Mercury is an ubiquitous environmental toxin that causes a wide range of adverse health effects in humans. Three forms of mercury exist: elemental, inorganic and organic. Each of them has its own profile of toxicity. Exposure to mercury typically occurs by inhalation or ingestion. Mercury can be an indoor air pollutant, however industry emission remains the most important source of inhaled mercury. Furthermore, fresh water and ocean fish may contain large amounts of mercury and dental amalgam can be another important source of inorganic and mercury vapor. The present review discusses the current information on mercury toxicity and the distinct toxicologic profile of the three forms of mercury. The existing therapeutics, new therapeutics development or agents for treating mercury poisoning will also discussed. Since in general low levels of mercurial are tolerable, herein, we also discuss the defensive mechanisms developed by the cell to protect itself against mercury injury. This aspect may be useful to provide a biological protection against toxic effects exerted by mercury or by specific forms of mercury in view of a medicinal purposes.