Leuprolide related drug information

- Sep 30, 2017 -

Pharmacological effects

Leuprolide and goserelin, triprelin and nafarelin are drugs commonly used in the treatment of premenopausal breast cancer and prostate cancer. (GnRH-a), GnRH-a is similar to GnRH, and it competes with pituitary GnRH receptors. When the pituitary GnRH receptor is filled and depleted by GnRH-a, the pituitary will degrade, That pituitary secretion of gonadotropin to reduce, resulting in ovarian secretion of sex hormones decreased significantly, similar to surgical removal of ovaries, known as the drug to remove ovarian (medical oophorectomy).

Leuprolide is a gonadotropin releasing hormone (GnRH) analogue, which is composed of 9 amino acids. This product can effectively inhibit the function of the pituitary - gonadal system, the proteolytic enzyme resistance and the pituitary GnRH receptor affinity is stronger than GnRH, promote luteinizing hormone (LH) release activity of about 20 times the GnRH, On the pituitary - gonadal function of the inhibitory effect is stronger than GnRH. In the early stages of administration, follicle stimulating hormone (FSH), LH, estrogen or androgen may be transiently elevated. Subsequently, the secretion of FSH, LH and estrogen or androgen is inhibited due to decreased responsiveness of the pituitary gland, Sexual diseases (such as prostate cancer, endometriosis, etc.) have therapeutic effects.

At present, the clinical use of leuprolide acetate is mainly due to the performance of leuprolide acetate at room temperature more stable, but once the injection solution or use a special solvent will be sterilized powder dubbed solution should be used immediately after the remaining drugs Liquid should be discarded. Can be used for endometriosis and uterine fibroids, adolescent central precocious puberty, premenopausal breast cancer and prostate cancer drug castration therapy, but also for conventional hormone therapy contraindications or ineffective functional uterine bleeding. But also for endometrial resection before surgery, can make the inner membrane even thinning, reduce edema, reduce the difficulty of surgery.

Pharmacokinetics

Leuprolide acetate is not effective. Subcutaneous or intramuscular injection is well absorbed. Single subcutaneous injection of 3.75mg, 1 to 2 days the peak plasma concentration of 1 ~ 2ng / ml. For prostate cancer, each subcutaneous injection of 3.75mg, once every 4 weeks, a total of injection 3 times, steady state blood concentration of 0.1 ~ 1ng / ml. This product in the body hydrolysis of four kinds of degradation products, excreted by the kidneys. The urinary excretion rates of protozoa and metabolites were 2.9% and 1.5%, respectively, after a single subcutaneous injection.

Dosage form and specification

Injection with leuprolide acetate: 10mg, leuprolide acetate injection: 10mg.

Indications

Endometriosis; uterine fibroids with menorrhagia, lower abdominal pain, low back pain and anemia; premenopausal breast cancer, and estrogen receptor-positive patients; prostate cancer; central precocious puberty.


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