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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

Ceftizoxime, a new cephalosporin preparation, was evaluated for its antibacterial activity, absorption, excretion and clinical effectiveness, and the following results were obtained. The minimum inhibitory concentrations (MICs) of ceftizoxime against 211 clinical isolates were determined in comparison with those of cefazolin, cefmetazole, cefotiam and 6059 S. Against S. pyogenes (50 strains), ceftizoxime was 1 tube inferior to cefazolin inoculum size of 10(8) cells/ml, but was 2--3 tubes superior to cefmetazole and 6059-S. Against E. coli (50 strains), ceftizoxime and 6059-S were significantly more active than the other drugs. The susceptibility pattern of Klebsiella sp. (50 strains) to ceftizoxime was similar to that to cefotiam and 6059-S. Against Proteus sp. (50 strains), cefotiam and 6059-S were more active than the other drugs. Ceftizoxime was intermediate in activity, and cefazolin was the least active. Against H. influenzae (11 strains), ceftizoxime was the most active, with concentrations of 0.1 mcg/ml required to inhibit 100% of strains with an inoculum size of 10(8) cells/ml and 10(6) cells/ml. A dose of ceftizoxime 10 mg/kg or 20 mg/kg was administered to 15 patients aged from 5 years to 12 years, and serum levels and urinary excretion of the drug were measured. Intravenous bolus injection of the drug in dose of 10 mg/kg and 20 mg/kg yielded mean serum levels of 26.6 mcg/ml and 55.7 mcg/ml at 30 minutes, respectively. The serum levels of the drug, thereafter, declined gradually but still remained 1.3 mcg/ml and 2.7 mcg/ml at 6 hours. The serum half-lives (T 1/2) were estimated to be 1.17 hours in dose of 10 mg/kg and 1.31 hours in dose of 20 mg/kg. When a dose of 20 mg/kg was infused over a period of 30 minutes, the serum levels attained the peak of 72.4 mcg/ml to 82.4 mcg/ml (mean 79.4 mcg/ml) at the end of infusion. The levels, thereafter, tapered to mean levels of 45.3 mcg/ml at 30 minutes, 24.7 mcg/ml at 1 1/2 hours, and 3.6 mcg/ml at 5 1/2 hours, with a T 1/2 of 1.22 hours. Meanwhile, when the same dose was infused over 1 hour, the serum levels attained the peak of 59.4 mcg/ml to 68.5 mcg/ml (mean 64.2 mcg/ml). The mean serum levels after the end of infusion were 41.3 mcg/ml at 30 minutes, 21.6 mcg/ml at 1 hour and 1.9 mcg/ml at 5 hours, with a T 1/2 of 0.97 hours. Urinary recovery of the drug was 69.2% to 79.9% after intravenous injection and 62.3% to 79.9% after drip infusion, most of the given drug was excreted in the first 2 hours after administration. In our clinical study, 27 children with moderate or severe infections (12 cases of bronchopneumonia or bronchitis, 5 of pyelonephritis, 3 of purulent meningitis, etc.) were treated with ceftizoxime at the daily dose of 30--309 mg/kg for 3--23 days. Clinical response was excellent in 10, good in 9, fair in 5 and poor in 3. The drug was proved to be very effective against infections due to H. influenzae K. pneumoniae, E. coli and S. aureus. No serious side effects were observed in any case.
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PMID:[Laboratory and clinical studies on ceftizoxime in the field of pediatrics (author's transl)]. 627 16

Laboratory and clinical studies were performed on cefmenoxime (CMX), a new cephalosporin antibiotic, and the following results were obtained. 1. Susceptibility of clinically isolated bacteria to CMX and cefotiam (CTM) or cefazolin (CEZ) Antimicrobial activity of CMX was compared with that of CTM and CEZ against S. aureus, S. epidermidis, S. pneumoniae, H. influenzae and E. coli. CEZ and CTM were more active than CMX against S. aureus, S. epidermidis and S. pneumoniae. But CMX was found to be more active by 1-10 tubes than CEZ and CTM against H. influenzae and E. coli. 2. Clinical efficacy. CMX was intravenously administered to 19 patients; 3 with lacunar tonsillitis, 2 with acute bronchitis, 8 with bronchopneumonia, 3 with UTI, 1 with septicemia, 1 with acute panperitonitis, 1 with S.S.S.S. at daily doses of 30-115 mg/kg (64.6 mg/kg on an average) t.i.d. or q.i.d. for 3-17 days (6.1 days on an average). The overall efficacy rate was 94.7%, i.e., efficacy was excellent in 10 cases (52.6%), good in 8 cases (42.1%), and poor in 1 case (5.3%). Bacteriological efficacy was good, i.e. 16 of the 19 strains disappeared. Transient eosinophilia was observed in 1 patient, but no other laboratory abnormality was observed during treatment. The above results suggest that CMX is 1 of the useful antibiotics in treatment of pediatric infections, especially due to Gram negative bacteria.
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PMID:[Laboratory and clinical studies of cefmenoxime in the pediatric field]. 630 38

Cefmenoxime (CMX) was evaluated in 25 children with a suspicion of bacterial infection. Of the 20 confirmed bacterial infections, 19 were cured by CMX therapy (effective rate, 95%). The diagnoses included acute pharyngotonsillitis (4), acute bronchitis (1), pneumonia (7), streptococcal dacryocystitis (1), infections accompanied with acute leukemia (4), and acute urinary tract infections (3). The etiologic pathogens were beta-hemolytic Streptococcus group A (1), and F (1), Staphylococcus aureus (4), Haemophilus influenzae (4), Escherichia coli (4), Klebsiella pneumoniae (2), etc. CMX was very effective for 2 children with respiratory infections due to ampicillin resistant H. influenzae type b. The half life of serum concentration of CMX was 0.76 +/- 0.17 hour after an intravenous bolus injection. A cerebrospinal fluid level of CMX was 5.2 mcg/ml 1 hour after intravenous injection of 1 g (23.8 mg/kg) in a child with inflamed meninges. However this level was not as high as those of cefotaxime, latamoxef, or ceftizoxime measured in the same case. No severe adverse reaction was encountered with CMX therapy. The data suggest that CMX is a safe and effective parenteral antibiotic when used in children with susceptible bacterial infections.
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PMID:[Clinical evaluation of cefmenoxime in the pediatric infections]. 630 92

A new cephalosporin antibiotic, cefmenoxime (CMX) was administered to 22 patients aged 5 days to 8 years, and who had moderate or severe pediatric infections, to examine its clinical effect. The infections were 3 of acute bronchitis, 2 cases of asthmatic bronchitis, 6 of acute pneumonia, 1 of Mycoplasma pneumonia, 2 of sepsis (1 accompanied with pneumonia), 3 of vacterial meningitis, 2 of urinary tract infection, 1 of acute appendicitis, 1 of aseptic meningitis and 1 of fever of undetermined origin. The drug was administered by one shot intravenous injection 4 times daily at the dose of 40 approximately 200 mg/kg/day. The drug was administered for 3 approximately 15 days, the total dosage administered being 0.7 approximately 43.5 g. Clinically, excellent, good and fair response was obtained in 2, 11 and 4 cases, respectively, the drug being effective in all cases excluding the 5 cases in which judgement was unknown. The 6 strains of bacteria isolated from the lesion as the assumed causative bacteria (1 strain of S. pneumoniae, 2 of H. influenzae, 2 of E. coli, 1 of K. pneumoniae) were all eradicated after drug administration. No notable side effects were produced.
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PMID:[Clinical studies on cefmenoxime in pediatric field]. 630 93

Studies on T-1982 (cefbuperazone), a new cephamycin antibiotic, were carried out in the field of pediatrics, and the following results were obtained. 1. Peak MIC of T-1982 against S. pyogenes (group A) lately isolated was 0.39 micrograms/ml, and the drug was active even against highly resistant strains of macrolides, lincomycin, tetracycline and chloramphenicol. 2. Peak MICs of T-1982 were 0.78 microgram/ml against B. pertussis, 0.2 microgram/ml against E. coli and less than or equal to 0.05 microgram/ml against K. oxytoca, and the drug was also active against ampicillin-resistant bacteria. 3. Serum levels and urinary excretions of T-1982 were investigated in 6 cases. When given at a dose of 20-28 mg/kg by 1 hour intravenous drip infusion, serum concentrations of T-1982 attained the peak level of 63.5-75.9 micrograms/ml at the end of administration and sustained the level of 0.9-2.6 micrograms/ml at 6 hours, the serum half-life (T 1/2) ranging 70-82 minutes. Approximately 20-72% of the dose were excreted in the active form into urine within 6 hours. 4. Twenty-seven cases of acute pediatric infections were treated with T-1982 mainly by intravenous drip infusion, and satisfactory clinical results were obtained in all the cases of angina lacunaris, bronchitis, bronchopneumonia, pertussis, sepsis caused by Serratia and acute urinary tract infections caused by ampicillin-resistant E. coli. The efficacy rate was 96.3%. In this study the drug was administered chiefly at a daily dose of 50-70 mg/kg 2-3 times a day for 2-12 days. 5. Gram-positive cocci (S. aureus, S. pneumoniae, S. pyogenes) and Gram-negative rods (H. influenzae, H. parainfluenzae P. vulgaris, B. pertussis, S. marcescens, E. coli) were eradicated by the treatment with T-1982. 6. No noticeable side effects were observed, except for temporary increase of eosinophil in 2 cases and slight elevation of GOT in 1 case.
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PMID:[Fundamental and clinical studies on T-1982 (cefbuperzone), a new cephamycin antibiotic, in the field of pediatrics]. 630 96

T-1982 (cefbuperazone), a new cephamycin antibiotic, was basically and clinically studied in the field of pediatrics, and the following results were obtained. 1. The antibacterial activity of T-1982 was compared with that of CEZ, CMZ and ABPC. T-1982 was more active than the other drugs against Gram-negative bacteria, the sensitivity of E. coli (22 strains), K. pneumoniae (18 strains), P. mirabilis (19 strains), P. vulgaris (4 strains), P. morganii (5 strains) and K. oxytoca (4 strains) distributing less than 0.39, 0.1, 1.56, 0.39, 6.25 and 0.2 microgram/ml, respectively. Two of 3 strains of C. freundii were inhibited by 12.5 micrograms/ml. Against Gram-positive bacteria, the activity of T-1982 was inferior to that of the other drugs. S. pyogenes (28 strains) were inhibited by 0.78 microgram/ml or less, but the sensitivity of S. aureus (34 strains distributed 12.5-100 micrograms/ml). 2. T-1982 was administered to each 3 children at a dose of 20 mg/kg by one shot intravenous injection or 1 hour drip infusion, or at dose of 40 mg/kg by 1 hour drip infusion. The mean serum levels at 0.25, 0.5, 1, 2, 4 and 6 hours after one shot intravenous injection of 20 mg/kg were respectively 74.3, 56.3, 42.3, 17.6, 5.7 and 1.2 micrograms/ml with the mean half-life of 1.01 hours. The values were 32.9, 50.0, 73.7, 27.5, 12.4 and 4.5 micrograms/ml and 1.31 hours by intravenous drip infusion of 20 mg/kg and 50.4, 104.7, 136.3, 62.3, 18.6 and 6.9 micrograms/ml and 1.16 hours by intravenous drip infusion of 40 mg/kg. The mean urinary recovery rates within 6 hours were 47.7, 67.6 and 60.9%, respectively. 3. Treatment with T-1982 was made in 28 cases of pediatric infections; 1 case of acute bronchitis, 19 cases of acute bronchopneumonia or lobar pneumonia, 2 cases of acute purulent cervical lymphadenitis, 4 cases of acute pyelonephritis and each 1 case of subcutaneous abscess and suspected bacterial endocarditis. The clinical responses assessed in 27 cases were excellent in 21 cases, good in 5 cases and poor in 1 case, the efficacy rate being 96.3%. Bacteriologically, 2 strains of S. aureus, 3 strains of S. pneumoniae, 4 strains of H. influenzae, 2 strains of E. coli and 1 strain of P. mirabilis were eradicated. One strain of S. faecalis was reduced. No side effects were observed in any cases. Slight elevation of GOT and GPT and that of GOT were noted in each 1 case.
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PMID:[Basic and clinical studies on T-1982 (cefbuperazone) in the field of pediatrics]. 634 36

In acute pneumococcal infection with the clinical picture of acute bronchitis or the exacerbation of chronic bronchitis 88-93% of patients showed the formation of secretory IgA to S. pneumoniae autostrains, i.e. a high correlation between the occurrence of these bacteria in the sputum and the local immune response of the body. The characteristic feature of antipneumococcal secretory IgA is their earlier, more intensive and less prolonged formation in comparison with that of serum antibodies. During the exacerbation of chronic bronchitis only in 28% of the patients secretory IgA to H. influenzae autostrains and low correlation between the formation of secretory and serum antibodies were detected.
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PMID:[Indirect immunofluorescence reaction of systemic and local humoral immunity in patients with inflammatory lung diseases. III. Secretory IgA antibodies to S. pneumoniae and H. influenzae autostrains]. 636 21

Twenty-four pediatric patients with infections were treated with ceftazidime (CAZ) by one-shot intravenous injection in the doses of 39 approximately 149 mg/kg/day in 4 divided doses as a rule. These patients' ages ranged from 2 months to 13 years 4 months. The duration of the administration ranged from 4 to 19 days, and total doses ranged from 1.38 to 57 g. Infections consisted of respiratory tract infections in 19 cases (acute tonsillitis in 3, acute bronchitis in 7, and pneumonia in 9), urinary tract infection in 1 case, acute peritonitis in 1 case, and suspected sepsis in 3 cases. Clinical efficacy was excellent in 18, good in 1, fair in 1, and poor in 4 cases, and the efficacy rate (excellent + good) was 79.2%. Bacteriological response was evaluated on 14 strains of bacteria isolated from lesions, assumed as the causative organisms (7 strains of S. aureus, 3 of P. aeruginosa, 1 of H. influenzae, 1 of K. pneumoniae, 1 of E. coli, and 1 of S. marcescens). Out of these strains, 10 were eradicated, and 1 (P. aeruginosa) decreased, but 2 strains (both S. aureus) persisted. (One strain of S. aureus was not examined.) No adverse effect suspected to be related to the drug was observed either in subjective symptom or in objective findings.
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PMID:[Clinical studies of ceftazidime in the pediatric field]. 637 55

Cefoperazone (CPZ) at dose levels of 80 approximately 100 mg/kg/day, divided 3 approximately 4 times, was drip-infused or intravenously injected for a period of 2 approximately 6 days to 10 patients. All 10 cases, 4 cases of bronchopneumonia from which H. influenzae was detected (Group A S. pyogenes and S. pneumoniae were also detected in each 1 case). 2 cases of coli urinary tract infection, 1 case of acute colitis from which pathogenic E. coli was detected, 1 case of E. coli carrier, 1 case of acute bronchitis (bacteria were not detected), and 1 case of urinary tract infection (bacteria were not detected) showed rapid improvement of clinical symptoms with rapid eradication of the pathogenic bacteria. In one case of urinary tract infection where S. epidermidis and S. faecalis were simultaneously detected, S. epidermidis was removed but S. faecalis was merely decreased. The effective antibacterial concentration after intravenous injection of CPZ in the feces was determined and found to be present in sufficient concentrations to prevent colon infection. No particular side effects were observed during CPZ therapy.
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PMID:[Clinical studies on cefoperazone in the pediatric field (author's transl)]. 645 26


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