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PubMed1987

Bowel flora changes in humans receiving cefixime (CL 284,635) or cefaclor.

Twelve healthy young male subjects received either cefixime, a new oral cephalosporin (CL 284,635), or cefaclor (six subjects on each drug) orally for 2 weeks. In the case of cefixime, single daily doses of 400 mg were taken; with cefaclor, the dosage was 250 mg three times daily. Modest changes in the fecal flora were noted in both drug groups, but the changes were of different types. In the case of cefixime, there was more of an impact on the indigenous flora, and in the case of cefaclor, there was more ingrowth of new flora. With cefixime, Enterobacteriaceae were usually decreased (the decrease in Escherichia coli count was statistically significant), as were counts of clostridia and sometimes Bifidobacterium spp.; the Bacteroides fragilis group was eliminated in one subject. Coincident with these decreases, four subjects had increases in counts of group D streptococci of 3 logs or more. There was new appearance of Clostridium difficile in four subjects and of Staphylococcus aureus in one; four new strains of Enterobacteriaceae appeared. With cefaclor, there was no decrease of E. coli counts; two subjects had elimination of Bifidobacterium spp. There was little change in counts of group D streptococci. On the other hand, there were 13 new strains of Enterobacteriaceae, two of S. aureus, and three of C. difficile.

Bacteria↗
PubMed1992

Modification of cefixime bioavailability by nifedipine in humans: involvement of the dipeptide carrier system.

We studied the action of nifedipine on the bioavailability of cefixime, a molecule absorbed via the gut wall dipeptide carrier system in the rat, and on the bioavailability of D-xylose, which is absorbed via a pH (and Na(+)-)-dependent transporter. Each compound was administered alone or in combination with 20 mg of nifedipine to eight healthy male volunteers. Nifedipine significantly increased the absorption rate of cefixime (20.7 +/- 4.3 versus 16 +/- 3.5 mg/h in the absence of nifedipine). The absolute bioavailability of cefixime alone was 31% +/- 6% compared with 53% +/- 1% (P < 0.01) in the presence of nifedipine. The observed peak concentrations in serum were significantly different (2.5 +/- 0.3 mg/liter without nifedipine and 3.7 +/- 1.1 mg/liter with nifedipine; P < 0.02). In contrast, nifedipine induced no significant differences in the pharmacokinetic profile of xylose following oral administration. We conclude that (i) cefixime is absorbed in humans by an apparently active process which can be enhanced by a calcium channel blocker, in this case, nifedipine; and (ii) nifedipine does not modify the activity of the pentose transporter.

Administration, Oral↗
PubMed1992

Presence of Clostridium difficile and antibiotic and beta-lactamase activities in feces of volunteers treated with oral cefixime, oral cefpodoxime proxetil, or placebo.

Three groups of six healthy adult volunteers were randomly assigned to a treatment with 400 mg of oral cefpodoxime proxetil, oral cefixime, or placebo per day for 10 days. Informed consent was obtained from all volunteers. Clostridium difficile was not detected in the feces of any subject before treatment or at any time in the subjects in the placebo group. C. difficile was, however, detected in all subjects treated with cefpodoxime proxetil and in five of six treated with cefixime. Genomic DNA restriction patterns showed that the strains of C. difficile differed from one volunteer to another. Two subjects both shed different strains at different times during the 25-day surveillance period. All isolates were resistant to cefixime and cefpodoxime (MIC for 90% of strains, 256 and 512 mg/liter, respectively). Antibiotic activity was found in the feces of one volunteer treated with cefpodoxime proxetil and of four volunteers treated with cefixime. It was inversely correlated with the presence of fecal beta-lactamase activity. Intestinal side effects were limited to modifications of stool consistency, which occurred in only 3 of the 12 treated volunteers and did not lead to cessation of treatment. These modifications were significantly associated with the presence of fecal antibiotic activity (P less than 0.05) but not with the shedding of toxigenic or nontoxigenic strains of C. difficile or with the presence of toxin A in feces, which was detected only in one perfectly healthy treated volunteer.

Administration, Oral↗
PubMed1996

Bactericidal activities of cefprozil, penicillin, cefaclor, cefixime, and loracarbef against penicillin-susceptible and -resistant Streptococcus pneumoniae in an in vitro pharmacodynamic infection model.

We examined the bactericidal activities of penicillin, cefprozil, cefixime, cefaclor, and loracarbef against three clinical isolates of Streptococcus pneumoniae which were susceptible, moderately susceptible, and resistant to penicillin. An in vitro two-compartment glass infection model was used to simulate human pharmacokinetics in the presence of bacteria. Also, changes in organism susceptibility and development of resistant subpopulations were evaluated. Simulated pediatric dosage regimens and target peak concentrations in the central compartment were as follows: penicillin V-potassium, 26 mg/kg of body weight every 6 h (q6h) and 14 micrograms/ml; cefaclor, 13.4 mg/kg q8h and 16 micrograms/ml; loracarbef, 15 mg/kg q12h and 19 micrograms/ml; cefprozil, 15 mg/kg q12h and 11 micrograms/ml; and cefixime, 8mg/kg q24h and 4 micrograms/ml. Targeted half-lives of each agent were 1 h for penicillin, cefaclor, and loracarbef; 1.3 h for cefprozil; and 3.5 h for cefixime. Growth controls were performed at two different pump rates, 0.8 and 2.0 ml/min (half-lives = 3.5 and 1 h, respectively). Each isolate demonstrated autolysis at the lower rate which was attributed to a decreased supply of fresh nutrients available to the organisms in the infection compartment. Against the susceptible isolate, the time to 99.9% killing was statistically significant between penicillin V-potassium and both cefaclor and cefixime (P < 0.029). Loracarbef never achieved a 99.9% reduction in the inoculum. At 48 h penicillin, cefprozil, and cefaclor were equivalent in extent of killing. Against the intermediately resistant isolate, cefprozil was superior to all other regimens with respect to rate of killing (P < 0.013) and extent of killing at 24 h (P < 0.0003). At 48 h penicillin, cefprozil, and cefaclor were equivalent in extent of killing. All of the regimens exhibited inferior activity against this penicillin-resistant isolate. A 99.9% kill was never obtained with any of the regimens, nor was there an appreciable decrease in the colony counts. In conclusion, it appears that cefprozil, penicillin, and cefaclor are effective therapies against sensitive and even intermediately sensitive isolates of S. pneumoniae. However, none of the oral therapies appear to be of any benefit against penicillin-resistant isolates. The in vitro model may be an effective tool in evaluating other multiple-dose therapies against this fastidious organism, since the continual supply of fresh medium maintains the viability of S. pneumoniae with minimal stationary-phase autolysis.

Cefaclor↗
PubMed1996

Penetration and bactericidal activity of cefixime in synovial fluid.

The penetration of oral cefixime into the synovial fluids of 16 patients (mean age, 50.6 years) who underwent joint taps for rheumatic noninfectious disorders was examined. The patients were each given a single dose (400 mg) 2 to 24 h prior to the tap. Cefixime concentrations in serum and joint fluid samples were measured by high-performance liquid chromatography, and the bactericidal activities of these fluids against three isolates each of Haemophilus influenzae and Escherichia coli were examined. The highest concentrations in serum and synovial fluid were achieved 4 h following drug intake, the mean values being 2.8 and 2.03 micrograms/ml, respectively. Effective bactericidal activities (bactericidal titer, > 1:2) against E. coli and H. influenzae were demonstrated in serum and joint fluid up to 10 h following oral intake of cefixime. These results suggest that cefixime penetrates well into joint fluid, achieving levels above the MIC for E. coli lasting as long as 10 h and levels above the MIC for H. influenzae lasting up to 24 h after administration. Good bactericidal activity against susceptible bacterial isolates was observed for at least 10 h after dosing.

Adult↗
PubMed2002

Mosaic-like structure of penicillin-binding protein 2 Gene (penA) in clinical isolates of Neisseria gonorrhoeae with reduced susceptibility to cefixime.

Neisseria gonorrhoeae strains with reduced susceptibility to cefixime (MICs, 0.25 to 0.5 micro g/ml) were isolated from male urethritis patients in Tokyo, Japan, in 2000 and 2001. The resistance to cephems including cefixime and penicillin was transferred to a susceptible recipient, N. gonorrhoeae ATCC 19424, by transformation of the penicillin-binding protein 2 gene (penA) that had been amplified by PCR from a strain with reduced susceptibility to cefixime (MIC, 0.5 micro g/ml). The sequences of penA in the strains with reduced susceptibilities to cefixime were different from those of other susceptible isolates and did not correspond to the reported N. gonorrhoeae penA gene sequences. Some regions in the transpeptidase-encoding domain in this penA gene were similar to those in the penA genes of Neisseria perflava (N. sicca), Neisseria cinerea, Neisseria flavescens, and Neisseria meningitidis. These results showed that a mosaic-like structure in the penA gene conferred reductions in the levels of susceptibility of N. gonorrhoeae to cephems and penicillin in a manner similar to that found for N. meningitidis and Streptococcus pneumoniae.

Amino Acid Sequence↗
PubMed1995

Methods for predicting susceptibility of Streptococcus pneumoniae to cefixime.

Among 698 Streptococcus pneumoniae isolates, 475 were penicillin susceptible and > 99% of those were susceptible to 0.5 microgram of cefixime per ml; other pneumococci were tentatively assumed to be resistant to cefixime. A 1-microgram oxacillin disk was more reliable than a 5-micrograms cefixime disk for predicting susceptibility to cefixime.

Cefixime↗
PubMed1992

Antibacterial activity of cefixime against Streptococcus pneumoniae, Streptococcus pyogenes, and Haemophilus influenzae in the presence of Moraxella (Branhamella) catarrhalis.

We measured the sizes of the inhibition zones of oral beta-lactam antibiotics for Streptococcus pneumoniae, Streptococcus pyogenes and Haemophilus influenzae in the presence of beta-lactamase-producing-Moraxella (Branhamella) catarrhalis by the agar double-layer method. The sizes of the zones of amoxicillin for S. pneumoniae alone were the largest, followed in a descending order by those of cefixime and cefaclor. In the presence of 10(7) CFU/ml of M.(B.) catarrhalis, however, significant reduction of the sizes of the zones was seen with amoxicillin and cefaclor; inhibition with cefixime was nearly unchanged. Similar results were observed in those for S. pyogenes. These variable findings were attributed to the difference in stability of these drugs to the beta-lactamase produced by M.(B.) catarrhalis. When the susceptibility of H. influenzae in the presence of 10(8) CFU/ml of M.(B.) catarrhalis to cefixime, cefoteram, cefpodoxime, cefotiam and cefuroxime was examined, the sizes of the inhibition zones of all the drugs were reduced by the presence of 10(8) CFU/ml of M.(B.) catarrhalis, but those of cefixime were the largest of all the drugs tested. Our agar double-layer method is simple and useful for evaluating the influence of beta-lactamase-producing organism, as M.(B.) catarrhalis, on the disk susceptibility of other pathogens to antibiotics.

Cefixime↗
PubMed1996

Comparative evaluation of cefixime versus amoxicillin-clavulanate following ceftriaxone therapy of pneumonia.

Preliminary results have recently shown that an early switch from parenteral antimicrobials to an oral substitute provides an effective means of treating pneumonia in pediatric patients. In a controlled randomized study, 62 children with community-acquired lobar/segmental pneumonia were selected to receive 8 days of cefixime or amoxicillin-clavulanate after an initial therapy of two doses of parenteral ceftriaxone. Enrollment criteria included: age 6 months to 5 years, fever > 38.5 degrees C, white blood cell (WBC) count > or = 15,000/ mm3, and lobar/segmental pneumonia on chest radiograph. Twenty-nine patients were randomized to receive oral cefixime and 33 to oral amoxicillin-clavulanate. The two groups were comparable in the following pretreatment parameters: age, duration of illness, temperature, mean WBC count, erythrocyte sedimentation rate, C-reactive protein, and need for hospitalization. Days of resolution of high fever, tachypnea, cough, grunting, and laboratory test abnormalities were similar in the two groups. Clinical response at the end of treatment showed cure, improvement, and failure in 97%, 3%, and 0%, respectively, in the cefixime group and in 88%, 6%, and 6%, respectively in the amoxicillin-clavulanate group (P = NS). We conclude that young children with community-acquired lobar/segmental pneumonia can be successfully treated with 2 days of parenteral ceftriaxone followed by 8 days of oral cefixime or amoxicillin-clavulanate.

Administration, Oral↗
PubMed2004

Effect of cefixime and cefdinir, oral cephalosporins, on cytochrome P450 activities in human hepatic microsomes.

The effects of two kinds of oral cephalosporins, cefixime and cefdinir, on cytochrome P450 (CYP) activities in human hepatic microsomes were investigated. Both cefixime and cefdinir at 2 mM concentration neither inhibited nor stimulated CYP1A1/2-mediated 7-ethoxyresorufin O-deethylation, CYP2A6-mediated coumarin 7-hydroxylation, CYP2B6-mediated 7-benzyloxyresorufin O-debenzylation, CYP2C8/9-mediated tolbutamide methylhydroxylation, CYP2C19-mediated S-mephenytoin 4'-hydroxylation, CYP2D6-mediated bufuralol 1'-hydroxylation, CYP2E1-mediated chlorzoxazone 6-hydroxylation, CYP3A4-mediated nifedipine oxidation, or CYP3A4-mediated testosterone 6beta-hydroxylation. The free fractions of cefixime and cefdinir in the incubation mixture, which were measured by ultracentrifugation, were 86.1-93.8% and 94.1-97.8%, respectively. These results suggest that both cefixime and cefdinir would not cause clinically significant interactions with other drugs, which are metabolized by CYPs, via the inhibition of metabolism.

Biotransformation↗
PubMed1991

Cefixime vs amoxicillin in the treatment of acute otitis media in infants and children.

Cefixime is a new oral cephamycin antibiotic with a broad spectrum of antibacterial activity in vitro. It is resistant to hydrolysis by most beta-lactamases and has pharmacokinetic characteristics which allow administration in a single daily dose for the treatment of some bacterial infections. The aim of this study was to compare the clinical efficacy of cefixime with that of amoxicillin in the treatment of acute otitis media in 40 children. Cefixime 8 mg/kg was given once daily at bedtime, whereas amoxicillin 50 mg/kg/day was administered in 3 divided doses; both drugs were given for 10 days. 15 days after starting the trial, a favourable clinical response was demonstrated in 18 of 20 children in both treatment groups. Cure rates, recurrences and persistent middle ear effusions were not significantly different in the 2 study groups during a 3-month follow-up. It was concluded that cefixime is clinically effective and well tolerated in the treatment of children with acute otitis media.

Acute Disease↗
PubMed1999

Bacteriological eradication of Streptococcus pneumoniae from patients with acute exacerbations of chronic bronchitis: cefuroxime axetil versus cefixime.

The bacteriological eradication rates of Streptococcus pneumoniae from sputum of patients experiencing acute exacerbations of chronic bronchitis (WHO definition) have been compared following therapy with either cefuroxime axetil 250 mg b.d. or cefixime 200 mg b.d. All patients were hospitalised for an acute exacerbation of chronic bronchitis. The study design was a multicentre, double-blind, randomised, parallel group with patients giving written informed consent initially. Patients were recruited to the study if they met the WHO definition of chronic bronchitis, were aged 30-75 years and had a high probability of S. pneumoniae infection based on initial sputum Gram stain. All S. pneumoniae isolates were serotyped and susceptibility tested at the National Reference Centre, Paris. S. pneumoniae was eradicated more rapidly following cefuroxime axetil administration than after cefixime and this difference was statistically significant (p = 0.002) at 2-4 days post-treatment. Clinical endpoints showed a similar trend--94% response to cefuroxime axetil compared with 71% response to cefixime (RR 6.39:1). Cefuroxime eradicated S. pneumoniae significantly more rapidly than cefixime and patients in the cefuroxime axetil arm had favourable clinical criteria. The data suggest that focused antibacterial studies may be helpful in evaluating antibiotics in acute exacerbation of chronic bronchitis.

Adult↗
PubMed1991

[Cefixime. Microbiologic, kinetic and clinical profile].

The microbiological, kinetic and clinical profile of cefixime, a IIIrd generation cephalosporin, administered orally, is presented. Cefixime is highly active versus Gram-negative aerobic bacteria while, with respect to Gram-positive bacteria, it is only active against Str. pneumoniae, Str. pyogenes, Str. agalactiae, and Str. bovis. It has no action against anaerobics. Endowed with good kinetics, cefixime possesses a favourable tissue distribution. Cefixime is highly indicated in infections of the upper and lower airways where the aethiology is prevalently due to Str. pneumoniae, H. influenzae and B. catarrhalis, that are extremely sensitive to the antibiotic. It is concluded that the therapeutic armamentarium has been enriched by a new, highly active antibiotic that, administered in a monodese/die, ca satisfy patient compliance.

Animals↗
PubMedDate not supplied

Efficacy and safety of oral cefixime therapy in common infectious diseases in children.

Twenty-nine children, including 20 boys and 9 girls, were enrolled in an open trial of oral cefixime therapy for common pediatric infectious diseases. Patients aged between 0.5 month and 12 years with a mean +/- standard deviation of 2.3 +/- 2.8 years. The diagnoses included 10 of acute otitis media, 2 of purulent rhinitis, 4 of acute enterocolitis, and 13 of urinary tract infection. Most children received 6-12 mg/kg/day of cefixime granules, orally twice daily for more than five days. All 10 cases (100%) of acute otitis media and 2 cases of purulent rhinitis were either cured, or improved by oral cefixime treatment. None of them was microbiologically evaluable. Four cases (100%) of acute enterocolitis, 3 due to Salmonella group B, one due to Shigella flexneri, were also successfully treated with bacteria eradication. However, the cure rate of 13 cases of urinary tract infection was only 85% (11/13). Seven Escherichia coli and 4 Proteus mirabilis infections were eradicated, whereas one each of Enterobacter cloacae and Klebsiella pneumoniae infections did not respond to treatment; these two cases had a complicated course. The overall cure and improvement rate was 93%. Although five patients had transient episodes of mild diarrhea, no significant adverse reaction was observed. In summary, oral cefixime given twice daily was effective and safe in the treatment of a variety of common infectious diseases in pediatric patients.

Administration, Oral↗
PubMed1991

[Penetration of cefixime in the anterior chamber of the human eye].

Penetration of cefixime in aqueous humor was investigated in 21 patients about to undergo elective cataract extraction. All subjects received a 400 mg oral dose. Aqueous humor was collected within 4, 6, 10 or 15 hours after the administration. Cefixime was measured by liquid chromatography. The concentration of cefixime in aqueous humor was below 0.05 mg/l in 17 patients. The highest level reached was 0.16 mg/l. In spite of lower minimal inhibitory concentrations than first generation oral cefalosporins, cefixime per os cannot be proposed for the treatment of postoperative ocular infections.

Administration, Oral↗
PubMed1991

Comparative in vitro activity of cefixime, cefaclor and loracarbef against urinary pathogens.

Minimum inhibitory concentrations of cefixime, cefaclor and loracarbef have been determined against 200 strains of bacteria, representing a wide selection of species causing urinary infections. Cefixime was poorly active against Gram-positive species, but was active (MIC90 less than 2 mg/l) against almost all the Gram-negative pathogens tested (except Pseudomonas aeruginosa), and particularly so against Klebsiella pneumoniae and members of the tribe Proteae. Cefaclor and loracarbef were more active against the Gram-positive species than was cefixime, but had a less broad spectrum against the Gram-negative species. Cefixime use seems more appropriate in nosocomial than in domiciliary urinary infections.

Anti-Infective Agents, Urinary↗
PubMed1990

Concentration of cefixime in bile, gallbladder wall and serum after preoperative administration in patients undergoing cholecystectomy.

Cefixime is a new oral cephalosporin antibiotic with improved activity against Gram-negative pathogens comparable to the parenteral third generation cephalosporins, high beta-lactamase stability and a long elimination half-life of about 3 h. 15 patients undergoing cholecystectomy received 2 x 200 mg/day cefixime for two days before surgery. The last application was administered 13-17 h preoperatively. Intraoperatively, the mean biliary level of cefexime was 199.3 micrograms/ml (8.8 micrograms/ml-1163.8 micrograms/ml). The mean level in gallbladder wall was 25.02 micrograms/g (0.68 micrograms/g-61.20 micrograms/g). Serum samples were taken simultaneously. Despite relevant concentrations in bile and gallbladder wall, no cefixime could be detected in the serum samples of two patients. The other 13 patients, however, showed relevant serum levels between 0.28 micrograms/ml and 2.98 micrograms/ml (mean 1.01 micrograms/ml). Side effects as well as an influence on laboratory parameters were not seen. After administration of cefixime in bile and gallbladder tissue high antibiotic levels were achieved, even 13-17 hours after the last application.

Adult↗
PubMed1989

[Cefixime, the first oral third-generation cephalosporin].

In the early 1980's parenteral third generation cephalosporins changed the hospital use of antibiotics. The MICs of these cephalosporins are several dozen times lower than those of first or second generation cephalosporins for Enterobacteriaceae and they are much more beta-lactamase stable than second generation cephalosporins. After years of research, is has finally been possible to develop orally active compounds possessing the same antibacterial activity as parenteral third generation cephalosporins, either through the use of prodrugs, or by modifying the molecular structure of drugs. Cefixime is an example of the latter. The vinyl group at the 3-position of the cephem nucleus is responsible for the intestinal absorption of the intact molecule, primarily by a carrier-mediated transport mechanism. The aminothiazole ring and the R-oxyimino group on the side-chain at the 7-position are associated with an antibacterial activity similar to that of third generation cephalosporins. Thousands of adults have been treated by cefixime for lower respiratory tract, ear-nose-throat and urinary tract infections, showing that cefixime is a safe and effective antimicrobial agent. The major clinical indications for cefixime in adults are bronchial and pulmonary infections, acute otitis or sinusitis, acute pyelonephritis with no underlying uropathy, and complicated or uncomplicated lower urinary tract infections excluding prostatitis. In all cases, the dosage is 200 mg b.i.d.

Administration, Oral↗