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[Laboratory and clinical studies on cefprozil in the field of pediatrics].

Laboratory and clinical studies on cefprozil (CFPZ, BMY-28100), a new cephem antibiotic, were carried out in the field of pediatrics. The results obtained are summarized as follows: 1. Serum concentrations, urinary concentrations and urinary recovery rates of CFPZ were determined upon oral administration of CFPZ after meal at doses of 4 mg/kg granules in a case, 7.5 mg/kg granules in 2 cases and 15 mg/kg granules in one. Peak serum levels of CFPZ were obtained at an hour in 3 cases and at 2 hours in 1 case after administration of the drug with a range of 2.7-8.6 micrograms/ml with half-lives of 0.69-0.95 hours. Urinary recovery rates in the first 6 hours after administration ranged from 59.4-71.3%. 2. MICs of CFPZ against 36 clinical isolates (Staphylococcus aureus 4 strains, Streptococcus pneumoniae 5, Streptococcus pyogenes 5, Escherichia coli 5, Haemophilus influenzae 12, Haemophilus parainfluenzae 4, and Branhamella catarrhalis 1) were compared with those of cefaclor (CCL) and ampicillin (ABPC). The antibacterial activity of CFPZ was superior to those of CCL against Gram-positive cocci, and to those of ABPC against E. coli, and was equal to those of CCL and inferior to those of ABPC against H. influenzae. 3. Thirty-seven pediatric patients with acute infectious diseases (pharyngitis/tonsillitis 17, bronchitis 7, pneumonia 3, skin and soft tissue infection 2, and urinary tract infection 8) were treated with CFPZ at daily doses of 10-47 mg/kg t.i.d. as a rule. The efficacy rates were 100% clinically and 56% bacteriologically. 4. Side effects or abnormal laboratory test values were not observed except for an increased platelet count in 1 case and elevated GOT, GPT values in 2 cases.

Bacteria↗

[Pharmacokinetic, bacteriological and clinical studies on cefprozil in pediatric patients].

Cefprozil (CFPZ, BMY-28100), a new oral cephem antibiotic, was studied for its antibacterial activities, absorption and excretion upon administration. Its clinical efficacies were also studied in pediatric patients with infections. A study on antibacterial activities of CFPZ against 11 clinical isolates including 6 species found that its activities against Staphylococcus aureus, alpha-hemolytic Streptococcus, Escherichia coli and Haemophilus influenzae were equal or superior to those of CCL. When CFPZ was given to patients orally at 15 mg/kg, maximum serum concentration was obtained between 1 to 2 hours after administration and urinary excretion rate in the first 6 hours was 33.8 +/- 17.6%. Clinical evaluation was done in a total of 25 patients with various infections. Responses were excellent in 15 cases and good in 10 cases, hence the efficacy rate was 100%. As side effect, soft stool was found in 1 case, and eosinophilia in 2 cases and elevation of GOT and GPT in 1 case were found as abnormal laboratory test results, but none of them was serious. It appears that CFPZ is an effective and safe antibiotic in the field of pediatrics.

Bacteria↗

[Laboratory and clinical studies of cefprozil in pediatric field].

Laboratory and clinical studies were done on cefprozil (CFPZ, BMY-28100). The results are summarized as follows. CFPZ was administered through the oral route to 2 children at a single dose of 7.5 mg/kg. After administration, peak serum levels of CFPZ obtained in the 2 cases were 6.71 micrograms/ml at 1 hour and 6.45 micrograms/ml at 2 hours, respectively and half-lives were 1.28 hours and 0.92 hour, respectively. The urinary excretion rates of CFPZ were 58.9% and 59.4%, respectively. Treatment with CFPZ was made in 37 cases of pediatric bacterial infections: 1 case of pharyngitis, 16 cases of tonsillitis, 16 cases of scarlet fever, 3 cases of impetigo, 1 case of UTI. Results obtained were excellent in 24 cases, good in 13 cases. No significant side effects due to the drug were observed, except 1 case of loose stool, 3 cases of eosinophilia, and 1 case each of elevated GOT and GPT.

Bacteria↗

Mode of antibacterial action of cefprozil, a new cephalosporin, on Escherichia coli, Serratia marcescens and Morganella morganii.

The mode of antibacterial action of cefprozil (CFPZ, BMY-28100), a newly developed cephalosporin, was investigated using Escherichia coli K12, Serratia marcescens IFO 12648 and Morganella morganii IFO 3848 as test organisms, in comparison with the action of cefaclor (CCL). The minimum inhibitory concentrations (MICs) of CFPZ for these organisms were 1.56, 800 and 25 micrograms/ml, whereas those of CCL were 1.56, 800 and 100 micrograms/ml, respectively. The addition of a subinhibitory concentration (1/4 MIC) of ethylenediaminetetraacetic acid (EDTA), which damages the permeability barrier of the outer membrane, markedly reduced the MICs of CFPZ for E. coli and S. marcescens, compared with those of CCL, whereas the MICs of both antibiotics for M. morganii were hardly affected by the presence of EDTA. CFPZ was more stable to beta-lactamase activities from these organisms than CCL. The cross-linking reactions of peptidoglycan synthesis catalyzed by the ether-treated cells from these organisms were inhibited by a lower concentration of CFPZ than of CCL.

Bacteria↗

Cefprozil and respiratory tract infections in children.

Respiratory tract infections are the leading cause of children's visits to physicians. Antibiotic resistance is increasing among the three most common bacterial respiratory pathogens, Streptococcus pneumoniae, Haemophilus influenzae and Moraxella catarrhalis, which cause acute otitis media and sinusitis. Therefore clinicians may need to reexamine their treatment strategies because these infections may cause complications. Antibiotic selection in such infections should take into account local bacterial resistance patterns, anticipated clinical efficacy against S. pneumoniae, H. influenzae and M. catarrhalis, including penicillin-resistant and beta-lactamase-producing strains, as well as the safety profile and compliance-enhancing features of the drug.

Cephalosporins↗

Cefprozil.

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Bacterial Infections↗

Antimicrobial drug suspensions: a blinded comparison of taste of twelve common pediatric drugs including cefixime, cefpodoxime, cefprozil and loracarbef.

We conducted a blinded taste test evaluating 12 antimicrobial suspensions by smell, texture, taste, aftertaste and overall acceptance. Drugs received cumulative scores in each category as well as a total score ranking. Overall Lorabid scored highest but not significantly higher than Keflex, Suprax and Ceclor, all of which score higher than the other test drugs. Cefzil and Augmentin scored just below this group of drugs and higher than all other test drugs. Vantin was inferior to these drugs primarily because of its low score in aftertaste. It was ranked along with V-Cillin-K, Veetids, Sulfatrim and Pediazole, the lowest scoring group of drugs other than Dynapen which scored lower than all other test drugs. No difference overall was detected between the two penicillin VK suspensions evaluated, V-Cillin-K and Veetids.

Analysis of Variance↗

[Cefprozil].

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Cephalosporins↗

[Resistance surveillance of common community respiratory pathogens isolated in China, 2002 - 2003].

OBJECTIVE: To investigate antimicrobial resistance of common community respiratory pathogens isolated in China, 2002 - 2003. METHODS: 779 strains of Streptococcus pneumoniae, Haemophilus influenzae, Moraxella catarrhalis, Group A beta-haemolytic Streptococci and oxacillin-susceptible Staphylococcus aureus (MSSA) were isolated from patients with community-acquired respiratory tract infections at 5 hospitals in China from April 2002 to 2003. Meanwhile, 185 strains of S. pneumoniae, H. influenzae and M. catarrhalis were isolated from nasopharynx swabs at 2 day-care centers in Beijing. Agar dilution method was used to determine the minimal inhibitory concentration (MICs) of cefprozil and other 9 antibiotics against these strains. RESULTS: The prevalence of penicillin-intermediate S. pneumoniae (PISP) was 23.9% and that of penicillin-resistant S. pneumoniae (PRSP) was 22.7% at 5 cities in China. The prevalence of PISP were 44.1% in Hangzhou, 26.2% in Wuhan, 21.5% in Shenyang, 20.8% in Shanghai, 18.5% in Beijing, and 12.7% at day-care centers in Beijing;the prevalance of PRSP were 34.9% in day-care centers, 31.9% in Shanghai, 27.9% in Wuhan, 22.1% in Hangzhou, 13.8% in Shenyang and 8.6% in Beijing. The susceptible rate of levofloxacin in S. pneumoniae was 96.3%. 9.5% of H. influenzae and 87.4% of M. catarrhalis produced beta-lactamases. The susceptibility of amoxicillin/clavulanate, cefaclor, cefprozil, cefuroxime, ceftriaxone, azithromycin, and levofloxain in these two species ranged from 96.4% to 100%. The resistance rate of azithromycin in S. pneumoniae was higher than 60%. Cefprozil MICs against PISP, Group A beta-haemolytic Streptococci and MSSA were 4 - 16 fold lower than cefaclor. CONCLUSIONS: Antimicrobial resistance in respiratory pathogens, especially S. pneumoniae is increasing. It brings concerns that high macrolide resistance was found in gram-positive cocci. Cefprozil was more active than cefaclor against respiratory pathogens.

Anti-Bacterial Agents↗