Skip to main content
NCBI home page
Antimicrobial Agents and Chemotherapy logoLink to Antimicrobial Agents and Chemotherapy
. 1974 Aug;6(2):124–135. doi: 10.1128/aac.6.2.124

Butirosin Compared with Gentamicin In Vitro and In Vivo

C L Heifetz 1, J A Chodubski 1, I A Pearson 1, C A Silverman 1, M W Fisher 1
PMCID: PMC444617  PMID: 15828182

Abstract

Butirosin (BTN) (P. W. K. Woo, G. L. Coffey, H. W. Dion, S. A. Fusari, and G. D. Senos, U. S. Patent 3,541,078, 1970) is a new aminoglycoside antibiotic notably active against opportunist bacterial species within Pseudomonas, Klebsiella, Enterobacter, Serratia, and Proteus. Numerous comparative tests were carried out with BTN and gentamicin (GTM) in vitro and in experimental infections in mice. BTN was more active in Mueller-Hinton broth than in agar, but its activity was lessened at acid pH or under anaerobiosis, as has been observed with other aminoglycosides. In standard agar diffusion tests, inhibition zones greater than 12 mm around 30-μg BTN disks generally denoted susceptibility, equivalent to minimal inhibitory concentrations [Formula: see text] 25 μg/ml. Cross-resistance between BTN and GTM occurred in a variable manner, with a number of bacterial strains strongly resistant to GTM being moderately susceptible to BTN. In mice, after a single subcutaneous injection, absorption of both antibiotics was rapid, with peak serum levels occurring in 15 min; this was followed by rapid elimination with estimated serum half-lives of about 20 min for each. After peroral administration of high doses in mice, there was no appreciable absorption of BTN. Several tests were carried out to compare BTN and GTM with respect to minimal inhibitory concentrations in vitro, acute subcutaneous median mouse protective doses, peak serum levels at such doses, and the therapeutic ratios derived from acute median protective and lethal doses. Although GTM usually proved to be more potent antibacterially on a weight basis, observations on BTN indicated a superior effectiveness in terms of therapeutic ratios.

Full text

PDF
124

Selected References

These references are in PubMed. This may not be the complete list of references from this article.

  1. Barber M., Waterworth P. M. Activity of gentamicin against Pseudomonas and hospital Staphylococci. Br Med J. 1966 Jan 22;1(5481):203–205. doi: 10.1136/bmj.1.5481.203. [DOI] [PMC free article] [PubMed] [Google Scholar]
  2. Bauer A. W., Kirby W. M., Sherris J. C., Turck M. Antibiotic susceptibility testing by a standardized single disk method. Am J Clin Pathol. 1966 Apr;45(4):493–496. [PubMed] [Google Scholar]
  3. Darrell J. H., Waterworth P. M. Dosage of gentamicin for pseudomonas infections. Br Med J. 1967 May 27;2(5551):535–537. doi: 10.1136/bmj.2.5551.535. [DOI] [PMC free article] [PubMed] [Google Scholar]
  4. Finegold S. M., Sutter V. L. Susceptibility of gram-negative anaerobic bacilli to gentamicin and other aminoglycosides. J Infect Dis. 1971 Dec;124 (Suppl):S56–S58. doi: 10.1093/infdis/124.supplement_1.s56. [DOI] [PubMed] [Google Scholar]
  5. Fisher M. W., Devlin H. B., Gnabasik F. J. New immunotype schema for Pseudomonas aeruginosa based on protective antigens. J Bacteriol. 1969 May;98(2):835–836. doi: 10.1128/jb.98.2.835-836.1969. [DOI] [PMC free article] [PubMed] [Google Scholar]
  6. Garrod L. P., Waterworth P. M. Effect of medium composition on the apparent sensitivity of Pseudomonas aeruginosa to gentamicin. J Clin Pathol. 1969 Sep;22(5):534–538. doi: 10.1136/jcp.22.5.534. [DOI] [PMC free article] [PubMed] [Google Scholar]
  7. Gilbert D. N., Kutscher E., Ireland P., Barnett J. A., Sanford J. P. Effect of the concentrations of magnesium and calcium on the in-vitro susceptibility of Pseudomonas aeruginosa to gentamicin. J Infect Dis. 1971 Dec;124 (Suppl):S37–S45. doi: 10.1093/infdis/124.supplement_1.s37. [DOI] [PubMed] [Google Scholar]
  8. Heifetz C. L., Fisher M. W., Chodubski J. A., DeCarlo M. O. Butirosin, a new aminoglycosidic antibiotic complex: antibacterial activity in vitro and in mice. Antimicrob Agents Chemother. 1972 Aug;2(2):89–94. doi: 10.1128/aac.2.2.89. [DOI] [PMC free article] [PubMed] [Google Scholar]
  9. Hewitt W. L. Reflections on the clinical pharmacology of gentamicin. Acta Pathol Microbiol Scand B Microbiol Immunol. 1973;(Suppl):151–151. [PubMed] [Google Scholar]
  10. Howells J. D., Anderson L. E., Coffey G. L., Senos G. D., Underhill M. A., Vogler D. L., Ehrlich J. Butirosin, a new aminoglycosidic antibiotic complex: bacterial origin and some microbiological studies. Antimicrob Agents Chemother. 1972 Aug;2(2):79–83. doi: 10.1128/aac.2.2.79. [DOI] [PMC free article] [PubMed] [Google Scholar]
  11. Kirby W. M., Standiford H. C. Gentamicin: in vitro studies. J Infect Dis. 1969 Apr-May;119(4):361–363. doi: 10.1093/infdis/119.4-5.361. [DOI] [PubMed] [Google Scholar]
  12. Marymont J. H., Jr, Wentz R. M. Serial dilution antibiotic sensitivity testing with the microtitrator system. Am J Clin Pathol. 1966 May;45(5):548–551. doi: 10.1093/ajcp/45.5.548. [DOI] [PubMed] [Google Scholar]
  13. Meyers B. R., Hirschman S. Z. Pharmacologic studies on tobramycin and comparison with gentamicin. J Clin Pharmacol New Drugs. 1972 Aug-Sep;12(8):321–324. doi: 10.1002/j.1552-4604.1972.tb00174.x. [DOI] [PubMed] [Google Scholar]
  14. Price K. E., Chisholm D. R., Misiek M., Leitner F., Tsai Y. H. Microbiological evaluation of BB-K 8, a new semisynthetic aminoglycoside. J Antibiot (Tokyo) 1972 Dec;25(12):709–731. doi: 10.7164/antibiotics.25.709. [DOI] [PubMed] [Google Scholar]
  15. RUBENIS M., KOZIJ V. M., JACKSON G. G. LABORATORY STUDIES ON GENTAMICIN. Antimicrob Agents Chemother (Bethesda) 1963;161:153–156. [PubMed] [Google Scholar]
  16. Riff L. J., Jackson G. G. Pharmacology of gentamicin in man. J Infect Dis. 1971 Dec;124 (Suppl):S98–105. doi: 10.1093/infdis/124.supplement_1.s98. [DOI] [PubMed] [Google Scholar]
  17. Rodriguez V., Stewart D., Bodey G. P. Gentamicin sulfate distribution in body fluids. Clin Pharmacol Ther. 1970 Mar-Apr;11(2):275–281. doi: 10.1002/cpt1970112275. [DOI] [PubMed] [Google Scholar]
  18. SACKS L. E. A pH, gradient agar plate. Nature. 1956 Aug 4;178(4527):269–270. doi: 10.1038/178269a0. [DOI] [PubMed] [Google Scholar]
  19. Waitz J. A. Interrelationships between disk and tube dilution sensitivity tests for the aminoglycoside antibiotics gentamicin, kanamycin, sisomicin, and tobramycin. Antimicrob Agents Chemother. 1973 Oct;4(4):445–454. doi: 10.1128/aac.4.4.445. [DOI] [PMC free article] [PubMed] [Google Scholar]
  20. Waitz J. A., Moss E. L., Jr, Oden E. M., Wagman G. H., Weinstein M. J. Biological activity of Sch 14342, an aminoglycoside antibiotic coproduced in the gentamicin fermentation. Antimicrob Agents Chemother. 1972 Dec;2(6):464–469. doi: 10.1128/aac.2.6.464. [DOI] [PMC free article] [PubMed] [Google Scholar]
  21. Washington J. A., 2nd, Hermans P. E., Martin W. J. In vitro susceptibility of staphylococci and streptococci and influence of agar media on minimum inhibitory concentration. Mayo Clin Proc. 1970 Jul;45(7):527–535. [PubMed] [Google Scholar]
  22. Young L. S., Hewitt W. L. Activity of five aminoglycoside antibiotics in vitro against gram-negative bacilli and Staphylococcus aureus. Antimicrob Agents Chemother. 1973 Dec;4(6):617–625. doi: 10.1128/aac.4.6.617. [DOI] [PMC free article] [PubMed] [Google Scholar]
  23. Zimelis V. M., Jackson G. G. Activity of aminoglycoside antibiotics aganst Pseudomonas aeruginosa: specificity and site of calcium and magnesium antagonism. J Infect Dis. 1973 Jun;127(6):663–669. doi: 10.1093/infdis/127.6.663. [DOI] [PubMed] [Google Scholar]

Articles from Antimicrobial Agents and Chemotherapy are provided here courtesy of American Society for Microbiology (ASM)

RESOURCES