material. Twelve symptomatic patients with previously untreated carcinoma of the prostate were treated with depot buserelin, administered once monthly. In all patients, depot buserelin suppressed serum testosterone into the range seen in castrate men at a rate equivalent to that provided by five times daily intranasal therapy. No significant increase in serum testosterone, luteinizing hormone or follicle-stimulating hormone concentrations occurred during the period of follow-up. Long-acting formulations of buserelin offer an advance in the management of prostatic cancer with agonist analogues of the gonadotrophin-releasing hormone.

Aged↗
PubMed1991

Direct action of gonadotropin-releasing hormone (LH-RH) analogue on ovary: an alternative acting mechanism of buserelin.

The mechanisms by which gonadotropin-releasing hormone (LH-RH) analogue buserelin exerts direct action on the ovary was investigated. The analogue inhibited the luteinizing hormone (LH)-induced increase of steroidogenesis by rat ovarian granulosa cells in a dose-dependent manner. The LH-RH analogue did not alter binding capacity and affinity of 125I-LH to granulosa cells, suggesting the involvement of post-receptor mechanism. Likewise, the analogue caused inositol trisphosphate (IP3) formation as a result of stimulated inositol-phospholipid turnover. Half maximal effects of both steroidogenesis suppression and IP3 production occurred at 10 nM buserelin. These findings indicate that the inhibitory action of buserelin on granulosa cell function is mediated by IP3 (or calcium)-dependent mechanisms. Buserelin, in addition to its well-known action at pituitary level, exerts a direct inhibition of ovarian steroidogenesis at gonadal level without changes in gonadotropin receptors.

Animals↗
PubMed1987

Treatment of central precocious puberty with an intranasal analogue of GnRH (Buserelin).

One boy and 13 girls with central precocious puberty were treated for 1 year using Buserelin, a GnRH analogue, given intranasally (0.3 mg, four times a day). After 1, 3 and 12 months of therapy, the gonadotropin responses to GnRH were abolished in all the patients whereas mean basal serum concentrations of luteinizing hormone (LH) remained similar to those of pubertal controls. During Buserelin treatment, genital development in the boy and breast development in the girls showed no further progress or some regression. In the boy, serum testosterone levels returned to prepubertal values. In the girls, serum oestradiol levels were variable and, in four of them, vaginal smears showed the persistence of a slight oestrogenic effect during therapy. Pelvic ultrasonography did not show any significant variation in ovarian and uterine lengths. Among the 14 patients, 3 had some progression of pubic hair development, irrespective of serum dehydroepiandrosterone sulphate (DHEAS) levels. In eight patients previously treated with cyproterone, elevated prolactin levels were observed before and during the first month of Buserelin administration. During treatment, mean height velocity was markedly reduced from 11.6 to 6.1 cm/year and mean bone age velocity (+/- 1SD) was 0.85 +/- 0.38 year/year. After 1 year of treatment, the differences in predicted adult height ranged between -0.74 and + 1.04 SDS (standard deviation score). These differences were inversely related (r = -0.72) to the prognosis of adult height calculated before treatment. We conclude that, in central precocious puberty, intranasal administration of Buserelin 1.2 mg/day, may arrest sexual development and reduce height velocity and bone maturation. Improvement of adult height prognosis may occur, especially when it was markedly impaired before treatment.

Administration, Intranasal↗
PubMed1984

A comparison of the LH-releasing activities of LH-RH and its agonistic analogue buserelin in the ovariectomized rat.

LH-RH and the potent agonistic analogue (D-Ser(But)6-des-Gly10)-LH-RH(1-9)-ethylamide (HOE-766 or buserelin) were at several doses either infused or injected intravenously in 5-weeks-ovariectomized rats, which had been treated with either 3 micrograms estradiol-benzoate (EB) or with oil, 24 h previously. Blood samples for assay of LH were taken during the subsequent 24 h. Pituitary glands were removed at the end of the experiments. Buserelin, when infused, was slightly more effective than LH-RH on releasing LH. When injected, however, buserelin was at the higher dose ranges increasingly more effective as an LH-releasing agent than LH-RH. EB-treatment increased the LH response of the pituitary gland to both peptides in an identical way. It was concluded that buserelin derives its high potency not from its intrinsic LH-releasing activity, which is only slightly greater than that of LH-RH, but from a longer duration of action.

Animals↗
PubMed1990

Clinical predictors for buserelin acetate treatment of uterine fibroids: a prospective study of 40 women.

Buserelin acetate, a luteinizing hormone-releasing hormone agonist, is known to be effective in the shrinkage of uterine fibroids. A prospective trial was undertaken (1) to compare the efficacy of intranasal (IN) and subcutaneous (SC) administration of buserelin acetate and (2) to assess if tumor regression correlated with fibroid size and/or patient age. Forty patients were randomly allocated to receive 6 months of either IN buserelin acetate (n = 21) or SC buserelin acetate (n = 19). Four patients did not complete the study and were excluded from statistical analysis. Fibroid regression occurred in all 36 patients. Overall regression to 66% or less of the initial fibroid volume occurred in 70% of subjects. There was no significant difference in fibroid shrinkage between the two administration routes. A significant positive correlation was found between initial fibroid size and subsequent fibroid regression, with larger tumors being more likely to shrink than smaller fibroids. No correlation was found between the patient's age and the extent of fibroid regression.

Administration, Intranasal↗
PubMed1993

Buserelin acetate in the treatment of pelvic pain associated with minimal and mild endometriosis: a controlled study.

OBJECTIVE: To evaluate the changes of pain symptoms induced by buserelin acetate, a gonadotropin-releasing hormone agonist, in a group of patients with endometriosis. DESIGN: Thirty-five infertile patients with one or more of the following symptoms (dysmenorrhea, pelvic pain, deep dyspareunia, and endometriosis stage I or II) were allocated randomly to treatment with buserelin acetate 1,200 micrograms/d IN for 6 months (n = 19) or expectant management (n = 16). Pain symptoms were recorded by the women themselves using a questionnaire that included two scales for pain evaluation: one analogue and one multidimensional. The treated and untreated patients were followed for a minimum of 18 and 12 months from the time of randomization, respectively. RESULTS: Buserelin acetate markedly reduced dysmenorrhea, pelvic pain, and dyspareunia during the treatment and also for the 12 subsequent months. During follow-up of the expectant management group, dysmenorrhea resolved in 19% (3/16) of the cases, and pelvic pain did not recur after diagnostic laparoscopy in one of the three women affected nor did deep dyspareunia in two of the five who reported the symptom before laparoscopy. CONCLUSION: Buserelin acetate induced a significant improvement of pain symptoms that persisted in approximately half of the patients even after withdrawal of the drug. However, symptoms associated with endometriosis showed a spontaneous remission in approximately one fifth of the untreated patients.

Buserelin↗
PubMed1988

Effect of a luteinizing hormone-releasing hormone agonist (Buserelin) on steroidogenesis of cultured human preovulatory granulosa cells.

In order to ascertain whether there is a direct effect of luteinizing hormone-releasing hormone (LH-RH) agonists on ovarian steroidogenesis, human preovulatory granulosa cells were cultured in the presence of an LH-RH agonist (Buserelin, Hoechst Roussel Pharmaceuticals, Paris, France). Cultures were performed without serum but with precursors of estrogens and progestins. In basal conditions, Buserelin, at 1 ng/ml, increased estradiol and progesterone (P) secretion, while at concentrations of 10 and 100 ng/ml, no effect was observed. In the presence of follicle-stimulating hormone (FSH) or LH, Buserelin at 1 and 10 ng/ml did not modify the cell's steroidogenesis. However, at a concentration of 100 ng/ml, Buserelin decreased LH stimulation of P secretion. These results suggest that LH-RH agonists, at concentrations in the range of those obtained in clinical use, can modulate ovarian steroidogenesis by direct action.

17-alpha-Hydroxyprogesterone↗
PubMed1989

Ovarian suppression induced with Buserelin or danazol in the management of endometriosis: a randomized, comparative study.

The effectiveness of Buserelin (Hoechst-Roussel Pharmaceuticals, Inc., Somerville, NJ) (0.2 mg subcutaneously [SC] or 1.2 mg intranasally [IN] per day) and danazol (800 mg per day) in inducing ovarian suppression for the management of endometriosis was compared in a prospective randomized study. During 6 months of treatment, peripheral follicle-stimulating hormone (FSH), luteinizing hormone (LH), and estradiol concentrations were suppressed to a similar degree in both groups. Symptomatic improvement and laparoscopically assessed regression of endometriotic lesions also were comparable. After treatment, 8 of 18 infertile women treated with Buserelin and 5 of 8 treated with danazol conceived. General and hypoestrogenic side effects were similar in both groups, while androgenic and anabolic were more frequent with danazol. High density lipoprotein (HDL)-cholesterol increased in the Buserelin and decreased in the danazol group. The study indicates that at the dose tested, buserelin and danazol induce a similar degree of ovarian suppression resulting in a comparable clinical improvement and regression of endometriotic lesions.

Adult↗
PubMed1982

Sustained suppression of testosterone production by the luteinising-hormone releasing-hormone agonist buserelin in patients with advanced prostate carcinoma. A new therapeutic approach?

Nine patients with advanced carcinoma of the prostate were treated with the luteinising-hormone-releasing-hormone agonist buserelin (2 mg/day subcutaneously for 3 days then 0.4-1.2 mg/day intranasally for up to 24 weeks). There was a rise in luteinising-hormone levels during the first few days of treatment, but levels fell after 3 weeks and remained lower than normal after 24 weeks' treatment. In patients receiving 0.6-1.2 mg buserelin per day testosterone levels fell to less than 1 ng/ml within 3 weeks and were still as low as those found in surgically castrated men after 24 weeks. Histology showed regressive changes in some tumours after 3-6 months' buserelin treatment similar to those seen in surgically castrated men. Buserelin treatment may be an alternative to surgery in patients with advanced carcinoma of the prostate.

Administration, Intranasal↗
PubMed1988

The adjuvant effect of bacitracin on nasal absorption of gonadorelin and buserelin in rats.

Nasal absorption of gonadorelin (luteinizing hormone-releasing hormone; LH-RH) and buserelin, an LH-RH agonist, was studied in anesthetized rats. Administration of peptides was by nasal instillation of aqueous peptide/buffer solutions. Peptide absorption was monitored using different techniques: (a) by specific radioimmunoassays for serum levels of lutropin (LH), (b) by the cumulative urinary excretion of buserelin, and (c) by the ovulatory activity after nasal LH-RH and buserelin, respectively. Without adjuvant the nasal absorption of LH-RH and buserelin was relatively poor compared to subcutaneous or intravenous injection. Using absorption adjuvants of different types, e.g., sodium taurodihydrofusidate (STDHF) and bacitracin, marked increases in nasal absorption and, therefore, significant nasal adjuvant activity were found, as demonstrated by an increase in the biological response after nasal administration of the peptides. The mucosal compatibility of bacitracin at the concentrations used for enhancement of absorption was confirmed by an in vitro investigation using isolated gastric mucosa of guinea pigs as a test model.

Absorption↗
PubMed1991

[Effect of the GnRH analog buserelin on sex hormone serum level in relation to treatment onset and duration].

Changes of serum estradiol, progesterone, LH, FSH, prolactin, testosterone, androstendione, DHEA and DHEAS levels during a GnRH-analogue (buserelin) treatment have been analysed retrospectively taking account of effectiveness of treatment and its relation to the beginning and duration of treatment. 1200 micrograms/day buserelin were administered intranasally from the first day of the menstrual cycle (n = 30) or the 7th hyperthermic day of the cycle (n = 22). The results proved, that the administration of buserelin to sterile women inhibits the ovarian (estradiol, progesterone) and pituitary (LH, FSH) hormone secretion during the first 10-14 days of treatment. The adrenal hormone secretion (DHEA, DHEAS) remained unaffected, whereas the androgens of ovarian origin (testosterone, androstendione) were suppressed during the GnRH analogue treatment. The serum prolactin level increased during the first two weeks of treatment and returned to pretreatment values within the following two weeks. On the basis of the faster suppression of estradiol secretion with buserelin treatment, beginning in the middle of the luteal phase, this therapy is recommended for ovarian suppression.

Adult↗