Pharmacokinetics and clinical studies on cefminox in the field of obstetrics and gynecology

Cefminox (CMNX, MT-141), a new cephamycin antibiotic, was studied in the field of obstetrics and gynecology, and the following results were obtained. The absorption and the penetration of CMNX into pelvic dead space exudate were good. The mean peak serum level after single intravenous injection was 190.8 micrograms/ml. The level in pelvic dead space exudate reached a peak of 36.6 micrograms/ml 4 hours after an intravenous injection of 1 g and 6.5 micrograms/ml after 12 hours, thus the level over MIC against main pathogenic organisms was maintained for a long time. CMNX was administered against gyneco-obstetrical infections such as intrauterine, intrapelvic, adnexal infections and postoperative wound infections with daily dose of 2 g and was effective in 11 cases out of 12 cases (91.7%), and 81.8% of bacteriological effect was obtained. No side effect was observed. From the above results the usefulness of CMNX in the field of obstetrics and gynecology was suggested.     

Basic and clinical studies on cefminox in the field of obstetrics and gynecology

Fundamental and clinical studies on cefminox (CMNX, MT-141), a new cephamycin antibiotic, were performed and the following results were obtained. Concentration of CMNX was examined in serum, internal genital organs and retroperitoneal fluid after a single intravenous administration of 1.0 g dose. The venous serum level of CMNX was 62.8 +/- 7.02 microgram/ml (Mean +/- S.D.) at 30 minutes after the administration. The sufficient transfer of CMNX to internal genital organs and retroperitoneal fluid was demonstrated. In clinical trial, CMNX was given to 10 cases with obstetrical and gynecological infections. 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 CMNX.     

Clinical studies on cefminox in the field of obstetrics and gynecology

Clinical and laboratory studies on cefminox (CMNX, MT-141), a new injectable cephamycin antibiotic, were made in the field of obstetrics and gynecology, and following results were obtained. In the clinical trial, 12 cases were treated with CMNX given by intravenous drip infusion. The results were excellent in 2 cases, good in 8 cases and poor in 2 cases. The effectiveness rate was 83.3%. No side effect was recognized. No significant changes of laboratory findings were noticed.     

Basic and clinical studies on cefminox in obstetrics and gynecology

Fundamental and clinical studies on cefminox (CMNX, MT-141), a new cephamycin antibiotic, were carried out and the results were as follows. After the intravenous one shot administration of 1 g CMNX to 17 cases, serum concentrations, tissue concentrations in pelvic organs and protein binding capacities in serum were measured. Blood concentrations ranged between 100-200 micrograms/immediately after the injection and declined gradually. Half-life (T1/2) was 75 minutes. Tissue concentrations were 30-70 micrograms/g (tissue weight) 10 minutes after injection and declined. Half-life was 90 minutes. The average serum protein binding rate was 66.3 +/- 8.4%. Correlation between tissue concentration (Y) and free serum concentration (X) was expressed as Y = 0.42 + 7.14X. Correlation coefficient (r) was 0.80 (r = 0.80). Correlation coefficient in serum concentrations between HPLC and bioassay was 0.83 and that in free concentration was 0.97. In clinical studies, CMNX was administered to 19 cases of obstetric and gynecological infections. The patients were constituted of 3 with puerperal endometritis, 3 with pyometra, 3 with pelvic peritonitis, 3 with parametritis, 3 with adnexitis, 2 with BARTHOLIN's abscess and 1 with retroperitoneal abscess and vulva abscess. Overall clinical efficacy was 89.5% (17/19). Bacteriologically 26 strains were isolated, 6 strains of E. coli, 4 strains of B. fragilis, 2 strains of P. anaerobius and P. asaccharolyticus and each one of E. faecalis, S. epidermidis, N. gonorrhoeae, S. marcescens, P. maltophilia, A. calcoaceticus, K. pneumoniae, P. mirabilis, H. influenzae, S. intermedius, E. lentum and F. varium. Twenty of these 24 strains were eliminated after the administration, K. pneumoniae was decreased, E. faecalis, S. marcescens and P. maltophilia remained unaffected. No side effects were observed but 1 case showed mild elevation of transaminases which normalized 1 week after CMNX was stopped.     

Fundamental and clinical studies on ceftazidime 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 .     

Fundamental and clinical studies on ceftriaxone in the field of obstetrics and gynecology

Fundamental and clinical studies on ceftriaxone (CTRX, Ro 13-9904) were performed in the field of obstetrics and gynecology and the following results were obtained. The serum concentration was maintained at a high level to remain 22 micrograms/ml about 24 hours after intravenous injection with 1 g CTRX. The level in each tissue except myometrium reached a peak of 50 micrograms/g or higher at 54 minutes after intravenous injection with 1 g CTRX. The peak level in the dead space exudate, obtained 4 to 6 hours after intravenous injection was 77 micrograms/ml with 1 g, and 125 micrograms/ml and 115 micrograms/ml with 2 g. The clinical efficacy was observed in all the cases (excellent in 1 and good in 3) consisting of 1 with Bartholin's abscess, 2 with adnexitis and 1 with pelvioperitonitis. Neither adverse reaction nor posttreatment laboratory test abnormality was observed in any case.     

Fundamental and clinical studies on piperacillin in the field of obstetrics and gynecology

Fundamental and clinical studies were made on piperacillin (PIPC) and the results were obtained as follows. Serum and uterine tissue concentrations of PIPC were obtained from 36 to 215 minutes after intravenous single shot of 2 g of PIPC. The cervix uteri, endometrium and corpus uteri showed the highest antibiotic levels of 38.0, 43.0 and 33.0 mcg/g, respectively, at 65 minutes after injection, and oviduct and ovary showed the highest level of 31.5 and 28.5 mcg/g at 36 minutes. Its concentrations were sufficiently effective against the major pathogens (Gram-negative bacilli and anaerobes) demonstrated in the field of obstetrics and gynecology. PIPC was administered 6 patients, including 3 of pelvic peritonitis (isolated organism was E. coli 1), 2 of acute endometritis (Klebsiella sp. 1, Peptococcus sp. + Bacteroides sp. 1) and 1 of acute adnexitis, in a dosage of 1 or 2 g twice or 3 times a day for a period of 5 to 8 days by intravenous administration or intravenous drip infusion. Clinical response was obtained excellent in 1 and good in 5. No adverse reaction as observed in any of the cases treated with PIPC, nor was there any marked changes in the laboratory findings.     

Fundamental and clinical studies on cefpiramide in the field of obstetrics and gynecology

Cefpiramide (SM-1652, CPM), a new cephem antibiotic was studied for the transfer into intrapelvic tissues and clinical efficacy in the field of obstetrics and gynecology. The results were obtained as follows. Clinical results of 17 patients with obstetrical and gynecological infection were excellent in 10 cases, good in 6, and poor in 1 with the efficacy rate of 94.1%. Following a single intravenous 30 minutes-drip infusion of 1 g dose of CPM, the peak of serum level and intrapelvic tissues were obtained at 30-60 minutes after completion of the administration. No adverse reaction or abnormal laboratory findings were observed.     

Fundamental and clinical studies on cefuzonam in the field of obstetrics and gynecology

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 on cefuzonam in the field of obstetrics and gynecology

Fundamental and clinical studies on cefuzonam (CZON, L-105), a new cephem antibiotic, were carried out. The results obtained are summarized as follows: 1. Upon drip infusion of 1 g CZON, a good transfer of the drug into female genital organ was observed. The transfer of CZON into exudates of the pelvic dead space was also good. 2. Clinical efficacy of CZON was good in 1 case we tested. No side effect was observed.     

Fundamental and clinical studies on cefpimizole in the field of obstetrics and gynecology

Fundamental and clinical studies on cefpimizole (AC-1370), a new cephalosporin derivative, in the field of obstetrics and gynecology have been investigated, and the following results were obtained. High concentrations of AC-1370 in internal genital organs were detected after intravenous administration of 1.0 g of AC-1370. In the treatment of 14 cases of infection, the therapeutic effects were excellent or good in 11 cases and overall efficiency rate excluding 1 case with side effects was 84.6% (11/13). No serious side effect was observed except 1 case of nausea and vomiting.     

Fundamental and clinical studies on aztreonam in the field of obstetrics and gynecology

Fundamental and clinical studies on aztreonam (AZT), a new synthetic monobactam antibiotic, were performed and following results were obtained. Concentration of AZT was examined in serum, internal genital tissues and retroperitoneal fluid after a single intravenous administration of 1 g dose. The venous serum level of AZT was 114.0 micrograms/ml at 10 minutes after the administration, then decreased to 7.0 micrograms/ml at 3 hours. Since concentration of AZT in examined tissues showed wide variation, it was irrelevant to calculate transfer ratio. Concentration in retroperitoneal fluid made the peak of 40.0 +/- 22.6 micrograms/ml at 1 hour after the administration, then slowly decreased to 13.4 +/- 3.2 micrograms/ml at 6 hours. Judging from above data, the transfer of AZT to retroperitoneal fluid was favorable. In clinical trial, AZT was given to 17 cases with obstetrical and gynecological infections such as endometritis, uterine adnexitis, pelvic peritonitis, parametritis and lymphocystitis. The efficacy was evaluated as excellent in 2 cases, good in 12 and poor in 3, and efficacy rate was 82.4%. No side effects were observed in any of the cases. In laboratory findings, transient elevation of liver function in 2 cases and eosinophilia in 1 case were noticed.     

Fundamental and clinical studies on fosfomycin sodium in the field of obstetrics and gynecology

Fosfomycin sodium (FOM-Na) was studied both fundamentally and clinically in the field of obstetrics and gynecology with following results. It showed good transference into the uterine tissues when given intravenously. The peak concentrations achieved in the uterine tissues following intravenous administration of 2 g of FOM-Na were 26.56 to 53.48 micrograms/g when given as one shot injection and 20.16 to 39.47 micrograms/g as drip infusion. In the serum of vein and uterine artery, peak concentrations of 163.6 to 143.40 micrograms/ml and 120 to 113.12 micrograms/ml were reached following one shot injection and drip infusion, respectively. In general, FOM-Na concentrations in the uterine tissues showed similar changes as those observed for serum concentrations. Clinically, FOM-Na was used in the treatment of 17 cases of obstetrical and gynecological infections at 2 g per dose twice daily as intravenous drip infusions. In all of these cases, good clinical efficacy was obtained. No side effects were observed.     

Fundamental and clinical studies of cefpiramide in the field of obstetrics and gynecology

Cefpiramide (CPM, SM-1652), a new cephem antibiotic, was fundamentally and clinically studied. The following results were obtained. Serum and internal genital tissue levels of CPM were measured following intravenous drip infusion of 1 g. High serum levels of 30 micrograms/ml and tissue levels of more than 4 micrograms/g were at least maintained for 8 hours. Favourable transfer of CPM into the pelvic dead space exudate was observed. The exudate level was 7.25 micrograms/ml on average even at 8 hours after intravenous drip infusion. A total of 6 cases comprising 4 with Bartholin's cyst, 1 with pelvic peritonitis and 1 with lymphocyst was treated with CPM at a dose of 0.5-2 g twice daily by intravenous injection or intravenous drip infusion. The clinical response was excellent in 1 case and good in 5 cases. Side effects and abnormal laboratory findings due to the drug were not noted.     

Fundamental and clinical studies of ceftriaxone in the field of obstetrics and gynecology

The study was done to evaluate the usefulness of ceftriaxone (Ro 13-9904, CTRX) injection for the treatment of infections in the field of obstetrics and gynecology. Fundamental and clinical studies were made and following results were obtained. When 1 g of CTRX is administered by intravenous single shot, the concentrations in various tissues of female genital organs were as follows: 40 micrograms/g in oviduct, 30 micrograms/g in ovary, 23 micrograms/g and 32 micrograms/g in corpus uteri and cervix uteri, respectively, at 2 hours 20 minutes after single shot. As for the transfer to the exudate in the pelvic dead space, the peak concentrations were 66-69 micrograms/ml after 4-5 hours. In the clinical studies, CTRX was given to 20 cases with female genital organ infections and others. As for the clinical effects, responses were excellent in 2 cases, good in 18 cases among 20 cases in total. The efficacy rate was 100%. As for the clinical effects on causative bacteria, the efficacy rates were 100% for single infections due to Gram-positive bacteria (6/6), due to Gram-negative bacteria (1/1), for mixed infection (3/3). Side effect was observed in 1 case with diarrhea. CTRX 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 CTRX will be a useful addition to the antibiotics for the therapy of these infections.     

Fundamental and clinical studies of ceftazidime in the field of obstetrics and gynecology

Ceftazidime ( CAZ ), a new cephalosporin antibiotic, was fundamentally and clinically studied. The following results were obtained. Serum and internal genital tissue levels of CAZ were measured following intravenous drip infusion of 1 g for 30 minutes. Serum levels of more than 10 micrograms/ml and tissue levels of more than about 7 micrograms/ml were maintained after 2 hours to 2 hours and 30 minutes, respectively. Favourable transfer of CAZ into the pelvic dead space exudate was observed. The exudate level attained its peak of 31.54 micrograms/ml on average at 2 hours and was 16.8 micrograms/ml on average even at 8 hours after intravenous drip infusion. A total of 6 cases comprising 1 of adnexitis, 2 of pyometra, 1 of endometritis and 2 of parametritis was treated with CAZ at a dose of 0.5 approximately 2.0 g twice daily by intravenous injection or intravenous drip infusion. The clinical response was excellent in 1 case, good in 4 cases and poor in 1 case. Abnormal laboratory findings and side effects due to the drug were not noted.     

Fundamental and clinical studies of aztreonam in the field of obstetrics and gynecology

Aztreonam (AZT, E-0734), a new beta-lactam antibiotic, was fundamentally and clinically studied. The following results were obtained. The serum and internal genital tissue levels for AZT after 1 g intravenous injection had been kept at more than about 20 micrograms/ml and 3.0 micrograms/g, respectively, during 1 hour. AZT was administered at 1-2 g of daily dose by intravenous injection or intravenous drip infusion to 5 patients with obstetric and gynecological infections, comprising 1 of pyometra, parametritis, Bartholin's abscess, puerperal endometritis and diffuse peritonitis. Clinical efficacy was; excellent in 1 puerperal endometritis case, good in 2 cases and poor in 2 cases. Neither side effect nor abnormal laboratory finding was observed.     

Basic study on cefminox in the field of obstetrics and gynecology

In patients with carcinoma of the uterine cervix, cefminox (CMNX, MT-141) was given intravenously after panhysterectomy and the pelvic dead space exudate and serum levels of the drug were determined at various periods. The pelvic dead space exudate level reached its peak of 67.21 +/- 39.81 micrograms/ml at 2 hours, which decreased gradually to 26.04 +/- 6.66 micrograms/ml at 6 hours. In the serum, the drug level attained the peak of 152.98 +/- 85.37 of 7.26 +/- 1.66 micrograms/ml was still detected. The pelvic dead space exudate level was much higher than its MIC or 3h-MBC at all periods studied. From these results it was considered that CMNX achieves levels high enough to be expected of clinical efficacy in the pelvic dead space exudate and serum.     

Fundamental and clinical studies on cefminox in the field of pediatrics

Cefminox (CMNX, MT-141) is a new injectable cephamycin antibiotic, which was studied for its antibacterial activity, absorption and excretion after administration and clinical efficacy of patients with infections. The following results were obtained. Antibacterial activity The antibacterial activity of CMNX against 19 clinical isolates consisting of 11 species made the results that its activity against E. coli, P. vulgaris and C. jejuni was superior to CMZ and CEZ. Concentration in serum and urine CMNX was given intravenously to 3 groups at 20 mg/kg by one shot (2 cases), 40 mg/kg by one shot (2 cases) and 40 mg/kg by 1 hour drip infusion (1 case). The half-lives were between 1.15 to 1.80 hours. We obtained over 70% of its excretion to urine within 6 hours after injection. Clinical efficacy Clinical evaluation was made on a total of 18 patients with various infections, 11 of whom had underlying diseases. The result was excellent in 1 case, good in 11 cases, fair in 2 cases and poor in 4 cases, and the effective rate was 66.7%. Side effect Clinical and laboratory abnormal findings related to CMNX were not found. It is concluded that CMNX seems to be effective and safetive antibiotic in the field of pediatrics.