Hickman J G, Huber F, Palmisano M
Education and Research Foundation Inc., 2602 Langhorne Road, VA 24501, USA.
Curr Med Res Opin. 2001;16(4):235-44. doi: 10.1185/030079901750176735.
Eflornithine HCl 13.9% cream (Vaniqa) is a novel treatment for the management of unwanted facial hair in women. This paper reports the results of four modified open-label, within-subject vehicle-controlled studies evaluating the dermal safety of this topical treatment. In a repeated insult patch test (230 subjects), erythema with oedema occurred in 38.9% of subjects treated with eflornithine HCl 13.9% cream and 4.8% of subjects treated with vehicle cream. Challenge applications at previously untested sites following the three-week induction period produced noticeable erythema or greater on only four sites treated with eflornithine HCl 13.9% cream and one vehicle-treated site. The erythema at these sites subsided substantially within 24 hours. In a three-week cumulative irritation study (30 subjects), the mean irritation score for sites treated with eflornithine HCl 13.9% cream was 1.33, compared with 0.76 at vehicle-treated sites and 3.09 at positive-control (sodium lauryl sulphate-treated) sites (p < 0.001 between all three groups). In a phototoxicity study (25 subjects), irradiated sites showed either no reaction (40% of both sites treated with eflornithine HCl 13.9% cream and vehicle-treated sites), or mild erythema subsiding in all cases but one within 24 hours. No reaction was seen at non-irradiated sites. In a photocontact allergy study (30 subjects), challenge with eflornithine HCl 13.9% cream or its vehicle alone produced either no reaction or mild erythema subsiding within 24 hours at both irradiated and non-irradiated sites. No serious adverse events were reported during the studies, and the only adverse events considered related to treatment were pruritus (three subjects) and dry skin at test site (one subject). These results demonstrate that eflornithine HCl 13.9% cream does not have contact sensitising, photocontact allergic or phototoxic properties. It can cause irritation under exaggerated conditions of use. Eflornithine HCl 13.9% cream, therefore, has a favourable dermal safety profile appropriate for a topical treatment to be applied routinely.
13.9%盐酸依氟鸟氨酸乳膏（凡立肯）是一种用于治疗女性面部多余毛发的新型药物。本文报告了四项改良的开放标签、自身对照的赋形剂对照研究结果，评估了这种局部治疗的皮肤安全性。在一项重复刺激斑贴试验（230名受试者）中，使用13.9%盐酸依氟鸟氨酸乳膏治疗的受试者中有38.9%出现红斑伴水肿，而使用赋形剂乳膏治疗的受试者中这一比例为4.8%。在为期三周的诱导期后，在先前未测试的部位进行激发应用，仅在4个使用13.9%盐酸依氟鸟氨酸乳膏治疗的部位和1个使用赋形剂治疗的部位出现了明显的红斑或更严重的反应。这些部位的红斑在24小时内基本消退。在一项为期三周的累积刺激研究（30名受试者）中，使用13.9%盐酸依氟鸟氨酸乳膏治疗部位的平均刺激评分为1.33，而使用赋形剂治疗部位的评分为0.76，阳性对照（经十二烷基硫酸钠治疗）部位的评分为3.09（三组之间p<0.001）。在一项光毒性研究（25名受试者）中，受照射部位要么无反应（使用13.9%盐酸依氟鸟氨酸乳膏治疗的部位和使用赋形剂治疗的部位均有40%），要么出现轻度红斑，除1例外在所有病例中24小时内均消退。未照射部位未见反应。在一项光接触过敏研究（30名受试者）中，使用13.9%盐酸依氟鸟氨酸乳膏或其赋形剂单独进行激发，在照射和未照射部位均未出现反应或出现24小时内消退的轻度红斑。研究期间未报告严重不良事件，唯一被认为与治疗相关的不良事件是瘙痒（3名受试者）和试验部位皮肤干燥（1名受试者）。这些结果表明，13.9%盐酸依氟鸟氨酸乳膏不具有接触致敏、光接触过敏或光毒性特性。在过度使用条件下它可能会引起刺激。因此，13.9%盐酸依氟鸟氨酸乳膏具有良好的皮肤安全性，适合作为常规应用的局部治疗药物。
