Objective: Ligustrazine is an amide alkaloid, with the active substance being Chuanxiong. Also known as tetramethylpyrazine (TMP), ligustrazine has various pharmacological effects and has been used to treat a variety of diseases. Many studies have demonstrated a role for ligustrazine in the treatment of several obstetrical and gynecological diseases. However, most results on the efficacy of ligustrazine have been obtained from basic laboratory experiments, with few clinical studies having validated these results. Mechanisms: In this narrative review we analyze the available literature summarizing the role and mechanism of ligustrazine in the treatment of obstetrical and gynecological diseases. Findings in Brief: TMP shows good results for the treatment of endometriosis, preeclampsia, ovarian cancer, as well as other obstetrical and gynecological diseases through its regulation of cell proliferation, invasion and metastasis, inflammation, immune response, apoptosis, autophagy, angiogenesis, endothelial protection, and fibrogenesis. Conclusions: TMP is therefore a promising drug with great research potential. Of note, ligustrazine is a complementary or alternative medicine and not the primary treatment. And most studies to date are laboratory-based experiments with low evidence levels. More in-depth research is needed to determine the pharmacological effects of ligustrazine in the clinic.