Grapevine (Vitis vinifera L.) represent an important crop, being cultivated in 2018 on 7.4 million hectares worldwide, and with a total production of 77.8 million tonnes. Grapes are susceptible to a large number of fungal pests and insects that may cause important economic losses, reduction of quality and undesired sensory characteristics in wines. A common practice in viticulture is the utilization of chemical reagents, as pesticides, that can insure constant production of high-quality grapes. The use of pesticides in vineyards is an old agricultural practice and although generally beneficial, some concerns are raising due to potential toxic compounds assimilation during wine consumption and human health risks. This chapter offers a complete overview of the most common pesticides used in vineyard and tracks them across grapes, winemaking stages and wines. The impacts of pesticide residues on phenolic compounds and volatile compounds are discussed in details, alongside with emerging technologies for removal of pesticide residues from grapes and wines.