Summary
Cefuroxime, a new cephalosporin antibiotic which is stable to most β-lactamases produced by Gram-negative bacteria, was given by bolus intravenous injection to six volunteers in doses of 500 mg and 750 mg. The concentrations of cefuroxime in serum and urine were measured at pre-determined times after injection and the data analysed by a two-compartment open system model. A serum concentration of 8 µg/ml was exceeded for 100.3 min (±18.3) after a 500 mg dose and for 144.5 min (±19.8) after 750 mg. The ultimate serum half-life was 1.1 h. Excretion of cefuroxime in the urine was almost complete in 24 h, the clearance being 150 ml/min/1.73 m2. About 45% was excreted through the renal tubules. The injections were well tolerated and no changes in haematological or biochemical values were seen. The resulting data are compared with those published for some other cephalosporins. It is concluded that the favourable pharmacokinetics, especially the high concentrations of unbound cefuroxime in the serum, are likely to aid effective therapy of human infection caused by sensitive bacteria.
Similar content being viewed by others
References
O'Callaghan, Cynthia H., Sykes, R.B., Ryan, D.M., Foord, R.D., Muggleton, P.W.: Cefuroxime — a new cephalosporin antibiotic. J. Antibiot. (Tokyo),29, 29–37 (1976)
O'Callaghan, Cynthia H., Sykes, R.B., Griffiths, A., Thornton, J.E.: Cefuroxime, a new cephalosporin antibiotic: activity in vitro. Antimicrob. Agents Chemother.9, 511–519 (1976)
Goodwin, C.S., Dash, C.H., Hill, Joyce, P., Goldberg, A.D.: Cefuroxime: pharmacokinetics after a short infusion, and in vitro activity against hospital pathogens. J. Antimicrob. Chemother.3, 253–261 (1977)
Foord, R.D.: Cefuroxime: human pharmacokinetics. Antimicrob. Agents Chemother.9, 741–747 (1976)
Goodwin, C.S., Raftery, E.B., Goldberg, A.D., Skeggs, H., Till, A.E., Martin, C.M.: Effects of rate of infusion and probenecid on serum levels, renal excretion, and tolerance of intravenous doses of cefoxitin in humans: comparison with cephalothin. Antimicrob. Agents Chemother.6, 338–346 (1974)
Meyers, B.R., Ribner, B., Yancovitz, S., Hirschman, S.Z.: Pharmacological studies with cefamandole in human volunteers. Antimicrob. Agents Chemother.9, 140–144 (1976)
Wagner, J.G., Northam, J.I.: Estimation of volume of distribution and half-life of a compound after rapid intravenous injection. J. Pharm. Sci.56, 529–531 (1967)
Kosmidis, J., Hamilton-Miller, J.M.T., Gilchrist, J.N.C., Kerry, D.W., Brumfitt, W.: Cefoxitin, a new semi-synthetic cephamycin, an in-vitro and in-vivo comparison with cephalothin. Brit. med. J.1973/4, 653–655
Brumfitt, W., Kosmidis, J., Hamilton-Miller, J.M.T., Gilchrist, J.N.C.: Cefoxitin and cephalothin antimicrobial activity, human pharmacokinetics and toxicology. Antimicrob. Agents Chemother.6, 290–299 (1974)
Fong, I.W., Ralph, E.D., Engelking, E.R., Kirby, W.M.M.: Clinical pharmacology of cefamandole as compared with cephalothin. Antimicrob. Agents Chemother.9, 65–69 (1976)
Kirby, W.M.M., Regamey, C.: Pharmacokinetics of cefazolin compared with four other cephalosporins. J. infect. Dis.128 (Oct Suppl), S341-S346 (1973)
Regamey, C., Libke, R.D., Clarke, J.T.: Pharmacokinetics of parenteral cephalexin in comparison with cephalothin and cefazolin. Infection2, 132–136 (1974)
Kirby, W.M.M., De Maine, J.B., Serrill, S.W.: Pharmacokinetics of the cephalosporins in healthy volunteers and uremic patients. Postgrad. med. J.47 (Feb Suppl), 41–46 (1971)
Weliky, I., Zaki, A.: Absorption, distribution and elimination of cephradine after oral and parenteral administration to humans. In: Progress in Chemotherapy,1, ed. Daikos, G.K., pp. 582–586. Athens: Hellenic Society for Chemotherapy 1974
Paradelis, A.G.: Absorption and excretion studies of cephalosporins in human subjects. In: Chemotherapy,5 (ed Williams, J.D. & Geddes, A.M.) pp. 283–292. New York & London: Plenum Press 1976
Neiss, E.S.: Cephradine, a summary of preclinical studies and clinical pharmacology. J. Irish med. Ass.66 (March Suppl), 1–12 (1973)
Welling, P.G., Craig, W.A., Amidan, G.L., Kunin, C.M.: Pharmacokinetics of cefazolin in normal and uremic subjects. Clin. Pharmacol. Ther.15, 344–353 (1974)
Author information
Authors and Affiliations
Rights and permissions
About this article
Cite this article
Gower, P.E., Dash, C.H. The pharmacokinetics of cefuroxime after intravenous injection. Eur J Clin Pharmacol 12, 221–227 (1977). https://doi.org/10.1007/BF00609865
Received:
Revised:
Accepted:
Issue Date:
DOI: https://doi.org/10.1007/BF00609865