Lanao J M, Domínguez-Gil A, Tabernero J M, De Castro S
Int J Clin Pharmacol Biopharm. 1979 Apr;17(4):171-5.
The pharmacokinetics of Amikacin (BB-K8) were determined after a single i.v. injection of 7.8 mg of the antibiotic/kg of body weight. It was administered to 10 patients with normal renal function and 19 patients with varying degrees of renal impairment. The elimination of Amikacin from plasma was seen to follow the course of an open two-compartment model system. From patients with normal renal function, values for the following pharmacokinetic parameters were obtained: alpha = 4.219 hr-1; beta = 0.292 hr-1; K12 = 2.218 hr-1; K21 = 0.859 hr-1; K13 = 1.432 hr-1; Vc = 3.125 1; Vp = 8.068 1 and Vdss = 11.193 1. As the relationship K12/K21 is greater than 1, it may be seen that there is a tendency for the antibiotic to accumulate in the peripheric compartment. Impaired renal function significantly diminishes the values recorded for alpha, beta, K12, K21, K13. Distribution volumes are significantly increased in patients with renal impairment. A linear relationship between the K13 of Amikacin and creatinine clearance is demonstrated. Adjustment of Amikacin dosage, according to the individual degree of renal impairment, may be obtained by spacing out the injections.
单次静脉注射7.8毫克抗生素/千克体重的阿米卡星(BB - K8)后,测定了其药代动力学。该药物被给予10名肾功能正常的患者和19名不同程度肾功能损害的患者。可见血浆中阿米卡星的消除符合开放二室模型系统的过程。从肾功能正常的患者中,获得了以下药代动力学参数值:α = 4.219小时⁻¹;β = 0.292小时⁻¹;K12 = 2.218小时⁻¹;K21 = 0.859小时⁻¹;K13 = 1.432小时⁻¹;Vc = 3.125升;Vp = 8.068升和Vdss = 11.193升。由于K12/K21的关系大于1,可以看出该抗生素有在外周室蓄积的趋势。肾功能损害显著降低了α、β、K12、K21、K13所记录的值。肾功能损害患者的分布容积显著增加。证明了阿米卡星的K13与肌酐清除率之间存在线性关系。根据个体肾功能损害程度调整阿米卡星剂量,可以通过延长注射间隔来实现。