In vitro antimicrobial activity comparison of cefaclor (compound 99638), cephradine, and cephalothin.
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Bacteria↗
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Cefaclor versus cephalexin: in vitro susceptibility testing of clinical isolates.
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Bacteria↗
[Cefaclor--a new, oral cephalosporin].
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Cephalosporins↗
[Cefaclor and its pathogen reducing effect in experimental acute pyelonephritis].
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Animals↗
In vitro and in vivo evaluations of BMY-28100, a new oral cephalosporin.
A new semisynthetic oral cephalosporin, BMY-28100, was evaluated for in vitro and in vivo antibacterial activities in comparison with cefaclor and cephalexin. BMY-28100 showed in vitro activity 3- and 10-fold more potent than that of cefaclor against Staphylococcus aureus and Streptococcus pneumoniae, respectively. BMY-28100 was slightly better than cefaclor and about 4 times more active than cephalexin against Haemophilus influenzae and Neisseria gonorrhoeae. Escherichia coli, Klebsiella pneumoniae and Proteus mirabilis were comparably susceptible to BMY-28100 and cefaclor. The bactericidal activity of BMY-28100 against S. aureus, E. coli and P. mirabilis was equal to or twice as high as MIC value, which was similar to that of cefaclor. The stability of BMY-28100 against penicillinases was nearly comparable to that of cefaclor, whereas cefaclor was somewhat unstable to cephalosporinases. BMY-28100 was about twice as active as cefaclor against three Gram-positive bacterial infections. BMY-28100 was also more potent against infections of H. influenzae and P. mirabilis, but slightly less active against E. coli Juhl than cefaclor. Blood level parameters of BMY-28100 were significantly superior to those of cefaclor and slightly better than cephalexin in mice and rats. The urinary recovery of BMY-28100 was somewhat higher and comparable to that of cefaclor and cephalexin, respectively. BMY-28100 was more stable than cefaclor in human and calf sera at 37 degrees C.
Animals↗
Cefprozil. A review of its antibacterial activity, pharmacokinetic properties, and therapeutic potential.
Cefprozil is an orally active cephalosporin which has demonstrated activity against a wide range of organisms in vitro. It is particularly active against the Gram-positive organisms Streptococcus pyogenes, pneumoniae and agalactiae and against methicillin-susceptible Staphylococcus aureus. Strains of methicillin-resistant S. aureus are not susceptible to cefprozil. Cefprozil is also moderately active against Haemophilus influenzae, Moraxella catarrhalis, Neisseria gonorrhoeae, many Enterobacteriaceae and certain anaerobic organisms, and is relatively stable to hydrolysis by a number of beta-lactamases. In comparative trials, the clinical and bacteriological efficacy of cefprozil 500mg or 20 mg/kg administered once or twice daily has been comparable with multiple daily dosage regimens of erythromycin in patients with tonsillitis or pharyngitis, with cefaclor and amoxicillin/clavulanate in lower respiratory tract infections, with amoxicillin/clavulanate and erythromycin in skin and skin-structure infections and with cefaclor in acute uncomplicated urinary tract infections. The clinical efficacy of cefprozil is similar to that of cefaclor in patients with tonsillitis or pharyngitis but the bacteriological efficacy of cefprozil is significantly greater than that of cefaclor. Cefprozil is clinically more effective than cefuroxime axetil in the treatment of lower respiratory tract infections and demonstrated greater efficacy than cefaclor in one of 2 comparative studies when administered twice daily in patients with skin and skin-structure infections. In children with acute otitis media, cefprozil 15 mg/kg twice daily was as effective as cefaclor or amoxicillin/clavulanate 13.3 mg/kg 3 times daily and was as effective as cefixime 8 mg/kg once daily. The most frequently reported adverse effects associated with cefprozil, diarrhoea and nausea, are usually mild to moderate in severity and discontinuation of treatment is rarely necessary. Thus, cefprozil with its convenient administration regimen appears to be a suitable alternative to cefaclor, cefixime, amoxicillin/clavulanate or erythromycin for the treatment of upper and lower respiratory tract infections, skin and skin-structure infections, and otitis media in children. While cefprozil has shown similar efficacy to cefaclor in the treatment of uncomplicated urinary tract infections, well-controlled clinical trials comparing its efficacy with that of cotrimoxazole (trimethoprim+sulfamethoxazole) in this indication are required.
Animals↗
[In vitro antibacterial activity of cefdinir against isolates of respiratory tract pathogens in children].
OBJECTIVE: To study the in vitro antibacterial activity of cefdinir against clinical isolates of respiratory tract pathogens in Children. METHODS: MIC values of cefdinir against 380 strains were determined with E-test method and compared with those of cefaclor. RESULTS: All penicillin-susceptible Streptococcus pneumoniae (PSSP) strains were also susceptible to cefdinir and cefaclor. Both cefdinir and cefaclor were not active against penicillin-resistant SP (PRSP). Against penicillin-intermediate SP (PISP) the susceptibility rates of cefdinir and cefaclor were 70.1% and 57.4%, respectively. The activity of cefdinir and cefaclor against beta-lactamases negative Hemophilus influenzae (HI) was excellent, but the susceptibility rates of cefdinir and cefaclor against beta-lactamases positive HI were 85.0% and 70.0%, respectively with MIC(90) of 1.5 mg/L vs. 256.0 mg/L. Cefdinir presented higher activities and lower MIC values than cefaclor against Moraxella catarrhalis (MC), Group A streptococcus (GAS), methicillin susceptible staphylococcus aureus (MSSA), and extended spectrum beta-lactamases (ESBLs) negative Escherichia coli (E. coli) or Klebsiella pneumoniae (K. pn). Both cefdinir and cefaclor were not susceptible to ESBLs positive E. coli and K. pn. CONCLUSIONS: Cefdinir exhibits excellent activity against PSSP, PISP, HI, as well as MC, GAS, MSSA and ESBLs negative E. coli or K. pn.
Anti-Bacterial Agents↗
Efficacy and safety of cefprozil versus other beta-lactam antibiotics in the treatment of lower respiratory tract infections.
Cefprozil was evaluated in four multicentre comparative studies in the treatment of acute respiratory tract infections. In two studies, cefprozil 500 mg q. 12 hours was compared to cefaclor 500 mg q. eight hours for ten days of therapy. Randomization was on a 2:1 (cefprozil:cefaclor) basis in the European centres and 1:1 in North America. The clinical efficacy in acute bronchitis was 88% (284 out of 324 patients) for cefprozil and 88% (183 out of 208) for cefaclor, with successful bacteriological eradication of the causative pathogen in 86% and 82% of the patients, respectively. Amongst the patients with acute exacerbations of chronic bronchitis, the clinical response rate of 80% (59 out of 74) for cefprozil appeared superior to that of cefaclor at 62% (p = 0.067), whilst the bacteriological response rates were 62% (36 out of 58) for cefprozil and 74% (20 out of 27) for cefaclor. In pneumonia, the clinical response rates for cefprozil and cefaclor therapy were similar, 82% vs. 79%, although bacteriological eradication rates were better for cefprozil at 82% than for cefaclor at 71%. In the comparison of cefprozil with cefuroxime axetil, a total of 170 patients were evaluable. The clinical and bacteriological response rates for cefprozil of 95% and 100% were better than those for cefuroxime axetil 500 mg q. 12 hours of 84% and 75%, respectively. In the cefprozil vs. amoxicillin-clavulanate, 500 mg q. eight hours comparative study, the two antibiotics displayed no significant difference in clinical or bacteriological responses.(ABSTRACT TRUNCATED AT 250 WORDS)
Adolescent↗
[Acute sinusitis in adults].
An average of 1.4% of the more than 30,000 participants in a treatment study were diagnosed as having acute sinusitis. 62% of all cases of sinusitis arose in patients aged between 15 and 44 years. Treatment with antibiotics is indicated in purulent sinusitis whilst non-purulent sinusitis is treated either with local or systemic antiphlogistic agents. The secondary bacterial infection is usually caused by Haemophilus influenzae, Streptococcus pneumoniae and anaerobic bacteria. In Scandinavia these probably account for 90% of the purulent sinusitis cases whilst Branhamella catarrhalis is responsible for the remaining 10%. Penicillin V is the agent of choice in acute sinusitis. Cefaclor is preferable in combatting H. influenzae. In a double blind study comparing doxycycline to cefaclor in the management of acute sinusitis (108 patients with cefaclor, 105 patients with doxycycline, no difference emerged between the two groups in the subjective assessment of the treatment results. Objective evaluation recorded excellent results for 88% and 83% of the patients in the cefaclor and doxycycline groups, respectively. Side-effects were noted by 7% of the cefaclor and by 13% of the doxycycline patients. The difference between the incidence of side-effects was not statistically significant. Taking into account the treatment results, the side-effects and ecological aspects, cefaclor is second only to penicillin as the agent of choice in suspected or confirmed purulent sinusitis (e. g. in presence of penicillin allergies or failure of the infection to respond to penicillin V).
Acute Disease↗
In vitro selection of resistance to four beta-lactams and azithromycin in Streptococcus pneumoniae.
Selection of resistance to amoxicillin (with or without clavulanate), cefaclor, cefuroxime, and azithromycin among six penicillin G- and azithromycin-susceptible pneumococcal strains and among four strains with intermediate penicillin sensitivities (azithromycin MICs, 0.125 to 4 microg/ml) was studied by performing 50 sequential subcultures in medium with sub-MICs of these antimicrobial agents. For only one of the six penicillin-susceptible strains did subculturing in medium with amoxicillin (with or without clavulanate) lead to an increased MIC, with the MIC rising from 0.008 to 0.125 microg/ml. Five of the six penicillin-susceptible strains showed increased azithromycin MICs (0.5 to >256.0 microg/ml) after 17 to 45 subcultures. Subculturing in medium with cefaclor did not affect the cefaclor MICs of three strains but and led to increased cefaclor MICs (from 0.5 to 2.0 to 4.0 microg/ml) for three of the six strains, with MICs of other beta-lactams rising 1 to 3 twofold dilutions. Subculturing in cefuroxime led to increased cefuroxime MICs (from 0.03 to 0.06 microg/ml to 0.125 to 0.5 microg/ml) for all six strains without significantly altering the MICs of other beta-lactams, except for one strain, which developed an increased cefaclor MIC. Subculturing in azithromycin did not affect beta-lactam MICs. Subculturing of the four strains with decreased penicillin susceptibility in amoxicillin (with or without clavulanate) or cefuroxime did not select for beta-lactam resistance. Subculturing of one strain in cefaclor led to an increase in MIC from 0.5 to 2.0 microg/ml after 19 passages. In contrast to strains that were initially azithromycin susceptible, which required >10 subcultures for resistance selection, three of four strains with azithromycin MICs of 0.125 to 4.0 microg/ml showed increased MICs after 7 to 13 passages, with the MICs increasing to 16 to 32 microg/ml. All azithromycin-resistant strains were clarithromycin resistant. With the exception of strains that contained mefE at the onset, no strains that developed resistance to azithromycin contained ermB or mefE, genes that have been found in macrolide-resistant pneumococci obtained from clinic patients.
Anti-Bacterial Agents↗
beta-Lactam drug allergens: fine structural recognition patterns of cephalosporin-reactive IgE antibodies.
Lack of experimental findings on the spectrum of cephalosporin allergenic determinants has hindered diagnosis of adverse reactions to these drugs and retarded understanding of allergenic cross-reactions between cephalosporins and between cephalosporins and penicillins. Subjects allergic to the widely used cephalosporin antibiotic cefaclor have serum immuno globulin (Ig) E antibodies that react with the drug. Quantitative hapten inhibition studies employing sera from subjects allergic to cefaclor revealed fine structural recognition differences between the combining site specificities of cefaclor-reactive IgE antibodies in the sera of different subjects. Unlike penicillins, where discrete side chain or thiazolidine ring determinants alone may be recognized, IgE binding determinants on cefaclor encompassed the entire molecule. Fine structural recognition specificity differences at positions R1 (side-chain) and R2 (substituent attached to dihydrothiazine ring) were detected between IgE antibodies in different sera. Some antibodies showed clear preferential recognition of the aminobenzyl group at position R1 and Cl at R2 while with others, a greater degree of recognition tolerance was seen at R1 where, for example, the aminohydroxybenzyl or aminodihydrobenzyl groups were recognized, and at R2 where a methyl or even an ester group was tolerated. As with the penicillins, cephalosporins as allergens cannot simply be considered as a group of compounds with a common allergenic determinant structure. IgE antibodies that bind to cefaclor show great heterogeneity indicated by clear, fine structural differences in recognition of the R1 and R2 groups on the drug.
Allergens↗
Antibiotic therapy for urinary tract infections.
Loracarbef, a member of the carbacephem class of beta-lactam antibiotics, was tested in randomized, double-blind, parallel studies for the treatment of uncomplicated urinary tract infections (UTIs). In one study conducted in the United States, a 7-day course of once-daily doses of loracarbef (200 mg) was compared with a 7-day course of multiple daily doses of cefaclor (250 mg three times a day). Analysis of data from a small, homogeneous patient population of 108 college-aged women showed that loracarbef produced clinical and bacteriologic responses similar to those produced by cefaclor. At 5-9 days posttherapy, bacteriologic cure was observed in 96% of patients in the loracarbef group and 90% of patients in the cefaclor group (p = 0.614); at 4-6 weeks post-therapy, the same cure rate (81%) was observed in both groups. Analysis of the larger (333 patients) and more heterogeneous study population containing several male and elderly female patients showed that loracarbef again produced responses similar to those produced by cefaclor, with no statistically significant differences seen between the groups at 5-9 days or at 4-6 weeks posttherapy. The adverse events reported by the loracarbef and cefaclor groups were also comparable in both the small and large patient populations analyzed. Similarly favorable results were seen when a 7-day regimen of loracarbef (200 mg once a day) was compared with a 7-day regimen of norfloxacin (400 mg twice a day) in a large European study of approximately 300 patients with uncomplicated cystitis. These studies demonstrate that the safety and efficacy of once-daily loracarbef are comparable to the safety and efficacy of multiple-dose/day therapy with other antimicrobial agents commonly used in the treatment of uncomplicated UTIs.
Cefaclor↗
[Cephalosporin treatment of maxillary sinusitis].
A new oral prodrug cephalosporin, cefcanel daloxate, was compared with cefaclor, another oral cephalosporin, in the treatment of acute purulent maxillary sinusitis. Three hundred fifty-four patients with purulent sinus secretion were recruited and randomized at thirteen European ENT clinics for the double blind study. The patients were treated with either cefcanel 300 mg tablets twice daily or cefaclor 250 mg capsules three times daily for ten days. Apart from the sinus puncture and secretion aspiration, the existence of sinus pain and purulent nasal secretion were inclusion criteria. Between days 12 and 15, reaspiration of the sinus was performed and signs and symptoms noted. The latter were checked again at the final visit between days 25 and 30. Samples of blood and urine were obtained for safety evaluation at inclusion, during and after treatment. The bacteriological culture of the purulent sinus secretion in 58.4% of patients revealed Haemophilus influenzae (37.9%) as the most prevalent pathogen followed by Streptococcus pneumonia (19.7%), while Streptococcus pyogenes, Branhamella catarrhalis, and Staphylococcus aureus amounted each to 6-7% only. The overall clinical outcome was defined as cure/improvement in 83.3% of the patients in the cefcanel group and 89.3% in the cefaclor group, respectively. No statistically significant differences with regard to efficacy were found between the two treatment groups. Adverse events, mostly related to gastrointestinal reactions, were reported by 36 patients (15.7%) in the cefcanel group and by 16 (13.4%) in the cefaclor group. Both cefcanel 300 mg twice daily and cefaclor 250 mg three times daily were highly effective with only minimal adverse events in the treatment of acute purulent maxillary sinusitis.
Acute Disease↗
Treatment of pharyngitis and tonsillitis with cefprozil: review of three multicenter trials.
Cefprozil is a new oral cephalosporin with an in vitro spectrum of activity that includes group A beta-hemolytic streptococci (Streptococcus pyogenes). Three multicenter, randomized trials were conducted for comparing the clinical efficacy and safety of cefprozil administered once or twice daily with that of cefaclor, penicillin, or erythromycin ethylsuccinate administered three or four times daily in the treatment of mild-to-moderate tonsillopharyngitis. In the cefprozil-cefaclor trial, the pathogen eradication rate for evaluable patients receiving cefprozil was 83%, which was significantly better than that for patients receiving cefaclor (76%) (P = .035). The rate of satisfactory clinical response was similar with cefprozil (89%) and cefaclor (84%). The overall response rate was significantly better with cefprozil (80%) than with cefaclor (72%, P = .018). Differences in response rates were not noted when analyzing only patients 2-12 years of age. In the cefprozil-penicillin trial, the eradication rate of bacteriologic pathogens was similar in patients receiving cefprozil (91%) and in patients receiving penicillin (87%). A satisfactory clinical response was seen in 95% of the evaluable cefprozil-treated patients, which was significantly better than the rate of satisfactory clinical response seen in the penicillin-treated patients (88%; P = .023). In addition, during-therapy cultures for penicillin-treated patients yielded a significantly higher rate of beta-lactamase-producing Staphylococcus aureus than did those for the group of cefprozil-treated patients (13% vs. 4.5%, respectively; P = .046). Significantly more clinically symptomatic bacteriologic failures occurred in the penicillin group (P = .037).(ABSTRACT TRUNCATED AT 250 WORDS)
Cefaclor↗
Effect of two antibiotics on human granulocyte activities.
As part of a study of the effects of antibiotic therapy upon human phagocytes, ampicillin and cefaclor were each administered orally to nine healthy adult subjects in a single dose of 500 mg. There was a significant difference in their effects on neutrophil myeloperoxidase (MPO) (EC.1.11.1.7) activity (P less than 0.05) in that ampicillin depressed, but cefaclor enhanced, the measured enzyme activity. Concomitantly ampicillin decreased but cefaclor increased, the rate of phagocytosis of staphylococci, the effects of the two antibiotics also being significantly different (P less than 0.05). Direct measurements of intracellular killing of staphylococci did not change. In four patients with chronic bacterial infections who had low levels of neutrophil MPO activity, treatment with cefaclor led to a significant increase in the MPO levels to within the normal range. Three patients responded satisfactorily to cefaclor despite having previously filed to respond to antibiotics which were similarly active in vitro against the causative bacteria. These findings lead us to suggest that, in patients with chronic refractory infections, attention must be given to the effect of drugs on the host defences in addition to a careful choice of the most active antibacterial agent.
Adult↗
Impaired bacteriologic response to oral cephalosporins in acute otitis media caused by pneumococci with intermediate resistance to penicillin.
BACKGROUND: Penicillin resistance of Streptococcus pneumoniae, one of the most common causes of acute otitis media, has recently increased and is now highly prevalent in many regions. However, its contribution to clinical failure still must be proved. Because the role of antibiotics in acute otitis media is to eradicate the pathogens present in the middle ear fluid, we conducted a randomized controlled study to determine bacterial eradication of pathogens in acute otitis media by two commonly used oral cephalosporins, cefuroxime axetil (30 mg/kg/day) and cefaclor (40 mg/kg/day). METHODS: Patients 6 to 36 months old with pneumococcal otitis media seen in the Pediatrics Emergency Room were studied. An initial middle ear fluid culture was obtained at enrollment, and a second culture was obtained on Day 4 or 5 during treatment. Follow-up was done also on Days 10, 17 and 42 after initiation of treatment. In cases of clinical relapse a third culture was obtained. RESULTS: In total 78 patients were enrolled, 41 in the cefuroxime axetil group and 37 in the cefaclor group. Of the 78 S. pneumoniae isolates 31 (40%) were intermediately penicillin-resistant (MIC 0.125 to 1.0 microgram/ml). Of the 47 patients with penicillin-susceptible organisms 3 (6%) had bacteriologic failure vs. 4 of 19 (21%) and 7 of 11 (64%) of those with MIC of 0.125 to 0.25 microgram/ml and 0.38 to 1.0 microgram/ml, respectively (P < 0.001). For intermediately resistant pneumococci, in 7 of 12 (58%) of those receiving cefaclor the isolate was not eradicated vs. only 4 of 19 (21%) of those receiving cefuroxime axetil (P = 0.084). MIC to the administered cephalosporin of > 0.5 microgram/ml was associated with bacteriologic failure. Clinical failure was observed in 9 of 14 (64%) patients with bacteriologic failure vs. 10 of 52 (19%) patients with bacteriologic eradication (P = 0.003). CONCLUSION: Intermediately penicillin-resistant S. pneumoniae is associated with an impaired bacteriologic and clinical response of acute otitis media to cefaclor and cefuroxime axetil. This effect was more pronounced with cefaclor than with cefuroxime axetil.
Acute Disease↗
In vitro and in vivo antibacterial properties of FK 027, a new orally active cephem antibiotic.
FK 027 was more active than cefaclor, cephalexin, and amoxicillin against stock strains of a wide variety of gram-negative bacteria, including such opportunistic pathogens as Citrobacter and Enterobacter species and Serratia marcescens. FK 027 was significantly more active than the three reference drugs against clinical isolates of Escherichia coli, Klebsiella pneumoniae, indole-positive and -negative Proteus species, Providencia species, Haemophilus influenzae, and Neisseria gonorrhoeae. It was less active than cefaclor, cephalexin, and amoxicillin against staphylococci, but it was similar to cefaclor in its activity against streptococci. With few exceptions, FK 027 was active against strains of E. coli, K. pneumoniae, and Proteus mirabilis that were resistant to the reference agents. The bactericidal activity of FK 027 against various gram-negative bacteria, including Proteus species, Citrobacter freundii, Enterobacter aerogenes, and S. marcescens, was greater than that of cefaclor, cephalexin, and amoxicillin. The therapeutic activities of FK 027 in mice infected with gram-negative bacilli were far superior to the activities of cefaclor, cephalexin, and amoxicillin, but they were inferior to the activities of these reference drugs against infection with Staphylococcus aureus.
Amoxicillin↗
BMY 28100, a new oral cephalosporin.
BMY 28100, a new oral cephalosporin with a (Z)-propenyl side chain at the 3 position and a p-hydroxyphenylglycyl substituent at the 7 position, was evaluated in comparison with cefaclor and cephalexin and, when appropriate, ampicillin and vancomycin. In vitro, BMY 28100 was more active than the reference cephalosporins against streptococci, Staphylococcus aureus, Staphylococcus epidermidis, Listeria monocytogenes, Haemophilus influenzae, Propionibacterium acnes, Clostridium perfringens, and Clostridium difficile. BMY 28100 was comparable to cefaclor and more active than cephalexin against Staphylococcus saprophyticus and ampicillin-susceptible strains of Branhamella catarrhalis; but against ampicillin-resistant strains of B. catarrhalis, BMY 28100 was comparable to cephalexin and more active than cefaclor. Against Neisseria gonorrhoeae, BMY 28100 was comparable to cephalexin, but less active than cefaclor. Members of the family Enterobacteriaceae overall were equally susceptible to BMY 28100 and cefaclor but were less susceptible to cephalexin. In human serum, BMY 28100 was 45% protein bound. After an oral dose to mice, 82% of the drug was recovered in urine. The oral therapeutic efficacy of BMY 28100 in systemically infected mice reflected its activity in vitro.
Animals↗