The critical factors related to the safety of obstetric anesthetics include placental drug transfer and neonatal drug metabolism. Almost all drugs can pass through the placenta to a certain extent and reach a particular concentration in the fetus. Therefore, it is of great clinical significance to understand the basic process and mechanism of placental transfer to balance fulfilling the cesarean section requirement and minimizing the impact on the neonates. This review article describes the related factors affecting the placental transfer of drugs and the effects of clinically relevant anesthesia drugs on mothers and neonates and discusses the influence of milk secretion after delivery. These can provide a theoretical basis for a more rational selection of obstetric anesthesia⁃related drugs. The safety of obstetric anesthesia still needs further research and exploration to reduce postoperative adverse effects.