The rectal route can be considered a good alternative to the oral route for the paediatric population because these dosage forms are neither to be swallowed nor need to be taste-masked. Rectal forms can also be administered in an emergency to unconscious or vomiting children. Their manufacturing cost is low with excipients generally regarded as safe. Some new formulation strategies, including mucoadhesive gels and suppositories, were introduced to increase patient acceptability. Even if recent paediatric clinical studies have demonstrated the equivalence of the rectal route with others, in order to enable the use of this promising route for the treatment of children in the 21st Century, some effort should be focused on informing and educating parents and care givers. This review is the first ever to address all the aforementioned items, and to list all drugs used in paediatric rectal forms in literature and marketed products in developed countries.