Nahata M C, Durrell D E, Barson W J
Clin Pharmacol Ther. 1982 Apr;31(4):528-32. doi: 10.1038/clpt.1982.71.
The kinetics of the R and S epimers of moxalactam were followed after single intravenous doses of 50 mg/kg to 12 patients, 8 to 45 mo old, with cellulitis or epiglottitis. High-pressure liquid chromatography was used to determine serum concentrations. Total body clearance and apparent volume of distribution of the R epimer were higher than those of the S epimer (P less than 0.004). Total body clearance of R, S, and R + S moxalactam ranged from 29.01 to 183.7, 19.00 to 79.95, and 23.34 to 113.6 ml/min/m2. Mean elimination half-lives of R, S, and R + X moxalactam were 2.04, 2.26, and 2.24 hr. The higher incidence of the more active R epimer and the 500% interpatient variation in clearance may indicate a need for monitoring serum and cerebrospinal fluid concentrations in patients with severe unresponsive central nervous system infectious treated with moxalactam.
对12例年龄在8至45个月、患有蜂窝织炎或会厌炎的患者单次静脉注射50mg/kg的羟羧氧酰胺菌素后,追踪其R型和S型差向异构体的动力学情况。采用高压液相色谱法测定血清浓度。R型差向异构体的总体清除率和表观分布容积高于S型差向异构体(P<0.004)。R、S及R+S型羟羧氧酰胺菌素的总体清除率范围分别为29.01至183.7、19.00至79.95及23.34至113.6ml/min/m²。R、S及R+X型羟羧氧酰胺菌素的平均消除半衰期分别为2.04、2.26及2.24小时。活性更强的R型差向异构体的较高发生率以及患者间清除率500%的差异可能表明,在用羟羧氧酰胺菌素治疗严重无反应性中枢神经系统感染的患者时,有必要监测血清和脑脊液浓度。