The long-term efficacy and tolerability of CV 205-502, a non-ergot dop
amine agonist with D-2 receptor affinity, were studied for up to 36 mo
nths in 16 patients with macroprolactinomas. Prolactin values were red
uced in all cases. becoming either normalized or suppressed in 12. The
pituitary tumor size was reduced in the 1 3 patients with an obvious
tumor and visual function normalized in all six patients with initial
defects. Concomitantly we observed improvement in gonadal function, ga
lactorrhea, headache, libido and general well-being. Adverse reactions
were experienced by 15 patients during dosage increment and caused on
e patient to discontinue the medication. Seven patients had persistent
adverse effects which prohibited a dosage increase of CV 205-502. suf
ficient to normalize PRL levels in three. Two patients experienced ser
ious adverse events, causing the discontinuation of treatment in one c
ase. In eight patients treatment with CV 205 502 and bromocriptine cou
ld be compared. Three patients responded better to CV 205-502 than to
bromocriptine treatment. Only one patient preferred bromocriptine to C
V 205-502 for long-term treatment. We conclude that CV 205-502 is an e
ffective and in most cases well-tolerated treatment for patients with
macroprolactinomas. CV 205-502 is preferable to bromocriptine as an in
itial treatment and should also be tried in patients where treatment w
ith bromocriptine has failed.