Kinetics and renal handling of cefonicid

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Abstract
Cefonicid kinetics were determined after i.v. and i.m. injection and the renal handling of the drug was examined [in humans], including the effect of probenecid on its excretion. Peak serum levels after 1000 and 500 mg i.v. were 221 and 91 .mu.g/ml. The half-life (t1/2) was the same for both regimens (3.5 h). I.m. injection of the 1000- and 500-mg doses resulted in peak serum levels of 112 and 40 .mu.g/ml. When probenecid was given with the 500-mg dose, the peak serum level was 61 .mu.g/ml and the time to peak level rose from 1.3 to 2.5 h. The t1/2 after 1000 and 500 mg alone was much the same at 4.8 and 4.9 h. The addition of probenecid to the 500-mg dose extended the t1/2 to 7.5 h. Renal clearance, excretion and secretion rates for cefonicid were reduced by the addition of probenecid. Cefonicid''s long t1/2 and high blood levels may provide clinical efficacy with a single daily dose.

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