We report the case of a man with an invasive macroprolactinoma who dev
eloped resistance to bromocriptine to which he had previously responde
d satisfactorily for 5 years. Subsequently, hyperprolactinemia was con
trolled equally well with 600 mu g quinagolide daily and later with 4.
5 mg cabergoline weekly. This observation suggests that a loss of dopa
mine receptors at the tumoral cell surface might be the mechanism unde
rlying acquired resistance to bromocriptine. In addition, no tumor gro
wth was observed over a 10-year follow-up, which virtually excludes a
malignant transformation of the prolactinoma. This case emphasizes the
need for close supervision of patients with macroprolactinoma, even a
fter the serum prolactin concentration has been normalized by bromocri
ptine. It furthermore illustrates the usefulness of quinagolide and ca
bergoline when resistance to bromocriptine develops after a prolonged
period of adequate response to this drug.