Study on tissue transfer of ceftriaxone in the field of obstetrics and gynecology

Ceftriaxone (Ro 13-9904, CTRX) was studied about the tissue transfer in the gyneco-obstetric field and the following results were obtained. The transfer of CTRX into the uterine tissues and adnexa was favorable following an intravenous injection with 1 g. The mean serum level 1 hour after administration was 123.3 micrograms/ml while the tissue level ranged from 26 to 48 micrograms/g. The level in the pelvic dead space exudate reached a peak 3 to 6 hours after administration and got higher than the serum level at 5 to 6 hours.     

A fundamental and clinical study of ceftizoxime in the field of obstetrics and gynecology (author's transl)

A fundamental and clinical study of ceftizoxime (CZX), a new cephalosporin antibiotic, has brought about the following results. 1. The antibacterial activity of CZX against Bacteriodes fragilis and B. thetaiotaomicron was superior to that of CEZ, but inferior to that of CFX. CZX was the most active of the 3 drugs against B. distasonis, and was as active as CFX against B. vulgatus. The MICs of CZX against Peptococcus, Peptostreptococcus and anaerobic Streptococcus were 1.56 microgram/ml or lower. CEZ was more active than CZX against these anaerobic cocci. 2. The concentrations of CZX in female genital organs and retroperitoneal dead space exudate after drip infusion of 1 g were high enough to fulfill the MICs of many bacterial isolates. 3. CZX administered intravenously to 9 patients in daily doses of 1 approximately 8 g for 4 approximately 11 days was 100% effective. Pathogenic bacteria in 6 of the patients were eradicated in 4 and partially eradicated in 1. The other patient had no bacteriological examination after therapy. 4. No adverse reaction was observed. From above results it is concluded that CZX must be one of the most effective antibiotics for the treatment of gynecological infections.     

Fundamental study on tissue distribution of ceftriaxone in the field of obstetrics and gynecology

Fundamental study on tissue distribution of ceftriaxone (Ro 13-9904, CTRX), a new cephalosporin parenteral antibiotic, was studied and the following results were obtained. CTRX had been administered by intravenous drip infusion with 1 g to 9 cases who received simple total hysterectomy. The level of CTRX in the cubital venous serum and uterine arterial serum was determined as well as the tissue concentration in the oviduct, ovary, endometrium, myometrium, cervix uteri and portio vaginalis. The level in the oviduct and portio vaginalis was generally high, although it was observed only in a few cases. The variation of the level in the myometrium was large. CTRX is expected to be clinically useful considering the fact that its half-life time is 8.5 hours, which is longer than that of existing cephalosporin antibiotics.     

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.     

Clinical studies on cefpiramide in the field of obstetrics and gynecology

Cefpiramide (CPM) was evaluated for clinical effects in the treatment of obstetrical and gynecological infections. The following results were obtained. CPM was given to 11 cases. Clinical efficacy was good in 8 cases and poor in 3 cases. The poor cases were parametritis and pyometra from those Serratia sp., K. pneumoniae, P. magnus, E. faecalis and B. ovatus were isolated. Other 1 case was external genital abscess with no isolated bacteria. There was a slight transaminase elevation in 1 case but no other appreciable side effects or abnormal laboratory findings were observed.     

Clinical studies on cefuzonam in the field of obstetrics and gynecology

Cefuzonam (CZON, L-105), a cephem type antibiotic, was clinically studied in the field of obstetrics and gynecology. The results are summarized as follows: CZON 1-2 g was administered by injection twice daily to 11 cases of infections (4 of endometritis, 2 of pyometra, 3 of adnexitis and peritonitis, 1 of abdominal abscess, and 1 of puerperal fever). Clinical efficacy was excellent in 2 cases and good in 9 cases, with a very high overall efficacy rate of 100%. Slight elevations of GOT and GPT in 1 case were noted in clinical laboratory tests. No side effects attributable to the drug were noted. CZON is considered to be a useful drug for obstetric and gynecological infections.     

Clinical studies on cefoxitin in the field of obstetrics and gynecology

Clinical studies were done on cefoxitin (CFX), the first cephamycin antibiotic, in the field of obstetrics and gynecology and following results were obtained. CFX was administrated by intravenous drip infusion for average 6.9 days at a daily dose of 2--6 g to 58 patients; 15 with intrauterine infections, 5 with intrapelvic infections, 11 with adnexitis, 3 with mastitis, 5 with urinary tract infections, 2 with other infections and 17 for prophylaxis of postoperative infections. The clinical results were excellent in 8 cases, good in 39 cases, fair in 4 cases, poor in 6 cases and unknown in 1 case, with the efficacy of 82.5%. Total bacteriological effective rate was 88.9%. As to side effects, eruption was observed only in 1 case. From the results of the present study, the usefulness of CFX was demonstrated in the field of obstetrics and gynecology.     

Clinical studies on cefpimizole in the field of obstetrics and gynecology

Cefpimizole (AC-1370), a new cephem antibiotic, was studied clinically in the field of obstetrics and gynecology, and the following results were obtained. AC-1370 was administered to 7 patients with gyneco-obstetrical infections, and the therapeutic efficacy was 85.7% (6 cases of 7 cases). E. coli was isolated as causative pathogen in 4 cases out of 7 cases, and was eliminated in all cases after the AC-1370 treatment. S. faecalis was eliminated in 2 cases out of 3 cases, and B. fragilis was eliminated in all 3 cases. As abnormal laboratory findings, transient elevation of GOT, GPT and A1-P was observed in 1 case but became normal after cessation of AC-1370 administration. The therapeutic effect was poor for this case.     

Clinical studies on cefodizime 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.     

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.     

Clinical studies on ceftriaxone in the field of obstetrics and gynecology

Clinical studies were made on ceftriaxone (CTRX, Ro 13-9904), a new long-acting cephalosporin antibiotic, with the following results. Following a single intravenous injection of 1 g, the transfer of CTRX to the internal genital organs was found to be good. The transfer of CTRX to exudate of the dead space of pelvis was also good. Elbow vein and uterine artery blood serum levels revealed marked increase immediately after administration, then followed by gradual reduction at very slow rate. CTRX was given to 3 patients of female genital infections. Efficacy was excellent in 1 case and good in 2 cases. As to side effect, 2 cases of diarrhea and 1 case of leukopenia were observed.     

Clinical studies on cefuzonam in the field of obstetrics and gynecology

In gynecological infections, especially intrapelvic infections, it is sometimes difficult to identify causal microorganisms. In those cases, it becomes a hard task to select most effective antibiotics, hence the use of wide-spectrum antibiotics becomes necessary. We recently had opportunities to clinically use cefuzonam (CZON, L-105) which has a wide range of spectrum against various bacteria including Staphylococcus aureus, Escherichia coli, Gram-positive and Gram-negative anaerobes, etc. The following is a summary of the clinical results: 1. In 7 cases of gynecological infections CZON was evaluated "excellent" in 1 case and "good" in 6 cases, thus the efficacy rate was 100%. 2. Against intrauterine infection caused by S. aureus, "excellent" effect was observed. 3. No sign of side effects was noted in any of the cases. 4. In 1 case, slight elevations of S-GOT and S-GPT were recorded but the elevations were transient.     

Experience with cefuzonam in the field of obstetrics and gynecology

Cefuzonam (CZON, L-105) was studied clinically in the field of obstetrics and gynecology, and the results obtained are summarized below: 1. The concentration of the drug in blood decreased rapidly after drip infusion was completed, and the concentration diminished after 1 hour to one tenth of the level detected at 5-9 minutes, and to an almost undetectable level after 3 hours. The rapid decrease of blood concentrations appears to indicate that the excretion of CZON was much faster than other antibiotics. No conclusive data were obtained on changes of concentrations with time in tissues due to the small number of cases analyzed and scattering of the data obtained. 2. The concentration in the pelvic dead space exudate reached a peak of 18.5 micrograms/ml at 30 minutes after the end of infusion and decreased to 0.092 microgram/ml after 10 hours. 3. CZON was administered to 5 cases of obstetric and gynecological infections. The efficacy was good in 4 cases and poor in 1 case. No side effects or laboratory test abnormalities were observed.     

Evaluation of the clinical effect and tissue distribution of piperacillin in the field of obstetrics and gynecology

Piperacillin (PIPC) was administered to patients with obstetrical and gynecological infectious diseases and we studied its clinical effect and tissue distribution. 1. Clinical results. PIPC was administered to 26 patients at a dose of 2--4 g per day (twice a day) by dripping infusion over a period of 3--10 days (total 8--30 g). These included 16 cases with intrauterine infection, 1 with adnexitis, 4 with pelvic inflammatory disease and 5 with infections of the external genitalia. The clinical results were excellent in 11 cases, good in 13 cases and poor in 2 cases so that the overall efficacy rate was 92.3%. For bacteriological study 33 strains were isolated from 20 patients. These included Gram positive bacteria (6 strains), Gram negative bacteria (23 strains) and anaerobes (4 strains). After PIPC treatment 32 strains (including S. epidermidis 4 strains, E. coli 12 strains, K. pneumoniae 3 strains, E. aerogenes 2 strains, P. aeruginosa 2 strains and anaerobes 4 strains, etc.) disappeared except for 1 strain of K. pneumoniae which persisted. The disappearance rate was 97.0%. The only side effect observed was a slight case of malaise during the first administration day, however the relationship between the appearance of this symptom and the drug was unclear. No adverse reaction in laboratory findings was observed. 2. Tissue distribution. We determined the tissue concentration from 90 to 240 minutes after dripping infusion for 1 hour at a dose of 2 g. PIPC concentrations in these tissues including the endometrium, myometrium, cervix uteri, portio vaginalis, oviduct and ovary showed the highest level (18.0--11.7 micrograms/g) at 90 minutes after the beginning of administration. These values were 48.6--31.6% in respect to the uterine arterial blood level (37 micrograms/ml at 90 minutes after infusion).     

Fundamental study on levofloxacin in the field of obstetrics and gynecology]

We performed a fundamental study on levofloxacin (LVFX, DR-3355), a new synthetic antimicrobial agent, in the field of obstetrics and gynecology. Concentrations in serum and intrapelvic genital organs (various regions in the uterus, ovary and oviduct) were determined following single oral administration. The transport of LVFX into genital tissues was found to be good, with the tissue levels of 0.64-2.13 micrograms/g after oral administration of 100 mg and 0.77-4.86 micrograms/g after administration of 200 mg. These tissue levels of LVFX were higher than those in serum and exceeded the MIC90 values against most causative organisms isolated from the lesions of obstetric and gynecological infections. These data indicate that LVFX should be useful in the field of obstetrics and gynecology.     

Bacteriological study of cefminox in the field of obstetrics and gynecology

Cefminox (CMNX, MT-141), a new cephem antibiotic, was determined of its antibacterial activity against 304 clinical isolates with following results. CMNX was inferior to CEZ or CMZ in the activity against 78 isolates of Staphylococcus sp., but it was superior to these antibiotics in the activity against 104 isolates of E. coli. Against 53 isolates of Bacteroides sp., CMNX showed higher activity than CEZ or CMZ. In the activity against 69 isolates of Peptococcus sp. and Peptostreptococcus sp., CMNX was almost equal to CEZ.     

Clinical studies of ceftibuten in the field of obstetrics and gynecology

Clinical studies on ceftibuten (CETB, 7432-S) were carried out in the field of obstetrics and gynecology. A total of 6 patients comprising 1 case of endometritis, 3 of bartholin's abscess, 1 of adnexitis and 1 of vulvar abscess was given 200-300 mg of CETB divided into 2 or 3 equal oral doses daily for 5 days. The clinical efficacy rate was 83 percent. Neither adverse reactions nor abnormal laboratory values were observed in any of the cases. From the results, it was concluded that CETB was an useful antibiotic in the field of obstetrics and gynecology.     

Clinical evaluation of aztreonam in the field of obstetrics and gynecology

Aztreonam (AZT), a new monobactam antibiotic was evaluated on clinical efficacy and bacteriological response in gynecological and obstetrical infections, and the following results were obtained. AZT was given to 22 cases with obstetrical and gynecological infections at a dose of 1 g X 2 times daily and 86.4% of clinical efficacy, 45.5% of eradicated rate on diagnosis, 52.5% of bacteriological response on isolated organisms and 83.3% of bacteriological effect on cases isolated Gram-negative bacteria were assessed. Side effect incidence was very low.     

Clinical evaluation of piperacillin in the field of obstetrics and gynecology

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 approximately 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.     

Clinical evaluation of piperacillin in the field of obstetrics and gynecology

Piperacillin (PIPC) was administered to 4 cases with obstetrical and gynecological infections and the following results were obtained. 1. PIPC was administered by intravenous drip infusion with 4 g per day for 7--14 days. The clinical efficacy was excellent in 2 cases with postoperative parametritis and good in 2 other cases, 1 with infectious ovarian cystoma and 1 with intrauterine infection. In the latter 2 cases surgical treatment was combined. 2. In laboratory findings GOT and GPT were slightly elevated in 2 cases. The relation between the drug and the abnormality was unclear because these rises may be considered due to the anesthesia or the operation itself.