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PubMed1992

Effect of antacid on the bioavailability of cefprozil.

The effect of antacid on the bioavailability of cefprozil was investigated in a two-way crossover study. Eight healthy male subjects received a single 500-mg oral dose of cefprozil with and without coadministration of 30 ml of an antacid suspension containing magnesium hydroxide and aluminum hydroxide (Maalox). Cefprozil consists of cis and trans isomers in an approximate 90:10 ratio. When cefprozil was administered alone (treatment A), the mean maximum concentrations (Cmax) of the cis and trans isomers were 9.2 and 1.2 micrograms/ml, respectively. When cefprozil was coadministered with Maalox (treatment B), the Cmax values of the cis and trans isomers were 8.7 and 1.3 micrograms/ml, respectively. The mean values of the area under the curve from time zero to infinity (AUC0-infinity) were 27.7 and 3.5 micrograms.h/ml for treatment A and 27.5 and 3.5 micrograms.h/ml for treatment B for the cis and trans isomers, respectively. The other pharmacokinetic parameters, time to Cmax, elimination half-life, mean residence time, renal clearance, and percent urinary excretion, were essentially the same for the two isomers. The respective values of the elimination half-life for the cis and trans isomers were 1.36 and 1.32 h for treatment A and 1.36 and 1.42 h for treatment B. Mean urinary excretion was 63 and 60% for treatment A and 58 and 56% for treatment B for the cis and trans isomers, respectively. No significant differences between the two treatments were found for any of the pharmacokinetic parameters for either isomer. For the cis isomer, bioavailability point estimates (90% confidence intervals) of the mean Cmax and AUG0-infinity values for the Maalox treatment relative to those for the reference treatment were 95% (87%, 103%) and 99% (95%, 104%), respectively. For the trans isomer, the value were 109% (92%, 126%) for Cmax and 97% (88%, 106%) for AUC0-infinity. On the basis of the results of this study, it is concluded that the bioavailability of cefprozil is not affected by the coadministration of Maalox.

Administration, Oral↗
PubMed1993

Penetration of cefprozil into tonsillar and adenoidal tissues.

Penetration of cefprozil into tonsillar and/or adenoidal tissues was investigated for patients undergoing tonsillectomy and/or adenoidectomy. A total of 29 patients ranging in age from 2 to 14 years participated in the study. The tonsils and/or the adenoids were removed at times ranging from 0.33 to 3.17 h after oral administration of a dose of either 7.5 or 20 mg/kg of body weight. A blood sample was also collected as soon as the tissue sample was removed. Plasma, tonsil, and adenoid samples were analyzed for cis and trans isomers of cefprozil by high-performance liquid chromatographic assays. The concentrations of the cis isomer of cefprozil in plasma ranged from 0.60 to 9.87 micrograms/ml at the 7.5-mg/kg dose level and from 1.04 to 20.40 micrograms/ml at the 20-mg/kg dose level. The corresponding concentrations of the cis isomer in tonsil tissue ranged from 0.48 to 2.42 micrograms/g and from 1.00 to 4.29 micrograms/g, respectively. The corresponding concentrations of the cis isomer in adenoid tissue ranged from 0.40 to 4.20 micrograms/g and from 1.74 to 4.94 micrograms/g, respectively. The concentrations of the trans isomer were about 1/10 of those observed for the cis isomer. The median ratios of the cefprozil concentration in tonsillar tissue to that in plasma were 0.37 and 0.47 for patients receiving a 7.5- or a 20-mg/kg oral dose of cefprozil, respectively. The corresponding median ratios for the adenoidal tissue were 0.46 and 0.82, respectively. The cefprozil concentrations in either the tonsillar or the adenoidal tissue at both dose levels over 3.17 h after dosing are much higher than the MICs for common pathogens which cause pharyngitis or tonsillitis.

Adenoidectomy↗
PubMed1994

Penetration of cefprozil into middle ear fluid of patients with otitis media.

Penetration of cefprozil into the middle ear fluid was investigated in patients with chronic otitis media. A total of 89 patients ranging from 7 months to 11 years old participated in the study. The middle ear fluid was removed by ventilation tubes inserted through the tympanic membrane at times ranging from 0.38 to 5.97 h after oral administration of a single dose of 15 or 20 mg/kg of body weight. A blood sample was also collected as soon as the middle ear fluid was removed. Plasma samples were analyzed for the concentration of cefprozil by a high-performance liquid chromatographic assay. Middle ear fluid samples were analyzed for the concentration of cefprozil by a microbiological assay. The concentrations of cefprozil in plasma ranged from 0.38 to 15.97 micrograms/ml at the 15-mg/kg dose level and from 1.28 to 21.47 micrograms/ml at the 20-mg/kg dose level. The corresponding middle ear fluid concentrations of cefprozil ranged from 0.06 to 4.44 micrograms/ml and from 0.17 to 8.67 micrograms/ml, respectively. Cefprozil penetrates well into middle ear fluid in patients with chronic otitis media.

Cephalosporins↗
PubMed1995

Cefprozil, a new cephalosporin: its use in various clinical trials.

Cefprozil is a new oral cephalosporin with a broad spectrum of activity against a wide range of aerobic gram-positive and gram-negative organisms, as well as certain anaerobic bacteria. Cefprozil has demonstrated good stability in the presence of beta-lactamase-producing organisms, a common cause of bacterial resistance with many older beta-lactam antibiotics. The relatively long half-life of cefprozil and its sustained duration in tissue (as measured by skin blister fluid concentrations) support once- or twice-daily dosing. Cefprozil is well tolerated and has a low incidence of adverse events. A review of clinical studies that evaluated cefprozil for the treatment of otitis media, sinusitis, pharyngitis, tonsillitis, lower respiratory tract infections, skin and skin structure infections, and urinary tract infections is presented in this article. In multicenter clinical trials, cefprozil was found to be comparable or superior to frequently prescribed antibiotics, including other cephalosporins, in terms of its safety profile and its bacteriologic and clinical response rates.

Cephalosporins↗
PubMedDate not supplied

[Efficacy and safety of cefprozil versus cefaclor in the treatment of acute otitis media in pediatric patients]

OBJECTIVE: To evaluate the efficacy and safety of two oral cephalosporins, cefprozil and cefaclor, in the treatment of acute otitis media in children.METHODS: Forty children with clinical diagnosis of acute otitis media were randomized in two groups. Twenty-one children were given cefprozil at the dose of 30/mg/kg/day, in two equally divided doses every twelve hours, for ten days. Nineteen children were given cefaclor at the dose of 40/mg/kg/day in three divided doses every eight hours, for ten days. Efficacy evaluation of the antibiotic was analyzed by the presence or absence of symptoms, fever and otoscopic abnormalities while the safety and tolerability were evaluated by spontaneous information for possible adverse events.RESULTS: There was a significant decrease in the number of observed alterations between days 3 and 5 of treatment among those of the cefprozil group in comparison to the cefaclor group, while between days 10 and 14 of treatment the observed cure rate was clinically similar in both groups. Both medications presented adequate safety profiles. Only three children receiving cefprozil presented mild adverse events, such as nausea and vomit, none of which required treatment interruption.CONCLUSIONS: The clinical efficacy of both cephalosporins was similar although a more rapid activity was observed for cefprozil between days 3 and 5 of treatment. The favorable clinical results, the low incidence of adverse events and the twice a day dose regimen suggest that cefprozil is one more antimicrobial of choice for the treatment of acute otitis media in children, when this therapeutic is indicated.

Journal Article↗
PubMed2004

Efficacy and tolerability assessment of cefprozil in children with acute otitis media.

Young children contract as many as six to eight upper respiratory tract viral infections per year, and these infections frequently lead to secondary bacterial infections such as acute otitis media and sinusitis. Cefprozil is an orally active third generation cephalosporin which has demonstrated activity against the gram-positive organisms Streptococcus pyogenes, pneumoniae and agalactiae and against methicilin-susceptible Staphylococcus aureus. Cefprozil is also active against various gram-ves and certain anaerobic organisms, and is stable to hydrolysis by a number of b-lactamases. Present study is an effort to study the efficacy and safety of cefprozil in children with acute otitis media. Three hundred and thirty four children aged 6 months through 12 years with clinical symptoms and tympanic membrane signs of AOM received cefprozil 30 mg/kg/day in two divided doses per day for 10 days. Clinically, 96.6% patients were cured, 2.4% improved and there was failure of therapy in 1% of the patients. There was no need for any rescue medication and any change in antibiotic in any patient. A satisfactory bacteriological outcome was (i.e. cure, presumed cure, and cure plus reinfection with a different pathogen) was achieved in 95% of patients. In conclusion, cefprozil is a well tolerated and effective drug for acute otitis media in children. Moreover, its expanded spectrum of activity, ability to achieve adequate concentrations in tissues, suitability for twice-daily dosing, and proven tolerability suggest that it is a better alternative to agents conventionally used in acute otitis media.

Acute Disease↗
PubMed1994

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↗
PubMed2006

Pharmacodynamics of cefprozil against Haemophilus influenzae in an in vitro pharmacodynamic model.

An in vitro pharmacodynamic model was used to determine the pharmacokinetic-pharmacodynamic (PK-PD) measure and magnitude most strongly related to cefprozil activity against Haemophilus influenzae. Using 3 clinical isolates of H. influenzae, a series of dose-fractionation studies were conducted, simulating cefprozil pediatric pharmacokinetics. The studies were designed to deliver a range of free cefprozil AUC(24) given once daily, twice daily, and by continuous infusion (CI). Drug effect, characterized by computing the log(10) ratio of the area under the 24-h bacterial colony-forming unit (CFU) (AUC(CFU)) curve to drug-free control, was fit to a Hill-type model for 3 PK-PD measures of activity: AUC(24)/MIC, C(max)/MIC, and %T > MIC. Once daily regimens provided much less activity than twice daily or CI regimens. AUC(24)/MIC and %T > MIC characterized the data well, whereas C(max)/MIC did not. Based on the PK-PD model results, for cefprozil twice daily, 50% and 80% of maximum drug effect (E(max)) was achieved at a %T > MIC of approximately 52% and 75%, respectively. A 2-log(10) reduction in log(10) ratio would require free drug %T > MIC of 58% or AUC(24)/MIC of 86. Bacteriostasis was achieved at a %T > MIC and an AUC(24)/MIC of approximately 25% and 30%, respectively. An in vitro pharmacodynamic model was able to characterize the PK-PD of cefprozil against H. influenzae. Consistent with limited clinical data, a minimum %T > MIC of 40% to 50% would be suggested to achieve in vivo activity in otitis media, with maximal activity at approximately 70%T > MIC.

Anti-Bacterial Agents↗
PubMed2004

HPLC method for simultaneous determination of cefprozil diastereomers in human plasma.

A high-performance liquid chromatography method was developed for the determination of cefprozil diastereomers in human plasma. Cefprozil exists as cis and trans isomer at the ratio of 90:10. Plasma samples were prepared by protein precipitation using acetonitrile, trichloroacetic acid and methylene chloride. After the mixtures were vortexed and centrifuged, the aqueous supernatant was injected into a reversed-phase C8 column. The mobile phase consisted of acetonitrile, glacial acetic acid and distilled water at the volume ratio of 5.5:1.75:92.75 (pH 2.7). The signals were monitored with UV detection at 280 nm. The calibration curves of cis and trans isomer were linear in concentration ranges of 0.1-25 and 0.02-2.5 microg/mL with the correlation coefficient of 0.9999 and 0.9989, respectively. After oral administration of cefprozil in humans, Cmax and Tmax of total cefprozil were 18.80 +/- 2.14 microg/mL and 2.06 +/- 0.62 h. This method was sensitive with excellent selectivity and reproducibility, and successfully applied to a bioavailability study of cefprozil in healthy subjects.

Biological Availability↗
PubMed2003

Penetration of cefprozil to middle ear effusion in children with chronic otitis media with effusion.

BACKGROUND: Because of chronic otitis media with effusion (COME) demonstrates pathogenic bacteria, treatment with appropriate antibiotic is reasonable. OBJECTIVE: We determined the penetration of cefprozil into the middle ear effusion (MEE) in children with COME. MATERIALS AND METHODS: 25 patients 2-13 years of age with COME were eligible for study. After the single dose of 15 mg/kg patients were assigned to have MEE, and serum samples were obtained during ventilation tube insertion at 0.5, 2, 3, 5, or 6 h after administration of the dose. The concentration of cefprozil was measured using validated high performance liquid chromatography method. RESULTS: The mean concentrations of cefprozil in the MEE ranged from 0.4 to 4.4 microg/ml. The penetration into MEE was rapid and effective. Cefprozil in the MEE was maintained at a greater level than MIC 90 in S. pneumoniae for at least 6 h after administration of 15 mg/kg. CONCLUSION: Cefprozil penetrated well into the MEE in children with COME.

Administration, Oral↗
PubMed1992

Pharmacology and pharmacokinetics of cefprozil.

Cefprozil is a new orally administered cephalosporin with a spectrum of in vitro activity similar to that of cefuroxime. The pharmacokinetics of cefprozil are linear relative to dose size. Gastrointestinal absorption produces maximal plasma concentrations of approximately 10 mg/L 1-2 hours after administration of an oral dose of 500 mg. Approximately 94% of the dose is absorbed, and 60%-70% is excreted in the urine as unchanged drug. The renal clearance exceeds the glomerular filtration rate, thus suggesting active tubular secretion. Administration with food or antacids produces negligible effects on the rate or extent of absorption. Kinetic disposition in the elderly is similar to that in young healthy individuals, but elimination is slightly slower in infants and children. Because renal impairment, but not hepatic dysfunction, significantly reduces the elimination of cefprozil, it is recommended that the dosage be reduced by 50% in patients whose creatinine clearance is less than 30 mL/min. Penetration of the interstitial fluid by cefprozil is excellent, with concentrations approaching those observed in the plasma. The pharmacokinetic disposition of cefprozil, coupled with its in vitro activity, supports the use of once- or twice-daily dosage regimens.

Age Factors↗
PubMed1992

Review of the experience with cefprozil for the treatment of lower respiratory tract infections.

A regimen of cefprozil (500 mg twice daily), a new oral cephalosporin with a broad in vitro spectrum of antimicrobial activity, was compared to standard regimens of cefaclor (500 mg three times daily), cefuroxime axetil (500 mg twice daily), or amoxicillin/clavulanate (500 mg/125 mg three times daily) for the treatment of lower respiratory tract infections (mainly bronchitis and acute exacerbations of chronic bronchitis) in adults in three open-label, randomized trials. In the first trial, in which bacterial pathogens were isolated in initial cultures for only one-third of the patients, 90% of the pathogens were susceptible to cefprozil. A satisfactory clinical response was noted for 84% of the evaluable patients who received cefprozil versus 79% of those who received cefaclor for treatment of lower respiratory tract infections; rates of bacteriologic efficacy were 82% and 78%, respectively. In the second study rates of satisfactory clinical response were 96% with cefprozil and 83% with cefuroxime axetil (P less than .03) for treatment of bronchitis; the respective bacteriologic response rates were 100% and 92%. In the third trial, clinical efficacy was 91% for cefprozil and 87% for amoxicillin/clavulanate for treatment of bronchitis; bacteriologic efficacy was 95% and 96%, respectively. Tolerability and safety profiles were comparable, except that there was a higher rate of diarrhea among patients who received amoxicillin/clavulanate (P = .03).

Acute Disease↗
PubMed1992

Safety profile of cefprozil.

The clinical and laboratory safety of cefprozil was analyzed with data from 4,227 patients who received the drug in North American and European clinical efficacy trials. Of these patients, 3,016 adults and children received capsules or tablets, while 1,211 patients (mostly children) were treated with cefprozil suspension. Cefprozil was used in single-daily or twice-daily dosing regimens for treatment of infections of the upper and lower respiratory tracts, sinuses, middle ear, urinary tract, and skin and skin structure. The incidence of adverse clinical events and laboratory abnormalities was similar to that associated with use of other oral cephalosporins. Gastrointestinal adverse effects were the predominant adverse clinical event, although the incidence of diarrhea with cefprozil was much lower than that with cephalosporins that are less well absorbed. The data confirm the safety of cefprozil in both adult and pediatric patients.

Cephalosporins↗
PubMed1991

Comparative efficacy and safety of cefprozil and cefaclor in the treatment of acute uncomplicated urinary tract infections.

Cefprozil is a new oral semi-synthetic cephalosporin with broad antibacterial spectrum and prolonged serum elimination half-life. In vitro, cefprozil demonstrates excellent activity against common urinary tract pathogens such as Escherichia coli and Klebsiella pneumoniae. Cefprozil, 500 mg once a day, was compared to cefaclor, 250 mg three times a day, in an open, randomized, comparative, clinical trial for the treatment of acute, uncomplicated, urinary tract infection. One hundred and two adult patients were eligible for safety evaluation; four patients were excluded due to side-effects (abdominal discomfort, nausea and vomiting). Ninety-eight patients were eligible for evaluation of efficacy. Clinical and bacteriological responses were comparable for both antibiotics. Leucopenia, nausea, and vaginal yeast infections were slightly more common in the cefprozil group. Cefprozil, 500 mg once daily, appears to be an appropriate alternative for the treatment of acute, uncomplicated urinary tract infections.

Acute Disease↗
PubMed1994

Comparative efficacy and safety of cefprozil and amoxycillin/clavulanate in the treatment of acute otitis media in children.

Cefprozil is a new oral cephalosporin with activity against the most common pathogens isolated in acute otitis media. This randomized study enrolled 361 patients (mean age 29 months). Physical examination and culture via tympanocentesis were required less than 48 h before therapy. One hundred and ninety-one patients were evaluable for clinical efficacy; 99 received cefprozil (20 mg/kg/day bd) and 92 received amoxycillin/clavulanate (13.3 mg/kg/day tid). Duration of treatment was 7-9 days for 81 patients, 10 days for 105 patients and 11-16 days for five patients. The treatment groups were comparable with respect to demographics, severity of infection and number of previous episodes. Clinical evaluations of efficacy were based on physical examination including otoscopy within a 14 day period after therapy. Satisfactory clinical responses were achieved in 84% of cefprozil-treated patients and 87% of amoxycillin/clavulanate-treated patients. Pathogens most commonly isolated included Haemophilus influenzae (33%) and Streptococcus pneumoniae (22%). All 361 patients were evaluable for safety. Adverse clinical events were reported in 13% (24) of cefprozil-treated patients and 20% (36) of amoxycillin/clavulanate-treated patients. Cefprozil, administered twice a day, is comparable to a regimen of amoxycillin/clavulanate three times a day in the treatment of acute otitis media in children.

Acute Disease↗
PubMed2000

Comparison of a 5 day regimen of cefdinir with a 10 day regimen of cefprozil for treatment of acute exacerbations of chronic bronchitis.

Patients with acute exacerbations of chronic bronchitis were treated with cefdinir 300 mg bd for 5 days or cefprozil 500 mg bd for 10 days in a prospective, randomized, double-blind, multicentre study. Of the 548 patients enrolled, 281 (51%) were evaluable. The clinical cure rates at the test-of-cure visit were 80% (114/142) and 72% (100/139) for the evaluable patients treated with cefdinir and cefprozil, respectively. Respiratory tract pathogens were isolated from 409 (75%) of 548 admission sputum specimens, with the predominant pathogens being Haemophilus parainfluenzae, Haemophilus influenzae, Staphylococcus aureus and Moraxella catarrhalis. The microbiological eradication rates at the test-of-cure visit were 81% (157 of 193 pathogens) and 84% (166 of 198 pathogens) for the evaluable patients treated with cefdinir and cefprozil, respectively. Adverse event rates while on treatment were equivalent between the two treatment groups. The incidence of diarrhoea during therapy was higher for patients treated with cefdinir (17%) than for patients treated with cefprozil (6%) (P < 0.01), but most cases were mild and did not lead to discontinuation of treatment. These results indicate that a 5 day regimen of cefdinir is as effective and safe in the treatment of patients with acute exacerbations of chronic bronchitis as a 10 day regimen of cefprozil.

Acute Disease↗
PubMed1991

Comparative trial of cefprozil vs. amoxicillin clavulanate potassium in the treatment of children with acute otitis media with effusion.

A total of 137 children with acute otitis media with effusion were randomly allocated to treatment with cefprozil (30 mg/kg/day divided into two equal doses), an investigational cephalosporin or amoxicillin clavulanate potassium (40 mg/kg/day divided into three equal doses) for 10 days. The most common pathogens obtained from middle ear cavities by tympanocentesis were Streptococcus pneumoniae (33%), Haemophilus influenzae (19.6%) and Moraxella catarrhalis (8.3%). Patients were scheduled for follow-up visits at midtreatment, at end of therapy and at 30 days. Of the 137 children 122 were evaluable. Five of 60 patients (8.3%) treated with cefprozil and 14 of 62 patients (22.5%) treated with amoxicillin clavulanate potassium were considered therapeutic failures because of persistence of symptoms and/or isolation of the original pathogen or superinfection (P = 0.05). Rates of relapse, reinfection and persistent middle ear effusion as documented by tympanogram were comparable in both groups. When persistent middle ear effusion was analyzed by pneumatic otoscopy, 64 of 103 affected ears (62.1%) treated with cefprozil and 80 of 105 affected ears (76.1%) treated with amoxicillin clavulanate potassium were abnormal (P = 0.04). Loose stools were more common in children treated with amoxicillin clavulanate potassium than in children treated with cefprozil (P = 0.0004). Based on the efficacy results from this study, the lower gastrointestinal side effects and the convenience of twice-a-day dosing, we believe that cefprozil in a dosage of 30 mg/kg/day divided every 12 hours represents a potential alternative for the treatment of acute otitis media with effusion in children.

Acute Disease↗
PubMed2000

Five-day cefdinir course vs. ten-day cefprozil course for treatment of acute otitis media.

OBJECTIVE: To compare the clinical efficacy of a 5-day cefdinir course with a 10-day cefprozil course in the treatment of pediatric acute otitis media (AOM). DESIGN: Comparative, investigator-blinded multicenter trial. SETTING: Primary care, ambulatory. PATIENTS: Children ages 6 months through 12 years with clinical symptoms and tympanic membrane signs of AOM, plus tympanometric-confirmed middle ear effusion in at least 1 ear. Of the 435 patients enrolled in the study, 373 were evaluable. INTERVENTION: Patients received cefdinir 14 mg/ kg/day divided twice a day for 5 days or cefprozil 30 mg/kg/day divided twice a day for 10 days. MAIN OUTCOME MEASURES: Clinical resolution of tympanic membrane signs and symptoms of AOM determined at end of therapy on Study Days 9 to 11. RESULTS: The clinical cure rate at end of therapy was 80% (152 of 190) for cefdinir-treated patients and 82.5% (151 of 183) for cefprozil-treated patients (95% confidence interval, 10.43% to 5.4%). Diarrhea and overall adverse reactions, respectively, occurred in 7.8 and 13% of cefdinir-treated patients and in 4.2 and 12% of cefprozil-treated patients. CONCLUSIONS: A short course 5-day regimen of cefdinir was as clinically effective and well-tolerated as a 10-day regimen of cefprozil in the treatment of nonrefractory AOM.

Acute Disease↗