While there are several comprehensive reviews on the toxic effects of methylxanthines in animals, data on the toxicity of these chemicals in humans has not been extensively reviewed in one document. In a previous paper (Stavric, Fd Chem. Toxic. 1988, 26, 541), the toxicity of theophylline was reviewed. This paper, the second of three, is intended to provide an overview of the human toxicity of caffeine. Only pertinent and recent information on caffeine toxicity is summarized. In addition, some information regarding the benefits of caffeine and the mechanism of its effects is also provided. The use, effects and toxicity of caffeine intake are reviewed separately for different segments of the population. Controversy concerning the possible association of caffeine with fibrocystic disease of the breast and over the behavioural effects of the drug is presented briefly.