cefdinir and Bacterial-Infections

Cefdinir is an extended-spectrum, third-generation, oral cephalosporin widely used in pediatric population to treat common bacterial infections, including otitis media and streptococcal pharyngitis. It is considered a safe and well-tolerated alternative to penicillin and macrolides.. This report describes a case series of 3 infants presenting to the emergency department for evaluation of "bloody diarrhea." The parents noticed red stools when their children were started on oral cefdinir when they were previously receiving iron-containing preparations. Reddish-colored heme-negative stools observed in all cases were due to the interaction of the drug with supplemental iron or iron-containing formula feeds. This adverse effect was reversible on discontinuation of cefdinir. WHY SHOULD AN EMERGENCY PHYSICIAN BE AWARE OF THIS?: Red stools due to cefdinir is an underreported benign adverse drug reaction with fewer than 10 cases described in the literature. Thorough history taking with an appropriate focus on diet and drug history are essential to avoid parental anxiety, unnecessary patient workup, and economic burden to the caregivers in these cases. Awareness of this unusual adverse effect among emergency physicians could prevent further inconvenience for already overburdened health systems.

Topics: Anti-Bacterial Agents; Bacterial Infections; Cefdinir; Cephalosporins; Child; Child, Preschool; Drug-Related Side Effects and Adverse Reactions; Humans; Infant; Iron

Acute otitis media (AOM) is diagnosed based on visualization of a full or bulging tympanic membrane with middle ear effusion. The distribution of bacteria causing AOM in North America under the influence of pneumococcal conjugate vaccination and antibiotic selection pressure has resulted in a predominance of β-lactamase-producing Haemophilus influenzae followed by penicillin-resistant Streptococcus pneumoniae. Although guidelines continue to endorse amoxicillin as the preferred treatment, amoxicillin/clavulanate in high dosage would be the preferred treatment based on the otopathogen mix currently. Antibiotic prophylaxis has fallen into disfavor as a preventative strategy for AOM recurrences.

Topics: Age Factors; Amoxicillin; Amoxicillin-Potassium Clavulanate Combination; Anti-Bacterial Agents; Bacterial Infections; Cefdinir; Cefpodoxime Proxetil; Ceftizoxime; Cefuroxime; Cephalosporins; Child; Child, Preschool; Haemophilus influenzae; Humans; Infant; Microbial Sensitivity Tests; Moraxella catarrhalis; Otitis Media; Otitis Media with Effusion; Otoscopy; Streptococcus pneumoniae; Time Factors; Tympanic Membrane

Topics: Anti-Bacterial Agents; Bacterial Infections; Cefdinir; Cephalosporins; Humans; Microbial Sensitivity Tests; Randomized Controlled Trials as Topic

Cefdinir is an advanced-generation, broad-spectrum cephalosporin antimicrobial agent that has been approved for the treatment of community-acquired pneumonia, acute bacterial exacerbations of chronic bronchitis, acute maxillary sinusitis, pharyngitis/tonsillitis, acute bacterial otitis media, and uncomplicated skin and skin-structure infections in adult and pediatric patients.. The purpose of this article was to review the in vitro antimicrobial activity, pharmacokinetics, clinical efficacy, safety, and potential role of cefdinir.. Studies were identified by a MEDLINE search (January 1983-September 2001) of the English-language medical literature, a review of identified articles and their bibliographies, and a review of data on file with the manufacturer. Clinical efficacy data were selected from all published trials mentioning cefdinir. Information concerning in vitro susceptibility, safety, chemistry, and the pharmacokinetic profile of cefdinir also was reviewed.. Cefdinir has a broad spectrum of activity against many gram-negative and gram-positive aerobic organisms, including Streptococcus pneumoniae, Staphylococcus aureus, Streptococcus pyogenes, Haemophilus influenzae, and Moraxella catarrhalis. Cefdinir is stable to hydrolysis by 13 of the common beta-lactamases. It is rapidly absorbed from the gastrointestinal tract (mean time to peak plasma concentration, 3 hours) and is almost entirely eliminated via renal clearance of unchanged drug. The terminal disposition half-life of cefdinir is approximately 1.5 hours. Efficacy has been demonstrated in 19 clinical trials in adults and children with upper and lower respiratory tract infections (eg, pharyngitis, sinusitis, acute otitis media, acute bronchitis, acute bacterial exacerbation of chronic bronchitis, community-acquired pneumonia), and skin and skin-structure infections. The adverse-event profile is similar to that of comparator agents, although in 4 adult and adolescent studies and 1 adult study, diarrhea occurred significantly more frequently in cefdinir recipients than in recipients of penicillin V, cephalexin, cefaclor, and cefprozil.. Cefdinir is an alternative to other antimicrobial agents and can be dosed once or twice daily for the treatment of upper and lower respiratory tract infections and skin and skin-structure infections. Similar to other oral expanded-spectrum cephalosporins, cefdinir has activity against common pathogens of the respiratory tract and skin and is stable in the presence of selected beta-lactamases. The clinical choice of an oral expanded-spectrum cephalosporin will be based on patient acceptance, frequency of administration, and cost.

Topics: Administration, Oral; Bacteria; Bacterial Infections; Cefdinir; Cephalosporins; Humans

Oral second and third generation cephalosporins are undergoing continuing research and development in the arena of pediatric infectious disease in an attempt to fill voids created by existing agents in the quest for the "ideal" antimicrobial. This paper reviews the in vitro antimicrobial activity (pharmacodynamics) and pharmacokinetics of cefdinir, an extended spectrum oral cephalosporin, with an emphasis on those aspects relevant to the pediatric patient population.. A MEDLINE literature search was conducted for the years 1985 through 2000, identifying all English language papers examining the in vitro antimicrobial activity and human pharmacokinetics of cefdinir. Bibliographies of these papers were reviewed, as were relevant data on file with the manufacturer.. Cefdinir exhibits broad range in vitro activity against Gram-positive and Gram-negative aerobes. It exhibits superior activity against Gram-positive aerobes, compared with drugs like cefixime, ceftibuten, cefuroxime and cefpodoxime. In addition it is stable to hydrolysis by many of the common betalactamases. The pharmacokinetic parameters of cefdinir in children are similar to those obtained in adults using similar milligram per m2 doses (300, 600 mg in adults = 7, 14 mg/kg in children, respectively).. The pharmacodynamic and pharmacokinetic characteristics of cefdinir as described in this paper, as well as the results of the clinical trials program, support the use of this agent in the treatment of a wide variety of pediatric infectious diseases.

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

This article reviews structure-activity relationships and biological properties of a new oral cephem, cefidinir (CFDN). It also describes a hypothesis concerning the absorption mechanism from the intestine. Antibacterial activities and the oral absorption efficiencies were studied with regard to 3-vinyl cephalosporins with various 7-acyl side chains. From the study, 2-(2-aminothiazol-4-yl)-2-hydroxyiminoacetyl group was selected and various 3-substituents were screened. As a result, it was found that the vinyl compound, CFDN, showed excellent antibacterial activity and good oral absorption in rats. In vitro and in vivo antibacterial activities, the affinity for PBPs and the stability to beta-lactamases revealed that CFDN had well balanced antimicrobial activities against Gram-positive and Gram-negative bacteria and good biological properties. The pharmacokinetics of CFDN in healthy volunteers showed that serum concentration and half life were good enough to make CFDN an effective therapeutic agent. The mechanism of intestinal absorption of CFDN and related oral cephems are discussed and a hypothesis for molecular recognition by the carrier protein in the intestine is proposed.

Topics: Animals; Bacteria; Bacterial Infections; Cefdinir; Cephalosporins; Drug Resistance, Microbial; Humans; Intestinal Absorption; Structure-Activity Relationship

Topics: Animals; Bacteria; Bacterial Infections; Bacterial Proteins; beta-Lactamases; Carrier Proteins; Cefdinir; Cephalosporins; Drug Evaluation; Drug Resistance, Microbial; Drug Stability; Hexosyltransferases; Humans; Muramoylpentapeptide Carboxypeptidase; Penicillin-Binding Proteins; Peptidyl Transferases; Protein Binding

To assess the efficacy and tolerability of three antibiotic regimens in patients with acute exacerbation of chronic bronchitis.. In this double-blind, randomized, multicentered, parallel-group study, patients received once-daily cefdinir 600 mg, twice-daily cefdinir 300 mg, or twice-daily cefuroxime axetil 250 mg for 10 days. Primary efficacy measures were microbiologic eradication rate, by pathogen and by patient, and clinical response rate, by patient.. Of 1045 patients, 589 were evaluable for efficacy. At baseline, most patients had moderate or severe cough and sputum production as well as rhonchi, wheezing, and dyspnea. The microbiologic eradication rates by pathogen were 90% with once-daily cefdinir, 85% with twice-daily cefdinir, and 88% with twice-daily cefuroxime. The corresponding values for microbiologic eradication rate by patient were 90% (once-daily cefdinir), 85% (twice-daily cefdinir), and 86% (twice-daily cefuroxime). The respective clinical response rates by patient were 81%, 74%, and 80%. There were no significant differences in the incidence of drug-related adverse events or discontinuations due to adverse events. Diarrhea was the most frequent complaint.. The results indicate that the efficacy and tolerability of cefdinir, once or twice daily, and cefuroxime were comparable with no significant differences between the regimens used.

Topics: Adolescent; Adult; Aged; Aged, 80 and over; Anti-Bacterial Agents; Bacteria; Bacterial Infections; Bronchitis; Cefdinir; Cefuroxime; Cephalosporins; Chronic Disease; Double-Blind Method; Female; Humans; Male; Middle Aged; Treatment Outcome

Cefdinir is a new, extended-spectrum, orally active, third-generation cephalosporin that is resistant to bacterial beta-lactamase production. To evaluate efficacy and safety of the antibiotic in maxillary sinusitis, its use was compared with amoxicillin/clavulanate (amox/clav), which is a well-accepted beta-lactamase-resistant antibiotic. In this investigator-blinded multicenter phase III clinical study, 569 patients were randomly assigned to one of three treatment regimens: one daily dose of cefdinir 600 mg (OD), cefdinir 300 mg every 12 h (BD), and amox/clav 500/125 mg every 8 h. All antibiotics were administered orally for 10 days. Maxillary sinusitis was documented by typical clinical signs and symptoms and was confirmed by X-ray imaging. Before treatment, the genus and species of any pathogens were determined from sinus aspirates. Cultures were tested for beta-lactmase production and in vitro resistance to cefdinir and amox/clav. The effectiveness of antibiotic treatment was evaluated 7-14 days after therapy and whether or not recurrent clinical symptoms or persistent infection was determined 21-35 days post-therapy. The appearance of any adverse events was classified as associated or not associated with the medication of the study. Present findings showed that the in vitro susceptibility of pathogens to cefdinir and amox/clav was similar. Cefdinir OD or BD was therapeutically as effective as or better than amox/clav, although cefdinir BD was not as useful as amox/clav clinically. Cefdinir OD and BD and amox/clav were well tolerated. The statistical incidence of adverse events was the same among the three treatment groups, although cefdinir OD treatment had significantly fewer treatment discontinuations due to adverse events than BD and amox/clav.

Topics: Administration, Oral; Adolescent; Adult; Aged; Amoxicillin-Potassium Clavulanate Combination; Anti-Infective Agents; Bacterial Infections; Cefdinir; Cephalosporins; Dose-Response Relationship, Drug; Drug Administration Schedule; Female; Humans; Male; Maxillary Sinusitis; Middle Aged; Treatment Outcome

To compare the efficacy and safety of five-day cefdinir treatment with seven-day loracarbef treatment in patients with acute exacerbations of chronic bronchitis, 586 patients were enrolled in a multicentre, randomised, double-blind trial. Patients received either five days of treatment with cefdinir (n = 291) at 300 mg twice daily or seven days of treatment with loracarbef (n = 295) at 400 mg twice daily. Microbiological assessments were done on sputum specimens obtained at admission and at the two post-therapy visits, if available. The clinical cure rates were 86% (138/160) and 85% (141/166) for the evaluable patients treated with cefdinir and loracarbef, respectively. Respiratory tract pathogens were isolated from 457 (78%) of 586 admission sputum specimens, with the predominant pathogens being Haemophilus parainfluenzae, H. influenzae, Moraxella catarrhalis and Staphylococcus aureus. The microbiological eradication rates at the test-of-cure visit were 88% (193/219 pathogens) and 90% (227/251 pathogens) for the evaluable patients treated with cefdinir and loracarbef, respectively. Adverse event rates while on treatment were 30% and 21% for cefdinir- and loracarbef-treated patients, respectively. These results indicate that a five-day regimen of cefdinir is effective and safe for the treatment of patients with acute exacerbations of chronic bronchitis.

Topics: Adolescent; Adult; Aged; Anti-Infective Agents; Bacterial Infections; Bronchitis; Cefdinir; Cephalosporins; Chronic Disease; Double-Blind Method; Drug Administration Schedule; Female; Humans; Male; Middle Aged; Prospective Studies; Sputum; Treatment Outcome

To examine the microbiologic and clinical efficacy of a 5-day course of cefdinir in the treatment of tympanocentesis-documented acute otitis media (AOM).. Open label noncomparative trial.. Primary care, ambulatory.. Children ages 6 months through 12 years with signs of AOM and middle ear effusion confirmed by tympanometry in at least one ear.. Patients underwent tympanocentesis at baseline and received cefdinir 7 mg/kg twice a day for 5 days.. Presumptive eradication of middle ear pathogens determined by clinical cure of signs and symptoms of AOM at end of therapy (Study Days 7 to 9) and Visit 3 (Study Days 16 to 21).. A total of 125 of 177 enrolled children had 134 pathogens isolated by tympanocentesis: Streptococcus pneumoniae, 69 (51.5%); Haemophilus influenzae 44 (32.8%; beta-lactamase-positive in 18 of 44 strains); beta-lactamase-positive Moraxella catarrhalis, 15 (11.2%); and Streptococcus pyogenes, 6 (4.5%). The clinical cure rates by patient in the microbiologically and overall clinically evaluable groups, respectively, were 73% (84 of 115) and 77.4% (130 of 168) at the end of therapy visit and 57.4% (66 of 115) and 61.9% (104 of 168) at Visit 3. Presumptive eradication rates at end of therapy were 8 of 11 (72.7%) and 4 of 8 (50%) for patients with penicillin-intermediate and -resistant S. pneumoniae isolates, respectively. Adverse reactions occurred in 16% of patients, with diarrhea (11%) occurring most frequently.. A 5-day regimen of cefdinir was effective in the eradication of the common causative pathogens of nonrefractory AOM, including intermediate penicillin-resistant S. pneumoniae and beta-lactamase-producing organisms. Cefdinir should be considered a suitable second line antibiotic for AOM.

Topics: Acoustic Impedance Tests; Acute Disease; Bacterial Infections; Cefdinir; Cephalosporins; Child; Child, Preschool; Female; Haemophilus influenzae; Humans; Infant; Male; Microbial Sensitivity Tests; Moraxella catarrhalis; Otitis Media; Otitis Media with Effusion; Penicillin Resistance; Streptococcus pneumoniae; Streptococcus pyogenes; Treatment Outcome

Cefdinir is an extended-spectrum oral cephalosporin that is active against pathogens commonly seen in acute community-acquired bacterial sinusitis (ACABS), including Streptococcus pneumoniae, Haemophilus influenzae, and Moraxella catarrhalis. Two randomized, investigator-blind, multicenter trials (one in the United States and one in Europe) compared two dosage regimens of cefdinir (600 mg once a day for 10 days and 300 mg twice a day for 10 days) to amoxicillin-clavulanate (A-C) (500 mg three times a day for 10 days) for adult and adolescent patients with ACABS. Twelve hundred twenty-nine patients entered the U.S. study, 698 with antral puncture; 569 patients entered the European study, all with antral puncture. Clinical response (cure or improvement) was determined 7 to 14 days and 3 to 5 weeks posttherapy. Microbiologic eradication rates were determined 10 to 30 days posttherapy in a subset of patients who underwent pre- and posttherapy sinus aspirate culture. Rates of adverse events and treatment discontinuations due to adverse events were examined. Cefdinir, given once or twice daily, was as effective clinically (approximately 90% cure rate) as amoxicillin-clavulanate given three times daily in the treatment of ACABS. Microbiologic eradication rates were also similar in the three groups. The major side effect was mild diarrhea, occurring in approximately 20% of each group. Cefdinir caused fewer adverse events requiring treatment discontinuation.

Topics: Adolescent; Adult; Aged; Aged, 80 and over; Amoxicillin; Amoxicillin-Potassium Clavulanate Combination; Bacterial Infections; Cefdinir; Cephalosporins; Child; Clavulanic Acids; Community-Acquired Infections; Drug Administration Schedule; Drug Therapy, Combination; Female; Humans; Male; Microbial Sensitivity Tests; Middle Aged; Single-Blind Method; Sinusitis; Treatment Outcome

Bacteriological, pharmacokinetic and clinical studies on cefdinir (CFDN, FK482), a new oral cephalosporin, 5% and 10% granules, were performed in the field of pediatrics. The results are summarized below. 1. Antibacterial activities Antibacterial activities of CFDN against Staphylococcus aureus, Streptococcus pyogenes, Streptococcus pneumoniae, Haemophilus influenzae, Branhamella catarrhalis, Escherichia coli and Klebsiella pneumoniae were studied in comparison with those of cefaclor (CCL), cefixime (CFIX) and amoxicillin (AMPC). MIC80's of CFDN against S. aureus, S. pneumoniae, S. pyogenes, H. influenzae, B. catarrhalis, K. pneumoniae and E. coli were 0.78, 0.20, less than or equal to 0.025, 0.39, 0.10, 0.20 and 0.10 micrograms/ml, respectively. These results show that CFDN has high antibacterial activities against these organisms. MIC80's of CFDN against Gram-positive bacteria were similar to those of AMPC, and was lower than those of CCL and CFIX. As for antibacterial activities against Gram-negative bacteria (GNB), the MIC80 of CFIX against H. influenzae was 0.05 micrograms/ml, which was slightly lower than that of CFDN. THe MIC80's of CFDN against other GNB were similar to those of CFIX. 2. Absorption and excretion Blood concentrations and urinary excretion rates of CFDN 5% and 10% granules and 100 mg capsule were determined. The data on CFDN 10% granules were similar to those on CFDN 5% granules. At a dose of 3 mg/kg, peak blood concentrations (Cmax's) of CFDN ranged from 0.20 to 2.12 micrograms/ml with 5% granules and from 0.50 to 1.15 micrograms/ml with 10% granules at 2 to 3 hours after dosing. At a dose of 6 mg/kg, peak concentrations were 0.66-2.06 micrograms/ml and 0.70-1.52 micrograms/ml with 5% granules and with 10% granules, respectively. At 8 hours after dosing, blood concentrations were 0.04-0.54 micrograms/ml at 3 mg/kg and 0.06-0.27 micrograms/ml at 6 mg/kg. Blood half-lives were 1.33-4.36 hours at 3 mg/kg and 1.14-3.27 hours at 6 mg/kg. AUC's were 1.7-11.0 micrograms.hr/ml with 3 mg/kg and 2.4-8.7 micrograms.hr/ml with 6 mg/kg. With administration of single 100 mg capsule, Cmax's, blood concentrations after 8 hours, T1/2's and AUC's were 0.79-1.88 micrograms/ml, 0.20 micrograms/ml, 1.54-2.72 hours, and 5.2 micrograms.hr/ml, respectively. Urinary recovery rates in the first 8 hours ranged from 6.85 to 39.2% with 3 mg/kg and 6.08-25.5% with 6 mg/kg.(ABSTRACT TRUNCATED AT 400 WORDS)

Topics: Adolescent; Amoxicillin; Anti-Bacterial Agents; Bacteria; Bacterial Infections; Cefaclor; Cefdinir; Cefixime; Cefotaxime; Cephalosporins; Child; Child, Preschool; Dose-Response Relationship, Drug; Female; Humans; Infant; Male; Microbial Sensitivity Tests

Cefdinir (CFDN), a newly developed oral cephalosporin in a 10% fine granular form, was administered to 8 children and concentrations of the drug in plasma and urine and urinary recovery rates of the drug were determined. The subjects were divided into 2 groups of 4 children each; one group received 3 mg/kg of CFDN at 1 hour before meal (in the fasting state), and the other, at 30 minutes after meal. To study clinical and bacteriological effects of this drug, a mean dose of 4.8 mg/kg t.i.d. was administered for 8 days on the average to 9 children with various infections; tonsillitis (3 cases), acute bronchitis (1), pneumonia (1), acute purulent otitis media (1), urinary tract infection (2), and impetigo (1). MICs were determined for 6 drugs including CFDN, cefaclor, cefixime (CFIX), methicillin, cloxacillin, amoxicillin (AMPC) against 4 strains freshly isolated from children receiving CFDN. An inoculum size of 10(6) cfu/ml was used in the MIC-determinations. Adverse reactions and abnormal laboratory findings attributable to this drug were also examined in these children. The results obtained are summarized as follows. 1. Mean plasma peak levels of CFDN were observed at 2 hours after administration in the before-meal group and 4 or 5 hours after administration in the after-meal group mean peak values of 0.88 and 0.50 micrograms/ml, respectively. Mean half-lives were 1.61 hours in the before-meal group and 2.54 hours in the after-meal group, and mean AUCs were 4.24 in the former and 3.59 micrograms.hr/ml in the latter. 2. Mean urinary peak concentrations of CFDN were observed during 2-4 hours after dosing in the before-meal group and during 6-8 hours in the after-meal group with values of 93.3 and 44.8 micrograms/ml, respectively, in cases for which plasma concentrations of drugs were determined. Mean urinary recovery rates during the first 8 hours after administration in the before- and after-meal groups were 16.6 and 13.4%, respectively. 3. Good clinical effects were obtained with an efficacy rate of 100% in 9 patients with 6 diseases due to bacterial infections. 4. Good bacteriological effects were also obtained against 2 strains of Streptococcus pyogenes, 2 strains of Escherichia coli and 1 strain of Haemophilus influenzae with an eradication rate of 100%. In 3 cases of these and another case (normal flora), strains present before the study were replaced by other strains.(ABSTRACT TRUNCATED AT 400 WORDS)

Topics: Amoxicillin; Anti-Bacterial Agents; Bacterial Infections; Cefdinir; Cephalosporins; Child; Child, Preschool; Cloxacillin; Eating; Escherichia coli; Female; Humans; Infant; Male; Methicillin; Microbial Sensitivity Tests; Streptococcus pyogenes

We studied pharmacokinetics and clinical effects of 5% and 10% fine granules of cefdinir (FK 482, CFDN), a new oral cephalosporin, in the pediatric field and the following results were obtained. 1. Pharmacokinetics (blood concentration and urinary excretion) Pharmacokinetics of CFDN in 163 children was investigated. Cmax and T 1/2 were 0.92 +/- 0.45 micrograms/ml and 1.95 +/- 1.06 hours, respectively, in the fasting state, and were 0.63 +/- 0.29 micrograms/ml and 2.26 +/- 0.65 hours, respectively, in the non-fasting state, at a dose level of 3 mg (potency)/kg. At a dose level of 6 mg (potency)/kg, Cmax and T 1/2 were 1.29 +/- 0.49 micrograms/ml and 2.11 +/- 1.85 hours, respectively, in the fasting state and were 1.28 +/- 0.48 micrograms/ml and 2.01 +/- 0.84 hours, respectively, in the non-fasting state. Data of Cmax and AUC showed that blood concentration of the drug depended on dose levels. Urinary recovery rates in the first 8 hours were 20.5 +/- 8.8% in the fasting state and 14.8 +/- 5.9% in the non-fasting at a dose level of 3 mg (potency)/kg and 16.5 +/- 6.7% and 17.8 +/- 2.4%, respectively, at 6 mg (potency)/kg. 2. Clinical effects Clinical effects of CFDN on various infections were studied in 612 children who were treated with 5% fine granules of CFDN (5% granule group) and in 208 with 10% fine granules of CFDN (10% granule group). CFDN granules were administered mainly at daily doses of 9.0-18.0 mg (potency)/kg in 3 divided portions. Clinical efficacy rates in 428 children of the 5% granule group and in 159 of the 10% granule group from whom causative bacteria were isolated, were 94.9% and 96.2%, respectively. The clinical efficacy rates for patients who were responsive to previous antibiotic therapy were 91.2% in the 5% granule group and 100% in the 10% granule group. Bacteriological eradication rate was 82.1% for 491 strains in the 5% granule group, and was 84.0% for 175 strains in the 10% granule group. The incidences of side effects were 3.9% (24/608) in the 5% fine granule group and 5.8% (12/206) in the 10% granule group. All of the side effects were slight gastrointestinal disorders, and no serious side effects were found. As for clinical laboratory test results, slight elevations of eosinophile, platelet or transaminase were observed. Based on the above results, it is considered that the appropriate dose levels of CFDN for pediatric infections ranged from 9.0 to 18.0 mg (potency)/kg a day, divided into 3 portions.

Topics: Administration, Oral; Adolescent; Age Factors; Bacteria; Bacterial Infections; Biological Availability; Cefdinir; Cephalosporins; Child; Child, Preschool; Dosage Forms; Drug Resistance, Microbial; Humans; Infant

Clinical evaluations of cefdinir (CFDN, FK482) were carried out. The obtained results are summarized as follows. 1. Clinical responses to CFDN of 43 patients with pediatric infections were excellent in 23, good in 15, fair in 4 and poor in 1. The overall efficacy rate was 88%. 2. Bacteriologically, the eradication rate for 34 isolates presumed to be pathogens was evaluated and the eradication rate was 85.3%. 3. Side effects observed were diarrhea in 4 of 48 patients. The incidence was 8.3%. Abnormal laboratory findings were an elevation of GOT, an elevation of eosinophils and an increase in platelet counts. The results suggested that CFDN might be a very useful and safe drug for the treatment of pediatric infections.

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

Cefdinir (CFDN, FK482) granules, a new oral antibiotic for children, were given to children with infections. The results obtained are summarized as follows. 1. The plasma level of CFDN peaked at 0.38-0.88 microgram/ml in 2-3 hours after administration of the drug at a dose of 3 mg/kg. Meanwhile, the plasma level peaked at 1.85 micrograms/ml in 3 hours after administration of 6 mg/kg. The plasma level was higher in the 6 mg/kg group than that in the 3 mg/kg group, thus a dose response was clearly observed. 2. The 8 hour urinary excretion accounted for 10.3-17.4% of administered amount of the drug in children with 3-6 mg/kg dosage. 3. CFDN granules were administered to a total of 42 children with upper or lower airway infections or with urinary tract infections at daily doses of 9.0-20.7 mg/kg in 3 divided portions. The clinical efficacy was "excellent" in 28 patients, "good" in 13, and "fair" in 1, hence an efficacy rate of 97.6% was obtained. 4. Bacteria identified from various diseases were 29 strains of 9 species, and the eradication rate was 82.8%. 5. No. side effects were noted in any of the children. Laboratory test results showed an abnormality in 1 case each with a rise of platelet count and eosinophilia.

Topics: Administration, Oral; Age Factors; Bacteria; Bacterial Infections; Cefdinir; Cephalosporins; Child; Child, Preschool; Female; Humans; Infant; Male

Surveillance studies conducted in the United States over the last decade have revealed increasing resistance among community-acquired respiratory pathogens, especially Streptococcus pneumoniae, that may limit future options for empirical therapy. The objective of this study was to assess the scope and magnitude of the problem at the national and regional levels during the 2005-2006 respiratory season (the season when community-acquired respiratory pathogens are prevalent) in the United States. Also, since faropenem is an oral penem being developed for the treatment of community-acquired respiratory tract infections, another study objective was to provide baseline data to benchmark changes in the susceptibility of U.S. respiratory pathogens to the drug in the future. The in vitro activities of faropenem and other agents were determined against 1,543 S. pneumoniae isolates, 978 Haemophilus influenzae isolates, and 489 Moraxella catarrhalis isolates collected from 104 U.S. laboratories across six geographic regions during the 2005-2006 respiratory season. Among S. pneumoniae isolates, the rates of resistance to penicillin, amoxicillin-clavulanate, and cefdinir were 16, 6.4, and 19.2%, respectively. The least effective agents were trimethoprim-sulfamethoxazole (SXT) and azithromycin, with resistance rates of 23.5 and 34%, respectively. Penicillin resistance rates for S. pneumoniae varied by region (from 8.7 to 22.5%), as did multidrug resistance rates for S. pneumoniae (from 8.8 to 24.9%). Resistance to beta-lactams, azithromycin, and SXT was higher among S. pneumoniae isolates from children than those from adults. beta-Lactamase production rates among H. influenzae and M. catarrhalis isolates were 27.4 and 91.6%, respectively. Faropenem MICs at which 90% of isolates are inhibited were 0.5 mug/ml for S. pneumoniae, 1 mug/ml for H. influenzae, and 0.5 mug/ml for M. catarrhalis, suggesting that faropenem shows promise as a treatment option for respiratory infections caused by contemporary resistant phenotypes.

Topics: Anti-Bacterial Agents; Azithromycin; Bacterial Infections; beta-Lactams; Community-Acquired Infections; Drug Resistance, Multiple, Bacterial; Geography; Haemophilus influenzae; Health Surveys; Humans; Moraxella catarrhalis; Penicillin Resistance; Respiratory Tract Infections; Streptococcus pneumoniae; Trimethoprim, Sulfamethoxazole Drug Combination; United States

The pathogenesis, bacteriology, diagnosis, and antimicrobial treatment of acute bacterial rhinosinusitis (ABRS) is reviewed. Most cases of ABRS arise as complications of the rhinosinusitis of colds and other acute viral respiratory infections. Nose blowing during colds may be a risk factor for ABRS by propelling bacteria-laden nasal fluid into the sinus cavity. The bacterial causes of ABRS continue to be S pneumoniae. H influenzae, other streptococcal species, M catarrhalis, anaerobes, and S aureus. Clinical diagnosis of ABRS is based on obtaining a history of a cold or influenza-like illness that is no better or worse after >/=7 days. A 10-day course of treatment with an antimicrobial effective against resistant S pneumoniae and H influenzae is recommended. A clinical trial was reviewed in which cefdinir was effective in treating ABRS.

Topics: Acute Disease; Anti-Bacterial Agents; Bacterial Infections; Cefdinir; Cephalosporins; Humans; Rhinitis; Sinusitis

Antibacterial activities of gatifloxacin (GFLX) and other antibacterial drugs against various fresh clinical strains (800 isolates) isolated from specimens of patients in 2002 were compared. GFLX was more active than levofloxacin and ciprofloxacin against Gram-positive bacteria such as methicillin susceptible Staphylococcus aureus and Streptococcus pneumoniae. For these isolates, clarithromycin and azithromycin were less active (MIC90; > 16- > 64 micrograms/mL), GFLX was more active than cefdinir. For Escherichia coli, Klebsiella pneumoniae, Acinetobacter species, Haemophilus influenzae and Moraxella (Branhamella) catarrhalis, three quinolones including GFLX were potently active (MIC90; < or = 0.06-0.5 microgram/mL). Pseudomonas aeruginosa isolated from urinary tract infections were resistant to three quinolones including GFLX (MIC90; 32-64 micrograms/mL), however P. aeruginosa isolated from respiratory and otolaryngological infections were more susceptible (MIC90; 0.5-2 micrograms/mL). Quinolones were less active against Neisseria gonorrhoeae as compared with the cephem antibiotics tested, but GFLX was the most active against N. gonorrhoeae among the quinolones tested. In this study, we investigated activity of GFLX against fresh clinical strains isolated early in 2002, GFLX is widely and potently active against S. aureus, S. pneumoniae and various Gram-negative bacteria.

Topics: Anti-Bacterial Agents; Anti-Infective Agents; Bacterial Infections; Cefdinir; Cephalosporins; Ciprofloxacin; Dosage Forms; Drug Resistance, Bacterial; Fluoroquinolones; Gatifloxacin; Gram-Negative Bacteria; Gram-Positive Bacteria; Humans; Levofloxacin; Macrolides; Ofloxacin; Otorhinolaryngologic Diseases; Respiratory Tract Infections; Staphylococcus aureus; Streptococcus pneumoniae; Time Factors; Urinary Tract Infections

As the post-marketing surveillance of cefpodoxime proxetil (Banan), MICs of cefpodoxime (CPDX, an active form of Banan) against 1090 clinical isolates of 22 species from 15 medical institutions all over Japan from June 2000 to March 2001 were measured using the broth microdilution method approved by the Japanese Society of Chemotherapy and compared with those of oral cephem antibacterials, cefaclor, cefdinir, cefditoren, and cefcapene. In this study, remarkable change in the activity of CPDX was observed in Streptococcus pneumoniae and Haemophilus influenzae compared with the susceptibility in the studies before Banan was launched. This cause is considered to be the increase in the incidence of the following resistant strains: penicillin-intermediate S. pneumoniae (47.3%), penicillin-resistant S. pneumoniae (PRSP, 15.1%), and beta-lactamase-negative ampicillin-resistant (BLNAR) H. influenzae (24.0%), which were scarcely isolated in 1989 when Banan was launched. Other tested drugs also exhibited low activity against these resistant strains. However, CPDX showed comparatively good activity with MIC90 of 2 micrograms/mL against PRSP. Against methicillin-susceptible Staphylococcus spp., Streptococcus pyogenes, Streptococcus agalactiae, and Moraxella catarrhalis, CPDX also showed comparatively good activity with MIC90 of < or = 4 micrograms/mL, which was almost equal to that in the studies before its marketing. Against quinolones-resistant Neisseria gonorrhoeae, CPDX showed excellent activity with MIC90 of 0.5 microgram/mL. Against members of the family Enterobacteriaceae except for Citrobacter freundii, Enterobacter spp., Proteus vulgaris, and Morganella morganii, CPDX showed good activity. However, in Escherichia coli, Klebsiella spp. Proteus spp., and Providencia spp., there are some high-resistant strains to all tested drugs including CPDX. Against Peptostreptococcus spp., MIC90 of CPDX was 8 micrograms/mL and its MIC range was widely distributed from 0.03 to 32 micrograms/mL, which were similar to those in the studies before its marketing. In this study, CPDX showed the decrease in the activity against several species as did other drugs tested, but against most of species tested, CPDX maintained good activity. Furthermore, it is necessary to pay much attention to the trend of resistant strains.

Topics: Adolescent; Adult; Bacteria; Bacterial Infections; Cefaclor; Cefdinir; Cefpodoxime; Cefpodoxime Proxetil; Ceftizoxime; Cephalosporins; Child; Drug Resistance, Bacterial; Humans; Japan; Product Surveillance, Postmarketing; Time Factors

The synthesis and biological properties of 1beta-methylcarbapenems with 1-methyl-5-oxopyrrolidin-3-ylthio group at the C-2 position were studied. The sodium (1R,5S,6S)-6-[(R)-1-hydroxyethyl]-1-methyl-2-[(R)-1-methyl-5-oxopyrro lidin-3-ylthio]-1-carbapen-2-em-3-carboxylate and its (S)-isomer at the 2-position show potent and well-balanced antibacterial activity. The pharmacokinetic parameters of the pivaloyloxymethyl esters of these two carbapenems were compared in mice. The in vivo potency of these carbapenems was compared with that of cefdinir. Good in vivo efficacy of these ester prodrugs reflected the high and prolonged blood levels in parent drugs achieved after oral administration to mice.

Topics: Administration, Oral; Animals; Anti-Bacterial Agents; Anti-Infective Agents; Area Under Curve; Bacterial Infections; Carbapenems; Cefdinir; Cephalosporins; Chromatography, High Pressure Liquid; Dose-Response Relationship, Drug; Half-Life; Male; Mice; Microbial Sensitivity Tests; Molecular Structure; Prodrugs; Stereoisomerism; Structure-Activity Relationship

Topics: Bacteria; Bacterial Infections; Cefdinir; Cephalosporins; Drug Resistance, Microbial; Humans

Cefdinir (CFDN, FK482) was evaluated in children with infections. CFDN was given at a daily dose of 6.4-19.8 mg/kg in 2 or 3 divided portions. CFDN was effective in 94% of 32 cases with respiratory tract, middle ear, urinary tract or skin structure infections. Side effects were loose stool and diarrhea (12.5%). In a pharmacokinetic study, 6.0 mg/kg of CFDN was given to each of the subjects before meal. Cmax was 0.81 +/- 0.38 microgram/ml, T 1/2 was 2.31 +/- 0.77 hours. Antibacterial activity against Staphylococcus aureus was the most excellent of oral cephem antibiotics tested. The data suggest that CFDN 10% granular preparation is safe and effective when used in children with infections caused by susceptible bacteria.

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

Ten% cefdinir (CFDN, FK482) granular preparation, a new oral cephalosporin preparation intended for children, was given to children with various infections. The results obtained are summarized as follows. 1. Ten% CFDN granules were administered to a total of 21 children with upper or lower respiratory tract infections, urinary tract infections or infectious impetigo at daily doses of 6.4-18 mg/kg divided into 3 portions. Clinical efficacies were "excellent" in 13 patients, "good" in 7 patients and "unknown" in 1 patient (viral infection), hence an efficacy of 100% was obtained. 2. Bacteria identified in various disease cases included 19 strains of 7 species, and the eradication rate was 100%. 3. No side effects were noted in any of the children. Laboratory test results showed an abnormality in 1 case with eosinophilia. These results suggest that 10% CFDN granules as well as 5% CFDN granules may be a very useful and safe drug for the treatment of pediatric infections.

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

Clinical evaluations of cefdinir (CFDN) 10% granule were carried out. The obtained results are summarized as follows. 1. Clinical responses to CFDN of 23 patients with pediatric infections were excellent in 11 and good in 8. The overall efficacy rate was 82.6%. 2. Bacteriologically, the eradication rate for 23 strains of bacteria identified to be pathogens was evaluated and was 82.6%. 3. Side effects observed were diarrhea in 2 of 25 patients. The incidence was 8.0%. Abnormal laboratory test results observed included 2 cases with elevation of GOT and 1 case with elevation of GPT. These results suggest that CFDN 10% granule, as well as 5% granule, may be a very useful and safe drug for the treatment of pediatric infections.

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

Cefdinir (CFDN) was administered to pediatric patients with acute infectious disease. A summary of the results obtained is as follows. 1. Pharmacokinetic parameters were determined in a girl. In comparison to reported data in adults, Tmax was shorter, Cmax was slightly lower, and the plasma half life of CFDN was somewhat longer. 2. Clinical efficacy was studied in 11 children with acute tonsillitis (6 patients), scarlet fever (1 patient), acute pharyngitis (1 patient), acute pneumonia (1 patient), acute otitis media (1 patient) and acute cervical lymphadenitis (1 patient). Responses to the treatment were excellent in 7 (63.6%) and good in 2 (18.2%). 3. No adverse reactions were noted in this study.

Topics: Acute Disease; Administration, Oral; Age Factors; Bacterial Infections; Cefdinir; Cephalosporins; Child; Child, Preschool; Dosage Forms; Drug Evaluation; Female; Humans; Male

Clinical evaluation in pediatrics on cefdinir (CFDN, FK482) (5% fine granules), a new oral cephem, was performed. 1. CFDN was administered to 112 pediatric patients with ages between 1 month to 13 years with various infections. Dose levels used were 3.0-8.9 mg/kg (mean 5.1 mg/kg) t.i.d. for 3-14 days (mean 6.7 days). The studied patients included 2 patients with scarlet fever, 6 with acute pharyngitis, 6 with acute rhinopharyngitis, 52 with acute purulent tonsillitis, 8 with acute bronchitis, 24 with acute pneumonia, 7 with acute urinary tract infections, 1 with acute vaginitis, and 6 with impetigo. Total doses ranged from 0.6 to 4.05 g. One hundred eleven of the 112 patients were evaluated for clinical efficacy and all the patients were evaluated for safety. 2. Clinical effects were excellent in 51 cases, good in 57, and fair in 3 with an extremely high efficacy rate of 97.3%. Efficacy rates were 100% in scarlet fever, acute pharyngitis, acute purulent tonsillitis, acute bronchitis, acute vaginitis and impetigo, and 83.3%, 95.7%, 85.7% in acute rhinopharyngitis, acute pneumonia, and acute urinary tract infections, respectively. Good clinical effects were observed regardless of diseases. 3. Causative organisms were identified in 79 cases, of which 71 were found to be monobacterial infections and 8 were found to be multi-bacterial infections. In mono-bacterial infections, clinical efficacies were 100% for those caused by Staphylococcus aureus/Streptococcus pyogenes/Streptococcus pneumoniae/beta-Streptococcus except those in A and B groups with an overall efficacy of 100% against Gram-positive cocci (GPC) and they were 89.5%, 100%, 100% for those caused by Haemophilus influenzae, Haemophilus parainfluenzae, and Escherichia coli, respectively, with an overall efficacy of 90.3% in Gram-negative rods (GNR). In multi-bacterial infections also, a clinical efficacy of 100% was obtained. 4. Bacteriological effects were studied for 89 strains in the 79 cases. The eradication rate for a few strains of S. pneumoniae was low, 25%, but it was 100% for S. aureus, with the same results for S. pyogenes, and beta-Streptococcus. The eradication rate on GPC was high 94.1%. Among GNR, 66.7% of E. coli, 50.0% of H. influenzae, and 71.4% of H. parainfluenzae was eradicated. The overall eradication rate for GNR was 55.3%, lower than that for GPC. Microbial substitutions were observed in 13 cases, with Haemophilus sp. replacing other bacteria. 5. Diarrhea and soft stools were not

Topics: Acute Disease; Administration, Oral; Age Factors; Bacteria; Bacterial Infections; Cefdinir; Cephalosporins; Child; Child, Preschool; Dosage Forms; Drug Evaluation; Drug Resistance, Microbial; Female; Humans; Infant; Male

Pharmacokinetic, bacteriological, and clinical studies on cefdinir (CFDN, FK482) (10% fine granules), a new oral cephem, were performed in pediatrics. 1. Bioequivalencies of plasma concentrations and urinary excretions of CFDN 5% and 10% fine granules were investigated on 3 pediatric patients with ages between 5 to 13 years administered with a drug in fasting state at a dose level of 3 mg/kg using a cross over method. Average plasma concentrations in a group of patients administered with 5% fine granules peaked at 3 hours after administration with a level of 1.05 +/- 0.29 micrograms/ml (mean +/- S.E.) and decreased to 0.12 +/- 0.05 micrograms/ml at 8 hours with a half-life of 1.48 +/- 0.09 hours. In the group administered with 10% fine granules, average plasma concentrations peaked at 2 hours after administration with a level of 1.32 +/- 0.12 micrograms/ml, and decreased to 0.20 +/- 0.11 microgram/ml at 8 hours with a half-life of 1.68 +/- 0.28 hours. The first 8-hour urinary recovery rates of CFDN in the 5% and 10% fine granules groups averaged 19.64 +/- 5.69% and 23.37 +/- 2.36%, respectively. Both average and individual plasma concentrations and urinary recovery rates in the patients of the 10% fine granules group were somewhat higher than those of the 5% fine granules group, but no significant differences were observed between the 2 groups including areas under concentrations. 2. CFDN 10% fine granule preparation was administered to 33 pediatric patients with ages between 1 to 13 years with various infections, and its clinical effects, bacteriological effects and safety were assessed. In 31 of the 33 patients (2 patients were excluded since they were with non-bacterial infections) clinical effects were excellent in all of 9 patients with scarlet fever (3), acute pharyngitis (3) or impetigo (3), excellent in 12 and good in 3 of 15 patients with acute purulent tonsillitis, and excellent in 4 and good in 3 of 7 patients with acute pneumonia. The overall efficacy rate was 100%. Bacteriological effects against causative organisms were evaluated. All the identified Staphylococcus aureus (4 strains) and Streptococcus agalactiae (1) were eradicated. Of 10 strains of Streptococcus pyogenes, 9 strains were eradicated and the other one was reduced. Of 7 strains of Haemophilus influenzae 4 were eradicated, 1 persisted and the fate of the remaining 2 were unknown. The overall eradication rate was 90.0%. Microbial substitutions were observed in 5 patients. The new,

Topics: Administration, Oral; Adolescent; Age Factors; Bacteria; Bacterial Infections; Biological Availability; Cefdinir; Cephalosporins; Child; Child, Preschool; Dosage Forms; Drug Evaluation; Female; Half-Life; Humans; Infant; Male

Clinical studies on 10% fine granules of cefdinir (CFDN), a new cephem antibiotic, were carried out in the field of pediatrics. The results obtained are summarized as follows. 1. Half-lives of CFDN in plasma in 3 children when administered on an empty stomach were 1.77 hours (3 mg/kg per os) and 1.47 hours (6 mg/kg per os), respectively. Eight hour urinary excretion rates of CFDN were 21.5% (3 mg/kg per os) and 16.4% (6 mg/kg per os), respectively. 2. CFDN was administered to 11 children with various bacterial infections: 1 patient with scarlet fever, 1 with pharyngotonsillitis, 3 with acute bronchitis, 3 with pneumonia and 3 with urinary tract infections. The overall clinical efficacy rate was 90.9%. 3. Loose stool was noted in 1 patient. No abnormal laboratory test values were encountered.

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

We have carried out laboratory and clinical studies on cefdinir (CFDN) 5% and 10% fine granule preparations. The results are summarized as follows. CFDN 5% fine granule preparation was given via oral route to each of 2 children in the fasting state at a single dose of 3 mg/kg. After administration, the mean peak plasma level of CFDN was 0.76 micrograms/ml at 4 hours and the mean half-life was 1.77 hours. The mean urinary excretion rate of CFDN was 31.5% in the first 12 hours after oral administration. CFDN 10% fine granule preparation and CFDN 100 mg capsule were given via oral route 3 children and to another child in the fasting state at single doses of 3 mg/kg and 2.63 mg/kg, respectively. After administration of 10% granules the mean peak plasma level of CFDN was 0.73 micrograms/ml at 2 hours and the mean half-life was 1.62 hours. The peak serum level obtained after administration of CFDN 100 mg capsule was 0.91 micrograms/ml at 2 hours and the half-life was 1.08 hours. The mean urinary excretion rate obtained with CFDN 10% fine granules was 26.2% in the first 8 hours after oral administration and the urinary excretion rate obtained with CFDN 100 mg capsule was 19.7% in the first 12 hours after oral administration. Treatment with CFDN 5% fine granules was made for a total of 48 cases of pediatric bacterial infections including 21 cases of tonsillitis, 12 cases of scarlet fever, 3 cases of pharyngitis, 5 cases of impetigo, 1 case of subcutaneous abscess, 1 case of furuncle, 5 cases of UTI. Results obtained were excellent in 30 cases, good in 18 cases. Treatment with CFDN 10% fine granules was made for a total of 16 cases of pediatric bacterial infections including 6 cases of tonsillitis, 3 cases of pneumonia, 4 cases of scarlet fever, 2 cases of impetigo, 1 case of UTI. Results obtained were excellent in 8 cases, good in 7 cases, poor in 1 case. No significant side effects due to the drugs were observed except 2 cases (1 case with 5% preparation and another with 10%) with eosinophilia, 3 cases (all with 5%) with diarrhea and 1 case each of elevated GOT & GPT (with 5%) and elevated GOT, GPT & Al-P (with 10%).

Topics: Administration, Oral; Adolescent; Age Factors; Bacteria; Bacterial Infections; Cefdinir; Cephalosporins; Child; Child, Preschool; Dosage Forms; Drug Evaluation; Humans; Infant

The Pharmacokinetics and clinical effectiveness of cefdinir (CFDN, FK482) were examined in pediatric patients. The results are summarized as follows. 1. Plasma concentrations and urinary excretions of CFDN after administration of 5% fine granules were investigated on 4 children at a dose level of 6 mg/kg. Average plasma concentrations peaked at 4 hours after administration at 0.99 micrograms/ml with a half-life of 2.12 hours. The first 24-hour urinary recovery rates of CFDN in 3 children averaged 22.0%. 2. CFDN was given to 24 children (11 with pharyngitis, 3 with tonsillitis, 8 with scarlet fever, 1 with urinary tract infection and 1 with enteritis due to Salmonella); 15 were treated with 5% fine granules and 9 with 10% fine granules at daily doses of about 10 mg/kg in 2 to 3 divided portions. Clinical effects were excellent in 16, good in 7 and not evaluable in 1, with an overall efficacy rate of 100%. 3. Identified causative organisms were 12 strains of Streptococcus pyogenes, 4 of Haemophilus influenzae, 5 of Haemophilus parainfluenzae, 1 of Escherichia coli, and 1 of Salmonella. Bacteriological effects were rated as "eradicated" for 19 strains, "unchanged" for 4 with an eradication rate of 82.6%. 4. No side effects were observed. As for abnormal laboratory test results, a transient decrease of white blood cells was observed in 1 patient. 5. The CFDN fine granule preparations were preferably accepted by the children. 6. The fine granular preparations of CFDN, a new oral antibiotic, were useful for the treatment of bacterial infections in pediatrics.

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

Cefdinir (CFDN) was evaluated for its efficacy and safety. The following results were obtained. 1. Pharmacokinetic study: CFDN was evaluated pharmacokinetically in 4 male children aged 9 to 13. CFDN was given orally to 3 children at a dose of 3 mg/kg. Peak plasma levels of 0.71 microgram/ml, 0.78 microgram/ml and 0.45 microgram/ml were attained in the 3 children, respectively, at 4 hours after dosing. Half-lives of CFDN in serum were 1.78 hours, 1.48 hours and 2.23 hours, respectively. The 12-hour urinary recovery rates of CFDN were 17.4%, 28.1% and 6.2%. When CFDN was given orally to the remaining child at a dose of 6 mg/kg, the peak plasma level was attained at 4 hours after dosing with a level of 1.16 micrograms/ml. T 1/2 was 1.78 hours. The 12-hour urinary recovery rate of CFDN was 15.0%. 2. Clinical study: CFDN 5 percent fine granules were given to 26 patients with infections; 2 with pneumonia, 4 with acute bronchitis, 1 with chronic bronchitis, 12 with pharyngitis, 4 with scarlet fever, 1 with otitis media and 2 with skin and soft tissue infections. Therapeutic responses were "excellent" in 15, "good" in 8, "fair" in 1 and "poor" in 2, with an efficacy rate of 88.5%. 3. Adverse reactions: As for adverse reactions, diarrhea was noted in 1 patient. It was concluded that CFDN is a useful drug for the treatment of the bacterial infections in pediatrics.

Topics: Administration, Oral; Adolescent; Age Factors; Bacterial Infections; Bronchitis; Cefdinir; Cephalosporins; Child; Drug Evaluation; Humans; Male; Pharyngitis

A new oral cephem, cefdinir (CFDN) was evaluated for its efficacy, safety and pharmacokinetics in 13 children. The results are summarized as follows. Plasma concentration peaked at 3-4 hours after administration of 3 mg/kg of CFDN with Cmax ranging from 0.57-0.89 microgram/ml except 1 case in which the absorption of the drug was poor. Recovery rates in urine averaged at 13.4%, with a large individual variation. Ten children with 12 bacterial infections were treated with 9 mg/kg/day of CFDN fine granule. Clinical responses were good in 10 patients and fair in 1 patient, with an efficacy rate of 90.9%. No clinical adverse reactions nor abnormal laboratory findings were encountered.

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

Cefdinir (CFDN), a newly developed oral cephalosporin in 5% fine granular form, was administered to 10 boys at 1 hour before meal (in the fasting state) and concentrations of the drug in plasma and urine and its urinary recovery rates were determined. The subjects were divided into 2 groups of 5 boys each; one group received 3 mg/kg of CFDN, and the other, 6 mg/kg. To 6 of the 10 children the drug was administered in the two different dose levels using the cross-over method. To study clinical and bacteriological effects of this drug, a mean dose of 4.6 mg/kg t.i.d. was administered for 8 days on the average to 40 children with various infections; pharyngitis (4 cases), tonsillitis (2), acute bronchitis (2), pneumonia (8), scarlet fever (6), acute purulent otitis media (1), urinary tract infection (12), impetigo (2), phlegmon (1), lymphadenitis (1) and subcutaneous abscess (1). MICs were determined for 6 drugs including CFDN, cefaclor, cefixime (CFIX), methicillin, cloxacillin (MCIPC), amoxicillin (AMPC) against 13 strains of 6 species freshly isolated from children receiving CFDN. An inoculum size of 10(6) cfu/ml was used in the MIC-determinations. Adverse reactions and abnormal laboratory findings attributable to this drug were also examined in these patients. The results obtained are summarized as follows. 1. Mean plasma peak levels of CFDN were observed at 3 hours after administration in both the 3 mg/kg and 6 mg/kg groups with mean peak values of 0.68 and 1.35 micrograms/ml, respectively. Mean half-lives were 2.06 hours in the 3 mg/kg group and 1.61 hours in the 6 mg/kg group, and mean AUCs were 3.5 in the former and 6.5 micrograms.hr/ml in the latter. Thus, dose-response between the 2 doses was observed in plasma levels and AUCs. 2. To 3 patients, CFDN was given in the two different doses using the cross-over method. Mean plasma peak levels of CFDN were 0.71 and 1.31 micrograms/ml in the doses of 3 mg/kg and 6 mg/kg, respectively. Half-lives were 1.39-2.90 hours in the 3 mg/kg group and 1.21-1.48 hours in the 6 mg/kg group, with AUCs of 3.4-3.7 and 4.1-7.5 micrograms.hr/ml, respectively.(ABSTRACT TRUNCATED AT 400 WORDS)

Topics: Administration, Oral; Age Factors; Bacteria; Bacterial Infections; Cefdinir; Cephalosporins; Child; Child, Preschool; Dosage Forms; Drug Evaluation; Drug Resistance, Microbial; Female; Humans; Infant; Male; Pharyngitis; Pneumonia; Urinary Tract Infections

Pharmacokinetic, bacteriological and clinical studies on cefdinir (CFDN), a newly developed oral cephalosporin, were performed on children with infections. The pharmacokinetics was examined in 3 patients. The peak plasma concentrations were 1.97 micrograms/ml, 0.84 microgram/ml and 1.67 micrograms/ml in the 3 patients. The 0 to 6 or 8-hour urinary excretion rates were 22.2%, 18.1%, and 32.7%, respectively. These results were similar to those in adult patients. Clinical response to CFDN was evaluated in 21 patients, 4 patients with pharyngitis (an efficacy rate of 100%), 7 with tonsillitis (85.7%), 1 with bronchitis (excellent), 1 with pneumonia (fair), 6 with scarlet fever (100%), 1 with staphylococcal scaled skin syndrome (good) and 1 with urinary tract infection (good). Thus, an overall efficacy rate of 90.5% was achieved. With regard to microbiological effect on pathogens, 14 of the 15 strains identified as pathogens were eradicated, with an eradication rate of 93.3%. The safety was evaluated in a total of 23 cases. Diarrhea, elevated eosinophil count and elevated S-GPT were observed in one patient each. The side effect and abnormalities in laboratory tests were not serious, however. It was concluded that CFDN, with its excellent antibacterial effect, was an efficacious and safe drug for the treatment of pediatric infections.

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

Pharmacokinetic and clinical studies on cefdinir (CFDN) capsule and fine granules in children were performed and the following results were obtained. 1. Plasma level and urinary excretion of CFDN were determined in 10 children with ages 7 to 13 years given single doses of 2.3 to 7.5 mg/kg. Six of the 10 children received the drug orally before meal and the other 4 after meal. Plasma concentration peaked at 2 to 4 hours in the children administered the drug before meal, and at 3 to 4 hours in those given the drug after meal. The 8-hour urinary recovery rate was 18.8%. 2. Clinical efficacies were evaluated in 23 children with bacterial infections. The children were given the drug orally at dose levels of 3.3 to 6.3 mg/kg 3 times a day. Clinical effects of CFDN were excellent in 7 and good in others, hence the overall clinical efficacy rate was 100%. 3. Bacteriologically, 18 of the 19 strains of causative organisms identified were eradicated, with an overall bacteriological eradication rate of 94.7%. 4. As for side effects, loose stool was observed in 1 case, but it disappeared in a few days. In laboratory tests a slight elevation of GOT and GPT were observed in 1 case, but no additional treatment was needed. 5. CFDN is a useful oral antibiotic for the treatment of bacterial infections in pediatric field.

Topics: Administration, Oral; Adolescent; Age Factors; Bacterial Infections; Cefdinir; Cephalosporins; Child; Drug Evaluation; Female; Humans; Male

Cefdinir (CFDN, FK482) was evaluated for its safety, efficacy and pharmacokinetics in 28 children. CFDN was effective in 100% of 22 evaluable cases with respiratory, middle ear, urinary or soft tissue infections. From the clinical response, adverse effects and the pharmacokinetic results, daily dose of 9-18 mg/kg, administered in 3 divided portions is suggested. Increase of dose will be associated with increase of gastrointestinal side effects. The data suggest that CFDN is safe and effective when used in children with infections caused by susceptible bacteria including Staphylococcus aureus.

Topics: Administration, Oral; Adolescent; Age Factors; Bacterial Infections; Cefdinir; Cephalosporins; Child; Child, Preschool; Drug Evaluation; Female; Humans; Infant; Male; Staphylococcus aureus

Cefdinir (CFDN), a new oral cephalosporin, was administered to 10 patients with various infections and the following results were obtained. 1. Clinical responses in 10 patients (1 patient with rhinitis, 2 with sinusitis, 1 with pharyngitis, 1 with tonsillitis, 4 with scarlet fever and 1 with abscess) were excellent in 6 and good in 4 with an efficacy rate of 100%. 2. Eleven species of bacteria were isolated (3 of Staphylococcus aureus, 6 of Streptococcus pyogenes and 2 of Haemophilus influenzae) and all of them were eradicated by the treatment with CFDN. 3. No side effects or abnormal laboratory test values were noted. None of the patients refused to take the drug.

Topics: Administration, Oral; Bacterial Infections; Cefdinir; Cephalosporins; Child; Child, Preschool; Drug Resistance, Microbial; Female; Humans; Infant; Male; Staphylococcus aureus; Streptococcus pyogenes

Clinical trials of cefdinir (CFDN) in pediatric infections were carried out. Results are summarized as follows. 1. Mean half-lives of CFDN in serum in children when administered on an empty stomach were 1.24 hours (3 mg/kg per os) and 1.85 hours (6 mg/kg per os). 2. Mean 8 hour urinary excretion rates of CFDN were 19.0% (3 mg/kg/per os) and 10.5% (6 mg/kg per os). 3. CFDN was administered to 28 children with various infections: 12 patients with tonsillitis, 8 with bronchitis, 2 with pneumonia, 4 with urinary tract infections, 1 staphylococcal scalded skin syndrome and 1 with impetigo. The overall efficacy rate was 89.3%. 4. Diarrhea was noted in 1 patient. Abnormal laboratory test values encountered were eosinophilia in 2 patients, thrombocytosis in 1.

Topics: Adolescent; Age Factors; Bacteria; Bacterial Infections; Cefdinir; Cephalosporins; Child; Drug Evaluation; Drug Resistance, Microbial; Female; Humans; Male

The therapeutic activities of orally administered FK482 were compared with those of reference antibiotics against systemic and local infections with a variety of bacteria in mice and rabbits. In systemic infections in mice, oral FK482 was almost as effective as oral cefaclor (CCL) and more effective than oral cephalexin (CEX) against Staphylococcus aureus, Escherichia coli, Klebsiella pneumoniae and Proteus mirabilis infections. However, FK482 afforded superior protective activity when given subcutaneously against E. coli infection in mice, and this activity was more potent than that of subcutaneously given CCL. In comparison with CCL, the reason that the in vivo activity of orally given FK482 against mouse systemic infections was weaker than had been anticipated from its potent in vitro activity was due to its poor oral absorption in mice. In local infections in rabbits, a species in which FK482 was better absorbed than in mice, FK482 was more effective than CCL, CEX or amoxicillin (AMPC). Against pneumonia induced by S. aureus or Streptococcus pyogenes, FK482 was as effective as AMPC and more effective than CCL in reducing the number of viable bacteria in the lungs of infected rabbits. In the oral treatment of experimental ascending pyelonephritis in rabbits, FK482 was superior to CCL and AMPC against methicillin-resistant S. aureus infection, as effective as AMPC and more effective than CCL against Enterococcus faecalis infection, and as effective as cefixime (CFIX) and more effective than CCL and AMPC against E. coli infection in reducing the number of viable bacteria in the kidneys and urine.

Topics: Administration, Oral; Animals; Bacterial Infections; Cefaclor; Cefdinir; Cephalosporins; Male; Mice; Mice, Inbred ICR; Pneumonia; Pyelonephritis; Rabbits