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Biomedical subjects

Y Sakata

Publications and source records attributed to Y Sakata.

At least 433 records · Page 24Linked to original sources
PubMed1985

[Effects of KS-R1 (ampicillin suppository) and ampicillin oral dosing on fecal flora of children].

A newly developed product, KS-R1 (a suppository containing 250 mg potency of ampicillin (ABPC)), was given to 7 children (5 boys and 2 girls) ranging from 4 years and 5 months to 8 years and 10 months in age, 3 times a day (average daily dose, 62.4 mg/kg) for 5 days. As a control, the same amount of ABPC dry syrup was given orally to 7 children (4 boys and 3 girls) ranging from 2 years and 8 months to 7 years and 7 months in age, 3 times a day (average daily dose, 55.3 mg/kg) for 5 days. The effects of these 2 preparations on the bacterial flora of the feces were investigated, and concentrations of ABPC in the feces and sensitivities of the isolated strains to ABPC were determined. The results were as follows. As for Gram-negative bacilli in the feces from children given KS-R1, there was no change in Escherichia coli, Klebsiella sp., Citrobacter sp. and Enterobacter sp. which were isolated from many children 3 days after the end of treatment, but they did not show any constant pattern of change in mean number. Other species did not show any pattern of increase in the number of children from whom they were isolated, or in the number of bacteria during the course after the beginning of treatment. The total number of bacteria identified as Enterobacteriaceae was at the level of 10(8) cells/g on any day of examination. Of Gram-negative bacilli other than Enterobacteriaceae, Pseudomonas sp. showed no constant pattern of change in number. On the other hand, of Gram-positive bacteria, there was no constant pattern of change in the number of Staphylococcus aureus, Coagulase-negative Staphylococci began to be isolated from many children 5 days after the beginning of treatment and were isolated from all children 5 days after the end of treatment, but there was no tendency for the mean number to increase. Enterococcus sp. was not isolated from 3 children 3 days after the beginning of treatment, and was decreased in number by one order in 3 out of other 4 children as compared with before-treatment. However, this species was isolated from all children 3 days after the end of treatment, and the mean number of bacteria was similar to that before-treatment although the number of bacteria was different in individual children.(ABSTRACT TRUNCATED AT 400 WORDS)

Administration, Oral↗
PubMed1985

[Fundamental and clinical studies on ceftizoxime suppositories in children].

The peak levels of serum ceftizoxime (CZX) after a single rectal administration of CZX-S at doses of 125 and 250 mg in 157 pediatric patients were occurred at 21 approximately 25 minutes in pediatric patients aged less than 1 year and over than 7 years, at 16-20 minutes in 1-3 years patients, at more than 26 minutes in 4-6 years patients. They were 9.45, 9.58, 11.71, 12.43 mcg/ml, respectively. The mean highest levels of serum CZX were 8.56, 10.66, 12.50 mcg/ml after the administration of CZX-S as less than 10.0, 10.1-15.0, 15.1-20.0 mg/kg dose respectively, all of which were occurred at 21-25 25 minutes. A close dose response was observed. The pain of insertion was not observed in any cases. The discharge of melted suppository or defecation after administration was observed in 15.2% of total 184 cases, which was noticed more frequently in the lower aged children. There was no influence by dose. Clinical effects of CZX-S were studied in 72 pediatric patients with various infections. CZX-S was administered rectally at the mean daily dose of 41.0 mg/kg divided into 3 or 4 times for 6 days. Clinical responses were excellent in 46 cases, good in 24 cases, fair in 2 cases. The efficacy rate was 97.2%. Regarding side effects, the pain of insertion was noted in 2 cases (2.8%), diarrhea in 6 cases (8.3%), the elevation of eosinophil in 1 case (1.7%). Bacteriologically, 23 strains (92.0%) out of 25 strains isolated from the patients were eradicated.

Bacteria↗
PubMed1985

[Fundamental study on ceftizoxime suppositories in adults and children].

The pharmacokinetics of newly developed ceftizoxime suppository (CZX-S) was studied in healthy volunteers and in children, compared with that of intramuscular CZX and intravenous CZX: In 8 volunteers (aged 19 to 24 years), each of 500 mg (potency) CZX-S containing 3%, 4% and 5% sodium caprate was compared with 500 mg intramuscular CZX and 500 mg intravenous CZX as a single administration in the cross-over method. In addition each of 500 mg CZX-S containing 4% and 5% sodium caprate was studied in 2 groups of 8 volunteers (aged 22 to 24 years) and of 8 volunteers (aged 19 to 27 years); each CZX-S was given 3 times a day successively for 5 days. The pharmacokinetics of 125 mg and 250 mg CZX-S, which contained 3% sodium caprate, were also evaluated as a single administration in 9 children (aged 6 years 4 months to 12 years 0 month) and in 11 children (aged 7 years 8 months to 12 years 4 months), respectively. The irritabilities of CZX-S were studied in all subjects who participated in this trial. The feeling of foreign body, the feeling of defecation, the burning sensation and the pain were evaluated in volunteers; the feeling of defecation and the pain were evaluated in children. The results were as follows: I. Pharmacokinetics in healthy volunteers 1. Given as a single administration The mean peak concentrations of serum CZX were occurred 30 minutes after 500 mg CZX-S containing 3%, 4% and 5% sodium caprate, which were 10.5 mcg/ml, 12.3 mcg/ml and 12.4 mcg/ml, respectively. These values were 1.35 mcg/ml, 1.60 mcg/ml and 1.69 mcg/ml at the conversion unit of 1 mg dose per 1 kg body weight. The mean peak serum CZX concentration of CZX-S containing 3% sodium caprate was slightly lower than that of CZX-S containing 4% or 5% sodium caprate, but was 1.9 times higher than that of the ABPC suppository. There was no marked difference among 3 preparations of CZX-S in mean Tmax and T1/2. Cmax of CZX-S containing 3% sodium caprate was 1.40 mcg/ml at the conversion unit of 1 mg/kg. AUC of CZX-S containing 3% sodium caprate was slightly smaller than that of CZX-S containing 4% or 5% sodium caprate, but 3.1 times that of the ABPC suppository in healthy volunteers. When 500 mg CZX was intramuscularly administered by one shot to 8 volunteers, Tmax was same as that of CZX-S or was slightly later.(ABSTRACT TRUNCATED AT 400 WORDS)

Adult↗
PubMed1985

[Basic and clinical trials of aztreonam in the field of pediatrics].

Serum and urinary concentrations and recovery rates of aztreonam (SQ26,776, AZT), a newly developed antibiotic, were studied for a total of 20 pediatric cases by one-shot intravenous injections of 10, 20 and 40 mg/kg to 3, 4 and 3 cases, respectively, and by intravenous drip infusion of 10, 20 and 40 mg/kg to 3, 4 and 3 cases for 1 hour, respectively. Clinical and bacterial effects of AZT were studied by administering 76.7 mg/kg per day on average for a total of 36 cases of tonsillitis (6), pneumonia (13), otitis media and pneumonia complication (1), pleurisy (1), sinusitis (1) and UTI (14). The above daily dose was given t.i.d. (9 cases) or q.i.d. (27 cases), by intravenous drip infusion for 30 minutes for one t.i.d. case and by one-shot intravenous injection for 7 days for the remaining 35 cases. Also, side effect and laboratory values were examined for 43 cases including 7 dropouts. Serum concentration of AZT in 10 pediatric cases were measured by dosing 10, 20 and 40 mg/kg by one-shot intravenous injection to 3, 4 and 3 cases, respectively. In every dosage group, the serum concentrations were highest 5 minutes after the intravenous injection with average values of 91.0, 174.0 and 175.3 mcg/ml, respectively. Dose response was observed between 10 mg/kg dose group and 20, 40 mg/kg dose groups, but it was not between 20 mg/kg group and 40 mg/kg group. This was considered to be attributable to the individual case-fluctuations in the 2 groups and to a high concentration case of 240.0 mcg/ml in the 20 mg/kg group. Half-life of each dosage group was 1.55, 1.65 and 1.93 hours. Serum concentrations of AZT in 10 pediatric cases at the dosage level of 10, 20 and 40 mg/kg for 3, 4 and 3 cases, respectively, by 1 hour intravenous drip infusion were highest at the end of the administration with average values of 95.7, 126.0 and 170.7 mcg/ml, respectively. There was a dose response among the 3 groups and the half-life of them were 1.02, 1.41 and 2.48 hours, respectively. A longer half-life of the 3rd group with 40 mg/kg administration than the other 2 groups was due to 1 particular case of 4.44 hours with unknown cause of such an exceptional extension.(ABSTRACT TRUNCATED AT 400 WORDS)

Adolescent↗
PubMed1985

[Phase II study of sustained released granules of tegafur (SF-SP) on inoperable or recurrent gastric cancer].

Twenty-eight patients with inoperable or recurrent gastric cancer were entered for a phase II study of SF-SP. Of these, 24 were evaluable for response. The SF-SP was given orally at a dose of 800 to 1,200 mg/body b.i.d. daily. Six at the evaluable 24 patients showed PR, 16 NC and 2 PD. Three of the 6 PR patients were administered 1000 mg/body/day of SF-SP and the other 3, 1200 mg/body/day. The hematological toxicities were anemia (5 cases), leukopenia (3 cases) and thrombocytopenia (3 cases). The other side effects were gastrointestinal complaints, such as anorexia (5 cases), nausea (5 cases) and stomatitis (5 cases), and a further toxic effect of pigmentation (4 cases). These side effects tended to develop dose-dependently and disappeared after the SF-SP was discontinued. It was concluded that SF-SP was beneficial for the treatment of advanced gastric cancer, and that its optimal dose was 1000 mg/body/day.

Adenocarcinoma↗
PubMed1985

[Fundamental and clinical studies of aspoxicillin in the pediatric field].

Aspoxicillin (ASPC), a new semisynthesized penicillin, was administered to 20 children; by one shot intravenous injection in the doses of 10, 20 and 40 mg/kg to each of 3 children, and by intravenous drip infusion in the doses of 20 and 40 mg/kg over a period of 1 hour to 8 and 3 children, respectively, and the serum levels, urinary levels and recovery rates were determined. ASPC was administered to 1 patient with tuberculous pleurisy in the dose of 20 mg/kg by one shot intravenous injection, then the thoracic fluid level and serum level were determined. In addition, ASPC was administered to 3 children with tonsillitis, 3 with bronchitis, 40 with pneumonia, one each for pleuropneumonia, pleurisy, lung abscess, scarlet fever, staphylococcal scalded skin syndrome and purulent lymphadenitis and 2 with UTI (total 54 children), in the mean dose of 81.4 mg/kg/day t.i.d. (12 children) or q.i.d. (42 children) by one shot intravenous injection for 6 days on the average, and clinical effectiveness and bacteriological response were evaluated in these cases, and adverse reactions and abnormal laboratory findings were examined in the 60 cases which included 6 drop-out cases. After the administration of ASPC to 9 children; 10, 20 and 40 mg/kg to each of 3 children, by one shot intravenous injection, the mean serum levels reached to the peak of 58.4, 147.0 and 221.0 mcg/ml, respectively, in 5 minutes. The mean half-lives were 1.03, 1.01 and 1.23 hours, and the mean areas under the curve (AUCs) were 44.9, 94.1 and 192.9 mcg X hr/ml, respectively. A dose response was seen among the 3 dosage levels. After the administration of ASPC to 11 children; 20 and 40 mg/kg to 8 and 3 children, respectively, by intravenous drip infusion over a period of 1 hour, the mean serum levels reached to the peak of 58.2 and 114.0 mcg/ml, respectively, on completion of the administration. The mean half-lives were 1.22 and 1.09 hours, and the mean AUCs were 109.4 and 181.7 mcg X hr/ml, respectively. A dose response was observed between the 2 dosage levels. In the above mentioned each 3 cases receiving one shot intravenous injection in the dose of 10, 20 and 40 mg/kg, the mean urinary levels of ASPC reached to the peak of 1,000.0, 2,300.0 and 4,350.0 mcg/ml, respectively, at 0 approximately 2 hours after the administration, and the urinary recovery rates during the first 6 hours were 66.1, 66.5 and 56.9%, respectively.(ABSTRACT TRUNCATED AT 400 WORDS)

Amoxicillin↗
PubMed1985

[Influence of ceftriaxone on bacterial flora in human feces].

Ceftriaxone (CTRX), a newly developed antibiotic agent, was administered at 1,000 mg intravenously twice a day for 5 days to 7 healthy volunteers aged 21 to 26, weighing 61 to 79 kg (mean: 67.7 kg). The fecal bacterial flora was examined and the fecal level of CTRX was determined before, on 3 and 5 days after starting the administration, and on 3, 5 and 10 days after terminating the administration. At the same time, various bacteria isolated from the collected fecal specimens were studied for the sensitivity to CTRX, CEZ, CMZ and CTX. Adverse reactions and influence on various clinical laboratory parameters of CTRX were also examined. The results were as follows. Fecal bacterial flora: Enterobacteriaceae was at the level of 10(5) to 10(8) cells/g (mean: 10(7) cells/g) before starting the administration. The bacteria were detected from none of the 7 subjects on 5 days after starting the administration and on 3 days after terminating the administration. On 10 days after terminating the administration, the bacteria were detected in 6 out of 7 subjects at the level of 10(3) to 10(7) cells/g (mean: 10(7) cells/g). The level was the same as before starting the administration as a whole, but it had not been recovered to the initial level in any individual subject. With regard to other Gram-negative bacilli, P. aeruginosa which was isolated from none of the 7 subjects before starting the administration was detected at the level of 10(2) to 10(6) cells/g in 1 or 2 subjects on 3 days after starting, and on 3, 5 and 10 days after terminating the administration. Concerning Gram-positive bacteria, Staphylococcus sp. was isolated at the level of 10(3) to 10(4) cells/g in 3 subjects before starting the administration. The detection rate was decreased after starting the administration; it was detected in 2 and 1 subjects on 3 and 5 days after starting the administration, respectively, and in 1 subject on 3 days after terminating the administration. Then the detection rate was gradually increased; i.e., in 3 and 5 subjects on 5 and 10 days after terminating the administration, respectively. The level became gradually higher from on 5 days after terminating the administration than before starting the administration. Enterococcus sp. was isolated at the level of 10(5) to 10(8) cells/g (mean: 10(7) cells/g) in all of the 7 subjects before starting the administration. It was was detected in 1 and 4 subjects on 3 and 5 days, respectively, after starting the administration.(ABSTRACT TRUNCATED AT 400 WORDS)

Adult↗
PubMed1985

[Clinical trial of SM-4300 in the pediatric field].

SM-4300, a newly developed human immunoglobulin for intravenous use, was administered to 6 patients in the pediatric field. Two cases out of 3 cases with immunodeficiency syndrome were studied in terms of absorption and excretion of SM-4300 and all of them were observed effect of preventive bacterial infection. Three cases were administered combination therapy with SM-4300 and antibiotics. Two cases were pneumonia and 1 case was pleurisy. The following results were obtained. Two cases with immunodeficiency syndrome were observed serum levels of immuno gammaglobulin before and after administration of SM-4300. At 2-3 hours after the administration of SM-4300, the serum levels got to peak and the half-lives were 22.1 days and 22.6 days, respectively. The half-lives of SM-4300 were similar to plasmin or polyethylene glycol treated and sulfonated human immunoglobulin. The clinical effects of substitution therapy against 3 patients with immunodeficiency syndrome were observed. Through the administration of SM-4300 every 18 to 21 days for 6 months, 1 case was doing well. One case with chronic bronchitis and otitis media was hanging in the balance as well as she has been administered other immunoglobulin preparations. The last case didn't control the serum levels of immunoglobulin because he did not visit a hospital until incidence of infectious disease.

Adolescent↗
PubMed1985

Synthesis and unusual reactivity of (1,5)pyrimidino(6,9)purinophane.

In order to elucidate the driving force of the unusual high reactivity of (1,3)pyrimidino(6,9)purinophanes 2 toward nucleophiles at 6-position, title compound 1 is synthesized. It is concluded on the basis of the similar unusual behavior of 1 to 2 that the stereoelectronic effect in the fairly rigid tetrahedral intermediate is responsible for the high reactivity of 1 and 2.

Indicators and Reagents↗
PubMed1985

[Effect of aztreonam on bacterial flora in human feces].

Aztreonam (AZT), a new injectable monobactam antibiotic, was administered to 7 healthy male volunteers, aged 21-28 years (23 years, on average) and weighing 60.5-87.0 kg, (69.5 kg, on average) by one shot intravenous injection of 1,000 mg twice a day for 5 days. The effect of AZT on the fecal flora was studied 3 days before administration, on the day of the initiation, 3 and 5 days (end of the administration course) after the initiation, and 3, 5 and 10 days after the end of the administration. Fecal concentration of AZT was also studied. Also, fecal concentration and recovery rate of AZT in 4 healthy male volunteers aged 23-31 years (26 years, on average), weighing 59.5-70.5 kg (65.6 kg, on average) were measured by injecting 1,000 mg of AZT by intravenous injection only one time. Susceptibility of the bacteria isolated from the 7 cases receiving consecutive dosage to AZT, cefmetazole (CMZ), latamoxef (LMOX), cefoperazone (CPZ) and ceftazidime (CAZ) as well as side effect and laboratory values were examined with the following results. In the fecal flora, the population of Enterobacteriaceae on average was 10(7) cells/g feces on the day of the initiation and decreased by 2 logarithms to 10(5) cells/g 3 days after the initiation, 10(5) cells/g feces 5 days after the initiation with no bacterial isolation in 2 cases, 10(7) cells/g feces on 3 and 5 days after the end of administration respectively with recovery of the population to the average population on the day of the initiation. However, it increased 10 days after the end of administration with the population of 10(9) cells/g feces due to the isolation of one 10(10) cells/g feces, which was an increase by 2 logarithms as compared with average population before the administration. It was also higher than the average population 3 days before the initiation of administration. Temporal decrease or disappearance of the bacteria were noted by the administration of AZT. As to other cases of Gram-negative bacilli, Pseudomonas sp. was detected from only 2 cases 3 days before the initiation of administration and on the day of the initiation, but there was an increase to 4 and 5 cases 3 and 5 days after the initiation respectively. Number of isolation returned to 2 cases, 3, 5 and 10 days after the end of administration respectively and it was same as the number before the initiation of administration.(ABSTRACT TRUNCATED AT 400 WORDS)

Adult↗
PubMed1984

Kinetics of human pancreatic and salivary alpha-amylases with carboxymethylamyloses as substrates.

The enzymatic measurement of alpha-amylase in human serum with chemically modified amylose as substrate was studied. Several substitutions of carboxymethylamylose were prepared from amylose, suitable amounts of monochloroacetic acid, and sodium hydroxide. The relationship between the degree of substitution of the carboxymethylamylose and the kinetic parameters of human pancreatic, salivary and porcine pancreatic alpha-amylases was determined. The action of alpha-amylases on such modified amyloses in the presence of glucoamylase was measured by a specific enzymatic assay having glucose as the product. The kinetic parameters of human pancreatic alpha-amylase were similar to those of human salivary alpha-amylase. It was possible to determine suitable sensitivities for the alpha-amylase assay using this substrate. These results suggested a subsite model.

Amylose↗
PubMed1984

Differences of frequency distributions of plasminogen phenotypes between Japanese and American populations: new methods for the detection of plasminogen variants.

Frequency distributions of various plasminogen phenotypes in Japanese and American white populations were studied using electrofocusing in polyacrylamide gels followed by zymography and immunofixation. Using a synthetic substrate, tosyl-lysine-alpha-naphthyl ester, for zymography allowed zymography and immunofixation to be performed sequentially on the same gel plate. By this method, a nonfunctional abnormal plasminogen variant, plasminogen Tochigi, was readily detected in both plasma and serum. The gene frequency of this abnormal variant in a Japanese population was 0.018, whereas the abnormal variant was not detected in an American white population, suggesting the very rare occurrence of this variant in whites. Two common alleles, A and B, clearly identified in neuraminidase-treated samples, were observed at gene frequencies of 0.98 and 0.003, respectively, in the Japanese. These values are significantly different from the reported values in whites of 0.69 for A and 0.3 for B.

Gene Frequency↗
PubMed1984

Activation of brain regions in rats during food-intake operant behavior.

The central nervous structures involved in bar pressing and feeding behavior during food-intake operant behavior were investigated in rats by the [14C]-deoxyglucose ( [14C]-DG) autoradiographic technique. During bar pressing behavior, the [14C]-DG incorporation increased in the sensory-motor cortex, ventromedial thalamus, zona incerta, pars reticulata of substantia nigra, ligular cortex of the cerebellum and the reticular formation of the medulla. On the other hand, an increase of the [14C]-DG incorporation induced by feeding behavior was observed in the fornix, medial forebrain bundle, parietal cortex, trigeminal nuclei and the solitary nuclei.

Animals↗
PubMed1984

Plasminogens Tochigi II and Nagoya: two additional molecular defects with Ala-600----Thr replacement found in plasmin light chain variants.

Previous studies in our laboratories (Miyata, T., et al. (1982) Proc. Natl. Acad. Sci. U.S. 79, 6132-6136) showed that the structural defect in a hereditarily abnormal plasminogen, plasminogen Tochigi, is due to replacement of Ala by Thr at position 600 from the NH2-terminal end. In the present studies, two abnormal plasminogens, plasminogens Tochigi II and Nagoya, obtained from other family members were analyzed to identify the structural impairment in these molecules. Amino acid sequence analysis of one of the tryptic peptides isolated, respectively, from plasminogens Tochigi II and Nagoya indicated that in both cases, Ala-600 (equivalent to Ala-55 of the chymotrypsin numbering system) had been replaced by Thr. No other substitutions at the active site and substrate-binding site residues, namely, His-57, Asp-102, Ser-195, and Asp-189, were found in the plasmin light chain variants, indicating that all these residues are intact. Moreover, the NH2-terminal heptapeptide sequences of the plasmin light chain variants isolated from plasminogens Tochigi II and Nagoya were identical to the sequence determined for the normal control. These results indicate that the absence of proteolytic activity of both abnormal molecules is due to the same amino acid substitution as that of previously reported plasminogen Tochigi.

Alanine↗
PubMed1984

Pharmacokinetics and therapeutic efficacy of imipenem, ceftazidime, and ceftriaxone in experimental meningitis due to an ampicillin- and chloramphenicol-resistant strain of Haemophilus influenzae type b.

The pharmacokinetics and therapeutic efficacy of imipenem, ceftazidime, and ceftriaxone were compared with those of ampicillin and chloramphenicol in rabbits with experimental meningitis due to an ampicillin- and chloramphenicol-resistant strain of Haemophilus influenzae type b. The mean bacterial colony counts in cerebrospinal fluid were reduced by 49% (-1.85 log10 CFU/ml), 92% (-3.37 log10 CFU/ml), and 92% (-4.30 log10 CFU/ml) after a single dose of imipenem, ceftazidime, and ceftriaxone, respectively. The median peak cerebrospinal fluid bactericidal titers against this multiply resistant strain of H. influenzae were 1:4 for thienamycin, 1:16 for ceftazidime, and 1:256 for ceftriaxone. By contrast, no bactericidal activity was observed in cerebrospinal fluid and the mean concentrations of H. influenzae were either unchanged or slightly increased in animals treated with ampicillin or chloramphenicol.

Ampicillin↗
PubMed1984

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

To 6 cases of children in 2 groups of 3 each, newly developed sulbactam/cefoperazone (SBT/CPZ) was given at 20 and 40 mg/kg by intravenous bolus injection, respectively, and the serum and urinary concentrations and recoveries of SBT and CPZ were determined. To 1 case of purulent meningitis, this drug was given at 40 mg/kg by intravenous bolus injection, and the cerebrospinal fluid and serum concentrations of SBT and CPZ were determined. Susceptibility tests to SBT/CPZ and CPZ of total 289 strains were conducted; Gram-positive cocci tested consisted of 26 S. aureus strains, 20 S. pyogenes strains and 21 S. pneumoniae strains, and Gram-negative bacilli consisted of 24 H. influenzae strains, 22 E. coli strains, 26 K. pneumoniae strains, 24 E. cloacae strains, 21 E. aerogenes strains, 19 Citrobacter sp. strains, 20 S. marcescens strains, 23 P. mirabilis strains, 23 indole-positive Proteus sp. strains and 20 P. aeruginosa strains. SBT/CPZ was given to total 43 cases at a mean daily dosage of 80.4 mg/kg, in 3 or 4 divided doses (6 cases in 3 and 37 cases in 4), 1 case receiving the drug by drip infusion over 30 minutes (in 3 divided doses) and all the other 42 cases by intravenous bolus injection, for 7 days on an average. They consisted of 2 cases of tonsillitis, 1 case of otitis media, 1 case of otitis media associated with mastoiditis, 30 cases of pneumonia, 1 case of suspected septicemia, 1 case of purulent meningitis, 5 cases of urinary tract infection, 1 case of purulent lymphadenitis and 1 case of submaxillaritis. And the clinical and bacteriological effects were evaluated. Also, side reactions and laboratory examinations for abnormal values due to administration of this drug were made on 47 cases including 4 drop-outs. The following results were obtained: After administration of this drug to 2 groups of 3 children each at 20 and 40 mg/kg by intravenous bolus injection, mean serum concentrations of both SBT and CPZ reached the peaks in 5 minutes; SBT levels were 60.9 and 124.7 micrograms/ml for the 2 groups and CPZ levels were 105.0 and 214.1 micrograms/ml, respectively. In either group, CPZ levels were 1.7 times as high as SBT levels, and there was observed a dose-response in both. In the 20 mg/kg group, mean half-lives of SBT and CPZ were 0.96 and 1.24 hours, respectively, and in the 40 mg/kg group, they were 1.01 and 1.32 hours, CPZ values tending to be longer.(ABSTRACT TRUNCATED AT 400 WORDS)

Adolescent↗
PubMed1984

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

Fundamental and clinical evaluation on ceftriaxone (Ro 13-9904, CTRX), a newly-developed injectable cephem antibiotic was performed as follows. The serum and urine concentrations of CTRX as well as the urinary recovery rate were determined in 7 children at 3 different dose levels; 3 cases administered with 10 mg/kg, 3 with 20 mg/kg and 1 with 48 mg/kg by one shot intravenous injection. The concentration in the cerebrospinal fluid was determined in 1 case of purulent meningitis associated with bacteremia, administered by one shot intravenous injection with 47.6 mg/kg. CTRX was also examined in its clinical and bacteriological efficacies by one shot intravenous injection for 8 days on average in a mean daily dose of 46.5 mg/kg, divided into twice a day in 31 cases, 3 times in 1 case, and 4 times changed from twice in 1 case; in a total of 33 children consisting of 3 with tonsillitis, 1 with chronic bronchitis, 20 with pneumonia, 2 with purulent meningitis associated with bacteremia, 3 with urinary tract infections, 1 with osteomyelitis associated with phlegmon, 3 with purulent lymphadenitis. The adverse reactions and laboratory test values were examined in a total of 40 cases, i.e., the above-mentioned 33 cases plus the 7 drop-out cases in which the clinical efficacy could not be evaluated. The results were as follows. The serum levels of CTRX in 7 cases consisting of 3 administered with 10 mg/kg, 3 with 20 mg/kg and 1 with 48 mg/kg reached their peaks 5 minutes after one shot intravenous injection and the mean values of them were 93.6 mcg/ml, 143.0 mcg/ml and 558.0 mcg/ml, respectively, indicating the existence of a dose-response among these groups, while the half-life times were 4.41, 5.86 and 4.09 hours. Among the 7 cases examined in the urinary levels as well as the serum levels, the 3 cases administered with 10 mg/kg reached the mean peak of 334.0 mcg/ml 2 to 4 hours after administration, while another 3 cases administered with 20 mg/kg showed peaks of 793.0, 522.0 and 536.0 mcg/ml, respectively, 2 to 4 hours, 4 to 6 hours and 6 to 12 hours after injection; this dispersion being partly because of that the urine specimen was unable to be collected regularly every hour in this dose group. In the case administered with 48 mg/kg, urinary level reached the highest value of 6,100.0 mcg/ml from 0 to 2 hours.(ABSTRACT TRUNCATED AT 400 WORDS)

Age Factors↗