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PubMed2004

[Surveillance of antimicrobial susceptibility of Haemophilus influenzae isolates from children in Beijing, Shanghai, and Guangzhou 2000 - 2002].

OBJECTIVE: To investigate the situation of antibiotic resistance of Haemophilus influenzae isolates from Chinese children. METHODS: Eight hundred and ninety-eight strains of H. influenzae isolated from randomly selected pediatric out-patients in Beijing, Shanghai and Guangzhou 2000 approximately 2002 underwent determination of antibiotic susceptibility by E test MIC method for beta-lactam antibiotics (ampicillin, amoxicillin/clavulanic acid, ceftriaxone, cefuroxime, and cefaclor) and KB disc diffusion method for chloramphenicol, tetracycline, sulfamethoxazole/trimethoprim (SMZ/TMP), azithromycin, and ciprofloxacin. RESULTS: The average rate of beta-lactamase production among these isolates was 12%. The MIC50 and MIC90 of ampicillin were 0.25 microg/ml and 4 microg/ml respectively for the 898 isolates, 88% of the isolates were susceptible to ampicillin and 10.6% was resistant. There was no beta-lactamase negative strains among the ampicillin intermediately-susceptible and resistant strains. All the isolates were susceptible to amoxicillin/clavulanic acid, ceftriaxone, cefuroxime and azithromycin. 96.1% of the H. influenzae isolates generally remained susceptible to cefaclor with a MIC50 of 1.5 microg/ml and a MIC90 of 3 microg/ml, and 99% of the isolates were susceptible to ciprofloxacin. The susceptibility rate to tetracycline of the isolates from Beijing and Shanghai areas were 57% and 61% respectively, both lower than the susceptibility rates of the isolates from Guangzhou (81%), while the resistant rate to SMZ/TMP of the isolates from Beijing was 35%, lower than those of the isolates from Guangzhou (47%) and Shanghai (54%). The resistant rate to ampicillin was 7.7% in 2000 and was increased to 14.5% in 2002. 34.5% of all the isolates were susceptible to 8 antimicrobial agents while 12.8% was multi-drug resistant. 58.5% of the isolates were distributed in five major antimicrobial resistance profiles in which SMZ/TMP resistance (29.8%) was the most prevalent, followed by SMZ/TMP and tetracycline combined resistance (12.5%) and tetracycline resistance (9.4). The ampicillin non-susceptible isolates had higher resistant rates to cefaclor (23.5%), tetracycline (63.3%), SMZ/TMP (74.5%) and chloramphenicol (63.3%) than the ampicillin susceptible strains (1.6%, 51.4%, 11.1% and 4.9% respectively). CONCLUSION: Beta-lactamase production and ampicillin resistance among the isolates from Chinese children are increasing generally during the period 2000 approximately 2002. There is variation of resistance among different regions. There are strong correlations between ampicillin resistance and resistance to cefaclor, chloramphenicol, and tetracycline among the H. Influenzae isolates.

Ampicillin↗
PubMed1998

Clinical microbiology laboratories do not always detect resistance of Haemophilus influenzae with disk or tablet diffusion methods. Finnish Study Group for Antimicrobial Resistance (FiRe).

The performance of disk diffusion testing of Haemophilus influenzae was evaluated in 20 laboratories. Thirteen disk-medium-breakpoint-inoculum modifications were used in Finnish clinical microbiology laboratories. The performance of various methods was evaluated by testing a susceptible control strain and one with non-beta-lactamase-mediated ampicillin resistance 10 times in 16 laboratories. Gaps in millimeters were measured between these two groups of results. The strains were separated by a gap of at least 5 mm in 8/16 laboratories testing ampicillin, in 7/15 laboratories testing cefaclor, in 5/ 16 laboratories testing cefuroxime, and in 15/16 laboratories testing trimethoprim-sulfa. Detection of ampicillin resistance was better with 2.5 microg tablets than with 10 microg disks or 33 microg tablets. For MIC-determinations, 785 isolates and their disk diffusion results were collected. None of the 12 clinical isolates with non-beta-lactamase-mediated ampicillin resistance was detected as resistant in the participating laboratories. The ampicillin and cefaclor results of the isolates were no better even when a laboratory was able to separate the control strains. Cefaclor results were unreliable because of poor disk diffusion-MIC correspondence and incoherent breakpoint references. Interlaboratory variation of the zone diameters caused false intermediate results of cefuroxime-susceptible strains. When ampicillin, cefaclor and cefuroxime were tested, the discrimination of laboratories using disks and tablets was equal, whereas the laboratories using paper disks were better able to detect trimethoprim-sulfa resistance.

Diffusion↗
PubMed2000

Antibiotic rashes in children: a survey in a private practice setting.

OBJECTIVE: To document the frequency and severity of various types of rashes seen with commonly used oral antibiotics in the pediatric outpatient setting. DESIGN: A retrospective review of 5923 patient records at a pediatric office. SETTING: A private group pediatric practice in northern Virginia with about 12,000 registered active patients. PATIENTS AND METHODS: Approximately 50% of the clinic medical records were reviewed. All children (defined as those aged 0-18 years in this study) identified on their medical records as having developed a rash following treatment with 1 or more of the commonly used oral antibiotics were included in the study. For further validation, a questionnaire about parental recollection of description of rash, other associated symptoms, physician verification, and outcome was mailed to families with children designated as being allergic to an antibiotic. RESULTS: On a prescription basis, significantly more rashes were documented for cefaclor (4.79%) compared with penicillins (2.72%), sulfonamides (3. 46%), and other cephalosporins (1.04%). Based on the number of patients for whom each group of antibiotic was prescribed, the documented frequencies of rashes were 12.3%, 7.4%, 8.5%, and 2.6% for cefaclor, penicillins, sulfonamides, and other cephalosporins, respectively. None of the children had rashes severe enough to require hospitalization. CONCLUSIONS: In a review of almost 6000 records in a private pediatric primary care setting, rashes occurred in 7.3% of children who were given the commonly used oral antibiotics. Significantly more rashes were documented with cefaclor use than with use of any of the other oral antibiotics.

Administration, Oral↗
PubMed1988

In vitro activity and beta-lactamase stability of LY163892.

Susceptibility testing of clinical isolates of several gram-negative and gram-positive species showed LY163892 to be more active than cefaclor and cephalexin. OXA-2, TEM-1, TEM-2, PSE-1, CEP-1, CARB-3 and SHV-1 beta-lactamases showed similar activity against LY163892 and cefaclor, whereas OXA-1 hydrolyzed the latter more rapidly. Organisms producing these beta-lactamases, but not TEM-2 and CEP-1, appeared to be more susceptible to LY163892 than cephalexin, although cephalexin proved to be more resistant to beta-lactamase activity. Strains producing TEM-2 and CEP-1 were resistant to LY163892, cefaclor and cephalexin.

Administration, Oral↗
PubMed1986

In vitro activity of amoxicillin plus clavulanic acid against Haemophilus influenzae and Branhamella catarrhalis.

The in vitro activity of amoxicillin in the presence of clavulanic acid against clinical isolates of Haemophilus influenzae and Branhamella catarrhalis was assessed in comparison with ampicillin, amoxicillin, cefaclor and erythromycin. The isolates were selected so as to yield equal numbers of beta-lactamase producing and non-beta-lactamase producing strains of the two species. MICs obtained by agar dilution indicated that amoxicillin in the presence of clavulanic acid was the most active of the drugs tested. Clavulanic acid potentiated the activity of amoxicillin against beta-lactamase-producing strains of both Haemophilus influenzae and Branhamella catarrhalis. Further studies on a few strains of each species revealed that the beta-lactamase of Haemophilus influenzae (TEM-1) rapidly inactivated ampicillin and slowly inactivated cefaclor but not cefuroxime. The Branhamella catarrhalis enzyme rapidly inactivated cefaclor, ampicillin and to some extent cefuroxime. Clavulanic acid afforded protection against the beta-lactamase action of both species when beta-lactam antibiotics were added to bacterial cultures.

Amoxicillin↗
PubMed1981

Concentrations of antimicrobial agents in middle ear fluid, saliva and tears.

Antibiotics concentrations in middle ear fluid (MEF), saliva and tears were measured in children with persistent middle ear effusions undergoing tympanostomy tube placement. In 31 children given cefaclor, specimens of serum, saliva and MEF were collected at 0.5, 1, 2, 3 or 5 h after a dose. Another group of 37 children were randomized to receive a single dose of penicillin V, amoxicillin, ampicillin, erythromycin estolate, erythromycin ethylsuccinate, trimethoprim-sulfamethoxazole or cefaclor. Concentrations of antibiotics in saliva and tears bore no consistent relationship to those in MEF. Mean concentrations of all drugs in MEF were several-fold greater than the usual minimal inhibitory concentrations (MIC) of pneumococci, but only with trimethoprim and cefaclor were they greater than in usual MIC's for Haemophilus influenzae. Concentrations of antibiotics in MEF in persistent effusions were comparable to those previously reported in acute purulent effusions.

Amoxicillin↗
PubMed1988

BMY-28100, a new oral cephalosporin: antimicrobial activity against nearly 7,000 recent clinical isolates, comparative potency with other oral agents, and activity against beta-lactamase producing isolates.

The antimicrobial activity of BMY-28100 was tested against approximately 7,000 bacterial pathogens in a multicenter, multiphased collaborative investigation. The BMY-28100 spectrum and antimicrobial potency was most similar to that of cefaclor and superior to that of cephalexin among currently available cephalosporins. Species that had greater than or equal to 90% of clinical strains inhibited by BMY-28100 (less than or equal to 8.0 micrograms/ml) were: Citrobacter diversus, Escherichia coli, Klebsiella spp., Proteus mirabilis, Salmonella spp., Branhamella catarrhalis, Haemophilus influenzae, Neisseria gonorrhoeae, N. meningitidis, methicillin-susceptible Staphylococcus supp., Streptococcus pneumoniae, S. pyogenes, S. agalactiae, S. bovis, serogroup C and G streptococci, Listeria monocytogenes and gm-positive anaerobes. BMY-28100 inhibited 9% more of the 6286 fresh clinical isolates at less than or equal to 8.0 micrograms/ml than cefaclor at the same concentration. BMY-28100 was generally bactericidal, but MICs for some species were markedly increased when an inoculum concentration of 10(7) CFU/ml was used. Strains producing plasmid-mediated beta-lactamases (TEM, OXA, SHV, HMS) were susceptible to BMY-28100, cefaclor, and cefuroxime. BMY-28100 was less active against strains producing chromosomal-mediated beta-lactamases (Types I and IV). BMY-28100 was not hydrolyzed significantly by the tested plasmid-mediated beta-lactamases, but was destroyed by Type I cephalosporinases and Klebsiella K1 enzymes.

Administration, Oral↗
PubMed1992

Pharmaceutical properties of loracarbef: the remarkable solution stability of an oral 1-carba-1-dethiacephalosporin antibiotic.

Loracarbef is an oral 1-carba-1-dethiacephalosporin antibiotic structurally related to cefaclor. Like many beta-lactam antibiotics, loracarbef exists in several hydrated crystalline forms. The pH-solubility profile curve for loracarbef monohydrate is U-shaped, resembling those of other zwitterionic cephalosporins. Loracarbef was found to be much more stable in solution than cefaclor. For example, in pH 7.4 phosphate buffer, loracarbef was unexpectedly found to be 130-150 times more stable than cefaclor and 10-12 times more stable than cephalexin, depending on the phosphate concentration. The pH-stability profile is U-shaped, similar to that of other zwitterionic cephalosporins, and shows maximum stability at the isoelectric point. At any given pH, loracarbef is more stable in solution than any other therapeutically useful cephalosporin. Acetate, borate, citrate, and especially phosphate buffers have catalytic effects on the rate of loracarbef hydrolysis.

Cefaclor↗
PubMed1992

Comparison of cefprozil with other antibiotic regimens in the treatment of children with acute otitis media.

In two randomized clinical trials in children with otitis media, the efficacy and safety of cefprozil are compared to those of amoxicillin/clavulanate (n = 530) and of cefaclor and cefixime (n = 394). The rate of clinical cure or improvement was similar among patients receiving each drug regimen, ranging from 78% for amoxicillin/clavulanate to 89% for cefaclor; for cefprozil, this rate was 84% and 85% in the two studies, respectively. In the first study, cefprozil was superior to amoxicillin/clavulanate in the satisfactory clinical response rate for Streptococcus pneumoniae (P = .049), but response rates were similar for Haemophilus influenzae and Moraxella catarrhalis. Significantly more patients treated with amoxicillin/clavulanate (P less than .001) in the first study or cefixime (P less than .01) in the second study developed diarrhea than did those treated with cefprozil. We conclude that cefprozil therapy for otitis media in children produces clinical and bacteriologic response rates similar to those seen with amoxicillin/clavulanate, cefixime, or cefaclor. Furthermore, diarrhea was significantly less common with cefprozil than with cefixime or amoxicillin/clavulanate.

Acute Disease↗
PubMed1982

Effects of ureteral obstruction on the toxicity of cephalosporins in the rabbit kidney.

The nephrotoxicity of the cephalosporin antibiotics is closely related to their secretory transport into the proximal tubular cell at the antiluminal (blood) site. The present report describes the effects of transient ureteral obstruction, which increases intracellular concentrations of secreted organic anions, on the cortical uptake and the proximal tubular toxicity of several cephalosporins given in mildly toxic doses. Unilateral obstruction for 1-2 hr increased the cytotoxicity of cephaloglycin and cefaclor, both of which are rapidly secreted across the tubular cell, but not of cephaloridine, which undergoes minimal secretion. Bilateral obstruction significantly increased the toxicity of cefaclor, which is rapidly secreted, but not of cefazolin, which is slowly secreted. Finally, there was a further augmentation of the effects of obstruction on the toxicity of cefaclor by a minimally toxic pretreatment regimen of neomycin. Studies of cortical antibiotic concentrations support the conclusion that the effects on toxicity are largely the result of the increased intracellular accumulation that results from obstruction.

Animals↗
PubMed1985

In-vitro activity of Ro-15-8074, a new oral cephalosporin.

The in-vitro activity of Ro-15-8074, a new oral cephalosporin, was tested against common clinical isolates, and compared with the in-vitro activity of cefaclor, cefadroxil, ampicillin and co-trimoxazole. Its activity against Enterobacteriaceae was better than those of the other antibiotics tested. It was also highly active against Haemophilus influenzae, including beta-lactamase producing strains. Its activity against Pseudomonas aeruginosa and Acinetobacter spp., was poor. Ro-15-8074 was less active against staphylococci and group D streptococci than were cefaclor, cefadroxil and ampicillin. It was equally or less active than cefaclor, cefadroxil, ampicillin and co-trimoxazole against other streptococci.

Ampicillin↗
PubMed1979

A pharmacological and in vitro comparison of three oral cephalosporins.

The pharmacology of cephradine, cephalexin and a new oral cephalosporin, cefaclor, has been compared in six volunteers. Cefaclor was absorbed rapidly and was cleared from the serum more rapidly than the other two agents. This was probably partially due to its instability in serum at body temperature, which was investigated. Against a wide range of common pathogens cefaclor was the more active oral cephalosporin. In particular the activity against Neisseria gonorrhoeae and Haemophilus influenzae was of interest.

Administration, Oral↗
PubMedDate not supplied

Comparison of oral cephalosporins with penicillin therapy for group A streptococcal pharyngitis.

The purpose of the study was to compare the efficacy of cefaclor with that of penicillin V potassium (penicillin) in patients with Group A streptococcal pharyngitis. One hundred four children with pharyngitis and serologically confirmed Group A streptococci were randomly treated with cefaclor or penicillin using a mean dosage of 20 mg/kg/day for 10 days. The difference in failure rates (14% for 51 cefaclor- and 30% for 53 penicillin V-treated patients) was statistically significant (P = 0.04). In four earlier similar studies I found that cephaloglycin, cephalexin (two studies) and cefatrizine were consistently but not significantly more effective than penicillin therapy. When the data from the five studies are combined the difference between the failure rates (11% for 263 oral cephalosporin- and 23% for 230 penicillin-treated patients) becomes highly significant (P less than 0.001). The 95% confidence interval for the odds for treatment failure are 2.4 times greater for patients receiving penicillin than for those receiving one of the oral cephalosporins. On the basis of these data I conclude that the oral cephalosporins appear to be more effective than penicillin for therapy of Group A streptococcal pharyngitis.

Administration, Oral↗
PubMed1994

Variation in acceptance of common oral antibiotic suspensions.

Palatability of oral antibiotic suspensions is important and may be a substantial factor in determining compliance in young pediatric patients. Because no comparative systematic data are available, we undertook the present study to assess the acceptance of and compliance with oral antibiotic suspensions commonly used in Israel. During a 4-month period lists of children receiving oral antibiotic suspensions were obtained from 3 major pediatric clinics, and parents were contacted by telephone 10 to 14 days after initiation of therapy, at which time information on age, sex, main disease, prescribed drugs and duration of treatment was obtained. Information regarding acceptance, side effects and compliance was obtained from 11 questions with graded scores. In the study 546 children received one of the following drugs: amoxicillin (n = 222); cefaclor (n - 142); cefuroxime axetil (n = 107); trimethoprim/sulfamethoxazole (n = 75). No major differences in background data were noted; more than 50% of each group had acute otitis media. Seventy-three percent of the cefaclor group reported acceptance of the drug with "pleasure" or "without problems" vs. 60, 55 and 20% for amoxicillin, trimethoprim/sulfamethoxazole and cefuroxime axetil, respectively, whereas "resentment" or "refusal" was reported in 11, 16, 26 and 56%, respectively (P < 0.0001). Mothers reported to be generally "satisfied" or "extremely satisfied" with the drug in 89, 81, 74 and 67% with cefaclor, amoxicillin, trimethoprim/sulfamethoxazole and cefuroxime axetil, respectively, and 85, 77, 73 and 67% of the children, respectively, received the drug for the entire prescribed course (P < 0.001). Our data demonstrate that marked variations exist in acceptance and compliance of oral antibiotic suspensions with children.(ABSTRACT TRUNCATED AT 250 WORDS)

Administration, Oral↗
PubMed2005

Different patterns of cytokines, ECP and immunoglobulin profiles at two adverse drug reactions in a patient.

OBJECTIVES: Drug-induced hypersensitivity syndrome (HS) is a rare but life-threatening disease. We experienced carbamazepine-induced HS in a 14-year-old boy, who had cefaclor-induced cutaneous eruptions 15 months later. To clarify the mechanisms of HS and the differences between two diseases we studied this case in detail. METHODS: We investigated the associated viral agents by polymerase chain reaction and the specific antibodies. We also studied the mechanism of diseases by measuring chemical mediators including cytokines, ECP and immunoglobulins. RESULTS: The patient was diagnosed as having carbamazepine-induced HS associated with reactivation of human herpesvirus 6 based on the clinical course and laboratory data including drug-induced lymphocyte stimulation tests. Similarly, the diagnosis of cefaclor-induced eruption without any viral reactivation was made. Serum levels of IFN-gamma, IL-6, TNF-alpha, IL-5 and ECP were increased significantly at HS but mildly at cefaclor-induced eruptions. Furthermore, we detected transient hypogammaglobulinemia only at HS. CONCLUSIONS: This is the first report of anticonvulsant-induced HS followed by antibiotic-induced eruptions in a patient. In addition, we demonstrated difference in serum levels of inflammatory cytokines, immunoglobulins, activated eosinophils and viral reactivation between these diseases. This case would contribute to the understanding of the pathophysiology of adverse drug reactions including HS.

Adolescent↗
PubMed1992

Development of revised quality control limits for disk diffusion susceptibility tests of selected cephem antibiotics with Haemophilus influenzae and description of a new control strain.

Inconsistent quality control results in disk diffusion testing of cefaclor, cefamandole, cefonicid, and cefuroxime with Haemophilus influenzae ATCC 49247 and Haemophilus test medium (HTM) prompted a search for an alternative control strain that would provide more reliable results. A five-laboratory study was conducted to evaluate two candidate H. influenzae strains as possible alternatives to the aforementioned strain. Repetitive testing of the candidate strains and H. influenzae ATCC 49247 over several days with a total of six different lots of HTM documented consistent performance of the two candidate strains and confirmed inconsistent results for some of the antibiotics with H. influenzae ATCC 49247. In particular, certain lots of HTM failed to yield cefaclor and cefamandole zone sizes within the quality control range advocated by the National Committee for Clinical Laboratory Standards. Because of the greater consistency offered by the new strains, one was selected (now designated H. influenzae ATCC 49766) to be recommended for routine quality control testing of cefaclor, cefamandole, cefonicid, cefuroxime, and the related carbacephem loracarbef. The new control strain and zone size ranges proposed here have been approved by the National Committee for Clinical Laboratory Standards in place of the previously recommended strain and zone size limits for testing of these five cephem antibiotics.

Ampicillin↗
PubMed1988

In vitro activity of BMY-28100, a new oral cephalosporin.

BMY-28100 is a new orally absorbed cephalosporin whose in vitro activity was compared with that of cefaclor. BMY-28100 was more active against Staphylococcus aureus and Haemophilus influenzae than was cefaclor. In addition, there was only a small rise in MIC50 and MIC90 values for BMY-28100 when the inoculum size was increased 100- or 10,000-fold. In contrast, MIC50 and MIC90 values increased significantly for cefaclor with similar increases in inoculum size. These data suggest that BMY-28100 may be a promising agent to test for oral administration in infections caused by S. aureus and H. influenzae.

Cefaclor↗
PubMed1992

Clinical trials on pediatric lower-respiratory-tract infection: results and comments with cefetamet pivoxil.

A total of 30 pediatric patients suffering from lower-respiratory-tract infections were admitted to a three-arm, open, randomized study comparing two different doses of cefetamet pivoxil (either 10 or 20 mg/kg b.i.d.; groups A and B, respectively) with the standard cefaclor treatment (10 mg/kg t.i.d.; group C) for 7-12 days. The 30 cases were randomly assigned to the three treatment arms which were comparable with regard to demographics as well as to diagnosis on admission and concomitant medication. The children ranged from 1.08 to 12 years in age, and comprised 18 males and 12 females, with a weight range of 11-42 kg. As is to be expected in these patients, bacteriology was mostly not assessable. The overall clinical outcome was cure in 9, 8 and 9 cases, respectively, and improvement in 1, 2 and 0 cases, respectively. In the cefaclor group 1 patient failed to respond. Signs and symptoms of disease improved significantly in the three treatment groups; there were no intergroup differences. Vital signs (morning and evening temperature and pulse rate) improved in parallel. Radiological results had improved by the end of treatment in 9/10 patients in group A, in 10/10 patients in group B, and in 9/10 evaluable patients in group C. Mild to moderate nausea or vomiting were each reported in 1 patient in group A. Platelet increase was reported as a mild adverse event in 2 patients in each of the cefetamet pivoxil groups and in 4 patients given cefaclor.(ABSTRACT TRUNCATED AT 250 WORDS)

Bacterial Infections↗