title: Comparison among different dopamine-agonists of new formulation in the clinical management of macroprolactinomas.
abstract: BACKGROUND
  In the last decade, the treatment of macroprolactinomas has been significantly improved by the introduction in the clinical practice of new drugs with dopamine-agonist properties. In particular, the availability of different forms of bromocriptine (BRC) with long duration of action and slow absorption, suitable for injectable (BRC-LAR) or oral (BRC-SRO) administration, has allowed one to obtain a more constant bromocriptinemia than with standard BRC, thus reducing adverse reactions. Moreover, a selective action on dopamine D2 receptors has been achieved using a new non-ergot derivative: the quinagolide (CV 205-502). The aim of this study was to evaluate the effects of BRC-LAR, BRC-SRO and CV 205-502 in 34 patients with macroprolactinoma. PROTOCOL OF THE STUDY: BRC-LAR was given at the monthly dose of 50-100 mg for 6-24 months to 8 patients whose PRL levels were 150-700 micrograms/l. BRC-SRO was given at the daily dose of 5-20 mg for 1-24 months to 10 patients whose PRL levels were 120-900 micrograms/l. CV 205-502 was given at the daily dose of 0.075-0.6 mg for 6-12 months to 16 patients whose PRL levels were 250-2,050 micrograms/l. CT and/or MRI scans were performed before and during treatment to evaluate tumor shrinkage. Data are presented as Mean +/- SD.
  
  
  RESULTS
  Serum PRL levels normalized in 8/8 with BRC-LAR, 7/10 with BRC-SRO and 12/16 patients with CV 205-502. A significant shrinkage of tumor mass was obtained in 7/8 with BRC-LAR, 9/10 with BRC-SRO and 16/16 patients with CV 205-502, with consequent improvement of visual-field defects. Overall, the drugs were rather well tolerated: no patient stopped BRC-LAR or BRC-SRO and only 2 stopped CV 205-502. In particular, nausea, vomiting, headache, hypotension that disappeared spontaneously were observed in 5/8 with BRC-LAR, 4/10 with BRC-SRO and 4/16 with CV 205-502.
  
  
  CONCLUSIONS
  The medical approach with long-acting BRC preparations and CV 205-502 which selectively binds D2 receptors allows one to obtain rapid normalization of PRL levels and shrinkage of macroprolactinomas in a large series of patients. These drugs are rather well tolerated also by patients proven to be untolerant to standard BRC.
authors.affiliation: Department of Molecular and Clinical Endocrinology and Oncology, Federico II University, Naples, Italy.
authors.forename: A
authors.initials: A
authors.lastname: Colao
authors.forename: B
authors.initials: B
authors.lastname: Merola
authors.forename: F
authors.initials: F
authors.lastname: Sarnacchiaro
authors.forename: A
authors.initials: A
authors.lastname: Di Sarno
authors.forename: M L
authors.initials: ML
authors.lastname: Landi
authors.forename: P
authors.initials: P
authors.lastname: Marzullo
authors.forename: G
authors.initials: G
authors.lastname: Cerbone
authors.forename: D
authors.initials: D
authors.lastname: Ferone
authors.forename: G
authors.initials: G
authors.lastname: Lombardi
mesh_terms: D000284:Administration, Oral; D000293:Adolescent; D000328:Adult; D000634:Aminoquinolines / Q000008:administration & dosage / Q000009:adverse effects / Q000627:therapeutic use*; D001971:Bromocriptine / Q000008:administration & dosage / Q000009:adverse effects / Q000627:therapeutic use*; D018491:Dopamine Agonists / Q000008:administration & dosage / Q000009:adverse effects / Q000627:therapeutic use*; D005260:Female; D006801:Humans; D007275:Injections, Intravenous; D008279:Magnetic Resonance Imaging; D008297:Male; D008875:Middle Aged; D010911:Pituitary Neoplasms / Q000000981:diagnostic imaging / Q000188:drug therapy* / Q000473:pathology; D011388:Prolactin / Q000097:blood; D015175:Prolactinoma / Q000000981:diagnostic imaging / Q000188:drug therapy* / Q000473:pathology; D011863:Radioimmunoassay; D011933:Reagent Kits, Diagnostic; D014057:Tomography, X-Ray Computed
chemical_list: D000634:Aminoquinolines; D018491:Dopamine Agonists; D011933:Reagent Kits, Diagnostic; D001971:Bromocriptine; C046650:quinagolide; D011388:Prolactin