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Inadequate handling of an uncooperative child preoperatively results in postoperative behavior problems. Premedication enables a calm induction and helps to decrease postoperative problems. Several premedicants will be covered in this review.Questions raised about the effects of oral midazolam use in children for premedication are now finding answers. New agents (dexmedetomidine and atypical antipsychotic agents) can be alternatives in premedication, especially in severely uncooperative children. The current literature highlights the missing information about the rather older premedicants.The benefits and disadvantages of new and older drugs should be weighed against each other, and decisions should be made according to the requirements of surgery, ward conditions and the severity of psychologic, developmental or mental disease. Further studies for the evaluation of the anxiolytic, sedative and antipsychotic drugs are still required.