Background and objectives: Biopharmaceutics explores the physicochemical properties of actives alongside their excipients in that complex and projects at adjusting the delivery of drugs in a manner that gives optimal therapeutic activity for safety and efficacy. Prescribing considerations, therefore, involve careful evaluation of the potential risks and benefits to every user. This review was aimed at highlighting the various mechanisms where lifestyle practices modulate physiologic changes impinging on the pharmacokinetic and pharmacodynamics vis-a-vis biopharmaceutics of drugs as it affects the pathophysiological/biochemical events in pharmacotherapy. Materials and Methods: Publications emanating on issues in this regard from 2000 to 2023 (137 articles) were examined and reviewed by searching the literature manually from Google Scholar and other scientific databases (e.g., PubMed, Web of Science, Embase and Scopus). Words and phrases such as “physicochemical", “lifestyle" “pharmacokinetics", “biopharmaceutical implications", “pharmacodynamics of medications", “biochemical changes", “pathophysiological changes" and “dosage adjustment". Results: Every individual is a physiological and biochemical complex defined by lifestyle preferences. Lifestyle research has demonstrated significant physiological changes that may influence the prescribing style and drug disposition. Consistent lifestyle practices present a platform for a pathophysiologic framework upon which the physiochemical and pharmacological basis of drugs interface. Conclusion: Alterations in the human physiology due to lifestyle practices require concerted and progressive biopharmaceutical research efforts to reflect the pharmacokinetic disposition cum pharmacodynamic responses of different chemical entities. Lifestyle practices vary widely, so also the expected physiological changes and consequent pharmacokinetic effects cum pharmacodynamic outcomes. This will be the research direction in the future.