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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↗

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↗

PubMed1989

Transport characteristics of ceftibuten, a new oral cephem, in rat intestinal brush-border membrane vesicles: relationship to oligopeptide and amino beta-lactam transport.

Ceftibuten undergoes H+-coupled uphill transport across rat small intestinal brush-border membrane vesicles. The effects of amino acids, peptides, folate, and beta-lactams on the uptake of ceftibuten were examined. Uptake of ceftibuten was competitively inhibited by dipeptides or tripeptides. A counter-transport effect on ceftibuten uptake was observed in the vesicle preloaded with these peptides, and the transport was temporarily against a concentration gradient (overshooting). On the other hand, ceftibuten uptake was not changed by amino acids and a tetrapeptide. Therefore, ceftibuten is predominantly transported via the oligopeptide transport system in the brush-border membranes. The relationship of ceftibuten transport to folate and other oral antibiotics was also investigated. Cyclacillin, cephradine, and cefadroxil exhibited both inhibitory and countertransport effects, but folate, cefaclor, and cephalexin showed only a slight inhibitory effect. As the transport of cefaclor showed no uphill uptake in the presence of a H+ gradient and its H+ stimulated uptake was small, a H+ gradient-independent carrier-mediated system seems to participate in its transport. These findings suggest that two different carrier-mediated transport systems, H+ gradient dependent and independent, may exist for oral cephems.

Amino Acids↗

PubMed1994

Characteristics of ceftibuten uptake into Caco-2 cells.

The characteristics of ceftibuten uptake into Caco-2 cells grown in a collagen-coated dish were examined. Ceftibuten showed stereoselective and pH-dependent uptake. The pH-dependency of ceftibuten was more marked than that of cefaclor or cephalexin, but all three antibiotics showed maximal uptake at pH 5.5. Ceftibuten uptake was linear for the initial 1 hr and then reached a plateau. The initial uptake (15 min) was markedly reduced by the addition of 2,4-dinitrophenol or FCCP (a protonophore), or by lowering the incubation temperature. The uptake of ceftibuten into the brush-border membrane vesicles prepared from cultured Caco-2 cells showed an overshoot in the presence of an H(+)-gradient. These findings indicated that the uptake of ceftibuten was energy-dependent, especially H(+)-gradient-dependent. Uptake inhibition by various compounds was compared using Caco-2 cells. Amino acids and a tetrapeptide did not inhibit uptake, whereas di- or tri-peptides were effective inhibitors. These observations suggest that ceftibuten is taken up by a carrier-mediated transport system(s) for dipeptides. Various antibiotics differed in their ability to inhibit uptake, with cyclacillin showing maximum inhibition. Differences in the inhibitory effect may be accounted for by the heterogeneity (multiplicity) of the transport systems.

2,4-Dinitrophenol↗

PubMed1991

Ceftibuten versus cefaclor for the treatment of bronchitis.

Ceftibuten is an oral third generation cephalosporin with potent antimicrobial activity against Enterobacteriaceae, beta-lactamase positive Haemophilus influenzae, Moraxella catarrhalis, Neisseria meningitidis, Neisseria gonorrheae, penicillin-susceptible pneumococci, and beta-hemolytic streptococci. To study the efficacy and safety of ceftibuten for treatment of bronchitis, 58 patients were randomized to therapy with either ceftibuten 400 mg once a day or cefaclor 250 mg every 8 h at a ratio of two to one. Of 45 clinically evaluable patients, 28 (87.5%) of the 32 ceftibuten patients and 12 (92.3%) of the 13 cefaclor patients were clinically improved or cured. Of 33 microbiologically evaluable patients, 21 (87.5%) of the 24 ceftibuten patients and eight (80%) of the ten cefaclor patients were cured. Of 56 patients evaluable for adverse effects, three (7.9%) of the 38 ceftibuten patients and one (5.6%) of the 18 cefaclor patients had adverse reactions. In this small study, once-daily ceftibuten appeared as safe and as effective as cefaclor for the treatment of bronchitis.

Bacteria↗

PubMed1996

Efficacy of ceftibuten compared with amoxicillin for otitis media with effusion in infants and children.

OBJECTIVES: This trial compared the efficacy of ceftibuten with that of amoxicillin in resolving otitis media with effusion. METHODS: Two hundred ten children with otitis media with effusion were randomly assigned to receive either ceftibuten (9 mg/kg/day in one daily dose) or amoxicillin (40 mg/kg/day divided into 3 daily doses) for 14 days. Outcome was assessed at 2 and 4 weeks in all subjects; those without middle ear effusion at the 4-week visit were examined at 8, 12 and 16 weeks. Middle ear status was determined by pneumatic otoscopy and by an algorithm combining pneumatic otoscopy with tympanometry. RESULTS: The percentages of subjects who were effusion-free in the ceftibuten and amoxicillin groups at 2 weeks by otoscopy were 29.8 and 27.2%, respectively (P = 0.59), and by the algorithm, 23.4 and 20.4%, respectively (P = 0.47). In children who were effusion-free at 2 weeks, recurrence of effusion by 16 weeks was noted in approximately 60% of the ceftibuten group and 67% of the amoxicillin group. No medication side effects were reported by 88% of subjects in the ceftibuten group and by 93% of subjects in the amoxicillin group. We found no significant differences between the ceftibuten and amoxicillin groups with respect to resolution of middle ear effusion, rate of recurrence or side effects. CONCLUSIONS: Amoxicillin remains the drug of first choice for treatment of otitis media with effusion when treatment is deemed advisable, but ceftibuten may be an alternative drug in selected situations.

Amoxicillin↗

PubMed1993

Efficacy of ceftibuten for acute otitis media caused by Hemophilus influenzae: an animal study.

Ceftibuten is a new oral cephalosporin with an unusual stability to beta-lactamases that can hydrolyze other extended-spectrum cephalosporins. Using the chinchilla animal model, we compared the efficacy of ceftibuten (n = 33) with that of saline (n = 34), ampicillin (n = 32), and cefixime (n = 31) for the treatment of acute otitis media caused by beta-lactamase-producing nontypeable Hemophilus influenzae. Ceftibuten was superior to ampicillin regarding the time necessary to sterilize the middle ear (p < .001) and eliminate effusion (p < .001). The mean days of therapy required for bacteriologic cure were 2.57 for ceftibuten, 2.95 for cefixime, 7.95 for ampicillin, and 8.16 for saline. At the conclusion of therapy, chinchillas treated with ceftibuten had a significantly lower prevalence of positive cultures and middle ear effusion than did animals treated with ampicillin. No significant differences were observed between ceftibuten and cefixime. The results of this randomized, investigator-blinded experiment warrant further consideration of ceftibuten as a second-line agent for acute otitis media caused by ampicillin-resistant H influenzae.

Acute Disease↗