Under the background of global climate change and due to the vulnerability and sensitivity of Karst ecosystems and rapid exchange of surface water and groundwater, Karst hydrodynamic systems respond promptly to human activities and environmental change. Human activity has already become the main driving force of environmental change in Karst areas. Environmental degradation caused by the use of Karst water resources and human activities directly or indirectly influences the Karst water system. For example, biodiversity of caves have declined due to groundwater pollution. Vegetation degeneration, soil erosion, stone desertification, and other environmental problems caused by human activities have had a serious impact on the hydrological processes in the Karst region. Thus water problem has become an important limiting factor to the development of the Karst region. Based on the research of Karst ecological system and hydro-environmental characteristics, this paper focuses on summarizing works on the following water-related issues in Karst areas: hydrological effects of land use change; impacts of vegetation change caused by human activities on precipitation and runoff; hydrological effects of Karst water conservancy projects and water resource use; groundwater pollution and transmission and transformation of the main pollutants. On this basis, the paper summarizes the coupling mechanism between human activities and Karst water environment in the face of global climate change, the impact of human activities on the hydrological cycle and geological carbon cycle, as well as Karst water resource use, vulnerability assessment, and cave biodiversity, including the impact of environmental change on water cycle in Karst areas owing to short-term development, the effects of water conservancy projects, especially large-scale projects (such as cascade development) on hydrology and ecology. In recent years, concerns of global environmental change, especially global climate change promote the rapid development of the global carbon cycle research. Further study of the global carbon cycle and carbon accumulation process is dependent on a better understanding of the social-ecological-hydrological-Karst system. This system restricts material recycling and energy conversion of the carbon, water, and calcium cycles in the Karst area. Current research of such system focuses on the impact of human activities on Karst system structure and function, which ignores the variation of human adaptation in response to global climate change. Because of the fragile natural environment in Karst regions, the impact of global climate change is more significant than other areas of the same latitude, which results in more significant adaptive changes in the socioeconomic systems. The study of adaptive changes in socioeconomic systems in Karst areas and ecological processes and their environmental and hydrological effects, therefore, will further the analysis of environmental impacts of human activities from the systematic and global perspective, which has important theoretical and practical significance for further understanding of the role of human activity in global environmental change. The research of complex hydrological models and uncertainty quantification, and the study of human response to environmental changes and water cycle feedback mechanisms are the focus of future research.