Naber K G, Westenfelder S R, Madsen P O
Antimicrob Agents Chemother. 1973 Apr;3(4):469-73. doi: 10.1128/AAC.3.4.469.
The pharmacokinetics, distribution, and plasma and renal clearance of a new aminoglycoside antibiotic, tobramycin, was studied in the treatment of 18 elderly male patients (average age, 69 years) with urinary tract infections. Ten of these patients had normal renal function and eight had impaired renal function of various degrees. After administration of 1 mg of tobramycin/kg of body weight every 6 to 8 h (two to three times the half-life), urine concentrations were found to be sufficient in the treatment of urinary tract infections caused by susceptible organisms. The renal clearance of tobramycin during constant intravenous infusion was also studied in eight patients. Good correlation was found between the patients serum creatinine and the half-life of tobramycin. The half-life of tobramycin in patients with normal renal function (serum creatine [Formula: see text] to 1.5 mg/100) was on the average 3 h. For practical purposes, therefore, the dosage of tobramycin in the treatment of urinary tract infections should be 1 mg/kg of body weight every 6 to 8 h in patients with normal renal function. For patients with impaired renal function, the dosage interval is calculated by multiplying the patients' serum creatinine by six. If the dosage intervals are kept unchanged, the dosage must be divided by the patients' serum creatinine. The initial loading dose should always be 1 mg/kg. The total renal clearance of tobramycin (92% of the glomerular filtration rate) was not influenced by the administration of probenecid, which indicates that tobramycin is excreted only by glomerular filtration.
对一种新型氨基糖苷类抗生素妥布霉素的药代动力学、分布以及血浆清除率和肾脏清除率进行了研究,该研究纳入了18名患有尿路感染的老年男性患者(平均年龄69岁)。其中10名患者肾功能正常,8名患者有不同程度的肾功能损害。每6至8小时给予1毫克妥布霉素/千克体重(为半衰期的两至三倍)后,发现尿液浓度足以治疗由易感菌引起的尿路感染。还对8名患者进行了持续静脉输注期间妥布霉素的肾脏清除率研究。发现患者血清肌酐与妥布霉素半衰期之间具有良好的相关性。肾功能正常(血清肌酐[公式:见原文]至1.5毫克/100)的患者中,妥布霉素的半衰期平均为3小时。因此,实际上,肾功能正常的患者在治疗尿路感染时妥布霉素的剂量应为每6至8小时1毫克/千克体重。对于肾功能受损的患者,给药间隔通过将患者的血清肌酐乘以6来计算。如果给药间隔保持不变,则剂量必须除以患者的血清肌酐。初始负荷剂量始终应为1毫克/千克。妥布霉素的总肾脏清除率(占肾小球滤过率的92%)不受丙磺舒给药的影响,这表明妥布霉素仅通过肾小球滤过排泄。