The pediatric age group includes a varied population, which does not express a linear change in body composition and function when progressing from birth into adolescence. Thus, there is an urgent need for lucidity in pediatric pharmacology. It is interesting to note that in infants and toddlers, orally administered drugs have varied absorption kinetics; while the gastric pH and emptying hinder the absorption, the immature intestinal mucosa hastens the process. Furthermore, it is observed that for children to attain complete adult homeostasis, it would take 10–12 years; thus, the larger vascular space, lower plasma protein concentrations, immature metabolism enzymes, and poor elimination process render drugs ineffective and, at times, expose them to adverse drug effects. The immature physiology of the age group makes it difficult to define the molecular soundness of the known drug mechanism in the population. This inability to understand the pharmacokinetics and pharmacodynamics stems from the lack of inclusivity of pediatric age groups in research. Further looking into the receptor physiology shows drastic variation in the expression of receptors in various tissues. For example, higher CNS expression of GABA A receptors in infants compared to older children and adults. In identifying these drawbacks, it is essential for one to understand the importance of flexible formulation options, the inclusion of a wide dose range, and a vigilant lookout for adverse drug events at every possible encounter.