Clinical studies in sultamicillin fine granule in the field of pediatrics

Clinical studies were carried out on sultamicillin (SBTPC) fine granule in the field of pediatrics. The results obtained are summarized below. 1. Thirty children with bacterial infections were treated with SBTPC fine granule. The clinical results were excellent in 24 and good in 5, with an efficacy rate of 96.7%. 2. Bacteriological screening identified 26 pathogenic organisms of which 14 were Gram-positive cocci and 12 Gram-negative rods. Eradication rates were 91.7% in Gram-positive cocci and 66.7% in Gram-negative rods. 3. As side effects, diarrhea was observed in 12.9%, loose stool in 16.1% and eosinophilia in 3.2% of the patients. From the above results, it appeared that SBTPC fine granule was a useful drug for treating bacterial infections in the field of pediatrics.     

Clinical studies on sultamicillin in pediatrics

Sultamicillin (SBTPC) fine granule was given orally to 15 children with acute bacterial infections including 4 with acute pharyngitis, 5 with acute tonsillitis, 2 each with acute bronchitis and urinary tract infections, and 1 each with acute pneumonia and cervical purulent lymphadenitis. Good to excellent clinical responses were obtained in all of the 15 patients and bacterial eradication of all 4 strains found in these cases. Loose stool was observed in 1 case. From the above clinical results, it appears that SBTPC is a useful antibiotics for the treatment of pediatric patients with various bacterial infections.     

Studies on cefuzoname in the field of pediatrics

Cefuzoname (CZON, L-105) a newly developed cephalosporin, has broad spectrum on Gram-positive or -negative bacteria and may also be effective against Staphylococcus aureus against which third generation cephalosporins are largely ineffective. We studied the pharmacokinetics and clinical effects of CZON on infectious disease of children. The diseases we studied included 2 cases of bacterial meningitis and 1 case each of viral meningitis, enterocolitis, upper respiratory infection, pneumonia, and mycoplasmal pneumonia. CZON was administered by drip infusion. Dose levels were 20-53 mg/kg/30-60 minutes, 3 times a day. For 5 cases, was studied time course of concentrations of CZON in plasma. Median T 1/2 was 0.96 hour. Concentrations in cerebrospinal fluid (CSF) were studied in cases of pneumonia and bacterial meningitis. In the case of pneumonia the CSF concentration of CZON was 0.272 microgram/ml after 45 minutes, in the case of meningitis they were 0.155 microgram/ml after 5 hours. Both of these values were higher than MIC of 0.025 microgram/ml against Haemophilus influenzae which was isolated from a case of bacterial meningitis. This MIC was lower than that of cefotiam and cefazolin, as well as of cefmenoxime. Clinical effects were excellent on pneumonia, good on upper respiratory infection, fair on mycoplasmal pneumonia. CZON, however, was ineffective in the treatment of a case of bacterial meningitis from which a susceptible strain of H. influenzae was isolated.(ABSTRACT TRUNCATED AT 250 WORDS)     

Studies on meropenem in the field of pediatrics]

The pharmacokinetics and the clinical effectiveness of meropenem (MEPM) were examined in the field of pediatrics. The results are summarized as follows. 1. A 4-year-6-month-old girl with suppurative meningitis (Haemophilus influenzae) was treated by intravenous drip infusion of MEPM in a daily dose of 29 mg/kg which was divided into 4 dosages, each dosage being infused over 30 minutes, and the drug concentration in cerebrospinal fluid was determined. Upon completion of infusion on the 2nd day of treatment, the drug concentration was 2.52 micrograms/ml, which corresponded to 3.6% of the drug concentration in the blood. 2. MEPM was used in 10 patients, including 3 with suppurative lymphnoditis, 2 with staphylococcal scalded skin syndrome (SSSS) and 1 each with pneumonia, suppurative meningitis, suppurative knee arthritis, facial phlegmon and pyelonephritis. The daily doses ranged from 30 to 117.6 mg/kg, divided into 3 to 4 dosages and administered via intravenous drip infusion over 30 minutes. Clinical responses were evaluated as very good in 7 patients, good in 2 patients and fair in 1 patient, with an efficacy rate of 90%. 3. Isolated pathogens were 2 strains of Staphylococcus aureus, 1 strain of Klebsiella pneumoniae and 3 strains of Haemopilus influenzae. All of the 6 strains were eradicated, with an eradication rate of 100%. 4. In the safety evaluation, none of the patients was observed to have any side effects. Furthermore, no abnormal variations were found in laboratory test data possibly attributable to administration of MEPM.     

Clinical and pharmacokinetic studies on sultamicillin fine granules in pediatrics

Sultamicillin (SBTPC) is a mutual prodrug of sulbactam (SBT) and ampicillin (ABPC). A study has been performed to evaluate pharmacokinetic properties and clinical usefulness of SBTPC fine granules in the treatment of pediatric infections. After an oral dose of 5-15 mg/kg of SBTPC fine granules, peak serum concentrations of ABPC and SBT were 1.18-3.26 micrograms/ml and 0.97-3.05 micrograms/ml, respectively at 1 hour. Serum half-lives for elimination (T 1/2 (beta] of ABPC and SBT were 0.83-1.83 hours and 0.94-1.71 hours, respectively. Serum concentrations of ABPC at 1-6 hours after an oral administration of SBTPC fine granules were similar to those of SBT. Serum concentrations of ABPC and SBT were proportional to dose levels of SBTPC fine granules. Following oral administrations of 5-15 mg/kg, 33.9-64.8% of ABPC and 38.1-76.6% of SBT were recovered in urine in 6 hours. SBTPC fine granules were administered in a daily dose of approximately 30 mg/kg divided into 3 doses to 14 pediatric patients with bacterial infections. All 14 were cured with 11 excellent and 3 good clinical response to this drug. Microbiological eradication was obtained in 85.7%. beta-Lactamase-producing ABPC-resistant strains were eradicated. Adverse effects including laboratory test values that may be attributed to the administration of SBTPC fine granules were not observed except a treatment episode of diarrhea in 1 patient.     

Studies on sulbactam/cefoperazone in the field of pediatrics

Microbiological, pharmacokinetic and clinical studies on sulbactam/cefoperazone (SBT/CPZ) were carried out in the field of pediatrics. Antimicrobial activity The MIC80 of SBT/CPZ was 6.25 micrograms/ml for clinically isolated 24 strains of S. aureus (24 beta-lactamase producing strains), 0.39 micrograms/ml for 17 strains of S. pyogenes, 3.13 micrograms/ml for 24 strains of E. coli (22 beta-lactamase producing strains), 3.13 micrograms/ml for 22 strains of K. pneumoniae (22 beta-lactamase producing strains), 1.56 micrograms/ml for 22 strains of P. mirabilis and 0.20 microgram/ml for 15 strains of H. influenzae (13 beta-lactamase producing strains). In comparison with CPZ in respect to the MIC, SBT/CPZ exhibited synergistic effect on 31 strains out of 81 beta-lactamase producing strains (included 6 strains of S. aureus, 9 of E. coli, 5 of K. pneumoniae and 11 of H. influenzae) which was scarcely observed against 43 non-beta-lactamase producing strains. Absorption and excretion Serum levels and urinary excretion of SBT/CPZ were studied in 7 children aged 5 to 12 years. The mean serum concentration of SBT at 15 minutes following a single intravenous injection of 10 mg/kg of SBT/CPZ was 14.2 micrograms/ml and that of CPZ was 30.4 micrograms/ml. The mean urinary recovery rates at 6 hours following the intravenous injection were 57.8% and 18.3%, respectively. The mean serum concentrations of SBT and CPZ after 1-hour infusion of 10 mg/kg of SBT/CPZ were 10.9 micrograms/ml and 17.6 micrograms/ml, respectively. The urinary recovery rates of SBT and CPZ at 7 hours after the infusion were 100.0% and 27.7% on average, respectively. The mean serum levels of SBT and CPZ at 15 minutes after a single intravenous injection of 20 mg/kg of SBT/CPZ were 25.6 micrograms/ml and 66.0 micrograms/ml, respectively and urinary elimination until up to 6 hours were 72.5% on average for SBT and 21.1% for CPZ. Clinical study SBT/CPZ was used for the treatment of a total of 20 pediatric patients aged 1 month to 14 years to evaluate its clinical effectiveness, bacteriological efficacy and adverse effects. The clinical efficacy in 6 patients with acute pneumonia, 3 with staphylococcal scalded skin syndrome, 2 each with acute purulent tonsillitis and acute pyelonephritis, 1 each with acute purulent lymphadenitis, acute sinusitis, acute bronchitis, peritonitis and acute enteritis was judged to be excellent in 15 cases and good in 3 cases with an efficacy ratio of 100%. The clinical efficacy in 6 patients whose infections were caused by beta-lactamase producing strains was judged to be excellent in all the cases.(ABSTRACT TRUNCATED AT 400 WORDS)     

Studies on sulbactam/ampicillin in the field of pediatrics

Pharmacokinetic and clinical studies on sulbactam/ampicillin (SBT/ABPC) were carried out in the field of pediatrics. 1. Absorption and excretion Serum levels and urinary excretion of SBT/ABPC were studied in 4 children with ages 6 to 8 years. The mean serum concentration of SBT at 15 minutes following a single intravenous injection of 30 mg/kg of SBT/ABPC was 27.4 +/- 2.2 micrograms/ml and that of ABPC was 42.8 +/- 3.9 micrograms/ml, and their concentrations declined with mean half-lives of 1.06 +/- 0.15 hours and 0.84 +/- 0.05 hour, respectively, and at 6 hours were 0.3 +/- 0.2 microgram/ml and 0.2 +/- 0.1 microgram/ml on the average, respectively. The urinary recovery rates of SBT and ABPC at 6 hours after the injection were 59.0 +/- 22.4% and 58.4 +/- 25.3% on the average, respectively. 2. Clinical study SBT/ABPC was used for the treatment of a total of 36 pediatric patients with ages ranging 2 months to 11 years and it's clinical effectiveness, bacteriological efficacy and adverse effects were evaluated. Clinical efficacies in 5 patients with acute purulent tonsillitis, 26 with acute pneumonia and 1 with acute pyelonephritis were judged to be excellent in 27 cases and good in 5 cases with an overall efficacy ratio of 100.0%. Clinical efficacies in 6 patients whose infections were caused by beta-lactamase producing strains were judged to be excellent in all cases. Bacteriological efficacies of SBT/ABPC were assessed on 1 strain of Staphylococcus aureus (beta-lactamase producing strain), 2 strains of Streptococcus pneumoniae, 16 strains of Haemophilus influenzae (5 beta-lactamase producing strains and 11 non-beta-lactamase producing strains), 1 non-beta-lactamase strain of Haemophilus parainfluenzae and 2 strains of Escherichia coli (non-beta-lactamase producing strains). All strains except 1 strain of H. influenzae (beta-lactamase producing strain) which decreased in number were eradicated with a bacteriological eradication rate of 95.5%. Only 1 patient complained of diarrhea which was suspected to be related to the drug. No other side effect was reported. Elevations of GOT and GPT were observed in only 1 patient. The above results suggested that SBT/ABPC was a useful drug with preferable safety profile in the treatment for pediatric patients with infectious disease caused by beta-lactamase producing strains as well as those by non-beta-lactamase producing strains.     

Pharmacokinetics and clinical effects of sultamicillin fine granules in pediatrics

We have evaluated sultamicillin (SBTPC) fine granules for pharmacokinetics and therapeutic effectiveness in children. The results are summarized as follows. 1. Pharmacokinetic parameters after the oral administration of single dose of 5.0 mg per kg body weight in 1 child were as follows: The peak serum concentrations of ampicillin (ABPC) and sulbactam (SBT) were 1.92 micrograms/ml at 1 hour and 1.85 micrograms/ml at 1 hour, respectively. The half-lives in serum and urinary excretion rate for ABPC and SBT were similar. 2. A clinical study was performed on 15 children with infections, including 4 with tonsillitis, 5 with pharyngitis, 2 each with bronchitis, cystitis, and urinary tract infections. Doses ranging from 6.7 to 18.2 mg/kg body weight were given tid. or qid. Lengths of treatment ranged from 5 to 10 days. The therapeutic responses were considered "excellent" in 6 and "good" in 9, with an effectiveness rate of 100%. 3. As to side effects of the drug, diarrhea was observed in 1 patient. It was concluded that SBTPC was a promising drug for the treatment of bacterial infections in children.     

Studies on imipenem/cilastatin sodium in the field of pediatrics

Pharmacokinetic and clinical studies on imipenem (MK-0787)/cilastatin sodium (MK-0791), a combined drug of carbapenem antibiotics (MK-0787) and renal depeptidase inhibitor (MK-0791) in a 1:1 ratio, were performed in the field of pediatrics. Absorption and excretion Serum levels and urinary excretion of MK-0787/MK-0791 were determined in 7 children aged 4 to 11 years. Four cases were administered with a single dose of MK-0787/MK-0791 at 10 mg/10 mg/kg by intravenous drip infusion and the other 3 cases were given a single dose of 20 mg/20 mg/kg. Serum concentrations of MK-0787 reached their peaks at the end of drip infusion where the mean level was 17.5 +/- 1.0 micrograms/ml for the group given 10 mg/10 mg/kg, and 43.6 +/- 2.1 micrograms/ml for the group given 20 mg/20 mg/kg. Concentrations decreased with half-lives of 0.82 +/- 0.10 hour and 0.74 +/- 0.04 hour for the low and high doses, respectively, and serum levels at 6 hours after administration were 0.3 +/- 0.1 microgram/ml and 0.4 +/- 0.1 microgram/ml, respectively. Peak concentrations of MK-0791 were 22.6 +/- 4.8 micrograms/ml in the 10 mg/10 mg/kg group and 52.9 +/- 4.7 micrograms/ml in the 20 mg/20 mg/kg group at the end of the drip infusion. Half-lives were 0.56 +/- 0.17 hour and 0.46 +/- 0.11 hour for the 2 doses, respectively while MK-0791 levels were below detection limit at 6 hours after administration. Mean urinary recovery rates in 6 hours after administration were 54.0 +/- 15.3% and 49.3 +/- 7.8% for MK-0787 and MK-0791, respectively, in the group of 10 mg/10 mg/kg, and 62.0 +/- 7.4% and 65.3 +/- 9.2%, respectively, in the group of 20 mg/20 mg/kg. These results showed that pharmacokinetics of MK-0787 and MK-0791 in children were similar to that in adults. Clinical study MK-0787/MK-0791 was used for treatment in a total of 22 pediatric patients to evaluate clinical effectiveness, bacteriological efficacy and adverse reactions. Each of patients was treated 3 or 4 times per day at a single dose of 11.4-22.8 mg/kg (of MK-0787). Duration of treatment ranged from 2.5 to 18 days and total doses ranged from 1.36 to 19.92 g. Clinical efficacy in cases including 2 with acute purulent tonsillitis, 1 with acute purulent otitis media, 9 with acute pneumonia, 1 with pythorax, 3 with acute purulent lymphadenitis, and 6 with acute pyelonephritis were judged excellent in 20 cases and good in 2 cases; an efficacy rate of 100%.(ABSTRACT TRUNCATED AT 400 WORDS)     

Studies on panipenem/betamipron in the field of pediatrics]

Pharmacokinetic and clinical studies in pediatrics were performed on panipenem/betamipron (PAPM/BP), a combined drug of a carbapenem antibiotic (panipenem) and organic ion inhibitor (betamipron) at a weight ratio of 1:1. 1. Plasma levels and urinary excretion were studied when PAPM/BP, at 10 mg/10 mg/kg (4 cases) or 20 mg/20 mg/kg (5 cases), was administered using intravenous drip infusion in 30 minutes to 9 children (4-14 years old). The plasma PAPM level at the end of drip infusion was 30.75 +/- 4.98 micrograms/ml in the cases administered with 10 mg/10 mg/kg and 68.72 +/- 5.73 micrograms/ml in the cases administered with 20 mg/20 mg/kg. Drug concentrations then gradually decreased with half-lives of 1.08 +/- 0.09 hours and 0.98 +/- 0.02 hour, and reached 0.39 +/- 0.14 micrograms/ml and 0.62 +/- 0.06 micrograms/ml, respectively, after 5.5 hours. Plasma BP levels at the end of drip infusion was 18.93 +/- 3.75 micrograms/ml in the cases administered 10 mg/10 mg/kg and 37.09 +/- 2.68 micrograms/ml in the cases administered 20 mg/kg, and half-lives were 0.55 +/- 0.07 hour and 0.61 +/- 0.03 hour, respectively; the plasma BP level could not be determined in any cases after 5.5 hours. Mean urinary recovery rates of PAPM in the first 6 hours after the start of intravenous drip infusion were 33.0 +/- 6.1% in the cases administered 10 mg/10 mg/kg and 21.8 +/- 2.3% in the cases administered 20 mg/20 mg/kg and those of BP were 77.0 +/- 2.4% and 76.6 +/- 7.3%, respectively. 2. When PAPM/BP, was administered at 31.3 mg/31.3 mg/kg thought by intravenous drip infusion in 30 minutes to 1 case of purulent meningitis, PAPM levels were 0.76 micrograms/ml at the end of drip infusion but varied between 0.80 to 1.97 micrograms/ml 30 minutes after the end of drip infusion during 8 days of treatment. 3. PAPM/BP was administered to 43 cases, 47 diseases of bacterial infections in the domain of pediatrics to study its clinical efficacy, bacteriological efficacy and adverse reactions. Single doses were 5.2mg/5.2mg to 31.3 mg/31.3 mg/kg; frequencies of administration were 3 to 4 times a day, and durations of administration were 3 1/3 to 11 days; and total dosages ranged between 1.125 g/1.125 g and 11.0 g/11.0 g.(ABSTRACT TRUNCATED AT 400 WORDS)     

舒他西林的药效学研究

本文报道国产舒他西林与氨苄西林／舒巴坦等４种对照抗生素对６３３株细菌的体外抗菌作用及其以氨苄西林为对照对３株细菌分别感染小鼠的体内抗菌作用。     

Clinical studies on sultamicillin fine granules in the urological field

Clinical studies of sultamicillin (SBTPC) fine granules, an oral antibiotic with ester linked ampicillin and beta-lactamase inhibitor, sulbactam, were performed in acute uncomplicated cystitis and complicated urinary tract infections. 1. SBTPC fine granules were administrated at a dose of 187.5 mg 2-3 times daily for 5-7 days to 6 patients with acute uncomplicated cystitis. Clinical efficacies as judged according to the criteria of the UTI Committee were excellent in 5 cases and moderate in 1 case with an effectiveness rate of 100%. All of 7 identified bacteria were eradicated by the treatment. 2. SBTPC fine granules were administrated at a dose of 187.5 mg or 375 mg 3 times daily for 5-7 days to 17 patients with complicated urinary tract infections. Clinical efficacies as judged according to the criteria of the UTI Committee were excellent in 8 cases, moderate in 4 cases and poor in 5 cases with an effectiveness rate of 70.6%. Out of 17 identified bacteria, 14 (82.4%) were eradicated by the treatment. 3. As adverse reactions, glossitis, diarrhea and pharyngeal redness were observed in 1 case out of 31 cases treated with the drug. These symptoms, however, were mild and transient. No abnormal laboratory test values were observed. From the above results, it appears that SBTPC fine granules are useful in the treatment of urinary tract infections.     

Clinical studies on sultamicillin fine granule in pediatric field

Pharmacokinetics, safety and effects on bacterial infection of sultamicillin (SBTPC) fine granule were evaluated in 17 children. The results obtained are summarized as follows. 1. Pharmacokinetics in 3 children receiving a single dose of 10 mg per kg body weight were evaluated. The half-life of ampicillin (ABPC) was 1.38 +/- 0.14 hours and that of sulbactam was 0.93 +/- 0.26 hour. 2. Fourteen cases, including 7 tonsillitis, 2 pharyngitis, 2 bronchitis, and 1 each of cystitis, scarlet fever and cellulitis were treated with SBTPC fine granule. The clinical efficacy rate was 100%. 3. Bacteriological efficacies classified by causative organisms were evaluated in 5 children. Staphylococcus aureus was responsible in 3 cases, Streptococcus pyogenes in 1 case, Escherichia coli and Proteus mirabilis in 1 case. Eradication rate was 100%. SBTPC was more active than ABPC against ABPC-resistant strains and almost equal to or more active than cephalexin or cefaclor. 4. The only abnormal laboratory test value observed was eosinophilia in 2 children. No side effects were recorded. From the above results it is concluded that SBTPC fine granule is one of first choices of effective, useful and safe antibiotics for the treatment of infections in pediatric field.     

Laboratory and clinical studies of sultamicillin in pediatric field

We have carried out laboratory and clinical studies on sultamicillin (SBTPC). The results are summarized as follows. SBTPC was given by oral administration to 2 children in a single dose at 5 mg/kg and to 3 children in a single dose at 10 mg/kg. After the oral administration, mean peak serum levels of ampicillin (ABPC) and sulbactam (SBT) obtained for the 2 dose levels were 1.91 +/- 1.34 and 2.06 +/- 1.06 micrograms/ml and 2.43 +/- 0.68 and 2.96 +/- 0.77 micrograms/ml at 1 hour, respectively, and mean half-lives were 0.80 +/- 0.10 and 0.98 +/- 0.46 hour and 1.57 +/- 0.57 and 2.01 +/- 0.70 hours, respectively. SBTPC was given to 2 children in a single dose at 15 mg/kg. After oral administration, the mean serum levels of ABPC and SBT at 30 minutes were 6.55 +/- 1.63 and 6.00 +/- 1.00 micrograms/ml, and the mean half-lives were 0.90 +/- 0.13 and 0.82 +/- 0.16 hour. SBTPC was given to 1 child at a single dose of 20 mg/kg. The peak serum levels of ABPC and SBT were 11.3 and 8.64 micrograms/ml, and the half-lives were 0.87 and 0.92 hour. Mean urinary excretion rates of ABPC and SBT were 38.4 +/- 2.7 and 34.6 +/- 4.7%, 43.0 +/- 3.6 and 41.6 +/- 5.8%, 47.7 +/- 5.2 and 51.6 +/- 3.5% in 6 hours and 66.1 and 59.2% in 8 hours after oral administration of 5 mg/kg, 10 mg/kg, 15 mg/kg and 20 mg/kg, respectively. Treatment with SBTPC was made in 34 cases of pediatric bacterial infections; 2 cases of pharyngitis, 19 cases of tonsillitis, 2 cases of bronchitis, 3 cases of impetigo, 2 cases of staphylococcal skalded skin syndrome, 4 cases of urinary tract infection and 1 case each of pneumonia and scarlet fever. Results obtained were excellent in 20 cases, good in 13 cases and poor in 1 case. No significant side effect due to the drug was observed in any cases.     

Pharmacokinetic and clinical studies of sultamicillin granule in the pediatric field

Sultamicillin (SBTPC) is a combined drug of ampicillin (ABPC) and sulbactam (SBT) which is an inhibitor of beta-lactamase, in a clinical form of tosylate with equivalent molecules in ester linkages. A tablet form of this combined drug has been released since July, 1987 in Japan and now a granular form for pediatric patients has been developed. Hence, the granular form of SBTPC was administered to 6 boys (age: 8 years 5 months-11 years 5 months) to determine plasma and urinary concentrations of the drug and its urinary recovery-rates. The dose of 10 mg/kg or 15 mg/kg was given orally just after meal to 3 boys. To study clinical and bacteriological effects of this drug, a mean daily dose of 27.1 mg/kg divided 2-4 times a day was administered for 9 days on the average to a total of 57 cases with pharyngitis (5), tonsillitis (5), laryngitis (1), bronchitis (1), pneumonia (8), scarlet fever (1), typhoid fever (1), impetigo (16), furuncle (2), abscess (6), lymphadenitis (1) and urinary tract infection (10) except 2 cases which were unevaluable for clinical effects. MICs of 7 drugs (SBTPC, ABPC, SBT, methicillin (DMPPC), cloxacillin (MCIPC), cephalexin and cefaclor) against 12 of 22 strains isolated from patients with infections of skin and soft tissue were determined with inoculum-sizes of 10(8) and 10(8) CFU/ml to study beta-lactamase producing activities. Adverse reactions and abnormal effects on laboratory test values attributable to this drug were studied in patients including dropped-out cases. The results obtained are summarized as follows. 1. Mean plasma peak levels of ABPC and SBT were observed at 1 hour after administration in both of the 10 mg/kg and the 15 mg/kg groups with values of 2.34 and 5.57 micrograms/ml for ABPC and 1.87 and 4.66 micrograms/ml for SBT, respectively. Mean concentrations of SBT were lower than those of ABPC in both groups and individuals. Dose-responses in plasma levels and AUCs were observed in both groups. Mean half-life values of ABPC and SBT in the 2 groups were 1.93 and 1.12 hours for ABPC and 1.97 and 1.22 for SBT, respectively. Mean half-life values for ABPC and SBT were similar in each group and this tendency was also seen among individuals.(ABSTRACT TRUNCATED AT 400 WORDS)     

Clinical experience with sultamicillin fine granules in pediatric field

Sultamicillin fine granules were used orally in 18 pediatric patients with infections in doses ranging 7.3-10.0 mg/kg t.i.d. or q.i.d. The following is a summary of the results: 1. Clinical efficacies in 16 cases with tonsillitis were excellent in 13 cases, good in 2 cases and fair in 1 case. Efficacy in 1 case of bronchitis and 1 case of pneumonia were good. The overall efficacy rate in the 18 cases was 94.4%. 2. Four out of 5 strains of Staphylococcus aureus were eradicated but 1 strain persisted. Three out of 7 strains of Haemophilus influenzae were rated as eradicated, 1 strain as decreased and 3 strains as persisted. Two strains of Streptococcus pyogenes and 3 strains of Haemophilus parainfluenzae were eradicated. The bacteriological efficacy rate for the 17 strains was 70.6%. Four strains out of the 17 were found to produce beta-lactamase and 3 strains were suspected, to produce the enzyme, but of these 7 strains, 5 strains were eradicated. 3. Diarrhea and loose stool were observed as side effects in each of 2 cases. It appeared that diarrhea was related to this drug. A slight elevation of GOT was observed in 1 case in laboratory tests. 4. This drug appears to be easy for children to take in terms of taste and smell.     

Clinical studies on norfloxacin in the field of pediatrics

We studied clinical effects of norfloxacin (NFLX, AM-715) tablets. The results we found are summarized as follows: 1. Ten patients with 5 diseases were medicated with 7.0-14.8 mg/kg of the drug 3 times daily for 6-8 days. They consisted of one-each with tonsillitis, pharyngitis, bronchitis, 4 with Campylobacter enteritis, 3 with other enteritis. Clinical responses to the treatment were excellent in 8, good in 1 and fair in 1, with an efficacy rate of 90%. Bacteriologically, of 9 isolates for which changes in populations were followed, 6 were eradicated and 3 remained unchanged, with an eradication rate of 66.7%. 2. No. adverse reactions nor abnormal laboratory test values attributable to the drug were observed. 3. These results suggest that this new quinolone drug may be useful, against bacterial infections in children 6 years and older.     

Clinical studies on cefminox in the field of pediatrics

A new antibiotic of cephamycin group, cefminox (CMNX, MT-141), was evaluated clinically in the treatment of bacterial infections in children. The following results were obtained. One case of lacunar tonsillitis (due to H. influenzae) and 5 cases of urinary tract infections (due to E. coli in 2 cases, mixed infection due to E. coli and E. faecalis in 1 case, due to K. pneumoniae in 1 case and causative organism was unknown in 1 case) were treated intravenously with CMNX at daily doses ranging from 58.1 to 122.7 mg/kg in 3 divided doses. One case in which the treatment was discontinued after 1 day because of rashes was excluded from assessment of efficacy. Among the remaining 5 cases, CMNX was found ineffective for 1 case of mixed infection due to E. coli and E. faecalis. However, in all of the other 4 cases excellent results were obtained. As side effects, rashes developed in 1 case and slight elevation in GOT in 1 case out of 6 cases. Blood levels following bolus intravenous injection of 20 mg/kg of CMNX were 68, 45, 27, 10.2 and 3.1 micrograms/ml at 1/2, 1, 2, 4 and 6 hours, respectively, with T 1/2 of 1.27 hours. The urinary recovery rate within the first 6 hours was 78.6%.     

Clinical studies on aspoxicillin in the field of pediatrics

Clinical studies were performed as follows on aspoxicillin (ASPC), a new semisynthetic penicillin. ASPC was intravenously given to 12 patients in doses of 57.7-129.0 mg/kg on average) t.i.d. or q.i.d. for 4-7 days (5.7 days on average): 9 with pneumonia, 1 with tonsillitis, 1 with purulent lymphadenitis and 1 with urinary tract infection. The overall efficacy rate was 83.3%, i.e. efficacy was excellent in 8 (66.7%), good in 2 (16.7%), fair in 1 (8.3%) and poor in 1 (8.3%). Bacteriological efficacy was excellent, i.e. 6 of the 6 strains disappeared. No clinical side effects were observed during treatment. Laboratory abnormalities were observed in 3 cases, slight elevation of GOT in 1, slight elevations of GOT and GPT in 1 and mild eosinophilia in 1. The above results suggest that ASPC is an useful antibiotic for treating pediatric bacterial infections.     

Studies of rokitamycin in pediatrics

Pharmacokinetic, bacteriological and clinical studies on a new macrolide antibiotic, rokitamycin (RKM) dry syrup for pediatric use, were done, and results as summarized below were observed: 1. Five children with ages between 6 and 10 years were administered orally with RKM at a dose level of 10 mg/kg either at 30 minutes before or 30 minutes after meal on a crossover design, and plasma concentrations and urinary excretion rates of the drug were measured. Plasma concentrations of RKM following the administration before meal were 0.50 microgram/ml at 1/2 hour, 0.43 microgram/ml at 1 hour, 0.15 microgram/ml at 2 hours, 0.03 microgram/ml at 4 hours, and not detectable at 6 hours. Plasma concentrations following the administration after meal were 0.11 microgram/ml at 1/2 hour, 0.15 microgram/ml at 1 hour, 0.09 microgram/ml at 2 hours, 0.03 microgram/ml at 4 hours, and not detectable at 6 hours. The 0-6 hour urinary recovery rates were 1.41% following the administration before meal, and 0.93% following the administration after meal. These results suggested that the drug might be absorbed more rapidly, giving a higher plasma concentration, when administered before meal than when administered after meal. Changes in plasma concentrations of RKM following the administration of 10 mg/kg before meal were similar to those of two 100 mg RKM tablets (TMS-19-Q.GC tablets) to adult patients. Therefore, it seemed optimal to administer 10 mg/kg 3 times daily at fasting to children as a rule.(ABSTRACT TRUNCATED AT 250 WORDS)