University of Canberra, Canberra, Australia.
Ann Pharmacother. 2013 Sep;47(9):1161-7. doi: 10.1177/1060028013500645.
To investigate the pharmacology, pharmacokinetics, efficacy, adverse effects, and place in therapy of a single application of topical ivermectin 0.5% lotion for head lice treatment.
Literature was obtained by searching MEDLINE, PubMed, CINAHL, and Scopus (January 1980 to January 2013). Abstracts were searched for the terms ivermectin AND (head lice or pediculus or pediculosis), topical ivermectin, ivermectin lotion, ivermectin AND (pharmacology OR pharmacokinetics). The New Drug Application filed with the Food and Drug Administration and the product data sheets for ivermectin were obtained.
All English-language articles retrieved from the search were evaluated for relevance to the objective.
The recommended first-line head lice treatments in the United States are permethrin 1% or pyrethrins, with malathion 0.5% lotion used as a second-line treatment. Significantly more of the 289 head lice-infested participants using topical ivermectin 0.5% lotion were lice-free at day 15 when compared with vehicle control (73.8% vs 17.6%; P < .001) in 2 studies. Although this rate is lower than other third-line treatments (eg, spinosad 0.9% or benzyl alcohol 5%), topical ivermectin 0.5% lotion is well tolerated (pruritus, the most common adverse event, 0.9%) and requires only a single application.
Topical ivermectin 0.5% lotion kills head lice by increasing chloride in muscle cells, causing hyperpolarization and paralysis. Only 1 application is required; when the treated eggs hatch, the lice are not viable because they cannot feed as a result of pharyngeal muscle paralysis. Minimal systemic absorption occurs following topical application. Studies have demonstrated that topical ivermectin 0.5% is a safe and efficacious treatment for head lice. Although it has no documented resistance, there is limited clinical experience, it requires a prescription, and it is expensive. Therefore it should be reserved as a third-line treatment for head lice in the United States.
研究单剂量应用 0.5%伊维菌素洗剂治疗头虱的药理学、药代动力学、疗效、不良反应及治疗地位。
通过检索 MEDLINE、PubMed、CINAHL 和 Scopus（1980 年 1 月至 2013 年 1 月）获取文献。检索的术语为伊维菌素和（头虱或体虱或虱病）、局部伊维菌素、伊维菌素洗剂、伊维菌素和（药理学或药代动力学）。获取了向美国食品和药物管理局提交的新药申请和伊维菌素产品数据表。
评估检索到的所有英语文章对目标的相关性。
美国推荐的一线头虱治疗药物为 1%扑灭司林或除虫菊酯，马拉硫磷 0.5%洗剂作为二线治疗药物。在 2 项研究中，与赋形剂对照组相比，使用 0.5%伊维菌素洗剂的 289 例头虱感染参与者在第 15 天的无虱率显著更高（73.8%比 17.6%；P<0.001）。虽然这一比率低于其他三线治疗药物（如螺旋霉素 0.9%或苯甲醇 5%），但 0.5%伊维菌素洗剂局部应用耐受性良好（瘙痒，最常见的不良反应，0.9%），且只需应用 1 次。
0.5%伊维菌素洗剂通过增加肌肉细胞内的氯离子，导致超极化和麻痹来杀死头虱。只需应用 1 次；当处理过的卵孵化时，由于咽肌麻痹，虱子无法进食而无法存活。局部应用后，几乎没有全身吸收。研究表明，0.5%伊维菌素洗剂是一种安全有效的头虱治疗方法。虽然它没有记录的耐药性，但临床经验有限，需要处方，且价格昂贵。因此，在美国，它应作为头虱的三线治疗药物。
