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PubMed1996

Dynamic reaction design of enzymic biotransformations in organic media: equilibrium-controlled synthesis of antibiotics by penicillin G acylase.

Parameters relevant to the thermodynamically controlled synthesis of cephalothin utilizing highly active stabilized penicillin G acylase derivatives were studied. These included solubility/stability of substrates, enzyme derivative activity/stability, reaction course and synthetic yields. These parameters were altered by varying the pH, dimethylformamide concentration and temperature. Simultaneous optimization of the selected parameters could not be achieved with a single set of conditions. However, continuous adjustment of conditions throughout the reaction course allowed each parameter to be optimized (dynamic reaction design). This strategy works by optimizing those parameters that are critical to the overall reaction at a given point, whilst leaving others sub-optimal when their contribution to the total is minimal. This strategy has achieved a 90% transformation of antibiotic nucleus to cephalothin at a final concentration of 20 g/l, high enzyme and reactant stability, with a reaction period of 3 h (using 1 ml of derivative/40 ml of reaction solution).

Anti-Bacterial Agents↗
PubMed1977

Effect of inline filtration on the potency of drugs administered intravenously.

The binding of cephalothin sodium, phenobarbital sodium, dexamethasone sodium phosphate, isoproterenol hydrochloride, digoxin, dactinomycin and phenytoin sodium to three intravenous inline filters--a 5-micrometer stainless steel depth filter, a 0.2-micrometer cellulose ester membrane and a 0.2-micrometer polycarbonate membrane--was studied. The experiments were conducted simulating inline i.v. filtration of these drugs in three i.v. solutions--lactated Ringer's, 5% dextrose and normal saline. Cephalothin was assayed colorimetrically, phenobarbital and phenytoin spectrophotometrically, and the other drugs by radiotracer technique. Binding of the drugs to the filter was found to be insignificant from a therapeutic standpoint, except for dactinomycin which bound to the 0.2-uicrometer filters. The binding of dactinomycin was approximately 13% of the amount administered through cellulose ester and polycarbonate membranes, respectively. The binding occurred during the initial period of filtration of the drug solution. It was concluded that inline filtration of drugs administered in relatively high does should not present any problem concerning the reduction of the therapeutic potency because of filtration.

Cephalothin↗
PubMed1976

Comparative stability of cephalosporins in aqueous solution: kinetics and mechanisms of degradation.

The acidic, neutral, and alkaline degradations of six therapeutically useful cephalosporins (cephalothin, cephaloridine, cephaloglycin, cephalexin, cephradine, and cefazolin), 7-amino-cephalosporanic acid, 7-aminodeacetoxycephalosporanic acid, and some 7-substituted derivatives were followed by high-pressure liquid chromatographic, UV spectrometric, iodometric, and hydroxamic acid assays. The pH-rate profiles were determined at 35 degrees and mu = 0.5. The acidic degradation pathway for the 3-acetoxymethyl and 3-pyridinylmethyl derivatives was the specific hydrogen-ion-catalyzed hydrolysis of the beta-lactam bonds. The beta-lactam hydrolyses of these antibiotics exhibited half-lives of about 25 hr at pH 1.0 and 35 degrees. The acetyl functions of 3-acetoxymethylcephalosporins were hydrolyzed eight times faster than their beta-lactam moieties to yield the corresponding deacetyl intermediates, which were rapidly converted to the lactones. Deacetoxycephalosporins were fairly acid stable; e.g., cephalexin and cephradine were about 25 times more stable than cephalothin, cephaloridine, and cephaloglycin and about 180 times more stable than ampicillin at pH 1.0. In the neutral degradation of 3-acetoxymethyl compounds, the competitive reactions of the direct water attack and intramolecular catalysis by the side-chain amido upon the beta-lactams were proposed. The pH-rate profiles near pH 8 for cephaloglycin, cephalexin, and cephradine could be explained by the intramolecular-nucleophilic attack of the side-chain alpha-amino group upon the beta-lactam carbonyls to produce diketopiperazine-type compounds. The reactivity of the cephalosporins in the hydroxideion-catalyzed degradation was influenced significantly by the C-3 methylene substituents.

Cephalosporins↗
PubMed1978

Quantitative crystallinity determinations for beta-lactam antibiotics by solution calorimetry: correlations with stability.

The solution calorimetry method is based on the observation that amorphous forms are normally significantly higher in energy than are crystalline forms. The utility and validity of the calorimetric method were investigated for cephalothin sodium, cefazolin sodium, cefamandole nafate, and cefamandole sodium. Amorphous, partially crystalline, and crystalline forms were prepared and characterized by X-ray diffraction (powder), by solution calorimetry, and, for cephalothin sodium, by the thermal decomposition rate at 50 degrees. Qualitatively, there was a good correlation between calorimetric crystallinity and the (less precise) crystallinity derived from X-ray data. The energy and structure of the amorphous state depend on the history of the sample; even samples of the same crystalline polymorph, containing no amorphous phase, may differ in energy. Thus, the absolute value of the crystallinity (X-ray or calorimetric) depends on the choice of amorphous and crystalline standards. The heat of solution is a precise (+/- 1%) and unambiguous measure of the relative crystallinity; and provided amorphous and crystalline standards are appropriately chosen, the calorimetric crystallinity correlates well with chemical stability.

Absorption↗
PubMed1994

Photolytic destruction and polymeric resin decontamination of aqueous solutions of pharmaceuticals.

Amoxicillin, ampicillin, bleomycin, carmustine, cephalothin, dacarbazine, lomustine, metronidazole, norethindrone, streptozocin, sulfamethoxazole, and verapamil were completely degraded in solution, without the production of mutagenic residues, by photolysis using a medium-pressure mercury lamp in an all-quartz apparatus. A stream of air was passed through the solution and for amoxicillin, ampicillin, bleomycin, lomustine, metronidazole, and norethindrone it was necessary to add hydrogen peroxide. Dilute aqueous solutions of ampicillin, bleomycin, carmustine, cephalothin, lomustine, norethindrone, streptozocin, trimethoprim, and verapamil can be decontaminated using polymeric Amberlite resins.

Animals↗
PubMed1980

Research on pharmacokinetics during pregnancy.

The pharmacokinetics of some drugs important for treatment in pregnancy were studied in several groups, women in stage III of pregnancy, women in labour and non-pregnant women as a control group. The half-life of elimination of the drugs is one of the most important parameters in pharmacokinetics. The following drugs were used: noramidopyrine methane sulphonate sodium, aminophenyzone, pethidine, methaqualone, ampicillin, cephalothin, chlorsulfamethin, and indocyanine green. The results show that all drugs except cephalothin had a prolonged half-life during labour. In contrast to this the half-life of most of the drugs is diminished in pregnancy. The extent and direction of the changes depend on the pathway of elimination and on the rate of biotransformation of the drug.

Biotransformation↗
PubMed1978

Therapy of serious infections with cefamandole.

Forty-four patients with serious bacterial infections were treated with cefamandole in a dose 1--2 g every four to six hours. Thirty-two patients were cured and six were markedly improved. Three of six failures were due to superinfection with cephalothin-resistant microorganisms. The over-all bacteriologic response was 80%. In 12 of 13 patients with bacteremia the blood was sterilized. Ten of 14 patients with gram-negative bacillary infections responded to treatment. Six of these were due to cephalothin-resistant microorganisms, three of which responded. Fifteen patients who were treated had a history of penicillin allergy. There were no serious reactions although skin rash did develop. Phlebitis was uncommon.

Adolescent↗
PubMed1985

Cefotaxime in combination with other antibiotics for the treatment of severe methicillin-resistant staphylococcal infections.

Methicillin-resistant staphylococci (M-R staphylococci) represent 30% of the staphylococcal strains isolated in our hospital and pose important therapeutic problems. In a preliminary in vitro checkerboard study the bactericidal effect of various cephalosporins (cephalothin, cefamandole, cefotaxime and cefoperazone) in combination with other antibiotics (netilmicin, amikacin, vancomycin and fosfomycin) was studied on ten M-R staphylococcal strains. The combinations of cefoperazone with amikacin, cephalothin with vancomycin and of the four cephalosporins with fosfomycin were synergistic on the ten strains (FBC indexes less than or equal to 0.75). According to the CSF and bone levels achieved by these antibiotics and their bactericidal concentrations in combination, the combination of cefotaxime and fosfomycin was the most interesting, a concentration of less than or equal to 2 mg/l cefotaxime being bactericidal on five homogeneous M-R Staphylococcus aureus when combined with 4 mg/l of fosfomycin. This combination of cefotaxime (25 mg/kg, i.v. infusion over 30 min) and fosfomycin (50 mg/kg, i.v. infusion over three hours) three to four times daily was used to treat 16 patients: three patients with meningitis, six with bone and joint infections and seven with persistent bacteremia. The FBC indexes were less than or equal to 0.625 for the 12 strains studied. All the patients were cured without relapses. The concentrations of cefotaxime, desacetyl cefotaxime and fosfomycin in the CSF during meningitis three hours after the end of the infusion on the second day of treatment were 8.76, 6.82 and 58.0 mg/l, respectively, for patient one and 2.0, 0.53 and 31.0 mg/l, respectively, for patient two.(ABSTRACT TRUNCATED AT 250 WORDS)

Adolescent↗
PubMed1995

Activity of beta-lactamase inhibitor combinations on Escherichia coli isolates exhibiting various patterns of resistance to beta-lactam agents.

The efficacy of the clinically available beta-lactam/beta-lactamase inhibitor combinations (amoxicillin/clavulanic acid (CA), ticarcillin/CA, amoxicillin/sulbactam, and piperacillin/tazobactam) was evaluated on 300 amoxicillin-resistant Escherichia coli isolates having the main patterns of beta-lactam resistance. The patterns, which reflect the production of various beta-lactamase enzymes, were analyzed by a principal component analysis of susceptibility to 11 beta-lactam antibiotics or beta-lactam/beta-lactamase inhibitor combinations. Sixty-two percent of strains were not very susceptible to penicillins, cephalothin, or any beta-lactam/beta-lactamase inhibitor combinations except for piperacillin/tazobactam; these strains may represent high-level broad-spectrum beta-lactamase (so-called penicillinase) production phenotype or inhibitor-resistant TEM-like enzyme production phenotype. Of the strains, 14.7% were resistant to amoxicillin and ticarcillin compatible with low-level broad-spectrum beta-lactamase production phenotype; 5.7% were cefoxitin resistant and were postulated to present a high-level cephalosporinase production phenotype; and 2.6% were resistant to cephalothin only, attributable to a low-level cephalosporinase production phenotype. Three percent of strains were intermediate or resistant to cefotaxime and may produce an extended-spectrum beta-lactamase, and the remaining strains (12 %), resistant to all tested antibiotics except for cefotaxime and piperacillin/tazobactam, were hypothesized to produce both broad-spectrum beta-lactamase plus cephalosporinase. The minimal inhibitory concentration (MIC) for these phenotype patterns indicated that combinations of CA plus amoxicillin or ticarcillin, or sulbactam plus amoxicillin, restored the activity of penicillins against phenotype 1 strains, whereas these combinations remained inactive against the other phenotype strains. Piperacillin plus tazobactam showed the best in vitro effect against the strains of all resistance phenotypes.

Amoxicillin↗
PubMed1985

Induction of IgG1 and IgE responses to protein-conjugated and unconjugated beta-lactam antibiotics in the mouse--efficacy of Freund's complete adjuvant.

One or two injections two weeks apart of protein-conjugated penicillin G, cephalothin or cefmetazole emulsified with Freund's complete adjuvant were quite effective in producing anti-antibiotic antibodies of the IgE as well as of the IgG1 class in mice. Long-lasting and boostable production of both antibody classes was also obtained against unconjugated cephalothin or cefmetazole, though the positivity depended on the mouse strain.

Animals↗
PubMed1982

Synergism of trimethoprim combined with aminoglycosides in vitro and in serum of volunteers.

In vitro synergism of trimethoprim plus amikacin and trimethoprim plus sisomicin against 66 gram-negative bacilli was studied by microtiter checkerboard dilution. Synergism was defined as an FIC or FBC index equal to or less than 0.5. Fifty-two percent of strains were inhibited and 65% killed synergistically by the former combination, and 27% and 36% respectively by the latter combination (p less than 0.01). Serum bactericidal activity against 16 strains resistant to ampicillin and/or cephalothin was studied using serum from five volunteers one and six hours after intravenous administration of trimethoprim (160 mg), amikacin (250 mg) or the combination, and from six volunteers after administration of trimethoprim, tobramycin (1 mg/kg) or the combination. With trimethoprim and amikacin serum bactericidal titers greater than or equal to 1:8 were found more frequently with the combination (77 of 80 samples) than with either drug alone (trimethoprim 19 of 80 samples, amikacin 60 of 80 samples, p less than 0.01). Trimethoprim plus amikacin may be useful in the treatment of infections with gram-negative rods resistant to cephalothin and ampicillin.

Aminoglycosides↗
PubMed1982

Speciation and antibiotic susceptibility patterns of coagulase-negative staphylococci.

During a six month period, 191 isolates of coagulase-negative staphylococci from blood, urine, cerebrospinal fluid and heart valves were identified to species level and tested for antimicrobial susceptibility. Seventy-one percent of isolates were Staphylococcus epidermidis, 8% Staphylococcus warneri, 7% Staphylococcus hominis, 7% Staphylococcus haemolyticus, 4% Staphylococcus capitis, 2% Staphylococcus saprophyticus and 1% Staphylococcus cohnii. Approximately 4% of isolates were felt to be associated with infection. Overall, 18% of isolates were susceptible to penicillin G, 61% oxacillin, 98% cephalothin, 98% cefamandole, 72% cefotaxime, 95% cefsulodin, 76% gentamicin, 64% clindamycin and 98% rifampicin. All isolates were susceptible to vancomycin. Vancomycin, rifampicin, cephalothin and cefamandole showed excellent activity against oxacillin-resistant isolates. With one exception, speciation was not helpful in determining whether or not an isolate was associated with infection.

Anti-Bacterial Agents↗
PubMedDate not supplied

Cefamandole preparation for colonic surgery.

A controlled, prospective, randomized study of 457 patients undergoing colonic surgery was done to compare systemic cefamandole therapy to neomycin-erythromycin in reducing postoperative septic complications. Parenteral cefamandole and cephalothin were given before, during, and after surgery to achieve maximal antimicrobial coverage in the blood, tissues, peritoneum, and urine. Such protection is not obtained with oral antibiotic preparation. Major surgical indications were carcinoma in 216 patients and diverticulitis in 107 patients. More than half the patients had colonic perforations, obstruction, or fistulas. All patients were operated upon by a single surgeon during 1975-1980. Cephalothin (151 patients), combined with neomycin-erythromycin, resulted in an 11.3 per cent rate of postoperative septic complications. Cefamandole treatment in 112 patients resulted in an 8.9 per cent postoperative infection rate compared with 16.3 per cent in 141 matched control patients.

Bacterial Infections↗
PubMedDate not supplied

The problem of infections in acute leukemias. Personal experience in diagnosis and treatment.

This report is based on experience over the last 5 years in the diagnosis and treatment of infections in 200 acute leukemic patients hospitalized in the Institute of Haematology, University of Rome. The relevant clinical and laboratory findings are discussed in relation to the diagnosis of secondary infections. Most of the febrile episodes were associated with infection. The frequently rapid development of the infections in these patients requires empirical antibiotic treatment. The best results were obtained when the combinations carbenicillin-cephalothin-gentamicin (success rate of 65%), and carbenicillin-cephalothin-gentamicin-lyncomycin-methicillin (success rate of 62%), were used as empirical therapy.

Acute Disease↗
PubMed1993

A comparison of antimicrobial sensitivities of urinary pathogens for the years 1980 and 1990.

Urinary tract infection is a major cause of morbidity in both the hospital and community which often requires empirical therapy. We have retrospectively studied laboratory diagnosed urinary tract infections for the years 1980 and 1990 to document the common pathogens and antimicrobial susceptibility patterns. In 1990 a significantly lower proportion of specimens yielded Proteus sp. or Klebsiella sp. than was the case in 1980. This was true of specimens from both the hospital and the community. There was an increase in the proportion of specimens yielding Pseudomonas sp. and coagulase negative Staphylococci (CNS). Significant changes in the antimicrobial susceptibility of urinary pathogens are also noted. In particular a greater proportion of isolates from the community were sensitive to cephalothin in 1990, while fewer isolates were sensitive to nalidixic acid and gentamicin. A greater proportion of isolated from hospital practice were sensitive to ampicillin, to cephalothin and to trimethoprim in 1990 while fewer isolates were sensitive to gentamicin. In relation to nitrofurantoin no significant change was noted. In respect of isolates from both community and hospital practice the agents ofloxacin, co-amoxiclav (not available in 1980) and gentamicin are those which are most consistently active.

Anti-Bacterial Agents↗
PubMed1979

Transient monoclonal proteins in drug hypersensitivity reactions.

Two patients were studied in whom monoclonal (M) immunoglobulin G (IgG) proteins developed during the course of a serum sickness-like drug hypersensitivity reaction to cloxacillin (Orbenin) and sodium cephalothin (Keflin), respectively. The clinical evidence and time sequence of events support this association. In both patients there was evidence of an active antibody response to the given antibiotic and to the benzylpenicilloyl group as well. However, protein fractions obtained by agar gel preparative electrophoresis failed to show a higher antibody concentration where the M peak was located, and absorption experiments performed with penicillin G-, cloxacillin- and cephalothin-coated red cells failed to absorb these M proteins. These transient paraproteins can be seen in association with antibiotic(s) administration in the context of a hypersensitivity reaction and do not apparently represent a specific immune response.

Adult↗
PubMed1976

The stability of ten antibiotics in artificial tear solutions.

We determined the relative potencies of penicillin G, carbenicillin, oxacillin, cephalothin, cephaloridine, gentamicin, kanamycin, neomycin, vancomycin, and bacitracin after their addition to three commercially available 0.5% hydroxypropyl methylcellulose artificial tear solutions in plastic squeeze bottles. We found no significant loss of antibiotic activity at room temperature over a period of seven days for all antibiotics except penicillin G, cephalothin, and cephaloridine. Three of the antibiotics were insoluble in one or more of the artificial tear solutions.

Anti-Bacterial Agents↗
PubMed1996

Drug resistance, plasmids, biotypes and susceptibility to bacteriophages of Salmonella isolated from poultry in Canada.

Salmonella isolates from 295 layer and 294 broiler flocks in Canada were examined to determine resistance to antimicrobial agents, plasmid profiles, biochemical properties, and susceptibility to polyvalent bacteriophages. Except for the high number of strains resistant to spectinomycin (97.8%), the frequency of drug resistance of Salmonella isolates from layer flocks was low. None of 457 isolates from layer flocks was resistant to amikacin or ciprofloxacin, and less than 2% of the strains were resistant to cephalothin, chloramphenicol, cotrimoxazole, gentamicin, kanamycin, neomycin, nitrofurantoin, and/or polymyxin B. About 3% of the strains were resistant to ampicillin, carbenicillin and/or tetracycline, whereas 8% of the strains were resistant to sulfisoxazole. Salmonella anatum var. O15+ and S. typhimurium var. copenhagen strains were resistant to multiple antimicrobial agents. None of 1159 Salmonella strains from broiler flocks was resistant to amikacin, cephalothin, ciprofloxacin or polymyxin B, less than 1% of the strains were resistant to chloramphenicol, 2% were resistant to ampicillin, carbenicillin and/or chloramphenicol; 5-7% were resistant to the aminoglycosides gentamicin, kanamycin and/or neomycin; 6% were resistant to nitrofurantoin; 10% to tetracycline; 14% to sulfisoxazole; and 99% to spectinomycin. A high percentage of S. binza, S. anatum var. O15+, S. schwarzengrund and S. heidelberg strains were resistant to antimicrobial agents. Some of the single or multiple resistances were encoded by conjugative plasmids or by plasmids that were thermosensitive for transfer. Eight percent of S. heidelberg strains did not produce hydrogen sulfide. Ninety-seven percent of the Salmonella strains were susceptible to the lytic effect of polyvalent bacteriophages.

Animals↗