The aim of this study was to compare the efficiency and safety of urapidil and nitroglycerin in treating elderly patients with acute heart failure. A total of 248 patients with acute heart failure were recruited randomly from 10 clinical centers. In this article, efficiency of medication to elderly patients (age = 60 yrs., n = 222) was specially focused. Patients were administrated with urapidil (n = 107) or nitroglycerin (n = 115) by micro-pump continuously for 48 hours. Compared with nitroglycerin, urapidil significantly increased ejection fraction (EF%), decreased left ventricular end diastolic volume (EDV) and end systolic volume (ESV). No significant difference of NT-pro BNP was detected (2-day: ESV, P = 0.067; EDV, P = 0.016; EF%, P = 0.054; NT-pro BNP, P = 0.853; 7-day: ESV, P = 0.039; EDV, P = 0.054; EF%, P = 0.035; NT-pro BNP, P = 0.931); Urapidil provided significantly lipid-decreasing effects, and showed no disadvantage effects on blood glucose (Delta 2d: cholesterol, P = 0.016; LDL, P = 0.031; blood glucose, P = 0.613;. Delta 7d: cholesterol, P = 0.012; LDL, P = 0.059; blood glucose, P = 0.422); More severely deteriorated baseline renal function was observed in urapidil group (P = 0.024), however, the increase amplitude of creatinine was comparable at all tested time points between the two groups (Delta 2d: P = 0.692;Delta 7d: P = 0.742); And 30-day incidence of re-hospitalization and deterioration of cardiac function was significantly lower in urapidil group (P = 0.046). Therefore, urapidil more effectively reduces cardiac load and improves cardiac function, while providing more significant protection to renal function and improving blood lipid metabolism. We recommended that urapidil should be preferably used for elderly patients with acute heart failure as an effective and safe vasodilator.