In this paper, we report the result of the bacteriological evaluation of ceftezole (CTZ) by using cefazolin (CEZ), a known cephalosporin antibiotic with similar structure to CTZ, as a control drug.
1) Antibacterial spectrum
CTZ as well as CEZ showed wide range antibacterial activity against Gram positive and Gram negative bacteria.
2) Susceptibility distribution of clinically isolated strains
Antibacterial activity of CTZ, expressed as MIC, against clinical isolates of Staph. aureus was about twice as strong as that of CEZ. As for E. coli and Proteus, CTZ showed almost the same antibacterial activity as CEZ, and cross resistance between two drugs was recognized.
3) Influence of various factors on antibacterial activity
Influence of medium pH under acid condition showed the increase in antibacterial activity of both CTZ and CEZ. As for the influence of horse serum protein and inoculum size, antibacterial activity of both drugs was decreased as serum concentration became higher and inoculum size larger. This tendency was more remarkable in the case of E. coli than Staph. aureus. And almost no difference was observed between CTZ and CEZ.
4) Stability of CTZ to β-lactamase
CTZ was more stable than ABPC to β-lactamase produced by E. coli strain which is resistant to penicillin and cephalosporin, while inactivated as well as CEZ at high enzyme concentration.
5) Effect of CTZ on growth curve
Bactericidal action of CTZ was observed at the level more than a half of MIC during 8 hour incubation against Staph. aureus 209P-JC, while that of CEZ at the level more than one MIC. Therefore, CTZ was more or less superior to CEZ in bactericidal action. In the case of E. coli NIH JC-2, both CTZ and CEZ showed bactericidal action at the level more than 4 MIC and there was no difference between two drugs
6) Protecting effect of CTZ against experimental infections in mice
Protecting effect of CEZ was superior to that of CTZ against Gram positive staphylococci, streptococci and pneumococci. But that effect against Gram negative E. coli was almost the same between two drugs. The increase in the protecting effect was recognized by twice divided administration of a dose compared with single administration, and this tendency was more remarkable in CTZ. This result would be caused by the difference between absorption, excretion and metabolism in the body of CTZ and those of CEZ.

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We studied on the antibacterial activity of ceftezole (CTZ) against various pathogens recently isolated from clinical materials and compared it with cefazolin (CEZ) and cephalothin (CET).
We used 699 strains of staphylococci, bata haemolytic streptococci, Enterococci, Corynebacterium, E. coil, Klebsiella, Enterobacter, Serratia, Citrobacter, Proteus and Pseudomonas aeruginosa isolated during 1974 and 173 strains of Haemophilus isolated during 1975.
Antibacterial activity was determined by agar plate dilution method.
1) Antibacterial spectrum and activity of CTZ are similar to CEZ.
2) Antibacterial activity of CTZ against Gram-positive bacteria is similar to CET. CTZ is more active against Enterobacteriaceae than CET, but less active against Haemophilus.

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Antibacterial activity of ceftezole (CTZ) against anaerobic bacteria was tested in vitro experiment in comparison with that of CEZ, CEX and CER with similar structure to CTZ.
CTZ showed low level of MIC against anaerobic cocci and Gram-positive anaerobic bacilli, while high level of MIC against subspecies of Bacteroides fragilis of Gram negative bacilli. CTZ showed, however, low level of MIC against B. praeacutus, B. furcosus, B. hypermegas and F. varium except Bacteroides fragilis. This result was common to other cephalosporin antibiotics which showed no antibacterial activity against Bacteroides fragilis.
CTZ showed low level of MIC against anaerobic bacteria similarly to CEZ, while its antibacterial activity was superior to CER and CEX.

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Ceftezole (CTZ), a new cephalosporin C derivative, is a broad-spectrum bactericidal antibiotic. It has almost indentical antimicrobial activity against pathogenic organisms isolated from patients with that of cefazolin (CEZ) which is similar in chemical structure. The therapeutic effect of CTZ on experimental infections in mice was similar to that of CEZ and was superior to cephalothin (CET). The binding of CTZ to serum proteins was somewhat lower than that of CEZ. It is apparent from other bacteriological studies that CTZ and CEZ do not differ significantly in antibacterial properties. The serum levels of CTZ in the test animals and volunteers were determined after i.m. injection of 20mg/kg and after a single dose of 500mg, respectively. The serum levels of CTZ in volunteers peaked at 24.9μg/ml 15min after injection and remained effective (about 2.6μg/ml) at 4 hours. The serum half-life under the same conditions was 56min, i.e., about one half that of CEZ. The 24 hr. urinary recovery rate was 86.6%. Most of the administered CTZ was excreted unchanged mainly through the urinary tract. The biliary excretion rate in SD strain rats after i.m. injection of 20mg/kg was about 4.4%. As compared with commercially available cephalosporins, CTZ was second only to CEZ in biliary excretion rate. Various tissue levels of CTZ in animals were higher than CET, but with the exception of renal levels in the early stage after administration, were lower than CEZ.

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Ceftezole (CTZ) is a new cephalosporin C antibiotic, which has a very similar chemical structure to cefazolin (CEZ). The antibacterial spectrum of CTZ was nearly the same as those of CEZ, cephaloridine (CER) and cephalothin (CET). The. antibacterial activity against clinically islated strains was nearly the same as that of CEZ, that is, the activity against Staph. aureus was next to CER, and the activities against E. coli, Klebsiella spp. and Pr. mirabilis were the strongest of all the cephalosporins tested. The bactericidal effect in vitro was observed similarly to CEZ. Binding rate of CTZ to human serum protein was lower than that of CEZ, and slightly higher than that of CET, but higher than that of CER. Protective effects of CTZ against experimental infection in mice were similar to those of CEZ and CER and stronger than those of CET.
Blood level of CTZ in rats and rabbits was lower than that of CEZ, but higher than those of CER and CET. Excretion rate of CTZ in 24-hour urine of rats and rabbits was the highest of all cephalosporins tested. CTZ, as well as CEZ, was stable in rat tissue homogenate. Its active metabolites were not detected in urine, but only CTZ itself was excreted. Biliary excretion amount of CTZ in rats and dogs was lower than that of CTZ, but much higher than those of CER and CET. As to the distribution into rat organs, CTZ was more rapidly and highly distributed into kidney than other cephalosporins tested, followed by liver, lung, heart and spleen. CTZ was rapidly distributed into lymph and exudate in inflammatory pouch, and attained high level. When CTZ was repeatedly administered to rabbit for a long term, no abnormal change in blood level and urinary excretion was observed, and its accumulation in the organs was not observed.

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A newly devised cephalosporin-derivative, ceftezole (CTZ), was investigated for its stability to various β-lactamases.
Though about 60% of clinically isolated, ampicillin resistant E. coil and Klebsiella spp. were found to produce penicillinase type β-lactamase mediated by conjugative R plasmids, CTZ was still highly effective against them because of its nonhydrolysable character by such types of β-lactamase.
On the other hand, some strains of Ent. cloacae, Serratia marcescens and Pr. vulgaris were highly resistant not only to penicillins but also cephalosporin derivatives including CTZ. Ent. cloacae Nek-39, one of the resistant strains, was confirmed to produce both plasmid-mediated penicillinase type and chromosomally originated cephalosporinase type f3-lactamases, by means of Sephadex G-75, CM-cellulose and DEAE-cellulose column chromatography. CTZ was tolerant to the former g-lactamase but not to the latter one.
CTZ was not hydrolysed also by penicillinase produced by penicillin G resistant Staph. aureus, and it showed marked antibacterial effect on that.
It may be concluded that CTZ is one of the excellent chemotherapeutics for infectious diseases caused by ampicillin resistant E. coli and Klebsiella, and by penicillin G resistant Staphylococcus as well.

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The antigenicity of ceftezole (CTZ) and its cross reactivity with cefazolin (CEZ), cephaloridine (CER), cephalothin (CET) and benzylpenicillin (PC G) were studied. Rabbits were immunized with protein conjugates of antibiotics, and precipitin and hemagglutinating antibodies were found in sera. PCA reactions were also positive between these sera and heterologous protein conjugates of CTZ.
CTZ showed a marked cross reactivity with CEZ as evidenced by passive hemagglutination and PCA reaction, however, a weak cross reactivity was observed with CER, CET and PC G.
CTZ was tested for its reactivity in direct Coombs' testin vitroin comparison with other ralated antibiotics. CET, CER and PC G made Coombs' reaction positive at low concentration, whereas higher concentration of CTZ almost same as CEZ was required to make Coombs' reaction positive.
These findings suggest that immunological properties of CTZ are very close to CEZ because of structural similarities of two drugs.

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The immunological properties of ceftezole (CTZ) were studiedin vitroand in experimental animals. Specific antisera to CTZ were produced in rabbits immunized with protein conjugates of this antibiotic. Its activity was demonstrated by passive hemagglutination, hapten inhibition of hemagglutination, hapten inhibition of quantitative precipitation and PCA reaction. CTZ gave a minimal cross-reactivity with penicillin G and cephalothin, whereas a strong cross-reactivity with cefazolin. This suggests that a strong cross reaction between CTZ and cefazolin may be correlated to the identity of 7-acyl side chain of two compounds.

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Absorption, excretion, tissue distribution and bio-transformation of ceftezole (CTZ), a new semisynthetic cephalosporin antibiotic, were investigated in rats and rabbits following intravenous or intramuscular injection of ¹⁴C-CTZ. Those of cefazolin (CEZ) were investigated similarly in order to compare with CTZ, farther metabolic differences in sex were studied in rats. In whole-body autoradiograms of rats 15 minutes after injection, considerable radioactivity was observed throughout the body and high radioactivity was distributed in kidneys, urinary bladder and intestinal contents, whereas no radioactivity was found at all in fetuses. Blood half-life of CTZ in rats and rabbits given intravenously was 22 minutes, and when given intramuscularly, that in both animals was prolonged. On the other hand, blood half-life of CEZ after intravenous injection was 36 minutes in rats and 46 minutes in rabbits. Within 24 hours 5.6% of the administered radioactivity of CTZ was recovered in bile of rats given intravenously and the biliary excretion of CEZ was higher than that of CTZ. Within 1 hour after injection_55.7% of the intravenously administered CTZ was excreted in urine of rats, 66.4% in urine of rabbits, indicating a rapid excretion of this antibiotic via urine. The studies on metabolites by autoradiography, radioscanning and autobiography of thin layer chromatograms of urine and bile revealed that no radioactive and biologically active metabolite was present both in urine and bile. Reverse isotope dilution analysis showed that CTZ was scarcely metabolized in the body. Disapearance of radioactivity was observed to be rapid in all tissues analyzed and no significant difference in sex was found between female and male rats.

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Acute, subacute and chronic toxicity, and teratogenicity of ceftezole (CTZ) were examined in laboratory aminals.
In acute toxicity tests, no specific symptoms were noticed. LD₅₀values of CTZ in various animals were as high as those of cefazolin.
In one-month, three-month and six-month toxicity tests by subcutaneous injections, both rats and dogs administered more than 500 mg/kg/day of CTZ showed a slight anemia caused by hemorrhage at the site of injection : a little decrease in number of erythrocytes, an increase in number of. reticulocytes and a slight hypererythropoiesis in the spleen and bone marrow.
These findings were also observed in a few dogs intravenously injected at the highest dose, 500 mg/kg/day for 3 and 6 months, whereas no significant findings were shown in the case administered less than 250 mg/kg/day.
No teratogenic effects were observed in mice and rats administered CTZ subcutaneously or intravenously.

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Potential nephrotoxicity of ceftezole (CTZ) and cefazolin (CEZ) was studied in rabbits by intravenous injections.
A single injection of 125, 250, 500 and 1000 mg/kg of CTZ or CEZ caused a dose-related renal injury. This was confirmed by the results of tests of clearance (PAH), PSP excretion, BUN and protein and sugar in urine, and also by macro-and micro-scopic examination of kidneys. CTZ or CEZ injection of 500 and 1000 mg/kg resulted in alteration of renal functions and caused a necrosis of proximal tubules, while 125 and 250 mg/kg administrations did not cause a renal injury.
In rabbits injected CTZ or CEZ, twice daily for 7 consecutive days at a dose of 64 and 125 mg/kg, no abnormalities were observed to be attributable to the drug treatment in both renal functions and kidney structure.
CTZ or CEZ injections at doses of 50 and 100 mg/kg/day for 21 consecutive days would have been not caused a renal injury, while 200 mg/kg dose caused a slight alteration in renal functions, and CTZ injection at doses of 200 mg/kg/day caused slight necrosis to the least extent in proximal tubules.
CTZ seemed to have much less nephrotoxic potential than CEZ.

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CTZは4,000 mg/kgの皮下投与でマウスの自発運動量の減少を, 1,000 mg/kgの静脈内投与でウサギの生体腸管ならびに子宮運動に軽度の変化をきたした。また, 250-1,000 mg/kgの静脈内投与で, イヌまたはネコにおいて血圧上昇, 心拍数変化, 大腿動脈血流増加, 自律神経作用薬の血圧作用増強などが認められた。
しかし, これらの量は臨床1回常用量 (500-1,000mg/人, すなわち体重50 kgとして10-20 mg/kg) と比べてかなり大量であり, 今回の動物実験の成績からみて, CTZは臨床上, とくに不都合な副作用を示さないであろうと思われた。

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Infections of the biliary tract require wide spectrum antibiotics providing high antibacterial concentrations in bile and gallbladder wall. The levels of ceftezole (CTZ) in serum, gallbladder bile, gallbladder tissue and common duct bile were studied in 9 (1 male and 8 female) Japanese patients with cholelithiasis. Following a single injection of CTZ 2g, the peak level in gallbladder bile was 37.5μg/ml on an average and the level in gallbladder tissues was 41.8μg/ml on an average. The maximal concentration in bile from patients with biliary drainage in common bile duct was 24.4μg/ml in 90 minutes after a single injection of CTZ 2g
The organisms most frequently islated from bile of patients with surgical diseases of biliary tract in our clinic were E. coli, Klebsiella, Enterobacter, Proteus and Pseudomonas. The results of sensitivity tests of antibiotics to these Gram negative organisms show that cefazolin (CEZ) is effective on E. coli and Klebsiella and that sulbenicillin is effective on E. coli, Enterobacter, Proteus and Pseudomonas. CTZ has an antimicrobial spectrum and activity similar to those of CEZ.
From these results, CTZ might be of value in the treatment of biliary infections, especially in cases caused by E. coli or Klebsiella.

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Comparative studies were performed on the concentration of ceftezole (CTZ) and cefazolin (CEZ) in sputum specimens collected successively from patients suffering chronic pulmonary disease after cross over administration of those drugs.
1) In a patient with destroyed lung, the concentration of CTZ in sputum specimen after intramuscular administration was measurable after 2-24 hours and the peak tended to attain after 6 hours.
2) CTZ concentration in sputum showed its maximum after 2-4 hours and it seemed to depend on the individual situation rather than the dosis of administrated drug at its effective concentration for about 6 hours.
3) Comparing with the patients administered either intramuscularly or by drip infusion, the latter showed higher concentration at their 2 hours point, while the former exhibited longer concentration.
4) In patients suffering pyothorax, it seemed that CTZ concentration depended on the characters of the lesions as well as the speculated amount of granuloma, and the drug concentration was less than that of CEZ.
5) The general character of CTZ, comparing with that of CEZ, was that concentration rises rapidly and decreases more rapidly after single administration.

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Ceftezole (CTZ) 1g was administered intravenously to 42 patients of operative tonsil in the field of otorhinolaryngology, and tonsillectomy was performed hourly under local anesthesia to assay immediately CTZ in extirpated tonsil by bioassay method.
As a result, CTZ transfer in tonsillar tissue attained to peak 1-1.5 hours after the administration, level being high as 9.1-9.2μg/g on an average. Higher average level of 3.2μg/g remained in tonsillar tissue 8 hours after the administration. It may be concluded thus that CTZ transfers well in tonsillar tissue.

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An experimental local infection system was established by inoculating E. coli, Strept. pneumoniae and Staph. aureus into the subcutancous aseptic inflammatory pouches of rats induced by coton oil. The inhibitory effect of Ceftezole (CTZ) on the growth of the bacteria inoculated into the pouches was compared with those of Cefazolin (CEZ), cephaloridine (CER) and cephalothin (CET), when given intramuscularly or intravenously. The results revealed that the effect of CTZ was nearly the same as those of CEZ and CER and superior to that of CET.

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Laboratory and clinical studies were carried out on a new cephalosporin - ceftezole (CTZ) - and the following results were obtained.
1) In the sensitivity test using plate dilution method, 20 strains of Staph. aureus and 7 strains of Klebsiella showed similar sensitivity pattern to cephalothin (CET), whereas those of 23 strains of E. coli were superior to CET.
2) Cup method using B. subtilis PCI 219 as a test organism would be recommended to measure CTZ in body fluid. In investigation of i.m. absorption and excretion study in human subjects. CTZ showed about 4.5 pg/ml of blood level at 1 hour and 50% of urinary recovery.
3) Clinical investigations of CTZ treatment were carried out on 39 cases with bacterial infections including 8 cases with upper respiratory infection, 3 pneumonia, 5 biliary tract infection, 2 suspicious sepsis and 21 urinary tract infections. Most of patients had underling diseases such as diabeted mellitus. Twenty nine cases responded well to the treatment clinially but 4 failed. Bacteriological cure rate was 78% in 27 cases. During treatment 3 patients complained of local irritation of injected site, 3 female patients showed anemia, and another one high transaminase and Al-P level, but these may be not attributable to the treatment.

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Basic and clinical studies have been performed on ceftezole (CTZ). MIC of CTZ showed a low value especially against Staph. aureus, as well as against other Gram negative cocci tested. CTZ was administered in thoracic cavity or injected intramuscularly in rabbits to compare their concentrations in serum. The ratio became larger with the lapse of time, and the concentration was maintained after CTZ administration in thoracic cavity, excretion in urine being about 60% of that of intramuscular injection within 24 hours. Active substance in urine was investigated by means of TLC-bioautography, and the result indicated that this substance is CTZ itself. By intravenous drip infusion of CTZ 3 g, a concentration was maintained nearly a constant level during drip infusion, and lowered rapidly after completion. Transfer in saliva was quite low. Urinary recovery was about 82% within 24 hours. After 500 mg were administered in thoracic cavity of the patient of spontaneous pneumothorax, it was clarified that a transfer from thoracic cavity is quite rapid in view of the transition of serum concentration, though the maintenance is shorter than that in rabbit. Concentration in saliva was low, and urinary recovery was about 52%.
CTZ was injected intravenously by drip infusion singly as chemotherapeutic drug for the patients of severe or over middle infection of respiratory apparatus in which an abnormal shadow was recognized distinctly in X-ray photograph, and a favorable result was noticed in all cases. There was encountered no finding which would have, been attributable to a side effect of CTZ.

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Ceftezole was administered intramuscularly for 7-29 days at a daily dose of 1.0-2.0g to 15 cases of various infections (respiratory organs infection 7 cases, urinary tract infection 5 cases and biliary tract infection 2 cases and sepsis 1 case), and the clinical effects of the drug were investigated.
As a result, the drug revealed to be effective in all cases except 1 case of which the effect was unknown due to the death. The effect of the drug was especially remarkable in urinary tract disease and acute cholecystitis.
As a side effect of the drug, eruption was noticed in 1 case, and no other untoward effects were observed in hematogenous functions and hepato-renal functions.

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Ceftezole, a new antibiotic of cephalosporin analogue, was applied to the treatment of 14 patients with respiratory infections. The drug was administered intravenously (0.5-1.0g×1 or 2/day) for the period of 5 to 47 days. The therapeutic effect was evaluated as summarized below.
1) Of 14 cases examined, 8 cases (57.1%) showed positive response : Each 3 cases were classified into “very effective” or “effective” and 2 cases were into “slightly effective”, while remaining 6 cases into not effective.
2) Classified into diagnosis, 4 of 5 patients of pneumonia, 2 of 5 cases of lung abscess, and 2 cases of acute bronchitis obtained positive response.
3) No abnormality was revealed by the clinical examinations in either the blood picture or the hepatic and renal functions, except drug eruption was observed in one case.

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1) The MIC of ceftezole (CTZ), using plate dilution method, against Staph.aureus, E. coli, Klebsiella, Enterobacter and Pr. mirabilis were found to be similar to those of cefazolin.
2) Concentrations of CTZ were determined in serum and urine of 3 normal volunteers. The concentrations of serum were 14.2 μg/ml at 2 hours after 500 mg intravenous injection. The serum levels were 6.8-8.6 μg/ml at 1 hour after 1 g and 2 g intravenous injection. Average urinary recoveries in these volunteers were about 70% during 6 hours.
3) CTZ was administered to a total of 7 cases, 6 cases of pneumonia and 1 case of cholecystitis. Clinical response of CTZ obtained in those cases was excellent in 2 cases and good in 5 cases. No side effect to be mentioned was observed.

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Experimental and clinical studies on ceftezole (CTZ), a new antibiotic, were performed, and the following results were obtained.
1) The sensitivity of clinical isolates against CTZ was almost comparable to that of CEZ, showing cross resistance between them.
2) The organ levels 30 minutes after CTZ intramuscular injection to mice ranked in order of kidneys, serum, liver and lungs.
3) Clinically seven patients were treated with CTZ.
Except for three patients in whom the judgement was impossible or remained indeterminable, one with binary tract infection and two with urinary tract infection responded well, but one patient with diffuse panbronchiolitis showed no effectiveness.

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Ceftezole (CTZ) was studied on its antibacterial activity, absorption, excretion and clinical effect, and the following results were obtained.
1) Antibacterial activity
Susceptibility of CTZ was distributed among 0.39 - 100 μ/g/ml with E. coli (100 strains), 90 of 100 strains. were inhibited at 0.8 μg/ml or less; 0.39 - 25 μg/ml with Klebsiella (37 strains), 35 of 37 were at 12.5 μg/ml or less and 0.2 - 100 μg/ml with Pr. mirabilis (70 strains), 48 of 70 were at 12.5 μg/ml or less. Antibacterial activity of CTZ against Gram negative bacteria was similar to cefazolin.
2) Serum levels and urinary excretion
Peak of serum level in healthy adults was attained 5 minutes after intravenous administration of 1, 000 mg dose, the value was 100 μg/ml, and then serum level was rapidly decreased, showing 2.5 μg/ml after 2 hours. The serum half life was 0.41 hour and urinary recovery within 4 hours was 79%.
A patient with chronic renal failure showed creatinine clearance value of 6.9 ml/min. was intravenously administrated 500 mg dose, and the peak of serum level was attained 5 minutes after, the value was 36.3 μg/ml, and then slowly decreased, and showed 12.5 μg/ml after 6 hours. The serum half life was 4.48 hours and urinary recovery within 6 hours was 40%.
3) Clinical results
CTZ was clinically applied to 14 cases with bacterial infections, including 2 cases of respiratory tract infection, 3 cases of cholecystitis and 9 cases of urinary tract infections, and the results obtained were excellent in one case, good in 7 cases and failed in 6 cases.
No marked side effects were observed, except eruption in one case.

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Ceftezole (CTZ) is a new cephalosporin derivative developed in Japan. This report describes the studies of antibacterial activities and the absorption and urinary excretion as well as the clinical trial with this drug.
The antibacterial activities to Staph. aureus, E. coli and Klebsiella were similar to those of CEZ.
The average serum concentrations in six healthy volunteers were 19.2, 14.8 and 0 μg/ml at 1/2, 1 and 6 hours after intramuscular administration of 500 mg of CTZ, which were a little lower than those of CEZ and the duration of detectable serum concentrations was shorter than that of CEZ.
The average urinary excretion within 6 hours was 66%, and the majority of injected CTZ was excreted within 2 hours.
The average concentrations were 36.3, 8.0, 3.8 and 0.6 μg/ml at 1/4, 1, 2 and 4 hours after intravenous administration of 500 mg of CTZ in six healthy volunteers, and CTZ was detectable at 6 hours after administration in only one case. The average urinary excretion was 78% within 6 hours, and most of injected CTZ was excreted within 2 hours.
The serum concentrations of two patients after intramuscular administration of 500 mg of CTZ were a little lower than those of volunteers. The peak of urinary excretion was at 2-4 hours after administration, and the excretion was somewhat delayed in comparison with that of volunteers.
The serum concentrations were 22.5-30.0 g/ml at 1/2 hour after intravenous administration of 1, 000 mg of CTZ in two patients, and 1.56 μg/ml at 6 hours after administration in one of these cases. The urinary excretion within 6 hours was 77.7 % in one case.
Clinical results of CTZ in various diseases, including 12 cases of bacterial pneumonia, 1 case of acute tonsillitis, 2 cases of acute cholecystitis, 2 cases of acute pyelonephritis, and 1 case of meningitis, were excellent or good in 13 out of 16 cases. Two cases were excluded since the administration period was less than 7 days.
In one case, urticaria-like eruption was seen. No abnormal findings were seen in laboratory tests.

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Ceftezole (CTZ) was evaluated on four aged patients with septicemia. Causative organisms were E. coli. Strept. faecalis, Klebsiella and Staph. aureus.
CTZ was given 1 g every 8 to 12 hours intramuscularly. The patient with E. coil septicemia and the patient with Streptococcal septicemia failed to respond satisfactorily to the treatment for 11 to 18 days.
The patient with Klebsiella septicemia and the patient with Staph. aureus septicemia showed adequate response. The MIC of each causative organism was as follows, E. coli : 50 μg/ml, Strept. faecalis : 25 μg/ml, Klebsiella : 12.5 μg/ml and Staph. aureus : 6.3 μg/ml.
No serious adverse effect or no significant deterioration of liver and kidney function were observed during CTZ therapy.
Simultaneous determination of the concentration in serum and cerebrospinal fluid was undertaken 2.5 hours after intramuscular injection of 1 g of CTZ on a patient with Streptococcal septicemia, who had recovered diabetic coma. Concentration in serum was 32 μg/ml and that in CSF was 10 μg/ml.

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Ceftezole (CTZ) is a new antibiotic which belongs to the cephalosporin C group, and has a similar chemical structure to Cefazolin.
In order to study the effectiveness and the side effect of this agent, we gave it to 15 patients (7 men and 8 women) with various kinds of infections, and obtained good result in 10 cases. Usual dosage of CTZ was 2.0 to 3.0 g per day, and this was administered I.M. or I.V., divided in 2 to 3 times daily, for 5 to 14 days. In 2 cases, higher dosages were used.
CTZ was excellent in 6 cases of urinary tract infections caused by E. coli, Enterobacter, Staph. aureus and Strept. faecalis and good in 2 cases, but poor in 1 case of urinary tract infection caused by mixed organisms.
One case of subacute bacterial endocarditis, 43 years old female, was treated with daily dose of 9 g of agent for 50 days (total dose 378 g). She responded well and remained asymptomatic for more than one year after cessation of therapy.
This drug was poor in 2 cases of sepsis. One was caused by E. coli, and the other was caused by Strept. pneumoniae and Pseudomonas. Remaining 3 cases consisted of bronchopneumonia, tonsillitis and cholecystitis responded all well to this agent.
No side effect was observed in any of these 15 cases studied. There was no effect in hemoglobin, WBC, GOT, GPT, BUN and serum creatinine level.

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Laboratory and clinical investigations have been carried out on ceftezole (CTZ), a new cephalosporin antibiotic, and following results were obtained.
1) Antimicrobial activity of CTZ against clinically isolated Staph. aureus, E. coli, Klebsiella and Pr. mirabilis was almost the same as that of cefazolin.
2) The peak blood concentration of CTZ was obtained 1/4-1/2 hours after a single intramuscular administration.
3) Average urinary recoveries of 6 healthy volunteers were over 80% within 6 hours after intravenous and intramuscular administration.
4) Clinically, CTZ was applied to 16 patients with infectious diseases, and 13 out of 16 patients, were improved.
5) No side effect was noticed

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The laboratory and clinical observations on ceftezole (CTZ) have been carried out as follows :
1) The in vitro binding to serum proteins was smaller with CTZ than with CEZ, indicating 67.7% and 84.8% respectively.
2) In patients with various degree of renal impairment, blood levels after intravenous injection of 500 mg of CTZ were higher in proportion to lowering of Ccreat.
The serum half life of CTZ was 0.5-1.4 hours in the normal or mildly impaired group (Ccreat > 60 ml/min.), 1.7-2.5 hours in the moderately impaired group (Ccreat 30-60 ml/min.), and 3.3-5.8 hours in the severely impaired group (Ccreat < 30 ml/min.).
The recovery rate of CTZ in urine from the patients decreased in the degree of impaired renal function.
3) CTZ was administered to 3 cases of infectious diseases; 1 patient with biliary tract infection and 2 patients with respiratory infection.<bR>All the cases were effective clinically without any detectable adverse reaction.

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Ceftezole (CTZ) has been studied clinically, and the following results were obtained.
1) CTZ was injected intravenously at a dose of 1 g to the patients with renal insufficiency under hemodialysis, and the blood concentrations were determined. The average values of 3 cases were 120, 90 and 48 μg/ml respectively 1, 6 and 24 hours after the administration on the days off hemodialysis, while 73 and 35 μg/ml respectively 6 and 24 hours after the administration on the days on hemodialysis for 6 hours.
2) CTZ was administered clinically at a daily dose of 1-6 g to 17 patients of various infections including the cases on hemodialysis. The therapeutic results obtained were excellent in 3cases, good in 9, fair in 1 and poor in 4.No side effects were observed with CTZ in kidney, liver and bone marrow.

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On a new synthetic cephalosporin C derivative, ceftezole (CTZ), some laboratory and clinical studies were performed.
The results were summarized as follows :
1) By the thin-layer cylinder-plate method using B. subtilis ATCC 6633 as a test organism, CTZ levels in body fluids were assayable to the lower limit of 0.05μg/ml.
2) Following a single intramuscular administration of 1, 000 mg of the agent, blood levels exhibited a peak concentration of 22-24μg/ml at 1 hour, with a persistence of effective levels over ensuing 6 hours.
Urinary peak levels, at that time, was 2, 500μg/ml and urinary recovery was 83.7% for 24 hours.
Active levels were also obtained in sputum and pleural effusion following CTZ administration.
3) Clinical effect with CTZ was excellent in 2 cases, i.e. bronchopneumonia and pulmonary abscess both due to Strept. pneumoniae. No side effect was noticed in these cases.
4) In a case of bronchopneumonia of old age, an allergy-like reaction (chill, fever, skin eruption) appeared immediately after intravenous drip infusion of CTZ on the third day of chemotherapy. Those symptoms disappeared within 3 hours after onset.

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The results obtained from the study on a new antibiotic, ceftezole (CTZ) was as follows.
1. The MIC value of most strains isolated from clinical specimen was almost the same as that of cefazolin (CEZ).
2. Clinically, effectiveness was obtained in 11 cases out of 12 cases (91.6%) of respiratory infection, while remarkable effect was observed in 2 cases out of 3 cases (66.6%) of urinary tract infection.
3. No noteworthy side effect was noticed with CTZ.

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Laboratory and clinical studies have been carried out on a new antibiotic ceftezole (CTZ), and the following results were obtained.
1. No large difference was noticed between antibacterial activity of CTZ and that of cefazolin (CEZ) against both standard strains of gram negative bacilli (E. coli, KL pneumoniae, Proteus species, Ps. aeruginosa) and isolated strains from lesion.
2. Biliary excretion amount of CTZ in perfusing isolated liver of rat, was distinctly lower than that of CEZ.
3. CTZ was administered clinically in 11 cases of internal infection mainly of respiratory tract infection, and the results obtained were remarkably effective in 3 cases, effective in 6 cases, and ineffective in 2 cases.
No noteworthy side effect was observed with CTZ, except eosinophilic leucocyte increased slightly in a case.

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Eleven in-patients with acute respiratory tract infection (7 cases), acute cholecystitis (2 cases) and acute pyelitis (2 cases) received the treatment of ceftezole (CTZ). Doses of 1 or 2.g were dissolved in 500 ml of 5% glucose solution and administered Intravenously ever one hour period once daily for 11-26 days.
The results obtained were “Excellent” In 5 and “Good” in 6 cases.
No side effect was observed with CTZ throughout all the cases.

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Ceftezole (CTZ) has been investigated, and the following results were obtained.
1) CTZ was injected intramuscularly at a dose of 500 mg to healthy adults, to investigate its serum concentration and urinary excretion. Peak serum level was attained in 30 minutes after administration, mean value of 3 cases indicating 16.5 μg/ml. Serum concentration lowered rapidly then, showing 2.9 μg/ml after 4 hours, and no antibacterial activity was noticed in serum after 6 hours. Urinary recovery demonstrated 77% on an average within 6 hours, and more than 2/3 was excreted in urine within 2 hours after administration.
2) CTZ was administered clinically at a daily dose of 2-6 g to each 1 case of bronchiectasis with infection, bronchopneumonia, lung cancer with infection, septicemia, reticulum cell sarcoma and leukemia with pyrexia, totaling 6 cases. The results obtained were excellent in 1 case, good in 1 case and poor in 2 cases among the above 4 cases which may have been considered to be indicated objects of antibacterial drug. No side effect was observed throughout all cases.

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Ceftezole (CTZ), a new cephalosporin C derivative, was examined in respect to its antibacterial activity, blood level, urinary excretion, and clinical effectiveness.
1) MIC of CTZ against clinically islated Staph. aureus distributed between 0.2 and 0.8 μg/ml, and those against E. coli showed a peak of distribution at 1.6-3.1μg/ml : Those antibacterial activities of CTZ were found to be rather stronger than cefazolin (CEZ), and decisively stronger than other cephalosporin antibiotics.
2) Four healthy volunteers were administered with CTZ 1g intramuscularly or intravenously. The blood levels reached the maximum of 22 μg/ml 1/2 hour after the intramuscular injection, descending thereafter, and disappeared 6 hours after. The intravenous administration of 1g CTZ gave blood level of 28-30 μg/ml 1/2 h. after the injection, lowering thereafter, and disappeared 6 hours after. The urinary excretion rate was higher than 70% in 6 hours. Those data were similar to those obtained by 0.5 g injection of CEZ.
3) Nine patients (bronchitis 3, pyelonephritis 5, post-operative infection 1) were treated with CTZ 1-6 g daily, administered i.m., i.v. (one shot) or by drip indusion. Seven of them showed favored response to the therapy. No side effects were found.

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CTZについて, 抗菌力, 投与後の血清中濃度を検討し, また少数例の呼吸器感染症に投与して, 以下の成績を得た。
1. CTZのブドウ球菌, 大腸菌, 変形菌に対する試験管内発育阻止作用は, CEZのそれとほぼ同程度であった。
2. CTZの筋肉注射後および静脈内注射後の血清中濃度は, CEZ投与後のそれらに比して低値であり, ことに4時間後ならびに静脈内注射後にその差が著明であった。
3. CTZ静脈内注射により治療を行なった呼吸器感染症2例中の1例で, 本物質投与後に, 発熱・発疹を認め, CTZに関係ある過敏反応が強く疑われた。
本論文の概要は, 第23回日本化学療法学会総会 (昭和50年5月24日・神戸) において報告した。

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1) There were no differences in the distribution of MIC between Ceftezole (CTZ) and Cefazolin (CEZ) against both 100 stock strains of Staph. aureus and Staph. epidermidis. MIC of CEZ against 100 stock strains of E. call was distributed to be lower concentration than that of CTZ.
2) From the results of MIC test against clinically isolated strains by the disc method, it could hardly be concluded that the antimicrobial activity of CTZ was specifically more effective than that of CEZ. The numbers of CTZ sensitive strains were slightly more than that of CEZ sensitive ones in the Gram negative bacteria, particularly Klebsiella.
3) From the determination of effective concentration of CTZ in the blood and urine, the intramuscular injection of CTZ lg twice a day was enough in the treatment of the urinary tract infection and other infections diseases needed the intramuscular injection of CTZ Ig 3 times a day.
4) Clinical effects of CTZ were studied in the followed 17 patients. Three cases in the urinary tract infection, 11 cases in the respiratory tract infection and 1 case of the Peptococcus sepsis could be cured by the injection of CTZ. But in the treatment of another 2 patients with the respiratory tract infection, the effect of CTZ is not found in 1 case and could not be determined in another case. No side effects were observed except one case in which eruption was noticed.
5) The clinical course of HB-Ag associated acute hepatitis was not changed by the administration of CTZ.

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Laboratory studies have been performed on ceftezole (CTZ), a newly developed cephalosporin antibiotic, and this drug has been applied clinically to various infections of respiratory organs. Results obtained were as follows.
1) Antibacterial activity : Minimum inhibitory concentrations of CTZ were determined by means of standard method of the Japan Society of Chemotherapy on 519 strains in total including 22 strains preserved in our department as standard and 497 strains isolated from various clinical materials (Staph. aureus 64, β-Streptococcus 32, Salmonella 16, Shigella 15, E. coli 64, Kl. aerogenes 64, Ent. aerogenes 32, Ent. cloacae 32, Serratia marcescens 64, Pr. vulgaris 20, Pr. mirabilis 30 and Ps. aeruginosa 64). Compared these results with those of cefazolin, antibacterial activity of two drugs was almost the same.
2) Distribution in organs of rat : CTZ was injected intramuscularly to male Wistar rats at a dose of 20 mg/kg, and the drug concentrations in various organs were measured. Peak was attained in 30 minutes, and levels were arranged in order of kidney > serum > lung > liver. Ratios of organs level to serum level were kidney 5.017, lung 0.569 and liver 0.353.
3) Blood level in human : CTZ was injected intramuscularly by drip infusion for 2 hours at a dose of 3 g with 5% glucose, and blood concentrations of the drug were measured. Peak value of 78-85 μg/ml was shown at termination of drip infusion, and no blood activity was noticed 6 hours after completion of the infusion. Half life time was about 30 minutes.
4) Level in sputum : CTZ was administered similarly to 3) to the cases of bronchiectasis expectorating purulent sputum, and CTZ activity of 0.8 μg/ml was noticed in sputum. Ratio of sputum level to maximum blood level was 0.01.
5) Clinical results of respiratory infections : CTZ was injected intravenously by drip infusion at a dose of 3 g once daily to 6 cases of respiratory infections. Results obtained were excellent in 3 cases of bacterial pneumonia, fair in 1 case of lung abscess, and failure in 2 cases of bronchiectasis.
6) Side effect : Slight elevation of GOT and GPT was observed in 1 case out of the above 6 cases, though the values were normalized after interruption of the drug administration. No abnormality was noticed in other subjective symptoms and hemato-biochemical findings.

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The present authors have carried out a double blind test on the patients of pneumonia hospitalized in 23 institutions as indicated in Table 1, to compare clinical effects of ceftezole (CTZ) with those of cefazoin (CEZ). Each drugs was administered intramuscularly at a daily dose of 2 g for 7-14 days, and both therapeutic efficacy and utility were investigated by comparison.
1. Prescribed dose of the drug was administered for 7-14 days and transfer of chest X-ray finding could be judged in 117 cases of pneumonia. Comparison was made between two drugs of CTZ and CEZ, and the following conclusions were obtained.
1) No significant difference was observed in the therapeutic effects on 7th or 14th day after administration between 53 cases of CTZ group and 64 cases of CEZ group.
2) No significant difference was shown between the utility of two drugs in 117 cases of pneumonia.
2. Investigation was performed on 167 cases, excluding the cases of whom a bacterial pneumonia was suspected at first visit and a prescribed treatment was commenced, however an against-rule or non-objective disease was confirmed distinctly after the examination completion. As a result, no significant difference was demonstrated in therapeutic effects between two drugs.
3. No difference was noticed between the side-effects of two drugs in total 182 cases including the above 117 cases.

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Ceftezole (CTZ), a new cephalosporin C derivative, has been applied in pediatric field, and the following conclusions were drawn.
1) Concentration in blood and excretory ratio in urine after CTZ injection were higher than those after cephaloridine, cephalothin, cephapirin and cephacetrile administrations, while similar to those after cefazolin application.
2) All cases of middle or severe respiratory tract infections (acute bronchitis and pneumonia) responded well to consecutive intramuscular injection of CTZ 50-100 mg/kg/day.
3) Large-dose intravenous injection of CTZ (200-400 mg/kg/day) was effective in a primary period of pyothorax. Concentration in blood was higher in acute period than in convalescent period, while excretory ratio in urine was rather lower in acute period.
4) Temporal elevation of GOT and GPT was observed with large-dose administration in 1 case out of 44 cases, and yet it was reversible, furthermore no abnormality was noticed in all cases tested on blood and urine.
5) From the above findings, CTZ may be considered to be worthy of a therapeutic drug for infantile infections.

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Ceftezole (CTZ) was administered to the children's bacterial infections, including 6 cases of urinary tract infections, 5 cases of pneumonia, 4 cases of lacunar tonsillitis, 3 cases of toxic epidermal necrolysis, 1 case of lymphadenitis colli purulenta and 1 case of periappendix abscess, totaling 20 cases.
Clinical effectiveness was obtained in 17 cases out of 20 cases, and bacteriological effectiveness in 10 cases out of 12 cases excluding 8 cases with unknown bacteria.
Haematological, renal and hepatic functions were performed in all the cases treated before and on the completion of CTZ therapy, and no untoward laboratory findings were noticed. No side reactions were observed throughout the clinical course of CTZ therapy.

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The authors have carried out the laboratory and clinical studies of ceftezole (CTZ).
The results were as follows;
The sensitivity was measured by the plate dilution method with 32 strains of Staph. aureus, 14 strains of E. coli and 8 strains of Klebsiella isolated from patients. The growth of all strains of Staph. aureus was inhibited at concentrations of less than 1.56 μg/ml. The growth of 11 strains of E. coliwas inhibited at concentrations of less than 6.25μg/ml, and 6 strains of Klebsiella, at less than 1.56μg/ml.
CTZ was given in a single intramuscular dose of 20 mg per kg b.w. to four children. The maximum blood level was reached at 30 minutes after administration. The levels were 24.0, 52.0, 96.0 and 98.0 μg/ml, respectively.
The excretion rates of CTZ in the urine after a single intramuscular dosing of 20 mg per kg b.w. were 13.1-77.2% up to 6 hours period.
CTZ was clinically applied to a. total of 8 cases of pneumonia, and good response was obtained in 6 cases.
No side effects were observed.

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Ceftezole (CTZ) was given to 54 children with the following acute bacterial infections : 33 patients with pneumonia, 5 with empyema, 3 with scarlet fever, 4 with lacunar tonsillitis, 5 with urinary tract infection, 2 with osteomyelitis and 2 with bacterial meningitis. The age of the patients ranged from 1 month to 13 years. The daily dose was 40 to 100 mg/kg in most cases and was given intramuscularly or by a one-shot intravenous route. The length of administration extended from 4 to 12 days in a majority of cases.
The results were as follows :
1) In 33 patients with pneumonia, the result was excellent in 23 patients, good in 7, and failure in 3; the overall efficacy rate was 90.9%. In 5 patients with empyema, it was good in3 and failure in 2; the overall efficacy rate was 60.0%. It was excellent in all 3 patients with scarlet fever. In 4patients with lacunar tonsillitis, it was excellent in 2 and good in 2, respectively. In 5 patients with urinary tract infection, it was excellent in 3 and good in 2. In each 2 patients with osteomyelitis and bacterial meningitis respectively, it was good in all. The overall efficacy rate in these 54 children was 90.7%; excellent in 31, good in 18, and failure in 5.
2) The concentration of this antibiotic in the cerebrospinal fluid (CSF) was determined in 2 patients with bacterial meningitis. Its disappearance from the CSF was found to be faster than that of cefazolin.
3) No adverse reaction was noted except for asymptomatic eosinophilia in 1 case. Little adverse reaction was considered to be one of the merits of this antibiotic.
4) Based on the above results, it was concluded that CTZ is a potent new antibiotic in acute bacterial infections in children.

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Ceftezole (CTZ) was given to 27 pediatric patients with acute bronchitis, acute pneumonia, pulurent meningitis, septicemia, pulurent lymphagitis, phlegmon and urinary tract infection, and its clinical effect and side effects were investigated.
CTZ was given intramuscularly to 3 patients in daily doses of 50-70 mg/kg (mean : 60 mg/kg) in 4 divided portions for an average of 10 days and by one-shot intravenous injection to 24 patients in daily doses of 50/200 mg/kg (mean : 100 mg/kg) in 4 divided portions for an average of 12 days. Of the total patients, response was marked in 30%; moderate in 55%; and 15% failed to respond. The effectiveness rate was 85%.
Clinical isolates were obtained from 11 patients : all six with β-haemolytic streptococci responded moderately; of the 4 with Staph. aureus, one responded moderately and one failed to respond; and the one patient with E. coli failed to respond.
The sensitivity of these organisms to cefazolin (CEZ) was determined by paper disc method : 8 strains ofβ-haemolytic streptococci showed 3 pluses (+++); of the 4 strains of Staph. aureus, 3 showed 3 pluses (+++) and one, 2 pluses (++); and one strain of E. coli showed one minus (-).
With CTZ, the following side effects developed : vascular pain at the time of one-shot intravenous injection in 2 patients; transient urticaria-like rash in 2; leukopenia in one; abnormally increased GOT values in only 2 (though one more patient with septicemia.also showed both increased GOT and GPT values, these findings were due to septicemia but not due to the drug); a slight increase of A 1-P in one. No abnormal BUN and creatinine values were noted.
From the above clinical results it is apparent that CTZ, like CEZ, is a useful antibiotic for treating pediatric patients with various kinds of bacterial infections.

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1) Antibacterial spectrum
Ceftezole (CTZ) showed excellent antimicrobial activity against both gram-positive and -negative bacteria except Strept. faecalis, B. cereus, Pr. morganii and Ps. aeruginosa.
2) Antimicrobial activities against clinically isolated strains
CTZ showed almost the same activities as those of CEZ against Staph. aureus and Klebsiella, but its activities against E. coli and Proteus were a little lower than those of CEZ.
3) Blood and urinary levels
Blood levels were assayed with cup-plate method using Moni-trol serum for the standard curve. CTZ was administered intramuscularly at a dose of 500 mg and 1000 mg, and blood levels attained a peak after 30 minutes with the mean value of 25.1μg/ml and 30.3μg/ml, respectively. Urinary levels attained a peak after 1 hour with the mean value of 1, 457ug/ml and 5, 233ug/ml, respectively. Mean recovery rates in urine during 6 hours were 66.5% and 81.1%, respectively.
4) Tissue levels
Twenty mg/kg of CTZ given intramuscularly to SD strain rats revealed that the tissue levels in radioassay were the highest in kindney, followed by serum, liver, lung, spleen and heart, with the same order as that in bioassay.
5) Metabolism
Metabolism of CTZ was examined in human urine after given CTZ, as well as rat urine after given ¹⁴C-labelled CTZ. The results of bioautogram, radioautogram and radioscanning on samples obtained by thin-layer chromatography revealed that CTZ was excreted in urine without being metabolized.
6) Clinical results
CTZ was administered to 25 cases of surgical infections. Clinical response was effective in 21 cases and failure in 4 cases with effectiveness of 84%. Adverse reactions were not observed in 31 cases including 6 cases of prevention of infection.

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Laboratory and clinical investigations have been performed on ceftezole (CTZ), and the following results were obtained.
1) CTZ was injected intravenously at a dose of 0.5 g, and the serum levels obtained were 36.5 μg/ml after 10 minutes, 23.8 μg/ml after 30 minutes, and 10.0 μg/ml after 60 minutes, and the bile levels obtained were 1/30-1/5 of that in serum after 10 minutes, and 15.5 μg/ml after 45 minutes.
2) CTZ was injected intramuscularly at a dose of 1.0 g, and the serum levels obtained were 10.7 Ag/ml after 1 hour, 3.2 μg/ml after 3 hours, and not proved after 6 hours. To the contrary, a certain level was proved in bile each after 2, 3 and 4 hours, while it was not proved at all there after 6 hours except a case with hepatic dysfunction.
3) Electrophoresis and bioautogram were investigated on human serum after CTZ administration, and electrophoretic characteristics were different between CTZ and albumin fraction.
4) CTZ was administered for 7-32 days to 4 cases of severe infection in surgical field at a dose of 0.2 g per day (total dose 6.4 g) in babies and 1.0-2.0 g per day (total dose 6.5-34 g) in adults, and the clinical effectiveness was observed in all cases.
5) Both clinical findings and laboratory results revealed no side-effect which would be attributed to CTZ.

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Following results were obtained in our fundamental and clinical studies on ceftezole (CTZ).
The antibacterial activity of CTZ was similar to that of cefazolin against Staph. aureus and GNB.
The excretion of CTZ in human bile was examined.
CTZ was administered to 18 cases of severe infections in surgical field, and clinical response was excellent in 4 cases, good in 10 cases, poor in 3 cases and unknown in 1 case. No side effect or adverse reaction was observed.

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Ceftezole (CTZ), a new antibiotic derived from cephalosporin-C, is a similar compound to cefazolin. The authors investigated on serum level, urinary excretion, clinical effectiveness and untoward side effects of the agent.
1) The mean serum level showed a peak of 11.0 μg/ml 30 minutes after a oneshot intravenous injection of 1 g CTZ in 3 healthy volunteers with mean urinary excretion of 807.6 mg (80.8%) within 6 hours.
2) CTZ was given on 28 patients with infections in the field of surgery, 6 cases intramuscularly and 22 ones intravenously. The clinical evaluation of results was classified into excellent in 7 cases, good 11, fair 6, poor 4, the effectiveness rate being counter 85.7 percent.
3) Among untoward side effects, there were experienced oral burning sensation in one case and liver and urinary dysfunctions (increased GOT, GPT and BUN values) in another case.

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Laboratory and clinical investigations have been carried out on ceftezole (CTZ), a new cephalosporin antibiotic.
1) Sensitivity distribution of CTZ to clinical isolates was investigated on Staph. aureus, E. coli, Klebsiella and Proteus. As a result, sensitivity of CTZ was almost the same to that of CEZ, and sensitivity distribution to Gram negative bacteria was 1-2 degrees higher than that to CET and CER.
2) Absorption and excretion of CTZ were studied. As a result, blood concentration attained to peak of about 20 μg/ml 30 minutes after an intramuscular injection of 1 g. As to excretion in urine, 65-70% was excreted within 4 hours. CTZ 1 g was injected intravenously by drip infusion for 1 hour, and concentration in bile was less than 4 μg/ml in 5 cases out of 6 cases, while 16.5 μg/ml in another case.
3) CTZ was applied clinically to 13 cases of surgical infections, and the results obtained were excellent in 2 cases, good in 6 cases, fair in 4 cases and failure in 1 case, effective ratio being about 60%.
4) As a side effect, 1 case complained of slight discomfort at intravenous injection. Blood finding and liver function did not demonstrate any side effect which would have been attributed to CTZ.

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Some laboratory and clinical studies in the surgical infection have been carried out on a new antibiotic ceftezole (CTZ) and the following results were obtained.
1) Absorption and excretion
CTZ (1.0 g) was administered intramuscularly. in 4 patients. The highest peak of blood level was at 30 minutes and the urinary excretion of the drug was 70.8% at 3 hours after administration. The biliary excretion of CTZ was relatively good and the mean concentration of the drug in 3 cases was about 4.1 gg/m1 in hepatic bile at 1 hour after intramuscular administration of 1.0 g, while the excretion into pancreatic juice was not so good.
2) Results of clinical application
CTZ was mainly applied in the treatment of infected wound after operation. The therapeutic reslults at 18 cases were excellent in 5 cases, good in 11 cases and poor in 2 cases.
There were no serieus side effects except one patient complained of itching and examthema.

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