The pineal hormone, melatonin, has widespread effects on the body. The aim of this review is to consider the specific interactions between melatonin and human physiological functions associated with sport and exercise medicine. Separate researchers have reported that melatonin concentrations increase, decrease and remain unaffected by bouts of exercise. Such conflicting findings may be explained by inter-study differences in lighting conditions and the time of day the study participants have exercised. Age and fitness status have also been identified as intervening factors in exercise-mediated changes in melatonin concentration. The administration of exogenous melatonin leads to hypnotic and hypothermic responses in humans, which can be linked to immediate reductions in short-term mental and physical performance. Depending on the dose of melatonin, these effects may still be apparent 3-5 hours after administration for some types of cognitive performance, but effects on physical performance seem more short-lived. The hypothesis that the hypothermic effects of melatonin lead to improved endurance performance in hot environments is not supported by evidence from studies involving military recruits who exercised at relatively low intensities. Nevertheless, no research group has examined such a hypothesis with athletes as study participants and with the associated more intense levels of exercise. The fact that melatonin has also been found to preserve muscle and liver glycogen in exercised rats adds weight to the notion that melatonin might affect endurance exercise in humans. Melatonin has been successfully used to alleviate jet lag symptoms of travellers and there is also a smaller amount of evidence that the hormone helps shiftworkers adjust to nocturnal regimens. Nevertheless, the symptoms of jet lag and shiftwork problems have primarily included sleep characteristics rather than performance variables. The few studies that have involved athletes and performance-related symptoms have produced equivocal results. Melatonin has also been found to be useful for treating some sleeping disorders, but interactions between sleep, melatonin and exercise have not been studied extensively with trained study participants. It is unknown whether melatonin plays a role in some exercise training-related problems such as amenorrhoea and over-training syndrome.