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A comparative study of cefixime (CFIX), a new oral cephem antibiotic, was carried out at the Department of Urology, Nagoya University Hospital and its four affiliated hospitals to evaluate the clinical efficacy and safety of two dosage regimens of CFIX, given either in twice daily doses (BID group) or once daily dose (UID group), in the treatment of acute uncomplicated cystitis. Forty six female patients (BID group) were administered the daily dose of 200 mg in two divided doses for 3 days, 30 female patients (UID group) were administered 200 mg once daily for 3 days. The clinical efficacy was evaluated in 33 cases from the BID group and in 22 cases from the UID group, respectively, according to the criteria recommended by the Japan UTI Committee. In the BID group, the clinical efficacy was evaluated as excellent in 18 cases, moderate in 13 and poor in 2, with an overall clinical effectiveness rate of 94%. In the UID group, it was evaluated as excellent in 9 cases, moderate in 12 and poor in 1, with an overall clinical effectiveness rate of 96%. Safety was monitored in 71 patients, and only one case of stomatitis was seen in the UID group. This findings suggest that 200 mg once daily dosing regimen of cefixime is as effective as 100 mg twice daily dosing regimen in treatment of acute uncomplicated cystitis, and is well tolerated in terms of safety.

The penetration of Cefixime (CFIX) into the prostatic tissue and the serum was examined in 54 patients with benign prostatic hypertrophy treated with transurethral resection of the prostate. CFIX was administered orally in a dose of 200 mg 2 times daily for 3 days preoperatively. The blood samples were taken at the time of the tissue sampling. The patients were divided into 2 groups. In group 1 (16 patients), the tissue sampling was done about 17 hours after the final drug administration. The mean concentration of CFIX was 0.83 +/- 0.49 micrograms/g in the prostatic tissue and 0.84 +/- 0.63 micrograms/ml in the serum. In the prostatic tissue, CFIX was detected in only 4 patients, in the other 12 patients, CFIX was not detected. In group 2 (38 patients), tissue sampling was done 5.5 hours after the final drug administration. The mean concentration of CFIX was 1.08 +/- 0.47 micrograms/g in the prostatic tissue and 3.18 +/- 1.28 micrograms/ml in the serum.

One gram of ceftizoxime (CZX) was administrated before transurethral resection in 38 cases of benign prostatic hypertrophy. Then the serum and tissue concentration of CZX was measured, and compared with the sensitivity of CZX to the bacteria separated from the urine of inpatients. The concentration of CZX in prostatic tissue was higher than the MIC80 for E. coli for 16.7 hr, for Klebsiella for 18.7 hr, for Proteus for 14.7 hr and for Serratia for 8.86 hr. Therefore, CZX was considered to be an effective drug against bacterial prostatitis.

Cefmenoxime (2 g) and cefsulodin (1 g) were given twice daily for 5 days by concomitant intravenous drip infusion (mixed infusion) to 135 patients with complicated urinary tract infection (c-UTI) probably caused by Pseudomonas aeruginosa. The clinical efficacy was evaluated according to the criteria proposed by the UTI committee in Japan. Ninety one subjects met the criteria for c-UTI and were evaluable for drug efficacy. P. aeruginosa was detected in 44 cases (including mixed infection with other organisms). The overall efficacy rate was 73% of the 91 cases; 75% of the 44 cases with P. aeruginosa and 70% in the 47 cases without P. aeruginosa infection. As to bacteriological response, the eradication rate was 91% (105/116) for all cases. By organism, the eradication rate for P. aeruginosa, Serratia spp. and Citrobacter spp. were 82 (36/44), 100 (12/12) and 100% (10/10), respectively. The eradication rate for gram-negative rods was 93% (99/107). Twenty-three strains appeared after treatment, and the majority of them (13) were yeast-like organisms. There was only one strain of P. aeruginosa. As for side effects, eruption was found in 2 cases. Cefmenoxime and cefsulodin were administered concomitantly to patients with c-UTI which was suspected to be caused by P. aeruginosa. The high overall efficacy rate of about 70% on the average was obtained regardless of the causative organism and disease state. The eradication rate of as high as about 90% was obtained excluding Enterococcus faecalis. Neither severe side effects nor abnormal laboratory values were found. It appeared, therefore, that this dosage regimen was useful for the treatment of refractory complicated urinary tract infection.

Prostatic and vesical tissue levels of Ceftizoxime (CZX) were determined in 21 patients with prostatic hyperplasia after the intravenous administration of 1 g of CZX. Serum concentration on prostatic surgery continued to be 1.3 fold higher than that of healthy adults. Prostatic tissue levels attained a peak of 40.7 +/- 1.6 micrograms/g (mean +/- SE) at 30 minutes after administration and vesical tissue levels attained a peak of 72.4 +/- 24.8 micrograms/g at 30 minutes. The mean value was 21.0 +/- 6.4 micrograms/g in prostatic tissue after administration for 120 minutes with the tissue/serum ratio of 0.91. Prostatic tissue level in glandular dominant were slightly higher than those of myoglandular hyperplasia (P less than 0.1). Judging from its favorable transfer into the prostatic tissue and MIC against clinically isolated E. coli, Proteus sp. and Klebsiella, CZX seemed to be clinically useful in the treatment of prostatic infection.

Basic and clinical studies were made on Cefmenoxime (CMX), a new cephalosporin antibiotic, and the following results were obtained. The serum concentration of CMX was examined in four healthy adults after administration of 250 mg of CMX by intramuscular injection, intravenous injection and one-hour intravenous drip infusion (cross over). In the case of intramuscular injection, the peak value of 5.9 micrograms/ml was obtained 30 minutes after administration, and the half-life in serum was 1.41 hours. In the case of intravenous drip infusion, injection, a concentration value of 11.1 micrograms/ml on the average was obtained after 15 minutes of administration, and the half-life in serum was 1.26 hours. In the case of intravenous drip infusion, the concentration was 12.4 micrograms/ml upon completion of drip infusion, and CMX disappeared from serum at a half-life of 0.94 hour. The urinary recovery up to 6 hours was from 60 to 70% in each The efficacy rate of this preparation was 100% for 4 cases of acute simple cystitis. The efficacy rate of CMX was 70% for 10 cases of complicated urinary tract infection; the 3 cases in which CMX was not effective were patients with a residual catheter and Pseudomonas persisting or appearing as superinfection. It was noted that Serratia, which was resistant to the conventional cephalosporin antibiotics, became negative. No subjective side effects due to the administration of this preparation were observed. As for abnormal laboratory findings, a slight and transient rise in transaminases was observed in one case. On the basis of the above-mentioned results, it was concluded that CMX is an effective preparation for the treatment of urinary tract infections.

Clinical efficacy of combination therapy using Fortimicin (ASTM) and Cefotax (CTX) was studied in 63 patients with complicated urinary tract infections. The patients received 200 mg of ASTM i.m. and 1 g of CTX i.v. twice a day. The overall clinical efficacy of the treatment was evaluated by criteria proposed by the Japanese UTI Committee. The overall clinical efficacy rate was 68.3%. The rate was 67.3% in the patients with single bacterial infection and 72.7% in those with mixed infections. Subjective side effects were observed in one of the patients. Drug related aggravation in laboratory tests was observed in 8 items in 8 patients, but these were mild changes. We concluded that combination therapy with ASTM and CTX was useful for the treatment of complicated urinary tract infections.

Claforan (CTX) was administered for 5 days at a daily dose of 4 g in two divided doses by intravenous injection to 18 in-patients, all of whom were over 70 years old and had chronic complicated urinary tract infections. The overall clinical efficacy of CTX was excellent in 4 cases, moderate in 8 cases and poor in 6 cases, the overall effectiveness rate being 66.7%. Twenty seven out of 34 organisms isolated from chronic complicated urinary tract infections before administration of CTX were eradicated after treatment. Both clinical findings and laboratory findings revealed no side effects. It is suggested that CTX is useful and a safe drug for elderly patients.

Cefmenoxime (CMX), a new semisynthetic antibiotic, was administrated in 29 cases diagnosed as complicated urinary tract infection. All patients received drip injection of 2 g (twice a day) for 5 days. Clinical results were excellent in 1 patient (3.4%), good in 15 patients (51.8%) and poor in 13 patients (44.8%). Effectiveness rate was 55.2%. In bacteriological response, out of 35 strains 27 (77.1%) strains were eradicated and 8 (22.9%) strains persisted. As for side effects, except one case of transient diarrhea after administration, no noteworthy reactions were observed. Laboratory abnormalities attributed to CMX treatment consisted of 4 cases of elevated serum transaminase and 2 cases of elevated serum creatinine.

Cefmenoxime (CMX) was intravenously administered to 106 patients with complicated urinary tract infection at a daily dose of 2-4 g for 5 days. An excellent response in overall clinical efficacy was seen in 15 cases (18.3%), a moderate response in 46 cases (56.1%) and poor response in 21 cases (25.6%). Pyuria was cleared in 20 cases (24.4%), decreased in 22 cases (26.8%) and unchanged in 40 cases (48.8%). Bacteriuria was eliminated in 41 cases (50.0%), decreased in 17 cases (20.7%), relapsed in 7 cases (8.5%) and unchanged in 17 cases (20.7%). Bacteriologically, 74 (76.8%) of the 95 strains isolated were eradicated by CMX, and 22 (23.2%) persisted. Side effects were observed in 3 (abdominal pain, diarrhea and elevation of trans amylase) of the 106 cases. Judging from the above results, CMX is considered to be a useful drug in the treatment of complicated urinary tract infections.

Ceftizoxime (CZX) was given clinically to 80 patients with urogenital tract infections, in which 34 cases of complicated UTI satisfied the criteria of the UTI committee. CZX was administered for at least five days at a daily dose of 1 to 4 g in two divided doses by intravenous drip infusion. The overall clinical efficacy of CZX in 34 cases of complicated UTI was 59%, estimated by the criteria of the UTI committee. The overall clinical efficacy rate according to group of infection was: 64% for the 11 patients in the 1st group, 56% for the 9 patients in the 2nd group, 100% for the 5 patients in the 3rd group, 50% for the 4 patients in the 4th group and 20% for the 5 patients in the 5th group. No serious side effects were observed in the clinical or laboratory findings except for slight elevation in GOT & GPT values in two cases (2.5%), which returned to normal after CZX treatment. It is therefore suggested that CZX is a clinically useful and safe drug in the treatment of complicated UTI.

The concentrations of Cefmenoxime (CMX) were examined in the serum and prostatic tissue of 25 patients with benign prostatic hypertrophy and of 1 patient with prostatic carcinoma. The CMX levels were measured at scheduled intervals after 2 g CMX administration by one hour drip infusion prior to prostatectomy. Pharmacokinetic analysis was performed based on the two compartment open model theory. 1) Maximum serum level of CMX was 124 micrograms/ml at the end of drip infusion and the biological half-life was 1.07 hrs. 2) CMX concentration in prostatic tissue reached a maximum level of 35.7 cg/g at 1.16 hrs after the start of CMX administration. Ratio of prostatic tissue to serum level in the area under curve (AUC) was 33% and biological half-life was 1.07 hrs. These results suggested that the CMX concentration in the prostatic tissue was higher than the MIC80 against pathogenic bacteria, particularly E.coli and Klebsiella sp. for a relatively long time. For this reason CMX is one of the more preferred drugs for treatment of chronic prostatitis and post-operative infection of prostate.

The efficacy and safety of ceftriaxone (Ro 13-9904, CTRX) a new broad-spectrum semisynthetic cephalosporin with an outstanding long serum half-life, was evaluated in 22 patients with chronic complicated urinary tract infections. Although the overall clinical efficacy evaluated on day 5 and 10 were similar, the rate of excellent effectiveness was higher on day 10 than on day 5. Eighteen bacterial strains were cultured from freshly voided urine. Eighty percent of the bacteria were eradicated on day 5 and 86.2% were eradicated on day 10. Bacterial replacement had occurred in 3 cases on day 5 and in 6 cases on day 10.

Cefixime (CFIX, Cefspan), a new oral cephem, was used in the treatment of urinary tract infections, and was evaluated for its therapeutic effectiveness and safety at the Department of Urology, Osaka University Hospital and 16 affiliated hospitals. A total of 238 patients were administered daily doses of 200 or 400 mg. Clinical efficacy was assessed on 92 female patients with acute uncomplicated cystitis and 42 patients with complicated UTI according to the Criteria for Clinical Evaluation of Antimicrobial Agents in UTI (3rd ed.) recommended by the Japan UTI Committee, to which we added our own minimum modification. Clinical efficacy was evaluated as excellent in 57 of the acute uncomplicated cystitis cases, moderate in 33 and poor in 2, with an overall clinical effectiveness rate of 98%. Clinical efficacy was evaluated as excellent in 12 of the complicated UTI cases moderate in 12 and poor in 18, with an overall clinical effectiveness rate of 57%. In one case of uncomplicated pyelonephritis, CFIX showed an excellent efficacy. Of the total of 102 bacterial strains isolated from uncomplicated UTIs, 95 (93%) were eradicated by CFIX, while 36 (72%) eradicated in 50 strains isolated from complicated UTIs. Subjective adverse reactions were seen in 4 cases (1.7%) of the 236 patients, as generalized pruritus and upper gastrointestinal discomforts. Abnormal laboratory findings were recorded in 6 out of 141 cases. They were increases in serum GPT, GOT, alkaline phosphatases, total bilirubin, as well as increases in peripheral leukocytes. These adverse symptoms and abnormal laboratory findings disappeared after the termination of CFIX administration. CFIX might therefore be considered as a clinically useful oral antibiotic in the treatment of UTI.