Antimetabolites have been used in combination with filtering surgery to improve surgical results for more than 10 years. Based on research published since the introduction of antimetabolites right up to date, we discuss the various forms of antimetabolites that have been used, including drugs and irradiation. Among the drugs used, mitomycin C and 5-fluorouracil are the most prominent. We discuss the background of these agents, the progress in the use of antimetabolites and the research done on these drugs. These agents have been used both intra-operatively and perioperatively. We discuss the indications for their use, their mode of action, the techniques of usage, their variations as well as the complications and the treatment of complications.