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Biomedical subjects

K Sunakawa

Publications and source records attributed to K Sunakawa.

At least 109 records · Page 6Linked to original sources

[Influence of cefroxadine dry syrup on intestinal bacterial flora].

Influence of cefroxadine (CXD) dry syrup on intestinal bacterial flora was studied in mice infected with 4 species of bacteria, namely, Escherichia coli, Enterococcus faecalis, Bacteroides fragilis and Bifidobacterium breve, and in pediatric patients having infections in the respiratory tract and cutaneous/soft tissues. The results were summarized as follows: CXD dry syrup was administered for 5 consecutive days to mice infected with the 4 species. No considerable changes were observed in levels of bacteria in the feces and in different parts of digestive tracts. Eleven pediatric patients were orally administered with 30-54 mg/kg of CXD dry syrup a day for 7-15 consecutive days. Symptom of diarrhea was noted in 2 patients. Dominant species of the intestinal flora such as E. coli, Bifidobacterium, and Bacteroides sometimes decreased in patients treated with CXD dry syrup. In general, however, decreases in numbers of these bacteria were insignificant. Changes of intestinal flora in patients treated with CXD dry syrup were apparently smaller than those treated with ampicillin and were similar to those treated with cephalexin or amoxicillin.

Animals↗

[Pharmacokinetic and clinical evaluation of ceftazidime in neonates and premature infants].

Pharmacokinetics and clinical efficacy of ceftazidime (CAZ) were evaluated in neonates. The results obtained are summarized below. After a bolus intravenous injection of 20 mg/kg CAZ to neonates, peak serum concentrations ranged 55.1-97.4 micrograms/ml with the mean half-life of 2.26 hours in neonates with birth weight of 2,500 g or more, and 59.3-60.7 micrograms/ml with half-lives ranging from 3.98 to 4.22 hours in neonates weighing less than 2,500 g at birth. In the time-course observation, it was noted that the half-life at 2 days after birth was longer than half-lives observed on 4 and 9 days after birth. Four cases were given CAZ for treatment, and 3 cases for prophylaxis of infections, and the clinical efficacy was either excellent or good in all of the cases. Neither adverse effects nor abnormal laboratory findings were observed except rash in 1 case. Intestinal flora was examined in 5 cases. It was found that the effect of CAZ was less than that of LMOX, although some delay was seen in the growth of intestinal flora. There was no vitamin K deficiency in any of 6 cases examined.

Bacterial Infections↗

[Basic and clinical studies of cefotiam in neonates and premature infants].

The effect of cefotiam (CTM) on neonates and premature infants was examined in basic and clinical studies. Minimum inhibitory concentrations of CTM against 190 clinically isolated strains kept by this department were investigated. This drug was found to have a strong antibacterial effect against Escherichia coli, Klebsiella spp., Proteus mirabilis and Streptococcus agalactiae, Staphylococcus aureus and Staphylococcus epidermidis, although some strains were resistant. The CTM was given to 0-3, 4-7, and greater than or equal to 8 day-old premature infants and neonates by intravenous injection at the dose of 20 mg/kg, and we studied changes in serum CTM levels over time. Mean serum CTM levels were 62.3 micrograms/ml at 15 minutes and 16.4 micrograms/ml at 6 hours after the injection, with the half-life of 3.6 hours, for the 0-3 day-old premature infants. They were 38.5 micrograms/ml at 15 minutes and 10.1 micrograms/ml at 6 hours, with the half-life of 2.9 hours, for the 0-3 day-old neonates. Those levels were 22.5 micrograms/ml at 15 minutes and 2.9 micrograms/ml at 6 hours, with the half-life of 1.9 hours, for the 4-7 day-old neonates, and 51.8 micrograms/ml at 15 minutes and 1.0 micrograms/ml at 6 hours, with the half-life of 1.1 hours, for the greater than or equal to 8 day-old neonates. The CTM was given to 0-3 and greater than or equal to 8 day-old premature infants and neonates by 1-hour intravenous drip infusion at the dose of 20 mg/kg, and changes in serum CTM levels after the infusion were followed. The 0-3 day-old premature infant (there was only one subject) had a peak serum CTM level of 21.0 micrograms/ml 1 hour after the start of the infusion (that is, at the time of its completion), with the level decreased to 8.6 micrograms/ml at 7 hours and the half-life was 5.4 hours. The mean peak serum CTM level in 0-3 day-old neonates were 36.7 micrograms/ml at 1 hour, which decreased to a mean of 7.0 micrograms/ml at 7 hours; the half-life was 2.3 hours.(ABSTRACT TRUNCATED AT 400 WORDS)

Bacterial Infections↗

[Fundamental and clinical studies of cefixime granules in pediatrics].

Fundamental and clinical studies of cefixime (CFIX) granules, a new oral cephalosporin, were carried out with the following results: The MICs of CFIX against 234 clinical isolates were determined. Antibacterial activities of the drug against S. aureus, S. epidermidis and E. faecalis were weaker than those of conventional oral cephalosporins but antibacterial activities against Gram-negative bacteria were almost the same as those of cephem antibiotics of the Fujii's group 5. Peak serum concentrations of CFIX after oral doses of 3 and 6 mg/kg were, respectively, 1.51-4.86 micrograms/ml at 2-6 hours and 3.22-7.76 micrograms/ml at 4-8 hours. Serum concentrations of CFIX were dose-dependent in a patient given 3 and 6 mg/kg in a cross-over study. CFIX granules were administered mainly to children suffering from respiratory tract infection, otitis media and urinary tract infection at a dose of 3 mg/kg b.i.d. or t.i.d. for 3-27 days. The clinical responses to CFIX were excellent to good in 44 of the 50 children with infections, with an effectiveness rate of 88%. Thirty-five strains of the 40 clinical isolates were eradicated by the treatment with CFIX. The bacteriological eradication rate was 87.5%. Side effects observed were diarrhea and soft stool in 2 patients each, and elevated GOT X GPT and eosinophilia in 1 patient each. These symptoms and laboratory abnormalities disappeared on the day after the completion of therapy with CFIX. From the above results it has been concluded that CFIX is a useful and safe antibiotic for treating various bacterial infections in children.

Adolescent↗

Clinical superinfection and its attendant symptomatic changes in pediatrics.

Studies were conducted on the effects of antibiotics on intestinal bacterial flora and symptomatic changes associated with possible superinfection following antibiotic treatment. Following the administration of oral antibiotics, there were no marked changes in the intestinal flora. After second and third-generation cephems were injected, most bacteria, excluding Streptococcus faecalis which is resistant to them, decreased and fungi increased. The incidences of diarrhea after administering oral antibiotics were high for amoxicillin and amoxicillin + clavulanic acid. In some patients with depressed immunity, such as leukemic patients and neonates, decreases in intestinal bacteria after doses of antibiotics led to increases in pathogenic bacteria. They invaded the circulating blood, leading to septicemia. Septicemia originating in the intestinal tract was frequently associated with the development of vitamin K deficiency. Besides changes in the intestinal flora, a decrease in oral food intake and the presence of a methylthiotetrazole group in the structure of the administered antibiotics were also found to play a crucial role in causing vitamin K deficiency.

Anti-Bacterial Agents↗

[Clinical studies of ceftizoxime suppositories in the pediatric field].

Ceftizoxime suppository (CZX-S) was given to 19 children with infections, including upper and lower respiratory tract infections, urinary tract infections and otitis media at dose level of 18-83 mg/kg/day divided into 2-3 times. Clinical response was excellent in 12 patients, good in 6 patients and poor in 1 patient. Bacteriological response was eradicated in 11 strains, decreased in 3 strains and unchanged in 4 strains. No severe side effects were observed with this drug. These results obtained suggest that CZX-S should be a useful antibiotic in treatment of infections in pediatric field.

Bacteria↗

[Experimental and clinical studies on BRL 25000 (clavulanic acid-amoxicillin) granules in the pediatric field].

BRL 25000 is a preparation comprising 2 parts of amoxicillin (AMPC) to 1 part of clavulanic acid (CVA). Basic and clinical studies have been performed on BRL 25000 granules in the pediatric field. The antibacterial activities of BRL 25000 and AMPC against 48 strains of E. coli isolated from patients with urinary tract infections were studied. The MICs of BRL 25000 were all below 100 micrograms/ml, except for 1 strain with MIC greater than or equal to 800 micrograms/ml. However, 19 strains (40%) were resistant to AMPC, with MICs more than 800 micrograms/ml. BRL 25000 granules were administered to 23 children with bacterial infections and the clinical response was assessed as excellent in 10, good in 9, fair in 3, poor in 1, giving an overall efficacy rate of 83% (19/23). Isolated organisms were eradicated in 12 out of the 16 strains which were evaluated bacteriologically. Changes in intestinal bacterial flora following administration of BRL 25000 granules were studied in several children and decreases in flora were observed in some cases. No severe side effects were observed although three seemed to be a slightly higher incidence of diarrhea than with other drugs.

Administration, Oral↗

[Bacteriological, pharmacokinetic and clinical studies on aztreonam in the pediatric field. Pediatric Study Group of Aztreonam].

This report summarizes the results of joint studies in pediatrics on aztreonam, the first monobactam antibiotic for practical use. Pharmacokinetics was studied in 53 cases administered with 10, 20, 40 and 50 mg/kg of aztreonam (AZT) by intravenous injection and 20 cases with 10, 20, 30, and 40 mg/kg by drip infusion. All the cases had normal hepatic and renal functions at the administration. T1/2 was in a relatively fixed range of 1.35-1.56 hours in intravenous injection cases and 1.30-1.55 hours in drip infusion. One hour after commencing administration of standard 20 mg/kg, the serum concentrations were 50.18 +/- 4.24 micrograms/ml in intravenous injection and 116.33 +/- 10.18 micrograms/ml in drip infusion and even 6 hours after the end of the administration, they were 5.80 +/- 1.16 micrograms/ml and 3.38 +/- 0.58 micrograms/ml, respectively. The cerebrospinal fluid penetration was studied on suppurative meningitis (5 cases) and nonbacterial meningitis (3 cases). The penetration was generally good with sufficient concentration for meningitis caused by E. coli and H. influenzae. Amount of the penetration decreased as the cases were improved. Twenty-nine (29) cases were excluded and 262 cases of total 291 were clinically assessed, and the pathogen-isolated 167 cases of 262 were principally analyzed. Efficacy of AZT was "excellent" for all 3 cases of E. coli sepsis and 1 case of N. meningitidis meningitis and "good" for 1 case of H. influenzae meningitis. The effective rate was 94.6% for 37 pneumonia cases, 94.7% for 76 UTI cases and 88.5% on the whole including as many as 98 "excellent" cases. However, the effective rate for 21 enteritis cases was only 52.4%. Similar trend was observed in the pathogen-unknown group and overall effective rate of total 267 cases was 86.8%. The clinical effect by pathogen was 97.7% for 44 E. coli cases and 97.1% for 34 H. influenzae cases, showing excellent results for the GNB group. AZT was also effective for 8 out of 11 P. aeruginosa cases. With regard to microbiological effect by pathogen, AZT showed a high rate of bacterial elimination for GNB, primarily 98.1% for E. coli and 100% for H. influenzae followed by 76.9% for P. aeruginosa. However, it was only 30.0% for Salmonella. Excluding the Salmonella cases, GNB elimination rate was 93.5%. Clinical and microbiological dose response was not clear partly because, same as the previous studies, the effective rate of AZT was high. It was considered, however, standard dose of 20 mg/kg X 3 approximately 4 times a day was recommendable.(ABSTRACT TRUNCATED AT 400 WORDS)

Age Factors↗

[Fundamental and clinical studies on aztreonam in pediatrics].

Fundamental and clinical results of AZT in pediatrics were as follows. Pharmacokinetics of AZT was studied for 1 case with resulting high serum concentration and a half-life of approximate 1 hour. AZT was administered to 10 patients with bacterial infections with 100% clinical efficacy and 62.5% bacterial elimination. Side effect was 1 case of diarrhea. There were no abnormal laboratory or coagulation test findings nor vitamin K deficiency, platelet hypofunction or effects on intestinal bacterial flora. AZT was considered to be high in safety. The administration of 20 mg/kg AZT 3 times a day was considered to be an effective treatment for pediatric Gram-negative infections.

Adolescent↗

The influence of cefotaxime on intestinal flora and bleeding diathesis in infants and neonates, compared with other beta-lactams.

Various second- and third-generation cephem antibiotics were administered to infants 2 years of age or less. Excluding Streptococcus faecalis, which is resistant to cephems, all of the intestinal bacteria decreased in number, and in many cases these were replaced by yeasts. A positive reaction for protein induced by vitamin K absence or antagonism (PIVKA II) occurred in 25 to 63% of the subjects administered cephems possessing a methylthiotetrazole group, but not in those dosed with cefotaxime or ceftazidime. The effects of cefotaxime and latamoxef (moxalactam) on platelet ADP aggregation were also investigated. When these drugs were administered to clinical patients, moxalactam showed stronger inhibition of aggregation than cefotaxime.

Adenosine Diphosphate↗

[Fundamental and clinical studies of sulbactam/cefoperazone in the pediatric field].

Fundamental and clinical studies were carried out on sulbactam/cefoperazone (SBT/CPZ) in the field of pediatrics. The following results were obtained: A total of 185 clinical isolates that had been stocked at our department was employed to determine the minimum inhibitory concentrations (MICs) of SBT/CPZ against various bacterial species. SBT/CPZ showed strong antibacterial potency against E. coli, Salmonella, Klebsiella and P. mirabilis, and relatively strong potency against S. marcescens, P. aeruginosa and S. aureus. Antibacterial potency of SBT/CPZ was stronger than that of CPZ alone against E. coli, and it also showed strong activity against strains of Salmonella, S. marcescens and S. aureus, moderately or highly resistant to CPZ. SBT/CPZ was administered by intravenous bolus infusion to pediatric patients to determine the serum concentrations of SBT and CPZ. At a dose of 10 mg/kg the mean serum levels of SBT and CPZ were as follows; 17.8 micrograms/ml, 40.7 micrograms/ml at 15 minutes and 0.3 microgram/ml at 6 hours, respectively. The half-lives of SBT and CPZ in the serum were 1.05 hours and 1.76 hours, respectively. Similarly, at a dose of 20 mg/kg the mean serum levels of SBT and CPZ were; 31.9 micrograms/ml, 81.0 micrograms/ml at 15 minutes and 0.5 microgram/ml, 6.1 micrograms/ml at 6 hours, and the half-lives were 1.00 hour and 1.72 hours, respectively. At a dose of 40 mg/kg, only 1 case was determined. The serum levels of SBT and CPZ were 34.4 micrograms/ml, 74.8 micrograms/ml at 30 minutes and 0.2 microgram/ml at 6 hours, and the half-lives were 0.78 hour and 1.38 hours, respectively. SBT/CPZ was drip-infused intravenously over a period of 1 hour, and the serum concentrations of SBT and CPZ were determined. At the dose of 10 mg/kg or 20 mg/kg, the peak serum levels of SBT and CPZ were observed at 1 hour or at the end of drip infusion. At a dose of 10 mg/kg the mean serum levels of SBT and CPZ were 14.4 micrograms/ml, 33.7 micrograms/ml at 1 hour and 1.4 micrograms/ml, 4.6 micrograms/ml at 7 hours, respectively. The half-lives was 1.86 hours for SBT and 2.23 hours for CPZ, respectively. Similarly at a dose of 20 mg/kg, the mean serum levels of SBT and CPZ were, 22.2 micrograms/ml, 34.6 micrograms/ml at 1 hour and 0.5 microgram/ml, 2.8 micrograms/ml at 7 hours, and the half-lives was 1.17 hours and 1.75 hours, respectively. The urinary recovery rate was determined for the 6 hours period after administration.(ABSTRACT TRUNCATED AT 400 WORDS)

Age Factors↗

[Fundamental and clinical evaluation of ceftriaxone in the pediatric field].

Fundamental and clinical evaluation of ceftriaxone (CTRX) was performed in the pediatric field and the following results were obtained. The MIC of CTRX against E. coli isolated from urinary tract infections in children ranged from less than or equal to 0.024 to 0.39 mcg/ml except for 1 strain. CTRX was superior to other 3rd generation cephalosporins such as CPZ and LMOX, showing effectiveness also against ABPC-resistant bacteria. The clinical efficacy and bacteriological efficacy in 6 children consisting of 5 with respiratory tract infections and 1 with urinary tract infection were 83% and 100%, respectively. As to the adverse reaction, diarrhea was observed in 2 cases. The determination of PIVKA-II performed during the therapy with CTRX, which is observed when vitamin K is deficient, showed positiveness in 2 cases out of 6 cases including 1 which the clinical efficacy could not be evaluated. The test of platelet function in 3 cases found no inhibition of agglutination. Twice-daily administration with 20 mg/kg CTRX was considered to be a useful and safe method for treatment of bacterial infections in children, although attention should be taken not to cause vitamin K deficiency as in other 2nd and 3rd generation cephalosporins.

Cefotaxime↗

[Basic and clinical studies on ceftazidime in the pediatric field].

Basic and clinical studies were made on ceftazidime (CAZ) in pediatric field, and the following results were obtained. The antibacterial activity of CAZ against clinically isolated and maintained strains was examined. CAZ was unequivocally more active than CEZ and CMZ against Gram-negative rods, with MIC distribution similar to that of CTX, except for that for P. aeruginosa. The MIC of CAZ was lower than that of CTX for P. aeruginosa. Compared with the MICs of CEZ, CMZ and CTX, CAZ showed slightly higher MICs for Gram-positive bacteria. The blood concentrations of CAZ, at 0.25, 0.5, 1, 2, 4 and 6 hours after a one shot intravenous injection of 10 mg/kg of CAZ were 64.9, 36.9, 28.3, 14.7, 4.92 and 2.42 micrograms/ml, respectively, with the half-life of 1.27 hours. The blood concentrations of CAZ, at 0.25, 0.5, 1, 2, 4 and 6 hours after a 1-hour drip infusion of 10 mg/kg of CAZ were 16.6, 24.5, 41.4, 17.1, 5.38 and 2.62 micrograms/ml, respectively, with the half-life of 1.28 hours. The blood concentrations of CAZ, at 0.25, 0.5, 1, 2, 4 and 6 hours after a one shot intravenous injection of 20 mg/kg of CAZ were 73.1, 60.8, 39.3, 17.3, 8.23 and 4.45 micrograms/ml, respectively, with the half-life of 1.42 hours. The blood concentrations of CAZ, at 0.5, 1, 2, 4 and 6 hours after a 1-hour drip infusion of 20 mg/kg of CAZ were 55.1, 69.0, 32.1, 11.4 and 4.56 micrograms/ml, respectively, with the half-life of 1.27 hours. Urinary recovery rate of CAZ during the first 6 hours after a one shot intravenous injection of 10 mg/kg of CAZ was 86.7%. CAZ was administered to 17 children with infections, and the clinical response was excellent or good in 94%. CAZ was bacteriologically effective in 14 patients, all bacteria having been eradicated in them. The bacteria were E. coli in 10 patients, H. influenzae in 2, P. aeruginosa in 1 and S. pneumoniae in 1. As for side effects, slight elevation in GOT was observed in 1 case and eosinophilia, in another case.

Adolescent↗

[Pharmacokinetic and clinical studies of latamoxef (moxalactam) in neonates and premature infants].

Studies were carried out on the in vivo kinetics and clinical efficacy of latamoxef (LMOX) in neonates and premature infants. The results are summarized below. Serum concentration and T1/2 following intravenous injection of LMOX to neonates LMOX was intravenously administered to neonates as one shot doses of 10 mg/kg and 20 mg/kg. The serum concentration of LMOX showed a dose-response to the 10 and 20 mg/kg doses in each of the 0--3 day-old group, 4--7 day-old group and 8--28 day-old group. The T 1/2 values were as follows; for the 10 mg/kg dose, 5.17 hours in the 0--3 day-old group, 3.28 hours in the 4--7 day-old group and 2.79 hours in the 8--28 day-old group; for the 20 mg/kg dose, 5.58 hours in the 0--3 day-old group, 3.46 hours in the 4--7 day-old group and 3.14 hours in the 8--28 day-old group. Thus, it is seen that the half-life of both dosages decreased as the infants became older. Serum concentration and T 1/2 following intravenous injection of LMOX to premature infants Similar to the case of neonates described above, the concentration of LMOX in the serum of the premature infants showed a dose-response to the 10 mg/kg and 20 mg/kg dosages. The T 1/2 values for the 0--3, 4--7 day-old and 8--28 day-old groups were 7.54, 3.93 hours and 6.25 hours, respectively, for the 10 mg/kg dose, and 10.8, 4.05 hours and 3.23 hours, respectively, for the 20 mg/kg dose. Again, it is seen that the half-life of both dosages decreased as the age of the prematurely-born infants increased. Serum concentration and T1/2 following 1-hour intravenous drip infusion of LMOX to neonates LMOX was administered to neonates in doses of 10 mg/kg and 20 mg/kg, by i.v. drip infusion over a 1-hour period. With both dosages, the peak serum concentration of LMOX occurred at the time of completion of the infusion. The T1/2 values for the 0--3, 4--7 day-old and 8--28 day-old groups were 5.41, 3.68 hours and 1.92 hours, respectively, for the 10 mg/kg dose, and 5.31, 2.67 hours and 4.86 hours, respectively, for the 20 mg/kg dose. Urinary excretion of LMOX in neonates and premature infants. The percentage of the administered LMOX dose contained in the urine excreted during the 6-hour period following intravenous administration of LMOX to neonates and premature infants was determined.(ABSTRACT TRUNCATED AT 400 WORDS)

Humans↗