Yamazaki I, Shirakawa Y, Fugono T
J Antibiot (Tokyo). 1981 Aug;34(8):1055-63. doi: 10.7164/antibiotics.34.1055.
The renal excretory mechanism of cefmenoxime was compared with those of 6 other cephalosporins (cefotaxime, deacetylcefotaxime, cefotiam, cefazolin, cephaloridine and cefsulodin) in rats and rabbits. In rats, renal clearance (Cf-Drug: corrected for serum protein binding) of cefmenoxime (4.06 ml/minute) was lower than that of cefazolin, similar to that of cefotiam, and higher than those of cefotaxime, deacetylcefotaxime, cephaloridine, and cefsulodin. In rabbits, the value for cefmenoxime (2,519 ml/minute) was markedly higher than those for the other drugs. If the clearance ratio (Cf-Drug/CInulin = CRf) is more than unity, tubular secretion of a drug is indicated. In rats, the tubular secretion of cefmenoxime equalled the glomerular filtration (CRf = 2.17). The tubular secretion of cefmenoxime was lower than that of cefazolin but similar to that of cefotiam. None of the other cephalosporins seemed to be secreted significantly. In rabbits, a large amount of cefmenoxime was secreted (CRf = 208). The tubular secretion was larger than those of the other cephalosporins. All the drugs except cefsulodin showed significant tubular secretion. A species difference was observed in the CRf of the cephalosporins: the values were generally higher in rabbits than in rats.
在大鼠和兔子中,比较了头孢甲肟与其他6种头孢菌素(头孢噻肟、去乙酰头孢噻肟、头孢替安、头孢唑林、头孢噻啶和头孢磺啶)的肾脏排泄机制。在大鼠中,头孢甲肟的肾脏清除率(Cf-药物:校正血清蛋白结合)为4.06毫升/分钟,低于头孢唑林,与头孢替安相似,高于头孢噻肟、去乙酰头孢噻肟、头孢噻啶和头孢磺啶。在兔子中,头孢甲肟的值(2519毫升/分钟)明显高于其他药物。如果清除率比值(Cf-药物/C菊粉=CRf)大于1,则表明药物有肾小管分泌。在大鼠中,头孢甲肟的肾小管分泌等于肾小球滤过(CRf=2.17)。头孢甲肟的肾小管分泌低于头孢唑林,但与头孢替安相似。其他头孢菌素似乎均无明显分泌。在兔子中,大量头孢甲肟被分泌(CRf=208)。其肾小管分泌大于其他头孢菌素。除头孢磺啶外,所有药物均显示有明显的肾小管分泌。观察到头孢菌素的CRf存在种属差异:兔子中的值通常高于大鼠。