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Biomedical subjects

K Sunakawa

Publications and source records attributed to K Sunakawa.

At least 91 records · Page 5Linked to original sources

[Bacteriological and clinical evaluations of cefmenoxime in neonates and premature infants].

The antimicrobial activity of cefmenoxime (CMX) against B group Streptococcus was investigated. The clinical efficacy of CMX was determined in neonates and premature infants. The results are summarized below. 1. MIC's of CMX against 39 strains of B group Streptococcus obtained from the pregnant vagina were below 0.05 micrograms/ml. 2. CMX was given in a dose of 20 mg/kg by intravenous bolus injection to 3 neonates with birth weight over 2,500 grams. Peak serum concentrations ranged from 54.0 to 199 micrograms/ml and the mean half-life was 1.8 hours. 3. Efficacies of CMX were good to excellent in 5 cases administered for treatment and in 4 cases for prophylaxis. As abnormal laboratory parameters, elevation of GOT and eosinophilia were observed in each 2 cases. 4. Examinations on intestinal bacteria in 2 cases revealed that CMX gave as much influences to the flora as other third-generation cephems. 5. The vitamin K deficiency were observed in 2 out of 6 cases examined.

Bacterial Infections↗

[Pharmacokinetic and bacteriological studies on sulbactam/ampicillin in the field of pediatrics].

Pharmacokinetic and bacteriological studies were carried out on sulbactam/ampicillin (SBT/ABPC) in the field of pediatrics. The results obtained are summarized as follows: 1. A total of 248 clinical isolates were employed to determine minimum inhibitory concentrations (MIC) of SBT/ABPC against various bacterial species. SBT/ABPC showed stronger antibacterial activity against Gram-positive organisms than against Gram-negative rods. 2. The peak serum level of ABPC was about twice as high as that of SBT, and serum levels of ABPC and SBT declined with time. Both drugs showed almost the same trend of changes in concentrations. The half-lives of both drugs were about 1 hour. 3. The urinary recovery rates over 6 hours after administration were 52-80% for ABPC and 70-73% for SBT. 4. The effect of SBT/ABPC on coagulation system was examined. No case showed changes in PT, APTT, TT and HPT before and after administration of SBT/ABPC. Platelet aggregation during administration of SBT/ABPC was slightly faster than that before administration, suggesting that SBT/ABPC had no effect on platelet aggregation. Generally speaking, it seemed that SBT/ABPC was a safe antibiotic for bleeding. 5. The effect of SBT/ABPC on the intestinal bacterial flora in experimental animals was examined. Escherichia coli, Enterococcus faecalis, Bacteroides fragilis and Bifidobacterium breve were reduced after administration of SBT/ABPC, suggesting that the intestinal bacterial flora was affected by the administration of SBT/ABPC more greatly than by the administration of ABPC alone. In a similar investigation being made with clinical cases, both aerobes and anaerobes showed great changes. Concentrations of the drugs in feces increased with increasing dosage, resulting in greater changes of the intestinal bacterial flora. Thus, the total number of aerobes and anaerobes was reduced. No diarrhea was observed in any subjects examined. From the above results, it appeared that SBT/ABPC was a safe and useful antibiotic for various bacterial infections in the field of pediatrics.

Age Factors↗

[Pharmacokinetic, bacteriological and clinical studies on cefpodoxime proxetil in the field of pediatrics].

Pharmacokinetic, bacteriological and clinical studies on cefpodoxime proxetil (CPDX-PR, CS-807), a newly developed oral cephem, were carried out in the treatment of infectious diseases in the field of pediatrics. 1. Since CPDX demonstrates very powerful antimicrobial actions against such Gram-negative bacilli as Escherichia coli, Salmonella sp., Klebsiella pneumoniae and Serratia sp., such Gram-positive cocci as Streptococcus pyogenes and Streptococcus pneumoniae, and beta-lactamase producing Branhamella catarrhalis and Haemophilus influenzae, this drug was thought to be useful for the treatment of pediatric infectious diseases when main causative bacteria in the field of pediatrics were taken into account. 2. When changes in blood and urine concentrations of CPDX following the administration of this drug at 3.7 mg/kg before meal were determined, Cmax and T1/2 were found to be 2.98 micrograms/ml at 2-hour and 1.73 hours, respectively; an urinary excretion rate in the first 6 hours and a maximum urine concentration were 32.5% and 52 micrograms/ml, respectively. 3. Clinically, 8 of 8 patients with the upper respiratory tract infections (100%), 28 of 29 patients with bronchitis and/or pneumonia (96.6%), 3 of 4 patients with otitis media (75%), 2 of 2 patients with sinusitis (100%), 3 of 3 patients with the skin soft tissue infections (100%), 1 of 1 patient with bacterial enteritis (100%) and 11 of 14 patients with urinary tract infections (78.6%) responded well to the treatment with CPDX-PR, showing a 91.8% efficacy rate in all the patients treated. 4. Bacteriologically, Staphylococcus aureus, Staphylococcus epidermidis, S. pyogenes, S. pneumoniae, E. faecalis, B. catarrhalis, H. influenzae, E. coli and Salmonella typhimurium were all eradicated from 5, 1, 4, 6, 1, 5, 5, 11 and 1 patient, respectively. An eradication rate in all the patients examined was 97.5% (39/40). 5. Gastrointestinal symptoms appeared as side effects in 2 of 71 patients (vomiting in 1 and diarrhea in 1), hence, an incidence of side effects was 2.8% (2/71). As for abnormal laboratory findings, eosinophilia, thrombocytosis and increases in GOT and GPT were observed in 3 of 39 patients examined (7.7%), 1 of 39 patients (2.6%) and 2 of 34 patients (5.9%), respectively. In addition, we also examined the effect of the drug on the hemostatic system, but found no changes upon the treatment. Based on these results, it appeared that CPDX-PR was a useful and safe drug in treatment of infectious diseases in the field of pediatrics when administered 2-3 times a day at a dose of 3-6 mg/kg.

Absorption↗

[The influence of cefteram pivoxil on the intestinal bacterial flora].

The influence of cefteram pivoxil (CFTM-PI), a new oral cephalosporin, on the intestinal bacterial flora was studied in tetra-contaminated mice and in pediatric patients. CFTM-PI in fine granular form was administered at a dose of 10 mg/kg once a day for 5 consecutive days to mice contaminated with 4 different species of organisms: Escherichia coli, Enterococcus faecalis, Bacteroides fragilis and Bifidobacterium breve. No remarkable change was observed in the fecal viable cell count except that slight decrease in E. coli count was observed on days 2 to 5 after starting administration. The subjects in pediatric study were 5 children, 3 boys and 2 girls at ages from 6 months to 10 years 4 months, with infections. Their body weights ranged from 3.5 to 28.0 kg. CFTM-PI in fine granular form was administered at each dose of 3.0 to 3.8 mg/kg, 3 times daily for 5 to 11 days. During the administration of CFTM-PI, there were some variations in the change of the fecal bacterial flora noticed between subjects. Although Enterobacteriaceae tended to decrease and Enterococci tended to increase, other main aerobes and anaerobes were almost unchanged in most cases. There was no case in which glucose non-fermenting Gram-negative rods and fungi became predominant. In a 10 years 4 months old boy, the fecal concentration of CFTM, the active form of CFTM-PI, was 72.20 micrograms/g and a remarkable decrease of total anaerobe count was observed. In feces, CFTM-PI and CFTM were detected in 4 and 2 cases respectively, and their concentrations were 1.50 approximately 89.65 micrograms/g and 2.25 approximately 72.20 micrograms/g, respectively. beta-Lactamase activities in feces were positive in all cases. From the above, CFTM-PI is considered to be a drug with relatively less influence on the intestinal bacterial flora. But as high concentrations of drugs were detected in feces under some circumstances, we need to pay attention to fecal drug concentrations.

Animals↗

[A clinical study on cefteram pivoxil in pediatrics].

Clinical evaluations of cefteram pivoxil (CFTM-PI, T-2588) were carried out. The obtained results are summarized as follows. 1. Clinical responses to CFTM-PI of 39 patients with pediatric infections were excellent in 16, good in 21, fair in 1 and poor in 1. The overall efficacy rate was 94.9%. 2. Bacteriologically, eradication rates for 39 isolates presumed to be pathogens were evaluated. The eradication rates obtained were 94.1% in 17 strains of Gram-positive cocci, 90.9% in 22 strains of Gram-negative rods. 3. Side effects observed were diarrhea in 2 patients, diarrhea and abdominal pain in 1, erythema and edema in 1. The incidence was 8.7%. An abnormal value found in clinical laboratory tests was eosinophilia in 1 patient. The results suggested that CFTM-PI might be a very useful and safe drug for the treatment of pediatric infections.

Bacterial Infections↗

[Bacteriological and clinical evaluations of imipenem/cilastatin sodium in neonates and premature infants].

The antimicrobial activity of imipenem against group B streptococci was investigated. The clinical efficacy of imipenem/cilastatin sodium (IPM/CS) was determined in neonates and premature infants. The results are summarized below. 1. The distribution of MIC values of IPM against 55 clinical isolates of group B streptococci isolated from the vagina of pregnant women peaked at 0.024 micrograms/ml. MIC values of IPM against all clinical isolates tested were 0.05 microgram/ml or less. 2. IPM/CS was used for treatment of bacterial infections in 9 neonates and premature infants. Among these patients, clinical responses were excellent in 5 patients and good in 4 patients. No adverse reaction was observed. Abnormal laboratory test values were observed in 4 patients, eosinophilia in 2 patients and increased platelets in 2. 3. In 7 neonates and premature infants, quantitative cultures for aerobic and anaerobic fecal flora were performed. Fecal flora change was not significantly different than those observed during treatment with latamoxef or cefmenoxime. 4. Ten neonates and premature infants were investigated for effects of IPM/CS on the blood coagulation system. Prolongations of prothrombin time (PT) and activated partial thromboplastin time (APTT) were observed in 1 patient. Abnormal prothrombin (PIVKA II) was detected in the same patient. There was no tendency for inhibition of platelet function.

Bacteria↗

[A clinical study of rokitamycin in pediatrics].

A total of 29 patients with pediatric infections was treated orally with 21.4-44.4 mg/kg/day of rokitamycin (RKM) dry syrup. The obtained results are summarized as follows. 1. Clinical responses to RKM in 24 evaluable patients were excellent in 2 and good in 3 of 5 patients with tonsillitis and laryngitis; excellent in 3 and good in 5 of 8 patients with bronchitis; excellent in 3, good in 2 and fair in one of 6 patients with bronchopneumonia; excellent in 2 and good in the other of 3 patients with psittacosis; and excellent in 2 of 2 patients with Campylobacter colitis. The overall efficacy rate was 95.8%. 2. Bacteriological responses to the drug were: reduction in 1 and no change in the other of 2 strains of Streptococcus pyogenes; eradication of a strain of Streptococcus pneumoniae and 2 strains of Staphylococcus aureus; eradication of 2 and no change in 3 of 5 strains of Haemophilus influenzae; and eradication of 2 out of 2 strains of Campylobacter spp. 3. Diarrhea was complained of as an adverse reaction to the RKM medication by 1 patient, abdominal pain was reported by another, and anorexia by another of the 27 patients treated. Laboratory examination was performed on some patients, but not abnormal test values were found except in 1 case showing an increase in platelet count from 27.6 to 78.2 X 10(4)/mm8. The results suggested that RKM dry syrup might be a very useful and safe drug for the treatment of pediatric infections.

Administration, Oral↗

[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.

Adolescent↗

[Influence of sultamicillin on intestinal bacterial flora].

Effects of sultamicillin (SBTPC) fine granules, a new oral beta-lactam antibiotic, on the intestinal bacterial flora were studied in tetra-contaminated mice and in pediatric patients. SBTPC was administered at a dose of 100 mg/kg once a day for 5 consecutive days to mice contaminated with 4 different species of organisms: Escherichia coli, Enterococcus faecalis, Bacteroides fragilis and Bifidobacterium breve. In all of the 4 species, bacterial populations in feces were markedly reduced on days 4 to 5 after the start of the treatment. Subjects in the pediatric study were 5 children with bacterial infections (4 boys and 1 girl) at ages from 1 year 3 months to 10 years 8 months and with their body weight ranging from 11.8 kg to 35.0 kg. SBTPC fine granule was administered at a dose of 10 mg/kg 3 to 4 times a day for 4 to 7 days. Although there were some variations in the fecal bacterial flora noticed among these subjects during the treatment, populations of main aerobes and anaerobes such as Enterobacteriaceae, Enterococcus, Bacteroides and Bifidobacterium decreased markedly in all cases. These decreases were more pronounced for anaerobes and total numbers of anaerobes were markedly reduced in all cases. Glucose non-fermenting Gram-negative rods and fungi tended to increase with administration of SBTPC fine granule. Although these changes tended to return to pre-dosing state after the cessation of the treatment with SBTPC fine granule, attention must be paid to possible occurrences of diarrhea, superinfection or bleeding tendency when treatment with the drug is continued for a long period of time. Fecal concentrations of both ampicillin and sulbactam during SBTPC fine granule treatment showed relatively high values except 1 sample with a high beta-lactamase activity in feces. These high concentrations suggest the possibility of biliary excretion of absorbed drugs and the possibility of hydrolysis of SBTPC in the intestine due to high pH. Fecal concentrations of the drug also appeared to be closely related to beta-lactamase activity in feces.

Ampicillin↗

[Fundamental and clinical evaluations of ceftriaxone in neonates].

The antibacterial efficacy of ceftriaxone (CTRX) against group B Streptococcus and its clinical efficacy in newborns were examined, and the results obtained are summarized as follows. 1. MIC's of CTRX against 55 strains of B group Streptococcus from the pregnant vagina were 0.10 micrograms/ml or lower. 2. Efficacies of CTRX were good to excellent in 8 cases administered for treatment, 3 cases for prophylaxis and 1 for observation of adverse reactions. Observed adverse reactions included diarrhea in 4 cases and vomiting in 2 cases. As abnormal laboratory parameters, eosinophilia and thrombocytosis were observed in 1 case each. 3. An examination of intestinal bacteria in 9 cases revealed that CTRX gave as much influence to the flora as other third-generation cephems. 4. An examination for the vitamin K deficiency in 11 cases found a prolongation of prothrombin time (PT) in 3 cases and protein induced by vitamin K absence (PIVKA) II positive in 2 cases. 5. Testing of platelet aggregation with adenosine diphosphate (ADP) in 7 cases showed little influence of CTRX.

Ceftriaxone↗

[Evaluation of the pharmacokinetics of ceftriaxone in neonates].

A pharmacokinetic study on ceftriaxone (CTRX) was conducted and the results obtained are summarized as follows. 1. CTRX was given in a dose of 20 micrograms/kg by intravenous bolus injection to 13 neonates, and satisfactory blood concentrations of the drug were achieved. However, since even a once daily administration revealed trough values of 10-20 micrograms/ml, CTRX may accumulate if administered to neonates of low weight. 2. The rate of CTRX transfer to cerebrospinal fluid was 5.7% in a neonate given a dose of 20 mg/kg by intravenous bolus injection. 3. The urinary recovery rate was 8.4% up to 12 hours in a neonate given a dose of 20 mg/kg by intravenous bolus injection.

Bacterial Infections↗

[Comparative, controlled study on an ampicillin suppository (KS-R 1) with an oral form of ampicillin in urinary tract infections].

Subjects were in-patients with bacterial urinary tract infections, ranging in age 4 months to 11 years 4 months. As a rule, daily dose was either four 125 mg (in potency) suppositories or four 125 mg (in potency) oral form given at 6-hour intervals over a period of 5 days. The number of children subjected to this study was 105. These children were divided into 2 groups (suppository 54; oral form 51) with matched pretreatment background factors. Therapeutic effectiveness rates were 70.4% for the suppository and 66.7% for the oral form, and no significant difference was observed between the 2 groups. Rates of efficacy by severity, presence or absence of underlying and/or complication diseases, daily dose and causative microorganisms did not differ significantly between the 2 groups. There was no significant difference in time-courses of improvement of clinical signs and symptoms between the 2 groups. Eradication rates for causative microorganisms were 65.9% for the suppository and 62.5% for the oral form. Most frequently isolated causative microorganisms were Escherichia coli and Proteus mirabilis. No significant differences were recognized in the therapeutic effect and usefulness evaluated by physicians in charge. The frequency of side effects did not differ significantly between the suppository group (6 with diarrhea and 1 with anal pain: 12.1%) and the oral form group (5 with diarrhea, 1 with displeasure and 1 with vomiting: 12.7%). Abnormal laboratory findings appeared in 6 cases (2 with eosinophilia, 2 with increased GOT and 2 with increased GPT) in the suppository group and 7 cases (2 with eosinophilia, 2 with thrombocytosis, 2 with increased GOT and 1 with increased GPT) in the oral form group.

Administration, Oral↗

[Bacteriological and clinical studies on flomoxef in the pediatric field].

Bacteriological and clinical studies on flomoxef (FMOX, 6315-S) were performed and the results obtained are summarized below. 1. The MIC values of FMOX against 307 clinically isolated strains of Staphylococcus aureus were 0.024 to 100 micrograms/ml with a peak MIC of 0.39 microgram/ml, and the MIC90 value was 1.56 micrograms/ml. The MIC90 against methicillin resistant S. aureus (MRSA) was 25 micrograms/ml. 2. FMOX was administered to 15 children with pediatric bacterial infections, and the effectiveness was rated excellent or good in all cases. 3. In bacteriological evaluation, 7 of 11 strains identified prior to the treatment were eliminated (63.6%). 4. As side effects, diarrhea or soft stool was found in 3 cases and eruption in 1 case. As abnormal laboratory values, eosinophilia and thrombocytosis were found in 1 case each. 5. On the intestinal bacterial flora, FMOX had a marked influence just as did other Group 4 and 5 cephems antibiotics. 6. FMOX interfered little with the coagulation system or platelet aggregation.

Age Factors↗

[Fundamental and clinical studies of cefuzonam in pediatrics].

Fundamental and clinical studies on cefuzonam (CZON, L-105) were carried out and the results obtained are summarized below: MICs against 451 clinical isolates of Staphylococcus aureus were determined. Antibacterial activity of CZON on S. aureus was similar to that of cefazolin, inferior to that of cloxacillin, and superior to those of benzylpenicillin and cefotaxime. With one-shot intravenous injection of CZON, peak serum concentrations were 40.0 micrograms/ml and 97.5-145 micrograms/ml with a dose of 10 mg/kg and 20 mg/kg, respectively. Half-lives of the drug in serum were 34.2-47.9 minutes. Urinary excretion rates were 46.8-67.3% in 4 hours after injection. In all of 13 cases of pediatric infections tested, the clinical efficacy was excellent or good. Side effects observed were diarrhea in 4 patients, and elevated GOT and thrombocytosis in 1 patient each. From the above results, we have concluded that CZON is useful and safe antibiotic for treating various bacterial infections in children.

Age Factors↗

[A pharmacokinetic study in (mature and premature) neonates treated with amikacin through intravenous drip infusion].

A pharmacokinetic study was conducted in neonates (mature, premature) to which amikacin (AMK) was administered through intravenous drip infusion. The results of the study are summarized below. 1. Changes in blood concentrations of AMK obtained after intravenous drip infusion over a period of 30 or 60 minutes were comparable to those after intramuscular injection. 2. When AMK was administered to neonates (mature, premature) at a single intravenous (30 or 60 minutes) dose of 6 mg/kg, peak levels of 15.5 to 26.3 micrograms/ml were attained. These values were within the range of 15 to 30 micrograms/ml which are considered to be safe and effective peak levels. 3. In 0 day-neonates, half-lives of blood AMK levels rather long and widely varied (3 to 8 hours) but, in about 7 day-neonates, half-lives were 3 to 4 hours. 4. It is considered from the above results that the safe and effective blood concentrations of AMK in 0 to 7 day-old neonates can be obtained from intravenous administrations at each dose of 6 mg/kg repeated with intervals of 12 or 24 hours and, in 8 days or older neonates, from intravenous drip infusions over 30 or 60 minutes at each dose of 6 mg/kg repeated with intervals of 12 hours. 5. For neonates with very low birth weights, individual doses and intervals should be separately investigated.

Age Factors↗

[Basic and clinical studies on imipenem/cilastatin sodium in the pediatric field].

Basic and clinical studies have been performed on imipenem/cilastatin sodium (MK-0787/MK-0791) in the pediatric field. Antibacterial activities of MK-0787 against 14 clinical isolates of S. aureus and 67 isolates of E. coli were determined. The MIC of MK-0787 was 0.10 microgram/ml or less against all 14 strains of S. aureus. The MIC of MK-0787 was 0.39 microgram/ml or less against all 67 strains of E. coli. The pharmacokinetics of MK-0787/MK-0791 was studied at dose levels of 10 mg/10 mg/kg and 20 mg/20 mg/kg. The peak serum levels of MK-0787 achieved approximately 1 hour after the administration of 10 mg/10 mg/kg and 20 mg/20 mg/kg doses were 38.6 micrograms/ml and 36.2 micrograms/ml, respectively. The serum half-lives were 0.8 hour and 0.9 hour, respectively. The total 6-hour urinary excretions were 82.1% and 66.7%, respectively. The MK-0787/MK-0791 was administered to 13 children with bacterial infections. The clinical results were excellent or good in all cases. The overall efficacy rate was 100%. As a side effect, diarrhea was observed in 1 patient. Abnormalities in laboratory findings observed were elevation of direct bilirubin in 1 patient, thrombocytosis in 2, and a prolonged prothrombin time in 1 patient. Based on the above results, it can be concluded that MK-0787/MK-0791 is a safe and effective drug to use for the treatment of pediatric infections.

Bacterial Infections↗