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Drugs Mar 1990The gonadotrophin releasing hormone (GnRH) [luteinising hormone-releasing hormone (LHRH); gonadorelin] agonist buserelin is a promising new agent in the treatment of a... (Review)
Review
The gonadotrophin releasing hormone (GnRH) [luteinising hormone-releasing hormone (LHRH); gonadorelin] agonist buserelin is a promising new agent in the treatment of a variety of disorders in gynaecology and andrology, paediatrics and oncology. While a single dose of buserelin stimulates the release of pituitary gonadotrophins, multiple doses produce reversible pituitary desensitisation, and this specific blockade of gonadotrophin support to the gonads provides the basis for the drug's efficacy in conditions dependent on sex hormone secretion. Thus, buserelin provides comparable efficacy to orchidectomy or high dose estrogens in the treatment of hormone-sensitive prostate cancer and exhibits a lower incidence of adverse effects. During the early phase of treatment it may be particularly useful in combination with antiandrogens. Buserelin also appears promising in hormone-sensitive premenopausal breast cancer. Extensive studies have proven the value of buserelin in endometriosis, where it produces a transient remission with gradual recurrence of the disease on cessation of treatment. Surgical intervention is necessary in severe disease after buserelin-induced involution of the lesions. In patients with uterine leiomyoma, preliminary data suggest that buserelin may be beneficial in rendering surgery more conservative by reducing fibroid size, although it appears unlikely to preclude surgical intervention. The use of buserelin to induce a state of reversible hypogonadotrophism before administration of exogenous gonadotrophins is a promising strategy in the treatment of infertility associated with polycystic ovary syndrome and other conditions of infertility with underlying ovarian dysfunction; such a strategy also clearly enhances the efficiency of in vitro fertilisation programmes. Initial studies suggest its potential usefulness as a female contraceptive when administered intermittently in conjunction with a progestogen. Buserelin represents a first-line treatment of central precocious puberty. In endometriosis the adverse effect profile of buserelin is generally favourable, with hypoestrogenic effects such as hot flushes and vaginal dryness, and decreased libido, predominating. There is no apparent detrimental effect on lipid metabolism. The potential for adverse hypoestrogenic effects on bone mineral content with long term administration remains to be clarified. Thus, the GnRH agonist buserelin represents an advance in the treatment of a variety of gynaecological and andrological as well as paediatric and oncological conditions, infertility and other sex-hormone dependent conditions, with a low incidence of adverse treatment effects.
Topics: Animals; Buserelin; Humans
PubMed: 2109679
DOI: 10.2165/00003495-199039030-00007 -
Biomedicine & Pharmacotherapy =... 1989Buserelin is a synthetic gonadotropin-releasing hormone (GnRH) analog which is more potent than natural GnRH. Prolonged administration of the drug produces, after a... (Clinical Trial)
Clinical Trial Review
Buserelin is a synthetic gonadotropin-releasing hormone (GnRH) analog which is more potent than natural GnRH. Prolonged administration of the drug produces, after a short phase of stimulation, a selective and durable inhibition of secretion of pituitary gonadotropins, resulting in medical castration. In pilot and controlled studies buserelin shows a response rate that is similar to that of diethylstilbestrol or orchiectomy in the palliative treatment of advanced prostatic cancer, but larger and better designed studies are needed before reaching definitive conclusions about the duration of response and survival. The most common adverse effects of buserelin are loss of libido and/or impotence, hot flushes and possible flare-up of prostatic carcinoma symptoms in the first week of therapy. The combination of buserelin with an antiandrogen could avoid the flare syndrome; whether the combination has advantages compared to administration of buserelin alone requires confirmation from the large randomized studies still in progress.
Topics: Androgen Antagonists; Antineoplastic Combined Chemotherapy Protocols; Buserelin; Clinical Trials as Topic; Humans; Male; Pilot Projects; Prostatic Neoplasms
PubMed: 2506941
DOI: 10.1016/0753-3322(89)90009-7 -
Deutsche Medizinische Wochenschrift... Apr 1994
Topics: Buserelin; Humans
PubMed: 8156885
DOI: 10.1055/s-0029-1235042 -
Gynecological Endocrinology : the... Mar 1992Buserelin, a luteinizing hormone releasing hormone agonist was administered nasally in doses of 900 micrograms daily to inhibit the ovarian cycle. Of 16 patients... (Clinical Trial)
Clinical Trial
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.
Topics: Administration, Intranasal; Adult; Buserelin; Double-Blind Method; Female; Humans; Premenstrual Syndrome; Severity of Illness Index
PubMed: 1580169
DOI: 10.3109/09513599209081007 -
Progress in Clinical and Biological... 1990The 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... (Clinical Trial)
Clinical Trial Comparative Study Randomized Controlled Trial Review
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.
Topics: Administration, Intranasal; Buserelin; Climacteric; Clinical Trials as Topic; Danazol; Endometriosis; Estradiol; Female; Humans; Infertility, Female; Ovulation; Pregnadienes; Pregnancy; Randomized Controlled Trials as Topic; Safety
PubMed: 2106146
DOI: No ID Found -
Domestic Animal Endocrinology Oct 2021This research aimed to examine for the first time the impact of single dose administration of gonadotropin-releasing hormone (GnRH) analog buserelin acetate on the...
This research aimed to examine for the first time the impact of single dose administration of gonadotropin-releasing hormone (GnRH) analog buserelin acetate on the testicular blood flow measurements (peak systolic velocity [PSV], end-diastolic systolic velocity [EDV], resistive index [RI], and pulsatility index [PI]) and the plasma steroids (testosterone and estradiol-17β) concentrations in rams. For this purpose, twelve adult Ossimi rams were randomly assigned into the buserelin group (n = 8) and were injected intravenously (iv) with buserelin acetate (0.008 mg/ram), whereas the remaining rams (n = 4) were injected with normal saline iv and served as a control group. Blood sampling and testicular pulsed-wave Doppler scanning were conducted immediately before (0) and 1, 3, 6, 24, 48, 72, 120, and 168 h after treatment. The control group did not reveal any substantial changes (P > 0.05) in the examined parameters, except for the EDV (P < 0.05). In the buserelin-treated group, a marked reduction in RI and PI values (P < 0.05) occurred 1 to 3 h after administration of buserelin. Besides, there was a significant increase in testosterone plasma concentrations following buserelin treatment. In conclusion, the administration of buserelin triggered a series of substantial changes in the testicular blood perfusion and steroidogenesis that could have a positive effect on testicular function in rams.
Topics: Animals; Buserelin; Estradiol; Male; Sheep; Sheep, Domestic; Testis; Testosterone
PubMed: 34175682
DOI: 10.1016/j.domaniend.2021.106646 -
Zhonghua Yi Xue Za Zhi = Chinese... Jan 1991Twenty five patients with endometriosis of varying degree had been treated with Buserelin (GnRH analogue) for 6 months. Among them, 83.4% reached castrated level by...
Twenty five patients with endometriosis of varying degree had been treated with Buserelin (GnRH analogue) for 6 months. Among them, 83.4% reached castrated level by measuring the serum estradiol (E2) 2 months after therapy. Dysmenorrhea was alleviated or completely disappeared during therapy. Hot flush was the one mostly complained. Vaginal dryness was the second and decreased libido the third. Persisted periodic bleeding was noted in 3 patients. Ovulation was suppressed as evidenced by low serum progesterone throughout the whole course of treatment. Second-look laparoscopy was done at the end of 6-month therapy. Scoring assigned by the American Fertility Society (AFS) was reduced by 27.5%. The adrenal gland, liver and renal functions as well serum calcium and phosphate were retained at the end of treatment. Ovulation and menstruation also returned to normal within 2 months after cessation of therapy. There were 4 pregnancies during the 6-month follow period (4/15 = 26.6% pregnancy rate). 7 patients had improved symptoms whereas 7 patients sustained recurrent dysmenorrhea. The hormonal profile showed that dysmenorrhea improved group had better ovarian suppression than the dysmenorrhea recurrent group.
Topics: Adult; Buserelin; Endometriosis; Estradiol; Female; Follow-Up Studies; Humans; Laparoscopy
PubMed: 1848456
DOI: No ID Found -
Animal Reproduction Science Oct 2020The aim of this study was to evaluate induced reproduction in tambaqui females using buserelin acetate as compared with the traditional treatment regimen with carp...
The aim of this study was to evaluate induced reproduction in tambaqui females using buserelin acetate as compared with the traditional treatment regimen with carp pituitary extract (CPE). Reproductive traits of females with a body weight (BW) of 8.47 ± 1.52 kg were evaluated in ten females treated with buserelin acetate at the dose of 0.5 mL/kg BW, in a single application, and in ten females treated with CPE at the dose of 5.5 mg/kg BW, in two applications (10 % and 90 %, with a 12-h interval between applications). Spawning rate did not differ between the females treated with buserelin acetate (40 %) and CPE (40 %). Weight, fertilization rate and hatching rate did not differ between the two treatment groups. Degree-hours (determined as the average temperature multiplied by time, in hours, for spawning after the treatment with the second dose of CPE and after the single treatment with buserelin acetate) for spawning and number of oocytes per gram of gametes collected were greater (P < 0.05) in the females treated with buserelin acetate than in the females treated with CPE. Production index, absolute fecundity and relative fecundity were greater (P < 0.05) in the females treated with CPE. The hormone buserelin acetate promotes reproduction in tambaqui females with there being a similar spawning rate and oocyte quality, however, lesser production indices and fecundity than when there is the conventional treatment regimen imposed with carp pituitary extract.
Topics: Animals; Buserelin; Characiformes; Female; Fertility Agents, Female; Reproduction
PubMed: 32931986
DOI: 10.1016/j.anireprosci.2020.106594 -
Ugeskrift For Laeger Sep 1986
Topics: Buserelin; Humans; Male; Prostatic Neoplasms
PubMed: 3095970
DOI: No ID Found -
Journal of the Medical Association of... May 2001To examine the treatment of pain in endometriosis by buserelin acetate implants.
OBJECTIVE
To examine the treatment of pain in endometriosis by buserelin acetate implants.
DESIGN
Fourteen patients with laparoscopically confirmed pelvic endometriosis were included in the study. All presented with severe dysmenorrhea with or without deep dyspareunia and pelvic pain. Buserelin acetate 6.6 mg. Implants were injected subcutaneously in the lateral region of the anterior abdominal wall, 3 doses every 8 weeks in group 1 (n=7) and 2 doses every 12 weeks in group 2 (n=7). Bone mineral density (BMD) was measured at the lumbar spine by dual energy X-ray absorptiometry (DEXA) before initiation of treatment and 1 year after. Symptoms, pelvic examination, ultrasonogram and serum estradiol were recorded every 4 weeks until two regular menses were established.
RESULTS
All the painful symptoms were relieved and eventually disappeared in every patient within 4-6 weeks. Mean duration of amenorrhea in group 1 (408.4+/-47.7 days) was significantly longer than group 2 (331.3+/-22.4 days), p < 0.01. Mean duration of first observed side effects was 2.7+/-1.6 weeks. Hot flushes were the most common side effects. Serum estradiol levels were below 15 pg/ml in all patients and there were no significant differences between the two groups during amenorrhea. There was significant bone loss in both groups, 6.49+/-4.90 per cent in group 1 and 7.71+/-5.67 per cent in group 2. However, there were no significant differences between the two groups for lumbar BMD before and after treatment.
CONCLUSION
Buserelin acetate implants are effective in the treatment of pain in endometriosis. These implants should have an important clinical application when chronic treatment is indicated. Further study is needed to design how this preparation should be used to minimize the adverse effects.
Topics: Absorptiometry, Photon; Adult; Bone Density; Buserelin; Drug Implants; Endometriosis; Female; Humans; Pain; Treatment Outcome
PubMed: 11560214
DOI: No ID Found