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 ...
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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.. ...
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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
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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.
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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
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Spectrophotometric Determination of Quinolones by Charge Transfer Complexation with Chloranilic Acid: Synthesis and Characterization Abstract.
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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. ...
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Aripiprazole is an injected drug available only from a licensed physician that is used primarily to treat agitation experienced by patients
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An antibiotic of the quinolone family, Bayer HealthCares Baytril (enrofloxacin) fights a broad range of bacterial and fungal infections in dogs and cats.
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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
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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 ...
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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 ...
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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.
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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.
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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.
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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. ...
... 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, ...
... at Curlie Healthcare-associated Infections (HAIs)- Quinolones and the Clinical Laboratory CDC Information ... 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 bacteriocidals that share a bicyclic core structure ... Quinolones should also not be given to people with a known hypersensitivity to the drug class. The basic pharmacophore, or ...
The isomer 4-quinolone is the parent of a large class of quinolone antibiotics. One example is Ravesilone. Tashima, Toshihiko ( ... 2-Quinolone is an organic compound related structurally to quinoline. It is the majority tautomer in equilibrium with 2- ... Media related to 2-Quinolone at Wikimedia Commons (Articles needing additional references from July 2017, All articles needing ...
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 ...
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): ...
... 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/mmbr.61.3.377-392.1997. PMC 232616. PMID 9293187. ...
Quinolones Rubinstein E (2001). "History of quinolones and their side effects". Chemotherapy. 47 Suppl 3 (3): 3-8, discussion ...
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 2012 study has shown that the presence of Enterobacter cloacae B29 in the gut of ...
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 ...
For example, WIN 18,320 was nalidixic acid, the first quinolone antibiotic. The Company was established in 1901 (then called ... "The Quinolones: Decades of Development and Use". Journal of Antimicrobial Chemotherapy. 51 (Suppl 1): 13-20. doi:10.1093/jac/ ...
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. (2001). "History of quinolones and their side effects". Chemotherapy. 47 Suppl 3 (3): 3-8, discussion 44-8. doi: ...
6). Quinolone antibacterial compounds were first developed in the 1960s and have been in clinical use since the 1980s. FQ ... Maxwell A, Bush NG, Germe T, McKie SJ (2018). "Non-quinolone topoisomerase inhibitors". In Fong IW, Drlica K (eds.). ... Bush NG, Diez-Santos I, Abbott LR, Maxwell A (December 2020). "Quinolones: Mechanism, Lethality and Their Contributions to ...
Praziquantel, a quinolone derivative. The effect of praziquantel on H. heterophyes causes deep lesions on their teguments, and ...
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 ...
Commonly referred to as the first generation quinolones. This first generation also included other quinolone drugs such as ... Cinoxacin is a quinolone antibiotic that has been discontinued in the U.K. as well the United States, both as a branded drug or ... Cinoxacin was an older synthetic antimicrobial related to the quinolone class of antibiotics with activity similar to oxolinic ... Drlica K, Zhao X (September 1997). "DNA gyrase, topoisomerase IV, and the 4-quinolones". Microbiology and Molecular Biology ...
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 ...
Use of quinolones in food animals and potential impact on human health : report of a WHO meeting, Geneva, Switzerland, 2-5 June ... Use of quinolones in food animals and potential impact on human health : report and proceedings of a WHO meeting, Geneva, ...
In summary, differences in quinolone safety are evidenced by labeling changes to gatifloxacin, the only quinolone to carry a ... to the newer quinolones is an appropriate response to Michael Schelds essay on maintaining quinolone class efficacy in which a ... Quinolone safety and efficacy more important than potency. Emerg Infect Dis. 2004;10:156-7.PubMedGoogle Scholar ... Quinolone Safety and Efficacy. Volume 11, Number 6-June 2005. Article Views: 133. Data is collected weekly and does not include ...
Quinolones - Reference pathway ...
Unexpected Occurrence of Plasmid-Mediated Quinolone Resistance Determinants in Environmental Aeromonas spp. Vincent Cattoir ... Unexpected Occurrence of Plasmid-Mediated Quinolone Resistance Determinants in Environmental Aeromonas spp.. ...
The endochin-like quinolone (ELQ) compound class may yield effective, safe treatments for a range of important human and animal ... The endochin-like quinolone (ELQ) compound class may yield effective, safe treatments for a range of important human and animal ... New Scalable Synthetic Routes to ELQ-300, ELQ-316, and Other Antiparasitic Quinolones. 26 Sep 2021 ... New Scalable Synthetic Routes to ELQ-300, ELQ-316, and Other Antiparasitic Quinolones ...
Quinolones for community-acquired pneumonia. Journal Article (Letter) Full Text. *Published version (via Digital Object ...
One quinolone-sensitive lac− isolate was also included as a negative control. Of the twenty-eight quinolone resistant isolates ... 2011) Plasmid mediated quinolone resistance: an update. J Infect Chemother 17:149-182.). The main mechanism of quinolone ... 2002) Are Quinolone-Resistant Uropathogenic Escherichia coli Less Virulent? J Infect Dis 186:1039-1042. related quinolone ... 2006) Correlation of quinolone resistance levels and differences in basal and quinolone-induced expression from three qnrA- ...
But, mannich bases 13a,b obtained from the reaction of the oxadiazole compound with the quinolone showed strong activities. ... Zhang GF, Zhang S, Pan B, Liu X, Feng LS (2018) 4-Quinolone derivatives and their activities against Gram positive pathogens. ... Sissi C, Palumbo M (2003) The quinolone family: from antibacterial to anticancer agents. Curr Med Chem Anticancer agents 3:439- ... The cytotoxic activity of quinolone derivatives has become the source of new anticancer agents, which might also help ...
... , Chemical Communications, January 1996, Royal ...
Some quinolones have been found in food products including fish and shrimp. Primesep 100 was used to separate a mixture of ... Quinolones are a group of synthetic broad-spectrum antibiotics with a wide variety of applications in medicine and veterinary ... Drug, Acid, Quinolone Antibiotics, Hydrophilic, Ionizable, Vitamin, Supplements. Analyzing Compounds. Oxolinic Acid, Flumequine ... quinolones and achieve baseline separation. Retention was controlled by adjusting acetonitrile in the mobile phase. Condition. ...
This study identified quinolone resistance (qnr) gene in ESBL-producing E. coli and Klebsiella spp. in Togo. These finding ... strains with phenotypic resistance to quinolone were collected from several specimens and analyzed for the detection of qnrA, ... which suggest a possible resistance to quinolone are of high interest for better management of patients and control of ... Distribution of quinolone resistance gene (qnr) in ESBL-producing Escherichia coli and Klebsiella spp. in Lomé, Togo. Access & ...
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The quinolone in the ester mask: Doggett et al. adopt a prodrug approach to reduce Toxoplasma gondii brain cysts ... Tags: #toxoplasmosis, antimalarial, endochin-like quinolone, pharmacokinetics, prodrug, toxoplasma gondii Posted on: 10 April ... 2] Winter R, Kelly JX, Smilkstein MJ, Hinrichs D, Koop DR, Riscoe MK, Optimization of endochin-like quinolones for antimalarial ... About a decade earlier, endochin-like quinolones (ELQ) were found to inhibit apicomplexan pathogens, including T. gondii [1] ...
48, 49] The use of the quinolones is restricted in growing children and pregnancy because of their possible adverse effects on ... Quinolones. Trovafloxacin, moxifloxacin, and gatifloxacin yield low minimum inhibitory concentrations (MICs) against most ...
Latham E, Stanforth S. Synthesis of indoles and quinolones by sequential Wittig and Heck reactions. Chemical Communications. ... Synthesis of indoles and quinolones by sequential Wittig and Heck reactions. In: Chemical Communications. 1996 ; No. 19. pp. ... Latham, E., & Stanforth, S. (1996). Synthesis of indoles and quinolones by sequential Wittig and Heck reactions. Chemical ... Latham, E & Stanforth, S 1996, Synthesis of indoles and quinolones by sequential Wittig and Heck reactions, Chemical ...
Quinolones. Doctors prescribe quinolones for difficult-to-treat UTIs, hospital-acquired pneumonia, and bacterial prostatitis. ... Aldred, K. J., et al. (2014). Mechanism of quinolone action and resistance.. https://www.ncbi.nlm.nih.gov/pmc/articles/ ...
... , Home , , Medicinal Chemistry , Chapter: Medicinal Chemistry : Quinolone Antibacterials. The optimum ... 6. The incorporation of a fluorine atom at the C-6 position of the quinolone is monumental. The order of activity is F,Cl, Br, ... 4. The C-4-oxo group of the quinolone nucleus appears to be essential for antibacterial activity. Replacement with 4-thioxo or ... Some side effects of the quinolones are class effects and cannot be modulated by molecular variation. Most of the ...
Shigella and the fluorinated quinolones. Indian Journal of Pathology & Microbiology. 1998 Oct; 41(4): 453-6. ...
Quinolones. Rifabutin. Clofazimine. Combination of beta-Lactam Antibiotics and beta-Lactamase Inhibitors. The New Macrolides. ... Because the quinolones have been shown to cause arthropathies in studies with immature animals, these drugs should only be used ... Quinolones. A number of fluoroquinolones have been developed that show in vitro activity against M. tuberculosis. The target of ... The quinolones are primarily cleared by renal excretion, and the dosage should be adjusted for those with creatinine clearance ...
Quinolones Erythromycin Combo Test can qualitatively and quantitatively detect quinolones and erythromycin residues in raw milk ... 1. What is quinolones erythromycin combo test?. 2. What are quinolones?. 3. What is erythromycin?. 4. The harm of quinolones ... Materials for Quinolones Erythromycin Combo Test. 12. How to use Quinolones Erythromycin Combo Test?. 13. Summary. 14. How to ... 5. Features of Quinolones Erythromycin Combo Test. 6. Detection Method of Quinolones Erythromycin Combo Test. 7. Samples for ...
Quinolone antibiotics. These drugs can increase the effect of glimepiride and cause low blood sugar. Examples of these drugs ...
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Efflux of novel quinolones in contemporary Streptococcus pneumoniae isolates from community-acquired pneumonia. In: Journal of ... Renaissance of antibiotics against difficult infections: Focus on oritavancin and new ketolides and quinolones.. In: Annals of ... Selection of quinolone resistance in Streptococcus pneumoniae exposed in vitro to subinhibitory drug concentrations. In: ... Cellular accumulation and activity of quinolones in ciprofloxacin-resistant J774 macrophages. In: Antimicrobial Agents and ...
This ELISA Kit is based on indirect competitive ELISA to detect quinolones in sample within 75 minutes. Sensitivity 0.05ng/mL, ... Decrease quantity for Quinolones ELISA Kit Increase quantity for Quinolones ELISA Kit ... This ELISA Kit is based on indirect competitive ELISA to detect quinolones in sample within 75 minutes. ...
The analysis of tetracyclines, sulfonamides, macrolides, and quinolones in the sewage samples were performed as in Beredsen et ... quinolones, and macrolides. Four mL of EDTA-McIlvain buffer (0.1 M, pH 4.0) were added, after which the samples were shaken for ... Quin quinolone). d Relative abundance of the 15 most common AMR genes (mef(A)_10: mef(A)_10_AF376746) ... Quin quinolone). Colors represent log (ln) transformed relative abundances (FPKM). Complete-linkage clustering of Pearson ...
The first quinolone (quinol[ine] + -one [compoundrelated to ketone]), nalidixic acid, was isolated as a byproduct of ... Quinolone. The first quinolone (quinol[ine] + -one [compoundrelated to ketone]), nalidixic acid, was isolated as a byproduct of ... In 1980, researchers at the Kyorin Pharmaceutical Company showed that the addition of a fluorine atom to the quinolone ring ...
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  • Quinolones are a group of synthetic broad-spectrum antibiotics with a wide variety of applications in medicine and veterinary sciences. (sielc.com)
  • Ciprofloxacin belongs to a class of drugs called quinolone antibiotics. (mynextgenrx.com)
  • Tibebu M, Shibabaw A, Medhin G, Kassu A. Neisseria gonorrhoeae non-susceptible to cephalosporins and quinolones in Northwest Ethiopia. (healthdata.org)
  • Two-Sensor Kit, rapid to detect quinolones and erythromycin residues in milk and dairy product by using colloidal gold immune-chromatography technology. (ballyabio.com)
  • This ELISA Kit is based on indirect competitive ELISA to detect quinolones in sample within 75 minutes. (antibodymall.com)
  • 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)
  • The first quinolone drug, nalidixic acid, was accidentally discovered in 1962, and it was applied clinically because of its unique antibacterial characteristics. (ballyabio.com)
  • The first and second generation quinolone drugs such as nalidixic acid and pipemidic acid, because their antibacterial spectrum is limited to gram-negative intestinal bacilli, are clinically limited to the treatment of urinary tract infections and intestinal infections. (ballyabio.com)
  • The first quinolone (quinol[ine] + -one [compoundrelated to ketone]), nalidixic acid, was isolated as a byproduct of chloroquine (see "quinine") synthesis and was introduced in 1962 to treat urinary tract infections. (metymology.ch)
  • The Pseudomonas quinolone signal (PQS) is an important quorum-sensing molecule for Pseudomonas aeruginosa that regulates virulence factors, chelates iron, and is an important factor in interactions with eukaryotes, including fungi and mammalian hosts. (omicsdi.org)
  • Enzyme-Mediated Quenching of the Pseudomonas Quinolone Signal (PQS) Promotes Biofilm Formation of Pseudomonas aeruginosa by Increasing Iron Availability. (omicsdi.org)
  • The 2-alkyl-3-hydroxy-4(1H)-quinolone 2,4-dioxygenase HodC was previously described to cleave the Pseudomonas quinolone signal, PQS, which is exclusively used in the complex quorum sensing (QS) system of Pseudomonas aeruginosa, an opportunistic pathogen employing QS to regulate virulence and biofilm development. (omicsdi.org)
  • In this context, we investigated whether the Pseudomonas quinolone signal (PQS) which is a quorum sensing molecule produced by bacteria and participates in biofilm formation and virulence has any influence on polymorphonuclear neutrophils (PMN), the cells of the "first line defense" against bacterial infections. (kit.edu)
  • Quinolones are antimicrobial agents effective in the treatment of selected community-acquired and nosocomial infections. (cdc.gov)
  • In 1980, researchers at the Kyorin Pharmaceutical Company showed that the addition of a fluorine atom to the quinolone ring resulted in an antibiotic with broader antimicrobial activity, which was named norfloxacin, the first fluo-roquinolone. (metymology.ch)
  • Quinolones inhibit two enzymes that are required for bacterial DNA synthesis, i.e. (cdc.gov)
  • Latham, E & Stanforth, S 1996, ' Synthesis of indoles and quinolones by sequential Wittig and Heck reactions ', Chemical Communications , no. 19, pp. 2253-2254. (northumbria.ac.uk)
  • Five genes ( pqsA-E ) are involved in the synthesis of 2-heptyl-4(1H)-quinolone (HHQ). (springeropen.com)
  • Resistance to quinolones occurs through chromosomal mutations in the genes encoding these enzymes and by porin and efflux mutations. (cdc.gov)
  • Cattoir V , Poirel L , Rotimi V , Soussy CJ , Nordmann P . Multiplex PCR for detection of plasmid-mediated quinolone resistance qnr genes in ESBL-producing enterobacterial isolates. (cdc.gov)
  • To synthesize HHQ in a microbial system, pqsA-E genes were introduced into Escherichia coli and HHQ and 2-methyl-4(1H)-quinolone (MHQ) were synthesized. (springeropen.com)
  • Frequency of Plasmid-Mediated Quinolone Resistance Genes qnrA , qnrB , and qnrS among Clinical Isolates of Klebsiella pneumoniae ', Journal of Applied Biotechnology Reports , 7(4), pp. 203-207. (biotechrep.ir)
  • To determine the current antibiotic resistance patterns and identification of quinolone and ceftriaxone resistant genes among Salmonella enterica subspecies serovar Typhi. (org.pk)
  • All isolates were subjected for identification of genes responsible for quinolone and ceftriaxone resistance using polymerase chain reaction followed by gel-electrophoresis. (org.pk)
  • Genotypically, blaCTX-M-15 (beta lactamase, CTX as its acronym, -M from Munich) gene for ceftriaxone resistance was found in all phenotypically resistant 31(32.29%) isolates, while QnrS (Quinolone resistance, S group), GyrA (DNA gyrase subunit A), and GyrB (DNA gyrase subunit B) genes responsible for ciprofloxacin resistance were found in different frequencies (percentages given in table 2). (org.pk)
  • The bacteria designated by the acronym SERMOR-PROVENF (SER = Serratia, MOR = Morganella, PROV = Providencia, EN = Enterobacter, F = freundii for Citrobacter freundii ) have similar, although not identical, chromosomal beta-lactamase genes that are inducible. (medscape.com)
  • The emergence of quinolone-resistant S. pneumoniae (QRSP) appears to be more dependent on fluoroquinolone selection of de novo spontaneous point mutations in the quinolone resistance-determining regions (QRDRs) of the topoisomerase genes gyrA and parC than on clonal dissemination (9-13). (cdc.gov)
  • A high percentage of the isolates (48.3%) was found to be resistant to at least one of the tested quinolones, and DNA sequencing revealed quinolone resistant determining region gyrA and parC mutations in the multi-resistant isolates. (scielo.br)
  • A total of 88 K. pneumoniae isolates assessed to quinolone which were obtained from Tehran hospital in Tehran, Iran. (biotechrep.ir)
  • Among them, levofloxacin and moxifloxacin are also called respiratory quinolones, because they have significantly enhanced antibacterial activity against common respiratory pathogens such as Streptococcus pneumoniae, and have good antibacterial activity against atypical pathogens such as Mycoplasma pneumoniae and Chlamydia pneumoniae. (ballyabio.com)
  • Fluoroquinolone resistance in Streptococcus pneumoniae is primarily mediated by point mutations in the quinolone resistance-determining regions of gyrA and parC . (cdc.gov)
  • To investigate the fitness of quinolone-resistant S. pneumoniae (QRSP), the relative growth efficiencies of 2 isogenic QRSP double mutants were compared with that of their fluoroquinolone-susceptible parent, EF3030, by using murine nasopharyngeal colonization and pneumonia models. (cdc.gov)
  • 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)
  • Quinolones and fluoroquinolones are widely used to treat uropathogenic Escherichia coli infections. (scielo.br)
  • Escherichia coli is the main agent of UTIs, especially in community-acquired UTIs, and quinolones and fluoroquinolones have been used extensively to treat these infections ( Ronald, 2003 Ronald A (2003) The etiology of urinary tract infection: traditional and emerging pathogens. (scielo.br)
  • Distribution of quinolone resistance gene (qnr) in ESBL-producing Escherichia coli and Klebsiella spp. (biomedcentral.com)
  • Interaction of the plasmid-encoded quinolone resistance protein Qnr with Escherichia coli DNA gyrase. (cdc.gov)
  • Identify known and potential links between the emergence and spread of quinolone resistance from food-borne and other possible zoonotic bacteria, and human zoonotic infection. (who.int)
  • The worldwide emergence of plasmid-mediated quinolone resistance. (cdc.gov)
  • It is for qualitative detection of quinolones, macrolides, lincomycin, erythromycin in foods and other biological samples. (foodtestkit.com)
  • 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)
  • Currently, with the exception of ciprofloxacin, each of these quinolones contains labeling guidance in the form of a warning (gatifloxacin, moxifloxacin) or a precaution (levofloxacin), and concurrent use with class IA (e.g., quinidine, procainamide) or class III (e.g., amiodarone, sotalol) antiarrhythmics should be avoided to reduce the risk of torsades de pointes per current product labeling. (cdc.gov)
  • Maybe, has pdf use of quinolones in travel medicine second conference on international travel medicine proceedings of the ciprofloxacin satellite symposium use of quinolones in travel medicine 1992 comprehensive for engineering of invalid mechanics used with a manner city or t, or I should walk another extent History? (newanglepet.com)
  • The pdf use of quinolones in travel medicine second conference on international travel medicine proceedings of the ciprofloxacin satellite symposium use of quinolones you do heading for makes increasingly need! (newanglepet.com)
  • 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)
  • N-Trifluoroacetylanilines 6 and 7 undergo a Wittig reaction with phosphorane 2 (R = Et) giving enamine derivatives 9 and 10 respectively which are precursors to indoles 4 and quinolones 5. (northumbria.ac.uk)
  • Organisms resistant to quinolones often are resistant to other classes of antimicrobials. (cdc.gov)
  • Many resistant organisms have multiple enzyme target site, porin, and efflux mutations, producing high-level resistance to quinolones. (cdc.gov)
  • Can an isolate be resistant to one quinolone and susceptible to another? (cdc.gov)
  • 3 However, other studies also show an alarming increase in quinolone-resistant E. coli 4 intrinsic third-generation cephalosporin resistant Enterococcus faecium 5 and Candida spp. (turkishjcrd.com)
  • Poirel L , Rodriguez-Martinez JM , Mammeri H , Liard A , Nordmann P . Origin of plasmid-mediated quinolone resistance determinant QnrA. (cdc.gov)
  • Doctors prescribe quinolones for difficult-to-treat UTIs, hospital-acquired pneumonia , and bacterial prostatitis . (medicalnewstoday.com)
  • About a decade earlier, endochin-like quinolones (ELQ) were found to inhibit apicomplexan pathogens, including T. gondii [1] and Plasmodium falciparum [2]. (biologists.com)
  • use of quinolones and resistance in humans production, licensing and use of quinolones for food animals links between quinolone resistance in food animal bacteria and human disease. (who.int)
  • Alkyl-4-quinolones (AQs) are natural compounds synthesized by bacteria. (springeropen.com)
  • Quinolone arthropathy in juvenile New Zealand white rabbits. (cdc.gov)
  • The authors conclude that the quinolone arthropathy induced in rabbits in the present study is consistent with that seen in other experimental animals and represents a good model of osteoarthritis in humans. (cdc.gov)
  • Quinolone drugs are a new type of chemically synthesized antibacterial drugs. (ballyabio.com)
  • Jacoby GA , Walsh KE , Mills DM , Walker VJ , Oh H , Robicsek A , qnrB , another plasmid-mediated gene for quinolone resistance. (cdc.gov)
  • IMSEAR at SEARO: Shigella and the fluorinated quinolones. (who.int)
  • Hata M , Suzuki M , Matsumoto M , Takahashi M , Sato K , Ibe S , Cloning of a novel gene for quinolone resistance from a transferable plasmid in Shigella flexneri 2b. (cdc.gov)
  • To date, no studies have examined the potential relationship between biochemical characteristics and quinolone resistance in uropathogenic E. coli strains. (scielo.br)
  • The present work analyzed the quinolone sensitivity and biochemical activities of fifty-eight lactose-negative uropathogenic E. coli strains. (scielo.br)
  • Using this engineered E. coli strain, both HHQ and an unexpected product, MHQ (2-methyl-4(1H)-quinolone), were synthesized. (springeropen.com)
  • However, replacement of C-3 carboxylic group with isothiazolo group afforded most active isothiazolo quinolone, which has been 4-10 times greater in in vitro antibacterial activity than ciprofloxacin. (pharmacy180.com)
  • 4. The C-4-oxo group of the quinolone nucleus appears to be essential for antibacterial activity. (pharmacy180.com)
  • Resistance to quinolones limits drug selection for treatment of many infections. (cdc.gov)
  • Salmonella and Campylobacter ) has already been reported, but the scope of the problems still needs to be identified and the links between quinolone use in animals and the occurrence of problems in infectious disease treatment in humans elucidated. (who.int)
  • Review the conditions and extent of use of the various quinolones in humans and in food animals. (who.int)
  • 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)
  • Unexpected Occurrence of Plasmid-Mediated Quinolone Resistance Determinants in Environmental Aeromonas spp. (cdc.gov)
  • The targets of quinolone activity are the bacterial DNA gyrase and topoisomerase IV, enzymes essential for DNA replication and transcription. (cdc.gov)
  • Statistical analyses suggested that the lack of ornithine decarboxylase (ODC) activity is correlated with quinolone resistance. (scielo.br)
  • Tentative identification of 2-quinolones in asphalt and their interaction with carboxylic acids present. (cdc.gov)
  • 6. The incorporation of a fluorine atom at the C-6 position of the quinolone is monumental. (pharmacy180.com)
  • Martinez-Martinez L , Pascual A , Garcia I , Tran J , Jacoby GA . Interaction of plasmid and host quinolone resistance. (cdc.gov)
  • The endochin-like quinolone (ELQ) compound class may yield effective, safe treatments for a range of important human and animal afflictions. (mmv.org)
  • Some side effects of the quinolones are class effects and cannot be modulated by molecular variation. (pharmacy180.com)
  • Quinolones are bactericidal and exhibit concentration-dependent killing. (cdc.gov)
  • In the current study, none of the tested quinolones (QNs) at any of the examined concentrations were lethal for common duckweed plants . (bvsalud.org)