Tanaka M, Isozaki H, Inanaga K, Ogawa N
Psychopharmacology (Berl). 1978 Jul 19;58(3):217-22. doi: 10.1007/BF00427382.
The effects of 7-chloro-5-(2-fluorophenyl)-1-methyl-1 H, 1.4-benzodiazepin-2(3H)-one (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 or placebo were investigated in six male Japanese students in a double-blind, crossover design. The peak latencies of PPR showed a statistically significant prolongation, with maximum level at 3 h after administration, which recovered to the initial level within 4 h. The amplitude of PPR failed to show a definite response to the drug. The serum concentration of ID-540 reached a peak level 2-3 h after administration, and then decreased at 4 h. N-Desmethyl-ID-540 exhibited a slow- gradual rise in serum. The latencies of PPR were positively correlated with the serum level of ID-540 but not with the N-desmethyl-ID-540. It is concluded that the PPR test may be a useful method for predicting the clinical effects of psychotropic drugs.
采用双盲交叉设计,对6名日本男学生口服0.5mg 7-氯-5-(2-氟苯基)-1-甲基-1H,1,4-苯并二氮杂卓-2(3H)-酮(ID-540,一种新推出的苯二氮卓衍生物)或安慰剂后,其平均光睑反射(PPR)、主观症状以及ID-540及其主要代谢物N-去甲基-ID-540的血清水平的影响进行了研究。PPR的峰值潜伏期出现了具有统计学意义的延长,给药后3小时达到最高水平,并在4小时内恢复到初始水平。PPR的幅度对该药物未表现出明确反应。ID-540的血清浓度在给药后2 - 3小时达到峰值水平,然后在4小时下降。N-去甲基-ID-540在血清中呈现缓慢逐渐上升。PPR的潜伏期与ID-540的血清水平呈正相关,但与N-去甲基-ID-540无关。结论是,PPR测试可能是预测精神药物临床效果的一种有用方法。