Psychopharmacological intervention is a major clinical and research area in oncology and palliative care. Over the last 35 years, psychotropic drugs have been shown to have a number of important indications for the treatment of the most common psychiatric disorders, such as depression, anxiety, stress-related syndromes, severe adjustment disorders, sleep disorders and delirium, which combined affect at least 30-40% of patients with cancer and even a higher percentage of patients in an advanced phase of illness. The availability of new drugs, with less side-effects and safer pharmacological profiles, has been a major advance in clinical psycho-oncology. Interestingly, several drugs have also been found to be helpful for the adjuvant treatment of cancer-related symptoms, such as pain, hot flashes, pruritus, nausea and vomiting, fatigue, and cognitive impairment, making psychopharmacology an important tool for the improvement of cancer patients' quality of life. The aim of this paper is to summarize recent relevant data concerning the use of psychotropic drugs, namely antidepressants, anxiolytics, antipsychotics, anticonvulsants and psychostimulants in patients with cancer.