The neurotransmitter/neuromodulator dopamine plays an important role in both the 
central nervous system and the periphery. In the hypothalamopituitary system its 
function is a dominant and tonic inhibitory regulation of pituitary hormone 
secretion including prolactin- and proopiomelanocortin-derived hormones. It is 
well known that dopamine agonists, such as bromocriptine, pergolide, 
quinagolide, cabergoline, and lisuride, can inhibit PRL secretion by binding to 
the D(2) dopamine receptors located on normal as well as tumorous pituitary 
cells. Moreover, they can effectively decrease excessive PRL secretion as well 
as the size of the tumor in patients having prolactinoma. Furthermore, dopamine 
agonists can also be used in other pituitary tumors. The major requirement for 
its use is that the tumor cells should express D(2) receptors. Therefore, in 
addition to prolactinomas, targets of dopamine agonist therapy are somatotroph 
tumors, nonfunctioning pituitary tumors, corticotroph pituitary tumors, Nelson's 
syndrome, gonadotropinomas, and thyrotropin-secreting pituitary tumors. It is 
also an option for the treatment of pituitary disease during pregnancy. 
Differences between the effectiveness and the resistance of different 
dopaminergic agents as well as the future perspectives of them in the therapy of 
pituitary tumors are discussed.