N-0923, A NOVEL SOLUBLE DOPAMINE D-2 AGONIST IN THE TREATMENT OF PARKINSONISM

N-0923, a novel aminotetralin dopamine D-2 agonist, was shown to effec tively reverse parkinsonian symptoms in nine dopa/agonist-responsive P arkinson's disease patients. The drug was given up to 4.5 hours by con tinuous intravenous (TV) infusion using an IV pump. The onset of anti- parkinsonian effect was seen within minutes of the initiation of the i nfusion and was absent within 90 minutes of cessation of the infusion. The short elimination half-life of N-0923 (90 min) would allow for th e rapid initiation of drug effect when necessary and at the same time permit the effect to be terminated quickly if necessary. The drug woul d be useful in situations where oral medication is not feasible or is associated with erratic absorption. The patients tolerated the drug we ll, Dose escalation load was limited by nausea and vomiting. It should be noted that the doses were increased until these symptoms occurred, but therapeutic effects were noted well before the side effects occur red. Using a modified Columbia scale, maximum improvement consisted of a 27-95% drop in score. Maximum response was obtained at infusion rat es varying from 2-16 mu g/kg per hour and at blood levels of 0.11-1.49 mu g/mL.