In order to assess occupational exposure of hospital personnel involved in the preparation and administration of antineoplastic drugs, biological and environmental monitoring are essential to identify the main exposure routes and to quantify potential health risks. If workplace contamination cannot be completely avoided, it is of utmost importance to reduce exposure to the lowest possible levels. To this aim, not only do education and training of the exposed subjects play an important role, but accurate standardized sampling techniques and analytical methods are also required. A critical overview of the most significant methods available in the literature is presented and their value is discussed, especially with respect to their sensitivity and specificity. In addition, attention is given to validation procedures and, consequently, to their reliability. The results from the most important surveys carried out at hospital departments are also discussed, with a view to improving both monitoring strategies and moreover working conditions.