EFFECTS OF ID-540 ON AVERAGED PHOTOPALPEBRAL REFLEX IN MAN

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Effects of ID-540, a recently introduced benzodiazepine derivative, on the averaged photopalpebral reflex (PPR), subjective symptoms and serum levels of ID-540 and its principal metabolite, N-desmethyl-ID-540 following an oral dose of 0.5 mg were insvestigated in 4 healthy male Japanese students in their early twenties. Both the latencies of PPR, P<SUB>1</SUB> and P<SUB>2</SUB> latency, showed a prolongation and maximum level at 2-2.5 hours after administration and tended to decline thereafter to control levels. The serum concentration of ID-540 shossed a peak level at 2 hours after dosing, then showed a decline at 4 hours. The N-desmethyl-ID-540 exhibited a slow, gradual rise in the serum over the first 4 hours and there was a tendency toward a continued rise even at 24 hours. These parameters were of striking resemblance in the time-course of changes after oral dosing. Thus the PPR test nay be a useful means of determining the clinical effects of anxiolytic agents. ID-540 appears to be an agent with remarkable anxiolvtic effects.
社団法人日本薬理学会の論文