Objective To understand the current state of research and clinical application of α-asarone injection. Method Literature search was conducted and the pharmacology, toxicology, preparation, clinical application and adverse reactions of α-asarone were reviewed. Results α-asarone injection has strong relieving effects on cough and asthma, but the quality of production is varying, adverse reactions are often reported, and the toxicological effects need to be further investigated. Conclusions α-asarone injection has a certain clinical effect, but the reports of related adverse reactions are gradually increased. Its toxicity remains to be further studied, and the product quality standard system and instructions need also to be further improved.