Efficient and safe pediatric perioperative pain therapy in the context of a multimodal pain therapy concept requires a slight to moderate opioid analgesic. Nalbuphine is a nearly ideal opioid for this purpose due to its unique pharmacological properties as a μ-receptor antagonist/κ-receptor agonist and a high safety profile. Nalbuphine is used clinically primarily in postoperative pain therapy administered as a bolus, continuous infusion and patient-controlled analgesia. Furthermore, it is administered in different regimens for pediatric diagnostic and interventional sedation.