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PubMed1969

In vitro susceptibility of Neisseria gonorrhoeae to nine antimicrobial agents.

The in vitro action of nine antibiotics was tested by the agar streak method against 45 gonococcal strains isolated from penicillin-therapy failures. The penicillin susceptibility range of these strains was 0.003 to 1.32 mug/ml, and the tetracycline susceptibility range was 0.125 to 2.0 mug/ml. Minimal inhibitory concentrations of minocycline and doxycycline paralleled the activity of tetracycline and ranged from 0.125 to 1.0 mug/ml and 0.125 to 2.0 mug/ml, respectively. Rifampicin, with a narrow range of 0.5 to 1.0 mug/ml, inhibited 75% of the strains at 0.5 mug/ml. The range for cephaloridine and cephaloglycine was 0.5 to 20.0 mug/ml, but another cephalosporium derivative, cephalexin, exhibited greater activity in its range of 0.25 to 20.0 mug/ml. A semisynthetic penicillin, carbenicillin, with a range of 0.025 to 0.75 mug/ml, displayed more activity against the lower susceptible penicillin G gonococcal strains.

Anti-Bacterial Agents↗
PubMed1970

Microbioassay of antimicrobial agents.

A previously described agar-diffusion technique for microbioassay of antimicrobial agents has been modified to increase sensitivity of the technique and to extend the range of antimicrobial agents to which it is applicable. This microtechnique requires only 0.02 ml of an unknown test sample for assay, and is capable of measuring minute concentrations of antibiotics in buffer, serum, and urine. In some cases, up to a 20-fold increase in sensitivity is gained relative to other published standardized methods and the error of this method is less than +/-5%. Buffer standard curves have been established for this technique, concurrently with serum standard curves, yielding information on antimicrobial serum-binding and demonstrating linearity of the data points compared to the estimated regression line for the microconcentration ranges covered by this technique. This microassay technique is particularly well suited for pediatric research and for other investigations where sample volumes are small and quantitative accuracy is desired. Dilution of clinical samples to attain concentrations falling with the range of this assay makes the technique readily adaptable and suitable for general clinical pharmacological studies. The microassay technique has been standardized in buffer solutions and in normal human serum pools for the following antimicrobials: ampicillin, methicillin, penicillin G, oxacillin, cloxacillin, dicloxacillin, cephaloglycin, cephalexin, cephaloridine, cephalothin, erythromycin, rifamycin amino methyl piperazine, kanamycin, neomycin, streptomycin, colistin, polymyxin B, doxycycline, minocycline, oxytetracycline, tetracycline, and chloramphenicol.

Agar↗
PubMed1970

Regression curve analysis of cephalosporin activity.

Regression lines were calculated for cephalothin, cephalexin, and cephaloridine by relating zone diameters of inhibition to minimal inhibitory concentrations (MIC) obtained in Mueller-Hinton agar and in Trypticase Soy Agar. A regression line was calculated for cephaloglycin by obtaining MIC values in Trypticase Soy Agar at pH 6.6. Regression lines calculated from MIC values in Mueller-Hinton agar were practically superimposable on those based on MIC values in Trypticase Soy Agar. Organisms susceptible by disc testing to cephalothin were usually susceptible to cephalexin and cephaloridine.

Agar↗
PubMed1999

The role of an alpha-amino group on H+ -dependent transepithelial transport of cephalosporins in Caco-2 cells.

The role of an alpha-amino group on interaction with the intestinal and renal peptide carriers (PEPT 1 and PEPT 2, respectively) has been the subject of much investigation. Studies have differed in their conclusions about the role of an alpha-amino group on carrier-mediated absorption. Most studies have used brush-border membrane vesicles or perfused intestinal segments. These techniques enable the determination of membrane uptake and luminal disappearance, respectively, but not transepithelial transport. Transepithelial transport should be more predictive of absorption because it includes basolateral efflux, which could be the rate-limiting process in drug absorption. The objective of this study was to evaluate the influence of an alpha-amino group on PEPT 1-mediated transepithelial transport in Caco-2 cells. The apical-to-basolateral permeability coefficients of cephalosporins with or without a free alpha-amino group were determined in the presence and absence of a pH gradient. Permeability coefficients obtained under these conditions were used to calculate a permeability ratio (i.e. P(app) (pH 6.0)/P(app) (pH 7.4)), which should indicate whether PEPT 1 is involved in transport. For cephalosporins with an alpha-amino group (cephalexin, cefaclor, cefadroxil, cephradine, cephaloglycin) the permeability ratios ranged between 1.77 and 2.77. In contrast, the permeability ratios for cephalosporins without an alpha-amino group were 1 (approx.; range = 0.74-1.26). These data suggest that the presence of an alpha-amino group on cephalosporins increases their PEPT 1-mediated transepithelial transport in Caco-2 monolayers.

Amines↗
PubMed1989

Determination of beta-lactam antibiotics in water by fluorescence quenching of mercurochrome, and application for simple investigation of potency.

The fluorescence quenching reaction between fluorescein mercury or halogeno-fluorescein mercury compounds (fl. Hg, 2,7- or 2,4-dichloro-fl.Hg, 3',4',5',6'-tetrachloro-fl.Hg, mercurochrome) and beta-lactam antibiotics (ampicillin (AB-PC) and cephalexin (CEX] was investigated, and mercurochrome was selected for the detection of beta-lactam antibiotics; the detection limit was about 0.8 micrograms/ml. A fluorimetric assay of beta-lactam antibiotics was established by measuring the fluorescence of mercurochrome and mercurochrome-beta-lactam antibiotics solutions in weakly basic media to determine the degree of fluorescence quenching. The maximum emission wavelength of mercurochrome solution was at 544 nm with excitation at 470 nm. The calibration graphs were linear over the ranges of about 0-6 micrograms/ml beta-lactam antibiotics penicillins (AB-PC, penicillin G, sulbenicillin, amoxicillin, cyclacillin, oxacillin, hetacillin and piperacillin) and cepham antibiotics (CEX, cefazolin, cephaloglycin, cephaloridine and cefpyramide), and the relative standard deviation was 2.7% for 1.4 micrograms/ml of AB-PC (n = 5). This fluorescence quenching reaction between mercurochrome and beta-lactam antibiotics was applied in a survey of decomposition and remaining potency of beta-lactam antibiotics.

Anti-Bacterial Agents↗
PubMed1976

Orally active 7-phenylglycyl cephalosporins. Structure-activity studies related to cefatrizine (SK&F 60771).

The synthesis of a series of related broad-spectrum 7-phenylglycyl cephalosporins with 3-heterocyclicthiomethyl substituents is described. The effects of benzene-ring hydroxylation and 3-substituent variation on the in vitro antibacterial activity, height and duration of mouse serum levels, and effectiveness in protecting against bacterial infection in the mouse are examined. Included for comparison are cephalexin, cephaloglycin and their ortho-, meta- and para-hydroxy derivatives. The biological properties examined were influenced by the position of the hydroxyl group and by the nature of the 3-substituent. The 7-(p-hydroxyphenylglycyl)-3-heterocyclicthiomethyl analogs were found to produce significantly higher serum levels on oral administration to mice than their unhydroxylated counterparts. This effect was not observed with the 7-(m-hydroxyphenylglycyl)-3-heterocyclicthiomethyl cephalosporins, nor with the p-hydroxyphenylglycyl analog of cephalexin. While m- and p-hydroxylation had little effect on in vitro activity and o-hydroxyphenylglycyl cephalosporins tested had very low antibacterial activities and were not examined further. One derivative, 7-[R-2-amino-2-(4-hydroxyphenyl)acetamido]-3-(1H-1, 2, 3-triazole-4(5)-ylthiomethyl)-3-cephem-4-carboxylic acid (SK&F 60771) was found to have outstanding in vitro and in vivo activities along with oral and subcutaneous serum levels in the mouse that were significantly higher than those obtained with cephalexin. This derivative which has been given the generic name cefatrizine was selected for extensive additional biological evaluation.

Animals↗
PubMed1980

Synthesis and biological activity of a new semisynthetic cephalosporin, CN-92,982.

A new broad spectrum semisynthetic cephalosporin (CN-92,982) was prepared from the condensation of an acetylaminoacylaminophenyl pyridone with trans-7-[(D-2-phenylglycyl) amino]-3-[[(1-methyl-1H-tetrazol-5-yl)thio]methyl]-delta 3-cephem-4-carboxylic acid. The new cephalosporin displayed an in vitro antibacterial spectrum similar to other cephaloglycine types such as cefoperazone and SM-1652. The compound produced a high and prolonged blood level following a single intramuscular dose in a dog.

Animals↗
PubMed1981

Protection of hydroxyl in the synthesis of semisynthetic beta-lactam antibiotics.

The 2-methoxypropan-2-yl group fulfills the need of a hydroxyl protecting group generally suitable for the synthesis of beta-lactam antibiotics, satisfying the criteria of low-cost, convenience and selectivity in formation, and, above all, ease of deprotection under conditions compatible to the highly sensitive beta-lactam function and without contamination of the final products. The use of this protecting group has enabled the successful attachment of 6-[4-(N-acetyl-4-hydroxyl-L-prolylamino)phenyl]-1,2-dihydro - 2 - oxo - 3 - pyridinecarboxyl group, through an amide linkage, to amoxicillin, cephaloglycin, and the 3[[(1-carboxymethyl)-1-H-tetrazol-5-yl]thio]methyl analogue of the latter, yielding broad-spectrum antibiotics with notably good activities against strains of Pseudomonas aeruginosa.

Anti-Bacterial Agents↗
PubMed2000

Metabolite anion carriers mediate the uptake of the anionic drug fluorescein in renal cortical mitochondria.

The fluorescent organic anion fluorescein (FL) accumulates in proximal tubular cells of the kidney during renal secretion. In freshly isolated and permeabilized proximal tubular cells, the uptake was reduced but still sensitive to probenecid, suggesting a concentrative mechanism that is associated with intracellular compartments. Previous studies have shown that one of these compartments may be mitochondrial. In this study, we further investigated the transport characteristics of FL in isolated rat kidney cortex mitochondria. Mitochondrial uptake of 100 microM FL was rapid, with an initial rate of 60 pmol/mg protein.min, and reached equilibrium after 5 min. To characterize the transport system(s) involved, FL uptake was studied in the absence and presence of substrates or inhibitors specific for the various mitochondrial anion carriers. Phenylsuccinate (10 mM), an inhibitor of the alpha-ketoglutarate carrier, reduced uptake significantly with a maximum inhibition of 33% and an inhibitory constant (-log IC(50)) of 4.0 +/- 0.4 (P <.05). The apparent K(m) for the phenylsuccinate-corrected FL uptake was 1.3 +/- 0.3 mM with a V(max) of 260 +/- 26 pmol/mg protein.15 s. Substrates for the tricarboxylate and glutamate-aspartate carriers significantly reduced the uptake of 100 microM FL with -log IC(50) values of 4.6 +/- 0.4 (citrate), 5.5 +/- 0.3 (glutamate), and 4.1 +/- 0.4 (aspartate). Substrates for the monocarboxylate and dicarboxylate carriers were without effect. The anionic drugs, valproate, indomethacin, and salicylate, significantly reduced FL uptake, whereas cephaloglycin and cephaloridine had no effect. Finally, a combination of phenylsuccinate, glutamate, and citrate reduced the uptake by 66%, indicating that at least three metabolite carriers contribute concomitantly to intramitochondrial FL transport.

Animals↗
PubMed1975

Comparison of absorption and excretion of cefazolin with cephalothin and cephapirin.

Since the discovery of cephalothin in 1962, many semi-synthetic cephalosporins have appeared. To choose the most suitable drug for the clinical treatment of infections, the characteristics of these antibiotics must be sufficiently understood. When cephalosporins which are or will be commercially available are divided into two categories, one consists of cephaloridine, cefazolin and cephalexin which are comparatively stable in the living body; and the other cephalothin, cephaloglycin, cephapirin and cephacetrile which are metabolized into desacetyl compounds with low antibacterial activity. In this study, the author compared the absorption, excretion and some other properties of cefazolin and cephalothin, (widely used clinically), and cephapirin (still under study in Japan).

Animals↗
PubMedDate not supplied

Continuous activity of significant antibiotics.

Respiratory tract infections (RTIs) are the primary cause of antibiotic use in general practice. Since the first penicillin was introduced for therapeutic purposes, several classes of antibiotics have been used in the treatment of community-acquired RTIs. The phase when penicillins G and V could be active in RTIs was relatively short lived due to the early emergence of resistant organisms. Ampicillin and amoxicillin have been used successfully for more than 20 years in the treatment of RTIs. In the late 1950s and 1960s, erythromycin, tetracyclines, and co-trimoxazole were also prescribed for RTIs. In the 1970s, other molecules belonging to the cephalosporin class of antibiotics, such as cephalexin, cephaloglycin, cefadroxil, and cephradine, were introduced in general practice for the same indication. Susceptibility of the predominant respiratory pathogens to these antimicrobial agents lasted for many years. However, Haemophilus influenzae responded poorly to erythromycin, and up to 30% of pneumococcal and streptococcal strains are resistant to macrolides, tetracyclines, and co-trimoxazole. Since 1976, increasing percentages of beta-lactamase producers (up to 20% in 1989) were found among Haemophilus species, and Moraxella catarrhalis, a frequent beta-lactamase producer, is increasingly isolated as a respiratory pathogen. These problems have led to the development of additional compounds, most characterized by their stability in the presence of beta-lactamases, such as amoxicillin + clavulanic acid, or exhibiting relative resistance to enzymatic inactivation, such as cefaclor. Treatment today of most RTIs also takes into account the cost-effectiveness relationship of these antibiotics.

Anti-Bacterial Agents↗
PubMed1990

The renal mitochondrial toxicity of cephalosporins: specificity of the effect on anionic substrate uptake.

Previous work in this laboratory has demonstrated a reduction by the nephrotoxic beta-lactam antibiotics cephaloridine, cephaloglycin and imipenem of renal mitochondrial uptake of and respiration with the anionic substrate succinate. The present studies were done to test further the hypothesis that reduced substrate uptake and decreased respiration are causally related. Using cephaloridine in the rabbit, we examined the specificity of this association in regard to the toxic cephalosporin insult, the involvement of renal mitochondria and the reduction of carrier-mediated anionic substrate transport. 1) Specificity of insult in renal cortical mitochondria: cephaloridine (300 mg/kg bwt. i.v., 1 hr before sacrifice) reduces both the uptake of and respiration with succinate, whereas the same dose of cephalexin, which is not nephrotoxic, has neither effect; 25 min of acute unilateral renal artery occlusion reduces both the uptake of and respiration with succinate, but, unlike cephaloridine, ischemia causes a large increase of substrate efflux; and the respiratory toxins cyanide (1 mM) and oligomycin (2 micrograms/g of protein) reduce respiration by a direct effect on the mitochondrial respiratory chain and therefore have no effect on substrate uptake. 2) Specificity of target organ: cephaloridine has no significant effect on either the uptake of or respiration with succinate in hepatic mitochondria.(ABSTRACT TRUNCATED AT 250 WORDS)

Adenosine Diphosphate↗
PubMed1983

Cephalexin in the treatment of upper respiratory tract infections.

Cephalexin, a semisynthetic cephalosporin antibiotic, has wide clinical application in respiratory infections of children and adults. In pharyngitis and tonsillitis due to beta-haemolytic streptococci, it is comparable to penicillin, cyclocillin, and cephaloglycin, as measured by clinical response, bacteriological cure rate, and incidence of relapse and reinfection. In otitis media, it is effective at dosages of 50-100 mg/kg/day except in those infections caused by Haemophilus influenzae, in which there is failure in 50% of the cases. In other infections of the upper respiratory tract, it appears to be effective except, again, in those caused by H. influenzae. Dosages of 1-2 g/day have been used in adults and 20-100 mg/kg/day in children. Adverse effects, mostly gastrointestinal upsets, rash, and urticaria, have been relatively infrequent and have not required discontinuance of the drug.

Adult↗
PubMed1984

Basic design of beta-lactam antibiotics--cephalosporins.

Since the introduction of cephaloglycin and cephalothin as the first commercially available cephalosporin C derivatives, there has been a proliferation of new agents, predominantly injectables. These have provided compounds with increased potency, improved spectrum, and/or pharmacokinetic advantages. The nature of the modifications producing these changes is the subject of the present report. The pathway generally followed by chemists working on a nucleus suitable for modification is initially a combination of trial and error and application of analogies from related areas. Once a moiety conferring a desirable effect has been identified, it or its analogs will be widely utilized in an effort to achieve further improvements. The choice of derivatives to be made is appreciably influenced by potential patentability and the feasibility of synthesis. For oral cephalosporins, to achieve adequate intrinsic bioavailability, the 7 beta-side chain has almost invariably been found to require a primary amino group on the alpha-carbon (D-configuration). This has limited potential changes at the 7 beta-position and leaves the 3-position as the major site for introducing novel substituents. Among thousands of derivatives prepared, only a few have actually been developed for clinical use. For injectables, where oral absorption is not a factor, there are no such specific preferred entities for either the 3- or 7 beta-position. Because of this, cephalosporin derivatives containing a large and diverse group of substituents at these positions have been prepared. In addition, another substitution site was identified upon discovery of the cephamycins, antibiotics which differ from cephalosporins by the presence of a methoxy group at the 7 alpha-position. Substitution at this site confers remarkable beta-lactamase stability, but only methoxy has given acceptable potency. First generation injectables which have in the 3-position the naturally occurring acetoxymethyl group or other relatively simply substituents are very active against Gram-positive organisms and a few species of Gram-negatives. As new 3- and 7 beta-side chain moieties were studied, appropriate combinations yielded compounds active vs. a broader spectrum of Enterobacteriaceae and/or Pseudomonas aeruginosa or Bacteroides fragilis. Furthermore, dramatic changes in pharmacokinetics (longer half-lives) were achieved by both 3- and 7 beta-side chain modifications.(ABSTRACT TRUNCATED AT 400 WORDS)

Administration, Oral↗
PubMed1995

Cephalosporin binding sites to human serum albumin and the relation with the N-B transition of this protein.

The binding of some cephalosporins to human serum albumin was studied using probes for the so-called I, II, bilirubin and fatty acids binding sites. The results showed that cephradine and cefsulodin bind to site II, cefaclor, cefamandole, cefsulodin, cephaloglycin and cefadroxil bind to the bilirubin binding site, while cefaclor does it to the fatty acid binding site. No binding of these cephalosporins to site I of albumin was found. The binding produced a perturbation on the N-B equilibrium of albumin, stabilizing the N conformational form, which suggests that the N form of albumin has more affinity with the cephalosporins than the B form. This finding gives support to the assumption that the binding of cephalosporins to site II, bilirubin and fatty acids binding sites affects the N-B transition of albumin.

Bilirubin↗
PubMed1994

Toxicity of cephaloridine to carnitine transport and fatty acid metabolism in rabbit renal cortical mitochondria: structure-activity relationships.

Cephaloridine (Cld), the most widely studied nephrotoxic cephalosporin, has significant structural homology with carnitine, which facilitates the transport of long-chain fatty acids into the mitochondrial inner matrix. Because of this homology, and evidence of a role of lipids in cephaloglycin (Cgl) nephrotoxicity, protocols were designed to compare the effects of Cld and Cgl on renal cortical mitochondrial carnitine transport, on long-chain fatty acylcarnitine-mediated respiration and on the in situ mitochondrial pools and urinary excretion of carnitine and acylcarnitines. The following was found: 1) both cephalosporins reduced carnitine-facilitated pyruvate oxidation (CFPO) and palmitoylcarnitine-mediated respiration (PCMR) by 40 to 50% in mitochondria exposed in vivo (300 mg/kg b.wt., 1 hr). CFPO could be decreased by reduction of carnitine uptake, pyruvate oxidation or carnitine acetyltransferase activity; 2) neither cephalosporin reduced mitochondrial carnitine acetyltransferase or carnitine palmitoyltransferase; 3) with in vitro exposure (2000 micrograms/ml, immediate effect) Cgl had no significant toxicity to mitochondrial CFPO. Cld inhibited CFPO in a dose-dependent manner, up to 100% at 2000 micrograms/ml; this effect was reduced by increasing carnitine concentrations; 4) in vitro Cld prevented the potentiation of PCMR by preloading with carnitine, reduced mitochondrial acetylcarnitine/carnitine exchange by 70% and reduced PCMR by 30%; 5) in vivo Cld increased mitochondrial-free carnitine in the in situ kidney by 100%; and 6) in vivo Cld increased the fractional renal excretion of carnitine from 0 +/- 0 to 0.29 +/- 0.03 and the fractional excretion of long-chain acylcarnitines from 0.06 +/- 0.01 to 0.79 +/- 0.17.(ABSTRACT TRUNCATED AT 250 WORDS)

Animals↗
PubMed1977

Positive interference with the Jaffé reaction by cephalosporin antibiotics.

Cephaloglycin, cephalothin, cephaloridine, cefoxitin, and cephacetrile are cephalosporin antibiotics that react with alkaline picrate solution to give a creatinine-like response. The mechanism of this reaction is not known, and several structurally similar compounds do not react under these same conditions. Because large quantities of a cephalosporin antibiotic may be administered to a patient with limited ability to excrete the drug (as occurs with compromised renal function), the magnitude of this interference can be appreciable. It does not appear possible to avoid the cephalosporin-caused interference by the use of "kinetic" creatinine methods.

Cephalosporins↗