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Chemical Compound Review

AG-H-77184     (6R,7S)-7-[[2-(2-amino-1,3- thiazol-4-yl)-2...

Synonyms: KBioGR_001651, KBioSS_002329, SPBio_001610, CCG-101138, AC1O4QTU, ...
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Disease relevance of Cefzon


Psychiatry related information on Cefzon

  • Based on its twice-a-day dosage and shorter course of therapy, leading to potentially greater patient compliance, cefdinir may be considered for use in the treatment of pharyngitis caused by GABHS [2].

High impact information on Cefzon

  • The LACL response to opsonized zymosan in cytochalasin B-treated neutrophils was, however, inhibited by cefdinir [6].
  • Taken together, these data strongly suggest that cefdinir directly inhibits the activity of myeloperoxidase-containing neutrophil extract released into the extracellular medium during neutrophil stimulation by soluble mediators, but has no effect on that released into the phagolysosome during phagocytosis [6].
  • Spontaneous and FMLP-induced neutrophil degranulation, assessed by lysozyme and beta-glucuronidase release, were not modified by cefdinir [6].
  • Core tonsillar cultures were obtained from 40 children with recurrent tonsillitis treated with either penicillin or cefdinir [7].
  • For most of the isolates with a mosaic PBP 2, the cefixime MICs were > or =0.5 microg/ml and the cefdinir MICs were > or =1 microg/ml [8].

Chemical compound and disease context of Cefzon


Biological context of Cefzon

  • The pharmacokinetics of cefdinir were investigated in six hemodialysis patients [13].
  • Cefdinir is stable to hydrolysis by commonly occurring plasmid-mediated beta-lactamases and retains good activity against beta-lactamase-producing strains of H. influenzae and M. catarrhalis [5].
  • This resulted in a lower AUC value than expected as well as a smaller fraction of cefdinir excreted unchanged at a dose of 600 mg [4].
  • The excretion ratio (ER; the renal clearance corrected for the fraction unbound and glomerular filtration rate) for cefdinir was 5.94, a value indicating net renal tubular secretion [14].
  • It is concluded that captopril and quinapril (and/or their metabolites) have a major impact on the disposition of cefdinir in rats, probably by competition at the plasma protein-binding level and at the tubular anionic carrier level [15].

Anatomical context of Cefzon


Associations of Cefzon with other chemical compounds


Gene context of Cefzon

  • Cefdinir appeared highly stable to the TEM-1 and SHV-1 beta-lactamases with only relatively minor degrees of hydrolysis being seen with TEM-3, -5 and -9 [22].
  • The effects of two kinds of oral cephalosporins, cefixime and cefdinir, on cytochrome P450 (CYP) activities in human hepatic microsomes were investigated [23].
  • The present study was undertaken to investigate the interaction of anionic cephalosporins (cefixime, ceftibuten, and cefdinir) with the renal peptide transporter (PEPT 2) and the intestinal peptide transporter (PEPT 1) using four different experimental model systems [24].
  • Clinical cure rates for infections caused by methicillin-susceptible (MSSA) and methicillin-resistant (MRSA) Staphylococcus aureus were 93% (37/40) and 92% (35/38) for cefdinir vs. 91% (29/32) and 90% (37/41) for cephalexin (p > 0.999 comparing treatment groups for MSSA; p > 0.999 for MRSA) [25].
  • In vitro evaluation of cefdinir (FK482), a new oral cephalosporin with enhanced antistaphylococcal activity and beta-lactamase stability [26].

Analytical, diagnostic and therapeutic context of Cefzon

  • Plasma cefdinir concentrations were measured by liquid chromatography, and the data were analyzed by a noncompartmental method [15].
  • Two randomized, investigator-blind, multicenter trials (one in the United States and one in Europe) compared two dosage regimens of cefdinir (600 mg once a day for 10 days and 300 mg twice a day for 10 days) to amoxicillin-clavulanate (A-C) (500 mg three times a day for 10 days) for adult and adolescent patients with ACABS [27].
  • The fractional removal of cefdinir by hemodialysis was 61% [13].
  • The pharmacokinetics and suction-induced blister fluid penetration of cefdinir following single oral administrations of 200, 300, 400, and 600 mg were studied in 16 healthy young male volunteers according to a Latin square design [4].
  • Finally, three groups of four or five rats each were set up as described above, but the cefdinir dose was 20 mg/kg and the animals were sacrificed 1 h after drug injection to collect blood to determine the unbound cefdinir fraction (fu) by ultrafiltration [15].


  1. Comparative kill and growth rates determined with cefdinir and cefaclor and with Streptococcus pneumoniae and beta-lactamase-producing Haemophilus influenzae. Yourassowsky, E., Van der Linden, M.P., Crokaert, F. Antimicrob. Agents Chemother. (1992) [Pubmed]
  2. Five-day cefdinir treatment for streptococcal pharyngitis. Cefdinir Pharyngitis Study Group. Tack, K.J., Henry, D.C., Gooch, W.M., Brink, D.N., Keyserling, C.H. Antimicrob. Agents Chemother. (1998) [Pubmed]
  3. Fluoroquinolone-resistant urinary isolates of Escherichia coli from outpatients are frequently multidrug resistant: results from the North American Urinary Tract Infection Collaborative Alliance-Quinolone Resistance study. Karlowsky, J.A., Hoban, D.J., Decorby, M.R., Laing, N.M., Zhanel, G.G. Antimicrob. Agents Chemother. (2006) [Pubmed]
  4. Suction-induced blister fluid penetration of cefdinir in healthy volunteers following ascending oral doses. Richer, M., Allard, S., Manseau, L., Vallée, F., Pak, R., LeBel, M. Antimicrob. Agents Chemother. (1995) [Pubmed]
  5. Cefdinir: a review of its use in the management of mild-to-moderate bacterial infections. Perry, C.M., Scott, L.J. Drugs (2004) [Pubmed]
  6. Cefdinir (CI-983), a new oral amino-2-thiazolyl cephalosporin, inhibits human neutrophil myeloperoxidase in the extracellular medium but not the phagolysosome. Labro, M.T., el Benna, J., Charlier, N., Abdelghaffar, H., Hakim, J. J. Immunol. (1994) [Pubmed]
  7. Efficacy of penicillin versus cefdinir in eradication of group A streptococci and tonsillar flora. Brook, I., Foote, P.A. Antimicrob. Agents Chemother. (2005) [Pubmed]
  8. Emergence and spread of Neisseria gonorrhoeae clinical isolates harboring mosaic-like structure of penicillin-binding protein 2 in Central Japan. Ito, M., Deguchi, T., Mizutani, K.S., Yasuda, M., Yokoi, S., Ito, S., Takahashi, Y., Ishihara, S., Kawamura, Y., Ezaki, T. Antimicrob. Agents Chemother. (2005) [Pubmed]
  9. Study of use of cefdinir versus cephalexin for treatment of skin infections in pediatric patients. The Cefdinir Pediatric Skin Infection Study Group. Tack, K.J., Keyserling, C.H., McCarty, J., Hedrick, J.A. Antimicrob. Agents Chemother. (1997) [Pubmed]
  10. Efficacy of CS-834 against experimental pneumonia caused by penicillin-susceptible and -resistant Streptococcus pneumoniae in mice. Fukuoka, T., Kawada, H., Kitayama, A., Koga, T., Kubota, M., Harasaki, T., Kamai, Y., Ohya, S., Yasuda, H., Iwata, M., Kuwahara, S. Antimicrob. Agents Chemother. (1998) [Pubmed]
  11. In vivo efficacy of telithromycin (HMR3647) against Streptococcus pneumoniae and Haemophilus influenzae. Okamoto, H., Miyazaki, S., Tateda, K., Ishii, Y., Yamaguchi, K. Antimicrob. Agents Chemother. (2001) [Pubmed]
  12. Interpretive accuracy of the disk diffusion method for testing newer orally administered cephalosporins against Morganella morganii. Biedenbach, D.J., Jones, R.N., Erwin, M.E. J. Clin. Microbiol. (1993) [Pubmed]
  13. Pharmacokinetic study of an oral cephalosporin, cefdinir, in hemodialysis patients. Hishida, A., Ohishi, K., Nagashima, S., Kanamaru, M., Obara, M., Kitada, A. Antimicrob. Agents Chemother. (1998) [Pubmed]
  14. Effects of organic anion, organic cation, and dipeptide transport inhibitors on cefdinir in the isolated perfused rat kidney. Lepsy, C.S., Guttendorf, R.J., Kugler, A.R., Smith, D.E. Antimicrob. Agents Chemother. (2003) [Pubmed]
  15. Pharmacokinetic interaction between cefdinir and two angiotensin-converting enzyme inhibitors in rats. Jacolot, A., Tod, M., Petitjean, O. Antimicrob. Agents Chemother. (1996) [Pubmed]
  16. Distribution of cefdinir, a third generation cephalosporin antibiotic, in serum and pulmonary compartments. Cook, P.J., Andrews, J.M., Wise, R., Honeybourne, D. J. Antimicrob. Chemother. (1996) [Pubmed]
  17. Cefdinir versus cefaclor in the treatment of uncomplicated urinary tract infection. Leigh, A.P., Nemeth, M.A., Keyserling, C.H., Hotary, L.H., Tack, K.J. Clinical therapeutics. (2000) [Pubmed]
  18. In vitro and In vivo activities of LB 10827, a new oral cephalosporin, against respiratory pathogens. Paek, K.S., Kim, M.Y., Lee, C.S., Youn, H. Antimicrob. Agents Chemother. (2000) [Pubmed]
  19. Comparative in vitro activity of telithromycin (HMR 3647), three macrolides, amoxycillin, cefdinir and levofloxacin against gram-positive clinical isolates in Japan. Okamoto, H., Miyazaki, S., Tateda, K., Ishii, Y., Yamaguchi, K. J. Antimicrob. Chemother. (2000) [Pubmed]
  20. Cefdinir vs. amoxicillin/clavulanic acid in the treatment of suppurative acute otitis media in children. Adler, M., McDonald, P.J., Trostmann, U., Keyserling, C., Tack, K. Pediatr. Infect. Dis. J. (2000) [Pubmed]
  21. Comparison of cefdinir and penicillin for the treatment of pediatric streptococcal pharyngitis. Nemeth, M.A., Gooch, W.M., Hedrick, J., Slosberg, E., Keyserling, C.H., Tack, K.J. Clinical therapeutics. (1999) [Pubmed]
  22. The in-vitro activity of cefdinir (FK482), a new oral cephalosporin. Wise, R., Andrews, J.M., Thornber, D. J. Antimicrob. Chemother. (1991) [Pubmed]
  23. Effect of cefixime and cefdinir, oral cephalosporins, on cytochrome P450 activities in human hepatic microsomes. Niwa, T., Shiraga, T., Hashimoto, T., Kagayama, A. Biol. Pharm. Bull. (2004) [Pubmed]
  24. Interaction of anionic cephalosporins with the intestinal and renal peptide transporters PEPT 1 and PEPT 2. Ganapathy, M.E., Prasad, P.D., Mackenzie, B., Ganapathy, V., Leibach, F.H. Biochim. Biophys. Acta (1997) [Pubmed]
  25. Cefdinir vs. cephalexin for mild to moderate uncomplicated skin and skin structure infections in adolescents and adults. Giordano, P.A., Elston, D., Akinlade, B.K., Weber, K., Notario, G.F., Busman, T.A., Cifaldi, M., Nilius, A.M. Current medical research and opinion (2006) [Pubmed]
  26. In vitro evaluation of cefdinir (FK482), a new oral cephalosporin with enhanced antistaphylococcal activity and beta-lactamase stability. Cohen, M.A., Joannides, E.T., Roland, G.E., Meservey, M.A., Huband, M.D., Shapiro, M.A., Sesnie, J.C., Heifetz, C.L. Diagn. Microbiol. Infect. Dis. (1994) [Pubmed]
  27. Comparative effectiveness and safety of cefdinir and amoxicillin-clavulanate in treatment of acute community-acquired bacterial sinusitis. Cefdinir Sinusitis Study Group. Gwaltney, J.M., Savolainen, S., Rivas, P., Schenk, P., Scheld, W.M., Sydnor, A., Keyserling, C., Leigh, A., Tack, K.J. Antimicrob. Agents Chemother. (1997) [Pubmed]
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