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PubMed1981

Azlocillin treatment of urinary tract infection in patients on haemodialysis.

Pharmacokinetic properties and clinical efficiency of azlocillin were investigated in three patients with terminal renal failure both during and without haemodialysis. All patients were treated for urinary tract infections with azlocillin 2 g three times daily for a period of ten days. Mean serum half-lives off dialysis were 251 min and on dialysis 202 min. Azlocillin clearances increased from a mean value of 58.7 ml/min off dialysis to 72.6 ml/min on dialysis. Urinary excretion of the total daily dose of azlocillin was less than 5% for all patients, but from day 2 onwards all patients had urine levels which were more than 8 times above the approximate MIC value of the infecting bacteria.

Aged↗

PubMed1995

Stability study of azlocillin sodium in glass bottles and PVC bags containing intravenous admixtures.

The kinetics of degradation of azlocillin sodium in four intravenous admixtures was investigated at different temperatures. The effect of temperature has been determined and from this data, by applying of Arrhenius-law, the stability of azlocillin sodium at 25 degrees C has been predicted and the t90 was determined. Admixtures containing azlocillin sodium (0.01 g ml-1) were prepared in 0.9% sodium chloride injection, in 5% dextrose solution, in 5% levulose solution and in Ringer's lactate solution. The admixtures were stored at 30 degrees, 40 degrees and 50 degrees C in either polyvinyl chloride bags and glass bottles. The change in the initial azlocillin sodium concentration was related to the type of intravenous solution. No dependence with material of container was found. After 24 hours, the change in the initial concentration of penicillin was less than 10% of the initial concentration in 0.9% sodium chloride and 5% levulose solution. However in Ringer's lactate and 5% glucose solution the t90 was lower. These results were found in agreement with experimental ones obtained at room temperature.

Azlocillin↗

PubMed1977

[In vitro activity of mezlocillin, azlocillin and carbenicillin against bacteroidaceae with particular reference to bacteroides fragilis (author's transl)].

The in vitro susceptibility of approximately 90 Bacteroidaceae strains to the the new broad-spectrum penicillins mezlocillin and azlocillin was determined by tube dilution tests and compared to susceptibility to carbenicillin. Bacteroides fragilis and Bacteroides thetaiotaomicron predominated among the strains tested. These strains are particularly important as pathogens and are known to produce beta-lactamase. At concentrations of 16 microng/ml or less, mezlocilin inhibited 81% of the Bacteroides cultures, and at 32 microng/ml 96% of the cultures. The amount of Bacteroides strains inhibited by 16 and 32 microng/ml of azlocillin was 67% and 93% respectively. Similar results were obtained with carbenicillin, concentrations of 32, 64 and 256 microng/ml inhibiting 55%, 87% and 94% of the strains respectively. Mezlocillin and azlocillin did not appear to be any more effective than carbenicillin against Sphaerophorus strains. Statistical analysis of the relationship between minimal inhibiting concentration and inhibition zone diameter showed that the susceptibility of Bacteroidaceae to mezlocillin, azlocillin and carbenicillin cannot be determined with sufficient accuracy by a standardized agar diffusion test.

Bacteroidaceae↗

PubMed1978

Activity of azlocillin and mezlocillin against gram-negative organisms: comparison with other penicillins.

The activities of azlocillin and mezlocillin were compared with those of carbenicillin, ticarcillin, and pirbenicillin against a wide range of gram-negative organisms. The two new drugs were considerably more active than carbenicillin against Klebsiella species and Escherichia coli. Carbenicillin was twice as active against Proteus mirabilis as mezlocillin and four times as active as azlocillin. Against Pseudomonas aeruginosa, azlocillin was eight times as active as carbenicillin. Azlocillin and mezlocillin were twice as active as carbenicillin against Bacteroides fragilis, and these drugs showed a high degree of activity against Haemophilus influenzae and Neisseria gonorrhoeae.

Bacteria↗

PubMed1978

Azlocillin and mezlocillin: new ureido penicillins.

The activity of azlocillin and mezlocillin, new semisynthetic ureido penicillins, was investigated and compared with that of other known beta-lactam antibiotics. At a concentration of 25 mug/ml, azlocillin inhibited 74% of Enterobacter, 97% of Proteus mirabilis, 64% of Citrobacter, 91% of Pseudomonas aeruginosa, and 82% of Bacteroides strains tested. Mezlocillin inhibited 86% of Shigella, 96% of Enterobacter, 80% of indole-positive Proteus, 88% of Bacteroides, and 63% of Pseudomonas strains tested. Azlocillin was more active against Pseudomonas than was ticarcillin, carbenicillin, or mezlocillin. Mezlocillin was more active than carbenicillin and ampicillin against Escherichia coli, Klebsiella, Enterobacter, Citrobacter, Acinetobacter, Serratia, and Bacteroides. Azlocillin and mezlocillin were less active than cefazolin against beta-lactamase-producing E. coli and Klebsiella strains but more active than cefazolin against Enterobacter, indole-positive Proteus, Acinetobacter, Citrobacter, and Serratia strains. Both compounds showed activity equivalent to that of cefoxitin against Bacteroides isolates. Both agents were destroyed by many of the beta-lactamases from gram-negative organisms.

Bacteria↗

PubMed1979

Comparative in vitro activity of azlocillin, ampicillin, mezlocillin, piperacillin, and ticarcillin, alone and in combination with an aminoglycoside.

The in vitro activities of the newer semisynthetic penicillins azlocillin, mezlocillin, and piperacillin were compared with those of ampicillin and ticarcillin by using 290 clinical laboratory isolates. Piperacillin and mezlocillin were the most active against Escherichia coli, Proteus mirabilis, Klebsiella spp., and Enterobacter spp. When Pseudomonas aeruginosa was tested, piperacillin and azlocillin were more active than either mezlocillin or ticarcillin. Streptococcus pneumoniae and Haemophilus influenzae species were highly susceptible to all of the penicillins tested. Ticarcillin had relatively poor activity against enterococci. The rate of bacterial killing with multiples of the minimal inhibitory concentration of azlocillin, ampicillin, or ticarcillin was tested for E. coli, P. mirabilis, P. aeruginosa, and Klebsiella spp. Increasing concentrations increased the bactericidal effect. The effect of combining azlocillin, ampicillin, or ticarcillin with an aminoglycoside was studied by using both killing curves and checkerboards. The isobolograms constructed from the checkerboards showed a synergistic pattern for the organisms tested, which included E. coli, P. aeruginosa, Klebsiella spp., P. mirabilis, and enterococci. However, the rate of killing was increased by the combination only for P. aeruginosa and enterococci.

Aminoglycosides↗

PubMed1979

[The pharmacocinetics of azlocillin (author's transl)].

Azlocillin concentrations in the rabbit eye were studied after intravenous and subconjunctival injections. The following results were found: therapeutic levels of Azlocillin were achieved in the aqueous humor, using either way of administration. Concentrations of the antibiotic were much higher after s. c. injection than after i. v. administration. The pharmacocinetics of Azlocillin proved to be comparable to those of other penicillins. No antibiotic could be detected in the vitreous body, irrespectively of the administration. With regard to the better antibacterial activity of Azlocillin in comparison with other known penicillins it should be preferred in eye infections caused by gramnegative rods, especially by Pseudomonas aeruginosa.

Animals↗

PubMed1983

Azlocillin concentrations in human aqueous humor after intravenous and subconjunctival administration.

Twenty-nine patients received either 4 g intravenous infusion or 100 mg subconjunctival application of azlocillin 1-12 h before cataract extraction. After intravenous application the mean aqueous humor concentration of azlocillin was 4.4 micrograms/ml after 3 h. The subconjunctival dose produced a mean aqueous humor concentration of 78 micrograms/ml and 3.4 micrograms/ml after 3 and 12 h, respectively. These levels are above the minimum inhibitory concentration of azlocillin for sensitive organisms.

Aqueous Humor↗

PubMed1982

Elimination of azlocillin in patients with biliary t-tube drainage.

The pharmacokinetic of azlocillin was followed in five elderly patients after biliary surgery. Total clearance was 138.6 +/- 17.7 ml/min when 2.0 g was given as an i.v. bolus injection. The half-life of the beta-phase averaged 110 min. The total clearance and the half-life of azlocillin were influenced by slight impairment of renal function (creatinine clearance 59.4 +/- 13.6 ml/min). In patients with normal liver function biliary excretion of the drug amounted to 5.3 +/- 2.8% of the dose (n = 3) and the kinetics of biliary excretion were linear. In contrast, in two patients with impaired liver function biliary excretion was 0.2% and 0.5% of the dose, and kinetic analysis of biliary excretion rates revealed at least one zero order step in the excretion process. Renal excretion of the drug amounted to 45.0 +/- 17.7% of the dose, which means that 50% of the total clearance of azlocillin has to be accounted for by metabolic clearance.

Aged↗

PubMed1982

The pharmacokinetics of azlocillin in the perilymph of guinea pigs and otitis media.

The results of studies on the pharmacokinetics of azlocillin in the perilymph of the guinea pig following the intramuscular administration of 200 mg per kg body weight are shown graphically. Similar to mezlocillin and the aminoglycoside antibiotics, this new acylureido penicillin is retained in the inner ear. The results of our studies, together with the data on the in vitro and in vivo activity of azlocillin and gentamicin and the applicable dosage for clinical purposes, indicate that the azlocillin levels in the perilymph are considerably more effective against Pseudomonas aeruginosa and many times more effective against the other microorganisms usually involved in acute otitis media than those of the aminoglycosides.

Animals↗

PubMed1987

[Ceftazidime with and without tobramycin versus azlocillin plus tobramycin in the therapy of bronchopulmonary infections in intensive care patients].

In a still ongoing open, randomized prospective trial the preliminary data of 50 intensive care patients on artificial ventilation were analysed. The evaluation included clinical and bacteriological efficacy and tolerance of ceftazidime alone or in combination with tobramycin versus azlocillin plus tobramycin. Artificially ventilated patients who had been treated in an intensive care unit for at least five days were selected to enter the study because of a high probability of colonisation with gram-negative bacteria. 16 patients were treated for bronchopulmonary infection with ceftazidime alone, and 17 each were treated with ceftazidime plus tobramycin or with azlocillin plus tobramycin. In the ceftazidime group nine patients were cured and three were improved (75% clinical success). Of the patients treated with ceftazidime plus tobramycin, 11 were cured and one was improved (75% clinical success); one patient died from very severe multiple trauma. In the azlocillin-tobramycin group, six patients were cured and two were improved (57% clinical success). Two patients from this group died from their underlying disease and another died from multiple organ failure due to septicemia.

Adult↗

PubMed1983

Effect of azlocillin and piperacillin in subinhibitory and inhibitory concentrations on Staphylococcus aureus and Pseudomonas aeruginosa in broth, in serum and in the presence of human polymorphonuclear leukocytes.

The bactericidal activity of azlocillin and piperacillin was tested at concentrations of 1/4 the MIC, the MIC and four-fold the MIC agents a serum-resistant Staphylococcus aureus and a serum-resistant Pseudomonas aeruginosa strain in broth, in serum and in the presence of leukocytes. The antibacterial activity of azlocillin and piperacillin in serum against Staphylococcus aureus was slightly better than in broth (p greater than 0.05); both compounds were distinctly less active against Pseudomonas aeruginosa in serum than in broth (p less than 0.05). Both antibiotics enhanced susceptibility of Pseudomonas aeruginosa to leukocyte killing without serum (p less than 0.05), whereas leukocyte killing of Staphylococcus aureus was hardly improved even at the MIC and four-fold the MIC of both compounds. The antibacterial activity of azlocillin and piperacillin against both bacterial strains was most pronounced in the presence of leukocytes and serum. A marked bactericidal effect was achieved at 1/4 the MIC, the effect not being further significantly enhanced (p greater than 0.05) at the MIC or four-fold the MIC.

Azlocillin↗

PubMed1989

Multicenter, randomized trial of ciprofloxacin plus azlocillin versus ceftazidime plus amikacin for empiric treatment of febrile neutropenic patients.

In a multicenter, randomized clinical trial, the efficacy of ciprofloxacin plus azlocillin was compared with that of a standard regimen of ceftazidime plus amikacin for the initial empiric treatment of fever in neutropenic cancer patients. In addition, the efficacy of early conversion from intravenous therapy to orally administered ciprofloxacin was compared with that of continued ceftazidime plus amikacin. Seventy-one oncology patients with 79 episodes of fever and neutropenia were randomly assigned to receive initial empiric antibiotic therapy with either intravenously administered ciprofloxacin and azlocillin followed by orally administered ciprofloxacin (regimen 1, 25 episodes); ceftazidime and amikacin (regimen 2, 30 episodes); or ceftazidime and amikacin followed by oral ciprofloxacin (regimen 3, 24 episodes). Microbiologically documented infections were the cause of fever in 10 (40 percent), seven (23 percent), and nine (38 percent) episodes in regimens 1, 2, and 3, respectively, including six, five, and four episodes of bacteremia. Patient survival was 90 to 92 percent in each regimen; however, some modification of antimicrobial therapy occurred in 65, 44, and 41 percent of surviving patients in regimens 1, 2, and 3, respectively. The rate of clearance of initial bacteremia was 67 percent (four of six) in regimen 1, 100 percent (five of five) in regimen 2 and 50 percent (two of four) in regimen 3. Patients in regimens 1 and 3 were able to convert to orally administered ciprofloxacin in 32 (65 percent) of 49 episodes after a mean of six days of intravenous therapy. Superinfections occurred in 24, 10, and 12 percent of patients receiving regimens 1, 2, and 3, respectively, and occurred similarly for patients receiving orally administered ciprofloxacin, 12 percent (four of 32), and intravenous therapy, 17 percent (eight of 47). Parenteral ciprofloxacin was generally well tolerated. One (4 percent) of 25 patients receiving regimen 1 experienced oto- or nephrotoxicity, compared with eight (15 percent) of 54 patients receiving regimens 1, 2, and 3 (p = 0.15), including three patients who required premature termination of aminoglycoside therapy. Our data suggest that the combination of ciprofloxacin and azlocillin is an effective alternative to ceftazidime and amikacin for the initial empiric therapy of febrile neutropenic patients, is generally well tolerated, and avoids the oto- and nephrotoxicity associated with aminoglycoside use. In addition, a majority of patients could change to orally administered ciprofloxacin alone after six days of parenteral therapy.

Adult↗

PubMedDate not supplied

Serum bactericidal activity from intravenous ciprofloxacin and azlocillin given alone and in combination to healthy subjects.

Ciprofloxacin plus azlocillin have been shown to exhibit in vitro synergy versus a variety of organisms, including Pseudomonas aeruginosa. This study examined this interaction in vivo, testing serum bactericidal activity (SBA) in six healthy male subjects after intravenous administration of ciprofloxacin 4 mg/kg (C), azlocillin 60 mg/kg (A), and the two simultaneously (C/A). Eight different organisms were tested: four isolates of P. aeruginosa with varying susceptibilities to C and A, and one isolate each of Escherichia coli (EC), Staphylococcus aureus (SA) Serratia marcescens (SM), and Klebsiella pneumoniae (KP), all of which were susceptible to both drugs. Blood samples were collected at the end of 30-min infusions and at 4 and 8 hr. Reciprocal titers were plotted versus time and area under the bactericidal titer curve (AUBC) calculated to assess antibacterial interactions. Results indicated that P. aeruginosa-1 (PA-1), EC, and KP were synergistically killed by C/A. AUBC for PA-1 were C = 36, A = 11, C/A = 144, p less than 0.05. AUBC for EC were C = 1059, A = 180, C/A = 1504, p = 0.05. AUBC for KP were C = 327, A = 97, C/A = 584, p = 005. Additive effects were demonstrated versus all of the other organisms except Serratia marcescens, where an indifferent effect was observed. Ciprofloxacin plus azlocillin may be a useful combination of the treatment of selected Gram-negative bacillary infections.

Adult↗

PubMed1985

Degradation of azlocillin in human serum.

We developed a rapid and precise high performance liquid chromatographic method (HPLC) for the determination of azlocillin and its metabolites penicilloate and penilloate in serum and tissue as well as in vivo as in vitro. The linear relationship (r greater than 0.99) of determination ranged between 0.05 and 10 micrograms. No interference with other serum components was observed. The metabolism of azlocillin in vitro was analysed in serum. Within 24 h the amount of penicilloate increased from 1.5% up to 18% and from penilloate up to 1% respectively. Buffer controls revealed a significant lower metabolism (4.7% penicilloate, 0.9% penilloate). These data suggest that the degradation of azlocillin does not only depend on bacterial beta-lactamase activity but is influenced by enzymatic activities within serum and human tissue.

Azlocillin↗

PubMed1988

Concentration of azlocillin in human chondral tissue.

The concentration of azlocillin was determined using high performance liquid chromatography in serum and chondral tissue after intravenous infusion of azlocillin (75 mg/kg body weight). In serum the levels of ten patients (2 to 27 years of age, body weight 12 to 69 kg) decreased from 478 (30 min post infusion) to 120 micrograms/ml (120 min). In contrast, the concentrations in chondral tissue ranged between 24 and 35 mg/g tissue at the corresponding times. Although the mean levels suggest a remarkable penetration of azlocillin into chondral tissue, the high individual differences observed in the tissue levels (2.1 to 138 micrograms/g tissue) require a higher dosage to ensure sufficient antimicrobial therapy in all patients.

Adolescent↗

PubMed1980

Intravenous azlocillin kinetics in patients on long-term hemodialysis.

The kinetics of the antipseudomonas penicillin, azlocillin, was studied after intravenous injection in 9 patients with creatinine clearance under 7 ml/min. All were on long-term hemodialysis; 3 were also studied during a dialysis-free period. Kinetic parameters were derived using a 2-compartment open model. The mean serum azlocillin half-life (t 1/2) was 1.93 hr in patients on dialysis and approximately 5 hr off dialysis. Thirty percent of the dose was recovered in the dialysate during a 4-hr period. An approach to the use of azlocillin in patients undergoing dialysis is presented.

Adult↗

PubMed1983

Review of the pharmacokinetics and dose dependency of azlocillin in normal subjects and patients with renal insufficiency.

Cross-over studies on volunteers with several doses of azlocillin ranging from 1.0 to 5.0 g have shown that azlocillin is subject to dose dependent pharmacokinetics, the area under the serum curve becoming larger than expected as doses increase. There was also a tendency towards longer serum half-life values and excretion of more unchanged compound as the doses increase. The serum half-life varied between 0.9 h after 1.0 g increasing to 1.5 h after intravenous doses of 5.0 g given to adults. In neonates, values around 2.6 h have been observed, and they were slightly longer in premature babies at approximately twice the value in adults receiving similar doses per kg body weight. In normal adults protein binding lies between 35 and 40% for therapeutic concentrations. Approximately 60-75% of the dose appears as unchanged azlocillin in the urine, increasing with higher doses. Reduced renal function lowers urinary excretion, but concentrations are always above the break point for sensitivity of 32 mg/l in patients with creatinine clearances above 10 ml/min. In anephric subjects T1/2 of 2.5-6 h is observed. Dosage modifications only to one-third of normal are needed for a renal clearance of 10-25 ml/min. The concentrations of active compound are high in the bile in subjects with normal liver function.

Azlocillin↗