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Cefaclor levels in human aqueous humor.

In an attempt to investigate penetration of cefaclor into human aqueous humor, we administered 500-mg and 1-g doses of cefaclor to 39 patients about to undergo cataract extraction. Average aqueous humor levels of 0.27, 0.27, and 0.17 microgram/mL were achieved at 1, 2, and 4 hours, respectively, after the 500-mg oral dose. After 1 g orally, we found average aqueous humor levels of 0.61, 0.64, 0.72, 0.4, and 0.31 microgram/mL at 1, 2, 3, 4, and 5 hours, respectively. Therapeutic levels in primary aqueous humor were consistently achieved against Streptococcus pneumoniae and St pyogenes, group A.

Aqueous Humor↗

[In vitro activity of cefaclor against Haemophilus influenzae in comparison to various oral chemotherapeutic agents (author's transl)].

The antibacterial activity of cefaclor against 100 non-beta-lactamase producing and 11 beta-lactamase producing isolates of Haemophilus influenzae was compared with that of cephalexin, ampicillin, chloramphenicol, tetracycline and co-trimoxazole. A new standardized microtiter dilution technique was used. Cefaclor showed greater activity than did cephalexin and inhibited beta-lactamase producing H. influenzae isolates. Ampicillin was the most active compound against non-beta-lactamase producing isolates. One of our strains was resistant to chloramphenicol and one resistant to tetracycline.

Ampicillin↗

[Influence of cefaclor on experimental pyelonephritis (author's transl)].

A comparative study on the antibiotic activity of cefaclor and cephradine was performed in an infection and therapy model of acute pyelonephritis in the rat. Pathogens were Escherichia coli and Klebsiella pneumoniae. The antibiotics, which were administered orally, both had a pronounced effect in comparison to the untreated control group. Cefaclor was superior to cephradine in infections caused by K. pneumoniae.

Animals↗

[Comparative study of cefaclor versus amoxicillin in urinary tract infections (author's transl)].

In a comparative, prospective, open randomised clinical study, the efficacy and tolerance of cefaclor (3 x 500 mg) and amoxicillin (3 x 750 mg) in the treatment of urinary tract infection (UTI) were investigated and compared. A total of 110 patients (51 males and 59 females) age 10 to 83 years were treated for a period of five to 14 days (average 10 days). Fifty-nine of the patients had complicated, and 51 uncomplicated UTI. In all patients , organisms were cultured from the urine which were sensitive to both antibiotics in vitro. In each group there were three cases of mixed infection and 35 cases of Escherichia coli monoinfection. The distribution of pathogens in the other patients was likewise very similar. Better results, i.e. a reduction in the cell count to < 10(4)/ml immediately after completion of therapy, were obtained in patients treated with cefaclor. This is largely due to a statistically significantly higher rate of elimination in E. coli infections. The long-term results at follow-up examinations 14 to 60 days after completion of therapy in both groups with uncomplicated infections were, however, equally as good in about half the cases. In complicated infections therapy was successful overall in only about a quarter of the cases, better results being obtained in the amoxicillin group. It must be taken into account that among the patients treated, the groups with complicated UTI are difficult to compare, relapses primarily being determined by underlying disease. Both antibiotics were tolerated well.

Adolescent↗

[Cefaclor in dermatological therapy (author's transl)].

Thirty patients suffering from bacteriogenic skin diseases were given cefaclor, in most cases simultaneously with classical external dermatological therapy. The results of therapy were satisfactory in 29 of the 30 patients. Only in one relatively severe case of erysipelas did the disease continue to spread despite the daily doses of 3 x 500 mg of oral cefaclor prescribed by the dosage regimen. Side-effects observed consisted of diarrhoea in one patient, and a transient slight increase of SGOT or alkaline phosphatase in another six patients.

Alkaline Phosphatase↗

Azithromycin versus cefaclor in the treatment of pediatric patients with acute group A beta-hemolytic streptococcal tonsillopharyngitis.

An open, comparative multicenter study was performed to evaluate the efficacy and safety of azithromycin (10 mg/kg) given once daily for three days in comparison with cefaclor (30 mg/kg) divided into three daily doses and given for a period of ten days. One hundred and twenty-two children aged 1-12 years with clinical symptoms of group A beta-hemolytic streptococcal tonsillopharyngitis and a positive throat culture were randomly allocated to the treatment groups. Overall, the clinical success (cure or improvement) of both regimens was identical in the evaluable patients (86.3%, 44 of 51 patients in either treatment group). In contrast, bacterial eradication after completion of treatment was lower with azithromycin than with cefaclor. Possible reasons for this discrepancy between clinical success and eradication rates could be antibiotic resistance, pre-disease carriage or insufficient dosage. Both agents were well tolerated; only mild or moderate side effects most frequently involving the gastrointestinal tract, were recorded in either therapy group.

Anti-Bacterial Agents↗

Revised disk diffusion interpretive criteria for cefaclor, loracarbef, cefprozil and cefixime when testing Haemophilus influenzae on haemophilus test medium.

The aim of the current five-center collaborative study was to reassess the interpretive criteria for cefaclor, loracarbef, cefprozil and cefixime previously adopted or proposed by the National Committee for Clinical Laboratory Standards (NCCLS) for disk diffusion susceptibility tests with Haemophilus influenzae on Haemophilus Test Medium (HTM) agar. MICs and zones of inhibition were determined using NCCLS methods, HTM and two collections of strains of Haemophilus influenzae. One group of strains consisted of 118 stock organisms taken largely from various recent U.S. antibiotic resistance surveillance studies. The emphasis in this selected group of organisms was on strains that were beta-lactamase negative but ampicillin resistant (BLNAR) by some other mechanism. The second collection of test organisms consisted of 50 recent clinical isolates of Haemophilus influenzae obtained from each of the five participating study centers. This group was considered representative of the type of Haemophilus influenzae currently recovered from clinical sources in the USA. Frequency distribution assessment and error-rate bounded analysis of scattergram comparisons of MICs and zone sizes were used to develop the following zone diameters interpretive for disk diffusion susceptibility tests with Haemophilus influenzae on HTM agar: cefaclor, > or = 20 mm (susceptible, S) and < or = 16 mm (resistant, R); loracarbef, > or = 19 mm (S) and < or = 15 mm (R); and cefprozil, > 18 mm (S) and < 14 mm (R). The respective MIC correlates for all three antimicrobial agents were < or = 8 micrograms/ml (S) and 32 micrograms/ml (R).(ABSTRACT TRUNCATED AT 250 WORDS)

Cefaclor↗

Semi-quantitative analysis of cefaclor in human serum by capillary high performance liquid chromatography/fast atom bombardment mass spectrometry.

Capillary high performance liquid chromatography (HPLC) was combined with frit fast atom bombardment (FAB) mass spectrometry (MS) and a detailed procedure has been established for on-line analysis of cefaclor in human serum. The capillary column (0.3 mm i.d.) enabled the introduction of entire effluent to the frit interface for FAB-MS; and a special column switching device for injection and concentration enabled the injection of as large as a 500-microliters volume sample. These conditions gave much higher sensitivity than that of previous HPLC/MS system. Thus, low levels of cefaclor could be successfully identified in sera by its mass spectral measurements 2 h after its single oral administration of a 250-mg capsule in two subjects.

Administration, Oral↗

Susceptibility of United States clinical trial isolates to cefprozil and cefaclor.

First bacterial isolates (n = 2022) from patients enrolled in the United States cefprozil clinical trials were tested for susceptibility to cefprozil and cefaclor. Cefprozil was two- to eightfold more active than cefaclor against Gram-positive bacteria based on minimum inhibitory concentration (MIC50 and MIC90) values. The differential was greatest, for the most part, for the 80% of isolates of each species with the lowest MICs. Against Gram-negative bacterial species, the two cephalosporins were very similar in activity and MIC90 values ranged from 2 to 8 micrograms/ml for the most prevalent pathogens except Enterobacter spp., which were resistant. The majority of streptococci (98%) were susceptible to < or = 0.5 microgram/ml of cefprozil, and the majority of staphylococci tested (> 90%) were susceptible to < or = 4 micrograms/ml of cefprozil. These results for isolates primarily from community-acquired infections were similar to previously reported results from uncharacterized or hospital-associated isolates.

Cefaclor↗

Serum sickness-like reactions from cefaclor in children.

Cefaclor is an oral semisynthetic cephalosporin that is popular in the treatment of infections in children. This drug has been associated with a serum sickness--like reaction characterized by an urticarial eruption, pruritus, arthritis, and/or arthralgias. We report 12 additional cases of cefaclor-related serum sickness--like reactions in children. All patients improved after discontinuation of the drug and no long-term complications resulted.

Cefaclor↗

Treatment of chronic sinusitis with open drainage and cefaclor.

A prospective study of 50 adult patients with chronic sinusitis was undertaken. Forty patients were treated with the Caldwell-Luc operation and postoperative cefaclor, and 10 underwent nasal antrostomy and treatment with cefaclor. Approximately 85% of the 40 patients had resolution of symptoms with this treatment. The microbiology of chronic sinusitis was studied through aerobic and anaerobic cultures of sinus secretions obtained at surgery. Staphylococcus aureus (coagulase-negative) and Propionibacterium sp were found to be the most common pathogens. The radiologic results of Caldwell-Luc surgery were studied through comparison of preoperative and postoperative radiographs in 33 of these patients. An air-fluid level is the only radiographic sign of consistent diagnostic significance in the postoperative radiograph.

Adult↗

Short-course therapy with cefaclor for treatment of streptococcal pharyngotonsillitis.

Short-course treatments for streptococcal pharyngotonsillitis with oral cephalosporins or macrolides have resulted in a similar bacteriological and clinical cure rate and better compliance compared with the conventional 10-day course. One hundred and thirty eight of 420 recruited patients had a positive culture for Streptococcus pyogenes and were randomly assigned to receive cefaclor (25 mg/kg/bid) for a 5-day (70 patients) or 10-day (68 patients) course. Patients were assessed clinically and bacteriologically 2-3 days after completing the course and followed up after 20-30 days. All 420 recruited patients belonged to a population of 2800 children who had been previously screened for a streptococcal carrier state to exclude carriers from final evaluation. Clinical cure and bacterial eradication was recorded in 92.8 and 92.6% of patients in groups A and B, respectively. Therefore, short-course therapy with cefaclor may offer an effective alternative treatment to conventional regimens, with potential for better compliance.

Cefaclor↗

Solid-state chemistry and crystal structure of cefaclor dihydrate.

Cefaclor [7-(D-2-amino-2-phenylacetamido)-3-chloro-3-cepham-4-carboxy lic acid] crystallizes as the dihydrate. Crystals belong to space group P21, with a = 10.626(3), b = 7.1288(9), c = 14.124(3), and beta = 121.6(2). The structure was solved using direct methods and refined to an R of 0.0535. The bond lengths, angles, and conformation determined are as expected for cephalosporins. The two water molecules are held in the crystal differently. The 13C solid-state NMR spectrum of cefaclor dihydrate is also reported and is consistent with its crystal structure.

Cefaclor↗

Cefaclor and amoxycillin in the treatment of infective exacerbations of chronic bronchitis.

The clinical effectiveness of cefaclor 500 mg three times daily in the treatment of acute infective exacerbations of chronic bronchitis has been investigated by a double-blind comparison with amoxycillin in the same dose in 30 in-patients and 50 out-patients. The two antibiotics were equally effective, in terms of resolution of presenting symptoms, sputum conversion and fall in 24 h sputum weight. Side effects were infrequent. Serum and sputum concentrations of antibiotics and 24 h urinary recovery were measured in 27 patients. Concentration of both cefaclor and amoxycillin was found to be significantly lower in mucoid sputum than in purulent sputum, in contrast to earlier reports in the case of amoxycillin. No clinical advantage was apparent for patients achieving higher sputum concentration of either antibiotic.

Aged↗

Effects of cefaclor, cefetamet and Ro 40-6890 on inflammatory responses of human granulocytes.

The effect of three cephalosporins (cefetamet, cefaclor and Ro 40-6890) upon human granulocytes and their ability to modulate the chemiluminescence response, phagocytose, kill bacteria and generate leukotrienes was studied. In the presence of the cephalosporins there was a significant increase in phagocytosis of Escherichia coli. The bactericidal activity of human granulocytes for several other bacteria was also enhanced. Cefetamet and cefaclor increased the chemiluminescence response of human neutrophils to Pseudomonas aeruginosa and Proteus mirabilis in contrast to Ro 40-68790, which decreased the chemiluminescence response. The cephalosporins decreased the synthesis of leukotrienes from human neutrophils after stimulation with Escherichia coli and Staphylococcus aureus. These data emphasize the immunomodulatory functions of various cephalosporins on cells involved in host defence.

Cefaclor↗

Amoxicillin-clavulanate potassium compared with cefaclor for acute otitis media in infants and children.

One hundred thirty-three infants and children with documented acute otitis media (OM) were randomized to receive the oral suspension of either amoxicillin-clavulanate potassium or cefaclor. Beta-lactamase-producing bacteria were found in 10.9 and 14.5% of subjects treated with amoxicillin-clavulanate potassium and cefaclor, respectively. Subjects were reexamined at 5, 10, 30, 60 and 90 days after the initiation of therapy and whenever signs/symptoms of acute otitis media recurred. All but two children had resolution of otalgia/otorrhea during the initial treatment period. The drug groups were not significantly different in the percentage of evaluable subjects with otitis media with effusion at each scheduled follow-up visit. Recurrence of acute OM/otorrhea [corrected] developed in a similar percentage of subjects in both treatment categories. Both subjects with and those without middle ear effusion at 10 days had approximately a 50% recurrence rate of subsequent middle ear disease. Adverse side effects/complaints, which occurred in significantly more children treated with amoxicillin-clavulanate potassium, were generally mild and primarily gastrointestinal.

Acute Disease↗

Pharmacokinetics of cefadroxil and cefaclor during an eight-day dosage period.

The concentrations of cefadroxil and cefaclor in serum were studied in eight healthy volunteers receiving 1,000 mg of both substances three times per day for 8 days. Intraindividual comparisons showed an increase in peak serum levels of cefadroxil from days 1 to 8 in seven of eight volunteers. Cefaclor peak concentrations did not rise during the 8 days.

Adult↗