Mechanism of Action

Leuprorelin is a synthetic GnRH analog that initially stimulates luteinizing hormone (LH) and follicle-stimulating hormone (FSH) release. With continuous use, it desensitizes pituitary GnRH receptors, decreasing LH and FSH, and subsequently lowering testosterone and estrogen levels.

Functions of Leuprorelin

Leuprorelin regulates LH and FSH release from the pituitary. It causes a transient increase in sex hormones followed by suppression due to receptor desensitization:

▸ Reduces testosterone in males and estrogen in females over time.

▸ Used to control hormone-sensitive conditions and reproductive processes.

Applications

▸ Prostate Cancer: Reduces testosterone to slow disease progression and manage metastatic conditions.

▸ Breast Cancer: Lowers estrogen in premenopausal women with hormone-sensitive tumors.

▸ Endometriosis: Reduces estrogen to alleviate pain and limit tissue growth.

▸ Central Precocious Puberty: Suppresses premature LH and FSH release to delay early puberty.

▸ Assisted Reproductive Techniques (ART): Controls ovulation timing to optimize fertilization and embryo implantation.

Characteristics of Leuprorelin

▸ Administration: Injectable (subcutaneous or intramuscular) with monthly, 3-monthly, or 6-monthly depot formulations.

▸ Duration of Action: Provides sustained hormone suppression over weeks or months per injection.

▸ Reversible Effect: Hormone levels return to normal after treatment cessation.

▸ Side Effects: Possible hot flashes, fatigue, mood swings, and long-term bone density reduction.

Conclusion

Leuprorelin is an essential tool in managing hormone-related conditions and reproductive medicine. Its functions, applications, and reversible nature make it versatile, with ongoing research expanding its medical uses.