Search PubMed⌕ Search

SEARCH · Search PubMed

Results for “Cefprozil”

Search indexed PubMed citations on genomics, clinical trials, systematic reviews and public health. Explore titles, authors and supplied subject terms, then open the PubMed record.

Quote a phrase for an exact phrase match. Source license links do not imply unrestricted reuse.

At least 37 records · Page 2Linked to original sources
PubMed1998

Evaluation of the in vitro Activity of Cefprozil Relative to Other Oral Antimicrobial Agents Against Bacteria in Clinical Specimens from Patients in São Paulo With Respiratory Tract Infections.

Cefprozil is a new oral second generation cephalosporin. Its in vitro antimicrobial activity was evaluated against 371 recent clinical isolates from patients with respiratory infections. We tested the susceptibility of 244 streptococci (96 Streptococcus pneumoniae, 105 group viridans streptococci, 32 Streptococcus agalactiae, and 11 group A beta-hemolitic streptococci) 107 Haemophilus influenzae, and 20 oxacillin-susceptible S.aureus (OSSA). The isolates were susceptibility tested against cefprozil, cefaclor and amoxicillin/clavulanic acid by the E-test method; and against cefadroxil, cefuroxime, cefetamet, erythromycin, and azythromycin by disk diffusion. The methods and the susceptibility categorization followed the National Committee for Clinical Laboratory Standards (NCCLS) procedures. Amoxicillin/clavulanic acid was slightly more active againstH.influenzae (MICs(90) 0.5µg/mL) than cefprozil or cefaclor (MICs(90) 4 and 2µg/mL respectively). Cefprozil demonstrated potent activity against streptococci. Against S.pneumoniae, cefprozil was 2-4 fold more active than cefaclor (MICs(90)0.125 and 0.38µg/mL, respectively). S. pneumoniae susceptibility was 84% to penicillin, 95% to erythromycin and 97% to azithromycin by disk diffusion. Viridans streptococci showed higher MICs for cefprozil and cefaclor (MICs(90) 4µg/mL and 8µg/mL, respectively) and only 50% susceptibility to the macrolides. Cefprozil was four times more active than cefaclor and as active as amoxieillin/clavulanic acid against group A beta-hemolytic streptococci and S.agalactiae. These three compounds showed similar activity against OSSA. In conclusion, cefprozil demonstrated excellent in vitro activity against bacterial species responsible for respiratory infections in São Paulo.

Journal Article↗
PubMed1994

Comparative efficacy and safety of cefprozil versus penicillin, cefaclor and erythromycin in the treatment of streptococcal pharyngitis and tonsillitis.

Cefprozil is a new oral cephalosporin with an enhanced in vitro spectrum of activity that includes group A beta-hemolytic streptococci (GABHS). Four multicenter randomized clinical trials were conducted to compare the clinical efficacy and safety of cefprozil administered once or twice a day for the treatment of mild to moderate GABHS tonsillitis and pharyngitis. A total of 1597 patients were enrolled in the trials. Patient demographics and severity of infection were similar for all treatment groups. In Study 1, cefprozil administered at 20 mg/kg once daily was clinically, in 68 of 76 patients (89%) and bacteriologically, in 66 of 74 patients (89%) superior to penicillin -51 of 69 (74%) and 46 of 69 (67%)--administered three times a day in patients of two to 12 years of age. In Study 2, the patients enrolled were 13 years of age and older, and cefprozil administered at 20 mg/kg once a day had similar clinical (93% vs. 90%) and bacteriological (95% vs. 94%) response rates as cefaclor administered three times a day. Study 3 demonstrated that cefprozil administered twice daily was similar to penicillin given three times a day, the clinical satisfactory response being 164 of 175 (94%) for cefprozil and 146 of 165 (88%) for penicillin. In Study 4, identical clinical and bacteriologic responses (95%) were observed for cefprozil administered once a day and erythromycin ethylsuccinate administered four times a day in children over two years of age. There were no significant differences in the incidence or severity of drug-related adverse events, which, when reported, were mild and transient.(ABSTRACT TRUNCATED AT 250 WORDS)

Adolescent↗
PubMed1994

Multi-investigator evaluation of the efficacy and safety of cefprozil, amoxicillin-clavulanate, cefixime and cefaclor in the treatment of acute otitis media.

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)

Acute Disease↗
PubMed2004

Pediatric tonsillopharyngitis--an evaluation of cefprozil in Indian patients.

OBJECTIVE: The emergence of penicillin resistant strains and the presence of co-pathogens have made the treatment of bacterial infections in children a challenge. Streptococcal tonsillopharyngitis, which is a common infection has been well treated with cefprozil, a novel third generation cephalosporin. The aim of the present study was to evaluate cefprozil in pediatric tonsillopharyngitis. An assessment of the clinical cure and bacteriological eradication rates and an overall tolerability was made. METHODS: It was a prospective, open, non-comparative multicentric study. 316 children (mean age 6.61 years) with tonsillopharyngitis were included. Patients were given cefprozil susp 15 mg/kg/day in two divided doses a day for 10 days. RESULTS: A clinical cure of 96.6% and bacteriological eradication of 94.29% was achieved with cefprozil. Overall tolerability of cefprozil was assessed by physicians and 46% rated tolerability of cefprozil as excellent, 38% as very good, 10% as good, 6% as fair and none as poor. CONCLUSION: Cefprozil has been found to be an excellent drug of superior microbiological and clinical activity in the treatment of pediatric patients with tonsillopharyngitis. The drug also has an expanded spectrum.

Anti-Bacterial Agents↗
PubMed2000

In vitro development of resistance to ceftriaxone, cefprozil and azithromycin in Streptococcus pneumoniae.

Approval of ceftriaxone for the treatment of otitis media has led to fear of selection of resistant mutants owing to widespread use. To test this, we examined the ability of sequential subcultures in sub-MICs of ceftriaxone, cefprozil and azithromycin to select resistant mutants in 12 pneumococci. Daily subculturing was performed 50 times or until mutants with raised ceftriaxone, cefprozil or azithromycin MICs were selected. Of eight ceftriaxone-susceptible parents, ceftriaxone did not select for any resistant mutants, while cefprozil selected for four mutants (MICs 2-4 mg/L after 21-50 subcultures). Among four ceftriaxone-resistant parents, subculturing in ceftriaxone selected for one stable mutant with raised ceftriaxone MIC (>16 mg/L after 21 subcultures) and subculturing in cefprozil selected for one mutant with raised cefprozil MIC (64 mg/L after 44 subcultures). Mutations were observed in pbp2x and pbp1a. Among six azithromycin-susceptible parents, subculturing in azithromycin selected for five resistant mutants (MIC 0.5-32 mg/L after 10-42 passages) and among six azithromycin-resistant strains, subculturing selected for mutants with raised azithromycin MICs in all six strains (MIC 16-32 mg/L after 4-18 passages). All azithromycin-resistant mutants derived from azithromycinsusceptible parents had mutations in domain V of 23S rRNA while all azithromycin-resistant parents and derived mutants had mefE. Single-step mutation rates among the 12 strains at the MIC ranged from 1.5 x 10(-6) to <6.2 x 10(-10) for ceftriaxone, >1.3 x 10(-5) to 8.9 x 10(-8) for cefprozil and >1.1 x 10(-6) to 6.7 x 10(-10) for azithromycin. Multi-step and single-step testing showed that ceftriaxone selected for resistant mutants less often than cefprozil and azithromycin.

Anti-Bacterial Agents↗
PubMed1991

Comparative efficacy and safety of cefprozil (BMY-28100) and cefaclor in the treatment of acute group A beta-hemolytic streptococcal pharyngitis.

Cefprozil (BMY-28100) is a semisynthetic cephalosporin with broad-spectrum antibacterial activity and prolonged serum elimination half-life allowing for once-a-day oral administration. In vitro, cefprozil demonstrates excellent activity against Staphylococcus aureus, Streptococcus pyogenes, Haemophilus influenzae, and Moraxella catarrhalis. Cefprozil (500 mg once daily) was compared to cefaclor (250 mg three times daily) in an open, randomized, comparative trial for the treatment of acute group A beta-hemolytic streptococcal pharyngitis. Ninety-four patients were enrolled in this study; 53 patients were evaluable for clinical and bacteriological response assessment. Seventy-eight patients were evaluable for safety assessment. Three patients (all in the cefprozil treatment group) required disenrollment because of side effects, mainly nausea. Clinical and bacteriological responses were comparable for both study drugs. Leukopenia and nausea, the most common side effects observed, were more common in the cefprozil-treated group. Cefprozil appears to be an appropriate alternative to cefaclor for the treatment of acute group A beta-hemolytic streptococcal pharyngitis. However, because of the small number of patients eligible for efficacy assessment, a large type II (beta) error was expected in our study, which may have resulted in a potential failure to detect a difference between both treatment groups. A larger study would be required to determine the proper role of cefprozil in the treatment of group A beta-hemolytic streptococcal infections.

Adolescent↗
PubMed1996

Bactericidal activities of cefprozil, penicillin, cefaclor, cefixime, and loracarbef against penicillin-susceptible and -resistant Streptococcus pneumoniae in an in vitro pharmacodynamic infection model.

We examined the bactericidal activities of penicillin, cefprozil, cefixime, cefaclor, and loracarbef against three clinical isolates of Streptococcus pneumoniae which were susceptible, moderately susceptible, and resistant to penicillin. An in vitro two-compartment glass infection model was used to simulate human pharmacokinetics in the presence of bacteria. Also, changes in organism susceptibility and development of resistant subpopulations were evaluated. Simulated pediatric dosage regimens and target peak concentrations in the central compartment were as follows: penicillin V-potassium, 26 mg/kg of body weight every 6 h (q6h) and 14 micrograms/ml; cefaclor, 13.4 mg/kg q8h and 16 micrograms/ml; loracarbef, 15 mg/kg q12h and 19 micrograms/ml; cefprozil, 15 mg/kg q12h and 11 micrograms/ml; and cefixime, 8mg/kg q24h and 4 micrograms/ml. Targeted half-lives of each agent were 1 h for penicillin, cefaclor, and loracarbef; 1.3 h for cefprozil; and 3.5 h for cefixime. Growth controls were performed at two different pump rates, 0.8 and 2.0 ml/min (half-lives = 3.5 and 1 h, respectively). Each isolate demonstrated autolysis at the lower rate which was attributed to a decreased supply of fresh nutrients available to the organisms in the infection compartment. Against the susceptible isolate, the time to 99.9% killing was statistically significant between penicillin V-potassium and both cefaclor and cefixime (P < 0.029). Loracarbef never achieved a 99.9% reduction in the inoculum. At 48 h penicillin, cefprozil, and cefaclor were equivalent in extent of killing. Against the intermediately resistant isolate, cefprozil was superior to all other regimens with respect to rate of killing (P < 0.013) and extent of killing at 24 h (P < 0.0003). At 48 h penicillin, cefprozil, and cefaclor were equivalent in extent of killing. All of the regimens exhibited inferior activity against this penicillin-resistant isolate. A 99.9% kill was never obtained with any of the regimens, nor was there an appreciable decrease in the colony counts. In conclusion, it appears that cefprozil, penicillin, and cefaclor are effective therapies against sensitive and even intermediately sensitive isolates of S. pneumoniae. However, none of the oral therapies appear to be of any benefit against penicillin-resistant isolates. The in vitro model may be an effective tool in evaluating other multiple-dose therapies against this fastidious organism, since the continual supply of fresh medium maintains the viability of S. pneumoniae with minimal stationary-phase autolysis.

Cefaclor↗
PubMed2005

[Cefprozil in the treatment of chronic maxillary sinusitis. Clinical and microbiological effectiveness and penetration into sinuses examination].

UNLABELLED: 40 patients with exacerbation of a chronic maxillary sinusitis were examined. Sinus puncture was performed (sinoject) in all of the patients. Before the treatment (500 mg cefprozil orally twice a day, the recommended duration of therapy was ten days) and on the fifth day, the microorganisms from sinus were isolated (the bacteriological culture, antibiogram and MIC were determined). On the second and the fifth day, blood cefprozil level and the presence of cefprozil in the washings from maxillary sinuses were investigated. RESULTS: 17 pathogens were isolated from maxillary sinuses, only two of them were anaerobic. The bacterial strains: Staphylococcus (55%), E.coli (15%), Klebsiella (10%) and 20% of others, were found. Four of them (23.5%) were resistant to cefprozil. In all patients cefprozil was identified in maxillary sinuses (0.87-2.52 ug/ml). The value of MIC were from 0.094 to 2.0 ug/ml. A satisfactory clinical response was observed in 92.5% persons but the eradication of pathogens was obtained in 70%. The adverse clinical events (diarrhea) were observed only in one patient (2.5%). CONCLUSIONS: cefprozil well penetrates into inflammable mucous membrane of maxillary sinuses. Cefprozil obtains efficient bactericidal concentration in relation to sensitive bacteria on the fifth day of therapy. It is also well tolerated by the patients.

Adolescent↗
PubMed1992

Pharmacokinetic interactions of cefprozil with food, propantheline, metoclopramide, and probenecid in healthy volunteers.

Cefprozil, a new oral cephalosporin antibiotic, is composed of cis and trans isomers in an approximate 90:10 ratio. The objectives of this study were: (1) to assess the effects of alterations in gastrointestinal motility by metoclopramide and propantheline on the pharmacokinetics of cis and trans isomers of cefprozil, and to compare them with the effects of food on the pharmacokinetics of cefprozil; (2) to assess the effects of inhibition of renal tubular secretion by probenecid on the pharmacokinetics of cefprozil isomers. In this four-way crossover study, 15 healthy male volunteers received a 1000-mg dose of cefprozil after fasting, pretreatment with metoclopramide or propantheline, after breakfast, or after probenecid in an incomplete, balanced block design. There was a 1-week washout period between each treatment. Blood and urine samples collected over a 24-hour period were assayed for the cis and trans isomers. The concentrations of the trans isomers were generally 1/10 of the cis isomer. The means and variances of the pharmacokinetic parameters of the cis and trans isomers of cefprozil were similar in fasting subjects and were affected in a parallel manner by food, metoclopramide, propantheline, and probenecid. The pharmacokinetics of the cis isomer under the fasting condition were as follows: maximum peak plasma concentration (Cmax), 14.0 +/- 2.7 micrograms/mL; median time to reach Cmax (tmax), 1.5 (range, 1.0-3.5) hours; half-life (t1/2), 1.24 +/- 0.27 hours; area under the concentration (AUC0-infinity), 47.3 +/- 7.7 micrograms.hour/mL; mean residence time after oral administration (MRTpo), 2.9 +/- 0.4 hours; CLR, 219 +/- 60 mL/minute; and Xu% (percent cumulative urinary excretion in 0-24 hours), 68.1 +/- 12.5.(ABSTRACT TRUNCATED AT 250 WORDS)

Adult↗
PubMed1992

Oral absolute bioavailability and intravenous dose-proportionality of cefprozil in humans.

The absolute bioavailability (F) and dose proportionality of cefprozil were investigated in a parallel design study with an embedded two-way crossover leg. Twenty-four healthy male subjects divided into 3 dosing groups received a single 250-, 500-, or 1000-mg dose of cefprozil by a 30-minute intravenous infusion. Subjects assigned to the 500-mg dose group also received a 500-mg oral dose of cefprozil in crossover manner with a wash-out period of 7 days between each treatment. Cefprozil consists of cis and trans isomers in an approximate 90:10 ratio. Serial blood and urine samples were collected and analyzed for the concentrations of the cis and trans isomers of the cephalosporin using high-pressure liquid chromatographic assay with UV detection methods. After the 250-, 500-, and 1000-mg intravenous administration of cefprozil, the peak concentrations were 13.2, 26.0, and 48.5 micrograms/mL, and area under the plasma concentration versus time profiles were 17.2, 31.4, and 58.1 micrograms.hour/mL, respectively, for the cis isomer increasing in a dose proportional manner. Total body clearance, renal clearance, and volume of distribution at steady state, adjusted for body weight, were not significantly different among all groups. Mean residence time, elimination half-life, and urinary recovery were invariant with the dose. Based on the plasma and urine data, the estimates of F were 89% and 94% for the cis isomer, respectively. The plasma concentrations of the trans isomer were about 1/10th of the cis isomer, and all parameters were similar to those observed for the cis isomer. In summary, cefprozil exhibits linear pharmacokinetics and is essentially completely absorbed after oral administration.

Adult↗
PubMedDate not supplied

In vitro activity of cefprozil (BMY 28100) and cefepime (BMY 28142) against Streptococcus pneumoniae, Branhamella catarrhalis, and Haemophilus influenzae, and provisional interpretive criteria for disk diffusion and dilution susceptibility tests with Haemophilus influenzae.

The in vitro activities of two new cephalosporins, an oral agent, cefprozil and a parenteral compound, cefepime, were assessed against recent clinical isolates of Streptococcus pneumoniae, Moraxella (Branhamella) catarrhalis, and Haemophilus influenzae. In general, both cefprozil and cefepime MICs were higher for beta-lactamase-producing strains of M. catarrhalis in comparison to strains that lacked beta-lactamase. By contrast, beta-lactamase-positive and -negative strains of H. influenzae had similar cefprozil and cefepime minimum inhibitory concentrations (MICs). The MIC90 values for cefprozil were 0.12, 32, 4.0, and 0.5 micrograms/ml versus S. pneumoniae, H. influenzae, and beta-lactamase-positive and negative strains of M. catarrhalis, respectively. In comparison to three other oral cephalosporins included in this study, cefaclor, cefuroxime axetil, and cefixime, cefprozil was the most active agent against S. pneumoniae, the least active against B. catarrhalis, and equivalent in activity to cefaclor against H. influenzae. The cefepime MIC values against S. pneumoniae, H. influenzae, and beta-lactamase-positive and negative strains of M. catarrhalis were 0.03, 0.25, 2.0, and 0.5 micrograms/ml, respectively. Cefepime was less active than ceftriaxone for all three organism groups, however, was in all cases more active than cefixime, cefuroxime, cefaclor, and cefprozil.(ABSTRACT TRUNCATED AT 250 WORDS)

Cefepime↗
PubMedDate not supplied

Comparison of the efficacy and tolerability of once-daily ceftibuten and twice-daily cefprozil in the treatment of children with acute otitis media.

In this multicenter, randomized, single (investigator)-masked study, the efficacy and tolerability of once-daily ceftibuten and twice-daily cefprozil were compared in the treatment of acute otitis media in patients 6 months to 10 years of age. Ceftibuten oral suspension 9 mg/kg once daily (maximum dose, 400 mg/d) and cefprozil oral suspension 15 mg/kg twice daily (maximum dose, 1000 mg/d) were given for 10 days. Clinical response, evaluated at the posttreatment visit (days 14 to 16), was rated as clinical cure, improvement, failure, relapse/recurrence, or not assessable. The clinical response was considered successful if the posttreatment assessment was clinical cure or clinical improvement and unsuccessful if the assessment was clinical failure, relapse/recurrence, or not assessable. Tolerability was evaluated by observed and spontaneously reported adverse events. A total of 205 patients were enrolled in the study. The ceftibuten group (51 males, 51 females; mean age, 4.8 years, range, 0.5 to 10.7 years) was similar in demographic characteristics to the cefprozil group (60 males, 43 females; mean age, 4.8 years, range, 0.7 to 10.7 years). In the ceftibuten-treated group, 83.3% (85) of the 102 patients had a successful response compared with 82.5% (85) of the 103 patients in the cefprozil-treated group. The incidence of treatment-related adverse events was similar in both groups, occurring in 5.9% (6) of the ceftibuten-treated patients and 5.8% (6) of the cefprozil-treated patients. Once-daily ceftibuten oral suspension was as effective and well tolerated as twice-daily cefprozil in the treatment of acute otitis media in children. The once-daily dosing schedule for ceftibuten therapy may aid patient compliance, particularly in the pediatric population. Ceftibuten should prove to be a useful alternative in the treatment of acute otitis media.

Acute Disease↗
PubMed1992

Review of the in vitro antibacterial activity of cefprozil, a new oral cephalosporin.

Cefprozil is a newer oral cephalosporin with a spectrum of activity against organisms that include gram-positive and gram-negative pathogens. A review of published data shows that cefprozil is active (susceptibility, less than or equal to 8 micrograms/mL; moderate susceptibility, 16 micrograms/mL; resistance, greater than or equal to 32 micrograms/mL) against gram-positive species such as streptococci, methicillin-susceptible staphylococci, and Listeria monocytogenes; it may have marginal activity against some enterococci. Among the gram-negative species, cefprozil has activity against Escherichia coli, Proteus mirabilis, Citrobacter diversus, Klebsiella pneumoniae, Klebsiella oxytoca, Haemophilus influenzae, and Moraxella catarrhalis. For anaerobic species, cefprozil has activity against clostridial species, including Clostridium difficile, peptostreptococci, and possibly Bacteroides melaninogenicus and Eubacterium. The activity of cefprozil is generally greater than that of cephalexin and generally similar to that of cefaclor. In these reports, cefprozil showed more in vitro activity than cephalexin and cefaclor against penicillin-resistant pneumococci, penicillin-resistant viridans streptococci, beta-lactamase-positive methicillin-susceptible Staphylococcus aureus, and C. difficile, although the clinical significance of some of these differences has yet to be studied.

Cephalosporins↗
PubMed1992

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

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

Acute Disease↗
PubMed1991

In-vitro activity of cefprozil (BMY 28100) and loracarbef (LY 163892) against pathogens obtained from middle ear fluid.

We compared the in-vitro activities of cefprozil, a novel oral cephalosporin, and of loracarbef, a new oral carbacephem, with other agents against middle ear fluid isolates obtained from children with acute otitis media. These included Streptococcus pneumoniae, Haemophilus influenzae and Branhamella catarrhalis. Cefprozil activity (MIC50 and MIC90) against S. pneumoniae was 0.25 and 0.50 mg/l; against H. influenzae 8 and 16 mg/l; against B. catarrhalis 2 and 2 mg/l. Loracarbef activity (MIC50 and MIC90) against S. pneumoniae was 1 and 2 mg/l; against H. influenzae 8 and 16 mg/l; against B. catarrhalis 1 and 8 mg/l. Cefprozil was four-fold more active against S. pneumoniae than loracarbef but similar to amoxycillin, amoxycillin/clavulanate, cefaclor, cefixime, cefuroxime and trimethoprim/sulfamethoxazole (TMP/SMX). Against H. influenzae, cefprozil was similar to loracarbef and other agents through less active than TMP/SMX and cefixime. Against B. catarrhalis, cefprozil was four-fold more active than loracarbef, cefaclor and cefixime but similar to the comparative antibiotics. Cefprozil and loracarbef activities were unaffected at pH 6 and 8 or in the presence of human serum, but there was a major diminution of activity for both agents at pH 5 and at inoculum sizes greater than or equal to 10(7) cfu/ml. Cefoprozil and loracarbef have consistent activity against middle ear pathogens and further pharmacokinetic and clinical studies appear warranted.

Acute Disease↗
PubMed1998

Comparison between cefprozil and penicillin to eradicate pharyngeal colonization of group A beta-hemolytic streptococci.

BACKGROUND: Our objective was to perform a prospective, randomized, double blinded study of cefprozil and penicillin therapy to eradicate group A beta-hemolytic streptococci (GABHS) in children who were bacteriologic failures after receiving a standard 10-day course of penicillin treatment for GABHS pharyngitis. METHODS: Children and adolescents 2 to 18 years of age were eligible for the study. From 3 to 7 days after completing oral penicillin therapy for pharyngitis caused by GABHS, the study was explained, informed consent was obtained, a history and physical examination were completed and a throat culture was performed. Children with throat cultures positive for GABHS were randomized to receive either cefprozil or penicillin for 10 days. Children who were bacteriologic failures after administration of the first study drug were crossed over to receive the alternate drug. RESULTS: Of 180 enrolled children 66 (37%) had throat cultures positive for GABHS. Seventeen were excluded from the study, leaving 49 who completed the protocol. Of the 49 participants 26 received cefprozil initially whereas 23 received penicillin. GABHS were eradicated from the pharynx of 73% of children who received cefprozil as the first antibiotic compared with 39% of penicillin recipients (chi square, 5.748, 0.01 < P < 0.025). After crossover of failures, the final efficacy rate for cefprozil was 65% compared with 36.7% for penicillin (chi square, 5.523, 0.01 < P < 0.025). CONCLUSIONS: Cefprozil was more effective than penicillin in treating children who were bacteriologic failures after a standard 10-day course of oral penicillin.

Adolescent↗
PubMed1992

Multiple-dose pharmacokinetics of cefprozil and its impact on intestinal flora of volunteers.

The pharmacokinetics of cefprozil were determined with 12 volunteers (8 received cefprozil and 4 received a placebo) after oral administration of 500 mg every 12 h over an 8-day period in a randomized, double-blind, placebo-controlled design. Concentrations in serum and urine were measured by high-pressure liquid chromatography and bioassay. The pharmacokinetic parameters were calculated on the basis of an open one-compartment model. The mean maximum concentration in serum on day 1 was 11.5 +/- 2.6 mg/liter, and the time to reach maximum concentration was 122.3 +/- 30 min after administration. Bioavailability parameters (area under the concentration-time curve from zero to infinity, maximum concentration of the drug in serum, and urinary recovery) indicated an excellent absorption. No accumulation over the 8-day period was registered. Cefprozil had a short biological elimination half-life of 58 +/- 10 min and a renal clearance of 210 +/- 51 ml/min, indicating high rates of renal excretion and tubular secretion. Analysis of the fecal flora showed an ecological impact of cefprozil on the intestinal microflora, such as a moderate decrease in enterobacteria and a slight increase in enterococci, staphylococci, and bacteroides during the study. The number of all bacterial species was already normalized 4 days after the administration period. The tolerance of cefprozil proved to be excellent; only a slight and reversible increase of liver enzymes (in two volunteers), mild cephalalgia, tiredness, and soft stool were registered during the 8-day period. Cefprozil had excellent absorption, no accumulation over an 8-day period, and only a limited impact on the intestinal microflora.

Administration, Oral↗
PubMed1992

Absolute bioavailability of cefprozil after oral administration in beagles.

The absolute bioavailability of cefprozil, a new oral cephalosporin, in four beagles was evaluated. In this two-way crossover study, each dog received a 125-mg dose of cefprozil either as an oral aqueous solution or as a 15-min intravenous infusion. A high-performance liquid chromatographic assay with UV detection was employed for the determination of cefprozil concentrations in plasma and urine. Key pharmacokinetic parameters were calculated by noncompartmental methods. Cefprozil was well absorbed after oral administration, and peak concentrations of 17.6 to 26.6 micrograms/ml were attained at 60 min after drug administration. The apparent elimination half-life of cefprozil was about 70 min. The renal clearance was about 60% of total body clearance and is suggestive of significant nonrenal clearance. The absolute bioavailability of cefprozil ranged from 67.1 to 79.1% in the dogs.

Administration, Oral↗