[Therapeutic use of gonadotropin-releasing hormone and its analogs]

The discovery of the structure of Gn-RH in 1971 has opened new ways of investigation and treatment. The anterior pituitary gland requires episodic Gn-RH stimulation in order to secrete the gonadotropins in a physiologic manner. Deficiency of Gn-RH leads in both sexes to functional disturbances which in females may produce chronic anovulation and amenorrhea. Replacement therapy with the administration of Gn-RH in a pulsatile rhythm corrects the deficiency of endogenous Gn-RH secretion and stimulates via gonadotropins the function of peripheral target organs. If given continuously, Gn-RH leads to desensitization of pituitary Gn-RH receptors and inhibition of LH and FSH secretion. Potent and long-acting agonistic Gn-RH analogs have been synthesized which are capable of producing a selective "medical castration". Indications and preliminary results of the administration of Gn-RH and its long-acting agonists in humans are reviewed.