PubMed · 10744868
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S Bhatnagar, J Chandra. 1999. Ceftibuten.. https://pubmed.ncbi.nlm.nih.gov/10744868/
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A prospective, comparative, multicentre trial was performed to study the efficacy and safety of ceftibuten in respiratory and complicated urinary tract infections. Patients (n = 152) requiring parenteral 2nd or 3rd generation cephalosporine therapy were randomly assigned to continue parenteral therapy (Group A) or to receive oral ceftibuten 400 mg, or 9 mg/kgbw/day (Group B) from the 3.-5. days on. The patients, whose conditions have not improved significantly at day 3-5, were omitted from the study, so the number of evaluated patients was 131. In Group A, out of 59 patients 51 were clinically cured, the bacteriological eradication rate was 47/54. In Group B, out of 72 patients 67 were cured and 62 out of 66 pathogens were eradicated. The cost of step-down therapy was 44.3% less than the parenteral one. No adverse effect was observed that could surely be attributed to ceftibuten. According to these data, ceftibuten can be used in step-down therapy in respiratory and urinary tract infections requiring parenteral therapy at first and that offers a safe and less expensive therapeutic approach.
The responses of ten isolates of Enterobacteriaceae to ceftibuten exposure were monitored by measuring several parameters. Post-antibiotic effect (PAE), control-related effective regrowth time (CERT) and post-antibiotic sub-MIC effect (PA-SME) were determined by bacterial enumeration carried out either by impedance in combination with viable counting (IMP/VC) or by impedance in combination with bioluminescence (IMP/BIOL). Kill curves were carried out by bioluminescence, viable counting and direct microscopy and post-exposure morphology was established. Ceftibuten primarily provoked filamentation. Over 24 h, kill of up to 3.6 log10 was evident by viable counting and direct microscopy at and above the MIC. Minimal kill, of up to 0.26 log10, was shown by bioluminescence. PAE was found to be method dependent, with statistical differences established by Student's t-test. PAE values of up to 0.48 h and 1.47 h (by IMP/BIOL and IMP/VC respectively) were not concentration dependent above 1 x MIC. CERT values were not method dependent, with values of up to 1.71 h also showing a lack of concentration dependence above 1 x MIC. PA-SME may reflect the situation in vivo more accurately than either PAE or CERT. In PAE and CERT studies the antibiotic is eliminated almost immediately, whereas in vivo there is gradual decrease in antibiotic levels. These persisting levels are reflected more accurately by PA-SME. Compared with PAE and CERT, significantly longer values, of up to 7.27 h, were obtained by PA-SME, although this parameter was also found to be method dependent. The results of the PA-SME studies, which may be the most clinically relevant pharmacodynamic parameter, confirm the appropriateness of the current once- or twice-daily dosing schedules despite the lack of PAE.
The isomerization reactions of ceftibuten and ceftibuten-related compounds in aqueous solution were investigated to estimate the substitution effect on the isomerization reaction and identify the three proximal dissociation constants of ceftibuten kinetically from the pH-rate profiles. The isomerization reaction of ceftibuten-related compounds was influenced by the substituents near the double bond at the C7-side chain, and the electron-withdrawing substituent was found to increase the isomerization rate. Ceftibuten isomerized at the C7-side chain, and the isomerization rate was influenced by the dissociation of the C7-side chain carboxylic acid and aminothiazole in the acidic pH region. The dissociation constants of ceftibuten were assigned by comparing the isomerization rates of ceftibuten with its related compounds at various pH conditions, and the pKas 2.3, 3.2, and 4.5 were attributed to the 4-carboxylic acid, 7-carboxylic acid, and 7-aminothiazole, respectively.