The prevalence of infectious diseases, whether caused by bacteria, fungi, viruses, or parasites, is escalating daily, posing new and complex challenges for effective treatment. Alongside the urgent need for the development of novel antimicrobial agents, it is crucial to gain a comprehensive understanding of the pharmacokinetic characteristics of existing medications to maximize their therapeutic efficacy and minimize the incidence of drug resistance. The aim of this thesis is to investigate the metabolism of select antimicrobial drugs, with a particular focus on biotransformation reactions, a thorough review of metabolites, and their corresponding properties. This research encompasses an analysis of the pharmacokinetic characteristics of these drugs, including their absorption, distribution, metabolism, and elimination. Moreover, the study delves into specific interactions between these drugs and the enzymes involved in their metabolism, notably cytochrome P450, which can profoundly influence both the efficacy and safety of therapeutic interventions. Furthermore, the thesis considers various factors that contribute to variability in pharmacokinetics, such as genetic polymorphisms, age, sex, and the presence of comorbid conditions. Overall, this knowledge underscores the critical importance of understanding the metabolism of antimicrobial drugs in order to optimize therapy and mitigate the risks of adverse effects and the development of drug resistance.