The cerebral circulation and metabolism of ten preoperative cardiac surgery patients were assessed. Alterations in regional cerebral blood flow (rCBF), measured by 123I-N-isopropyl-p-iodo-amphetamine singlephoton emission computed tomography, and in cerebral oxygen metabolism, simultaneously detected by near-infrared spectroscopy (NIRS) before and after acetazolamide administration, were investigated. The rCBF (ml/min/100 g) increased significantly from 40.21±7.65 to 56.24±13.69 (p<0.001), and a significant increase in oxyhemoglobin (Oxy-Hb) of 13.9% (p=0.0022) and total hemoglobin (Total-Hb) of 5.7% (0.0047) along with a significant decrease in deoxyhemoglobin (Deoxy-Hb) of 8.9% (p=0.0414) were observed concomitantly. Thus, the Oxy-Hb/Total-Hb ratio (%Oxy-Hb) rose significantly from 67.26±9.82% to 72.98 ±8.09% (p=0.0022). Examination of the relationships between individual parameters showed that the percentage changes in rCBF and Oxy-Hb were significantly correlated (r=0.758, p=0.011). The percentage changes in rCBF and %Oxy-Hb were also correlated significantly (r=0.740, p=0.014). In conclusion, this evidence suggested that NIRS is able to detect relative changes in cerebral hemodynamics and reflect luxury perfusion induced by acetazolamide.