Qiu H, Jun H W, McCall J W
Department of Pharmaceutics, College of Pharmacy, University of Georgia, Athens 30602, USA.
J Am Mosq Control Assoc. 1998 Mar;14(1):12-27.
This review is intended to provide the reader with an overview of the all-purpose topical insect repellent N,N-diethyl-3-methylbenzamide (deet), with emphasis on its pharmacokinetics, formulation, and safety aspects. N,N-diethyl-3-methylbenzamide is effective against a variety of mosquitoes, flies, fleas, and ticks, and its protection efficacy depends on factors such as type of formulation, application pattern, physical activity of the user, environment, and species and feeding behavior of the insects. It offers an inexpensive and practical means of preventing the attack of biting insects and, more importantly, the transmission of vector-borne diseases. In both humans and animals, deet skin penetration and biodistribution are rapid and extensive, and metabolism and elimination appear to be complete. As evidenced by over 4 decades of human experience and rigorous animal testing, deet is generally safe for topical use if applied as recommended, although it has occasionally been related to side effects such as toxic encephalopathy, seizure, acute manic psychosis, cardiovascular toxicity, and dermatitis, along with a few cases of death due to extensive skin absorption. N,N-diethyl-3-methylbenzamide may compete in metabolism with and alter the biodistribution properties of other compounds to which a subject is simultaneously exposed, resulting in an added risk of side effects. The appropriate use of formulation techniques and new formulation excipients not only offers a way to extend the duration of protection, but also reduces deet skin penetration. In addition to extended repellency, minimal skin penetration of deet should be an important consideration in the evaluation of a deet formulation during new product development.
本综述旨在为读者提供通用型外用驱虫剂N,N-二乙基-3-甲基苯甲酰胺（避蚊胺）的概述，重点介绍其药代动力学、制剂和安全性方面。N,N-二乙基-3-甲基苯甲酰胺对多种蚊子、苍蝇、跳蚤和蜱虫有效，其防护效果取决于制剂类型、应用方式、使用者的身体活动、环境以及昆虫的种类和摄食行为等因素。它提供了一种廉价且实用的方法来防止叮咬昆虫的攻击，更重要的是，防止媒介传播疾病的传播。在人类和动物中，避蚊胺的皮肤渗透和生物分布迅速且广泛，代谢和消除似乎是完全的。超过40年的人类经验和严格的动物试验证明，如果按推荐使用，避蚊胺一般外用是安全的，尽管它偶尔会与诸如中毒性脑病、癫痫、急性躁狂性精神病、心血管毒性和皮炎等副作用有关，还有几例因广泛皮肤吸收导致死亡的病例。N,N-二乙基-3-甲基苯甲酰胺可能在代谢过程中与受试者同时接触的其他化合物竞争并改变其生物分布特性，从而增加副作用风险。适当使用制剂技术和新型制剂辅料不仅提供了延长防护时间的方法，还能减少避蚊胺的皮肤渗透。除了延长驱避性外，避蚊胺最小的皮肤渗透在新产品开发过程中评估避蚊胺制剂时应是一个重要考虑因素。
