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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↗
PubMed1986

Control of Pseudomonas sepsis in mice with azlocillin combined with gentamicin.

The antibacterial activity of azlocillin VUFB and gentamicin was tested in vivo. To mice with Pseudomonas sepsis the test substances were injected either alone or combined, and the mortality was assessed. The test substances were freeze dried injectable azlocillin and gentamicin (Pharmachim). Azlocillin was injected into mice either intravenously or intramuscularly in graduated doses of 50-500 mg/kg once daily. The therapeutic effect was assessed on the basis of survival of the treated mice. Our expectation of a potentiated effect of the azlocillin-gentamicin combination was confirmed. After intramuscular administration of azlocillin plus gentamicin 90% of the mice survived, in comparison with 40% only after either azlocillin or gentamicin alone.

Animals↗
PubMed1984

[Pseudomonas aeruginosa meningitis treated with azlocillin. 5 cases].

Prior to the introduction of new beta-lactam antibiotics, such as ureidopenicillins and some third generation cephalosporins, the choice of antibiotics for the treatment of meningitis caused by Ps. aeruginosa was limited, and even now, this infection remains of poor prognosis. Five patients with meningitis, aged from 18 to 75 years, were treated with azlocillin. The strains of Ps. aeruginosa isolated were all sensitive to azlocillin, the zones of inhibition being greater than 20 mm in diameter with bacteriostatic concentrations. Azlocillin was administered 8-hourly by intravenous injection in doses of 30 g/day in 3 cases and 15 g/day in 2 cases. The mean duration of treatment was 33 days (range 23-50 days). In addition to azlocillin 4 patients received an aminoglycoside (tobramycin or amikacin) parenterally and, in one case, intrathecally. Four patients underwent a surgical operation on the focus of infection between the 9th and 13th days of treatment. In 3 of these 4 patients surgery was necessary to obtain apyrexia, but in all cases the CSF was already sterile when it was performed. The outcome was favourable in all 5 cases. One patient relapsed on 4 occasions due to persistent petrous bone fistula; each time, the azlocillin treatment was reinstituted and brought about clinical and bacteriological cure. The germ was eradicated in CSF on the 3rd day of treatment in 3 patients and on the 7th day in one. One patient developed transient eosinophilia and another, transient neutropenia after 30 days. It is concluded that azlocillin, associated with an aminoglycoside, is an active and effective antibiotic for the treatment of Ps. aeruginosa meningitis.

Adolescent↗
PubMed1984

[Role of azlocillin in the treatment of Pseudomonas urinary infections].

Ten cases of urinary tract infection (6 acute and 3 relapsing) treated with azlocillin are reported. Nine patients had a history of urinary tract catheterization or in-dwelling catheter and 6 had previously undergone surgery. Prior to receiving azlocillin, 6 of the patients had been unsuccessfully treated with other antibiotics. Renal function was altered in 6 cases. Azlocillin was administered intravenously in doses of 5 grams three times or twice a day for periods ranging from 8 days (in 2 cases) to 26 days. The antibiotic was given alone in all but 2 cases where it was associated with amikacin. Excellent clinical and bacteriological results were obtained in 9 of the 10 cases, with only one failure. No local, systemic or biochemical side-effect was recorded. Bacteriological results were most satisfactory. The minimum inhibitory concentrations of azlocillin were lower than those of carbenicillin in all cases. Sensitivity of azlocillin was even good in 3 and intermediate in 2 of the 5 cases where Pseudomonas was indifferent or resistant to carbenicillin. In spite of the small number of cases in this series, these results indicate that azlocillin ranks among antibiotics that are effective in urinary tract infections due to Pseudomonas.

Adolescent↗
PubMed1983

In vitro activity of azlocillin, metronidazole and its hydroxy metabolite against anaerobes. Bacteriostatic synergism studies.

The in vitro inhibitory activity of azlocillin (Securopen), metronidazole (Cloni) and its hydroxy metabolite was determined against 27 gram-negative and 13 gram-positive species of anaerobes by means of agar dilution tests. The 63 anaerobic strains were also tested against the pairs azlocillin-metronidazole and azlocillin-hydroxy metabolite by means of agar dilution tests. Gram-negative species (Bacteroides spp., Fusobacterium spp. etc.) were inhibited by 0.125-256 micrograms/ml azlocillin, 0.01-4 micrograms/ml metronidazole and 0.01-4 micrograms/ml hydroxy metabolite. With gram-positive anaerobes (Clostridium spp., Peptococcaceae etc.) the MIC ranges were 0.125-4 micrograms/ml for azlocillin, 0.03-1 micrograms/ml for metronidazole and 0.125-2 micrograms/ml for the hydroxy metabolite. A synergistic effect was observed exclusively with gram-negative anaerobes (Bacteroides fragilis, B. thetaiotaomicron, B. disiens etc.). There were few instances of antagonism, likewise with gram-negative species. The preponderant combination effect against gram-positive anaerobes was addition. In view of the broad antiaerobic spectrum of azlocillin, the present in vitro findings do not preclude combined therapy with metronidazole in cases of anaerobic-aerobic poly-bacterial infections.

Anaerobiosis↗
PubMed1978

Synergy of azlocillin and mezlocillin combined with aminoglycoside antibiotics and cephalosporins.

Synergistic activity between both azlocillin and mezlocillin and aminoglycosides or cefazolin could be demonstrated by checkerboard dilution, isobologram, and killing curve techniques. Azlocillin and mezlocillin combined with gentamicin, netilmicin, or amikacin were synergistic against Escherichia coli, Klebsiella, Citrobacter, Enterobacter, Serratia, and indole-positive Proteus. Synergy was observed with isolates that were susceptible or resistant to azlocillin or mezlocillin. Synergy was seen most often when azlocillin or mezlocillin were combined with amikacin, gentamicin, or netilmicin against Pseudomonas aeruginosa. The combination of mezlocillin and an aminoglycoside produced synergy more often than did carbenicillin plus an aminoglycoside. No antagonism was seen when aminoglycoside antibiotics were combined with azlocillin or mezlocillin. Cefazolin was synergistic against Pseudomonas, Providencia, P. mirabilis, indole-positive Proteus, Citrobacter, Klebsiella, and Escherichia coli, when combined with azlocillin or mezlocillin. However, the combination of either agent with cefazolin was antagonistic when tested against selected indole-positive Proteus and Enterobacter isolates.

Aminoglycosides↗
PubMed1982

Combined action of decreasing concentrations of azlocillin and sisomicin on Pseudomonas aeruginosa as assessed in a dynamic in vitro model.

The effect of decreasing concentrations of azlocillin and sisomicin on Pseudomonas aeruginosa was examined. Logarithmically growing bacterial cultures were incubated in an ultrafiltration cell, and after adding the antibiotics, the culture medium was diluted every 20 min without any decrease in cell density. The turn-over of medium resulted in the elimination of azlocillin with a half-life of 75 min. This simulated serum kinetics in vivo. When testing sisomicin, small amounts of this agent were added during every dilution step to achieve a half-life of 120 min. Growth conditions were comparable in all experiments. The simultaneous combination of azlocillin and sisomicin resulted in strong synergism as assessed by higher killing rates and more prolonged growth inhibition of surviving bacteria. Comparable results were observed when both drugs were added at intervals of 40 min. When applied at intervals of 120 min, the combined effect of azlocillin and sisomicin was reduced, but still superior to the effect of double the concentration of each compound alone. Thus, neither pre-treatment with azlocillin nor with sisomicin impaired the antibacterial activity of the combination partner. This seems to be of clinical importance since the agents may be administered at different times during combined therapy.

Azlocillin↗
PubMed1986

Synergy of ciprofloxacin and azlocillin in vitro and in a neutropenic mouse model of infection.

Combinations of ciprofloxacin with azlocillin, piperacillin and ticarcillin were tested in vitro against clinical isolates. Azlocillin plus ciprofloxacin showed synergy against 30% of Pseudomonas aeruginosa isolates; it was either synergistic or additive against 78% of all isolates tested even those resistant to the beta-lactam. Synergism was rarely noted for Klebsiella pneumoniae, Escherichia coli, Enterobacter spp. or Branhamella spp. isolates. Minimum inhibitory concentrations of ciprofloxacin plus azlocillin, plus piperacillin and plus ticarcillin against Pseudomonas spp. were reduced 4 or 2 fold, respectively. However, the combination azlocillin plus ciprofloxacin showed primarily indifference against gram-positive strains. Neutropenic mice infected with a lethal challenge of Pseudomonas spp. were protected by a combination of azlocillin and ciprofloxacin. Its additive and/or synergistic effects and expanded spectrum of activity against streptococci, methicillin-resistant staphylococci and JK corynebacteria may provide an alternative to traditional therapy.

Animals↗
PubMed1983

Treatment of serious Pseudomonas infections with azlocillin.

Azlocillin is a semisynthetic acylureidopenicillin with increased activity against most strains of Pseudomonas aeruginosa. It was given as the sole antibacterial agent in the treatment of 21 patients with serious pulmonary, wound, bone or joint, or urinary tract infections, endocarditis, or malignant external otitis caused by Pseudomonas sp. In preliminary in vitro tests, azlocillin inhibited 90% of 36 clinical isolates, while carbenicillin and ticarcillin inhibited only 60% and 73%, respectively. Mean MIC of azlocillin against Ps. aeruginosa isolated from the 21 study patients was 9.8 mg/l; more than 50% of the strains were inhibited by a concentration of 6.25 mg/l. Intravenous administration of the antibiotic at a mean dosage of 17 g/day for 6 to 59 days resulted in an excellent or good clinical response in 90% (19) of the patients treated. Pseudomonas sp. was eliminated from the site of infection in 67% (14) of the patients. Azlocillin therapy was well tolerated; in only two patients, both of whom had penicillin-type rashes, was it necessary to discontinue therapy. Azlocillin was a safe and effective antimicrobial agent for the treatment of serious infections caused by strains of Pseudomonas sp., primarily Ps. aeruginosa.

Adult↗
PubMed1983

A comparative study of the efficacy and safety of azlocillin and gentamicin in the treatment of serious infections.

Azlocillin, a new semisynthetic ureidopenicillin, has increased in-vitro activity against Pseudomonas aeruginosa and good activity against other Gram-negative organisms. In a comparative clinical study, azlocillin was administered intravenously at 18 g/day to 24 patients and gentamicin intramuscularly at 3 to 5 mg/kg/day to 25 patients, most of whom had infections of the skin and skin structure, intra-abdominal cavity, or lower respiratory tract. Gram-negative organisms, usually Ps. aeruginosa or Escherichia coli, and Staphylococcus aureus, were isolated most frequently. At the end of therapy, 18/24 (75%) of the patients with one infection site had an excellent clinical response after azlocillin, as compared with 7/20 (35%) after gentamicin (P = 0.014). The overall response to treatment was cure in 17/24 (70.8%) of the azlocillin patients and 9/24 (37.5%) of the gentamicin patients (P = 0.042). Bacteriological response was in the azlocillin group 28/33 or 84.8% as compared to the gentamicin group 38/51 or 74.5%.

Adolescent↗
PubMed1983

Azlocillin: a new broad spectrum penicillin.

Azlocillin is a new semisynthetic penicillin with a broad spectrum of antibacterial activity. Azlocillin is highly active against Pseudomonas aeruginosa including many strains that are resistant to carbenicillin and ticarcillin. Unlike many other penicillins with activity against Enterobacteriaceae and Pseudomonas, azlocillin retains a high degree of potency against Gram-positive organisms, fastidious Gram-negative organisms, and many obligate anaerobes. Because azlocillin is susceptible to certain beta-lactamases it is not highly active against bacteria that are resistant to other penicillins and/or cephalosporins due to the production of such enzymes. Like other penicillins, azlocillin is bactericidal for susceptible strains. It also interacts synergistically with aminoglycosides against enterococci, certain Enterobacteriaceae, and Ps. aeruginosa.

Azlocillin↗
PubMed1986

Behaviour of TEM-1 beta-lactamase as a resistance mechanism to ampicillin, mezlocillin and azlocillin in Escherichia coli.

Escherichia coli isolates which synthesised the extremely common 'TEM-1' plasmid mediated beta-lactamase were more resistant to the alpha-aminopenicillins, ampicillin, mezlocillin and azlocillin, than were strains which lacked this enzyme. However, many TEM-1+ isolates remained sensitive to therapeutic concentrations of mezlocillin (less than 64 mg/l), whereas virtually none was susceptible to such levels of ampicillin or azlocillin. Transconjugants of E. coli K12 into which we introduced various TEM-1 coding plasmids similarly acquired lower levels of resistance to mezlocillin than to ampicillin and azlocillin. Those which expressed relatively small amounts of enzyme remained sensitive to 64 mg/l of mezlocillin, whereas they were substantially resistant (MIC greater than 64 mg/l) to the other alpha-aminopenicillins. These data suggested that the enzyme afforded weaker protection against mezlocillin than against azlocillin and ampicillin and we attempted to relate this finding to its hydrolytic activity. Extracted TEM-1 beta-lactamase hydrolysed high concentrations of mezlocillin more rapidly than ampicillin and azlocillin; however, mezlocillin was calculated to be the weakest substrate at the low concentrations which are likely to be obtainable in the bacterial cell. These data may partly account for the residual activity of mezlocillin against enzyme producers, but target and permeability factors probably also contribute.

Ampicillin↗
PubMed1983

The response of Pseudomonas aeruginosa to azlocillin, ticarcillin and cefsulodin.

The morphological response of Pseudomonas aeruginosa to azlocillin, ticarcillin and cefsulodin was investigated by electron microscopy. Each antibiotic initially caused the formation of filaments. On further incubation in the presence of azlocillin, deposits of dense intracellular material were observed; these were absent from cells exposed to the other two antibiotics. On continued incubation, lysis of the filaments occurred, but the mode of lysis differed between the antibiotics: azlocillin caused breakage at a restricted number of sites in the cell wall, ticarcillin produced breakage at many points and cefsulodin caused extensive cell-wall damage. In addition, ticarcillin and cefsulodin appeared to cause more lysis and spheroplast formation than did azlocillin. The morphological changes correlated with turbidimetric measurements of bacterial response to the three antibiotics, which showed ticarcillin and cefsulodin to act more rapidly than azlocillin.

Azlocillin↗
PubMed1980

Comparative bactericidal effects of azlocillin and ticarcillin against Pseudomonas aeruginosa.

Azlocillin was relatively ineffective against actively growing cultures of Pseudomonas aeruginosa in tests of bacteriolytic and bactericidal activity in which ticarcillin demonstrated pronounced bactericidal effects over a wide range of concentrations. Microscopic observation showed that azlocillin generally induced the formation of filamentous cells of P. aeruginosa which lysed only slowly, but ticarcillin caused the production of spheroplasts and subsequent rapid lysis. During the course of the bactericidal tests, azlocillin was inactivated, presumably by the beta-lactamase produced by P. aeruginosa, and the filamentous cells resumed normal cell division and growth. In contrast, there was no loss of ticarcillin activity, and there was no evidence of resumption of growth of P. aeruginosa in the presence of ticarcillin. These results suggest that the different bactericidal effects demonstrated by azlocillin and ticarcillin against P. aeruginosa are related primarily to dose-related differences in inhibition of cell wall synthesis and secondarily to the instability of azlocillin to pseudomonal beta-lactamase.

Azlocillin↗
PubMed1984

Azlocillin pharmacokinetics in patients with cystic fibrosis.

The pharmacokinetics of azlocillin were studied in 10 cystic fibrosis patients, ranging in age from 11 to 28 years. The patients received a 9- to 23-day course of 350 mg of azlocillin per kg in four or six divided daily doses in combination with am aminoglycoside. Blood and urine samples were collected at specified times after the last dose of the course of azlocillin therapy and then assayed for azlocillin content. Pharmacokinetic parameters were determined by noncompartmental analysis. Mean values for serum half-life (1.74 h), disposition constant (0.41 h-1), total body clearance (123 ml/kg per h), and renal clearance (58 ml/kg per h) were determined. All patients exhibited improvement with respect to clinical and laboratory parameters and displayed no adverse reactions. The pharmacokinetic analysis offers further evidence of the dose-dependent nature of azlocillin elimination, but elimination did not appear to be altered in cystic fibrosis patients.

Adolescent↗
PubMed1980

Azlocillin in respiratory tract infections with Pseudomonas aeruginosa in children with cystic fibrosis.

In 5 children with cystic fibrosis, 13 courses of lower respiratory infections due to Pseudomonas aeruginosa were treated with azlocillin, 100--200 mg/kg body weight intravenously every 8 h for 10--15 days. The clinical course during azlocillin treatment was more favourable than had been the case previously in the same patients when treated with combinations of carbenicillin and aminoglycosides. No side effects ascribable to azlocillin were observed, although one allergic reaction occurred, but this was probably elicited by another allergen. Upon repeated courses of treatment, the minimum inhibitory concentration of the infecting organisms increased steadily against both azlocillin and carbenicillin. It is concluded that azlocillin represents an important alternative in the treatment of lower respiratory tract infections due to P. aeruginosa in patients with cystic fibrosis.

Adolescent↗
PubMed1988

Azlocillin and mezlocillin concentration in human prostatic tissue.

The concentrations of azlocillin and mezlocillin in human prostatic tissue obtained by transurethral resection or enucleation were measured after two 2.0-gram doses of either drug. The average plasma concentration of azlocillin and mezlocillin at time of tissue sampling was 64.9 and 36.3 micrograms/ml, respectively, and tissue concentration at the time of sampling was 22.9 micrograms/g for azlocillin and 9.4 micrograms/g for mezlocillin. The plasma/tissue concentration ratio for mezlocillin was 0.25 and for azlocillin 0.35. Concentrations of mezlocillin in tissue obtained by transurethral resection were similar to those obtained by enucleation. Azlocillin and mezlocillin in appropriate doses achieve a concentration in human prostatic tissue above the inhibitory concentration for common bacterial pathogens.

Aged↗
PubMed1984

[Pharmacokinetics of azlocillin in chronic renal failure and hemodialysis patients].

The pharmacokinetics of azlocillin were studied in 16 patients with varying degrees of renal impairment (creatinine clearance Ccr ranging from 0 to 52 ml/min/1.73 m2) and on and off sessions in 4 of these patients on periodical haemodialysis. A single dose of azlocillin 80 mg/kg was given by intravenous infusion over 30 min. Maximum concentrations in the sera of patients with renal impairment were the same as in normal subjects, ranging from 300 to 400 micrograms/ml. The elimination half-life (t 1/2) increased as renal function deteriorated, with values of 1.11 h in subjects with healthy kidneys to 5.66 h in patients with Ccr less than 15 ml/min (maximum 8.38 h). The apparent volume of distribution (Vd) was unchanged in patients with renal impairment but was significantly increased in patients on haemodialysis. The mean percentage of the dose administered excreted in the urines decreased from 60-70% in normal subjects to about 11% in patients with severe renal failure, but urinary concentrations remained above therapeutic levels. The extra-renal elimination of azlocillin was unmodified by renal impairment. Azlocillin is easily removed by dialysis: t 1/2 values between and during 6 h sessions of haemodialysis were 6.55 h and 2.81 h respectively, corresponding to a 45.8% extraction on the dialyser. These results are comparable to those found in the literature and can be used as a basis for adjusting azlocillin dosage to the degree of renal function.

Adolescent↗