This study provides an overview of the theoretical discussion on potential uses for biological monitoring of exposure to chemical substances as related to human health, considering different concepts: definitions, uses, and limitations of internal dose and biological effect indicators and their availability for the substances to be quantified; knowledge of reference values, action levels, and limits based on health and negotiated patterns in biological monitoring interpretation and perspectives; and ethical and social problems in practice and within different preventive practices and their use in public health. Biological monitoring is the result of an exposure situation with conclusions based on scientific and consensus values, rules, and legislation. Biological monitoring as a continuous process and related to actually observed cases has helped establish technological exposure reference values and consensus levels as indicators for improving the environment and the workplace. As a step in the decision-making process in risk analysis, biological monitoring needs to be critically assessed as to its ethical aspects in light of the end use of results and values, which are references for application of this methodology.