MATERIALS AND METHODS: To evaluate the evidence for clinically established pharmacological therapies for constipation in palliative care, a systematic literature review was performed in different databases (Cochrane Library, Embase, PubMed, Ovid MEDLINE, CINAHL), textbooks, and publications. RESULTS: Whereas 130 randomized controlled trials were found with patients outside of palliative care settings, only 10 controlled studies with patients in end-of-life situations were identified: three RCTs with methylnaltrexone and one with the combination of oxycodone and naloxone showed the effect and safety of opiate antagonists for patients who are not at risk of gastrointestinal perforation. There have been no studies which test methylnaltrexone against the optimization of therapy with conventional laxatives. Six other controlled studies of limited quality in design and execution and with only few participants tested naloxone, senna, lactulose, Co-danthramer, an Ayurvedic preparation (Misrakasneham), magnesium hydroxide, fluid paraffin, sodium picosulfate and docusate without finding statistically significant differences in efficacy or side effects. Most patients in these studies had cancer. Only case studies with few patients in palliative care were found for meglumine, neostigmine, and other substances mentioned above. CONCLUSION: Evidence on medical treatment of constipation in palliative care is sparse and guidelines have to refer to evidence from outside the palliative care setting and to expert opinions. Results from studies with other patient groups can only be transferred with limitations to very ill patients at the end of life who might have a higher risk for potential side effects such as gastrointestinal perforation in case of abdominal tumor manifestation. Therefore further studies are required to evaluate the medical treatment of multiple reasons for constipation in these patients. These studies should focus on feasibility, clinical relevance and quality of life. The English full text version of this article will be available in SpringerLink as of November 2012 (under "Supplemental").