s-1108 and Respiratory-Tract-Infections

Excessive use of broad spectrum antibiotics is related to the spread of drug resistant bacterial strains in the community.. The effects of immediate testing for C reactive protein (CRP) and white blood cell count (WBC) on physicians' choices of antibiotic was investigated in patients with acute infection. Acutely febrile new outpatients were randomised into two groups: group 1 (147 patients) underwent CRP and WBC testing before initial consultation (advance testing). Prescriptions were compared with those in group 2 (no advance testing; 154 patients).. In non-pneumonic acute respiratory tract infections, 61 (58%) and 122 (91%) of group 1 and 2 patients were prescribed antibiotics, respectively. Cefcapene pivoxil (third generation cephalosporin) and amoxicillin were the most frequently chosen drugs for group 1 and 2, respectively. Total prescriptions of newer, extended spectrum antibiotics (cefcapene pivoxil and clarithromycin (advanced macrolide)) were reduced by 25% in group 1, although they increased in rate (41 (67%) v 55 (45%) prescriptions) because of the decreased prescription of amoxicillin. In group 1, cefcapene pivoxil was preferentially selected when WBC values were greater than 9 x 10(9)/litre. Prescription shifted to macrolides (mainly clarithromycin) in patients without leucocytosis. Patient treatment outcome did not significantly differ between the two groups.. The availability of CRP and WBC data during initial consultation greatly reduced prescription of amoxicillin, but had a lesser effect on newer, potent, broad spectrum antibiotics.

Topics: Acute Disease; Adult; Amoxicillin; Anti-Bacterial Agents; Bacterial Infections; Biomarkers; C-Reactive Protein; Cephalosporins; Clarithromycin; Fever; Humans; Japan; Leukocyte Count; Middle Aged; Outpatient Clinics, Hospital; Practice Patterns, Physicians'; Respiratory Tract Infections; Treatment Outcome

We studied the pharmacokinetics of a new cephem antibiotic, S-1108, in patients with impaired kidney functions. Serum and urinary levels of S-1006 were determined after oral administration of S-1108 at 150 mg to 9 patients with renal dysfunction. In patients with severe renal impairment, high serum levels were maintained over long periods of time. Urinary excretion rates of S-1006 were lower as degrees of kidney failure were severer. S-1108 was administered to treat 27 patients with respiratory tract infections, and its clinical efficacy and safety were evaluated. The clinical efficacies were good in 26 patients, but poor in 1, yielding an efficacy rate of 96.3%. As to adverse reactions; diarrhea was observed in one case. Laboratory tests revealed elevated GOT and GPT in 1, and elevated gamma-GTP in another. These abnormalities, however, were slight and no severe side effects were caused by the drug.

Topics: Administration, Oral; Adult; Aged; Aged, 80 and over; Cephalosporins; Female; Half-Life; Humans; Kidney Diseases; Male; Middle Aged; Prodrugs; Respiratory Tract Infections

We studied the clinical use of S-1108 granules in the pediatric field. The results are summarized as follows. 1. S-1108 was administered orally at doses ranging 6.85 and 17.6 mg/kg/day t.i.d. to 9 patients, including 5 cases of pharyngitis and 1 case each of lacunar tonsillitis, bronchitis, pneumonia and urinary tract infection. Clinical efficacies were excellent in 4 cases and good in 5 cases, hence an efficacy rate of 100% was obtained. 2. Haemophilus influenzae, Haemophilus parainfluenzae (2 strains each) and Streptococcus pyogenes, Staphylococcus aureus, Escherichia coli and Enterococcus faecalis (1 strain each) were identified in these cases. Seven of the 8 strains were eliminated upon treatment and the other strain was decreased, hence an eradication rate of 87.5% was obtained. 3. Side effects observed were 1 case each of soft stools and diarrhea. As an abnormal laboratory test result, an increase in GPT level was observed. 4. No refusal of the drug occurred. 5. From the above results, we consider that this drug would be a useful new oral antibiotic for the pediatric field.

Topics: Administration, Oral; Cephalosporins; Child; Child, Preschool; Diarrhea; Female; Humans; Infant; Male; Prodrugs; Respiratory Tract Infections; Urinary Tract Infections

We have evaluated S-1108 fine granules for therapeutic effectiveness in children. The results are summarized as follows. 1. A clinical study was performed with 16 children with infections, including 8 with acute tonsillitis, 3 with acute pharyngitis, 2 with scarlet fever, 1 each with acute bronchitis, pertussis and urinary tract infection. Doses ranging from 8.8 to 10.6 mg/kg body weights were given in 3 divided portions. Durations of treatment ranged from 2 to 15 days. The therapeutic responses were considered "excellent" in 1 and "good" in 13, with an efficacy rate of 87.5%, and the bacteriological eradication rate was 91%. 2. No adverse reactions were observed. In laboratory tests, eosinophilia was observed in one patient. It was concluded the S-1108 was promising drug for the treatment of bacterial infections in children.

Topics: Administration, Oral; Cephalosporins; Child; Child, Preschool; Female; Humans; Male; Prodrugs; Respiratory Tract Infections; Urinary Tract Infections

Clinical studies of S-1108, a new oral cephem, in pediatric patients were conducted and results are summarized below. 1) Clinical effects of S-1108 against 18 cases of bacterial infections were excellent in 5 cases, good in 10 cases, fair in 1 case and poor in 2 cases, thus the clinical efficacy rates was 83.3%. 2) Bacteriological effects were evaluated in 16 strains. The elimination rate was 100%. 3) No adverse effects nor abnormal laboratory test results were observed in any of the cases.

Topics: Administration, Oral; Adolescent; Cephalosporins; Child; Child, Preschool; Female; Humans; Infant; Male; Prodrugs; Respiratory Tract Infections; Urinary Tract Infections

To evaluate the efficacy, the safety and the usefulness of a novel and esterified cephem antibiotic for oral use, S-1108, in pediatric infections, a clinical trial was performed. The study subjects were 15 patients including 9 with acute pharyngitis, 1 with acute tonsillitis, 2 with acute bronchitis, 1 with chronic pyelonephritis, 1 with acute abscess of the skin and 1 with impetigo contagiosa. S-1108 was administered orally at a dose of 3.7 mg/kg to 12.5 mg/kg t.i.d. for 4 to 9 days. Clinical effects were excellent in 7 cases, good in 6, fair in 1 and poor in 1. The Overall efficacy rate was 86.7%. Bacteriologically, causative organisms were all eradicated in evaluable 4 cases. As to side effects, diarrhea was observed in 2 cases. No abnormal laboratory test values were obtained.

Topics: Adolescent; Bacteria; Bacterial Infections; Cephalosporins; Child; Child, Preschool; Diarrhea; Female; Humans; Infant; Male; Respiratory Tract Infections

A post-marketing clinical study was previously conducted in pediatric patients with respiratory infection to evaluate the pharmacokinetics, efficacy and safety of cefcapene pivoxil (CFPN-PI) fine granules for children. Based on the results from this study, we evaluated PK/PD breakpoints and clinical/bacteriological effects of CFPN-PI at free drug concentrations in pediatric patients with respiratory infection to determine an effective and safe dosage regimen of CFPN-PI. The following results were obtained from 61 pediatric patients evaluated in our research. 1) The response rate of pediatric respiratory infection to CFPN-PI was 100% for laryngopharyngitis, 84.6% for acute bronchitis, 100% for tonsillitis, 100% for pneumonia and 95.8% for all. 2) The bacteriological response (eradication rate of Haemophilus influenzae, Streptococcus pyogenes, Moraxella catarrhalis, Streptococcus pneumoniae, etc.) of pediatric respiratory infection to CFPN-PI was 87.5% for laryngopharyngitis, 66.7% for acute bronchitis, 75.0% for tonsillitis, 63.6% for pneumonia and 73.8% for all. 3) The blood concentration simulation demonstrated that the PK/PD breakpoint exceeding the time above MIC (TAM) of 40% after administration of CFPN-PI 3 mg/kg three times daily was 0.27 microg/mL. 4) The pediatric patients with respiratory infection were stratified by the TAM (%) of CFPN-PI into 40% to 100% (TAM > or = 40% group) and 0% to 40% (TAM < 40% group) to compare the clinical and bacteriological effects of CFPN-PI. The clinical and bacteriological response rates, respectively, were 97.4% and 77.8% in the TAM > or = 40% group, and 88.9% and 62.5% in the TAM < 40% group. There was no difference in the clinical effect between the two TAM-stratified groups. On the other hand, the bacteriological effect, i.e., eradication rate, tended to be higher in the TAM > or = 40% group than in the TAM < 40% group, although the between-group difference was not statistically significant.

Topics: Bacteria; Cephalosporins; Child; Humans; Product Surveillance, Postmarketing; Respiratory Tract Infections

Topics: Ampicillin Resistance; Anti-Bacterial Agents; beta-Lactams; Cephalosporins; Child; Child, Preschool; Community-Acquired Infections; Haemophilus Infections; Haemophilus influenzae; Humans; Infant; Lactams; Otitis Media; Penicillin Resistance; Pneumococcal Infections; Respiratory Tract Infections; Retrospective Studies; Streptococcus pneumoniae; Treatment Outcome

In order to evaluate antimicrobial activity of cefcapene (CFPN), minimum inhibitory concentrations (MICs) of CFPN and reference drugs were determined against clinical isolates from respiratory tract infection of out patients that were obtained in our laboratory from January to June of 1997. The results are summarized as follows; 1. The MIC90 of CFPN against penicillin (PC)-susceptible Streptococcus pneumoniae (PSSP) was equal to those of benzylpenicillin (PCG), ampicillin (ABPC) and cefditoren (CDTR), and was lower than those of cefaclor (CCL), cefdinir (CFDN) and erythromycin (EM). 2. The MIC90 of CFPN against PC-intermediate S. pneumoniae (PISP)/PC-resistant S. pneumoniae (PRSP) was equal to that of CDTR, and was lower than those of PCG, ABPC, CCL, CFDN and EM. CFPN showing strong antimicrobial activities against PISP. 3. CFPN showed strong antimicrobial activities against beta-lactamase producing and non-producing Haemophilus influenzae. The MIC90 of CFPN was stronger than those of ABPC, CCL, CFDN and EM, and was approximately equal to that of CDTR. CFPN also showed strong antimicrobial activities against strains which did not produce any beta-lactamase and were resistant to CCL with MIC of > or = 25 micrograms/ml. 4. Antimicrobial activities of CFPN against Moraxella subgenus Branhamella catarrhalis was stronger than that of ABPC and CCL, though the MIC90 of CFPN was rather high, 3.13 micrograms/ml. 5. CFPN showed strong antimicrobial activities against PISP and beta-lactamase producing H. influenzae, and also against the CCL-resistant H. influenzae indicative mutations of penicillin-binding proteins (PBPs). From those results, cefcapen-pivoxil was found to be clinically effective against community acquired respiratory tract infection.

Topics: Cephalosporins; Community-Acquired Infections; Drug Resistance, Microbial; Haemophilus influenzae; Humans; Moraxella catarrhalis; Outpatients; Prodrugs; Respiratory Tract Infections; Streptococcus pneumoniae

We performed laboratory and clinical evaluation of S-1108 granules, a new oral cephalosporin antibiotic, in the pediatric field. 1. Pharmacokinetics of S-1108 was examined with 6 patients, at a dose of 4 mg/kg that was orally ingested 30 minutes after meal. Mean plasma concentrations at 30 minutes, 1, 2, 4, 6 and 8 hours after dose were 0.35, 0.63, 0.86, 0.75, 0.37 and 0.09 microgram/ml, respectively, with a half life of 1.14 hours. The urinary recovery rate in the first 8 hours was 25.5%. 2. The clinical efficacy of S-1108 was evaluated in 31 patients with various infectious diseases. S-1108 was administered at doses ranging 2 to 4.2 mg/kg/dosage, 3 times a day for 1/3 to 10 days. Clinical effects were excellent in 19, good in 12, with an efficacy rate of 100%. Bacteriologically, all causative organisms except two of Staphylococcus aureus and Haemophilus influenzae were eradicated, with an eradication rate of 80%. As an adverse reaction, mild diarrhea was noted in 2 patients. Slight elevations of GOT and/or GPT were noted in 2 patients. Only 1 child had difficulty ingesting the antibiotic preparation. From the above results, we have concluded that S-1108 is a highly effective and safe for patients with various infectious diseases in the pediatric fields.

Topics: Absorption; Alanine Transaminase; Aspartate Aminotransferases; Bacteria; Bacterial Infections; Cephalosporins; Child; Child, Preschool; Diarrhea; Drug Evaluation; Female; Humans; Infant; Male; Respiratory Tract Infections; Urinary Tract Infections

We administered S-1108 to 16 children with ages ranging from 7 month to 15 years at doses between 1.8 and 6.0 mg/kg x 3/day for 3 to 13 days. We evaluated the efficacy and safety of S-1108 in 11 children with respiratory tract infections, 3 urinary tract infections, and 2 skin infections. The efficacy rate of S-1108 was 100% and bacteriological eradication rate was 83.3%. No adverse effects were observed. These results suggested that S-1108 could be used safely in children.

Topics: Adolescent; Bacteria; Bacterial Infections; Cephalosporins; Child; Child, Preschool; Drug Evaluation; Female; Humans; Infant; Male; Microbial Sensitivity Tests; Respiratory Tract Infections; Skin Diseases, Bacterial; Urinary Tract Infections

A new oral cephem antibiotic, S-1108, was evaluated for its clinical efficacy and safety in children. S-1108 was effective in 95% of the 59 examined cases of respiratory, middle ear, skin and urinary tract infections. S-1108 was highly effective in infections of Streptococcus pyogenes, Haemophilus influenzae and Escherichia coli, but was less effective in penicillin-resistant Streptococcus pneumoniae and Staphylococcus aureus infections. The serum half-life was 1.26 +/- 0.36 hours upon after meal administration of 4 mg/kg. No severe adverse reaction was encountered. From these data, S-1108 appears to be safe and effective in children with susceptible bacterial infections.

Topics: Bacterial Infections; Cephalosporins; Child; Child, Preschool; Drug Evaluation; Escherichia coli Infections; Female; Haemophilus Infections; Haemophilus influenzae; Humans; Infant; Male; Respiratory Tract Infections; Streptococcal Infections; Streptococcus pyogenes; Urinary Tract Infections

Laboratory and Clinical Studies on S-1108, a new oral cephem antibiotic, were carried out to evaluate its usefulness at a dose between 2 and 4 mg/kg a day for 7 to 14 days in the pediatric field. 1) Pharmacokinetic studies S-1108 at a dose of 2 mg/kg was administered to evaluate the pharmacokinetic parameters in 1 subject. Cmax, T1/2 and AUC were 0.69 hour, 1.42 hours and 2.15 micrograms.hr/ml, respectively. 2) Antimicrobial activities MICs against various clinically isolated organisms (Staphylococcus aureus, Streptococcus pyogenes, Streptococcus pneumoniae, Branhamella catarrhalis, Escherichia coli and Haemophilus influenzae) were determined. The MIC values of S-1006 were similar to those of cefteram, the MICs against S. pyogenes, and H. influenzae were < or = 0.025 and 0.10 microgram/ml, respectively. 3) Clinical studies S-1108 was administered to patients with various pediatrics infections in 34 cases (upper respiratory tract infections: 12 cases, lower respiratory tract infections: 5 cases, urinary tract infections: 9 cases, skin and soft tissue infection: 6 cases, otitis media: 2 cases). Clinical efficacy rate was evaluated according to "Standard of clinical evaluation in pediatrics field". The responses were all good or excellent. 4) Side reactions There were no serious adverse reactions in any cases. The above results suggest that S-1108 is potent effective and safe agent in the pediatric field at a dose between 2-4 mg/kg (t.i.d.) a day.

Topics: Bacteria; Bacterial Infections; Cephalosporins; Child; Child, Preschool; Drug Evaluation; Female; Humans; Infant; Male; Microbial Sensitivity Tests; Respiratory Tract Infections; Urinary Tract Infections