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PubMed1986

Azlocillin serum levels on repetitive dosage in patients with normal and abnormal renal function.

Azlocillin serum concentrations were followed in 9 severely ill patients with various degrees of renal dysfunction after single and repetitive dosage. All patients were treated concomitantly with a cephalosporin and/or an aminoglycoside antibiotic. Elimination halflives (t1/2 beta) were highly variable (62-1, 194 min), but no significant increase occurred in patients with stable renal function during repetitive dosage due to previously described nonlinear pharmacokinetic behavior of azlocillin. However, drug accumulation was observed in patients with deterioration of renal and hepatic function. The rise in drug accumulation can be disproportionally high if both routes of elimination are affected. In such cases, careful dosage adjustment of azlocillin is required to avoid toxic side effects.

Adult↗
PubMed1983

Comparative in vitro activity of ticarcillin, piperacillin, azlocillin and mezlocillin.

The in vitro activity of ticarcillin, piperacillin, azlocillin and mezlocillin was determined against 403 clinical isolates. At MIC50, piperacillin was 2 to 8 times more active than the other three compounds against Pseudomonas, Escherichia coli, Proteus, Citrobacter, Acinetobacter and Salmonella species. Against Klebsiella, Enterobacter, Haemophilus, Bacteroides spp. and non-beta-lactamase producing Staphylococcus aureus the activity of piperacillin was similar to one or more of the most effective agents. However, azlocillin and mezlocillin were more active than piperacillin against enterococci. Ticarcillin was the least active in vitro. Despite these significant differences at MIC50 amongst the four compounds, they became much less discernible at MIC90, obviously due to beta-lactamase producing strains under study. The spectrum of activity of piperacillin encompasses those of azlocillin and mezlociLlin together except for Gram-positive organisms.

Azlocillin↗
PubMed1979

Pseudomonas infections of the lung treated with azlocillin. Microbiology, pharmacokinetics, clinic.

6-[(R)-2-(2-Oxo-imidazolidine-1-carboxamido)-2-phenyl-acetamido]-penicillanic acid sodium salt (azlocillin, Securopen), has a special activity against Pseudomonas species besides is broadspectrum character. We confirmed the high in vitro potency of that antibiotic in 200 clinical Pseudomonas isolates. Good penetration of azlocillin into bronchial secretions was found, especially through the inflamed bronchial mucosa, but also in the post-inflammatory phase. In 16 patients with serious Pseudomonas infections of the respiratory tract the good efficacy of azlocillin was shown. There were no tolerance problems.

Azlocillin↗
PubMed1986

Pharmacokinetics of azlocillin after intramuscular application.

The first pharmacokinetic data are reported of azlocillin injected intramuscularly to adult probands. The blood serum and urinary levels of azlocillin were determined microbiologically in 8 healthy volunteers after intramuscular injection of 2 grams. Peak serum levels of azlocillin were found by the end of hour 1 after injection, average level was (55.06 +/- 10.25) mg/l. At hour 2 the average level was (33.64 +/- 6.46) mg/l. and at hour 4, (9.47 +/- 1.79) mg/l. The biological half-life was 1.4 hour. In urine, (41.2 +/- 7.7)% of the administered dose was eliminated within 8 hours on average.

Azlocillin↗
PubMed1987

[Azlocillin stability in solutions and the solid state].

Stability of azlocillin in aqueous solutions at pH 1.5-12.5 was studied at various temperatures. It was shown that degradation of the antibiotic proceeded as an irreversible first order reaction. Dependence of 1gk on the reverse temperature was described by the Arrhenius equation. The highest levels of azlocillin stability in solutions were observed at pH about 6.0. In solid state azlocillin was stable under the effect of the environmental factors. In the atmosphere of oxygen and carbon dioxide and on exposure to light the quality parameters of the antibiotic powder maintained at the control levels.

Azlocillin↗
PubMed1986

Efficacy of single-agent therapy with azlocillin, ticarcillin, and amikacin and beta-lactam/amikacin combinations for treatment of Pseudomonas aeruginosa bacteremia in granulocytopenic rats.

The efficacy of azlocillin, ticarcillin, and amikacin as single agents and the penicillin/amikacin combinations for treatment of Pseudomonas aeruginosa bacteremia during cyclophosphamide-induced severe neutropenia in a rat model were assessed. Equivalent antibiotic dosing was based on the time rat serum antibiotic levels were above the minimal bactericidal concentration for the challenge organism. Antibiotic therapy was administered for 62 hours after bacterial challenge. Antimicrobial efficacy was based on the rate of bacteremia, the emergence of resistant organisms during therapy, life-table survival analysis, and rat survival seventy-two hours after bacterial challenge. For infection with a P. aeruginosa strain susceptible to all study antibiotics, therapy with azlocillin and ticarcillin (given so as to be equipotent) were equivalent, as judged by bacteremia rates or rat survival. However, combination therapy prevented the emergence of organisms resistant to azlocillin, but not to ticarcillin. Amikacin-containing combinations were more effective than single-agent regimens.

Agranulocytosis↗
PubMed1986

Pharmacokinetics of azlocillin in children with and without cystic fibrosis treated for infectious diseases.

The pharmacokinetic characteristics of azlocillin were compared in 7 children with cystic fibrosis (CF) and 6 children without this disease who were all treated for infectious diseases. Azlocillin was administered as intravenous bolus injections in doses of 200 mg/kg. The serum concentrations were somewhat lower in CF than in non-CF as reflected by total areas under the serum concentration curves of 594 and 677 mg h/1, and serum levels after 8 hrs of 10.7 mg/1 in non-CF vs. a concentration below the detection limit in CF. The CF children had a lower serum half-life (1.1 hrs) than the children without this disease (3.3 hrs). The difference is explained by higher total body clearance in CF (12.7 1/h) than the non-CF group (8.4 1/h). The dose interval should either be shorter, or the doses increased, when azlocillin is administered to patients with CF.

Adolescent↗
PubMedDate not supplied

[Pharmacokinetic studies of azlocillin in pregnancy].

Examining blood level values and urinary concentrations taken from pregnant and nonpregnant women, the pharmacokinetic dates of azlocillin have been evaluated. We used a computer program based on the two-compartment model. The evaluation of azlocillin concentrations in serum and urine has been realized with the two following methods: polarography and agar diffusion test. We found nearly equal values of serum concentrations when using both methods. There are no statistical differences between pharmacokinetic dates of pregnant and nonpregnant women. Therefore we state: It is not necessary to change the dosage and the application interval of azlocillin during pregnancy.

Adult↗
PubMed1985

[Treatment of acute and chronic urological infections with azlocillin--clinical and microbiological research].

The authors present their results from the treatment of urological infections with the new semisynthetic penicillin antibiotic azlocillin (acyl-ureide-penicillin) in 86 patients with various, in kind and clinical manifestations, infections of the urinary system. The susceptibility was determined of the isolated bacterial causative agents of the urological infections to azlocillin and to the other antibacterial preparations available in our country. It was established that 52,7% of Gram-negative microorganisms were susceptible to the preparation, and over 80%--of the Gram-positive microorganisms. The highest number of susceptible strains were established in pseudomonas, coli, enterobacter, klebsiella and proteus. The results from the clinical study reveal that 51,2% of the patients were cured by the end of the therapeutic course and abatement or considerable improvement, was observed in all, of the clinical and paraclinical indices, suggesting urological infection. No allergic or toxic manifestations were observed. The absence of nephrotoxicity makes that new, for our practice, antibiotic extremely valuable for the patients with renal insufficiency. The most general conclusion from that study is that azlocillin, with its effectiveness, comes close to the most potent modern antibacterial preparations, with no toxicity characteristic for aminoglucoside antibiotics.

Adolescent↗
PubMed1985

[The effect of infusion rate on pharmacokinetic parameters of azlocillin and mezlocillin].

Azlocillin (Securopen) and mezlocillin (Baypen) were given to 3 healthy subjects as intravenous infusion. The dose of 4 g was administered to each person within 5, 15, and 30 min in a randomized crossover design. Using HPLC the unchanged penicillin antibiotics were determined quantitatively, their metabolites were assessed qualitatively. The same specimens were also studied by means of a bioassay (agar diffusion technique). Both methods yielded similar serum and urine concentrations besides the urinary excretion of azlocillin. Here the bioassay measured higher amounts indicating an antibacterially active metabolite being excreted in the urine. No dependence upon infusion time was found. Since both drugs were tested with the same dosis in the same subjects, their pharmacokinetic parameters could be compared: mezlocillin, being more lipophilic than azlocillin, showed a higher volume of distribution and therefore lower serum concentrations. Renal clearance was the same for both drugs, but mezlocillin was excreted to a smaller extent in the urine. Higher total clearance and shorter elimination half-life of mezlocillin indicate a greater extrarenal elimination. The results suggest fast application of both penicillins. There is no pharmacokinetic reason for a prolongation of infusion times.

Adult↗
PubMed1985

The safety and tolerance of azlocillin.

631 patients treated with azlocillin were evaluated for adverse reactions. Azlocillin doses ranged from 37-714 mg/kg/day (mean 260 mg/kg/day) and duration of treatment ranged from 1 to 276 days (mean 11.1 days). 82% of patients were treated for more than 7 days. 92 (14.6%) experienced systemic and 20 patients (3.2%) experienced local adverse reactions. Hypersensitivity, manifest by drug fever, cutaneous reactions, or eosinophilia occurred in 0.3, 1.8 and 1.1%, respectively. Hypokalemia developed in 0.5% overall and was dose and duration related. Hepatotoxicity occurred in 1.7%, diarrhea in 1.9% and leukopenia in 0.3%. Nephrotoxicity, expressed as elevated serum creatinine, was seen in 0.5%. Bleeding was seen in one group of patients that received cefamandole concomitantly. As these complications were not seen in other patients, these complications are probably due to cefamandole. In comparison with ticarcillin, carbenicillin, piperacillin, and mezlocillin, a similar number and severity of adverse reactions were seen. Although the incidence of certain adverse reactions may be underestimated due to the short duration of therapy, azlocillin appears to be exceptionally safe and well tolerated.

Adolescent↗
PubMed1979

Studies on the antibacterial activity of two new acylureidopenicillins, mezlocillin and azlocillin.

The antimicrobial activity of 6-[(R)-2[3-methylsulfonyl-2-oxo-imidazolidine-1-carboxamido]-2-phenylacetamido]-penicillanic acid sodium salt (mezlocillin, Baypen) and 6-[(R)-2-(2-oxo-imidazolidine-1-carboxamido)-2-phenylacetamido-a1-penicillanic acid sodium salt (azlocillin, Securopen) was measured against 545 clinical isolates, including gram-negative rods, gram-positive cocci and Bacteroides. Mezlocillin was more effective than azlocillin against the majority of the strains studied, but azlocillin was more effective against Pseudomonas strains. The minimal bactericidal concentration was equal to the minimal inhibitory concentration for the strains tested, but it was twice or four-fold as high for Staphylococcus.

Azlocillin↗
PubMed1984

[Mechanisms of azlocillin resistance in Pseudomonas aeruginosa].

The authors have evaluated the susceptibility of azlocillin to beta-lactamases habitually produced by Pseudomonas aeruginosa, i.e. TEM and CARB types penicillinases and the so-called Sabath and Abraham cephalosporinase. As all penicillins, azlocillin is liable to hydrolysis by penicillinases that also affect, through to a lesser extent, some cephalosporin. It is also degraded, albeit moderately by the Sabath and Abraham cephalosporinase. The authors have also compared the behaviour of azlocillin towards beta-lactamases to that of other beta-lactam antibiotics, notably carbenicillin, cefoperazone and cefsulodin.

Azlocillin↗
PubMed1984

[Antibacterial effects of the combinations of azlocillin with other antibiotics].

Evaluating the synergistic effects of antibiotic associations is by no means an easy task owing to the diversity of the test methods utilized for this purpose. Data extracted from 11 reports published between 1975 and 1982 and concerning associations of azlocillin with various aminoglycosides (gentamicin, sisomycin, netilmicin, amikacin, tobramycin and dibekacin) and with two beta-lactam antibiotics (cloxacillin and cefotaxime) are reviewed in this article. On the whole, a synergistic effect against Staphylococcus aureus, Pseudomonas aeruginosa and Enterobacteriaceae was most frequently observed with the azlocillin-aminoglycoside association. This effect was usually more pronounced with organisms showing low sensitivity to azlocillin and less pronounced with organisms resistant to aminoglycosides. As often pointed out, there is no general rule that would help predict with certainty from the sensitivity of a strain whether or not any given antibiotic association will act synergistically on that strain.

Aminoglycosides↗
PubMed1984

[Bone and blood levels of azlocillin after intra-arterial injection in the dog].

Pharmacokinetic values of azlocillin--a semisynthetic penicillin of the ureidopenicillin family--were determined in dogs after injection of the drug into the right femoral artery by measuring plasma concentrations in the right femoral artery and left femoral vein and tissue concentrations in ipsi- and contralateral bones. Two different doses of azlocillin were administered, one group of dogs receiving 100 mg X kg-1 by fast (1 min) bolus injection and the other group receiving 250 mg X kg-1. The drug was assayed by high performance liquid chromatography in reverse phase, which proved to be the simplest, most rapid and most sensitive method. Changes in plasma and bone tissue concentrations after intra-arterial injection were interpreted as order one kinetics with a two-compartment open model. Following the 100 mg/kg dose, concentrations versus time corresponded to the following equations: --Arterial blood (mg/l) = 7570 e-0.15 t (min) + 240 e-0.017 t --Venous blood (mg/l) = 553 e-0.13 t + 222 e-0.016 t --Bone tissue (micrograms/g) = 15 e-0.0115 t (elimination phase). Distribution and elimination constants were identical in arterial and venous blood. Distribution half-life was 5 +/- 1 min in arterial blood and biological half-life was 42 +/- 11 min. However, bioavailability was comparatively lower in veins due to higher levels in arteries during the distribution phase. Bone tissue concentrations were much lower than plasma concentrations and were identical on both sides despite high arterial levels on the ipsilateral side during the distribution phase. Bone concentrations diminished rapidly and elimination kinetic values were the same in bone and in plasma. It is concluded that bone tissue concentrations of azlocillin after intra-arterial injection are highest during the distribution phase.

Animals↗
PubMed1984

[Evaluation of the clinical activity of azlocillin. A multicenter study conducted in 14 centers].

Azlocillin, an acylureidopenicillin particularly active against Pseudomonas aeruginosa, was used to treat 124 patients, 36 of whom were children, presenting with pulmonary infections (including cystic fibrosis), urinary, genital, intra-abdominal, osteoarticular and skin infections as well as septicaemia, otitis and meningitis. The causative agent in all cases was Ps. aeruginosa either alone or associated with other pathogens. Azlocillin was administered alone in 75% of the cases and in combination with an aminoglycoside in 25%. Dosage was 240 mg/kg/24 h in three intravenous infusions in adults and in children older than 3 months, and 75 to 225 mg/kg/24 h in two intravenous injections in neonates and prematures. The duration of treatment varied according to the site of infection, with a mean of 10 days. One-hundred and eight pathogenic organisms were isolated, including 114 strains of Pseudomonas, 43 of which were carbenicillin-resistant. A satisfactory clinical response was observed in 86.5% of the infections. The bacteriological response was similar to the clinical response, with 76.6% cures, 10% improvements and 13.5% failures. Microbiologically, 77.5% of the germs were eradicated, 7.5% reappeared and 15% persisted. Azlocillin was well tolerated systemically and biochemically and had no detrimental effect on renal function.

Adult↗
PubMed1984

[Monotherapy of Pseudomonas aeruginosa septicemia with azlocillin].

Azlocillin was administered alone to seven patients without malignant or blood disease presenting with septicaemia caused by Pseudomonas aeruginosa. In 6 cases the infection developed after surgery and in 3 of these it was responsible for a state of shock, twice associated with acute anuric renal failure. The minimum inhibitory concentrations of azlocillin varied from 2 to 32 micrograms/ml; 5 strains were resistant to carbenicillin. The minimum inhibitory to minimum bactericidal concentrations ratio, measured on five occasions, was equal to 2. Bacterial eradication was obtained in 6 patients. One patient with multivisceral failure died during treatment and in this case the responsible organism had become resistant to azlocillin.

Adult↗
PubMed1983

In vitro and in vivo action of mezlocillin and azlocillin combined with sisomicin.

Combined action in vitro and in vivo of ureidopenicillins (azlocillin and mezlocillin) with sisomicin has been studied with employment of strains of Escherichia coli, Klebsiella pneumoniae and Pseudomonas aeruginosa. In vitro effects of these combinations were most spectacular with Pseudomonas aeruginosa; azlocillin and sisomicin were potently synergistic. Other tested microorganisms reacted also but less markedly. Evaluation of therapeutic efficacy of ureidopenicillins combined with sisomicin was performed on 90 rabbits, infected intravenously with heavy inocula. Synergistic action has been confirmed in vivo during treatment of infections evoked by Escherichia coli and Pseudomonas aeruginosa. Therapy of these infections may be successful with doses of azlocillin or mezlocillin combined with sisomicin diminished by half, as compared with treatment of these infections with above antibiotics applied singly. Further decrease of sisomicin dosage in combined therapy of P. aeruginosa infections with ureidopenicillin is possible.

Animals↗