Background: Salmonella enterica serovar typhimurium is the most important serotype of Salmonella transmitted from animals to humans in most parts of the world. They are associated with an estimated 1 million deaths annually. Quinolones, an important class of broad-spectrum antimicrobials, have been utilized as a treatment option for salmonellosis for over 40 years. Despite the number of available quinolone agents, many of them failed in the clinical stage and never make it to FDA approval. Despite considerable evidence reveals the importance of different drug discovery process of S. typhimurium, there are no systematic review outlining the pharmacokinetic and pharmacodynamic parameters of quinolones. Keeping this in mind, the present study aims to provide a systematic review on metabolism and pharmacokinetics of different quinolones. Methods: Information from all relevant bibliographic databases was used. Additionally, the recent journal articles and textbooks were searched manually in the preparation of this review article. Results: A total of 136 journal articles and textbooks were included in the preparation of the review. Majority of research articles defines about the metabolism, pharmacodymanics and pharmacokinetics of different quinolones. Twenty eight papers outlined about the mechanism and challenges faced by the quinolones and fluoroquinolones. Finally, information on drug interactions, adverse effects and drug resistance of quinolones and fluoroquinolones were supported with forty two research articles. Note that the importance of computational biology in the field of drug discovery was also addressed with appropriate literatures. Conclusion: Overall, the findings of this review highlight the importance of pharmacokinetic profiling of different quinolones in developing novel drugs to overcome drug resistance in the near future. © 2017 Bentham Science Publishers.