Leuprolide acts as an agonist at pituitary GnRH receptors. By interrupting the normal pulsatile stimulation and the desensitization of the GnRH receptors; it indirectly down regulates the secretion of gonadotropins luteinizing hormone (LH) and follicle-stimulating hormone (FSH) leading to hypogonadism and thus a dramatic reduction in estradiol and testosterone levels in both sexes.