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The basic and clinical studies of cefotiam (CTM) in pediatric infections were carried out, and the following results were obtained: 1. The antibacterial activity of CTM against S. aureus was equal or slightly less than that of cefazolin (CEZ). Those of CTM against E. coli and K. pneumoniae were eight times more active than those of CEZ. 2. CTM 20 mg/kg was administered wither by 30 minutes or 1 hour intravenous drip infusion. The peak serum levels were obtained at the end of each drip infusion, with the mean peak levels being 44.8 and 41.4 mcg/ml respectively. The serum levels at 1.5 and 2 hours after drip infusion were 2.8 and 2.2 mcg/ml respectively, and at 3.5 and 4 hours after drip and 4 hours after drip infusion were 0.3 and 0.7 mcg/ml respectively. The half lives were 0.62 and 1.15 hours, respectively. The mean urinary excretion over 6 hours were 52.8% in ;the 30 minutes drip infusion group and 42.6% in the 1 hour drip infusion group. 3. Clinical efficacy was evaluated in sixteen cases suffering from tonsillitis (4 cases), pneumonia (4), bronchitis (2), cervical lymphadenitis (2), purulent meningitis (2), suppurative arthritis (1) and suspected sepsis (1). Good and excellent responses were obtained in 15 of 16 cases (93.8%). Bacteriological response in the form of eradication was noted in 4 of 6 cases. Side effect observed was rash in 1 case, and laboratory abnormalities were elevation of BUN in 1 case and elevation of GPT in 2 cases.
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PMID:[Basic and clinical studies of cefotiam in pediatric field (author's transl)]. 627 Apr 19

Pharmacokinetics and clinical effects of ceftizoxime (CZX), a new cephalosporin antibiotic, were investigated and following results were obtained. 1) Ceftizoxime was given by intravenous injection or drip infusion for 1 hour at a single dose of 30 mg/kg. After intravenous injection, the mean peak serum level of 3 children was 95.9 mcg/ml at 15 minutes and half-life time was 1.18 hours. After 1 hour drip infusion, the mean peak serum level of 3 children was 79.5 mcg/ml at the end of infusion and half-life time was 1.20 hours. The urinary level was high and the mean urinary recovery rate was 69.6% and 63.4% up to 6 hours after intravenous injection and 1 hour drip infusion, respectively. 2) CZX was administered in dose of 39--76 mg/kg to 7 pediatric patients (4 cases of purulent meningitis, 2 of septicemia with purulent meningitis, and 1 of aseptic meningitis) by a single intravenous injection. In patients with purulent meningitis, passage into the cerebrospinal fluid was relatively as good as 30% of serum level at the same time in the presence of remarkable signs of inflammation, but poor in cases of mild inflammation or aseptic meningitis. 3) Cerebral puncture fluid level in 1 patient with cerebral abscess was as good as 65.5% of serum level at the same time. 4) CZX was given to 28 cases of respiratory tract infection, 1 of tonsillitis with otitis media, 6 of scarlet fever, 1 each of maxillary sinusitis and bacterial endocarditis, 6 of purulent meningitis, 2 of septicemia, 5 of septicemia suspected, 2 of septicemia with purulent meningitis, 1 each of osteomyelitis, typhoid fever, peritonitis and biliary tract infection, 16 of urinary tract infection, 14 of skin and soft tissue infection, and 1 of external otitis, totaling 87 cases. The mean daily dose of 101.6 mg/kg was administered for an average of 10 days mainly by intravenous injection 4 times daily. Clinical results obtained were excellent in 34 cases, and good in 46. Bacteriological effectiveness rate was 100%. As for side effects, fever, fever with rash, fever with cough and diarrhea appeared in 1 each case out of 182 cases including 95 drop out cases. As for laboratory findings, eosinophilia, thrombocytopenia, elevation of GOT, that of GOT with GPT, and that of GOT with LDH appeared in 10, 2, 2, 3 and 1 cases, respectively.
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PMID:[Pharmacokinetics and clinical effects of ceftizoxime in pediatric field (author's transl)]. 627 4

Pharmacokinetics of ceftizoxime (CZX), a new cephalosporin antibiotic, was investigated in 9 children with normal renal and hepatic function. In addition, the clinical effect of CZX was evaluated in 26 pediatric patients with various infections. In 4 of the 9 children with normal renal and hepatic function, intravenous bolus injection of CZX in a dose of 20 mg/kg yielded a mean peak serum level of 36.5 micrograms/ml at 1/2 hour after infusion, and mean serum levels of 12.5 micrograms/ml at 2 hours and 6.0 micrograms/ml at 4 hours after infusion. The biological half-lives of CZX were estimated to be 1.25--2.55 hours. In another child, serum levels of CZX at 1/2, 2 and 4 hours after intravenous bolus injection in a dose of 10 mg/kg were 19.60, 5.96 and 2.06 micrograms/ml, respectively. The clear difference in dose response between 20 mg/kg and 10 mg/kg reflected the doubled dose levels. In the remaining 4 children, drip infusion of CZX in a dose of 20 mg/kg (1 child 17 mg/kg) over 0.5--1.5 hours yielded peak serum levels at the end of infusion. The biological half-lives of CZX were estimated to be 0.95--1.50 hours. About 80% of CZX was excreted in the urine within 6 hours after infusion in the 4 children tested. Twenty-six pediatric patients with various infections were treated with CZX intravenous doses of 20 mg/kg to 118 mg/kg b.i.d.--q.i.d. for 3--14 days. Of the 12 patients with acute bronchitis and pneumonia, 5 showed excellent response, 6 good and 1 fair response. Of the 5 patients with urinary tract infection, 4 showed excellent response and 1 good response. One patient each with colitis, tonsillitis and facial cellulitis, pharyngitis showed excellent response and 1 patient each with purulent thyroiditis and gluteal abscess showed good response. The single patients with sepsis showed excellent response. One patient each with pyothorax, purulent arthritis and cerebral abscess showed poor response. Overall effectiveness rate was 84.6%. although 22 of all 26 patients treated had serious underlying diseases such as APL, AML. A mild increase in GOT and GPT was observed in 1 patient during treatment with CZX, and the values returned to normal after discontinuation of the drug. These results suggest that ceftizoxime is 1 of the most important antibiotics for treating a wide range of infections in children as well as in adults.
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PMID:[Pharmacokinetics and clinical evaluation of ceftizoxime (author's transl)]. 627 8

Fundamental and clinical studies of ceftizoxime, a new cephalosporin antibiotic, in children led to the following results. 1. Ceftizoxime compared favorably with cefazolin (CEZ) and cefmetazole (CMZ) for in vitro activity against clinically isolated strains of Staphylococcus aureus (31 strains), Escherichia coli (29), Klebsiella pneumoniae (30) and Pseudomonas aeruginosa (16). While somewhat less active against S. aureus than CEZ and CMZ, ceftizoxime was far more active than these 2 cephalosporin antibiotics against the test strains of E. coli and K. pneumoniae, which included strains resistant to the 2 drugs. Ceftizoxime was not particularly active against Ps. aeruginosa, but this seeming disadvantage was offset by the absolute ineffectiveness of the 2 reference drugs on this obstinate organism. 2. The time course of mean serum ceftizoxime levels in 3 pediatric patients of 5--10 years old given a single intravenous dose of 20 mg/kg was as follows: 45.4 micrograms/ml at 15 minutes, 40.4 micrograms/ml at 30 minutes, 22.1 micrograms/ml at 1 hour, 10.4 micrograms/ml at 2 hours, 2.9 micrograms/ml at 4 hours and 0.9 microgram/ml at 6 hours. The mean serum half life was 1.12 hours. The mean urinary levels of ceftizoxime at serial 2-hour collection intervals were as follows: 2,477 micrograms/ml for 1--2 hours, 1,235 micrograms/ml for 2--4 hours and 462 micrograms/ml for 4--6 hours. The mean urinary recovery up to 6 hours was 61.0%. 3. The clinical response of 28 children with infection to ceftizoxime treatment was 'excellent' in 22 children, 'good' in 4, and 'poor' in 2. These children comprised 11 with acute pneumonia, 3 with acute bronchitis, 4 with acute pyelonephritis, 2 each with acute purulent arthritis and acute enterocolitis, and 1 each with acute purulent tonsillitis, acute purulent lymphadenitis, furunculosis, subcutaneous abscess, subdural abscess and sepsis. The overall rate of effectiveness was 92.9%. Successfully eradicated strains in the bacteriological sense consisted of 4 strains each of H. influenzae and E. coli, 1 strain each of P. morganii, S. pneumoniae and S. pyogenes, 1 of the 2 strains of S. enteritidis, and 1 of the 3 strains of S. aureus. The overall rate of bacteriological effectiveness was 81.3%. No clinical side effects were observed. Changes in laboratory test findings included slightly and transiently elevated GOT and GPT in 1 child and GOT alone in another child.
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PMID:[Fundamental and clinical studies on ceftizoxime in pediatric field (author's transl)]. 627 13

Two to 6 g of CMX was administered daily to 9 patients who were admitted to ICU, i.e. 5 cases with pneumonia and 4 with sepsis. In all cases, CMX was administered concomitantly with aminoglycoside which had been administered, and additional administration of other antibiotics was avoided. Bacteriologically, P. aeruginosa was isolated from 4 cases, K. pneumoniae from 4 cases, S. marcescens, P. mirabilis and P. cepacia respectively from 1 case. The CMX treatment was considered effective in 4 of 5 pneumonia cases and in 3 of 4 sepsis cases. In total, 7 of 9 cases responded effectively. The clinical effective rate was 77.8%. Elevation of GOT and GPT values was noticed in 1 case, however, the causality with CMX administration was unclear.
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PMID:[Clinical studies on cefmenoxime in the intensive care unit]. 629 78

To evaluate the antibacterial potency of cefotiam (CTM) clinical and laboratory studies were carried out and the results were as follows. Clinical evaluation and adverse reaction CTM was given to total of 23 patients, 10 with bronchopneumonia, 10 with bronchitis and one each with cystitis, enteritis and suspected sepsis. Overall efficacy rate was 78.3% (18/23) (excellent 9, good 9, fair 3, poor 2). Only 1 case showed a side effect of slightly elevated GOT and GPT. Antibacterial activities MIC of CTM against isolates from sputum was investigated on those patients mentioned above and was compared with MIC of CEZ and CMZ. CTM showed superior antibacterial activity against almost all strains. Especially on Haemophilus and Klebsiella antibacterial activity of CTM was impressive. Organisms in sputum Four out of 8 causative bacteria disappeared and 1 out of 8 decreased after administration of CTM. Thus CTM is considered to be the useful drug for the treatment of respiratory infection.
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PMID:[Antibacterial potency of cefotiam based on the clinical effect, MIC and decrement of organisms in the sputum]. 631 12

T-1982 (cefbuperazone), a new injectable cephamycin antibiotic, was studied for its antibacterial activity, concentration in serum and urine, penetration into cerebrospinal fluid (CSF) as well as clinical application. The following results were obtained. 1. Antibacterial activity: The susceptibilities of clinically isolated K. pneumoniae, E. coli and E. cloacae to T-1982 were superior to those of CEZ CMZ, and ABPC. T-1982 seemed to be useful for various infections due to Gram-negative rods. 2. Concentration in serum and urine: Subjects were 10 children with congenital heart failure but no abnormal renal and liver functions. T-1982 was given intravenously to 3 groups at 200 mg/kg by one shot (4 cases), 20 mg/kg by 1 hour drip infusion (3 cases) and 10 mg/kg by 1 hour drip infusion (3 cases). The half-lives were 60, 78 and 85 minutes, respectively. 3. Penetration into cerebrospinal fluid: Three children with malignant tumor were injected 20 mg/kg intravenously. A small amount of T-1982 was penetrated into CSF. 4. Clinical efficacy: T-1982 was administered daily 40-116 mg/kg t.i.d. or q.i.d. for 2-14 days to 17 children comprising 1 bronchopneumonia, 1 bronchitis, 4 tonsillitis, 1 lymphadenitis, 1 sepsis, 1 pharyngitis, 1 impetigo, 1 acute sinusitis and 6 pyelonephritis. Clinical efficacy was excellent in 10, good in 2, fair and poor in 3, and the efficacy rate was 70.6%. Bacteriological effect was as follows; eradicated in 9 cases and unknown in 8 cases. As side effect, GOT and GPT elevations unrelated to the drug were observed in 2 cases. Other abnormal findings were not found. T-1982 seems to be safe antibiotic in the field of pediatrics.
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PMID:[Fundamental and clinical studies on T-1982 (cefbuperazone) in the field of pediatrics]. 634 37

Ceftazidime ( CAZ ), a new injectable cephem antibiotic, was used for treatment of infections in children, and the following results were obtained. After an intravenous injection of CAZ at a dose of 20 mg/kg, the mean blood levels in 2 patients were 41.5 micrograms/ml at 30 minutes, 18.1 micrograms/ml at 2 hours and 2.55 micrograms/ml at 6 hours, with the half-life (T 1/2) of 1.37 hours. In a 22-day-old baby with meningitis given CAZ intravenously at a dose of 43.5 mg/kg, the blood levels were 100 micrograms/ml at 30 minutes, 68 micrograms/ml at 2 hours and 25 micrograms/ml at 6 hours, with the half-life (T 1/2) of 2.96 hours. After intravenous administration of CAZ in doses ranging from 35.7 to 50 mg/kg, CSF concentrations ranged from N.D. to 6.3 micrograms/ml in 3 patients with purulent meningitis, although 19 micrograms/ml at 1 hour and 13 micrograms/ml at 2 hours in 1 patient after intravenous administration of 46.7 mg/kg. In patient with mumps meningitis, CSF concentrations were undetectable after intravenous administration of 35.7 mg/kg. Seventeen patients (each 1 patient with lymphadenitis, tonsillitis and septicemia, each 2 patients with pneumonia, bronchiectatic bronchitis, pyothorax and purulent meningitis, each 3 patients with pyelonephritis and enteritis) were treated with CAZ intravenously, at the daily doses of 178.2 mg/kg and 200 mg/kg in 4 divided doses in patients with meningitis and 44.1 to 103.4 mg/kg in 3 divided doses in patients with other infections (two of them were given by intravenous drip infusion for 30 minutes). The clinical responses were excellent or good in all the patients except for 1 case of Salmonella enteritis (poor) and 1 case of Campylobacter enteritis (poor). The efficacy rate was 88.2%. It was noteworthy that the clinical response was excellent in 1 case of septicemia with P. aeruginosa with leukemic stage of malignant lymphoma and in 2 cases of purulent meningitis. As side effects, fever, eruption, leukocytopenia, elevation in GOT and positive CRP considered to be allergic, were observed on day 16 of administration in 1 case of pyothorax. These symptoms disappeared by discontinuance of administration. In addition, there were elevation in GOT and GPT in 2 cases and elevation in GOT in 2 cases and elevation in GPT in 1 case; they were all mild or transient, and there was nothing to be worried about.(ABSTRACT TRUNCATED AT 400 WORDS)
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PMID:[Clinical evaluation of ceftazidime in paediatrics]. 637 60

A total of 466 patients were treated with cefoperazone. The drug was usually administered by drip infusion of 2 to 4 gm/day. Therapy was described as markedly effective and moderately effective in 64 of 77 patients (83.1%) treated for urinary tract infections; 253 of 316 patients (80.1%) treated for respiratory infections; 37 of 48 patients (77.1%) treated for liver biliary duct infections; ten of 16 patients (62.5%) treated for septicemia; and seven of nine patients (77.8%) being treated for other infections. Overall, cefoperazone was effective 79.6% of all patients treated. With respect to bacteriological activity, the overall eradication rate for gram-negative organisms (including Pseudomonas aeruginosa, Klebsiella sp, Escherichia coli, Haemophilus influenzae, Enterobacter sp, and Proteus sp) was 81% (182/225) and for gram-positive (Staphyloccocus aureus, Streptococcus pneumoniae and Streptococcus faecalis) 90% (36/40). Of 205 patients who failed to respond to previous antibiotic therapy, 67.8% were treated effectively with cefoperazone. Side effects, such as skin eruption, pyrexia and diarrhea, occurred in only 4.8% of patients treated, while laboratory abnormalities, such as elevated glutamic-oxaloacetic transaminase, glutamic-pyruvic transaminase, alkaline phosphatase, and eosinophil values, occurred in only 6.4% of the treated patients. None of these abnormal values were of clinical significance.
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PMID:Clinical trials with cefoperazone in the field of internal medicine in Japan. 644 92

A new semisynthetic 1-oxa-beta-lactam derivative, 6059-S, was evaluated for its safety and efficacy in children. Twenty-five patients were treated with 10 to 274 mg/kg per day of 6059-S by intravenous administrations. The diagnosis of the patients were acute pharyngitis (2), acute bronchitis (2), pneumonia (4), pertussis (4), acute enterocolitis (2), recurrent urinary tract infection (2), suspected septicemia (3), and acute purulent meningitis (1); and the remaining 5 patients were considered to have nonbacterial infections. The pathogens recovered were Streptococcus pneumoniae (1), Haemophilus influenzae (4), Haemophilus parainfluenzae (1), Enterobacter cloacae (1), Enterobacter aerogenes (1), Proteus morganii (1), Psuedomonas aeruginosa (2) and Salmonella typhimurium (1). All the patients of bacterial infections were cured after the 6059-S therapy. However, Pseudomonas aeruginosa and Salmonella typhimurium were not eradicated after the 6059-S therapy, and the rate of bacterial disappearance was 75%. Diarrhea (3), precordial pain (2, only in cases with high-dose therapy), transient elevation of GOT and GPT (2), and transient eosinophilia (2) were found to be associated with the 6059-S therapy. However, no severe adverse reactions were encountered. Half life of the serum 6059-S level was 1.34 +/- 0.16 hours. CSF concentrations in a case with Haemophilus influenzae meningitis ranged 4.0 to 9.7 mcg/ml after an intravenous injection of 34.3 to 75 mg/kg of 6059-S. From the present study, 6059-S appears to be a safe and effective antibiotic when used in children with susceptible bacterial infections. It remains to be further determined whether 6059-S is superior to ABPC in the treatment of Haemophilus influenzae meningitis.
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PMID:[Clinical evaluation of 6059-S therapy in children (author's transl)]. 645 68


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