Alexander F, Stote R M, Allison N, Familiar R G, Tatoian D, Dubb J W
J Int Med Res. 1986;14(4):200-4. doi: 10.1177/030006058601400406.
Temelastine is a selective, competitive histamine H1-receptor antagonist which does not penetrate the central nervous system. The effect of varying doses of temelastine was compared in a randomized, double-blind, controlled study by measuring the inhibition of cutaneous histamine wheals. In twelve subjects single oral doses of 50, 100 and 200 mg of temelastine produced dose-dependent reductions in wheal areas. The inhibition of wheal size was maximal by 2 hr after dosing and was present at 8 hr. At 2 hr the 50, 100, and 200 mg doses reduced the wheal size by 53, 64, and 78%, respectively. Chlorpheniramine, 4 mg, reduced wheal size by 32% at the same period. The ability of temelastine to antagonize the histamine-induced skin reaction over 20 hr was evaluated in a second randomized, double-blind study. Eight subjects participated. Temelastine, 100 mg, produced reductions of 64, 49, 56 and 51% in histamine wheal area at 8, 12, 16 and 20 hr, respectively. Plasma concentrations at these times were 4.04, 2.77, 1.88, and 1.44 mumol/l, respectively. These data suggest that blood levels as low as 1.44 mumol/l may be sufficient to produce an antihistaminic effect, and that daily or twice daily dosing with 100 mg may be adequate to control allergic symptoms.
替美斯汀是一种选择性、竞争性组胺H1受体拮抗剂，不会穿透中枢神经系统。在一项随机、双盲、对照研究中，通过测量皮肤组胺风团的抑制情况，比较了不同剂量替美斯汀的效果。在12名受试者中，单次口服50、100和200毫克替美斯汀可使风团面积产生剂量依赖性减小。给药后2小时风团大小的抑制作用最大，8小时时仍存在。在2小时时，50、100和200毫克剂量分别使风团大小减小了53%、64%和78%。4毫克氯苯那敏在同一时期使风团大小减小了32%。在第二项随机、双盲研究中，评估了替美斯汀在20小时内拮抗组胺诱导的皮肤反应的能力。8名受试者参与。100毫克替美斯汀在8、12、16和20小时时分别使组胺风团面积减小了64%、49%、56%和51%。这些时间点的血浆浓度分别为4.04、2.77、1.88和1.44微摩尔/升。这些数据表明，低至1.44微摩尔/升的血药浓度可能足以产生抗组胺作用，每日或每日两次服用100毫克可能足以控制过敏症状。
