SEARCH · PubMed Health

Results for “Cefozopran”

Explore indexed PubMed citations for clinical trials, systematic reviews and public health research. Read source abstracts and follow each citation to its original PubMed record.

Quote a phrase for an exact phrase match. Source license links do not imply unrestricted reuse.

At least 19 recordsLinked to original sources

PubMed1994

[Pharmacokinetic and clinical studies with cefozopran in the pediatric field. Pediatric Study Group of Cefozopran].

We investigated pharmacokinetics and clinical effectiveness of a newly developed cephem antibiotic cefozopran (SCE-2787, CZOP) against various pediatric infections in 18 institutions and their affiliates. We obtained the following results. 1. Serum concentration and urinary excretion rates Pharmacokinetics of CZOP in children was examined after intravenous injection and 30-minute drip infusion of 10, 20 and 40 mg/kg of CZOP. Peak serum concentrations of CZOP in 30 minutes after intravenous injection were 21.7, 51.5 and 77.8 micrograms/ml, respectively, showing a clear dose response. Half-lives were 1.99, 1.85 and 1.67 hours, respectively. In the first 6 hours after administration, urinary excretion rates of CZOP were 87.3, 67.4 and 84.1%, respectively. In the cases of 10, 20 and 40 mg/kg administration of CZOP 30-minute drip infusion, peak serum concentration of CZOP in 30 minutes, when the infusion was completed, were 38.1, 72.8 and 95.6 micrograms/ml, respectively. Again, there was a clear dose response. Half-lives were 1.67, 1.69 and 1.43 hours, respectively. In the first 6 hours after administration, urinary excretion rates of CZOP were 53.9, 59.7 and 77.3%, respectively. Cerebrospinal fluid concentrations of CZOP administered by intravenous injection of 50 mg/kg to patients with purulent meningitis were 1.6 to 43.4 micrograms/ml in 1 to 1.5 hours after administration. 2. Clinical study Clinical efficacy was evaluated in 337 cases. The largest number of cases, 138 cases, were found in 2 to < 6-year olds. The majority of the patients were under age 9, and 70 cases were of less than 1-year old infants. 183 cases were males and 154 cases were females. In terms of illness, a majority, or 185 cases, suffered from pneumonia, followed by 39 cases of UTI and 23 infections of the skin and soft tissue. There were 7 cases of purulent meningitis. In 218 cases, CZOP was administered at a daily dose of 60- < 80 mg/kg. The drug was administered for 6-10 days, the most frequent duration, in 188 cases. In the cases where causative organisms were identified (group A), the efficacy rates ("excellent" and "good") obtained were 100% (5/5) against purulent meningitis, 100% (2/2) against sepsis, 98.3% (119/121) against pneumonia, 100% (13/13) against acute bronchitis, 100% (11/11) against upper respiratory tract infection, 96.3% (26/27) against UTI. Overall, "excellent" and "good" responses were observed in 97.5% (197/202) of cases with known causative organisms.(ABSTRACT TRUNCATED AT 400 WORDS)

Adolescent↗

PubMed1996

[Pharmacokinetic, bacteriological and clinical studies on cefozopran in neonates and premature infants. A study of cefozopran in the perinatal co-research group].

The following results were obtained in pharmacokinetic, bacteriological and clinical investigations of a cephem antibiotic for injection, cefozopran (SCE-2787, CZOP), administered to neonates and premature infants. 1. Pharmacokinetics (1) Half-lives (T 1/2's) of CZOP in 0-day-old (less than 24 hours after birth) neonates and premature infants were longer than those in 1-day-old or older infants. When half-lives were compared between 0-day-old neonates and 0-day-old premature infants, longer half-lives were observed in premature infants. (2) When CZOP was intravenously administered to 1-day-old or older neonates and premature infants at a dose of 20 mg/kg, no differences were noted in blood concentrations between neonates and premature infants from 30 minutes to 6 hours after administration as well as T 1/2's. (3) Blood concentration of CZOP administered at doses of 10, 20 and 40 mg/kg were dose-dependent. (4) Urine excretion rates of CZOP administered to 1-day-old or older neonates and premature infants were approximately 30 to 60% in the first 6 hours after administration. Urine excretion rates in 0-day-old neonates and premature infants were low. 2. Clinical results (1) Of a total of 136 cases to which CZOP was administered, clinical efficacy evaluation was possible in 96 cases, and safety evaluation in 132 cases. (2) The clinical efficacy rates were 78.6% (22/28) in 28 cases in which causative organisms were detected (Group A), and 97.1% (66/68) in 68 cases in which no such organisms were detected (Group B), with the total efficacy rate (Groups A and B) of as high as 91.7% (88/96). (3) Bacteriological evaluations were made with 33 strains isolated from the 28 cases of Group A. Elimination rates for Gram-positive and Gram-negative bacteria were 88.2% (15/17) and 92.3% (12/13), respectively, with the total elimination rate of 90.0% (27/30). No microbial substitution was noted. (4) As an adverse reaction, diarrhea was noted in one case (0.8%). Abnormal laboratory test values were noted in 15 cases (12.3%) including eosinophilia, elevated GPT, and elevated gamma-GTP. All of these abnormalities were transitory, and none of them critical. As a result of above pharmacokinetic and clinical investigations, CZOP is considered to be highly useful in the treatment of indicated infections in neonates and premature infants. It appears that 20 mg/kg of CZOP can be administered by intravenous injection or intravenous drip infusion to neonates and premature infants aged 0-day (less than 24 hours after birth) once or twice daily, to those aged 1 (24 or more hours after birth) to 7 days twice or three times daily, and to those aged 8 or more days three to four times daily, and that the dose can be increased up to 40 mg/kg in cases of critical or intractable infections.

Bacterial Infections↗

PubMed1993

Therapeutic effect of cefozopran (SCE-2787), a new parenteral cephalosporin, against experimental infections in mice.

The therapeutic effect of cefozopran (SCE-2787), a new semisynthetic parenteral cephalosporin, against experimental infections in mice was examined. Cefozopran was more effective than cefpiramide and was as effective as ceftazidime and cefpirome against acute respiratory tract infections caused by Klebsiella pneumoniae DT-S. In the model of chronic respiratory tract infection caused by K. pneumoniae 27, cefozopran was as effective as ceftazidime. The therapeutic effect of cefozopran against urinary tract infections caused by Pseudomonas aeruginosa P9 was superior to that of cefpirome and was equal to those of ceftazidime and cefclidin. In addition, cefozopran was more effective than ceftazidime and was as effective as flomoxef in a thigh muscle infection caused by methicillin-sensitive Staphylococcus aureus 308A-1. Against thigh muscle infections caused by methicillin-resistant S. aureus N133, cefozopran was the most effective agent. The potent therapeutic effect of cefozopran in those experimental infections in mice suggests that it would be effective against respiratory tract, urinary tract, and soft tissue infections caused by a variety of gram-positive and gram-negative bacteria in humans.

Animals↗

PubMed2004

The combination of aztreonam and cefozopran against Stenotrophomonas maltophilia.

Aztreonam is suited for combination chemotherapy because it could be a potent Beta-lactamase inhibitor. We designed a study to show the inhibitory activity of aztreonam, using Stenotrophomonas maltophilia, which produces both carbapenemase L1 and penicillinase L2. Aztreonam showed considerable synergy with cefpirome and contributed to a decrease in minimum inhibitory concentrations of cefozopran. In further examinations, the mean viable bacterial counts in cultures treated with aztreonam-cefozopran were 1 log lower than those in cultures treated with cefozopran alone. These results confirm that inhibition of penicillinase L2 occurred. We hope that a combination chemotherapy using aztreonam and cefozopran will be used to prevent the emergence of penicillinase-producers.

Anti-Bacterial Agents↗

PubMed2004

Development and validation of a MEKC method for the direct determination of cefozopran in human serum.

A method for determining the concentration of cefozopran, a cephem anti-microbial agent which has a broad spectrum, in human serum using micellar electrokinetic capillary chromatography (MEKC) by serum direct injection is developed and the validation of the assays of this method is performed. A borate buffer (25mM; pH 10.0) containing sodium dodecyl sulfate (SDS) (50mM) is used as a run buffer. The electrophoresis of serum samples is carried out at 25kV and the detection of cefozopran at 244nm as its absorption maximum at the cathodic side of the capillary. The migration time of cefozopran is 6.5min. Linearity (0-200mg/l) is good and limit of quantification is 0.5mg/l at a signal-to-noise ratio of 3. Coefficient of variation (CV) of intra-day precision and that of inter-day precision are 2.4-4.0% (7.3-92.0mg/l) and 2.9-7.7% (22.5-71.4mg/l), respectively, and the recovery rate is 92-109%. The detection results of 12 other cephem anti-microbial agents under the analytical conditions of this method show that the migration time of cefmetazole is identical with that of cefozopran, making it impossible to separate these two anti-microbial agents. This method is characterized by the fact that simple and economic determination can be achieved by directly injecting the serum samples of micro-quantities into the capillary.

Cephalosporins↗

PubMed1996

Penicillin-binding protein 5 as an inhibitory target of cefozopran in Enterococcus faecalis.

The concentration of cefozopran which inhibits binding of [14C]benzylpenicillin to penicillin-binding protein (PBP) 5 of Enterococcus faecalis TN2OO5 by 50% was 11 mg/L, and its MIC was 12.5 mg/L. Ceftazidime and cefmenoxime, which were inactive at 100 mg/L, showed no affinity for PBP 5 at this concentration. Ampicillin, benzylpenicillin and imipenem showed higher affinity for PBPs 3/4 and PBP 5 than cefozopran, and their MICs were lower than that of cefozopran. No correlation between MICs of the test compounds and the affinity for PBP 1, 2 or 6 was found. These results suggest that cefozopran exhibits antimicrobial activity against E. faecalis TN2OO5 by binding to PBP 5.

Anti-Bacterial Agents↗

PubMedDate not supplied

Therapeutic efficacy of cefozopran in a murine model of haematogenous pneumococcal meningitis.

Antimicrobial regimens for the treatment of pneumococcal meningitis are not established. We have produced a murine model of haematogenous pneumococcal meningitis and have examined its usefulness for determining the required dosage and term of antimicrobial agents. Streptococcus pneumoniae serotype 6 was injected intraperitoneally (inoculum: about 1 x 10(4) CFU) into mice. Although half of the mice died within 2 days, the surviving mice showed positive bacterial cultures, increase of the protein level, decrease of the glucose level and infiltration of polymorphonuclear leucocytes into cerebrospinal fluids (CSF). When cefozopran was administered subcutaneously twice a day for 1-3 days starting 2 days after infection, dose- and duration-dependent effects were observed and all mice treated with 20 mg/kg of cefozopran for 3 days survived. The penetration rate of cefozopran from blood to CSF in infected mice was 44.7%, which was 6 times higher than that obtained in uninfected mice. This model may be useful for investigating the pathogenesis of haematogenous pneumococcal meningitis and its therapy.

Animals↗

PubMed1997

Therapeutic effects of cefozopran against experimental mixed urinary tract infection with Enterococcus faecalis and Pseudomonas aeruginosa in mice.

The therapeutic activity of cefozopran, a new semisynthetic parenteral cephalosporin, was compared with those of ceftazidime, ampicillin, imipenem/cilastatin and ofloxacin against an ascending mixed urinary tract infection induced in mice with Enterococcus faecalis TN2005 and Pseudomonas aeruginosa P9. Cefozopran significantly reduced viable cell counts of both organisms in the kidneys. Ceftazidime, imipenem/cilastatin and ofloxacin were active against only P. aeruginosa, and ampicillin was active against only E. faecalis.

Ampicillin↗

PubMed2001

Outbreak of cefozopran (penicillin, oral cephems, and aztreonam)-resistant Neisseria gonorrhoeae in Japan.

We have previously reported that the Neisseria gonorrhoeae isolates from clinical failure cases treated with cefdinir and aztreonam, beta-lactams exhibited high MICs. These resistant isolates were clearly separated from the isolates exhibiting a low level of resistance to beta-lactams as shown by the MIC distribution of cefozopran. Restriction fragment length polymorphism DNA typing revealed that the outbreak of cefozopran-resistant isolates in Kitakyushu, Japan, occurred as a result of clonal spread.

Adult↗

PubMed1999

[Bacteriological and clinical break points: evaluation of the usefulness of cefozopran based on MIC].

Drug sensitivity of clinically isolated bacteria to cefozopran (CZOP), which is a new cephem antibiotic, was investigated, and the usefulness of the drug was evaluated from the viewpoint of bacteriological and clinical (pneumonia) break points. The following results were obtained. 1. According to bacteriological break points, methicillin-resistant Staphylococcus aureus (MRSA) and Enterococcus spp. showed low sensitivity to cefozopran (CZOP). However, the sensitivity of methicillin-sensitive Staphylococcus aureus (MSSA), E. coli, and Klebsiella spp., which are often isolated as pathogens of common infections, was 100%, that of Enterobacter spp., Serratia sp., and Citrobacter sp. was 90% or higher, and that of Pseudomonas aeruginosa was 80% or higher; the values were comparable to or better than those for ceftazidime (CAZ). These results suggest a expanded antibacterial spectrum and enhanced antibacterial potency of CZOP. 2. The estimated response rate of pneumonia to CZOP was 87.5% in outpatients and 51.9% in inpatients. Therefore, CZOP is considered to be one of the first choices especially in outpatient empiric therapy.

Cephalosporins↗

PubMed1994

[Pharmacokinetic and clinical studies on cefozopran in the field of pediatrics].

Blood and urine levels of cefozopran (CZOP) were determined, and its efficacy and safety profile was evaluated in the field of pediatrics. The results of this study are summarized as follows. 1. Blood levels of CZOP peaked in 30 minutes to 1 hour (initial blood collection) after intravenous administration at a dose of 20 or 40 mg/kg. Its blood levels at 6 hours after intravenous administration were 1.6 micrograms/ml (HPLC) or 1.9 micrograms/ml (bioassay) at a dose of 20 mg/kg and 2.9 to 9.1 micrograms/ml (HPLC) or 2.9 to 8.4 micrograms/ml (bioassay) at a dose of 40 mg/kg. The half-lives were 1.58 to 2.27 hours (HPLC) and 1.53 to 1.85 hours (bioassay), respectively. The rate of recovery of CZOP in the urine in the first 8 hours after intravenous administration at a dose of 20 mg/kg was 61.5% (HPLC) or 54.6% (bioassay), and urine levels of CZOP at 6 to 8 hours after administration were 157.3 micrograms/ml (HPLC) and 129.7 micrograms/ml (bioassay). 2. When CZOP was administered to 16 patients with respiratory tract infections, 2 patients with urinary tract infections, 2 patients with acute enteritis, 1 patient with skin soft tissue infection, and 1 patient with purulent lymphadenitis, the responses were excellent in 68% of patients and good in 32% with an overall efficacy rate of 100%. 3. Bacteriological effect of CZOP was excellent and the rate of bacterial eradication was 100% (9/9). 4. MICs of CZOP against clinical isolates (Staphylococcus aureus, methicillin-resistant S. aureus (MRSA), Streptococcus pneumoniae, Escherichia coli, Moraxella (Branhamella) catarrhalis) were compared to those of other injectable cephems ceftazidime (CAZ), cefuzonam (CZON), flomoxef (FMOX), cefmetazole (CMZ). The MICs of cefozopran (CZOP) against Gram-positive organisms, S. aureus, MRSA, and S. pneumoniae, were nearly as low as those of CZON and were clearly lower than those of CAZ. MICs of CZOP against Gram-negative organisms were examined and the MIC against E. coli was as low as those of other antibiotics but the MIC of CZOP against M. (B.) catarrhalis was higher, at 1.56 micrograms/ml, than those of CAZ, FMOX, and CMZ. 5. Diarrhea was experienced by 1 of 22 patients as a side effect from CZOP, and abnormal laboratory tests including increases of eosinophil counts in 2 patients (9.1%), a decrease of neutrophil counts in 1 patient (4.5%), thrombocytosis in 1 patient (4.5%), and an elevation of GPT in 3 patients (13.6%).(ABSTRACT TRUNCATED AT 400 WORDS)

Bacteria↗

PubMed1997

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

Cefozopran (CZOP) was administered to nine newborn patients with infections at a dose of 20 mg/kg twice or three times daily for 5 to 6 days to evaluate the efficacy, safety and pharmacokinetics of cefozopran. 1. Blood concentrations CZOP was intravenously given to 6 newborn patients by drip infusion at a dose of 20 mg/kg over 30 minutes. The maximum blood concentrations (Cmax) were 38.4 micrograms/ml in a patient aged 0 day, 37.7 and 54.3 micrograms/ml in two patients aged 1 day, 51.3 and 64.1 micrograms/ml in two patients aged 3 days and 51.0 micrograms/ml in a patient aged 5 days. Cmax was lower in the patient aged 0 day. The elimination half life (T 1/2) was 9.2 hours in the patient aged 0 day, 4.9 and 3.7 hours in the patients aged 1 day, 3.1 and 2.4 hours in the patients aged 3 days and 2.9 in the patient aged 5 days, showing a prolongation of T 1/2 in patients of lower age. 2. Urinary excretion Of the 6 patients given CZOP at a dose of 20 mg/kg by intravenous drip infusion over 30 minutes, urine was collected in 5 patients. The cumulative excretion rate within 6 hours after infusion was as low as 19.8% of dose in the patient aged 0 day. The rates were elevated as high as 46.3 and 57.0% of dose in the patients aged 1 day. In the patient aged 3 days, the recovery within 4 hours after infusion was 47.3%. It was 70.6% of dose within 6 hours after dosing in the patient aged 5 days. The urinary recovery within 6 hours after dosing increased with the advance of age. 3. Clinical results Efficacy was evaluable in 7 patients. Of them, 3 had suspected septicemia, 2 pneumonia, 1 intrauterine infection and 1 urinary tract infection. The clinical efficacy was judged "excellent" in all the evaluable patients. Neither adverse drug reactions of signs and symptoms nor abnormal alterations of the laboratory test values were recognized in the 9 patients evaluable for safety. These results suggest that CZOP is an effective and safe drug for treatment of infections in the newborns. As for the dosage and method of administration from the view of the pharmacokinetic data obtained, intravenous drip infusion of 20 mg/kg once or twice daily was considered to be sufficient for patients aged 0 day. For patients aged 1 to 7 days and those aged 8 days or elder, the administration of twice to 3 times daily and 3 to 4 times daily were considered to be sufficient, respectively.

Bacterial Infections↗

PubMedDate not supplied

Therapeutic effects of cefozopran on polymicrobial infections associated with Enterococcus faecalis in a Rat pyometra model.

Enterococcus faecalis plays an important role as a pathogen in polymicrobial infections. We evaluated the efficacy of cefozopran (CZOP) using polymicrobial pyometra rats. Rats were infected with a mixed intrauterine inoculation of E. faecalis plus either Bacteroides fragilis or Prevotella bivia (minimal inhibitory concentration of CZOP; E. faecalis: 6.25 micrograms/ml, B. fragilis: 12.5 micrograms/ml, P. bivia: 12.5 micrograms/ml). Immediately after inoculating 10(5) CFU of each organism/rat, CZOP (either 40 mg/kg, i.v., q.i.d., for 5 days or 80 mg/kg, i.v., b.i.d., for 5 days) was administered. The intrauterine inflammatory change and bacterial counts in the CZOP-treated group were compared with those in the nontreated control group. CZOP significantly (p < 0.01) decreased the bacterial counts except for B. fragilis in the regimen of 80 mg/kg b.i.d. However, the 40 mg/kg, q.i.d., regimen significantly (p < 0.05) reduced bacterial counts compared to 80 mg/kg, b.i.d. These results suggest that CZOP in a more divided dose is efficacious for the treatment of polymicrobial infections associated with E. faecalis in pyometra.

Animals↗

PubMed1999

[Pharmacokinetic analysis of cefozopran in neonatal infections--population pharmacokinetics using nonmem].

This report describes the results on pharmacokinetics, efficacy and safety of cefozopran (CZOP) in neonatal patients. Enrolled patients were 136 in total whose informed consents to enter this study had been given by their parents. Among them, blood samples were collected from 42 neonates to analyze concentrations of CZOP by population pharmacokinetics (PPK) methods. Based on this analysis, the average pharmacokinetic parameters of CZOP and the variabilities of them in different morbid pharmacological backgrounds and in different subjects were evaluated. This PPK analysis showed that clearance (CL) and distribution volume (Vd) of CZOP could be estimated by the following equations; CL = 0.0452 x WT1.75 (in the case of the postnatal age of over than 1 day) CL = 0.623 x 0.0452 WT1.75 (in the case of the postnatal age of 1 day or less) Vd = 0.455 x WT where WT indicates body weight in kg. The coefficients of variation among individual subjects on CL and Vd were found to be 20.7% and 20.0%, respectively. From this PPK analysis it was indicated that the elimination of CZOP is dependent on the postnatal age and is approximately 38% lower in the younger group than in the older group. Therefore, it could be concluded that, though the cases of evaluation were small in number, adjustment of dosing of CZOP is necessary, particularly in prolongation of intervals of administration, in cases of postnatal age of 1 day or less.

Cephalosporins↗

PubMed1999

[Clinical effects of combination therapy with cefozopran and tobramycin for severe infections in patients with hematologic diseases].

We studied clinical effect of a combination therapy with cefozopran (CZOP) and tobramycin (TOB) for infections in 80 patients with hematologic diseases in 15 institutes. Combined doses with CZOP 2 g and TOB 60-90 mg twice a day had been given intravenously. Of the 80 patients, 61 patients (42 with acute leukemia, 10 with malignant lymphoma, 3 with aplastic anemia, 2 with chronic myeloid leukemia, 2 with multiple myeloma, and 2 with myelodysplastic syndrome) were evaluable. Those consisted of 6 patients with septicemia, 49 with suspected septicemia, 3 with pneumonia, and 3 with other infections. Clinical efficacy by the treatment was excellent in 24, good in 17, fair in 9, and poor in 11 patients, and the overall efficacy rate including excellent and good was 67.2%. Microbiologically, 5 of the 6 patients with septicemia (1 coagulase negative Staphylococcus, 2 S. pneumoniae, 1 S. oralis, and 1 E. coli) were responded. The efficacy rate in patients with severe granulocytopenia showing 100/microliter or lesser neutrophil counts during the drug administration was 57.1% (12/21). Side effects and abnormal changes of clinical laboratory findings were observed in 5 patients, and 16 patients, respectively, but most of them were mild. The findings above suggested that the combination therapy with CZOP and TOB is useful as an empiric therapy for severe infections in patients with hematologic diseases.

Adult↗

PubMed2000

[A comparative study on the clinical utility of cefozopran and cefpirome against complicated urinary tract infections].

Aiming at evaluating the utility of cefozopran (CZOP) against complicated urinary tract infections with the velocity of eradication of causal bacteria in early treatment and clinical efficacy by new criteria of UTIs, a comparative study was conducted using cefpirome (CPR) as the control drug. CZOP and CPR were administered by intravenous drip infusion at a dose of 1 g twice daily. The duration of treatment was for 5 days. The study method involved randomized assignment of the subjects to either group CZOP or group CPR. The results were as follows: 1. Of a total of 80 cases treated, 65 (CZOP group--32 cases, CPR group--33 cases) were evaluated for efficacy. 2. The overall clinical efficacy evaluation according to the criteria proposed by Japanese UTI Committee rated the CZOP group as 90.6% (29/32), and the CPR group as 90.9% (30/33), with no significant difference between the 2 groups. Clinical efficacy evaluated by attending physicians rated the CZOP group as 93.8% (30/32) and the CPR group as 90.9% (30/33). There was no significant difference between the 2 groups. 3. The efficacy rates to pyuria on day 2 were 26.7% and 0% for the CZOP group and the CPR group, respectively, indicating a higher efficacy rate for the former (p < 0.05). Those on after treatment were 59.4% and 54.5% for the CZOP group and the CPR group, respectively, with no significant difference between the 2 groups. 4. Regarding the bacteriological effect, the eradication rates of both groups were over 90% on day 1 and after treatment. There was no significant difference between the 2 groups. 5. Side effects occurred in 1 case (2.6%) out of 39 in the CZOP group and in 1 case (2.4%) out of 41 in the CPR group. Laboratory test value fluctuation was noted in 8 (20.5%) of 39 cases in the CZOP group and 11 (26.8%) of 41 cases in the CPR group. There was no significant difference between the 2 groups. The results indicate that CZOP achieves an early efficacy to pyuria, and is as useful as CPR against complicated urinary tract infections.

Adult↗

PubMed2001

[Clinical effects of combination therapy with cefozopran and amikacin for infections in patients with hematological disorders].

Cefozopran (CZOP) and amikacin (AMK) were used concomitantly to treat infections complicated by hematological diseases. A total of 103 subjects were evaluated, and the all over efficacy rate was 69.9%. Acute leukemia was found in the largest number of patient, 57, followed by 29 cases of malignant lymphoma and 7 cases of myelodysplastic syndrome. By type of infection, patients having unknown origin were the largest in number, being 66, and the efficacy rate was 71.2%. The efficacy rates for sepsis, pneumonia and upper respiratory infection were 42.9% (7 cases), 71.4% (14 cases) and 90% (10 cases) respectively. The efficacy rates by neutrophil counts before administration of CZOP and AMK and at 1 week after administration were both 53.3% in the group of less than 100/microliter, both 60% in the group of less than 500/microliter. The efficacy rate by neutrophil counts at 1 week after administration was 58.6% in the group of less than 100/microliter. The efficacy rate was 75.4% in the group of granulocyte colony stimulating factor (G-CSF) concomitant usage, and 61.9% in the group of non-concomitant usage group. The efficacy rates by serum albumin levels before administration of CZOP and AMK and at 1 week after administration were both 92.9% in the group of over than 4 g/dl, both 50% in the group of less than 3 g/dl. Concomitant treatment with CZOP and AMK exhibited a high level of safety and efficacy rates in infections complicated by hematological diseases.

Adult↗

PubMed2002

[Post-marketing surveillance of antibacterial activities of cefozopran against various clinical isolates--I. Gram-positive bacteria].

As a post-marketing surveillance, the in vitro antibacterial activities of cefozopran (CZOP), an agent of cephems, against various clinical isolates were yearly evaluated and compared with those of other cephems, oxacephems, penicillins, and carbapenems. Changes in the bacterial sensitivity for CZOP were also evaluated with the resistance ratio calculated with breakpoint MIC. Sixteen species (1,913 strains) of Gram-positive bacteria were isolated from the clinical materials annually collected from 1996 to 2000, and consisted of methicillin-susceptible Staphylococcus aureus (MSSA; n = 178), methicillin-resistant S. aureus (MRSA; n = 199), methicillin-susceptible Staphylococcus epidermidis (MSSE; n = 98), methicillin-resistant S. epidermidis (MRSE; n = 164), Staphylococcus haemolyticus (n = 72), Staphylococcus saprophyticus (n = 28), Enterococcus faecalis (n = 206), Enterococcus faecium (n = 91), Enterococcus avium (n = 72), Streptococcus pyogenes (n = 133), Streptococcus agalactiae (n = 138), penicillin-susceptible Streptococcus pneumoniae (PSSP; n = 133), penicillin-intermediate resistant S. pneumoniae (PISP; n = 100), penicillin-resistant S. pneumoniae (PRSP; n = 29), Streptococcus milleri group (n = 135) and Peptostreptococcus spp. (n = 137). CZOP possessed comparable antibacterial activities against MSSA and MSSE to other cephems, and was also effective on MRSE but not on MRSA. An antibacterial activity of CZOP against S. saprophyticus was comparable to or higher than other cephems. CZOP, however, did not indicate an antibacterial activity against S. haemolyticus, just like other cephems. An antibacterial activity of CZOP against E. faecalis was comparable to cefpirome (CPR) and higher than other cephems. No antibacterial activity of CZOP against E. faecium and E. avium was observed, just like other drugs. An antibacterial activity of CZOP against S. pyogenes was as potent as that of cefotiam (CTM), cefepime (CFPM) and CPR, and that against S. agalactiae was also preferable. CZOP and other cephems also had a preferable antibacterial activity against S. milleri group that was most sensitive to benzylpenicillin. An antibacterial activity of CZOP against Peptostreptococcus spp. was preferable but weaker than that of cefazolin, CTM and cefmetazole. The resistance ratio estimated with breakpoint MIC of CZOP was 96.5% in MRSA, 93.1% in PRSP, 60.0% in PISP, 40.3% in S. haemolyticus, 22.3% in E. faecalis, and 15.9% in MRSE. Those resistance ratios were similar to those for CFPM, but E. faecalis showed 90.8% resistance for CFPM. The difference in the resistance ratio of E. faecalis demonstrated that CZOP successfully maintained its antibacterial activity against this species. In conclusion, no remarkable annual change in the antibacterial activities of CZOP against the Gram-positive bacteria was observed. The sensitivities of PISP and PRSP to CZOP, however, was suggested to be decreasing.

Cephalosporins↗