PHARMACOKINETICS OF CINOXACIN IN PATIENTS WITH IMPAIRED RENAL FUNCTION

The pharmacokinetics of cinoxacin, a new synthetic antibacterial agent, were examined in 6 healthy volunteers and 12 patients with different endogeneous creatinine clearances (Ccr) on the basis of a one-compartment open model. Each subject received a single 400mg oral dose of cinoxacin, and serum an...

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Published inCHEMOTHERAPY Vol. 28; no. Supplement4; pp. 133 - 138
Main Authors OHKAWA, MITSUO, SUGATA, TOSHIAKI, KURODA, KYOICHI, OKASHO, AKIRA, SAWAKI, MASARU, KAWAGUCHI, KOHEI, TAKANO, MANABU
Format Journal Article
LanguageJapanese
Published Japanese Society of Chemotherapy 01.01.1980
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ISSN0009-3165
1884-5894
DOI10.11250/chemotherapy1953.28.Supplement4_133

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Summary:The pharmacokinetics of cinoxacin, a new synthetic antibacterial agent, were examined in 6 healthy volunteers and 12 patients with different endogeneous creatinine clearances (Ccr) on the basis of a one-compartment open model. Each subject received a single 400mg oral dose of cinoxacin, and serum and urinary concentrations of free cinoxacin and cinoxacin conjugate were measured by a fluorometric method. The mean peak concentration of free cinoxacin in serum was achieved 3 hours after administration in normal subjects. The mean serum half-life of free cinoxacin was calculated for 66 minutes in normal subjects, and increased in patients along with increasing impairment of renal function. A significant correlation between the elimination rate constant and Ccr was demonstrated (p<0.001). In normal subjects, 62% of the drug was excreted in the urine as free cinoxacin within the first 12 hours, 95% as total cinoxacin including cinoxacin conjugate. The urinary excretion rate declined gradually in patients as a degree of renal impairment advanced.
ISSN:0009-3165
1884-5894
DOI:10.11250/chemotherapy1953.28.Supplement4_133