Prevention and treatment of pain in preterm and term neonates became major issues in neonatal care since the landmark observations of Anand et al. on the impact of (in) adequate analgesia on mortality and morbidity after surgery in preterm neonates. Safe and effective analgesia does require thorough understanding of maturational clinical pharmacology. In the current review we summarized the available data on both pharmacokinetics and – dynamics of analgesics of various potency (potent opioids, moderate potent opioids, non-selective cyclo-oxygenase inhibitors and acetaminophen) in neonates. The available information on developmental pharmacology in neonates has extended significantly, but we have to be aware that most studies focussed on aspects of pharmacokinetics, and not yet on aspects of pharmacodynamics. The currently available information on developmental pharmacology of analgesics in neonates still needs to be further integrated in a multimodal, approach to prevent and treat pain in the neonate.