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PubMed1985

Decreased biliary excretion of piperacillin after percutaneous relief of extrahepatic obstructive jaundice.

The biliary excretion of piperacillin has been assessed in 11 patients with obstructive jaundice due to hilar cholangiocarcinoma. After a 1-g intravenous dose administered 30 min before preliminary percutaneous transhepatic cholangiography, no drug was detected in the bile of seven patients; in four others, drug concentrations were far below the corresponding level in serum. After a period of external biliary drainage of up to 28 days, levels of antibiotic in bile after intravenous administration were only minimally increased. The results suggest that although the impairment of hepatic function may be improved by external biliary decompression when assessed by a fall in plasma bilirubin, the biliary elimination of piperacillin and related beta-lactam antibiotics may remain impaired for prolonged periods.

Adult↗
PubMed1994

Penetration of piperacillin-tazobactam into cancellous and cortical bone tissues.

The penetration characteristics of piperacillin-tazobactam into cortical and cancellous bone tissues were investigated in 10 patients undergoing total hip replacement. The concentration ratios of piperacillin/tazobactam were 9.4 +/- 1.8 in cancellous bone tissue and 8.0 +/- 2.2 in cortical bone tissue, which were close to the 8:1 ratio of drugs administered. The mean ratios of drug concentrations in bone and plasma for cancellous and cortical tissue were 23 and 18%, respectively, for piperacillin and 26 and 22%, respectively, for tazobactam. The concentrations of tazobactam achieved are sufficient to exert anti-beta-lactamase activity and supportive of clinical trials involving bone and joint infections, including those caused by beta-lactamase-producing pathogens.

Adult↗
PubMed1997

Efficacies of piperacillin-tazobactam and cefepime in rats with experimental intra-abdominal abscesses due to an extended-spectrum beta-lactamase-producing strain of Klebsiella pneumoniae.

The in vivo activities of piperacillin-tazobactam and cefepime were compared with those of ticarcillin-clavulanate, ceftazidime, cefotaxime, and imipenem in a rat model of intra-abdominal abscess with a strain of Klebsiella pneumoniae elaborating an extended-spectrum beta-lactamase (TEM-26). With the exception of ceftazidime, all of the antimicrobial agents significantly reduced bacterial counts within abscesses at the end of therapy compared with those in untreated controls. Residual viable cell counts (mean +/- standard deviation in log10 CFU/gram) were as follows: control, 8.76 +/- 0.97; ceftazidime, 8.00 +/- 0.76; piperacillin-tazobactam, 3.87 +/- 1.72; ticarcillin-clavulanate, 3.74 +/- 1.34; cefepime, 3.15 +/- 1.19; cefotaxime, 2.61 +/- 0.77; imipenem, 2.41 +/- 0.93. Imipenem was more effective than either of the inhibitor combinations (P < 0.05). Cefotaxime was unexpectedly effective given its poor in vivo activity against this organism in our earlier studies, which used a different dose and total duration of therapy (L. B. Rice, J. D. C. Yao, K. Klimm, G. M. Eliopoulos, and R. C. Moellering, Jr., Antimicrob. Agents Chemother. 35:1243-1244, 1991). These observations suggest that the effectiveness of cephalosporins in the treatment of experimental infections caused by extended-spectrum beta-lactamase-producing K. pneumoniae may be highly dependent on dosing regimens, even for a specific organism and site of infection.

Abdominal Abscess↗
PubMed2001

Cefepime, piperacillin-tazobactam, and the inoculum effect in tests with extended-spectrum beta-lactamase-producing Enterobacteriaceae.

There is little information about the clinical effectiveness of cefepime and piperacillin-tazobactam in the treatment of infections caused by extended-spectrum beta-lactamase (ESBL)-producing pathogens. Some inferences have been drawn from laboratory studies, which have usually involved only one or a few strains of ESBL-producing Klebsiella pneumoniae or Escherichia coli that produced only a limited range of ESBLs. Such studies are indirect, sometimes conflicting, indicators of efficacy. To extend previous laboratory findings, a study was designed to investigate organism-drug interactions by determining the in vitro activities of eight parenteral beta-lactam agents against 82 clinical and laboratory strains of Klebsiella, Escherichia, Enterobacter, Citrobacter, Serratia, Morganella, and Proteus species that produced 22 different ESBLs, alone or in combination with other beta-lactamases. Activities were determined in broth microdilution MIC tests using standard and 100-fold-higher inocula. An inoculum effect, defined as an eightfold or greater MIC increase on testing with the higher inoculum, was most consistently detected with cefepime, cefotaxime, and ceftriaxone and least frequently detected with meropenem and cefoteten. Piperacillin-tazobactam was intermediate between these two groups of agents. Although the inoculum effect is an in vitro laboratory phenomenon, if it has any predictive value in identifying increased risk of therapeutic failure in serious infections, these results support suggestions that cefepime may be a less-than-reliable agent for therapy of infections caused by ESBL-producing strains.

Anti-Bacterial Agents↗
PubMed1993

Susceptibility of Haemophilus influenzae to piperacillin-tazobactam combinations: interpretive criteria and quality control limits for standardized tests.

In vitro studies evaluated methods for testing the susceptibility of Haemophilus influenzae to piperacillin-tazobactam combinations. Ampicillin-resistant beta-lactamase-nonproducing strains of H. influenzae may be presumed to be relatively resistant to combinations of piperacillin-tazobactam, even though they frequently appear to be susceptible by disk diffusion methods. Other ampicillin-resistant or -susceptible strains were predictably susceptible; i.e., 130 such strains gave zones of inhibition > or = 26 mm in diameter, and MICs for these strains were < or = 0.125/4.0 micrograms/ml (< or = 1.0/0.12 micrograms/ml when an 8:1 ratio was tested). A resistant category has yet to be defined. For quality control purposes, H. influenzae ATCC 49247 should give zones of inhibition 32 to 38 mm in diameter, and broth microdilution MICs should be 0.12/4.0 to 0.5/4.0 micrograms/ml.

Ampicillin Resistance↗
PubMed1987

Single dose piperacillin in treating uncomplicated gonococcal urethritis in men.

A single intramuscular dose of piperacillin 2 g, with probenecid 1 g orally, was used to treat 82 men with uncomplicated gonococcal urethritis due to penicillinase producing strains of Neisseria gonorrhoeae (PPNG) or non-PPNG. All 49 patients infected with non-PPNG strains were cured, as opposed to only 25 (76%) of 33 patients infected with PPNG strains, giving an overall success rate of 90%. No serious side effects of treatment were observed. Post gonococcal urethritis (PGU) occurred in 18% of the patients treated. Antibiotic susceptibility tests showed that 44 (96%) of the 46 non-PPNG strains tested had MICs of piperacillin of 2 mg/l or less and 26 (76%) of the 34 PPNG strains had MICs of 32 mg/l or more. This regimen is not recommended for use as first line treatment in areas where there is a high incidence of infection with PPNG strains. It is, however, highly effective against non-PPNG strains.

Drug Administration Schedule↗
PubMed1982

Dose dependence of piperacillin pharmacokinetics.

Pharmacokinetics were evaluated for piperacillin given as doses of 15, 30 and 60 mg/kg body weight to 12 healthy volunteers subdivided into three groups which were each given different dosage levels. For the 15, 30 and 60 mg/kg doses, the serum half-lives were 0.8, 1.0 and 0.9 h, and the disposition phase distribution volume coefficients, delta d. beta, 0.31, 0.30, ad 0.25 l/kg. The total body clearances for the three doses normalized to 70 kg body weight were 18.53, 14.00 and 13.53 l/h for the 15, 30 and 60 mg/kg doses, respectively. The corresponding values for the total area under the curves per 1.0 g dose were 57.1, 75.0 and 79.6 micrograms/ml. The urinary elimination of the antibiotic corresponding to the antimicrobial activity of unchanged drug rose from 50.0 to 71.3% of the dose, for a dose increment of 15 to 60 mg/kg. These results document that piperacillin is subject to dose-dependent pharmacokinetics. Capacity-limited kinetics is a property shared by other ureidopenicillins.

Adult↗
PubMed1984

Fosfomycin, piperacillin, azlocillin. Correlation between therapeutic response of mice infected with Pseudomonas aeruginosa and in vitro data.

Intramuscular infections of mice with eight different strains of Pseudomonas aeruginosa were treated with three doses each of fosfomycin, piperacillin and azlocillin. The therapeutic response (measured as decrease in colony-forming units in the homogenized infected tissue) was compared with the 'aggregate suprainhibitory time' (the time for which the serum concentration exceeds the minimal inhibitory concentration of the infecting bacteria during the whole treatment period). The therapeutic response improved with increasing aggregate suprainhibitory time. The correlation was better for fosfomycin than for piperacillin and, especially, azlocillin.

Animals↗
PubMed1985

Penetration of latamoxef, cefoperazone and piperacillin into the sputum of patients with cystic fibrosis.

Concentrations of latamoxef, cefoperazone and piperacillin, administered intravenously, were measured in serum and sputum of cystic fibrosis patients with recurrent pulmonary infections, chronically colonized with Pseudomonas aeruginosa. Serum pharmacokinetic data were consistent with prior reports. Peak sputum to peak serum concentrations were approximately 3% for each antimicrobial. However, the more prolonged sputum concentrations of piperacillin were reflected in greater areas under the sputum concentration-time curve and a longer duration above the MIC50 of tested P. aeruginosa strains for that drug.

Adolescent↗
PubMed1991

[The effect of sulbactam on the in vitro activity of mezlocillin, piperacillin and cefotaxime].

The in vitro activity of mezlocillin (MZL, CAS 51481-65-3), piperacillin (PIP, CAS 61477-96-1) and cefotaxim (CTX, CAS 63527-52-6) alone and in combination with sulbactam (SBT; CAS 68373-14-8) against mezlocillin-resistant pathogens was determined in a multicenter study. A total of 870 strains were investigated (481 Enterobacteriaceae, 57 Pseudomonas aeruginos, 41 Acinetobaster spp., 194 Bacteroides fragilis, and 97 Staphylococcus spp.). Determinations of MIC were performed according to DIN-guidelines (agar-dilution method for aerobes and microbroth-dilution method for anaerobes). Sulbactam was added in fixed concentrations of 5 mg/l and 10 mg/l. In all sulbactam-combinations examined mean MIC as well as MIC50 and MIC90 were reduced compared to the respective values for the antibiotics alone. Consequently, percentages of susceptible strains increased significantly: i.e. for Enterobacteriaceae: MZL 1% vs. MZL + 10 mg/l SBT 53%; PIP 4% vs. PIP + 10 mg/l SBT 54%; CTX 52% vs. CTX + 10 mg/l SBT 68%. The effect of sulbactam was most pronounced in Bacteroides spp. with an increase in susceptible strains from 2% to 97% for MZL, from 6% to 95% for PIP and from 7% to 98% for CTX. The results indicate that by adding sulbactam the in vitro activity of mezlocillin, piperacillin and cefotaxim against resistant pathogens is augmented significantly. In addition, the spectrum of antibacterial activity is extended to anaerobic pathogens such as Bacteroides spp. The availability of sulbactam as a monosubstance for combination with various beta-lactam-antibiotics thus represents a useful improvement of therapeutic options in bacterial infections.

Acinetobacter↗
PubMed1991

[Sulbactam in combination with mezlocillin, piperacillin or cefotaxime. Clinical and bacteriological results in the treatment of severe bacterial infections].

An open multicenter study on inpatients of 12 german hospitals was performed to investigate efficacy and safety of sulbactam in combination with mezlocillin, piperacillin or cefotaxim in severe bacterial infections. In total 155 patients were enrolled. The following infections were diagnosed: 48 lower respiratory tract infections, 66 intraabdominal infections, 34 skin/soft tissue infections including post operative wound infections and 5 complicated urinary tract infections. 55 patients received 3 daily doses of 4 g mezlocillin + 1 g sulbactam, 52 patients received 3 daily doses of 4 g piperacillin + 1 g sulbactam and 48 patients received 3 daily doses of 2 g cefotaxim + 1 g sulbactam. Antibiotics and sulbactam were administered concomitantly via intravenous short infusion. Mean duration of therapy was 8 days. Endpoints for assessment of therapeutic efficacy were cure (complete resolution of pretreatment signs and symptoms of the infection) or improvement (marked reduction or partial disappearance or pretreatment signs and symptoms, no further antibiotic therapy required) as well as eradication of pretreatment pathogens. 141 (92%) of 153 evaluable patients were successfully treated (98 cures and 43 improvements), therapy failed in 12 patients (7.8%). Success rates of the 3 sulbactam combinations were almost identical: 91% for mezlocillin/sulbactam, 92% for piperacillin/sulbactam and 93% for cefotaxim/sulbactam. 106 patients (68.4%) were also bacteriologically evaluable. In these patients 192 bacterial pathogens were isolated prior to study therapy, 55 patients had mixed infections. In 96 patients (90%) pretreatment pathogens were eradicated (180 strains = 94%).(ABSTRACT TRUNCATED AT 250 WORDS)

Adolescent↗
PubMedDate not supplied

[Antibiotic prophylaxis. Single-dose piperacillin in abdominal hysterectomy].

Several studies have confirmed the effectiveness of antibiotic prophylaxis in gynecological surgery. We prospectively evaluated 181 women undergoing abdominal hysterectomy, randomly divided in two groups. One of them received 2 g of piperacillin 30 minutes before the operation and the other 4 g of the same group with the same interval. The effectiveness of both prophylactic piperacillin regimens for the prevention of infective postoperative morbidity was compared. Statistically significant differences between the two prophylactic regimens were not found in the analysis of the results.

Adult↗
PubMed1990

[Antibiotic prophylaxis with piperacillin in vaginal hysterectomy. Study of 1 dose versus 3 doses].

A homogeneous and consecutive series of 93 patients treated with vaginal hysterectomy is studied in a controlled, randomized clinical essay. The patients were divided in two groups. One of the groups received one single dose of 49 of piperacillin 30 minutes before surgery; the other, three doses of 4 g of the same antibiotic 30 minutes before surgery and 6 & 12 hours after it. No significant difference was found between both groups and therefore it is fair to suppose that one single preoperative dose of piperacillin shows similar efficacy to the usually used three doses, one preoperative and two postoperative.

Bacterial Infections↗
PubMed1990

The postantibiotic effect of amikacin alone and in combination with piperacillin on gram-negative bacteria.

The in vitro postantibiotic effect (PAE) of amikacin was investigated using a bioluminescent assay of bacterial ATP. Two strains each of Escherichia coli, Pseudomonas aeruginosa and Serratia marcescens were exposed for one hour to different concentrations of amikacin. The aminoglycoside was removed by a 10(-3) dilution and regrowth of bacteria was followed at hourly intervals by monitoring bacterial ATP. The length of the PAE was concentration-dependent and was approximately four to six hours for the three strains at amikacin concentrations normally reached in serum during standard dosing. The PAE of amikacin in combination with 32 mg/l piperacillin on Ps. aeruginosa was also studied. These cultures were incubated with piperacillin for one hour. Thereafter different concentrations of amikacin 0.5-64 mg/l were added and the incubation then continued with the combinations for one more hour. The PAEs produced by the drugs in combination were longer than the sum of the individual effects of the drugs when they were used alone. Knowledge of synergistic PAE could have clinical implications for optimal dosing schedules during combination antimicrobial chemotherapy.

Amikacin↗
PubMedDate not supplied

Multicenter in vitro comparison of piperacillin and nine other antibacterials against 1,629 clinical isolates.

The antibacterial spectrum of activity of piperacillin was compared with that of other antibiotics against isolates of Escherichia coli, Enterobacter cloacae, Haemophilus influenzae, Klebsiella pneumoniae, Pseudomonas aeruginosa, Pseudomonas cepacia, Pseudomonas maltophilia, Serratia marcescens, Enterococcus sp, Bacteroides fragilis, Bacteroides bivius, and Clostridium difficile obtained from laboratories at hospitals in St. Louis, in Memphis, and in Newark, New Jersey. Of the 1,629 isolates tested, 91% were susceptible to piperacillin, 90% to mezlocillin, 87% to ticarcillin/clavulanate and imipenem, 83% to ceftazidime, 81% to cefoperazone, 80% to ciprofloxacin, 77% to ceftriaxone, 71% to aztreonam, and 51% to cefoxitin.

Anti-Bacterial Agents↗
PubMed1990

[Clinical comparative study of intravenous piperacillin sodium or injection of scutellaria compound in patients with pulmonary infection].

In this survey, 60 patients with pulmonary infection (mainly nosocimial pneumonia) were divided into two groups randomly. 30 patients treated by injection of Scutelleria compound and 30 patients by intravenous piperacillin sodium as control. Before treatment there was no significant difference of clinical data between two groups. The total efficacy was evaluated after treatment for one week. 40%, 36.7% were marked effective in corresponding. 33.3%, 40% were effective and 26.7%, 23% were ineffective respectively. Total effective rates were 73.3% and 76.7% in corresponding group. Temperature was average decreased for 7.43 +/- 3.02 and 7.63 +/- 5.79 days, symptoms disappeared or relieved for 11.67 +/- 6.75 days and 11.53 +/- 7.30 days, leucocyte decreased to normal on 9.03 +/- 6.53 days and 10.13 +/- 6.23 days, roentgenographical shadows disappeared or became smaller for 16.1 +/- 7.02 days and 16.1 +/- 9.88 days in corresponding group. There were no side-effect of the functions of liver, kidney and medulla ossium in two groups. In piperacillin sodium group, fungal infection were found in 4 of 30 patients, but there was no any case suffered from fungal infection in injection of Scutelleria compound group. It was suggested that injection on Scutelleria compound is a hopeful preparation and should be studied further.

Adult↗
PubMed1990

[Clinical experience with piperacillin in the prophylaxis of post-operative infections].

Ninety patients who had undergone surgery have been treated with piperacillin as a prophylaxis for hospital infections. Twenty-two (24.4%) emergency operations and sixty-eight (75.6%) elective ones have been performed. Thirty-five open drainages, seven vacuum drainages and fifty-five urinary catheters have been placed. Post-operative infections occurred in 18 patients (20%), five of them submitted to emergency operations and thirteen submitted to elective operations. In eight cases an open drainage had been placed and in three cases a vacuum rate. The Author concludes that the hospital infections rate agrees with that occurring in the quoted sources; that open drainages, especially if placed through surgical wound, have main responsibilities for infections, and that piperacillin acted as a very well tolerated antibiotic and a highly manageable and effective one, offering therefore a good prophylaxis for hospital infections.

Adolescent↗