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PubMed1989

Transport characteristics of ceftibuten (7432-S), a new oral cephem, in rat intestinal brush-border membrane vesicles: proton-coupled and stereoselective transport of ceftibuten.

The transport characteristics of ceftibuten in rat intestinal brush-border membrane vesicles were investigated by a rapid filtration technique. Ceftibuten uptake was markedly stimulated by an inwardly directed H+ gradient (pH 7.5 inside, pH 5.5 outside) in comparison with that in the absence of a H+ gradient. The uptake at 30 sec was four times greater than that observed at equilibrium (overshoot phenomenon), while the H+ gradient-stimulated uptake of ceftibuten was markedly reduced in the presence of FCCP, a protonophore. These results suggested H+-coupled uphill transport of ceftibuten. In contrast, an inwardly directed Na+ gradient had no effect on ceftibuten uptake. The valinomycin-induced K+ diffusion potential (inside positive) significantly stimulated the ceftibuten uptake, suggesting net transfer of the negative charge. In contrast to the cis-isomer ceftibuten, the trans isomer of ceftibuten is not readily absorbed from the intestine, and its uptake was found not to be affected by a H+ gradient. Since the lipophilicity of the trans isomer is similar to that of ceftibuten, the uptake process appears to be stereoselective. The initial uptake of ceftibuten and its analogue cefaclor was concentration dependent under a H+ gradient. The apparent Km value was 0.2 mM for ceftibuten and 3.0 mM for cefaclor.

4,4'-Diisothiocyanostilbene-2,2'-Disulfonic Acid↗
PubMed1995

Multinational multicenter controlled trial comparing ceftibuten with cefaclor for the treatment of acute otitis media. Members of the Ceftibuten Otitis Media International Study Group.

A randomized, controlled, single blind clinical trial was conducted in children with acute otitis media to evaluate the safety and efficacy of a 10-day course of therapy with ceftibuten 9 mg/kg taken as a single daily dose, up to a maximum daily dose of 400 mg, compared with cefaclor 40 mg/kg/day in three divided doses, up to a maximum of 1 g/day. Patients were evaluated any time from 1 to 3 days after completion of therapy (posttreatment follow-up). A total of 154 patients (106 ceftibuten, 48 cefaclor) were evaluable for efficacy. Clinical success as determined by resolution (cure) or improvement of signs and symptoms of infection were seen in 89 and 88% of patients treated with ceftibuten and cefaclor, respectively, at the posttreatment follow-up visit. At the extended follow-up visit (any time from 2 to 4 weeks after completion of therapy), clinical success was sustained in 88 and 82% of the ceftibuten-treated and cefaclor-treated patients, respectively. A total of 391 patients (264 ceftibuten, 127 cefaclor) were included in the safety analysis. Treatment-related adverse experiences occurred in 8% of ceftibuten-treated patients and 14% of cefaclor-treated patients. All were mild or moderate and the majority were gastrointestinal. There were no deaths or serious adverse events. The results of this study suggest that ceftibuten is an effective and well-tolerated alternative to other antibiotic therapies for the treatment of children with acute otitis media.

Acute Disease↗
PubMed1994

Susceptibility of respiratory and urinary pathogens to ceftibuten and other comparative drugs: results of an Italian multicenter survey. The Italian Ceftibuten Study Group.

A survey aimed at assessing the ability of ceftibuten, a new oral third-generation cephalosporin, to eradicate in vitro selected bacterial pathogens was conducted in 1991 in 17 microbiology laboratories evenly distributed in Italy. Over 8700 organisms collected from in- and outpatients affected mainly by respiratory and urinary tract infections were analyzed. This collection of bacteria did not include staphylococci, enterococci, Pseudomonas and other oxidative species naturally refractory to the action of most antibiotics employed. Susceptibility to ceftibuten, cefaclor, cefuroxime, amoxicillin, amoxicillin-clavulanate, cotrimoxazole and erythromycin was assessed using a standardized agar-diffusion method. Production of beta-lactamases was confirmed by the nitrocefin test. Among the microorganisms studied E. coli (32.1%) prevailed, followed by P. mirabilis (17.1%), K. pneumoniae (10.9%), S. pyogenes (6.6%), E. cloacae (5.1%), Serratia spp. (4.5%), Enterobacter spp. (4.2%), H. influenzae (3.6%), S. pneumoniae (2.2%) and M. catarrhalis (2%). Within this group of pathogens amoxicillin resistance, often mediated by synthesis of beta-lactamases, was widely diffused (46.2%). The overall inhibitory activity of the drugs tested decreased as follows: ceftibuten (90.4%), cefuroxime (80.4%), amoxicillin-clavulanate (77.4%), cotrimoxazole (75.3%), cefaclor (72.6%), amoxicillin (53.8%) and erythromycin (32.8%). When the efficacy of the antibiotics was assessed against the collection of respiratory isolates producing beta-lactamases only ceftibuten maintained the same overall potency manifested against the general population while the comparative agents were far less effective. The results of this national survey indicate that, given the low incidence of resistance among the most prevalent causative agents of respiratory and urinary tract infections, ceftibuten can be safely used at present in the empiric therapy of these conditions especially when they occur in community settings.

Ceftibuten↗
PubMed1995

Ceftibuten vs. penicillin V in group A beta-hemolytic streptococcal pharyngitis. Members of the Ceftibuten Pharyngitis International Study Group.

The efficacy and safety of a 10-day course of ceftibuten oral suspension (9 mg/kg once daily) were compared with those of penicillin V (25 mg/kg/day in 3 divided doses) in children 3 to 18 years old treated for symptomatic pharyngitis and scarlet fever caused by group A beta-hemolytic streptococci (Streptococcus pyogenes). The study was prospective, randomized, multicenter and investigator-blinded; patients were randomized in a 2:1 ratio (ceftibuten:penicillin V). Overall clinical success (cure/improvement) at the primary end point of treatment (5 to 7 days posttherapy) was achieved in 97% (285 of 294) of ceftibuten-treated patients vs. 89% (117 of 132) of penicillin V-treated patients (P < 0.01). Elimination of infecting streptococci 5 to 7 days posttherapy was achieved in 91% (267 of 294) of ceftibuten-treated patients vs 80% (105 of 132) of penicillin V-treated patients (P < 0.01). A significant rise in anti-streptolysin O or anti-DNase B was observed in approximately 30% of patients in both treatment groups. No patient developed rheumatic fever or nephritis. Treatment-related adverse events were similar between the two groups; mild vomiting (2%) was most frequently reported. These data suggest that once daily ceftibuten is as safe as and more effective than three times daily penicillin V for the treatment of group A beta-hemolytic streptococcal pharyngitis.

Adolescent↗
PubMed1995

Multicenter controlled trial comparing ceftibuten with amoxicillin/clavulanate in the empiric treatment of acute otitis media. Members of the Ceftibuten Otitis Media United States Study Group.

The efficacy and safety of ceftibuten (9 mg/kg daily for 10 days) were compared with those of amoxicillin/clavulanate (Augmentin 40 mg/kg/day given every 8 hours for 10 days) in the empiric treatment of acute otitis media in children. This was a multicenter, investigator-blinded study with 1:1 randomization. Overall clinical response and signs and symptoms of otitis were collected prospectively pretreatment, 3 to 5 days during treatment, 1 to 3 days post-treatment and at 2- to 4-week follow-up. In addition to spontaneous reports of other adverse events, gastrointestinal adverse events were prospectively elicited at each visit. Two hundred ninety-six patients (146 ceftibuten and 150 amoxicillin/clavulanate) were treated with at least 1 dose of study medication. Compliance with dosing was assessable with weight of drug consumed in 127 patients in each treatment group. Five percent (6 of 127) of ceftibuten patients and 11% (14 of 127) of amoxicillin/clavulanate patients received < 80% of prescribed drug (P = 0.10) and were therefore not valid. Two hundred twenty-two patients (121 ceftibuten and 101 amoxicillin/clavulanate) received a minimum of 80% of prescribed medication and were compliant with the protocol. Ceftibuten and amoxicillin/clavulanate groups were comparable both for demographic variables and for baseline signs and symptoms.(ABSTRACT TRUNCATED AT 250 WORDS)

Acute Disease↗
PubMed1994

Ceftibuten pharmacokinetics and pharmacodynamics. Focus on paediatric use.

Ceftibuten is an extended-spectrum, cephem antimicrobial agent formulated for oral administration. Ceftibuten is absorbed by carrier-mediated processes and passive diffusion. The absorption of ceftibuten is described adequately by a first-order process. Following oral administration, peak serum ceftibuten concentrations are reached within 2 to 3 hours. Although the absolute bioavailability of ceftibuten in humans is not known, its relative bioavailability indicates that there is relatively rapid and complete absorption of the drug. Administration of ceftibuten with food may decrease the rate of absorption and, in the case of high fat meals, may decrease the extent of absorption by approximately 20 to 30%. The results of limited studies indicate that the drug distributes well into various body tissues and fluids, with relatively high concentrations being achieved in organs that receive a significant portion of the cardiac output. In adults with normal renal function or chronic renal failure, the apparent volume of distribution (Vd/F) for ceftibuten ranges from 0.2 to 0.4 L/kg and the total plasma clearance (CL/F) ranges from approximately 61 to 75 ml/min (3.7 to 4.5 L/h). Studies of ceftibuten elimination in adults have demonstrated positive linear correlation between CL/F and creatinine clearance. Following administration of a single dose of ceftibuten, approximately 67 to 94% of the drug has been recovered in the urine unchanged. The elimination half-life (t1/2 beta) of ceftibuten in adults with normal renal function is approximately 2.5 hours. Significant accumulation of ceftibuten does not occur with repeated administration. Despite the fact that the mean time taken to achieve maximal serum concentration (tmax) [1.1 to 2 hours] and t1/2 beta (2.1 hours) following administration of a single dose of ceftibuten to infants and children were similar to values previously reported in adults, the Vd/F (0.42 L/kg) and CL/F (3.1 ml/h/kg) were considerably greater in children younger than 5 years. Additionally, the apparent nonrenal clearance of ceftibuten in paediatric patients (52% of CL/F) was greater than reported for adults (approximately 32% of CL/F) with normal renal function. Thus, developmental differences appear to affect the pharmacokinetic profile of ceftibuten. Ceftibuten has a wide spectrum of antimicrobial activity against both Gram-positive and Gram-negative pathogens, and is stable to hydrolysis by a large number of beta-lactamases. Notable exceptions with regard to the Gram-positive spectrum for ceftibuten include relative or documented resistance for most strains of Listeria, Staphylococcus aureus, S. epidermidis, penicillin-resistant strains of Streptococcus pneumonia and S. enterococcus.(ABSTRACT TRUNCATED AT 400 WORDS)

Adolescent↗
PubMed1994

Multiple-dose pharmacokinetics of ceftibuten after oral administration to healthy volunteers.

The pharmacokinetics of ceftibuten in plasma and urine were investigated after oral administration. Twelve healthy subjects were treated orally twice daily with 400 mg of the drug for 7 days; on day 8, the subjects received a last dose of 400 mg of ceftibuten. Ceftibuten and its metabolite, the trans isomer of ceftibuten, were assayed in plasma and urine by a specific HPLC method with UV detection. Ceftibuten was rapidly absorbed, as evidenced by the mean time to the maximum observed cis-ceftibuten concentration of 2.4 h. To describe the drug intake process, a Weibull model was used. For the metabolite, the mean time to maximum concentration in plasma was 3.25 h. Mean values for the terminal half-life in plasma were 2.17 h for cis-ceftibuten and 3.19 h for trans-ceftibuten. The overall elimination half-life, tmax, and total and renal clearances of cis-ceftibuten were invariant with respect to duration of dosing. The area under the plasma concentration versus time curve from 0 to infinity and the Cmax of this drug were significantly higher on day 8 than the values predicted from the elimination half-life computed on day 1 of treatment and the dosing interval. The pharmacokinetic parameters of trans-ceftibuten were invariant with respect to duration of dosing. Ceftibuten was well tolerated; there were no clinically significant adverse clinical events. The results from the present study indicate that the levels of cis-ceftibuten in plasma as well as in urine remain above the MICs for susceptible organisms over the dosing interval.

Administration, Oral↗
PubMed1995

Postantibiotic effect of ceftibuten on respiratory pathogens.

The postantibiotic effect (PAE) of ceftibuten, a novel beta-lactamase-stable cephem, was determined for Streptococcus pyogenes, Streptococcus pneumoniae, Haemophilus influenzae and Moraxella catarrhalis. The ceftibuten PAE after a 2-hour exposure to 2 micrograms/ml (4 x minimum inhibitory concentration) for S. pyogenes was 2.7 to > 10 hours. The PAE for S. pneumoniae after a 2-hour exposure to 15 micrograms/ml, concentrations that are achieved in man after usual therapeutic doses, was 1.1 to 3.4 hours and the PAE for H. influenzae was 1 to 1.1 hours. M. catarrhalis had a PAE of 1.5 to 1.8 hours after exposure to 15 micrograms/ml of ceftibuten. The ceftibuten PAE was not affected by serum. The ceftibuten PAE was prolonged by exposure to a sub-minimum inhibitory concentration concentration of ceftibuten as would occur in the clinical situation. The PAE of ceftibuten was not affected by the copresence of erythromycin as would occur when treating infections in which atypical organisms are suspected. There was no correlation between bacterial reduction in colony-forming units and the duration of PAE. A level of 6 micrograms/ml of ceftibuten had a similar bacterial killing activity compared with a 6-hour exposure to 15 micrograms/ml of ceftibuten against S. pneumoniae, H. influenzae and M. catarrhalis. This study suggests that ceftibuten can be administered orally, once daily in an adult dose of 400 mg or a pediatric dose of 9 mg/kg, to treat respiratory infections caused by the most common pathogens.

Bacterial Infections↗
PubMedDate not supplied

Randomized comparison of once-daily ceftibuten and twice-daily clarithromycin in the treatment of acute exacerbation of chronic bronchitis.

In an evaluator-blind, parallel-group, multicenter study, the efficacy and tolerability of ceftibuten 400 mg capsules once daily were compared with clarithromycin 500 mg twice daily for 7-14 days in the treatment of 309 patients with acute exacerbation of chronic bronchitis (AECB). Clinical (n = 262) and microbiological (n = 71) assessments were conducted before treatment, during days 4-6 of treatment, and at 0-6 and 7-21 days after treatment. Clinical efficacy success rates (cure/improvement) at the end of treatment (0-6 days) were 91.0% for ceftibuten and 93.0% for clarithromycin. In the intent-to-treat population, the overall clinical assessment showed a success rate of 77.6% (121/156) in the ceftibuten group and 78.4% (120/153) in the clarithromycin group (95% confidence interval, -10.8 to +9.0%). One patient in each of the ceftibuten and clarithromycin groups had a microbiological relapse and became a treatment failure. The overall success rate was 84.3% for ceftibuten and 86.7% for clarithromycin (C.I. -11.7%, +6.9). Overall eradication of the target pathogens (Haemophilus influenzae, Moraxella catarrhalis, and Streptococcus pneumoniae) was 84.8% for ceftibuten and 89.5% for clarithromycin. Eradication rates for ceftibuten at 0-6 days post treatment were 95.2% (H. influenzae), 87.5% (M. catarrhalis), and 100% (S. pneumoniae), compared with 85.7%, 100% and 100%, respectively, for clarithromycin. Significantly fewer patients in the ceftibuten group experienced treatment-related adverse events than in the clarithromycin group (5.3 vs 21.9%; p < 0.001). This difference was due to a large number of patients in the clarithromycin group reporting taste perversion (12.6%) or gastrointestinal adverse events (9.9%). Given its tolerability and efficacy profiles, and the advantage of once-daily administration, ceftibuten provides a rational alternative for the treatment of AECB.

Acute Disease↗
PubMedDate not supplied

Comparison of ceftibuten once daily and amoxicillin-clavulanate three times daily in the treatment of acute exacerbations of chronic bronchitis.

In medical practice, antibiotics are generally given empirically for the treatment of acute exacerbations of chronic bronchitis (AECB). To be effective, antibiotic therapy should be broad in spectrum, and it should also cover the common beta-lactamase-producing pathogens. In this multicenter, randomized, investigator-masked study, 469 patients with AECB were randomized (in a ratio of 2:1) to receive 400-mg oral ceftibuten capsules once daily or 500-mg amoxicillin-clavulanate tablets three times daily for 5 to 15 days. Patients receiving ceftibuten were further divided into those who took the capsule with a meal (fed) and those who took the capsule 1 hour before a meal (fasted). Clinical and microbiologic responses were evaluated after treatment at 0 to 6 days (end of treatment) and 7 to 21 days (follow-up). Overall clinical success was determined by cure/improvement of signs and symptoms of AECB at the end of treatment and at follow-up. Overall microbiologic assessment was graded as eradication, persistence, relapse, reinfection, colonization, superinfection, or unassessable. Tolerability was evaluated by grading observed adverse events. The mean duration of treatment was 10.4 days for patients who received ceftibuten and 10.1 days for patients who received amoxicillin-clavulanate. A total of 252 patients receiving ceftibuten and 117 patients receiving amoxicillin-clavulanate were evaluable for clinical efficacy, and 55 patients were evaluable for microbiologic response. Both treatments improved the signs and symptoms of bronchitis, and overall clinical success rates were equivalent for patients treated with ceftibuten (211 of 252 [84%]) and amoxicillin-clavulanate (93 of 117 [79%]) (95% confidence interval [CI], -4.5% to 13.6%). Overall microbiologic eradication rates were also similar for patients treated with ceftibuten (36 of 37 [97%]) and amoxicillin-clavulanate (12 of 14 [86%]) (95% CI, -5.2% to 21.2%). The most frequently reported treatment-related adverse events were gastrointestinal disturbances, which occurred in 15% (47 of 316) and 24% (36 of 152) of patients treated with ceftibuten and amoxicillin-clavulanate, respectively. No significant difference was observed in the ceftibutenfed and ceftibuten-fasted groups in overall clinical assessments of the clinical efficacy population and safety population. In conclusion, 400 mg oral ceftibuten once daily has a similar clinical success rate to 500 mg amoxicillin-clavulanate three times daily, with a trend toward fewer gastrointestinal side effects, in the treatment of patients with AECB.

Adolescent↗
PubMed1997

Ceftibuten: a new expanded-spectrum oral cephalosporin.

OBJECTIVE: To review the antimicrobial activity, pharmacokinetics, clinical efficacy, and tolerability of ceftibuten, a new expanded-spectrum oral cephalosporin. DATA SOURCES: Literature was identified by a MEDLINE search (January 1983-June 1996) of the medical literature, review of English-language literature and bibliographies of these articles, and data on file. STUDY SELECTION: Clinical efficacy data were selected from all published and unpublished trials and abstracts that mentioned ceftibuten. Additional information concerning in vitro susceptibility, safety, chemistry, and pharmacokinetic profile of ceftibuten also was reviewed. DATA SYNTHESIS: Ceftibuten, an oral expanded-spectrum cephalosporin, has a broad spectrum of activity against many gram-negative and selected gram-positive organisms, including Streptococcus pneumoniae, Streptococcus pyogenes, Moraxella catarrhalis, and Haemophilus influenzae. Ceftibuten is stable to hydrolysis by many common beta-lactamases. Ceftibuten is rapidly and almost completely absorbed from the gastrointestinal tract and is primarily eliminated renally as unchanged drug. The elimination half-life of ceftibuten is slightly longer than 2 hours. Efficacy has been demonstrated in a number of clinical trials in adults and children with upper and lower respiratory tract infections (e.g., acute otitis media, pharyngitis, sinusitis, bronchitis) and urinary tract infections. The adverse effect profile is equal to that of comparator agents. CONCLUSIONS: Ceftibuten is an alternative to other antimicrobial agents with convenient once-daily dosing in the treatment of upper and lower respiratory tract infections. Similar to other oral expanded-spectrum cephalosporins, ceftibuten has antimicrobial activity against common pathogens of the respiratory tract and is stable in the presence of many beta-lactamases. The clinical choice of an oral expanded-spectrum cephalosporin will be based on patient acceptance, frequency of administration, and cost.

Administration, Oral↗
PubMed1998

Pharmacokinetic drug interaction study: administration of ceftibuten concurrently with the antacid mylanta double- strength liquid or with ranitidine.

This study investigated the influence of antacid (Mylanta Double-Strength Liquid; J & J-Merck Consumer, Fort Washington, PA) and the H2 antagonist ranitidine on the pharmacokinetics of ceftibuten, a once-daily oral cephalosporin. Eighteen male volunteers received, in a randomized, three-way, crossover design, a single oral 400-mg dose of ceftibuten after an overnight fast (1) alone, (2) with antacid (60 mL), and (3) with ranitidine (after 3 days of dosing, 150 mg/12 hours). Serial blood and urine samples were collected during a 24-hour period after each administration, with a 1-week washout between treatments. Ceftibuten, and its metabolite ceftibuten-trans, were analyzed in plasma and urine by high-performance liquid chromatography. Bioavailability parameters, maximum plasma concentration and area under the plasma concentration-time curve to infinity of ceftibuten were unaffected by treatment with antacid. These parameters were somewhat higher when ceftibuten was administered with ranitidine, but they were still within the ranges seen in normal healthy volunteers. The excretion of ceftibuten was independent of treatment. The concentrations of ceftibuten-trans were low in both plasma and urine with all three treatments. It is concluded that the co-administration of antacid and ranitidine are unlikely to affect the bioavailability and antibacterial efficacy of ceftibuten.

Administration, Oral↗
PubMed1995

Ceftibuten: a review of antimicrobial activity, spectrum and other microbiologic features.

Ceftibuten is a new, orally administered cephalosporin with exceptional beta-lactamase stability and potency against commonly isolated Gram-negative pathogens. More than 90% of recent Enterobacteriaceae clinical isolates were inhibited by < or = 8 micrograms/ml of ceftibuten. In only five enteric species (Citrobacter freundii, Enterobacter aerogenes, Enterobacter cloacae, Morganella morganii, Serratia marcescens) were more than 15% of strains resistant (minimal inhibitory concentrations (MIC, with percent of strains inhibited in subscript numbers) > 16 micrograms/ml) to ceftibuten. Enteritis-producing bacteria such as Salmonella, Shigella, Escherichia coli and Yersinia were very ceftibuten-susceptible (MIC50 < or = 0.13 microgram/ml). Fastidious Gram-negative species causing respiratory tract or genital infections had very low ceftibuten MICs, including beta-lactamase-positive Haemophilus influenzae (MIC90 0.06 to 2 micrograms/ml), Moraxella catarrhalis (MIC90 0.25 to 4 micrograms/ml), and Neisseria gonorrhoeae (MIC90 0.015 to 0.5 microgram/ml). Beta-hemolytic streptococci and penicillin-susceptible pneumococci were also inhibited by ceftibuten. Staphylococci, enterococci, Pseudomonas species and Gram-negative anaerobic bacteria were generally resistant to ceftibuten. Ceftibuten has demonstrated bactericidal activity against susceptible pathogens, has high affinity for several lethal penicillin-binding proteins and possesses stability to common plasmid- or chromosomal-mediated beta-lactamases, including those enzymes that hydrolyze parenteral third generation cephalosporins. The microbiologic features for ceftibuten indicate its clinical potential as chemotherapy for community-acquired respiratory tract infections.

Bacteria↗
PubMedDate not supplied

Comparison of the efficacy and tolerability of once-daily ceftibuten and twice-daily cefprozil in the treatment of children with acute otitis media.

In this multicenter, randomized, single (investigator)-masked study, the efficacy and tolerability of once-daily ceftibuten and twice-daily cefprozil were compared in the treatment of acute otitis media in patients 6 months to 10 years of age. Ceftibuten oral suspension 9 mg/kg once daily (maximum dose, 400 mg/d) and cefprozil oral suspension 15 mg/kg twice daily (maximum dose, 1000 mg/d) were given for 10 days. Clinical response, evaluated at the posttreatment visit (days 14 to 16), was rated as clinical cure, improvement, failure, relapse/recurrence, or not assessable. The clinical response was considered successful if the posttreatment assessment was clinical cure or clinical improvement and unsuccessful if the assessment was clinical failure, relapse/recurrence, or not assessable. Tolerability was evaluated by observed and spontaneously reported adverse events. A total of 205 patients were enrolled in the study. The ceftibuten group (51 males, 51 females; mean age, 4.8 years, range, 0.5 to 10.7 years) was similar in demographic characteristics to the cefprozil group (60 males, 43 females; mean age, 4.8 years, range, 0.7 to 10.7 years). In the ceftibuten-treated group, 83.3% (85) of the 102 patients had a successful response compared with 82.5% (85) of the 103 patients in the cefprozil-treated group. The incidence of treatment-related adverse events was similar in both groups, occurring in 5.9% (6) of the ceftibuten-treated patients and 5.8% (6) of the cefprozil-treated patients. Once-daily ceftibuten oral suspension was as effective and well tolerated as twice-daily cefprozil in the treatment of acute otitis media in children. The once-daily dosing schedule for ceftibuten therapy may aid patient compliance, particularly in the pediatric population. Ceftibuten should prove to be a useful alternative in the treatment of acute otitis media.

Acute Disease↗
PubMed1988

Antimicrobial activity, spectrum, and recommendations for disk diffusion susceptibility testing of ceftibuten (7432-S; SCH 39720), a new orally administered cephalosporin.

The antimicrobial activity and spectrum of ceftibuten (7432-S; SCH 39720) was determined on a wide variety of bacterial species selected for resistance to oral and parenteral beta-lactam antimicrobial agents. Ceftibuten was found to be the most active beta-lactam tested against members of the family Enterobacteriaceae, inhibiting 81.6% of strains at less than or equal to 8.0 micrograms/ml compared with 75.0 and 54.8% of strains inhibited by cefixime and cefuroxime, respectively. All strains of Haemophilus influenzae (MIC for 90% of strains [MIC90], less than or equal to 0.06 microgram/ml), Branhamella catarrhalis (MIC90, 3.0 micrograms/ml), and pathogenic Neisseria spp. (MIC90, less than or equal to 0.06 and 0.019 microgram/ml) were susceptible to ceftibuten. Beta-hemolytic Streptococcus spp. (serogroups A, B, C, and G) were also inhibited by ceftibuten, but penicillin-resistant pneumococci were generally resistant to cefixime and ceftibuten. The activity and spectrum of ceftibuten seem most applicable to infections of the respiratory and urinary tract plus those infections caused by pathogenic Neisseria spp. Ceftibuten disks (30 micrograms) were evaluated and found to have an acceptable correlation (r = 0.88) with ceftibuten MICs. Preliminary zone size interpretive criteria for MIC breakpoints of less than or equal to 4.0 and less than or equal to 8.0 micrograms/ml were calculated.

Administration, Oral↗
PubMedDate not supplied

Comparative antimicrobial activity of ceftibuten against multiply-resistant microorganisms from Belgium.

To study the activity of ceftibuten, we obtained multiply-resistant isolates from approximately 20 hospitals in Belgium. Against Enterobacteriaceae, all of the tested comparative compounds were more active than cefaclor, and ceftibuten and tigemonam were the most active of the agents tested. Ceftibuten MIC50s were less than or equal to 1 microgram/ml for most enteric bacilli species and 85% of strains were susceptible (less than or equal to 8 micrograms/ml). This level of activity compared favorably to that recorded for cefaclor (less than or equal to 8 micrograms/ml), cefetamet (less than or equal to 4 micrograms/ml), and cefteram (less than or equal to 1 microgram/ml), that is, 37%, 69%, and 59%, respectively. Ceftibuten, cefetamet, cefteram, and tigemonam were highly active against isolates of Haemophilus influenzae and Neisseria gonorrhoeae. None of the comparative agents were as active as cefaclor against staphylococcal isolates. Against streptococci, cefteram was the most active, and tigemonam the least active of the agents. The MIC90s of ceftibuten for strains of Streptococcus pneumoniae and Streptococcus pyogenes were 2 micrograms/ml and 0.5 microgram/ml, respectively. Strains of Streptococcus agalactiae were resistant to both ceftibuten and tigemonam; cefaclor and cefteram inhibited 100% of isolates of this species. Strains of Enterococcus faecalis and Pseudomonas aeruginosa were consistently resistant to all of the compounds. Overall, ceftibuten exhibited potent activity against many multiply-resistant clinical isolates.

Bacteria↗
PubMedDate not supplied

Randomized comparative study of ceftibuten versus cefaclor in the treatment of acute lower respiratory tract infections.

In a randomized, single-blind trial, ceftibuten in doses of 200 mg and 300 mg administered b.i.d., was compared with cefaclor 500 mg t.i.d. in acute lower respiratory tract infections. A total 545 patients were enrolled, of which 263 were evaluable for efficacy. All patients were adults with a diagnosis of either bacterial pneumonia or bronchitis. The infective organism was eliminated in 83% of the patients in the ceftibuten 200-mg b.i.d. treatment group and in 85% of patients in the 300-mg b.i.d. treatment group. The organisms were eliminated in 79% of cefaclor-treated patients. Satisfactory clinical responses were obtained in 91% of patients in the ceftibuten 200-mg b.i.d. treatment group and in 92% of patients in the ceftibuten 300-mg b.i.d. group. Satisfactory clinical responses were obtained in 91% of cefaclor-treated patients. Predominant pathogens isolated were Streptococcus pneumoniae, Haemophilus influenzae, Moraxella (Branhamella) catarrhalis, and strains of Enterobacteriaceae. Adverse experiences reported were similar for the ceftibuten and cefaclor treatment groups. Gastrointestinal side effects occurred in 6% of patients treated with ceftibuten 200 mg BID, 9% in those treated with 300 mg BID, and 7% of cefaclor-treated patients. Ceftibuten 200 and 300 mg twice daily was as effective as cefaclor bacteriologically and clinically in the treatment of lower respiratory tract infections.

Acute Disease↗
PubMed1998

Isomerization of ceftibuten in aqueous solution.

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.

Ceftibuten↗