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GnRH Antagonists in the Treatment of Uterine Fibroids
Published in John C. Petrozza, Uterine Fibroids, 2020
Tejumola Adegoke, Shruthi Mahalingaiah
Felberbaum et al. [12] performed a prospective randomized phase II trial of cetrorelix for preoperative treatment in twenty premenopausal patients. Each subject received 60 mg of intramuscular cetrorelix pamoate salt on day 2 of their menstrual cycle. Patients were then randomized to a second dose of either 30 or 60 mg of cetrorelix administered on day 21 in subjects with day 21 estradiol >50 pg/mL (n = 4), or on day 28. Outcome measures included weekly serum levels of gonadotropins, estradiol, progesterone, and cetrorelix. The authors also assessed volume of the 4 largest fibroids and the uterus using weekly transvaginal ultrasound and pre- and post-treatment MRI. Sixteen patients completed the study.
Medical management of endometriosis
Published in Seema Chopra, Endometriosis, 2020
Leuprolide, goserelin, nafarelin, triptorelin, and buserelin are various GnRH analogues found to be effective in endometriosis-associated pain [44]. They are still considered the gold standard treatment in women with endometriosis [45,46]. GnRH therapy may reduce pain and delay recurrence of symptoms in women with residual endometriosis [47]. Their prolonged use is limited by various side effects associated with a hypoestrogenic state: depression, loss of libido, hot flashes, genitourinary atrophy, and altered lipid profile. The long-term consequences of the hypoestrogenic state on calcium metabolism and bone are of concern. It is recommended to monitor bone density during the GnRH therapy. The addition of add-back therapy minimizes side effects; therefore, they can be given for up to 2 years [48]. The GnRH antagonists may appear superior to agonists because of immediate suppression of LH and follicle-stimulating hormone (FSH). A subcutaneous administration of cetrorelix has shown significant improvement in clinical symptoms and staging of disease [49]. A weekly dose of 3 mg given for 8 weeks has been found to induce regression of endometriotic implants. An oral GnRH antagonist, elagolix, demonstrated acceptable response in endometriosis-associated pain in a phase 2 randomized trial [50].
Drugs used for ovarian stimulation Clomiphene citrate, aromatase inhibitors, metformin, gonadotropins, gonadotropinreleasing hormone analogs, and recombinant gonadotropins
Published in David K. Gardner, Ariel Weissman, Colin M. Howles, Zeev Shoham, Textbook of Assisted Reproductive Techniques, 2017
The introduction of GnRH antagonists into clinical use was delayed owing to the property of the first generation of antagonists to induce systemic histamine release and a subsequent general edematogenic state. Studies in rat mast cells confirmed that incorporation of D-Cit at position 6 of antagonists results in reduced histamine release (223,224). This characteristic of cetrorelix was first assessed in in vitro assays that demonstrated effective plasma concentrations to be significantly lower (<103) than the median effective dose for systemic histamine secretion, and therefore could confidently be regarded as insignificant. Owing to large disparities in such assays, cetrorelix safety was further tested in in vivo settings.
Repeated application of luteal phase oestradiol/GnRH antagonist priming increases IVF success for poor ovarian reserve patients
Published in Journal of Obstetrics and Gynaecology, 2023
Temel Ceyhan, Mustafa Ozturk, Ummu Gul Yıldız, Ulas Fidan, Elif Agacayak, Mustafa Ulubay, Cem Korkmaz
LPP group patients: 10 days after ovulation confirmation with LH peak and transvaginal ultrasonography (TV USG) in patients whose LH peak was followed on the 8th, 10th and 12th days of the cycle before starting treatment, Estrofem TB (2 mg oestradiol hemihydrate, Novo Nordisk, Istanbul, Turkey) usage of 1 in the morning and 2tb in the evening was started. One day later, Cetrotide (cetrorelix 0.25 mg Sc., Merck Serono, İstanbul, Turkey) 0.25 mg/day was applied for three days. 300 IU FSH (Gonal-F; Merck Serono, Istanbul, Turkey), 300 IU hMG (Merional; IBSA, Istanbul, Turkey) was started on the second day of the menstruation. Follicular development was followed by serial TV USG and serum E2 levels. Cetrorelix (Cetrotide; Merck Serono, Istanbul, Turkey) 0.25 mg/day subcutaneously leading follicle >12 mm or E2 >300 pg/mL human chorionic gonadotropin (hCG) was administered until the day of injection.
Current status and challenges of drug development for hormonal treatment of endometriosis: a systematic review of randomized control trials
Published in Gynecological Endocrinology, 2022
Vendy Zajec, Mislav Mikuš, Salvatore Giovanni Vitale, Maurizio Nicola D’alterio, Marija Gregov, Marko Jakov Šarić, Jose Carugno, Stefano Angioni, Mario Ćorić
An alternative pharmacological approach to GnRH receptor agonists is the use of GnRH receptor antagonists, which competitively binds to the GnRH receptor resulting in downregulation of the hypothalamic-pituitary-gonadal axis, producing a hypoestrogenic state similar to the one obtained with GnRH agonists. GnRH antagonists do not cause a transient increase in gonadotropin secretion and therefore do not cause an initial transient exacerbation of symptoms [25]. The injectable GnRH antagonist cetrorelix demonstrated optimal efficacy in the treatment of EAPP with an acceptable safety profile. Recently, oral nonpeptide forms of GnRH antagonists have become available. They can be administered orally at different doses, providing dose-dependent estrogen suppression with more tolerable side effects at lower doses [9]. We found four new GnRH antagonists that have been studied in phase 2 or phase 3 RCTs for the treatment of EAPP during the last decade.
Dual trigger with the combination of gonadotropin-releasing hormone agonist and standard dose of human chorionic gonadotropin improves in vitro fertilisation outcomes in poor ovarian responders
Published in Journal of Obstetrics and Gynaecology, 2022
Ilknur Mutlu, Erhan Demirdag, Funda Cevher, Ahmet Erdem, Mehmet Erdem
Antral follicle count (AFC) measurements were carried out on the 3rd day of the cycle. GnRH antagonist protocol was used for all poor-responder patients. The stimulation protocol in both groups included exogenous gonadotropins to a maximum of 375 units in the form of recombinant FSH (Gonal-F, Merck Serono, Turkey) in combination with hMG (Menogon, Ferring, Turkey). Follicular growth monitorization and gonadotropin dose adjustments were performed with serial transvaginal ultrasound and serum E2 measurements to determine the ovarian response to the gonadotropin stimulation. All the sonographic exams were conducted by the Voluson 730 Pro machine (GE Healthcare Austria GmbH & Co OG). 0.25 mg/day subcutaneous cetrorelix (Cetrotide; Asta Medica, Frankfurt, Germany) was started when the leading follicle ≥13 mm or E2 > 300 pg/mL and was continued until the day of ovulation trigger. When at least two follicles were 17 mm or more in mean diameter, final oocyte maturation was triggered by 250 mcg of recombinant hCG (choriogonadotropin alfa) (Ovitrelle, Merck Serono, Turkey) alone in the control (hCG trigger) group or by 250 mcg of recombinant hCG (choriogonadotropin alfa) (Ovitrelle, Merck Serono, Turkey) plus 0.2 mg of triptorelin (Decapepty, Ferring, Turkey) in the study (dual trigger) group. None of the patients were given adjuvant treatments.