Disease relevance of Cefzon

• Comparative kill and growth rates determined with cefdinir and cefaclor and with Streptococcus pneumoniae and beta-lactamase-producing Haemophilus influenzae [1].
• Five-day treatment with cefdinir is safe and effective therapy for GABHS pharyngitis [2].
• Ciprofloxacin-resistant Escherichia coli isolates (n = 1,858) from outpatient midstream urine specimens at 40 North American clinical laboratories in 2004 to 2005 were frequently resistant to ampicillin (79.8% of isolates) and trimethoprim-sulfamethoxazole (66.5%); concurrent resistance to cefdinir (9.0%) or nitrofurantoin (4.0%) was less common [3].
• On the basis of the concentrations in blister fluid and the in vitro MIC data, we estimated that cefdinir at 200 to 400 mg administered twice daily would be adequate to treat uncomplicated skin infections caused by Streptococcus pyogenes [4].
• In adults and adolescents, cefdinir is an effective treatment for both lower (acute bacterial exacerbations of chronic bronchitis [ABECB], community-acquired pneumonia) and upper (acute bacterial rhinosinusitis, streptococcal pharyngitis) respiratory tract infections, and uncomplicated skin infections [5].

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

• A multicenter, randomized, controlled, investigator-blind study was performed to evaluate the safety and efficacy of oral cefdinir versus oral penicillin V for the treatment of pharyngitis due to group A beta-hemolytic streptococci (GABHS) [2].
• Three hundred ninety-four patients, aged 6 months to 12 years, entered a multicenter, randomized, controlled, investigator-blind study comparing cefdinir, 7 mg/kg of body weight twice a day, with cephalexin, 10 mg/kg four times a day, each given for 10 days [9].
• The efficacy of CS-834, a novel oral carbapenem, was assessed by using a murine model of pneumonia caused by penicillin-susceptible and penicillin-resistant Streptococcus pneumoniae and was compared with those of oral cephems, i.e., cefteram pivoxil, cefpodoxime proxetil, cefdinir, and cefditoren pivoxil [10].
• The in vivo activity of telithromycin against erythromycin A- and penicillin G-resistant Streptococcus pneumoniae was superior to that of azithromycin, clarithromycin, cefdinir, and levofloxacin [11].
• Eight newer orally administered cephems (cefdinir, cefetamet, cefixime, cefpodoxime, cefprozil, ceftibuten, cefuroxime, and loracarbef) were tested against 100 clinical strains of Morganella morganii to determine the extent of serious interpretive very major (false-susceptible) errors when current criteria for the disk diffusion test are applied [12].

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

• Furthermore, cefdinir inhibited LACL generation in cell-free systems consisting of H2O2, NaI, and either horseradish peroxidase or a myeloperoxidase-containing neutrophil extract [6].
• In patients taking 300 mg of cefdinir, the median concentrations of cefdinir were 2.00 mg/L (range 1.40-8.00) in serum, 0.78 mg/L (range 0-1.33) in bronchial mucosa, and 0.29 mg/L (range 0-4.73) in ELF [16].
• A microbiological assay for cefdinir was performed in serum, bronchial mucosa, ELF and alveolar macrophages [16].
• Cefdinir did not penetrate macrophages [16].
• CONCLUSION: Empiric therapy with cefdinir appears to be a reasonable choice for patients with uncomplicated urinary tract infection in whom cephalosporin treatment is indicated [17].

Associations of Cefzon with other chemical compounds

• The in vitro antibacterial activities of LB 10827, a new oral cephalosporin, against common respiratory tract pathogens were compared with those of six beta-lactams (cefdinir, cefuroxime, cefprozil, penicillin G, amoxicillin-clavulanate, and ampicillin), two quinolones (trovafloxacin and ciprofloxacin), and one macrolide (clarithromycin) [18].
• Captopril increased the cefdinir half-life from 0.62 +/- 0.17 to 2.92 +/- 0.95 h [15].
• Comparative in vitro activity of telithromycin (HMR 3647), three macrolides, amoxycillin, cefdinir and levofloxacin against gram-positive clinical isolates in Japan [19].
• Patients 6 months to 12 years of age were randomized in a 1:1:1 ratio to receive cefdinir 14 mg/kg once-daily, cefdinir 7 mg/kg b.i.d., or amoxicillin/CA 13.3 mg/kg t.i.d. Test-of-cure was determined 11 to 16 days posttherapy [20].
• The eradication rates of S pyogenes, determined 4 to 9 days after completion of therapy, were 94.3% in the cefdinir QD group, 94.3% in the cefdinir BID group, and 70.0% in the penicillin V group (95% confidence interval [CI] 17.6%-30.9%, P < 0.001 for cefdinir QD vs penicillin; CI 17.5%-30.9%, P < 0.001 for cefdinir BID vs penicillin) [21].

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].

References