Insect pests are found commonly in two critical areas of human life: the farms and crop storage facilities and the home, where they cause a number of problems, including the destruction of various forms of materials such as clothes and cellulose-based items by ants, as well as nuisances and disease-transmitting activities perpetrated by mosquitoes, flies, cockroaches, and bugs. For ages, man has tried to fight the menace of insects using traditional and scientific methods, including the use of chemicals. In this work, the historical aspect of the use of insecticides for pest control, the challenge of the development of insect resistance, the potential for and incidences of environmental and health hazards, adverse effects on climate change, and the search for new agents, particularly from natural products of plant origin, are discussed. The challenges and the strategic advantages of the use of various classes of insecticides are also presented. The need for the application of lessons learned from human pharmaceutical science, the deployment of emerging technologies in the search for new insecticidal moieties and biopesticides, and the development of new and more efficient insecticide application tools and technologies are also discussed.