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Fundamental and clinical studies on gynecological use of cefotetan (CTT), a new cephamycin antibiotic, were performed with following results. Following the intravenous administration of 2.0 g of CTT, T 1/2 beta in serum was 3.1 hours and longer than the previous cephamycin antibiotics. The yields of CTT from serum to various uterine tissues and discharge from retroperitoneum were about 30 approximately 50%. In clinical use, 14 patients with gynecological infections were administrated CTT, and it showed excellent or good efficacy in all patients. No side effects were noted except 1 transient disturbance in liver function.

The study group was organized to evaluate the usefulness of cefmenoxime (CMX) injection, a new synthetic cephalosporin, for the treatment of infections in the field of obstetrics and gynecology. Fundamental and clinical studies were made by the society and the following results were obtained. 1. The peak distribution of CMX's MIC for E. coli, Klebsiella sp., Enterobacter sp., Bacteroides sp. and Peptococcus sp. isolated from obstetrical and gynecological infections with relatively high frequencies area 0.1, less than or equal to 0.05, 0.2, 3.13, 1.56 micrograms/ml, respectively, with an inoculation of 10(6) cells/ml. 2. When 1 g of CMX is administered by intravenous drip infusion for 1 hour, the maximum concentrations in various tissues of female genital organs were as follows: 14.2 and 13.2 micrograms/g in ovary and oviduct, respectively, at 1.20 hours after the start of administration, and 16.9 and 26.3 micrograms/g in corpus uteri and cervix uteri, respectively, after 1 hour. As for the transfer to the exudate in the pelvic dead cavity, the peak concentration was 15.6 micrograms/ml after 2.13 hours. 3. In the clinical studies, CMX was given to 258 cases with female genital organ infections and others. As for the clinical effects, with exclusion of 3 cases in which other antibiotics are concomitantly used, responses were excellent in 76 cases, good in 162 cases and poor in 17 cases, among 255 cases in total. The efficacy rate was 93.3%. The efficacy rates by diseases were 97.1% (68/70) for intrauterine infections, 88.8% (79/89) for intrapelvic infections, 98.4% (62/63) for adnexitis, and 100% (23/23) for infections of external genital organs. As for the clinical effects on causative bacteria, the efficacy rates were 100% (19/19) for single infections due to Gram-positive bacteria, 94.8% (55/58) for single infections due to Gram-negative bacteria, and 88.2% (15/17) for single infections due to anaerobic bacteria. And its efficacy rates were 89.6% (69/77) for mixed infection cases. Side effects were observed in 2 cases (0.8%); 1 case with eruption, and 1 case with diarrhea and vomiting. As for abnormal laboratory findings, lower white blood cell count was observed in 2 cases and elevation of the values regarding hepatic functions in 9 cases. All cases were returned to the normal after the completion of the administration. Cefmenoxime showed a satisfactory clinical efficacy and a potent bacteriological effect in treatment of the infections in the field of obstetrics and gynecology, and it has been concluded that cefmenoxime will be useful addition to the antibiotics for the therapy of these infections.

Fundamental and clinical studies on sulbactam/cefoperazone (SBT/CPZ), a newly developed combined beta-lactam antibiotics, were carried out and the following results were obtained. 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 micrograms/ml, 122.3 micrograms/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 approximately 321.7%, and the latter was about 27.2 approximately 93.2% respectively. 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.

Fundamental and clinical studies were performed on ceftazidime ( CAZ ), a new cephem antibiotic. Following a single intravenous administration of 1 g dose of CAZ , the transfer of CAZ to the internal genital organs was good. The transfer of CAZ to retroperitoneal fluid was excellent. In a clinical trial, CAZ was given to 6 patients with obstetrical and gynecological infections. The efficacy was evaluated as excellent in 3 cases and good in the other 3 cases. No adverse effects were observed in any of the patients treated with CAZ .

This study was to investigate the transfer of cefmenoxime (CMX) to the retroperitoneal fluid after extensive panhysterectomy. Twenty-two cases were examined and they were divided into 2 groups, 10 with 1.0 g and 12 with 2.0 g bolus intravenous administration of CMX. In 1.0 g group, CMX concentration in the retroperitoneal fluid was observed 42.0 +/- 9.59 micrograms/ml (Mean +/- S.D.) at 1 hour and thereafter decreased gradually, but it still remained 7.91 +/- 5.18 micrograms/ml at 6 hours after the administration. In 2.0 g group, its concentration was 33.4 +/- 34.5 micrograms/ml at 30 minutes and reached to the peak level of 45.1 +/- 24.6 micrograms/ml at 1 hour and then declined slowly, but it remained 13.3 +/- 8.28 micrograms/ml at 6 hours after the injection. The results demonstrated sufficient transfer of CMX to the retroperitoneal fluid.

Fundamental and clinical studies on imipenem/cilastatin sodium (MK-0787/MK-0791), a new carbapenem antibiotic, were performed and the following results were obtained. Concentrations of MK-0787 and MK-0791 in serum, internal genital organs and retroperitoneal fluid were determined after a 30 minutes drip infusion of 500 mg/500 mg dose. Venous serum levels of MK-0787 and MK-0791 were 47.3 to 67.5 micrograms/ml and 44.2 to 61.4 micrograms/ml, respectively, at the end of the administration. Sufficient transfer of MK-0787 and MK-0791 to internal genital organs and retroperitoneal fluid was demonstrated. In clinical trials, MK-0787/MK-0791 was given to 18 cases with obstetrical and gynecological infections, such as endometritis, puerperal fever, pelvic peritonitis, parametritis and lymphocystitis. The clinical efficacy was evaluated as excellent in 1 case, good in 14 and poor in 3. The efficacy rate was 83.3%. In a bacteriological study, 43 strains were isolated from 16 cases and the eradication rate was 61.1%. No side effects were observed in any of the cases. In laboratory findings, a transient elevation of GOT, GPT was noted in 1 case. From the above results, it was concluded that MK-0787/MK-0791 was useful drug for infections in the field of obstetrics and gynecology.

Fundamental and clinical studies were made on cefotaxime (HR-756, CTX), a new cephalosporin antibiotic, with the following results. 1. Cefotaxime was given to 22 patients. Efficacy was excellent in 3 cases, good in 17 cases and poor in 2 cases. No side effects were observed in any cases. 2. Following a single intravenous injection of 1.0 or 2.0 g, the transfer of CTX to the internal genital organs was found to be good. The transfer of CTX to exudate of the dead space of pelvis was also good. 3. The above data demonstrated that CTX is a safe and effective drug.

Fourteen patients suffering from female genital organ infections including mastitis and urinary tract infections were treated with cefoperazone (CPZ). CPZ was administered intravenously or by drip infusion at a dose of 2.0-4.0 g/day for 3-7 days. Clinical results obtained were as follows: Of 8 patients with genital organ infections, excellent responses were seen in 2 patients, good responses in 5 patients. Of 3 patients with mastitis, good responses were seen in all the patients. Of 3 patients with pyelonephritis, excellent and good responses were seen in all the patients. No adverse effects and abnormal laboratory findings were observed. From the above results, we concluded that CPZ was an effective and safe antibiotic against infections in the field of obstetrics and gynecology.

Clinical studies on cefodizime (THR-221, CDZM), a new injectable cephem antibiotic, were performed and the following results were obtained. Ten patients with obstetrical and gynecological infections such as intrauterine infections, pyometra, adnexitis, parametritis and lymphocystitis. The clinical results were evaluated as excellent in 1 case, good in 4 cases and poor in 5 cases. The efficacy rate was 50.0%. Bacteriologically, 10 organisms were isolated from 8 patients and the eradication rate was 44.4%. No side effects were observed in any of the cases treated with CDZM. In laboratory examinations, transient elevations of serum GOT, GPT and Al-P were noted in 1 case.

Fundamental and clinical studies on cefpimizole (AC-1370), a new cephem antibiotic, were performed and the following results were obtained: Concentration of AC-1370 was examined in serum, internal genital organs and retroperitoneal fluid after single intravenous administration of 2.0 g dose. The venous serum level of AC-1370 was 243 micrograms/ml at 30 minutes after the administration. The sufficient transfer of AC-1370 to internal genital organs and retroperitoneal fluid was recognized. In clinical trial, AC-1370 was given to 10 cases with obstetrical and gynecological infections. The efficacy was evaluated as good in 8 cases and poor in 2 cases. No side effects were observed in any of the cases treated with AC-1370.

Fosfomycin sodium was administered to 36 cases with obstetrical and gynecological infection. Efficacy was excellent in 6 cases, good in 27 cases and poor in 3 cases and so effective ratio obtained was 91.7% in all. No side effects were observed in all patients except transient increase of serum transaminase in 2 cases.

Fundamental and clinical studies on cefuzonam (CZON, L-105), a new oxime type cephalosporin, were performed and the results obtained are summarized below: 1. Concentrations of CZON were determined in serum, internal genital organs and retroperitoneal fluid after a single intravenous administration of 1 g dose. The peripheral serum level of CZON was 74.0 micrograms/ml at 15 minutes after the administration. A sufficient transfer of CZON into internal genital organs and retroperitoneal fluid was demonstrated. 2. In clinical trial, CZON was given to 11 cases with obstetrical and gynecological infections. Efficacies were evaluated as good in 9 cases and poor in 2 cases. No side effects were observed in any of the cases treated with CZON. In laboratory examinations, transient elevation of serum GOT, GPT and alkaline phosphatase was noted in 1 case.

Fundamental and clinical studies were performed on cefpiramide (CPM), a new cephem antibiotic, with following results. Following a single intravenous administration of 1.0 g dose of CPM, the average serum level of CPM was 129.5 micrograms/ml after 1 hour and the half-life in beta-phase was about 5.0 hours. The transfer of CPM to the internal genital organs was found to be good. the transfer of CPM to retroperitoneal fluid was moderate. In clinical trial, CPM was given to 9 patients with obstetrical and gynecological infection. Efficacy was excellent in 1 case and good in 6 cases (effectiveness rate: 77.8%). No side effects were observed. In laboratory findings, a mild elevation of S-GOT was noted in 1 case.

Fundamental and clinical studies on ceftriaxone (CTRX, Ro 13-9904), a new cephalosporin antibiotic, were carried out with the following results. Concentration of CTRX was examined in serum, internal genital organs and retroperitoneal fluid after single intravenous administration of 1.0 g dose. The venous serum level of CTRX was 156 micrograms/ml at 5 minutes after the administration. The favorable transfer of CTRX to internal genital organs and retroperitoneal fluid was demonstrated. In clinical trial, CTRX was given to 10 cases with obstetrical and gynecological infections such as endometritis, adnexitis, pelvic peritonitis and parametritis. The efficacy was evaluated as excellent in 1 case, good in 8 cases and poor in 1 case. No side effects were observed in any of the cases treated with CTRX.