Objective To determine the effects of valsartan on the plasma levels of N-terminal pro-B-type natriuretic peptide (NT-proBNP) and copeptin in the elderly patients with chronic heart failure (CHF), and to investigate the possible mechanism of valsartan to prevent ventricular remodeling. Methods A total of 99 CHF elderly patients aged from 60～81(68±12)years who were hospitalized in our department from June 2011 to September 2012 were recruited in this study. They were randomly divided into 2 groups: valsartan and conventional treatment group (valsartan group, n=50), and conventional treatment (control group, n＝49). The plasma levels of NT-proBNP and copeptin, and the structural function of left ventricle were measured at the baseline, 1 and 6 months after valsartan treatment. Results The levels of NT-proBNP and copeptin were decreased in both groups at 1 month after treatment, and more significantly at 6 months (P＜0.05 or 0.01). Their levels were significantly lower in the valsartan treatment group than in the control group at 1 and 6 months after treatment respectively (P＜0.05 or 0.01). No significant difference was found in the left ventricular ejection fraction (LVEF), left ventricular end systolic diameter (LVESD) and left ventricular end diastolic diameter (LVEDD) in the 2 groups at 1 month after treatment, and between the 2 groups before and at 1 month after treatment (P＞0.05). But at 6 months after treatment, the LVEF was significantly higher (P＜0.01), while the LVESD and LVEDD were significantly lower in the valsartan treatment group than in the control group (P＜0.01). Conclusion Angiotensin Ⅱ receptor antagonist valsartan could inhibit the secretion of NT-proBNP and copeptin in the plasma of elderly patients with CHF, and then suppresses neuroendocrine factors, prevents ventricular remodeling, and therefore improves the heart function.