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PubMed1992

[Synthesis and antibacterial activity of benzoylaminoacyl-penicillins and related compounds with and without acylated catechol substituents].

Synthesis and Antibacterial Activity of Benzoylaminoacyl Penicillins and Related Compounds with and without Acylated Catechol Substituents. Syntheses of benzoyl, cinnamoyl, and benzoylhydrazido glyoxyloyl aminoacyl penicillins with and without acylated catechol substituents by condensation of corresponding acids or acylchlorides with ampicillin or amoxycillin and also of a 6-a-methoxy-derivative and corresponding esters are reported. Acylated catechol substituents improve the antibacterial activity against Gram-negative bacteria, especially against Pseudomonas strains and Salmonella. MIC tests of bacterial mutants with higher outer membrane penetrability and of the corresponding wild typs show that the increase of antibacterial activity by catechol substituents is caused by improvement of the penetration through the bacterial outer membran. The affinity to penicillin binding proteins is not influenced by catechol substituents. Stability against beta-lactamases is partly higher than that of azlocillin.

Bacteria↗
PubMedDate not supplied

[Enzyme immunoassay of ampicillin in milk].

An indirect immunoassay for quantitative determination of ampicillin (range, 10-1000 ng/ml) in buffer or milk has been developed. Polyclonal antibodies were obtained against ampicillin conjugated with bovine serum albumin; the conjugate was synthesized by direct condensation using carbodiimide. The antibodies were specific for ampicillin and exhibited low cross-reactivity to other penicillins (azlocillin, 17%; penicillin G, 10%; piperacillin, 5%; and carbenicillin, 4%). Matrix effects were minimized by combining the use of a casein-supplemented buffer (content of casein, 1%) with sample dilution. The threshold of ampicillin detection in milk (diluted tenfold) was equal to 5.0 ng/ml (which corresponded to 50 ng/ml of the original sample).

Ampicillin↗
PubMed1991

[Sensitivity of bacteria of the genus Acinetobacter to antibiotics and ofloxacin].

Between 1989-1989 276 strains of Acinetobacter genus were isolated which contained: Acinetobacter calcoaceticus subsp. anitratus (n = 167), Acinetobacter calcoaceticus subsp. Iwoffi (n- = 83), Acinetobacter haemolyticus (n = 26). Their sensitivity to aminoglycoside antibiotics, beta-lactams, tetracyclines, chloramphenicol, colistin, and ofloxacin was tested. More than 90% of strains were sensitive to colistin and ofloxacin. The sensitivity to remaining antibiotics differentiated depending on species. Acinetobacter anitratus were highly resistant to Ist and IInd generation of cephalosporins, and moreover to penicillins, tetracyclines, and chloramphenicol. Cephalosporins of IIIrd generation were active against 70% of strains with exception of cefoperazone what was also the case for representatives of aminoglycosides as netilmicin and amikacin. Strains of Acinetobacter Iwoffi were in majority sensitive to all antibiotics with exception of cephalothin, cephradine and cefoperazone. More than 90% of Acinetobacter haemolyticus strains were sensitive to gentamicin, carbenicillin, azlocillin, ceftriaxone, cefotaxime and tetracyclines.

Acinetobacter↗
PubMed1990

[Occurrence of Clostridium difficile in feces of children with dysfunction of the digestive tract and other disorders].

Thousand and six hundred ninety two fecal samples from children of few weeks old up to over ten years were tested for the presence of Clostridium difficile. Most of them were treated with antibiotics and showed diarrhea symptoms. Hundred and twenty three strains of C-difficile were submitted to serological typing and their sensitivity to 10 selected antibiotics and chemotherapeutic agents was determined. Among 109 strains of C. difficile tested for enterotoxin production by latex test 82 strains (75.2%) were positive. Almost half (48%) of the isolated strains belonged to serotype C. Most of the strains were resistant to cefoxitin (88%) and clindamycin (76%). Over 90% of strains were sensitive to vancomycin and azlocillin and 86% to chloramphenicol and metronidazole. In the majority of patients with positive C. difficile cultures diarrhea was present, however, it was difficult to find a direct link between these symptoms and antibiotic therapy.

Adolescent↗
PubMed1990

[Antibacterial activity of carumonam and cefpirome on hospital strains resistant to gentamicin and cephalothin: comparison with other beta-lactam antibiotics, new fluoroquinolones, aminoglycosides and other antibiotics].

The antibacterial in vitro activity of carumonam, a new monobactam, and cefpirome, a new cephalosporin, was studied on 483 hospital strains resistant to gentamicin and cephalothin, in comparison with amikacin, azlocillin, aztreonam, cefmenoxim, cefoperazone, cefotaxim, cefsulodin (for Pseudomonas), ceftazidime, ceftriaxone, cefuroxim, chloramphenicol, ciprofloxacin, doxycycline, enoxacin, netilmicin, norfloxacin, pefloxacin, piperacillin, rifampicin, tobramycin and trimethoprim. In general the two compounds have a very good in vito activity on Enterobacteriaceae but are less active on non-fermenting microorganisms. For the Enterobacteriaceae the minimal inhibitory concentrations 90% for carumonam was less than or equal to 1.1 mg/l excepted for Enterobacter spp. (43,6 mg/l) and M. morganii (56.8 mg/l) . All the Enterobacteriaceae are susceptible to cefpirome (minimal inhibitory concentrations 90% less than or equal to 5.3 mg/l). The activity of carumonam and cefpirome on Enterobacteriaceae is comparable with that of the third generation cephalosporins. Carumonam is more active than cefpirome and other beta-lactams, ceftazidime excepted, on Pseudomonas aeruginosa and Pseudomonas spp. On the other hand, both compounds reveal to have only a low activity on the other non-fermenters which minimal inhibitory concentrations 90% values of 115.4 mg/l for carumonam and 32.0 mg/l for cefpirome.

Aminoglycosides↗
PubMed1990

Antibiotic therapy in septic shock.

Septic shock is a life-threatening illness characterized by hypotension, impaired organ function and/or failure, and metabolic abnormalities. Septic shock can develop in patients infected with a variety of gram-positive and gram-negative bacteria, viruses, fungi, rickettsiae, spirochetes, protozoa, and parasites. Immediate recognition, diagnosis, and treatment are key elements in reducing the morbidity and mortality associated with this condition. Rapid administration of appropriate antibiotics in correct doses plays a major role in patient survival. Infections with gram-negative bacteria appear to be associated with septic shock more than any other etiologic agent; therefore, antibiotic selection must include those drugs with superior gram-negative coverage. The selection of appropriate antibiotics should be based on sound clinical judgement plus knowledge of the antimicrobials used. The principles of rational therapy include the following: (1) know the type of microorganisms or suspected organism being treated; (2) be familiar with resistant organisms in both the community as well as the hospital; and (3) initiate combination therapy with a beta-lactam antibiotic plus an aminoglycoside or use monotherapy with either a carbapenem or selected third generation cephalosporin. After culture results are known, the antibiotic regimen should be narrowed to cover the specific infecting microorganism using the least expensive, least toxic antibiotic available. The beta-lactam antibiotics include all penicillins, cephalosporins, carbapenems, and monobactams. Penicillins with extensive gram-negative coverage include all the carboxy (carbenicillin, ticarcillin, and ticarcillin plus clavulanic acid) and ureido (piperacillin, mezlocillin, azlocillin) penicillins. The third generation cephalosporins (cefoperazone, cefotaxime, ceftazidime, ceftizoxime, ceftriaxone, and moxalactam) have the broadest gram-negative coverage within the cephalosporin family.(ABSTRACT TRUNCATED AT 250 WORDS)

Anti-Bacterial Agents↗
PubMed1990

Phenotypic properties of Klebsiella pneumoniae and K. oxytoca isolated from different sources.

474 Klebsiella pneumoniae and K. oxytoca strains isolated from different sources (human clinical material, feces of healthy subjects, sewage) were investigated for phenotypic properties. Characteristics analyzed were cultural activities, antimicrobial susceptibilities and capsule types. Comparison of both species revealed differences in adonitol fermentation and resistance to tetracycline, nalidixic and pipemidic acid. Capsule types 2, 7 and 33 were frequently found in K. pneumoniae, but not in K. oxytoca. On the other hand, K 66 was common in K. oxytoca, but not in K. pneumoniae. With regard to the source of isolation, clinical strains of both species proved to be more resistant to mezlocillin, azlocillin and cephalothin than fecal and sewage strains. Similarly, resistances of K. pneumoniae to cotrimoxazole, nalidixic and pipemidic acid were most frequent in clinical strains. Multiple drug resistances were found most often in clinical isolates. Biochemically, different frequencies of positive reactions for urease, lysine decarboxylase activity and acetoin production were found between the groups. Capsule typing demonstrated K2 and K7 in K. pneumoniae and K55 and K66 in K. oxytoca to be more common in clinical and fecal isolates than in sewage strains. While cultural characteristics did not allow discrimination of strains from different sources, capsule typing indicated clinical isolates to be more phenotypically related to strains from feces than to sewage isolates.

Bacterial Typing Techniques↗
PubMed1986

[Antibacterial activity of a number of preparations and their combination with a proteolytic enzyme against the microflora of burn and surgical wounds].

Antibacterial activity of antibiotics (azlocillin, tobramycin and piperacillin), antiseptics (metacid, chlorhexidine and quinosoline) and some other drugs (dioxidine and mafenide acetate) against the main representatives of the burn and surgical wound microflora, i. e. Staphylococcus, P. aeruginosa, Proteus, Providencia, Serratia, Klebsiella and E. coli was studied. Tobramycin and piperacillin were highly active against P. aeruginosa, Staphylococcus and Proteus. It was shown that in the presence of terrilytin, a proteolytic enzyme the activity of the combinations of chlorhexidine with dioxidine or mafenide acetate against all microorganisms occurring in burn and surgical wounds markedly increased.

Administration, Topical↗
PubMedDate not supplied

[Sensitivity to antibiotics of Pseudomonas aeruginosa isolated from patients in the years 1986-1988].

Pseudomonas aeruginosa strains (240 in all) isolated from various clinical materials in the years 1986-1988 showed a high sensitivity to amikacin (92.3-100%), colistin (84.6-100%) and ceftazidim (84.6-100%). Netilmycin acted on 75.4% of the strains, and penicillins (carbenicillin, ticarcillin and azlocillin) similarly as gentamicin, tobramycin, cefotaxim, cefoperazon and ceftriaxon were active only against 51.3-66.7% of the tested strains.

Anti-Bacterial Agents↗
PubMed1989

[Listeriosis in the adult: presentation of 14 cases].

The incidence of Listeria monocytogenes (LM) infection has increased in recent years, particularly in immunocompromised patients or in those with severe underlying diseases. However, it still is an unusual pathogen. In the present study we report 14 cases of listeriosis in adults, seen from 1978 to 1988. The organism was isolated from the blood in 10 instances, from cerebrospinal fluid in 5, and from a cervical abscess in one. The ages of the patients ranged from 29 to 81 years and there was a clear male predominance. In all cases except in one there was a previous underlying disease, and four had received immunosuppressant therapy. Listeria monocytogenes was sensitive to ampicillin, erythromycin, vancomycin, gentamicin, rifampicin, ticarcillin, azlocillin, mezlocillin and tetracyclines.

Adult↗
PubMed1989

[Analysis of phenotype resistance of clinical strains of Escherichia coli].

The multiplasmid clinical E. coli KL4 strain isolated from urine of a patient was examined for resistance to antibacterial substances and the number of plasmids. The distribution of resistance genes to antibiotics in different plasmids was assessed. All assessed resistances were transmitted by the mechanism of bacterial conjugation. By means of conjugation of the clinical E. coli strain KL4 and E. coli DH1, transformation of the DH1 strain by plasmid DNA and electrophoretic analysis two R plasmids were identified. The largest plasmid carries the gene for resistance against tetracycline and it is conjugative. Another three plasmids were mobilized by this plasmid during conjugation. The largest among them codes resistance against ampicillin, azlocillin and ticarcillin. From the total of five plasmids of the KL4 strain three were cryptic with regard to the resistance phenotype.

Drug Resistance, Microbial↗
PubMed1989

[Affinity of penicillin-binding proteins of Escherichia coli K-12 for furbenicillin and other beta-lactam antibiotics].

Penicillin-binding proteins (PBP) are vitally important targets in relation to the killing of bacteria by beta-lactams. The affinities of PBP of Escherichia coli K 12 for ampicillin, mecillinam and for ureidopenicillins were studied by sodium dodecylsulphate polyacrylamide slab gel electrophoresis and fluorography. The results showed that furbenicillin, a semisynthetic ureidopenicillin developed in China, bound to all 3 essential target proteins of E coli. The IC50 values of furbenicillin to PBP 1 b, PBP 2 and PBP 3 were 4.55 mg/L, 0.37 mg/L and 0.06 mg/L, respectively. The affinities of the 3 proteins of E coli for furbenicillin were 2.5-, 3.5-, and 2.5-fold, respectively higher than that of azlocillin. Mecillinam bound exclusively to PBP 2 (IC50: 0.16 mg/L). Mezlocillin and piperacillin showed higher affinities for PBP 3 than furbenicillin, but their affinities for PBP 1 b and PBP 2 were much lower than furbenicillin.

Anti-Bacterial Agents↗
PubMed1989

[Why is peroperative antibiotic prophylaxis of infectious complications most effective?].

The concentrations of oxacillin, azlocillin, temocillin, amoxycillin, cefoperazone, cefazoline, netilmicin, clindamicin, ofloxacine in serum and coagulum take a parallel course but their content in the coagulum is ten times lower than in serum--with the exception of doxycycline which reached a 40% value of the serum level in the coagulum. From this ensues that most effective are those antibiotics which can be administered in large doses and which have a long half-life. Unfavourable are antibiotics with a narrow therapeutic range and those with a short half-life. Preoperative application of such doses which create sufficiently high and prolonged levels is the optimal method of antibiotic prophylaxis of infectious complications during surgical operations.

Anti-Bacterial Agents↗
PubMed1989

[Effect of beta-lactam antibiotics on lipid bilayer membranes. I. Penicillin antibiotics].

Interaction between penicillins and model membrane systems, flat black bilayer lipid membranes (BLM) composed of vegetable or bacterial phospholipids was studied with an account of the complicated structure of bacterial cell membranes and possible presence in them of "pure" bilayer lipid areas. By their effect on electroconductivity of the BLM the antibiotics could be divided into three groups: those having no effect on the BLM electroconductivity at the maximum concentrations i.e. benzylpenicillin, carbenicillin, piperacillin (at pH 6.0 and 7.0) and ampicillin (at pH 6.0), those insignificantly changing electroconductivity of the BLM i.e. carfecillin and azlocillin and those having a significant effect on the BLM electroconductivity i.e. ampicillin N-acyl derivatives and 6-APA. The effect of ampicillin on the BLM conductivity markedly depended on the electrolite pH. The penicillins bound to the bilayer and induced changes in the transmembrane potential (evident from the changes in the second harmonic of the capacitive current) and the BLM elasticity-capacitance parameters (evident from the changes in the ratio of the amplitudes of the first and third harmonics). It was shown that all the penicillins penetrated through the BLM composed of either vegetable or bacterial phospholipids. The capacity for the transmembrane transfer without changing of the bilayer conductivity must be connected with the fact that the penetrating antibiotics did not induce any changes in the BLM structure. The effect on the conductivity probably depended in its turn on the form of the molecule and the ratio of the hydrophilic and hydrophobic parts in it.

Electrolytes↗
PubMed1986

Sensitivity of 115 strains of the genus Brucella to some antibiotics (cephalosporins, ureidopenicillins and aminoglycosides).

The Authors tested piperacillin, azlocillin, aztreonam, cefotaxime, ceftizoxime, ceftriaxone, cefotetan, moxalactam, gentamicin, sisomicin and dibekacin, on about 120 strains of the genus Brucella, using as control drugs tetracycline, streptomycin and rifampicin. Cefotaxime, ceftizoxime, gentamicin, and sisomicin exhibited antibrucella activity comparable to that of tetracycline and just a little superior to that of rifampicin. Among the aminoglycosides tested, gentamicin, sisomicin and dibekacin were, in decreasing order, more active than streptomycin. For all the other drugs tested there was a large variability among the brucella strains, with roughly a peak of activity on the strains which have a history of repeated in vitro passages.

Aminoglycosides↗
PubMed1988

[The new penicillins].

During recent years, new antibacterial beta-lactams have been identified. The association of beta-lactams and beta-lactamase inhibitors (clavulanic acid or sulbactam) represent a new therapeutic approach. The other drugs are classified into ureodopenicillins (mezlocillin, azlocillin, piperacillin), amidinopenicillins (mecillinam, pivmecillinam), monobactam (aztreonam) and penems (imipenem). Three mechanisms are involved in the bacterial resistance to these beta-lactams: inability to cross the bacterial membrane, inactivation of the antibiotic by a beta-lactamase, modification of the number of porines. The tolerance to these new products is good but they present a high risk for selection of resistant bacteria. These antibiotics markedly improve the treatment of beta-lactamase producing bacterial infections, particularly related to Pseudomonas aeruginosa.

Anti-Bacterial Agents↗
PubMed1987

Emerging microorganisms in cystic fibrosis.

Pseudomonas aeruginosa is the most common bacterial isolate obtained from patients with cystic fibrosis of the lungs. Recently, however, new multiresistant organisms have emerged, whose identification may be difficult and whose pathogenic role proves hard to define. Of the 71 strains isolated from 24 patients with cystic fibrosis during acute flareups of pulmonary symptoms, 48 turned out to be Pseudomonas aeruginosa (67.6%); 11 were Pseudomonas non-aeruginosa (15.5%); and 12 were Achromobacter xylosoxidans (16.9%). Each bacterial isolate was tested for sensitivity to nine antibiotics (ceftazidime, azlocillin, piperacillin, aztreonam, cefsulodin, cefoperazone, amikacin, tobramycin, and sisomycin) in terms of minimum inhibitory concentration and minimum bactericidal concentration values. In this series, Achromobacter xylosoxidans proved the species least responsive to treatment, and ceftazidime the most active antibiotic both against Achromobacter and against strains of the genus Pseudomonas. Twenty-three different associations of ceftazidime with aminoglycosides, tested for activity on the multiresistant strains, failed to show synergism of action.

Alcaligenes↗
PubMed1987

N-acetylcysteine and 2-mercaptoethane sulphonate inhibit anti-pseudomonas activity of antibiotics in vitro.

The in vitro activity against Pseudomonas aeruginosa was investigated for serial dilutions of eight anti-Pseudomonas antibiotics in combination with serial dilutions of N-acetylcysteine (NAC) and 2-mercaptoethane sulphonate (MES). The results indicated that addition of NAC and MES to the antibiotics increased the MIC values for tobramycin, netilmicin, piperacillin, azlocillin, cefsulodin, ceftazidime and imipenem but not for colistin. The decrease of MIC found in high concentrations of NAC and MES was probably due to the bacteriostatic effect of the drugs per se and not to synergism with the antibiotics.

Acetylcysteine↗