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PubMed1984

[Use of azlocillin in the treatment of Pseudomonas bronchopulmonary infections].

Eleven patients with severe bronchopulmonary infection due to Pseudomonas were treated with azlocillin in doses of 250 mg/kg/day. Severe preexisting respiratory diseases, such as bronchopulmonary carcinoma, bronchiectasis or respiratory insufficiency were present in all cases. All patients had been unsuccessfully treated with various antibiotics before they received azlocillin. The pathogenicity of the isolates was assessed by germ counts in sputum. Comparative in vitro sensitivities to carbenicillin and azlocillin were determined by the disc method and by measurement of the minimum inhibitory concentrations in liquid medium. All strains of Pseudomonas aeruginosa isolated were sensitive to azlocillin with minimum inhibitory concentrations of 0.5 to 64 micrograms/ml. When tested against carbenicillin, 4 of the strains were resistant and 1 had intermediate sensitivity. The carbenicillin/azlocillin minimum inhibitory concentrations ratio was usually equal to 4. Clinical results were satisfactory in 7 cases; inadequate response or failure was observed in 4 cases and attributed to the replacement of Pseudomonas by another pathogen (Proteus morganii or Klebsiella pneumoniae). This study suggests that azlocillin is of value in the treatment of bronchopulmonary infections caused by Ps. aeruginosa.

Adult↗
PubMed1984

[Comparative activity of azlocillin on Pseudomonas species excluding Pseudomonas aeruginosa].

The minimal inhibitory concentrations (MIC) of three acylureidopenicillins (azlocillin, mezlocillin, piperacillin) and three third generation cephalosporins (cefotaxime, cefoperazone, cefsulodin) against 249 randomized strains of Pseudomonas spp. representing 10 species other than Pseudomonas aeruginosa, were determined by the agar dilution method in Mueller-Hinton agar and compared by parametric statistical tests. Fresh clinical and environmental hospital isolates belonged to the following species: P. fluorescens (35), P. putida (37), P. stutzeri (17), P. mendocina (4), P. cepacia (37), P. pickettii (22), P. acidovorans (36), P. diminuta (5), P. paucimobilis (23), P. maltophilia (37). Azlocillin inhibited over 88% of Pseudomonas spp at 64 mg/l or less. This good antipseudomonal activity in vitro was comparable to those of piperacillin and cefotaxime with a minimal inhibitory concentrations 50 value of 8 mg/l. Against these Pseudomonas spp, the ranking order of activity was azlocillin = piperacillin = cefotaxime greater than cefoperazone greater than mezlocillin greater than cefsulodin. Like piperacillin or cefotaxime, azlocillin, was effective against ticarcillin--and aminoglycoside--resistant Pseudomonas spp. Against P. maltophilia and P. cepacia, the two Pseudomonas spp other than P. aeruginosa that are important pathogens in opportunistic infections and in their vast majority are resistant to amino glycosides, azlocillin was significantly active. Only in the case of P. maltophilia, cefoperazone had a lower minimal inhibitory concentrations 50 (8 mg/l vs. 32 mg/l).

Anti-Bacterial Agents↗
PubMed1981

[Bactericidal activity against P. aeruginosa in serum and bronchial secretion in patients under continuous infusion of azlocillin].

The azlocillin level and killing activity in serum and bronchial secretions against 10 strains of P. aeruginosa were studied in 7 intubated or tracheotomized patients with severe bronchial infection who were receiving the drug as continuous i.v. infusion. In 5 out of 7 patients azlocillin was absent or present only in traces in bronchial secretions in spite of plasma levels ranging between 170 to 340 micrograms/ml. In the other 3 patients azlocillin levels of 23 and 39 micrograms/ml and moderate bactericidal activity against P. aeruginosa could be detected in bronchial secretions. Penicillinase producing strains of Staph. aureus were isolated from the sputum of the 5 patients with extremely low azlocillin level in bronchial secretions. The strain of Staph. aureus isolated from one patient was shown to destroy azlocillin rapidly. In bronchopulmonary infections, Staph. aureus may not only be directly pathogenic but also interfere with the action of beta-lactamase unstable drugs against other microorganisms.

Azlocillin↗
PubMed1981

Azlocillin with and without an aminoglycoside against respiratory tract infections in children with cystic fibrosis.

Nine patients with cystic fibrosis have been treated with azlocillin alone and later with azlocillin combined with an aminoglycoside (gentamicin or tobramycin) for 50 treatment courses. In the initial series when azlocillin was employed alone, a gradual increase in MIC during successive courses was observed in Pseudomonas aeruginosa. When the beta-lactam antibiotic was combined with an aminoglycoside, the MIC was either maintained or reduced. Objective criteria like peak expiratory flow, erythrocyte sedimentation rate, fever, body weight or bacterial cultures could not clearly identify the combination therapy as better clinically than azlocillin monotherapy. However, the patients subjective and our clinical impression is that the combination therapy was better. The clinical course and the lack of increased resistance on combination therapy make a combination of azlocillin and an aminoglycoside preferable to the beta-lactam alone.

Aminoglycosides↗
PubMed1993

[Therapeutic effect of azlocillin and its combinations with other antibiotics in experimental plague infection].

The therapeutic effect of azlocillin and its combinations with other antibiotics was studied in a model of experimental plague of albino mice. Azlocillin was shown to be efficient in the prophylaxis and treatment of the experimental plague infection. The optimal doses of azlocillin were determined. The protective action of the drug depended on the dose and the time of its administration. The therapeutic effect was mainly defined by the antibiotic dose. The use of azlocillin in not sufficiently active doses in combination with aminoglycosides (gentamicin, sisomicin and amikacin), rifampicin or doxycycline significantly increased the percentage of the animal survival by comparison with that after the use of every antibiotic alone. A synergistic effect was observed when azlocillin was used in combination with rifampicin or amikacin.

Aminoglycosides↗
PubMed1977

[Azlocillin and mezlocillin: two new semisynthetic acylureido-penicillins (author's transl)].

The pharmacokinetic parameters of two new ureido-penicillins (azlocillin and mezlocillin) were determined in 12 healthy subjects after a half-hour continuous infusion of 5,000 mg. The agar diffusion test (test strain Bacillus subtilis ATCC 6633) was used for the microbiological assays. The mean azlocillin serum concentration after the half-hour infusion was 431.0 +/- 75.0 microgram/ml; after eight hours it had fallen to a mean value of 4.7 +/- 2.6 microngram/ml. The mean elimination half-life was 77.5 +/- 10.4 minutes, and the relative distribution volume was 19.4 +/- 1.9% of the bodyweight. At the end of the infusion, mezlocillin showed a mean serum concentration of 426.0 +/- 61.0 microgram/ml and after eight hours an average of 1.1 +/-0.9 microgram/ml; the half-life was shorter (56.9 +/- 9.9 minutes) and the distribution volume lower (14.8 +/- 3.1%) than that of azlocillin. The renal clearance values measured in three subjects during a four-hour continuous infusion were: azlocillin 111.6 ml/min/1.73 m2, mezlocillin 121.5 ml/min/1.73 m2. The kinetic behaviour of the two ureido-penicillins was essentially very similar to that of ampicillin and carbenicillin, 38 patients with bronchopneumonia, cholangitis or urinary tract infections, which in some instances were severe, were treated for an average of 10 days with an average daily dosage of 3X4.0 g azlocillin or 3X5.0 g mezlocillin. 30 patients showed clinical improvement, and in 17 of these the pathogen was eliminated. These therapeutic results appear more favourable than those obtained with the newer aminoglycoside antibiotics (amikacin, sisomicin); in particular the drug was well tolerated.

Adult↗
PubMed1977

Azlocillin: in vitro studies of a new semisynthetic penicillin.

The activity of azlocillin, a new semisynthetic penicillin, was determined against 582 clinical isolates of gram-negative bacilli and gram-positive cocci. Over 75% of the isolates of Pseudomonas aeruginosa were inhibited at a concentration of 12.5 mug or less per ml. Azlocillin is also active against indole-negative and -positive Proteus spp., inhibiting 98 and 71%, respectively, at a concentration of 12.5 mug or less per ml. Isolates of Klebsiella spp. and Enterobacter spp. showed less susceptibility than isolates of Escherichia coli and Serratia spp. Gram-positive cocci except penicillin G-resistant Staphylococcus aureus were susceptible to azlocillin. Azlocillin failed to inhibit the growth of gram-negative bacilli when large inocula were used. It was more active in alkaline pH, but the type of medium used had little effect on its activity. Azlocillin was more active than mezlocillin, ticarcillin, and carbenicillin and as active as BLP-1654 against isolates of P. aeruginosa. It was not as active as mezlocillin against the majority of the other gram-negative bacilli.

Bacteria↗
PubMed1978

Pharmacokinetics of azlocillin in persons with normal and impaired renal functions.

The pharmacokinetics of azlocillin, a new wide-spectrum antibiotic of the N-substituted group of ureidomethyl penicillins, was investigated in 10 subjects with normal and in 32 subjects with impaired renal functions. After intravenous injection of 2 g of azlocillin, serum concentrations of drug were measured microbiologically. The half-lives of azlocillin were 47 +/- 8.8 min in patients with normal renal function, and 293.3 min in patients with severely impaired renal function. The correlation of half-life to renal functions is shown by the equation: t/2 = 425.03.Cl(In) (-0.4509), where Cl(In) is inulin clearance. The volume of distribution of the azlocillin was 17.7% of the body weight. Protein binding was similar in patients with normal renal function and in those with severely impaired renal functions. The urinary excretion rate of azlocillin in patients with normal renal function was 64.8 +/- 8.8% in 24 h.

Adolescent↗
PubMed1987

The novel therapeutic implications of azlocillin's dose-dependent pharmacokinetics: contributing physiologic mechanisms and a prospective, cross-over designed trial.

Azlocillin is an important acylureido penicillin antibiotic for the management of complex gram-negative infections particularly those caused by Pseudomonas species. The current studies demonstrate that it manifests dose-dependent pharmacokinetics during the usual regimens of clinical dosing, that enterohepatic recirculation does not occur and that renal tubular secretion (maximum renal tubular secretory capacity 300 +/- 30 micrograms/min) and hepatic metabolism appear to be the dominant contributors to the dose-dependent nature of azlocillin. The possible therapeutic implications of azlocillin's dose dependency were evaluated by undertaking a six-day randomized, prospective, cross-over design study to evaluate the pharmacokinetic disposition of the drug during a 3-g q4h (typically used in adults) regimen versus a 5-g q8h regimen. By using the area under the serum-time concentration curve (AUC) as the major comparative parameter for these two regimens, the results demonstrate that both regimens provide approximately equal quantitative amounts of the drug systemically as a result of azlocillin's dose dependency. The AUC values, although not therapeutic end points, nonetheless correlate well with clinical response to antibiotic therapy. The 5-g q8h regimen was well tolerated. It is less disruptive for patients, requires half the number of intravenous administrations, 17% less drug, and is more cost effective than the 3-g q4h regimen.

Adult↗
PubMed1982

[Azlocillin--a new anti-pseudomonas penicillin. A review of the literature and pharmacokinetic studies].

We studied the pharmacokinetics of azlocillin in 11 healthy persons following an i. v. infusion of 5 g over 30 minutes. The azlocillin concentrations in serum and urine were measured microbiologically. The serum concentrations averaged 530.5 (+/- 79.2) mg/l at the end of the infusion and 9.4 (+/- 4.3) mg/l six hours later. 73.8% of the dose was excreted in the urine during a period of six hours. The serum concentrations of azlocillin were analysed using a two-compartment model, and the pharmacokinetic constants were calculated by a computer. The average biological half-life (beta-phase) of azlocillin was 70.2 (+/- 7.8) min, the plasma clearance was 1.869 (+/- 0.284) ml/sec and the distribution volume (Vd area) was 11.34 (+/- 2.05) l, i. e. 0.17 l/kg.

Adult↗
PubMed1987

In vivo and in vitro activity of ciprofloxacin plus azlocillin against 12 streptococcal isolates in a neutropenic site model.

Closed-space neutropenic infection sites were simulated in rabbits by subcutaneous semipermeable chambers that were inoculated with 5 X 10(4) CFU/ml of various strains of Streptococcus pneumoniae, Streptococcus faecalis, and Streptococcus avium. Four hours after inoculation, treatment was begun with ciprofloxacin, 10 or 30 mg/kg, azlocillin, 100 mg/kg, amikacin, 15 mg/kg, procaine penicillin G, 300 U/dose, or gentamicin, 2 mg/kg, alone and in two-drug combinations. Antimicrobials were given intramuscularly every 6 hr for 16 doses. Extravascular chambers were sampled throughout the treatment course for bacterial counts and antimicrobial concentration. In vivo results were compared to in vitro tests of inhibition, killing, and synergism. Ciprofloxacin alone had little effect on the animal infection sites. Azlocillin alone reduced, in vivo, eight of 12 isolates greater than or equal to 5 log10 CFU/ml by 92 hr as compared to control. Azlocillin plus ciprofloxacin reduced all 12 isolates greater than or equal to 5 log10 CFU/ml by 92 hr, whereas amikacin plus azlocillin reduced only three and penicillin plus gentamicin only one of the six group D streptococcal isolates greater than or equal to 5 log10 CFU/ml.

Amikacin↗
PubMedDate not supplied

[Azlocillin--synovial fluid levels after intravenous doses].

The corresponding levels of azlocillin in serum and in synovial fluid in the knee-joint were investigated in patients who had undergone aseptic surgery of the lower limbs. The mean synovial fluid concentrations for azlocillin were determined on the basis of 30 samples. Clinically relevant azlocillin levels of approximately 40 mu g/ml were recorded in synovial fluid 10 minutes after start of a short infusion of 5 gm. These increased until about 90 minutes after commencement of antibiotic administration when the maximum level was attained. Subsequently synovial fluid levels decreased slowly and approximately 170 minutes after commencement of the short infusion the mean for serum and synovial concentrations corresponded. The results confirm that with an i.v. infusion of 5 g azlocillin levels can be attained for 3 hours in the synovial fluid that are above the break-point for this antibiotic of 64 mu g/ml. However, despite these good pharmacokinetic data it should be remembered that experience has shown that surgical reintervention is often necessary in addition in joint infections to achieve ultimate cure.

Adolescent↗
PubMed1987

Comparative efficacy of ciprofloxacin, azlocillin, and tobramycin alone and in combination in experimental Pseudomonas sepsis.

Ciprofloxacin, azlocillin, and tobramycin, used alone and in combination, were studied in a model of lethal pseudomonas sepsis in rats. Ciprofloxacin alone at all doses studied and tobramycin alone at the highest dose reduced mortality significantly compared with saline controls. In contrast, survival was not improved with either azlocillin alone at all doses studied or lower doses of tobramycin alone. The combination of ciprofloxacin and azlocillin was synergistic in rats with systemic pseudomonas infection. Ciprofloxacin was rapidly absorbed, and effective levels persisted for 1-4 hr relative to the dose administered. These data suggest that ciprofloxacin may be a potent agent, either alone or in combination with azlocillin, in the treatment of severe pseudomonas infections.

Animals↗
PubMed1983

The in-vitro activity of azlocillin: a community hospital study of 1900 clinical isolates.

The in-vitro activity of azlocillin was evaluated against 1900 fresh clinical isolates from a 320-bed community hospital. Azlocillin inhibited over 90% of Pseudomonas aeruginosa isolates at less than or equal to 16 mg/l; it was four-fold more active than ticarcillin and 8- to 16-fold more active than carbenicillin. Against members of the Enterobacteriaceae azlocillin was less active than piperacillin but still inhibited over 90% of Klebsiella, Serratia and Proteus mirabilis at achievable blood levels (less than or equal to 64 mg/l). It was the most active agent against enterococci inhibiting 80% at less than or equal to 1 mg/l. Azlocillin will be a useful addition to the antibiotic formulary of the community hospital because of its exceptional anti-pseudomonal activity.

Anti-Bacterial Agents↗
PubMed1983

Comparative clinical evaluation of azlocillin and gentamicin.

Forty-four patients with severe systemic bacterial infection were treated with azlocillin (20) or gentamicin (24). The commonest sites of infection were skin and soft tissue, lungs and bone. Thirty-eight patients had received previous antimicrobial therapy. The commonest infecting organism was Pseudomonas aeruginosa. The overall response rate in the azlocillin group was cure or partial cure in 18 patients and failure in one patient, and in the gentamicin group 15 cures or partial cures and six failures. Four patients, one on azlocillin and three on gentamicin, could not be evaluated. Azlocillin was an effective and safe therapy for the treatment of Ps. aeruginosa infections.

Adolescent↗
PubMed1983

Synergy of azlocillin with aminoglycosides.

The combination of azlocillin and the aminoglycosides amikacin, gentamicin, netilmicin, sisomicin, and tobramycin was synergistic. The FIC index was less than or equal to 0.5 for 28 to 42% of Pseudomonas aeruginosa isolates tested and with an additive FIC index greater than 0.5-1 for 53 to 63% of the isolates. Antagonism was not encountered. Isolates resistant to azlocillin (MIC greater than 100 mg/l) were more often synergistically inhibited by the combination of azlocillin and an aminoglycoside. The concentrations of antibiotics that synergistically inhibited Pseudomonas were those readily achieved in man. The combination of azlocillin and aminoglycosides prevented regrowth of isolates that grew after initial suppression by the antibiotics alone.

Aminoglycosides↗
PubMed1983

Clinical experience with azlocillin.

Mezlocillin and azlocillin are new semi-synthetic ureidopenicillins. Both possess a broad spectrum of activity in vitro. Potency of activity against Gram-positive and fastidious Gram-negative organisms and against obligate anaerobes is comparable. Mezlocillin is more active against Enterobacteriaceae while azlocillin is more potent against Pseudomonas species. Although direct comparative studies in serious Gram-negative bacillary infections have not been performed, it would appear prudent to administer mezlocillin in disease due to Enterobacteriaceae, and to prescribe azlocillin preferentially when the aetiological agent is presumed or known to be Pseudomonas. The use of azlocillin to treat serious infections with Ps. aeruginosa is described here. A variety of clinical and laboratory observations may permit implication of Pseudomonas in the aetiology of specific infections.

Adult↗
PubMed1983

Pharmacokinetics of azlocillin in normal renal function: single and repetitive dosing studies.

Systemic and urinary pharmacokinetic studies of the disposition of azlocillin were performed in seven male and six female healthy volunteers. Four separate studies identified the kinetics of the drug following a single 2, 3 or 4 g administration and during the repetitive administrations of 3 g of the drug over a five-day period. Peak plasma concentrations were 174 +/- 19 mg/l, 214 +/- 17 mg/l and 286 +/- 11 mg/l in the 2, 3 and 4 g single dose studies respectively. Trough values at 4 h post-dosing were 6 +/- 1 mg/l, 10 +/- 1 mg/l and 26 +/- 3 mg/l respectively. The plasma half-life of azlocillin was approximately 60 min. A dose-dependent phenomenon was observed. This was characterized by a slight but significant progressive increase in the plasma half-life of the drug as increasing amounts of drug were given and as the same amount was given repeatedly. No significant systemic accumulation of azlocillin was noted during the repetitive dosing study. The urinary excretion of the compound was prompt with most of the bioactive drug being eliminated in the first 4-6 h following dosing. The apparent volume of distribution of azlocillin was slightly greater than the extracellular fluid compartment. For the therapy of systemic infections in adults with normal renal function a 4 h or 6 h dosing cycle would be appropriate.

Azlocillin↗