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PubMed1983

Treatment of chronic pseudomonas aeruginosa infection in cystic fibrosis patients with ceftazidime and tobramycin.

50% inhibitory concentration (IC50) and minimum inhibitory concentration (MIC) of ceftazidime, cefsulodin, cefotaxime, moxalactam, azlocillin, carbenicillin, netilmicin and tobramycin against 90 strains of Pseudomonas aeruginosa isolated from cystic fibrosis (CF) patients were determined by means of the agar plate dilution method. Ceftazidime was most active of the antibiotics in vitro; the geometric mean of IC50 was 0.2 and of MIC 0.4 micrograms/ml. 11 CF patients suffering from P. aeruginosa infection were treated with 14 day courses of ceftazidime (100 mg/kg/24 h) and tobramycin (10 mg/kg/24 h). P. aeruginosa was only temporarily eradicated in one of the patients, but a significant improvement of respiratory function and a significant fall in white blood cell count was recorded in the patients during chemotherapy. There was no development of resistant strains against ceftazidime during treatment and no side-effects were observed. Ceftazidime is a promising new antimicrobial agent with high in vitro activity which deserves further in vivo evaluation in CF patients.

Adolescent↗
PubMed1999

The penicillins.

The penicillin family of antibiotics remains an important part of our antimicrobial armamentarium. In general, these agents have bactericidal activity, excellent distribution throughout the body, low toxicity, and efficacy against infections caused by susceptible bacteria. The initial introduction of aqueous penicillin G for treatment of streptococcal and staphylococcal infections was an important pharmacologic landmark. The emergence of penicillinase-producing Staphylococcus aureus prompted the development of the penicillinase-resistant penicillins (for example, methicillin, oxacillin, and nafcillin), in which an acyl side chain prevented disruption of the beta-lactamase ring. Subsequently, the aminopenicillins (ampicillin, amoxicillin, and bacampicillin) were developed because of the need for gram-negative antimicrobial activity. Their spectrum initially included Escherichia coli, Proteus mirabilis, Shigella, Salmonella, Listeria, Haemophilus, and Neisseria. The search for a penicillin with additional antimicrobial activity against the Enterobacteriaceae and Pseudomonas aeruginosa led to the development of the carboxypenicillins (carbenicillin and ticarcillin) and the ureidopenicillins (mezlocillin, azlocillin, and piperacillin). Finally, the combination of a beta-lactamase inhibitor (clavulanic acid, sulbactam, or tazobactam) and an aminopenicillin, ticarcillin, or piperacillin has further extended their antibacterial spectra by inhibiting certain beta-lactamases (non-group 1) of resistant bacteria. The development of an ideal penicillin that is rapidly bactericidal, nonsensitizing, nontoxic, bioavailable, and resistant to beta-lactamases and that has a high affinity for penicillin-binding proteins remains the goal.

Humans↗
PubMed2006

Placental transfer of antibiotics administered to the mother: a review.

BACKGROUND: The purpose of antibiotic treatment in pregnant women is to treat the mother and/or the fetus since it is known that antibiotics administered to the mother cross the placenta and reach the fetus. A comparison of the drug concentration in maternal and fetal plasma gives an indication of the exposure of the fetus to the maternally administered antibiotics. AIM: The aim of this study was to review the literature pertaining to the placental transfer of antibiotics in man and to classify the antibiotics according to the type of transfer involved. A table has been developed for use by physicians that lists the name of the antibiotic, the drug concentration in the cord and maternal plasma at delivery and the type of transfer involved. METHODS: An initial medline search was performed with the key words "placental transfer of antibiotics" with the limit of "human". A second medline search was performed with the key words "placental transfer of..." followed by the class names of the antibiotic such as penicillins, cephalosporins, aminoglycosides, tetracyclines and macrolides. The bibliographic search on the placental transfer of antibiotics covered the period up to July 2005. RESULTS: 3 types of placental transfers were identified. A few antibiotics cross the placenta rapidly and equilibrate in the maternal and cord plasma; this type of transfer is termed "complete" and include the antibiotics ampicillin, methicillin, cefmenoxime and cefotiam. Antibiotics which show incomplete transfer to the placenta where concentrations are lower in the cord than maternal plasma are said to have "incomplete" transfer and these include azlocillin, dicloxacillin, piperacillin, sulbenicillin, cefoxitin, amikacin, gentamicin, kanamycin, streptomycin, fosfomycin, thiamphenicol, griseofulvin, vancomycin and colistimethate. Ceftizoxime is the only antibiotic so far known whose concentrations are higher in the cord than maternal plasma. This type of transfer is called "exceeding" transfer. CONCLUSION: All examined antibiotics cross the human placenta including those with a molecular weight greater than 1000 kDa such as vancomycin and colistimethate but there are 3 distinct types of placental transfer: complete, incomplete and exceeding and most antibiotics exhibit incomplete transfer.

Anti-Bacterial Agents↗
PubMed1977

A new pencillin with anti-klebsiella activity: 3-(5-tetrazolyl) penam.

The in vitro activity of a new semi-synthetic penicillin, CP-35,587, 3-(5-tetrazolyl) penam, was investigated against 496 clinical isolates of gram-negative bacilli and 113 clinical isolates of gram-positive cocci. All of the gram-positive cocci were sensitive to CP-35,587 except penicillin G resistant isolates of Staphylococcus aureus. This antibiotic inhibited a majority of isolates of Escherichia coli, Klebsiella spp. and Proteus mirabilis at a concentration of 6.25 microgram/ml. Also, approximately half of the isolates of Serratia marcescens and Enterobacter spp. were inhibited at a concentration of 12.5 microgram/ml. CP-35,587 was inactive when high concentrations of organisms were used as inocula. CP-35,587 was more active than mezlocillin, azlocillin, amoxicillin, ticarcillin and carbenicillin against isolates of K. pneumoniae, but other penicillins were more acte than CP-35,587 against other species of gram-negative bacilli.

Bacteria↗
PubMed1991

Acclimatization resistance of a Pseudomonas aeruginosa prototype strain to imipenem.

A prototype sensitive strain of Pseudomonas aeruginosa (IRs) was acclimatized in vitro to imipenem by serial transfers in broth containing increasing concentrations of the antibiotic up to 32 micrograms/ml. Serial subculture of the resistant progeny (IR1r) in antibiotic-free solid media resulted in a "revertant" progeny (IR2r) that retained resistance to imipenem. Acclimatization resistance to imipenem and the attempted reversion procedure affected colony morphology, growth rate, pigment production, growth at 42 degrees C and glucose oxidation. SDS-PAGE analysis of the outer membrane proteins revealed in strain IR1r a complete loss of 6 proteins that were present in IRs (85 kdaltons, 46 kdaltons or porin D1, 45.5 kdaltons or porin D2, 43 kdaltons or porin E, 21 kdaltons or protein H1 and 20.5 kdaltons or lipoprotein H2) and in strain IR2r a complete loss of 3 proteins (46 kdaltons, 43 kdaltons, 20.5 kdaltons), while three others were found only in trace amounts (75 kdaltons, 45.5 kdaltons and 21 kdaltons). In the outer membranes of strains IR1r and IR2r an acquisition of a 56-kdalton protein was noted. Lipopolysaccharide chemical analysis revealed a marked, partially reversible increase in 2-keto-3-deoxyoctonate, total hexose and heptose constituents; readily extractable lipid chemical analysis and TLC, revealed a marked, partially reversible, increase in the phospholipid content of the outer membrane. Acclimatization resistance to imipenem was accompanied by cross-resistance to gentamicin, by partially reversible cross-resistance to moxalactam, carbenicillin and ticarcillin and by fully reversible cross-resistance to aztreonam. Sensitivity to azlocillin and polymyxin B remained unaltered. To explain this type of resistance to imipenem, an irreversible, non-inducible "loss" mutation mechanism, working in concert with a partially reversible mechanism, is proposed.

Cell Membrane Permeability↗
PubMed1989

The extended-spectrum penicillins: microbiologic, utilization, and cost review in a community hospital.

The extended-spectrum penicillins have a similar spectrum of activity and clinical efficacy. The newer acylaminopenicillins (azlocillin, mezlocillin, piperacillin) offer several potential therapeutic advantages over the carboxypenicillins (carbenicillin, ticarcillin), but they are more expensive per gram. Literature reviews of these penicillins suggest that individual hospital susceptibility patterns and cost should guide selection of the most appropriate antibiotic for formulary addition. Consequently, the authors performed a microbiologic, utilization, and cost review of these antibiotics in a community hospital. From this hospital and literature review, the authors were able to make the following conclusions: (1) the newer acylaminopenicillins exhibited similar activity against common clinical pathogens and were microbiologically more active than the carboxypenicillins; (2) none of these antibiotics used alone appears adequate for empiric treatment of serious systemic gram-negative bacillary infections; (3) the extended-spectrum penicillins were prescribed in a similar fashion and usually in conjunction with an aminoglycoside; and (4) significant cost savings can be realized when less expensive drugs are used. The authors found only minor differences in microbiologic activity and clinical use among the newer extended-spectrum penicillins. Therefore, they recommend the least expensive drug for routine use in the hospital.

Ampicillin↗
PubMed1989

Focus on oral ciprofloxacin; clinical and economic considerations.

Ciprofloxacin, a recently released oral fluorinated quinolone structurally related to nalidixic acid, joins norfloxacin as the second drug of this class to be released. Ciprofloxacin has a wide spectrum of antimicrobial activity and importantly demonstrates little cross resistance to non-quinolone drug classes (e.g. ureidopenicillins, cephalosporins, monobactams, carbapenems, aminoglycosides). Unlike other antibacterial classes such as the beta-lactams or aminoglycosides, ciprofloxacin does not suffer from transferable plasmid-mediated (i.e. R-factor) antibiotic resistance. Against gram-positive (including penicillin-resistant and methicillin-resistant staphylococci aureus) and gram-negative aerobic bacteria including Pseudomonas aeruginosa, ciprofloxacin demonstrates excellent activity. Ciprofloxacin is inactive against Trichomonas sp., treponemes, and fungi and anaerobes are considered resistant. Ciprofloxacin is rapidly absorbed from the gastrointestinal tract (i.e. 70-80% bioavailable), demonstrates extensive extravascular distribution, and its 3.5-5 hour half-life allows twice daily dosing. The bacteriologic and clinical efficacy of oral ciprofloxacin was shown to be comparable to third generation cephalosporins or aminoglycosides for osteomyelitis, cefotaxime for skin structure infections, and to a combination of tobramycin with azlocillin for pulmonary exacerbation of cystic fibrosis. Adverse events associated with ciprofloxacin are related mostly to gastrointestinal disturbance and consist of nausea/vomiting or diarrhea. Concomitant administration of ciprofloxacin and theophylline may lead to decreased theophylline clearance and necessitates periodic measurements of theophylline levels to avoid toxic levels. Treatment with oral ciprofloxacin should offer substantial cost savings over a variety of parenteral antimicrobial regimens (e.g. aminoglycoside + beta-lactams) for difficult to treat infections such as chronic pyelonephritis, osteomyelitis, and skin structure infections. Consideration of important precautions (e.g. contraindications, drug interactions) and potential disadvantages (e.g. emergence of resistance) must also guide the rational use of oral ciprofloxacin.

Administration, Oral↗
PubMed1999

[The diabetic foot syndrome--antibiotic therapy].

The authors present an account on cultivation findings assembled in defects of the lower extremities of diabetic patients hospitalized at the surgical department of the Pelhrimov hospital. In the polymicrobial flora a relatively high ratio of anaerobic microorganisms was found (58%). Based on the sensitivity, a combination of antibiotics was recommended which could be used in empirical treatment before cultivation results (clindamycin, ofloxacin, gentamycin and azlocillin). The authors prefer results of actual sensitivity tests. The authors discuss principles of collection and processing of microbiological material and treatment. Anaerobic cultivation is specially emphasized.

Aged↗
PubMed1999

[Drug resistance of Enterococcus species isolated from the urogenital system].

Despite low virulence of enterococci, they have become important nosocomial pathogens. This has been correlated with the increased use of broad-spectrum antibiotics, particularly cephalosporins. Many strains of enterococci exhibit multiple drug resistance; the most important being high-level resistance (HLR) to penicillin (MIC > 100 mg/l) and gentamicin (MIC > 500 mg/l and 2000 mg/l) and/or streptomycin (MIC > 2000 mg/l). The investigation was performed on 92 strains, isolated from genito-urinary tract and recognised as Enterococcus sp. All strains were obtained from several microbiological laboratories of Gdańsk, Gdynia and Tczew. On biochemical reaction profiles species of enterococci were identified as: E. faecalis (72.8%), E. faecalis varians (9.8%), E. durans (7.6%) and E. faecium (9.8%). The minimal inhibitory concentration (MICs) of penicillin, ampicillin, azlocillin, imipenem, gentamicin, amicacin, ciprofioxacin and vancomycin were determined by the agar dilution method. None of these 92 enterococcal strains was vancomycin resistant. 22.2% of E. faecium and 7.5% of E. faecalis showed high-level resistance to penicillin. None of these strains were produced beta-lactamase. High-level resistance to streptomycin and gentamicin was detected. Both--high-level resistance to streptomycin and gentamicin--were found in 6% E. faecalis; 11.1% E. faecalis varians and 22.2% E. faecium.

Drug Resistance, Microbial↗
PubMed2000

[Antibiotics sensitivity and characteristics of the esculin-positive Pseudomonas aeruginosa biovar].

Strains of Pseudomonas aeruginosa hydrolyzing esculin were isolated for the first time. They amount to 17.1 +/- 2.0% (60 from 325) of the investigated P. aeruginosa strains isolated from the clinical material in St. Petersburg. Esculin hydrolysis was measured by micromethod in plates, results were analysed after 3-hours incubation at 37 degrees C. Esculin-positive strains possesed biovar properties: they are widely spread, demonstrated other characteristic features (absence of triethylamine odour, specific colonies lysis), are stable on ability to hydrolyse esculin while culture storage and after repeated culturing. Typical strain of esculinolytica biovar was deposited into the culture collection of the National Research Institute of Agricultural Microbiology as P. aeruginosa ARRIAM 64-A. Susceptibility testing of the esculin-positive strains by disk-diffusion method revealed that most strains were inhibited by imipenem (86.6%), amikacin (75.0%), ceftazidime (65.0%), meropenem (60.0%), aztreonam (51.6%). The percent of strains susceptible to other antibiotics was lower: azlocillin--33.3%, netilmycin--33.3%, piperacillin--26.6%, ceftriaxon--18.3%. Only small number of strains were inhibited by ciprofloxacin (8.3%), gentamycin (3.4%), cefoperazone (1.7%) and carbenicillin (1.7%). The results may be used for empiric therapy before the isolated strain susceptibility is tested but only according to positive esculin-hydrolysis express-test evaluated in 3-hours period.

Anti-Bacterial Agents↗
PubMed1979

[Preventive and therapeutic application possibilities of newer antibiotics (author's transl)].

Today, however aminoglycosides are nearly indispensable owing to their broad antibacterial spectrum and genuine bactericidal effect as well as the possible synergic effect with beta-lactam preparations. The new cephalosporins are distinguished by a high beta-lactam stability and are active against the majority of pathogens causing nosocomial infections. An exceptional position is held by cefotaxim with its generally outstanding antibacterial potency, and by cefoxitin with its activity against Bacteroides fragilis. The ureidopenicillin azlocillin is superior to the Pseudomonas penicillins so far used. It acts against enterococci and H. influenzae as reliably as does mezlocillin.

Aminoglycosides↗
PubMed2001

[Hoigne syndrome as an acute non-allergic reaction to different drugs: case reports].

In 1959 Hoigne described the first cases of pseudo-anaphylactic reactions induced by intramuscular administration of procaine penicillin G. This complication, characterized by acute psychological and neurological manifestations, is still of current interest. We report cases of patient, whose Hoigne syndrome was not due to procaine penicillin G (i.e. lidocaine, edan, azlocillin, gentamycin, klaritromycin and cefuroxime). It is accepted that Hoigne syndrome can be caused by lidocaine. Further Stell i.m. and Ojo OA published similar case report of Amoxycillin-induced hallucinations. These clinical observations indicate also that using term "acute non-allergic reaction to procaine penicillin G" as synonym of Hoigne syndrome is not precise. Further classification of the reaction among psychic disturbances or adverse drug reactions is very difficult. Much of literature is devoted to the differentiation from anaphylaxis rather than other symptoms of main disease or side effects. Harmful effect of main disease is very likely. Lidocaine was taken intravenously by patient with diabetes and heart attack or locally with chronic hepatitis during topical anesthesia. Benzylpenicillin, azlocycillin, gentamycin, klaritromycin and cefuroxime was used during serious bacterial infections. These observations indicate that pathogenesis of Hoigne syndrome may be associated with main disease and organic brain disease. Then procaine kindling mechanism partly explain Hoigne syndrome. Therefore pathogenesis, definition, differentiation and classification of this complication is still unclear.

Acute Disease↗
PubMedDate not supplied

[Clinical significance of microbiological monitoring of infective agents in an urological hospital in the selection of antibacterial therapy regimens].

Individual microbiological examination of each patient can improve significantly the response of urological patients to antibacterial therapy. 6000 cultures of opportunistic microorganisms isolated from patients with various infectious-inflammatory diseases were studied. Most of them were gram-negative: P. aeruginosa, E. coli, Enterobacter spp., Proteus spp. Of gram-positive most frequently occurred Staphylococcus spp and Enterococcus faecalis. The cultures showed different spectrum of the sensitivity to antibacterial drugs used in urological practice. The choice of etiotropic therapy was the easiest in E. coli infection, the hardest in P. aeruginosa and Enterobacter pylori infection. Combined treatment of complicated urological infections with gentamycin, ampicillin, carbnicilline, azlocillin is much more effective than monotherapy. P. aeruginosa is more sensitive to cephalosporins, fluoroquinolins, carbapenems and combination of aminoglycosides with betalactame drugs.

Anti-Bacterial Agents↗
PubMed2001

[Microbiology of open surgical wounds after delivery--episiotomy and cesarean section].

UNLABELLED: The aim of the study is to assess the microbe find in the secretion of the open surgical wounds of the Cesarean Section and the perineal wounds. 81 young mothers have been examined--57 with open perineal wounds on 5th day after the delivery and 24 with open surgical wounds of Cesarean Section on the 7th day after the operation. RESULTS: The west frequent microbe find in the open perineal wounds is Streptococcus group "D" (enterococcus sp.)--53% of the cases and E. coli--26% of the cases. The most frequent microbe find in the open surgical wounds in the Cesarean Section is Enterococcus sp.--42% of the cases and St. aureus--21% of the cases. Considering the effectiveness of Penicillins (Ampicillin, Augmentin, Azlocillin, Karbencillin)--94%-99% against Enterococcus spp. and of Gentamycin against E. coli and St. aureus--90%-95% their application is recommended if is necessary.

Adult↗
PubMedDate not supplied

[Pseudomonas aeruginosa and beta-lactam resistance phenotypes (Tunisia 1989-1990)].

366 strains of P. aeruginosa were studied. More than half of samples were issued from urology (40%) and general surgery (21%) and samples are mostly urine specimens (46%). The phenotypes of resistance to 3 beta-lactams (respectively ticarcillin, cefotaxime and ceftazidime) showed that 73% of the strains were wild phenotype (SSS-SIS-SRS). The MIC of ticarcillin +/- clavulanic acid, azlocillin, cefoperazone, cefsulodin, cefotaxime and ceftazidime against 93 strains chosen among different phenotypes of resistance showed that ceftazidime is the most active beta-lactam, 93% of strains being inhibited by 16 micrograms/ml. These MIC and iodometric test performed on 33 strains with ticarcillin MIC > 128 mg/l showed that acquired resistance was non enzymatic in 21% of cases and was related to beta-lactamase production in 79% of cases.

Cefotaxime↗
PubMed1992

[Studies of susceptibility to antibiotics in strains of E. coli isolated from urine in the years 1986-1990].

From 1986 to 1990 research was conducted on E. coli strains isolated from patients with clinical symptoms of urinary tract infection. The paper-disk-plate technique was applied to determine their susceptibility to ampicillin, carbenicillin, azlocillin, cefamandole, cefotaxime, ceftriaxone, ceftazidime, cefoperazone, amikacin, netilmicin, gentamycin, vibramycin, and colistin. According to the authors' results the efficacy of ampicillin against the examined strains is as low as 3.4%. Aminoglycosides were traditionally recommended in therapy of urinary tract infections. Our research proves amikacin and netilmicin to be more effective against E. coli than gentamycin. The third-generation cephalosporins are recommended as alternative to aminoglycosides, especially since they are proved to be non-nephrotoxic. According to the results of the authors' research ceftazidime, cefotaxime and particularly ceftriaxone show the highest activity against the used strains of E. coli.

Aminoglycosides↗
PubMed1992

[Effectiveness of empirical antibiotic therapy in the control of infections in patients with acute leukemia during severe neutropenia].

The clinical efficacy of empiric antibiotic treatment regimen for infection in 38 neutropenic patients with acute leukemia during induction and intensification therapy was evaluated. The therapy, which was applied in 74 episodes of fever in patients with neutrophil count less then 0.5 G/l, consisted of three sets of antibiotics (gentamycin + carbenicillin or azlocillin, amikacin + cephradine++ or cefuroxime, netilmicin+cefotaxime or ceftazidime) used one after another in case of persistence of fever in spite of 72 hours of treatment: In addition, flucytosine was applied in case of stable fever after 72 hours of antibiotic therapy. Flucytosine was replaced by amphotericin after 72 hours of ineffective treatment. The response rate of 68% and 96% was observed for patients during induction and intensification chemotherapy respectively. Low clinical efficiency of gentamicin and carbenicillin/azlocillin during induction treatment indicates that the therapy with antibiotics of broader range of activity is needed for this group of patients.

Adolescent↗
PubMed1992

Comparative efficacy of fluoroquinolones, aminoglycosides, ureidopenicillins & newer cephalosporins against Pseudomonas species.

A total of 74 strains of Pseudomonas aeruginosa and 18 strains of Ps. putrefaciens were tested for sensitivity to 14 different antimicrobial agents. Ps. aeruginosa were mostly sensitive to netilmicin (81%), piperacillin (78%), amikacin (73%), azlocillin (70%), ceftazidime (69%) and pefloxacin (65%). Only 66 per cent strains of Ps. putrefaciens were sensitive to netilmicin, ceftazidime and ceftriaxone. The MIC values of the different drugs for the sensitive strains were comparable with the results of susceptibility testing. The Ps. putrefaciens strains showed greater resistance than Ps. aeruginosa.

4-Quinolones↗