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PubMed1984

Kinetic interactions between azlocillin, cefotaxime, and cefotaxime metabolites in normal and impaired renal function.

Cefotaxime (CTX) kinetics, alone and in combination with azlocillin (AZ), were determined in 18 subjects with either normal or impaired renal function. After the single dose and with increasing renal insufficiency, total CTX clearance fell from 266 to 71 ml/min/1.73 m2. At the same time the terminal t1/2 rose from 1.1 to 2.8 hr. Regardless of the degree of renal function, CTX clearance in combination with AZ in all patients was only 50% to 60% of that with CTX alone. This reduction in total body clearance was due to a parallel decrease in renal and nonrenal clearance. In advanced renal failure, particularly after AZ, the terminal t1/2 of the CTX metabolites increased up to 1000% to 1500% of normal. On the basis of these findings, CTX dosage adjustment is recommended only in patients with a glomerular filtration rate (GFR) below 20 ml/min. After AZ, however, dosage reduction of CTX seems to be advisable at an earlier stage of renal impairment (GFR 40 ml/min).

Adult↗
PubMedDate not supplied

Immunoglobulin G: potentiation of tobramycin and azlocillin in the treatment of Pseudomonas aeruginosa sepsis in neutropenic mice and neutralization of exotoxin A in vivo.

Mice with cyclophosphamide-induced neutropenia were challenged with four immunotypes of Pseudomonas aeruginosa by contamination of a small dorsal surface wound. The infections were lethal; 100% of control animals (n = 80) treated only with albumin died. Administration of an immunoglobulin G intravenous preparation (IGIV) and/or therapy with tobramycin or azlocillin was begun 16 hr after challenge. Mortality among mice (n = 120) treated only with an antibiotic was 75.0%, while that among mice (n = 80) treated only with IGIV was 78.8%. Combination therapy with IGIV and an antibiotic (n = 120) resulted in mortality of 38.3%. The protection afforded by IGIV may have resulted in part from neutralization of exotoxin A, as mice treated with IGIV before challenge with exotoxin A were subject to lower mortality and had lower levels of serum aspartate and alanine aminotransferases than controls.

ADP Ribose Transferases↗
PubMed1991

Combination therapy with ciprofloxacin plus azlocillin against Pseudomonas aeruginosa: effect of simultaneous versus staggered administration in an in vitro model of infection.

The effect of dose scheduling on the pharmacodynamics of simulated human doses of ciprofloxacin (200 mg intravenously [iv] every 12 h) and azlocillin (4 g iv every 12 h) alone or in combination against Pseudomonas aeruginosa was studied in a two-compartment in vitro kinetic model of infection. Studies with the two drugs in combination were compared using simultaneous or staggered (first doses of each drug were administered 6 h apart) dosing schedules. Bacterial regrowth and resistance were prevented by all combination dosing schedules; however, the simultaneous regimen consistently provided the greatest extent of killing for all strains, particularly in those initially resistant to ciprofloxacin. These enhanced effects of the combination were corroborated by an increase in the peak and duration of bactericidal activity in the analogous "serum" compartment of the model. These data show the potential usefulness of simultaneous dosing of an antipseudomonal beta-lactam with ciprofloxacin against P. aeruginosa.

Azlocillin↗
PubMed1983

In-vitro activity of azlocillin and other beta-lactam antibiotics against enterococci.

The susceptibility of enterococci to 16 beta-lactam antibiotics (5 penicillins, 11 cephalosporins) was evaluated by determining MICs. All cephalosporins are ineffective against these bacteria. Penicillin G should not be used to treat infections with enterococci. For less serious infections due to enterococci, ampicillin is certainly the drug of first choice. Azlocillin, mezlocillin and piperacillin are the most effective drugs to prevent superinfections with enterococci in clinically and bacteriologically defined situations.

Anti-Bacterial Agents↗
PubMed1984

Pseudomonas aeruginosa beta-lactamase as a defence against azlocillin, mezlocillin and piperacillin.

Azlocillin, mezlocillin and piperacillin are weak substrates for the chromosomal beta-lactamase of Pseudomonas aeruginosa, and hydrolysis kinetics were calculated. Enzyme function in the living cell was studied by comparing antibiotic activity against a typical Ps. aeruginosa strain with inducible beta-lactamase expression with antibiotic activity against beta-lactamase uninducible and constitutive mutants. The inducible organism was less sensitive than its uninducible mutant to all three agents; this difference was more apparent at high inocula than low and in broth than in agar. These differences involved both enzyme induction and selection of genotypically enzyme derepressed variants. The penicillins were not, however, efficient beta-lactamase inducers at low concentrations and their activity against the inducible organism was antagonized by more potent inducers. Secondary inducers did not antagonize antibiotic activity against beta-lactamase uninducible and constitutive organisms. The beta-lactamase constitutive mutants were highly resistant to the three antibiotics tested.

Azlocillin↗
PubMed1992

A randomized trial of high-dose ciprofloxacin versus azlocillin and netilmicin in the empirical therapy of febrile neutropenic patients.

A prospective, randomized trial comparing monotherapy with high-dose ciprofloxacin versus a standard combination regimen of azlocillin and netilmicin in the empirical treatment of febrile episodes in neutropenic patients was performed. One hundred and forty-six patient episodes were randomized, but ten (seven ciprofloxacin and three azlocillin/netilmicin) were considered unevaluable for efficacy, and three episodes were withdrawn due to incorrect randomization or non-neutropenia. Of the remaining 133 episodes, infections resolved without modification of therapy in 25/66 (38%) versus 28/67 (42%) of ciprofloxacin and azlocillin/netilmicin treated groups respectively (P = 0.72). Considering all randomized episodes, therapy was modified in 46/73 (63%) episodes with ciprofloxacin and 39/70 (56%) with azlocillin/netilmicin (P = 0.40). Of 73 patient episodes randomized to ciprofloxacin, 25 (34%) received oral follow-on therapy after a median of three days of intravenous therapy. Infections were microbiologically documented in 31/73 (42%) ciprofloxacin and 32/70 (46%) azlocillin/netilmicin, of which 8/27 (30%) and 14/31 (45%) of evaluable episodes resolved without modification of therapy respectively (P = 0.28). Gram-positive organisms accounted for 78% of all organisms cultured with 36% coagulase-negative staphylococci. Bacteriological eradication was recorded in 18/24 (75%) and 26/29 (90%) evaluable patient episodes treated with ciprofloxacin and azlocillin/netilmicin respectively (P = 0.27). Superinfections were seen in 14% of episodes in both groups, and subsequent infections in 12% ciprofloxacin and 14% azlocillin/netilmicin treated patients. Two patients (one ciprofloxacin and one azlocillin/netilmicin) died within 48 h of randomization, and a further 13 patients (four ciprofloxacin and nine azlocillin/netilmicin) died before resolution of neutropenia. Adverse events were recorded in 9% and 15% of ciprofloxacin and azlocillin/netilmicin treated patients respectively, with skin rash (five ciprofloxacin and four azlocillin/netilmicin), nephrotoxicity (two azlocillin/netilmicin), abnormal liver function tests (two azlocillin/netilmicin), ototoxicity (one azlocillin/netilmicin) and nausea (one ciprofloxacin) being the major events recorded. It was concluded that monotherapy with ciprofloxacin at this dosage is a safe alternative to combination therapy with azlocillin/netilmicin, and has the advantages of twice daily administration, iv and oral presentations, no cross allergy in beta-lactam-hypersensitive patients, and no nephro- or oto-toxicity.

Adolescent↗
PubMed1986

Antimicrobial therapy of Pseudomonas pulmonary exacerbations in cystic fibrosis. A prospective evaluation of netilmicin plus azlocillin versus netilmicin plus ticarcillin.

High-dose anti-Pseudomonas chemotherapy is mandatory in the treatment of acute pulmonary exacerbations in patients with advanced cystic fibrosis and Pseudomonas aeruginosa isolated from their sputum. However, neither the regimen itself nor its objective evaluation have been optimized yet. In a prospective controlled evaluation 42 such exacerbations were treated for two weeks with netilmicin combined by randomisation with either azlocillin or ticarcillin. Other aspects of therapy were constant. The two therapy groups were comparable in all aspects. Both regimens produced similar improvements in clinical, radiological, laboratory, bacteriological and pulmonary function measurements. Concentrations of sputum bacteria were significantly reduced; transient eradication was documented in 29% and correlated with antibiotic susceptibility of the initially isolated Pseudomonas strains. The highly dosed antibiotics were well tolerated and emergence of resistance was rarely observed. It is concluded that both antibiotic combinations are beneficial and safe in cystic fibrosis. Monitoring of such intensive hospital treatment must include multiple parameters.

Adolescent↗
PubMed1980

Pharmacokinetics of azlocillin in subjects with normal and impaired renal function.

The pharmacokinetics of azlocillin were investigated in five healthy subjects and in 16 subjects with chronic renal failure. After intravenous bolus injection of a single dose of 30 mg/kg in normal subjects, pharmacokinetic data were calculated, using a two-compartment open body model. The mean distribution serum half-life (T(1/2alpha)) was 0.11 h, and the mean elimination serum half-life (T(1/2beta)) was 0.89 h. The volume of the central compartment (V(C)) was 7.36 liters/1.73 m(2), and the apparent volume of distribution (V(dss)) was 14.15 liters/1.73 m(2), i.e., 21.9% of body weight. The T(1/2beta) after a 30-min intravenous infusion of 80 mg/kg to the same healthy subjects was 1.11 h. Serum clearances (C(S)) for the 30- and 80-mg/kg doses were 215.0 and 152.9 ml/min per 1.73 m(2). The mean renal clearances (C(R)) were 145.2 and 94.1 ml/min per 1.73 m(2) for the respective doses. Between 61.8 and 69.6% of the injected dose was recovered in urine during the first 24 h. The elimination half-life in subjects with chronic renal impairment increased with the degree of renal insufficiency. After a 30-min intravenous infusion of 80 mg/kg the T(1/2beta) values were 2.03, 4.01, and 5.66 h with creatinine clearances (C(cr)) within 30 to 50, 10 to 30, and <10 ml/min per 1.73 m(2), respectively. Urinary elimination was inversely related to the degree of renal impairment. In four patients out of and on a 6-h hemodialysis session mean elimination half-life values were 6.53 and 2.81 h, respectively. The fraction of drug removed by dialysis was 45.8%. The linear relationships between the elimination of half-life (T(1/2beta)) and serum creatinine and the elimination rate constant (beta) and creatinine clearance (C(cr)) provided a basis for adjustment of dosage in renal failure.

Adult↗
PubMed1980

In vitro antimicrobial activity of cefoperazone, cefotaxime, moxalactam (LY127935), azlocillin, mezlocillin, and other beta-lactam antibiotics against Neisseria gonorrhoeae and Haemophilus influenzae, including beta-lactamase-producing strains.

Minimum inhibitory concentrations and agar disk diffusion tests were determined on clinical isolates of beta-lactamase-positive and beta-lactamase-negative Neisseria gonorrhoeae and Haemophilus influenzae with the newer beta-lactam antibiotics, cefoperazone, cefotaxime, moxalactam (LY127935), azlocillin, mezlocillin, and piperacillin, and with seven older beta-lactam antibiotics. All the drugs were active against beta-lactamase-negative strains of N. gonorrhoeae and H. influenzae. The drug most active against beta-lactamase-positive N. gonorrhoeae was cefotaxime, followed closely by cefoperazone, moxalactam, piperacillin, and mezlocillin. The drugs most active against beta-lactamase-positive strains of H. influenzae were cefotaxime, moxalactam, cefoperazone, and cefamandole.

Azlocillin↗
PubMed1982

Comparative penetration of azlocillin and mezlocillin into cerebrospinal fluid of normal rabbits and rabbits with experimentally induced Pseudomonas aeruginosa meningitis.

The impacts of meningeal infection with Pseudomonas aeruginosa and route of drug administration on the penetration of azlocillin and mezlocillin into the cerebrospinal fluid of rabbits were evaluated. The penetration of both agents was increased to a similar degree in rabbits with meningitis compared with normal rabbits. The increase in penetration was greater after intravenous administration than after intramuscular administration.

Animals↗
PubMed1984

Comparative efficacies of piperacillin, azlocillin, ticarcillin, aztreonam, and tobramycin against experimental Pseudomonas aeruginosa pneumonia.

The therapeutic efficacies of the newer beta-lactam antibiotics piperacillin, azlocillin and aztreonam were compared with the efficacies of ticarcillin and tobramycin in a guinea pig model of experimental Pseudomonas aeruginosa pneumonia. For animals challenged with 2 X 10(8) CFU, tobramycin treatment resulted in survival rates and intrapulmonary killing of pseudomonads which were significantly greater than those found with any of the beta-lactam agents. There were no significant differences noted among the individual beta-lactam agents. When animals were challenged with 200-fold-fewer organisms (10(6) CFU), there was no significant difference between the efficacy of tobramycin and those of the various beta-lactams. These data suggest that tobramycin is particularly valuable in treating more severe P. aeruginosa pneumonia, whereas a number of different beta-lactam agents are of equivalent value in less severe lung infections.

Animals↗
PubMed1984

Azlocillin and cefonicid penetration into bone enhanced by probenecid.

Azlocillin (AZL) and cefonicid (CFD) penetration into rabbit humerus and scapula was evaluated with and without concomitantly administered probenecid. Groups of animals received either 70 mg of AZL intravenously or 20 mg of CFD intramuscularly per kg of body weight; other groups were pretreated with 40 mg of probenecid per kg before the administration of antibiotics. Peak levels of AZL in the sera of animals not receiving probenecid were 76.0 micrograms/ml at 30 min and declined to 7.7 micrograms/ml by 2.0 h. Maximum concentrations in bone were 2.7 micrograms/g in the humerus and 7.1 micrograms/g in the scapula at 1 h. Pretreatment with probenecid significantly elevated levels of AZL in both serum and bone while increasing the half-life in serum from 0.44 to 0.65 h. Maximum drug concentrations in bones of probenecid-pretreated animals were 3.9 and 11.7 micrograms/g in the humerus and scapula, respectively, with detectable levels persisting in bone for up to 4 h. The peak level of CFD alone in serum was 36.7 micrograms/ml at 30 min and declined to 0.86 micrograms/ml at 8 h. Maximum concentrations in bone were 0.66 micrograms/g in the humerus at 1 h and 1.8 micrograms/g in the scapula at 2 h. Pretreatment with probenecid significantly elevated levels of CFD in both serum and bone while increasing the half-life in serum from 1.4 to 2.94 h. Pretreatment with probenecid achieved maximum concentrations of 1.7 and 2.8 micrograms/g in the humerus and scapula, respectively. Detectable levels of CFD persisted in the humerus for up to 4 h and in the scapula for 8 h.

Animals↗
PubMed1985

In vitro activity of ciprofloxacin combined with azlocillin.

A ciprofloxacin plus azlocillin broth microdilution checkerboard was evaluated against 125 aerobic gram-negative and gram-positive bacteria. Synergism (sigma FIC less than or equal to 0.5) occurred among 56% of Pseudomonas aeruginosa, 30% of Acinetobacter species, and 40% of Staphylococcus aureus studied. Antagonism (sigma FIC greater than or equal to 2) was present in less than 1% of the organisms.

Anti-Bacterial Agents↗
PubMed1990

In vitro activity of ciprofloxacin in combination with ceftazidime, aztreonam, and azlocillin against multiresistant isolates of Pseudomonas aeruginosa.

The combinations of ciprofloxacin plus ceftazidime, ciprofloxacin plus aztreonam, and ciprofloxacin plus azlocillin were evaluated for the presence of synergy against multiresistant isolates of Pseudomonas aeruginosa. The frequency of synergy was dependent on antibiotic susceptibilities. If the organism was resistant to ciprofloxacin, synergy was observed in more than 50% of the isolates; however, if the organism was resistant to the beta-lactam (with the exception of ceftazidime), synergy was generally observed in less than 10% of the isolates. Antagonism was not observed with any of the combinations. These results may be helpful in making clinical decisions in treating P. aeruginosa infections.

Azlocillin↗
PubMed1985

Pharmacokinetic studies of azlocillin and piperacillin during late pregnancy.

In this paper pharmacokinetic data of acylureidopenicillins (azlocillin and piperacillin) in pregnant women in the last trimenon are compared with those from nonpregnant controls. Four g of each drug was administered as slow bolus injection intravenously. The concentrations in serum and urine of both drugs were determined by polarographic and microbiological methods, for comparison. We used for evaluation of pharmacokinetic data a computer program based on the equations of a two-compartment open pharmacokinetic model. Our investigations show that there are not any different pharmacokinetic values of both antibiotics between pregnant women and healthy nonpregnant volunteers. We can state that both antibiotics are well determined by both analyzing methods which give us identical pharmacokinetic results.

Adult↗
PubMed1981

Interstitial fluid concentrations of cefsulodin, azlocillin and carbenicillin.

Cefsulodin, azlocillin and carbenicillin were administered by intramuscular injection to rats in a dose of 100 mg/kg. THe serum concentration in frequent samples after administration was determined and compared with the interstitial fluid (IF) concentration, measured with implanted paper discs enveloped in a dialysis tube. The IF concentration of cefsulodin was significantly higher than that of the other two antibiotics. The AUC in the IF was also larger for cefsulodin.

Animals↗
PubMed1989

In vitro activity of netilmicin alone and in combination with azlocillin, mezlocillin and imipenem against 149 coagulase-negative staphylococci.

Coagulase-negative staphylococci (CNS) have long been regarded as innocuous skin commensals with little pathogenic potential but they have recently become, under appropriate conditions, an important cause of infections. In fact, infections caused by CNS are an increasing problem especially, but not exclusively, in immuno-compromised patients. A total of 149 strains of CNS were identified from 47 patients admitted to the Haematology Department of Pescara Hospital from October 1986 to November 1987. The strains, isolated from different parts of the body and characterized by their methicillin susceptibility, were classified by API-Staph in 11 different groups. MICs and MBCs of netilmicin alone and combined with azlocillin, mezlocillin and imipenem were studied. For all combinations FIC and FBC indices were determined. The killing kinetics of the drugs mentioned above were also determined. Except for a few microorganisms (less than 5%), the associations showed a synergic or additive effect.

Azlocillin↗
PubMed1986

In vitro activity of piperacillin, ticarcillin, mezlocillin, ticarcillin-clavulanic acid, aztreonam, ceftazidime, azlocillin, cefoperazone, and thienamycin against Pseudomonas aeruginosa.

The in vitro susceptibility of 103 well-characterized strains of Pseudomonas aeruginosa to nine antimicrobial agents was assessed by means of the Kirby-Bauer disk diffusion assay and the microtiter minimal inhibitory concentration assay. The antimicrobials, from the most to the least active against P aeruginosa, were thienamycin greater than ceftazidime greater than piperacillin greater than azlocillin greater than cefoperazone greater than aztreonam greater than ticarcillin greater than ticarcillin-clavulanic acid greater than mezlocillin. The resistance patterns of the antimicrobial agents suggest that P aeruginosa resistant to a penicillin, cephalosporin, or aztreonam may be susceptible to thienamycin.

Anti-Bacterial Agents↗