title: CV 205-502 treatment of hyperprolactinemia.
abstract: CV 205-502 is a nonergot oral dopamine agonist with specific D2 activity, which has a prolonged suppressive effect on serum PRL and may have fewer side-effects than other dopamine agonists. We treated 26 hyperprolactinemic women with this compound given as a single bedtime (hs) dose for up to 12 weeks. All had gonadal dysfunction, either amenorrhea or oligomenorrhea, and 15 had galactorrhea. The initial and subsequent doses were administered in a randomized fashion; the initial dose ranged from 0.01-0.05 mg, and the dose at 12 weeks ranged from 0.03-0.09 mg. The women were evaluated every 2 weeks, and the dose was increased by 0.02 mg every 4 weeks if the serum PRL level was greater than 20 micrograms/L. Of the 26 women initially enrolled, 24 completed 12 weeks of therapy, and 2 discontinued therapy because of side-effects. Thirteen women (54%) had return of menses, and 12 (80%) had either a decrease in or disappearance of galactorrhea. Serum PRL concentrations decreased to a variable degree in all patients; 13 (54%) achieved a normal serum PRL level (less than or equal to 20 micrograms/L). The mean (+/- SE) pretreatment serum PRL concentration was 129 +/- 34, and it was 29.9 +/- 5.9 micrograms/L after 12 weeks of treatment (P = 0.005). The mean (+/- SE) percent reduction in serum PRL was 66.5 +/- 5.0% (median, 78.0%). A dose response was not demonstrated (r = -0.08; P = 0.70) among the 6 dose groups during the last 4 weeks of therapy. In 5 women, serum PRL levels, measured frequently for 24 h after treatment remained low. Side-effects after the initiation of therapy included nausea, headache, and morning fatigue in 10 women. These symptoms caused 2 women to discontinue therapy; they subsided in the other women. An optimal dose was not determined and will probably need to be determined by titration in each patient. CV 205-502, given once daily, appears to be a safe and effective alternative to other dopamine agonists in the treatment of hyperprolactinemia.
authors.affiliation: Department of Internal Medicine, University of Virginia Medical Center, Charlottesville 22908.
authors.forename: M L
authors.initials: ML
authors.lastname: Vance
authors.forename: J R
authors.initials: JR
authors.lastname: Cragun
authors.forename: C
authors.initials: C
authors.lastname: Reimnitz
authors.forename: R J
authors.initials: RJ
authors.lastname: Chang
authors.forename: E
authors.initials: E
authors.lastname: Rashef
authors.forename: R E
authors.initials: RE
authors.lastname: Blackwell
authors.forename: M M
authors.initials: MM
authors.lastname: Miller
authors.forename: M E
authors.initials: ME
authors.lastname: Molitch
mesh_terms: D000568:Amenorrhea / Q000097:blood; D000634:Aminoquinolines / Q000009:adverse effects / Q000627:therapeutic use*; D018492:Dopamine Antagonists; D004305:Dose-Response Relationship, Drug; D005260:Female; D006801:Humans; D006966:Hyperprolactinemia / Q000188:drug therapy*; D009839:Oligomenorrhea / Q000097:blood; D010053:Ovary / Q000187:drug effects / Q000502:physiology; D011388:Prolactin / Q000097:blood; D017448:Receptors, Dopamine D2
chemical_list: D000634:Aminoquinolines; D018492:Dopamine Antagonists; D017448:Receptors, Dopamine D2; C046650:quinagolide; D011388:Prolactin