This work compared the efficacy ergometrine maleate and carbetocin in prevention of postpartum hemorrhage in cesarean section and their effects on inflammatory factors. Eighty high-risk pregnant women receiving cesarean section were randomly divided into ergometrine maleate and carbetocin groups, 40 cases in each group. After the delivery, based on using oxytocin, the ergometrine maleate and carbetocin groups received the treatment using ergometrine maleate and carbetocin, respectively. Results showed that, the hemorrhage volume within 2 h and 24 h after fetal delivery in carbetocin group was obviously lower than ergometrine maleate group, respectively (p < 0.05). At 24 h after delivery, the prothrombin time and activated partial thromboplastin time in carbetocin group were significant shorter than ergometrine maleate group, respectively (p <0.05), and the serum interleukin-2 and interleukin-10 level in carbetocin group were obviously lower than ergometrine maleate group, respectively (p < 0.05). No significant change in blood pressure or heart rate or obvious adverse reaction was found in two groups. In conclusion, for high-risk pregnant women receiving cesarean section, carhoxytocin is more effective in preventing the postpartum hemorrhage, improving the coagulation function and reducing the inflammatory response, compared with ergometrine maleate. Both drugs are safe in use.