The pharmacokinetics of ceftriaxone (Ro 13-9904, CTRX) was studied in 14 children receiving a dose of 10, 20 mg/kg or 1 g as a intravenous bolus. The mean half-lives of CTRX were 4.5, 6.3±0.5 and 5.2±0.7 hours, respectively, while the urinary recovery rates up to 12 hours were 51.7, 48.6 and 48.9%.
Forty-one patients, aged 2 months to 10 years, w ere treated with an intravenous dosage of 10 to 58 mg/kg CTRX every 12 hours for 2 to 29 days. The diseases consisted of upper respiratory tract infections (4), bronchitis (7) pneumonia (18). pyothorax (2), urinary tract infections (4), pertussis (4), meningitis (1) and endocarditis (1). Clinical cures w ere achieved in 38 cases. overall clinical response rate being 92.7%.
No serious side effects were observed, although mild diarrhea was seen in 2 cases.

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Clinical studies on ceftriaxone (Ro 13-9904, CTRX) were carried out and the results were as follows: Twelve patients (acute purulent tonsillitis 1, pneumonia 6, urinary tract infection 5) were treated with CTRX, in doses of 21-48 mg/kg divided 2 times per day for 3.5-8 days intravenously. The overall efficacy rate was 100%. No adverse reactions were observed. No abnormal laboratory data were noted.

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Ceftriaxone (Ro 13-9904, CTRX) was evaluated in 20 children with a suspicion of bacterial infections, 18 were shown to be effective (efficacy rate, 90%). The diagnosis included upper respiratory tract infection (3), bronchitis (3), pneumonia (8) and urinary tract infection (6).
The etiologic pathogens isolated were S. pneumoniae (1), and enteropathogenic E. coli (6). These strains were eradicated after treatment.
No severe adverse reaction was encountered with the CTRX therapy. The data suggest that CTRX is an effective and safe parenteral antibiotic in the treatment of susceptible pediatric bacterial infections.

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Fundamental and clinical evaluation on ceftriaxone (Ro 13-9904, CTRX) was performed and the following results were obtained.
1. As to bacteriological efficacy, bacteria were reduced in the case with S. panama bacteremia, while they were eradicated within 2 to 5 days after CTRX administration in 2 cases with acute urinary tract infections and 1 with recurrent urinary tract infection, both caused with E. coli, and in 1 with acute urinary tract infection with P. mirabilis.
2. The clinical efficacy was excellent in 2 cases and good in 3, the efficacy rate being 100%.
3. No side effects were observed to require the withdrawal of CTRX.

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Ceftriaxone CTRX was evaluated about its antibacterial activity against clinical isolates at our department and tried clinically in 10 children of 6 months to 10 years and 6 months of age. The antibacterial activity was equal to cefotaxime or higher while the clinical results were almost satisfactory. Three out of 4 strains were eradicated (75%).
As to the adverse reaction, eosinophilia was observed only in 1 case.

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Fundamental and clinical evaluation on ceftriaxone (Ro 13-9904, CTRX) was performed in the field of pediatrics and the following results were obtained.
1. The antibacterial activity of CTRX was determined against clinically isolated strains at our department. CTRX was definitely superior to CEZ and CMZ and almost equal or slightly superior to CTX in activity against Gram-negative bacteria, while the MIC of CTRX against Gram-positive bacteria was higher than that of CEZ and CMZ and about equal to that of CTX.
2. The blood concentration of CTRX after one shot intravenous injection with 10mg/kg was 67.98μg/ml at 15 minutes, 51.96μg/ml at 30 minutes, 37.51μg/ml at 1 hour, 28.91μg/ml at 2 hours, 20.71 μg/ml at 4 hours, 13.97μg/ml at 6 hours and 6.45μg/ml at 12 hours, while the half-life time was 3.74 hours.
The blood concentration of CTRX after one shot intravenous injection with 20mg/kg was 179.55μg/ml at 15 minutes, 120.01μg/ml at 30 minutes, 100.01μg/ml at 1 hour, 53.75μg/ml at 2 hours, 33.13μg/ml at 4 hours, 26.41μg/ml at 6 hours and 21.49μg/ml at 12 hours, while the half-life time was 4.15 hours.
The blood concentration of CTRX after intravenous drip infusion for 1 hour with 10mg/kg was 19.54μg/ml at 15 minutes, 27.19μg/ml at 30 minutes, 36.57μg/ml at 1 hour, 23.83μg/ml at 2 hours, 19.69μg/ml at 3 hours, 14.46μg/ml at 5 hours, 11.02μg/ml at 7 hours and 7.27μg/ml at 13 hours, while the half-life time was 6.59 hours.
The blood concentration of CTRX after intravenous drip infusion for 1 hour with 20mg/kg was 61.72μg/ml at 30 minutes, 108.1μg/ml at 1 hour, 54.95μg/ml at 2 hours, 35.68μg/ml at 3 hours, 28.13μg/ml at 5 hours, 20.51μg/ml at 7 hours and 11.43μg/ml at 13 hours, while the half-life time was 4.23 hours.
There was noticed a tendency of the blood level being elevated by consecutive administration.
3. The urinary recovery rate of CTRX ranged from 36.5 to 71.6%.
4. The excretion rate of CTRX into the cerebrospinal fluid ranged from 5.2 to 11.6%.
5. The excretion rate of CTRX into the pleural fluid was 31.0%.
6. The clinical efficacy rate was 87.5% (excellent or good) in 8 children with infections treated with CTRX.
7. The eradication of bacteria was observed in all of 5 cases bacteriologically evaluated.
The identified bacteria consisted of Klebsiella in 3 cases, E. coli in 1 case and S. marcescens in 1 case.
8. As adverse reactions, thrombocytosis and diarrhea were seen each in 1 case.

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Ceftriaxone (Ro 13-9904, CTRX) was evaluated for its safety and efficacy in 33 children with various bacterial infections including 10 cases of bacterial meningitis. CTRX was effective in all but 1 case who had acute mucositis due to a resistant strain of Enterobacter cloacae. The serum half-life (T1/2β) was 4.5±1.6 hours after an intravenous bolus injection in children. Cerebrospinal fluid levels of CTRX in the acute phase of bacterial meningitis w ere 7.69±4.75mcg ml. The only side effect was mild to moderate diarrhea observed in 10 of the 33 cases, but in no case w as it necessary to discontinue the drug.

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Fundamental and clinical evaluation on ceftriaxone (Ro 13-9904, CTRX) was performed. CTRX was compared with CEZ, CMZ, CTX and LMOX in the antibacterial activity against the clinical isolates such as S. aureus, E. coli, P. mirabilis, K. pneumoniae and S. marcescens. Against S. aureus, the MIC of CTRX ranged from 0.2 to > 100 μg/ml with a peak of 3.13 μg/ml, showing that CTRX was almost equal to CTX in activity, slightly superior to LMOX and much inferior to CMZ and CEZ, although some strains were not susceptible to CEZ.
Against the intestinal strains of E. coli, K. pneumoniae and P. mirabilis, the MIC distribution of CTRX was similar to that of CTX and LMOX while CTRX showed the MIC as high as 3.13 μg/ml or above against 44% of all strains including the β-lactamase producing strains of E. coli and K. pneumoniae, indicating a slight tendency of their becoming resistant. The MIC peaks against E. coli, K. pneumoniae and P. mirabilis were ≤ 0.1, 0.39 and ≤ 0.1 μg/ml, respectively.
As to S. marcescens which is drawing attention as a causative agent for infections inside of hospitals or those among young infants, CTRX inhibited 84% of the strains at 3.13 μg ml, showing a definite superiority to CEZ and CMZ and a slight superiority to CTX and LMOX.
The serum concentration after a single intravenous injection with 40mg/kg reached a mean peak of 168.8 μg/ml at the first bloodsampling (at 30 minutes) and gradually decreased to 137.5 μg/ml at 1 hour, 30.9 μg/ml at 6 hours, 12.6 μg/ml at 12 hours and 3.8 μg/ml at 24 hours, while the half-life time was 6.0 hours. The comparison of the serum level by 1 hour intravenous drip infusion between the dosage groups of 20mg/kg and 40mg/kg revealed that the former group reached a peak of 85.4 μg/ml at the termination of drip while the latter's peak was 176.6 μg/ml observed during the drip (30 minutes after the initiation of drip). The respective levels of the 2 groups were 15.4 and 32.1 μg/ml at 6 hours, 5.1 and 15.0 μg/ml at 12 hours, and 1.6 and 4.1 μg/ml at 24 hours, indicating a distinct dose-response 2 hours after the initiation of drip administration. The half-life times were 4.9 and 6.2 hours, respectively, which are the longest among the cephalosporins presently being developed. The urinary recovery rates evaluated in 11 cases were similar to those of other cephalosporins, ranging from 44.5 to 76.8%.
The levels of CTRX in the cerebrospinal fluid (CSF) of 2 children with meningitis, unlike other cephalosporins, showed only a small difference between the acute period and the recovery period, ranging from 5.9 to 13.3 μg/ml, while the rate of CTRX level in the CSF to the serum was 7.2 to 30.9%, indicating a high excretion despite the fact that some sample was collected as late as on the 20th day.
CTRX was administered into a total of 31 cases (33 diseases) consisting of 4 with purulent meningitis 1 with mediastinal abscess 5 with septicemia 14 with respiratory tract infections, 5 with urinary tract infections, 2 with lymphadenitis, 1 with peritonitis and 1 with cellulitis; 2 cases had a complication. The efficacy was good or higher in 28 cases (30 diseases) out of 30 cases (32 diseases), the efficacy rate being 93.3% (93.8%).
The dosage was in principal 50mg/kg twice daily for meningitis and septicemia and ≤60mg/kg, day in many cases for other infections. It was not necessary to administer it more than twice a day even for such serious diseases as meningitis and septicemia. No special adverse reactions were observed except for erythema or urticaria in 2 cases and elevation of GOT, GPT in 1 case.

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Fundamental and clinical evaluation on ceftriaxone (CTRX, Ro 13-9904) was performed in the pediatric field and the following results were obtained.
1. The MIC of CTRX against the recently isolated 10 strains of B. pertussis was ≤0.05μg/ml at inoculum size of 10⁶ CFU/ml.
2. The blood level of CTRX after intravenous drip infusion with 10 to 20mg/kg for 30 minutes to 1 hour reached a peak ranging from 45.3 to 137μg/ml at the end of infusion. The effective blood level was maintained up to 12 hours to be 3.52 to 26.7μg/ml at that time. The half-life time was over 6 hours in most cases, but the multiple intravenous dosage did not cause any elevation of the blood level.
3. The urine excretion rate till 12 to 24 hours after intravenous drip infusion ranged from 58.2 to 84.2%.
4. The excretion of CTRX into the cerebrospinal fluid was favorable in the acute period when administered by intravenous drip infusion in the child with S. pneumoniae purulent meningitis, which was considered to be satisfactory for treatment against the bacteria susceptible to CTRX. The active CTRX was transferred into the feces by the multiple dosage.
5. CTRX was administered by intravenous drip infusion in 26 cases with acute pediatric infections. The clinical efficacy was observed in all the cases with upper/lower respiratory tract infections including bronchopneumonia and pertussis, and the cases with acute urinary tract infections caused by ABPC-resistant E. colt, administered by intravenous drip infusion twice daily with about 40-50mg/kg/day.
The bactericidal efficacy was seen against all bacteria except Salmonella.
6. CTRX by intravenous drip infusion was effective against S. pneumoniae purulent meningitis; the clinical symptom was rapidly improved while the culture of causative strains from the cerebrospinal fluid turned negative.
7. Although CTRX was clinically effective against Salmonella enteritis and typhoid, bacteriological and symptomatological relapses were observed in some cases. An increase in dose of CTRX is considered to be needed for these diseases.
8. No adverse reaction was found clinically but soft stool in 1 case while eosinophilia and throm-bocytosis were observed each in 1 out of 30 cases in laboratory test.
9. The efficacy was good or higher in all the 26 cases (100%) administered by intravenous drip infusion.
The above-mentioned results indicate that CTRX is useful in the pediatric field.

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Fundamental and clinical evaluation of ceftriaxone (CTRX) was performed in the pediatric field and the following results were obtained.
1. The MIC of CTRX against E. coli isolated from urinary tract infections in children ranged from ≤0.024 to 0.39mcg/ml except for 1 strain. CTRX was superior to other 3rd generation cephalosporins such as CPZ and LMOX, showing effectiveness also against ABPC-resistant bacteria.
2. The clinical efficacy and bacteriological efficacy in 6 children consisting of 5 with respiratory tract infections and 1 with a urinary tract infection were 83% and 100%, respectively. As to the adverse reaction, diarrhea was observed in 2 cases.
3. The determination of PIVKA-II performed during the therapy with CTRX, which is observed when vitamin K is deficient, showed positiveness in 2 cases out of 6 cases including 1 which the clinical efficacy could not be evaluated. The test of platelet function in 3 cases found no inhibition of agglutination.
Twice-daily administration with 20mg/kg CTRX was considered to be a useful and safe method for treatment of bacterial infections in children, although attention should be taken not to cause vitamin K deficiency as in other 2nd and 3rd generation cephalosporins.

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Fundamental and clinical evaluation of ceftriaxone (Ro 13-9904, CTRX) was performed in the pediatric field.
1. Antibacterial activity
The MIC₈₀ of CTRX against clinical isolates such as S. aureus (23 strains), S. pyogenes (23 strains), E. coli (20 strains), K. pneumoniae (23 strains), H. influenzae (15 strains) and P. aeruginosa (23 strains) were 6.25μg/ml, 0.024μg/ml, 0.20μg/ml, 0.05μg/ml, ≤0.006μg/ml and 12.5μg/ml, respectively. The antibacterial activity of CTRX was therefore poor against S. aureus and P. aeruginosa, but quite excellent against S. pyogenes, E. coli, K. pneumoniae and H. influenzae.
Compared with cefotaxime (CTX), cefoperazone (CPZ), cefmetazole (CMZ), cefazolin (CEZ) and ceftazidime (CAZ), CTRX was the highest in the antibacterial activity against H. influenzae, next to CTX against S. pyogenes, E. coli and K. pneumoniae, similar to CTX, CPZ and CAZ against S. aureus and similar to CTX against P. aeruginosa.
2. Absorption, Excretion
The mean serum levels of CTRX after an intravenous one shot injection with about 20mg/kg in 3 children aged 10 to 14 years were 160.0±23.3μg/ml after 1/4 hour, 134.3±27.5μg/ml after 1/2 hour, 115.0±33.2μg/ml after 1 hour, 95.3±28.4μg/ml after 2 hours, 75.3±14.5μg/ml after 4 hours, 30.3±13.5μg/ml after 12 hours and 8.2±3.1μg/ml after 24 hours, while the half-life time was 5.92±0.43 hours on the average.
The mean urinary levels were 1,060±461μg/ml from 0 to 2 hours, 309±122μg/ml from 2 to 4 hours, 375±83μg/ml from 4 to 6 hours, 237±77μg/ml from 6 to 12 hours and 122±23g/ml from 12 to 24 hours, the mean urinary recovery rate up to 24 hours being 38.9±13.6%.
3. The concentration in the cerebrospinal fluid
The mean levels of CTRX in the cerebrospinal fluid of the patients with purulent meningitis were 4.30±4.22μg/ml 1 hour after an intravenous one shot injection with 42 to 51mg/kg, 4.64±3.53μg/ml after 3 1/2 hours to 6 hours, 3.79±2.15μg/ml after 7 1/2 hours to 12 hours and 1.79±0.23μg/ml after 19 hours.
4. Clinical results
The clinical results of CTRX in 1 case with acute bronchitis, 1 with chronic bronchitis, 5 with acute pneumonia, 3 with purulent meningitis, 5 with acute pyelonephritis, 1 with acute purulent osteomyelitis, 1 with purulent lymphadenitis, 1 with acute enteritis were excellent in 13 cases, good in 4 and poor in 1, the efficacy rate being 94.4% (excellent and good).
As to the bacteriological efficacy against the causative pathogens such as S. aureus (1 strain), S. agalactiae (2 strains), H. infiuenzae (4), E. coli (4), K. pneumoniae (1), C. freundii (1), S. typhimurium (1) and P. aeruginosa (2), all the strains other than S. aureus (1) and P. aeruginosa (2) were eradicated, the eradication rate being 81.3%.
No clinical adverse reactions were observed, while the laboratory test abnormalities were found in 4 cases (elevation of GOT and GPT in 2 and eosinophilia in 2).

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The authors have carried out the laboratory and clinical studies of ceftriaxone (Ro 13-9904, CTRX) and obtained the following results.
The antibacterial activities of CTRX against the clinical isolates of S. aureus, E. coli, K. pneumoniae, E. cloacae, E. aerogenes, S. marcescens, Citrobacter sp. and P. aeruginosa were measured by the agar dilution method with inoculum size of 10⁶ cells/ml.
The susceptibility distribution of S. aureus to CTRX ranged from 0.2 to 12.5μg/ml, and the peak of distribution was 3.13μg/ml. The peak of susceptibility distribution of E. coli and K. pneumoniae were 0.1μg/ml or lower, and the distribution of E. aerogenes and E. cloacae ranged from 0.1 to 100μg/ml, Citrobacter sp. and S. marcescens, from 0.1 to 12.5μg/ml and that of P. aeruginosa, from 0.39 to 100μg/ml or more.
For pharmacokinetic study, CTRX was given in a single dose of 10mg/kg in 1 child and 20mg/kg in 2 children by drip infusion for 1 hour.
After drip infusion of CTRX in a single dose of 10mg/kg, the peak serum level was 61.4μg/ml on completion of the infusion, and 8.43μg/ml at 12 hours. Half-life time was 4.6 hours. With drip infusion of CTRX in a single dose of 20mg/kg, the peak serum level was 105.5μg/ml on completion of the infusion, and 19.1μg/ml at 12 hours. Half-life time was 8.7 hours.
CTRX was effective all ceses out of 8 cases with bacterial infection.
No side effect was observed except for elevation of serum GOT in 2 cases and eosinophilia in 1 case.

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Ceftriaxone (Ro 13-9904, CTRX), a new parenteral cephalosporin, was used for pediatric infections and the following results were obtained.
1. CTRX was administered twice daily by intravenous injection with about 20mg/kg in 6 cases consisting of 2 cases with purulent lymphadenitis of the neck, 2 with urinary tract infection, 1 with sepsis and pyelonephritis and 1 with sepsis and purulent lymphadenitis of the neck. The result was excellent in 4 and good in 2.
2. One case withH. influenzae meningitis, receiving 50mg/kg CTRX by intravenous injection twice daily, showed an excellent response without having any sequela.
3. Among those mentioned above, diarrhea in 2 cases and elevated GOT and GPT in 2 were observed, all of which were transitory and not serious.
4. The blood level of CTRX at 1/2, 1, 2, 4, 6 and 8 hours after intravenous injection with 20mg/kg to a girl of 8 years and 8 months of age with urinary tract infection was 114, 86, 70, 42, 29 and 21.8μg/ml, respectively. The half-life time was 3.5 hours while the urinary recovery rate up to 6 hours was 58.0%.
5. The concentration in the cerebrospinal fluid of 1 case withH. influenzae meningitis ranged from 2.1 to 8.2μg/ml at 3 hours after administration and from 1.15 to 2.65μg/ml after about 12 hours (prior to the next administration).
6. The above-mentioned results suggest that CTRX is a new antibiotic useful for pediatric infections caused with susceptible bacteria and is effective by intravenous injection with 10mg/kg twice daily for moderate infections and with 20mg/kg twice daily for severe ones, except for meningitis. As for purulent meningitis, the administration dosage and frequency will have to be further examined based on the intravenous injection with 50mg/kg twice daily.

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Fundamental and clinical evaluation on ceftriaxone (Ro 13-9904, CTRX), a newly-developed injectable cephem antibiotic was performed as follows. The serum and urine concentrations of CTRX as well as the urinary recovery rate were determined in 7 children at 3 different dose levels; 3 cases administered with 10mg/kg, 3 with 20mg/kg and 1 with 48mg/kg by one shot intravenous injection. The concentration in the cerebrospinal fluid was determined in 1 case of purulent meningitis associated with bacteremia, administered by one shot intravenous injection with 47.6mg/kg. CTRX was also examined in its clinical and bacteriological efficacies by one shot intravenous injection for 8 days on average in a mean daily dose of 46.5mg/kg, divided into twice a day in 31 cases, 3 times in 1 case, and 4 times changed from twice in 1 case; in a total of 33 children consisting of 3 with tonsillitis, 1 with chronic bronchitis, 20 with pneumonia, 2 with purulent meningitis associated with bacteremia, 3 with urinary tract infections, 1 with osteomyelitis associated with phlegmon, 3 with purulent lymphadenitis. The adverse reactions and laboratory test values were examined in a total of 40 cases, i. e., the above-mentioned 33 cases plus the 7 drop-out cases in which the clinical efficacy could not be evaluated. The results were as follows.
1. The serum levels of CTRX in 7 cases consisting of 3 administered with 10mg/kg, 3 with 20mg/kg and 1 with 48mg/kg reached their peaks 5 minutes after one shot intravenous injection and the mean values of them were 93.6mcg/ml, 143.0mcg/ml and 558.0mcg/ml, respectively, indicating the existence of a dose-response among these groups, while the half-life times were 4.41, 5.86 and 4.09 hours.
2. Among the 7 cases examined in the urinary levels as well as the serum levels, the 3 cases administered with 10mg/kg reached the mean peak of 334.0mcg/ml 2 to 4 hours after administration, while another 3 cases administered with 20mg/kg showed peaks of 793.0, 522.0 and 536.0mcg/ml, respectively, 2 to 4 hours, 4 to 6 hours and 6 to 12 hours after injection; this dispersion being partly because of that the urine specimen was unable to be collected regularly every hour in this dose group. In the case administered with 48mg/kg, urinary level reached the highest value of 6,100.0mcg/ml from 0 to 2 hours.
The mean urinary recovery rates up to 12 hours of 10mg/kg and 20mg/kg groups were 37.0%, 42.3%, respectively, and that of the case of 48mg/kg was 54.9%.
3. CTRX was administered by one shot intravenous injection to the case with purulent meningitis associated with bacteremia caused by H. influenzae on 3, 8 and 18 days of illness and the levels in the cerebrospinal fluid determined 70, 60 and 60 minutes after administration were 4.89, 5.29 and 2.15mcg/ml, respectively. CTRX's excretion into the cerebrospinal fluid was good at the acute period.
4. The clinical efficacy was good or higher in 32 out of 33 cases (97.0%).
5. Among the 33 cases, the bacteriological efficacy was able to be evaluated in 13 out of 15 cases where causative pathogens or possible pathogens were isolated. The eradication of bacteria was observed in 12 cases, indicating a high eradication rate of 92.3% (12/13).
6. The adverse reactions, examined in the 40 cases including 7 drop-outs, consisted of feeling warm, facial edema and urticaria each in 1 case, and diarrhea in 2 cases, while the laboratory test found leukopenia in 1, eosinophilia in 2, elevation of GOT in 1 and elevation of GOT and GPT in 2 cases.

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Ceftriaxone was used in single intravenously dose of 1g to treat 20 men with gonorrhoea caused by penicillinase-producing Neisseria gonorrhoeae (PPNG) and non-PPNG. Of 14 patients followed up, 13 (92.9%) were cured. Cure rates for PPNG infections and non-PPNG infections were 100% and 90.9% respectively.
No side effect was observed except 1 case of vomiting out of 20 cases.
It is concluded that this drug is safe and effective in treating both PPNG and non-PPNG infections.

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Sulbactam/cefoperazone (SBT/CPZ) was evaluated in the treatment of pediatric patients to have the following results:
1. Peak serum concentrations which occurred just after the drip infusion of 20mg/kg SBT/CPZ were 36.4μg/ml and 8.6μg/ml for CPZ and SBT, respectively. The half-life of CPZ was 1.91 hours, and that of SBT, 0.97 hour. Following the 40mg/kg drip infusion, the peak serum concentration of CPZ was 79.1μg/ml, and that of SBT, 27.0μg/ml. The half-lives were 1.99 hours for CPZ, and 1.07 hours for SBT, respectively.
2. In 6 hours after drip infusion of 20mg/kg and 40mg/kg 21.7, 37.0% of CPZ and 41.6, 85.6% of SBT were excreted in urine.
3. Daily doses of about 50-90mg/kg SBT/CPZ were administered by intravenous or drip infusion to 26 pediatric patients with acute infections such as lacunar tonsillitis, bronchitis, bronchopneumonia, suppurative diseases caused by Staphylococcus (staphylococcal scalded skin syndrom), purulent parotitis, cervical lymphadenitis, phlegmon and acute UTI related with ABPC/CPZ resistant betalactamase producing E. coli. SBT/CPZ demonstrated the bacteriological effect on all the causative organisms. The clinical efficacy was also confirmed with the efficacy rate of 88.5%.
4. No side effects were observed in all the cases though transient eosinophilia developed in 2 patients.

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Sulbactam/cefoperazone (SBT/CPZ) was administered to 8 cases with gynecologic infections including pelvic peritonitis (2 cases), pyometra (2 cases), acute adnexitis, BARTHOLIN abscess, endometritis and infected lymphocyst. The clinical efficacy was assessed as effective in 7 cases and poor in 1 case. The effective rate was 87.5%.
No adverse reactions including clinical signs were observed. But slight elevation of GOT was observed in 1 case.

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Concentrations of sulbactam/cefoperazone (SBT/CPZ) in the pelvic dead space exudate were examined in 5 patients who received radical hysterectomy due to uterocervical cancer. Data analysis was performed by the simulation curves prepared from pharmacokinetics parameters using a three-compartment model. Following 1 hour intravenous drip infusion of 2g of SBT/CPZ, the mean drug concentration in venous blood was 50.62 μg/ml for SBT and 120.16 μg/ml for CPZ at 1 hour after start of the infusion. The peak SBT level in the pelvic dead space exudate was 21.24 μg/ml at 1.58 hours after start of the infusion. The peak CPZ level was 19.13 μg/ml at 3.46 hours after start of the infusion.
In the treatment of 4 cases with gynecological infections, the clinical efficacy of SBT/CPZ was assessed as effective in 3 cases and poor in 1 case.

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Sulbactam, cefoperazone (SBT/CPZ), a new developed antibiotic, was clinically studied. The following results were obtained.
Total of 5 cases comprising 1 with endometritis, 3 with BARTHOLIN'S abscess, 1 with pyometra (due to corpus cancer) were treated with SBT/CPZ at a dose of 1g twice daily for 4-5 days by intravenous injection or intravenous drip infusion.
The clinical response was good in all cases. A case with pyometra did not respond to the therapy in bacteriologically.
Side effects and abnormal laboratory findings due to the drug were not noted.

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Sulbactam (SBT), a new β-lactamase inhibitor, in combination with cefoperazone (CPZ) was studied for the clinical efficacy in the field of obstetrics and gynecology.
SBT/CPZ was given to 5 cases with the following infections; 2 of pyometra, 2 of endometritis and 1 of abscess of adnexa. Clinical efficacy was good in 3 cases and poor in 2 cases.
Bacteriologically, only 1 strain of P. vulgaris was β-lactamase producer but was persisted after treatment.
Neither side effects nor abnormal laboratory findings was observed.

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Fundamental and clinical studies on sulbactam/cefoperazone (SBT/CPZ), a newly developed combined β-lactam antibiotics, were carried out and the following results were obtained.
1. Each concentration of SBT and CPZ was examined in serum and internal genital organs after single intravenous administration of 2.0 g dose of SBT/CPZ. Each venous serum level of SBT and CPZ was 41.5 μg/ml, 122.3 μg/ml at 30 minutes after administration respectively. The transfer of SBT and CPZ to internal genital organs was similarly good.
Each concentration of SBT and CPZ was examined in serum and retroperitoneal fluid after 1 hour drip infusion of 2.0 g dose of SBT/CPZ. The transfer of SBT and CPZ to retroperitoneal fluid was similarly excellent and the transfer ratio vs. serum level of the former was about 76.2-321.7%, and the latter was about 27.2-93.2% respectively.
2. In clinical trial, SBT/CPZ was given to 10 patients with obstetrical and gynecological infections. The efficacy was evaluated as good in 9 patients and poor in 1 patient.
As the side effects, diarrhea was appeared in 1 case. In laboratory findings, a transient elevation of serum transaminase was noticed in another one case.
From the above results, it was concluded that SBT/CPZ was useful drug for infections in the field of obstetrics and gynecology.

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Fundamental and clinical studies on sulbactam/cefoperazone (SBT/CPZ), a combination drug of sulbactam and cefoperazone, were carried out in the field of obstetrics and gynecology. The following results were obtained:
1. Transfer into female genital organ tissues
Following 1 hour intravenous drip infusion of SBT/CPZ, favourable transfers of both of SBT and CPZ to female genital organ tissues and pelvic dead space exudate were observed.
2. Clinical evaluation
A total of 12 cases comprising 6 with intrauterine infection, 1 with pyometra, 1 with abscess of portio vaginalis, 2 with parametritis, 1 with pelvioperitonitis and 1 with purulent lymphocyst was treated with SBT/CPZ. Clinical efficacy was excellent in 6 cases, good in 5 cases and poor in 1 case, with overall efficacy rate of 92%.
The bacteriological efficacy was judged as eradicated in 3, and as decreased in 2 out of 5 evaluable cases. In all of the 5 cases, isolated organisms were β-lactamase producing organisms.
No notable side effects or abnormal laboratory findings were observed except 1 case with elevations of GOT and GPT.

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The study was done to evaluate the usefulness of sulbactam/cefoperazone (SBT/CPZ) injection for the treatment of infections in the field of obstetrics and gynecology. Fundamental and clinical studies were made and the following results were obtained.
In the clinical studies, SBT/CPZ was given to 19 cases with female genital organ infections. As for the clinical effects, responses were excellent in 4 cases, good in 15 cases among 19 cases in total. The efficacy rate was 100%. The efficacy rate on disease was 100% in all cases (9 cases of puerperal uterine infection, 1 case of endometritis, 1 case of pyometra, 5 cases of adnexitis, 2 cases of pelveoperitonitis and 1 case of abscess of vulva). As for causative bacteria, the efficacy rate was 100% for all infections due to single or mixed infection, due to aerobic Gram-negative,-positive or anaerobic bacteria. Side effect was observed in 1 case with diarrhea. SBT/CPZ showed a satisfactory clinical efficacy and a potent bacteriological effect in treatment of the infection in the field of obstetrics and gynecology, and it has been concluded that SBT/CPZ will be a useful addition to the antibiotics for the therapy of these infections.

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Sulbactam (SBT), a new β-lactamase inhibitor, in combination with cefoperazone (CPZ) to 1 to 1 was clinically studied in the field of obstetrics and gynecology.
SBT/CPZ was administered to 13 subjects at a daily dose of 2g in 2 divided dose by intravenous infusion for 4-6 days.
The subjects were patients with the following infections: 2 of intrauterine infections, 5 of intrapelvic infections, 4 of adnexitis and 2 of vulvar infections.
The overall clinical efficacy was good in all. Neither adverse reactions nor abnormal laboratory findings were observed in any of the cases.

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Sulbactam/cefoperazone (SBT/CPZ), a combination drug of SBT and CPZ, was administered to 5 cases with obstetrical and gynecological infections in a daily dose of 2-6g for 3-5 days. Clinical efficacy was good in 4 cases and poor in 1 case with adnexitis. Bacteriologically, organisms were detected in 2 out of 5 cases, β-lactamase producing P. aeruginosa was detected in 1 case, but, their bacteriological responses were not clarified.
Neither side effect nor abnormal laboratory findings due to this drug were observed.
From the results we concluded that SBT/CPZ was an effective and safe antibiotic in the field of obstetrics and gynecology.

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