Residues and distribution of neonicotinoid insecticides (NEOs) in soil-water-sediment systems of the urban and rural areas of Guangzhou, South China were investigated. A total of 104 soil samples from 7 different functional zones and 29 water/sediment samples from creeks were collected. The results showed that at least one neonicotinoid insecticide was detected in all samples. The summed levels of five target neonicotinoids (∑5neonics) were in the range of 0.003-229 ng/g dw for soil samples, 7.94-636 ng/L for water samples, and 0.017-31.3 ng/g dw for sediment samples, with a geometric mean of 0.59 ng/g dw, 153 ng/L and 1.11 ng/g dw, respectively. Soils from agricultural areas contained the highest residual NEOs, followed by commercial, traffic, residential, industrial, educational zones and parks. Among the seven different functional zones studied, imidacloprid was the most dominant NEO in the agricultural areas and commercial zones, whereas acetamiprid was dominant in the other five functional zones with different land-use types. Thiamethoxam and acetamiprid were the main NEOs in water and sediment samples collected from 29 creeks. The pollution of NEOs in soils, water and sediments from rural areas was higher than that in the counterparts from urban areas. Residual concentration of NEOs detected in soils, water and sediments showed significant correlations with each other. The distribution of NEOs in soil-water-sediment systems indicated that NEOs tended to concentrate in water, followed by sediments and soils, especially in urban areas. An evaluation of the exposure to the current level of the ∑5NEOs in Guangzhou suggests a significant risk for aquatic and soil organisms, particularly under chronic exposures. The results of the present study offer valuable data to better understand the contamination and ecological risks of neonicotinoid insecticides in the rapidly developing urbanized region of South China.