The choice of antimicrobial dosing in clinical practice in the past was based upon a 'penicillin mentality', that is, on the assumption that the in vivo antimicrobial efficacy is dependent on the duration of drug levels above the minimum inhibitory concentration of target microorganisms. Really, a rational antimicrobial therapy is strongly related to a basic understanding of the influence the patient has on the antibiotic (pharmacokinetics [PKs]) and the patient's response to the specific drug effects (pharmacodynamics [PDs]). PK/PD parameters are essential in facilitating the translation of microbiological activity into clinical situations, ensuring a successful outcome. This review will analyze the typical patterns of antimicrobial activity and the corresponding PK/PD parameters, with a special focus on a PK/PD dosing approach with the most commonly utilized antimicrobial agent classes.