OBJECTIVE: To observe the clinical efficacy and safety of Ligustrazine injection, α-ketoacid combined with levamlodipine in the treatment of chronic renal failure. METHODS: 92 patients with chronic renal failure were randomly divided into observation group (46 cases) and control group (46 cases). All patients received electrolyte, vitamins and essential amino acid, low salt, low fat, hypoglycemic and hypolipemic, anti-infection, correcting anemia and other conventional symptomatic treatment. Based on it, control group received 8 Compound α-ketoacid tablets, 3 times a day + 1 Benzenesulfonic acid levamlodipine tablet, once a day. Observation group additionally received 150 mg Ligustrazine hydrochloride injection, adding into 250 ml 5% Glucose injection, intravenous infusion, once a day. The treatment course for both groups was 3 months. Clinical efficacy, and urea nitrogen (BUN), serum creatinine (Scr), serum cystatin (CysC), low-density lipoprotein cholesterol (LDL-C), total cholesterol (TC), triglyceride (TG) levels before and after treatment and the incidence of adverse reactions in 2 groups were observed. RESULTS: The total effective rate in observation group was significantly higher than control group, the difference was statistically significant (P<0.05). Before treatment, there were no significant differences in the BUN, Scr, CysC, LDL-C, TC and TG between 2 groups (P>0.05). After treatment, BUN, Scr, LDL-C, TC and TG in 2 groups were significantly lower than before, and observation group was lower than control group, CysC was significantly higher than before, and observation group was higher than control group, the differences were statistically significant (P<0.05). And there was no significant difference in the incidence of adverse reactions (P>0.05). CONCLUSIONS: Based on conventional treatment, Ligustrazine injection, α-ketoacid combined with levamlodipine show obvious efficacy in the treatment of chronic renal failure, they can improve the renal functions, with good safety.