Although pesticides have increased crop production and controlled disease, they have produced a number of adverse health effects. Pesticides have potential human toxicity and a variety of groups, such as farmers or industrial workers, as well as the general population, are exposed to pesticides. The purpose of this article, therefore, is to provide an overview of pesticide exposure and health through a literature review, focusing on exposure assessment, acute poisoning, chronic health effects, and future research needs. The exposure types and levels of pesticides vary by study subjects and need to be assessed by integrating several methods focused on the epidemiological purpose. Acute pesticide poisoning is a major public health problem in the world. Paraquat is the main causative pesticide for acute poisoning in Korea and should be banned in order to save several thousands of lives every year. Occupational pesticide exposure also causes numerous chronic diseases among farmers and industrial workers, including cancers, respiratory diseases, depression, retinal degeneration, diabetes, and abnormal menstrual cycle. However, controversy exists regarding the long-term effects of low-dose environmental pesticide exposure. The area of pesticide study is relatively new with broad study populations and it has received little academic and policy attention, particularly in Korea. More detailed studies investigating the risk of pesticide-related health effects and intervention efforts to reduce the problems are needed in Korea.