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Quinolones

Distribution by Scientific Domains

Medical Sciences	60%
Chemistry	26%
Life Sciences	7%
Earth and Environmental Science	4%

Terms modified by Quinolones

quinolone antibiotics

Selected Abstracts

A New Quinolone and Other Constituents from the Fruits of Tetradium ruticarpum: Effects on Neutrophil Pro-Inflammatory Responses

CHEMISTRY & BIODIVERSITY, Issue 7 2010
Tzu-Ying Wang
Abstract The fruit of Tetradium ruticarpum is widely used in healthcare products for the improvement of blood circulation, headache, abdominal pain, amenorrhea, chill limbs, migraine, and nausea. A new quinolone, 2-[(6Z,9Z)-pentadeca-6,9-dienyl]quinolin-4(1H)-one (1), has been isolated from the fruits of T. ruticarpum, together with eleven known compounds. The structure of the new compound was determined by NMR and MS analyses. Rutaecarpine (4), evodiamine (5), and skimmianine (7) exhibited inhibition (IC50,20.9,,M) of O generation by human neutrophils in response to N -formyl- L -methionyl- L -leucyl- L -phenylalanine/cytochalasin B (fMLP/CB). In addition, 1, evocarpine (2), 4, 7, and evodol (8) inhibited fMLP/CB-induced elastase release with IC50 values ,14.4,,M. [source]

Effect of quinolone treatment on selection and persistence of quinolone-resistant Escherichia coli in swine faecal flora

JOURNAL OF APPLIED MICROBIOLOGY, Issue 4 2005
C. Belloc
Abstract Aims:, To study the effect of oral administration of a quinolone on emergence of resistance in an indicator bacterial species from faecal flora. Methods and Results:, Quinolone resistance was studied in Escherichia coli obtained from the faecal contents of pigs housed in nine commercial farrow-to-finish herds in France after administration of flumequine to sows. The percentage of quinolone-resistant E. coli increased in the faeces of sows after administration of flumequine (mean 21·78% at day 7 vs 6·42% before treatment for nalidixic acid) and then decreased (mean 12·6 and 10·4 at days 30 and 60, respectively for nalidixic acid), being not significantly different from initial values 1 month post-treatment. In young pigs, the proportion of resistant strains was lower and decreased over rearing period. Moreover, changes over time of both total E. coli and the proportion of resistant bacteria exhibited great inter-individual variability. Conclusions:, Restoration of susceptible faecal flora occurred within 2 months after flumequine treatment. Significance and Impact of the Study:, Effect of flumequine treatment of sows on the quinolone resistance of faecal E. coli of both sows and their progeny is noticeable but transitory. [source]

Detection of quinolone-resistance genes in Photobacterium damselae subsp. piscicida strains by targeting-induced local lesions in genomes

JOURNAL OF FISH DISEASES, Issue 8 2005
M-J Kim
Abstract Quinolone-resistant strains of the fish-pathogenic bacterium, Photobacterium damselae subsp. piscicida are distributed widely in cultured yellowtail, Seriola quinqueradiata (Temminck & Schlegel), in Japan. The quinolone resistance-determining region (QRDR) was amplified with degenerate primers, followed by cassette ligation-mediated PCR. Open reading frames encoding proteins of 875 and 755 amino acid residues were detected in the gyrA and parC genes, respectively. Resistant strains of P. damselae subsp. piscicida carried a point mutation only in the gyrA QRDR leading to a Ser-to-Ile substitution at residue position 83. No amino acid alterations were discovered in the ParC sequence. A mutation in the gyrA gene was also detected in nalidixic acid-resistant mutants of strain SP96002 obtained from agar medium containing increased levels of quinolone. These results suggest that GyrA, as in other Gram-negative bacteria, is a target of quinolone in P. damselae subsp. piscicida. Furthermore, we attempted to detect a point mutation using targeting-induced local lesions in genomes (TILLING), which is a general strategy used for the detection of a variety of induced point mutations and naturally occurring polymorphisms. We developed a new detection method for the rapid and large-scale identification of quinolone-resistant strains of P. damselae subsp. piscicida using TILLING. [source]

Indole and 7-hydroxyindole diminish Pseudomonas aeruginosa virulence

MICROBIAL BIOTECHNOLOGY, Issue 1 2009
Jintae Lee
Summary Indole is an extracellular biofilm signal for Escherichia coli, and many bacterial oxygenases readily convert indole to various oxidized compounds including 7-hydroxyindole (7HI). Here we investigate the impact of indole and 7HI on Pseudomonas aeruginosa PAO1 virulence and quorum sensing (QS)-regulated phenotypes; this strain does not synthesize these compounds but degrades them rapidly. Indole and 7HI both altered extensively gene expression in a manner opposite that of acylhomoserine lactones; the most repressed genes encode the mexGHI-opmD multidrug efflux pump and genes involved in the synthesis of QS-regulated virulence factors including pyocyanin (phz operon), 2-heptyl-3-hydroxy-4(1H)-quinolone (PQS) signal (pqs operon), pyochelin (pch operon) and pyoverdine (pvd operon). Corroborating these microarray results, indole and 7HI decreased production of pyocyanin, rhamnolipid, PQS and pyoverdine and enhanced antibiotic resistance. In addition, indole affected the utilization of carbon, nitrogen and phosphorus, and 7HI abolished swarming motility. Furthermore, 7HI reduced pulmonary colonization of P. aeruginosa in guinea pigs and increased clearance in lungs. Hence, indole-related compounds have potential as a novel antivirulence approach for the recalcitrant pathogen P. aeruginosa. [source]

Semi-automated risk estimation using large databases: quinolones and clostridium difficile associated diarrhea,

PHARMACOEPIDEMIOLOGY AND DRUG SAFETY, Issue 6 2010
Robertino M. Mera
Abstract Purpose The availability of large databases with person time information and appropriate statistical methods allow for relatively rapid pharmacovigilance analyses. A semi-automated method was used to investigate the effect of fluoroquinolones on the incidence of C. difficile associated diarrhea (CDAD). Methods Two US databases, an electronic medical record (EMR) and a large medical claims database for the period 2006,2007 were evaluated using a semi-automated methodology. The raw EMR and claims datasets were subject to a normalization procedure that aligns the drug exposures and conditions using ontologies; Snowmed for medications and MedDRA for conditions. A retrospective cohort design was used together with matching by means of the propensity score. The association between exposure and outcome was evaluated using a Poisson regression model after taking into account potential confounders. Results A comparison between quinolones as the target cohort and macrolides as the comparison cohort produced a total of 564,797 subjects exposed to a quinolone in the claims data and 233,090 subjects in the EMR. They were matched with replacement within six strata of the propensity score. Among the matched cohorts there were a total of 488 and 158 outcomes in the claims and the EMR respectively. Quinolones were found to be twice more likely to be significantly associated with CDAD than macrolides adjusting for risk factors (IRR 2.75, 95%CI 2.18,3.48). Conclusions Use of a semi-automated method was successfully applied to two observational databases and was able to rapidly identify a potential for increased risk of developing CDAD with quinolones. Copyright © 2010 John Wiley & Sons, Ltd. [source]

Influence of dose on the distribution kinetics of ciprofloxacin and ofloxacin in the isolated hindlimb of the rat

BIOPHARMACEUTICS AND DRUG DISPOSITION, Issue 8 2000
A.C. Casquero-Dorado
Abstract The aim of this study was to determine whether the dose influences the distribution kinetics of ciprofloxacin and ofloxacin in muscle- bone- and skin-tissues included in the isolated hindlimb of the rat. Experiments were carried out in the isolated perfused hindlimb of the rat, administering a single dose of 45, 450 or 900 µg of each quinolone as a bolus injection. Outflow perfusate samples were collected for 20 min and drug levels were determined by an HPLC technique. The mean transit time (MTT) and the distribution volume of ciprofloxacin significantly increased with the dose injected (MTT=1.47±0.69, 8.74±0.27 and 9.52±2.95 min for 45, 450 and 900 µg, respectively). A similar situation was observed with ofloxacin, although the increase in these parameters was less pronounced (MTT=3.65±0.86, 7.92±2.03 and 8.32±1.70 min for 45, 450 and 900 µg, respectively). The distribution of ciprofloxacin and ofloxacin in the rat hindlimb appears to be a dose-dependent process, at least for the dose range considered in this study. This might explain the high variability in the distribution coefficients reported for these drugs in literature. Copyright © 2000 John Wiley & Sons, Ltd. [source]

Experimental Escherichia coli epididymitis in rats: a model to assess the outcome of antibiotic treatment

BJU INTERNATIONAL, Issue 9 2002
M. Ludwig
Objective ,To assess the effect of initial antimicrobial therapy with a new highly potent quinolone (sparfloxacin) on the outcome of infection, especially acute and chronic inflammation, in a rat model of unilateral Escherichia coli epididymitis. Materials and methods ,The study included 60 Sprague-Dawley rats, each of which received 0.1 mL of an E. coli (0:6 strain) suspension (106 colony forming units/mL) injected into the right ductus deferens. At 24 h after infection an oral antimicrobial treatment with sparfloxacin was initiated in half of the animals. The rats were killed 14 days, 3 and 6 months after infection, and both epididymes and the prostate gland cultured to re-isolate E. coli. To evaluate the grade of inflammation in both epididymes, histological variables, including acute and chronic inflammation and scar formation, were evaluated and a total inflammatory score, representing the sum of all variables, computed. Results ,Whereas antimicrobial therapy eradicated the pathogen, in untreated animals the pathogen was detectable for up to 6 months after infection in the infected epididymis and/or the prostate gland, while the contralateral epididymis was sterile. The inflammatory reaction in the infected epididymis was significantly less in treated animals (P < 0.001). Subclinical nonbacterial inflammation was present in the contralateral epididymis. Conclusions ,Although adequate antimicrobial treatment eradicated the pathogen and reduced the grade of epididymal damage, inflammation was not avoided. Subclinical inflammation of the contralateral epididymis may contribute to impaired fertility. These results indicate that an inflammatory reaction initiated by bacteria might persist as a nonbacterial process despite early therapy, or by bacteria undetectable by conventional culture techniques, and may compromise male fertility. [source]

A New Quinolone and Other Constituents from the Fruits of Tetradium ruticarpum: Effects on Neutrophil Pro-Inflammatory Responses

Photofading of phenylazo-aniline, -pyridone and -quinolone disperse dyes on a nylon 6 substrate

COLORATION TECHNOLOGY, Issue 2 2009
Yasuyo Okada
The photofading of phenylazo-aniline, -pyridone and -quinolone disperse dyes on nylon fabric was analysed using the Kubelka,Munk (K/S) spectra of fabrics exposed to a carbon arc in air. The exposure of dyed fabric through ultraviolet and coloured filters, which do not shield the main absorption band, showed a large decrease in the initial rate (KPA) of fading. Compared with the KPA values without filters, the values using filters were half as large for dyes without the nitro groups and a quarter as large for dyes with the nitro groups. The KPA values may be qualitatively explained by the sum of azo scission (decrease of K/S value at ,max) and the conversion of nitro groups to nitroso groups. These phenomena occur, respectively, via thermal disproportionation reactions between hydrazinyl radicals (from the azo group) and the reaction between hydrazinyl and N-centred nitrosyl hydroxide radicals (from the nitro group). The azo scission is promoted by N-centred nitrosyl hydroxide radicals via the latter reactions. [source]

Antimicrobial therapy in Dermatology

JOURNAL DER DEUTSCHEN DERMATOLOGISCHEN GESELLSCHAFT, Issue 1 2006
Cord Sunderkötter
Antiseptika; Antibiotika; ,-Laktam-Resistenz; Weichteilinfektion Summary The extensive and sometimes indiscriminate use of antibiotics sometimes without strict indications has led to increases in both bacterial resistance and sensitization of patients. Systemic antibiotics in skin infections are indicated when a severe local infection occurs which spreads into the surrounding tissue or when there are signs of systemic infection. There are special indications in patients with peripheral arterial occlusive disease,diabetes or immunosuppression. Topical use of antibiotics should be abandoned and replaced by antiseptics. The ,-lactam antibiotics are the antibiotics of first choice for many skin infections. They are usually effective, have a well-defined profile of adverse events and most are affordable. Penicillin G or V are the first line treatment for erysipelas. Infections with Staphylococcus aureus are usually treated with isoxazolyl penicillins or second generation cephalosporins. In mixed infections in patients with diabetes or peripheral arterial occlusive disease,the treatment of choice is metronidazole plus ,-lactam-/,-lactamase inhibitor antibiotics, but quinolones or second generation cephalosporins can also be used, once again with metronidazole. The aim of this review is to define the indications for antibiotics in dermatology, to highlight their modes of action and adverse effects and to make suggestions for rational antibiotic therapy in cutaneous infections frequently encountered in the practice of dermatology. Zusammenfassung Der bisweilen unkritische Einsatz von Antibiotika hat die Resistenzentwicklung beschleunigt und die Sensibilisierungsrate bei Patienten erhöht. Systemische Antibiotika sind bei kutanen Superinfektionen in der Regel dann indiziert, wenn eine schwere lokale Infektion mit Ausbreitung in das umgebende Gewebe vorliegt oder wenn sich gleichzeitig Zeichen einer systemischen Infektion einstellen. Bei peripherer arterieller Verschlusskrankheit, Diabetes mellitus oder Immunsuppression kann die Indikation auch früher gestellt werden. Lokale Antibiotika sollten in der Regel gemieden und durch moderne Antiseptika ersetzt werden. ,-Laktam-Antibiotika stellen für viele bakterielle Infektionserkrankungen in der ambulanten und klinischen Dermatologie die Antibiotika der ersten Wahl dar. Sie sind häufig ausreichend wirksam, besitzen ein gut definiertes Nebenwir-kungsprofil und sind zumeist preisgünstig. So wird das klassische Streptokokken-Erysipel mit Penicillin G oder V therapiert, bei Infektionen durch S. aureus kommen primär Isoxazolyl-Penicilline oder Zweit-Generations-Cephalosporine zum Einsatz. Im Falle von Mischinfektionen bei Diabetes mellitus oder pAVK sind ,-Laktam/,-Laktamaseinhibitoren indiziert, alternativ auch Chinolone oder Zweitgenerations-Cephalosporine, jeweils in Kombination mit Metronidazol. Diese Übersicht möchte die Indikationen für Antibiotika in der Dermatologie aufzeigen, das Wichtigste zu deren Wirkungsweise und Nebenwirkungen aufzählen und Therapievorschläge für häufige Infektionen der Haut in der dermatologischen Praxis geben. [source]

Bacteriological study of shrimp, Penaeus monodon Fabricius, hatcheries in India

JOURNAL OF APPLIED ICHTHYOLOGY, Issue 2 2001

Shrimp hatcheries often face problems of mortality caused by diseases. To understand the bacteriological status of shrimp, Penaeus monodon Fabricius, hatcheries in India, a study of hatchery water at different points was conducted in several hatcheries located along the east and west coast of India. The species composition of the bacterial flora was also determined. The total plate counts of raw sea water on tryptic soya agar ranged from 102 to 104 ml,1, whereas it ranged from 104 to 106 ml,1 in larval tanks. In the larval tanks, the proportion of Vibrio species ranged from 50% to 73%, as compared to 31% in raw sea water. A mixed bacterial flora was observed in hatchery water; however, in the larval tanks, the flora in the larvae was predominantly made up of Vibrio species. A few of the tested Vibrio isolates were non-virulent to shrimp larvae under experimental conditions. Over 90% of the strains were resistant to amoxycillin, ampicillin, cephalexin, cephazolin, cloxacillin and sulphafurazole. Most strains showed sensitivity to tetracycline, chloramphenicol, and quinolones such as norfloxacin and ciprofloxacin. [source]

Proarrhythmia as a Class Effect of Quinolones: Increased Dispersion of Repolarization and Triangulation of Action Potential Predict Torsades de Pointes

JOURNAL OF CARDIOVASCULAR ELECTROPHYSIOLOGY, Issue 6 2007
PETER MILBERG M.D.
Background: Numerous noncardiovascular drugs prolong repolarization and thereby increase the risk for patients to develop life-threatening tachyarrhythmias of the torsade de pointes (TdP) type. The development of TdP is an individual, patient-specific response to a repolarization-prolonging drug, depending on the repolarization reserve. The aim of the present study was to analyze the underlying mechanisms that discriminate hearts that will develop TdP from hearts that will not develop TdP. We therefore investigated the group of quinolone antibiotics that reduce repolarization reserve via IKr blockade in an intact heart model of proarrhythmia. Methods and Results: In 47 Langendorff-perfused, AV-blocked rabbit hearts, ciprofloxacin (n = 10), ofloxacin (n = 14), levofloxacin (n = 10), and moxifloxacin (n = 13) in concentrations from 100 ,M to 1,000 ,M were infused. Eight monophasic action potentials (MAPs) and an ECG were recorded simultaneously. After incremental pacing at cycle lengths from 900 ms to 300 ms to compare the action potential duration, potassium concentration was lowered to provoke TdP. All antibiotics led to a significant increase in QT interval and MAP duration, and exhibited reverse-use dependence. Eight simultaneously recorded MAPs demonstrated an increase in dispersion of repolarization in the presence of all antibiotics. MAP triangulation (ratio: MAP90/50) and fluctuation of consecutive action potentials were increased for all tested drugs at high concentrations. In the presence of low potassium concentration, all quinolones led to TdP: ciprofloxacin, 4 out of 10 (40%); ofloxacin, 3 out of 14 (21%); moxifloxacin, 9 out of 13 (69%); and levofloxacin, 2 out of 10 (20%). Hearts that developed TdP demonstrated a significant greater influence on dispersion of repolarization and on triangulation as compared with hearts without TdP. Conclusion: Quinolone antibiotics may be proarrhythmic due to a significant effect on myocardial repolarization. The individual response of a heart to develop TdP in this experimental model is characterized by a greater effect on dispersion of repolarization and on triangulation of action potential as compared with hearts that do not develop TdP. [source]

Incidence, spectrum and antibiotic sensitivity pattern of bacterial infections among patients with acute pancreatitis

JOURNAL OF GASTROENTEROLOGY AND HEPATOLOGY, Issue 9 2001
Pramod Kumar Garg
Abstract Background and Aim: Secondary infection of pancreatic necrotic tissue and peripancreatic fluid is a serious complication of acute pancreatitis resulting in significant morbidity and mortality. The aim of this study was to find out the spectrum of bacterial infections, and their antibiotic sensitivity pattern in patients with acute pancreatitis. Methods: All consecutive patients with acute pancreatitis were studied prospectively. Detailed investigations were carried out to identify bacterial infections and their antibiotic sensitivities in patients with suspected infection. These investigations included cultures of various body fluids, throat swabs, indwelling cannula and catheter tips. Pancreatic tissue was obtained by using needle aspiration or at surgery for Gram's stain, culture and sensitivity. All cultures were repeated until the presence of infection was confirmed or excluded. Results: A total of 169 patients with acute pancreatitis were studied during the period between January 1997 and June 2000 (mean age 41.3 years; 116 males and 53 females). Of the 169 patients, 63 had infections at various sites. A total of 80 cultures were positive, and 12 different bacterial isolates were cultured from samples taken from these 63 patients. Polymicrobial infection was seen in 32% of patients. Twenty-four patients had a confirmed pancreatic infection. Blood cultures had a growth of organisms in 19 patients, with evidence of ongoing or worsening pancreatitis, thus raising a strong suspicion of infected necrosis in them. The commonest organisms were Escherichia coli from 20 cultures and Pseudomonas aeruginosa from 18 cultures. The antibiotic sensitivity pattern showed that most bacteria were sensitive to third generation cephalosporins and quinolones; notably among them were cefotaxime, ceftazidime, and ciprofloxacin. Conclusion: Bacterial infections were seen in 37% of patients with acute pancreatitis. The commonest organisms were Pseudomonas aeruginosa and Escherichia coli. Most bacterial isolates were sensitive to third generation cephalosporins and quinolones. [source]

Quinolone analogues 10: Synthesis of antimalarial quinolones having pyridyl moiety in N1-side chain

JOURNAL OF HETEROCYCLIC CHEMISTRY, Issue 3 2010
Yoshihisa Kurasawa
Novel 4-quinolone-3-carboxylates 6,7 and 4-quinolone-3-carboxylic acids 8,11 were synthesized from 4-hydroxyquinoline-3-carboxylates. Ethyl 1-[1-ethoxycarbonyl-2-(4-pyridyl)vinyl]-6-fluoro-4-oxoquinoline-3-carboxylate 7a was found to show antimalarial activity from the screening data. J. Heterocyclic Chem., (2010). [source]

Oral quinolones in hospitalized patients: an evaluation of a computerized decision support intervention,

JOURNAL OF INTERNAL MEDICINE, Issue 4 2004
T. Hulgan
Abstract. Objective., To determine whether a computerized decision support system could increase the proportion of oral quinolone antibiotic orders placed for hospitalized patients. Design., Prospective, interrupted time-series analysis. Setting., University hospital in the south-eastern United States. Subjects., Inpatient quinolone orders placed from 1 February 2001 to 31 January 2003. Intervention., A web-based intervention was deployed as part of an existing order entry system at a university hospital on 5 February 2002. Based on an automated query of active medication and diet orders, some users ordering intravenous quinolones were presented with a suggestion to consider choosing an oral formulation. Main outcome measure., The proportion of inpatient quinolone orders placed for oral formulations before and after deployment of the intervention. Results., There were a total of 15 194 quinolone orders during the study period, of which 8962 (59%) were for oral forms. Orders for oral quinolones increased from 4202 (56%) before the intervention to 4760 (62%) after, without a change in total orders. In the time-series analysis, there was an overall 5.6% increase (95% CI 2.8,8.4%; P < 0.001) in weekly oral quinolone orders due to the intervention, with the greatest effect on nonintensive care medical units. Conclusions., A web-based intervention was able to increase oral quinolone orders in hospitalized patients. This is one of the first studies to demonstrate a significant effect of a computerized intervention on dosing route within an antibiotic class. This model could be applied to other antibiotics or other drug classes with good oral bioavailability. [source]

Fluoroquinolone efflux mediated by ABC transporters

JOURNAL OF PHARMACEUTICAL SCIENCES, Issue 9 2008
Ana I. Alvarez
Abstract Quinolones and fluoroquinolones are broad spectrum bactericidal drugs, which are widely used in both human and veterinary medicine. These drugs can quite easily enter cells and are often used to treat intracellular pathogens. Some fluoroquinolones have been reported to undergo efflux, which could explain their low bioavailability. There is a growing need to understand resistance mechanisms to quinolones, involving for instance mutations or the action of efflux pumps. Several members of the ATP-binding cassette (ABC) drug efflux transporter family (MDR, MRP, ABCG2) significantly affect the pharmacokinetic disposition of quinolones. Active secretory mechanisms common to all fluoroquinolones have been suggested, as well as competition between fluoroquinolones at transporter sites. For grepafloxacin and its metabolites, MRP2 has been demonstrated to mediate biliary excretion. However, MDR1 is responsible for grepafloxacin intestinal secretion. Recently it has been shown that ciprofloxacin and enrofloxacin are efficiently transported ABCG2 substrates which are actively secreted into milk. It appears that multiple ABC transporters contribute to the overall secretion of fluoroquinolones. The objective of this work is to review the recent advances in insights into ABC transporters and their effects on fluoroquinolone disposition and resistance including data on drug secretion into milk. © 2008 Wiley-Liss, Inc. and the American Pharmacists Association J Pharm Sci 97:3483,3493, 2008 [source]

Multiresidue HPLC analysis of ten quinolones in milk after solid phase extraction: Validation according to the European Union Decision 2002/657/EC

JOURNAL OF SEPARATION SCIENCE, JSS, Issue 15 2007
Eleni A. Christodoulou
Abstract A rapid and sensitive analytical method was developed for the residue analysis of ten quinolones (enoxacin (ENO), ofloxacin (OFL), norfloxacin (NOR), ciprofloxacin (CIP), danofloxacin (DAN), enrofloxacin (ENR), sarafloxacin (SAR), oxolinic acid (OXO), nalidixic acid (NAL), and flumequine (FLU)) in cow's milk. The analytes were extracted from milk by a deproteinization step followed by a simple SPE cleanup procedure using LiChrolut RP-18 Merck cartridges. Recoveries varied between 75 and 92%. HPLC separation was performed at 25°C using an ODS-3 PerfectSil® Target (250×4 mm2) 5 ,m analytical column (MZ-Analysentechnik, Germany). The mobile phase consisted of a mixture of TFA 0.1%,CH3CN,CH3OH, delivered by a gradient program at the flow rate of 1.2 mL/min. Elution of the ten analytes and the internal standard (caffeine, 7.5 ng/,L) was completed within 27 min. Column effluent was monitored using a photodiode array detector, set at 275 and 255 nm. The developed method was validated according to the criteria of Commission Decision 2002/657/EC. The LODs of the specific method of quinolones' determination in milk varied between 1.5 and 6.8 ng/,L. [source]

Chronic prostatitis and chronic pelvic pain in men: aetiology, diagnosis and management,

JOURNAL OF THE EUROPEAN ACADEMY OF DERMATOLOGY & VENEREOLOGY, Issue 3 2002
GA Luzzi
ABSTRACT Patients with chronic prostatitis/pelvic pain syndrome typically report genital or pelvic pain (in or around the penis, perineum, scrotum) lasting >3 months. Whereas true chronic bacterial prostatitis is an uncommon condition characterised by recurrent prostatic and urinary infection, chronic pelvic pain syndrome (CPPS) is a common condition in which no infection is found. Recent surveys suggest a prevalence of 2.5,3% for CPPS. The four-glass test, traditionally used to distinguish inflammatory and inflammatory forms of CPPS, has not been adequately validated; whether the distinction is clinically meaningful is increasingly questioned. The aetiology of CPPS is not known; urodynamic studies imply a neuromuscular origin. More recent work supports a role for proinflammatory cytokines in the pathogenesis. In the management of chronic bacterial prostatitis, trials support the use of quinolone antibiotics as first-line treatment. In contrast, the management of CPPS is generally unsatisfactory, as no reliable treatment has been identified. Treatments commonly tried include antibiotics (notably tetracyclines, quinolones and macrolides), anti-inflammatory agents, and alpha blockers. Newer approaches include trials of finasteride, quercetin and rofecoxib. A recent systematic review demonstrated that none of the current diagnostic and treatment methods for CPPS is supported by a robust evidence base. [source]

Preparation of anti-danofloxacin antibody and development of an indirect competitive enzyme-linked immunosorbent assay for detection of danofloxacin residue in chicken liver

JOURNAL OF THE SCIENCE OF FOOD AND AGRICULTURE, Issue 7 2009
Zhongqiu Liu
Abstract BACKGROUND: Danofloxacin is used widely as both a clinical medicine for humans and a veterinary drug in animal husbandry. In this study a polyclonal anti-danofloxacin antibody was prepared for the first time and a simple and rapid indirect competitive enzyme-linked immunosorbent assay (cELISA) method based on the antibody was developed to monitor danofloxacin residue in chicken liver. RESULTS: The prepared antibody showed high sensitivity, with an IC50 value of 2.0 ng mL,1 towards danofloxacin, and good specificity, with significant cross-reactivity only towards pefloxacin (22%) and fleroxacin (21%) among commonly used (fluoro)quinolones evaluated in the study. The developed cELISA test kit had a detection limit of 0.8 ng mL,1, and satisfactory results were obtained when it was applied to chicken liver spiked with various levels of danofloxacin. The cELISA test kit was also used to detect danofloxacin in chicken liver samples purchased from a local food market, and the results were confirmed by liquid chromatography/mass spectrometry. CONCLUSION: The anti-danofloxacin antibody prepared in this study exhibits excellent quality, with high sensitivity and good specificity. The cELISA test kit based on the antibody has a very low detection limit and is suitable for use as an efficient screening method to detect danofloxacin residue in foods and food products. Copyright © 2009 Society of Chemical Industry [source]

Bacterial infections in cirrhosis

LIVER INTERNATIONAL, Issue 4 2004
Miguel Navasa
Abstract: Spontaneous bacterial peritonitis, urinary tract infections, respiratory infections and bacteremia are the most frequent infective complications in cirrhosis. These infections are due to the concomitant presence of different facilitating mechanisms including changes in the intestinal flora and in the intestinal barrier, depression of activity of the reticuloendothelial system, decreased opsonic activity of the ascitic fluid, neutrophil leukocyte dysfunction and iatrogenic factors among others. The fact, that the probability of having a microorganism responsible for the infection quinolone resistant is higher than 30% should be taken into account when treating any infection in a cirrhotic patient receiving selective intestinal decontamination with quinolones, and therefore, quinolones as empiric treatment are not indicated. [source]

Semi-automated risk estimation using large databases: quinolones and clostridium difficile associated diarrhea,

Risk of drug-related problems for various antibiotics in hospital: assessment by use of a novel method,

PHARMACOEPIDEMIOLOGY AND DRUG SAFETY, Issue 8 2008
Hege Salvesen Blix MSc
Abstract Purpose To investigate the use of antibiotics in hospitals, to explore drug-related problems (DRPs) linked to antibiotics and to introduce a novel way of expressing the risks accompanying use of various antibiotics. Methods Patients from internal medicine departments in four Norwegian hospitals were prospectively included in 2002. Demographics, drugs used, medical history, laboratory data and clinical/pharmacological risk factors were recorded. DRPs were identified by clinical pharmacists and assessed in multidisciplinary hospital teams. A new term, the drug risk ratio, was established and defined as the number of times the antibiotic was associated with DRPs in relation to the number of times it was used. Results Out of the 668 patients included, 283 patients (42%) used antibiotics (AB users). AB users were older (76.2 vs. 73.9), used more drugs on admission (5.1 vs. 4.4) and had more DRPs (3.0 vs. 2.2) than non-users. The DRP categories no further need for drug, non-optimal drug and non-optimal dose were most frequently observed. The drug risk ratio, calculated for 12 antibiotic groups, was highest for aminoglycosides (0.77), , -lactamase-resistant penicillins (0.56), macrolides (0.54) and quinolones (0.48) and lowest for first- and third-generation cephalosporins, 0.17 and 0.13, respectively. Conclusions Nearly half of the hospitalised patients were prescribed antibiotics and antibiotic associated DRPs occurred frequently. The drug risk ratio for the different antibiotic groups varied with a factor of six from the lowest to the highest. A high drug risk ratio would alert of antibiotics which require heightened awareness when going to be used in clinical practice. Copyright © 2008 John Wiley & Sons, Ltd. [source]

Antibiotics in Dutch general practice: nationwide electronic GP database and national reimbursement rates,

PHARMACOEPIDEMIOLOGY AND DRUG SAFETY, Issue 4 2008
Annemiek E. Akkerman PhD
Abstract Purpose In order to assess whether different databases generate information which can be reliable compared with each other, this study aimed to assess to which degree prescribing rates for systemic antibiotics from a nationwide electronic general practitioner (GP) database correspond with national reimbursement rates, and to investigate for which indications antibiotics are prescribed. Methods Nationwide GP prescribing data were collected from the Second Dutch National Survey of General Practice (DNSGP-2) based on 90 general practices serving 358 008 patients in 2001. Dutch national reimbursement rates for GPs were derived from claims data of the Dutch Drug Information System/Health Care Insurance Board (GIP/CVZ) from 2001. We calculated antibiotic prescribing rates per 1000 patients/inhabitants for each database, and these rates were compared for the total rates and according to antibiotic subgroups. Indications for which GPs prescribed antibiotics were described. Results In national reimbursement data, 339 antibiotic prescriptions per 1000 inhabitants were prescribed by GPs, while the nationwide GP database showed 255 prescriptions per 1000 patients (75% coverage with reimbursement rates). The nationwide GP database showed high volumes of sulphonamides & trimethoprim, and small volumes of macrolides and quinolones. Half of the prescriptions (48%) were prescribed for respiratory diseases, a quarter (26%) for urinary diseases and 7% for ear diseases. Conclusions GPs voluntarily participating in a research network prescribe less antibiotics than Dutch GPs in general, and are cautious in prescribing newer and more broad-spectrum antibiotics. This point has to be taken into account when databases will be compared with each other. Copyright © 2007 John Wiley & Sons, Ltd. [source]

Trends in antimicrobial utilization at a Spanish general hospital during a 5-year period

PHARMACOEPIDEMIOLOGY AND DRUG SAFETY, Issue 3 2003
Lorena Hermosilla Nájera
Abstract Purpose Antimicrobials are a major part of hospital pharmacy budgets and must be considered in resource planning and spending projections. This study describes the profile of antibiotic use at a medium-sized hospital (by examining the ICU separately) and analyses its evolution over the period 1996,2000. Methods Descriptive and retrospective study. Pharmacy records were reviewed to identify oral and parenteral antimicrobial agents administered to inpatients. Results were expressed in Daily Defined Doses (DDD) per 100 stays and day. Results During the 5-year study period 176.162 DDD/100 s-d of antibiotics were consumed in the ICU, whereas in the rest of the hospital usage was much lower (54.438 DDD/100 s-d). Aminoglycosides, cephalosporins, penicillins, glycopeptides and carbapenems were the most commonly used groups of antimicrobials in the ICU, and penicillins, cephalosporins, trimethoprim/sulfonamide combinations, aminoglycosides and quinolones in the rest of the hospital. Conclusions ICUs have some special features which make them different to the other inpatient areas. Because of that fact we consider it important to study this specific patient-care area separately. Copyright © 2003 John Wiley & Sons, Ltd. [source]

Multicentre evaluation of prescribing concurrence with anti-infective guidelines: epidemiological assessment of indicators

PHARMACOEPIDEMIOLOGY AND DRUG SAFETY, Issue 5 2002
Roel Fijn
Abstract Purpose To assess indicators for anti-infective prescribing not concurrent with regional pharmacotherapeutic treatment guidelines (PTGs) on infectious diseases. Methods A retrospective explorative cohort study based on hospital-wide anti-infective prescription data of a 2-month cross-sectional period (n=1037). Risk rates (absolute risks: AR), risk rate ratios (relative risks: RR) and odds ratios (OR) with 95% confidence intervals (95%CI) were estimated for patient, disease, drug, and prescriber variables considered to be potential indicators. Univariable and multivariable logistic regression analyses were performed. Findings Non-concurrence existed of non-indicated prescribing of (particular) anti-infectives (24.3%) and prescribing of non-first choice anti-infectives (55.2%). Non-concurrent durations of treatment and dosing issues accounted for 17.2% and 16.2% respectively. Non-concurrence was associated with empirical therapy, with certain diagnoses, such as skin and soft tissue, urinary, and osteoarthrological infections, and with prescriptions involving topical dosage forms, cephalosporins, macrolides and lincosamides, and quinolones. There was also an association with certain hospitals and with prescribing by geriatricians, surgeons, pulmonologists, and urologists and, in general, junior clinicians in training. Conclusions Other hospitals could use our epidemiological framework to identify their own indicators for non-concurrent prescribing. Our findings suggest tailor-made enforcement of PTG adherence for certain prescribers while conversely, adaptation of the PTGs will be required for some infectious diseases. Copyright © 2002 John Wiley & Sons, Ltd. [source]

Construction of the Korea Elderly Pharmacoepidemiologic Cohort: drug utilization review of cephalosporins in geriatric inpatients

PHARMACOEPIDEMIOLOGY AND DRUG SAFETY, Issue 6 2001
Byung Joo Park MD
Abstract We performed a cohort-based pharmacoepidemiologic study in order to evaluate the pattern of cephalosporin prescriptions in elderly inpatients in Korea. The Korea Elderly Pharmacoepidemiologic Cohort was composed of a geriatric population of beneficiaries of the Korea Medical Insurance Corporation residing in Busan in 1993. The cohort consisted of 23,649 members, comprising 15,221 women (64.4%) and 8428 men (35.6%). The study population for drug utilization review consisted of those cohort members who were admitted into hospitals during the period January 1993 through December 1994. The number of hospitalized patients was 4262, comprising 2631 women (61.7%) and 1681 men (38.3%). The trend of cephalosporin prescriptions over the 2-year period showed that the use of second and third generation cephalosporins increased relative to the use of first generation. The use of cephalosporins combined with other antibiotics was found to occur in 22.8% aminoglycosides (76.7%) and quinolones (17.1%) being the most common antibiotics combined with cephalosporins. Our result demonstrates an increase in the prescription of second and third generation cephalosporins in Korea, which has implications not only for the elderly population but also for the total population because of the impact on health care costs and the potential for the emergence of antimicrobial resistance. Copyright © 2001 John Wiley & Sons, Ltd. [source]

Real-time Visualization of Photochemically Induced Fluorescence of 8-Halogenated Quinolones: Lomefloxacin, Clinafloxacin and Bay3118 in Live Human HaCaT Keratinocytes,

PHOTOCHEMISTRY & PHOTOBIOLOGY, Issue 4 2010
Edmond B. Koker
Halogenoquinolones are potent and widely used antimicrobials blocking microbial DNA synthesis. However, they induce adverse photoresponses through the absorption of UV light, including phototoxicity and photocarcinogenicity. The phototoxic responses may be the result of photosensitization of singlet oxygen, production of free radicals and/or other reactive species resulting from photodehalogenation. Here, we report the use of laser scanning confocal microscopy to detect and to follow the fluorescence changes of one monohalogenated and three di-halogenated quinolones in live human epidermal keratinocyte cells during in situ irradiation by confocal laser in real time. Fluorescence image analysis and co-staining with the LysoTracker probe showed that lysosomes are a preferential site of drug localization and phototransformations. As the lysosomal environment is relatively acidic, we also determined how low pH may affect the dehalogenation and concomitant fluorescence. With continued UV irradiation, fluorescence increased in the photoproducts from BAY y3118 and clinafloxacin, whereas it decreased for lomefloxacin and moxifloxacin. Our images not only help to localize these phototoxic agents in the cell, but also provide means for dynamic monitoring of their phototransformations in the cellular environment. [source]

Conformationally Constrained Analogs of N -Substituted Piperazinylquinolones: Synthesis and Antibacterial Activity of N -(2,3-Dihydro-4-hydroxyimino-4H -1-benzopyran-3-yl)-piperazinylquinolones

ARCHIV DER PHARMAZIE, Issue 7 2009
Saeed Emami
Abstract A series of novel quinolone agents bearing a particular bulky and conformationally constrained bicyclic substituent (2,3-dihydro-4-hydroxyimino-4H -1-benzopyran-3-yl- moiety) on the piperazine ring of 7-piperazinyl quinolones (norfloxacin, enoxacin, ciprofloxacin, and levofloxacin) were synthesized and evaluated against a panel of Gram-positive and Gram-negative bacteria. Among these derivatives, ciprofloxacin counterpart 9c, highly inhibited the tested Gram-positive bacteria, superior to that of the reference drugs, and displayed antibacterial activity at non-cytotoxic concentrations. [source]

65 Multi-resistant Escherichia coli septicaemia following transrectal ultrasound guided prostate biopsy , an emerging risk

BJU INTERNATIONAL, Issue 2006
A.-J. DAVIDSON
Introduction:, Transrectal ultrasound (TRUS) guided biopsy of the prostate is the standard procedure for diagnosing prostate carcinoma. Complications range from discomfort and bleeding to asymptomatic bacteruria and sepsis. Rarely, sepsis is fatal. E. coli is the most common pathogen causing infection and although no international standard for the use of prophylactic antibiotics exists their use has decreased the incidence of infection to around 2%. Worldwide the incidence of multi-resistant E. coli (MREC) is increasing, and we report two cases of septicaemia secondary to MREC infection postprostate biopsy. Methods:, We performed a review of case records involving postprostate biopsy MREC infection. A comprehensive literature review of TRUS guided biopsy of the prostate was also performed. Results:, All patients in our series had MREC cultured following TRUS guided biopsy of the prostate. All received the same prophylactic antibiotic regime (norfloxacin and gentamicin). They required admission to hospital for intravenous antibiotics and in two cases inotropic support, eventually making full recoveries. All had a history of recent travel to a developing country whilst two had self-limiting diarrhoea and this is the first report in the English literature of MREC following prostate biopsy. Other risk factors for acquiring multi-resistant urinary tract infections have been identified including age and previous quinolone therapy. Conclusion:, Antibiotic prophylaxis for biopsy of the prostate, being predominantly quinolones, will continue to aid in reducing morbidity. However, with the prevalence of MREC increasing current regimens will not cover such organisms potentially leading to sepsis. In our cases travel to developing countries appeared to be a risk factor for being colonised with MREC. We believe through careful history risk factors for multi-resistant urinary tract infection including travel may alert doctors to the potential risk of MREC at the time of biopsy leading to the addition of a broader spectrum antibiotic such as intravenous meropenem. [source]

Oral ciprofloxacin plus colistin: prophylaxis against bacterial infection in neutropenic patients.

BRITISH JOURNAL OF HAEMATOLOGY, Issue 1 2001
A strategy for the prevention of emergence of antimicrobial resistance
Following a 2-year study, the combination of oral ciprofloxacin and colistin has been used continuously for 10 years without the emergence of resistance. During a 2-year period (1987,1989), we compared ciprofloxacin + colistin (CIP + COL) with neomycin + colistin (NEO + COL) in a randomized trial , combinations chosen because of the potential for prophylaxis of Gram-negative infection by ciprofloxacin, with colistin given to reduce the risk of emergence of resistance. Sixty-four patients with similar demographics in each arm were evaluable for efficacy analysis. Patients on CIP + COL had a significantly lower proportion of neutropenic days with fever (P < 0·001) and neutropenic days on intravenous antibiotics (P < 0·001) than patients on NEO + COL. A total of 54 (15 bacteriologically documented) pyrexial episodes occurred in patients on CIP + COL and 77 (41 bacteriologically documented) in patients on NEO + COL. Only two Gram-negative bacterial infections occurred in the CIP + COL arm compared with 16 in the NEO + COL arm. No Staphylococcus aureus infections occurred in the CIP + COL group compared with 10 in the other patients. Two CIP-resistant Gram-negative bacilli were isolated from patients on CIP + COL compared with 13 NEO-resistant Gram-negative bacilli from patients on NEO + COL. Following a subsequent decade of unchanged use of this prophylactic strategy in neutropenic patients, a 2-year follow-up study between 1 January 1998 and 31 December 1999 showed 66 significant infections during 350,400 neutropenic episodes. Eight of the 111 (7·2%) isolates were with ciprofloxacin-resistant organisms, involving 2% of the neutropenic episodes, indicating that the strategy of combining colistin with ciprofloxacin has been effective in the prevention of Gram-negative sepsis in neutropenic patients without the emergence of significant resistance despite widespread concurrent hospital and community use of the quinolones. [source]