In vitro activity of piperacillin (PIPC) against 150 recent clinical isolates from obstetric and gynecologic infections was performed in comparison with sulbenicillin (SBPC), cefmetazole (CMZ), cefotiam (CTM) and cefsulodin (CFS). At 6.25μglml PIPC inhibited 93% of S. epidermidis, 86% of S. faecalis, 67% of E. coli and 80% of Klebsiella. At 0.2μg/ml PIPC inhibited 100% of Peptococcus, 73% of Peptostreptococcus and 100%, of B. melaninogenicus group. At 3.13μg/mi PIPC inhibited 71% of B. fragilis 9 strains, B. distasonis 3 strains, B. thetaiotaomicron 1 strain, B. ovatus 1 strain.PIPC was constantly more active than SBPC, and it was especially more active against S. faecalis, Peptococcus, Peptostreptococcus and B. melaninogenicus group than other antibiotics. These findings show that PIPC is a broad spectrum penicillin against both Gram-positive and Gram-negative organisms including anaerobic organisms.
PIPC was administered to 5 patients intravenously and all cases proved to be effective. No side effects and no abnormalities in laboratory findings were observed.
These results suggest that PIPC may be highly effective in the treatment of bacterial infections.

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We administered piperacillin (PIPC) to patients with obstetrical and gynecological infectious diseases and obtained the following results.
1.Sixteen patients were administered PIPC at a dose of 4 or 9 g by dripping infusion 2 or 3 times a day for a period of 4-14 days. Eight cases had cancer as their underlying disease (including cervical cancer etc.).The clinical effect was good in 3 of these 8 patients with cancer so that the efficacy rate was 37.5%.But the other 8 cases without cancer all responded effectively, so their efficacy rate was 100%.The efficacy was good in 11 out of 16 cases so the overall efficacy rate was 68.8%.
2.No side effect was observed.
3.No adverse reaction in laboratory findings (including hematological findings, hepatic function tests, renal function tests) was observed.

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We conducted a study on the utility in the obstetric and gynecological field of piperacillin (PIPC) which is a broad spectrum penicillin developed here in Japan.
After administration of PIPC by intravenous one shot injection or intravenous dripping infusion the yield of PIPC to the various uterine tissues was a favorable 30-40% in comparison with the serum concentration and the discharge from retroperitoneum was about 100% to 300% in 4 hours.Thus it is thought to be useful in the treatment of infections of the retroperitoneum.
During a clinical trial PIPC was administered to 16 patients with obstetrical and gynecological infections and it proved to be excellent in 4 patients, good in 10 patients and ineffective in 2 patients. Thus an overall efficacy rate of 87.5% was obtained.The only side effects observed was a slight transitory abnormality of liver function in 2 patients.
Thus in the overall evaluation, this drug was considered to be useful in the treatment of infections in the obstetric and gynecological field.

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We administered piperacillin (PIPC), a semisynthetic penicillin antibiotic, to 11 patients with obstetrical and gynecological infections and obtained the following results.
1.PIPC was administered at a dose of 1 or 2 g by intravenous bolus injection or dripping infusion 1 or 2 times a day for a period of 3-8 days.
The clinical effect was excellent in 5 cases and good in 6 cases and all the cases showed good effectiveness.These included good in 1 case of adnexitis, excellent in 3 cases and good in 1 case of intrauterine infections, excellent in 2 cases and good in 2 cases of pelvic inflammatory diseases and good in 2 cases of bartholinitis.
Bacteriological findings indicated that S.faecalis, Staphylococcus, E.coli, K.pneumoniae, P.magnus, etc.isolated in 6 cases were eradicated after the administration of this drug.
2.Neither side effects nor abnormalities in laboratory findings caused by this drug were observed.
3.Based on these results PIPC should be considered a very safe and useful drug for treating obstetrical and gynecological infections.

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1.Tissue concentrations of piperacillin (PIPC) between 80 to 150 minutes after the completion of 2g/1 hour dripping infusion were 4.6-6.4μg/g in the uterus, ovary and oviduct.These concentrations were higher than 80% MIC of the causative organisms, including Staphylococcus aureus, Escherichia coli, Proteus mirabilis, Bacteroides and Peptococcus, isolated from infections in the field of obstetrics and gynecology.
2.The PIPC concentration in the retroperitoneal space exudate reached a peak value of 34.7μg/ml at 2 hours after the completion of 2g/l hour dripping infusion and thereafter maintained a constant level.These concentrations were sufficient for the therapy of parametritis.
3. We administered PIPC at 4g per day for a period of 4-8 days to 4 patients with obstetrical and gynecological infectious diseases.All cases proved to respond effectively.No adverse effects and abnormal laboratory findings were observed.
From the above, we considered that PIPC was an effective and safe antibiotic against infections in the field of obstetrics and gynecology.

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We studied piperacillin (PIPC) clinically to evaluate its utility and safety, and obtained the following results.
PIPC was given at a daily dose of 1-4g for 3-10 days by bolus injection or dripping infusion to 18 patients with various infections in the field of obstetrics and gynecology.
Four of 5 cases with intrauterine infection, 2 of 3 cases with focus infection of uterine cancer, 2 cases with perinatal intrauterine infection, 2 of 6 cases with adnexal infection and 2 cases with vulvar infection proved to respond effectively.
The overall efficacy rate was 66.7%.
No side effect or abnormal laboratory findings were observed except for 1 case with rash.

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Human pharmacokinetics and clinical studies of piperacillin (PIPC) were carried out and the following results were obtained.
1. Transference into various uterine tissues
PIPC transference into various uterine tissues was 27.3-67.9% (the ratio with respect to uterine artery blood level) at 1 hour after the completion of PIPC 1 or 2 g dripping infusion for 1 hour in S cases.
2.Transference into retroperitoneal space exudate
PIPC level in retroperitoneal space exudate shoWed the peak level 38.0μg/ml at 30 minutes after the completion of PIPC 2 g dripping infUsion for 1 hour in 1 case. The pattern of the concentration trends was more continuous than that of venous blood level.
3. Clinical study
We i.dmitiiitered PIPC to patients wiih pelvioperitonitis in 3 cases, Puefpera.I fever in 1 case and wound infection in 1 case at a dose of 4 g per day (twice a day) for a period of 5-9 days.The clinical effect was excellent in 1, good in 3 and poor in 1 case.
Neither side effects nor abnormality of laboratory findings.were observed.

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We have conducted fundamental and clinical trials of a new penicillin derivative, pipaenradc oilbltiani (nPIPC) and obtained the following results.
1.We administered PIPC to 6 cases with abdominal simple hysterectomy due to myoma ute ri ata dose of 2 g by intravenous bolus injection and studied the average level of transfer measured at various locations in the uterine tissues and adnexa on an average of 36 minutes,(A group: n=4) or average 159 minutes (B groups: n=2) after administratio.
In the A group PIPC level was highest in the myometrium, 33.5μg/g (ratio with respect to the uterine arterial blood: 75.0%), followed by the cervix uteri, was lowest in the oviduct, 11.3μg/g (25.1%).
In the B group PIPC level was highest in the cervix uteri, 5.2μg/g followed by the portio vaginalis and ovary, and was lowest in the oviduct, endometrium and myometrium, 3.9μg/g.
In the PIPC concentration of each case, the values of the A group showed more than 8.25μg/g, and the values of the B group showed more than 2μg/g.
2. For the study of PIPC transfer to pelvic cavity fluid, we administered PIPC to 6 cases, with total hysterectomy due to cervical cancer of uterus etc.at a dose of 2 g by intravenous bolus injection.
The drug was transferred at very high levels to the pelvic cavity fluid.It showed 47.6μg/ml at 3 hours after total hysterectomy and it was 5 times as high as the venous blood level.It maintained a continuously higher level than the level of venous blood.
These concentrations in uterine tissues and pelvic cavity fluid were higher than the MIC of many strains of Gram positive and negative bacteria and anaerobes, so that we considered these to be therapeutically effective concentrations.
3. Seven cases of gynecological infections receiving in total 6 to 40 g of PIPC demonstrated “excellent” results in 1 case, “good” in 5 cases, and “no effect” in 1 case.Twelve strains of organisms were isolated from 4 cases and half of them proved to be anaerobes.
Neither side effects nor abnormalities of laboratory findings were observed in 7 cases during a clinical trial and in 12 cases during a fundamental test.
Based on the results of fundamental and clinical studies as described above, this drug was considered to have excellent efficacy and safety.

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[in Japanese]

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[in Japanese]

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The present study was performed to evaluate the clinical effectiveness and safety of cefmenoxime (CMX), a new cephalosporin antibiotic for injection in the field of pediatrics.Thirty-one cases, including 2 cases with sepsis, 18 cases with respiratory tract infections and 7 cases with urinary tract infections, were given CMX at daily doses of 30 mg/kg to 125 mg/kg divided into 3 or 4 for 3 days to 13 days.Clinical responses were excellent in 16 cases, good in 9 cases and poor in 6 cases, the satisfactory response being 80.6%.No side effects and no abnormal laboratory findings relating to the drug were observed.

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Cefmenoxime (CMX) is a newly developed cephalosporin. Basic and clinical studies on this drug was carried out and the results were as follows.
1.Serum level and urinary recovery
A 7 years old male was administered 10 mg per kilogram of CMX by one shot intravenous injection.Serum levels were 23.3 1Cg/ml at the time of 15 minutes after injection, 12.0μg/ml at 30 minutes, 3.9μg/ml at 1 hour, 2.0 μg/ml at 2 hours, and 0.3μg/ml at 4 hours.In this same patient, 6-hour urinary recovery was 54.7%.
2.Clinical evaluation and adverse reaction
Thirty-seven patients (upper respiratory infection 4, pneumonia 20, pyothorax 1, purulent lymphadenitis 1, cellulitis 2, sepsis 1 and urinary tract infection 8) were treated with CMX in doses of 30-212 mg/kg divided 3-4 times per day for 1.5-21 days intravenously.The ovarall efficacy rate was 94.6%.
As to adverse reaction, exanthema and drug fever were observed in 1 patient respectively.Abnormal laboratory data noted were eosinophilia in 2.3%, and elevation of serum transaminase in 9.8%.

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[in Japanese]

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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 β-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 5.2mcg/ml 1 hour after intravenous injection of 1 g (23.8mg/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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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 40-200 mg/kg/day.The drug was administered for 3-15 days, the total dosage administered being 0.7-43.5 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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[in Japanese]

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Basic and clinical studies were made on cefmenoxime (CMX) in pediatric field, and the following results were obtained.
1.The antibacterial activity of CMX against clinically isolated and maintained strains was examined. CMX had stronger antibacterial activity than CEZ against Escherichia coli, Salmonella, Klebsiella pneumoniae, Proteus mirabilis, Serratia marcescens and Pseudomonas aeruginosa, but CEZ had stronger antibacterial activity against Staphylococcus aureus.
2.The blood concentrations of CMX, 0.5, 1, 2, 4 and 6 hours after a one-shot intravenous injection of 20mg/kg of CMX were 33.6, 15.1, 4.5, 2.5 and 0.6mcg/ml, respectively, with the half-life of 1.04 hours.
3.The blood concentrations of CMX, 0.5, 1, 2, 4 and 6 hours after a 1-hour intravenous drip infusion of 20 mg/kg of CMX were 32.0, 55.2, 8.4, 4.2 and 1.0 mcg/ml, respectively, with the half-lite of 0.96 hour.
4.A complete or partial clinical response to therapy with CMX was obtained in all 10 children with infectious diseases.
5.Bacteriological examination made on 3 patients showed that all bacteria had been eradicated, and that therapy was effective. The bacteria were E. coli in 2 patients and Proteus mirabilis in 1 patient.
6.The side effects produced were neutropenia, eosinophilia and skin eruption in 1 patient, and diarrhea in 1 patient.

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A newly synthesized cephalosporin antibiotic, cefmenoxime (CMX), was applied to pediatric patients, and the following results were obtained.
1.Absorption: The blood concentrations of CMX in a 4-year and 8-month-old child, weighing 16.5 kg, and an 8-year and 10-month-old child, weighing 26.5 kg, who both received 15 mg/kg of CMX by a 30-minutes intravenous drip infusion were 23.5, 8.75, 2.3, 0.35 and 0.1 μg/ml, on average, 0.5, 1.5, 2.5, 4.5 and 6.5 hours after administration, respectively, with the half-life of 0.75 hour.The blood concentrations of CMX in a 2-year and 10-month-old child weighing 15 kg, and an 8-year and 1-month-old child weighing 25 kg, who both received 20 mg/kg of CMX by a 30-minutes intravenous drip infusion were 51.7, 15.9, 5.25, 0.85 and 0.1 μg/ml, on the average, 0.5, 1.5, 2.5, 4.5 and 6.5 hours after administration, respectively, with the half-life of 0.7 hour.
2.Clinical results: CMX was administered to 3 patients with acute tonsillitis, 4 with acute bronchitis, 5 with bronchopneumonia, 1 with the S.S.S.syndrome, 1 with acute enteritis, 1 with measles and 1 with Mycoplasma pneumonia.The dose of 35-59 mg/kg/day was administered to 12 patients and that of 79-111 mg/kg/day to 4 patients, in 3-4 divided doses by intravenous drip infusion (30 minutesfor 10 patients, 60 minutes for 6 patients) for 1-8 days.The cases of measles and Mycoplasma pneumonia were judged to beyond indication.The efficacy determined on the other 14 cases was 92.9%, the drug being ineffective only in 1 case of tonsillitis.
Clinically, no side effects were produced.The blood urea nitrogen in 1 patient, which was 5 mg/dl before treatment, was elevated to 17 mg/dl after treatment, but it was soon lowered.

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The antimicrobial activity of cefmenoxime (CMX) against clinical isolatedorganlsms was measured; CMX was more active than cefbtiam and cefazolin against Escherichia coli and Haemophilus influenzae.
The serum concentrations of CMX following intravenous injection of 20 mg/kg were 25.6, 10.3, 3.0μg/ml at 30, 60,120 minutes after injection, respectively. CMX was excreted 60.9% in urine within 6 hours after injection.
CMX was administered clinically to 22 pediatric patients with various infections (respiratory tract infection 16 including 1 pyothorax, urinary tract infection 4, tonsillitisw ith sinusitis2) at the dose of 39-96mg/kg/day for4-9 days, and the following satisfactory results were obtained; excellent in 11, good in 9, and poor in 2. The rate of satisfactory clinical response was 90.9%.
Eosinophilia 2 cases, slight elevation of transaminase 3 cases, slight elevation of BUN 1 case and transient diarrhea 1 case were observed. But no other serious side effects were observed.

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Basic and clinical studies in pediatric field were made on a novel cephalosporin antibiotic, cefmenoxime (CMX).
1.The minimum inhibitory concentrations of CMX, CTM and CEZ against the following clinically isolated strains were compared: 33 strains of S.aureus, 39 0f E.coli, 23 of K.pneumoniae, 15 of P. mirabilis, 3 of P.vulgaris, 2 of P.morganii, 1 of S.marcescens and 39 of P.aeruginosa.CMX had strong antibacterial activity against E.coli, K.pneumoniae, P.mirabilis, P.vulgaris, P.morganii and S.marcescens, its activity being much stronger than that of CTM, and very much stronger than that of CEZ. In particular, CMX had strong antibacterial activity against P.vulgaris and P.morganii for which CEZ was ineffective and against S.marcescens for which both CTM and CEZ were in effective.The antibacterial activity of CMX against P.aeruginosa was not very strong, but CTM and CEZ had no antibacterial activity against this bacteria.This drug was slightly less active against S.aureus than that of CTM or CEZ.
2.The serum concentrations of CMX in 3 children aged 5-11years, who received20.0-23.5mg/kg in one-shot intravenously, were on the average50.7, 16.8, 6.8, 2.7and0.2μg/ml and trace, respect1-vely, 0.25, 0.5, 1, 2, 4and 6 hours after administration, with the half-1ife of 0.58 hour on the average. The urinary CMX concentrations on the average0-2, 2-4 and 4-6 hours after administration were 2,767,236 and 12.6μg/ml, respectively, the urinary recovery rate up to 6 hours being 78.7% on the average.
3.The clinical efrect was examined on 26 patients: 15with acute bronchopneumonia and acute pneumonia, 2 with acute bronchitis, 3 with acute purulent tonsillitis, 2with acute purulent lymphadenitis and l each with staphylococcal scalded skin syndrome, acute pyelonephritis, acute cholangitis and asePtic meningitis.Clinically, all the patients except for 2 who were excluded, responded to therapy. The efficacy rate was 100% when complete and partial responses were included Bacteriologically, 1 strain each of S.mreus, S.pneumoniae and E.coli and 2 strains of S.pyogenes were eradicated.Seven of 8 strains of H.influenzae were eradicated and l was reduced in number.The overall eradication rate was 92.3%.Clinically, no side effects were seen.The only abnormality in laboratory findings was elevation of glutamic oxaloacetic transaminase and glutamic pyruvic transaminase values in 1 patient, which were later lowered to their normal levels.

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