Kassem N, Roman I, Gural R, Dyer J G, Robillard N
Pharmaceutical Research Division, Schering-Plough Corporation, Kenilworth, New Jersey.
Ann Allergy. 1988 Jun;60(6):505-7.
The efficacy and safety of single oral doses (10, 20, 40, and 80 mg) of loratadine (SCH 29851) in suppressing formation of histamine-induced wheals were assessed in a crossover study in 29 healthy male subjects. One hour prior to dosing and 1, 2, 3, 4, 6, 8, 12, 16, 24, 28, 32, 36, 40, and 48 hours after dosing, histamine and saline were injected intradermally into opposite arms. Measurements of resulting wheal areas showed loratadine suppressed wheal formation significantly better than placebo; suppression was dose related. The mean suppression over 48 hours was 16% in placebo-treated subjects and 35%, 45%, 51%, and 67% in the 10, 20, 40, and 80 mg loratadine-treated subjects, respectively. The onset of action occurred within the first hour. Duration of suppression was dose related, ranging from 12 hours with the lowest dose (10 mg) to 48 hours with the higher doses (40 and 80 mg). Incidence of sedation and other side effects were comparable among all doses of loratadine and placebo.
在一项针对29名健康男性受试者的交叉研究中，评估了单剂量口服氯雷他定（SCH 29851）10、20、40和80毫克抑制组胺诱导风团形成的疗效和安全性。给药前1小时以及给药后1、2、3、4、6、8、12、16、24、28、32、36、40和48小时，将组胺和生理盐水皮内注射到双臂的对侧。对产生的风团面积进行测量，结果显示氯雷他定抑制风团形成的效果明显优于安慰剂；抑制作用与剂量相关。在安慰剂治疗的受试者中，48小时内的平均抑制率为16%，而在10、20、40和80毫克氯雷他定治疗的受试者中，分别为35%、45%、51%和67%。起效发生在第一小时内。抑制持续时间与剂量相关，最低剂量（10毫克）为12小时，较高剂量（40和80毫克）为48小时。在所有剂量的氯雷他定和安慰剂中，镇静及其他副作用的发生率相当。
