Gonadorelin analogue | a synthetic gonadotropin-releasing hormone
Gonadorelin is a synthetic gonadotropin-releasing hormone, a decapeptide of the peptide family. It is used for the diagnosis of hypothalamic, pituitary, and gonadal dysfunction and can be based on alters in gonadotropin and sex hormone levels therein. The T1/2 initial phase after intravenous injection is 2-10 minutes and the terminal phase is 10-40 minutes. The duration of action is 3 to 5 hours, and it is quickly metabolized to inactive fragments in the plasma and excreted via urine.
Gonadotropin-releasing hormone (GnRH), also known as luteinizing hormone-releasing hormone (LHRH), is secreted in the body by the hypothalamus, which stimulates the pituitary gland It stimulates the secretion of gonadotropins, namely follicle-stimulating hormone (FSH) and luteinizing hormone (LH); LH can promote the synthesis and secretion of androgens in male testes, while the dual action of LH and FSH can promote the synthesis and secretion of estrogens in female ovaries.
When used continuously in clinical practice, GnRH exercises a biphasic impact on the pituitary gland, initially promoting the secretion of LH and FSH from the anterior pituitary gland, resulting in an increase in plasma LH, FSH, and sex hormones.
In women, it can block the synthesis and secretion of estrogen to achieve an impact comparable to ovariectomy, so it can be used for the therapy of hormone-dependent prostate cancer and breast cancer, and also for endometriosis. It is chiefly used as an ovulation promoter to treat infertility triggered by hypothalamic amenorrhea and primary ovarian insufficiency, especially for patients who are ineffective to clomiphene; it is also used for pediatric cryptorchidism and androgen excess, pituitary tumor, etc.
It is also used in pediatric cryptorchidism and androgen excess, pituitary tumor, etc. The peak blood concentration of this product is reached by 3 minutes of sedation, and the t1/2 is about 6 minutes, which is excreted after rapid metabolism by the kidney. Its impact on the increase of LH in plasma is faster and stronger, while the impact on the increase of FSH is slower and weaker.
gonadorelin analogue stimulates the synthesis and delivers of luteinizing hormone (LH) and follicle-stimulating hormone (FSH) from the anterior pituitary gland, whereby pituitary gonadotropin reserve function can be detected. In normal individuals, the increase in LH is significantly higher than that of FSH, and the response of FSH is higher than that of LH in prepubertal females; delayed response may occur after injection of gonadotropin-releasing hormone, and sometimes the response is tested after several days of intravenous injection of the product.
If the rhythm of gonadotropin-releasing hormone secretion by the hypothalamus is simulated in normal time, small doses of pulsed administration can treat delayed puberty, amenorrhea, and infertility triggered by hypothalamic pathology. If large doses are administered continuously, paradoxical effects may occur after short-term excitation of pituitary gonadotropins, which may inhibit pituitary-gonadal function. This phenomenon is more pronounced with the use of analogues with stronger and longer-lasting effects than the product.
Gonarelin is a synthetic gonadotropin-releasing hormone, a decapeptide of the peptide family. It stimulates the synthesis and delivers of sex hormones from the pituitary gland.
Gonadotropins (FSH and LH), and gonadotropins stimulate the deliver of sex hormones from the gonads. Hypothalamic secretion of gonadotropin-releasing hormone is regulated by a number of factors, including circulating sex hormones. Single doses increase circulating sex hormones; continuous use triggers downregulation of gonadotropin-releasing hormone receptors in the pituitary gland, thereby decreasing sex hormone secretion.
IV:5-20μg per minute for 90 minutes on days 2~4 of the cycle. If there is no ovulation (basal body temperature is measured), the drug can be re-administered; after ovulation, intramuscular injection of chorionic gonadotropin (HCG), 1 time 1500 units, 1 time 1500 units again in 3 days interval, more often than not pregnancy will occur after 2~4 cycles.
Nasal: For unilateral or bilateral cryptorchidism in children, the best time for therapy is between 1~2 years old, 1 time 0.2mg, 3 times a day (sprayed before breakfast, lunch, and dinner), and 4 weeks for a course of therapy. If necessary, it can be repeated after an interval of 3 months.
Subcutaneous or intravenous injection:①Diagnostic use:100μg/dose, given as early as possible in the follicular phase of the menstrual cycle in women;②Amenorrhea and infertility: given via pulse pump, each time for 5~20μg in 1 min, once every than 90min, for 6 months or until pregnancy.
There is nausea, abdominal discomfort, head testicles, excessive menstruation, vaginal dryness, facial flushing, and loss of libido. Pain at the injection site, rash, blood thrombophlebitis, swelling, and pruritus. There have been reports of allergic reactions, including bronchospasm and hypersensitivity. Others are specific to the therapy of certain diseases, such as exacerbation of the disease at the beginning of therapy for prostate cancer, with increased bone and testicular aggravation, hematuria, and increased urethral obstruction. For the reason of increased testosterone concentrations at the beginning, the anti-androgen drug cyproterone may be added for several weeks.
It is chiefly used clinically as an ovulation promoter to treat infertility due to hypothalamic amenorrhea, and primary ovarian insufficiency, especially in patients who are ineffective to clomiphene It is also used in pediatric cryptorchidism and androgen excess, pituitary tumors, etc. It is used to diagnose hypothalamic-pituitary-gonadal dysfunction, which can be based on alters in the levels of gonadotropins and sex hormones therein. therapy of amenorrhea and infertility in hypogonadism due to insufficient gonadotropin secretion and infertility in multi-follicular ovaries.
Amenorrhea associated with weight loss should be preceded by weight correction with diet. It is also used for prostate cancer (often in combination with cyproterone or fluocinolone), delayed or early puberty, and endometrial disorders.
There may be multiple pregnancies, inflammation at the injection site, and occasional temporary penile hypertrophy. Contraindicated in patients with hypersensitivity to benzyl alcohol. Patients should discontinue the drug immediately in case of pregnancy. Contraception should be used to avoid unwanted ovulation. Contraindicated in patients with adenopituitary tumors. Concomitant administration of prescriptions that affect gonadotropin secretion by the pituitary gland substances can alter the body's response to the product. Other hormonal therapies and corticosteroids can also affect the response. Spironolactone and levodopa stimulate gonadotropin secretion, whereas phenothiazines, dopamine antagonists, digoxin, and sex hormones inhibit secretion.
1. Adrenal glucocorticoids, estrogens, androgens, and progestins affect the consequences of gonadotropin-releasing hormone tests through negative feedback effects on the pituitary gland.
2. Oral contraceptives and digoxin can inhibit gonadotropin secretion and deliver.
3. Levodopa and spironolactone can increase the serum gonadotropin concentration and affect the results of the gonadotropin-releasing hormone test.
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