The antiparkinsonian actions and pharmacokinetics of transdermal (+)-4-propyl-9-hydroxynaphthoxazine (+PHNO): preliminary results.
(+)-4-Propyl-9-hydroxynaphthoxazine (+PHNO) is a potent dopamine agonist that has been administered transdermally to four patients with Parkinson's disease and "on-off" fluctuations. Skin patches of increasing size were used to treat these patients, who also received infrequent doses of oral levodopa if required. The effect of +PHNO was measured as an increased duration of action of individual levodopa doses. The clinical effect measured in this way was directly proportional to the plasma concentrations of +PHNO achieved. The plasma concentrations of +PHNO began to rise 4-6 h after patch application and reached a steady state by 24 h. The final plasma concentration of +PHNO was proportional to the area of skin covered.
Coleman
R J
RJ
Institute of Neurology, London, U.K.
Lange
K W
KW
Quinn
N P
NP
Loper
A E
AE
Bondi
J V
JV
Hichens
M
M
Stahl
S M
SM
Marsden
C D
CD
D000279:Administration, Cutaneous; D000328:Adult; D000978:Antiparkinson Agents / Q000037:antagonists & inhibitors* / Q000493:pharmacokinetics; D018492:Dopamine Antagonists; D004334:Drug Administration Schedule; D004359:Drug Therapy, Combination; D006801:Humans; D007980:Levodopa / Q000008:administration & dosage; D008875:Middle Aged; D009048:Motor Skills / Q000187:drug effects; D010078:Oxazines / Q000008:administration & dosage* / Q000493:pharmacokinetics; D010300:Parkinson Disease / Q000097:blood / Q000188:drug therapy*
D000978:Antiparkinson Agents; D018492:Dopamine Antagonists; D010078:Oxazines; C042631:naxagolide; D007980:Levodopa