cefuzonam and Bacterial-Infections

Topics: Bacteria; Bacterial Infections; Ceftizoxime; Cephalosporins; Humans; Microbial Sensitivity Tests; Tissue Distribution

Cefuzonam (CZON) was used to treat severe infections in 151 patients with hematopoietic disorders, and its efficacy and safety were assessed. The drug was given in doses of 2.0 to 6.0 g a day, divided into 2 or 3, intravenously by injection or infusion. The clinical effects were excellent in 34 cases, good in 40 cases, fair in 5 cases, and poor in 57 cases. Therefore, the results were excellent or good in 54.4% of the patients treated. The efficacy rates were 43.8 and 35.9% for groups of patients whose neutrophil counts were 500/microliters or less and 100/microliters or less, respectively. It was excellent or good in 70.6% of patients in whom causative agents were identified, and in 66.7 and 80.0% of patients infected with Gram-negative and -positive bacilli, respectively. The efficacy rate for patients infected with unidentified agents was 52.1%. The rate for patients who had received other antibiotics previously was 41.5%. The rate for patients having received only one antibiotic for the preceding treatment was 50.0%. Six (3.9%) of the treated patients experienced adverse effects including changes in laboratory test results observed in 4.

Topics: Adolescent; Adult; Aged; Bacteria; Bacterial Infections; Ceftizoxime; Child; Female; Hematologic Diseases; Humans; Male; Middle Aged; Neutrophils

A double blind study was conducted to objectively evaluate the usefulness of Cefuzonam (CZON) in the treatment of bacterial pneumonia and lung abscess. Cefotiam (CTM) was used as a control drug. Each drug was administered by intravenous drip infusion at 1 g at a time, twice daily, for 14 days as a rule. The results are as follows: 1. Enrolled in this study were 145 cases in total, comprising 72 of CZON group and 73 of CTM group. Of the total cases, 109 (53 of CZON group and 56 CTM group) were evaluated for clinical efficacy by the evaluation committee. Exclusion rate and background of patients were not significantly different between the two groups. 2. Clinical effectiveness assessed by the committee showed the efficacy rates of 84.9% (45 cases out of 53) for the CZON group and 83.3% (47 cases out of 56) for the CTM group, with no significant difference between the two groups. 3. The bacteriological eradication rates were 89.5% (17 strains out of 19) for the CZON group and 78.3% (18 strains out of 23) for the CTM group, with no significant difference between the two groups. 4. The incidence of side effects was 5 cases (7.5%) for the CZON group and 3 cases (4.2%) for the CTM group. The incidence rate of laboratory test abnormality was 28.4% (19 cases out of 67) for the CZON group and 31.3% (12 cases out of 67) for the CTM group. There was no significant difference between the two groups. 5. Usefulness rates calculated by the committee were 79.2% (42 cases out of 53) for the CZON group and 76.8% (43 cases out of 56) for the CTM group. There was no significant difference between the two groups. These results show that CZON is a useful drug in the treatment of bacterial pneumonia and lung abscess.

Topics: Adolescent; Adult; Aged; Bacterial Infections; Cefotiam; Ceftizoxime; Female; Humans; Lung Abscess; Male; Middle Aged; Pneumonia

Cefuzonam (CZON) which has a broad spectrum on both Gram-negative and Gram-positive bacteria including methicillin-resistant Staphylococcus aureus was evaluated in severe infections associated with hematological disorders. Sixty five patients were treated with CZON. Among them, 56 patients were evaluable for effectiveness. Nine patients were not evaluable because 3 patients were treated with combination of other antibiotics such as ceftizoxime, norfloxacin, ofloxacin, 1 patient was subjected to additional therapy of G-CSF and gamma-globulin, 4 were the patients with other disease than hematologic disorder (3 malignant mesotheliomas, 1 ovarian cancer), and the remaining one was prophylactically treated. Excellent responses were observed in 21 (37.5%) patients, good responses in 11 (19.6%) patients, with an overall efficacy rate of 57.1%. The efficacy rate in septic patients was 80% (4/5), and that in patient whose peripheral granulocytes were continuously below 100/microliters was 60% (3/5). Three patients who suffered from malignant mesothelioma, one patient who suffered from ovarian cancer, one patient who was treated prophylactically were included in the final evaluation of side effects. Side effects were observed in 2 patients (2/61, 3.3%). In a patient of 7 years, mild liver disfunction (GOT/GPT, 46/55) was found in 10 days after CZON treatment was started. In a patient of 65 years, mild appetite loss was identified in 2 days after CZON administration was begun. The liver disfunction was improved soon after the cessation of the treatment. The mild appetite loss disappeared while the treatment was continued. These results showed that CZON was an effective and safe antibiotic for the treatment of severe infections in patients with hematological disorders.

Topics: Adult; Aged; Aged, 80 and over; Anti-Bacterial Agents; Bacterial Infections; Ceftizoxime; Child; Female; Hematologic Diseases; Humans; Infusions, Intravenous; Leukemia; Male; Middle Aged

A multi-center open study was conducted to investigate cefuzonam (CZON, L-105) regarding to its pharmacokinetic, bacteriological and clinical aspects in the field of obstetrics and gynecology with the participation of 31 medical institutions and the related facilities. The results are summarized as follows. 1. Peak MICs of CZON for Staphylococcus aureus, coagulase (-) staphylococci, Escherichia coli, Klebsiella pneumoniae, Bacteroides fragilis group, Peptostreptococcus spp. isolated from obstetrical and gynecological infections with relatively high frequencies were 0.39, 0.20, 0.024, 0.024-0.05, 12.5, 0.20 microgram/ml, respectively, with an inoculum size of 10(6) CFU/ml. 2. When 1 g of CZON was given through bolus injection, the maximum concentration (Cmax) of CZON in pelvic dead space exudate was 18.7 micrograms/ml at 60.9 minutes (Tmax) after the injection; Cmax's in all female genital tissues were observed at 0.6-27.9 minutes and ranged from 11.9-26.3 micrograms/g. The Cmax 8.3 micrograms/ml, in the pelvic dead space exudate was noted at 97.0 minutes after the end of the intravenous drip infusion of 1 g over 1 hour, and Cmax's in genital tissues were 14.3-30.0 micrograms/g at the end of infusion. With 1 hour drip infusion of 2 g, Cmax's in genital tissues were 35.0-53.9 micrograms/g at the end of infusion. 3. The clinical efficacy of CZON was evaluated in 206 evaluable patients with obstetric and gynecologic infections. Efficacy rates classified by types of infections were 97.1% (67/69) for intrauterine infections, 81.6% (31/38) for intrapelvic infections, 91.8% (45/49) for adnexitis, 95.2% (20/21) for infections of the external genital organs and 86.2% (25/29) for other infections. 4. Side effects were observed in 7 of the 262 patients: eruption in 6 cases, itching in 2, diarrhea in 1. Abnormal laboratory test values were noted in 9 of the 256 patients. Most of them were slight elevation of hepatic function values. CZON showed satisfactory clinical efficacy and potent antibacterial activity, hence it appears that CZON will be a very useful antibiotic for obstetric and gynecologic infections.

Topics: Bacterial Infections; Ceftizoxime; Drug Evaluation; Drug Resistance, Microbial; Escherichia coli; Female; Humans; Klebsiella pneumoniae; Multicenter Studies as Topic; Pelvic Inflammatory Disease; Staphylococcus; Uterine Diseases; Uterus

Ten patients (3 cases of abscess of vaginal cuff, 1 case of abscess of vaginal cuff complicated with parametritis, 2 cases of pyosalpinx, 1 case each of abscess of abdominal wall, pelvic cellulitis, pyometra with cervical cancer and paraovarian abscess were treated with cefuzonam (CZON), which was administrated by intravenous drip infusion at a dose of 1,000 mg twice a day for 3 to 10 days (6 g to 19 g total). The clinical effectiveness reached 70.0% including 1 excellent case, 6 good cases and 3 poor cases. Bacteria were detected in all the 10 cases, and with CZON treatment, bacterial eradication were obtained in 3 cases, bacteria decreased in 3 cases, no change in 2 cases and bacterial replacement occurred in 2 cases. No abnormal laboratory findings and side effects were noted. From the above results, CZON seemed to be a highly effective and useful agent for gynecological infections.

Topics: Adult; Aged; Bacteria; Bacterial Infections; Ceftizoxime; Cephalosporins; Clinical Trials as Topic; Drug Evaluation; Female; Genital Diseases, Female; Humans; Infusions, Intravenous; Middle Aged

To evaluate the usefulness and the safety of cefuzonam (CZON, L-105) against obstetric and gynecological infections, we conducted clinical trials and obtained the results summarized as follows. 1. Thirteen patients with obstetric and gynecological infections (intrauterine infection 2 cases, adnexitis 7, 1 case each of abscess of adnexa uteri, abscess of the vaginal wall, pyelonephritis, and mammitis) were treated with CZON. The CZON was administered by intravenous injection or intravenous drip infusion, 1 g twice daily for 4 to 7 days (8 g to 14 g in total). The clinical effect was good in 12 and poor in 1. 2. Four cases, on which other antimicrobial agents were ineffective, responded well to CZON. 3. The CZON displayed excellent effects on anaerobic bacteria (Peptostreptococcus anaerobius, Bacteroides fragilis) and Gram negative rods (Escherichia coli, Klebsiella pneumoniae). 4. No side effects or laboratory abnormalities were observed. 5. From the above results, CZON appeared to be an effective and useful drug for obstetric and gynecological infections.

Topics: Adult; Bacteria; Bacterial Infections; Ceftizoxime; Cephalosporins; Female; Genital Diseases, Female; Humans; Middle Aged

We investigated the postoperative bile excretion and serum concentration of cefuzonam (CZON) in 6 cholecystectomized patients with postsurgical biliary drainage. CZON was administered intravenously by infusion at a dose of 1.0 g immediately following the operation. Serum and bile concentrations of CZON were determined on the day of the operation and the second day after the operation. The following results were obtained. 1. Serum concentrations of CZON were at their highest levels at 30 minutes after administration of CZON. Levels were 45.8 +/- 13.8 micrograms/ml on the day of the operation and 60.9 +/- 12.2 micrograms/ml on the second postsurgical day. 2. Bile concentration peaked 1 hour after administration (4,083 +/- 1,427 micrograms/ml on the day of the operation and 4,376 +/- 630 micrograms/ml on the second postsurgical day). In particular, bile concentrations of CZON at 6 hours (259 +/- 140 micrograms/ml and 154 +/- 23 micrograms/ml) exceeded MIC80 of CZON against Gram-negative bacteria except for Pseudomonas aeruginosa. 3. Serum and bile concentrations were higher on the second postsurgical day than on the day of the operation, but the differences between these 2 days were not significant. These results have indicated that CZON is a useful drug with excellent bile excretion following cholecystectomy, and that bile concentrations of CZON are maintained at high levels for 6 hours after intravenous administration.

Topics: Adult; Aged; Bacterial Infections; Bile; Ceftizoxime; Cholecystectomy; Cholecystitis; Cholelithiasis; Female; Humans; Injections, Intravenous; Male; Middle Aged; Postoperative Complications; Premedication

Ten patients with moderate or severe bacterial pneumonia with underlying diseases or complications were treated with cefuzonam (CZON) at a daily dose of 2 g to 4 g. The clinical effectiveness was good in 9 patients. No side effects or abnormal laboratory test results were observed in any patient. These results suggest that CZON may be useful in the treatment of bacterial pneumonia.

Topics: Aged; Aged, 80 and over; Bacterial Infections; Ceftizoxime; Drug Evaluation; Female; Humans; Male; Middle Aged; Pneumonia

Cefepime (BMY-28142), a new semisynthetic cephalosporin, was evaluated for in vitro and in vivo antibacterial activities in comparison with ceftazidime, cefuzonam, cefotaxime and cefmenoxime. Cefepime showed a well-balanced, broad spectrum of activity against a number of clinical isolates collected in Japan. The activity of cefepime against Gram-positive bacteria was several times greater than that of ceftazidime, nearly comparable to cefotaxime and cefmenoxime, and slightly weaker than cefuzonam. Against Enterobacteriaceae, cefepime showed superior activity to the reference cephalosporins against Proteus inconstans, Providencia rettgeri, Morganella morganii, Citrobacter freundii and Enterobacter cloacae. The activity of cefepime against Pseudomonas aeruginosa was nearly comparable to that of ceftazidime. Cefotaxime, cefuzonam and cefmenoxime were substantially less active against P. aeruginosa. Cefepime was more stable than cefuzonam, cefotaxime and cefmenoxime to various types of beta-lactamases from Gram-negative bacteria. The high in vitro activity of cefepime was reflected in its in vivo efficacy against experimental infections in normal and immuno-suppressed mice. Cefepime was the most effective among the cephalosporins tested against four Gram-negative bacterial infections.

Topics: Animals; Bacteria; Bacterial Infections; beta-Lactamases; Cefepime; Cefmenoxime; Cefotaxime; Ceftazidime; Ceftizoxime; Cephalosporins; Immunosuppression Therapy; Mice; Microbial Sensitivity Tests

Cefuzonam (CZON, L-105), an antibiotic injectable of cephalosporin family, was studied pharmacokinetically, clinically and bacteriologically to examine its distribution to female genital tissues and the activity on infections in the field of obstetrics and gynecology. Maximum concentrations in serum and genital tissues achieved 19-46 minutes after intravenous injection of CZON 1 g were 69.6 micrograms/ml for serum, 63.1 micrograms/g for oviduct, 34.2 micrograms/g for ovary, 22.5 micrograms/g for endometrium, 33.4 micrograms/g for myometrium, 30.7 micrograms/g for cervix uteri, and 37.1 micrograms/g for portio vaginalis. Clinical efficacies on 15 cases of intrauterine infection and adnexitis were proved with 4 cases of 'marked improvement' and 11 cases of 'improvement', thus the efficacy rate was 100%. Of 21 strains of aerobes and anaerobes isolated from infectious lesions, 19 strains were eliminated after administration of the drug. No side effects were observed. From these results of fundamental and clinical studies CZON appeared to be a highly useful drug fro the obstetric and gynecological infections.

Topics: Adnexa Uteri; Adult; Bacterial Infections; Ceftizoxime; Drug Evaluation; Drug Resistance, Microbial; Escherichia coli; Female; Humans; Infusions, Intravenous; Middle Aged; Pseudomonas; Staphylococcus aureus; Uterine Diseases; Uterus

Cefuzonam (CZON, L-105) was used clinically for the treatment of obstetrical and gynecological infections at a dosage of 1 g once or twice daily by intravenous drip infusion. The results obtained are summarized as follows. 1. Clinical effects of CZON were analyzed in 10 patients, including 5 patients with intrapelvic infections, 3 with intrauterine infections, and 1 each with adnexitis and an external genital infection. Excellent responses were observed in 1 patient (11.1%), good responses in 7 (77.8%), poor responses in 1 (11.1%), and one remaining case was unevaluable. The efficacy ratio was 88.9%. 2. Upon the treatment, eradications of causative bacteria were observed in all 4 cases tested. Staphylococcus sp. (2 strains), Staphylococcus epidermidis (1 strain), Klebsiella oxytoca (1 strain) and Pseudomonas putida (1 strain) were all eradicated by the CZON treatment. 3. The safety of the drug was analyzed in the 10 patients and rash occurred in 1 patient as a side effect. 4. One patient showed eosinophilia after the CZON treatment. It appeared that CZON would be useful for the treatment of obstetrical and gynecological infections.

Topics: Adult; Aged; Bacterial Infections; Ceftizoxime; Drug Evaluation; Female; Humans; Infusions, Intravenous; Middle Aged; Pelvic Inflammatory Disease; Uterine Diseases

Cefuzonam (L-105, CZON), a new beta-lactam antibiotic, was studied for its transfer into intrapelvic tissues and for clinical efficacy in the treatment of obstetrical and gynecological infection. 1. Following an intravenous 1 hour drip infusion of 1 g, the transferred CZON into uterine tissues reached and was maintained at effective concentrations which were defined as levels exceeding MICs against clinical isolates frequently obtained from patients in the field of obstetrics and gynecology. The peak concentration of CZON in the pelvic dead space exudate was estimated to be 20 micrograms/ml at 0.5-1 hour after infusion. 2. Subjects studied were 5 patients with the following infections: pyometra (3 cases), puerperal intrauterine infection (1 case), vaginal cuff infection (1 case). Clinical efficacies were good in 4 cases and poor in 1 case. No notable side effects or abnormal laboratory test results were noted.

Topics: Adnexa Uteri; Adult; Aged; Bacterial Infections; Ceftizoxime; Drug Evaluation; Female; Humans; Infusions, Intravenous; Middle Aged; Uterine Diseases; Uterus

Pharmacokinetic and clinical studies on cefuzonam (CZON) were performed to evaluate its usefulness in the field of obstetrics and gynecology. A summary of the results is as follows: 1. Concentrations of CZON in female genital organ tissues showed a little variance among organs. Mean concentrations were 3.34-7.83 micrograms/g at 40 minutes, 0.523-1.08 micrograms/g at 2 hours 15 minutes and 0.286 micrograms/g (in the myometrium) at 3 hours 10 minutes after the end of drip infusion. 2. Mean concentrations of CZON in the pelvic dead space exudate were 31.0 micrograms/ml immediately after the end of drip infusion (1 hour after the start of infusion), and 37.2 micrograms/ml 1 hour after the end of infusion, then they gradually decreased to 25.6 micrograms/ml after 3 hours and 21.4 micrograms/ml after 5 hours. Mean serum concentrations of CZON in concurrently collected samples from the peripheral vein were 30.0 micrograms/ml immediately after the end of drip infusion, 14.4 micrograms/ml after 1 hour, 4.00 micrograms/ml after 3 hours and 1.84 micrograms/ml after 5 hours. The T 1/2 beta was 1.03 hours. 3. Clinical trial in 7 patients, with CZON administered at a dose level of 1 g at a time, twice daily, showed "excellent" and "good" efficacy in all the patients. No side effects were noted. From the results of the above studies, CZON seems to be highly useful for infections in the field of obstetrics and gynecology.

Topics: Adult; Bacterial Infections; Ceftizoxime; Cephalosporins; Female; Genital Diseases, Female; Genitalia, Female; Humans; Middle Aged; Pregnancy; Pregnancy Complications, Infectious

The distribution of the new cephem antibiotic, cefuzonam (CZON) into adnexa uteri and uterine tissues, and clinical efficacy on patients with obstetric and gynecologic infections were studied. The results obtained are summarized as follows. 1. Concentrations of CZON in arterial and venous blood, oviduct, ovary, endometrium, myometrium, cervix uteri and portio vaginalis tissues were measured. The results demonstrated good transfer of the drug into various internal genital organs. 2. In clinical studies, CZON was given to 5 cases with various infections such as pyometra, acute vulvitis, pelvic peritonitis, pyelonephritis and puerperal intrauterine infection. Clinical efficacies were evaluated as excellent in 2 cases, and good in 3 cases. The efficacy rate was 100%. No side effects were observed in any cases. In laboratory tests, transient elevations of GOT, GPT and gamma-GTP were observed in 1 case. Therefore, it is concluded that CZON is a useful drug for various types of infections in the field of obstetrics and gynecology.

Topics: Adult; Bacteria; Bacterial Infections; Ceftizoxime; Cephalosporins; Drug Evaluation; Female; Genital Diseases, Female; Genitalia, Female; Humans; Middle Aged; Tissue Distribution

Fundamental and clinical studies on cefuzonam (L-105, CZON), a newly semisynthesized cephem antibiotic, were carried out in the field of pediatrics and the following results were obtained. Antibacterial activities of CZON against clinically isolated strains of Staphylococcus aureus, S. epidermidis, Streptococcus pneumoniae, S. pyogenes, Escherichia coli, Klebsiella pneumoniae, Haemophilus parainfluenzae and H. influenzae were compared with those of cefmenoxime (CMX), latamoxef (LMOX), cefoperazone (CPZ), cefmetazole (CMZ), cefotiam (CTM) and cefazolin (CEZ). CZON was nearly as active as CEZ against S. aureus and S. epidermidis and superior to other antibiotics against other Gram-positive cocci. Against Gram-negative rods, CZON was as active as CMX and superior to other 5 antibiotics compared. Serum concentrations and urinary excretion rates after intravenous bolus injection of CZON at doses of 10 mg/kg, 20 mg/kg and 40 mg/kg for 5 minutes in 1, 5 and 4 cases, respectively, were determined. Mean serum concentrations of CZON at these dose levels were 11.0, 43.8 and 111.5 micrograms/ml at 15 minutes, 2.4, 10.3 and 30.3 micrograms/ml at 1 hour and 0.17, 0.72 and 1.28 micrograms/ml at 4 hours, with serum half-lives of 1.79, 0.88 and 1.19 hours, respectively. Mean cumulative urinary excretion rates within 6 hours after administration were 47.9, 56.3 and 40.3%, respectively. Thirty-four pediatric patients with various bacterial infections (tonsillitis 2, acute bronchitis 1, pneumonia 14, pyothorax 1, sepsis 1, suppurative lymphadenitis 1, UTI 13 and enteritis 1) were treated with CZON at a daily dose of 40-94 mg/kg t.i.d. or q.i.d.. The overall clinical efficacy rate was 94.1%. No adverse reactions were observed except 2 cases with mild diarrhea. Abnormal laboratory findings were also mild; slight elevation of GOT and GPT in 2, eosinophilia in 1 and thrombocytosis in 1. These results clearly indicate the usefulness of CZON in the treatment of bacterial infections in children.

Topics: Age Factors; Bacteria; Bacterial Infections; Ceftizoxime; Cephalosporins; Child; Child, Preschool; Drug Evaluation; Drug Resistance, Microbial; Female; Humans; Infant; Male

Analysis on serum concentrations of cefuzonam (CZON, L-105) in 7 children who received different doses of CZON revealed a dose-response relationship. The half-life of the drug in blood was 0.90 hour. CZON was administered to 17 pediatric patients with bacterial infections. The clinical efficacy rate was 88% (15/17), and the eradication rate of pathogens was 80% (4/5). Only one case of mild diarrhea (1/17) was observed as a side effect associated with CZON.

Topics: Adolescent; Age Factors; Bacterial Infections; Ceftizoxime; Cephalosporins; Child; Child, Preschool; Drug Evaluation; Female; Half-Life; Humans; Kinetics; Male

We have carried out laboratory and clinical studies of cefuzonam. The results were summarized as follows: The effectiveness of cefuzonam was estimated by a plate dilution method on 26 strains each of S. aureus, E. coli, K. pneumoniae, Salmonella spp. and P. aeruginosa and 27 strains of S. marcescens isolated from patients. The distribution of MIC's of cefuzonam against S. aureus was 0.39 approximately 1.56 micrograms/ml and the peak of the distribution was 0.39 microgram/ml. Strains of 96.2% of E. coli and Salmonella spp. were inhibited at cefuzonam concentrations less than 0.39 microgram/ml. Strains of 92.3% of K. pneumoniae were inhibited at drug concentrations less than 0.20 microgram/ml. The distribution of MIC's of cefuzonam against S. marcescens was less than or equal to 0.025 approximately 12.5 micrograms/ml and the peak of the distribution was 0.2 microgram/ml and 1.56 microgram/ml. MIC's against P. aeruginosa was 12.5 approximately greater than 100 micrograms/ml. Cefuzonam was given by 5-minute intravenous administration to 4 children and 1-hour drip infusion to 1 child at a single dose of 20 mg/kg. After the intravenous administration, mean serum levels of cefuzonam were 30.8 +/- 4.55 microgram/ml at 30 minutes, 13.8 +/- 1.83 micrograms/ml at 1 hour, 0.4 +/- 0.159 microgram/ml at 6 hours. The half-life was 1.12 +/- 0.198 hours. After the drip infusion, the serum levels of the drug were 38.7 micrograms/ml at 1 hour, 5.25 micrograms/ml at 2 hours and 0.087 microgram/ml at 7 hours. The half-life was 0.93 hour. The mean urinary excretion rate was 58.1% and 33.4% up to 6 hours after the intravenous administration and the drip infusion, respectively. Cefuzoname was effective in 4 out of 5 cases with bacterial infections. No side effect due to the drug was observed in any case.

Topics: Adolescent; Age Factors; Bacteria; Bacterial Infections; Ceftizoxime; Cephalosporins; Child; Child, Preschool; Drug Evaluation; Drug Resistance, Microbial; Female; Humans; Infant; Male

Cefuzonam (L-105, CZON), a new injectable cephalosporin, was used in 12 pediatric patients with infections. The following is a summary of the results: The 12 cases included 3 cases of tonsillitis (pathogen: Haemophilus parainfluenzae in 1 case, Haemophilus influenzae in 2 cases), 4 cases of pneumonia (Staphylococcus aureus in 1 case, pathogen unknown in 3 cases), 2 cases of nephropyelitis (Escherichia coli in 2 cases), 1 case of purulent lymphadenitis (pathogen unknown), 1 case of purulent thyroiditis (mixed infection of Streptococcus milleri, Haemophilus aphrophilus and anaerobes), and 1 case of vulvar abscess (E. coli). Dose levels of CZON were 42.9 approximately 93.3 mg/kg/day divided into 3 or 4 times and the drug was intravenously injected for 6 to 12 days. Clinical efficacies were excellent in 4 cases, good in 5 cases, and poor in 3 cases, with the efficacy rate of 75.0%. The 3 cases with poor efficacy consisted of 1 case each of pneumonia complicated with chronic granulomatosis, purulent thyroiditis associated with piriform recess fistula, and purulent lymphadenitis of armpit developed after surgical operation of congenital heart disease. In the first 2 cases satisfactory efficacy was not obtained by chemotherapy alone, and complete cure was seen after surgical operation. Side effects were not observed clinically. One case each of slight prolongation of prothrombin time and transient elevations of GOT and GPT values were noted but no severe abnormalities were found in laboratory tests.(ABSTRACT TRUNCATED AT 250 WORDS)

Topics: Age Factors; Bacterial Infections; Ceftizoxime; Cephalosporins; Child; Child, Preschool; Drug Evaluation; Female; Humans; Infant; Injections, Intravenous; Male

Clinical studies were performed on cefuzonam (L-105, CZON), a new cephem antibiotic, as follows. Cerebrospinal fluid (CSF) and serum concentrations. CSF and serum concentrations of CZON were measured in 1 case of septic arthritis without meningitis. One hour after 50 mg/kg intravenous bolus injection, the CSF and serum concentrations were 0.10 and 18.1 micrograms/ml, respectively, and CSF to serum concentration ratio was 0.55%. Clinical efficacy CZON was administered to 15 patients in doses ranging 54.5 approximately 212.4 mg/kg/day (94.1 mg/kg/day on average) t.i.d. or q.i.d. for 4 approximately 12 days (6.5 days on average). Of those patients, 9 were with pneumonia, one each was with bronchitis, with tonsillitis, with septic arthritis, with septicemia, with purulent meningitis and with urinary tract infection. The overall efficacy rate was 100%, i.e., efficacy was excellent in 12, good in 3. Bacteriological efficacy was excellent, i.e., 8 of 8 strains were eradicated. Side effects were observed in 2 cases, i.e., one case with loose stool and another with eruption. Laboratory abnormalities to the drug were not observed during the treatment. The above results suggested that CZON would be a useful antibiotic for treating pediatric bacterial infections.

Topics: Adolescent; Age Factors; Bacterial Infections; Ceftizoxime; Cephalosporins; Child; Child, Preschool; Drug Evaluation; Female; Humans; Infant; Male; Staphylococcus aureus

For the evaluation of efficacy of cefuzonam (CZON) on biliary infection, the drug was administered to 12 cases of hepatic, biliary, and pancreatic diseases with postoperative/post-percutaneous transhepatic biliary drainage (PTBD) infections. The results were summarized as follows: The bacterial eradication rate was 33.3% (9/27 strains). Nine strains of bacteria appeared during the administration of CZON. MIC's of CZON against 14 strains including 4 of K. oxytoca out of 53 strains tested were below 1.56 micrograms/ml, whereas MIC's against 39 strains including 22 Pseudomonas spp. were higher than 12.5 micrograms/ml. Leukocyte counts in bile decreased in 6 cases, increased in 2 cases, and not detected in 1 case, showing no correlation with changes in bacteriology or clinical symptoms. Improvements of clinical symptoms such as reduced pain and decreased fever were noted in all cases. No case of adverse reaction was observed. The results indicated that CZON would be an antibiotic with a high efficacy and safety on biliary infections.

Topics: Adult; Aged; Bacterial Infections; Bile; Biliary Tract Diseases; Ceftizoxime; Cephalosporins; Drug Evaluation; Female; Humans; Infusions, Intravenous; Male; Middle Aged

Cefuzonam (L-105, CZON) was studied in pediatric infections. A summary of the results it as follows: For recently isolated Staphylococcus aureus strains, Peak MICs of CZON were distributed between 0.39 and 0.78 micrograms/ml showing a greater susceptibility of S. aureus to CZON than to cefoperazone (CPZ), latamoxef (LMOX), and cefmenoxime (CMX). Peak MICs of CZON for Escherichia coli were 0.10-0.20 micrograms/ml, similar to those of CPZ, LMOX, and CMX. Ampicillin (ABPC)-resistant strains were also susceptible to CZON. MICs for Salmonella were similar to those for E. coli. Peak MICs of CZON for Vibrio parahaemolyticus were 0.20-0.39 micrograms/ml. The susceptibility of the bacteria to CZON was far greater than to ABPC, and was similar to CPZ, LMOX, and CMX. With 20 mg/kg drip infusion, serum concentrations reached their peaks at the end of administration with values of 20.6-68.7 micrograms/ml, which decreased to 0.43-1.70 micrograms/ml after 2 hours. Half-lives of CZON in serum were 0.68-1.2 hours. With 50 mg/kg drip infusion, serum concentrations reached their peaks at the end of administration with levels of 69.0-82.0 micrograms/ml, and at after 2 hours 1.85-3.45 micrograms/ml. Thus, an apparent dose response was observed. Half-lives of CZON in serum were 0.63-0.99 hours. Urinary recovery rates in 6 hours were 39.9-80.5%. A total of 44 cases of 10 different types of acute pediatric infections was treated by CZON intravenous drip infusion as the main therapeutic procedure. The efficacy rate was 93.2%, and the compound was effective on purulent infections, acute urinary tract infection, etc. with pathogens such as ABPC-resistant S. aureus, E. coli, and Enterococcus faecalis. Dosage levels per day were 50 to 80 mg/kg in most cases. In infections with S. aureus (8 strains), Streptococcus pneumoniae (3 strains), E. faecalis (1 strain), Haemophilus parahaemolyticus (1 strain), Haemophilus parainfluenzae (2 strains), Haemophilus influenzae (11 strains), Bordetella pertussis (1 strain), E. coli (3 strains), a total of 30 strains, bacterial elimination was noted with an exception of 1 strain of S. aureus. The compound was used for 4 to 15 days, but side effects observed clinically were only 1 case of diarrhea and 1 case of thrombocytosis.

Topics: Adolescent; Bacteria; Bacterial Infections; Ceftizoxime; Cephalosporins; Child; Child, Preschool; Drug Evaluation; Female; Humans; Infant; Male

A new parenteral cephalosporin antibiotic, cefuzonam (L-105, CZON), was evaluated for its safety, efficacy and pharmacokinetics in children. Twenty-two cases of bacterial infections including pneumonia, lung abscess, sepsis, urinary tract infection and soft tissue infections were treated with CZON. Clinical effective rate was 95%. Serum half-lives of CZON were 1.04-1.33 hours in children with normal renal and hepatic functions. Significant depressions of the normal fecal flora were observed and diarrhea or loose stool was encountered in 7 of the 22 treated cases (32%).

Topics: Adolescent; Adult; Bacteria; Bacterial Infections; Ceftizoxime; Cephalosporins; Child; Child, Preschool; Drug Evaluation; Drug Resistance, Microbial; Female; Humans; Infant; Kinetics; Male

Studies were carried out on the penetration of cefuzonam (L-105, CZON), a new synthetic cephalosporin antibiotic, into cerebrospinal fluid, and on the clinical efficacy against bacterial infections. The results are summarized as follows: Concentrations of CZON in cerebrospinal fluid at 1 hour after intravenous administration of 100 mg/kg in cases of furunculosis of the external canal, encephalitis and mumps meningitis were 0.56 micrograms/ml, 1.44 micrograms/ml and 0.33 micrograms/ml, respectively. Concentrations of CZON in cerebrospinal fluid at 1 hour after intravenous administration of 100 mg/kg in 3 cases of purulent meningitis were 2.80-6.40 micrograms/ml at the acute stage and 0.56-1.45 micrograms/ml even at the recovering stage. Sensitivities of clinically isolated strains to CZON were determined and expressed as MIC. MICs of CZON on Haemophilus influenzae, Escherichia coli, Proteus mirabilis and Klebsiella pneumoniae were similar to MIC's of cefmenoxime (CMX), and lower than those of cefoperazone (CPZ), cefmetazole (CMZ), cefatiam (CTM) and Cefazolin (CEZ). The MIC of CZON on Staphylococcus aureus was similar to those of CEZ, CMZ and CTM, and lower than those of CMX and CPZ. Clinical responses of CZON were good in 2 cases of purulent meningitis, good in 2 cases of pyothorax, excellent in 1 case of septicemia, excellent in 3 cases of urinary tract infections, excellent in 7 cases and good in 3 cases out of 10 cases of pneumonia. Clinical responses of other diseases were excellent in 4 cases of bronchitis, good in 1 case of furunculosis of the external canal, excellent in 1 case of tonsillitis. No side effects nor abnormal laboratory findings were observed except 2 cases of mild diarrhea out of 24 cases.

Topics: Bacterial Infections; Ceftizoxime; Cephalosporins; Child, Preschool; Drug Evaluation; Empyema; Female; Humans; Infant; Infant, Newborn; Male; Meningitis; Time Factors

Pharmacokinetic and clinical studies were conducted to evaluate cefuzonam (L-105, CZON), a new cephem type antibiotic, in the pediatric field. A total of 9 pediatric patients (2-14 years) was treated with intravenous injection of CZON: 4 cases with one shot of 20 mg/kg, 2 cases with one shot of 40 mg/kg and 3 cases with drip infusion over 1 hour of 40 mg/kg. CZON concentrations in serum and the excretion in urine were determined. Mean serum concentrations of CZON after one shot intravenous injection of 20 mg/kg were 49.0, 22.7, 9.03, 2.13, 0.37, and 0.09 micrograms/ml at 15, 30 minutes, 1, 2, 4 and 6 hours, respectively. With 40 mg/kg one shot intravenous injections, mean serum concentrations were 117.5, 68.0, 26.2, 8.80, 0.63 and 0.19 micrograms/ml at 15, 30 minutes, 1, 2, 4 and 6 hours, respectively. With 40 mg/kg intravenous drip infusions over 1 hour, mean concentrations were 57.1, 78.8, 12.9, 1.12 and 0.23 micrograms/ml at 30 minutes, 1, 2, 4 and 6 hours, respectively. Mean half-lives were 0.69 hour for 20 mg/kg one shot injections, 0.44 hour for 40 mg/kg one shot injections, and 0.58 hour for 40 mg/kg 1 hour drip infusions. Urinary recovery rates in 6 hour after administration were 70.8% (mean) for the 20 mg/kg one shot injection, 44.1% (1 case) for the 40 mg/kg one shot injection, and 60.0% (mean) for the 40 mg/kg 1 hour drip infusion. CZON was administered in 26 cases of pediatric infections, and the clinical efficacy, antibacterial activity, and side effects were evaluated. Of the 26 cases 2 were excluded for the reason of not having bacterial infection, and the remaining 24 cases were assessed. Included in the 24 cases were 16 cases of acute pneumonia, 2 cases of acute purulent lymphadenitis, and 1 case each of acute bronchitis, acute purulent otitis media, acute apical periodontitis, staphylococcal scalded skin syndrome (SSSS), acute pyelonephritis, and acute enteritis. Clinical efficacy evaluation showed 19 excellent cases and 5 good cases, with an efficacy rate of 100%. Bacteriologically, Staphylococcus aureus 1 strain, Streptococcus pneumoniae 1 strain, beta-Streptococcus 1 strain, Haemophilus influenzae 10 strains, Haemophilus parainfluenzae 1 strain, Proteus mirabilis 1 strain, and Campylobacter jejuni 1 strain were determined or assumed as pathogens, but all of them were eradicated.(ABSTRACT TRUNCATED AT 400 WORDS)

Topics: Acute Disease; Adolescent; Bacterial Infections; Ceftizoxime; Cephalosporins; Child; Child, Preschool; Drug Evaluation; Enteritis; Female; Humans; Lymphadenitis; Male; Pneumonia

Cefuzonam (L-105, CZON) was given intravenously to 20 pediatric patients with the following acute bacterial infections: 13 of bronchopneumonia and 1 each of tonsillitis, purulent cervical lymphadenitis and acute tonsillitis, laryngitis, bronchitis, pyothorax, purulent meningitis complicated with septic arthritis, and urinary tract infection. Good clinical responses were obtained in all of the 20 patients and bacterial eradication of all 16 strains. No side effect was observed except 3 cases of slight elevation of transaminase, and 1 case each of soft stool and eosinophilia. From the above clinical results, it appears that CZON is a useful antibiotic for the treatment of pediatric patients with various kinds of bacterial infections.

Topics: Acute Disease; Arthritis, Infectious; Bacterial Infections; Bronchitis; Ceftizoxime; Cephalosporins; Child; Child, Preschool; Drug Evaluation; Empyema; Female; Humans; Infant; Laryngitis; Male; Meningitis; Pneumonia; Tonsillitis; Urinary Tract Infections

A new cephem antibiotic, cefuzonam (L-105, CZON) was studied for its concentrations in serum and clinical efficacy in the field of pediatrics. To examine the concentration of CZON in serum, 20 mg/kg of CZON was administered by intravenous drip infusion to a male patient of 6 years and 7 months. The half-life of the drug in serum was 0.97 hour after administration. CZON was administered to 7 cases of pediatric infections, and clinical result were "excellent" in 4, "good" in 1, "poor" in 2: the efficacy rate was 71.4% or 5 cases out of 7. As an adverse reaction, eruption was observed in 1 patient.

Topics: Bacterial Infections; Ceftizoxime; Cephalosporins; Child; Child, Preschool; Drug Evaluation; Female; Humans; Infant; Male

Cefuzoname (CZON) one of the aminothiazolyloxyiminoacetamido cephalosporins, was studied for its antibacterial activity, absorption and excretion, concentration in the cerebrospinal fluid (CSF) and the penetration, and clinical efficacy. The following are a summary of the results: 1. Antibacterial activity; The antibacterial activity of CZON was studied on clinically isolated Staphylococcus aureus (cefazolin (CEZ)-susceptible and CEZ-tolerant strains), Escherichia coli, Klebsiella pneumoniae, Proteus mirabilis. Compared with CZON were cefmenoxime (CMX), latamoxef (LMOX), cefoperazone, cefmetazol (CMZ), cefotiam and CEZ, but for S. aureus cefamandole (CMD) was replaced for CPZ. Activities of CZON against S. aureus, both CEZ-susceptible and CEZ-tolerant strains, were superior to those of 6 control drugs. The distribution of MICs for the CEZ-susceptible strains was 0.10-12.5 micrograms/ml, and for the CEZ-tolerant strains 0.20-greater than 100 micrograms/ml. MIC peaks were 0.39 micrograms/ml and 0.78-1.56 micrograms/ml for CEZ-susceptible and CEZ-tolerant strains, respectively. Against both susceptible and tolerant strains, CZON showed superiority to CMZ and CMD, which are used prevalently and used for Methicillin-resistant S. aureus also. Distributions of MICs of CZON (and the peak of MICs) on E. coli, K. pneumoniae, and P. mirabilis were less than or equal to 0.025-1.56 (less than or equal to 0.025), less than or equal to 0.025-25 (less than or equal to 0.025-0.05), less than or equal to 0.025-25 (less than or equal to 0.025) micrograms/ml, respectively, showing CZON's similar antibacterial activity to those of cephalosporins, CMX and LMOX, which are 5th group. 2. Absorption and excretion: Eight patients, aged 10 months to 15 years, were administered with CZON 20 mg/kg, one shot intravenously. Serum concentrations somewhat varied from patient to patient, but the mean value was 48.7 micrograms/ml after 30 minutes of administration which decreased rapidly to 13.3 micrograms/ml after 1 hour, to 3.4 micrograms/ml after 2 hours, to 1.14 micrograms/ml after 4 hours, and to 0.15 microgram/ml after 6 hours. Half-lives were 0.67-1.47 hours, with the mean of 0.87 hour. Urinary recovery rates were 24.7-55.9%, with the mean of 45.1%, in 6 hours after administration. 3. CSF concentration and penetration rate: To 4 pediatric patients with purulent meningitis, CZON 25 mg/kg or 50 mg/kg was administered and the concentration in CSF was measured.(ABSTRACT TRUNCATED AT 400

Topics: Adolescent; Age Factors; Bacteria; Bacterial Infections; Ceftizoxime; Cephalosporins; Child; Child, Preschool; Drug Evaluation; Drug Resistance, Microbial; Female; Humans; Infant; Male

Newly developed cefuzoname (CZON) was tested in 21 children and serum and urinary concentration and urinary recovery rates were determined. To 9 cases, 3 groups of 3 cases each, CZON was given at 10, 20 or 40 mg/kg one shot intravenously, and to 12 cases, 3 groups of 5, 3, 4 cases each, 10, 20 or 40 mg/kg was drip-infused over 1 hour. To 1 case of purulent meningitis 55.6 mg/kg was given one shot intravenously and concentrations in cerebrospinal fluid (CSF) and serum were measured. In 37 pediatric patients comprising 1 with tonsillitis, 24 with pneumonia, 1 with purulent meningitis and bacteremia, 7 with urinary tract infection, and 1 each with staphylococcal scalded skin syndrome, purulent lymphadenitis, periarthritis of jaw joint, maxillary sinusitis and orbital abscess, CZON was tried at 21.6 mg/kg (mean) per dose, 3 or 4 doses daily, one shot intravenously, for 7 days (mean). The clinical efficacy and antibacterial effectiveness were investigated. Also, the side effects were investigated and clinical laboratory tests done in the 37 pediatric cases plus 6 cases in which CZON was used but which were excluded from the efficacy analysis because they did not involve infections. The following is a summary of the results: 1. To 3 groups of 3 children each, 10, 20 or 40 mg/kg of CZON was given one shot intravenously. In each case the maximum serum concentration was observed at 5 min. after injection, and mean values of 3 groups with 10, 20 and 40 mg/kg dosing were 57.1, 147.2 and 316.7 mcg/ml respectively, indicating a dose-dependent response among the 3 groups. Mean half-lives were 0.83, 1.10 and 0.79 hours for 10, 20 and 40 mg/kg groups, respectively. The 10 mg/kg and the 40 mg/kg groups showed similar half-lives but the half-life of the 20 mg/kg group was a little longer than those of the other 2. 2. CZON was drip-infused over 1 hour to a total of 12 children divided into 3 groups of 5, 3 and 4 children at dose levels of 10, 20 and 40 mg/kg, respectively.(ABSTRACT TRUNCATED AT 400 WORDS)

Topics: Adolescent; Age Factors; Bacterial Infections; Ceftizoxime; Cephalosporins; Child; Child, Preschool; Drug Evaluation; Female; Humans; Infant; Kinetics; Male

Cefuzoname (CZON) was administered to 50 pediatric patients with infections, and the efficacy was investigated in 49 patients. The efficacy rate was 83.7% and the drug was evaluated to be highly effective for diseases in the pediatric field. The activity of CZON was especially good against Staphylococcus aureus, and the efficacy rate for 13 clinical isolates was 69.2%, which was comparable to that of cefotiam or cefazolin. CZON appeared to be useable alone in Gram-positive infections. It might be very powerful in the control of infections in secondary immunodeficiency.

Topics: Adolescent; Age Factors; Bacterial Infections; Ceftizoxime; Cephalosporins; Child; Child, Preschool; Drug Evaluation; Drug Resistance, Microbial; Female; Humans; Infant; Male; Staphylococcus aureus

Cefuzoname (CZON, L-105) a newly developed cephalosporin, has broad spectrum on Gram-positive or -negative bacteria and may also be effective against Staphylococcus aureus against which third generation cephalosporins are largely ineffective. We studied the pharmacokinetics and clinical effects of CZON on infectious disease of children. The diseases we studied included 2 cases of bacterial meningitis and 1 case each of viral meningitis, enterocolitis, upper respiratory infection, pneumonia, and mycoplasmal pneumonia. CZON was administered by drip infusion. Dose levels were 20-53 mg/kg/30-60 minutes, 3 times a day. For 5 cases, was studied time course of concentrations of CZON in plasma. Median T 1/2 was 0.96 hour. Concentrations in cerebrospinal fluid (CSF) were studied in cases of pneumonia and bacterial meningitis. In the case of pneumonia the CSF concentration of CZON was 0.272 microgram/ml after 45 minutes, in the case of meningitis they were 0.155 microgram/ml after 5 hours. Both of these values were higher than MIC of 0.025 microgram/ml against Haemophilus influenzae which was isolated from a case of bacterial meningitis. This MIC was lower than that of cefotiam and cefazolin, as well as of cefmenoxime. Clinical effects were excellent on pneumonia, good on upper respiratory infection, fair on mycoplasmal pneumonia. CZON, however, was ineffective in the treatment of a case of bacterial meningitis from which a susceptible strain of H. influenzae was isolated.(ABSTRACT TRUNCATED AT 250 WORDS)

Topics: Age Factors; Bacteria; Bacterial Infections; Ceftizoxime; Cephalosporins; Child; Child, Preschool; Drug Resistance, Microbial; Female; Humans; Infant; Infant, Newborn; Male

Cefuzonam (CZON, L-105), a new semisynthetic cephem antibiotic, was studied in the field of obstetrics and gynecology, pharmacokinetically and clinically. Following is a summary of the results. 1. Concentrations of CZON in serum and genital organs following intravenous drip infusion of 1 g of the drug over 60 minutes were measured. Samples were taken during 40 to 190 minutes after the end of the infusion. Ratios of concentrations of the drug transferred into genital organs to the concentration in the cubital venous serum were 0.5 to 1.5 in many cases. Levels of the drug in the genital organs examined well exceeded MICs for common causative organisms in obstetric and gynecologic infections. 2. Therapeutic effects of 1 g or 2 g of CZON by drip infusion twice daily were evaluated in 8 patients. Overall clinical efficacy was 62.5% (5/8). No side effects or abnormal laboratory findings due to the drug were noted. The results suggest that CZON is a useful antibiotic for obstetric and gynecologic infections.

Topics: Adolescent; Adult; Aged; Bacterial Infections; Ceftizoxime; Cephalosporins; Female; Genital Diseases, Female; Genitalia, Female; Humans; Middle Aged

Cefuzonam (CZON), a new cephem antibiotic agent, was studied in terms of its pharmacokinetics and clinical efficacy in the field of obstetrics and gynecology, and the results were summarized as follows. 1. The absorption and the tissue penetration of CZON into intrapelvic genital organs were good. The peak serum level in uterine artery after an intravenous drip infusion of 1.0 g was 49.0 micrograms/ml, and the highest peak level of 23.0 micrograms/g in tissues was obtained. After drip infusion of 2.0 g, the peak serum level in uterine artery was 137 micrograms/ml and the highest peak tissue concentration was 54.6 micrograms/g. Tissue concentrations of the drug changed in a similar pattern to serum levels and a dose-dependent response was recognized. 2. The penetration of CZON into intrapelvic dead space exudate was good. The level reached a peak of 8.17 micrograms/ml 4 hours after and intravenous drip infusion of 1.0 g and diminished slowly. 3. The clinical efficacy of CZON at a daily dose of 2 g was evaluated in 21 cases of obstetrics and gynecologic infections. The efficacy rate was 85.7% (18/21 cases). Bacteriologically, the eradication rate obtained was 93.3%. No side effects or abnormal laboratory values were observed.

Topics: Adult; Aged; Bacteria; Bacterial Infections; Ceftizoxime; Cephalosporins; Exudates and Transudates; Female; Genital Diseases, Female; Genitalia, Female; Humans; Middle Aged; Pelvis

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.

Topics: Adult; Bacterial Infections; Ceftizoxime; Cephalosporins; Exudates and Transudates; Female; Genital Diseases, Female; Genitalia, Female; Humans; Middle Aged; Pelvis

Seventeen patients with gynecological infections (5 cases each of Bartholin's abscess and adnexitis, 4 cases of endometritis and 1 case each of bartholinitis, pyosalpinx and vulvar abscess) were treated with cefuzonam (CZON, L-105) administered by intravenous drip infusion, 1-2 g twice daily, for 4 to 12 days (6 g to 23 g in total). The clinical effectiveness reached 94.1%, including 1 excellent case, 15 cases good, and a poor case. Bacteria were detected in 9 cases, and with CZON treatment, bacterial eradications were obtained in 6 case, but, in 3 cases, bacterial replacements were observed. No abnormal laboratory findings were noted. From the above results, CZON seemed to be a highly effective and useful agent for gynecological infections.

Topics: Adult; Aged; Bacteria; Bacterial Infections; Ceftizoxime; Cephalosporins; Female; Genital Diseases, Female; Humans; Middle Aged

The distribution of cefuzonam (CZON, L-105) into the uterus and uterine adnexa was investigated and the usefulness and the safety of CZON in obstetric and gynecological infections were studied. The results are summarized as follows: 1. Following one shot intravenous injection of CZON 1 g, a good distribution of the drug into tissues of uterus and uterine adnexa was observed, with Cmax values of 15.7-33.9 micrograms/g, Tmax of 7.3-34.0 minutes and AUC values of 18.7-35.3 micrograms X hr/g. 2. In all of the 30 cases of obstetric and gynecological infections treated, CZON was evaluated effective. 3. Bacteriologically, 93.9% of total bacteria that had been isolated were eliminated by the administration of the drug. 4. Against all the strains of bacteria isolated before the treatment and replaced bacteria, MIC50, MIC80 and MIC90 of CZON were 0.20 micrograms/ml, 12.5 micrograms/ml and 25 micrograms/ml, respectively, showing low values. 5. Subjective and objective findings and clinical laboratory test values during and after the trial showed no side effects associated with CZON.

Topics: Adult; Bacteria; Bacterial Infections; Ceftizoxime; Cephalosporins; Female; Genital Diseases, Female; Humans; Microbial Sensitivity Tests; Middle Aged; Uterus

To study the transfer of cefuzonam (CZON, L-105) into female genital organs, concentrations of the compound in pelvic dead space exudate were measured in cases of radical hysterectomy due to cervical cancer and analyzed by the two-compartment model. When CZON 1 g was drip-infused intravenously, the concentration in the cubital vein blood was 46.95 micrograms/ml at 1 hour after the start of infusion. Concentrations in the pelvic dead space exudate reached the peak of 11.29 micrograms/ml at 2.44 hours after the start, were higher than 4 micrograms/ml after 8 hours and were higher than 1.7 micrograms/ml after 12 hours. The area under the concentration-time curve in the pelvic dead space exudate was 77.85 micrograms X hr/ml. From these results CZON was considered to be effective when administered at 1 g against infections of Staphylococcus aureus, Escherichia coli, Klebsiella pneumoniae, Proteus mirabilis, Proteus vulgaris, and haemophilus influenzae, but increased dose levels seemed necessary against infections of Staphylococcus epidermidis and Bacteroides fragilis. In 3 cases of obstetric and gynecological infections the efficacy of CZON was good in 2 cases and unknown in the other case.

Topics: Adult; Aged; Bacteria; Bacterial Infections; Ceftizoxime; Cephalosporins; Exudates and Transudates; Female; Genital Diseases, Female; Humans; Microbial Sensitivity Tests; Middle Aged; Pelvis

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.

Topics: Adult; Aged; Bacteria; Bacterial Infections; Ceftizoxime; Cephalosporins; Exudates and Transudates; Female; Genital Diseases, Female; Genitalia, Female; Humans; Microbial Sensitivity Tests; Middle Aged; Pelvis

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.

Topics: Adult; Aged; Bacterial Infections; Ceftizoxime; Cephalosporins; Female; Genital Diseases, Female; Humans; Middle Aged

Concentrations of cefuzonam (CZON) in peripheral venous serum, uterine arterial serum and intrapelvic female organs of 29 women undergone simple total hysterectomy were determined by bioassay, using the cylinder-plate diffusion method. With an intravenous injection of CZON 1 g, the concentration at time 0 (Cp0) of peripheral venous serum and uterine arterial serum were 148.1 micrograms/ml and 155.4 micrograms/ml, respectively. Biological half-lives (T 1/2) of CZON were 1.07 hours in peripheral venous serum and 1.02 hours in uterine arterial serum. Concentrations in peripheral arterial serum were higher than 1.0 micrograms/ml at 4 hours after injection and remained at higher levels than minimal inhibitory concentrations necessary for most Escherichia coli strain for at least 4 hours. Concentrations of CZON in female organs were kept as high as peripheral venous serum, and ratios of CZON concentrations in uterine tube and endometrium to that in peripheral venous serum were 0.74 +/- 0.34 and 0.44 +/- 0.25, respectively. Since CZON is characterized by potent antibacterial activity and broad spectrum, it should be effective for infectious diseases of the female uro-genital tract.

Topics: Adult; Bacterial Infections; Ceftizoxime; Cephalosporins; Female; Genital Diseases, Female; Genitalia, Female; Humans; Middle Aged; Uterus; Veins

Clinical studies of cefuzonam (CZON, L-105) were performed in patients of obstetrics and gynecology, and the results obtained are summarized below. 1. CZON was intravenously administered at a daily dose of 1-2 g to 11 cases including 3 cases with intrauterine infection (pyometra), 2 cases of intrapelvic infection (1 case of pelvic dead space infection and 1 case of pelvic peritonitis), 1 case of adnexitis, and others (2 cases of vaginal cuff infection, and 1 case each of vaginal abscess, Baltholin's abscess, and vulvar abscess). Clinical efficacy was excellent in 1 case and good in 10 cases. 2. CZON showed a good antibacterial effect in single and mixed infections. 3. Neither side effects nor abnormal values in clinical laboratory findings attributable to the drug were observed.

Topics: Adult; Aged; Bacteria; Bacterial Infections; Ceftizoxime; Cephalosporins; Female; Genital Diseases, Female; Humans; Middle Aged

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.

Topics: Adult; Aged; Bacterial Infections; Ceftizoxime; Cephalosporins; Female; Genital Diseases, Female; Humans

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.

Topics: Bacterial Infections; Ceftizoxime; Cephalosporins; Exudates and Transudates; Female; Genital Diseases, Female; Humans; Pelvis; Pregnancy; Puerperal Infection

Topics: Adult; Aged; Aged, 80 and over; Bacterial Infections; Cefotaxime; Cefotiam; Ceftizoxime; Cephalosporins; Female; Humans; Lung Diseases; Male; Middle Aged; Pneumonia; Suppuration