K. Kieburtz et al., ENTACAPONE IMPROVES MOTOR FLUCTUATIONS IN LEVODOPA-TREATED PARKINSONS-DISEASE PATIENTS, Annals of neurology, 42(5), 1997, pp. 747-755
Motor fluctuations associated with levodopa therapy are common problem
s encountered in the long-term treatment of Parkinson's disease (PD).
Entacapone, a peripherally acting, reversible inhibitor of catechol-O-
methyltransferase, slows the elimination of levodopa in humans by redu
cing the formation of 3-O-methyldopa. We conducted a placebo-controlle
d, double-blind, parallel-group, multicenter trial of entacapone in PD
patients with motor fluctuations. Two hundred five patients were rand
omized to receive either entacapone 200 mg or matching placebo with ea
ch dose of levodopa and were followed for 24 weeks. The primary measur
e of efficacy was the change in percentage of ''on'' time (relief of p
arkinsonism) while awake, as recorded by subjects at home in diaries c
ompleted at 30-minute intervals. At baseline, patients averaged approx
imately 10 hours of ''on'' time per day while awake (60.5% ''on'' time
), and entacapone treatment increased the percent ''on'' time by 5.0 p
ercentage points. The effect of entacapone was more prominent in patie
nts with a smaller percent ''on'' time (<55%) at baseline, and increas
ed as the day wore on. Entacapone is effective at increasing the durat
ion of response to levodopa and at relieving parkinsonism in patients
experiencing motor fluctuations and was well tolerated during the 24 w
eeks of treatment.