Mattila M J, Koski J, Strömberg C
Br J Clin Pharmacol. 1987 Feb;23(2):219-27. doi: 10.1111/j.1365-2125.1987.tb03033.x.
Three doses (15, 30 and 60 mg) of Org 2305 (O 15, O 30 and O 60 respectively), a novel anxiolytic drug chemically related to mianserin, were compared with placebo and 15 mg diazepam (DZ) on human psychomotor performance in a double-blind, cross-over study with 15 healthy volunteers. Objective measurements (choice reaction, tracking, flicker fusion, Maddox wing, digit symbol substitution, memory recall) and subjective assessments (visual analogue scales) were done at baseline and 2 and 13 h after the first dose. This testing procedure was repeated on day 7 when administering the seventh consecutive daily night-time dose. After the first dose O 15 did not differ from placebo and O 30 rarely differed from placebo. O 60 impaired various objective functions similarly to, or less than DZ. Subjectively, DZ and O 60 were felt as sedative. During subchronic treatment, DZ caused some impairment of baseline due to accumulation of bioassayable benzodiazepines, but significant responses to the last DZ dose were less than those to the first dose. DZ but not O 60 was reported to have caused lethargy and clumsiness during subchronic treatment. In the doses used Org 2305 impaired psychomotor performance less than diazepam did. A dose of 60 mg Org 2305 may offer some advantage over 15 mg diazepam, provided that their anxiolytic effects are about similar.
在一项针对15名健康志愿者的双盲交叉研究中,将三种剂量(分别为15毫克、30毫克和60毫克)的Org 2305(分别为O 15、O 30和O 60),一种与米安色林化学相关的新型抗焦虑药物,与安慰剂和15毫克地西泮(DZ)在人体精神运动性能方面进行了比较。在基线以及首次给药后2小时和13小时进行了客观测量(选择反应、跟踪、闪烁融合、马多克斯翼、数字符号替换、记忆回忆)和主观评估(视觉模拟量表)。在连续第七天夜间给药的第7天重复此测试程序。首次给药后,O 15与安慰剂无差异,O 30与安慰剂很少有差异。O 60对各种客观功能的损害与DZ相似或小于DZ。主观上,DZ和O 60都被认为有镇静作用。在亚慢性治疗期间,由于生物可测定苯二氮䓬类药物的积累,DZ导致基线出现一些损害,但对最后一剂DZ的显著反应小于对第一剂的反应。据报道,在亚慢性治疗期间,DZ会导致嗜睡和笨拙,而O 60不会。在所使用的剂量下,Org 2305对精神运动性能的损害小于地西泮。如果60毫克Org 2305和15毫克地西泮的抗焦虑作用大致相似,那么60毫克Org 2305可能比15毫克地西泮具有一些优势。