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Leuprolide acetate is a synthetic, long-acting gonadotropin-releasing hormone (GnRH) agonist with high affinity for pituitary GnRH receptors. Its mechanism of action is dose- and time-dependent:
Leuprolide acetate acts as a gonadotropin-releasing hormone (GnRH) agonist. It is widely used to regulate hormone production by initially stimulating and subsequently suppressing gonadotropin secretion, which in turn lowers sex hormone levels in the body.
Upon initial administration, Leuprolide acetate causes a transient increase in circulating levels of gonadotropins (flare effect). Over time, continuous administration leads to the downregulation of pituitary GnRH receptors, resulting in a significant decrease in LH and FSH secretion.
It is commonly prescribed for hormone-responsive conditions such as advanced prostate cancer, endometriosis, uterine fibroids, and central precocious puberty.
It is administered parenterally, usually via subcutaneous or intramuscular injection. Depending on the formulation, it can be given as a daily injection or as a depot formulation designed for monthly or multi-month sustained release.
Yes, the reduction in sex hormones can lead to side effects similar to menopause or andropause, including hot flashes, sweating, fatigue, mood fluctuations, and injection site reactions.
After the initial transient hormonal surge during the first one to two weeks, hormone levels typically drop to castrate or postmenopausal levels within two to four weeks of continuous treatment.
