Abstract
The simulated intravascular and extravascular kinetics of cefotaxime were studied in an in vitro model to evaluate the effect of antibiotic protein binding in the "intravascular" and "extravascular" space. Intravascular fluid consisted of either phosphate-buffered saline, which has no cefotaxime binding, or 3% bovine albumin, which has 63% cefotaxime binding. Extravascular spaces were filled with phosphate-buffered saline, 1.5% bovine albumin (46.6% cefotaxime binding), or 3% bovine albumin. Cefotaxime (80 mg per dose) was infused every 3 h for eight doses, and intravascular and extravascular drug concentrations were measured after doses one and eight. The corresponding intravascular and extravascular spaces were at (phosphate-buffered saline) or approaching (3% bovine albumin) equilibrium by dose eight. There were marked differences in drug concentrations achieved in the various extravascular spaces, but all could be explained on the basis of differing amounts of albumin present and the resultant differences in cefotaxime binding.
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Selected References
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- Bergan T. Pharmacokinetics of tissue penetration of antibiotics. Rev Infect Dis. 1981 Jan-Feb;3(1):45–66. doi: 10.1093/clinids/3.1.45. [DOI] [PubMed] [Google Scholar]
- Fasching C. E., Peterson L. R. Anion-exchange extraction of cephapirin, cefotaxime, and cefoxitin from serum for liquid chromatography. Antimicrob Agents Chemother. 1982 Apr;21(4):628–633. doi: 10.1128/aac.21.4.628. [DOI] [PMC free article] [PubMed] [Google Scholar]
- LOWRY O. H., ROSEBROUGH N. J., FARR A. L., RANDALL R. J. Protein measurement with the Folin phenol reagent. J Biol Chem. 1951 Nov;193(1):265–275. [PubMed] [Google Scholar]
- Murakawa T., Sakamoto H., Hirose T., Nishida M. New in vitro kinetic model for evaluating bactericidal efficacy of antibiotics. Antimicrob Agents Chemother. 1980 Sep;18(3):377–381. doi: 10.1128/aac.18.3.377. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Peterson L. R., Gerding D. N. Influence of protein binding of antibiotics on serum pharmacokinetics and extravascular penetration: clinically useful concepts. Rev Infect Dis. 1980 May-Jun;2(3):340–348. doi: 10.1093/clinids/2.3.340. [DOI] [PubMed] [Google Scholar]
- Peterson L. R., Gerding D. N., McLinn D., Hall W. H. Prediction of peak penicillin and cephalosporin concentrations in canine serum as derived from in vitro serum and tissue quantitative protein binding. J Antimicrob Chemother. 1979 Mar;5(2):219–227. doi: 10.1093/jac/5.2.219. [DOI] [PubMed] [Google Scholar]
- Peterson L. R., Gerding D. N. Prediction of cefazolin penetration in high- and low-protein-containing extravascular fluid: new method for performing simultaneous studies. Antimicrob Agents Chemother. 1978 Oct;14(4):533–538. doi: 10.1128/aac.14.4.533. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Peterson L. R., Hall W. H., Zinneman H. H., Gerding D. N. Standardization of a preparative ultracentrifuge method for quantitative determination or protein binding of seven antibiotics. J Infect Dis. 1977 Dec;136(6):778–783. doi: 10.1093/infdis/136.6.778. [DOI] [PubMed] [Google Scholar]
- Van Etta L. L., Fasching C. E., Peterson L. R., Gerding D. N. Comparison study of the kinetics of ceftizoxime penetration into extravascular spaces with known surface area/volume ratio in vitro and in vivo in rabbits. Antimicrob Agents Chemother. 1983 Jan;23(1):49–53. doi: 10.1128/aac.23.1.49. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Van Etta L. L., Peterson L. R., Fasching C. E., Gerding D. N. Effect of the ratio of surface area to volume on the penetration of antibiotics in to extravascular spaces in an in vitro model. J Infect Dis. 1982 Sep;146(3):423–428. doi: 10.1093/infdis/146.3.423. [DOI] [PubMed] [Google Scholar]