Plants and plant products are directly associated with the existence of human race on earth. Plants are used in several systems of medicine in almost all countries of the world. Many of the medicinal plants have been explored and their contents have been extracted, isolated and identified using a combination of chromatographic and spectral methods. Some of the medicinal plants yield important chemical compounds with a good degree of biological activities. Such plants and chemical compounds find usage in medicine, agriculture, veterinary science, dental practice etc. The exact mechanism of action of most of phytopharmaceuticals is yet to be completely identified. Many people have reported adverse events with the usage of phytopharmaceuticals and their bioactive molecules. Phytopharmaceuticals also have a potential to cause interactions with food and drugs. In very few cases, phytopharmaceuticals may cause toxicity issues. It has been seen many a times, physicians are not aware of the phytopharmaceuticals available for management of certain diseases and disorders. It is expected more sophisticated omic technologies will be employed to sort out the issues concerning safety and efficacy of phytopharmaceuticals in therapeutic arena. It is prime time to present an overview of the issues related to the pharmacology and toxicology of phytopharmaceuticals.