Methods and compositions for regulating food intake in a human subject; for improving a compliance of a human subject to caloric restriction; and for reducing a desire of a human subject to consume fats, utilizing H1-receptor agonists that have a pharmacological half-life that allows an efficient treatment regime thereof are disclosed. The methods and compositions can be efficiently used for treating conditions such as overeating, overweight, obesity, binge eating disorder, night eating syndrome, obsessive eating, compulsive eating and bulimia, as well as conditions associated with metabolic derangement such as dyslipidemia and for preventing or reducing weight gain due to factors such as drug use, cessation of smoking, and the like in a human subject.