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PubMed1980

In vitro activity of piperacillin compared with that of ampicillin, ticarcillin, azlocillin, and mezlocillin.

The antibacterial activity of ampicillin, ticarcillin, azlocillin, mezlocillin and piperacillin was investigated in 1112 fresh clinical isolates using the microdilution technic. Ampicillin was the most active agent against enterococci and ticarcillin against Staphylococcus aureus, 91% of the latter being inhibited by 32 mg/l. 95% of strains of Pseudomonas aeruginosa were susceptible to piperacillin and 90% to ticarcillin and azlocillin. Piperacillin was still active against half of the azlocillin-resistant strains of Pseudomonas aeruginosa. Against the Enterobacteriaceae, mezlocillin and piperacillin were equally active: 31% of these strains were resistant to both drugs. Amongst the various strains the percentage of resistance was highest in Klebsiella (60%). Analysis of resistance patterns of Enterobacteriaceae showed almost completely parallel resistance between these two drugs the difference being less than 3%. Piperacillin, however, had the broadest spectrum of all the penicillins tested.

Ampicillin↗
PubMed1981

In vitro inactivation of gentamicin, tobramycin, and netilmicin by carbenicillin, azlocillin, or mezlocillin.

The in vitro inactivation of gentamicin, tobramycin, and netilmicin, when combined with carbenicillin, azlocillin, and mezlocillin, was studied. Plasma samples containing the aminoglycosides at a concentration of 5-8 micrograms/ml in combination with the penicillins in concentrations of 500, 250, and 50 micrograms/ml were incubated at room temperature and 37 degrees C for 0.3, 1, 3, 6, and 9 days. The aminoglycoside concentration was determined by radioimmunoassay or enzyme immunoassay. The extent of inactivation was dependent on penicillin concentration, contact time, and temperature. Penicillin concentrations of 500 micrograms/ml caused the greatest loss of aminoglycoside, while little loss occurred at the 50-micrograms/ml penicillin level. Carbenicillin, in concentrations of 250 and 500 micrograms/ml, inactivated all three aminoglycosides to a greater extent than either azlocillin or mezlocillin. The initial rate of decline in aminoglycoside concentration was greater at 37 degrees C than at room temperature. The new acylureidopenicillins, azlocillin and mezlocillin, inactivate the aminoglycosides studied, in a similar manner to that previously described for carbenicillin.

Anti-Bacterial Agents↗
PubMed1981

In vitro activity of azlocillin, carbenicillin, mezlocillin and piperacillin against Pseudomonas aeruginosa.

50% inhibitory concentration (IC50) of azlocillin, carbenicillin, mezlocillin and piperacillin against 157 strains of P. aeruginosa were determined by means of the agar plate-dilution method. The 3 new semisynthetic penicillins were significantly more active against P. aeruginosa than carbenicillin; azlocillin and piperacillin were 8-fold, and mezlocillin was 2-4-fold more active than carbenicillin. More than 95% of the P. aeruginosa strains were inhibited by 16 micrograms/ml of azlocillin or piperacillin whereas 64 micrograms/ml of mezlocillin and 256 micrograms/ml of carbenicillin, respectively, were necessary to inhibit 95% of the strains.

Azlocillin↗
PubMed1983

Azlocillin in cystic fibrosis.

The combination of azlocillin and gentamicin or tobramycin, in the treatment of lower respiratory tract infection due to Pseudomonas aeruginosa in patients with cystic fibrosis, was evaluated. Twenty patients, 10 boys and 10 girls (mean age 13 1/2 years) who had lower respiratory tract infection with positive sputum culture for P. aeruginosa, were given azlocillin i.v. 20 mg/kg every 8 hours for 10 to 12 days. In addition, either gentamicin, 2.5 to 4 mg/kg i.v. every 12 hours, or tobramycin, 4 to 5 mg/kg i.v. every 8 hours, was given. The antibiotics were given in short-term infusions (20 minutes). Besides the antibiotic treatment, the patients received inhalation therapy, pulmonary physiotherapy, and pancreatic enzymes. Pharmacokinetic studies showed that azlocillin concentrations in serum were within therapeutic levels, and in sputum they inhibited 75% of all P. aeruginosa strains. However, in only 12 of the 52 treatment courses was Pseudomonas eliminated from the sputum.

Adolescent↗
PubMed1983

Comparison between the combination of azlocillin-gentamicin and ampicillin-gentamicin in the treatment of a nursery population.

Newborn, and particularly premature infants are prone to life-threatening infections. The combination of ampicillin-gentamicin (AM-G) has been used extensively in neonatal intensive care units (NICU). Because resistant bacteria emerged, a new drug--an acylureidopenicillin, azlocillin, with a wide antibacterial spectrum--has been developed. A prospective randomized study was performed in order to evaluate the combination of AM-G vs. azlocillin-gentamicin (AZ-G). Thirty neonates received AM-G and 28 received AZ-G. Definite infection was found in 15 AM-G patients and in 10 AZ-G patients. In these patients, the antibiotic regimen was changed in six of the AM-G and in one of the AZ-G patients. In each of the two treatment groups, one very-low-birth-weight baby died due to overwhelming sepsis. In vitro sensitivity to AZ-G was higher than to AM-G, according to azlocillin blood levels obtained. Infants weighting less than 2,350 g had lower clearance and volume of distribution than did infants weighing greater than 2,350 g. The serum half-life was approximately the same in both groups. It appears to be that in the NICU, the combination of AZ-G may be more effective than the AM-G combination.

Ampicillin↗
PubMed1982

[Synergistic activity between ticarcillin, azlocillin, cefsulodin, ceftazidime and tobramycin or amikacin against Pseudomonas aeruginosa (author's transl)].

Activity of azlocillin, cefsulodin, ceftazidime, ticarcillin in combination with amikacin or tobramycin was investigated against 17 Pseudomonas aeruginosa isolates. Synergistic activity was evaluated by the microtiter checkerboard technique. The bactericidal effect of the antibiotic combination was determined by subculturing onto agar and into broth. Synergistic activities of cefsulodin and ticarcillin combined with amikacin or tobramycin were similar in the inhibitory as well as in the bactericidal tests. Synergistic effects of the combination of ceftazidime and amikacin or tobramycin were moderate or indifferent in the inhibitory and bactericidal tests. The combination of azlocillin and amikacin or tobramycin produced synergistic effects greater in bactericidal tests than in inhibitory tests. The bactericidal synergistic activities of the combinations of azlocillin, cefsulodin, ticarcillin were similar. There was no difference between amikacin and tobramycin combined with a beta-lactamine. Antagonism was not observed. A synergistic effect of the combinations was observed against 4 isolates resistant to tobramycin and/or ticarcillin. However the result of the interaction seemed to depend upon the level of resistance to the antibiotic : if the MIC or the MBC of either antibiotic in the test combination was very high, synergy could not be achieved.

Amikacin↗
PubMed1979

Comparative antibacterial activity of azlocillin, mezlocillin, carbenicillin and ticarcillin and relative stability to beta-lactamases of pseudomonas aeruginosa and klebsiella aerogenes.

The antibacterial activities of two ureidopenicillins, azlocillin and mezlocillin, were compared with those of the alpha-carboxypenicillins, carbenicillin and ticarcillin, against a large number of gram-positive and gram-negative bacteria. All four penicillins were active against a wide range of bacteria including Pseudomonas aeruginosa, but there were differences in the antibacterial spectra and in the antibacterial effects demonstrated by the two classes of penicillins. In particular, the minimum inhibitory concentrations of azlocillin and mezlocillin against Klebsiella aerogenes and against P. aeruginosa were greatly influenced by the size of bacterial inoculum tested whereas there was no significant inoculum effect with carbenicillin and ticarcillin. In stability tests, the ureidopenicillins were inactivated rapidly by the beta-lactamases of K. aerogenes and P. aeruginosa whereas the alpha-carboxypenicillins were stable. It seems probable that the inoculum effect seen with azlocillin and mezlocillin in antibacterial tests with K. aerogenes and P. aeruginosa is associated with the instability of the compounds to the beta-lactamases of these bacteria.

Carbenicillin↗
PubMed1987

Azlocillin, cephalothin, and tobramycin therapy in febrile solid tumor patients with chemotherapy-induced leukopenia.

Although the semisynthetic broad-spectrum acylureido-penicillin, azlocillin has been demonstrated to have significant antibiotic activity in leukemic patients, its role in combination therapy of febrile granulocytopenic patients with chemotherapy-treated solid tumors has not been clearly delineated. Thirty-five solid tumor patients with chemotherapy-induced absolute granulocytopenia (less than 1000 granulocytes/ml) associated with fever (greater than 38.3 degrees C) were treated on a prospective study with a combination of azlocillin 4 g intravenously (IV) every 6 hours, cephalothin 2 g IV every 6 hours, and tobramycin 80 to 100 mg IV every 8 to 12 hours. Prior chemotherapy included doxorubicin combinations in 18 patients and other combinations in 17 patients. Granulocyte counts preantibiotic therapy were greater than 100 granulocyte/ml in 14 patients, 100 to 499 in nine patients, and 500 to 1000 in 12 patients. Granulocyte nadirs were less than 100 in 20 patients, 100 to 499 in nine patients, and 500 to 1000 in six patients. Times for granulocytes to rise towards normal were 1 to 3 days in eight patients, 4 to 6 days in 18 patients, and 7 or more days in nine patients. Tobramycin levels were primarily in the peak range of 3 to 6 micrograms/ml and trough range of 0 to 1.9 micrograms/ml. The site and pathogen were identified in nine patients, the infection site clinically documented without isolated pathogen in three patients, and no site or pathogen identified in 23 patients. Of the 35 patients, 34 had good responses to the antibiotic combination (complete disappearance of fever and other evidence of infection). Serum creatinine rose 0.4 to 0.6 mg/dl in nine patients, 0.7 to 1.5 in four patients, and 1.5 in one patient (obstructive uropathy). The only other noted antibiotic-related side effect was hypokalemia. This antibiotic combination had little toxicity with marked efficacy.

Adult↗
PubMed1982

Pharmacokinetic studies of azlocillin, mezlocillin, cephalothin and sisomicin in rabbits.

Pharmacokinetic parameters of two new acylureido penicillins (azlocillin and mezlocillin) and of cephalothin and sisomicin were compared in rabbits after the subcutaneous administration of 50 mg or 100 mg. It was found that the highest serum level of the antibiotics was reached 15 to 30 min after administration. Only sisomicin, applied in a higher dosage, reached its peak value after 60 min. The half-lives for azlocillin and mezlocillin were 1.35 h and 1.38 h, respectively. The half-lives for cephalothin and sisomicin were 0.65 h and 5.7 h, respectively.

Animals↗
PubMed1982

[Studies with azlocillin, mezlocillin, penicillin-g-potassium and sisomicin on tolerance in the cornea and the kinetics of inhibiting concentrations in the cornea and aqueous humor in rabbits].

We studied the effect of azlocillin, mezlocillin and sisomicin in concentrations of 1, 2.5 and 5% on the regeneration of stromal corneal wounds in rabbits following subconjunctival injections and treatment with eye drops. Concentrations of the antibiotics were also determined in corneal tissue and in aqueous humor and compared with that of penicillin G-potassium. Together with azlocillin, sisomicin proved to be the most effective and the safest. Mezlocillin only inhibited wound regeneration slightly and thus mezlocillin appears to be inferior to the other two antibiotics investigated in the local treatment of the eye.

Animals↗
PubMed1983

The combined action of azlocillin and sisomicin in a model simulating the in vivo serum kinetics.

The in vivo serum kinetics of azlocillin and sisomicin were simulated in a new in vitro test model. A strong synergistic effect against Pseudomonas aeruginosa resulted when both compounds were administered simultaneously and eliminated according to their individual half-life values, even when the decreasing drug concentrations exceeded the MICs for only a short period of time. When applied at intervals, neither pretreatment with azlocillin nor with sisomicin blocked the antibacterial activity of the combination partner.

Azlocillin↗
PubMedDate not supplied

Comparative efficacy of ciprofloxacin, azlocillin, imipenem/cilastatin and tobramycin in a model of experimental septicemia due to Pseudomonas aeruginosa in neutropenic mice.

The in vivo activity of ciprofloxacin against Pseudomonas aeruginosa was studied in a septicemia model in neutropenic mice and compared to that of other antibiotics with established activity against P. aeruginosa. When given as a single agent, ciprofloxacin proved to be as effective as imipenem/cilastatin, whereas azlocillin and tobramycin were rather ineffective. After infection with higher challenge inocula, combinations of two (synergistic) antibiotics were more effective than single agent therapy in most instances. The combination of ciprofloxacin with azlocillin was at least as effective as that of imipenem/cilastatin with tobramycin. Selection of mutants with decreased sensitivity to ciprofloxacin occurred during therapy, however, post-therapy MICs of ciprofloxacin did not exceed a level of 1 mg/l and rises of MICs did not detrimentally influence treatment outcome. Taken together with the results of earlier studies, our data encourage the use of ciprofloxacin in gram-negative septicemia in neutropenic patients.

Agranulocytosis↗
PubMed1985

Azlocillin levels in human tears and aqueous humor.

We administered 4 g of azlocillin sodium intravenously to 24 patients scheduled to undergo elective intraocular surgery and collected specimens of serum, tears, and aqueous humor from zero to six hours after infusion for assay by high-pressure liquid chromatography. We found that azlocillin is distributed into tears and penetrates into the aqueous humor of human volunteers with noninflamed eyes after a single intravenous dose. Levels of 4.17 micrograms/ml and 4.44 micrograms/ml were achieved in tears and aqueous humor, respectively.

Aqueous Humor↗
PubMed1990

Ceftriaxone vs. azlocillin and netilmicin in the treatment of febrile neutropenic children.

Efficacy of the cephalosporin, ceftriaxone, was compared with that of the combination of the aminoglycoside, netilmicin, and the penicillin, azlocillin, in the treatment of febrile episodes in immunocompromised neutropenic children undergoing chemotherapy for neoplastic disease. During 100 separate febrile episodes, 40 strains of bacteria were isolated from the blood of 34 patients and a further 55 strains from other sites. Nine strains (four of which were staphylococci) to both netilmicin and azlocillin. There was no difference in clinical response between the two therapeutic regimens as assessed 4 and 7 days after treatment began. Ceftriaxone had the considerable practical advantages of once daily dosage without a need for blood monitoring. Ceftriaxone would appear to be effective as initial monotherapy in the treatment of bacterial infections in severely neutropenic children.

Adolescent↗
PubMed1989

Evaluation of azlocillin-amikacin combination for empirical therapy of infection in febrile neutropenic patients.

We have evaluated the azlocillin-amikacin combination, given at a daily dose of 200 mg/kg and 15 mg/kg respectively, in the treatment of 62 consecutive febrile granulocytopenic patients (less than 500 PMN/microliters) affected by hematological disease. The effectiveness of the treatment was assessed in 60 patients, 44 (73%) of whom responded within 96 hours from the beginning. 36 of the responders showed microbiological and clinical infections, 2 had clinically documented pneumonia and 6 a possible infection. No improvement was obtained in 16 patients; 7 of whom suffered from clinical and microbiological infection, 2 from pulmonary mycosis, 4 from possible infection and 3 from doubtful infection. Seven of these patients subsequently responded to a proven antibiotic treatment, while only one of the remaining responded to a second-line empirical antibiotic schedule. These results suggest that the combination of azlocillin-amikacin was able to overcome about two-thirds of the infections, representing an effective remedy for the empiric treatment of febrile neutropenic patients.

Adolescent↗
PubMedDate not supplied

The acylampicillins: mezlocillin, piperacillin, and azlocillin.

The new acylampicillin derivatives azlocillin, mezlocillin, and piperacillin have an increased activity against many gram-negative bacilli, especially Klebsiella pneumoniae, Serratia marcescens, and Pseudomonas aeruginosa, when compared with the carboxypenicillins carbenicillin and ticarcillin. The new penicillins show synergistic activity in combination with aminoglycosides but, when combined with other beta-lactams, may be synergistic (piperacillin and moxalactam; mezlocillin and cefoperazone), indifferent, or antagonistic (azlocillin, mezlocillin, or piperacillin and cefoxitin or cefamandole). The in vitro activity of these agents, either alone or in combination, appears to correlate with in vivo efficacy in animal models. The new penicillins are clinically effective for a very broad range of infections, including life-threatening nosocomial infections. Adverse effects with these, as with other semisynthetic penicillins, are minimal. Attention must be paid to the potential for infection by naturally resistant, gram-negative bacilli such as beta-lactamase-producing Escherichia coli and for the emergence of resistance during therapy. The granulocytopenic patient should receive these agents only in conjunction with another agent, such as an aminoglycoside; this combination will often result in a synergistic effect when tested in vitro. The carboxypenicillins and the newer penicillins have substantial similarities, and prospective, comparative studies have so far failed to demonstrate significant clinical superiority. However, the increased activity of the acylampicillins may be advantageous for the treatment of infections due to K. pneumoniae and P. aeruginosa.

Agranulocytosis↗
PubMed1983

Pharmacokinetics of azlocillin after discontinuous intravenous administration of high dose.

Azlocillin, an acylureido-penicillin, is often used in severe, and sometimes in life-threatening infections because of its good therapeutic effect, even against bacteria resistant to many other agents. In these patients sometimes doses of 10 g may be administered in order to improve therapeutic efficacy. In this study the serum concentrations and urinary excretion of azlocillin were investigated in 2 volunteers and 11 patients after the intravenous injection (5 min) of 2 g followed by intravenous infusion of 8 g over 4 h. The serum concentrations increased during infusion in volunteers and patients from a median value of 180 mg/l up to 317 mg/l. After the end of infusion the median concentrations fell through 94 mg/l at 2 h, and 43 mg/l at 4 h to 11 mg/l at 6 h. The median cumulative urinary excretions in patients were 2.50 g up to 4 h, 4.51 g up to 8 h, 4.89 g up to 12 h, and 5.43 g up to 24 h after the end of infusion. The median plasma half-life calculated from the last five serum concentrations (6-10 h after start of administration) was 100 min (range 60-180 min). The study showed that using this dose and mode of administration high serum concentrations can be maintained over many hours, which would be sufficient to treat life-threatening or difficult infections. The dose interval would have to be 12 h. The local and systemic tolerability was good, as shown by the laboratory parameters measured.

Adult↗
PubMed1983

An azlocillin dosing nomogram for renal insufficiency.

We have developed an azlocillin dosing nomogram suitable for use in patients with various degrees of renal functional impairment. A total of 50 kinetic studies undertaken by us and an additional 60 similar kinetic investigations as reported in the literature formed the basis for the construction of our nomogram. This renal failure dosing nomogram gives immediate information to the physician who needs to give azlocillin to a patient with renal failure.

Azlocillin↗