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Y Taneda

Publications and source records attributed to Y Taneda.

At least 19 recordsLinked to original sources

[Variation of chemical constituents in processed licorice roots: quantitative determination of saponin and flavonoid constituents in bark removed and roasted licorice roots].

As a continuing study of chemical characterization of crude drug processing, we have been analyzing the chemical constituents in licorice roots before and after processing. At first, we analyzed chemical constituents in licorice roots of various origins. Next, we have developed the HPLC analytical method, by which saponins and flavonoids, major constituents in various licorice roots, were determined simultaneously in a quantitative manner. In this paper, by means of the HPLC analytical method, chemical constituents in licorice roots, processed and unprocessed, were determined. It was found that nonglycosidic flavonoid constituents were mostly lost while root bark removing, whereas, in roasted licorice roots, sugar chains in the saponin and glycosidic flavonoid constituents were hydrolyzed stepwise during roasting through hydrothermolysis.

Chromatography, High Pressure Liquid↗

Studies of the neutral trisaccharides of goat (Capra hircus) colostrum and of the one- and two-dimensional 1H and 13C NMR spectra of 6'-N-acetylglucosaminyllactose.

Four neutral trisaccharides were isolated from goat colostrum by dialysis, and ion-exchange, activated charcoal column, preparative paper, and Bio-Gel P-4 column chromatography. The following structures were elucidated by GC analysis of hydrolysis products and by 400-MHz 1H NMR spectroscopy: alpha-L-Fuc p-(1-->2)-beta-D-Gal p-(1-->4)-D-Glc, alpha-D-Gal p- (1-->3)-beta-D-Gal p-(1-->4)-D-Glc, beta-D-Gal p-(1-->3)-beta-D-Gal p-(1-->4)-D-Glc, and beta-D-Gal p-(1-->6)-beta-D-Gal p-(1-->4)-D-Glc. beta-D-Glc pNAc-(1-->6)-beta-D-Gal p-(1-->4)-D-Glc, previously reported to be present in goat milk, was not detected in this study. beta-D-Glc pNAc-(1-->6)-beta-D-Gal p-(1-->4)-D-Glc (6'-N- acetylglucosaminyllactose) was prepared by beta-D-galactosidase digestion of beta-D-Gal p-(1-->3)[beta-D-Glc pNAc-(1-->6)]-beta-D-Gal p-(1-->4)-D-Glc (lacto-N-novotetraose) and characterized by one- and two-dimensional NMR spectroscopy at 600 MHz.

Animals↗

Chemical characterization of sialyl oligosaccharides isolated from tammar wallaby (Macropus eugenii) milk.

Two components of the sialyl oligosaccharides were separated from milk of the tammar wallaby (Macropus eugenii) by gel filtration and ion exchange chromatography. Their molecular weights, estimated by gel filtration on HPLC using 5 mM triethylamine-acetate buffer (pH 5.0), were approx. 3,000. Their monosaccharide compositions, determined by GC analysis after methanolysis and by colorimetric assay, were (Glc)1(Gal)9(GlcNAc)2(Neu5Ac)1, and (Glc)1(Gal)8(GlcNAc)2(Neu5Ac)2. Their chemical structures were further elucidated by 1H-NMR and methylation analysis. The results suggest that their approximate structures are: [formula: see text]

Animals↗

[Pharmacokinetic and clinical evaluation of cefozopran in the pediatric field].

We conducted a pharmacokinetic and clinical studies on cefozopran (CZOP), a new cephem antibiotic for injection. 1. Changes in serum levels of the agent after intravenous bolus injection at a dose of 20 mg/kg to 4 pediatric patients (age: 5-10 years) were observed. The levels at 30 minutes after injection were 32.9-73.4 micrograms/ml average: 55.4 +/- 18.1 micrograms/ml), then the levels gradually decreased with half-lives of 1.67-2.24 hours (average: 1.85 +/- 0.27 hours) to 0.8-1.8 micrograms/ml (average: 1.2 +/- 0.4 micrograms/ml) at 8 hours after injections. Urinary levels reached at the maximum as, 1,773-3,450 micrograms/ml (average: 2,693 +/- 698 micrograms/ml) within 0-2 hours or 2-4 hours after injection, and recovery rates from urine in the first 8 hours after injection were 55.4-91.1% (average: 71.6 +/- 16.8%). 2. Transition to cerebrospinal fluid was examined in cases with purulent meningitis and aseptic meningoencephalitis. In the meningitis case, the level in cerebrospinal fluid 1 hour after administration was 8.8 micrograms/ml in the second day after the start of 4 times a day intravenous bolus injections with 42.5 mg/kg at each dose; The ratio of the drug level in cerebrospinal fluid to that in serum was 24.0%. In the meningoencephalitis, the levels in cerebrospinal fluid 1 hour after administrations were 1.1 micrograms/ml and 1.5 micrograms/ml in the second and the sixth days respectively, after the start of 4 times a day intravenous bolus injections with 50 mg/kg at each dose; the ratio of the levels in cerebrospinal fluid to those in sera were 0.93% and 2.41% respectively, at the second and the sixth day. 3. CZOP was clinically evaluated in 29 cases (ages: 2 months to 15 years) of pediatric infectious diseases. The agent was administered 3-4 times daily with 17-50 mg/kg at each dose, continued for 5-13 days. Total doses were 1.95-24.05 g. Clinical efficacy was evaluated in a total of 28 cases (1 case of purulent meningitis, 2 cases of acute purulent tonsillitis, 20 cases of acute pneumonia, 3 cases of urinary tract infections, 1 case of purulent lymphadenitis in cervical part and 1 case of cellulitis in face); The efficacies were "excellent" in 22 cases and "good" in 6 cases.(ABSTRACT TRUNCATED AT 400 WORDS)

Acute Disease↗

[Pharmacokinetic, bacteriological and clinical evaluation of biapenem (L-627) in the pediatric field].

Pharmacokinetic, bacteriological and clinical studies on biapenem (L-627), a newly developed carbapenem antibiotic, were performed in the field of pediatrics. 1. Antibacterial activities of biapenem against 54 strains of Streptococcus pneumoniae isolated in 1993 were compared with those of 13 other antibiotics, consisting primarily of beta-lactam compounds. Minimal inhibitory concentrations (MICs) of biapenem were < or = 0.78 micrograms/ml against all strains, and excellent values were obtained even against benzylpenicillin (PCG)-resistant strains. Based on MIC80 values, biapenem, imipenem, and cefuzonam showed highest antibacterial activities, followed by cefotaxime. 2. Blood concentrations and urinary excretion were studied after intravenous drip infusion of 6.0 mg/kg and 6.1 mg/kg of biapenem, given over 30 min., to two children (ages: 4 years and 11 years). Blood drug concentrations were 14.7 and 37.6 micrograms/ml, respectively (mean: 26.2 micrograms/ml), at 30 min. after starting infusion (at completion of infusion). Blood concentrations then declined gradually with half-lives of 0.66 and 1.16 hrs., respectively (mean: 0.91 hrs.). After 5.5 hrs., blood concentrations were no longer measurable in the former and 0.46 micrograms/ml in the latter. Urinary recovery rates of drug in the first 6 hrs. after starting administration were 65.8% and 60.9%, respectively (mean 63.4%). 3. Penetration of the drug to the cerebrospinal fluid (CSF) was studied in 2 patients with purulent meningitis. Biapenem, 31.6 mg/kg, was administered four times daily by 30-min. intravenous drip infusion. CSF concentration 1 hr. after administration was 8.54 micrograms/ml on the day of the start of treatment (day 0), and 3.00, 2.04, 16.1, 4.16, 3.24, and 1.60 micrograms/ml on days 1-7 of treatment, respectively. In a patient similarly administered with the drug at 33.7 mg/kg four times daily, the CSF concentration at 1.5 hrs. after administration was 2.62 micrograms/ml on the next day of the start of treatment. On days 2-7 of treatment, CSF concentrations at 0.5-1 hr. after administration were 4.60, 12.9, 20.6, and 1.32 micrograms/ml, respectively. 4. Clinical efficacy was evaluated in 27 patients with pediatric infections. The dose administered per dosage was 5.2-33.7 mg/kg. Three or four dosages were given daily. The duration of therapy ranged from 3 1/3 to 11 days. Total administered doses were between 0.675 and 20.475 g. Clinical efficacy was evaluated in a total of 24 patients (purulent meningitis 1, acute otitis media 1, acute bronchitis 2, acute pneumonia 19, acute urinary tract infection 1). Responses to treatment were excellent in 14 patients and good in 10 patients.(ABSTRACT TRUNCATED AT 400 WORDS)

Adolescent↗

Insulin stimulates hydrolysis of plasmanylinositol-glycan and phosphatidylinositol-glycan in rat adipocytes. Insulin-induced generation of inositol glycan, alkylacylglycerol, and diacylglycerol.

Insulin binding to its receptor has been known to induce hydrolysis of phosphatidylinositol-glycan and release inositol-glycan and diacylglycerol, two putative second messengers of insulin actions. We metabolically labeled and purified PIG in rat cultured adipocytes. The treatment of [3H]glycerol-labeled PIG with phosphatidylinositol-specific phospholipase C released [3H]glycerol-labeled DAG and [3H]glycerol-labeled 1-alkyl,2-acyl-glycerol, suggesting that PIG has not only PIG but also plasmanylinositol-glycan moiety. Insulin induced hydrolysis of PIG/PMIG and generation of IG, DAG, and AAG in a dose-dependent manner. This report shows the first demonstration of insulin-sensitive PMIG in rat adipocytes. These results provide evidence that insulin-induced generation of IG, DAG, and AAG might be early events in the insulin-signaling mechanism in rat adipocytes, and insulin-releasable AAG seems to mediate some actions of insulin.

Adipose Tissue↗

Mutated insulin receptor Val996 reduces insulin-dependent generation of inositol glycan and diacylglycerol.

We evaluated whether insulin-receptor tyrosine kinase activity is required for activation of PDH, insulin-induced hydrolysis of PIG and generation of IG and 1,2-DAG. For the analysis, we used stable-transfected CHO cell lines expressing wild-type human insulin receptor (CHO-wt cells) or the mutant receptor (Val996) that lacks tyrosine kinase activity (CHO-mut cells) (1,2). Insulin stimulated PDH activity in three CHO cell lines in a dose-dependent manner. Half-maximal concentrations of insulin to activate PDH was 7 x 10(-11) M in the CHO-wt cells, 10(-9) M in the parental cells, and 8 x 10(-9) M in the CHO-mut cells. Insulin stimulated hydrolysis of PIG and generation of IG and DAG in three CHO cell lines in a dose-dependent manner. Half-maximal concentrations of insulin to induce generation of IG was 8 x 10(-11) M in the CHO-wt cells, 10(-9) M in the parental CHO cells, and 10(-8) M in the CHO-mut cells. ED50 for the stimulation of DAG generation was 7 x 10(-11) M in the CHO-wt cells, 10(-9) M in the parental cells, and 10(-8) M in the CHO-mut cells. It is concluded that insulin-dependent PDH activation, PIG hydrolysis, and IG and DAG generation are mediated by the wild-type but not by the mutated insulin receptor of Val996. This study suggests that tyrosine kinase activity of the insulin receptor might be a prerequisite for insulin-stimulated generation of IG and DAG.

Amino Acid Sequence↗

[Laboratory and clinical evaluation of meropenem in pediatric field].

We performed laboratory and clinical evaluation of meropenem (SM-7338, MEPM), a new carbapenem antibiotics, in pediatric field. Pharmacokinetics of MEPM was examined with 5 patients, at a dose of 10 mg/kg via 30 minutes drip infusion. Mean plasma concentrations at 30 minutes, 1, 1.5, 2.5, 3.5 and 5.5 hours after dose were 18.8, 6.97, 3.62, 1.14, 0.43 and 0.12 micrograms/ml, respectively, with a half life of 0.96 hour. The urine recovery rate in 6 hours was 70.4%. Clinical efficacy of MEPM was evaluated in 36 patients with various infectious diseases. MEPM was administered at doses ranging 9.5 to 30.6 mg/kg/dosage, 3 to 4 times a day, 21/3 to 10 days. Clinical effects were excellent in 24, good in 11, fair in 1, with an efficacy rate of 97.2%. Bacteriologically, all causative organisms except one each of Haemophilus influenzae and Salmonella enteritidis were eradicated, an eradication rate for Gram-positive and Gram-negative bacteria were 100% and 93.3%, respectively. No side effects were observed. Elevations of GOT and/or GPT were noted in 2 patients. From the above results, we believe that MEPM is a highly effective and safe drug for patients with various infectious diseases in pediatric fields.

Age Factors↗

[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)

Adolescent↗

[A case of subaortic stenosis due to parashute accessory mitral valve tissue].

An 11-year-old boy with subaortic stenosis due to parashute accessory mitral valve tissue was treated successfully with surgery. He had a mild left ventricular-aortic pressure gradient associated with mild aortic regurgitation. The abnormal subaortic tissue was attached to the anterior leaflet of the mitral valve and was complicated with discrete subaortic stenosis. This tissue had five chordae connecting to the anterior papillary muscle and the anterior leaflet of the mitral valve. By resection of this accessory tissue and the part of the septal discrete stenotic tissue, stenosis of the left ventricular outflow tract was relieved completely.

Aortic Stenosis, Subvalvular↗

[Clinical evaluation of cefdinir 5% fine granules in pediatrics].

Clinical evaluation in pediatrics on cefdinir (CFDN, FK482) (5% fine granules), a new oral cephem, was performed. 1. CFDN was administered to 112 pediatric patients with ages between 1 month to 13 years with various infections. Dose levels used were 3.0-8.9 mg/kg (mean 5.1 mg/kg) t.i.d. for 3-14 days (mean 6.7 days). The studied patients included 2 patients with scarlet fever, 6 with acute pharyngitis, 6 with acute rhinopharyngitis, 52 with acute purulent tonsillitis, 8 with acute bronchitis, 24 with acute pneumonia, 7 with acute urinary tract infections, 1 with acute vaginitis, and 6 with impetigo. Total doses ranged from 0.6 to 4.05 g. One hundred eleven of the 112 patients were evaluated for clinical efficacy and all the patients were evaluated for safety. 2. Clinical effects were excellent in 51 cases, good in 57, and fair in 3 with an extremely high efficacy rate of 97.3%. Efficacy rates were 100% in scarlet fever, acute pharyngitis, acute purulent tonsillitis, acute bronchitis, acute vaginitis and impetigo, and 83.3%, 95.7%, 85.7% in acute rhinopharyngitis, acute pneumonia, and acute urinary tract infections, respectively. Good clinical effects were observed regardless of diseases. 3. Causative organisms were identified in 79 cases, of which 71 were found to be monobacterial infections and 8 were found to be multi-bacterial infections. In mono-bacterial infections, clinical efficacies were 100% for those caused by Staphylococcus aureus/Streptococcus pyogenes/Streptococcus pneumoniae/beta-Streptococcus except those in A and B groups with an overall efficacy of 100% against Gram-positive cocci (GPC) and they were 89.5%, 100%, 100% for those caused by Haemophilus influenzae, Haemophilus parainfluenzae, and Escherichia coli, respectively, with an overall efficacy of 90.3% in Gram-negative rods (GNR). In multi-bacterial infections also, a clinical efficacy of 100% was obtained. 4. Bacteriological effects were studied for 89 strains in the 79 cases. The eradication rate for a few strains of S. pneumoniae was low, 25%, but it was 100% for S. aureus, with the same results for S. pyogenes, and beta-Streptococcus. The eradication rate on GPC was high 94.1%. Among GNR, 66.7% of E. coli, 50.0% of H. influenzae, and 71.4% of H. parainfluenzae was eradicated. The overall eradication rate for GNR was 55.3%, lower than that for GPC. Microbial substitutions were observed in 13 cases, with Haemophilus sp. replacing other bacteria. 5. Diarrhea and soft stools were noted in 4 and 2 patients, respectively. The severity of these side effects, however, was slight and it was possible to continue the CFDN treatment.(ABSTRACT TRUNCATED AT 400 WORDS)

Acute Disease↗

[Laboratory and clinical evaluations of flomoxef sodium in neonates].

Flomoxef sodium (FMOX) was evaluated experimentally and clinically in neonates. 1. Serum concentrations and urinary excretions of the drug were examined after a bolus intravenous injection at 20 mg/kg to 22 neonates 1-30 days after birth (durations of pregnancy 31-43 weeks, weights at birth 1,650-4,040 g) and 5 infants 50-95 days after birth (durations of pregnancy 33-40 weeks, weights at birth 1,720-3,308 g). Serum concentrations were 10.8-67.6 micrograms/ml (mean 32.7 +/- 2.8 micrograms/ml) and 25.1-52.0 micrograms/ml (mean 38.9 +/- 4.3 micrograms/ml) in the neonates and the infants, respectively, at their peaks (0.5 hour value), decreased thereafter with half-lives of 0.96-5.59 hours (mean 2.20 +/- 0.26 hours value), and 0.97-1.54 hours (mean 1.22 +/- 0.12 hours value), respectively. Serum levels decreased to 0.2-17.1 micrograms/ml (mean 2.9 +/- 0.6 micrograms/ml) and N.D. -1.1 micrograms/ml (mean 0.4 +/- 0.2 micrograms/ml) after 8 hours, respectively. The urinary recovery rates of the drug in the first 8 hours after administration were 15.0-96.0% (mean 53.7 +/- 4.9%) and 29.9-73.3% (mean 62.4 +/- 9.4%) in the neonates and in the infants, respectively. 2. FMOX was administered to 78 neonates (durations of pregnancy 31-42 weeks, weights at birth 1,420-3,860 g) in whom bacterial infections were established or suspected, and clinical, bacteriological, and side effects were evaluated. In 47 neonates examined (1 with sepsis, 3 with acute upper respiratory infections, 18 with acute pneumonia, 1 with umbilical infection, 1 with impetigo, 4 with acute urinary tract infections, 1 with acute otitis externa, 1 with periproctal abscess, and 17 with intrauterine infections), the treatment was markedly effective in 41, and effective in 6, with an overall efficacy rate of 100%. The bacterilogical effects of the drug on 3 strains of Staphylococcus aureus, 1 strain of Streptococcus pneumoniae, 1 strain of Streptococcus agalactiae, 9 strains of Escherichia coli, and 2 strains of Haemophilus influenzae which were responsible for these infections were all rated as "eradicated". Moreover, the drug, administered with or without prophylactic intentions showed complete prophylactic effects in all 27 cases tested. No side effects were observed in any of the patients. Concerning abnormal clinical laboratory results, increases in GOT were noted in 2, eosinophilia in 1, and thrombocytosis in 1, but these abnormalities were invariably mild and the normalized in 1 patient without treatment. The results suggest that FMOX is useful and safe also in neonates.

Bacterial Infections↗

[Clinical features and evaluation of initial antibiotic treatment in 125 cases with purulent meningitis in infancy and childhood].

A survey of purulent meningitis in infancy and childhood from 1980 through 1986 was made by sending questionnaires to 32 pediatric institutions in Aichi, Gifu and Shizuoka prefectures. Case cards of 125 patients were collected and analyzed. The results are summarized as follows: 1. The sex ratio (male/female) was 1.78. The age distribution for all patients was as follows: younger than 1 month, 24.8%; 1-12 months, 32.8%; 1 year, 19.2%; 2-5 years, 16.0%; older than 6 years, 7.2%. Nearly 3/4 of all purulent meningitis cases occurred in infancy. 2. The isolation rate of causative organisms was 71.2%. The 4 major causative organisms were Haemophilus sp. (28 cases), Streptococcus pneumoniae (14 cases), Streptococcus agalactiae (13 cases), and Escherichia coli (12 cases). Haemophilus sp. was dominant in patients over 3 months of age, and S. pneumoniae was noted in all age groups. The latter 2 were dominant under 3 months of age. 3. The outcome of 125 cases was as follows: cured, 73 cases (58.4%); improved, 26 cases (20.8%); dead, 15 cases (12.0%); unknown, 11 cases (8.8%). As to the outcome by age, the mortality of infants within 1 month old was the highest, 29.0%, and then decreased with increasing age. As to the outcome by causative organisms, Haemophilus sp. and E. coli were associated with good outcome, whereas S. pneumoniae and S. agalactiae with poor outcome. 4. Among several antibiotics, ampicillin was the most frequently used in 94 cases, followed by cefotaxime in 50 cases. 5. As to the initial antibiotic treatment, 51 cases were treated with penicillins (PCs) (including PCs + aminoglycosides (AGs], 9 cases with cephalosporins group I, II, IV, (CEPs I, II, IV) (including CEPs I, II, IV + AGs), 25 cases with CEPs V (including CEPs V + AGs) and 31 cases with CEPs V + PCs (including CEPs V + PCs + AGs). No significant differences were observed in the outcome among these initial treatment group. 6. Compared with the initial treatments of CEPs V or CEPs V + PCs groups, other antibiotics were used more frequently in those of PCs + AGs and CEPs I, II, IV groups. In the light of this analysis, the initial treatments of purulent meningitis with PCs + AGs or CEPs I, II, IV were not so effective as those with CEPs V or CEPs V + PCs.

Aminoglycosides↗

[Laboratory and clinical studies on cefpirome in pediatrics].

Cefpirome (HR 810, CPR), a new cephem antibiotic, was investigated for its experimental and clinical studies in pediatrics. The results obtained are summarized as follows. 1. Plasma and urinary levels of CPR were determined in 2 children (age 5 and 7 years) after the one shot intravenous injection of the drug at 20 mg/kg. Average plasma levels of the drug were 44.7 micrograms/ml, 28.5 micrograms/ml, 10.5 micrograms/ml, 4.6 micrograms/ml and 1.5 micrograms/ml at 1/2 hour, 1 hour, 2 hours, 4 hours and 6 hours, respectively, and the average half life was 1.57 hours. Average urinary levels of the drug were 1,785 micrograms/ml, 545 micrograms/ml and 198 micrograms/ml at 0-2 hours, 2-4 hours, 4-6 hours, respectively and the average urinary elimination rate was 52.0%. The results were nearly equivalent to those in adults except for urinary elimination rate which tended to be slightly lower than that in adults. 2. Cerebrospinal fluid levels in 3 cases of purulent meningitis treated with CPR were investigated. Cerebrospinal fluid levels in a case of Neisseria meningitidis were 11.5-23.1 micrograms/ml at 1 hour and 0.94 microgram/ml at 5 hours after intravenous injection of 44.4 mg/kg, 4 times a day. Cerebrospinal fluid levels in a case of Streptococcus pneumoniae were 1.01-4.23 micrograms/ml at 1 hour after intravenous injection of 49.0 mg/kg, 6 times a day, and in the other case with Streptococcus pneumoniae, the levels were 16.8-37.1 micrograms/ml at 1 hour, 11.3 and 3.60 micrograms/ml at 3 and 4 hours after intravenous injection 52.2 mg/kg, 6 times a day. These results are not inferior to those with cefotaxime or ceftriaxone. These levels appear to be higher than MIC90 values against Escherichia coli, Streptococcus agalactiae, S. pneumoniae or Haemophilus influenzae which are the major pathogens of these diseases. 3. CPR was given to 62 patients and clinical efficacy, bacteriological response and adverse reactions were evaluated. Evaluated cases for clinical efficacy included 3 cases of purulent meningitis, 1 case of acute purulent otitis media, 2 cases of acute purulent tonsillitis, 1 case of acute bronchitis, 49 cases of acute pneumoniae, 1 case of scarlet fever, 1 case of acute osteomyelitis, 1 case of acute enterocolitis, and 2 cases of acute UTI, totalling 61 cases. Clinical efficacies were excellent in 38 cases, good in 22 cases and fair in 1 case with an efficacy rete of 98.4% (excellent + good).(ABSTRACT TRUNCATED AT 400 WORDS)

Acute Disease↗

[Clinical evaluation of cefixime in pediatric respiratory tract infections].

Cefixime (CFIX) was evaluated clinically in pediatric respiratory tract infections, particularly those caused by Haemophilus influenzae: 1. The total number of children in this study treated with CFIX was 232, out of which 215 cases were evaluated for clinical efficacy and 224 cases were investigated for safety. A daily dosage of 3-6 mg/kg/day was given divided into 2 to 3 times daily for 3-15 days. 2. Causative organisms were identified in 146 cases, out of which 128 cases were found to be single microbial infections and 18 cases were mixed infections. In single microbial infections, clinical efficacy was 100% for those caused by H. influenzae/Haemophilus parainfluenzae, and was 95% for Streptococcus pyogenes with an overall efficacy of 96.9%. In mixed infections, the clinical efficacy was 100% for those caused by a combination of H. influenzae and Streptococcus pneumoniae, and the overall rate was 94.4%. An involvement of H. influenzae was observed in 108 cases with a clinical efficacy rate of 99.1%, and definite involvement of beta-lactamase secreting strains of H. influenzae was found in 32 cases with a clinical efficacy of 96.9%. 3. Bacteriological effect was studied for 164 strains identified in 146 cases, and eradication rates were 89.5% for H. influenzae, 100% for H. parainfluenzae and S. pyogenes, and 71.4% for S. pneumoniae. The overall eradication rate was 91.4%. Superinfection was observed in 21 cases. MICs against 78 strains of H. influenzae were in a range of less than or equal to 0.10 microgram/ml regardless of beta-lactamase production, and far superior to cefaclor and amoxicillin. MICs against S. pyogenes and S. pneumoniae were in ranges of less than or equal to 0.10 microgram/ml and 0.39 micrograms/ml, respectively. 4. Clinical efficacy was 93.0% in 215 cases (excellent: 136, good: 64, fairly good: 10, poor: 5). CFIX attained a high efficacy in the range of 89.4-95.7% in acute pharyngitis, acute tonsillitis, acute bronchitis and acute pneumonia. 5. Safety was monitored in 224 cases and there were only one case of loose stool and another of diarrhea as side effects. There were no abnormal findings in 31 cases of the laboratory test. In conclusion, it was confirmed that CFIX is excellent and safe in the treatment of the respiratory tract infections.

Age Factors↗

[Pharmacokinetic, bacteriological and clinical studies on aztreonam in neonates].

Pharmacokinetic, bacteriological and clinical studies on aztreonam (AZT) were performed in neonates. The results obtained are summarized as follows. 1. Plasma levels and urinary excretion of AZT were determined in 18 neonates with ages between 1 and 30 days (gestation periods were 36 to 40 weeks and birth weights were 1,890 to 4,300 g) and in 2 infants with 54 and 60 days of age (gestation periods were 36 and 40 weeks, and birth weights were 2,300 and 3,300 g, respectively) upon one-shot intravenous injection of AZT 10 mg/kg (7 cases) or 20 mg/kg (11 cases) to the 18 neonates and 20 mg/kg to the 2 infants. Ampicillin (ABPC) 25 mg/kg was simultaneously injected to 5 cases of the neonates given AZT 20 mg/kg by one-shot intravenous injection and plasma concentrations of ABPC in these 5 cases were also studied. Plasma concentrations in neonates at 0.5 hour after intravenous injection of AZT 10 mg/kg were 11.5 to 27.6 micrograms/ml (average 20.3 +/- 5.5 micrograms/ml) and decreased with half-lives of 2.72 to 5.70 hours (average 3.81 +/- 1.28 hours), and the plasma levels at 8 hours after administration were 3.3 to 8.7 micrograms/ml (average 5.8 +/- 2.5 micrograms/ml). In the cases given AZT at 20 mg/kg, plasma levels at 0.5 hour were 12.4 to 48.8 micrograms/ml (average 35.9 +/- 11.6 micrograms/ml) and decreased with half-lives of 1.69 to 4.14 hours (average 2.94 +/- 0.76 hours) and AZT levels at 8 hours were 1.1 to 10.6 micrograms/ml (average 5.6 +/- 3.6 micrograms/ml). Urinary recovery rates in the first 8 hours after intravenous injection of the 10 mg/kg group were 15.5 to 61.9% (average 37.8 +/- 21.8%) and 16.3 to 62.2% (average 43.5 +/- 16.2%) for the 20 mg/kg group. Plasma concentrations in infants after administration of AZT 20 mg/kg were 33.0 to 35.6 micrograms/ml (average 34.3 +/- 1.8 micrograms/ml) at 0.5 hour and decreased with half-lives of 1.76 to 3.77 hours (average 2.77 +/- 1.42 hours) and AZT plasma levels at 8 hours were 1.4 to 5.8 micrograms/ml (average 3.6 +/- 3.1 micrograms/ml). Urinary recovery rates were 35.4 to 64.8% (average 50.1 +/- 20.8%). These results suggested that AZT shows a dose-dependent, high plasma concentration even in the neonatal period, as well as good urinary excretion from an early stage of the administration.(ABSTRACT TRUNCATED AT 400 WORDS)

Ampicillin↗

Arthroscopic versus open synovectomy in the rheumatoid knee.

We report the clinical and radiological results after arthroscopic synovectomy (41 knees) and open capsulosynovectomy (26 knees) in patients with rheumatoid arthritis, with an average follow-up of more than ten years. The clinical outcome was much the same in both groups, but there was gradual deterioration, especially after eight years. Radiological changes of osteoarthritis were worse in the knees treated by open capsulosynovectomy compared with the arthroscopic group. Arthroscopic synovectomy has many advantages and we believe that it is better than open capsulosynovectomy for patients with rheumatoid arthritis of the knee.

Adolescent↗

[Basic and clinical studies on clarithromycin in pediatrics].

Clarithromycin (TE-031, A-56268) is a new macrolide antibiotic developed by Taisho Pharmaceutical Co., Ltd. Basic and clinical studies in the field of pediatrics were carried out on a granular preparation and 50 mg tablets of TE-031 designed for use in children. The following results were obtained. 1. Concentrations of TE-031 in the serum and its excretion in the urine were investigated in children. Six children were orally administered with a TE-031 granular preparation at 10 mg/kg in a cross-over study 30 minutes before meal and 30 minutes after meal. When the drug was ingested before meal, the mean peak serum concentration occurred 1 hour later and was 5.32 +/- 1.20 micrograms/ml. The mean half-life of TE-031 in the serum was 3.6 +/- 1.0 hours, and drug levels decreased to 1.94 +/- 0.55 micrograms/ml at 6 hours after dosing. In cases of the postprandial administration, the mean peak serum level was 4.21 +/- 1.25 micrograms/ml, occurring 2 hours after ingestion. The mean serum half-life in these cases was 3.5 +/- 1.3 hours, and serum levels decreased to 1.66 +/- 0.47 micrograms/ml at 6 hours after dosing. Mean urinary recovery rates during the initial 6 hours after ingestion were 30.5 +/- 6.4% in the cases of preprandial administration and 34.7 +/- 7.3% with postprandial administration. In addition, 30 minutes before meal, 50 mg tablets of TE-031 were orally administered to 3 children in a dose level equivalent to approximately 10 mg/kg, followed by monitoring of serum and urinary levels. It was found that the mean serum concentration showed a peak value of 4.10 +/- 0.44 micrograms/ml at 2 hours after dosing, the mean serum half-life was 3.5 +/- 0.7 hours, and the mean level fell to 1.90 +/- 0.55 micrograms/ml by 6 hours after dosing. The mean 6-hour urinary recovery rate was 32.7 +/- 12.1%. On the basis of the above results, it has been surmised that, in comparison to conventional macrolide antibiotics. TE-031 is better maintained in the blood at a high concentration and is more efficiently excreted into the urine. In addition, the data show that the bioavailability of TE-031 is slightly superior when the drug is administered on an empty stomach compared with after a meal. And finally, it was found that the granular and 50 mg tablet preparations of TE-031 are almost equivalent in terms of the absorption and the excretion of the drug.(ABSTRACT TRUNCATED AT 400 WORDS)

Age Factors↗