Shaw C A, Sellers E M, Sullivan J T, Kaplan H L
Clinical Pharmacology Program, Addiction Research Foundation, Toronto, Ontario, Canada.
J Clin Psychopharmacol. 1988 Jun;8(3):189-92.
Suriclone selectively displaces benzodiazepines from their binding sites but is structurally unrelated to benzodiazepines. Neurologic effects of suriclone were compared to those of diazepam in 54 subjects in a sequential, double-blind, single dose, randomized study (placebo; diazepam 10 mg; suriclone 0.2, 0.4, 0.6, or 0.8 mg). Data were collected on-line by microcomputer. Suriclone 0.2 mg did not differ from placebo. Suriclone 0.4 mg and 0.6 mg did not differ from diazepam 10 mg. Suriclone 0.8 mg caused significantly more decrement than diazepam 10 mg (p less than 0.05) in manual tracking, force platform stability, and Heath rail walking and in total severity of symptoms. Suriclone 0.8 mg caused nausea (p = 0.02), clumsiness (p = 0.02), and loss of balance (p = 0.01) more frequently than diazepam 10 mg. Suriclone 0.8 mg produced symptoms and signs qualitatively and quantitatively different from diazepam 10 mg, such as vomiting, unusual ocular movement effects, and difficulty walking. Possibly the differences in CNS drug binding for anxiolytics are associated with clinical differences in toxicity.
舒立克隆能选择性地将苯二氮䓬类药物从其结合位点上置换出来，但在结构上与苯二氮䓬类药物无关。在一项序贯、双盲、单剂量、随机研究中，对54名受试者比较了舒立克隆与地西泮的神经学效应（安慰剂；地西泮10毫克；舒立克隆0.2、0.4、0.6或0.8毫克）。数据通过微型计算机在线收集。0.2毫克舒立克隆与安慰剂无差异。0.4毫克和0.6毫克舒立克隆与10毫克地西泮无差异。在手动跟踪、测力平台稳定性、希思轨行走以及症状总严重程度方面，0.8毫克舒立克隆比10毫克地西泮导致的下降明显更多（p<0.05）。0.8毫克舒立克隆比10毫克地西泮更频繁地引起恶心（p = 0.02）、笨拙（p = 0.02）和平衡失调（p = 0.01）。0.8毫克舒立克隆产生的症状和体征在性质和数量上与10毫克地西泮不同，如呕吐、异常的眼球运动效应和行走困难。可能抗焦虑药在中枢神经系统的药物结合差异与毒性的临床差异有关。
