Department of Clinical Pharmacology, Vienna University Hospital, Medical University of Vienna, Waehringer Guertel 18-20, 1090, Vienna, Austria.
Clin Pharmacokinet. 2020 Jul;59(7):827-847. doi: 10.1007/s40262-020-00871-5.
About one-sixth of the world's population is affected by a neglected tropical disease as defined by the World Health Organization and Center for Disease Control. Parasitic diseases comprise most of the neglected tropical disease list and they are causing enormous amounts of disability, morbidity, mortality, and healthcare costs worldwide. The burden of disease of the top five parasitic diseases has been estimated to amount to a total 23 million disability-adjusted life-years. Despite the massive health and economic impact, most drugs currently used for the treatment of parasitic diseases have been developed decades ago and insufficient novel drugs are being developed. The current review provides a compilation of the systemic and target-site pharmacokinetics of established antiparasitic drugs. Knowledge of the pharmacokinetic profile of drugs allows for the examination and possibly optimization of existing dosing schemes. Many symptoms of parasitic diseases are caused by parasites residing in different host tissues. Penetration of the antiparasitic drug into these tissues, the target site of infection, is a prerequisite for a successful treatment of the disease. Therefore, for the examination and improvement of established dosing regimens, not only the plasma but also the tissue pharmacokinetics of the drug have to be considered. For the current paper, almost 7000 scientific articles were identified and screened from which 429 were reviewed in detail and 100 were included in this paper. Systemic pharmacokinetics are available for most antiparasitic drugs but in many cases, not for all the relevant patient populations and only for single- or multiple-dose administration. Systemic pharmacokinetic data in patients with organ impairment and target-site pharmacokinetic data for relevant tissues and body fluids are mostly lacking. To improve the treatment of patients with parasitic diseases, research in these areas is urgently needed.
据世界卫生组织和疾病控制中心定义，世界上约有六分之一的人口受到被忽视的热带病的影响。寄生虫病构成了大多数被忽视的热带病清单，它们在全球范围内造成了巨大的残疾、发病率、死亡率和医疗保健成本。据估计，前五种寄生虫病的疾病负担总计达到 2300 万残疾调整生命年。尽管这些疾病对健康和经济造成了巨大的影响，但目前用于治疗寄生虫病的大多数药物都是几十年前开发的，而且开发的新型药物不足。本综述提供了已确立的抗寄生虫药物的系统和靶部位药代动力学的汇编。了解药物的药代动力学特征可以检查并可能优化现有的给药方案。寄生虫病的许多症状是由寄生虫在不同的宿主组织中引起的。抗寄生虫药物进入这些组织（感染的靶部位）是成功治疗疾病的前提。因此，为了检查和改进现有的给药方案，不仅要考虑药物的血浆药代动力学，还要考虑药物的组织药代动力学。在目前的论文中，从近 7000 篇科学文章中进行了鉴定和筛选，其中 429 篇进行了详细审查，100 篇被纳入本文。大多数抗寄生虫药物都有系统药代动力学数据，但在许多情况下，并非所有相关患者群体都有，并且仅适用于单次或多次给药。在有器官损伤的患者中，系统药代动力学数据以及相关组织和体液中的靶部位药代动力学数据大多缺乏。为了改善寄生虫病患者的治疗效果，迫切需要在这些领域开展研究。
