antigonadotrope

Antigonadotropes, or antigonadotropic agents, are substances that suppress the secretion or action of the gonadotropins—luteinizing hormone (LH) and follicle-stimulating hormone (FSH)—from the anterior pituitary, or block the effects of gonadal steroids. By dampening the hypothalamic-pituitary-gonadal axis, these agents reduce gonadal production of sex steroids (estrogen and testosterone) and thereby decrease gonadal function.

The pharmacologic approaches fall into several categories. GnRH (gonadotropin-releasing hormone) agonists, such as leuprolide and goserelin, initially stimulate LH and FSH release but, with continuous use, desensitize GnRH receptors and suppress LH/FSH and sex steroids. GnRH antagonists, such as degarelix and cetrorelix, block GnRH receptors directly and suppress LH/FSH without an initial surge. Exogenous estrogens or progestins can also exert antigonadotropic effects through negative feedback on the hypothalamus and pituitary. In some contexts, prolactin-suppressing agents (dopamine agonists like bromocriptine or cabergoline) reduce GnRH pulse frequency, indirectly lowering gonadotropin release in hyperprolactinemic states.

Clinical uses include management of hormone-sensitive cancers (e.g., prostate cancer, certain breast cancers), treatment of endometriosis and uterine fibroids, control of precocious puberty, and facilitation of controlled ovarian stimulation in assisted reproductive technologies. They are also used in gender-affirming therapy to suppress endogenous gonadotropin production.

Common adverse effects reflect induced hypogonadism: hot flashes, decreased libido, bone density loss, vaginal atrophy in women, potential fatigue, and injection-site reactions. Long-term use requires monitoring of bone health and hormonal status.