Constipation is a common symptom in palliative care patients which can generate considerable suffering. There is uncertainty about the choice of treatment options from varying recommendations for management of constipation and a varying clinical practice in palliative care settings. The purpose of the review was to evaluate the current recommendations of therapy guidelines for the management of opioid-induced constipation in palliative care patients with a focus on methylnaltrexone bromide. Recent findings in the literature and related information on the opioid-induced gastrointestinal disorders in patients with advanced illness, as well as information on the opioid-antagonist methylnaltrexone, are discussed. Knowledge of the role of definitions, the causes of constipation and the pathophysiology of opioid-induced constipation must be given high priority in the treatment of patients receiving opioids. Diagnosis and therapy of constipation, therefore, should relate to findings in clinical investigation. Opioid-induced constipation and its adequate treatment is an important issue for patients with advanced illness and also poses therapeutic challenge for clinicians in daily routine. Methylnaltrexone bromide may represent an important therapeutic option for palliative care patients who are suffering from opioid-induced constipation with failure of conventional prophylactic oral laxative treatment.