Positive response to compound CV 205-502 in hyperprolactinemic patients resistant to or intolerant of bromocriptine.
The clinical effects of CV 205-502, a potent and non-ergot-derived dopamine agonist, were investigated in 24 selected patients with hyperprolactinemia previously treated with standard oral bromocriptine, the slow-release oral form of bromocriptine (BRC-SRO) and/or the long-acting injectable form of bromocriptine (BRC-LAR); 14 were chosen because of their resistance to treatment and ten because they were intolerant of the different forms of bromocriptine. A macroprolactinoma was present in seven patients and a microprolactinoma in ten, whereas seven had no radiological images of a pituitary tumor and were classified as having non-tumoral hyperprolactinemia. All the 24 patients were treated with CV 205-502 at a daily dose of 0.075-0.6 mg for 3-12 months. All the patients had gonadal dysfunction and galactorrhea. Basal serum prolactin values ranged from 70 to 1677 ng/ml. CV 205-502 was effective in 11 of the 14 patients resistant bromocriptine, BRC-SRO and BRC-LAR; serum prolactin levels became normal within 6 months and a tumor shrinkage was obtained in five of the seven macroprolactinomas. In general, the drug was effective and well tolerated. Only three patients (two resistant and one intolerant) manifested nausea, vomiting and postural hypotension. In conclusion, this study shows that CV 205-502 is effective in bromocriptine-resistant hyperprolactinemic patients. Furthermore, CV 205-502 has insignificant and tolerable side-effects in patients intolerant of bromocriptine. CV 205-502 can, therefore, be considered a useful and effective drug, and an interesting therapeutic alternative to the ergot-derived dopamine-agonist drugs in use today.
Merola
B
B
Department of Endocrinology and Clinical and Molecular Oncology, Federico II University, Faculty of Medicine and Surgery, Naples, Italy.
Sarnacchiaro
F
F
Colao
A
A
Di Somma
C
C
Di Sarno
A
A
Ferone
D
D
Selleri
A
A
Landi
M L
ML
Schettini
G
G
Nappi
C
C
D000284:Administration, Oral; D000328:Adult; D000634:Aminoquinolines / Q000008:administration & dosage / Q000009:adverse effects / Q000627:therapeutic use*; D001971:Bromocriptine / Q000008:administration & dosage / Q000009:adverse effects* / Q000627:therapeutic use; D003692:Delayed-Action Preparations; D018491:Dopamine Agonists / Q000008:administration & dosage / Q000009:adverse effects / Q000627:therapeutic use*; D004351:Drug Resistance; D005260:Female; D006801:Humans; D006966:Hyperprolactinemia / Q000188:drug therapy*; D008279:Magnetic Resonance Imaging; D008297:Male; D010911:Pituitary Neoplasms / Q000097:blood / Q000000981:diagnostic imaging / Q000473:pathology; D011388:Prolactin / Q000097:blood; D015175:Prolactinoma / Q000097:blood / Q000000981:diagnostic imaging / Q000473:pathology; D013997:Time Factors; D014057:Tomography, X-Ray Computed
D000634:Aminoquinolines; D003692:Delayed-Action Preparations; D018491:Dopamine Agonists; D001971:Bromocriptine; C046650:quinagolide; D011388:Prolactin