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PubMed1994

[Clinical studies on cefozopran in pediatrics].

Cefozopran (CZOP) was administered via intravenous injection to 9 patients (ages ranging from 1 month to 13 years) with pediatric bacterial infections, at daily dose levels between 56.7 and 200 mg/kg, divided into 3 or 4 doses. The following results were obtained. 1. Eight patients, including 1 with purulent meningitis, 1 with sepsis, 3 with acute pneumonia and 3 with lymphadenitis, were treated and subjected to clinical evaluation. Clinical effects were excellent in 6 cases and good in 2, with an overall efficacy rate of 100%. One case with pyoderma was not evaluated because of a combined use of an external antibiotic. 2. Organisms suspected as pathogens included 5 strains: 3 strains of Haemophilus influenzae, 1 strain of Staphylococcus aureus and 1 of Escherichia coli. Bacteriologically, all the strains were eradicated. 3. Side effects or abnormal laboratory test results were observed in 4 cases; wheal in 1 case, elevated GOT and GPT in 2 cases and eosinophilia in 1 case. 4. From the results described above, we considered that CZOP would be an effective drug for use in pediatric bacterial infections.

Adolescent↗
PubMed1994

[Clinical studies on cefozopran in pediatrics].

We conducted clinical studies on cefozopran (CZOP), a newly developed parenteral cephalosporin, for its clinical application in the field of pediatrics. 1. A clinical study was performed on 16 children with infections, including 9 with pneumonia, 1 each with acute bronchitis, enterocolitis, purulent lymphadenitis, 4 with skin and soft tissue infections. CZOP was administered by 30 minutes intravenous drip infusion. Doses varying from 20 to 35 mg/kg body weight were given t.i.d. Lengths of treatment ranged from 4 to 14 days. 2. Clinical efficacies were excellent in 10 and good in 6 cases, with an efficacy rate of 100%. The overall bacterial eradication rate for the pathogenic bacteria was also 100%. 3. Side effect was noted in 1 case with skin rash. Abnormal laboratory test data were found in 5 cases including slight elevations of GPT in 4 cases and GOT in 2 cases.

Adolescent↗
PubMed1994

[Clinical studies on cefozopran in pediatrics].

Cefozopran (CZOP, SCE-2787) was given intravenously to 12 children with acute bacterial infections including 9 with acute pneumonia, 1 each with acute pyothorax, impetigo and staphylococcal scalded skin syndrome. Good or excellent clinical responses were obtained in all of the 12 patients and bacterial eradications were achieved for all 10 strains identified in these cases. No side effects were noted. Eosinophilia was observed in one case, however. From the above clinical results, it appears that CZOP is a useful antibiotic for treatment of pediatric patients with various bacterial infections.

Bacteria↗
PubMed1994

[Pharmacokinetic, bacteriological and clinical studies on cefozopran in the pediatric field].

Cefozopran (CZOP, SCE-2787), a newly developed parenteral cephem antibiotic, was administered to children with bacterial infections. We determined its antibacterial activity, pharmacokinetics, efficacy and safety in these patients. 1. Antibacterial activity MICs of cefmetazole, ceftazidime, cefuzonam, flomoxef and CZOP were determined against a total of 19 strains. For Gram-positive cocci, MICs of CZOP ranged from 0.39 to 0.78 microgram/ml against Staphylococcus aureus (3 strains), from 0.05 to 6.25 micrograms/ml against Streptococcus pneumoniae (5 strains), and 12.5 micrograms/ml against Enterococcus faecalis (1 strain). These MICs were generally similar to those of other cephems, but the MIC of CZOP against E. faecalis was lower than those of the other cephems examined. For Gram-negative bacilli, MICs of CZOP were 25 micrograms/ml against Citrobacter freundii (1 strain), and 6.25 micrograms/ml against Pseudomonas aeruginosa (1 strain). These values were similar to or lower than those of other cephems, MICs of CZOP against Haemophilus influenzae (7 strains) ranged from 0.1 to 0.39 microgram/ml. However, the MIC of CZOP against Serratia marcescens (1 strain) was higher than 100 micrograms/ml, and CZOP was as ineffective as the other cephems against this organism. 2. Pharmacokinetics CZOP was administered to children at 20 or 40 mg/kg via intravenous injection, and determinations were made for its serum concentrations, urinary concentrations and concentrations in cerebrospinal fluid (CSF) using the bioassay. Serum concentrations at 30 minutes after administration were 60.4 micrograms/ml with a dose of 20 mg/kg to one patient and 93.9 and 99.0 micrograms/ml with 40 mg/kg to two patients. The corresponding half-lives were 1.55 hours for 20 mg/kg administration, and 1.10 and 3.41 hours for 40 mg/kg, while the AUCs were 136.5 micrograms.hr/ml for 20 mg/kg, and 194.4 and 264.5 micrograms.hr/ml for 40 mg/kg. The rates of urinary recovery in the first 8 hours after administration were 45.0% in the patient receiving 20 mg/kg, and 84.6 and 97.6% in the two patients receiving 40 mg/kg. The concentrations in the CSF determined in 3 patients with purulent meningitis ranged from 2.6 to 16.0 micrograms/ml 1 hour after administration, and the CSF/serum concentration ratio ranged from 6.5 to 39.0%. These values for pharmacokinetic parameters obtained in the bioassay were similar to those obtained using HPLC. 3. Clinical evaluation Forty-eight patients were clinically evaluated. Of these patients, 75% were less than 3 years of age and there were slightly more male children than female children.(ABSTRACT TRUNCATED AT 400 WORDS)

Bacteria↗
PubMed1996

[Transferability of cefozopran to cerebrospinal fluid in rabbits with meningitis caused by Staphylococcus aureus].

The transferability of cefozopran (CZOP) to cerebrospinal fluid (CSF) was studied employing rabbits with experimental meningitis caused by Staphylococcus aureus. The mean plasma concentration was 293 +/- 17.6 micrograms/ml at 15 minutes after intravenous administration of CZOP at a dose level of 100 mg/kg. The mean concentration in CSF reached its maximum, 16.5 +/- 2.74 micrograms/ml at 60 minutes after administration. Pharmacokinetic parameters calculated from these values were as follows: Cmax (CSF/plasma) 5.72%, AUC (CSF/plasma) 6.61% between 15 and 60 minutes, 9.38% between 15 and 120 minutes and 11.2% between 15 and 180 minutes, T 1/2 for CZOP in CSF: 138 minutes, T 1/2 (CSF/plasma): 2.81. In comparison to those of beta-lactams that were obtained in the same way, the transferability of CZOP to CSF was moderate but concentration in CSF was high, hence, in consideration of the antimicrobial potency against the main pathogens of meningitis, it appears worthwhile of running clinical trials for CZOP.

Animals↗
PubMed1996

[Optimum dose study of cefozopran in the pediatric field].

Cefozopran (SCE-2787, CZOP) was administered to patients with pediatric infections three to four times daily by intravenous injection or 30-minute intravenous drip infusion, and investigations were made in individual cases, on relationships among doses, pharmacokinetics, effects on pathogenic bacteria and MIC against them, and clinical effects. The following results on optimal doses of CZOP were obtained. 1. Clinical cases in which CZOP was administered at a dose of 10 mg (potency)/kg The subjects were 7 patients including 4 patients with pneumonia. Severities of the diseases were severe in one of the patients with pneumonia, and moderate in the other patients. The MIC against pathogenic bacteria (4 strains) isolated from these cases ranged from 0.2 to 1.56 micrograms/ml. The serum concentrations were in a range between 1.4 and 7.6 micrograms/ml at 4 hours after administration. In some cases, the serum concentrations were lower than the MICs, though slightly. In the clinical evaluation, CZOP was excellent in 3 cases, good in 2 cases and fair in 1 case. The evaluation was impossible in 1 case. The efficacy rate was 83.3% (5/6). In bacteriological evaluation, 3 out of the 4 strains disappeared. Adverse reactions and abnormal laboratory test values were not observed. 2. Cases in which CZOP was administered at a dose of 20 mg (potency)/kg The subjects were 5 patients including 2 with pneumonia, and severities were severe in one of the patients with pneumonia, and moderate in the other patients. The MICs against the pathogenic bacteria (3 strains) isolated from these cases ranged from 0.1 to 1.56 micrograms/ml. While, serum concentrations at 4 hours after administration were in a range between 3.0 and 7.7 micrograms/ml sufficiently exceeding the MICs. In the clinical evaluation, CZOP was excellent in 1 case and good in four cases, with an efficacy rate of 100% (5/5). In the bacteriological evaluation, all the 3 strains disappeared. No adverse reactions were observed, but an abnormal laboratory test value showing eosinophilia was noted in one case. 3. Cases in which CZOP was administered at a dose of 40 mg (potency)/kg The subjects were 5 patients including 3 with pneumonia. The severity was moderate in 2 of the pneumonia patients, and severe in the other three cases. The MICs against the pathogenic bacteria (4 strains) isolated from these cases were in a range between 0.1 and 0.78 micrograms/ml. The serum concentrations at 4 hours after administration ranged from 6.5 to 21.9 micrograms/ml, sufficiently exceeding the MICs. In the clinical evaluation, CZOP was excellent in 4 cases and good in 1 case, with an efficacy rate of 100% (5/5). The efficacy rate in the bacteriological evaluation was also 100%. As adverse reaction, red urine was observed in one case. Eosinophlia was noted in one case in the laboratory tests. When CZOP was administered to patients with pediatric infections at a dose of 10 mg (potency)/kg, the clinical effect of the drug was insufficient in a case in which serum concentration of CZOP at 4 hours after administration was lower than the MICs against the pathogenic bacteria. When CZOP was administered at a dose of 20 mg (potency)/kg, sufficient concentrations were obtained, and the drug efficacies were found to be excellent or good in all cases. Therefore, the effective dose normally used is considered to be 20 mg (potency)/kg. When CZOP was administered at a dose of 40 mg (potency)/kg, the drug was found to be excellent or good in all of the cases although the severities were high in more than half of the cases tested. In addition, the rate of excellent efficacies was 80% (4/5). Furthermore, no severe adverse reactions were observed. It was, therefore, confirmed that CZOP should be administered at a dose of 40 mg (potency)/kg in severe or intractable cases.

Bacterial Infections↗
PubMed1996

[Antimicrobial activities of cefozopran against Streptococcus pneumoniae from children].

In order to evaluate antimicrobial activity of cefozopran (CZOP), minimum inhibitory concentrations (MICs) of CZOP and control drugs were determined against Streptococcus pneumoniae from children that were isolated from October of 1995 to January of 1996. Determinations were made for the detection frequency of penicillin-insensitive or resistant strains in biovar utilizing hydrolysis products, and for the correlation of antibacterial susceptibility and macrolides (MLs)-resistant patterns. The results are summarized as follows; 1. MIC90 of CZOP was < or = 0.025 micrograms/ml against benzylpenicillin (PCG)-susceptible S. pneumoniae (PSSP, 50 strains). MIC distribution of CZOP against these strains was approximately equal to that of PCG, and showed stronger activities of CZOP than those of ceftazidime (CAZ), flomoxef (FMOX) and erythromycin (EM). 2. MIC90 of CZOP was 0.39 micrograms/ml against 50 strains of PCG-insensitive S. pneumoniae (PISP) and PCG-resistant S. pneumoniae (PRSP). Antimicrobial activities of CZOP against these strains were stronger than those of CAZ, FMOX, PCG and EM. 3. These isolated strains of PISP and PRSP did not show type III biovar, but showed types I and II. The detection frequency of MLs-constitutive resistant strains were high among type III PSSP and those of MLs-inductive resistant strains were high among types I and II PISP and PRSP. These data suggested that CZOP had strong antimicrobial activities against multiple drug resistant S. pneumoniae including penicillin-resistant strains. CZOP will be effective against S. pneumoniae which often are causative organisms in infections of children.

Anti-Bacterial Agents↗
PubMed1996

Pharmacokinetics and clinical effects of cefozopran in pediatric patients.

An investigation was made into pharmacokinetics and clinical effects of the newly-developed cephem antibiotic for injection, cefozopran (SCE-2787, CZOP), in pediatric patients. In 26 patients in whom pharmacokinetics were investigated, peak serum concentrations of CZOP administered at doses of 10, 20 and 40 mg/kg by i.v. injection were 21.3 +/- 10.0 (mean +/- standard deviation), 51.0 +/- 9.9 and 68.3 +/- 0.7 micrograms/ml, respectively. Serum concentrations at 6 hours after administration were 2.9 +/- 1.7, 2.3 +/- 0.9 and 4.6 +/- 2.6 micrograms/ml, with the levels roughly above MIC90s for dominating pathogenic bacteria being maintained until 6 hours after treatment. Urine concentrations were in the range between 200 and 560 micrograms/ml at 4 to 6 hours after dosing. Cumulative urine excretion accounted for 70 to 80% of dose. In 11 patients in whom pharmacokinetic investigations were performed, peak serum concentrations of CZOP administered at doses of 10, 20 and 40 mg/kg by 30-min. i. v. drip infusion were 37.1, 66.3 +/- 25.5 and 95.7 +/- 8.9 micrograms/ml, respectively. Serum concentrations at 6 hours after dosing were 1.6, 2.3 +/- 0.8 and 3.0 +/- 0.4 micrograms/ml, respectively, with the levels above MIC90s for dominating pathogenic bacteria also being maintained until 6 hours after administration. Urine concentrations were 190 micrograms/ml or more until 8 hours after dosing and the cumulative urinary excretion accounted for 50 to 70% of dose. In 9 patients with meningitis in whom CZOP penetration into cerebrospinal fluid was investigated, concentrations in the fluid of the compound i.v. injected at doses from 40 to 53 mg/kg were in the range between 1.6 and 43.4 micrograms/ml exceeding MICs for pathogenic bacteria at 1 to 1.5 hours after dosing. In all of the 38 patients in whom pharmacokinetic investigations and clinical evaluations were performed, CZOP was good to excellent (excellent in 22 patients and good in 16 patients). Also in bacteriological evaluations, all of the 31 strains of investigated pathogenic bacteria were eradicated. The clinical efficacy rates for the 335 subjects for clinical evaluations were 97.0% (195/201) for patients in whom pathogenic bacteria were detected (group A), and 95.5% (128/134) for patients in whom no pathogenic bacteria were detected (group B). In bacteriological evaluations, the eradication rates of Gram-positive and Gram-negative bacteria were 96.3% (77/80) and 94.5% (155/164), respectively, with the eradication rate in total being 95.1% (232/244). Safety investigations were performed in 364 patients. Adverse reactions were reported in 11 patients (3.0%), including diarrhea (aqueous stool and soft stool) in 7 patients (1.9%) and drug rash (rash, eruption and wheal) in 4 patients (1.1%). Abnormal laboratory test values were noted in 54 patients, including eosinophilia in 20 patients (6.3%) and elevated GPT in 20 patients (6.3%). The adverse reactions and abnormal laboratory test values were not serious, disappearing or improving during the continued treatment period or as a result of discontinuation of the treatment. Serum and urine concentrations of CZOP, when administered by i.v. injection and 30-min, i.v. drip infusion at doses of 10, 20 and 40 mg/kg, were higher than the MICs for pathogenic bacteria until 6 hours after dosing. The drug also showed favorable penetration into cerebrospinal fluid. It was therefore considered that CZOP was a highly useful drug for the treatment of pediatric infections with sufficient bacteriological and clinical efficacy when administered at a dose of 40 to 80 mg/kg three to four times daily.

Bacteria↗
PubMed1997

[The in vitro antibacterial activity of cefozopran against clinically isolated bacteria].

The in vitro antibacterial activity of cefozopran (CZOP) against recent clinical isolates was evaluated and compared with those of ceftazidime (CAZ), cefpirome (CPR), cefepime (CFPM), cefotaxime (CTX), sulbactam/cefoperazone (S/C), imipenem (IPM), oxacillin (MPIPC), and flomoxef (FMOX). MIC80 values of CZOP for methicillin-susceptible Staphylococcus aureus (MSSA, n = 41), methicillin-resistant Staphylococcus aureus (MRSA, n = 57), Streptococcus pneumoniae (n = 45), Enterococus faecalis (n = 49), Enterobacter cloacae (n = 50), Citrobacter freundii (n = 45), Serratia marcescens (n = 45), and Pseudomonas aeruginosa (n = 100) were 1, 32, 2, 16, 4, 1, 0.25, 8 micrograms/ml, respectively. CZOP was more active than CPR against P. aeruginosa and exhibited similar activity to CPR against other species. CZOP was especially active against S. marcescens with MIC values lower than 1 microgram/ml against all strains tested. CZOP was similarly active to or more active than CFPM against all species except for C. freundii. CZOP was not active against MRSA. Thus, we investigated the in vitro combination effects of CZOP/vancomycin (VCM) and CZOP/arbekacin (ABK) using the checkerboard method. The interaction between CZOP and VCM ranged from additive activity (0.5 < FIC index < or = 1.00, n = 37) to synergistic activity (FIC index < 0.50, n = 1), except for one strain showing indifference (1.00 < FIC index < or = 2.00). The interaction between CZOP and ABK ranged from additive activity (n = 22) to synergistic activity (n = 1). These date suggest the potential effect of combination therapy of (CZOP) and VCM or ABK against MRSA. The combined therapy is suggested to be useful to reduce side effects in patients with impared renal function, to reduce the administration dose of VCM or to treat infections of sites where achievable drug concentrations are lower than those commonly achieved in the bloodstream. We also investigated the combination effects of CZOP/AMK and CZOP/GM against CZOP-resistant P. aeruginosa (MIC > 16 micrograms/ml). The combination of CZOP/AMK showed additive activity (n = 9) to synergistic activity (n = 2). The combination of CZOP/GM showed additive activity (n = 5). These results suggest that combinations of CZOP with AMK or GM are effective in treating P. aeruginosa.

Aminoglycosides↗
PubMed1997

[Fundamental and clinical evaluation of cefozopran in low birth weight infants and neonates].

We conducted fundamental and clinical evaluations of a cephem antibiotic, cefozopran (SCE-2787, CZOP), in infants with low birth weights and mature infants. (1) Blood concentrations CZOP was intravenously given in bolus dose of 20 mg/kg to the newborn. The blood antibiotic concentrations were 69.7 micrograms/ml at 30 minutes after administration and the elimination half life was 2.99 hours in mature infants aged 1 to 3 days. They were 38.7 micrograms/ml and 2.85 hours in those aged 4 to 7 days, and 40.8 micrograms/ml and 3.81 hours in those aged 8 days or elder, respectively. In infants with lower birth weights aged 4 to 7 days the blood antibiotic concentrations were 48.6 micrograms/ml at 30 minutes after i.v. administration and the elimination half life was 3.77 hours. The blood antibiotic concentrations at 30 minutes after intravenous doses of 10, 20 and 50 mg/kg in mature infants aged 8 days or elder were 21.1, 40.8 and 153.6 micrograms/ml (value at 60 minutes) and the elimination half lives were 2.24, 3.81 and 3.07 hours, respectively. Administration of CZOP at doses of 20 and 40 mg/kg by intravenous drip infusion over 30 minutes gave the blood drug concentrations of 48.0 and 103.2 micrograms/ml at the end of the infusion and the half lives were 2.60 and 3.33 hours, respectively. (2) Urinary excretion The urinary excretion rates after i.v. bolus doses of 10, 20 and 40 mg/kg were 28.4 to 58.6% of dose. The urinary excretion rate after i.v. drip infusion of 40 mg/kg over 30 minutes was 49.0% of dose. (3) Transfer into cereblospinal fluid The transfer of the antibiotic into cereblospinal fluid in patients with serous meningitis was 4.1 to 15.5 micrograms/ml at 1 hours after administration. (4) Clinical results The clinical efficacy was judged "good" or "excellent" in 2 of the 3 patients with septicemia and in all of the 10 patients with suspected septicemia. It was judged "excellent" in all of the 9 patients with pneumonia, 3 with urinary tract infections and 3 with intrauterine infections. Prophylactic use of the antibiotic was effective in all of the 12 patients. Of the patients in whom bacteriological evaluation was successful, 7 of the 10 causative organisms were confirmed to be eradicated. No adverse drug reactions of signs and symptoms were recognized. Fourteen abnormal alterations of the laboratory test values such as elevation of gamma-GTP and that of GPT were recognized in 8 patients (16.7%). None of them were particularly serious. These results indicate that CZOP is a drug useful for treatment and prevention of infections in infants with lower birth weights as well as in mature infants.

Bacterial Infections↗
PubMed1997

[Pharmacokinetic, bacteriological and clinical studies on cefozopran in neonates].

The efficacy, safety and pharmacokinetics of cefozopran (CZOP) were evaluated in neonates and the following results were obtained: 1. Of the 12 patients treated with CZOP, judgment of clinical efficacy was evaluable in 10 patients (including 5 with pneumonia and 3 with urinary tract infections). The treatment was effective and the causative organism was eradicated in 100% of the patients. 2. No adverse signs and symptoms were recognized during the treatment with CZOP. A slight elevation of direct bilirubin was recognized as an abnormal alteration of laboratory test values in one patient. The value, however, returned to the normal range after the completion of treatment. 3. The pharmacokinetic evaluation was made in 3 of the 12 patients. The blood CZOP levels were recognized in proportion with the dosages. The elimination half lives (T 1/2) in those patients were 8.92, 2.90 and 2.76 hours. Prolongation of T 1/2 was recognized in the patient aged 0 day. It was possible to examine the urinary excretion only in one patient aged 18 days. The excretion rate of the drug was 68.6% of dose by 8 hours after administration. These results suggest that CZOP is a drug useful for treatment of infections in neonates as well, with high efficacy and safety.

Bacterial Infections↗
PubMed1997

[Pharmacokinetic and clinical evaluation of cefozopran in premature and newborn patients].

Cefozopran (SCE-2787, CZOP), which is already on the market with a variety of approved indications in infectious diseases for adult patients, was administered to premature and newborn patients to evaluate the pharmacokinetics and the clinical efficacy. 1. Pharmacokinetics CZOP was intravenously administered at doses of 10.0 mg/kg, 21.4 mg/kg and 40.0 mg/kg to premature and newborn patients, and the blood concentrations and urinary excretion rate were examined. The blood CZOP concentrations were 31.7 and 65.5 micrograms/ml at 30 minutes after administration of 10.0 mg/kg and 40.0 mg/kg, respectively. The elimination half life was 1.78 hours and 2.31 hours, and the urinary recovery was 110.7% and 53.7% within 6 hours after administration, respectively. In the patient given 21.4 mg/kg, the blood CZOP concentration was 36.4 mg/kg at 1 an hour after administration and the elimination half life was 3.97 hours. The urinary recovery was 29.6% within 5 hours after administration. 2. Clinical results The clinical efficacy was evaluated in 19 patients and judged "good" or better in 13 of them with the efficacy rate or 68.4%. The bacteriological response was evaluated in 10 patients from whom Gram-positive cocci of S. aureus (6 strains), S. pneumoniae (1 strain) and E. faecalis (1 strain) and Gram-negative bacilli of H. influenzae (2 strains) and E. coli (2 strains) were isolated as possible causative organisms. With exception of 1 strain each of S aureus and H influenzae, which were not tested after the treatment with CZOP, all of these strains were found to be eradicated. 3. Adverse drug reactions (ADRs) of signs and symptoms and abnormal alterations of laboratory test values. Safety evaluation was made in 24 patients. ADRs of signs and symptoms were recognized in none of them. As abnormal alterations of laboratory test values, increased eosinophils in 3 patients, elevated GOT in one and elevated GPT in one were recognized. These results indicate that CZOP is a drug useful for treatment of infections in premature and newborn patients.

Bacterial Infections↗
PubMed1997

[Pharmacokinetic and clinical evaluation of cefozopran in newborn patients].

Pharmacokinetic and clinical evaluation of an injectable cephem antibiotics, cefozopran (SCE-2787, CZOP), was conducted in newborn patients and the following results were obtained: 1. Clinical results The clinical efficacy of CZOP was evaluated in one each patient with intrauterine infection and suspected septicemia. The efficacy was "excellent" in both patients. No clinically serious adverse drug reactions of signs and symptoms and abnormal alterations of the laboratory test values were recognized. 2. Pharmacokinetics CZOP was intravenously given to newborn patients at doses of 25.0, 20.0, and 18.75 mg/kg. The blood CZOP concentrations were 44.7 +/- 7.0 micrograms/ml (n = 3), 48.3 micrograms/ml and 48.2 micrograms/ml at one hour after administration, respectively. The elimination half life (T 1/2) was 4.22 +/- 1.17 hours (n = 3) in the patients given 25.0 mg/kg and 2.74 hours in the patient given 20.0 mg/kg. The urinary drug excretion rate was 44.5 +/- 8.7% and 31.3 +/- 9.7% of dose within 8 hours after administration of 25.0 mg/kg and 20.0 mg/kg, respectively.

Bacterial Infections↗
PubMed1998

[Clinical evaluation of cefozopran for infections associated with hematological malignancies].

Cefozopran (CZOP) was used as an initial antibacterial therapy for infections in patients with hematological malignancies. CZOP was given at a daily dose of 4 g by drip intravenously to patients who were febrile over 38 degrees C and were suspected as having bacterial infections. As underlying diseases, 8 patients had acute lymphoblastic leukemia (ALL), 9 acute myeloblastic leukemia (AML), 2 aplastic anemia (AA), 2 adult T cell leukemia/lymphoma (ATLL), 28 non Hodgkin lymphoma (NHL), and 2 multiple myeloma (MM). Bacterial infections diagnosed were sepsis in 7 patients, suspected sepsis in 32, bronchitis in 6, pneumonia in 5 and acute peritonitis in 1. Clinical responses among 51 evaluable cases were excellent in 14, good in 15, fair in 3, poor in 19 and the overall response rate was 57%. The overall response rates for AML, ALL, AA, ATLL, NHL and MM were 56%, 63%, 100%, 50%, 50%, and 100%, respectively. Those for sepsis, suspected sepsis, bronchitis, pneumonia and acute peritonitis were 14%, 63%, 100%, 40%, and 0%, respectively. This therapy was effective in 53% (9/17) of patients whose granulocyte count remained below 500/microliter throughout the course of CZOP therapy. Six bacterial and one fungal strains were isolated from blood and sputum of six patients including five sepsis cases; two bacteria were eradicated and bacterial change was observed in one case. As side adverse effects, 10 patients had liver dysfunction, 1 anemia, 2 proteinemia, 1 indirect bilirubinemia, 2 thrombocytopenia, and 1 eosinophilia. We tried to establish a scoring system for the severities of patients with their infections, underlying diseases, treatments for the underlying disease, and granulocyte counts in order to evaluate the efficacy of CZOP more precisely. This scoring system was consisted of three grades; severe, moderate, and mild. CZOP was effective on mild and moderate grades. These results indicate that the initial antibacterial therapy by CZOP is useful for the treatment of mild and moderate grade infections complicated with hematological malignancies.

Acute Disease↗
PubMed2000

[Efficacy and safety of cefozopran (CZOP) monotherapy and combination therapy with CZOP and amikacin (AMK) for infections accompanying hematological diseases].

We evaluated efficacy and safety of monotherapy with CZOP (1-2 g x 2/day) and combination therapy with CZOP (1-2 g x 2/day) and AMK (200 mg x 2/day) for infections in patients with hematological diseases. Efficacy was evaluated in 71 patients of monotherapy group and 70 patients of combination therapy group. Underlying diseases were mostly leukemia and lymphoma. Infections included sepsis, suspected sepsis, pneumonia and so on. Efficacy in CZOP monotherapy was excellent in 21 patients (31.3%), good in 23 patients (34.3%), fair in 5 patients (7.5%) and the efficacy rate was 65.7%. On the other hand, in combination therapy, each was 14 patients (21.2%), 23 patients (34.8%), 12 patients (18.2%) and the efficacy rate was 56.1%. Side effects such as eruption were noted in 2 patients. Abnormal laboratory findings were noted in 9 patients. All side effects as well as abnormal laboratory findings were minimal. It was concluded that CZOP monotherapy was effective in the treatment of various infections accompanying hematological diseases.

Adolescent↗
PubMed1997

[Possibility of drug design of beta-lactam antibiotics effective for multiresistant gram-positive pathogens].

Since infectious diseases are caused by various bacteria and most of them are treated empirically, broad-spectrum antibiotics are required. To expand the spectrum, an imidazopyridazinium group and aminothiadiazole group were introduced to 3- and 7-side chain of cephem nucleus, respectively. The resulting compound, cefozopran, was able to permeate not only outer membrane of Pseudomonas aeruginosa but also envelope of gram-positive bacteria, which functioned as a barrier to antipseudomonal cephalosporins, and showed potent activity against wide variety of bacteria including those which produced a large amount of cephalosporinase and were resistant to third-generation cephalosporins. In spite of the broad antibacterial spectrum, cefozopran only weakly affected gastrointestinal flora of mice and prevented colonization by MRSA.

Animals↗