[in Japanese]

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Antibacterial activity of cefotiam (CTM) against clinically isolated organisms in the field of obstetrics and gynecology was discussed as follows:
In the point of view of the MICs peak, CTM was 1-fold worse than CEZ against Gram-positive bacteria, while, in the case of the concentration of CTM required to inhibited the growth of 80% or 90% of the total number of tested Gram-positive organism,antibacterial activity of CTM was approximately identical with that of CEZ, CMZ or SBPC. CTM against E. coil, K.pneumoniae, P. mirabilis was 16-32-fold more effective than CEZ and 4-16-fold than CMZ.Against indole-positive organisms which CEZ was no effective, CTM was considerably effective. But antibacterial activity of CTM againstB. fragilis was insufficient. However, in the case that no spore forming anaerobic organism involved in infectious disease,it is said that existence of aerobic organism is important. As E.coli is representative of aerobic organism, CTM with potent antibacterial activity against this organism is seemed to be effective antibiotic for the gynecological infection.

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Renal accumulation,nephrotoxicity and serum concentration of gentamicin (GM) by intravenous infusion were studied in rabbits, and compared with those observed by bolus intravenous and intramuscular administrations. The results were as follows.
1. Concentration of GM in renal cortex was determined in time course after a single administration of 30 minutes intravenous infusion, bolus intravenous and intramuscular injections at a dose of 5mg/kg. Distribution patterns into renal cortex were almost identical after these administration routes. Also, no significant difference was found in each time point of cortical concentration among 30 minutes intravenous infusion, bolus intravenous and intramuscular injections.
2. Concentrations of GM in renal cortex and medulla determined at 24 hours after the final administration of 30 minutes intravenous infusion at doses of 3mg/kg and 30mg/kg for 10 consecutive days were compared with those obtained by intramuscular administration. Concentration of GM in renal cortex was related to doses, andthere was no significant difference between intravenous infusion and intramuscular injection. Concentration of GM in renal medulla was a very low compared with that of renal cortex, and there was no significant difference between both dministration routes. Histopathological examination of kidney revealed changes of proximal tubular epithelial cells,and there were no differences in the histopathological changes between intravenous infusion and intramuscular injection.
3. Serum concentrations of GM after 30 minutes intravenous infusion were compared with that of intramuscular injection, using the cross-over method. A peaked serum concentration with intravenous infusion occurred immediately after the end of intravenous infusion, whereas that of intramuscular injection occurred 1/2 to 1 hour after injection. Also, there was no significant difference in each time point of serum concentration between both administration routes.

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Antibiotics of tetracycline and macrolide groups are mainly used in treatment ofMycoplasma pneumonia.
In this study, acetylspiramycin (ASPM), an antibiotic of macrolide group, was given to 15 cases ofMycoplasmapneumonia who visited this institute during the period from January, 1980 to March, 1981, and its clinical effects and side effects were investigated. The therapeutic effects were evaluated by days to the normal body temperature, to improvement in cough and to improvement in X-ray findings. The increase in serum antibody value was adopted as the diagnostic index ofMycoplasma infection.
The patients who entered into this study were 7 males and 8 females, ranged from 19 to 60 years of age with an average of 36.3 years. The daily dose of ASPM was 600 to 1,200 mg (potency), and the mean administration period was 18.1 days.
The results obtained were as follows.
1. The temperature fell to the normal within 2 to 7 days.
2. Cough disappeared in 2 days at shortest and in 55 days at longest. The mean period to cough disappearance was 14.5 days.
3. In 10 cases who could be followed up,shadows in X-ray films disappeared in 3 days at shortest and in 40 days at longest. The mean period to shadow disappearance was 18.6 days.
4. As regards clinical effects,marked improvement was obtained in 2 cases,improvement in 9, slight improvement in 4, and no change in 0 (improvement rate: 73.3%).
5. As a side effect,nausea was found in 1 case, but it was improved by discontinuance of administration.

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Susceptibilities of 227 strains of 34 bacterial species to cefatrizine (CFT) were determined by the 2-fold agar dilution method in parallel with the diameter of inhibition zones by the single-disc method, under the experimental condition established by KANAZAWA.
The experiments demonstrated significant correlation between MIC by the dilution method and diameter of inhibition zone in each of conventional assay of the over-night (about 16 hours) incubation,delayed assay (about 24 hours incubation), and rapid assay (after 3-4 or 5-6 hours incubation), thus confirming applicability of the single-disc assay for CFT.
Analysis of the data obtained by using CFT disc containing 30,μg revealed the primary regression equation to be: D (diameter, mm)=25.6-9.6 log MIC (μg/ml) in conventional assay, D=33.2-13.2 log MIC (μg/ml) in delayed assay, D=15.8-4.7 log MIC(μg/ml) in 3-4 hours rapid assay and D=20.2-7.0 log MIC (μg/ml) in5-6 hours rapid assay, respectively.
The range of variations in MICs estimated from the diameter of inhibition zone by the disc test was then calculated in comparison with that in MIC determined by the 2-fold agar dilution assays, as reference for the experimental errors which may be involved in the estimation of MIC of CFT by the single-disc assay.

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Susceptibilities of 169 strains of 30 bacterial species to cefaclor (CCL) were determined by the 2-fold agar dilution method in parallel with the diameter of inhibition zones by the single-disc method, under the experimental condition established by KANAZAWA.
The experiments demonstrated significant correlation between MIC by the dilution method and diameter of inhibition zone in each of conventional assay of the over-night (about 16 hours) incubation, delayed assay (about 24 hours incubation),and rapid assay (after 3-4 or 5-6 hours incubation), thus confirmin applicability of the single-disc assay for CCL.
Analysis of the data obtained by using CCL disc containing 30 μg revealed the primary regression equation to be: D (diameter, mm)=28.2-10.2 log MIC(μg/ml) in conventional assay, D=33.8-13.0 log MIC (μg/ml) in delayed assay, D=17.9-5.1 log MIC (μg/ml) in 3-4 hours rapid assay and D=22.6-7.4 log MIC (μg/ml) in 5 6 hours rapid assay, respectively.
The range of variations in MICs estimated from the diameter of inhibition zone by the disc test was then calculaed in comparison with that in MIC determined by the 2-fold agar dilution assays, as reference for the experimental errors which may be involved in the estimation of MIC of CCL by the single-disc assay.

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Cefoperazone (CPZ), 50-200mg/kg/day, divided into 3 to 4 times/day was drip-infused for 3-20 days to 52 patients (41 patients with acute respiratory tract infection, 6 with urinary tract infection, and 5 with sepsis and/or meningitis). The overall efficacy rate was 92.3%. No adverse reaction was noted. These results indicate the usefulness of CPZ in the treatment of bacterial infections in children.

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T-1982 (cefbuperazone) was evaluated in 25 children with a suspicion of bacterial infections, of the 1confirmed bacterial infections, 18 were shown it be effective (efficacy rate, 85.7%). The diagnosis included pneumonia (4), bronchopneumonia (3), acute bronchitis (4), acute pharyngitis (1), acute laryngitis (1), acute piglottitis (1), acute enterocolitis (3), cervical lymphadenitis (1), acute pyelonephritis (1) and suspected septicemia (2).
The etiologic pathogens recovered were Haemophilus influenzae (4), Staphylococcus aureus (2), almonella typhimurium (1), Salmonella subgenus (1), and enteropathogenic Escherichia coli (2).Among these strains, 7 strains were eradicated after treatment.
A case of suspected septicemia and 2 cases of acute enterocolitis with Salmonella infection were not effectively treated with T-1982.
The serum half-life of T-1982 was 1.2 hours after an intravenous bolus injection. No severe adverse reaction was encountered with the T-1982 therapy. The data suggest that T-1982 is an effective and safe parenteral antibiotic in the reatment of susceptible pediatric bacterial infections.

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T-1982 (cefbuperazone) is a newly developed cephamycin.Clinical studies on this drug were carried out and the results were as follows:
Eighteen patients (pneumonia 13, purulent tonsillitis 1, acute bronchitis 1, cellulitis 1, urinarytract infection 2) were treated intravenously with daily 27.4-100.2mg/kg of T-1982 in 3-4 divided dose for 3-6.7 days.
The overall efficacy rate was 94.4%.
No adverse reactions were observed. Abnormal laboratory data noted were liver dysfunction in 1 case (4.8%), eosinophilia in 2 cases (9.5%), and anemia in 1 case (4.8%).

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T-1982 (cefbuperazone), a new 7 α-methoxycephem antibiotic, was fundamentally and clinically studied, and the following results were obtained.
The antibacterial activities of T-1982 against clinical isolates of S.aureus,E.coli,K.pneumoniae, S. marcescens, P. mirabilis andP. aeruginosa were determined in comparison with those of CER, CEZ, CMZ and CTT. Against S. aureus, CER and CEZ exhibited excellent activity, whereas T-1982 was less active withthe peak MIC of 12.5mu;g/ml even with the inoculum size of 106 cells/ml. The activity of T-1982 was equal to that of CTT and by far superior to that of CER, CEZ and CMZ against E.coli,K.pneumoniae and P. mirabilis,the peak MICs with the inoculum size of 106 cells/ml being≤0.1-0.2μg/ml, 0.1-0.2μg/ml and 0.2-0.39μg/ml, respectively. Against S. marcescens,T-1982 was superior to CMZ and CTT and 48% of the strains were inhibited by 3.13μg/ml or less,whereas all the strains were resistant to CER and CEZ. The MIC of T-1982 against most strains of P. aeruginosa was more than 100μg/ml.
10mg/kg or 20mg/kg of T-1982 was administered by one shot intravenous injection or 1 hour drip infusion to 23 pediatric patients to measure serum levels and urinary recovery. At 30 minutes after one shot injection of 10mg/kg and 20mg/kg, the highest serum levels of 22.0-38.8μg/ml and 52.4-80.0μg/ml were observed, the half-lives being 1.32 hours and 1.76 hours. When given by 1 hour drip infusion, the serum levels attained the peaks of 29.2-42.6μg/ml and 49.0-75.6μg/ml at the end of infusion, the half-lives being 1.24 hours and 1.19 hours. The urinary recovery rates within 6 hours were 74.2-92.5% and 50.2-66.5% by one shot injection and 63.4-84.2% and 53.9-79.0% by drip infusion.
T-1982 was administered at a dose of 50mg/kg by 30 minutes drip infusion to a child with purulent meningitis. The levels of T-1982 in the cerebrospinal fluid at 1 hour after administration were 4.8-6.7μg/ml with the CSF/serum ratios of 4.4-8.4%.
A total of 36 pediatric patients (21 cases of respiratory tract infection, 9 cases of urinary tract infection and each 1 case of purulent cervical lymphadenitis, scarlet fever, purulent meningitis, acute colitis, peritonitis and sinusitis) was treated with 40-80mg/kg/day of T-1982(252.6mg/kg/day in purulent meningitis). The response was excellent in 27 patients and good in 7 patients, the efficacy rate being 94.4%. Diarrhea or eruption were observed in each 1 case. No abnormal laboratory findings were noted in any cases.

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Studies on T-1982 (cef buperazone), 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 0.39μg/ml, and the drug was active even against highly resistant strains to macrolides, lincomycin, tetracycline and chloramphenicol.
2. Peak MICs of T-1982 were 0.78μg/ml against B. pertussis, 0.2μg/ml against E.coli and≤0.05μg/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 63.5-75.9μg/ml at the end of administration and sustained the level of 0.9-2.6μg/ml at 6 hours, the serum half-life (T 1/2) ranging 70 82 minutes. Approximately 20-72% of the dose were xcreted 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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Laboratory and clinical studies were carried out with T-1982 (cefbuperazone) in pediatric infectious diseases. Results were as follows.
1. The average serum concentrations of T-1982 following intravenous injection of 10mg/kg and 20mg/kg were 35.3, 64.7μg/ml at 30 minutes, 25.5, 41.5μg/ml at 1 hour, 12.4, 21.8μg/ml at 2 hours, respectively. Doseresponse was observed. Urinary recovery rates of T-1982 during 6 hours after injection of 10mg/kg and 20mg/kg were 57.3% and 73.6%, respectively.
2. The antibacterial activity of T-1982 against clinically isolated organisms was determined. T-1982 was more active than cefazolin and cefmetazole against K.pneumoniae, H. influenzae and E. coll. It was also effective against ampicillin-resistant E.coli.
3. Thirty-seven patients received daily 30-69mg/kg of T-1982 t. i. d. for 5-9 days. The rate of satisfactory clinical response was 91.9%.
4. Side effects were diarrhea in 4 cases, diarrhe and rash in 1 case and slight elevation of GOT and GPT in 1 case. But these were transient and mild.

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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 0.2μg/ml, respectively. Two of 3 strains of C. freundii were inhibited by 12.5μg/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 0.78μg/ml or less, but the sensitivity of S. aureus (34 strains) distributed 12.5-100μg/ml.
2. T-1982 was administered to each 3 children at a dose of 20mg/kg by one shot intravenous injection or 1 hour drip infusion, or at a dose of 40mg/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 20mg/kg were respectively 74.3, 56.3, 42.3, 17.6, 5.7 and 1.2μg/ml with the mean half-life of 1.01 hours. The values were 32.9, 50.0, 73.7, 27.5, 12.4 and 4.5μ/ml and 1.31 hours by intravenous drip infusion of 20mg/kg and 50.4, 104.7, 136.3, 62.3, 18.6 and 6.9μg/ml and 1.16 hours by intravenous drip infusion of 40mg/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 ubcutaneous 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.coil 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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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 isolatedK. pneumoniae, E. coliandE. 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. Concentrations 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 20 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 in 2 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 filed of pediatrics

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The authors have carried out the laboratory and clinical studies of T-1982 (cefbuperazone). The results were as follows:
The sensitivity was estimated by the plate dilution method on 28 strains ofS. aureus, 26 strains ofE. coli, 27 strains ofK. pneumoniae, 25 strains ofS. marcescens and 14 strains of Proteus sp. isolated from patients.
The distribution of susceptibility of S. aureus was 12.5 25μg/ml and the peak of distribution was 12.5μg/ml. The strains of 84.6% of E. coil were inhibited at concentration of less than 0.39μg/ml. The strains of 77.8% of K. pneumoniae were inhibited at concentration of less than 0.2μg/ml. The strains of 96% of S. marcescens was inhibited at concentration of less than 3.13μg/ml. The distribution of susceptibility of Proteus sp. was 0.39-25 μg/ml.
T-1982 was given by intravenous administration for 5 minutes and drip infusion for 30 minutes a single dose of 20 mg/kg of T-1982 to 2 and 2 children respectively. After intravenous administration of T-1982, the mean serum level was peak 88.4±8.7μg/ml at 15 minutes, 52.5±2.7μg/ml at 1 hour, 4.6±0.15μg/ml at 6 hours respectively. Half-life was 89 minutes.
And after drip infusion of T-1982, the mean serum level was 75.5±3.5μg/ml at 30 minutes and 3.1±0.6μg/ml at 6.5 hours respectively. Half-life was 82 minutes.
The mean urinary excretion rate was 94.7%, 57.4±11.0% up to 6 hours after intravenous administration and drip infusion respectively.
T-1982 was effective in 13 cases out of 13 cases with bacterial infections. No side effects were observed except for 1 case with elevation of serum GOT, 1 case with elevation of serum GPT and 2 cases with eosinophilia.

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T-1982 (cefbuperazone),a new injectable cephamycin antibiotic,was employed for bacterial infections in children, and the following results were obtained.
1. When administered intravenously at a dose of 20mg/kg to a 6-year-old female child,serum levels were 62μg/ml at 30minutes, 39μg/ml at 1 hour, 17.6μg/ml at 2 hours, 6.8μg/ml at 4 hours and 2.9μg/ml at 6 hours with serum half-life (T1/2) of 76 minutes.Urinary excretion rates were 41.0,5.3% and 2.4% respectively at 0-2, 2-4 hours and 4-6 hours,and urinary levels were 820μg/ml, 182μg/ml and 310μg/ml, respectively. The total urinary recovery within 6 hours was 48.7%.
2. A total of 11 cases of pediatric infections was treated with T-1982.The clinical efficacy evaluated for 9 cases,excluding 2 cases of non-bacterial infections,was as follows;excellent in 4,good in 1 out of 5 cases of pneumonia,good in 1 case of cervical purulent lymphadenitis, and excellent in 1,good in 1,poor in 1 out of 3 cases of urinary tract infection.
3. As side effects, mild diarrhea in 1 case and slight elevation of GOT,GPT in 2 cases were observed.
4. These results suggest that T-1982 is of good use for bacterial infections in children and the expectative efficacy is obtained at a dose of 20mg/kg 3 times a day.

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T-1982 (cefbuperazone) was given intravenously to 21 children with the following acute bacterial infections; 13 cases of bronchopneumonia, 2 cases of urinary tract infection, 1 case of subcutaneous abscess, 1 case of cervical purulent lymphadenitis and acute tonsillitis,and 4 cases of acute bronchitis.
Clinical effectiveness was obtained in 20 cases out of 21 cases and bacteriological effectiveness in 7 cases out of 8 cases.
As for the side effects, 1 patient had asymptomatic eosinophilia, but no other laboratory abnormalities were observed.
Above results suggest that T-1982 is a useful antibiotic for treating pediatric patients with various kinds of bacterial infections.

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T-1982 (cefbuperazone) was administered to 20 pediatric patients with various infections by intravenous injection.
The therapeutic efficacy was excellent in 13 cases,good in 6 and poor in 1, the efficacy rate being 95%.
As for side effects, slight elevation of GOT and GPT was observed in 1 case, but disappeared soon after discontinuation of the therapy.

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Laboratory and clinical studies were performed as follows on T-1982 (cefbuperazone),a new cephamycin antibiotic.
1. Susceptibility of clinically isolated bacteria to T-1982,cefazolin (CEZ), cefmetazole (CMZ) and ampicillin (ABPC) T-1982, CEZ,CMZ and ABPC were inactive against β-lactamase producing S.aureus and S.epidermidis.
T-1982 was less active than CEZ,CMZ and ABPC by 2-5 tubes against S.pyogenes,but was found to be more active than CMZ by 1-3 tubes against H. influenzae, K. oxytoca, E. coli, P. vulgaris and P.mirabilis.
2. Serum concentration and urinary recovery Serum concentrations of T-1982 were measured in 6 patients given T-1982 for prophylactic purpose during cardiac catheterization.In 3 patients given 20mg/kg of T-1982 intravenously,the average of peak serum concentration was 71.5μg/ml at 15 minutes after intravenous bolus injection.In 3 patients given 10mg/kg of T-1982 intravenously,the average of peak serum concentration was 54.4μg/ml at 15 minutes after intravenous bolus injection. Urinary recoveries in 5 patients tested were 52.2-94.6% within 9 hours after intravenous bolus injection.
3. Clinical efficacy T-1982 was administered intravenously to 15 patients in doses of 44.1-100mg/kg (67.5mg/kg on average) t.i.d. or q.i.d. for 3-12 days (6.1 days on average); 2 with tonsillitis, 1 with bronchitis, 11 with pneumonia and 1with UTI.The overall efficacy rate was 93.3%,i.e.,efficacy was excellent in 11(73.3%),good in 3(20.0%) and poor in 1(6.7%).
Bacteriological efficacy was excellent,i.e.7 of the 7 strains disappeared.
Slight transient elevation of S-GOT,S-GPT was observed after administration in 1 case,and no other side effect was noted.The above results suggest that T-1982 is a useful antibiotic for treating pediatric bacterial infections,especially due to Gram-negative bacteria.

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T-1982 (cefbuperazone) was given at a daily dose of 42-80mg/kg to 7 children with bacterial infections; 3 with bacterial intestinitis, 1 with bronchitis, 1 with tonsillitis and 2 with urinary tract infections.
Clinical effectiveness was obtained in 6 cases,and the rate was 85.7%.
Bacteriological responses were “disappeared” in 4 Zases,“decreased” in 1 case and “unknown” in 2 cases.
No noticeable side effects were observed except elevation of eosinophil in 1 case.

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T-1982 (cefbuperazone), a new cephamycin antibiotic,was clinically and bacteriologically studied in 25children with bacterial infections. The following results were obtained.
1. The antibacterial activity of T-1982 was determined against clinically isolated bacteria. T-1982demonstrated excellent activity against Gram-negative bacilli, the MICs being<0.39μg/ml against E.coli and K. oxytoca, <1.56μg/ml against H. influenzae.
2. Clinical response was excellent or good in all 24 cases evaluated. The efficacy rate was 100%.
3. As for side effects associated with T-1982, slight and transient elevation of GOT,GPT and eosinophil, slight decrease of platelet and eruption were observed.
From these results, T-1982 is considered to be a useful antibiotic for treating bacterial infections in children.

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T-1982 (cefbuperazone), a newly synthesized cephamycin,was administered in doses of 10 or 20mg/kg by intravenous drip infusion respectively to 2 children and 40mg/kg by intravenous injection to 6 children. Serum levels, urinary concentrations and recovery rates were measured in these cases. Cerebrospinal fluid (CSF) level was also measured in a patient with purulent meningitis. Susceptibility to T-1982, CEZ, CFX, CMZ and LMOX was determined for 19 strains of S.aureus, 13 strains of S. agalactiae, 2 strains of L. monocytogenes, 25 strains of H.influenzae, 30 strains of E. coli, 20 strains of K.pneumoniae, 9 strains of P.mirabilis, 17 strains of P.morganii,8 strains of E. cloacae, 6 strains of C. freundii and 19 strains of S. marcescens. In addition, 38 patients with various infections were given T-1982 in mean daily dose of 92.8mg/kg, in 2-6 divided doses, for a mean period of 8 days, by intravenous injection. Clinical and bacteriological effects were evaluated. Adverse reactions were investigated in a total of 46 patients,including 8 drop out cases. The following results were obtained.
1. After 1 hour drip infusion in doses of 10 or 20 mg/kg, in the former, the mean peak serum level of 2 children was 35.1μg/ml at the end of infusion and the mean half-life was 83.9 minutes, in the latter, the peak serum level of only 1 child was 47.4μg/ml at the end of infusion and the mean half-life was 86.9 minutes.
2. After intravenous injection in doses of 40 mg/kg, the mean peak serum level of 6 children was 236.1μg/ml at 5minutes and the mean half-life was 81.7minutes.
3. The urinary concentration maintained high values, and the urinary recovery rate was 67.4% (10mg/kg case), 58.2% (20mg/kg cases) and 76.9% (40mg/kg cases) up to 7 hours and 6 hours after administration respectively.
4. CSF level was determined in 1 patient with purulent meningitis by L. monocytogenes. After intravenous injection in dose of 40.3mg/kg of T-1982, CSF level was 2.86μg/ml at 66 minutes after administration.
5. In sensitivity tests of 11 species of bacteria to T-1982, CEZ, CFX, CMZ and LMOX by inoculum size of 10⁶cells/ml, antibacterial activity of T-1982 was next to CEZ against S. agalactiaeand next to LMOX against H.influenzae and intraintestinal Gram-negative rods,but less superior to the others against S. aureus and L. monocytogenes.
6. Among the 38 patients with various infections, T-1982 was clinically effective in 84.2% and bacteriologically effective in 93.8%.
7. As adverse reactions, in a total of 46 patients including 8 drop out cases, diarrhea appeared in 2 patients, eosinophilia in 2 patients, elevation of GOT in 1 patient and that of GOT and GPT in 2 patients.

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