Ceftezole, a new derivative of cephalosporin, was applied clinically in 20 cases of bone and joint infections, and the results obtained were remarkably effective in 4 cases, effective in 6 cases, slightly effective in 6 casses and not effective in 4 cases.

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Antibacterial activity, concentration in blood and urinary excretion were studied with ceftezole (CTZ) and the results obtained were as follows;
1) Minimal inhibitory concentrations (MIC) values obtained with CTZ against clinically isolated E. coil were distributed mostly between 1.56 and 50 μg/ml, peaked at 6.25 μg/ml when inoculated with 10⁸ cells/ml, while the values were between 1.56 and 25 μg/ml, peaked at 1.56 μg/ml when inoculated with 10⁶ cells/ml.
2) Mean serum level of three healthy adults 1/2 hour after intravenous administration of 1 g of CTZ was 20 μg/ml.
3) Following the intravenous administration of 1 g of CTZ, the average urinary level was 1, 500 μg/ml in 0-2 hour specimen, and recovery rate was 40.6% in 0-24 hours specimen.
CTZ was administrated intravenously at a dose of 1 to 2 g daily to eighteen patients with complicated urinary tract infection, four with fever and fourteen without fever. Clinical response to the complicated urinary tract infection with fever was found to be excellent in one case, good in one, failed in one and undetermined in one. When the infection was without fever, the result was good in five cases, fair in two, failed in five and undetermined in two.
No hematological abnormalities were noted.

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Ceftezole (CTZ), a new cephalosporin antibiotic, was bacteriologically evaluated, comparing with cefazolin (CEZ) and cephaloridine (CER).
1) In sensitivity test for 55 strains of E. coli, 18 strains of Klebsiella, 13 strains of Pr. mirabilis, 7 strains of Pr. vulgaris, 7 strains of Ps. aeruginosa and 13 strains of Staph. epidermidis which were clinically isolated, they were more susceptible to CTZ then to CER. However there was no significant difference between CEZ.
2) CTZ was administered at the dosis of 0.5 to 2.0 g for 2 to 4 days to 31 patients, including 24 acute cystitis, 7 acute pyelonephritis. Clinical results were excellent in 24 (77.4%), good in 7 (22.6%). The good and excellent rate was 100%.
3) No allergic reaction was observed.

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Ceftezole was administered once daily to 13 patients with acute urinary tract infection or acute epididymitis at a dose of 1 g or 2 g by intravenous drip, and the effective ratio obtained was 84.6%. Any notable side effect was not observed.

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1) Ceftezole (CTZ) was administered once daily to 14 cases with acute simple urinary tract infection at a dose of 500 mg or 1, 000 mg by intramuscular injection for 2 days. In 7 cases with a dose of 500 mg, the result was excellent in 3 cases, effective in 2 and ineffective in 2. In 7 cases with 1, 000 mg, the result was excellent in 5 cases, effective in 1 and ineffective in 1. The recurrence for 2 weeks after the treatment was found in each one case of two groups.
2) CTZ was administered to 5 cases with chronic complicated urinary tract infection at a daily dose of 1.0-2.0 g by intramuscular injection for 5 days. The result was excellent in 1 case, effective in 2 and ineffective in 2.
3) Bacteriological effects in acute simple cases were found in 8 strains out of 11 in E. coli and 3 out of 3 in Staph. epidermidis. In chronic complicated cases, bacteriological effects were found in 1 out of 3 in E. coli, 0 out of 1 in Pseudomonas and 1 out of 3 in Enterobacter.
4) As side effects with CTZ, anorexia was noticed in only one case. No other abnormal symptoms and laboratory findings were noticed.

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Ceftezole (CTZ), a new cephalosporin derivative synthesized in Japan, has been evaluated experimentally and clinically on urinary tract infections.
1) Minimum inhibitory concentration of CTZ was determined on 231 strains isolated from urinary tract infections by plate dilution method. Compared with CEZ, both antibiotics have good antimicrobial activity.
2) In 19 cases of urinary tract infections, CTZ was administered intramuscularly at a daily dose of 1 g.
The therapeutic results were excellent in 7 patients, good in 5, poor in 7, with the effectiveness rate of 63 percent. No side effects were found in any of the patients except temporal elevation of serum transaminase in one case.

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A new cephalosporin antibiotic, ceftezole (CTZ) has been employed in our service to evaluate it clinically in urinary tract infections. In three rather simple infections, one acute prostatitis, one acute epididymitis and one acute pyelonephritis, CTZ was effective in an erradication of bacteria and an improvement of symptoms. However, in two complicated infections CTZ was not effective due mainly to selective growth of resistant organisms (Pr. vulgaris and Pseudomonas strains) and to complicated predisposing factors in urinary tract. In no case pathological laboratory data concerning hematology, renal function and liver damage did not reveal any side-effect throughout the cases. Moderate pain at injection site was the chief complaint of patients by intramuscular administration.

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Ceftezole (CTZ) was used for treatment of 32 cases with post-operative urinary infection.
1) Clinical response was excellent in 8, good in 15 and the over-all effectiveness was 71.9%, after administrating the daily dose of 2 g CTZ for 6 days.
2) Serum concentration following an intravenous administration of 1, 000 mg in 7 subjects with various renal function, reached the peak level of 31.9 μg/ml on average after 30 minutes. The average rate of urinary recovery in 6 subjects was 60.3% after 6 hours.
3) No significant changes in blood chemistry were noticed in the patients.

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1) Antibacterial activity of ceftezole (CTZ) against E. coil was almost the same as cefazolin one.
2) Blood level after an intramuscular injection of CTZ 500mg, attained to peak of 9.7μg/m1 in 30 minutes, and it was a grade of trace in 6 hours. Recovery ratio of CTZ in urine was 65.8% on an average within 6 hours, most of the drug having been excreted until 2 hours.
3) CTZ was injected intravenously by drip infusion to 16 cases of complicated pyelonephritis accompanied with a complication, and the results obtained were excellent in 3 cases and effective in 7 cases, effective ratio being 62.5%.
4) Any noteworthy side effect was not observed at all with CTZ.

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1) Minimal inhibitory concentration of ceftezole (CTZ) was determined on 73 strains isolated from urinary tract infections by the plate dilution method. Most strains of E. coli and Pr. mirabilis were inhibited at the concentration of 6.25 μg/ml. All strains of Pr. vulgaris and Pseudomonas were resistant to 100 pg/ml CTZ.
2) In one case with normal renal function, the blood level reached to the maximum (14.6 μg/ml) at 30 minutes after i.m. administration of CTZ 500 mg, decreased rapidly thereafter, and the urinary recovery rate was 74.4% within 6 hours after injection of CTZ 500 mg.
3) Seventeen cases with urinary tract infections were treated with CTZ 2.0 g per day, and excellent or good results were obtained in 10 cases.
4) Side effect (elavation of GOT and GPT) was observed in 1 of 17 cases throughout the treatment.

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Ceftezole (CTZ) was given at the daily dosage of 2 g for 7 days to 21 patients with lower urinary tract infections after the operation.
Clinical results were excellent in 8 (38.1%), good in 2 (9.5%), poor in 11 (52.4%). The effective rate was 47.6%.
In bacteriological results, there were eradication of the organisms in 9 (39.1%), decrease in 2 (8.7%), unchange in 7 (30.4%), colonization in 5 (21.8%) out of 23 strains. No effectiveness was found in the infection of Pseudomonas and Serratia.
No serious side effects were noted except a severe local pain by injection in 2 cases.

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1) Ceftezole (CTZ) was administered in 20 cases (in- and out-patients) of various urinary tract infections diagnosed by Department of Urology of Kyushu University.
2) CTZ was administered intramuscularly 1 g per day for 3 days to the patients of acute simple urinary tract infections, while it was administered intramuscularly 2 g per day for 5 to 7 days, or intramuscularly 1 g and by drip infusion 3 g per day (totalling 4 g per day) for 5 days to the patients of complicated urinary tract infections.
3) The result obtained was excellent in 9 cases, good in 5 cases and poor in 6 cases, the effective ratio being 70%. Among 8 cases of acute simple urinary tract infections, it was excellent in 7 cases and good in one case, the effective ratio being 100%, while 12 cases of complicated urinary tract infections, excellent in 2 cases, good in 4, cases and poor in 6 cases, the effective ratio being 50%.
4) As to the bacteriological result, there were eradication of the organisms in 12 (60%) out of 20 strains, and 9 in the above 12 strains were E. coli.
5) No side effects were observed except the pain at the site of intramuscular injection.

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Ceftezole (CTZ) was administered in 20 cases of urinary tract infections (inpatients of the Department of Urology, University of Kurume) to investigate the clinical effects of this drug, and the results were obtained as follows.
1) CTZ was administered in 20 cases of urinary tract infections due to Gram-negative bacilli, and the results. obtained were excellent in 5 cases, good in 6 cases and poor in 9 cases, effective ratio being 55%. Classified by kind of infections, the effective ratio was 100% in acute and simple urinary tract infection, while it was 40.0% in chronic one and 43.7% in complicated one.
2) Classified by kind of pathogens, the effective ratio was 72.7% in the infections due to E. coli, while it vas 25.0%, 33.3% and 50% respectively in those due to Strept. pneumoniae, Ps. aeruginosa and Pr. vulgaris.
3) As for the side effects of CTZ, the rise of BUN, GOT and GPT was observed in 1 case, though it recovered normal values on the 7th day of administration, without performing any special treatment.

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Fifteen patients suffering from complicated urinary tract infections were treated with ceftezole (CTZ).
CTZ was administrated intramuscularly at the dosage of 0.5 to 1.0 g or by drip infusion at the dosage of 1.0 to 2.0 g for 5 to 27 days.
Of 15 patients, good clinical response was seen in 10 patients.
The effective ratio was 66.6%.
As a side effect with the drug, injection pain was noticed in 2 cases, though it was transient.

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1) Bacteria isolated in the field of obstetrics and gynecology demonstrated that ceftezole (CTZ) sensitivity is distributed almost the same to cefazolin. Peak value of MIC was ≤0.39 zg/ml in Staphylococcus and 3.12 /1g/ml in E. coli.
2) Blood level after intramuscular injection of CTZ 500 mg, attained to peak in 30 minutes, and decreased gradually after 2 hours. About 60% of the dose was excreted in urine within 6 hours.
3) CTZ transfer to fetus was proved in umbilical cord blood and amniotic water.
4) CTZ was injected intramuscularly or intravenously for 4-8 days at a daily dose of 1-3 g to 22 cases of various infections, and the clinical effects of the drug were investigated. As a result, efficacy of the drug was recognized in 13 cases (effective ratio 72.2%) of intramuscular injection group and in all 4 cases of intravenous injection group. No notew orthy side effect was noted with CTZ.

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The clinical studies on ceftezole (CTZ), a new derivative of cefazolin, were made in the field of obsterics and gynecology. The results obtained were as follows.
1) The serum levels in 2 patients with normal renal function after intramuscular injection of CTZ were determined. The average peak level of CTZ after a single dose of 500 mg reached more than 201.1g/ml at 30 minutes. The urinary excretion rate in the other patients was about 72% within 6 hours.
2) CTZ was administered at a daily dose of 500 mg to 4 g to 21 patients (7 with urinary tract infections, 5 with wound infection after operation and 5 with the other various infections).
Clinical response was excellent in 3 cases, good in 13, undecided in 2 and poor in3, effectiveness rate being about 76%.
No noteworthy side effect was encountered except one case of elevation of GOT and GPT.

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A new antibiotic, ceftezole was administered intramuscularly or by drip intravenous infusion to 30 cases of infectious diseases in the field of obstetrics and gynecology. A daily dose of 0.5-2.0 g was injected for 3-16 days. The results were obtained as follows.
1. The results obtained were remarkably effective in 22 cases, effective in 5 cases and ineffective in 3 cases. A ratio of effectiveness was 90%.
2. The comparative examination of haematological, renal and hepatic function tests before and after injection days. The results were obtained as follows.
3. No side effects were observed except one case in which a slight and transitory rash was noticed.

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Ceftezole (CTZ) was given intramuscularly or by intravenous drip infusion in doses of 1-2 g once or twice daily to 20 patients with severe infections, and the clinical results obtained are as follows :
1) Clinical effect of CTZ in 12 patients with urinary tract infections associated with the underlying disease of uterine cervical carcinoma and vulvar cancer was excellent in 66.7%, good in 25.0%, and the total effective rate was 91.7%.
2) Clinical effect of CTZ in 8 patients with other infections in the field of obstetrics and gynecology was excellent in 50.0%, and good in 12.5% and the total effective rate was 62.5%.
3) The following 24 strains were isolated from the patients treated : 16 strains of E. coli, 2 of Pr. mirabilis, 1 of Pr. vulgaris, 1 of Klebsiella, 2 of Pseudomonas, 1. of Salmonella enteritidis, and 1 of anaerobic gram positive bacilli. Of these strains, 22 except one of Pseudomonas causing chronic pyelonephritis and 1 of E. coli causing pyometrium disappeared after the treatment.
4) No subjective side effects were observed except soft stool in 2 patients. No abnormal laboratory findings were noted.

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Ceftezole (CTZ) treatment has been performed in 24 cases of skin infections (furuncle, furunculosis, folliculitis, inflammatory atheroma with infection, purulent hidradenitis and others). Dose of 500 mg in adults or that of a half in children was administered intramuscularly once daily for 2-22 days, and the results obtained were excellent in 7 cases, good in 11 cases, fair in 4 cases and failure in 2 cases. One case of latent syphilis received CTZ for a long period of 40 days at a daily dose of 1-2 g, though this was out of objective diseases of the drug.
No side effect was noticed with CTZ in all cases.

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1) Ceftezole (CTZ) sensitivity to Staph. aureus was rather better than cefazolin one.
2) Blood level after an intramuscular injection of CTZ 500 mg, attained to peak in 30 minutes, then. decreased rapidly, and yet an effective blood level was noticed in 5 hours taking MIC into account.
3) CTZ was administered intramuscularly consecutively at a dose of 500 mg once daily to 23 cases of profund pyodermia, and an effective ratio was 73.0% when calculated regarding slightly effective as ineffective.
4) No side effect was observed with CTZ

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1) MIC of ceftezole (CTZ) against strains of Staph. aureus isolated from skin infection were 0.2 in 3 strains, 0.4 in 17 strains, 0.8 in 11 strains, 1.6 in 1 strain.
2) Serum and skin levels after intramuscular injection of 20 gm/kg in rats were studied. Serum levels were 61.0 μg/ml at 30 minutes, 23.0 μg/ml at 1 hour, 7.1 μg/ml at 2 hours and trace at 4 hours. Skin levels were 9.6 Ag/g at 30 minutes, 5.3 μg/g at 1 hours, 4.8 μg/g at 2 hours and trace at 4 hours.
3) Two cases of furuncle were treated with two daily intramuscular injections of 500 mg of CTZ. The result was excellent in a case and good in another case. No subjective side effect was complained.

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Laboratory and clinical studies on a new antibiotic, ceftezole (CTZ), were made with the results as follows :
1) Minimum inhibitory concentration against coagulase positive Staphylococci (20 strains) isolated from ocular suppurative lesions in 1974, was in a range of 0.39-0.78 μg/ml.
2) Penetration of the drug into rabbit aqueous humor was measured simultaneously with the measurement of serum concentration. Aqueous humor concentration of CTZ reached maximum (2.6 μg/ml) 1 hour after an intramuscular administration of 50 mg/kg, and the maximum serum concentration (13.5 μg/ml) was obtained 1 hour after the injection.
3) Aqueous humor concentration of CTZ reached maximum (19.5 μg/ml) 1 hour after a subconjunctival injection (2.5% solution, 0.2 ml).
4) Seven patients of ocular suppurative disease were successfully treated by a daily dose of 1, 000 mg CTZ.

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The basic and clinical experiments for ophthalmic use of ceftezole (CTZ) were performed. The results were summarized as follows.
1) CTZ has an antibacterial spectrum resembling that of cefazolin (CEZ) and shows wide ranging antibacterial activity against Gram positive and negative bacteria.
2) The sensitivity of Staph. aureus strains to CTZ was distributed over ≤0.19-1.56 μg/ml with peaks at≤0.19 and 0.39μg/ml.
3) The peak level of blood concentration was obtained 1/2 hours (7. 3 μg/ml) after a single intramuscular injection of 500mg CTZ, then decreased rather rapidly until 4 hours.
4) When rabbits were given one injection of 50mg/kg intramuscularly, the aqueous humor concentration reached a peak of 1.36μg/ml after 1 hour and penetration could be detected thereafter for 2 hours. The aqueous/serum ratio at the peak was 7.41%.
After intravenous injection of 50mg/kg, a peak value of 2.8μg/ml was observed after one half hour. After 2 hours, the concentration was 0.63, μg/ml, but after 4 hours, none could be detected. The aqueous/serum ratio at the peak was 11.79%.
In investigations of ocular tissue concentration at the times of peak aqueous humor levels, CTZ was found in both the outer and inner parts of the eye. There were higher concentrations with intravenous than with intramuscular injections.
5) A total of 20 cases of external and internal hordeolum, chronic and acute dacryocystitis, corneal infiltration, corneal ulcer, corneal abscess, orbital phlegmone and endophthalmitis were treated with 1-2 injections per day of 1.0g each intramuscularly or one intravenous or drip intravenous injection of 2.0 g of CTZ per day. There were excellent results in 5 cases, good in 11 cases, fair in 3 cases and no effect in 1 case.
6) No noteworthy side effects were observed.

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Fundamental and clinical evaluation of a new semisynthetic cephalosporin C, ceftezole (CTZ), were performed, with the result which lead to the following conclusion.
1) In vitro antibacterial activity : the minimum inhibitory concentration (MIC) of CTZ was measured by an agar plate dilution method using Heart Infusion Agar (Eiken). CTZ revealed an excellent, broad spectrum antibacterial activity against 30 standard strains of various bacteria. CTZ had the same antibacterial spectrum as those of other cephalosporin C antibiotics. The MIC of CTZ against 80 strains of coagulase positive Staph. aureus isolated from otorrhoea was distributed over range of ≤ 0.2 to 50 μg/ml with a peak being observed particulary at 0.39 μg/ml. Clinical isolated strains of E. coli, Pr. mirabilis, and Kl. pneumoniae were inhibited at 1.56 μg/ml to 50 μg/ml of CTZ.
2) Concentration in blood : the blood level of CTZ in healthy adults who were given 500 mg by a single intramuscular injection reached maximum of 11μg/ml at 30 minutes after administration. Even at 6 hours after injection, clinically effective serum CTZ concentration 0.7 jig/ml was still demonstrable.
3) Concentration in tissues : CTZ activity was demonstrable at the concentration of 0.9 to 2 μg/g in human palatine tonsilla, and mucous membrane of maxillary specimen one hour after the intramuscular injection of 500 mg. Further, the serum concentration of CTZ was then 6.4 to 7 jig/ml.
4) Results of clinical treatment : when CTZ was intramuscularly injected in 33 cases of representative infection in the otorhinolaryngologic field. The result was excellent in 16 cases, good in 13 cases, fair in 2 cases and poor in 2 cases. When the cases responded excellent and good were considered together, good results were obtained in 29 cases, that is a ratio of effectiveness of 87.9 per cent.
5) Side effect : no side effect was shown with the intramuscular injection of CTZ. The comparative examination of hepatic function, electrolyte and audiotory activity before and after intramuscular injection showed no significant disturbance.

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Some laboratory examinations were made with a new antibiotic, ceftezole (CTZ), as well as the drug was applied clinically to several otorhinolaryngological infections, and the good results were obtained as follows.
1) The peak of MIC of CTZ was 0.39 μg/ml against Staph. aureus isoleted from lesions.
2) Observing by biophotometer, the growth of Staph. aureus 209 P was inhibited well by the serum (diluted 10 fold) 1/2, 1, 2 and 3 hours after 500 mg and 1, 000 gm of CTZ were injected intramuscularly.
3) Serum concentration was determined by thin-layer cup method with B. subtilis ATCC 6633 as the test organism. The peak of serum level was obtained at 30 minutes after a single intramuscular injection of CTZ.
4) CTZ concentration in tissues one hour after intramuscular injection of 500 mg dosis of CTZ, the concentrations of palatine tonsilla and mucous membrane of sinusitis maxillaris were titrated. The concentrations of blood and palatine tonsilla were 13.0 μg/ml and 1.4 kg/g respectively, the concentrations of blood and mucous membrane of sinusitis maxillaris were 10.8 12g/ml and 0.9 μg/g respectively.
5) CTZ was administered by intramuscular injection to 32 cases of various infections in otorhinolaryngological field and the clinical results were excellent in 24 cases (75.0%), good in 5 cases (15.6%) and poor in 3 cases (9.5%).
6) Side effects were not obtained out of 32 cases.

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From the laboratory and clinical studies on ceftezole (CTZ), the following results were obtained.
1) Activity of CTZ was measured by the plate dilution method on 121 strains isolated from pathological materials in our clinic. The peaks of MIC were ≤0.19 and 0.78 μg/ml with Staph. aureus (55 strains).Pseudomonas species were highly resistant to this antibiotic similarly to other cephalosporin antibiotics.
2) Tissue (tonsil and sinus membrane) and blood concentrations of CTZ were determined 30 minutes after I.M. injection, 1.6 μg/g in tonsil (mean value of 3 cases) and 7.4 μgig in sinus membrane (mean value of 6 cases), 4.9μg/ml and 7.2 μg/ml in serum concentration were detected respectively.
3) CTZ was used clinically in 26 cases of ear, nose and throat infections, and effective rate was 84.0%
4) Adverse reaction was observed in one case; eruption appeared 2 days after I. M. injection.

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Ceftezole (CTZ), a new cephalosporin antibiotic, was administered intravenous and intramuscularly for 15 cases of acute infections in maxillo-facial region, and the clinical effects were investigated.
The results obtained were excellent in 1 case, good in 12 cases, poor in 1 case, effective ratio being 92.7%, with additional 1 case of administration interruption. CTZ may be expected as an effective drug for infections of oral and maxillo-facial region, though its administration method is limited. As a side effect of the drug, only 1 case complained of general fever feeling on the second day which was obliged to interrupt the administration of CTZ.

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Laboratory and clinical studies on ceftezole (CTZ) have been performed, and the following results were obtained.
1) CTZ was administerd intramuscularly at a dose of 100 mg/kg in a group consisting of 3 Wister Imamichi strain rats, and the level was highest in the dental pulp followed by serum, gingiva, tongue, submaxillary lymphonodi, submaxillary glands, and parotid glands in order. The patterns of the distribution were similar to those of cefazolin.
2) Thirtyone patients of acute oral infections were administered intramuscularly at a daily dose of 2 g in adults or 40 mg/kg in children, and good results were obtained in 27 out of 31 cases.
No side effects were observed.

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A new antibiotic ceftezole (CTZ) has been applied to the infectious diseases and the postoperative infection prophylaxis in the field of oral surgery, and the results were obtained as follows :
1) CTZ was administered principally intramuscularly for 4-14 days at a daily dose of 0.5-2.0 g to 15 cases of oral infection and 5 cases of postoperative infection prophylaxis. The results revealed excellent in 2 cases, good in 9 cases, fair in 2 cases, poor in 2 cases in the former, and all cases good in the latter.
2) No side effect was observed with CTZ.
3) No abnormality was observed in blood finding and hepatic function after CTZ administration.

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