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PubMed2003

Antimicrobial resistance in Cairo, Egypt 1999-2000: a survey of five hospitals.

Antimicrobial resistance among bacterial pathogens is a global problem, but in Egypt data are sparse. We reviewed the antimicrobial susceptibility patterns of bloodstream isolates of Gram-positive cocci and Gram-negative bacilli in five hospitals in Cairo, Egypt, from 1999 to 2000. In addition, susceptibilities of non-bloodstream isolates of Streptococcus pneumoniae and Enterococcus spp. were analysed. High rates of resistance were found in most of the bacteria studied. In the hospitals, a variety of methods were used for identification and susceptibility testing, but in the laboratories quality controlled strains were utilized routinely, to ensure accurate performance of the assays. Only 29% of Staphylococcus aureus isolates and 23% of coagulase-negative staphylococcal isolates were oxacillin susceptible. Both groups of staphylococci were also highly resistant to erythromycin, co-trimoxazole, clindamycin and doxycycline; all isolates were susceptible to vancomycin. Susceptibility of S. pneumoniae isolates to penicillin, ceftriaxone and fluoroquinolones was 63%, 84% and 82%, respectively. Vancomycin susceptibility of the enterococci was 96%; susceptibility to high-level gentamicin and streptomycin was 54% and 48%, respectively. Resistance to most relevant antimicrobials was commonplace among the Gram-negative bacilli; however, most remained susceptible to imipenem. The percentage of bloodstream isolates of Escherichia coli susceptible to common antimicrobial agents was as follows: ampicillin (6%), ampicillin-sulbactam (38%), co-trimoxazole (38%) and aminoglycosides (52%). The susceptibility of isolates of E. coli, Klebsiella and Enterobacter spp. to ceftazidime was 62%, 40% and 46%, respectively. This suggests a potentially high rate of extended-spectrum beta-lactamase (ESBL) and/or Amp-C enzyme production. These results call for a nationwide surveillance programme to monitor microbial trends and antimicrobial resistance patterns in Egypt.

Cross Infection↗
PubMed2005

Linezolid in the treatment of Gram-positive prosthetic joint infections.

OBJECTIVES: To investigate the clinical efficacy and safety of linezolid in the treatment of Gram-positive prosthetic hip and knee infections. MATERIALS AND METHODS: A retrospective evaluation of patients hospitalized in the Department of Infectious Diseases of San Martino Hospital in Genoa with the diagnosis of Gram-positive prosthetic joint infection and treated with intravenous and/or oral linezolid. Primary end points were the patient clinical outcome at the end of treatment and at long-term follow-up (up to 12 months after the end of treatment). RESULTS: Between May 1999 and September 2003, 20 patients with prosthetic joint infection were treated with linezolid. Pathogens isolated were: methicillin-resistant Staphylococcus aureus (MRSA), 14 strains; methicillin-resistant coagulase-negative staphylococci, five strains; and Enterococcus spp., one strain. The overall duration of treatment was 7.2 +/- 2 weeks (range 6-10 weeks). Patients were given intravenous therapy for 3-7 days as inpatients, then were changed as outpatients to oral therapy under weekly laboratory testing. At long-term follow-up (1 year), we observed four cases of failure due to relapsing infections. The other 16 patients treated with linezolid did not need further surgical substitution of prosthesis or surgical joint revision. Linezolid was well tolerated, and no drug-related events leading to discontinuation of treatment were recorded. CONCLUSIONS: Our data indicate that linezolid may be an effective alternative therapy for orthopaedic infections caused by Gram-positive resistant pathogens and that a prospective and comparative evaluation of linezolid in this setting is necessary.

Acetamides↗
PubMed2005

Multiple-dose pharmacokinetics of linezolid during continuous venovenous haemofiltration.

OBJECTIVES: Linezolid is a new antibacterial agent with a broad spectrum of activity against Gram-positive pathogens including methicillin-resistant Staphylococcus aureus, vancomycin-resistant Enterococcus spp., and penicillin-resistant Streptococcus pneumoniae. The aim of this prospective, single-centre, open-label, two-arm study was to investigate the pharmacokinetics of linezolid during continuous venovenous haemofiltration (CVVH) in critically ill patients and to derive a dosage recommendation. PATIENTS AND METHODS: Twenty anuric ICU patients undergoing CVVH (mean age and body weight 60.7 +/- 10.9 years and 86.0 +/- 18.0 kg) were included. All patients received linezolid 600 mg intravenously every 12 h. CVVH was performed using highly permeable polysulphone membranes (PSHF 1200, Baxter, Germany and AV 400, Fresenius, Germany). Mean blood flow rate and ultrafiltration rate were 186 +/- 15 and 40 +/- 8 mL/min, respectively. Post-dilution was performed. RESULTS: The pharmacokinetics of linezolid in critically ill patients with acute renal failure undergoing CVVH were comparable to healthy subjects and patients without renal impairment. The elimination half-life, total clearance and haemofiltration clearance were 4.3 +/- 1.7 h, 9.3 +/- 3.5 L/h and 1.9 +/- 0.8 L/h, respectively. CONCLUSIONS: Our results showed that linezolid was highly removable by CVVH. These data suggest that a schedule of 600 mg linezolid at least twice daily may also be an appropriate dosing for patients with severe Gram-positive infections undergoing CVVH with both types of membranes.

Acetamides↗
PubMed2004

The effects of supplementation of humate and probiotic on egg production and quality parameters during the late laying period in hens.

This study was designed to investigate whether inclusions of humate and probiotic into diets of hens during the late laying period increases egg production and improves egg quality. Hisex Brown layers (n = 300), 54 wk of age, were fed a control diet, 0.1% humate, 0.2% humate, 0.1% probiotic, or 0.2% probiotic for 75 d. Active ingredients of humate and probiotic were polymeric polyhydroxy acids (humic, fulvic, ulmic, and humatomelanic acids) and bacterial cultures (Lactobacillus, Bifidobacterium, Streptococcus, and Enterococcus spp.), respectively. Egg production and feed intake were measured daily, and egg weight was measured biweekly. Also, a sample of 12 eggs from each group was collected randomly to determine egg quality every 25 d. The data were analyzed as repeated measures with time as subplot. There were no effects of dietary treatments on feed intake and egg weight. Egg production for hens supplemented with humate and probiotic was not different but was greater than for control hens. Egg production increased linearly and mortality and feed conversion efficiency (weight of feed/weight of eggs) decreased linearly with increasing levels of supplemental humate and probiotic. There were no effects of treatments on egg quality. In conclusion, supplementation of humate and probiotic during the late laying period increased egg production, reduced mortality, and improved feed conversion efficiency but did not improve egg quality.

Animal Nutritional Physiological Phenomena↗
PubMed2001

Risk factors for nosocomial pneumonia in critically ill trauma patients.

OBJECTIVE: To determine risk factors for nosocomial pneumonia in critically ill trauma patients. DESIGN: Prospective cohort study. SETTING: The trauma intensive care unit (ICU) of a 1500-bed tertiary-care hospital. PATIENTS: All critically ill trauma patients (n = 103) admitted consecutively between November 1995 and October 1996. INTERVENTIONS: A comparison of data recorded at the time of ICU admission and during the clinical evolution in patients with (n = 23) and without (n = 80) nosocomial pneumonia was made. Data referred mainly to possible risk factors were recorded; they also included factors related to pneumonia etiology and evolutive factors. Predictors of nosocomial pneumonia were assessed by logistic regression analysis. MEASUREMENTS AND MAIN RESULTS: The presence of significant growth on quantitative cultures of the protected specimen brush (> or = 103 colony forming units/mL) was required to accept pneumonia as microbiologically proven, as well as the concurrence of a cohort of clinical and radiologic signs. Twenty-three (22.3%) patients developed nosocomial pneumonia. The mean age of these patients was 41.7 yrs; 18 of them (78.3%) were men. The microorganisms isolated in significant concentrations were Acinetobacter baumanii (ten cases), Staphylococcus aureus (11 cases), Pseudomonas aeruginosa (five cases), Haemophilus influenzae (two cases), and Klebsiella pneumoniae, Citrobacter freundii, Serratia marcescens, Enterococcus spp., Enterobacter spp., coagulase-negative Staphylococcus, and Streptococcus intermedius (one case each one). Risk factors for pneumonia by univariate analysis included nasogastric tube; continuous enteral feeding; prolonged mechanical ventilation (>1 day); use of H2-receptor antagonist, sucralfate, muscle relaxants, corticosteroids, barbiturates, and inotropic agents; positive end-expiratory pressure; intense sedation; re-intubation; tracheotomy; urgent brain computed tomography (CT) scan; craniotomy; iatrogenic event; and hyperventilation. The mortality rate was 43.5% (10 of 23) in the nosocomial pneumonia group and 18.8% in patients without nosocomial pneumonia (p =.02). Also, the mean stay in the ICU, the therapeutic charge (measured with total and mean punctuation of the Therapeutic Intervention Scoring System) and the complications, infectious and noninfectious, of the clinical evolution were significantly more frequent in patients with nosocomial pneumonia than in those without pneumonia (p <.05). In the multivariate analysis, continuous enteral feeding, craniotomy, prolonged mechanical ventilation (>24 hrs), use of positive end-expiratory pressure, and corticotherapy were independent predictors of nosocomial pneumonia. CONCLUSIONS: It seems that factors related to the patient's clinical course, rather than variables registered on the first days of ICU admission, are those that would exert an influence on the development of nosocomial pneumonia in critically ill trauma patients. In this way, from our point of view, in our study the main risk factors are the use of prolonged mechanical ventilation (>4 hrs) and positive end-expiratory pressure. At the same time, we can conclude that the reduction of this infection incidence could decrease the mean stay in the ICU, the therapeutic charge, and the prognosis in terms of mortality and morbidity.

Adult↗
PubMed2004

Surgical site infection in living-donor liver transplant recipients: a prospective study.

BACKGROUND: Infection is a constant threat for the living-donor liver transplantation (LDLT) recipients, although little information is available on the occurrence of infection in such patients. METHODS: One hundred and thirteen consecutive LDLT recipients were prospectively followed for the presence of surgical site infections (SSIs) defined by CDC from April 2001 to March 2002. Risk factors for SSIs were evaluated by univariate and multivariate analysis. RESULTS: Of the 113 LDLT recipients, 42 (37%) developed 57 episodes of SSIs (21 intraabdominal abscess, 20 peritonitis, 8 cholangitis, and 9 wound). Of the 57 episodes, 29 (51%) had secondary bacteremia in 19 patients. Causative pathogens, including 17 episodes of polymicrobial infections, were 37 gram-positive cocci (17 Staphylococcus aureus, 16 Enterococcus spp., and 4 others), 40 gram-negative rods (25 Enterobacteriaceae, 13 Pseudomonas aeruginosa, and 4 others), and 2 Candida albicans. Univariate analysis revealed that ABO incompatibility and repeat surgery were associated with the development of SSIs. Also, univariate analysis revealed that adult recipients, ABO incompatibility, total operation duration, repeat surgery, and NNIS risk index were associated with secondary bacteremia. Multivariate analysis revealed that ABO incompatibility (OR: 14.0; 95% CI, 2.52-77.2) and repeat surgery (OR: 9.29; 95% CI, 2.00-43.1) were independently associated with secondary bacteremia. Eleven of the 42 cases (26%) who developed SSIs died. Of these 11 cases, 5 (45%) developed secondary bacteremia within 30 days before death. CONCLUSION: SSIs occurred in 37% of LDLT recipients. ABO incompatibility and repeat surgery increased the risk of developing SSIs with secondary bacteremia, which correlated with poor prognosis.

Adolescent↗
PubMed2004

AZD2563, a novel oxazolidinone: definition of antibacterial spectrum, assessment of bactericidal potential and the impact of miscellaneous factors on activity in vitro.

AZD2563, a new oxazolidinone targeted at Gram-positive bacteria, was evaluated and compared with linezolid and other agents against 802 aerobic bacterial isolates for spectrum of activity, bactericidal activity, and the effect of miscellaneous factors upon activity in vitro. At a concentration of 2 mg/L, AZD2563 inhibited 98% of all Gram-positive bacteria tested (100% at 4 mg/L), including susceptible and resistant isolates of Staphylococcus aureus, coagulase-negative staphylococci, Enterococcus spp., Streptococcus pneumoniae, other Streptococcus spp. and Corynebacterium spp. Conversely, all Enterobacteriaceae and non-fermenting Gram-negative bacteria had MICs > 128 mg/L, and only a few Haemophilus or Moraxella spp. had MICs < 8 mg/L. By conventional laboratory definition, AZD2563 and linezolid were bacteriostatic against staphylococci and enterococci, with variable bactericidal activity against Strep. pneumoniae. The in-vitro activity of AZD2563 was essentially unaffected by altering pH, inoculum size, the type of testing medium, or the inclusion of human serum up to 25% v/v.

Bacteria↗
PubMedDate not supplied

Infectious complications after kidney transplantation: current epidemiology and associated risk factors.

BACKGROUND: The impact of newer immunosuppressive and antimicrobial prophylactic agents on the pattern of infectious complications following kidney transplantation has not been well studied. METHODS: This is an observational study in 127 adult recipients transplanted from 2001 to 2004. Patients received thymoglobulin (ATG) (50%) or basiliximab (50%) for induction and were maintained on mycophenolate mofetil, either tacrolimus (73%) or sirolimus (SRL) (27%), and prednisone (79%). Antimicrobial prophylaxis included perioperative cefazolin, trimethoprim/sulfamethaxazole for six months, valganciclovir for three months and nystatin for two months. Regression models were used to examine the association of various factors with infections. RESULTS: We observed 127 infections in 65 patients, consisting of urinary tract infection (UTI) (47%), viral infections (17%), pneumonia (8%) and surgical wound infections (7%). UTI was the most common infection in all post-transplant periods. Enterococcus spp. (33%) and Escherichia coli (21%) were the most prevalent uropathogens. Of six patients with cytomegalovirus infection, none had tissue-invasive disease. There were no cases of pneumocystis pneumonia or BK nephropathy. Six patients developed fungal infections. Two deaths due to disseminated Rhizopus and Candida albicans accounted for a 1.5% infection-related mortality. Retransplantation and ureteral stents were independently associated with UTI (OR=4.5 and 2.9, p=0.06 and 0.03, respectively), as were ATG and SRL with bacterial infections (OR=3.3 and 2.5, p=0.009 and 0.047, respectively). CONCLUSION: This study suggests that the use of newer immunosuppressive agents in recent years is associated with some changes in the epidemiology of post-transplant infections. Enterococci have become the predominant uropathogen. Invasive fungal infections, although rare, are often fatal.

Adult↗
PubMedDate not supplied

Glycopeptide resistant Staphylococcus.

Insensitivity of Staphylococcus aureus to glycopeptides became known at the end of the 1990s. To distinguish intermediate (VISA and GISA) and full resistance (vancomycin-resistant Staphylococcus aureus, VRSA) is of both epidemiological and clinical importance. The VISA (GISA) phenotype is obviously selected by glycopeptide usage in individual patients and can be disseminated by clonal spread of particularly affected staphylococcal isolates, preferentially methicillin-resistant S. aureus (MRSA). In the meantime emergence of VISA became known worldwide. VRSA evolve by acquisition of the vanA gene from enterococci, which are of significance as reservoir of resistance genes among gram-positive bacterial pathogens. Until now three independent single cases of emergence of VRSA became known from the USA, in two of them an association with vanA containing Enterococcus spp. at the same site of the affected patients could be established. The frequency of VISA (GISA) among MRSA in Central Europe is still low (<0.1%); no VRSA have been detected until now.

Animals↗
PubMed2004

Infective endocarditis in Greece: a changing profile. Epidemiological, microbiological and therapeutic data.

The epidemiology, and clinical and microbiological spectrum, of infective endocarditis (IE) in Greece was analysed in a prospective 4-year study in a tertiary hospital and a heart surgery centre in Athens. In total, 101 cases of IE (71 men, 30 women, aged 54.4 +/- 17.1 years) were studied, with a follow-up period of 3 months. Seventy-seven cases were definite and 24 possible; 59 involved native valves (native valve endocarditis; NVE), 31 prosthetic valves (prosthetic valve endocarditis; PVE), of which nine were early and 22 late, and 11 permanent pacemakers (pacemaker endocarditis; PME). There was a predominant involvement of aortic (48/101) and mitral (40/101) valves. Seven patients had rheumatic valvular disease, two had mitral valve prolapse, and eight had a previous history of IE. Thirteen and six patients had undergone dental and endoscopic procedures, respectively. In 13 patients, intravenous catheters were used within the 3 months before diagnosis of IE. There were three intravenous drug users among the patients. Staphylococcus aureus was the most important pathogen, isolated in 22% of cases, followed by viridans streptococci (19%) and coagulase-negative staphylococci (16%). Enterococcus spp. were responsible for 3%, HACEK group for 2%, and fungi for 6% of cases. Viridans streptococci were the leading cause of NVE (29%), Staphylococcus epidermidis of PVE (16%), and S. aureus of PME (54.5%). Six of 22 S. aureus and ten of 16 S. epidermidis isolates were methicillin-resistant. Surgical intervention, including total pacemaker removal, was performed in 51.5% of patients. Overall mortality was 16%, but was 29% with PVE, and was significantly higher with medical than with combined surgical and medical therapy (24.5% vs. 8%). Compared with previous studies, there were changing trends in the epidemiology, microbiology, treatment and prognosis of IE in Greece.

Adolescent↗
PubMed2006

Treatment of acute post-surgical infection of joint arthroplasty.

The best antibiotic regimen for acute prosthetic joint infection, treated without removal of the implant, has not been well-defined. This study describes the use of a protocol based on oral rifampicin combinations to treat 47 cases that were followed prospectively for a 2-year period. The regimen used most commonly was levofloxacin 500 mg/24 h plus rifampicin 600 mg/24 h for a mean duration of 2.7 +/- 1 months. The cure rate was 76.9%, and the only independent risk-factor associated with treatment failure was infection caused by methicillin-resistant Staphylococcus aureus or Enterococcus spp. (OR 17.6, p 0.003). Overall, the results suggested that use of oral antibiotics, including rifampicin, for 2-3 months was a good treatment option.

Acute Disease↗
PubMed1991

[Bacteriological studies on pharyngeal and tracheal colonization in patients of operations and patients in ICU].

Bacterial colonization of the pharynx before and one week after operation, and contamination of the trachea during intubation in 7 patients who underwent operations were investigated. And bacterial colonization of pharynx, tracheas, and mechanical-ventilators in 7 ICU patients was investigated. Flora of palms of 10 ICU personnel was also examined: 1) Oral bacteria began to be found in the trachea several hours after intubation. 2) In oropharyngeal flora, one week after operation, Neisseria and anaerobes which belong to normal flora decreased because of antibiotics, but no new resistant bacteria appeared. 3) Although isolates from pharynx of preoperative patients were normal flora, those of ICU patients were Staphylococcus epidermidis, Enterococcus spp., gram-negative rods such as Pseudomonas aeruginosa, and yeast liked organisms etc, which were resistant to antibiotics. 4) From the trachea of intubated patients in ICU, oral bacteria were isolated. 5) Pseudomonas pickettii was isolated from the expiratory side of ventilator circuits in one patient, but it was not isolated from the patient. 6) From hands of ICU personnel, gram-positive bacteria such as coagulase negative staphylococci, Coryne bacterium spp. and Bacillus spp. were isolated. 7) One patient in ICU, who developed pneumonia due to resistant Bacteroides fragilis following oropharyngeal colonization, was reported. These studies suggested the importance of environmental control, careful selection of antibiotics, and attention to change of flora.

Aged↗
PubMed1978

Diffusion disk susceptibility testing with cefaclor.

The reliability of the standardized 30-mug cephalothin disk and that of an experimental 30-mug cefaclor disk in predicting probable clinical susceptibility to cefaclor were compared. Quantitative determinations of cefaclor susceptibility were measured by the World Health Organization International Collaborative Study agar dilution procedure; diffusion disk tests were performed by the standardized U.S. Food and Drug Administration disk test. The cephalothin disk erred in predicting probable susceptibility in 52% of isolates of Enterococcus spp. resistant to 16 mug or less of cefaclor per ml; the cefaclor disk did not. The cephalothin disk erred in correctly predicting susceptibility in only 20% of cefaclor-susceptible isolates of Enterobacter spp.; the cefaclor disk correctly predicted susceptibility for 70%. These results indicate the need for further evaluation of a separate cefaclor disk for use in susceptibility testing with this new cephalosporin.

Cephalosporins↗
PubMed1988

In vitro and in vivo antibacterial activities of T-3262, a new fluoroquinolone.

T-3262, a new fluoroquinolone, showed a broad spectrum of activity against gram-positive and gram-negative bacteria. T-3262 had most potent activity against gram-positive cocci, such as Staphylococcus, Streptococcus, and Enterococcus spp. The MICs of T-3262 for 90% of strains tested were between 0.05 and 1.56 micrograms/ml. Against members of the family Enterobacteriaceae and Pseudomonas aeruginosa, the activities of T-3262 were almost equal to those of ciprofloxacin. Obligate anaerobes were also susceptible to T-3262. T-3262 was bactericidal for one strain each of Staphylococcus aureus, Escherichia coli, and P. aeruginosa at concentrations near its MIC; and fluoroquinolones, including T-3262, inhibited DNA gyrase activity at low concentrations. The 50% effective dose of T-3262 after oral administration against systemic infections with S. aureus in mice was about 6 times lower than that of ofloxacin and about 20 times lower than that of norfloxacin.

Animals↗
PubMed1991

Ofloxacin versus parenteral therapy for chronic osteomyelitis.

We conducted a randomized comparison of oral ofloxacin (400 mg twice a day) and parenteral agents (cefazolin, 1.0 g intravenously every 8 h, or ceftazidime, 2.0 g intravenously every 12 h) in biopsy-confirmed, nonprosthesis osteomyelitis. A total of 19 subjects received ofloxacin for an average of 8 weeks, and 14 received parenteral antibiotics for an average of 4 weeks; both therapies were well tolerated. Infections were due to Staphylococcus aureus (40%), Enterococcus spp. (3%), Pseudomonas aeruginosa (15%), and other gram-negative organisms (42%). At the completion of therapy, one P. aeruginosa infection in the ofloxacin group persisted and the organism acquired resistance, accompanied by a resistant Acinetobacter superinfection. In the parenteral group, one S. aureus infection persisted, and there was a resolved superinfection due to S. aureus as well. Eighteen-month follow-up data have been obtained. Among those treated with ofloxacin, four subjects whose initial response to therapy was successful suffered relapses of infection, three due to S. aureus and one due to P. aeruginosa, while in the parenteral group, one subject with a P. aeruginosa infection relapsed. Long-term response to therapy was successful for 14 of 19 (74%) subjects who received ofloxacin and 12 of 14 (86%) who received parenteral antibiotics; the difference was not significant. Oral ofloxacin appears comparable to parenteral antibiotics in chronic osteomyelitis due to susceptible organisms, and oral ofloxacin offers advantages in economics and convenience.

Administration, Oral↗
PubMed1993

In vitro and in vivo antibacterial activities of E-4868, a new fluoroquinolone with a 7-azetidin ring substituent.

E-4868, (-)-7-[3-(R)-amino-2-(S)-methyl-1-azetidinyl]-1-(2,4- difluorophenyl)-1,4-dihydro-6-fluoro-4-oxo-3-quinolinecarboxylic acid, is a new fluoroquinolone with an azetidine moiety at the 7 position. The in vitro activity of E-4868 has been compared with those of ciprofloxacin, ofloxacin, and fleroxacin, while the activity of ciprofloxacin was used as reference for in vivo studies. The MICs of E-4868 for 90% of the isolates tested (MIC90s) were 0.06 to 0.5 microgram/ml against gram-positive organisms, including Staphylococcus, Streptococcus, and Enterococcus spp. In general, the in vitro potency of E-4868 against gram-positive bacteria was higher than those of all of the other fluoroquinolones tested. MIC90s against members of the family Enterobacteriaceae between 0.03 and 1 microgram/ml were observed, with the exception of those against Serratia marcescens and Providencia spp., and a MIC90 of 2 micrograms/ml against Pseudomonas aeruginosa was obtained. E-4868 inhibited 90% of the Clostridium spp. and Bacteroides spp. at 2 micrograms/ml and was twofold more active than ciprofloxacin. An increase in the Mg2+ concentration from 1 to 10 mM increased the MIC between two and three times. Human urine caused a significant decrease in activity of E-4868, which was more pronounced at pH 5.5 than at pH 7.2. The presence of serum also decreased the activity of E-4868. Fifty percent effective dose (ED50) values against experimental Escherichia coli HM-42 infections in mice were 3.9 mg/kg of body weight with E-4868 and 3.5 mg/kg of body weight with ciprofloxacin. Corresponding ED50 values against P. aeruginosa HS-116 were 93.2 and 107.8 mg/kg, respectively, and those against Staphylococcus aureus HS-93 were 6.5 and 44.6 mg/kg, respectively. In experimental infections with Streptococcus pneumoniae 84551, the ED50 value of E-4868 was 154.4 mg/kg, while ciprofloxacin proved totally inactive at a dose of 400 mg/kg. When E-4868 was administered orally at a dose of 50 mg/kg in mice, the area under the concentration-time curve (0 to 4 h) value was 28.4 microgram . h/ml, while an area under the concentration-time curve value of 2.3 microgram . h/ml was observed for ciprofloxacin at the same dose. In these studies, levels of the two agents in blood 1 h postadministration were 7.6 and 1.2 microgram/ml, respectively.

Animals↗
PubMed1995

In vitro evaluation of DV-7751a, a new fluoroquinolone with an enhanced spectrum of activity against gram-positive aerobic organisms and anaerobes.

DV-7751a is an investigational fluoroquinolone with improved spectrum and potency against gram-positive bacteria. We studied the in vitro activity of this compound against 771 recent clinical isolates by the reference agar and broth microdilution methods. Its activity was compared with those of ciprofloxacin, levofloxacin, and ofloxacin and with those of ceftazidime, oxacillin, and gentamicin where relevant. DV-7751a was four- to eightfold more active than the comparison fluoroquinolones against Enterococcus spp. (including vancomycin-resistant strains), Staphylococcus spp. (including oxacillin-resistant Staphylococcus aureus), Streptococcus spp., other gram-positive pathogens, and some anaerobes. The DV-7751a activity against most gram-negative species was similar to that of ofloxacin and ciprofloxacin. DV-7751a appears to be a candidate for the therapy of some mixed-flora infections and the treatment of bacteria resistant to the current fluoroquinolones.

Anti-Infective Agents↗
PubMed1990

Plasmid-associated bacteriocin production by a strain of Carnobacterium piscicola from meat.

Carnobacterium piscicola LV17 isolated from vacuum-packed meat produces bacteriocin(s) that is active against closely related lactic acid bacteria, Enterococcus spp., and a strain of Listeria monocytogenes but not against gram-negative bacteria. The bacteriocin has a bactericidal mode of action, is heat resistant, and is stable over a wide range of pH but is inactivated by proteolytic enzymes. Sensitive and resistant cells were shown to adsorb the bacteriocin, but cell death depended on contact of the bacteriocin with the cell membrane. Bacteriocin production is detected early in the growth cycle of the organism in APT broth, but it is not produced in APT broth adjusted to pH 5.5. Bacteriocin production and resistance to the bacteriocin produced are associated with two plasmids of 40 and 49 megadaltons. The possibility that two bacteriocins are produced is indicated because the inhibitory substances of the mutant strains containing either the 40- or 49-megadalton plasmids have different antimicrobial spectra.

Bacteriocins↗