cefzil and Bacterial-Infections

To discuss the pharmacokinetics, spectrum of activity, clinical trials, and adverse effects of cefprozil, cefpodoxime proxetil, loracarbef, cefixime, and ceftibuten, an investigational cephalosporin.. Literature was identified by a MEDLINE search from 1986 to January 1995.. Randomized, controlled studies were selected for evaluation; however, uncontrolled studies were included when data were limited for indications approved by the Food and Drug Administration.. Data were evaluated with respect to in vitro activity, study design, clinical and microbiologic outcomes, and adverse drug reactions.. Cefprozil, cefpodoxime proxetil, loracarbef, cefixime, and cefributen are active in vitro against organisms frequently involved in community-acquired infections such as Streptococcus pneumoniae, Escherichia coli, beta-lactamase-positive or -negative Haemophilus influenzae, and Moraxella catarrhalis. Except for cefixime and ceflibuten, they all are active against methicillin-susceptible Staphylococcus aureus. Even though there were problems in study design (discussed within the text), clinical data demonstrate that these new oral beta-lactam compounds are as efficacious as conventional therapies for a variety of community-acquired infections.. Cefprozil, cefpodoxime, cefixime, loracarbef, and ceftibuten demonstrate in vitro activity against the major organisms that cause community-acquired infections. Clinical trials confirm that these agents are as effective as traditional therapies for the management of acute otitis media, pharyngitis/tonsillitis, sinusitis, bronchitis, pneumonia, urinary tract infections, and skin and skin-structure infections. In addition, cefixime and cefpodoxime are effective therapies for uncomplicated gonococcal infections. Selection of a specific agent will be influenced by susceptibility data and safety, as well as issues of compliance and cost.

Topics: Bacterial Infections; Cefixime; Cefotaxime; Cefpodoxime Proxetil; Cefprozil; Ceftibuten; Ceftizoxime; Cephalosporins; Humans; Microbial Sensitivity Tests; Prodrugs; Randomized Controlled Trials as Topic

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)

Topics: Adolescent; Adult; Amoxicillin; Amoxicillin-Potassium Clavulanate Combination; Anti-Bacterial Agents; Bacterial Infections; Bronchitis; Cefaclor; Cefprozil; Cefuroxime; Cephalosporins; Clavulanic Acids; Drug Therapy, Combination; Female; Humans; Male; Multicenter Studies as Topic; Pneumonia; Prodrugs; Randomized Controlled Trials as Topic; Respiratory Tract Infections

Cefprozil was evaluated in the treatment of acute otitis media with effusion in three open, randomized, multicenter comparative clinical trials. In two trials, 891 pediatric patients were enrolled to either cefprozil or amoxicillin-clavulanate dosage regimens. The treatment groups were comparable in demographic characteristics, and presented with otalgia, middle-ear effusion, or inflamed or bulging tympanic membrane on otoscopic examination. In all patients, tympanocentesis and a culture were required. Two cefprozil oral doses were evaluated, 30 mg/kg/day and 40 mg/kg/day divided into two equal doses (b.i.d.). Amoxicillin-clavulanate was administered at 40 mg/kg/day in three divided doses (t.i.d.). The recommended duration of therapy was ten days. The predominant bacteria isolated were Haemophilus influenzae and Moraxella catarrhalis. The overall satisfactory clinical response rates were similar for cefprozil (83%) and amoxicillin-clavulanate (81%). The bacteriological response rates did not differ significantly, at 84% and 82%. Cefprozil eradicated the most common pathogen, Streptococcus pneumoniae, more often at 91%, vs. 84% for amoxicillin-clavulanate. The eradication rates were similar against Haemophilus influenzae and Moraxella catarrhalis. The patients treated with cefprozil had a lower rate of adverse clinical events (11%) compared to those with amoxicillin-clavulanate (20%). More gastrointestinal adverse experiences, including diarrhea, were reported in the amoxicillin-clavulanate-treated patients. In Study 3, cefprozil 30 mg/kg/day (b.i.d.) was compared to cefaclor 40 mg/kg/day (t.i.d.) and cefixime 8 mg/kg/day (q.d) in the treatment of acute otitis media in 388 pediatric patients. The patients were treated for 10 days, with a follow-up of 18 days. The overall clinical cure rates were 85%, 89% and 85%, respectively.(ABSTRACT TRUNCATED AT 250 WORDS)

Topics: Acute Disease; Amoxicillin; Amoxicillin-Potassium Clavulanate Combination; Anti-Bacterial Agents; Bacterial Infections; Cefaclor; Cefixime; Cefotaxime; Cefprozil; Cephalosporins; Child; Child, Preschool; Clavulanic Acids; Drug Therapy, Combination; Female; Humans; Infant; Male; Microbial Sensitivity Tests; Multicenter Studies as Topic; Otitis Media; Randomized Controlled Trials as Topic

Six multicenter clinical trials comparing cefprozil with cefaclor, amoxicillin-clavulanate or erythromycin in the management of skin and soft-tissue infections caused by susceptible bacteria demonstrate that cefprozil, given once or twice daily, is an effective chemotherapeutic agent in this context. Its pharmacokinetic behavior is compatible with once-daily or twice-daily administration, with a probability of improved patient compliance. Safety and tolerability compare favorably with other agents used in skin and soft-tissue infections.

Topics: Adolescent; Adult; Aged; Amoxicillin; Amoxicillin-Potassium Clavulanate Combination; Anti-Bacterial Agents; Bacterial Infections; Cefaclor; Cefprozil; Cephalosporins; Child; Child, Preschool; Clavulanic Acids; Clinical Trials as Topic; Drug Therapy, Combination; Erythromycin; Female; Humans; Male; Middle Aged; Multicenter Studies as Topic; Skin Diseases, Bacterial; Soft Tissue Infections

Topics: Administration, Oral; Anti-Bacterial Agents; Anti-Infective Agents; Azithromycin; Bacterial Infections; Cefixime; Cefotaxime; Cefpodoxime Proxetil; Cefprozil; Ceftibuten; Ceftizoxime; Cefuroxime; Cephalosporins; Child; Clarithromycin; Fluoroquinolones; Humans

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 indicat

Topics: Animals; Bacteria; Bacterial Infections; Cefprozil; Cephalosporins; Humans; Microbial Sensitivity Tests; Otitis Media; Skin Diseases, Infectious; Urinary Tract Infections

Cefprozil is a new, orally bioavailable, cephalosporin with significant activity against the bacteria commonly associated with upper and lower respiratory tract infection, and skin and soft tissue infections. Its absorption and elimination dynamics suggest once- or twice-daily dosing. The low-rate of gastrointestinal and dermatologic side effects associated with cefprozil administration suggest that it may have a significant role in the management of patients with these infections. Children with pharyngitis or urinary tract infection are more appropriately treated with antibiotics having a narrower spectrum of activity. With a variety of newer cephalosporins being marketed in the early 1990s, it will be important for the clinician to examine the data from ongoing comparative clinical trials to determine which antibiotic is best for a patient with a specific infection and whether the added cost justifies its use.

Topics: Adult; Bacteria; Bacterial Infections; Cefprozil; Cephalosporins; Child; Humans; Microbial Sensitivity Tests; Otitis Media; Pharyngitis

Shorter than traditional 7- to 14-day treatment regimens have demonstrated efficacy in treatment of an acute exacerbation of chronic bronchitis (AECB).. Perform a clinical efficacy study comparing 5 days of cefprozil therapy to 10 days of clarithromycin in treating an AECB.. A multicenter, randomized, double-blind study comparing efficacy and safety of cefprozil, 500 mg twice daily, for 5 days with clarithromycin, 500 mg twice daily, for 10 days in treatment of 295 subjects with AECB. Concomitantly, among all treated subjects, 39% (115 of 295) had a history of chronic obstructive pulmonary disease/emphysema; 21% (62 of 295) had a history of asthma/reactive airway disease; and 31% (90 of 295) had environmental allergies.. There were no statistically significant differences among clinically evaluable subjects' cure rates; 82% (109 of 133) treated with cefprozil versus 85% (105 of 123) treated with clarithromycin were cured at test-of-cure visit (95% confidence interval, -12.0 to 5.1%). Clinical cure rates at end of study were 80% and 81%, respectively (95% confidence interval, -10.8 to 7.9%). Before treatment, 99% (85 of 86) of Gram-positive organisms isolated were susceptible to cefprozil and 78% (67 of 86) were susceptible to clarithromycin. A total of 84% (96 of 114) of Gram-negative organisms were susceptible to cefprozil and 63% (72 of 114) were susceptible to clarithromycin. Of clinically evaluable Streptococcus pneumoniae-infected subjects, 100% (11 of 11) of cefprozil subjects and 93% (14 of 15) of clarithromycin subjects experienced clinical cure. The most frequently reported adverse effects were nausea, 5% (7 of 150), and diarrhea, 9% (14 of 150), for cefprozil. For clarithromycin, the adverse effects were nausea, 8% (11 of 145); diarrhea, 12% (18 of 145); taste perversion, 8% (11 of 145); and dry mouth, 5% (7 of 145).. Five days of cefprozil is as effective as 10 days of clarithromycin for treatment of an AECB.

Topics: Adult; Anti-Bacterial Agents; Bacterial Infections; Bronchitis, Chronic; Cefprozil; Cephalosporins; Clarithromycin; Demography; Double-Blind Method; Drug Administration Schedule; Humans; Microbial Sensitivity Tests; Middle Aged; Recurrence; Treatment Outcome

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)

Topics: Adolescent; Adult; Amoxicillin; Amoxicillin-Potassium Clavulanate Combination; Anti-Bacterial Agents; Bacterial Infections; Bronchitis; Cefaclor; Cefprozil; Cefuroxime; Cephalosporins; Clavulanic Acids; Drug Therapy, Combination; Female; Humans; Male; Multicenter Studies as Topic; Pneumonia; Prodrugs; Randomized Controlled Trials as Topic; Respiratory Tract Infections

Cefprozil was evaluated in the treatment of acute otitis media with effusion in three open, randomized, multicenter comparative clinical trials. In two trials, 891 pediatric patients were enrolled to either cefprozil or amoxicillin-clavulanate dosage regimens. The treatment groups were comparable in demographic characteristics, and presented with otalgia, middle-ear effusion, or inflamed or bulging tympanic membrane on otoscopic examination. In all patients, tympanocentesis and a culture were required. Two cefprozil oral doses were evaluated, 30 mg/kg/day and 40 mg/kg/day divided into two equal doses (b.i.d.). Amoxicillin-clavulanate was administered at 40 mg/kg/day in three divided doses (t.i.d.). The recommended duration of therapy was ten days. The predominant bacteria isolated were Haemophilus influenzae and Moraxella catarrhalis. The overall satisfactory clinical response rates were similar for cefprozil (83%) and amoxicillin-clavulanate (81%). The bacteriological response rates did not differ significantly, at 84% and 82%. Cefprozil eradicated the most common pathogen, Streptococcus pneumoniae, more often at 91%, vs. 84% for amoxicillin-clavulanate. The eradication rates were similar against Haemophilus influenzae and Moraxella catarrhalis. The patients treated with cefprozil had a lower rate of adverse clinical events (11%) compared to those with amoxicillin-clavulanate (20%). More gastrointestinal adverse experiences, including diarrhea, were reported in the amoxicillin-clavulanate-treated patients. In Study 3, cefprozil 30 mg/kg/day (b.i.d.) was compared to cefaclor 40 mg/kg/day (t.i.d.) and cefixime 8 mg/kg/day (q.d) in the treatment of acute otitis media in 388 pediatric patients. The patients were treated for 10 days, with a follow-up of 18 days. The overall clinical cure rates were 85%, 89% and 85%, respectively.(ABSTRACT TRUNCATED AT 250 WORDS)

Topics: Acute Disease; Amoxicillin; Amoxicillin-Potassium Clavulanate Combination; Anti-Bacterial Agents; Bacterial Infections; Cefaclor; Cefixime; Cefotaxime; Cefprozil; Cephalosporins; Child; Child, Preschool; Clavulanic Acids; Drug Therapy, Combination; Female; Humans; Infant; Male; Microbial Sensitivity Tests; Multicenter Studies as Topic; Otitis Media; Randomized Controlled Trials as Topic

Cefprozil (CFPZ), a newly developed oral cephalosporin in a fine granular form for pediatric use, was administered to children with bacterial infections. MICs were determined for 6 drugs including CFPZ, cephalexin (CEX), cefaclor (CCL), ampicillin (ABPC), methicillin (DMPPC) and cloxacillin (MCIPC) against the following 84 strains isolated from cases to which CFPZ was administered; 55 strains of Gram-positive cocci (GPC) including 2 strains of Staphylococcus aureus, 49 strains of Streptococcus pyogenes, 4 strains of Streptococcus pneumoniae, and 29 strains of Gram-negative bacilli (GNB) including 10 strains of Haemophilus influenzae, 18 strains of Escherichia coli, and 1 strain of Proteus mirabilis. MIC determination of these strains was done with an inoculum size of 10(6) CFU/ml. In pharmacokinetic studies, serum concentrations, urinary concentrations and urinary recovery rates were investigated using bioassay and high-performance liquid chromatography (HPLC). CFPZ was orally administered 30 minutes before meals to 9 children with ages ranging from 7 years and 1 month to 12 years and 3 months. Three groups of 3 children were tested with doses of 4.0, 7.5 and 15.0 mg/kg, respectively. In addition to the above, clinical and bacteriological studies were performed in a total of 160 cases consisting of children with ages ranging 5 months to 12 years and 5 months. A mean dose of 8.6 mg/kg in 3-4 divided doses (130 cases of t.i.d. and 30 cases of q.i.d.) was administered for an average of 7 days. The 160 cases included 34 cases of pharyngitis, 5 cases of tonsillitis, 8 cases of acute bronchitis, 8 cases of pneumonia, 52 cases of scarlet fever, 4 cases of acute purulent otitis media, 47 cases of urinary tract infection, 1 case of purulent lymphadenitis and 1 case of posthitis. Adverse reactions and abnormal clinical laboratory test results were also examined in 166 cases, including 6 cases excluded from the evaluation of clinical efficacy. The results obtained are summarized as follows: 1. With regard to GPC, MICs of CFPZ against 2 strains of S. aureus were 0.78 or 1.56 micrograms/ml and CFPZ showed the second highest activity to MCIPC. MICs of CFPZ against 49 strains of S. pyogenes were all less than 0.025 micrograms/ml.(ABSTRACT TRUNCATED AT 400 WORDS)

Topics: Administration, Oral; Age Factors; Bacteria; Bacterial Infections; Cefprozil; Cephalosporins; Child; Child, Preschool; Drug Resistance, Microbial; Female; Humans; Infant; Male; Respiratory Tract Infections; Urinary Tract Infections

Topics: Bacterial Infections; Cefaclor; Cefprozil; Cephalosporins; Child; Child, Preschool; Female; Humans; Male; Prospective Studies; Skin Diseases, Infectious; Staphylococcal Infections; Streptococcal Infections; Streptococcus pyogenes

Cefprozil (CFPZ, BMY-28100) was evaluated for its efficacy, safety and pharmacokinetics in children. CFPZ was effective against streptococcal pharyngitis, pneumococcal lower respiratory tract infections, staphylococcal skin infections and Escherichia coli urinary tract infections, but was less effective against lower respiratory tract infections and otitis media due to Haemophilus influenzae. No adverse reactions were encountered in 46 cases treated with CFPZ. With a premeal administration of 7.5 mg/kg, the Cmax was approximately 3.2 micrograms/ml and the T 1/2 beta was 1.4 hours. From the present study, CFPZ appears to be safe and effective against community-acquired childhood infections.

Topics: Administration, Oral; Bacteria; Bacterial Infections; Cefprozil; Cephalosporins; Child; Child, Preschool; Female; Humans; Infant; Male; Microbial Sensitivity Tests

Cefprozil (CFPZ, BMY-28100) granules was administered to a group of pediatric patients. The new oral cephalosporin, CFPZ, was evaluated clinically in 42 pediatric patients, and a pharmacokinetic study was performed in 6 patients. Serum and urinary concentrations of CFPZ were determined in 6 patients who were given single dose of 7.5 or 15.0 mg/kg. Serum concentrations were determined at 1, 2, 3, 4 and 6 hours after dosing. Urinary concentrations were measured for periods of 0-6 hours after dosing. With oral administrations of 7.5 mg/kg and 15.0 mg/kg, peak serum concentrations were 2.13 micrograms/ml and 6.22 micrograms/ml, respectively, at 2 hours, and biological half-lives were 1.06 hours and 1.36 hours, respectively. Urinary recovery rates were 44.8% and 56.1%. The clinical evaluation was conducted in 41 patients including 16 patients with acute tonsillitis, 8 patients with lacunar tonsillitis, 4 patients with scarlet fever, 3 patients with acute bronchitis, 1 patient each with pertussis, furuncle, impetigo and lymphadenitis, and 6 patients with urinary tract infections. The ages of the patients were 10 month to 11 years 1 month, and they were treated with CFPZ at doses ranging 9.0-45.0 mg/kg daily for 3-14 days, the overall clinical efficacy rate was 92.7%. An eradication rate of 79.2% was achieved for 28 strains of 8 species identified in the patients. No side effects were observed. Abnormal laboratory test results obtained were eosinophilia in 2 patients.

Topics: Administration, Oral; Bacteria; Bacterial Infections; Cefprozil; Cephalosporins; Child; Child, Preschool; Drug Administration Schedule; Female; Humans; Infant; Male; Microbial Sensitivity Tests

Fundamental and clinical effects of cefprozil (CFPZ, BMY-28100) granules, a new oral cephalosporin antibiotic, in pediatric field were investigated. The result obtained were summarized as follows. 1. CFPZ (10% granules) was given to 1 child in a single dose of 7.5 mg/kg. The peak serum concentration of CFPZ was 4.51 micrograms/ml at 2 hours after administration. Half-life and AUC values were 0.98 hour and 20.7 micrograms.hr/ml. The mean peak urinary concentrations of CFPZ and 6 hours recovery rates were over 200 micrograms/ml at 2-6 hours and 27.6%, respectively. 2. Clinical efficacy of CFPZ was investigated in a total of 41 children, including 14 with upper respiratory tract infections, 6 with acute bronchitis and pneumonia, 2 with acute otitis media, 3 with skin and soft tissue infections and 16 with urinary tract infections. The clinical efficacy rate was 95.1%. The bacteriological eradication rate was 84.6%. 3. Two patients showed abnormal laboratory test results. One had elevations of both GOT and GPT, and another had eosinophilia which were attributed to this antibiotic as side effects.

Topics: Bacteria; Bacterial Infections; Cefprozil; Cephalosporins; Child; Child, Preschool; Drug Administration Schedule; Female; Humans; Infant; Male; Microbial Sensitivity Tests

Clinical efficacy and safety of cefprozil (CFPZ, BMY-28100), a newly developed oral cephalosporin, were studied in our pediatric department. Clinical effectiveness, bacteriological effectiveness and side effects were studied in 116 pediatric patients with ages ranging 4 months to 11 years. CFPZ was given 4.6-14.1 mg/kg daily in 3 times for 3-10 days. Clinical efficacies were evaluated in 112 patients, and the therapeutic effectiveness were excellent in 1 and good in 6 for 7 patients with acute pharyngitis, excellent in 24 and good in 26 for acute purulent tonsillitis, excellent in 3, good in 8 and fair in 1 for acute bronchitis, excellent in 21, good in 7, fair in 1 and poor in 1 for acute pneumonia, excellent in 1 acute purulent parotitis, excellent in 2 and good in 7 for acute UTI, good in 1 impetigo, fair in 1 periproctal abscess and good in 1 acute enteritis. The effectiveness rate was 96.4%. Bacteriologically, 4 strains of Staphylococcus aureus (beta-lactamase producing strains), 1 strain of Staphylococcus epidermidis (beta-lactamase producing strain), 2 strains of Streptococcus pneumoniae, 2 strains of Streptococcus agalactiae, 4 strains of beta-Streptococcus, 1 strain of Klebsiella pneumoniae (beta-lactamase producing strain) and 1 strain of Salmonella C2 were all disappeared, and of 22 strains of Streptococcus pyogenes, 20 strains were disappeared, 1 was decreased and 1 was unknown, of 5 strains of Escherichia coli (3 beta-lactamase producing strains), 4 were disappeared and 1 was decreased, of 29 strains of Haemophilus influenzae (14 beta-lactamase producing strains), 14 were disappeared, 11 were decreased, 3 persisted and 1 was unknown and of 2 strains of Haemophilus parainfluenzae (1 beta-lactamase producing strain), 1 was disappeared and 1 persisted. The bacteriological eradication rates for Gram-positive bacteria and Gram-negative bacteria were 97.1% and 56.8%, respectively, and the drug was especially effective against Gram-positive bacteria. No side effects nor refusal of ingestion were observed. As abnormalities in laboratory test results, 3 cases of elevation of eosinophil counts and 1 of elevation of platelet counts were observed. In conclusion, CFPZ was considered to be a safe and highly effective antibiotic in pediatric infections.

Topics: Bacteria; Bacterial Infections; Cefprozil; Cephalosporins; Child; Child, Preschool; Drug Administration Schedule; Female; Hematologic Tests; Humans; Infant; Male

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.

Topics: Bacteria; Bacterial Infections; Cefprozil; Cephalosporins; Child; Child, Preschool; Drug Administration Schedule; Female; Hematologic Tests; Humans; Male; Microbial Sensitivity Tests

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.

Topics: Bacteria; Bacterial Infections; Cefprozil; Cephalosporins; Child; Child, Preschool; Drug Administration Schedule; Female; Humans; Infant; Male; Microbial Sensitivity Tests

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.

Topics: Bacteria; Bacterial Infections; beta-Lactamases; Cefprozil; Cephalosporins; Child; Child, Preschool; Chromatography, High Pressure Liquid; Drug Administration Schedule; Female; Humans; Infant; Male; Microbial Sensitivity Tests

Cefprozil (CFPZ, BMY-28100) granule preparation was studied for pharmacokinetic, bacteriological and clinical aspects in the pediatric infections. The results obtained are summarized as follows: 1. Serum concentrations and urinary excretion. The pharmacokinetics of CFPZ in pediatrics was investigated by single oral administration of fine granules at doses of 4.0, 7.5 and 15.0 mg/kg. Peak blood levels of CFPZ were 3.06, 4.62 and 9.65 micrograms/ml, respectively, at 1.00-1.30 hours after each dose and AUCs were 7.44, 12.50 and 27.01 micrograms.hr/ml, respectively. These data showed that Cmax and AUC depended on dose levels. T 1/2 (beta) at these dose levels were 1.03, 0.94 and 1.01 hours, respectively. There were no differences related to dose. Urinary recovery rates in the first 6 hours after administration were 51.5-57.1%. The pharmacokinetics of CFPZ before or after meals were also investigated at a dose of 7.5 mg/kg. Peak blood levels were 4.88 micrograms/ml at 1.17 hours after administration in the fasting state, and 4.30 micrograms/ml at 1.54 hours after administration in the non-fasting state. Delay of Tmax and slight decrease of Cmax were observed in the non-fasting state, but T 1/2 and AUC were 0.91 hour and 12.96 micrograms.hr/ml, respectively, in the non-fasting state, and were similar to those in the fasting state, 0.93 hour and 12.82 micrograms.hr/ml, respectively. Urinary recovery rates in the first 6 hours after administration were 63.8% in the fasting state and 50.7% in the non-fasting state. 2. Clinical results. Clinical efficacies of CFPZ granules in various infectious diseases were studied in 804 cases. Twenty nine cases, mostly viral or mycoplasmal infections, were excluded from the statistical analysis. The clinical efficacy rate in 527 cases with causative bacteria isolated was 97.2%; and in 248 cases from whom no significant isolate had been obtained was 96.0%. The clinical efficacy rate in 475 cases with monobacterial infections (proven by culture of isolates) was 97.3%, and that in 52 case with polybacterial infections was 96.2%. Haemophilus influenzae was isolated mostly from acute respiratory infections. In 88 cases from whom H. influenzae was isolated, clinical efficacy rate was 95.5%. In cases from whom H. influenzae was found concomitant by with Staphylococcus aureus, Streptococcus pyogenes or Streptococcus pneumoniae, the clinical efficacy rates were also high. The bacteriological eradication rate in cases with 582 strains was

Topics: Adolescent; Bacteria; Bacterial Infections; Cefprozil; Cephalosporins; Child; Child, Preschool; Drug Administration Schedule; Female; Food; Hematologic Tests; Humans; Infant; Male

The efficacy, safety and usefulness of BMY-28100 for the treatment of bacterial pneumonia were compared with those of cefaclor (hereinafter referred to as CCL) in a double-blind study. The daily dosages were 750 mg for BMY-28100 and 1,500 mg for CCL, divided into 3 administrations daily. These drugs were administered orally for at least 14 days. A total of 172 cases were enrolled in this study. Of these, cases which deviated from the protocols were excluded from evaluations. Thus, clinical efficacy was evaluated in 124 cases, adverse reactions were evaluated in 160 cases, and abnormal laboratory test values were evaluated in 146 cases. The following results were obtained. 1. Efficacy rates ("good" or better responses) in bacterial pneumonia cases as evaluated by the subcommittee were 81.7% (49/60) in the BMY-28100 group and 89.1% (41/46) in the CCL group, thus no significant difference was found between the 2 groups. 2. Efficacy rates ("good" or better responses), as evaluated by investigators, in the same bacterial pneumonia cases which were subjected to the evaluation by the subcommittee were 83.3% (50/60) in the BMY-28100 group and 88.9% (40/45) in the CCL group, thus no significant difference between the 2 groups was found also. 3. Bacteriological response rates in bacterial pneumonia cases were 86.2% (25/29) in the BMY-28100 group and 85.7% (18/21) in the CCL group with no significant difference between the 2 groups. 4. Incidences of subjective/objective clinical adverse symptoms were 3.5% (3/85) in the BMY-28100 group and 1.3% (1/75) in the CCL group, and no significant difference was observed between the 2 groups. No significant difference was also found between the 2 groups in incidences of abnormal laboratory test values, as abnormalities were found in 21.1% (16/76) of the cases in the BMY-28100 group and 25.7% (18/70) in the CCL group. 5. As for overall usefulness of the drug in bacterial pneumonia cases, utility rates ("useful" or better evaluations) as evaluated by the subcommittee were 83.6% (46/55) in the BMY-28100 group and 90.5% (38/42) in the CCL group, and the rates as evaluated by investigators in cases judged as evaluable by the subcommittee were 78.3% (47/60) and 82.2% (37/45), respectively. There were no significant differences between the 2 groups. The utility rates as evaluated by investigators in cases in which diseases were diagnosed as bacterial pneumonia or lung abscess by investigators were 78.3% (47/60) in the BMY-28100 group

Topics: Administration, Oral; Adult; Aged; Aged, 80 and over; Bacterial Infections; Cefaclor; Cefprozil; Cephalosporins; Double-Blind Method; Female; Humans; Male; Middle Aged; Pneumonia

Antibiotics profoundly affect the gut microbiome and modulate microbial communities. We recently observed that antimicrobial drugs also impact the abundance and distribution of antibiotic resistance genes. In this addendum, we reanalyze our ∼1 trillion nucleotide shotgun metagenomic dataset to quantify comprehensive genomic differences at the sequence level before and after antibiotic treatment. We show that 7 day exposure to cefprozil leads to a statistically significant loss of metagenome sequences. Recovery of gut microbiomes 3 months after antibiotherapy was characterized by the emergence of new genome sequences not observed prior to antibiotic exposure. Participants with low initial gut microbiome diversity had an increased amount of sequences related to antibiotic resistance. Therefore, we suggest that while the taxonomical composition of microbiomes is partially affected by the antibiotic, the genomic content and population structure of bacterial communities is noticeably impacted.

Topics: Anti-Bacterial Agents; Bacteria; Bacterial Infections; Bacterial Proteins; Cefprozil; Cephalosporins; Gastrointestinal Microbiome; Gastrointestinal Tract; Humans

To evaluate the palatability of antimicrobial agents effective against beta-lactamase-producing bacteria in American children.. In a taste test of 4 antimicrobial agents, azithromycin (cherry flavored), cefprozil (bubble gum flavored), cefixime (strawberry flavored), and amoxicillin-clavulanic acid (banana flavored) were compared.. An urban inner-city primary care clinic.. A volunteer sample of 30 healthy children (aged 5-8 years).. Palatability was determined using a single-blind taste test of 4 flavored antimicrobial agents. The 4 antimicrobial agents used were azithromycin, cefprozil, cefixime, and amoxicillin-clavulanic acid.. After each antimicrobial test dose, subjects rated the taste on a 10-cm visual analog scale incorporating a facial hedonic scale. Preference assessments for the best-tasting and worst-tasting agent were also conducted.. Of the 20 children who expressed a preference, significantly more children (9 [45%], P<.05) selected the cefixime preparation as the best-tasting formulation compared with the other preparations. The cefixime preparation was also significantly the least likely to be selected as the worst-tasting preparation (2 [10%], P<.05). There were no significant differences between the other 3 preparations with respect to being selected as either the best or worst tasting. The mean (+/- SD) visual analog scale score for cefixime was highest (8.53 [2.49]) compared with the scores for azithromycin (6.78 [3.45]), cefprozil (6.26 [4.04]), and amoxicillin-clavulanic acid (6.24 [4.01]).. The cefixime preparation was most commonly rated as best tasting by children.

Topics: Administration, Oral; Amoxicillin-Potassium Clavulanate Combination; Anti-Bacterial Agents; Azithromycin; Bacterial Infections; Cefixime; Cefprozil; Cephalosporins; Child; Child, Preschool; Female; Flavoring Agents; Humans; Male; Pain Measurement; Patient Acceptance of Health Care; Taste; Urban Population

Topics: Administration, Oral; Bacterial Infections; Biopsy, Needle; Bone Diseases; Cefprozil; Cephalosporins; Child; Child, Preschool; Humans; Joint Diseases; Joints; Microbial Sensitivity Tests; Staphylococcal Infections; Staphylococcus aureus

Cefprozil (CFPZ, BMY-28100), a new oral cephalosporin, was evaluated for its efficacy and safety in 42 children with bacterial infections (Table 1), and the following results were obtained. 1. CFPZ was administered in 3 or 4 divided doses at daily dosages ranging from 15.3 to 60.0 mg/kg to 42 patients (19 cases of acute tonsillitis and/or laryngitis, pharyngitis, 13 cases of pneumonia, 2 cases each of suppurative cervical lymphadenitis and UTI, and 1 case each of scarlet fever, acute otitis media, suppurative parotitis, impetigo contagiosa, furuncle and acute enteritis) and the following clinical results were obtained: excellent; 24 cases, good; 14 cases, fair; 4 cases. The overall efficacy rate was 90.5% (Table 3). 2. MICs of CFPZ against 50 strains of isolated organisms are shown in Table 4. In 19 cases out of 28 cases examined, causative organisms were successfully eradicated and strain of Staphylococcus aureus was decreased in 1 case. 3. Diarrhea was observed in 2 cases (cases 8, 11). In case 8, the symptom disappeared spontaneously. Case 11 improved immediately after the administration of the drug was stopped. Among 39 children who went through laboratory tests, eosinophilia which seemed to be related to the administration of this drug was observed in 2 cases (cases 29, 38). Slight elevations of S-GOT and S-GPT were found in 1 case (case 22) (Table 7). 4. These data suggest that CFPZ is a safe and useful new antibiotic in the treatment of children with susceptible bacterial infections.

Topics: Administration, Oral; Age Factors; Bacteria; Bacterial Infections; Cefprozil; Cephalosporins; Child; Child, Preschool; Drug Evaluation; Drug Resistance, Microbial; Female; Humans; Infant; Male

Cefprozil granule preparation was administered orally to 16 patients (ages ranging 8 months to 9 years and 6 months) with pediatric bacterial infections at daily dose levels between 29.4 and 35.7 mg/kg divided into 3 or 4 doses. The following results were obtained. 1. Sixteen patients including 5 with pharyngitis, 3 with tonsillitis, 3 with lacunar tonsillitis, 2 with pneumonia, 2 with contagious impetigo and 1 with scarlet fever were treated. Clinical effects were excellent in 9 cases and moderate in 7, with an overall efficacy rate of 100%. 2. Organisms suspected as pathogens included 17 strains (10 strains of haemophilus influenzae, 2 of Haemophilus parainfluenzae, 3 of Streptococcus pyogenes and 2 of Staphylococcus aureus). Bacteriologically, eradication of pathogens were observed for 11 strains, but no changes were obtained for 5 (all Haemophilus), and unknown results were obtained for 1, thus the eradication rate was 68.8%. 3. No side effects were observed. Abnormal laboratory test results included 2 cases of increase in platelets, and 2 of increase in eosinophils, but those were not significant. 4. No refusal of the drug occurred due to its taste or odor.

Topics: Administration, Oral; Age Factors; Bacteria; Bacterial Infections; Cefprozil; Cephalosporins; Child; Child, Preschool; Drug Evaluation; Female; Humans; Infant; Male; Respiratory Tract Infections

Cefprozil (CFPZ, BMY-28100), a new oral cephalosporin, was evaluated for its antibacterial activity and clinical efficacy. Thirty-four patients were treated with 7.7-36.2 mg/kg per day of CFPZ divided into 3 times. A total of 33 patients including 3 with acute pneumonia, 2 with acute bronchitis, 17 with acute upper respiratory tract infections, 4 with urinary tract infections, 1 with suppurative lymphadenitis and 6 with other soft tissue infections were evaluated for clinical efficacy except for 1 patient whose general conditions were too serious to continue to be treated with orally medication. Clinical effects were excellent in 8 patients and good in 23 but 2 cases were excluded because they were suspected for viral infections, hence the overall efficacy rate was 100%. Bacteriological responses were confirmed on 6 (66.7%) strains which were eradicated by the treatment out of 9 strains identified. CFPZ showed stronger antibacterial activities than those of cefaclor. Side effects or abnormal laboratory test results were observed in 2 patients; nausea and pallor of face in 1 patient and an increase of eosinophil in 1. The above findings suggest that CFPZ is a safe and useful antibiotics for the treatment of bacterial infections in pediatric patients.

Topics: Age Factors; Bacteria; Bacterial Infections; Cefprozil; Cephalosporins; Child; Child, Preschool; Drug Evaluation; Drug Resistance, Microbial; Female; Humans; Infant; Male; Respiratory Tract Infections; Urinary Tract Infections

Cefprozil (CFPZ, BMY-28100) granules were administered to 20 children with bacterial infections: acute tonsillitis 8, acute bronchitis 10, purulent lymphadenitis 1, urinary tract infection 1. Daily doses ranged 29-50 mg/kg. The drug was given orally, 3 times a day and the durations of administration were 5 to 9 days. Clinical efficacies were excellent in 16 cases and good in 4 cases, hence the overall efficacy rate was 100%. No side effects were observed in any of these cases. As for abnormal laboratory test values, thrombocytosis was observed in 1 case. From the above results, we consider CFPZ granules to be a useful drug for the treatment of pediatric patients with various bacterial infections.

Topics: Administration, Oral; Age Factors; Bacteria; Bacterial Infections; Cefprozil; Cephalosporins; Child; Child, Preschool; Drug Evaluation; Female; Humans; Infant; Male; Thrombocytosis

Cefprozil (CFPZ, BMY-28100), a new non-ester cephem, was administered to 15 pediatric patients with infectious diseases. The patients included 6 boys and 9 girls from 10 months to 11 years old and they were given oral doses of 18.5-41.7 mg/kg/day for 3 to 8 days. Clinical efficacies were excellent in 3 cases and good in 12 cases, hence the total efficacy rate was 100%. Eosinophilia occurred in 1 case as side effect of the drug, but no other side effects were not found during or after the treatment.

Topics: Administration, Oral; Age Factors; Bacterial Infections; Cefprozil; Cephalosporins; Child; Child, Preschool; Drug Evaluation; Eosinophilia; Female; Humans; Infant; Male

Therapeutic effects of cefprozil (CFPZ, BMY-28100), a new cephalosporin, were examined in various infectious diseases in children. Clinical efficacy rates were 50% (2/4) in acute bronchitis, 80% (4/5) in pharyngitis, 0% in laryngitis, 100% (7/7) in tonsillitis, 100% (8/8) in impetigo contagiosa, furuncle and posthitis. Hence, the overall efficacy rate was 84% (21/25). Adverse effects were observed in 1 case with slightly elevated serum GOT and GPT. Changes in serum concentrations and urinary excretion of CFPZ were examined in 4 and 2 children without infection, respectively. T 1/2 values obtained were between 1 hour to 2 hours (bioassay). Six hour recovery rates in urine were 51.8% and 77.8% (bioassay). CFPZ was considered to be a safe and useful drug in treating various infectious diseases in children.

Topics: Administration, Oral; Adolescent; Age Factors; Bacteria; Bacterial Infections; Cefprozil; Cephalosporins; Child; Child, Preschool; Drug Evaluation; Drug Resistance, Microbial; Female; Humans; Infant; Male

Topics: Bacterial Infections; Cefprozil; Cephalosporins; Humans

Topics: Administration, Oral; Bacteria; Bacterial Infections; Cefprozil; Cephalosporins; Drug Resistance, Microbial; Humans

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.

Topics: Animals; Bacteria, Aerobic; Bacterial Infections; beta-Lactamases; Cefaclor; Cefprozil; Cephalexin; Cephalosporins; Mice; Microbial Sensitivity Tests; Rats

The antibacterial activity of BMY-28100, a new oral cephalosporin, was measured against 300 bacterial isolates from pediatric infections by standard agar dilution methodology. The effect of inoculum size on activity was also assessed. BMY-28100 was more active than cephalexin or cefaclor against all bacterial species tested.

Topics: Bacteria; Bacterial Infections; Cefprozil; Cephalosporins; Child; Humans; Microbial Sensitivity Tests