Capsaicinoids, main capsaicin and dihydrocapsaicin, are a group of chemicals naturally occurring in chilli peppers with bioactive properties, such as analgesic, anti-cancer, weight loss, and lowering blood glucose and lipid. The metabolic disorder of body glucose and lipid is one of the main factors that lead to obesity, hyperlipidemia, and diabetes. Capsaicinoids have better effects on glucose control, lipid-lowering, and weight loss in animal and human experiments and the mechanisms have been widely noted. This paper reviewed effects of capsaicinoids on regulating glucose and lipids metabolism, and the possible mechanisms of capsaicinoids acted on capsaicin receptor TRPV1 channel, dietary carbohydrate and lipids digestion and absorption, the gut microbiota and the relation gene in liver, pancreas, adipose tissue, and nervous system. This review could provide a reference for the utilization of capsaicinoids.