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At least 19 recordsLinked to original sources
PubMed1982

Comparative in vitro activities of azlocillin-cefotaxime and azlocillin-tobramycin combinations against blood and multi-drug resistant bacterial isolates.

The in vitro activities of azlocillin and cefotaxime in combination and of azlocillin and tobramycin in combination against 100 blood isolates and 50 multidrug-resistant isolates were compared. With both combinations, antibacterial spectrums were complementary. Although synergy against individual strains was infrequently observed (except for azlocillin-cefotaxime against Streptococcus faecalis and azlocillin-tobramycin against Pseudomonas aeruginosa), 97% of blood isolates and 76% of multidrug-resistant isolates were susceptible to azlocillin-cefotaxime, and 94% of blood isolates and 36% of multidrug-resistant isolates were susceptible to azlocyclin-tobramycin.

Anti-Bacterial Agents↗
PubMed1990

Randomized multicentre study of ciprofloxacin and azlocillin versus gentamicin and azlocillin in the treatment of febrile neutropenic patients.

In a randomized multicentre study ciprofloxacin combined with azlocillin was compared with gentamicin and azlocillin for the treatment of febrile episodes in neutropenic patients. In 147 evaluable episodes in 108 patients, 80 patients received ciprofloxacin/azlocillin and 67 received gentamicin/azlocillin. The two treatment groups were comparable in terms of age, underlying diagnosis, and duration of neutropenia. Microbiologically documented infections were the cause of fever in 34 (42.5%) and 29 (43.3%) episodes in the ciprofloxacin/azlocillin and gentamicin/azlocillin groups respectively. At the end of therapy, 46 patients (57.5%) receiving ciprofloxacin/azlocillin showed complete resolution compared with 30 (44.7%) for the gentamicin/azlocillin group (P = 0.14). The clinical response rate for microbiologically documented episodes was 58.8% and 48.3% respectively (P = 0.45). Among the microbiologically documented infections with follow-up cultures available, 24 (92.3%) of 26 isolates from patients receiving ciprofloxacin/azlocillin were eradicated, in comparison with 19 (86.4%) of 22 in the gentamicin/azlocillin group (P = 0.65). There were five superinfections, all in the gentamicin/azlocillin group. Significant resistance to the study drugs was not seen. Of all evaluable patients, including those subsequently withdrawn because of early modification of therapy, there were 12 deaths within the study period; six (6.8%) of these occurred in 88 patients randomized to the ciprofloxacin/azlocillin group, compared with two of 80 (2.5%) in the gentamicin/azlocillin group. Both treatments were generally well-tolerated; one patient in the ciprofloxacin/azlocillin group developed convulsions, probably related to ciprofloxacin. The combination of ciprofloxacin and azlocillin is as effective as gentamicin plus azlocillin and offers a useful alternative for the empirical treatment of febrile neutropenic patients.

Adolescent↗
PubMed1983

Clinical and bacteriological responses to three antibiotic regimens for acute exacerbations of cystic fibrosis: ticarcillin-tobramycin, azlocillin-tobramycin, and azlocillin-placebo.

In a randomized, double-blind study, cystic fibrosis patients 11-30 years of age with an acute exacerbation of their pulmonary disease were treated with either ticarcillin-tobramycin, azlocillin-tobramycin, or azlocillin-placebo for 10 days. There was significant improvement in Shwachman scores and pulmonary function tests. Concentrations of sputum bacteria were significantly reduced, but after therapy patients had a mean of 10(7) bacteria/ml of sputum. Pseudomonas was transiently eliminated in only one patient. The three regimens had similar impacts on pulmonary function and sputum bacterial concentration. Antibiotic resistance was noted more frequently in the azlocillin-placebo group, but this trend was not statistically significant. Improvement in pulmonary function did not correlate with bacteriological response. Four weeks after discharge, 62% of the improvement in forced expiratory volume in one second and 75% of the improvement in vital capacity remained, but concentrations of sputum bacteria had returned to pretreatment levels, and antibiotic-resistant bacteria persisted.

Acute Disease↗
PubMed1986

Multiple-dose pharmacokinetics of piperacillin and azlocillin in 12 healthy volunteers.

The pharmacokinetic profile of piperacillin and azlocillin after multiple-dose administration to healthy volunteers was studied. Twelve healthy volunteers received either piperacillin 4 g (as the sodium salt) or azlocillin 4 g (as the sodium salt) as a 20-minute infusion every six hours for five doses. After a one-week washout period, subjects received identical treatment with the alternate drug. Serum and urine concentrations of piperacillin and azlocillin were measured using a reversed-phase high-performance liquid chromatographic assay, and the pharmacokinetic analysis of serum concentration-versus-time data was performed using a computerized program. A standard open-model equation for i.v. infusions was used. Mean serum concentrations of piperacillin and azlocillin after dose 5 were 344 +/- 66 micrograms/mL and 414 +/- 86 micrograms/mL, respectively. The terminal elimination half-life of azlocillin (1.1 +/- 0.2 hr) was significantly longer than that of piperacillin (0.75 +/- 0.13 hr) (p less than 0.05). Total body clearance of azlocillin (125 +/- 25 mL/min) was significantly less than that of piperacillin (226 +/- 43 mL/min) after dose 5. Azlocillin showed accumulation between the first and fifth doses. Twelve hours after administration of dose 5, 75% of azlocillin and 57% of piperacillin were excreted unchanged into the urine. In healthy volunteers, azlocillin produced higher and more prolonged serum concentrations than piperacillin after administration of equivalent i.v. doses. Further studies are needed to determine the clinical importance of these observations.

Adult↗
PubMedDate not supplied

Pharmacokinetics of high-dose azlocillin sodium in patients with cystic fibrosis.

The pharmacokinetics of high-dose azlocillin sodium was studied in 18 patients with cystic fibrosis. Nine male and nine female patients with a mean age of 14.7 years (range 3 to 29 years) participated in the study. They received azlocillin 450 mg/kg/day (as the sodium salt) in six divided doses. During a steady-state dosing interval, a dose of azlocillin was coadministered with a 10-mg/kg dose of iothalamate sodium as a 30-minute infusion. Serum concentrations of azlocillin and iothalamate were determined by high-pressure liquid chromatography assay. The data were analyzed using model-independent methods. The mean elimination rate constant for azlocillin was 0.64 +/- 0.22 hr-1 and the mean serum half-life was 1.22 +/- 0.39 hr. Total clearance of azlocillin, calculated by noncompartmental analysis, was 77.2 +/- 26.4 mL/min/sq m. Glomerular filtration rate, as estimated by measuring iothalamate clearance, was 79.6 +/- 21.9 mL/min/sq m. The total clearance of azlocillin correlated with iothalamate clearance. Patients with cystic fibrosis appear to eliminate azlocillin more rapidly than healthy individuals. This rapid elimination warrants the use of high doses to maintain high serum concentrations.

Adolescent↗
PubMed1990

[The effect of continuous arteriovenous hemofiltration on the pharmacokinetics of azlocillin in anuric patients].

The influence of continuous arteriovenous hemofiltration on the pharmacokinetics of azlocillin was examined in eight anuric intensive care patients, each of whom received a short infusion of 5.0 g azlocillin. Azlocillin concentrations in blood were measured simultaneously in the afferent and efferent loops of the amicon Dia 20 hemofilter and in the ultrafiltrate by means of an agar diffusion technique. Pharmacokinetic parameters were calculated by a computer program based on a two compartment model. We found that the elimination half-life of azlocillin ranged between 218.8 and 342.8 min, a result comparable to those of other investigators, who found similar elimination half-lives in anuric patients. During an observation period of 270 min, only 0.2-1.1% of the total dose of azlocillin was eliminated by way of the hemofilter. Apparently, continuous arteriovenous hemofiltration has no clinically relevant implications for the dosage or the dosage intervals of this antibiotic. On the other hand, azlocillin was taken up by the amicon Dia 20 hemofilter during the infusion. After the infusion was stopped the filter released azlocillin to blood and ultrafiltrate. The ratio of concentration in ultrafiltrate to plasma concentration in the afferent loop of the hemofilter was higher for about 45 min during the elimination phase than during the infusion. The volume of distribution was much larger (mean 28.5 l) than that found by other investigators. Therefore, the amicon-Dia 20 hemofilter seems to function as an additional distribution space.(ABSTRACT TRUNCATED AT 250 WORDS)

Anuria↗
PubMed1984

[Clinical pharmacokinetics of azlocillin].

The pharmacokinetics of azlocillin have been studied in healthy subjects and in patients, in children and in adults, using different doses, either single or repeated. Following intravenous injection of doses ranging from 1 to 5 g, plasma concentrations increase in relation to dosage. Maximum concentrations at the end of an injection or infusion average 100-200 micrograms/ml with 1 g and 400-500 micrograms/ml with 5 g. Azlocillin has a low degree of plasma protein binding: 30% to 40% depending on concentrations. Its volume of distribution is approximately 0.2 l/kg. Tissue distribution has been studied by various authors: with a 2 to 5 g dose, therapeutically active concentrations have been found in a variety of tissues, including bronchial secretions, bone, etc. Azlocillin crosses the placenta; the ratio of maternal to foetal plasma concentrations is 0.50. Azlocillin undergoes little metabolic degradation and its metabolites (penicilloates) amount to less than 15% of the dose administered. Most of the drug is excreted by the kidneys, 50% to 70% of the dose injected being recovered in the 24 h urines; the remainder is excreted in the bile, and biliary concentrations may be as high as 15-fold the corresponding plasma concentrations. Azlocillin is rapidly cleared. Its plasma half-life varies from 45 to 75 min according to different authors. The fact that it increases slightly with dosage suggests the kinetics of the drug might be dose-dependent. In view of the intervals between doses, this is certainly not of therapeutic importance. Total and renal clearance values are 150-200 ml/min and 100-140 ml/min respectively. In patients with renal impairment azlocillin is eliminated more slowly, with a half-life of up to 6-10 h when creatinine clearance is below 5 ml/min. The reduced urinary excretion may partly be compensated for by increased biliary excretion. The proportion of drug removed by haemodialysis is 40-50%. Azlocillin excretion is slowed down in children under 3 months of age, with half-lives of 4.5 h, 3.0 h and 2.0 h respectively in prematures, neonates and infants.

Azlocillin↗
PubMed1984

[Azlocillin treatment of Pseudomonas aeruginosa bronchopulmonary infections in children with cystic fibrosis].

From April, 1980 to December, 1981 ten children aged from 2 to 14 years presenting with cystic fibrosis were admitted to hospital for exacerbation of their chronic bronchial infection. Mucous Pseudomonas aeruginosa was present in sputum. Seven of the 10 strains isolated were susceptible to azlocillin and 3 were classified as intermediate. Eight children were treated with azlocillin alone in doses of 200-300 mg/kg/day and two with combined azlocillin 300 mg/kg/day and amikacin 16 and 23 mg/kg/day respectively. In both groups the antibiotics were administered 8-hourly by short (30 min) intravenous infusions and the duration of treatment ranged from 8 to 21 days (mean 14 days). Both drugs were well tolerated. Antibacterial activity was assessed as "cure" when Pseudomonas could not be isolated in sputum for at least 2 weeks after the end of the treatment, as "relapse" when that organism reappeared in sputum within the same period of time, and as "failure" when it persisted in sputum. On this account, among the 8 children treated with azlocillin alone 3 were cured, one relapsed and 4 failed. One of the two children treated with the azlocillin-amikacin association was cured, the other failed. Clinical results correlated roughly with antibacterial activity. Five distinct improvements were observed: 2 were associated with bacteriological cure, 2 with transient eradication followed by relapse and 1 occurred although the responsible organism persisted in bronchial secretions. Two children showed poor clinical results; 2 with failure and 1 with bacteriological cure. In two other children treatment was ineffective both clinically and bacteriologically. This study confirms that high parenteral doses of azlocillin have a beneficial effect on exacerbations with Ps. aeruginosa of chronic bronchial infection in cystic fibrosis. Clinical improvement usually correlates with antibacterial activity when the organism is eliminated, even temporarily, from bronchial secretions. The synergistic azlocillin-aminoglycoside association should probably be recommended, at least to reduce the risk of emergence of resistant strains.

Adolescent↗
PubMed1979

Comparative study of anti-pseudomonas activity of azlocillin, mezlocillin, and ticarcillin.

The anti-pseudomonas activities of azlocillin and mezlocillin were compared with that of ticarcillin. We measured the minimal inhibitory and minimal bactericidal concentrations of the three drugs against 20 different strains of Pseudomonas aeruginosa and found significantly lower values for azlocillin than for the other two drugs. We then infused 5 g of each drug into 10 volunteers on three consecutive days and determined the serum levels of the three antibiotics at 1-h intervals from 1 to 6 h after injection. The levels of azlocillin were significantly higher than those of mezlocillin and ticarcillin (at 1 h: 236.55 mug/ml +/- 12.9 for azlocillin, 192.45 mug/ml +/- 28.8 for mezlocillin, and 131.5 mug/ml +/- 10.9 for ticarcillin). The inhibitory and bactericidal activities of the sera obtained 1 and 6 h after the injection against the same 20 strains of P. aeruginosa demonstrated a significantly greater anti-pseudomonas activity of azlocillin when compared with mezlocillin and ticarcillin; mezlocillin and ticarcillin had approximately the same activity. The mean values for bactericidal activity against the strains tested were 1/32 for azlocillin, 1/8 for mezlocillin, and 1/8 for ticarcillin. Azlocillin thus appears to be a promising anti-pseudomonas drug and should be tested in clinical trials.

Humans↗
PubMedDate not supplied

Efficacy of ciprofloxacin alone and in combination with azlocillin in experimental endocarditis due to Pseudomonas aeruginosa.

The efficacy of ciprofloxacin alone and in combination with azlocillin was compared with that of azlocillin plus tobramycin in a rat model of aortic valve endocarditis due to Pseudomonas aeruginosa. MICs against the infecting strain of ciprofloxacin, azlocillin and tobramycin were 0.125, 8, and 0.5 mg/l, respectively. Antimicrobials were administered 24 h after bacterial challenge and for six days. Mean peak/trough serum levels for ciprofloxacin (50 mg/kg i.v. q 12 h), azlocillin (500 mg/kg i.v. q 12 h) and tobramycin (6.5 mg/kg i.v. q 12 h) were: 10.5/0.2, 386/less than 16, and 6.2/less than 0.6 mg/l, respectively. Ciprofloxacin alone was more effective than the combination azlocillin-tobramycin in increasing survival (p less than 0.05), sterilizing blood (p less than 0.05) and valves (p less than 0.001), and in reducing bacterial titers in vegetations (p less than 0.001). Ciprofloxacin-azlocillin combination was not more effective than ciprofloxacin alone. Drug resistance was not encountered in post-treatment isolates with any therapy regimen.

Animals↗
PubMedDate not supplied

[Experiences using acylureido-penicillins (azlocillin, mezlocillin) in pediatrics].

The acylureidopenicillins azlocillin and mezlocillin cover a broad spectrum of bacteria, including gramnegative and grampositive species as well as anaerobes. Azlocillin is especially active against P. aeruginosa. Mezlocillin has a good activity against Klebsiella. Both antibiotics inhibit Hemophilus, N. meningitidis and D. pneumoniae in low concentrations. Clinical and kinetic studies were made in more than 300 pediatric patients. Elimination-constant halflife, distribution volume and area under the curve were determined to propose dosage recommendations. Concentrations of azlocillin (44) and mezlocillin (77) were measured in the bronchial secretions. Up to hour 5 after i.v. injection a wide range of concentration values were observed. Azlocillin was found in the meconium in different concentrations after a single injection into the newborn. Mezlocillin diffused into the CSF even in uninflamed meninges, 3 h after injection the mean concentrations were 5.5 mg/l. 39 patients, 35 of them infected by P. aeruginosa, were treated by azlocillin. Urinary tract infections, wound infections and dacryocystitis were cured with one exception. Less convincing were the results in complicated bronchopulmonary diseases. The clinical efficacy of mezlocillin was similar. In a group of 59 patients there were only 3 without effect and some with improvement again in complicated pulmonary diseases. Side effects worth to be mentioned were not seen. In 2 patients the azlocillin injection caused nausea. Mezlocillin led to some minor transitory elevations of the transaminases and dyspepsia in some patients.

Adolescent↗
PubMed1983

A comparison of azlocillin and ticarcillin in the treatment of complicated urinary tract infections.

In a prospective, controlled, and randomized study, 79 patients with urinary tract infections primarily caused by Pseudomonas aeruginosa were treated with azlocillin at 8 g/day or ticarcillin at 12 g/day for 5 to 23 days. The evaluations of clinical and bacteriological responses of the patients to therapy were made by a 'blind' third-party observer. Overall, 74% of the 38 patients treated with azlocillin were cured, as were 67% of the 33 treated with ticarcillin. A favourable clinical response to azlocillin was achieved in 34 (89.4%) of the patients; 30 (93.8%) of the ticarcillin-treated patients had a favourable clinical response. Bacteriologically, administration of azlocillin eliminated the causative organisms in 31 of the infections (92.1%); the causative organisms were eliminated in 31 of the infections (96.9%) treated with ticarcillin. In both groups, in addition to bacterial persistence, treatment failures were due to bacteriological superinfection, generally with Escherichia coli or Klebsiella pneumoniae. No local reactions were reported for either treatment group. One 80-year-old patient with prostatic carcinoma treated with azlocillin had a mild and reversible decrease in renal function during therapy, and another developed a mild pruritic rash. The results of this study indicate that azlocillin at 8 g/day is as effective as ticarcillin at 12 g/day for the treatment of urinary tract infections caused by Ps. aeruginosa; both drugs were tolerated well.

Adolescent↗
PubMed1983

Materno-fetal transfer of azlocillin.

We studied 20 patients to assess transfer of azlocillin to the fetus at parturition. The elimination half-life of approximately 1.3 h in these mothers was similar to that reported for normal subjects. Azlocillin quickly reached umbilical cord blood, amniotic fluid, the placenta and the urine of the neonate, achieving substantial concentrations. Azlocillin then disappeared from umbilical cord blood with an elimination half-life of 2.3 h, i.e., similar to that of the mother. At 6 h, concentrations of azlocillin were still increasing in amniotic fluid and placenta. In addition, in two stillborn infants, azlocillin was found to reach substantial concentrations in all tissues analysed except brain. Concentrations of azlocillin achieved in fetal tissues are sufficient to have important therapeutic effects.

Amniotic Fluid↗
PubMed1982

Activities of tobramycin and azlocillin alone and in combination against experimental osteomyelitis caused by Pseudomonas aeruginosa.

Azlocillin and tobramycin were used alone and in combination in the treatment of chronic osteomyelitis due to Pseudomonas aeruginosa in rabbits. This combination showed in vitro synergy measured by both the checkerboard technique and time-kill curves. A marked inoculum effect was demonstrated in vitro with azlocillin and the infecting strain of P. aeruginosa. The minimal inhibitory concentration of azlocillin, with an inoculum of 10(5) organisms, was 12.5 micrograms/ml; when the inoculum size was increased to 10(7) organisms, the minimal inhibitory concentration rose to more than 500 micrograms/ml. In therapeutic trials, the combination of azlocillin and tobramycin, given for 28 days, was significantly better than either no therapy or azlocillin alone, but was not significantly better than tobramycin alone. Even after 4 weeks of combined therapy with azlocillin and tobramycin, P. aeruginosa was recovered from the bones of 60% of the treated rabbits.

Animals↗
PubMed1985

Comparison of ciprofloxacin with azlocillin plus tobramycin in the therapy of experimental Pseudomonas aeruginosa endocarditis.

The efficacy of ciprofloxacin (Bay o 9867), a promising new quinolone, was compared with the efficacy of azlocillin plus tobramycin in rabbits with experimentally induced Pseudomonas aeruginosa endocarditis. The MBCs of ciprofloxacin, azlocillin, and tobramycin against the test strain were 0.5, 8, and 4 micrograms/ml respectively. Ciprofloxacin at a concentration of 50 mg/kg or azlocillin at a concentration of 200 mg/kg in combination with tobramycin at a concentration of 5 mg/kg was administered intramuscularly at 8-h intervals for 4 days. Both regimens produced median peak serum bactericidal titers of 1:8. The concentrations of ciprofloxacin, azlocillin, and tobramycin in serum, 1.8 +/- 0.7, 154 +/- 48, and 9.1 +/- 2.4 micrograms/ml (mean +/- standard deviation), respectively, closely approximated concentrations found in humans after accepted dosages. At the end of treatment, the titers of P. aeruginosa were 3.0 +/- 1.6 log10 CFU/g of vegetation (mean +/- standard deviation) for recipients of ciprofloxacin and 3.2 +/- 1.3 log10 CFU/g of vegetation for recipients of azlocillin plus tobramycin. These values compared with control titers of 7.3 +/- 1.6 CFU/g. These data indicate that at the doses used, ciprofloxacin was as effective as azlocillin plus tobramycin in the treatment of P. aeruginosa endocarditis in rabbits. Since the latter drug combination has proven efficacy, ciprofloxacin deserves further evaluation in the therapy of systemic infections in animal models and in humans.

Animals↗
PubMed1982

Dose-dependent pharmacokinetics of azlocillin compared to mezlocillin.

The pharmacokinetics of azlocillin at intravenous doses of 1.0, 2.0 and 5.0 g and of 2.0 g mezlocillin were studied in a cross-over study on 10 healthy volunteers. The serum concentrations and total area under the serum curves for azlocillin increased more than expected from the multiples of the dose size. Likewise, the percentage of urinary excretion of an antibacterially active agent increased steadily with higher doses. The same applied to the serum half-life (t 1/2), whereas the total body clearance was reduced. All these characteristics are indicative of dose-dependent, i.e. capacity-limited pharmacokinetics. The t 1/2 was 0.89, 0.98, and 1.53 h for each dose. For 2.0 g mezlocillin, the serum values, urinary recovery, and t 1/2 were lower than the values after the same dose of azlocillin. The t 1/2 was 0.64 h. The total body clearance was 12,0, 9.2, and 6.4 liters/h for the three doses of azlocillin and 14.4 liters/h for 2. g mezlocillin. Dose dependence appears to be more pronounced with azlocillin than found previously with mezlocillin. Unchanged azlocillin and its biotransformation products are excreted more slowly than mezlocillin and its metabolites.

Adult↗