OBJECTIVE: To compare the efficacy and safety of metoprolol and bisoprolol in the treatment of diastolic heart failure. METHODS: 150 patients with diastolic heart failure were randomly divided into group A(75 cases) and group B(75 cases). All patients received aspirin, angiotensin-converting enzyme inhibitors, angiotensin receptor antagonists, calcium antagonists, diuretic and cardiac drugs and other conventional treatment; based on it, group A received Metoprolol tartrate tablet with initial dose of 6.25 mg, orally, twice a day, then increased to 100-200 mg based on improvement and tolerability; group B received 1.25 mg Metoprolol tartrate tablet, orally, once a day, then increased to 10 mg based on improvement and tolerability. The treatment course for 2 groups was 12 weeks. Clinical efficacy, and left ventricular end systolic diameter (LVESD), left ventricular ejection fraction (LVEF) and left ventricular end-diastolic diameter (LVEDD), myocardial performance index (LVTei index), brain natriuretic peptide (BNP), interleukin (IL)-1,IL-6, tumor necrosis factor (TNF)-α before and after treatment, and incidence of adverse reactions in 2 groups were observed. RESULTS: The efficacy in group B was significantly higher than group A, incidence of adverse reactions were significantly lower than group A, the differences were statistically significant (P<0.05). Before treatment, there were no significant differences in the LVESD, LVEF, LVEDD, LVTei index, BNP, IL-1, IL-6 and TNF-α in 2 groups (P>0.05). After treatment, LVESD,LVEDD, LVTei index, BNP, IL-1, IL-6 and TNF-α in 2 groups were significantly lower than before, and group B was lower than group A, LVEF was significantly higher than before, and group B was higher than group A, the differences were statistically significant(P<0.05). CONCLUSIONS: Based on the conventional treatment, bisoprolol is significantly superior to metoprolol in terms of efficacy, relieving clinical symptoms and improving cardiac functions in the treatment of diastolic heart failure, with better safety.