This review presents several clinical examples indicating that physiological changes in the body dependent and/or independent of developmental age, genetic polymorphisms, different disease states, acute and/or chronic inflammations, and physicochemical properties of drugs as well as some environmental factors, such as viral infections, may exert a significant effect on the first-time assessment of kinetic parameters of drug absorption, disposition, metabolism, and excretion after a single-dose administration in children and adults. The available pharmacokinetic data in the literature suggest that one must be cautious in interpretation and practical use of pharmacokinetic variables derived from either single-dose studies or bayesian methods, especially in a pediatric population.