The therapeutic use of antihormones plays a significant and increasing role in gynecological practice. Antihormones in their true sense such as antiestrogens, antiandrogens, and antigestagens are defined as compounds competing with a given hormone at the receptor level of the target organ. Antihormones in a broader sense are compounds such as Gn-RH agonists, Gn-RH antagonists, and dopaminagonists. The mode of action of these compounds and the indication for their clinical application are outlined.