Gastro-oesophageal reflux (GOR) is the effortless passage of gastric contents into the distal oesophagus. It can be classified as functional (or symptomatic), in which the infant remains free from disease, or a pathological (GOR disease, GORD), in which gastrointestinal, respiratory or neurobehavioural signs occur with intraoesophageal acidification and the development of oesophagitis. Functional or symptomatic GOR is successfully treated by conservative measures and does not require investigative diagnostic tools; however, both drug administration and an investigative approach are mandatory in patients with GORD. There is currently a great range of proven therapeutic options for GORD that are directed at counteracting the pathogenetic components of the disorder. In this report we discuss the role of different drug classes for treating GORD in children. The choice of therapy for GORD depends upon the severity of signs and the degree of oesophagitis. The presence of oesophagitis, as documented by endoscopy, suggests the use of antisecretory drugs; H2 receptor antagonists are the first-line agents. Nevertheless, individuals with refractory disease or those patients requiring potent inhibition of acid secretion (for example, GORD with respiratory involvement) can be given proton pump inhibitors. Other groups of patients who need potent inhibition of acid secretion are children with neurological dysfunction and those with Barrett's oesophagus. It is still unclear whether patients with frequent relapses are candidates for long term administration of antisecretory drugs or for surgical fundoplication.