s-1108 and Diarrhea

Cefcapene pivoxil hydrochloride (CFPN-PI), an ester cephem antibiotic, was orally given at a dose of 100 mg three times daily in patients with infection and soft stool or diarrhea, and its absorption was determined using the recovery ratio of 12-h urine pooled after the initial administration as an index. The primary endpoint, the recovery ratio of 12-h urine pooled after oral administration, could be evaluated in six of the eight patients finally gathered, and the mean value was 30.1 +/- 5.8%, which was not considered to differ from the mean value of 34.4 +/- 5.5% obtained in six healthy adult volunteers in the previous phase I study. Clinical efficacy in the eight patients was rated as very effective, effective, and ineffective in two, five, and one patients, respectively, with an effective ratio of 87.5% (7/8). Neither adverse drug reactions nor abnormal laboratory data were observed in any patient. These results indicate that CFPN-PI, at the routine oral dose, does not cause any problems in terms of absorption, efficacy, and safety when it is used in patients with infection and soft stool or diarrhea.

Topics: Absorption; Adult; Aged; Aged, 80 and over; Cephalosporins; Communicable Diseases; Diarrhea; Feces; Female; Gastrointestinal Diseases; Humans; Male; Middle Aged; Treatment Outcome; Urine

A clinical study in children has been performed on S-1108, a newly developed cephem antibiotic. S-1108 was given orally to 30 patients, at doses between 8 and 12 mg/kg/day in 3 divided doses for 2 to 10 days. Clinical evaluations were made on 26 patients consisting of 12 patients of pharyngitis, 5 of tonsillitis and of impetigo, one each of bronchitis, cystitis, lymphadenitis and cellulitis. Overall clinical effects were excellent in 10, good in 15, fair in 1 with an efficacy rate of 96%. As to adverse reactions, mild diarrhea (2 patients) and transients elevation of transaminases (one patient) were observed. These data suggest that S-1108 is a useful oral antibiotic for the treatment of bacterial infections in children.

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

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

S-1108 in a fine granular form was administered in 14 children and its safety and efficacy in bacterial infections were evaluated. Among them, 2 cases of cystitis and 1 case of pneumonia were considered unevaluable for the efficacy. The results obtained are summarized as follows. 1. The overall clinical efficacy rate was 81.8% in the eleven evaluable cases treated with S-1108 fine granules including 5 cases of pharyngitis, 2 cases each of tonsillitis, pertussis and cystitis. 2. Bacteriological efficacy of 100% was achieved against pathogens identified in 5 children including 1 case each of Staphylococcus aureus, Streptococcus pyogenes and Haemophilus influenzae and 2 cases of Escherichia coli. 3. The only abnormal laboratory test results observed were eosinophilia and leukocytopenia in one case each. Diarrhea was recorded in 1 case. Judging from the above results, it appears that S-1108 in the fine granular form is an effective, useful and safe antibiotic of first choice for the treatment of infections in the pediatric field.

Topics: Administration, Oral; Bacterial Infections; Cephalosporins; Child; Child, Preschool; Diarrhea; Female; Humans; Infant; Leukopenia; Male; Prodrugs

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

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