6种抗菌药在呼吸系统感染病人中的临床药动学

Clinical pharmacokinetics of six antibacterials in patients with respiratory tract infections

目的 :为研究临床常用抗菌药头孢呋辛酯 (CAE) ,头孢唑肟 (CZX) ,头孢克肟 (CFX) ,环丙沙星 (CPFX) ,左旋氧氟沙星 (LVFX)和阿米卡星 (AMK)在呼吸系统感染病人中药动学 ,以指导临床合理用药。方法 :CAE、CZX、CFX、CPFX和LVFX血药浓度应用高效液相色谱法 (HPLC)测定 ,AMK采用荧光偏振免疫分光光度法 (FPIA)测定。数据应用 3P87软件处理。结果 :临床药动学研究结果显示 ,所研究的 6种抗菌药中 ,消除半衰期依CAE、CZX、AMK、CFX、CPFX和LVFX顺序增加。其中4种口服给药抗菌药的吸收速率依CFX、CAE、CPFX和LVFX顺序增加 ;其达峰时间依CPFX、LVFX、CAE和CFX顺序延长 ;显然 ,喹诺酮类的CPFX和LVFX的吸收速率大于头孢类的CAE和CFX ,且达峰时间也快于头孢类的CAE和CFX ;但剂量相等时 ,头孢类抗菌药的CAE和CFX的峰浓度则高于喹诺酮类药物的峰浓度。结论 :临床在选择这几种抗菌药时 ,在充分考虑抗菌谱及适应症时 ,可根据研究结果 ,设计给药方案。

OBJECTIVE To study pharmacokinetics of six antibacterials commonly used in clinic: cefuroxime axetil(CAE), ceftizoxime(CZX), cefixime( CFX),ciprofloxacin(CPFX),levofloxacin(LVFX) and amikacin(AMK)in patients with respiratory tract infections.METHODS Serum concentrations of CAE,CZX, CFX, CPFX, LVFX and AMK were measured by high pressure liquid chromatography(HPLC)or fluorescence polarization immunoassay(FPIA).RESULTS The results of clinical pharmacokinetics showed that half life of elimination of CAE was the shortest, while that of CZX, AMK, CFX, CPFX and LVFX increased in order. The absorption rates of the four oral amtibacterials CFX, CAE, CPFX and LVFX increased accordingly. Therefore, the peak time for CPFX, LVFX, CAE and CFX increased in a order. It was clear that oral absorption rate and peak time of CPFX and LVFX of the quinolone antibacterials were faster than those of CAE and CFXof cephalosporin antibacterials when dose was equal, the peak level of CAE(500 mg, 6.13 , 2.07 μg·ml -1 ) and CFX(200mg, 2.44 , 0.25 μg·ml -1 ) of cephalosporin was higher than that of CPFX(500 mg, 2.57 , 1.20 μg·ml -1 ) and LVFX(200 mg, 1.97 , 0.24 μg·ml -1 ) of quinolone.CONCLUSIONS The optimal dosage of the six antibacterials for clinical therapy can be formulated and its rationality can be evaluated according to clinical pharmacokinetics and pharmacodanymics.