EFFECT OF ENTACAPONE, A PERIPHERALLY ACTING CATECHOL-O-METHYLTRANSFERASE INHIBITOR, ON THE MOTOR RESPONSE TO ACUTE TREATMENT WITH LEVODOPA IN PATIENTS WITH PARKINSONS-DISEASE
M. Merello et al., EFFECT OF ENTACAPONE, A PERIPHERALLY ACTING CATECHOL-O-METHYLTRANSFERASE INHIBITOR, ON THE MOTOR RESPONSE TO ACUTE TREATMENT WITH LEVODOPA IN PATIENTS WITH PARKINSONS-DISEASE, Journal of Neurology, Neurosurgery and Psychiatry, 57(2), 1994, pp. 186-189
Catechol-O-methyltransferase (COA IT) inhibitors may be useful in the
treatment of Parkinson's disease by improving the bioavailability of l
evodopa and by prolonging its effects. Entacapone (OR-611), a novel CO
MT inhibitor, which does not cross the blood brain barrier, was assess
ed in 12 patients with Parkinsons disease and motor fluctuations in a
randomised, double-blind, cross-over, single dose study. The magnitude
and duration of the therapeutic response to a single dose of 200 mg l
evodopa/50 mg carbidopa was evaluated after concomitant placebo, or 20
0 or 800 mg entacapone. A significant increase in the duration of the
motor response to levodopa was seen when 200 mg entacapone was given w
ith levodopa/carbidopa. Plasma levodopa concentrations were increased
with both doses of the COMT inhibitor. The latency to onset of motor r
esponse did not differ significantly between active drug and placebo.
Entacapone may prove useful in prolonging the duration of the benefit
obtained from individual doses of levodopa.