Cohen A F, Hamilton M, Philipson R, Peck A W
Clin Pharmacol Ther. 1985 Oct;38(4):381-6. doi: 10.1038/clpt.1985.191.
The new H1-antagonist acrivastine (BW825C) in doses of 4, 8, and 16 mg was compared with triprolidine HCl (2.5 and 5 mg) in a double-blind crossover study in 12 subjects. Adaptive tracking performance 1.5 hours after dosing was impaired by triprolidine, 2.5 and 5 mg; the impairment was still detectable 3.5 hours after 5 mg. Acrivastine did not impair adaptive tracking after any of the doses. Triprolidine increased reaction times after 1.5 hours (2.5 and 5 mg) and 3 hours (5 mg), but acrivastine did not have any effect on reaction time at any dose. Both doses of triprolidine caused subjective central nervous system effects after 1.5 hours, and triprolidine, 5 mg, still had some detectable effects on subjective rating scales after 3 hours. No subjective effects were noted after acrivastine. We conclude that acrivastine at doses causing more peripheral H1-antagonism than triprolidine has considerably reduced central nervous system activity.
在一项针对12名受试者的双盲交叉研究中，将剂量为4毫克、8毫克和16毫克的新型H1拮抗剂阿伐斯汀（BW825C）与盐酸曲普利啶（2.5毫克和5毫克）进行了比较。服用2.5毫克和5毫克曲普利啶后1.5小时，适应性跟踪表现受到损害；服用5毫克曲普利啶后3.5小时，这种损害仍可检测到。阿伐斯汀在任何剂量下均未损害适应性跟踪。曲普利啶在1.5小时（2.5毫克和5毫克）和3小时（5毫克）后增加反应时间，但阿伐斯汀在任何剂量下对反应时间均无影响。两种剂量的曲普利啶在1.5小时后均引起主观中枢神经系统效应，服用5毫克曲普利啶3小时后，在主观评分量表上仍有一些可检测到的效应。服用阿伐斯汀后未观察到主观效应。我们得出结论，与曲普利啶相比，阿伐斯汀在引起更多外周H1拮抗作用的剂量下，其对中枢神经系统的活性有显著降低。
