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Objectives: Despite the fact that delirium is a frequent neuropsychiatric disorder in cancer patients, there are, in Korea, no guidelines for the pharmacological treatment of such delirium. This systematic review evaluated the efficacy and safety of some pharmacological interventions and summarized the results. Methods: We searched PubMed, Embase, CINAHL, the Cochrane Library, and the KMbase, targeting from January 1990 to October 2008, using key words. Moreover, we included systematic reviews, meta-analyses, and randomized controlled trial literature in the search. Then, we stratified the trials based on their evidence levels. Results and Conclusion: We identified 13 randomized, controlled studies and 2 case-control studies that met our inclusion criteria. These showed that haloperidol was the medication of choice to treat delirium. In addition, they revealed that atypical antipsychotics have not shown clear superiority with regard to effectiveness as compared to haloperidol. Neither donepezil nor rivastigmine were shown to be effective in preventing or treating delirium.