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PubMedDate not supplied

Interference of new penicillins and cephalosporins with urine glucose monitoring tests.

The possibility that three new penicillins (mezlocillin, pipericillin, and azlocillin) and two new cephalosporins (ceftazidime and cefoperazone) might give false positive urine glucose testing results was studied. High and low concentrations of antibiotics were dissolved in urine and tested with Clinitest (Ames Division, Miles Laboratories, Elkhart, Indiana) and Tes-Tape (Eli Lilly and Company, Indianapolis, Indiana) at four different concentrations of glucose. None of the antibiotics interfered with the accuracy of Tes-Tape readings. All antibiotics interfered with Clinitest readings; the greatest interference was noted at high concentrations of antibiotics and low concentrations of glucose, and with the two cephalosporins. A summary of all reported cephalosporin interactions with Clinitest urine glucose testing is included.

Azlocillin↗
PubMed1979

[Antibacterial activity of mezlocillin and azlocillin/A survey (author's transl)].

A review of the antibacterial activity of 6-[(R)-2-[3-methylsulfonyl-2-oxo-imidazolidine-carboxamido]-2-phenyl-acetamido]-penicillanic acid sodium salt (mezlocillin, Baypen) and 6-[(R)-2-(2-oxo-imidazolidine-1-carboxamido)-2-phenyl-acetamido]-penicillanic acid sodium salt (azlocillin, Securopen) is given on the basis of extensive in vitro studies. The action of each of the preparations is compared with that of important antibiotics of other substance classes from the group of penicillins and cephalosporins.

Azlocillin↗
PubMed1992

[Experiences with triple antibiotic combination in neonatal infection].

BACKGROUND: In-vitro and clinical efficacy of a combination therapy consisting of 3 antibiotic agents was to be assessed in neonatal septicemia. METHODS: From 1980 to 1987, 152 newborns with septicemia as proven by blood culture were treated with an initial antibiotic regimen consisting of azlocillin (150 mg/kg bw), cefotaxime (100 mg/kg bw), and tobramycin (5 mg/kg bw). RESULTS: According to the microbiologic testing, antimicrobic therapy was effective in each of the 152 organisms: 101/152 bacteria were susceptible to all 3 agents; resistance to 1 or 2 of the antibiotics was evident in 33/152 and in 18/152 organisms, respectively. Mortality due to septicemia was 7.2%. CONCLUSION: As no difference was observed in the frequency in which one of the three antibiotic substances was the only effective drug, each of the 3 agents seemed to be necessary for clinical effectiveness of this antibiotic combination.

Azlocillin↗
PubMed1991

[Chemotherapy of Pseudomonas aeruginosa infections in children during the first three months of life].

The data on the efficacy of antibacterial drugs and their combinations in treatment of 150 three-month old infants with generalized infection due to Pseudomonas aeruginosa are presented. The clinical isolates of P. aeruginosa were found to be carriers of multiple drug resistance which markedly complicated the chemotherapy. Only combined antibacterial therapy of such infants proved to be rational. High activity of aminoglycosides, azlocillin and cefotaxime against P. aeruginosa and the synergistic action of their combinations observed in the patients permitted to recommend the use of combinations of the above drugs in the empirical chemotherapy.

Aminoglycosides↗
PubMed1990

Interactions of antimicrobial combinations in vitro: the relativity of synergism.

Interactions of combinations of netilmicin, amikacin, piperacillin, imipenem, azlocillin, ceftazidime or moxalactam were studied in vitro against Pseudomonas aeruginosa, Escherichia coli, Klebsiella pneumoniae and Staphylococcus aureus. Microtiter checkerboard technique was compared with standard killing curve method and with killing curves obtained in kinetic in vitro models mimicking single or multiple dosing regimens according to human pharmacokinetics. Antibiotic combinations were classified as antagonistic, indifferent or synergistic. Disagreement between classification by checkerboard and by kinetic model was found in 14 of 33 combinations studied (42%). Further analysis by standard killing curve method demonstrated that synergism or antagonism is a relative, not an absolute feature of drug combinations against given pathogens. Factors contributing to disagreements included the concentrations studied relative to the bacterial sensitivity, the ratio of concentrations of the two drugs tested, the size of the bacterial inoculum and the endpoint of the interaction assessment. Standard in vitro methods do not consider changes of antibiotic concentrations over time during combination therapy. Concentrations studied are defined according to bacterial sensitivity (fractions of MIC). Therefore, they may or may not relate to those at the infected site. The observed discrepancies between standard methods for testing drug interaction and a model which more closely reflects human pharmacokinetics support the argument that standard synergy testing provides incomplete data to reliably design clinical combination therapy.

Amikacin↗
PubMedDate not supplied

[Perioperative antimicrobial prophylaxis in Obwegeser-Dal Pont surgery for prognathism].

The value of ultra short antimicrobial prophylaxis using azlocillin in preventing postoperative wound infections was studied in a prospective clinical/bacteriological study in 41 orthognathic operations. Preoperatively the oral mucosa and pharyngeal flora of each patient was subjected to bacteriological identification with particular emphasis on anaerobes and sensitivity tests for organisms with established pathogenic potential. The results of a bacteriological examination of the redon drains on day 1 postoperatively indicated a contamination of the surgical wound. Clinically 31 patients showed moderate postoperative edema of the buccal soft tissues and 10 patients had hematomas or hemorrhages. In all patients the operation was followed by primary intraoral wound healing without any signs of an early infection.

Adult↗
PubMed1989

[Combined chemotherapy of experimental infection in neutropenia].

A significant decrease in resistance to infections caused by gramnegative pathogens was observed in mice with neutropenia induced by cytostatics. Efficacy of schemes for combined chemotherapy with beta-lactams, aminoglycosides and a novel peptide antibiotic was studied on model infections in mice with neutropenia. In the neutropenic mice with sepsis caused by Pseudomonas the peptide antibiotic administered parenterally in a single dose of 50 micrograms/kg provided high therapeutic activity. In combination with azlocillin, cefotaxime and amikacin the peptide antibiotic has a synergistic therapeutic action.

Agranulocytosis↗
PubMed1986

In vitro activity of ciprofloxacin compared with other agents against recent hospital isolates.

Ciprofloxacin's in vitro activity was tested against 385 hospital isolates originating from three geographically distinct regions. Of all strains tested, only three (1 Acinetobacter sp. and 2 Pseudomonas aeruginosa) were ciprofloxacin resistant. Ciprofloxacin was more active against Escherichia coli, Enterobacter cloacae, Enterobacter aerogenes, Acinetobacter sp., Proteus sp., Shigella sp. than gentamicin, mezlocillin and cefotaxime. It was more active than azlocillin and cefsulodin against P. aeruginosa. It was more active than cloxacillin and cefamandole against staphylococci. It was as active as cefotaxime against Klebsiella pneumoniae, Citrobacter freundii and Serratia marcescens. Ciprofloxacin demonstrated similar activity in broth and solid agar. The minimal inhibitory concentrations (MIC's) of all strains were similar to the minimal bactericidal concentrations (MBC's). Ciprofloxacin's MIC was not influenced by increase of the inoculum or addition of human serum and only slightly influenced by anaerobic conditions. Decrease of the medium pH increased the MIC substantially. Ciprofloxacin exhibited a rapid bactericidal effect and had only a minimal post-antibiotic effect. These favorable in vitro characteristics of ciprofloxacin warrant further studies.

Acinetobacter↗
PubMed1985

Assessment of the in vitro and in vivo activity of ciprofloxacin measured against current standards of therapy.

The bactericidal activity of ciprofloxacin in active human serum was investigated using serum-resistant Escherichia coli C14 and Pseudomonas aeruginosa 220 as test organisms. In 100% or 80% human serum the growth rate of E. coli C14 was lower than in broth. This also influenced the killing rate of ciprofloxacin. Ciprofloxacin was more active in serum than norfloxacin or ofloxacin and killed Pseudomonas aeruginosa 220 much more rapidly than azlocillin or tobramycin. Rapid killing was also observed in vivo in the blood of intraperitoneally infected mice, ciprofloxacin being superior to norfloxacin, ofloxacin and sisomicin. In mouse protection studies with E. coli Neumann as infecting organism, the dose-effect ratio showed that, despite extremely low blood concentrations, ciprofloxacin had a full therapeutic effect at a dose of 2.5 mg/kg p.o. or less than or equal to 0.5 mg/kg s.c., whereas cefotaxime, despite similar low MIC values in vitro, had to be administered at a dose of 20 mg/kg s.c. in order to achieve 100% survival. These data indicate that ciprofloxacin is effective at low concentrations both in vitro and in vivo.

Ampicillin↗
PubMed1986

[In vitro effect of piperacillin on aerobic bacteria. Variations according to the phenotypes of resistance to beta-lactam antibiotics].

In a first study the MICs of piperacillin (PIP), mezlocillin (MEZ), azlocillin (AZL), carbenicillin (CARB) and ticarcillin (TIC) against 563 strains of aerobic bacteria were compared. The MIC50 of PIP against E. coli and P. mirabilis was 0.5 to 1 mg/l, that is equal to those of MEZ and TIC but 2 or 3 times lower than those of AZL and CAR. The MIC50 of PIP and MEZ against Klebsiella, a species that is naturally resistant to TIC and CAR, was 4 mg/l. Enterobacter, Serratia and Citrobacter showed two populations of strains: the first was sensitive to the five penicillins tested (MIC50 of PIP: 1 to 2 mg/l); the second was resistant to all of them. PIP and AZL were more active (MIC50 8 mg/l) against Ps. aeruginosa than MEZ, TIC and CAR. All five penicillins had limited activity against Acinetobacter (MIC50 less than 16 mg/l). PIP, MEZ and AZL were more active than TIC and CAR against enterococci. In a second study, the activity of PIP was evaluated by standard sensitivity tests on 4993 strains of enterobacteria, Ps. aeruginosa and Acinetobacter classified according to their phenotype of resistance to beta-lactam antibiotics. PIP was regularly active against enterobacteria and Ps. aeruginosa strains devoid of acquired resistance. The activity of PIP was significantly reduced against enterobacteria strains with a phenotype suggesting induced penicillinase production. However, the inhibition zone diameters, although reduced, remained within what is now considered the sensitivity range (notably with E. coli and Proteus spp), which raises the problem of in vitro tests interpretation. PIP was active against E. coli strains with a "cephalosporinase" phenotype, but inactive against cefotaxime resistant strains of: Enterobacter, Citrobacter and Serratia. The activity of PIP on CAR-resistant Ps. aeruginosa strains was significantly reduced, but the inhibition zone diameter in one quarter of them was still within limits of sensitivity.

Azlocillin↗
PubMed1986

Transferable resistance to cephalosporins, ureidopenicillins and trimethoprim.

Transferable resistance to classical Cephalosporins emerged three years ago among Enterobacteriaceae simultaneously in several hospitals and was associated with resistance to other betalactam drugs, i.e. with a transmissible TEM-like betalactamase. A systematic survey of incidence of R plasmids in Proteus sp. lead, in two district PHLs, to demonstration of transferable Azlocillin resistance. This resistance was most frequently associated with that for Carbenicillin, but also strains susceptible to CAR but resistant to AZL have been isolated. Trimethoprim resistance was in this country first described by Schŏn, but, since then, it is now frequently found transferable in polyresistant strains from hospitals, resistant also to betalactam antibiotics, Gentamicin and other drugs.

Azlocillin↗
PubMed1985

Potential of moxalactam and other new antimicrobial agents for bilirubin-albumin displacement in neonates.

The effects of several novel antibiotics on in vitro binding of bilirubin to human serum albumin were investigated. At physiologic bilirubin-albumin ratios and pH values, aztreonam, imipenem, azlocillin, enoxacin and ciprofloxacin did not compete with bilirubin at drug concentrations less than 900 micrograms/mL. Cefoperazone caused an apparent increase in unbound bilirubin only at concentrations greater than 35 microM (330 micrograms/mL). Moxalactam, however, caused a linear increase in unbound bilirubin, greater than that seen with sulfisoxazole, over the entire range of antibiotic concentrations. These results may have implications for the use of these newer antimicrobial agents in neonatal infections.

Anti-Bacterial Agents↗
PubMed1987

[Comparative activity of ticarcillin-clavulanic acid and various beta-lactams against Pseudomonas maltophilia].

An increase is observed in the isolation of P. maltophilia as a casual agent of nosocomial infection, particularly in hospitalized immunocompromised patients. These infections are associated with the acute problem of their treatment as most of the P. maltophilia strains are generally resistant to many of the commonly used antimicrobial agents, including those active against Pseudomonas aeruginosa: beta lactams, aminoglycosides and imipenem. This resistance is correlated with two inducible beta lactamases (L1, pI = 6.9; L2, pI = 8.4). Azlocillin, piperacillin, cefoperazone, ceftazidime, latamoxef, ticarcillin, ticarcillin and clavulanic acid in combination were tested against 93 P. maltophilia isolates by disk diffusion testing and agar dilution technique. The association of clavulanic acid with ticarcillin resulted in better MIC values for ticarcillin (MIC 50 = 32, MIC 90 = 128). 96% of strains were sensible to the breakpoint of 128 mg/l. Other beta lactam antibiotics showed a loss of activity except for latamoxef (67% of strains susceptible to 4 mg/l) which is a potent inhibitor of both beta-lactamases. According to these results, the combination of clavulanic acid with ticarcillin may be useful in the treatment of P. maltophilia acquired hospital infections.

Anti-Bacterial Agents↗
PubMed1986

[In vitro model for the study of the concentration kinetics of antibiotic combinations and their antibacterial activity].

The concentration kinetics of combinations of antibiotics similar to those taking place after i.v. administration was simulated in an in vitro model taking into account the different half-life periods of the antibiotics. A hose pump was used for continuous supply of sterile nutrient to a liquid bacterial culture containing both antibiotics in a preselected concentration and for removal of fluid from the system at an identical flow rate. To account for the different half-life periods of the antibiotics, a solution containing the antibiotic having a longer half-life in a corresponding concentration was continuously added by pumping. Samples were taken at fixed intervals to determine bacterial counts and check the expected concentrations of active substance did not contain antibiotics. This model has been developed to enable a determination of the dynamic relationship between the course of concentrations of antibiotics and their antibacterial activity. To permit a statement on the synergistic, indifferent or antagonistic activity of the combination, in analogy to the FIC indices in the checkerboard technique, the relative reduction of the bacterial count by the combination as compared to the individual components at time t was calculated. The model has been demonstrated by the example of the combined action of azlocillin and gentamicin against a strain of Klebsiella pneumoniae. In a simple way, the model permits any increase in the number of combination partners having different half-life periods. The mathematical development of the model is explained in detail.

Anti-Bacterial Agents↗
PubMed1987

Ciprofloxacin: comparative data in cystic fibrosis.

Ciprofloxacin, a 4-quinolone bactericidal antimicrobial, has a high activity against a broad spectrum of bacterial microorganisms, including Pseudomonas aeruginosa. The fact that ciprofloxacin can be administered orally would represent a cost-efficient advance in the management of patients with cystic fibrosis, most of whom must be treated frequently with anti-pseudomonal antibiotics. In this study, 11 adult patients received 26 therapeutic courses of ciprofloxacin at a dose of 750 mg orally every 12 hours. In addition, a 13-year-old patient received 500 mg orally every 12 hours. The length of therapy was usually two weeks, but some patients received treatment for up to eight weeks. The mean serum concentration at two to three hours after administration of a dose was 3.68 micrograms/ml (range, 1.85 to 7.25 micrograms/ml). The mean trough level was 0.85 microgram/ml (range, 0.36 to 1.65 micrograms/ml). A comparable group of 11 patients matched by age and severity of disease were treated with conventional doses of tobramycin and azlocillin administered intravenously for at least two weeks. Sputum cultures from all the patients grew P. aeruginosa, except for one patient with Pseudomonas cepacia infection; the minimal inhibitory concentration of ciprofloxacin for these organisms ranged from 0.05 to 1.56 micrograms/ml. The clinical and microbiologic results obtained with these two antimicrobial regimens were similar. A therapeutic failure was noted in the patient infected with P. cepacia whose organism became resistant after one week of therapy (minimal inhibitory concentration greater than 4.58 micrograms/ml). Emergence of resistant strains was not observed in any of the other patients.

Adolescent↗
PubMed1987

Ciprofloxacin therapy in cystic fibrosis.

There is great need for an oral agent that could be used to treat pulmonary exacerbations in patients with cystic fibrosis. In this study, the use of oral ciprofloxacin as sole therapy was evaluated in 18 patients with 39 infectious episodes; 13 episodes were classified as severe, 19 were classified as moderate, and seven were classified as mild. Patients ranged in age from eight to 36 years (mean, 23 years). Dosage varied according to severity of disease, body size, and the susceptibility of the Pseudomonas isolate to ciprofloxacin; the dose ranged from 750 to 2,250 mg daily (mean, 1,800 mg). Ten patients received one course of ciprofloxacin, and eight received repeated courses. The overall clinical response rate was 82 percent. There was a response to the initial treatment course in 96 percent of the patients. Those in whom therapy failed had been re-treated with ciprofloxacin and were severely ill. Failure to respond correlated poorly with pretreatment minimal inhibitory concentration (MIC) values (0.6 microgram/ml for failures versus 0.4 microgram/ml for responses). Pseudomonas could not be eradicated from the sputum of any of the patients, although there was a marked reduction in purulence and bacterial counts. In general, patients who did not require re-treatment for three months would again have susceptible organisms. When organisms became resistant to ciprofloxacin (MIC greater than 2 micrograms/ml), they showed no concomitant new aminoglycoside or beta-lactam resistance. No serious toxicity occurred in any of the 39 episodes of treatment. In seven patients treated with combination therapy (tobramycin or azlocillin), the infecting organisms were reduced in number, but eradication of Pseudomonas generally could not be achieved. Increases in MIC occurred during combination therapy. Ciprofloxacin is a major advance in the treatment of bronchopulmonary infection in patients with cystic fibrosis.

Adolescent↗
PubMed1979

[Mezlocillin concentrations in human bone tissue].

20 patients undergoing extended hip surgery received a single i.v. injection of 2 g 6-[(R)-2-[3-methylsulfonyl-2-oxo-imidazolidine-1-carboxamido]-2-phenyl-acetamido]-penicillanic acid sodium salt (mezlocillin, Baypen). At different times after the infections but simultaneously 31 samples of blood and bone (spongiosa) were collected for determination of mezlocillin concentrations. On an average, maximum concentrations of approximately 20 microgram/g bone were demonstrated 30 min after injection, these being within the clinico-therapeutical range. The concentration of azlocillin--another acylureido-penicillin--was comparatively higher.

Adolescent↗
PubMed1984

[Development and current status of Pseudomonas aeruginosa sensitivity to antibiotics].

The response of Pseudomonas aeruginosa to antibacterial drugs is remarkably stable and is characterized by multiresistance. This organism is uniformly resistant to ampicillins, first and second generation cephalosporins and kanamycin and most often resistant to streptomycin, tetracyclines, chloramphenicol, nalidixic acid, sulphonamides, co-trimoxazole and nitrofurans. Very few of the conventional antibiotics are active against Pseudomonas spp.: polymyxin is virtually always active in vitro but gives disappointing therapeutic results; little change has been observed over years in the incidence of strains resistant to carbenicillin and to some aminoglycosides, such as gentamicin, tobramycin and amikacin. Recently developed antibacterial agents of the beta-lactam and quinolone groups offer hopes of better therapeutic effectiveness. Among beta-lactam antibiotics, new penicillins, including azlocillin, are more active than carbenicillin and some third generation cephalosporins, notably cefoperazone, cefsulodin and ceftazidime, also show anti-Pseudomonas activity. The same applies to new beta-lactam antibiotics with a novel structure, such as thienamycins and monobactams. Several new quinolones are active in vitro against Ps. aeruginosa; these are rosoxacin, norfloxacin, enoxacin, pefloxacin, ciprofloxacin and ofloxacin.

Ampicillin↗