hr-810 and Bacterial-Infections

Topics: Bacterial Infections; Cefepime; Cefpirome; Cephalosporins; Clinical Trials as Topic; Humans; Microbial Sensitivity Tests; Streptococcus pneumoniae

Cefpirome is an injectable extended-spectrum or 'fourth generation' cephalosporin. Its antibacterial activity encompasses many of the pathogens involved in hospital-acquired infections such as Enterobacteriaceae, methicillin-susceptible Staphylococcus aureus, coagulase-negative staphylococci and viridans group streptococci. Cefpirome also has in vitro activity against Streptococcus pneumoniae regardless of penicillin susceptibility. It is stable against most plasmid- and chromosome-mediated beta-lactamases, with the exception of the extended-spectrum plasmid-mediated SHV enzymes. Intravenous cefpirome 2g twice daily has shown clinical efficacy comparable to that of ceftazidime 2g 3 times daily in the treatment of hospitalised patients with moderate to severe infections. Clinical response and bacteriological eradication rates were similar in patients with severe pneumonia or septicaemia treated with either cefpirome or ceftazidime. Cefpirome appeared more effective than ceftazidime in the eradication of bacteria in patients with febrile neutropenia in 1 study; however, clinical response rates were similar in the 2 treatment groups. The tolerability of cefpirome appears similar to that of ceftazidime and other third generation cephalosporins, diarrhoea being the most frequently observed event. Thus, cefpirome is likely to be a valuable extended-spectrum agent for the treatment of severe infections. Cefpirome offers improved coverage against some Gram-positive pathogens and Enterobacteriaceae producing class I beta-lactamases compared with the third generation cephalosporins, although this has yet to be demonstrated in clinical trials.

Topics: Animals; Bacterial Infections; Cefpirome; Cephalosporins; Fever; Humans; Neutropenia

The author reviews the comparative and non-comparative studies of cefepime and cefpirome, from which it is evident that both cephalosporins are extremely effective both clinically and bacteriologically. Success rates of about 90% have been reported for both drugs as therapy for complicated urinary tract infections, lower respiratory tract infections of the community as well as of nosocomial origin, including a large number of penicillin-resistant Streptococcus pneumoniae infections, skin and soft-tissue infections, surgical infections, as well as therapy for infections in neutropenic hosts. Cure rates are similar to or better than those obtained with ceftazidime, cefotaxime and ceftriaxone. The author also points out the various precautions necessary in utilizing these two antimicrobial agents.

Topics: Bacterial Infections; Cefepime; Cefpirome; Cephalosporins; Clinical Trials as Topic; Humans; Respiratory Tract Infections; Urinary Tract Infections

In-vitro studies with cefpirome or cefepime prove that both agents are highly active against Gram-negative bacilli and Gram-positive cocci. They possess a broader spectrum of activity than ceftazidime. In clinical trials cefpirome at doses ranging from 1 g to 2 g b.i.d. was compared to ceftazidime at a dose ranging from 1 g to 2 g b.i.d. or 2 g t.i.d. Cefepime at a dose of 2 g b.i.d. was compared to ceftazidime at a dose of 2 g t.i.d. Both cefpirome and cefepime were found to be as effective as ceftazidime in patients with septicemia. These new compounds are a valuable addition to the range of drugs available for empiric treatment of serious bacterial infections.

Topics: Bacteremia; Bacteria; Bacterial Infections; Cefepime; Cefpirome; Cephalosporins; Clinical Trials as Topic; Humans; In Vitro Techniques; Microbial Sensitivity Tests

Topics: Animals; Bacteria; Bacterial Infections; Cefpirome; Cephalosporins; Drug Resistance, Microbial; Humans; Infusions, Intravenous; Injections, Intravenous

We organized a study group to conduct a clinical trial in patients with various gynaecological infections, and we also assessed the efficacy of a single dose of cefpirome sulphate as prophylaxis after vaginal hysterectomy. Cefpirome sulphate (CROM) was administered to 100 patients with gynaecological infections and the clinical and antibacterial efficacy was evaluated in 88 patients. The improvement rate was 77.0% (67/87) and the bacterial eradication rate 67.8% (40/59). Nineteen of the 210 patients enrolled in the comparison of CROM with cefmetazole sodium (CMET) prophylaxis developed postoperative infections. The incidence of infection showed no significant difference between the CROM group (n=11, 10.6%) and the CMET group (n=8, 7.5%) (P=0.56). Although these results suggest that CROM may be effective for the treatment of gynaecological infections and has a good safety profile, it was not superior to CMET as prophylaxis in women undergoing non-laparotomy procedures at our hospital.

Topics: Adult; Aged; Antibiotic Prophylaxis; Bacterial Infections; Cefmetazole; Cefpirome; Cephalosporins; Female; Genital Diseases, Female; Humans; Middle Aged

Recent data indicate a higher level of effectivity of beta-lactam antibiotics if serum concentrations are kept above the minimal inhibitory concentration (MIC) of the pathogen. This concept would favor continuous infusion over bolus dosing. However, it is usually not the serum concentration but the free interstitial concentration in the target tissue that determines antibiotic activity. We therefore set out to measure effective drug concentrations in the interstitial space of muscle and subcutaneous adipose tissue and to compare trough levels and times above the MIC after bolus versus continuous infusion of cefpirome.. Twelve healthy volunteers received a single dose of 2 g cefpirome as an intravenous bolus or as a continuous infusion over 8 hours in a crossover design, and the resulting free interstitial tissue concentrations were measured with use of microdialysis.. After bolus injection, mean interstitial trough concentrations were 3.0 +/- 1.9 microg/mL and 2.1 +/-1.0 microg/mL for muscle and subcutaneous tissue, respectively; continuous infusion resulted in trough levels of 10.1 +/- 6.8 microg/mL and 10.1 +/- 4.6 microg/mL for muscle and subcutaneous tissue, respectively. This resulted in significantly longer times above the MIC with continuous infusion for Staphylococcus epidermidis and Enterobacter cloacae. Bacteria with an MIC < or =1 would be covered by either method, whereas higher doses seem to be necessary for Pseudomonas aeruginosa.. Although susceptible organisms will usually be covered sufficiently with standard dosing regimens, soft tissue infections with bacteria that have MIC values of 2 to 8 may profit from continuous application. Coverage of P aeruginosa, however, would be inadequate with conventional daily doses of 4 g cefpirome regardless of the method of application.

Topics: Adult; Bacterial Infections; Cefpirome; Cephalosporins; Cross-Over Studies; Humans; Infusions, Intravenous; Injections, Intravenous; Male; Microbial Sensitivity Tests; Reference Values; Tissue Distribution

Cefpirome (CPR) and amikacin (AMK) were used concomitantly to treat infections complicated by hematological diseases. A total of 100 subjects were evaluated, and the allover efficacy rate was 72.0%. Acute leukemia was found in the largest number of patient, 55, followed by 12 cases of malignant lymphoma and 6 cases of chronic myelogenous leukemia. By type of infection, patients having suspected sepsis were the largest in number, being 50, and the efficacy rate was 68.0%. The efficacy rates for sepsis and pneumonia were 57.1% (7 cases) and 61.1% (18 cases), respectively. The efficacy rates by neutrophil counts before administration of CPR and AMK and at 7 days after administration were both 71.9% in the group of less than 500/microliter, both 60.0% in the group of less than 100/microliter. The efficacy rate was 75.0% in the group of granulocyte colony stimulating factor (G-CSF) concomitant usage, and 70.0% in the non-concomitant usage group. Concomitant treatment with CPR and AMK exhibited a high level of safety and efficacy rates in infections complicated by hematological diseases and high.

Topics: Adolescent; Adult; Aged; Amikacin; Anti-Bacterial Agents; Bacterial Infections; Cefpirome; Cephalosporins; Drug Therapy, Combination; Female; Hematologic Neoplasms; Humans; Immunocompromised Host; Male; Middle Aged; Treatment Outcome

We investigated the therapeutic efficacy and safety of cefpirome sulfate (CPR) in treatment of hematopoietic disorder-associated infections. A total of 219 patients were admitted to 12 hospitals of Hanshin Study Group of hematopoietic disorders and infections between April 1994 and March 1996 and were enrolled in this study. Most patients received intravenously infused CPR at a dose of 1 or 2 g twice a day for 3 days or more. Twenty nine patients dropped out or were excluded and remaining 190 patients were adopted for the evaluation. A overall response rate was 58.4% (111/190). Among neutropenic patients, the response rate was 50% (8/16) in patients whose peripheral neutrophil counts (PNC) remained less than 100/microliter throughout the observation period and was 53.7% (22/41) in patients with PNC remained less than 500/microliter. In contrast, in patient whose PNC was below 500 before the treatment but exceeded 501/microliter during of at the end of the treatment, the response rate was as high as 78.4% (29/37). When G-CSF was combined, the response rate became significantly (P < 0.05) higher, 68.5% (50/73), as compared with that, 52.1% (61/117), in patients without it. In cases in which the causative organisms could be identified, the organisms were eliminated in 81.8% (9/11) of the patients infected with Gram-positive bacteria, whereas in 100% (12/12) in those infected with Gram-negative bacteria. Skin eruption developed in 6 patients during the treatment with CPR, and vascular pain and parosmia in one each other. These symptoms subsided soon after discontinuation or even without discontinuation of CPR. Abnormal laboratory findings, mainly liver dysfunction, i.e. elevation of slight degree of serum transaminase levels, were observed. The values, however, turned to normal immediately after the cessation or completion of the treatment. In conclusion, CPR is considered to be an antibiotic of value with high efficacy and safety in treatment of hematopoietic disorder-associated infections.

Topics: Adolescent; Adult; Aged; Aged, 80 and over; Bacterial Infections; Cefpirome; Cephalosporins; Drug Therapy, Combination; Female; Granulocyte Colony-Stimulating Factor; Hematologic Diseases; Humans; Injections, Intravenous; Male; Middle Aged; Opportunistic Infections

Twenty two patients with inflammatory respiratory tract infection were treated with cefpirome. Among the patients 14 were with severe pneumonia, 4 with exacerbated obstructive chronic purulent bronchitis and 4 with mucoviscidosis. All the patients were subjected to clinical, laboratory and x-ray examinations, electrocardiography, estimation of the external respiration and sputum bacteriological tests. The cefpirome susceptibility was determined by the agar diffusion assay with standard disks from Roussel Uclaf. Cefpirome was administered by slow intravenous infusion in a daily dose of 2 to 4 g every 12 hours depending on the disease severity. After 2 or 3 days of the patient afebrile temperature and normal differential blood count the therapy was discontinued. The favourable time course of the disease was recorded in 12 out of the 14 patients with pneumonia. Recovery and clinical improvement were stated in 64.3 and 21.4 per cent of the cases respectively. In 2 patients the treatment failed. In all the patients with exacerbated severe chronic purulent bronchitis the cefpirome therapy resulted in the disease remission. The clinical effect of the mucoviscidosis treatment was observed in 3 out of the 4 patients. The drug tolerance in the doses used was good.

Topics: Adolescent; Adult; Aged; Bacterial Infections; Bronchitis; Cefpirome; Cephalosporins; Chronic Disease; Cystic Fibrosis; Female; Humans; Male; Microbial Sensitivity Tests; Middle Aged; Pneumonia, Bacterial; Pseudomonas aeruginosa; Staphylococcus; Treatment Outcome

Twenty patients with lower respiratory tract infection were treated with cefpirome: 16 patients with pneumonia and 4 patients with chronic bronchitis which developed at the background of other diseases such as chronic somatic diseases, lung cancer, exudative pleurisy and others. The drug was administered intravenously in a dose of 1 g twice a day for 7 to 10 days. The clinical efficacy was stated in 80 per cent of the cases. In 95 per cent of the cases the drug tolerance was good. The isolates from the patients were susceptible to cefpirome in 83 per cent of the cases.

Topics: Adult; Bacterial Infections; Bronchitis; Cefpirome; Cephalosporins; Chronic Disease; Female; Humans; Male; Microbial Sensitivity Tests; Pneumonia, Bacterial; Treatment Outcome

The clinical efficacy and tolerance of cefpirome were estimated in the treatment of patients with bacterial infection of the respiratory tract. The estimate included 15 patients with acute and chronic bronchopulmonary diseases: 6 patients with acute pneumonia, 5 with exacerbated chronic purulent obstructive bronchitis and 4 with primary immune deficiency (agammaglobulinemia and acute pneumonia). Excellent and good total efficacy of the drug was stated in 6 and 8 patients respectively. In 1 patient the treatment was discontinued because of acute urticaria. Therefore, cefpirome is to be recommended as a highly efficient agent for the treatment of bronchopulmonary infection.

Topics: Acute Disease; Adolescent; Adult; Agammaglobulinemia; Bacterial Infections; Bronchitis; Cefpirome; Cephalosporins; Female; Humans; Male; Middle Aged; Pneumonia, Bacterial; Treatment Outcome

Two hundred and two isolates of gram-positive and gram-negative pathogens of urinary tract infection were tested for their susceptibility to cefpirome. In 64 to 97 per cent of the cases the susceptibility was high and exceeded that of other cephalosporins used in the treatment of urological patients. Cefpirome was used in the treatment of 26 patients with signs of urinary tract infection: 19 patients with pyelonephritis and 7 patients with prostatitis. The antibiotic was administered intravenously in a dose of 1 g twice a day for the treatment course of 5-7-10 days. The clinical and bacteriological efficacies amounted to 92 and 87 per cent respectively. The drug tolerance was good. The results demonstrated that cefpirome was useful in the empirical therapy of urinary tract infection.

Topics: Adolescent; Adult; Aged; Bacterial Infections; Cefotaxime; Cefpirome; Ceftazidime; Cephalosporins; Cephalothin; Gram-Negative Bacteria; Gram-Positive Bacteria; Humans; Microbial Sensitivity Tests; Middle Aged; Treatment Outcome; Urinary Tract Infections

From a total of 4180 patients entered in 15 phase II-III clinical trials involving cefpirome, an analysis was carried out on 378 patients with bacteriologically confirmed or suspected septicaemia who were treated with cefpirome (n = 282) or comparator drugs (ceftazidime, n = 80; ceftriaxone, n = 15; imipenem/cilastatin, n = 1). Gram-negative organisms were the causative pathogens in over half of the patients, with Escherichia coli being the most common species found. The most frequently isolated Gram-positive bacterium was Streptococcus pneumoniae. Causative organisms were eradicated in over 90% of patients receiving cefpirome or comparators. Only 4/230 pathogens tested were resistant to cefpirome in vitro. Among patients with bacteriologically confirmed septicaemia, a satisfactory clinical response was documented in 131/176 (74%) cefpirome vs 34/50 (68%) ceftazidime vs 5/10 (50%) ceftriaxone recipients, improvement in 39/176 (22%) vs 11/50 (22%) vs 5/10 (50%), and failure in 6/176 (4%) vs 5/50 (10%) vs 0/10 (0%), respectively. Similar results were achieved in patients with 'suspected' septicaemia. Cefpirome 1 or 2 g twice daily offers an effective treatment option for patients with septicaemia. The higher dosage regimen produced superior bacteriological clearance rates and is therefore preferable in patients with severe septicaemia.

Topics: Anti-Bacterial Agents; Bacteremia; Bacteria; Bacterial Infections; Cefpirome; Cephalosporins; Double-Blind Method; Humans; Microbial Sensitivity Tests; Single-Blind Method

Two hundred and seventy-six hospitalized patients with severe infection (complicated UTI, pneumonia, skin and soft tissue infection or septicaemia) were randomly allocated to receive either 1g or 2g cefpirome bd. Two hundred and seventy-four patients were evaluable for tolerance, 210 for bacteriological efficacy. The two groups were similar in terms of underlying disease, age, sex, and general condition on admission. The overall clinical and bacteriological response rates were 97/103 (94%) and 68/76 (90%) respectively in the 1g group, compared with 102/107 (95%) and 67/71 (94%) in the 2g group. There was no significant difference between the treatment groups. Eighteen adverse events, possibly or probably drug related, were reported (7 in the 1g group, 11 in the 2g group). This resulted in discontinuation of therapy in four cases (two in each group). Fourteen of the adverse events were local (five receiving 1g, nine receiving 2g), mainly phlebitis or pain at the injection site. Thirteen patients died during the study period (up to 14 days after the last dose) but in no case was death attributed to cefpirome. A review of routine laboratory parameters revealed no abnormalities which could definitely be attributed to cefpirome although in four cases a relationship was considered possible; these included two increases in serum creatinine, one increase in SGPT, and one episode of neutropenia. Cefpirome administered as 1 or 2g twice daily was a well tolerated, effective agent for the treatment of severe sepsis in hospitalized patients.

Topics: Adolescent; Adult; Aged; Aged, 80 and over; Bacterial Infections; Cefpirome; Cephalosporins; Cross Infection; Dose-Response Relationship, Drug; Drug Evaluation; Female; Humans; Infusions, Intravenous; Male; Middle Aged; Prospective Studies

Cefpirome serum concentrations were measured by microbiological assay in 30 patients after five to nine days of treatment with 1 or 2 g bd for moderate to severe infection of presumed bacterial origin. Patients with serum creatinine (SCr) greater than 220 mumol/L were excluded. The age of patients ranged from 34-86 years. Creatinine clearance (Clcr) was calculated from age, sex, weight and SCr. The range of SCr was 63-220 mumol/L and the range of Clcr was 18-169 mL/min. The correlation coefficient with cefpirome clearance was 0.464 for SCr and 0.747 for Clcr. More than half of the patients with Clcr less than 50 mL/min had SCr within the normal range of 70-150 mumol/L. Mean cefpirome clearance in patients with Clcr 18-50 mL/min was 42.7 mL/min, which is very similar to the figure of 43.5 mL/min reported in a single dose volunteer study in patients with renal failure. Mean cefpirome clearance in patients with Clcr greater than 80 mL/min was 107.6 mL/min. In conclusion, these data on cefpirome clearance obtained after multiple dose treatment of patients with presumed bacterial infection are consistent with data previously obtained from single dose volunteer studies and support the currently recommended dose regimens. Clinicians should take account of age, weight and sex when estimating renal function from SCr.

Topics: Adult; Age Factors; Aged; Bacterial Infections; Body Weight; Cefpirome; Cephalosporins; Creatinine; Female; Humans; Injections, Intravenous; Male; Metabolic Clearance Rate; Middle Aged

Laboratory and clinical studies on cefpirome (CPR, HR 810), a newly developed cephem antibiotic, were performed. The results obtained are summarized as follows: 1. Absorption and elimination of the drug were examined in a total of 7 children including 3 cases of administered with 20 mg/kg intravenous bolus injection (i.v.), 2 cases with 20 mg/kg drip infusion (d.i.v.) for 60 minutes and 2 cases with 40 mg/kg (d.i.v.) for 60 minutes. Maximum serum levels were attained immediately after i.v. or d.i.v. Cmax's were 233 +/- 7.6, 88.5 +/- 14.5, and 116 +/- 15 micrograms/ml, respectively for the above 3 modes of administration. These values were determined using a bioassay method with Bacillus subtilis ATCC 6633. T 1/2 (beta)'s were 1.18 +/- 0.17, 1.61 +/- 0.28 and 2.68 +/- 0.83 hours, respectively. Cumulative urinary recovery rates were 40.2-69.8% in a period of 0-6 hours after admissions. 2. Clinical efficacies were evaluated in a total of 20 patients with ages ranging from 9 months to 11 years. The treated cases were 6 cases of acute pneumonia, 4 cases of acute bronchitis, 4 cases of acute purulent tonsillitis, 2 cases of acute urinary tract infections, 2 cases of cellulitis, 1 case of purulent lympadenitis and 1 case of acute otitis media. The clinical efficacy rate was 94.7%. Adverse reactions occurred in no patients. Abnormal changes in laboratory test values involved only 1 case with elevated GOT and GPT. CPR was considered to be a safe and useful drug in treating various infectious diseases in children.

Topics: Bacterial Infections; Cefpirome; Cephalosporins; Child; Child, Preschool; Female; Humans; Infant; Infusions, Intravenous; Male

We carried out a randomized multi-center study comparing cefpirome (CPR) 0.5 g b.i.d. (1 g group), 1.0 g b.i.d. (2 g group) and ceftazidime (CAZ) 1.0 g b.i.d. (CAZ group) in the treatment of complicated urinary tract infections. Patients who were over 16 years old and had underlying urinary tract disease, with bacteriuria of more than 10(4) cells ml or more and pyuria of more than 5 WBCs/hpf (x 400) or more were randomly allocated to receive either 0.5 g of CPR, 1.0 g of CPR or 1.0 g of CAZ twice a day for 5 days by intravenous drip infusion. The overall clinical efficacy of the treatment was evaluated by the criteria of the Japanese UTI Committee as excellent, moderate or poor, on the basis of the changes in pyuria and bacteriuria. A total of 530 patients were treated. Of these, 141 patients in the 1 g group, 136 in the 2 g group, and 140 in the CAZ group were evaluable for clinical efficacy. No significant differences in background characteristics were observed among the treatment groups. The overall clinical efficacy rate of the 1 g group, the 2 g group and the CAZ group was 80.1%, 76.5% and 71.4%, respectively. The differences were not statistically significant. The overall bacteriological eradication rate of the 1 g group, the 2 g group and the CAZ group was 81.0%, 88.1% and 83.8%. The differences were not statistically significant either. Against the enterococcus group, however, eradication rates were higher significantly in the 1 g and 2 g groups than in the CAZ group. The incidence of adverse reactions was 2.2% in the 1 g group, 0.6% in the 2 g group and 2.9% in the CAZ group. Abnormal laboratory data after medication were observed in 10.8% of the 1 g group, 12.1% of the 2 g group and 10.2% of the CAZ group, the difference not being statistically significant. There were no serious untoward reactions to medication. From the results obtained in this study, we consider that CPR is at least as useful as CAZ in the treatment of complicated urinary tract infections.

Topics: Adolescent; Adult; Aged; Aged, 80 and over; Anti-Infective Agents, Urinary; Bacterial Infections; Cefpirome; Ceftazidime; Cephalosporins; Female; Humans; Infusions, Intravenous; Male; Middle Aged; Urinary Tract Infections

A research group was organized with the purpose of making basic and clinical studies on cefpirome sulfate (HR810, CPR), a newly developed cephalosporin antibiotic, in the pediatric field. Through meetings a joint research was done involving 19 key institutions and their related facilities throughout Japan. The obtained results are summarized as follows. 1. Antibacterial Activities Minimum inhibitory concentrations (MICs) were determined against 71 Gram-positive and 110 Gram-negative bacteria in the present clinical trials. CPR showed antibacterial activities 2-16 times higher than those of ceftazidime (CAZ) against Staphylococcus aureus and other Gram-positive bacteria including MRSA. Against Gram-negative bacteria, CPR showed a somewhat broad range of distribution in MIC against Branhamella catarrhalis, while the antibiotic inhibited the growth of all the strains of Escherichia coli and Haemophilus influenzae at concentrations no more than 0.10 and 0.20 micrograms/ml, respectively. 2. Blood Concentrations and Urinary Excretion Rates The pharmacokinetics in pediatric patients was investigated with a dose of 20 mg/kg in most cases via one shot intravenous injection or 30- and 60-minute intravenous drip infusion. Mean blood concentrations of CPR at 15 minutes after one shot intravenous injection of 10, 20, and 40 mg/kg were 51.2, 70.5, and 123.5 micrograms/ml, with half-lives of 1.21, 1.39, and 1.53 hours, respectively. Urinary excretion rates in 6 hours were 63.6, 66.0 and 71.6%, respectively for the 3 dose levels. After 30- and 60-minute intravenous drip infusions at the same dose, the pharmacokinetic parameters observed were similar to those obtained with one shot injections. 3. Concentration in the Cerebrospinal Fluid CPR penetrated well into the cerebrospinal fluid in patients with purulent meningitis and levels of 1.85-24.2 micrograms/ml 45-60 minutes were achieved after intravenous injection at a dose of 40-80 mg/kg, the penetration rate of CPR was at an intermediate degree compared with other cephalosporin antibiotics. 4. Clinical Results Clinical efficacies of CPR on infectious diseases were analyzed in 454 plus 3 cases which were complicated with other infectious diseases, hence totaling 457 cases out of 499 cases originally chosen for clinical evaluation. The remaining 45 cases were excluded from the clinical evaluation. As for the clinical efficacy, CPR was found to be effective (good or excellent) in 430 (94.1%) of the 457 cases. CPR was found

Topics: Adolescent; Age Factors; Bacteria; Bacterial Infections; Cefpirome; Cephalosporins; Child; Child, Preschool; Drug Resistance, Microbial; Humans; Infant

In this study, we evaluated the current effectiveness of 11 beta-lactam antibiotics for treatment of orofacial odontogenic infections by determining the antimicrobial susceptibility of the major pathogens. The antimicrobial susceptibilities of viridans streptococci (n = 47), Peptostreptococcus (n = 67), Porphyromonas (n = 18), Fusobacterium (n = 57), black-pigmented Prevotella (n = 59) and non-pigmented Prevotella (n = 47) isolated from pus specimens of 93 orofacial odontogenic infections to penicillin G, cefmetazole, flomoxef, cefoperazone, cefoperazone/sulbactam, ceftazidime, cefpirome, cefepime, cefoselis, imipenem and faropenem were determined using the agar dilution method. Penicillin G, most cephalosporins, imipenem and faropenem worked well against viridans streptococci, Peptostreptococcus, Porphyromonas and Fusobacterium. Penicillin G and most cephalosporins, including fourth-generation agents, were not effective against beta-lactamase-positive Prevotella, though they were effective against beta-lactamase-negative strains. Cefmetazole, cefoperazone/sulbactam, imipenem and faropenem expressed powerful antimicrobial activity against beta-lactamase-positive Prevotella. In conclusion, penicillins have the potential to be first-line agents in the treatment of orofacial odontogenic infections. Most of the other beta-lactam antibiotics, including fourth-generation cephalosporins, were not found to have greater effectiveness than penicillins. In contrast, cefmetazole, cefoperazone/sulbactam, imipenem and faropenem were found to have greater effectiveness than penicillins.

Topics: Anti-Bacterial Agents; Bacteria; Bacterial Infections; Bacteroidaceae Infections; beta-Lactams; Cefepime; Cefmetazole; Cefoperazone; Cefpirome; Ceftazidime; Ceftizoxime; Cephalosporins; Drug Resistance, Bacterial; Drug Therapy, Combination; Fusobacterium; Fusobacterium Infections; Gram-Positive Bacterial Infections; Humans; Imipenem; Lactams; Microbial Sensitivity Tests; Mouth Diseases; Penicillin G; Penicillins; Peptostreptococcus; Porphyromonas gingivalis; Prevotella; Streptococcal Infections; Streptococcus; Sulbactam

Topics: Bacterial Infections; Cefpirome; Cephalosporins; Cross Infection; Data Collection; Gram-Negative Bacteria; Gram-Positive Bacteria; Hematology; Hospital Units; Humans; Intensive Care Units; Microbial Sensitivity Tests; Netherlands; Species Specificity

Topics: Australia; Bacterial Infections; Cefpirome; Cephalosporins; Drug Resistance, Microbial; Gram-Negative Bacteria; Gram-Positive Bacteria; Hematologic Neoplasms; Hospital Units; Humans; Intensive Care Units; Microbial Sensitivity Tests

Topics: Bacterial Infections; Cefpirome; Cephalosporins; Gram-Negative Bacteria; Gram-Positive Bacteria; Humans

The preparation and biological evaluation of a series of 7-[2-(2-aminothiazol-4-yl)-2-(Z)-[(cyclopentyloxy)imino]acetamido] optically active 2-oxaisocephems, substituted at the 3-position with [(N-alkylpyridinium-4'-yl)thio]methyl groups, are described. The resulting family of parenteral compounds displays a broad spectrum of in vitro antibacterial activity. These compounds exhibit increased activity against Gram-positive organisms including methicillin-resistant Staphylococcus aureus and Enterococcus faecalis which are resistant to most cephalosporins with a similar level of Gram-negative activity to that of the third-generation antibiotics. In vivo efficacy of new antibacterial agents in this investigation is excellent against both Gram-positive and Gram-negative bacteria as compared with reference compounds. The in vitro and in vivo antimicrobial activity and the structure-activity relationships are presented.

Topics: Animals; Anti-Bacterial Agents; Bacterial Infections; Cephalosporins; Gram-Negative Bacteria; Gram-Positive Bacteria; Male; Mice; Mice, Inbred ICR; Microbial Sensitivity Tests; Stereoisomerism

Topics: Bacterial Infections; Cefepime; Cefpirome; Cephalosporins; Gram-Negative Aerobic Bacteria; Gram-Positive Bacterial Infections; Humans; Microbial Sensitivity Tests

Cefpirome (CPO) is a new parenteral cephalosporin with a wide antibacterial spectrum. In order to explore the possibility of using CPO in late pregnancy, we studied its placental transfer in vitro in a model of human placenta infusion. Mother-to-foetus in vitro transfer of CPO is high, similar to that of amoxicillin, with a placental clearance index of 0.20. A pharmacokinetic simulation based upon this result and data from literature suggests that CPO concentrations in foetal blood and amniotic fluid should be appropriate for the treatment of severe materno-foetal infections in late pregnancy. These preliminary results need to be confirmed by in vivo pharmacokinetic and clinical studies before recommending the use of CPO in late pregnancy.

Topics: Antipyrine; Bacterial Infections; Cefpirome; Cephalosporins; Female; Humans; Infant, Newborn; Maternal-Fetal Exchange; Pregnancy; Pregnancy Complications, Infectious

The in vitro activity of cefpirome against ceftazidime-resistant (MIC > 16 mg/l) isolates from two multicenter studies was analyzed. The first investigation carried out in the USA, was an in vitro comparison of cefpirome and five third-generation cephalosporins in which more than 6,000 isolates were evaluated, including 97 Enterobacteriaceae and 1,509 staphylococci resistant to ceftazidime. The second study was a multicenter international study (> 5,000 strains total) in which 160 ceftazidime-resistant gram-negative bacilli and 509 staphylococci from five countries (Australia, France, Germany, Italy and UK) were tested against cefpirome. The results from the US trial indicated that only 0.8% of enteric bacilli were resistant to cefpirome compared to 4.9% and 4.7% resistant to ceftazidime and cefoperazone, respectively. In the international trial, cefpirome was also active against ceftazidime-resistant, class I beta-lactamase producing enteric bacilli (75% susceptibility, MIC50 of 4 mg/l) especially against Citrobacter spp., Enterobacter spp. and Morganella morganii. Cefpirome was 8- to 64-fold more active than ceftazidime against seven different staphylococcal species. The antimicrobial activity of cefpirome against routine clinical isolates and those organisms resistant to third-generation cephalosporins was highly consistent within a nation (USA) and among various developed countries.

Topics: Bacterial Infections; Cefpirome; Ceftazidime; Cephalosporin Resistance; Cephalosporins; Gram-Negative Bacteria; Humans; Microbial Sensitivity Tests

A multicenter in-vitro study was conducted in 13 countries between May and November, 1992 to determine both the current bacterial epidemiology in Intensive Care and Hematology/Oncology units and the susceptibility of the organisms to cefpirome and other commonly used antibacterials. Eighty-nine hospitals each collected 100 consecutive nonduplicate aerobic clinical isolates from patients in either an Intensive Care (81%) or Hematology/Oncology (19%) unit. The major sources of isolates were respiratory, skin/wound, blood and urine. The MIC of eight different antibiotics was determined using a custom microdilution plate. Predominant bacteria accounting for 80% of the 8625 isolates included: staphylococci (26%); Escherichia coli (17%); Pseudomonas aeruginosa (12%); Klebsiella spp. (10%); Enterobacter spp. (8%) and enterococci (7%). Gram-positive isolates accounted for more than 35% of all isolates. Based on the susceptibility results to the predominant pathogens, the activity of the drugs tested could be categorized into three groups. Cefpirome and imipenem had the most potent in-vitro activity, followed by the third generation cephalosporins cefotaxime, ceftazidime and ceftriaxone, and then piperacillin. The large percentage of Gram-positive bacterial isolates in this patient population indicates the utility of antimicrobial agents that are equally effective against both Gram-positive and Gram-negative organisms.

Topics: Anti-Bacterial Agents; Bacterial Infections; Cefpirome; Cephalosporins; Cross Infection; Drug Resistance, Microbial; Europe; Gram-Negative Bacteria; Gram-Positive Bacteria; Hospital Units; Humans; Intensive Care Units; Microbial Sensitivity Tests; Prevalence

A multi-centre in-vitro study (8625 isolates) was conducted in 13 countries between May and November, 1992 to determine both the current bacterial epidemiology in intensive care and haematology/oncology units and the cross-susceptibility of the organisms to cefpirome, ceftazidime, ceftriaxone, imipenem and piperacillin. Bacterial species with 20 or more isolates resistant to one of the six antibiotics were examined for their susceptibility to the beta-lactams. Cefpirome and imipenem had the smallest total numbers of isolates. Bacteria resistant to ceftazidime or ceftriaxone were often susceptible (> 50%) to cefpirome. Conversely, cefpirome resistant isolates were frequently resistant (> 90%) to ceftazidime and ceftriaxone. P. aeruginosa was an exception, exhibiting cross-resistance to all cephalosporins. beta-lactamase producing Enterobacter, Citrobacter and Klebsiella spp. were especially resistant to piperacillin and ceftazidime but not cefpirome or imipenem. Two-thirds or more of coagulase-negative staphylococci resistant to any single agent, including imipenem, maintained their susceptibility to cefpirome. Cross-class resistance was not exhibited by imipenem and cefpirome against ciprofloxacin resistant isolates but was more evident for piperacillin, ceftazidime and ceftriaxone. Cefpirome was more active than ceftazidime against bacteria resistant to both piperacillin and gentamicin, especially coagulase-negative staphylococci (76% vs. 6%) and Enterobacter spp. (56% vs. 21%). Many coagulase-negative staphylococci and Enterobacter spp. susceptible to cefpirome (50-89%). These results suggest that cefpirome has a potential clinical advantage against gram-positive and gram-negative bacteria resistant to other beta-lactams, including imipenem.

Topics: Anti-Bacterial Agents; Bacterial Infections; Cefpirome; Ceftazidime; Ceftriaxone; Cephalosporins; Cross Infection; Drug Resistance, Microbial; Europe; Gram-Negative Bacteria; Gram-Positive Bacteria; Hospital Units; Humans; Imipenem; Intensive Care Units; Microbial Sensitivity Tests; Piperacillin; Prevalence

The antimicrobial activity of cefpirome was compared with amoxycillin/clavulanic acid, ampicillin/sulbactam, cefuroxime, ceftazidime, gentamicin and amikacin against 743 non-duplicate clinical isolates. MIC50 and MIC90 showed that the antibiotic was active against both Gram-negative and Gram-positive organisms. Cefpirome was highly active against most of the Enterobacteriaceae, including indole-positive Proteus spp., Aeromonas spp. (MIC < or = 1 mg/L) and Salmonella spp. (MIC < or = 0.5 mg/L). Neisseria gonorrhoeae and Haemophilus influenzae (including beta-lactamase producers) were all susceptible, with MIC less than 0.5 and 0.25 mg/L respectively. Cefpirome was more active than cefuroxime and ceftazidime against Campylobacter spp. (MIC < or = 2 mg/L), but less active than ceftazidime against Pseudomonas aeruginosa. Cefpirome was active against Streptococcus pneumoniae. Streptococcus bovis and coagulase-negative staphylococci (MIC < or = 0.5 mg/L) and methicillin-sensitive Staphylococcus aureus (MIC < or = 2 mg/L). Methicillin-resistant S. aureus, Gram-positive and Gram-negative anaerobes were resistant to cefpirome. The stability of cefpirome to TEM-1, TEM-2, PSE-1, SHV-1 and the chromosomal-mediated P99 and K-1 beta-lactamases was comparable to ceftazidime.

Topics: Acinetobacter; Anti-Bacterial Agents; Bacteria; Bacteria, Anaerobic; Bacterial Infections; beta-Lactamases; Cefpirome; Cephalosporins; Citrobacter; Enterobacter; Gram-Negative Aerobic Bacteria; Gram-Positive Bacteria; Methicillin Resistance; Microbial Sensitivity Tests; Staphylococcus aureus; Xanthomonas

We conducted a study on the pharmacokinetics and clinical application of cefpirome (CPR) in children. 1. A single intravenous injection of 20 mg/kg of CPR was given to a two-month-old boy, and the concentration of the drug in the blood was measured. Fifteen minutes after administration, the concentration was 53.3 micrograms/ml, and it gradually decreased thereafter, reaching a level of 5.18 micrograms/ml after 8 hours with a half-life in the plasma of 2.36 hours. 2. A single intravenous injection of 700 mg (50 mg/kg) of CPR and that of cefotaxime (CTX) were given to a girl with suppurative meningitis (3 years old, 14 kg, causative bacteria, Haemophilus influenzae), and concentrations of the drugs in plasma and cerebrospinal fluid after 1 hour were measured. On the second day of illness, the concentration of CTX in the plasma was 39.4 micrograms/ml and the concentration of desacetyl-CTX (D-CTX) was 25.2 micrograms/ml, while concentrations in the cerebrospinal fluid were 6.22 micrograms/ml (15.8%) for CTX and 3.94 micrograms/ml (15.6%) for D-CTX. On the third day of illness, concentration of CPR in the plasma was 59.3 micrograms/ml, while its concentration in the cerebrospinal fluid was 7.44 micrograms/ml (12.5%). 3. CPR was intravenously administered in daily dosages of 37.7-75.0 mg/kg in 2-3 portions for periods of 4-15 days to 2 patients with septicemia (causative bacteria, Klebsiella pneumoniae in 1 case and Escherichia coli in the other), 1 patient with bronchitis (K. pneumoniae), 9 patients with pneumonia (1 case of Staphylococcus aureus, 3 cases of H. influenzae, 2 cases of Haemophilus parainfluenzae, 1 case of K. pneumoniae + Pseudomonas cepacia, 2 cases of H. influenzae + Branhamella catarrhalis), 2 patients with cellulitis (1 case of S. aureus, 1 case, causative agent unknown), 1 patient with suppurative lymphadenitis (causative agent, unknown), 1 patient with staphylococcal scalded skin syndrome, 1 patient with renal abscess (causative agent, unknown), and 1 patient with a urinary tract infection (E. coli), for a total of 18 patients, with excellent results in 9 cases and good results in 9 cases, hence an efficacy rate of 100% was obtained. 4. As an accompanying side-effect, eruption was observed in 1 of the 18 patients, but when administration was discontinued, the symptom gradually receded, and it disappeared by the 4th day.(ABSTRACT TRUNCATED AT 400 WORDS)

Topics: Adolescent; Bacterial Infections; Cefpirome; Cephalosporins; Child; Child, Preschool; Drug Eruptions; Drug Evaluation; Eosinophilia; Female; Humans; Infant; Male; Thrombocytosis

Pharmacokinetic and clinical evaluations of cefpirome (CPR), a newly developed cephalosporin, were performed in the field of pediatrics. The results are summarized as follows. 1. Peak serum concentrations of CPR after a dose of 20 mg/kg via 30 minutes and that via 60 minutes intravenous drip infusion and a dose of 40 mg/kg via 60 minutes intravenous drip infusion were 80.8, 63.7 and 128.8 micrograms/ml, respectively, with half-lives being 1.41, 1.28 and 1.79 hours, respectively. Urinary excretion rates for CPR in the first 6 hours after administration ranged 66.7-77.1%. 2. The clinical efficacy rate in pediatric infections obtained at daily dose levels ranging 55.6-166.7 mg/kg was 95.7%. 3. The eradication rate for 22 strains identified in the study was 95.5%. 4. Side effects were found in 2 cases of diarrhea. The abnormal laboratory test results were observed in 5 cases with 7 test items (increased number of platelets; 2 cases, increased activity of GOT; 2 cases and increased activity of GPT; 1 case). According to these results, CPR was considered to be a useful antimicrobial agent in pediatric infections.

Topics: Adolescent; Age Factors; Bacterial Infections; Cefpirome; Cephalosporins; Child; Child, Preschool; Drug Evaluation; Female; Half-Life; Humans; Infant; Infusions, Intravenous; Male

Cefpirome (CPR, HR 810), a new cephem antibiotic, was investigated for its penetration into cerebrospinal fluid (CSF), and its clinical efficacy against bacterial infections. 1. CSF concentrations of CPR following intravenous injection was investigated in 2 patients with purulent meningitis. In one of them, the concentrations were 2.11 micrograms/ml and 1.31 micrograms/ml on 3 and 8 days, respectively, after start of administration. In the other patient, they were 24.2 micrograms/ml, and 1.35 micrograms/ml on 2 days and 7 days after administration, respectively. 2. Antibacterial activities of CPR against clinical isolates, Escherichia coli, Haemophilus influenzae, Staphylococcus aureus and Streptococcus pneumoniae, except those against Pseudomonas aeruginosa, were clearly superior to those of ceftazidime. 3. Clinical efficacies evaluated in 15 patients were "excellent" in 9, "good" in 5 and "unknown" in 1. The overall efficacy rate was 93.0%. 4. Clinical efficacies were "excellent" in 1 patient with bacteremia, "excellent" in 6 and "good" in one of 7 patients with pneumonia, and "good" in both of the 2 patients with purulent meningitis. Clinical efficacies against other diseases were "excellent" or "good", in 1 patient with pyothorax, 1 patient with purulent lymphadenitis, and 2 patients with facial cellulitis. In 1 patient with biliary tract infection, the results of treatment with CPR were "unknown" due to insufficient clinical data. 5. No adverse reactions were observed except in 1 patient who showed an increase in platelet count.

Topics: Adolescent; Age Factors; Bacteria; Bacterial Infections; Cefpirome; Cephalosporins; Child; Child, Preschool; Drug Evaluation; Drug Resistance, Microbial; Female; Humans; Infant; Injections, Intravenous; Male

Cefpirome (HR 810, CPR), a new cephem antibiotic, was investigated for its experimental and clinical studies in pediatrics. The results obtained are summarized as follows. 1. Plasma and urinary levels of CPR were determined in 2 children (age 5 and 7 years) after the one shot intravenous injection of the drug at 20 mg/kg. Average plasma levels of the drug were 44.7 micrograms/ml, 28.5 micrograms/ml, 10.5 micrograms/ml, 4.6 micrograms/ml and 1.5 micrograms/ml at 1/2 hour, 1 hour, 2 hours, 4 hours and 6 hours, respectively, and the average half life was 1.57 hours. Average urinary levels of the drug were 1,785 micrograms/ml, 545 micrograms/ml and 198 micrograms/ml at 0-2 hours, 2-4 hours, 4-6 hours, respectively and the average urinary elimination rate was 52.0%. The results were nearly equivalent to those in adults except for urinary elimination rate which tended to be slightly lower than that in adults. 2. Cerebrospinal fluid levels in 3 cases of purulent meningitis treated with CPR were investigated. Cerebrospinal fluid levels in a case of Neisseria meningitidis were 11.5-23.1 micrograms/ml at 1 hour and 0.94 microgram/ml at 5 hours after intravenous injection of 44.4 mg/kg, 4 times a day. Cerebrospinal fluid levels in a case of Streptococcus pneumoniae were 1.01-4.23 micrograms/ml at 1 hour after intravenous injection of 49.0 mg/kg, 6 times a day, and in the other case with Streptococcus pneumoniae, the levels were 16.8-37.1 micrograms/ml at 1 hour, 11.3 and 3.60 micrograms/ml at 3 and 4 hours after intravenous injection 52.2 mg/kg, 6 times a day. These results are not inferior to those with cefotaxime or ceftriaxone. These levels appear to be higher than MIC90 values against Escherichia coli, Streptococcus agalactiae, S. pneumoniae or Haemophilus influenzae which are the major pathogens of these diseases. 3. CPR was given to 62 patients and clinical efficacy, bacteriological response and adverse reactions were evaluated. Evaluated cases for clinical efficacy included 3 cases of purulent meningitis, 1 case of acute purulent otitis media, 2 cases of acute purulent tonsillitis, 1 case of acute bronchitis, 49 cases of acute pneumoniae, 1 case of scarlet fever, 1 case of acute osteomyelitis, 1 case of acute enterocolitis, and 2 cases of acute UTI, totalling 61 cases. Clinical efficacies were excellent in 38 cases, good in 22 cases and fair in 1 case with an efficacy rete of 98.4% (excellent + good).(ABSTRACT TRUNCATED AT 400 WORDS)

Topics: Acute Disease; Adolescent; Bacterial Infections; Bronchitis; Cefpirome; Cephalosporins; Child; Child, Preschool; Enterocolitis; Female; Humans; Infant; Male; Meningitis; Osteomyelitis; Otitis Media; Pneumonia; Scarlet Fever; Tonsillitis; Urinary Tract Infections

Cefpirome (CPR, HR 810), a new parenteral cephalosporin antibiotic, was studied for its pharmacokinetics, bacteriological and clinical effects in the field of pediatrics. 1. CPR was very active against Staphylococcus aureus, Staphylococcus epidermidis, Coagulase-negative staphylococci, Streptococcus pneumoniae among Gram-positive cocci. Antibacterial activities of CPR were also strong against Branhamella catarrhalis, Haemophilus influenzae, Escherichia coli, Salmonella sp., Klebsiella oxytoca, Enterobacter cloacae, Pseudomonas aeruginosa among Gram-negative rods. 2. The plasma concentration 15 minutes after a bolus intravenous injection of 20 mg/kg was 80.4 micrograms/ml, and the T 1/2 (beta) was 1.03 hours. Plasma concentrations after intravenous drip infusion over 30 minutes of 20 mg/kg and 25 mg/kg were 48.3 and 117 micrograms/ml at the end of infusion, and T 1/2 (beta) for these dosage were 1.14 and 1.45 hours. 3. The urinary recovery rates over 6 hours after administration were 45.2-63.9% for CPR. 4. Clinical efficacies of CPR were excellent in 31 patients and good in 30 patients with an efficacy rate of 98.4%. In bacteriological examinations, causative organisms were eradicated with an eradication rate of 95.7%. 5. As side effects, diarrhea was observed in 5 patients and loose stool in 1 patient with an incidence of 8.2%. Abnormal values were found in some patients in clinical laboratory tests for eosinophilia, thrombocytosis and an elevation of GOT, GPT and triglyceride. These findings indicate that CPR will be useful against bacterial infections in pediatrics.

Topics: Adolescent; Bacteria; Bacterial Infections; Cefpirome; Cephalosporins; Child; Child, Preschool; Drug Evaluation; Female; Humans; Infant; Male; Microbial Sensitivity Tests

A new injectable cephem antibiotic, cefpirome (CPR), was evaluated clinically in children. CPR was effective in all the 17 evaluable cases with acute bacterial infections including 1 case of purulent meningitis due to Haemophilus influenzae type b. Diarrhea and elevation of serum GOT and GPT were associated with CPR therapy in 2 young infants, although they were mild and transient. The plasma T 1/2 beta of CPR was 1.17 +/- 0.22 hours after bolus injection and mostly excreted in 6 to 8 hours into urine of children with normal renal functions. The data indicate that CPR is safe and effective, when used in children with susceptible bacterial infections.

Topics: Bacterial Infections; Cefpirome; Cephalosporins; Child; Child, Preschool; Drug Evaluation; Female; Half-Life; Humans; Infant; Male; Pneumonia, Pneumococcal

We conducted a pharmacokinetic and clinical study on cefpirome (HR 810, CPR), an aminothiazolylmethoxyiminoacetamido cephalosporin (ATOIC), and obtained the following results. 1. Concentrations in blood/excretion in urine. We studied pharmacokinetic in children upon intravenous bolus injections and 30-minute and 1-hour intravenous drip infusions in single dosages of 10, 20, and 40 mg/kg, and obtained virtually the same results as those found in adult subjects. Upon intravenous bolus injections, mean blood concentrations 30 minutes after administration of 10, 20, and 40 mg/kg were 26.1, 47.8, and 82.8 micrograms/ml, respectively, and half-lives were 1.13, 1.43, and 1.26 hours, respectively. Upon 30-minute intravenous drip infusion, mean blood concentrations on completion of the drip infusions of 10, 20, and 40 mg/kg were 43.2, 106.9, and 163.0 micrograms/ml, respectively, and half-lives were 1.15, 1.09, and 1.15 hours, respectively. In addition, upon 1-hour intravenous drip infusion, mean blood concentrations on completion of infusion were 27.1 micrograms/ml for 10 mg/kg and 47.5 micrograms/ml for 20 mg/kg, and half-lives were 1.09 and 1.40 hours, respectively. A clear dose response was observed at all dosages for either administration method. Mean excretion rates in urine in the first 8 hours after administration were 60.6-71.1% upon intravenous bolus injections of 10-40 mg/kg, and upon intravenous drip infusion, the values were 50.2-83.8% for administration of 10-40 mg/kg 6 or 7 hours after completion of drip infusion. 2. Concentrations in the cerebrospinal fluid Penetration into the cerebrospinal fluid was studied in 2 subjects, and a concentration of 0.28-5.19 micrograms/ml was observed upon administration of 50 mg/kg, a moderate degree of penetration compared to the penetration of cephalosporins of group 5 studied up to now. 3. Clinical results Evaluation of clinical effects of CPR on various types of bacterial infections was conducted in 56 subjects, excluding 3 subjects who had diseases which were excluded from the study. The breakdown was as follows: 3 cases of meningitis, 1 case of septicemia, 25 cases of bronchial pneumonia, 1 case each of tonsillitis and infection of the external acoustic meatus, 2 cases each of scarlet fever and phlegmon, 8 cases each of lymphadenitis and urinary tract infections, and 5 cases of staphylococcal scalded skin syndrome. Results of excellent or good were obtained in 54 subjects for an efficacy rate of 96.4%.(ABSTRAC

Topics: Absorption; Adolescent; Bacterial Infections; Bronchopneumonia; Cefpirome; Cephalosporins; Child; Child, Preschool; Drug Evaluation; Female; Humans; Infant; Male

Pharmacokinetics and clinical effects of cefpirome (CPR, HR 810) in children were studied. When 20 mg/kg and 40 mg/kg doses of CPR were administered to 4 children through 30 minutes' drip infusion, half-lives were 1.23 +/- 0.23 (mean +/- S.D.) hours and 1.37 +/- 0.35 (mean +/- S.D.) hours, respectively for the 2 dose levels, and recovery rates in urine in the first 6 hours after administration were 74.8% and 56.1%, respectively. CPR was administered to 15 cases (3 tonsillitis, 3 bronchitis, 5 bronchopneumonia, 1 acute cystitis, 1 coxoiliatitis, 1 otitis media, 1 otitis externa). The efficacy rate was 86.7%. Seven strains of bacteria were isolated and identified 4 Haemophilus influenzae, 3 Staphylococcus aureus, 1 Pseudomonas sp. from these cases. These bacteria in children were followed after administration of CPR. Six strains were eradicated and one was reduced in number. No adverse effects of CPR were observed except in 2 cases, one of which showed transient eosinophilia and the other showed a transient increase of transaminase. These results suggest that CPR may be an effective and safe drug to use on children clinically.

Topics: Absorption; Adolescent; Bacterial Infections; Cefpirome; Cephalosporins; Child; Child, Preschool; Drug Evaluation; Female; Haemophilus Infections; Haemophilus influenzae; Half-Life; Humans; Infant; Male; Respiratory Tract Infections; Staphylococcal Infections

Pharmacokinetic and clinical studies of cefpirome (CPR) in children were carried out, and the following results were obtained. 1. Peak serum levels were obtained at the end of drip infusion of 20.0, 17.5 and 6.8 mg/kg for 30 minutes and the half-lives were 1.93, 1.91 and 0.48 hours, respectively. 2. Urinary excretion rates in 6 hours were 40.0-96.2%. 3. Thirty-two patients including 17 with respiratory infections, 7 with urinary tract infections and 8 with skin and soft tissue infections were treated with CPR at 52.2-92 mg/kg per day by intravenous administration. Clinical effects were excellent in 12 cases, good in 13 cases, fair in 3 cases and unknown in 4 cases, and the overall efficacy rate was 89.3% (25 cases/28 cases). 4. Bacterial eradication rate was 93.8% (15 strains/16 strains). 5. Rash and diarrhea were found in 1 case each, and abnormal laboratory test values were found in 7 cases.

Topics: Adolescent; Bacterial Infections; Cefpirome; Cephalosporins; Child; Child, Preschool; Drug Evaluation; Female; Half-Life; Humans; Infant; Male; Respiratory Tract Infections; Urinary Tract Infections

This study describes the pharmacokinetic characteristics and clinical usefulness of cefpirome (CPR) in children. Mean half-lives of 20 mg/kg and 40 mg/kg of CPR injected intravenously in one shot were 1.18 and 1.34 hours, respectively, and their mean recovery rates into urine were 69.8 and 72.2%, respectively. Minimum inhibitory concentrations of CPR against Staphylococcus aureus, Streptococcus pneumoniae, Klebsiella pneumoniae, Escherichia coli and Haemophilus influenzae were the same as or lower than those of ceftazidime. CPR was clinically effective in 14/15 of patients with bacterial infections; 8/9 of pneumonia, 2/2 of bronchitis, 1/1 of pharyngitis, 1/1 of tonsillitis, 1/1 of osteomyelitis, 1/1 of urinary tract infection. No clinically overt side effects of CPR were found, while an increase of eosinophils in blood was observed in 2 cases, and an increase of platelet in blood in 1 case and an elevation of serum GPT activity in 1 case were also observed. These findings indicate that CPR is useful for the treatment of bacterial infections in children.

Topics: Adolescent; Bacteria; Bacterial Infections; Cefpirome; Cephalosporins; Child; Child, Preschool; Drug Evaluation; Female; Half-Life; Humans; Infant; Male; Microbial Sensitivity Tests; Respiratory Tract Infections

The clinical efficacy and the pharmacokinetics of cefpirome (CPR, HR 810), a new semisynthetic cephalosporin derivative, were investigated in children with various infectious diseases. CPR showed high blood peak levels, relatively long half-life and high levels in urine. Excellent clinical efficacy was obtained in 2/3 cases with pneumonia, 3/4 cases with upper respiratory infection, 2/2 cases with cutaneous and soft tissue infection and 1/1 case with urinary tract infection. The overall efficacy rate was 80%. No clinical adverse effects were observed while slightly elevated GPT and GOT, decreased platelet were detected in 4 cases without clinical problems. CPR should be an useful and safe drug in treating infectious diseases in children.

Topics: Adolescent; Bacterial Infections; Cefpirome; Cephalosporins; Child; Child, Preschool; Drug Evaluation; Female; Humans; Infant; Male; Respiratory Tract Infections; Urinary Tract Infections

Using a broth microtiter dilution method, minimum inhibitory (MIC) and minimum bactericidal concentrations (MBC) were determined for the aminothiazolyl cephalosporins cefpirome and cefotaxime against 436 blood culture isolates. At concentrations of less than or equal to 16 mg/l, cefpirome inhibited 82.3% of the isolates and cefotaxime 66.5%. At the same concentrations, cefpirome killed 60.0% of the isolates and cefotaxime 46.7%. Whereas the MIC values indicated a far better activity of cefpirome than cefotaxime against oxacillin-resistant Staphylococcus aureus, Enterococci and Pseudomonas aeruginosa, the MBC values showed a poor activity of both drugs against these strains. By comparison, cefpirome was the more active agent, covering a similar spectrum to that of cefotaxime with a slight additional activity against oxacillin-susceptible S. aureus and Staphylococcus epidermidis.

Topics: Bacterial Infections; Bacteriological Techniques; Cefotaxime; Cefpirome; Cephalosporins; Culture Media; Enterobacter; Escherichia coli; Klebsiella; Pseudomonas aeruginosa; Staphylococcus aureus

In systemic and local infections, the therapeutic efficacy of cefpirome was compared to that of imipenem and cefotaxime. Murine septicemia induced with methicillin-sensitive and methicillin-resistant Staphylococcus aureus strains responded well to cefpirome and imipenem therapy, the ED50 values ranged from 0.8 to 28.40 mg/kg and 0.5 to 15.58 mg/kg, respectively. The carbapenem also displayed high efficacy against Enterococci and was more potent than cefpirome. Cefotaxime, however, exhibited lower activity or proved to be inactive against these strains. With ED50 values of 0.03 to 31.33 mg/kg, cefpirome was the most active of the three antibiotics in protecting mice challenged with Enterobacteriaceae. The corresponding ED50 values of imipenem and cefotaxime ranged from 0.72 to 70.95 mg/kg and 0.06 to 66.30 mg/kg, respectively. Despite distinctly lower in vitro activity against the infecting organism, cefpirome showed efficacy similar to imipenem in the treatment of subcutaneous S. aureus abscesses in mice. It was more effective than imipenem and cefotaxime against experimental Klebsiella pneumonia in mice and the Escherichia coli infected granuloma pouch in rats.

Topics: Abscess; Animals; Bacterial Infections; Cefotaxime; Cefpirome; Cephalosporins; Enterobacteriaceae Infections; Escherichia coli Infections; Female; Granuloma; Imipenem; Male; Mice; Mice, Hairless; Mice, Inbred C3H; Pneumonia; Rats; Rats, Inbred Strains; Sepsis; Staphylococcal Skin Infections; Staphylococcus aureus; Streptococcal Infections

Topics: Bacteria; Bacterial Infections; Cefixime; Cefotetan; Cefpirome; Cephalosporins; Humans; Microbial Sensitivity Tests; Regression Analysis

Cefpirome (HR 810), a new semisynthetic cephalosporin derivative, was found to have a broad antibacterial spectrum against gram-positive and gram-negative bacteria. Against Staphylococcus aureus, cefpirome was more active than not only cefotaxime and ceftazidime but also cefotiam. Against gram-negative bacteria, especially, Enterobacter cloacae and Citrobacter freundii, it was also more active than the other antibiotics tested, but against Pseudomonas aeruginosa, it was less active than ceftazidime. Cefpirome was stable to hydrolysis by the common plasmid mediated beta-lactamases and was stable to the action of chromosomal cephalosporinases. But it was slightly hydrolyzed by both Rms 213 mediated penicillinase and oxyiminocephalosporinases produced by Proteus vulgaris and Pseudomonas cepacia. When cefpirome was administered subcutaneously to mice experimentally infected with Staphylococcus aureus, Escherichia coli, Klebsiella pneumoniae or Pseudomonas aeruginosa, its efficacy well reflected its in vitro potency.

Topics: Animals; Bacteria; Bacterial Infections; beta-Lactamases; Cefpirome; Cephalosporins; Drug Stability; Male; Mice; Mice, Inbred ICR; Microbial Sensitivity Tests

Therapeutic effects of intravenously administered cefpirome on experimental bacterial infections in croton oil-induced rat granuloma pouches were compared with those of ceftazidime, moxalactam, cefoperazone, and cefotaxime. Its pharmacokinetic profile in pouch exudate was also examined. Cefpirome showed bactericidal effects and long-lasting bacterial growth-inhibitory effects in granuloma pouches infected in Escherichia coli Ec-7, and its effects were almost equal to those of the other antibiotics. Against Pseudomonas aeruginosa TM-11 infection, cefpirome was more active than moxalactam, cefoperazone, and cefotaxime and comparable to ceftazidime. Cefpirome had the strongest activity against Staphylococcus aureus Smith infection among the five antibiotics, showing bactericidal effects and long-lasting bacterial growth-inhibitory effects. The level of cefpirome in pouch exudate peaked at 1 h after administration, with a value of 16.4 micrograms/ml, and declined in a pattern similar to that of ceftazidime. When compared in peak level, the exudate level of cefpirome was 1.8 to 2.6 times higher than the values of moxalactam, cefoperazone, and cefotaxime. The in vitro exudate protein binding of cefpirome was 8.8%, which was the lowest among the antibiotics used.

Topics: Animals; Bacterial Infections; Cefpirome; Cephalosporins; Croton Oil; Exudates and Transudates; Granuloma; Male; Microbial Sensitivity Tests; Protein Binding; Rats; Rats, Inbred Strains

Sixty adult patients with suspected systemic bacterial infections were treated with cefpirome 1 g or 2 g twice daily for 5-22 days. Forty-seven patients were evaluable for clinical efficacy. Diagnoses in evaluable patients were urinary tract infections (20), pneumonia (10), soft tissue infections (17), and bone and joint infections (4); four patients had two infections each. Nine patients were bacteraemic and all were cured; the responsible bacteria were Escherichia coli (6), Streptococcus pneumoniae (1), Pseudomonas aeruginosa (1), and Haemophilus influenzae (1). One patient with a soft tissue infection failed to respond clinically to cefpirome. Bacteriologically, 41 of 48 isolated pathogens (85%) were eradicated. In wound cultures, three strains of Staphylococcus aureus and one each of Ps. aeruginosa and Str. faecalis persisted. One Enterobacter sp. relapsed in urine. Of isolated strains, only Str. faecalis and methicillin resistant Staph, epidermidis were resistant to cefpirome. Staph, aureus strains were inhibited in vitro by 0.25 to 2 mg/l of cefpirome in agar dilution. Adverse effects, probably or possibly related to cefpirome, were skin reactions (3), fever (1), Clostridium difficile diarrhoea (2), and disturbed taste sensation (1). Tolerance was good. Cefpirome is suitable for large-scale comparative trials.

Topics: Adult; Aged; Aged, 80 and over; Bacterial Infections; Cefpirome; Cephalosporins; Drug Evaluation; Female; Humans; Male; Middle Aged; Pneumonia; Urinary Tract Infections

Cefpirome and six other antimicrobial agents were tested against 884 blood culture isolates from cancer patients. Cefpirome was highly active against aerobic gram-negative bacilli including Acinetobacter spp., and the Enterobacteriaceae. Only imipenem was more active than cefpirome against Pseudomonas aeruginosa. Cefpirome was also extremely active against beta-hemolytic streptococci and methicillin-susceptible staphylococci.

Topics: Anti-Bacterial Agents; Bacterial Infections; Cefpirome; Cephalosporins; Gram-Negative Bacteria; Gram-Positive Bacteria; Humans; Microbial Sensitivity Tests; Neoplasms

Topics: Bacterial Infections; Cefoperazone; Cefpirome; Cephalosporins; Humans

HR 810 or cefpirome is a new amino thiazole cephalosporin whose specific characteristic is a cyclopentenopyridinium group in position 3 of the cephem nucleus. This structure is responsible for a broad spectrum of activity, covering Enterobacteriaceae, including cephalosporinase-producing Enterobacter spp. and Citrobacter spp., Staphylococcus aureus, Pseudomonas aeruginosa and group D Streptococci.

Topics: Animals; Bacterial Infections; Cefpirome; Cephalosporins; Citrobacter; Enterobacter; Enterobacteriaceae; Enterococcus faecalis; Klebsiella Infections; Male; Mice; Microbial Sensitivity Tests; Pseudomonas aeruginosa; Pseudomonas Infections; Salmonella Infections, Animal; Salmonella typhimurium; Staphylococcal Infections; Staphylococcus aureus; Streptococcal Infections; Streptococcus pyogenes