Telekes A, Holland R L, Withington D A, Peck A W
Br J Clin Pharmacol. 1987 Jul;24(1):43-50. doi: 10.1111/j.1365-2125.1987.tb03134.x.
1 Twelve healthy volunteers took part in a study of the interaction between the antihistamine triprolidine and the opioid dipipanone in the cold induced pain (CP) test and tests of sedation. They received placebo, triprolidine 2.5 mg, dipipanone 8 mg or the combination of the two active treatments according to a double-blind, randomised, balanced, crossover design. 2 Antihistamine activity was demonstrated by triprolidine reducing the size of wheals and flares produced by intradermal histamine 1.6 micrograms. However, triprolidine produced no analgesia in the CP test, nor did it enhance the analgesia produced by dipipanone alone. 3 Neither treatment alone produced statistically significant sedation, assessed by visual analogue scales (VAS), side effect check list, body sway and reaction times. However, the combination did cause significant sedation. 4 Dipipanone reduced pupil size, depressed respiration, and decreased salivation. Triprolidine had no effects on pupil size and respiration, but reduced salivation slightly. It was concluded that histaminergic (H1) mechanisms are unlikely to be involved in pain produced by cold.
12名健康志愿者参与了一项关于抗组胺药曲普利啶与阿片类药物地匹哌酮在冷诱导疼痛(CP)试验及镇静测试中相互作用的研究。他们按照双盲、随机、均衡、交叉设计接受了安慰剂、2.5毫克曲普利啶、8毫克地匹哌酮或两种活性治疗药物的组合。
曲普利啶使皮内注射1.6微克组胺所产生的风团和潮红大小减小,从而证明了其抗组胺活性。然而,曲普利啶在CP试验中未产生镇痛作用,也未增强单独使用地匹哌酮所产生的镇痛效果。
单独使用这两种治疗药物,通过视觉模拟量表(VAS)、副作用检查表、身体摆动和反应时间评估,均未产生具有统计学意义的镇静作用。然而,两种药物组合确实导致了显著的镇静作用。
地匹哌酮可使瞳孔缩小、呼吸抑制并减少唾液分泌。曲普利啶对瞳孔大小和呼吸无影响,但可轻微减少唾液分泌。研究得出结论,组胺能(H1)机制不太可能参与冷诱导的疼痛。