Alcohol-related disorders are multifaceted since ethanol can induce profound metabolic perturbations when taken in excess. Global metabolic profiling strategies may aid the understanding of ethanol-related effects by shedding light on these metabolic changes and potentially revealing unknown mechanisms of ethanol toxicity. Here an overview of studies designed to explore the effects of alcohol (ethanol) consumption using holistic metabolite profiling approaches (metabonomics/metabolomics) is presented, demonstrating the potential of this methodology. The analytical technologies used (NMR, GC-MS and LC-MS), have been applied to the profiling of serum, plasma, urine and tissues, obtained from animal models or humans, after exposure to alcohol. From the metabolic profiling data of a range of biological samples, a number of endogenous metabolites have been proposed as potential ethanol consumption-related biomarkers. The biomarkers suggested by these studies, and the biochemical insights that they provide for understanding the effects of ethanol mechanisms of toxicity, are discussed.