The control of pests and vector-borne diseases (VDBs) are considered public health issues Worldwide. Among the control techniques and pesticides used so far, photodynamic inactivation (PDI) has been shown as an eco-friendly, low cost, and efficient approach to eliminate pests and VDBs. PDI is characterized using a photosensitizing molecule, light and molecular oxygen (O2) resulting in production of reactive oxidative species which can promote the oxidation of biomolecules on pests and vectors. Herein, we review the past 51 years (1970–2021) regarding the use of photo pesticides, reporting the most important parameters for the protocol applied, the results obtained, and limitations. Moreover, we described the mechanism of action of the PDI, main classes of photopesticides used so far as well as the cell death mechanism resulting from the photodynamic action.