Lv. Metman et al., MOTOR EFFECTS OF THE PARTIAL DOPAMINE AGONIST (-)-3-(3-HYDROXYPHENYL)-N-N-PROPYLPIPERIDINE (PRECLAMOL) IN PARKINSONS-DISEASE, Movement disorders, 9(5), 1994, pp. 577-581
The motor effects of the partial dopamine agonist (-)-3-(3-hydroxyphen
yl)-N-n-propylpiperidine [(-)-3-PPP, preclamol] were evaluated in nine
patients with Parkinson's disease using a double-blind, placebo-contr
olled design. (-)-3-PPP monotherapy had an antiparkinsonian effect in
five of nine patients at a mean dose of 37 +/- 10 mg intramuscularly.
The co-administration of(-)-3-PPP and a mildly dyskinetic dose of levo
dopa, infused intravenously at steady-state, resulted in complete supp
ression of dyskinesias and reemergence of parkinsonian signs in two of
seven patients. These dopamine antagonist effects of(-)-3-PPP occurre
d at relatively low (2.5 and 5 mg) doses. Our results suggest that par
tial dopamine agonists can exert agonist or antagonist activity in par
kinsonian patients depending on concurrent dopaminergic tone. Although
this dual action of(-)-3-PPP and other partial agonists could be ther
apeutically important on theoretical grounds, the small number of pati
ents manifesting a clinically significant response and the frequently
inconsistent effects could indicate that this class of agents may have
relatively limited clinical utility.