INFLUENCE OF APPLICATION SITE OF A NEW TRANSDERMAL CLONIDINE, M-5041T, ON ITS PHARMACOKINETICS AND PHARMACODYNAMICS IN HEALTHY-SUBJECTS

Influence of application site of a new transdermal clonidine, M-5041T( M), on its pharmacokinetics and pharmacodynamics were evaluated in eig ht human subjects. One patch of M-6 mg was applied for 3 days on the r ight chest (first trial), on the left arm (second trial), and on the u pper abdomen (third trial). Blood samples for clonidine concentration were taken, and blood pressure (BP) was measured for a 120-hour postap plication period. Plasma concentrations of clonidine increased after a pplication of M in each trial. This parameter in the second trial was significantly greater than that of the first and third trials. The val ues of maximum plasma concentration and area under the plasma concentr ation-time curve in the second trial were greater than those of other trials, but the differences did not reach significance. The BP-lowerin g effect of M in the second trial was significantly greater than that of the third trial. These results suggest that the plasma concentratio ns of clonidine after application of M and its hypotensive effect are affected by the site of application in human subjects.