What Is Gonadorelin Acetate
Gonadorelin, also known as gonadorelin acetate, is a synthetic gonadotropin releasing hormone(GnRH), which belongs to peptide compounds. Easily hydrolyzed by various proteases, it can only be used for injection and can be quickly absorbed and distributed in various tissues. The bioavailability is 100%. It is physiochemically consistent with the endogenous bovine hypothalamic releasing factor. After intramuscular injection, it can exert a similar effect to pure natural hormones, increasing the secretion of specific gonadotropins LH and FSH in the anterior pituitary. Gonadorelin is mainly used in fertility medicine, used to treat amenorrhea and hypogonadism.
- Used to diagnose hypothalamic pituitary gonad dysfunction.
- Treatment of infertility caused by amenorrhea, insufficient gonadotropin secretion and multiple follicular ovaries.
- Used for contraception, cryptorchidism, malignant tumors (especially prostate cancer), delayed and early puberty.
- Used for endometriosis.
- Used to promote ovulation to treat infertility and primary ovarian insufficiency caused by hypothalamic amenorrhea, especially for patients who are ineffective to clomiphene.
- Used for pediatric cryptorchidism, androgen excess, and pituitary tumors.
Gonadotropin releasing hormone(GnRH), also known as luteinizing hormone releasing hormone(LHRH), is secreted by the hypothalamus in the body. It can stimulate the anterior pituitary gland to secrete gonadotropins, namely follicle stimulating hormone(FSH) and luteinizing hormone(LH). LH can promote the synthesis and secretion of androgens in the testicular interstitium of men, while the dual effects of LH and FSH can promote the synthesis and secretion of estrogen in the ovaries of women.
In continuous clinical use, GnRH has a biphasic effect on the pituitary. At the beginning, it can promote the secretion of LH and FSH in the anterior lobe of the pituitary, and increase the levels of LH, FSH and sex hormones in the plasma. LH is secreted, thereby blocking the synthesis and secretion of testosterone, achieving an effect equivalent to orchiectomy.
For women, it can block the synthesis and secretion of estrogen and achieve the effect of ovariectomy, so it can be used to treat hormone-dependent prostate cancer and breast cancer, and it is also suitable for endometriosis.
Clinically, it is mainly used as an ovulation-stimulating drug to treat infertility and primary ovarian insufficiency caused by hypothalamic amenorrhea, especially for patients who are ineffective to clomiphene. Also used in children with cryptorchidism, androgen excess, and pituitary tumors, etc.
- After gonadorelin acetate in injected, LH peaks appear successively, followed by FSH peaks, which are much stronger than FSH peaks.Normal reaction, 25 minutes to 45 minutes after injection, the LH value rises to more than 3 times its base value, and the FSH rises more than 2 times. Delayed response, LH does not reach its peak value until 120 minutes to 180 minutes after injection. Low weak response, the peak value of LH after injection is only twice or less than two times the base value. No response, the LH peak value remains unchanged or changes little before and after injection.
- During the follicular phase of normal menstruation, contraceptive measures should be taken.
- Patients who use this medicine shouldn’treceive drugs that directly affect the secretion of gonadotropins by the pituitary gland.
LH-RH is a peptide hormone secreted by the hypothalamus. It releases LH-RH from the hypothalamus every 90 minutes and binds to the LH-RH receptor of the pituitary to produce and release LH (luteinizing hormone) and FSH (follicle-stimulating Vegetarian). After the application of LH-RH receptor antagonist, it binds most of the receptors of the pituitary LH-RH through competition, and the production and release of LH and FSH are temporarily enhanced. However, the continuation of this stimulation will lead to increased phagocytosis and decomposition of receptors, a decrease in the number of receptors, a decrease in the response of pituitary cells, and a decrease in the secretion capacity of LH and FSH, thus inhibiting the production of ovarian estrogen. Gonadorelin acetate inhibits the function of the pituitary gland through this negative feedback effect, and has a therapeutic effect.
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