Search PubMed⌕ Search

SEARCH · Search PubMed

Results for “Azlocillin”

Search indexed PubMed citations on genomics, clinical trials, systematic reviews and public health. Explore titles, authors and supplied subject terms, then open the PubMed record.

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

At least 73 records · Page 4Linked to original sources
PubMed1985

Comparison of the antibacterial activity of azlocillin and ticarcillin in vitro and in irradiated neutropenic mice.

The antibacterial efficacy of azlocillin against Pseudomonas aeruginosa was quantitatively assessed in short-term growth curves in vitro and in a short-term thigh muscle infection in granulocytopenic mice. Ticarcillin was used as the reference drug. The antibacterial effect in vitro was expressed as the difference between the logarithms of the numbers of cfu in the presence and absence of antibiotics (log ratio). The log ratio-time curves could be described by a concentration-dependent parameter, i.e., the inhibition constant (i). According to a standard parallel line bio-assay, based on values of i, azlocillin was 3.80 times more active than ticarcillin (coefficient of variation 27%). Tobramycin in a concentration of 0.19 mg/l, which is not effective in itself, potentiated both drugs by a factor of 3.85 (coefficient of variation 26%). In the in vivo model ticarcillin showed a dose-dependent antibacterial effect, whereas the effect of azlocillin was limited and not dose dependent. The effect of tobramycin in a dose of 4 mg/kg was additive for both penicillins. The results obtained in vivo were less favourable for azlocillin than would be predicted on the basis of the in-vitro results.

Animals↗
PubMed1984

Importance of methodology in determining bactericidal and bacteriostatic activities of azlocillin and ticarcillin against Pseudomonas aeruginosa.

The activities of azlocillin and ticarcillin against Pseudomonas aeruginosa were compared by estimating minimum inhibitory and bactericidal concentrations (MIC and MBC) in liquid and solid media, and by constructing killing curves from sequential viable counts. In MIC studies, azlocillin was about three times more active than ticarcillin in solid medium (agar dilution test) and in liquid media (tube and microdilution tests). When the MBC was measured, however, results varied according to the technique used. On agar and in microdilution tests, both azlocillin and ticarcillin were bactericidal, the MBC being 1.3-3 MIC. In the tube test, the MBC for ticarcillin was again about 3 MIC, but azlocillin appeared not to be bactericidal (MBC greater than 1 mg/ml). However, sequential viable counts of four clinical isolates showed that at 4 MIC both antibiotics reduced viable counts by a factor of 10(4) in 8 h. Our results stress the importance of methodology when assessing the antibacterial activity of an antibiotic.

Azlocillin↗
PubMed1984

Serum and sputum concentrations of azlocillin, cefoperazone and ceftazidime in patients with cystic fibrosis.

Single-dose pharmacokinetics of azlocillin, cefoperazone and ceftazidime were studied in 17 patients with cystic fibrosis (CF). All patients had broncho-pulmonary infections caused by Pseudomonas aeruginosa. Three groups of five, six, and six patients were treated with azlocillin, cefoperazone, or ceftazidime, respectively. The size of the single dose was 133 mg/kg for azlocillin, 66.7 mg/kg for ceftazidime and 66.7 mg/kg for cefoperazone. The clearance values for the three antibiotics calculated from the single-dose data were, on the average, higher than the values previously reported for normal subjects. After the first dose, the patients received a repeated-dose treatment with the same antibiotic. During the first 5 days of therapy, a complement postural drainage of sputum was obtained four times a day for each patient. Cefoperazone could be measured in 47 (39.2%) of the 120 sputum samples assayed while ceftazidime was shown to be present in all 120 sputum samples examined. Azlocillin was not detected in any of the 100 sputum samples assayed.

Adolescent↗
PubMed1984

Augmentation of the in vitro activity of azlocillin against Bacteroides fragilis by clavulanic acid.

Azlocillin was active against 90% of 154 strains of Bacteroides fragilis at a concentration of 64 micrograms/ml. Twenty-eight strains of B. fragilis with an azlocillin MIC of greater than or equal to 8 micrograms/ml were retested with a combination of azlocillin plus clavulanic acid. Of these strains, 71% showed a 4- to 32-fold decrease in the MIC of azlocillin plus clavulanic acid.

Azlocillin↗
PubMed1986

Comparative pharmacokinetics of azlocillin and piperacillin in normal adults.

The single-dose pharmacokinetics of azlocillin and piperacillin were compared by using a randomized, crossover design. The concentrations of azlocillin in serum were consistently higher than those of piperacillin throughout an 8-h study. The area under the time-concentration curve of azlocillin was significantly greater than that of piperacillin, and the total body clearance of azlocillin was significantly lower than that of piperacillin.

Adult↗
PubMed1990

Alteration in the pharmacokinetic disposition of ciprofloxacin by simultaneous administration of azlocillin.

Healthy subjects were given single intravenous doses of ciprofloxacin, azlocillin, and the two drugs simultaneously on separate occasions. High-pressure liquid chromatographic analysis was used to assay the concentrations of both drugs in serum and urine. Pharmacokinetic parameters were calculated by noncompartmental methods. The total body (CL), renal (CLR), and nonrenal (CLNR) clearances; steady-state volume of distribution (Vss); and fractional urinary excretion of ciprofloxacin were all markedly decreased with the simultaneous administration of azlocillin. The disposition of azlocillin was unchanged when it was given with ciprofloxacin compared to when it was given alone. The pharmacokinetic parameters (mean +/- standard deviation) of ciprofloxacin given alone versus in combination with azlocillin were as follows: CL, 52.2 +/- 9.2 versus 33.9 +/- 6.0 liters/h (P less than 0.0005); CLR, 26.5 +/- 4.8 versus 16.2 +/- 4.2 liters/h (P less than 0.0005); CLNR, 25.8 +/- 5.5 versus 17.7 +/- 4.0 liters/h (P less than 0.03); Vss, 224 +/- 30 versus 166 +/- 41 liters (P less than 0.01); fractional urinary excretion, 0.56 +/- 0.06 versus 0.43 +/- 0.04 (P less than 0.002), respectively. This interaction resulted in significantly higher and more prolonged concentrations of ciprofloxacin in serum, which may be beneficial in the treatment of serious gram-negative bacterial infections, but it could also produce greater toxicity or result in more pronounced effects on oxidative drug metabolism of other medications.

Adult↗
PubMed1994

Time-survival studies for quantifying effects of azlocillin and tobramycin on Pseudomonas aeruginosa.

Time-survival studies were conducted to estimate the effects of azlocillin and tobramycin on Pseudomonas aeruginosa NCIMB 8295 (in the exponential phase of growth) at concentrations ranging from one-quarter to twice the MIC. The effects of the individual agents and their combinations were determined by measuring the viable counts (CFU per milliliter) over a 24-h period. The typical pattern observed from the plot of the logarithm of the CFU per milliliter against time was an initial rapid killing; this was followed by a period of stasis and regrowth. Initial rates of killing by tobramycin were concentration dependent, whereas this was not the case with azlocillin. From the time-survivor plots, the area under the curve for viable bacteria was also calculated. It offered a useful method of interpreting the results of time-kill studies, taking the overall pattern of killing and regrowth into consideration. The area under the curve for viable bacteria was concentration dependent for both antibiotics. A 2(2) factorial experimental design was used to analyze the joint effects of azlocillin and tobramycin. In such a factorial experiment, an interaction between two factors, in this case, azlocillin and tobramycin concentrations, is shown by a change in the slope of the plot when the concentration of the interactant is changed. Analysis of variance showed that the combination was synergistic at low concentrations, but this was not significant when the concentration of either interactant was increased.

Azlocillin↗
PubMed1991

Clinical efficacy and in vitro activity of the ciprofloxacin-azlocillin combination (ratio 1:10) against gram-negative bacteria from non-neutropenic haematologic patients.

The authors report treatment of eighteen haematologic patients (twelve male, six female, age between 21 and 78 years), suffering from upper respiratory tract (ten patients) and/or lower urinary tract (eight patients) infections caused by Gram-negative germs, with a combination of ciprofloxacin-azlocillin in the ratio 1:10. Before treatment, the Minimum Inhibitory Concentration (MIC), Minimum Bactericidal Concentration (MBC) and Fractional Inhibitory Concentration (FIC) index of Gram-negative isolates from patients for the ciprofloxacin-azlocillin combination were evaluated. The in vitro experiments revealed a synergistic activity of the combination for 85% of isolates, while at the same concentration ciprofloxacin alone was 100% effective, and azlocillin alone was 50% effective. The combination was administered to patients as follows: ciprofloxacin: 750 mg "per os" every 12 h; azlocillin 5 g intravenously every 8 h for a therapeutic cycle of 8 days. Seventeen of the eighteen patients that were treated with the combination showed complete eradication of the causative pathogen, sixteen of the eighteen patients recovered fully, whereas the other two showed significant improvements. The tolerability of the combination was excellent in seventeen patients and only one patient developed symptoms of mild gastric intolerance. The results presented here warrant further interest in studies of this antibiotic combination.

Adult↗
PubMedDate not supplied

[Azlocillin in the treatment of pulmonary infections in patients with cystic fibrosis: plasma concentrations and therapeutic indications].

Azlocillin plasma concentrations have been studied in 10 cystic fibrosis patients suffering from chronic pulmonary infections with Pseudomonas aeruginosa. Patients were given single i.v. doses of 100 e 200 mg/kg body weight as intravenous infusion over 30 minutes. Azlocillin plasma levels have been assayed by a rapid, sensitive and precise high performance liquid chromatographic method. After the dose of 100 mg/kg body weight concentrations of azlocillin decreased below the therapeutic concentrations after three hours; dose of 200 mg/kg was followed by plasma concentrations in the therapeutically desirable range during the 6-8 hours study period. The pharmacokinetic analysis offers further evidence of the dose-dependent nature of azlocillin elimination. Higher dosage of 200 mg/kg body weight and monitoring of plasma drug levels are recommended in the therapy of patients with cystic fibrosis.

Adolescent↗
PubMed1986

[Bacteriostatic activity of azlocillin, gentamycin, amikacin singly or in combination on 200 strains of Pseudomonas aeruginosa].

In vitro activity of azlocillin, gentamicin, and amikacin, alone or in combination was evaluated against 200 clinical isolates of Pseudomonas aeruginosa. The minimum inhibitory concentrations (MICs) were determined by a standard technique. For the evaluation of synergistic activities, one antibiotic was added in a concentration equivalent to one-fourth its MIC to increasing concentrations of the other antibiotic. The MIC for 50% of the strains was 3.25 micrograms/ml for gentamicin, 3 micrograms/ml for amikacin and 7 micrograms/ml for azlocillin. No significant difference could be seen between the two combinations, the percentage of synergy was 37% for azlocillin-gentamicin and 36% for azlocillin-amikacin. No antagonism was observed.

Amikacin↗
PubMed1988

[Antimicrobial effectiveness of azlocillin in cholesteatoma in parenteral administration].

Azlocillin has a broad spectrum particularly against pseudomonas and should therefore be useful for preoperative parenteral treatment of infected cholesteatomas in those cases which cannot be controlled by local therapy. To determine the efficacy in treatment of cholesteatoma the concentration of azlocillin in separate tissue fractions of cholesteatoma matrix, cholesteatoma debris and granulation tissue surrounding cholesteatoma was determined. In 9 cases 2 g azlocillin was injected and in 5 cases 4 g. The concentration drop between the different tissue fractions was equal in all cases. However, as clinical experience has shown, differing high levels of azlocillin were found in comparable tissue fractions of the 14 cholesteatomas. In some of the cases the minimal antibacterial activity was not attained in the cholesteatoma fractions.

Azlocillin↗
PubMed1987

[General toxic and organotropic properties of azlocillin in acute and chronic experiments].

The general toxic and organotropic properties of azlocillin were studied in acute and chronic experiments with various animal species. By the body surface area the doses of azlocillin were equivalent to the drug average and maximum course doses for humans. The aim of the study was to determine the drug dose inducing certain side effects. It was found that only in a dose equivalent to the maximum course dose for humans i. e. 300 g the drug induced a transient increase in the blood levels of aspartate aminotransferase and alkaline phosphatase and some increase in the coagulation time. The allergenic properties of the drug were slightly pronounced. Within the tested doses azlocillin did not affect the peripheral blood indices and showed no immunomodulating embryotoxic, teratogenic or mutagenic effect. The experimental data indicated that the range between the drug therapeutic course doses and the doses inducing certain side effects was significant. This is evidence of a sufficiently high level of azlocillin safety.

Adjuvants, Immunologic↗
PubMed1979

[On the excretion of azlocillin with bronchial secretion in children (author's transl)].

This pharmacokinetic study involved school children who were treated with 6-[(R)-2-(2-oxo-imidazolidine-1-carboxamido)-2-phenyl-acetamido]-penicillanic acid sodium walt (azlocillin, Securopen) at doses of 50 mg/kg bodyweight or 75 mg/kg body weight i.v. Kinetics of the first order were found for the concentrations measured at the same time, being proportionate to the administered dose, while there was no dose dependence for the relative distribution volume. The elimination half-life was about 55 min. In 25 children of different age who had to undergo bronchoscopy for diagnositic and therapeutic reasons, the azlocillin concentrations in the bronchial secretions were measured 1 h and 4 h after the administration of 75 mg/kg quantity of bronchial secretion was obtained, azlocillin concentrations of 30 - 240 microgram/g were found. Measurements of azlocillin concentration in the bronchial secretion and in the serum, which were made at the same time, did not show any correlation.

Adolescent↗
PubMed1984

[Role of azlocillin in the treatment of Pseudomonas aeruginosa otitis in children].

From May, 1978 to October, 1983, 88 children with otitis due to Pseudomonas aeruginosa were seen at Paediatric Unit E.N.T. consultation of the University Hospital of Tours. Epidemiologically, it is worth mentioning that the majority of these infections was not of nosocomial origin: 56 children were infected outside the hospital and 26 during their stay in hospital; 3 neonates were referred directly from the Maternity Unit. Most strains of Ps. aeruginosa, with various serotypes, were sensitive to azlocillin. Twenty-four children received a systemic treatment required by their local or general condition. Azlocillin was used in 24 cases on the basis of positive sensitivity tests and was occasionally combined with topical treatment using antiseptics or the antibiotic itself. Or the 3 failures observed, 2 were due to acquired resistance to azlocillin and 1 to chronic otitis. An incomplete result was obtained in a case of otitis externa caused by a strain of intermediate sensitivity. The remaining 19 cases were cured, including 3 neonates with otitis externa or media, 1 child with otitis externa, 1 with combined otitis externa and media, 10 with otitis media, usually protracted, 2 with mastoiditis medically cured and 1 with superinfection following mastoidectomy for cholesteatoma. Secretions dried up within 3 to 4 days and treatment was discontinued after clinical cure was obtained in 9 to 19 days. Fever, which was present in 7 cases, abated within 2 to 8 days. The only relapse that occurred, one month after treatment of an otitis media, responded to a second course of azlocillin.

Adolescent↗
PubMed1984

[Role of azlocillin in the treatment of immunocompromised patients. Results of the EORTC (European Organization for Research on the Treatment of Cancer) study)].

A multicentre clinical trial was organized by the International Antimicrobial Therapy Project Groups of the European Organisation for Research on the Treatment of Cancer (E.O.R.T.C.) to compare the effectiveness of three combinations of antibiotics (azlocillin + amikacin; cefotaxime + amikacin and ticarcillin + amikacin) in patients with malignant leukopenic and febrile diseases (polymorphonuclears less than 1000/mm3; temperature greater than 38.5 degrees C). Some 800 patients from 20 centres entered the study. Preliminary results in 421 assessable patients showed a 62% positive response rate. The response rate in patients with bacteraemia was twice as high in the azlocillin group than in the other groups, the difference being significant at p less than 0.02. This difference does not seem to be due to a distribution bias, since the responsible micro-organisms, the severity of granulopenia, the incidence of bacterial-resistant strains, etc., were similar in all three groups. Similarly, the death rate was 12% in the azlocillin-amikacin group as against 15% and 17% respectively in the other groups. It would appear from this trial that the azlocillin-aminoglycoside treatment is superior to the other antibiotic combinations tested in this category of patients.

Agranulocytosis↗
PubMed1982

Chemotherapy against Pseudomonas aeruginosa in cystic fibrosis. A study of carbenicillin, azlocillin or piperacillin in combination with tobramycin.

A comparative study was made on tobramycin combined with either carbenicillin (500 mg/kg/day) or one of the new penicillins: azlocillin or piperacillin (both 300 mg/kg/day) in 50 cystic fibrosis patients with chronic Pseudomonas aeruginosa infection. Average 2-h levels of penicillins in serum were 46 micrograms/ml (piperacillin), 88 micrograms/ml (azlocillin) and 66 micrograms/ml (carbenicillin). The Pseudomonas strains were significantly more sensitive to piperacillin and azlocillin than to carbenicillin (minimal inhibitory concentrations 1.9, 2.3 and 4.2 micrograms/ml). In 21 of 54 treatment course temporary eradication of Pseudomonas was achieved. Improved ventilatory capacity and diminished proteolytic activity in sputum were seen in most patients with or without bacteriological treatment success. Resistant strains - often belonging to other types - appeared in the patients with treatment failure. With increased number of precipitating antibodies against Pseudomonas and with increased minimal inhibitory concentrations, the chance of eradication was smaller. Seven out of 20 treated with azlocillin and 14 out of 30 treated with piperacillin developed fever and exanthema by the end of treatment. Our experience suggests caution in the use of the new penicillins.

Anti-Bacterial Agents↗
PubMed1984

Comparison of the in vitro activity of azlocillin and carbenicillin against 856 clinical bacterial isolates.

Eight hundred and fifty-six strains of more than ten species: Staphylococcus aureus, Staphylococcus epidermidis, Streptococcus faecalis, Escherichia coli, Klebsiella spp, Proteus mirabilis, Proteus vulgaris, Enterobacter spp, Pseudomonas spp and Acinetobacter spp, were tested by the disc diffusion method against azlocillin and carbenicillin. Azlocillin was found to be superior to carbenicillin against Pseudomonas spp, and more than 90% of the tested strains had minimal inhibitory concentration (MIC) values well below the serum levels attainable after recommended doses of azlocillin. Against Enterobacteriaceae and Gram-positive cocci, however, azlocillin seemed to have little to offer.

Acinetobacter↗
PubMed1981

Pharmacokinetics of azlocillin in healthy subjects.

The pharmacokinetics of azlocillin were investigated in six healthy subjects with normal renal function. 40.4 to 69.6% of the injected dose was recovered, estimated as unchanged form, in urine during 24 h. After intravenous bolus injection of 15 and 30 mg/kg doses, pharmacokinetic data were calculated, using a two-compartment open body model. The mean distribution serum half-life (T1/2 alpha) was 0.11-0.12 h and the mean elimination serum half-life (T1/2 beta) was 0.79-0.89 h. The volume of the central compartment (Vc) was 7.36-8.01 1/1.73 m2 and the apparent volume of distribution (Vdss) was 14.12-14.32 1/1.73 m2. The mean T1/2 beta after a 30 min i.v. infusion of 80 mg/kg to the same healthy subjects was 1.10 h. Serum clearances (Cs) for 15, 30 and 80 mg/kg were 251.1, 214.0 and 152.9 ml/min/1.73 m2 and renal clearance (Cr) were 99.7, 145.2 and 94.1 ml/min/1.73 m2, respectively. Azlocillin pharmacokinetics were found to be dose dependent. Administration of probenecid increased the terminal serum half-life and the total area under the serum azlocillin concentration-time curve and decreased renal clearance, indicating that azlocillin is eliminated by both glomerular filtration and tubular secretion.

Adult↗