Pharmacokinetic and clinical studies on cefodizime in the field of obstetrics and gynecology

Pharmacokinetic and clinical studies on cefodizime (THR-221, CDZM) were carried out and the following results were obtained. Concentrations of CDZM in serum and uterine tissues were determined from 38 to 282 minutes after drip infusion of 1 g CDZM. CDZM reached peak level of 25.0 micrograms/g or higher in each tissue during a period of 38 to 83 minutes. Concentrations of CDZM in the dead space exudate after drip infusion of 2 g CDZM were also studied. At 240 minutes after injection, CDZM concentration in exudate reached a peak of 46.88 micrograms/ml. These levels far exceeded MICs of CDZM against major pathogens most often isolated in the field of obstetrics and gynecology. CDZM was administered to 7 patients with their diseases diagnosed as pelvic peritonitis (4 cases) or acute adnexitis (3 cases) at a dose of 2-4 g per day for 6-14. days. Clinical response was good in all cases. Transient elevation of liver function was noticed in 2 cases. No other adverse reactions were noted during the study.     

Pharmacokinetic and clinical studies of cefodizime in the field of obstetrics and gynecology

Cefodizime (THR-221, CDZM), a new antibiotic, was studied pharmacokinetically and clinically. The results obtained are summarized as follows: 1. Concentrations of CDZM in internal genital tissues were quite high after an intravenous infusion. 2. Clinical effects of the therapy with CDZM using intravenous infusion twice daily were evaluated in 1 patient with endometritis, 2 patients with pyometra, 1 patient with extragenital abscess and 1 patient with BARTHOLIN'S gland abscess. Clinical responses were good in all 5 patients. No side effects nor abnormal laboratory test values due to the drug were noted.     

Pharmacokinetic and clinical studies on cefodizime in obstetrics and gynecology

Cefodizime (CDZM), a new cephem antibiotic, was studied in terms of its pharmacokinetics and clinical efficacy in the field of obstetrics and gynecology, and the results are summarized as follows: Concentrations of CDZM in serum and genital tissues following 1 g drip infusion (30 min.) were determined and good penetration of CDZM into tissues was recognized. The maximum level in uterine arterial serum was 56.25 micrograms/ml and maximum tissue levels ranged 23.56-40.64 micrograms/g which were above its MIC80's for main pathogenic organisms. Peak concentrations of CDZM in pelvic dead space exudates following 1 g intravenous bolus injection or drip infusion ranged 6.25-6.52 micrograms/ml. The clinical efficacy of CDZM in 17 cases of obstetrical and gynecological infections was investigated using a dose of 1-3 g daily. The clinical efficacy rate was 88.2% (15/17 cases). Bacteriologically, the eradication rate was 83.3%. No side effects or abnormal laboratory test values were observed.     

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 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 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.     

Clinical effects of cefodizime against infectious diseases in obstetrics and gynecology

Clinical studies on cefodizime (CDZM) were performed in patients of obstetrics and gynecology. CDZM was given to patients via drip infusion at a daily dose of 2-4 g, and the results obtained are summarized as follows: 1. A total of 10 cases included 5 cases of intrauterine infections (3 cases of puerperal endometritis, 1 endometritis and 1 puerperal fever), 2 intrapelvic infections (1 pelvic dead space infection and 1 parametritis), and 3 Bartholin's abscess. Clinical efficacies were excellent in 3 cases, good in 6 and poor in 1. The efficacy rate was 90% (9/10). 2. Bacteriological efficacies were as follows: eradicated in 3 cases, replaced in 2, decreased in 1, persisted in 1 and unknown in 3. 3. Neither subjective and objective adverse reactions nor abnormal changes in laboratory test values were observed.     

Clinical studies of flomoxef in the field of obstetrics and gynecology

Flomoxef (FMOX, 6315-S) is a new oxacephem antibiotics chemically related to latamoxef. Clinical studies on FMOX were carried out in the field of obstetrics and gynecology. A total of 9 patients comprising 4 cases of endometritis, 4 of Bartholin's abscess and 1 of vulvar abscess were treated with FMOX using intravenous injection at a dose of 1 g twice daily for 5-6 days. The clinical efficacy was good in all cases. Neither adverse reactions nor abnormal laboratory values were observed in any of the cases. From the results, it was concluded that FMOX was an useful antibiotic in the field of obstetrics and gynecology.     

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 studies of piperacillin in the field of obstetrics and gynecology

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 approximately 4 g for 3 approximately 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.     

Clinical studies on sulbactam/cefoperazone in the field of obstetrics and gynecology

Efficacy and safety of sulbactam/cefoperazone (SBT/CPZ) was studied on gynecological infections. The results obtained are as follows: In the treatment of 31 cases of gynecological infections, the clinical efficacy of SBT/CPZ was assessed as excellent in 9 cases and effective in 22 cases. As for the bacteriological effects of SBT/CPZ, clinically isolated organisms were completely (100%) eradicated. In comparison with MICs of CPZ, SBT/CPZ was found to show a combined effect on Gram-negative and Gram-positive organisms in the order mentioned, but this effect was not observed against anaerobes. The combined effect of SBT/CPZ on beta-lactamase producing bacteria was also investigated in the same manner. As a result, SBT/CPZ was found to exert a combined effect on beta-lactamase strains of S. aureus, S. epidermidis, E. coli, B. catarrhalis and B. fragilis. The laboratory tests performed before and after administration of SBT/CPZ revealed rise in GOT and GPT values in 1 case, GPT values in 2 cases and eosinophil in 1 case. However, these rises were all mild and required no particular measures.     

Clinical studies on sulbactam/cefoperazone in the field of obstetrics and gynecology

Sulbactam (SBT), a new beta-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 beta-lactamase producer but was persisted after treatment. Neither side effects nor abnormal laboratory findings was observed.     

Clinical studies of faropenem in the field of obstetrics and gynecology]

The clinical effect of faropenem was evaluated in 165 ambulatory patients with various infections in the field of obstetrics and gynecology at 10 institutions in Yamagata Prefecture. The results obtained are summarized below. 1. The rate of efficacy, as determined from the clinical effect following 3- to 7-day repeated administration at a dose of 600 mg/day, was 97.9% (46/47) for intrauterine infections, 92.0% (23/25) for adnexitis, 93.8% (15/16) for external genital infections, 88.9% (8/9) for mastitis, 94.0% (63/67) for cystitis, and 100% (1/1) for cervicitis. The overall efficacy rate was estimated to be 94.5% (156/165). 2. The rate of clinical efficacy, as classified by isolate, was high, 95.1% for Gram-positive bacteria, 100% for Gram-negative bacteria, and 100% for anaerobes. As for bacteriological response classified by isolate, the eradication rate was high, 91.4% (74/81) for Gram-positive bacteria, 98.4% (62/63) for Gram-negative bacteria, 89.5% (17/19) for anaerobes, and 93.9% (153/163) in all. 3. No adverse reactions or laboratory abnormalities were observed in any patient. The results presented suggest that faropenem is a highly safe and effective antibiotic for the treatment of obstetric or gynecological infections of various kinds in an ambulatory setting.     

Clinical studies on imipenem/cilastatin sodium in the field of obstetrics and gynecology

The penetration of imipenem/cilastatin sodium (MK-0787/MK-0791) into tissues of 6 patients and clinical efficacy in 21 patients with infectious diseases were studied in the field of obstetrics and gynecology. The results are summarized below. The transfer of MK-0787/MK-0791 into genital organ tissues was very good. The clinical efficacy was evaluated for 11 patients with intrauterine infections, 5 patients with intrapelvic infections and 5 patients with other infections. Clinical responses were excellent in 7 (33.3%), good in 13 (61.9%) and poor in 1 patient (4.8%), and the efficacy rate was 95.2 percent. Infective bacteria were eradicated in 4, diminished in 2, unchanged in 1 and replaced by other bacteria in 2 patients. No side effect was observed.     

Fundamental and clinical evaluation of cefodizime in obstetrics and gynecology

Cefodizime (CDZM, THR-221), a newly developed injectable cephem antibiotic agent, was evaluated for its distribution in intrapelvic genital organ tissues, penetration into exudate of retroperitoneal space and breast milk and therapeutical effects on some infections in obstetrics and gynecology. The results obtained are summarized as follows. 1. When 1 g of CDZM was administered by drip infusion over a 60 minutes period, its serum concentration reached 53.51 micrograms/ml at the completion of drip infusion, then declined rapidly. Peak concentrations of CDZM in intrapelvic genital organ tissues were higher than 20 micrograms/g at different times. CDZM was transferred to the exudate of retroperitoneal space and its concentration reached a peak of 7.01 micrograms/ml at 2.67 hours after initiation of 60 minutes drip infusion at a dose of 1 g, then declined slowly but stood at 4.93 micrograms/ml even at 8 hours. The transfer of CDZM to breast milk was similar to other cephem antibiotic agents and peak levels of CDZM in milk were 0.13-0.36 microgram/ml at 2 or 3 hours after administration of a dose of 1 g. 2. In the clinical study, CDZM was administered by drip infusion over 60 minutes to 6 patients with obstetrical and gynecological infections at a daily dose of 2-6 g. Clinical results were good in 5, poor in 1, and the efficacy rate was 83.3%. No side effects nor abnormal laboratory test results were observed.     

Clinical studies on imipenem/cilastatin sodium in the field of obstetrics and gynecology]

The efficacy and safety of imipenem/cilastatin sodium (IPM/CS) were studied in patients with obstetric and gynecologic infections and in those given the drug as prophylaxis against postoperative infections. The following results were obtained: 1. Efficacy rates were 96.0% (48/50) in patients with obstetric and gynecologic infections and 100% (28/28) in those with urinary tract or other infections. The overall efficacy rate was 97.4% (76/78). Bacteriologically, 30 organisms were isolated from 28 patients. The eradication rate was 95.2% (20/21) and the efficacy rate was 96.4% (27/28). 2. Changes in blood elastase before and after treatment were compared with those in CRP, WBC, and ESR in the patients with obstetric and gynecologic infections. The changes in elastase were similar to those in CRP. 3. The efficacy rate was 98.0% (48/49) in the patients given prophylaxis against postoperative obstetric and gynecologic infections. 4. An adverse reaction was observed in only one patient (diarrhea), and abnormal laboratory findings were noted in 2 patients (elevation of GOT and GPT). These results indicate that IPM/CS is very useful for the treatment of obstetric and gynecologic infections.