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Chemical Compound Review

AC1NUOUJ     (6R,7S)-7-[[(2E)-2-(2-amino- 1,3-thiazol-4...

Synonyms: 90712-47-3, Ammcgab methyl ester
 
 
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Disease relevance of LY097964

 

High impact information on LY097964

 

Chemical compound and disease context of LY097964

 

Biological context of LY097964

  • Two studies examining the bioavailability of cefetamet pivoxil in healthy male subjects were conducted [12].
  • The maximum cefetamet concentration in plasma (Cmax) and the area under the plasma cefetamet concentration-time profiles (AUC) in the BE, WI, and AF groups were 5.50 +/- 1.06, 5.47 +/- 1.4, and 6.57 +/- 0.93 micrograms/ml and 38.2 +/- 10.1, 35.7 +/- 11.9, and 42.8 +/- 6.8 micrograms.h/ml, respectively [13].
  • The pH-rate profiles for hydrolysis of cefetamet pivoxil were obtained at 333, 343, 353 and 363K [14].
  • The permeability coefficient of cefetamet was measured in E. coli C600 carrying a pUC18 plasmid derivative, in which the gene of a transferable cephamycinase (CMY-2) was cloned, whereas diffusion of cefixime and cefuroxime was measured in E. coli C600 harbouring the OXA-1 beta-lactamase gene [15].
 

Anatomical context of LY097964

  • Cefetamet pivoxil is also effective in the treatment of urinary tract infections, although further trials are required to define any comparative advantages over other oral agents [1].
  • During ingestion of S. aureus by granulocytes, the activity of cefetamet was equal to that found in the absence of cells [16].
  • Cefetamet was also more active against S. aureus ingested by monocytes than against bacteria in medium (ERmax 0.97 and 0.77 log/h, respectively) [16].
 

Associations of LY097964 with other chemical compounds

 

Gene context of LY097964

  • Furthermore, time-killing analyses at 4 x MIC demonstrated that cefetamet was bactericidal against beta-lactamase-producing H. influenzae, M. catarrhalis, and K. pneumoniae within 6 h and S. pneumoniae within 4 h [22].
  • Moderate resistance to cefetamet is observed only in strains producing either the TEM-3 or the TEM-4 enzyme, whereas the prevalence of the other enzymes is of no consequence for the activity of cefetamet [23].
  • Cefetamet pivoxil offers effective alternative oral therapy for outpatient treatment of community-acquired respiratory tract infections, with the advantage of improved activity against H. influenzae and increased beta-lactamase stability [1].
  • Two isolates showed intermediate susceptibility to cefixime (MIC 2 mg/L) but none was resistant to the new oral cephalosporin cefetamet or to the oral carbacephem loracarbef.(ABSTRACT TRUNCATED AT 250 WORDS)[24]
  • In this strain, cefetamet and cefixime shared the same inhibitory activity (MIC = 1 microgram/ml for both antibiotics) and the same affinity for PBP 3 (ID50 = 0.25 micrograms/ml) [15].
 

Analytical, diagnostic and therapeutic context of LY097964

References

  1. Cefetamet pivoxil. A review of its antibacterial activity, pharmacokinetic properties and therapeutic use. Bryson, H.M., Brogden, R.N. Drugs (1993) [Pubmed]
  2. Comparative clinical efficacy of cefetamet pivoxil in lower respiratory tract infection. Grassi, G.G. Drugs (1994) [Pubmed]
  3. Comparative in vitro antibacterial activities of two new oral cephalosporins, ceftetrame (Ro 19-5247) and cefetamet (Ro 15-8074). Chau, P.Y., Leung, Y.K., Ng, W.W., Arnold, K. Antimicrob. Agents Chemother. (1987) [Pubmed]
  4. Pharmacokinetics of cefetamet in plasma and skin blister fluid. Zimmerli, W., Sansano, S., Wittke, B. Antimicrob. Agents Chemother. (1996) [Pubmed]
  5. Penetration of cefetamet pivoxil and cefuroxime axetil into the maxillary sinus mucosa at steady state. Stoeckel, K., Harell, M., Dan, M. Antimicrob. Agents Chemother. (1996) [Pubmed]
  6. Stability in the presence of widespread beta-lactamases. A prerequisite for the antibacterial activity of beta-lactam drugs. Schito, G.C., Pesce, A., Debbia, E.A. Drugs (1994) [Pubmed]
  7. Cefetamet pivoxil vs cefaclor in the treatment of acute otitis media in children. Furman, S., Berkowicz, L., Dippenaar, J., Hellenberg, D.A., Montanus, M.S., Steinberg, A., Schall, R. Drugs (1994) [Pubmed]
  8. Different doses of cefetamet pivoxil (Ro 15-8075) in the treatment of acute uncomplicated gonococcal urethritis in men. Tio, T.T., Sindhunata, I.R., Wagenvoort, J.H., Michel, M.F., Stolz, E. Antimicrob. Agents Chemother. (1990) [Pubmed]
  9. In vitro activities of fleroxacin, cefetamet, ciprofloxacin, ceftriaxone, trimethoprim-sulfamethoxazole, and amoxicillin-clavulanic acid against rare members of the family Enterobacteriaceae primarily of human (clinical) origin. Hohl, P., Lüthy-Hottenstein, J., Zollinger-Iten, J., Altwegg, M. Antimicrob. Agents Chemother. (1990) [Pubmed]
  10. In vitro activities of new oral beta-lactams and macrolides against Campylobacter pylori. García-Rodríguez, J.A., García Sánchez, J.E., García García, M.I., García Sánchez, E., Muñoz Bellido, J.L. Antimicrob. Agents Chemother. (1989) [Pubmed]
  11. Cefetamet pivoxil in the treatment of pharyngitis/tonsillitis in children and adults. Guggenbichler, J.P. Drugs (1994) [Pubmed]
  12. Bioavailability of syrup and tablet formulations of cefetamet pivoxil. Ducharme, M.P., Edwards, D.J., McNamara, P.J., Stoeckel, K. Antimicrob. Agents Chemother. (1993) [Pubmed]
  13. Effects of timing of food and fluid volume on cefetamet pivoxil absorption in healthy normal volunteers. Tam, Y.K., Kneer, J., Dubach, U.C., Stoeckel, K. Antimicrob. Agents Chemother. (1990) [Pubmed]
  14. The influence of pH, temperature and buffers on the degradation kinetics of cefetamet pivoxil hydrochloride in aqueous solutions. Jelińska, A., Dobrowolski, L., Oszczapowicz, I. Journal of pharmaceutical and biomedical analysis. (2004) [Pubmed]
  15. PBP binding and periplasmic concentration as determinants of the antibacterial activities of three new oral cephalosporins in Escherichia coli. Cornaglia, G., Ligozzi, M., Bauernfeind, A., Satta, G., Fontana, R. New Microbiol. (1994) [Pubmed]
  16. The influence of human granulocytes and monocytes on the antibacterial activity of cefetamet against Staphylococcus aureus. van den Broeck, P.J., Seymonsbergen, E.M. J. Antimicrob. Chemother. (1995) [Pubmed]
  17. Pharmacokinetics of cefetamet pivoxil (Ro 15-8075) with ascending oral doses in normal healthy volunteers. Tam, Y.K., Kneer, J., Dubach, U.C., Stoeckel, K. Antimicrob. Agents Chemother. (1989) [Pubmed]
  18. Influence of antacid and ranitidine on the pharmacokinetics of oral cefetamet pivoxil. Blouin, R.A., Kneer, J., Ambros, R.J., Stoeckel, K. Antimicrob. Agents Chemother. (1990) [Pubmed]
  19. In vitro activity of ceftriaxone, cefetamet (Ro 15-8074), ceftetrame (Ro 19-5247; T-2588), and fleroxacin (Ro 23-6240; AM-833) versus Neisseria gonorrhoeae and Haemophilus ducreyi. Le Saux, N.M., Slaney, L.A., Plummer, F.A., Ronald, A.R., Brunham, R.C. Antimicrob. Agents Chemother. (1987) [Pubmed]
  20. Parenteral-oral switch in the management of paediatric pneumonia. Dagan, R., Syrogiannopoulos, G., Ashkenazi, S., Engelhard, D., Einhorn, M., Gatzola-Karavelli, M., Shalit, I., Amir, J. Drugs (1994) [Pubmed]
  21. Effects of cefaclor, cefetamet and Ro 40-6890 on inflammatory responses of human granulocytes. Scheffer, J., Knöller, J., Cullmann, W., König, W. J. Antimicrob. Chemother. (1992) [Pubmed]
  22. Cefetamet pivoxil: comparable evaluation with other orally available antibiotics against selected species of respiratory pathogens. Speciale, A., Caccamo, F., Blandino, G., Giacchi, G.T., Aleo, G., Nicoletti, G. Chemotherapy. (1996) [Pubmed]
  23. The threat of resistance to the new oral cephalosporins. Cullmann, W. Chemotherapy. (1992) [Pubmed]
  24. The antimicrobial susceptibility of Moraxella catarrhalis isolated in England and Scotland in 1991. Fung, C.P., Powell, M., Seymour, A., Yuan, M., Williams, J.D. J. Antimicrob. Chemother. (1992) [Pubmed]
  25. Pharmacokinetics of intravenous cefetamet and oral cefetamet pivoxil in children. Hayton, W.L., Walstad, R.A., Thurmann-Nielsen, E., Kufaas, T., Kneer, J., Ambros, R.J., Rugstad, H.E., Monn, E., Bodd, E., Stoeckel, K. Antimicrob. Agents Chemother. (1991) [Pubmed]
  26. Cefetamet pivoxil clinical pharmacokinetics. Blouin, R.A., Stoeckel, K. Clinical pharmacokinetics. (1993) [Pubmed]
 
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