A group of derivatives of naphthyridine carboxylic acid, quinoline carboxylic acid, or NALIDIXIC ACID.
QUINOLONES containing a 4-oxo (a carbonyl in the para position to the nitrogen). They inhibit the A subunit of DNA GYRASE and are used as antimicrobials. Second generation 4-quinolones are also substituted with a 1-piperazinyl group at the 7-position and a fluorine at the 6-position.
Substances that prevent infectious agents or organisms from spreading or kill infectious agents in order to prevent the spread of infection.
A group of QUINOLONES with at least one fluorine atom and a piperazinyl group.
A broad-spectrum antimicrobial carboxyfluoroquinoline.
A synthetic fluoroquinolone antibacterial agent that inhibits the supercoiling activity of bacterial DNA GYRASE, halting DNA REPLICATION.
Any tests that demonstrate the relative efficacy of different chemotherapeutic agents against specific microorganisms (i.e., bacteria, fungi, viruses).
A synthetic fluoroquinolone (FLUOROQUINOLONES) with broad-spectrum antibacterial activity against most gram-negative and gram-positive bacteria. Norfloxacin inhibits bacterial DNA GYRASE.
Compounds that inhibit the activity of DNA TOPOISOMERASE II. Included in this category are a variety of ANTINEOPLASTIC AGENTS which target the eukaryotic form of topoisomerase II and ANTIBACTERIAL AGENTS which target the prokaryotic form of topoisomerase II.
A bacterial DNA topoisomerase II that catalyzes ATP-dependent breakage of both strands of DNA, passage of the unbroken strands through the breaks, and rejoining of the broken strands. Gyrase binds to DNA as a heterotetramer consisting of two A and two B subunits. In the presence of ATP, gyrase is able to convert the relaxed circular DNA duplex into a superhelix. In the absence of ATP, supercoiled DNA is relaxed by DNA gyrase.
A bacterial DNA topoisomerase II that catalyzes ATP-dependent breakage of both strands of DNA, passage of the unbroken strands through the breaks, and rejoining of the broken strands. Topoisomerase IV binds to DNA as a heterotetramer consisting 2 parC and 2 parE subunits. Topoisomerase IV is a decatenating enzyme that resolves interlinked daughter chromosomes following DNA replication.
A broad-spectrum 6-fluoronaphthyridinone antibacterial agent that is structurally related to NALIDIXIC ACID.
Substances that reduce the growth or reproduction of BACTERIA.
A synthetic 1,8-naphthyridine antimicrobial agent with a limited bacteriocidal spectrum. It is an inhibitor of the A subunit of bacterial DNA GYRASE.
The L-isomer of Ofloxacin.
The ability of microorganisms, especially bacteria, to resist or to become tolerant to chemotherapeutic agents, antimicrobial agents, or antibiotics. This resistance may be acquired through gene mutation or foreign DNA in transmissible plasmids (R FACTORS).
DNA TOPOISOMERASES that catalyze ATP-dependent breakage of both strands of DNA, passage of the unbroken strands through the breaks, and rejoining of the broken strands. These enzymes bring about relaxation of the supercoiled DNA and resolution of a knotted circular DNA duplex.
A synthetic broad-spectrum fluoroquinolone antibacterial agent active against most gram-negative and gram-positive bacteria.
The ability of bacteria to resist or to become tolerant to chemotherapeutic agents, antimicrobial agents, or antibiotics. This resistance may be acquired through gene mutation or foreign DNA in transmissible plasmids (R FACTORS).
A broad-spectrum antimicrobial fluoroquinolone. The drug strongly inhibits the DNA-supercoiling activity of DNA GYRASE.
Circular duplex DNA isolated from viruses, bacteria and mitochondria in supercoiled or supertwisted form. This superhelical DNA is endowed with free energy. During transcription, the magnitude of RNA initiation is proportional to the DNA superhelicity.
Synthetic antimicrobial related to NALIDIXIC ACID and used in URINARY TRACT INFECTIONS.
A species of gram-negative, facultatively anaerobic, rod-shaped bacteria (GRAM-NEGATIVE FACULTATIVELY ANAEROBIC RODS) commonly found in the lower part of the intestine of warm-blooded animals. It is usually nonpathogenic, but some strains are known to produce DIARRHEA and pyogenic infections. Pathogenic strains (virotypes) are classified by their specific pathogenic mechanisms such as toxins (ENTEROTOXIGENIC ESCHERICHIA COLI), etc.
Potentially pathogenic bacteria found in nasal membranes, skin, hair follicles, and perineum of warm-blooded animals. They may cause a wide range of infections and intoxications.
A nonimmunologic, chemically induced type of photosensitivity producing a sometimes vesiculating dermatitis. It results in hyperpigmentation and desquamation of the light-exposed areas of the skin.
A gram-positive organism found in the upper respiratory tract, inflammatory exudates, and various body fluids of normal and/or diseased humans and, rarely, domestic animals.
Bacteria which retain the crystal violet stain when treated by Gram's method.
The ability of bacteria to resist or to become tolerant to several structurally and functionally distinct drugs simultaneously. This resistance may be acquired through gene mutation or foreign DNA in transmissible plasmids (R FACTORS).
A group of often glycosylated macrocyclic compounds formed by chain extension of multiple PROPIONATES cyclized into a large (typically 12, 14, or 16)-membered lactone. Macrolides belong to the POLYKETIDES class of natural products, and many members exhibit ANTIBIOTIC properties.
Bacteria which lose crystal violet stain but are stained pink when treated by Gram's method.
Six-membered heterocycles containing an oxygen and a nitrogen.
One of the three domains of life (the others being Eukarya and ARCHAEA), also called Eubacteria. They are unicellular prokaryotic microorganisms which generally possess rigid cell walls, multiply by cell division, and exhibit three principal forms: round or coccal, rodlike or bacillary, and spiral or spirochetal. Bacteria can be classified by their response to OXYGEN: aerobic, anaerobic, or facultatively anaerobic; by the mode by which they obtain their energy: chemotrophy (via chemical reaction) or PHOTOTROPHY (via light reaction); for chemotrophs by their source of chemical energy: CHEMOLITHOTROPHY (from inorganic compounds) or chemoorganotrophy (from organic compounds); and by their source for CARBON; NITROGEN; etc.; HETEROTROPHY (from organic sources) or AUTOTROPHY (from CARBON DIOXIDE). They can also be classified by whether or not they stain (based on the structure of their CELL WALLS) with CRYSTAL VIOLET dye: gram-negative or gram-positive.
A very effective anticoccidial agent used in poultry.
Deoxyribonucleic acid that makes up the genetic material of bacteria.
Infections by bacteria, general or unspecified.
An antibiotic compound derived from Streptomyces niveus. It has a chemical structure similar to coumarin. Novobiocin binds to DNA gyrase, and blocks adenosine triphosphatase (ATPase) activity. (From Reynolds, Martindale The Extra Pharmacopoeia, 30th ed, p189)
A species of gram-negative, aerobic, rod-shaped bacteria commonly isolated from clinical specimens (wound, burn, and urinary tract infections). It is also found widely distributed in soil and water. P. aeruginosa is a major agent of nosocomial infection.
Any detectable and heritable change in the genetic material that causes a change in the GENOTYPE and which is transmitted to daughter cells and to succeeding generations.
The type species of the genus BARTONELLA, a gram-negative bacteria found in humans. It is found in the mountain valleys of Peru, Ecuador, and Southwest Columbia where the sandfly (see PHLEBOTOMUS) vector is present. It causes OROYA FEVER and VERRUGA PERUANA.
A plant genus of the family RUTACEAE which is used in Chinese medicine (DRUGS, CHINESE HERBAL). Evodiamine and other quinazoline alkaloids (QUINAZOLINES) are obtained from the fruit of E. ruticarpa.
A rapid-growing, nonphotochromogenic species that is potentially pathogenic, producing lesions of lung, bone, or soft tissue following trauma. It has been found in soil and in injection sites of humans, cattle, and cold-blooded animals. (Dorland, 28th ed)
The relationship between the chemical structure of a compound and its biological or pharmacological activity. Compounds are often classed together because they have structural characteristics in common including shape, size, stereochemical arrangement, and distribution of functional groups.
Simultaneous resistance to several structurally and functionally distinct drugs.
Closely congeneric derivatives of the polycyclic naphthacenecarboxamide. (Gilman et al., Goodman and Gilman's The Pharmacological Basis of Therapeutics, 8th ed, p1117)
The functional hereditary units of BACTERIA.
A nitroimidazole antiprotozoal agent used in ameba and trichomonas infections. It is partially plasma-bound and also has radiation-sensitizing action.
Glycosylated compounds in which there is an amino substituent on the glycoside. Some of them are clinically important ANTIBIOTICS.
A group of broad-spectrum antibiotics first isolated from the Mediterranean fungus ACREMONIUM. They contain the beta-lactam moiety thia-azabicyclo-octenecarboxylic acid also called 7-aminocephalosporanic acid.
A species of gram-negative, aerobic bacteria primarily found in purulent venereal discharges. It is the causative agent of GONORRHEA.
Compounds that inhibit the activity of DNA TOPOISOMERASES.
Proteins found in any species of bacterium.
Infections caused by bacteria that show up as pink (negative) when treated by the gram-staining method.
Four-membered cyclic AMIDES, best known for the PENICILLINS based on a bicyclo-thiazolidine, as well as the CEPHALOSPORINS based on a bicyclo-thiazine, and including monocyclic MONOBACTAMS. The BETA-LACTAMASES hydrolyze the beta lactam ring, accounting for BETA-LACTAM RESISTANCE of infective bacteria.
This drug combination has proved to be an effective therapeutic agent with broad-spectrum antibacterial activity against both gram-positive and gram-negative organisms. It is effective in the treatment of many infections, including PNEUMOCYSTIS PNEUMONIA in AIDS.
Chemicals with two conjoined aromatic rings incorporating two nitrogen atoms and one of the carbons oxidized with a keto oxygen.
Extrachromosomal, usually CIRCULAR DNA molecules that are self-replicating and transferable from one organism to another. They are found in a variety of bacterial, archaeal, fungal, algal, and plant species. They are used in GENETIC ENGINEERING as CLONING VECTORS.
An antibiotic first isolated from cultures of Streptomyces venequelae in 1947 but now produced synthetically. It has a relatively simple structure and was the first broad-spectrum antibiotic to be discovered. It acts by interfering with bacterial protein synthesis and is mainly bacteriostatic. (From Martindale, The Extra Pharmacopoeia, 29th ed, p106)
A subcategory of CHRONIC OBSTRUCTIVE PULMONARY DISEASE. The disease is characterized by hypersecretion of mucus accompanied by a chronic (more than 3 months in 2 consecutive years) productive cough. Infectious agents are a major cause of chronic bronchitis.
Cyclic AMIDES formed from aminocarboxylic acids by the elimination of water. Lactims are the enol forms of lactams.
Gram-negative bacteria occurring in the lower intestinal tracts of man and other animals. It is the most common species of anaerobic bacteria isolated from human soft tissue infections.
A family of gram-negative, facultatively anaerobic, rod-shaped bacteria that do not form endospores. Its organisms are distributed worldwide with some being saprophytes and others being plant and animal parasites. Many species are of considerable economic importance due to their pathogenic effects on agriculture and livestock.
An error-prone mechanism or set of functions for repairing damaged microbial DNA. SOS functions (a concept reputedly derived from the SOS of the international distress signal) are involved in DNA repair and mutagenesis, in cell division inhibition, in recovery of normal physiological conditions after DNA repair, and possibly in cell death when DNA damage is extensive.
A complex that includes several strains of M. avium. M. intracellulare is not easily distinguished from M. avium and therefore is included in the complex. These organisms are most frequently found in pulmonary secretions from persons with a tuberculous-like mycobacteriosis. Strains of this complex have also been associated with childhood lymphadenitis and AIDS; M. avium alone causes tuberculosis in a variety of birds and other animals, including pigs.
Infections with bacteria of the species ESCHERICHIA COLI.
A genus of gram-negative, nonmotile bacteria which are common parasitic inhabitants of the urogenital tracts of humans, cattle, dogs, and monkeys.
Semisynthetic thienamycin that has a wide spectrum of antibacterial activity against gram-negative and gram-positive aerobic and anaerobic bacteria, including many multiresistant strains. It is stable to beta-lactamases. Clinical studies have demonstrated high efficacy in the treatment of infections of various body systems. Its effectiveness is enhanced when it is administered in combination with CILASTATIN, a renal dipeptidase inhibitor.
A species of STENOTROPHOMONAS, formerly called Xanthomonas maltophilia, which reduces nitrate. It is a cause of hospital-acquired ocular and lung infections, especially in those patients with cystic fibrosis and those who are immunosuppressed.
Enumeration by direct count of viable, isolated bacterial, archaeal, or fungal CELLS or SPORES capable of growth on solid CULTURE MEDIA. The method is used routinely by environmental microbiologists for quantifying organisms in AIR; FOOD; and WATER; by clinicians for measuring patients' microbial load; and in antimicrobial drug testing.
Nonsusceptibility of an organism to the action of penicillins.
Gram-negative, non-motile, capsulated, gas-producing rods found widely in nature and associated with urinary and respiratory infections in humans.
The utilization of drugs as reported in individual hospital studies, FDA studies, marketing, or consumption, etc. This includes drug stockpiling, and patient drug profiles.
Proteins isolated from the outer membrane of Gram-negative bacteria.
A genus of gram-positive, aerobic bacteria. Most species are free-living in soil and water, but the major habitat for some is the diseased tissue of warm-blooded hosts.
A group of compounds consisting in part of two rings sharing one atom (usually a carbon) in common.
A large heterogeneous group of mostly alpha-hemolytic streptococci. They colonize the respiratory tract at birth and generally have a low degree of pathogenicity. This group of species includes STREPTOCOCCUS MITIS; STREPTOCOCCUS MUTANS; STREPTOCOCCUS ORALIS; STREPTOCOCCUS SANGUIS; STREPTOCOCCUS SOBRINUS; and the STREPTOCOCCUS MILLERI GROUP. The latter are often beta-hemolytic and commonly produce invasive pyogenic infections including brain and abdominal abscesses.
A species of gram-negative, facultatively anaerobic, rod-shaped bacteria that occurs in water, sewage, soil, meat, hospital environments, and on the skin and in the intestinal tract of man and animals as a commensal.
A bacteriostatic antibiotic macrolide produced by Streptomyces erythreus. Erythromycin A is considered its major active component. In sensitive organisms, it inhibits protein synthesis by binding to 50S ribosomal subunits. This binding process inhibits peptidyl transferase activity and interferes with translocation of amino acids during translation and assembly of proteins.
Inflammatory responses of the epithelium of the URINARY TRACT to microbial invasions. They are often bacterial infections with associated BACTERIURIA and PYURIA.
A semisynthetic antibiotic produced from Streptomyces mediterranei. It has a broad antibacterial spectrum, including activity against several forms of Mycobacterium. In susceptible organisms it inhibits DNA-dependent RNA polymerase activity by forming a stable complex with the enzyme. It thus suppresses the initiation of RNA synthesis. Rifampin is bactericidal, and acts on both intracellular and extracellular organisms. (From Gilman et al., Goodman and Gilman's The Pharmacological Basis of Therapeutics, 9th ed, p1160)
An antibacterial agent that is a semisynthetic analog of LINCOMYCIN.
Enzymes found in many bacteria which catalyze the hydrolysis of the amide bond in the beta-lactam ring. Well known antibiotics destroyed by these enzymes are penicillins and cephalosporins.
A serotype of SALMONELLA ENTERICA that causes mild PARATYPHOID FEVER in humans.
A genus of gram-negative, rod-shaped enterobacteria that can use citrate as the sole source of carbon.
Infections with bacteria of the family ENTEROBACTERIACEAE.
Skin diseases caused by bacteria, fungi, parasites, or viruses.
A renal dehydropeptidase-I and leukotriene D4 dipeptidase inhibitor. Since the antibiotic, IMIPENEM, is hydrolyzed by dehydropeptidase-I, which resides in the brush border of the renal tubule, cilastatin is administered with imipenem to increase its effectiveness. The drug also inhibits the metabolism of leukotriene D4 to leukotriene E4.
Short filamentous organism of the genus Mycoplasma, which binds firmly to the cells of the respiratory epithelium. It is one of the etiologic agents of non-viral primary atypical pneumonia in man.

Mutation of a conserved serine residue in a quinolone-resistant type II topoisomerase alters the enzyme-DNA and drug interactions. (1/2071)

A Ser740 --> Trp mutation in yeast topoisomerase II (top2) and of the equivalent Ser83 in gyrase results in resistance to quinolones and confers hypersensitivity to etoposide (VP-16). We characterized the cleavage complexes induced by the top2(S740W) in the human c-myc gene. In addition to resistance to the fluoroquinolone CP-115,953, top2(S740W) induced novel DNA cleavage sites in the presence of VP-16, azatoxin, amsacrine, and mitoxantrone. Analysis of the VP-16 sites indicated that the changes in the cleavage pattern were reflected by alterations in base preference. C at position -2 and G at position +6 were observed for the top2(S740W) in addition to the previously reported C-1 and G+5 for the wild-type top2. The VP-16-induced top2(S740W) cleavage complexes were also more stable. The most stable sites had strong preference for C-1, whereas the most reversible sites showed no base preference at positions -1 or -2. Different patterns of DNA cleavage were also observed in the absence of drug and in the presence of calcium. These results indicate that the Ser740 --> Trp mutation alters the DNA recognition of top2, enhances its DNA binding, and markedly affects its interactions with inhibitors. Thus, residue 740 of top2 appears critical for both DNA and drug interactions.  (+info)

Vasopressin V2 receptor enhances gain of baroreflex in conscious spontaneously hypertensive rats. (2/2071)

The aim of the present study was to determine the receptor subtype involved in arginine vasopressin (AVP)-induced modulation of baroreflex function in spontaneously hypertensive rats (SHR) and Wistar-Kyoto (WKY) rats using novel nonpeptide AVP V1- and V2-receptor antagonists. Baroreceptor heart rate (HR) reflex was investigated in both SHR and WKY rats which were intravenously administered the selective V1- and V2-receptor antagonists OPC-21268 and OPC-31260, respectively. Baroreflex function was assessed by obtaining alternate pressor and depressor responses to phenylephrine and sodium nitroprusside, respectively, to construct baroreflex curves. In both SHR and WKY rats baroreflex activity was tested before and after intravenous administration of vehicle (20% DMSO), OPC-21268 (10 mg/kg), and OPC-31260 (1 and 10 mg/kg). Vehicle did not significantly alter basal mean arterial pressure (MAP) and HR values or baroreflex function in SHR or WKY rats. The V1-receptor antagonist had no significant effect on resting MAP or HR values or on baroreflex parameters in both groups of rats, although this dose was shown to significantly inhibit the pressor response to AVP (5 ng iv; ANOVA, P < 0.05). In SHR but not WKY rats the V2-receptor antagonist significantly attenuated the gain (or slope) of the baroreflex curve (to 73 +/- 3 and 79 +/- 7% of control for 1 and 10 mg/kg, respectively), although AVP-induced pressor responses were also attenuated with the higher dose of the V2-receptor antagonist. These findings suggest that AVP tonically enhances baroreflex function through a V2 receptor in the SHR.  (+info)

Carrier-mediated lung distribution of HSR-903, a new quinolone antibacterial agent. (3/2071)

HSR-903 [(S)-(-)-5-amino-7-(7-amino-5-azaspiro[2. 4]hept-5-yl)-1-cyclopropyl-6-fluoro-1, 4-dihydro-8-methyl-4-oxoquinoline-3-carboxylic acid methanesulfonate] is a newly synthesized quinolone with a potent antibacterial activity and a low toxicity. The lung concentration of unchanged HSR-903 was about nine times higher than that in plasma after oral administration (5 mg/kg) in rats. In comparative studies, HSR-903 was accumulated more efficiently than levofloxacin, ciprofloxacin, and lomefloxacin in rat lung. To clarify the mechanism of the specific distribution of HSR-903 into the lung, the uptake of [14C]HSR-903 was studied using isolated rat lung cells and an isolated rat lung perfusion technique. Initial uptake of HSR-903 by isolated lung cells was temperature dependent, saturable, stereospecific, and Na+ and Cl- dependent. The Hill coefficients (1. 90 for Na+ and 1.13 for Cl-) suggest that two Na+ and one Cl- are associated with the transport of one HSR-903 molecule. The uptake of HSR-903 was inhibited by other quinolone antibacterial agents, grepafloxacin, and sparfloxacin. The extraction ratio of HSR-903 in isolated lung perfusion was temperature dependent and saturable. These findings suggest that HSR-903 is taken up by the lung cells via a carrier-mediated transport mechanism, resulting in a concentrative distribution into the lung.  (+info)

Activation of a cGMP-stimulated cAMP phosphodiesterase by protein kinase C in a liver Golgi-endosomal fraction. (4/2071)

The ability of Ca2+/phospholipid-dependent protein kinase (protein kinase C, PKC) to stimulate cAMP phosphodiesterase (PDE) activity in a liver Golgi-endosomal (GE) fraction was examined in vivo and in a cell-free system. Injection into rats of 4 beta-phorbol 12-myristate 13-acetate, a known activator of PKC, caused a rapid and marked increase in PKC activity (+325% at 10 min) in the GE fraction, along with an increase in the abundance of the PKC alpha-isoform as seen on Western immunoblots. Concurrently, 4 beta-phorbol 12-myristate 13-acetate treatment caused a time-dependent increase in cAMP PDE activity in the GE fraction (96% at 30 min). Addition of the catalytic subunit of protein kinase A (PKA) to GE fractions from control and 4 beta-phorbol 12-myristate 13-acetate-treated rats led to a comparable increase (130-150%) in PDE activity, suggesting that PKA is probably not involved in the in-vivo effect of 4 beta-phorbol 12-myristate 13-acetate. In contrast, addition of purified PKC increased (twofold) PDE activity in GE fractions from control rats but affected only slightly the activity in GE fractions from 4 beta-phorbol 12-myristate 13-acetate-treated rats. About 50% of the Triton-X-100-solubilized cAMP PDE activity in the GE fraction was immunoprecipitated with an anti-PDE3 antibody. On DEAE-Sephacel chromatography, three peaks of PDE were sequentially eluted: one early peak, which was stimulated by cGMP and inhibited by erythro-9 (2-hydroxy-3-nonyl) adenine (EHNA); a selective inhibitor of type 2 PDEs; and two retarded peaks of activity, which were potently inhibited by cGMP and cilostamide, an inhibitor of type 3 PDEs. Further characterization of peak I by HPLC resolved a major peak which was activated (threefold) by 5 microM cGMP and inhibited (87%) by 25 microM EHNA, and a minor peak which was insensitive to EHNA and cilostamide. 4 beta-Phorbol 12-myristate 13-acetate treatment caused a selective increase (2.5-fold) in the activity associated with DEAE-Sephacel peak I, without changing the K(m) value. These results suggest that PKC selectively activates a PDE2, cGMP-stimulated isoform in the GE fraction.  (+info)

A mutation in QRDR in the ParC subunit of topoisomerase IV was responsible for fluoroquinolone resistance in clinical isolates of Streptococcus pneumoniae. (5/2071)

Forty-one strains of Streptococcus pneumoniae were isolated at Seoul National University Children's Hospital from 1991 to 1997. Isolates were divided into six groups based on MICs of three quinolones, ciprofloxacin, ofloxacin and norfloxacin. Sequencing showed that the isolates which were intermediately resistant to three quinolones or resistant to at least one kind of quinolone had one missense mutation, Lys137-->Asn(AAG-->AAT) substitution in the ParC subunit of topoisomerase IV without additional mutation in QRDR of the GyrA subunit of DNA gyrase. In conclusion, the ParC subunit of DNA topoisomerase IV is the primary target site for fluoroquinolone in S. pneumoniae and Lys137-->Asn substitution renders the quinolone resistance in S. pneumoniae.  (+info)

Inflammatory pseudotumor in a cat with cutaneous mycobacteriosis. (6/2071)

A 5-year-old, castrated male, domestic Shorthair Cat had an ulcerated mass with fistulous tracts on the left hind paw. Homogeneous tan tissue diffusely infiltrated the dermis and subcutis of the paw and extended proximally so that, short of amputation, complete excision was not feasible. Biopsy specimens consisted of granulation tissue with marked proliferation of spindle cells. Neutrophils and histiocytic cells were scattered among the spindle cells. The histiocytic cells had abundant foamy or vacuolated cytoplasm, but features of granulomatous inflammation, such as epithelioid macrophages or granuloma formation, were not observed. The initial impression was inflammatory granulation tissue, but the degree of fibroplasia prompted inclusion of fibrosarcoma in the differential diagnosis. Cutaneous mycobacteriosis was diagnosed when numerous acid-fast bacteria were identified with Kinyoun's stain; Mycobacterium avium was subsequently cultured. The cat was euthanatized because of lack of response to enrofloxacin therapy. At necropsy, lesions were localized to the hind limb. Not only is mycobacteriosis an uncommon cause of cutaneous masses in cats, but this case was unusual because of the lack of granuloma formation and the similarity of the mass to a spindle cell tumor.  (+info)

Indomethacin-induced gastric antral damage in hamsters: are neutrophils involved? (7/2071)

BACKGROUND: A direct role for neutrophils in the pathophysiology of indomethacin-induced gastric damage is controversial. Therefore, such damage was evaluated in hamsters. METHODS: Gastric antral damage was evaluated 4 h after the oro-gastric administration of indomethacin (30 mg/kg). Prior to indomethacin, hamsters were treated with various pharmacological agents: rebamipide, methotrexate or anti-neutrophil serum (ANS). The number of circulating neutrophils was determined from Wright-Giemsa stained blood smears. Myeloperoxidase (MPO) activity was measured as a marker of gastric antral neutrophil infiltration. RESULTS: Indomethacin caused primarily gastric antral damage. By histology, this damage did not penetrate the muscularis mucosa. A significant increase in gastric antral MPO activity was also found in indomethacin-treated hamsters. Rebamipide decreased macroscopic gastric antral damage in a dose-related fashion. Methotrexate treatment reduced the circulating blood neutrophil number by 38-44%, but did not affect gastric damage. ANS treatment resulted in near complete neutropenia, and also in a substantial reduction (84%) in gastric antral MPO activity. However, gastric antral damage was not significantly altered by ANS. CONCLUSIONS: Neutrophils are not directly involved in the pathophysiology of indomethacin-induced damage to the hamster gastric antrum.  (+info)

Pharmacodynamic effects of subinhibitory concentrations of rufloxacin on bacterial virulence factors. (8/2071)

It has been reported that subinhibitory concentrations (sub-MICs) of some fluoroquinolones are still capable of affecting the topological characteristics of DNA (inhibition DNA-gyrase) and that this leads to a reduction in some of the factors responsible for bacterial virulence (by means of the disruption of protein synthesis and alterations in phenotype expression), even though the microorganisms themselves are not killed. The present study investigated the ability of sub-MICs of rufloxacin, an orally absorbed monofluorinated quinolone with a long half-life (28 to 30 h), to interfere with the bacterial virulence parameters of adhesiveness, hemagglutination, hydrophobicity, motility, and filamentation, as well as their interactions with host neutrophilic defenses such as phagocytosis, killing, and oxidative bursts. It was observed that Escherichia coli adhesiveness was significantly reduced at rufloxacin concentrations of 1/32 MIC, hemagglutination and hydrophobicity were significantly reduced at concentrations of, respectively, 1/4 MIC and 1/8 MIC, and motility was significantly reduced at concentrations of 1/16 MIC; filamentation was still present at concentrations of 1/4 MIC. Phagocytosis was not affected, but killing significantly increased from 1/2 MIC to 1/8 MIC; oxidative bursts measured by means of chemiluminescence were not affected. The fact that sub-MICs are still effective in interfering with the parameters of bacterial virulence is useful information that needs to be correlated with pharmacokinetic data in order to extend our knowledge of the most effective concentrations that can be used to optimize treatment schedules, for example, single administrations, particularly in noncomplicated lower urinary tract infections.  (+info)

Purpose. The aim of the study was to investigate the prevalence of plasmid-mediated quinolone resistance (PMQR) genes in an unselected collection of bloodstream isolates recovered over an 18-month period in a laboratory affiliated to a university hospital in Athens, Greece, and to assess their impact on the in vitro activity of ciprofloxacin and levofloxacin. Methods. Eight PMQR genes were screened by PCR and sequencing. All PMQR-positive isolates were submitted to isoelectric focusing for β-lactamase detection, conjugation or transformation, time-kill assays, mutant prevention concentrationand inoculum effect evaluation. PCR and sequencing of gyrA and parC were performed for detection of chromosomal mutations. Results. Among 96 Gram-negative isolates, 7 (7.3 %) carried one or more PMQR genes. qnrS1 was the most prevalent (5.2 %), followed by aac(6′ )-Ib-cr (4.2 %) and their combination (2 %). Cloning was successful for three isolates. The presence of a single PMQR determinant without any target
Background. Plasmid-mediated quinolone resistance (PMQR) has received considerable attention recently. Data analysis in Jawaharlal Institute of Postgraduate Medical Education & Research (JIPMER) revealed 75% of the Enterobacteriaceae isolates to be ciprofloxacin-resistant in 2012. Few reports regarding the prevalence of PMQR are available from India. Hence, the present study was carried out to ascertain the prevalence of PMQR genes among clinical isolates of ciprofloxacin-resistant Enterobacteriaceae in JIPMER. Methods. The study included 642 ciprofloxacin-resistant clinical Enterobacteriaceae isolates. JIPMER hospitals annual consumption data for fluoroquinolones were retrieved from the Department of Pharmacy. The test isolates were screened for the presence of qnr A, B, D, S and aac(6′)-Ib-cr genes. PMQR-positive isolates alone were tested for the presence of class I (intI1) and class II (intI2) integrons. Randomly selected PCR amplicons were sequenced and analysed using MEGA software. A total of
Profiles of gyrA Mutations and Plasmid-Mediated Quinolone Resistance Genes in Shigella Isolates with Different Levels of Fluoroquinolone Susceptibility
The effects of 7-(4-[4-(2,3-dichlorophenyl)-1-piperazinyl]butyloxy)-3,4-dihydro-2 (1H)- quinolinone (OPC-14597), a derivative of the dopamine (DA) autoreceptor agonist 7-(3-[4-(2,3-dimethylphenyl)piperazinyl]propoxy)-2(1H)-quinolinone (OPC-4392), on DA receptors were biochemically and behaviorally studied and compared with those of OPC-4392. Both OPC-14597 and OPC-4392 inhibited reserpine- and gamma-butyrolactone (GBL)-induced increase in tyrosine hydroxylase activity in the mouse and rat brain. The effects of OPC-14597 were comparable to those of OPC-4392 and were completely antagonized by haloperidol. OPC-14597, unlike apomorphine, did not evoke postsynaptic DA receptor-stimulating behavioral signs such as hyperlocomotion in the reserpinized mice and contralateral rotation in rats with unilateral striatal 6-hydroxydopamine lesions. Both OPC-14597 and OPC-4392 inhibited such apomorphine-induced postsynaptic behavioral changes as stereotypy and hyperlocomotion in mice and rats and rotation in ...
aripiprazole white tablet.aripiprazole.15 mg aripiprazole.what is the ingredients of aripiprazole.aripiprazole buy u k suppliers.aripiprazole for long term usage.aripiprazole virginia doctors.aripiprazole images.aripiprazole can cause suicide.aripiprazole and zopiclone.mix aripiprazole and xanax.aripiprazole dosage for anxiety.ordering aripiprazole without percription.aripiprazole equivalent to 1 mg xanax.aripiprazole stay in system.exercise aripiprazole ...
Close The Infona portal uses cookies, i.e. strings of text saved by a browser on the users device. The portal can access those files and use them to remember the users data, such as their chosen settings (screen view, interface language, etc.), or their login data. By using the Infona portal the user accepts automatic saving and using this information for portal operation purposes. More information on the subject can be found in the Privacy Policy and Terms of Service. By closing this window the user confirms that they have read the information on cookie usage, and they accept the privacy policy and the way cookies are used by the portal. You can change the cookie settings in your browser. ...
TY - JOUR. T1 - Prevalence of quinolone resistance mechanisms and associations to minimum inhibitory concentrations in quinolone-resistant Escherichia coli isolated from humans and swine in Denmark. AU - Cavaco, Lina. AU - Frimodt-Møller, Niels. AU - Hasman, Henrik. AU - Guardabassi, Luca. AU - Nielsen, Lene. AU - Aarestrup, Frank Møller. PY - 2008. Y1 - 2008. N2 - Prevalence of quinolone resistance mechanisms and associations to minimum inhibitory concentrations (MICs) of nalidixic acid (NAL) and ciprofloxacin (CIP) were investigated in 124 Escherichia coli isolated from humans (n = 85) and swine (n = 39) in Denmark. The collection included 59 high-level CIP-resistant isolates (MIC ,= 4) from human (n = 51) and pig origin (n = 8) and 65 low-level CIP-resistant isolates (MIC ,= 0.125) from human (n = 34) and pig origin (n = 31). Resistance by target modification was screened by PCR amplification and sequencing, of the quinolone resistance determining regions (QRDRs) of gyrA, gyrB, parC, and ...
In this study, the prevalence of plasmid-mediated quinolone resistance (PMQR) was investigated in 495 Escherichia coli isolates from diseased food-producing animals in Guangdong province, China. The quinolone resistance-determining regions (QRDRs) of the gyrA and parC genes were analysed for mutations in 55 isolates harbouring only oqxAB and all isolates harbouring other PMQR genes. Overall, 282 (57.0 %) E. coli isolates had at least one PMQR gene. oqxAB was detected in 215 isolates and predominated the PMQR genes, followed by qnrS (63 isolates), aac(6′)-Ib-cr (56 isolates), qnrB (39 isolates) and qepA (18 isolates). qnrA, qnrC and qnrD were not found in any of the isolates. The rates of resistance to ciprofloxacin, enrofloxacin, levofloxacin and nalidixic acid were 75.2, 81.0, 70.5 and 97.4 %, respectively, among the 495 isolates. Eight types of mutation in gyrA were detected in 154 PMQR-positive isolates, and 147 isolates were found to have mutations in parC. PFGE analysis indicated that the PMQR
1-(2-(1H-1,2,3,4-tetrazol-5-yl)ethyl)-5,7-dimethoxy-3-(4-methoxyphenyl)-1,2-dihydro-2-quinolinone: an antimigratory agent; structure in first source
Patients with major depressive disorder who had been nonresponsive to treatment with escitalopram were found to have an improvement in treatment outcomes with adjunctive treatment with aripiprazole, according to research study data from the CAN-BIND Investigator Team.
Aripiprazole is a D2-like receptor (D2R) partial agonist with a favourable clinical profile. Previous investigations indicated that acute and short-term administration of aripiprazole had effects on PKA activity, GSK3β-dependent pathways, GABAA receptors, NMDA receptor and CREB1 in the brain. Since antipsychotics are used chronically in clinics, the present study investigated the long-term effects of chronic oral aripiprazole treatment on these cellular signalling pathways, in comparison with haloperidol (a D2R antagonist) and bifeprunox (a potent D2R partial agonist). We found that the Akt-GSK3β pathway was activated by aripiprazole and bifeprunox in the prefrontal cortex; NMDA NR2A levels were reduced by aripiprazole and haloperidol. In the nucleus accumbens, all three drugs increased Akt-GSK3β signalling; in addition, both aripiprazole and haloperidol, but not bifeprunox, increased the expression of Dvl-3, β-catenin and GABAA receptors, NMDA receptor subunits, as well as CREB1 phosphorylation
Quinolone resistance is usually caused by various chromosomal mutations that alter the target enzymes, such as DNA gyrase and topoisomerase IV, or activate efflux systems (2). Plasmid-mediated quinolone resistance has only recently been discovered (5). The plasmid gene responsible for quinolone resistance, termed qnr, is carried on class 1 integrons of the In4 family, downstream of the conserved region containing the orf513 recombinase gene (4, 10, 12), and encodes a 218-amino-acid protein that belongs to the pentapeptide-repeat family of proteins (10). The presence of qnr increases the resistance to nalidixic acid and fluoroquinolones by four- to eightfold (5).. The presence of the qnr gene in clinical isolates from Korea has not yet been reported. Therefore, in this study we screened for the presence of the qnr gene in clinical isolates of Escherichia coli from patients in Korea and analyzed the transferability and the genetic context of the qnr gene.. The presence of the qnr gene was screened ...
The aim of the study was to analyse the influence of enrofloxacin and pradofloxacin administered orally for 14 days on the ECG in dogs. The ECG was performed before and after a 14 day period of quinolone administration. There was an increase in the QTc and the TpTe interval in the group treated with quinolones. QTc was prolonged by 24 ms (p=0.001). The TpTe interval was shortened, on average, by 6.55 ms (p=0.048). In the group treated with enrofloxacin, QTc was prolonged by 16.27 ms (p=0.006) and the TpTe interval was shortened by 9.64 ms (p=0.050), the TpTe/QT index was reduced by 0.034 (p=0.050) on average. In dogs treated with pradofloxacin, QTc was prolonged by 21.55 ms (p=0.012) on average. The results suggest that a prolonged administration of quinolones can increase the risk of arrhythmias. Furthermore, different generations of these drugs increase this risk to various degrees. The study proved that second generation quinolones, such as enrofloxacin, significantly change the phase of
PubMed comprises more than 30 million citations for biomedical literature from MEDLINE, life science journals, and online books. Citations may include links to full-text content from PubMed Central and publisher web sites.
Previously, aripiprazole has been shown to be a partial agonist at the D2 dopamine receptor[4].The stabilizing effect of aripiprazole on the dopamine system was attributed to its targeting of presynaptic (auto-receptors) and post-synaptic D2 receptors[3]. Therefore, it is effective to positive symptoms, negative symptoms as well as symptoms of cognitive impairments. In addition, aripiprazole is classified as a medication with significant 5HT2A-antagonism, and with still other additional secondary binding characteristics such as 5-HT2C, 5-HT7, epinephrine α1 and histamine H1 receptors. Its unique mechanism of action makes aripiprazole as a favorable clinical treatment choice over others, i.e. high efficacy, fewer extrapyramidal reactions (EPS), does not cause weight gain, does not cause the incensement of prolactin (PRL)[3, 12-13]. Consistently, our results showed that the overall response rate of aripiprazole treatment was 70.4 %, which was similar to that reported by Beijing Anding ...
Lomefloxacin, a difluorinated quinolone derivative, is a bacterial gyrase inhibitor, effective against gram positive and gram negative bacteria. The acute toxicity of Lomefloxacin following systemic and topical ophthalmic application is low. Lomefloxacin interferes with bacterial DNA related processes like initiation, elongation, and termination phases of replication, transcription, DNA repairing, recombination, transposition, supercoiling and relaxation of DNA. The target molecule for quinolones is the A-subunit of bacterial enzyme gyrase (topoisomerase II). The forming of a stable complex between the quinolone and the whole gyrase teramer A2B2 leads to impaired enzyme functions, resulting in a rapid killing of sensitive bacteria.. Cross-resistance has only been reported with other quinolones, but not with any other group of antibiotics. No clinical studies are available about the efficacy in cases of infections with chlamydia.. ...
Before you buy medication levaquin 650 mg quinolone antibiotic, compare the best prices on tabs levaquin 650 mg quinolone antibiotic from licensed, top-rated pharmacies in the U.S., Canada, and internationally.
Aripiprazole, a quinolinone derivative, is an atypical antipsychotic drug indicated for the treatment of adult patients with schizophrenia. Aripiprazole 10 or 15mg once daily is effective and well tol
Sandoo Pharmaceutical is dedicated to producing 3 4-Dihydro-7-hydroxy-2(1H)-quinolinone, find compete details about 3 4-Dihydro-7-hydroxy-2(1H)-quinolinone from Sandoo Pharmaceutical.
Resistance to quinolones can develop rapidly, even during a course of treatment. Numerous pathogens, including Staphylococcus aureus, enterococci, and Streptococcus pyogenes now exhibit resistance worldwide.[3] Widespread veterinary usage of quinolones, in particular in Europe, has been implicated. There are three known mechanisms of resistance.[4] Efflux pumps can be used to decrease intracellular drug concentration. In gram-negative bacteria, plasmid-mediated resistance genes produce proteins that can bind to DNA gyrase, protecting it from the action of quinolones. Finally, mutations at key sites in DNA gyrase or topoisomerase IV can decrease their binding affinity to quinolones, decreasing the drug effectiveness. ...
Results Oral treatment with laquinimod (especially 0.5 mg/kg bw) not only improved motor impairment but also weight course and extended survival in R6/2 mice. R6/2 mice that were treated with 0.5 mg laquinimod showed longer life spans, as determined by Kaplan Meier analysis (p-value = 0.1). Upon analysis of motor performance, latency-to-fall values during rotarod testing in R6/2 mice were significantly different at the age of 12 weeks in the 0.5 and 25 mg/kg bw treated group (p*,0.05).. In the histological analysis, laquinimod treatment resulted in preservation of morphologically intact neurons in the motor cortex and striatum as revealed by neuronal marker NeuN and medium spiny neurons (MSNs) marker DARPP-32. Biochemical analysis also showed significant increase in brain derived neurotrophic factor (BDNF) level in the cortical (*p , 0.05) but not in striatal neurons. These effects seem to be mainly based on BDNF-pathways, influence on oxidative stress, and possibly reduction of ...
Patients who had no history of tolerability to oral aripiprazole received 10-15 mg/day (up to 30 mg/day) oral aripiprazole for 1 to 4 weeks to determine tolerability in the Tolerability Assessment Phase prior to receiving treatment with aripiprazole IM Depot. In the Open-label Aripiprazole IM Depot Phase, participants received aripiprazole intramuscular (IM) Depot 400 mg injection (dosage could be adjusted to 300 mg at the investigators discretion) monthly in the clinic for a total of 6 injections + concomitant oral aripiprazole 10-15 mg/day for the first 14 days. Participants at the investigators discretion were eligible to continue to receive aripiprazole IM depot (400 or 300 mg) injection monthly in the Open-label Aripiprazole IM Depot Extension phase. Oral aripiprazole was available as rescue medication if necessary ...
Pentapeptide repeats are a class of proteins characterized by the presence of multiple repeating sequences five amino acids in length. The sequences fold into a right-handed β-helix with a roughly squ
Antibiotics are considered one of the most crucial medical therapies available, and whether they are given for a simple urinary tract infection or for a serious disease, such as bacterial meningitis, the fact is that these medications have the capacity to eradicate a multitude of illnesses. Among the different antibiotic classes, the quinolone group (e.g. ciprofloxacin and levofloxacin) has risen as one of the most popular antibiotics, given that this class possesses remarkable versatility. They can easily wipe out pneumonia as well as obliterate harmful bacteria such as those that cause anthrax. Not surprisingly, following from their ample utility value, in 2010 the quinolones became the 5th most commonly prescribed antibiotic type within the U.S. However, this popularity and increase in antibiotic use contributed to our current issue with quinolone antibiotic resistance. In addition to this, the quinolones are known to be associated with an array of serious adverse effects, and patients taking ...
PRIMARY OBJECTIVES:. I. To define the maximum tolerated dose (MTD) of R115777 (tipifarnib) in patients with relapsed, refractory, or high risk myeloid leukemias treated according to this regimen.. II. To assess the toxicity and preliminary assessment of efficacy of R115777 in patients with relapsed, refractory, or high risk myeloid leukemias.. OUTLINE: This is a dose-escalation, multicenter study.. Patients receive oral tipifarnib twice daily on days 1-7 and 15-21. Courses repeat every 28 days in the absence of unacceptable toxicity or disease progression. Patients achieving a complete response (CR) receive 2 additional courses beyond CR. Patients experiencing relapse after previously achieving CR may receive additional tipifarnib at the current dose level for newly registered patients.. Cohorts of 3-6 patients receive escalating doses of tipifarnib until the MTD is determined. The MTD is defined as the dose preceding that at which 2 of 3 or 2 of 6 patients experience dose-limiting ...
New restrictions and precautions for use have been implemented for quinolone antibiotics following very rare reports of disabling, long-lasting or potentially irreversible adverse reactions affecting the musculoskeletal and nervous systems.
Aripiprazole Oral Solution (Aripiprazole Oral Solution) may treat, side effects, dosage, drug interactions, warnings, patient labeling, reviews, and related medications including drug comparison and health resources.
A comprehensive guide to side effects including common and rare side effects when taking Aripiprazole Oral Solution (Aripiprazole Oral Solution) includes uses, warnings, and drug interactions.
Aripiprazole is a second generation anti psychotic agent. Aripiprazole is an atypical anti psychotic agent. Aripiprazole is given via oral route.
We carried out an sRNA screen to identify genes whose knockdown restores quinolone sensitivity in E. coli. Following an initial screen of ∼5000 sRNA-bearing clones, and secondary screening of over 500 clones, we found 30 genes whose disruption increases sensitivity of a gyrA S83L mutant by twofold or more. Our findings expand knowledge of the genetic interaction network of the essential gene gyrA, and provide potential targets for the development of antibiotic adjuvants to restore sensitivity in quinolone resistant pathogens.. Chemical-genetic sensitivity screens have largely used knockout approaches, whereby a library of knockout mutants is screened for sensitivity or resistance to an antibiotic at sub-lethal concentrations (e.g., Tamae et al. 2008; Breidenstein et al. 2008; Fajardo et al. 2008; Gomez and Neyfakh 2006; Liu et al. 2010). Typically, such screens are carried out on a wild-type, antibiotic susceptible background, so they are not well-suited to identifying genes whose knockdown ...
Overview of Quinolones, General information, Mechanism of action, Pharmacokinetics, Classification, Therapeutic use, Adverse effects
Get Quinolones at Spectrum Chemical. SpectrumChemical.com carries a full line of fine chemicals, lab appliances and lab supplies. Spectrum Chemical offers fine chemicals in lab and production sizes.
Spectrophotometric Determination of Quinolones by Charge Transfer Complexation with Chloranilic Acid: Synthesis and Characterization Abstract.
Get Information of Aripiprazole Intermediates Manufacturers, Suppliers, Dealers, Exporters, Traders, Producers, Wholesalers, Aripiprazole Intermediates Companies in Nasik, India
Find the best coupon for Aripiprazole and Save up to 80% off Aripiprazole prices at the pharmacy. You can also find manufacturer offers and receive a pharmacy savings card instantly.
Cost medicamento purchase cheap aripiprazole europe aripiprazole how to order shopping generic aripiprazole purchase shop europe aripiprazole buy now payment australia Aripiprazole - Best Drugstore Ch
This trial was about to investigate the tolerability and efficacy of flexible dose oral aripiprazole (OPC-14597) as maintenance treatment in adolescent patients
Hi Pat, I was told that it takes the counts longer to come up every time you have chomo and that after the first time the platelets are the most effected. I had Induction and then 30 days later a second round follow up round of 2 of the three drugsI had for induction. I too went into remission with the first round but so far I have not relapsed. It took my counts over 30 days to come back the second time. Then they put me on a Zarnestra trial for a year hoping to increase my chances of staying in remission. I am a little younger then your Mom-Im 63 & had no other medical problems. If you Mother is in remission again, you might check on the zarnestra trial going now in many places that is open to patients in a second remission but I do think they will want her counts up to a certain level. Barbras husband Ron is on that one. It is listed on the government list and is being run by Encologists instead of Hemos. I have had almost no side effect since they got the right dosage level for me. ...
The APP Rapid Test is a rapid chromatographic immunoassay for the qualitative detection ofDehydroaripiprazole (primary metabolite of Aripiprazole) in human urine at a cut-off concentration of 5000 ng/mL.
Aripiprazole is an injected drug available only from a licensed physician that is used primarily to treat agitation experienced by patients
MCE (MedChemExpress) 提供 Aripiprazole 相关产品,包含各种抑制剂、激动剂和化合物库,专注于信号通路和疾病研究领域,致力于为生命科学研究提供高质量的试剂类产品和服务。
Buy Microxin Online! Microxin medication belongs to a class of drugs called quinolone antibiotics. Microxin works by stopping the growth of bacteria. Microxin is used to treat a variety of bacterial infections.
Buy Noprose Online! Noprose medication belongs to a class of drugs called quinolone antibiotics. Noprose should not be used for colds, flu, other virus infections, sore throats or other minor infections, or to prevent infections. Noprose works by stopping the growth of bacteria.
Buy Noroxin Online! Generic Noroxin medication belongs to a class of drugs called quinolone antibiotics. Generic Noroxin is used to treat a variety of bacterial infections. Generic Noroxin works by stopping the growth of bacteria.
Purchase Aripiprazole Medications! Order Cheap Abilify Over The Counter!Approved Pharmacy Catalog - Abilify - Aripiprazole - 10 mg Best Online shop for ... How to Purchase Low Price Abilify 10 mg 2018 ,天堂Z
An antibiotic of the quinolone family, Bayer HealthCares Baytril (enrofloxacin) fights a broad range of bacterial and fungal infections in dogs and cats.
Pill with imprint TV 7569 is Blue, Capsule-shape and has been identified as Aripiprazole 5 mg. It is supplied by Teva Pharmaceuticals USA Inc.
Palmatine Is a Plasmid-Mediated Quinolone Resistance (PMQR) Inhibitor That Restores the Activity of Ciprofloxacin Against QnrS and AAC(6ʹ)-Ib-cr-Producing Escherichia coli Peng Wang,1 Longfei Hu,1 Zhihui Hao2 1Agricultural Bio-Pharmaceutical Laboratory, Qingdao Agricultural University, Qingdao 266109, Peoples Republic of China; 2National Centre for Veterinary Drug Safety Evaluation, College of Veterinary Medicine, China Agricultural University, Beijing 100089, Peoples Republic of ChinaCorrespondence: Zhihui HaoNational Centre for Veterinary Drug Safety Evaluation, College of Veterinary Medicine, China Agricultural University, Beijing 100089, Peoples Republic of ChinaEmail [email protected]: The emergence of plasmid-mediated quinolone resistance (PMQR) is a global challenge in the treatment of clinical disease in both humans and animals and is exacerbated by the presence of different PMQR genes existing in the same bacterial strain. Here, we discovered that a natural isoquinoline alkaloid
Looking for online definition of quinolones in the Medical Dictionary? quinolones explanation free. What is quinolones? Meaning of quinolones medical term. What does quinolones mean?
Quinolone antibacterial drugs,Prulifloxacin,123447-62-1,US $ 100 - 1,000 / Kilogram, 123447-62-1, Prulifloxacin, C21H20FN3O6S.Source from Baoji Guokang Bio-Technology Co., Ltd. on Alibaba.com.
Quino-what?. We hear that a lot.. Before we explain what it is and why we are committed to helping victims, lets start with how it is pronounced.. Quinolone: kwĭnə-lōn. Fluoroquinolone: flu̇r-ō-ˈkwi-nə-ˌlōn\ History and difference between quinolones and fluoroquinolones.. The words quinolone and fluoroquinolone are often interchanged but there is a difference between the two. Both are terms for a class of antibiotics based on Nalidixic acid.. Nalidixic acid is the first of the synthetic quinolone antibiotics. It was discovered in 1962 by George Lesher and used clinically in 1967. Originally, in smaller doses Nalidixic acid inhibited growth and replication of bacteria; in higher doses it killed bacteria.. The addition of a fluorine atom is what differentiates quinolones from fluoroquinolones. Fluorine is an element; F2 on the Periodic Table. It is a toxic gas and is considered one of the most reactive elements. The addition of the fluorine atom and a piperazine ring make ...
This page displays a blog entry. Lomefloxacin Pharmacie Acheter - Ou Acheter Du Maxaquin A Lyon Quel Site Pour Acheter Du Lomefloxacin Lomefloxacin Commander Luxembourg, Achat Vrai Lomefloxacin 400, Acheter Du Lomefloxacin 400 Pharmacie En Ligne ACHETER Lomefloxacin (Maxaquin) EN LIGNE...
Quinolones are potent synthetic antimicrobials first developed in the 1960s. Since then several agents have been synthetised by modification of basic bicyclic chemical structure. Quinolones and fluoroquinolones are classified based on their chemical structure, antibacterial spectrum and pharmacokinetic features. Each agent inhibits bacterial DNA synthesis by forming a ternary complex with a DNA molecule and gyrase and topoisomerase IV enzymes, thus blocking bacterial DNA supercoiling [1-3].. The first quinolone agents were nalidixic acid, cinoxacin and oxolinic acid, each had basic bicyclic quinolone ring. These agents achieved 20-40 mg/L peak serum concentrations (Cmax) after a treatment with doses of 500-1000 mg. These agents and their metabolites were excreted by kidney and they reached 500-1000 mg/L peak urine concentrations 2-4 h following adminstration. The narrow-spectrum activity of these quinolones limited their use in clinical practice [4, 5].. Substituents on certain part of quinolone ...
In this report, we evaluated oral laquinimod in 2 EAE models that require B-T cell cooperation. Laquinimod treatment of rMOG-induced EAE interfered with development of Tfh, B cell activation, secretion of MOG-specific antibodies, and EAE. Similarly, laquinimod treatment of spontaneous EAE reduced expansion of Tfh cells but also prevented accumulation of meningeal B cell aggregates, lymphoid structures that have been observed in tissues of patients with progressive MS, and impeded disability progression when treatment was initiated after mice developed paralysis. Collectively, these findings may be relevant to the potential application of laquinimod to treatment of patients with progressive MS. Furthermore, our observation that laquinimod inhibits MOG-induced antibodies suggests that laquinimod could interfere with formation of pathogenic antigen-specific antibodies in humoral autoimmune diseases, including neuromyelitis optica.33. CD4+ DCs have a key role in the development of Tfh cells and ...
Escherichia coli is an important bacterial species based on incidence and associated infection severity. Some E. coli strains produce extended-spectrum beta lactamase (ESBL) and are called ESBL-producing E. coli. These strains are resistant to most classes of cephalosporin and a number of other classes of antibiotics. Plasmids carrying qnr genes have been found to transmit quinolone resistance.The aim of this study was to determine the frequency of qnr genes in ESBL-producing and non-ESBL-producing E. coli isolated from outpatient and hospitalized patient clinical specimens from Imam Reza hospital in Mashhad, Iran.Two hundred E. coli strains, isolated from different clinical specimens were used. ESBL-producing E. coli were detected by determining susceptibility to ceftazidime, cefotaxime, and cefpodoxime with the phenotypic confirmatory test (PCT). PCR analysis was employed to detect the qnrA, qnrB, qnrS, blaTEM, and blaSHV genes.Eighty-six (43%) isolates were ciprofloxacin-resistant. The PCT identified
Mono- and Stereopictres of 5.0 Angstrom coordination sphere of Arsenic atom in PDB 2o6w: Crystal Structure of A Pentapeptide Repeat Protein (RFR23) From the Cyanobacterium Cyanothece 51142
Objective: To assess the impact of adjunctive aripiprazole versus adjunctive placebo treatment on suicidality in patients with major depressive disorder.. Method: Data were pooled from 2 identical aripiprazole augmentation studies. Patients with DSM-IV-TR-diagnosed major depressive disorder with an inadequate response to 8 weeks of prospective antidepressant treatment were randomly assigned to adjunctive placebo or adjunctive aripiprazole (2-20 mg/d) treatment for 6 weeks. Adverse events related to suicidality were identified in the adverse event database using the Medical Dictionary for Regulatory Activities-preferred term. Treatment-emergent suicidal ideation was defined using item 10 (suicidality) of the Montgomery-Åsberg Depression Rating Scale (MADRS) and item 18 (suicidality) of the Inventory of Depressive Symptomatology (IDS).. Results: In total, 737 patients were included in the safety database (aripiprazole n = 371; placebo n = 366). No suicides were reported. There were no ...
PubMed comprises more than 30 million citations for biomedical literature from MEDLINE, life science journals, and online books. Citations may include links to full-text content from PubMed Central and publisher web sites.
We look forward to submitting these data to the EMA in support of a potential indication expansion of the EU label following initial approval. About the 445-104 Study The data announced today are from a global Phase 3, randomized, double-blind, parallel-group study to evaluate the efficacy and safety of TRIKAFTA in people with CF ages 12 years and older who have one copy of the F508del mutation and one gating mutation (F/G), or one copy of the F508del mutation and one residual function mutation (F/RF). All participants had a 4-week run-in period of either ivacaftor or tezacaftor/ivacaftor. Following the run-in, patients were randomized to receive TRIKAFTA or to remain on their prior regimen of ivacaftor or tezacaftor/ivacaftor for 8 weeks. Baseline was measured at the end of the run-in period, prior to the start of the 8-week treatment period. A total of 132 participants received TRIKAFTA and 126 patients were in the control group that received either ivacaftor or tezacaftor/ivacaftor. The ...
This paper proposes a microbiological method in microtitre plates for the detection of residues of quinolones in milk. The method uses spores of Bacillus licheniformis in culture medium with a redox combination of indicators and gives a response time of 5.5 h. This method detects 92 μg L−1 of ciprofloxacin, 63 μg L−1 of danofloxacin, 109 μg L−1 of enrofloxacin, 101 μg L−1 of marbofloxacin and 109 μg L−1 of sarafloxacin in milk. Therefore, the assay is easy to develop and to use in laboratory, allowing analysis of large numbers of samples at low cost. Due to its good sensitivity to quinolones, this assay can be used as a complementary test of commercial microbiological methods and thereby improve food security ...
Intracellular receptors (IRs) form a class of structurally-related genetic regulators scientists have named ligand dependent transcription factors. R.M. Evans, Science, 240:889 (1988). Steroid receptors are a recognized subset of the IRs, including the progesterone receptor (PR) androgen receptor (AR), estrogen receptor (ER), glucocorticoid receptor (GR) and mineralocorticoid receptor (MR). Regulation of a gene by such factors requires both the IR itself and a corresponding ligand, which has the ability to selectively bind to the IR in a way that affects gene transcription ...
Close The Infona portal uses cookies, i.e. strings of text saved by a browser on the users device. The portal can access those files and use them to remember the users data, such as their chosen settings (screen view, interface language, etc.), or their login data. By using the Infona portal the user accepts automatic saving and using this information for portal operation purposes. More information on the subject can be found in the Privacy Policy and Terms of Service. By closing this window the user confirms that they have read the information on cookie usage, and they accept the privacy policy and the way cookies are used by the portal. You can change the cookie settings in your browser. ...
Buy Aripiprazole Online! Aripiprazole is an atypical antipsychotic drug which belongs to the benzisoxazole derivatives. Aripiprazole is available in many salts and polymorphs forms.
A recombinant plasmid containing gyr A encoding wild-type Escherichia coli quinolone susceptible DNA gyrase A subunits has been used as a broad host range gene probe. Strains expressing gyr A-mediated quinolone resistance become susceptible to quinolones upon insertion of the plasmid, whereas the plasmid without gyrA (pLA2917, vector) has no effect. Fifteen highly ciprofloxacin-resistant E. coli and three Klebsiella pneumoniae (MICs 2-64 mg/L) were isolated from clinical specimens in the Hospital de la Princesa, Madrid, Spain. Plasmid pNJR3-2 and pLA2917 were introduced into the clinical isolates by conjugation, and transconjugants selected with tetracycline or kanamycin (for which the plasmids encode resistance). Ten transconjugants from each mating, the original isolates, the gene probe and vector control were screened for susceptibility to nalidixic acid, ciprofloxacin, ofloxacin, norfloxacin, tetracycline, chloramphenicol, cefoxitin and trimethoprim. Lower MICs of quinolones were seen for ...
Supplementary MaterialsSupplemental Data 1. mobile machinery Bmp6 necessary for proteins folding, disulfide relationship development, glycosylation, and quality control takes on an essential part in planning precursors for transit with the secretory pathway. The production of product peptides requires the participation of multiple proteases frequently. Amidation from the COOH-terminus of the peptide, that is frequently needed for biological activity, requires the participation of peptidylglycine bond in glycine, producing amidated peptide plus glyoxylate. When expressed individually, both catalytic domains of buy Zarnestra PAM are active, and each is efficiently stored in secretory granules. Although this finding suggests that PHM and PAL activities do not need to be encoded by the same gene, species ranging from human to suggests that this enzyme has an ancient role in detecting and responding to environmental stimuli. PAM requires molecular oxygen along with ascorbate, copper, and zinc, and ...
A 52-week, haloperidol-controlled, long-term, maintenance trial (n=1294) was conducted in patients with acute relapse of chronic schizophrenia. In this trial involving the administration of aripiprazole 30 mg/day and haloperidol 10 mg/day, with a one-time option to decrease aripiprazole to 20 mg/day and haloperidol to 7 mg/day, aripiprazole was at least comparable to haloperidol in time-to-failure to maintain response in responders. Based on patients who responded at any time during the 52-week study (610/853, 72% in the aripiprazole group and 298/430, 69% in the haloperidol group), there was a 12% lower risk of subsequent failure with aripiprazole relative to haloperidol (relative risk: 0.881, 95% CI: 0.645 - 1.204). Aripiprazole was comparable to haloperidol in time-to-failure to maintain response in all randomized patients. Patients in the aripiprazole group had a 14% lower risk of failure compared with the haloperidol group (relative risk: 0.858, 95% CI: 0.721, 1.021). Aripiprazole was ...
Important warning for older adults with dementia:. Studies have shown that older adults with dementia (a brain disorder that affects the ability to remember, think clearly, communicate, and perform daily activities and that may cause changes in mood and personality) who take antipsychotics (medications for mental illness) such as aripiprazole have an increased chance of death during treatment. Older adults with dementia may also have a greater chance of having a stroke or ministroke or other severe side effects during treatment.. Aripiprazole is not approved by the Food and Drug Administration (FDA) for the treatment of behavior problems in older adults with dementia. Talk to the doctor who prescribed this medication if you, a family member, or someone you care for has dementia and is taking aripiprazole. For more information visit the FDA website: Web Site. Important warning for people who have depression:. A small number of children, teenagers, and young adults (up to 24 years of age) who took ...
The FDA is requiring a warning that quinolone antibiotics can cause inflamed or ruptured tendons...... Learn more with Pharmacists Letter.
Niksan Pharmaceutical - Supplier and Exporter of Aripiprazole Tablet 5 Mg from Ankleshwar,Gujarat,India. Get best quality Aripiprazole Tablet 5 Mg at market leading price.
Our case had hiccups arising in an adolescent with the attention deficit and hyperactivity disorder (ADHD) and conduct disorder (CD) after adding aripiprazole treatment to extended-release methylphenidate. Actually ...
Aripiprazole is a psychotropic drug that is available as ABILIFY® (aripiprazole) Tablets, ABILIFY DISCMELT® (aripiprazole) Orally Disintegrating Tablets, ABILIFY® (aripiprazole) Oral Solution, and ABILIFY® (aripiprazole) Injection, a solution for intramuscular injection. Aripiprazole is 7-[4-[4-(2,3dichlorophenyl)-1-piperazinyl]butoxy]-3,4-dihydrocarbostyril. The empirical formula is C23H27Cl2N3O2 and its molecular weight is 448.38. The chemical structure is: ABILIFY® (aripiprazole) Structural Formula Illustration ABILIFY… Read More ». ...
A family of dihydroquinolinones that inhibited the proliferation of a number of cancer cell lines and targeted the oncogenic activities of the late simian virus 40 factor (LSF) was discovered. The lead quinolinone inhibitors, 8-(2-propoxyphenyl)-7,8-dihydro-[1,3]dioxolo[4,5-g]quinolin-6(5H)-one, FQI1, and 8-(2-propoxyphenyl)-[1,3]dioxolo[4,5-g]quinolin-6(5H)-one, FQI2, were determined by a comprehensive SAR study. The lead compounds had low micromolar to nanomolar Gi50S and IC50S (concentrations that induced 50% inhibition) in cell growth and LSF-directed luciferase reporter assays, respectively. A distinct correlation between the GI50 and IC50 values indicated antiproliferative effects resulted from inhibition of LSF activity. FQI1 had no growth effects on immortalized human hepatocytes or primary mouse hepatocytes. Overall, FQI1 proved a good drug candidate for hepatocellular carcinoma (HCC). It possessed a low molecular weight and moderate solubility, which was improved by substitution of the ...
Aripiprazole. Grady, Michelle A.; Gasperoni, Timothy L.; Kirkpatrick, Peter // Nature Reviews Drug Discovery;Jun2003, Vol. 2 Issue 6, p427 Focuses on the use of aripiprazole drugs in the treatment of schizophrenia. Properties of aripiprazole; Functionality of the drug; Impact of application of aripiprazole on schizophrenics; Definition of schizophrenia; Symptoms of the disease; Drugs previously used for the treatment of schizophrenia. ...
This study investigated the effects of aripiprazole on cognitive function in patients with schizophrenia or schizoaffective disorder and matched volunteers.
GONZALEZ M, Claudio et al. Safety of fluoroquinolones: risks usually forgotten for the clinician. Rev. chil. infectol. [online]. 2017, vol.34, n.6, pp.577-582. ISSN 0716-1018. http://dx.doi.org/10.4067/S0716-10182017000600577.. Quinolones are a group of widely used antimicrobials. Although they are considered safe for patients, knowledge of the safety profile is necessary so that professionals become aware of what is necessary to monitor. At the musculoskeletal level, quinolones have the potential to damage cartilage, causing even tendon rupture in infrequent cases. Hypoglycemia / hyperglycemia has been observed at the endocrine level, thus, careful monitoring of glycemia in patients with quinolone is recommended in diabetic patients. At the cardiovascular level, arrhythmias induced by these antimicrobials are rare but severe. At the level of the nervous system, the appearance of alterations of the central nervous system and the peripheral neuropathy are emphasized. When assessing the safety of ...
A babys body and most internal organs are formed during the first 12 weeks of pregnancy. It is mainly during this time that some medicines are known to cause birth defects. Four well-designed studies all found that birth defects were no more common in babies born to pregnant women who took a quinolone antibiotic in early pregnancy than in babies of women not taking quinolones. One study that investigated whether use of a quinolone antibiotic in early pregnancy may increase the likelihood of specific types of heart defects found possible links with two types: conotruncal defects and tetralogy of Fallot. Because these study findings were based on small numbers of babies exposed in the womb they require confirmation with further research.. All of the four studies of women specifically using ciprofloxacin, and eight of nine studies of women using norfloxacin, found no increased occurrence of birth defects in their babies. Single studies specifically investigating levofloxacin, moxifloxacin, ...
Aripiprazole is an eff ective and well-tolerated treatment for ADHD and CD symptoms; however, additional studies (specifically, placebo-controlled and double-blind studies) are needed to better defi ne the clinical use of aripiprazole in children and adolescents with ADHD-CD.
Aripiprazole can also the lower the threshold for trouble sleeping in certain circumstances. I like do nt know if youre still calculated using or intuition not, but adding prescription medicine to your opioid dosage will only increase in unusually pale clear skin. The principles recommended elapsed time between trees a dose of Metformin and a dose of dangerous substance depends on whic
8-(TRIFLUOROMETHYL)QUINOLIN-4-OL chemical properties, What are the chemical properties of 8-(TRIFLUOROMETHYL)QUINOLIN-4-OL 23779-96-6, What are the physical properties of 8-(TRIFLUOROMETHYL)QUINOLIN-4-OL ect.
Provide fine chemicals, building blocks and pharmaceutical intermediates. PI-10488 Cilostazol (73963-72-1) Synonym: 6-[4-(1-Cyclohexyl-1H-tetrazol-5-yl)-butoxy]-3,4-dihydro-2(1H)-quinolinone Molecular Formula: C20H27N5O2 Weight: 369.46 CAS No: 73963-72-1 Appearance: white to off white crystalline powder Purity:99.0% FM Point:158-162 deg C Order online from laboratory chemical supplier and distributor.
Wholesale various high quality Enrofloxacin Injection, Enrofloxacin Oral Solution, Enrofloxacin Injection For Animal, Enrofloxacin Oral Solution For Animal from China. We rest assured that you will find your favorite.
Medscape - COPD dosing for Arcapta Neohaler (indacaterol inhaled), frequency-based adverse effects, comprehensive interactions, contraindications, pregnancy & lactation schedules, and cost information.
Indacaterol helps people with asthama or COPD to breathe more easily, relaxing the muscles surrounding the airways so that air can pass through more easily.
Teva Pharmaceutical and Active Biotech announced results from their Phase 3 ALLEGRO study of laquinimod for the treatment of relapsing forms of multiple sclerosis (MS).
Looking for 10 enrofloxacin? Here you can find the lowest price products about 10 enrofloxacin. We Provide for you about 10 enrofloxacin page2
Quinolones are one the most commonly prescribed classes of antibacterials in the world and are used to treat a broad variety of Gram-negative and Gram-positive bacterial infections in humans.
A Moderate Drug Interaction exists between aripiprazole and brexpiprazole. View detailed information regarding this drug interaction.
Thiyagarajan S, Sivaraman P. Aripiprazole dose for schizophrenia. Cochrane Database of Systematic Reviews 2012, Issue 4. Art. No.: CD009800. DOI: 10.1002/14651858. ...
Reactions of the gastrointestinal tract, the CNS and the skin are the most often observed adverse effects during therapy with fluoroquinolones. At least for some of the newer fluoroquinolones a steep...
Aripiprazole is one of the top selling drugs an atipsychotic medication marketed as Abilify used in the treatment of Psychosis and depression.
My Switch Shop Varilight V-Dim Series 3 Gang 40-250 Watt Dimmer [HDQ43S] - Varilight V-Dim Series 3 Gang, for either 1 or 2 Way circuits, 3x40-250 Watt Push on/Push off Leading Edge Dimmer Switch, on a Double Plate, is ideal for dimming incandescent lighting including mains and low voltage................................................... VARILIGHT Dimmer Switches have an industry-wide reputation for exceptional performance, long life and innovation
Endogenousmatrix interference using a similar m/z value is usually problematic. Many factors ought to be examined before an Tipifarnib method can be reliably applied to test analysis, especiallymultiple analytes with similar structures andmasses dont createa cross-talk phenomenon. Metabolites with a very close m/zvalue to that in the analyzed parent drug is usually problematicin SRM acquisition that will possibly be resolved just by highresolutionaccurate mass (HR) acquisition. Moreover, the selective nature of SRM acquisition can maskvaluable information including co-eluting matrix ions, degradationproducts or adducts with the analytes of interest.. It can have asignificant impact with assay quality and robustness when runninglarge number of various samples in some sort of routine manner. The mainadvantages ofHRover SRMacquisition in quantitative-qualitative(Quan-Qual) analyses have already been described. In add-on, the SRM-based approach is cumbersome not fast enoughto perform quantitation ...
Hurley KA, Santos TMA, Fensterwald MR, Rajendran M, Moore JT, Balmond EI, Blahnik BJ, Faulkner KC, Foss MH, Heinrich VA, et al. Targeting quinolone- and aminocoumarin-resistant bacteria with new gyramide analogs that inhibit DNA gyrase. Med. Chem. Commun. 2017 ;8:942-951. ...
Andriole, VT The Quinolones. Academic Press, 1989. *^ Andersson MI, MacGowan AP (2003). "Development of the quinolones". ... Although not formally a quinolone, nalidixic acid is considered the first quinolone drug. It was introduced in 1962 for ... A quinolone antibiotic is a member of a large group of broad-spectrum bactericides that share a bicyclic core structure related ... Quinolones are contraindicated if a patient has epilepsy, Ehlers-Danlos Syndrome,[41] QT prolongation, pre-existing CNS lesions ...
Andriole, VT The Quinolones. Academic Press, 1989. *^ Andersson MI, MacGowan AP (2003). "Development of the quinolones". ... Quinolone antibiotic at Curlie (based on DMOZ). *Healthcare-associated Infections (HAIs)- Quinolones and the Clinical ... Norris, S; Mandell, GL (1988). "The quinolones: history and overview". The quinolones: history and overview. San Diego: ... Although not formally a quinolone, nalidixic acid is considered the first quinolone drug. It was introduced in 1962 for ...
Committee on Safety of Medicines; Medicines and Healthcare products Regulatory Agency (2008). "Quinolones". United Kingdom: ...
... like other quinolones and fluoroquinolones, are bactericidal drugs, actively killing bacteria. Quinolones inhibit the bacterial ... Quinolones can enter cells easily and therefore are often used to treat intracellular pathogens such as Legionella pneumophila ... Quinolones Psaty, BM. (Dec 2008). "Clinical trial design and selected drug safety issues for antibiotics used to treat ...
Allergy to quinolones Eight cases of quinolone allergy F. F. Arboit 1, JC Bessot 2, F. Arboit 1, JC Bessot 2, F. De Blay 2, A. ... Although quinolones are highly toxic to mammalian cells in culture, its mechanism of cytotoxic action is not known. Quinolone ... Flumequine is the first quinolone compound with a fluorine atom at the C6-position of the related quinolone basic molecular ... Significant and harmful residues of quinolones have been found in animals treated with quinolones and later slaughtered and ...
It is usually resistant to a variety of antibiotics including penicillins, ; cephalosporins, quinolones, and aminoglycosides. ...
... is a quinolone antibiotic useful for the treatment of a number of bacterial infections. When taken by mouth or ... quinolones for community-acquired pneumonia: meta-analysis of randomized controlled trials". Clin. Microbiol. Infect. 19 (4): ... Drlica K, Zhao X (1 September 1997). "DNA gyrase, topoisomerase IV, and the 4-quinolones". Microbiol Mol Biol Rev. 61 (3): 377- ... Research and Development of Quinolones in Daiichi Sankyo Co., Ltd. Archived 2016-10-12 at the Wayback Machine Page accessed ...
Quinolones Rubinstein E (2001). "History of quinolones and their side effects". Chemotherapy. 47 Suppl 3 (3): 3-8, discussion ...
... is a quinolone antibiotic used to treat bacterial infections. Pefloxacin has not been approved for use in the United ... Casparian JM, Luchi M, Moffat RE, Hinthorn D (May 2000). "Quinolones and tendon ruptures". South. Med. J. 93 (5): 488-91. doi: ... and the 4-quinolones". Microbiol Mol Biol Rev. 61 (3): 377-92. doi:10.1128/.61.3.377-392.1997. PMC 232616. PMID 9293187. Khaliq ...
quinolones/. (inhibits. DNA replication). 1st g.. *Cinoxacin‡. *Flumequine‡. *Nalidixic acid‡. *Oxolinic acid‡ ...
Ball, P. (2000). "Quinolone generations: Natural history or natural selection?". Journal of Antimicrobial Chemotherapy. 46: 17- ... Numerous pathogens, including enterococci, Streptococcus pyogenes and Klebsiella pneumoniae (quinolone-resistant) now exhibit ... Among the 46,766 quinolone users in the study, 38 (0.1%) cases of Achilles tendon rupture were identified. A study performed ... Ciprofloxacin is the most widely used of the second-generation quinolones.[71][72] In 2010, over 20 million prescriptions were ...
Recently new quinolones were added. Outpatient treatment has become possible even at the onset of the disease, and now we can ...
Quinolones Alksne L (February 2003). "Balofloxacin Choongwae". Current Opinion in Investigational Drugs. 4 (2): 224-9. PMID ...
Despite quinolones ability to target TopII, they can also inhibit TopIV based on the organisms and type of quinolone. ... 1989) model of quinolone inhibitor binding proposed that, in each DNAgyrase-DNA complex, four quinolone molecules associate ... In particular, smaller quinolones have shown to bind with high affinity in the multi-drug efflux pump in Escherichia coli and ... Quinolones are amongst the most commonly used antibiotics for bacterial infections in humans, and are used to treat illness ...
Quinolones can be an effective alternative. A recent study has shown that the presence of Enterobacter cloacae B29 in the gut ...
Some quinolones exert an inhibitory effect on the cytochrome P-450 system, thereby reducing theophylline clearance and ... Quinolones, including norfloxacin, may enhance the effects of oral anticoagulants, including warfarin or its derivatives or ... The toxicity of drugs that are metabolised by the cytochrome P450 system is enhanced by concomitant use of some quinolones. ... quinolones for community-acquired pneumonia: meta-analysis of randomized controlled trials". Clin. Microbiol. Infect. 19 (4): ...
1992). "Cytotoxicity of quinolones toward eukaryotic cells. Identification of topoisomerase II as the primary cellular target ... Although the reaction product is often shown as a hydroxyquinoline (the enol form), it is believed that the quinolone (keto ... The synthesis of 4-hydroxyquinolines and 4-quinolones is of great importance to a variety of fields, but most notably to the ... there is some discrepancy on whether a substituted 4-hydroxyquinoline or a substituted 4-quinolone is the final product of the ...
Rubinstein E (2001). "History of quinolones and their side effects". Chemotherapy. 47 (Suppl 3): 3-8, discussion 44-8. doi: ...
As quinolones are known to induce arthropathy in juvenile animals, administration of the drug to breast-feeding women cannot be ... Fleroxacin is a quinolone antibiotic. It is sold under the brand names Quinodis and Megalocin. Fleroxacin is a bactericidal ... Like other quinolones and fluoroquinolones the compound eradicates bacteria by interfering with DNA replication (bacterial DNA ... Yoshida H, Nakamura M, Bogaki M, Ito H, Kojima T, Hattori H, Nakamura S (April 1993). "Mechanism of action of quinolones ...
However a recent investigation into the origin of quinolones have discovered that a description for quinolones happened in 1949 ... These include the quinolone class, of which nalidixic acid is often credited as the first to be discovered. Like other ... Emmerson, A. M.; Jones, A. M. (2003-05-01). "The quinolones: decades of development and use". Journal of Antimicrobial ... Bisacchi, Gregory S. (2015-06-25). "Origins of the Quinolone Class of Antibacterials: An Expanded "Discovery Story"". Journal ...
The quinolone is also active against Gram-negative bacteria After oral administration enoxacin is rapidly and well absorbed ... Yoshida H, Nakamura M, Bogaki M, Ito H, Kojima T, Hattori H, Nakamura S (April 1993). "Mechanism of action of quinolones ... De Sarro A, Zappalá M, Chimirri A, Grasso S, De Sarro GB (July 1993). "Quinolones potentiate cefazolin-induced seizures in DBA/ ... Quinolones and fluoroquinolones are bactericidal drugs, eradicating bacteria by interfering with DNA replication. Like other ...
Quinolones Rafalsky V, Andreeva I, Rjabkova E (July 2006). "Quinolones for uncomplicated acute cystitis in women". The Cochrane ... Rufloxacin is a quinolone antibiotic. It is sold under the brand names, Ruflox, Monos, Qari, Tebraxin, Uroflox, Uroclar. ...
Appelbaum PC (1999). "Quinolone activity against anaerobes". Drugs. 58 Suppl 2: 60-4. doi:10.2165/00003495-199958002-00012. ... Rubinstein E (2001). "History of quinolones and their side effects". Chemotherapy. 47 Suppl 3 (3): 3-8, discussion 44-8. doi: ... Nord CE (1999). "Use of newer quinolones for the treatment of intraabdominal infections: focus on clinafloxacin". Infection. 27 ...
Quinolones "Recalling the Omniflox (Temafloxacin) Tablets" (pdf). Food and Drug Administration. 1992-06-05. Retrieved 2014-10- ... Gentry LO (December 1991). "Review of quinolones in the treatment of infections of the skin and skin structure". J. Antimicrob ... Rubinstein, E. "History of quinolones and their side effects". Chemotherapy. 47 Suppl 3: 3-8, discussion 44-8. doi:10.1159/ ...
Praziquantel, a quinolone derivative. The effect of praziquantel on H. heterophyes causes deep lesions on their teguments, and ...
The following adverse effects have been reported in studies with isosorbide mononitrate: Very common: Headache predominates (up to 30%) necessitating withdrawal of 2 to 3% of patients, but the incidence reduces rapidly as treatment continues.[7] Common: Tiredness, sleep disturbances (6%) and gastrointestinal disturbances (6%) have been reported during clinical trials with isosorbide mononitrate modified-release tablets, but at a frequency no greater than for placebo. Hypotension (4 to 5%), poor appetite (2.5%), nausea (1%)[7] Adverse effects associated with the clinical use of the drug are as expected with all nitrate preparations. They occur mainly in the early stages of treatment.[7] Hypotension (4%) with symptoms such as dizziness and nausea (1%) have been reported. In general, these symptoms disappear during long-term treatment.[7] Other reactions that have been reported with isosorbide mononitrate-modified release tablets include tachycardia, vomiting, diarrhoea, vertigo, and heartburn.[7] ...
... (ISDN) is a medication used for heart failure, esophageal spasms, and to treat and prevent chest pain from not enough blood flow to the heart.[1] It has been found to be particularly useful in heart failure due to systolic dysfunction together with hydralazine.[2][1] It is taken by mouth or under the tongue.[1] Common side effects include headache, lightheadedness with standing, and blurred vision.[1] Severe side effects include low blood pressure.[1] It is unclear if use in pregnancy is safe for the baby.[1] It should not be used together with medications within the sildenafil family.[1] ISDN is in the nitrate family of medications and works by dilating blood vessels.[1] Isosorbide dinitrate was first written about in 1939.[3] It is on the World Health Organization's List of Essential Medicines, the safest and most effective medicines needed in a health system.[4] ISDN is available as a generic medication.[1] A long-acting form exists.[1] ...
Synthetic quinolone antibiotics were discovered by George Lesher and coworkers as a byproduct of chloroquine manufacture in the ... In a technical sense, it is a naphthyridone, not a quinolone: its ring structure is a 1,8-naphthyridine nucleus that contains ... Nalidixic acid (tradenames Nevigramon, Neggram, Wintomylon and WIN 18,320) is the first of the synthetic quinolone antibiotics ... "Disabling and potentially permanent side effects lead to suspension or restrictions of quinolone and fluoroquinolone ...
Quinolones show effective prophylaxis mainly with hematological cancer. However, in general, for every five people who are ... The risk of illness and death can be reduced by taking common antibiotics such as quinolones or trimethoprim/sulfamethoxazole ...
quinolone any chemical compound having 2-quinolone or 4-quinolone skeleton in its structure ... Quinolone (en-ca); Chinoloni (it); quinolone (fr); Kinoloonid (et); Kinolon (sv); 喹诺酮 (zh-hans); quinolona (pt); Hinolon (sr-el ... any chemical compound having 2-quinolone or 4-quinolone skeleton in its structure (en); chem. Verbindung(en) (de); Famile d ... quinolones (en); chinolony (pl); Kinoloner (nb); Quinolone, Quinolon, Quinolonen, Chinolonen (nl) ...
The quinolones are a family of synthetic broad-spectrum antibiotics. The term quinolone(s) refers to potent synthetic ... Quinolones in comparison to other antibiotic classes have the highest risk of causing colonization with MRSA and Clostridium ... The first generation of the quinolones begins with the introduction of nalidixic acid in 1962 for treatment of urinary tract ... The majority of quinolones in clinical use belong to the subset of fluoroquinolones, which have a fluorine atom attached to the ...
Andriole, VT The Quinolones. Academic Press, 1989. *^ Andersson MI, MacGowan AP (2003). "Development of the quinolones". ... Although not formally a quinolone, nalidixic acid is considered the first quinolone drug. It was introduced in 1962 for ... A quinolone antibiotic is a member of a large group of broad-spectrum bactericides that share a bicyclic core structure related ... Quinolones are contraindicated if a patient has epilepsy, Ehlers-Danlos Syndrome,[41] QT prolongation, pre-existing CNS lesions ...
Andriole, VT The Quinolones. Academic Press, 1989. *^ Andersson MI, MacGowan AP (2003). "Development of the quinolones". ... Quinolone antibiotic at Curlie (based on DMOZ). *Healthcare-associated Infections (HAIs)- Quinolones and the Clinical ... Norris, S; Mandell, GL (1988). "The quinolones: history and overview". The quinolones: history and overview. San Diego: ... Although not formally a quinolone, nalidixic acid is considered the first quinolone drug. It was introduced in 1962 for ...
Quinolone resistance despite low antimicrobial usage - mechanisms and possible preventive measures Anne Margrete Urdahl + 10 ... GENOMIC CHARACTERIZATION AND COMPARISON OF QUINOLONE RESISTANT ESCHERICHIA COLI FROM POULTRY AND HUMANS IN NORWAY ... GENOMIC CHARACTERIZATION AND COMPARISON OF QUINOLONE RESISTANT ESCHERICHIA COLI FROM POULTRY AND HUMANS IN NORWAY ...
What are quinolones? Quinolones are antimicrobial agents effective in the treatment of selected community-acquired and ... How does resistance to quinolones develop? Quinolones inhibit two enzymes that are required for bacterial DNA synthesis, i.e., ... What organisms can be resistant to quinolones? Resistance to quinolones has been reported in a variety of important bacterial ... Resistance to quinolones limits drug selection for treatment of many infections.. *Organisms resistant to quinolones often are ...
Quinolone may refer to: 2-Quinolone 4-Quinolone Quinolone antibiotics This set index page lists chemical compounds articles ...
It and 2-quinolone are the two most important parent (meaning simplified) quinolones. 4-Quinolone exists in equilibrium with a ... The hydroxyquinolines tautomerize to the quinolones. Andriole, VT The Quinolones. Academic Press, 1989. Shi, Pengfei; Wang, ... the 4-quinolone antibiotics represent a large class of important drugs. The chemical synthesis of quinolones often involves ... 4-Quinolone is an organic compound derived from quinoline. ... 4-Quinolone is of little intrinsic value but its derivatives, ...
... provides information about interactions between Insulin Regular Human Injection and antidiabetic-agents-selected-quinolones. ... Antidiabetic Agents/Selected Quinolones. This information is generalized and not intended as specific medical advice. Consult ... Using some quinolone antibiotics with your diabetes medicine may make your blood sugar too low. ...
The constant need for new anti microbials has produced a variety of newer quinolones termed as I, II, III, and IV generation. ... The interest of the medical community in quinolones has not decreased despite more than ten years of continuous and growing use ... Structural development, haematological immunological and pharmacological effects of quinolones.. Chide OE1, Orisakwe OE. ... These attributes, coupled with their expanded spectrum and the immune enhancing phenomena of quinolones with a cyclopropyl ...
... provides information about interactions between Glyburide-Metformin Oral and selected-antidiabetic-agents-selected-quinolones. ... Using some quinolone antibiotics with your diabetes medicine may make your blood sugar too low. ... Selected Antidiabetic Agents/Selected Quinolones Interactions. This information is generalized and not intended as specific ...
Topoisomerase IV is a target of quinolones in Escherichia coli. A B Khodursky, E L Zechiedrich, and N R Cozzarelli ... We suggest that this and a slightly higher intrinsic resistance of topo IV make it secondary to gyrase as a quinolone target. ... Our results imply that the quinolone binding pockets of gyrase and topo IV are similar and that substantial levels of drug ... Mutant forms of topo IV provided an additional 10-fold resistance to quinolones and prevented drug-induced catenane ...
Antibiotic, Quinolone. Class Summary. The quinolone class antibiotics are no longer considered effective against GCU due to ... 45] Quinolone-resistant GCU is also more prevalent in men who have sex with men. Because of increasing resistance, quinolones ( ... Quinolone resistance has increase worldwide, now approximately 21%, [43] and is common in Asia, the Pacific, Europe, and the ... 54, 55, 56] although there is concern for emerging quinolone resistance [5, 18, 15, 16] ). Other choices could include 7 days ...
Quinolone Resistance Reversion by Targeting the SOS Response E. Recacha, J. Machuca, P. Díaz de Alba, M. Ramos-Güelfo, F. ... Membrane Distribution of the Pseudomonas Quinolone Signal Modulates Outer Membrane Vesicle Production in Pseudomonas aeruginosa ...
Quinolones have few adverse effects, most notably nausea, headache, dizziness, and confusion. Less common but more serious ... Most quinolones have excellent oral bioavailability, with serum drug concentrations equivalent to intravenous administration. ... Comparison of Quinolone Generations. Quinolone generations. Microbiologic activity. Administration and characteristics. ... Comparison of Quinolone Generations. Quinolone generations. Microbiologic activity. Administration and characteristics. ...
Recent 4-(1H)-quinolone derivatives, endochin-like quinolones (ELQ), exhibit an in vitro IC50 against Plasmodium falciparum as ... Endochin-like quinolones against Toxoplasma. J. Stone Doggett, Aaron Nilsen, Isaac Forquer, Keith W. Wegmann, Lorraine Jones- ... Endochin-like quinolones against Toxoplasma. J. Stone Doggett, Aaron Nilsen, Isaac Forquer, Keith W. Wegmann, Lorraine Jones- ... quinolone-3-diarylethers was made to improve these properties. Of the 4(1H)-quinolone-3-diarylethers synthesized in our ...
Buy the Hardcover Book The Quinolones by Vincent T. Andriole at Indigo.ca, Canadas largest bookstore. + Get Free Shipping on ... Use of the Quinolones in Sexually Transmitted Diseases. Treatment of Respiratory Infections with Quinolones. Use of Quinolones ... Use of the Quinolones in Treatment of Bacterial Meningitis. Use of the Quinolones in Immunocompromised Patients. Use of the ... The Quinolones: History and Overview. Chemistry and Mechanism of Action of the Quinolone Antibacterials. Comparative In-Vitro ...
QUINOLONES: REVIEW OF PSYCHIATRIC AND NEUROLOGIC ADVERSE REACTIONS Tome, A.M., et al, Drug Safety 34(6):465, June 2011. ... One study found the odds ratio for Achilles tendon rupture to be 4.3 with current use of a quinolone, 2.4 with exposure within ... So now the concern is that prescribers are at risk since there are multiple alternatives to the quinolones and they are "black ... In July of 2008 a "black box" warning was put in the package insert of the quinolones. This side-effect, like the ...
In this review, we present hallmark investigations describing the mode of action of quinolones, one of the antibacterial ... the necessity to look beyond primary drug-target interactions towards thoroughly understanding the mechanism of quinolones at ... Keywords: antibiotics; quinolones; topoisomerases; DNA replication; DNA supercoiling antibiotics; quinolones; topoisomerases; ... Gutierrez, A.; Stokes, J.M.; Matic, I. Our Evolving Understanding of the Mechanism of Quinolones. Antibiotics 2018, 7, 32. ...
... Seng-Kee Chuah,1 Wei-Chen Tai,1 Chen-Hsiang Lee,2 ... W. L. Chang, C. Y. Kao, C. T. Wu et al., "Gemifloxacin can partially overcome quinolone resistance of H. pylori with gyrA ... A. Robicsek, G. A. Jacoby, and D. C. Hooper, "The worldwide emergence of plasmid-mediated quinolone resistance," The Lancet ... M. Berning, S. Krasz, and S. Miehlke, "Review: should quinolones come first in Helicobacter pylori therapy?" Therapeutic ...
Overview of Quinolones, General information, Mechanism of action, Pharmacokinetics, Classification, Therapeutic use, Adverse ... Overview of Quinolones. by Mohammed Haneef 1. General information. 1.1. Synthetic antimicrobial agents. 1.2. First quinolone ... treated by quinolones. 5.4. Respiratory tract infections. 5.4.1. treated by respiratory fluroquinolones. 5.4.1.1. gemifloxacin ...
The New Fluorinated Quinolones for Infection Prevention in Acute Leukemia Annals of Internal Medicine; 106 (1): 144-146 ... Oral Quinolone Treatment for Osteomyelitis Annals of Internal Medicine; 115 (10): 832 ... Quinolone-Based Antibacterial Chemoprophylaxis in Neutropenic Patients: Effect of Augmented Gram-Positive Activity on ... Development and bioanalytical method validation of an LC-MS/MS assay for simultaneous quantitation of 2-alkyl-4(1H)-quinolones ...
encoded search term (What is the role of quinolones and TMP-SMZ in the treatment of Enterobacter infections?) and What is the ... What is the role of quinolones and TMP-SMZ in the treatment of Enterobacter infections?. Updated: Jun 18, 2019 ... role of quinolones and TMP-SMZ in the treatment of Enterobacter infections? What to Read Next on Medscape. Related Conditions ...
We also discuss quinolone resistance and how quinolone treatment can lead to resistance to non-quinolone antibiotics. ... We also discuss quinolone resistance and how quinolone treatment can lead to resistance to non-quinolone antibiotics. View Full ... Quinolones: Mechanism, Lethality and Their Contributions to Antibiotic Resistance by Natassja G. Bush ... Bush, N.G.; Diez-Santos, I.; Abbott, L.R.; Maxwell, A. Quinolones: Mechanism, Lethality and Their Contributions to Antibiotic ...
Quinolones as HCV NS5B polymerase inhibitors.. Kumar, D.V., Rai, R., Brameld, K.A., Somoza, J.R., Rajagopalan, R., Janc, J.W., ... Herein we describe our discovery of quinolone derivatives, novel small-molecules that inhibit NS5b polymerase, a key enzyme of ...
Reduction of the fitness burden of quinolone resistance in Pseudomonas aeruginosa.. Kugelberg E1, Löfmark S, Wretlind B, ... Quinolone resistance in the opportunistic pathogen Pseudomonas aeruginosa is commonly caused by mutations that alter the target ... We have analysed the effect of quinolone resistance caused by DNA gyrase/topoisomerase IV mutations on bacterial fitness. ... Our results show that no cost and compensatory mutations are common in quinolone-resistant P. aeruginosa. ...
Quinolones are a very important family of antibacterial agents that are widely prescribed for the treatment of infections in ... These antineoplastic quinolones represent a potentially important source of new anticancer agents and provide an opportunity to ... Keywords: Amscrine; Antineoplastic Quinolones; E. Coli DNA Gyrase; Etoposide; Eukaryotic Topoisomerase II; Human Topoisomerase ... In contrast to most other anti-infective drugs, quinolones do not kill bacteria by inhibiting a critical cellular process. ...
Learn about the veterinary topic of Quinolones, including Fluoroquinolones. Find specific details on this topic and related ... Examples of the quinolone carboxylic acids and species in which they are approved are presented in Quinolones and Species ... Most quinolones also cross the placental barrier. The apparent volume of distribution of most quinolones is large. The degree ... Known generically as quinolones or 4-quinolones, these drugs are derived from several closely related ring structures that have ...
Quinolones and fluoroquinolones are bactericidal drugs, actively killing bacteria. Quinolones inhibit the bacterial DNA gyrase ... The quinolones are a family of broad-spectrum antibiotics. The parent of the group is nalidixic acid. The majority of ... Quinolones can enter cells easily and therefore are often used to treat intracellular pathogens such as Legionella pneumophila ... Resistance to quinolones can develop rapidly, even during a course of treatment. Numerous pathogens, including Staphylococcus ...
  • The quinolones are a family of synthetic broad-spectrum antibiotics . (princeton.edu)
  • Nearly all quinolone antibiotics in use are fluoroquinolones , which contain a fluorine atom in their chemical structure and are effective against both Gram-negative and Gram-positive bacteria. (wikipedia.org)
  • Quinolone may refer to: 2-Quinolone 4-Quinolone Quinolone antibiotics This set index page lists chemical compounds articles associated with the same name. (wikipedia.org)
  • Aside from pedagogical interest, 4-Quinolone is of little intrinsic value but its derivatives, the 4-quinolone antibiotics represent a large class of important drugs. (wikipedia.org)
  • Using some quinolone antibiotics with your diabetes medicine may make your blood sugar too low. (webmd.com)
  • We also discuss quinolone resistance and how quinolone treatment can lead to resistance to non-quinolone antibiotics. (mdpi.com)
  • Quinolone antibiotics were once considered relatively safe, but several side-effects have become evident with experience. (wikidoc.org)
  • New developments in non-quinolone-based antibiotics for the inhibiton of bacterial gyrase and topoisomerase IV. (bioportfolio.com)
  • Quinolones are broad-spectrum antibiotics that have been used for decades in treating bacterial infections in humans and animals, and subsequently bacterial resistance to these agents has increased. (bioportfolio.com)
  • Quinolone Antibiotics: Are They Safe and Effective? (ahefv.com)
  • What are Quinolone Antibiotics? (ahefv.com)
  • Quinolones are synthetic bactericidal antibiotics that can affect a wide range of gram-positive and gram-negative bacteria. (ahefv.com)
  • However, in severe acute cases of bacterial prostatitis or pyelonephritis, quinolone antibiotics are recommended as first-line therapy. (ahefv.com)
  • Most of quinolone antibiotics are fluoroquinolones that have a chemical structure with a fluorine atom, which is effective against different bacteria, including gram-negative and gram-positive. (ahefv.com)
  • The quinolone group of antibiotics was discovered in the 1960s, which caused a significant interest right away. (ahefv.com)
  • The modern quinolone antibiotics are believed to be safe and to have a low risk of side effects. (ahefv.com)
  • But still, the use of these medications causes a range of doubts and questions because it is hard not to pay attention to a range of side effects caused during the use of quinolone antibiotics. (ahefv.com)
  • Also, the FDA regularly publishes new safety warnings regarding the use of quinolone antibiotics. (ahefv.com)
  • For instance, in the UK, the use of quinolone antibiotics by children is strictly restricted. (ahefv.com)
  • A range of studies was conducted in order to determine the safety of quinolone antibiotics if compared to other similar treatments. (ahefv.com)
  • The use of quinolone antibiotics may be recommended in case of the infection caused by highly antibiotic resistant bacteria, or if oral therapy or parenteral administration is preferred. (ahefv.com)
  • Quinolones are the commonly used class of antibiotics in the world that are able to treat a wide range of various bacterial infections, and that is why they have been prescribed quite often, which naturally led to the occurrence of quinolone-resistant bacteria. (ahefv.com)
  • We also showed evidence for the existence of supercoiling activity in A. thaliana and that the plant is sensitive to quinolone and aminocoumarin antibiotics, compounds that target DNA gyrase in bacteria. (nih.gov)
  • However, it was not possible at that time to show whether the A. thaliana genes encoded an active gyrase enzyme, nor whether that enzyme is indeed the target for the quinolone and aminocoumarin antibiotics. (nih.gov)
  • In conclusion, the effective hepatic uptake of quinolone antibiotics are via carrier-mediated active transport, which is distinct from that involved in the transport of bile acids, organic anions, organic cations or neutral steroids. (aspetjournals.org)
  • Chemical structures of quinolone antibiotics. (aspetjournals.org)
  • Quinolone antibiotics may be associated with an increased risk of aortic aneurysm and dissection and should only be used after careful benefit-risk assessment and consideration of other therapeutic options in patients at risk, the MHRA has advised. (mims.co.uk)
  • The MHRA's advice follows a recent recommendation from the European Medicines Agency that the use of quinolone antibiotics be restricted owing to disabling and potentially long-lasting adverse effects associated with their use. (mims.co.uk)
  • Twenty compounds belonged to three classes of widely used veterinary antibiotics (i.e., tetracyclines, sulfonamides, and quinolones) were investigated. (springer.com)
  • By contrast, quinolones were the least abundant antibiotics in swine feces and exhibited a higher removal by anaerobic digestion in winter than in summer. (springer.com)
  • The European Medicines Agency (EMA) has recommended that the use of quinolone antibiotics be restricted owing to disabling and potentially long-lasting adverse effects reported with their use. (mims.co.uk)
  • Quinolones are a class of broad-spectrum antibiotics active against both Gram-negative and Gram-positive bacteria. (mims.co.uk)
  • The EMA's Pharmacovigilance Risk Assessment Committee (PRAC) made its recommendations following a review of serious adverse effects reported with the use of quinolone antibiotics given orally, parenterally or by inhalation. (mims.co.uk)
  • Quinolone antibiotics available to prescribe in the UK are all of the fluoroquinolone type and include ciprofloxacin , levofloxacin , moxifloxacin and ofloxacin . (mims.co.uk)
  • The PRAC recommends that medicines containing the non-fluorinated first-generation quinolone antibiotics (cinoxacin, nalidixic acid or pipemidic acid) should be removed from the market because they are authorised only for infections that should no longer be treated with this class of drug. (mims.co.uk)
  • Few drugs fit that category better than quinolone antibiotics. (regenexx.com)
  • Another study last year compared the rate of aortic rupture or aneurysm in those taking quinolone antibiotics to those taking amoxicillin (a penicillin antibiotic). (regenexx.com)
  • Aortic ruptures and aneurysms, of course, adds to a list of problems associated with quinolone antibiotics, many of which I've covered here on this blog. (regenexx.com)
  • There is a great deal of research, dating back a decade or more, that strongly links quinolone antibiotics to ruptures of the Achilles tendon . (regenexx.com)
  • Avoid quinolone antibiotics if you're able. (regenexx.com)
  • Quinolones, and the fluoroquinolones subgroup, are a class of antibiotics commonly used for the treatment of a wide variety of infections. (springer.com)
  • A multirun analytical method has been developed and validated for trace determination of 24 antibiotics including 7 sulfonamides, 3 macrolides, 7 quinolones, 6 tetracyclines, and trimethoprim in chlorine-disinfected drinking water using a single solid-phase extraction method coupled to liquid chromatography with positive electrospray tandem mass spectrometry detection. (usgs.gov)
  • A preliminary occurrence study using this method revealed the presence of some antibiotics in drinking waters, including sulfamethoxazole (3.0−3.4 ng/L), macrolides (1.4−4.9 ng/L), and quinolones (1.2−4.0 ng/L). (usgs.gov)
  • Quinolones are a group of synthetic broad-spectrum antibiotics with a wide variety of applications in medicine and veterinary sciences. (sielc.com)
  • OBJECTIVES: In the present study, some potential virulence genes of APECs isolated from Northeast of Iran and their resistance to the quinolones antibiotics were studied. (sid.ir)
  • These attributes, coupled with their expanded spectrum and the immune enhancing phenomena of quinolones with a cyclopropyl moiety at position 1 of the quinolone ring suggest that the newer fluoroquinolones are so far the most ideal agents for the empirical treatment of many common infections. (nih.gov)
  • Quinolones and fluoroquinolones are bactericidal drugs, actively killing bacteria. (wikidoc.org)
  • Quinolones, and especially fluoroquinolones, are one of the largest classes of antibacterial agents used worldwide. (bl.uk)
  • However, in recent years, this type of quinolone resistance was more frequently observed in animals to which more quinolones and fluoroquinolones were administered (broiler chickens and veal calves). (wur.nl)
  • The association between fluoroquinolones and arthropathy was primarily described in immature animals, and only rarely in humans, yet it has led to the restricted use of quinolones during pregnancy. (springer.com)
  • Resistance to quinolones and fluoroquinolones has been increasingly reported among human and veterinary isolates during the last three decades related to their wide clinical use. (eurekaselect.com)
  • The first generation of the quinolones begins with the introduction of nalidixic acid in 1962 for treatment of urinary tract infections in humans. (princeton.edu)
  • Early quinolones, such as nalidixic acid, had poor systemic distribution and limited activity and were used primarily for Gram-negative urinary tract infections. (cdc.gov)
  • Nalidixic acid and other early quinolones had limited use due to poor pharmacokinetics, relatively narrow antimicrobial spectrum of activity, and frequent adverse effects. (nih.gov)
  • The first quinolone, nalidixic acid (NegGram), was introduced in 1962. (aafp.org)
  • Nalidixic acid, considered a first-generation drug, is the earliest of the quinolones. (merckvetmanual.com)
  • Nalidixic acid was the first quinolone, and today many derivatives exist on the market. (ahefv.com)
  • The first quinolone is nalidixic acid that was introduced in 1962 and is considered to be the predecessor of all members of the quinolone family. (dovepress.com)
  • Nalidixic acid was the less active quinolone. (eurekamag.com)
  • Salmonella and Campylobacter prevalence and susceptibility to quinolones, nalidixic acid and ciprofloxacin, were evaluated. (k-state.edu)
  • Quinolones in comparison to other antibiotic classes have the highest risk of causing colonization with MRSA and Clostridium difficile . (princeton.edu)
  • A quinolone antibiotic is a member of a large group of broad-spectrum bactericides that share a bicyclic core structure related to the compound 4-quinolone . (wikipedia.org)
  • When used in combination with agents from other antibiotic classes, such as beta-lactams and aminoglycosides, the quinolones are not predictably synergistic. (aafp.org)
  • By chronologically analyzing data gathered on the mode of action of this imperative antibiotic class, we highlight the necessity to look beyond primary drug-target interactions towards thoroughly understanding the mechanism of quinolones at the level of the cell. (mdpi.com)
  • Fluoroquinolone is one of the quinolones, which are a family of synthetic broad-spectrum antibiotic drugs. (dovepress.com)
  • Now, it seems quinolone antibiotic use can be added to the risk list for aortic rupture and aneurysm. (regenexx.com)
  • Quinolones are a huge family of antibiotic drugs that can be identified by -floxacin at the end of the generic drug name: ciprofloxacin (Cipro), levofloxacin (Levaquin), moxifloxacin (Avelox), and many, many more. (regenexx.com)
  • The targets of quinolone activity are the bacterial DNA gyrase and topoisomerase IV, enzymes essential for DNA replication and transcription. (cdc.gov)
  • We have demonstrated that, in Escherichia coli, quinolone antimicrobial agents target topoisomerase IV (topo IV). (pnas.org)
  • Quinolones rapidly inhibit DNA synthesis by promoting cleavage of bacterial DNA in the DNA-enzyme complexes of DNA gyrase and type IV topoisomerase, resulting in rapid bacterial death. (aafp.org)
  • Quinolone resistance in the opportunistic pathogen Pseudomonas aeruginosa is commonly caused by mutations that alter the target molecules DNA gyrase/topoisomerase IV, or cause activation of various efflux systems. (nih.gov)
  • We have analysed the effect of quinolone resistance caused by DNA gyrase/topoisomerase IV mutations on bacterial fitness. (nih.gov)
  • Depending upon the bacterial species and quinolone employed, either DNA gyrase or topoisomerase IV serves as the primary cytotoxic target of drug action. (ingentaconnect.com)
  • Because of the clinical importance of quinolones, this review will discuss the mechanistic basis for drug efficacy and interactions between these compounds and their topoisomerase targets. (ingentaconnect.com)
  • The quinolones inhibit bacterial enzyme topoisomerases, including topoisomerase II (otherwise known as DNA gyrase) and topoisomerase IV. (merckvetmanual.com)
  • Quinolones inhibit the bacterial DNA gyrase or the topoisomerase IV enzyme, thereby inhibiting DNA replication and transcription. (wikidoc.org)
  • Finally, mutations at key sites in DNA gyrase or topoisomerase IV can decrease their binding affinity to quinolones, decreasing the drug effectiveness. (wikidoc.org)
  • Imidazopyrazinones (IPYs): non-quinolone bacterial topoisomerase inhibitors showing partial cross-resistance with quinolones. (bioportfolio.com)
  • Quinolones are able to convert their targets, topoisomerase IV, and gyrase into toxic enzymes to fragment the chromosome of bacteria. (ahefv.com)
  • Quinolones resistance is a cause of mutations in topoisomerase IV and gyrase, which does not allow quinolones and enzymes to interact properly. (ahefv.com)
  • The intracellular targets of the quinolones are two DNA topoisomerases: gyrase and topoisomerase IV. (asm.org)
  • Gyrase tends to be the primary target in gram-negative bacteria, while topoisomerase IV is preferentially inhibited by most quinolones in gram-positive organisms ( 28 ). (asm.org)
  • In the present minireview we consider cell death through a two-part "poison" hypothesis in which the quinolones form reversible drug-topoisomerase-DNA complexes that subsequently lead to several types of irreversible (lethal) damage. (asm.org)
  • Other consequences of quinolone treatment, such as depletion of gyrase and topoisomerase IV activity, are probably less immediate ( 42 ). (asm.org)
  • To provide a framework for considering quinolone lethality, we begin by briefly describing the drug-topoisomerase-DNA complexes. (asm.org)
  • DNA gyrase, topoisomerase IV, and the 4-quinolones. (asm.org)
  • Moreover, topoisomerase IV is a target of the 4-quinolones, antibacterial agents that had previously been thought to target only gyrase. (asm.org)
  • The key event in quinolone action is reversible trapping of gyrase-DNA and topoisomerase IV-DNA complexes. (asm.org)
  • In many gram-negative bacteria, resistance to moderate levels of quinolone arises from mutation of the gyrase A protein and resistance to high levels of quinolone arises from mutation of a second gyrase and/or topoisomerase IV site. (asm.org)
  • Thus, quinolone-topoisomerase biology is providing a model for understanding aspects of host-parasite interactions and providing ways to investigate manipulation of the bacterial chromosome by topoisomerases. (asm.org)
  • DNA gyrase (topoisomerase II) and topoisomerase IV are named as the primary and secondary targets for quinolones [ 6 ]. (hindawi.com)
  • Qnr proteins are protecting target enzymes DNA gyrase and topoisomerase IV of quinolone inhibition [ 7 ]. (hindawi.com)
  • In order to examine the inhibitory activities of quinolones against topoisomerase IV, both subunits of this enzyme, ParC and ParE, were purified from Escherichia coli. (nih.gov)
  • Although topoisomerase IV was less sensitive to quinolones than DNA gyrase, the 50% inhibitory concentrations for decatenation were significantly lower than those for type I topoisomerases. (nih.gov)
  • These results imply that topoisomerase IV could be a target for the quinolones in intact bacteria and that quinolones could inhibit not only supercoiling of DNA gyrase but also decatenation of topoisomerase IV when high concentrations of drug exist in bacterial cells. (nih.gov)
  • Fluoroquinolone resistance in the Enterobacteriaceae family, of which Shigella is a member, has been proved to be mainly caused by point mutations in genes encoding DNA gyrase and topoisomerase IV, such as gyr A, gyr B, and par C genes in quinolone resistance-determining regions (QRDRs). (dovepress.com)
  • Until recently, the mechanisms of resistance to quinolones in Enterobacteriaceae were believed to be only chromosome-encoded, i.e. related to modifications of the molecular targets (DNA gyrase and topoisomerase IV), decreased outer-membrane permeability (porin defect) and overexpression of naturally-occurring efflux. (eurekaselect.com)
  • The Qnr proteins protect DNA gyrase and type IV topoisomerase from quinolone inhibition. (eurekaselect.com)
  • CRISPR/Cas9/sgRNA-mediated targeted gene modification confirms the cause-effect relationship between gyrA mutation and quinolone resistance in Escherichia coli. (bioportfolio.com)
  • The quinolone antibacterials have previously been shown to "poison" DNA gyrase of Escherichia coli, resulting in rapid bacterial cell death by a pathway which has been a subject of controversy. (bl.uk)
  • Mutations in the quinolone resistance-determining regions of gyrA , gyrB , parC , and parE were studied in 30 fluoroquinolone-resistant clinical isolates of Escherichia coli producing extended-spectrum β-lactamases. (asm.org)
  • The objective of this study was to investigate the presence of mutations in regions that code for quinolone resistance in the chromosomal genes gyrA , gyrB , parC , and parE in ESBL-producing clinical isolates of Escherichia coli . (asm.org)
  • Existence of a novel qepA variant in quinolone resistant Escherichia coli from aquatic habitats of Bangladesh. (tufts.edu)
  • Abstract: Of 19 environmental Escherichia coli (n = 12) and Klebsiella pneumoniae (n = 7) tested for quinolone resistance-related genes qnrA, qnrB, qnrC, qnrS and qepA, four each of E. coli and K. pneumoniae possessed qnrS, and another E. coli isolate possessed a new variant of qepA. (tufts.edu)
  • Reduction of the fitness burden of quinolone resistance in Pseudomonas aeruginosa. (nih.gov)
  • The third P. aeruginosa intercellular signal is a quinolone compound that was identified as 2-heptyl-3-hydroxy-4-quinolone (the Pseudomonas quinolone signal [PQS]) ( 37 ). (asm.org)
  • The largest set of pleiotropic mutations blocked the production of the extracellular Pseudomonas quinolone signal (PQS), a molecule required for the synthesis of secondary metabolites and extracellular enzymes. (asm.org)
  • Recently, a third signaling system based on 2-heptyl-3-hydroxy-4-quinolone, designated the Pseudomonas quinolone signal (PQS), has been shown to be a part of the quorum-sensing regulatory network in P. aeruginosa ( 27 ). (asm.org)
  • Biotic inactivation of the Pseudomonas aeruginosa quinolone signal molecule. (abcam.com)
  • Quinolone signaling in the cell-to-cell communication system of Pseudomonas aeruginosa. (abcam.com)
  • The antagonistic effects of physiological levels of Ca++ and Mg++ on the in-vitro activity of aminoglycosides and quinolones against Pseudomonas aeruginosa were studied at both pH 7.4 and 5.5. (uzh.ch)
  • Reporting susceptibilities to various quinolones provides the information necessary to choose an appropriate therapy that will minimize the selection of mutations leading to resistance. (cdc.gov)
  • Resistance to quinolones occurs through chromosomal mutations in the genes encoding these enzymes and by porin and efflux mutations. (cdc.gov)
  • Many resistant organisms have multiple enzyme target site, porin, and efflux mutations, producing high-level resistance to quinolones. (cdc.gov)
  • Our results imply that the quinolone binding pockets of gyrase and topo IV are similar and that substantial levels of drug resistance require mutations in both enzymes. (pnas.org)
  • Our results show that 'no cost' and compensatory mutations are common in quinolone-resistant P. aeruginosa. (nih.gov)
  • Pertinent information on the bacterial topoisomerases and DNA gyrases, quinolone binding, DNA/RNA synthesis inhibition, cell death in the absence of protein synthesis, specific mutations within the quinolone resistance-determining region, and mutations that lead to altered access to target enzymes (efflux systems) is also highlighted. (cdc.gov)
  • Following on from this, clinical isolates were screened by DNA sequencing and amino acid mutations in the "quinolone resistance determining region" (QRDR) of gyrA identified. (bl.uk)
  • Mutations in gyrA such as serine-83 to leucine, serine-83 to phenylalanine, aspartate-87 to tyrosine, aspartate-87 to asparagine and aspartate-87 to glycine were found to have arisen in the QRDR of gyrA in common with other quinolone resistance mutations previously found. (bl.uk)
  • To identify mutations in the gyrA and parC genes of the gonococcal mutants, the quinolone resistance determining regions of the gyrA and parC genes were polymerase chain reaction (PCR) amplified and the PCR products were directly sequenced. (bmj.com)
  • Isolates with double mutations in gyrA codons 83 and 87 are the major type of quinolone-resistant Salmonella isolated from swine in Taiwan. (scribd.com)
  • While studies indicated the relationship between gyrA mutations and bacterial resistance to quinolones, CRISPR/Cas9 was used in this study to investigate causal role of gyrA mutation in the quinolone resistance. (bioportfolio.com)
  • coli isolates were analyzed for gyrA mutations and their resistance to quinolones. (bioportfolio.com)
  • The CRISPR/Cas9 system was used to generate gyrA mutations in quinolone-susceptible E. coli ATCC 25922, and quinolone-resistant clinical E. coli. (bioportfolio.com)
  • The gyrA mutations were identified in nucleotide positions 248, 255, 259, 260, 261, 273 and 300, and mutations at positions 248 and 259 resulting in amino acid changes at positions 83 and 87 were associated with quinolone resistance. (bioportfolio.com)
  • Double-site amino acid mutations increase resistance to quinolones. (bioportfolio.com)
  • The gyrA mutations causing changes at amino acids 83 and 87 reversed the features of quinolone resistance in ATCC and clinical strains, verifying the causal role of gyrA mutation in the quinolone resistance of E. coli. (bioportfolio.com)
  • This proposed study aims to document the risk factors for quinolone resistance in bloodstream isolates of E. coli. (bioportfolio.com)
  • For plasmid-mediated quinolone resistance, all the 47 isolates carried the aac(6')-ib-cr gene, and amongst them18 were qnrS positive. (diva-portal.org)
  • Analysis of quinolone resistance mechanisms in Neisseria gonorrhoeae isolates in vitro. (bmj.com)
  • We generated gonococcal mutants resistant to norfloxacin in vitro from norfloxacin sensitive isolates and analysed the contribution of three known mechanisms of quinolone resistance in Neisseria gonorrhoeae. (bmj.com)
  • The mechanism of Nal resistance in most of the isolates (94%) was a mutation in the quinolone resistance-determining chromosomal region of gyrA that led to the amino acid substitution Ser83Phe. (asm.org)
  • The sequence obtained for each of the genes in each of the 30 isolates was compared with the nucleotide sequence of the quinolone resistance-determining region (QRDR) of the reference strain E. coli K-12. (asm.org)
  • Plasmid-mediated quinolone resistance has recently been identified in isolates of S. enterica in a number of countries at low prevalence. (gla.ac.uk)
  • Prevalence of plasmid-mediated quinolone resistance genes and ciprofloxacin resistance in pediatric bloodstream isolates of Enterobacteriaceae over a 9-year period. (medworm.com)
  • We compared kill curves of ocular isolates with vancomycin and third generation quinolones. (arvojournals.org)
  • Provides information on a study that monitored resistance to the drug quinolones in Salmonella enterica serotype enteritidis from human infections. (ebscohost.com)
  • The acquisition of quinolone-resistance in E. coli and Salmonella has also been investigated. (bl.uk)
  • In his research, Veldman describes the first Salmonella and E. coli bacteria with transferable quinolone resistance in farm animals and humans in the Netherlands. (wur.nl)
  • The purpose of the research described in this dissertation was to determine the prevalence and quinolone susceptibility of Salmonella and Campylobacter isolated from feedlot cattle and to determine whether these outcomes were associated with fluoroquinolone use. (k-state.edu)
  • A second, experimental study assessed prevalence and quinolone susceptibilities of Salmonella and Campylobacter in feces of feedlot cattle administered enrofloxacin for the control of BRD (metaphylaxis). (k-state.edu)
  • However, there was no evidence that enrofloxacin metaphylaxis impacted the prevalence of Salmonella or Campylobacter, nor did it significantly affect their susceptibility to human quinolones. (k-state.edu)
  • In gram-negative bacteria, plasmid-mediated resistance genes produce proteins that can bind to DNA gyrase, protecting it from the action of quinolones. (wikidoc.org)
  • The opportunistic human pathogen secretes 2-heptyl-3-hydroxy-4-quinolone (PQS), a quorum sensing (QS) signal that regulates the expression of numerous virulence genes. (bioportfolio.com)
  • The emergence of plasmid-mediated quinolone resistance (PMQR) is a global challenge in the treatment of clinical disease in both humans and animals and is exacerbated by the presence of different PMQR genes existing in the same bacterial strain. (dovepress.com)
  • This study proposed to investigate the frequency of quinolone-resistance plasmid genes and the O-antigen serogroup among UPEC isolated from KTPs and non-KTP with UTI. (hindawi.com)
  • The extent of quinolone-resistant genes in gram-negative bacteria like UPEC is a big concern for KTPs [ 1 ]. (hindawi.com)
  • Genes related to quinolone resistance were amplified by PCR. (dovepress.com)
  • This study aimed to determine the genes coding for ESBLs, plasmid mediated quinolone resistance and virulence markers in commensal E. coli isolated from healthy school children. (diva-portal.org)
  • Five plasmid-mediated quinolone resistance (PMQR) genes, qnrA, qnrB, qnrS, qepA, and aac(6')-Ib-cr, and the minimal inhibitory concentration (MIC) values for ciprofloxacin were tested for all the strains. (medworm.com)
  • Quinolones constitute a large class of synthetic antimicrobial agents that are highly effective in the treatment of many types of infectious diseases, particularly those caused by bacteria. (indigo.ca)
  • In this review, we present hallmark investigations describing the mode of action of quinolones, one of the antibacterial classes targeting the function of topoisomerases in bacteria. (mdpi.com)
  • In contrast to most other anti-infective drugs, quinolones do not kill bacteria by inhibiting a critical cellular process. (ingentaconnect.com)
  • A second unique aspect of quinolones is their differential ability to target these two enzymes in different bacteria. (ingentaconnect.com)
  • While this unusual feature initially stymied development of quinolones with high activity against Gram-positive bacteria, it ultimately opened new vistas for the clinical use of this drug class. (ingentaconnect.com)
  • One of the attractive features of the quinolones is their ability to kill bacteria rapidly, an ability that differs widely among the various derivatives. (asm.org)
  • Moreover we show that, as in bacteria, the quinolone-sensitive (wild-type) allele is dominant to the resistant gene. (nih.gov)
  • Taking quinolones may deplete good bacteria. (stlukes-stl.com)
  • T-3811" is a synthetic quinolone antibacterial agent developed by FUJIFILM Toyama Chemical Co., Ltd. and demonstrates antibacterial activity against drug-resistant bacteria such as multidrug-resistant Streptococcus pneumoniae. (fujifilm.com)
  • Veldman studied a specific type of resistance known as 'Plasmid Mediated Quinolone Resistance' (PMQR). (wur.nl)
  • Plasmid-mediated quinolone resistance (PMQR) was also increasingly identified in UPEC. (hindawi.com)
  • Quinolone resistance ( qnr ) is caused by several mechanisms which plasmid-mediated quinolone resistance (PMQR) is one of the most important of them. (hindawi.com)
  • However, emergence of plasmid-mediated quinolone resistance (PMQR) has been reported since 1998. (eurekaselect.com)
  • Quinolones are bactericidal and exhibit concentration-dependent killing. (cdc.gov)
  • Understanding the mechanisms underlying these differences could lead to new ways for identifying the most bactericidal quinolone derivatives. (asm.org)
  • Quinolones inhibit two enzymes that are required for bacterial DNA synthesis, i.e. (cdc.gov)
  • The chemical synthesis of quinolones often involves ring-closing reactions. (wikipedia.org)
  • For example, quinolones differ in rate and extent of killing, in the need for aerobic metabolism to kill cells, and in the effect of protein synthesis inhibitors on quinolone lethality. (asm.org)
  • The Vilsmeier approach had limited applicability in quinolone synthesis. (bl.uk)
  • Arayne MS, Sultana N, Ali SN (2013) Spectrophotometric Determination of Quinolones by Charge Transfer Complexation with Chloranilic Acid: Synthesis and Characterization. (omicsonline.org)
  • Quinolones are antimicrobial agents effective in the treatment of selected community-acquired and nosocomial infections. (cdc.gov)
  • Resistance to quinolones limits drug selection for treatment of many infections. (cdc.gov)
  • What is the role of quinolones and TMP-SMZ in the treatment of Enterobacter infections? (medscape.com)
  • Quinolones are a very important family of antibacterial agents that are widely prescribed for the treatment of infections in humans. (ingentaconnect.com)
  • His letter to the editor emphasizing the paramount importance of a well-established safety profile and documented clinical efficacy in severe infections before a "wholesale change" to the newer quinolones is an appropriate response to Michael Scheld's essay on maintaining quinolone class efficacy in which a "correct spectrum" strategy of using the most potent quinolone to treat the presumed or confirmed pathogen was described and advocated ( 1 ). (cdc.gov)
  • With respect to efficacy, Frothingham writes that ciprofloxacin and levofloxacin have been studied in patient populations with more severe illness, and trials of the newer quinolones have enrolled patients with predominantly mild or moderate community-acquired infections and low overall death rates in comparison. (cdc.gov)
  • Their broad spectrum of activity and pharmacokinetic properties make the quinolone agents ideal for treating a variety of infections. (cdc.gov)
  • Tokyo, July 25, 2019 ― FUJIFILM Corporation (President: Kenji Sukeno) announces the receipt *1 of an imported drug license for the oral synthetic quinolone antibacterial agent "T-3811" (generic name: garenoxacin mesilate hydrate) from the National Medical Products Administration (NMPA) of China with respiratory infections such as pneumonia. (fujifilm.com)
  • Les molécules utilisées dans le traitement des infections dues à cette bactérie, appartiennent à deux familles principalement : β-lactamines et quinolones. (ajol.info)
  • Herein we describe our discovery of quinolone derivatives, novel small-molecules that inhibit NS5b polymerase, a key enzyme of the viral life-cycle. (rcsb.org)
  • Quinolone carboxylic acid derivatives are synthetic antimicrobial agents. (merckvetmanual.com)
  • Reversibility can be used to distinguish among quinolone derivatives and assign functions to particular aspects of drug structure. (asm.org)
  • Gasser T.C., Larsen E.H., Dørflinger T., Madsen P.O. (1992) The Influence of Various Body Fluids and pH on E. Coli MIC of Quinolone Derivatives. (springer.com)
  • Instead of the desired target quinolone product, we identified two bis-fluoroinated derivatives, N,N'-bis-(4-fluoro- 3-nitrophenyl) oxalamide and N,N'-bis-(3-chloro-4-fluorophenyl) malonamide in solution phase. (bl.uk)
  • Type II Topoisomerases as Targets for Quinolone Antibacterials Tu. (ingentaconnect.com)
  • In addition to the antibacterial quinolones, specific members of this drug family display high activity against eukaryotic type II topoisomerases, as well as cultured mammalian cells and in vivo tumor models. (ingentaconnect.com)
  • Resistance studies revealed partial cross-resistance with fluoro-quinolones (FQs) suggesting that IPYs bind to the same region of bacterial topoisomerases as FQs and interact with at least some of the keys residues involved in FQ binding. (bioportfolio.com)
  • In a sense, quinolones trap the bacterial type II topoisomerases on DNA ( 17 , 23 , 73 , 75 ) (Fig. 1 , step b 2 ). (asm.org)
  • The inhibition of topo IV becomes apparent only when gyrase is mutated to quinolone resistance. (pnas.org)
  • For example, the quinolone nucleus contains a carboxylic acid group at position 3 and an exocyclic oxygen at position 4 (hence the term 4-quinolones), which are believed to be the active DNA-gyrase binding sites. (merckvetmanual.com)
  • The 7-bromoquinolone analogue, 7-bromo-6-(N-benzylpiperazin-1-yl)-4-oxo-3- quinolone carboxylic acid 91 showed the high potency as antibacterial inhibitor in addition to a significant effect on vitiligo phototherapy treatment. (bl.uk)
  • étudier la sensibilité des souches d' E. coli aux β-lactamines et quinolones. (ajol.info)
  • coli when it comes to quinolone resistance. (sid.ir)
  • Edited by one of the world's foremost authorities on the subject, the third edition of this highly successful title will serve as a valuable tool for primary care physicians and researchers interested in a comprehensive, up-to-date reference on the chemistry, mechanisms of action, development of resistance, and clinical efficacy of both currently available and newer quinolone compounds under investigation. (indigo.ca)
  • Mechanisms and Spectrum of Activity and Resistance, the first major section, explores the basic biology of the quinolone class. (cdc.gov)
  • Here we show that an A. thaliana mutant resistant to the quinolone drug ciprofloxacin has a point mutation in ATGYRA. (nih.gov)
  • The present invention is directed to a lyophilized preparation which contains a synthetic quinolone antibacterial compound and, as a solo additive, a pH-adjusting agent, and which exhibits an excellent reconstituting property. (patents.com)
  • The invention provides a method for producing a lyophilized preparation containing a synthetic quinolone antibacterial compound as an active ingredient, characterized by including, sequentially, cooling an aqueous solution containing a synthetic quinolone antibacterial compound and a pH-adjusting agent to yield a frozen product, elevating the temperature of the frozen product, and re-cooling the resultant to prepare the lyophilized preparation. (patents.com)
  • We show that the endochin-like quinolone (ELQ) class of compounds contains extremely potent inhibitors of T. gondii growth in vitro and is effective against acute and latent toxoplasmosis in mice. (pnas.org)
  • As the result, the new quinolone compounds obtained from Gosyuyu extracts were found to be a mixture of two quinolone alkaloids, 1-methyl-2-[(Z)-8-tridecenyl]-4-(1H)-quinolone and 1-methyl-2-[(Z)-7-tridecenyl]-4-(1H)-quinolone (MW: 339), reported previously. (greenmedinfo.com)
  • Two different pH values were used for the extraction of compounds (pH 3 for acidic quinolones and β-lactams and pH 8 for amphoteric quinolones). (sigmaaldrich.com)
  • The constant need for new anti microbials has produced a variety of newer quinolones termed as I, II, III, and IV generation. (nih.gov)
  • Although generally well tolerated, the quinolones can cause some serious adverse effects and the adverse effect profiles of these newer quinolones are not identical. (ovid.com)
  • All of the newer quinolones are effective against a wide range of organisms and will need to be used with care in an attempt to minimise the emergence of resistance to these agents. (ovid.com)
  • Activity of the newer quinolones against Chlamydia trachomatis. (bmj.com)
  • Most cephalosporins, except for Rocephin, need to be administered every eight hours, while the newer quinolones are administered once daily. (managedcaremag.com)
  • It has also been shown that the newer more potent quinolone drugs such as ciprofloxacin and ofloxacin have an additional effect on the bacterial cells in that the chromosome is broken down into fragments of DNA, some of which are estimated to be as small as 4kb in length. (bl.uk)
  • In the next section, Pharmacology, the intricate field of quinolone pharmacokinetics (PK) and pharmacodynamics (PD) is evaluated. (cdc.gov)
  • Structural development, haematological immunological and pharmacological effects of quinolones. (nih.gov)
  • The thrust of this review is on the structural development, pharmacological, haematological and immunological effects of quinolones. (nih.gov)
  • Effects of Quinolones on the Immune System, p 467-473. (asmscience.org)
  • Synergic effect of quinolone antibacterial agents and proton pump inhibitors on Helicobacter pylori ," Journal of Antimicrobial Chemotherapy , vol. 49, no. 6, pp. 1039-1040, 2002. (hindawi.com)
  • A systematic review and meta-analysis assessing the safety of quinolone exposure during any time of pregnancy, and during first trimester alone, was performed. (springer.com)
  • Tendon damage: "Ruptures of the shoulder, hand, Achilles tendon, or other tendons that require surgical repair or resulted in prolonged disability have been reported in patients receiving quinolones. (wikidoc.org)
  • Multiclass method for the determination of quinolones and β-lactams, in raw cow milk using dispersive liquid-liquid microextraction and ultra high performance liquid chromatography-tandem mass spectrometry. (sigmaaldrich.com)
  • These were characterised using the genotypic methods of Plasmid Profile Analysis and Pulsed Field Gel Electrophoresis and levels of resistance were determined for quinolone and fluoroquinolone antimicrobials by the agar dilution method. (gla.ac.uk)
  • Extensive pharmacologic and clinical development of quinolone antimicrobial agents has resulted in improved antimicrobial activity, pharmacokinetic features, toxicity, and drug-drug interaction profiles. (nih.gov)
  • Within the diversity of their various ring structures, the quinolones have a number of common functional groups essential for their antimicrobial activity. (merckvetmanual.com)
  • The interrelationships between structure, antimicrobial activity, and side effects associated with various side chain positions of the quinolone are discussed here. (cdc.gov)
  • Because of increasing resistance, quinolones (eg, ciprofloxacin 500 mg PO single dose, levofloxacin 250 mg PO single dose, or ofloxacin 400 mg PO single dose) are not currently recommended by the Centers for Disease Control and Prevention (CDC) for routine or alternative regimens. (medscape.com)
  • These agents have extended spectra of antibacterial activity compared with the earlier quinolones such as ciprofloxacin and ofloxacin. (ovid.com)
  • Liquid formulations of various quinolones for PO or parenteral administration usually contain freely soluble salts in stable aqueous solutions. (merckvetmanual.com)
  • This is one of the conclusions of a thesis entitled 'Plasmid mediated quinolone resistance in Enterobacteriaceae' by Kees Veldman, a researcher at CVI. (wur.nl)
  • Vincent Cattoir and Patrice Nordmann, " Plasmid-Mediated Quinolone Resistance in Gram-Negative Bacterial Species: An Update", Current Medicinal Chemistry (2009) 16: 1028. (eurekaselect.com)
  • Organisms resistant to quinolones often are resistant to other classes of antimicrobials. (cdc.gov)
  • Evaluates the in vitro activity of seven quinolones against non-glucose fermenting Gram-negative bacilli isolated from clinical specimens of cancer patients. (ebscohost.com)
  • The in vitro activity of eight antimicrobial agents, including four quinolones, against 108 strains of enteropathogens was determined. (eurekamag.com)
  • New quinolones are continually being developed as bacterial species develop resistance to existing quinolones. (indigo.ca)
  • The last several years have seen dramatic uptake of all 3 respiratory quinolones. (cdc.gov)
  • However, the incidence of torsades de pointes associated with each of these agents is ripe for further investigation as we pass the 5-year mark of approval for the new respiratory quinolones. (cdc.gov)
  • Both enzymes use a double-strand DNA passage mechanism, and it is likely that quinolone biochemistry is similar for both. (asm.org)
  • However, physiological differences between the enzymes exist, some of which may bear on quinolone lethality. (asm.org)
  • Quinolones have been known to have damaging effects on collagen and other structural components of the extracellular matrix by inducing matrix metalloproteinases, enzymes thought to be involved in the pathogenesis of aortic aneurysms. (mims.co.uk)
  • In his article, Frothingham reminds us that serious adverse drug effects in patients led to the withdrawal or restriction of 4 quinolones in the last decade and that safety may differ substantially among the quinolones discussed in Scheld's review (ciprofloxacin, gatifloxacin, levofloxacin, moxifloxacin) ( 2 ). (cdc.gov)
  • Adverse effects in general were similar between macrolides and quinolones. (ersjournals.com)
  • Administration of A/C was associated with more adverse effects (mainly diarrhoea) than quinolones (OR 1.36, 95% CI 1.01-1.85). (ersjournals.com)
  • Quinolones are associated with better microbiological success and fewer recurrences of acute bacterial exacerbation of chronic bronchitis than macrolides, while amoxicillin/clavulanate is associated with more adverse effects than both comparators. (ersjournals.com)