Induced by fluoroquinolone antibiotics gyrase and topoisomerase fluoroquinolones. Medical search. Frequent questions

Fluoroquinolones, including levofloxacin, may exacerbate muscle weakness in patients with myasthenia gravis. (nih.gov)
Levofloxacin is a fluoroquinolone antibacterial indicated in adults (18 years of age and older) with infections caused by designated, susceptible bacteria and in pediatric patients where indicated (1, 12.4). (nih.gov)
We demonstrated that Escherichia coli cells exposed to levofloxacin (LVFX), a fluoroquinolone (FQ), induce the syntheses of heat shock proteins and RecA. (biomedcentral.com)
To analyze the role of DNA gyrase in quinolone resistance of B. fragilis, we isolated mutant strains by stepwise selection for resistance to increasing concentrations of levofloxacin. (omicsdi.org)
Based on data on other fluoroquinolones and very limited data on levofloxacin, it can be presumed that levofloxacin will be excreted in human milk. (drugcentral.org)
Levofloxacin and sparfloxacin are examples of third generation quinolones, also known as fluoroquinolones, but they are more effective against gram-positives organism. (hindawi.com)
As a fluoroquinolone antibacterial agent, levofloxacin inhibits bacterial type II topoisomerases-DNA gyrase and topoisomerase IV. (medico-labs.com)
Levofloxacin preferentially targets DNA gyrase in Gram-negative bacteria and topoisomerase IV in Gram-positive bacteria. (medico-labs.com)
Tendon inflammation and rupture may occur with systemic fluoroquinolone therapy including levofloxacin, particularly in older patients and those treated concurrently with corticosteroids. (medico-labs.com)

Antibiotics are often used in clinical in vitro tests known as antimicrobial susceptibility tests or ASTs to determine their efficacy against certain bacterial species. (goldbio.com)
A nitro imidazole derivative, Antiprotozoal antibiotic,Antimicrobial. (medicineindia.org)
Gemifloxacin is a fluoroquinolone antibiotic with the antimicrobial property. (illnesshacker.com)
According to the results of antimicrobial susceptibilities, 76.32% (29/38) of S. dysenteriae isolates were resistant to fluoroquinolone and showed multidrug resistance. (researchsquare.com)
Our analysis includes the antimicrobial resistance profiles, the molecular characterization of the mechanisms of resistance to fluoroquinolones, virulence gene profiles and the molecular characterization of S. dysenteriae isolates by pulsed-field gel electrophoresis (PFGE) and multilocus sequence typing (MLST). (researchsquare.com)
The antibiotic minimum inhibitory concentration (MIC) was determined for ten antimicrobial compounds, along with the minimum biofilm inhibitory concentration (MBIC) and minimum biofilm eradication concentration (MBEC), followed by PCR identification of genetic determinants of biofilm production and antimicrobial resistance. (biomedcentral.com)

Now fluoroquinolones are broad spectrum bactericidal antibiotics and ciprofloxacin in particular is widely used. (osmosis.org)
Although cross-resistance can occur between gemifloxacin and other fluoroquinolones, gemifloxacin may be active against some strains of S. pneumoniae resistant to ciprofloxacin and other fluoroquinolones. (illnesshacker.com)
Ciprofloxacin has been found to affect mammalian topoisomerase II, especially in mitochondria. (hormonesmatter.com)
Further analysis found protein-linked double-stranded DNA breaks in the mtDNA from ciprofloxacin-treated cells, suggesting that ciprofloxacin was targeting topoisomerase II activity in the mitochondria. (hormonesmatter.com)
6 Fluoroquinolone, especially ciprofloxacin, was the first-line antibiotic for the treatment of shigellosis as recommended by the WHO. (researchsquare.com)
Increased susceptibility of all the tested isolates to ciprofloxacin and norfloxacin in the presence of the pump inhibitor implies that efflux pumps contributed to the resistance against fluoroquinolones. (ophrp.org)
Expression of the efflux pump-related genes, tolC , mdfA , and ydhE , were induced in isolates EACR 07, EACR 29, and EACR 33 in the presence of ciprofloxacin. (ophrp.org)
Ciprofloxacin is a fluoroquinolone anti-infective agent. (antiinfectivemeds.com)
If acute overdosage of ciprofloxacin occurs, the stomach should be emptied by inducing emesis or by gastric lavage. (antiinfectivemeds.com)
Like other fluoroquinolone anti-infectives, ciprofloxacin inhibits DNA synthesis in susceptible organisms via inhibition of the enzymatic activities of 2 members of the DNA topoisomerase class of enzymes, DNA gyrase and topoisomerase IV. (antiinfectivemeds.com)

There are plenty of processes and enzymes involved that we can target and the quinolones and fluoroquinolones inhibit an enzyme called DNA topoisomerase. (osmosis.org)
Now, quinolones are created to target bacterial topoisomerases, but it was soon discovered that by adding a fluorine molecule to the quinolones, they become more effective. (osmosis.org)
So these newer medications, called fluoroquinolones, replaced the older quinolones in most clinical settings. (osmosis.org)
A second generation fluoroquinolone(quinolones), Antibiotic. (medicineindia.org)
EAEC strains are known to be highly resistant to antibiotics including quinolones. (ophrp.org)
Mutagenesis in the alpha3alpha4 GyrA helix and in the Toprim domain of GyrB refines the contribution of Mycobacterium tuberculosis DNA gyrase to intrinsic resistance to quinolones. (omicsdi.org)
These results suggest that DNA gyrase is an important target for quinolones in B. fragilis. (omicsdi.org)

The discovery of an allosteric binding site on the established antibacterial target DNA gyrase offers a new medicinal chemistry strategy. (bvsalud.org)

Fluoroquinolones are a group of broad-spectrum antibiotics that inhibit DNA synthesis. (goldbio.com)
Gemifloxacin acts by inhibiting DNA synthesis through the inhibition of both DNA gyrase and topoisomerase IV, which are essential for bacterial growth. (illnesshacker.com)
Like other fluoroquinolone anti-infective agents, gemifloxacin inhibits DNA synthesis in susceptible organisms via inhibition of type II DNA topoisomerases (DNA gyrase, topoisomerase IV). (illnesshacker.com)
A broad-spectrum carbapenem antibiotic, meropenem inhibits cell wall synthesis and has bactericidal activity. (medscape.com)
Fluoroquinolones inhibit bacterial DNA synthesis and, consequently, growth by inhibiting DNA gyrase and topoisomerases, which are required for replication, transcription, and translation of genetic material. (medscape.com)
These proteins were also induced by lower concentrations of LVFX, but increasing concentrations increased the rate of synthesis. (biomedcentral.com)
Levofla kills bacteria by turning two bacterial enzymes, topoisomerase IV and DNA gyrase, into harmful enzymes that impair DNA synthesis and repair, as well as other DNA activities, thereby killing the bacterium. (healthsoothe.com)

All 29 fluoroquinolone-resistant isolates were positive for the aac(6')-Ib-cr gene but negative for qepA , except SD001. (researchsquare.com)
The only antibiotics able to inhibit biofilm eradication on 50 % of isolates were ceftaroline and gentamicin. (biomedcentral.com)
The gyrA and gyrB sequence information will facilitate analysis of the mechanisms of resistance to drugs which target the gyrase and the implementation of rapid strategies for the estimation of FQ susceptibility in clinical M. tuberculosis isolates. (omicsdi.org)
Cloning and nucleotide sequence of the DNA gyrase gyrA gene from Serratia marcescens and characterization of mutations in gyrA of quinolone-resistant clinical isolates. (omicsdi.org)
DNA gyrase mutations are a major cause of quinolone resistance in Mycobacterium tuberculosis We therefore conducted the first comprehensive study to determine the diversity of gyrase mutations in pre-extensively drug-resistant (pre-XDR) (n = 71) and extensively drug-resistant (XDR) (n = 30) Thai clinical tuberculosis (TB) isolates. (omicsdi.org)

For 26 EAEC strains highly resistant to fluoroquinolone, minimal inhibitory concentrations for fluoroquinolones were determined, mutations in the quinolone target genes were identified by PCR and sequencing, the presence of transferable quinolone resistance mechanism were identified by PCR, and the contribution of the efflux pump was determined by synergy tests using a proton pump inhibitor. (ophrp.org)
The mechanism by which ciprofloxacin's inhibition of DNA gyrase or topoisomerase IV results in death in susceptible organisms has not been fully determined. (antiinfectivemeds.com)

By preventing the formation of single-stranded DNA, fluoroquinolones inhibit bacterial replication. (goldbio.com)
Gemifloxacin enters bacterial cells by diffusion through integral membrane porin pathway before targeting both DNA gyrase and topoisomerase IV, two enzymes critical for DNA replication and repair. (illnesshacker.com)
Gemifloxacin is bactericidal and its mode of action depends on blocking of bacterial DNA replication by binding itself to an enzyme called DNA gyrase, which allows the untwisting required to replicate one DNA double helix into two. (illnesshacker.com)
DNA gyrase and topoisomerase IV have distinct essential roles in bacterial DNA replication. (antiinfectivemeds.com)
DNA gyrase introduces negative superhelical twists in DNA, an activity important for initiation of DNA replication. (antiinfectivemeds.com)
DNA gyrase also facilitates DNA replication by removing positive super helical twists. (antiinfectivemeds.com)
Topoisomerase IV acts at the terminal states of DNA replication by allowing for separation of interlinked daughter chromosomes so that segregation into daughter cells can occur. (antiinfectivemeds.com)
by inhibiting the activity of DNA gyrase and topoisomerase, enzymes essential for bacterial DNA replication. (msdmanuals.com)

This agent binds to the DNA/DNA-gyrase complex and inhibits the A subunits of the enzyme thereby preventing the bacterial chromosome from rejoining. (illnesshacker.com)
DNA gyrase is a tetramer composed of 2 GyrA and 2 GyrB subunits. (antiinfectivemeds.com)
Topoisomerase IV, another type II DNA topoisomerase, is composed of 2 ParC and 2 ParE subunits. (antiinfectivemeds.com)
The genes encoding the DNA gyrase A and B subunits of Bacteroides fragilis were cloned and sequenced. (omicsdi.org)

Gemifloxacin is a broad-spectrum antibiotic that is active against both Gram-positive and Gram-negative bacteria. (illnesshacker.com)
The purpose of the study is to discuss the correlation between the resistance rate of gram negative bacteria to fluoroquinolones (FQ) and antibiotic consumption intensity of 145 China tertiary hospitals in 2014. (biomedcentral.com)
Each participating hospital required to report annual consumption of each antibiotic, and the resistance rate of gram negative bacteria to FQ. (biomedcentral.com)
A strong correlation was demonstrated between the antibiotic consumption and the rates of FQR gram-negative bacteria. (biomedcentral.com)
In this study, the aim was to investigat the correlation between resistance rate of gram-negative bacteria and antibiotic usage. (biomedcentral.com)
They are broad-spectrum bacteriostatic antibiotics that are used to treat infections caused by many gram-positive and gram-negative bacteria. (medscape.com)

This series was evaluated in vitro against Escherichia coli DNA gyrase and E. coli topoisomerase IV with the most potent compounds exhibiting IC50 values towards the low micromolar range for DNA gyrase and only â ¼2-fold less active against topoisomerase IV. (bvsalud.org)

The use of fluoroquinolones is not recommended in patients with myasthenia gravis. (medscape.com)

Although all fluoroquinolones generally are active against both DNA gyrase and topoisomerase IV, the drugs differ in their relative activities against these enzymes. (antiinfectivemeds.com)
This resistance is caused by the development of many different "escape strategies", such as the alteration of the target, the development of pumps to export the antibiotics outside the microbial cell, and in particular for β-lactam antibiotics, the widespread diffusion of β-lactamases, enzymes able to inactivate their pharmacophoric core by hydrolysis of the β-lactam ring [ 11 ] . (encyclopedia.pub)
The replacement of M74 in GyrA, A83 in GyrA, and R447 in GyrB of Mycobacterium tuberculosis gyrase by their Escherichia coli homologs resulted in active enzymes as quinolone susceptible as the E. coli gyrase. (omicsdi.org)

We analyzed the proteins induced in Escherichia coli by exposure to FQs, then examined the susceptibilities to these agents of E. coli strains with mutations in the genes encoding these proteins. (biomedcentral.com)

Results demonstrate that very high concentrations of the most used antibiotics in treating diabetic foot infections (DFI) are required to inhibit S. aureus biofilms in vitro, which may explain why monotherapy with these agents frequently fails to eradicate biofilm infections. (biomedcentral.com)

Ofloxacin inhibits DNA gyrase which results in abnormal linkage between opened DNA and gyrase and negative supercoiling is also impaired. (medicineindia.org)

The other classes of β-lactam antibiotics, namely carbapenems and monobactams, were discovered more recently [ 7 ] [ 8 ] , in an effort to identify new members of this broad group of molecules. (encyclopedia.pub)

The control of DNA-supercoiling in S. pneumoniae occurs mainly via the regulation of topoisomerase gene transcription: relaxation triggers the up-regulation of gyrase and the down-regulation of topoisomerases I and IV, while hypernegative supercoiling down-regulates the expression of topoisomerase I. Relaxation affects 13% of the genome, with the majority of the genes affected located in 15 domains. (ucm.es)
However, unlike many other fluoroquinolones, gemifloxacin targets both DNA gyrase and topoisomerase IV in susceptible S. pneumoniae. (illnesshacker.com)
Streptococcus pneumoniae), the principal target depends on the specific fluoroquinolone. (antiinfectivemeds.com)

Trovafloxacin (sold as Trovan by Pfizer and Turvel by Laboratorios Almirall) is a broad spectrum antibiotic that inhibits the uncoiling of supercoiled DNA in various bacteria by blocking the activity of DNA gyrase and topoisomerase IV. (wikipedia.org)
Fluoroquinolones (FQs) were introduced as broad-spectrum antibiotics. (biomedcentral.com)

On many levels, it makes sense that fluoroquinolone toxicity syndrome is a disease of mitochondrial damage and ensuing oxidative stress. (hormonesmatter.com)
Mitochondrial damage and oxidative stress are almost certainly part of the fluoroquinolone toxicity puzzle. (hormonesmatter.com)

Based on reported resistance of Ng strains, the CDC currently prescribes a two antibiotic protocol using ceftriaxone (a β-lactam) and azithromycin (a macrolide). (elifesciences.org)
MRSA strains have the ability to be resistant to most β-lactam antibiotics, but also to a wide range of other antimicrobials, making infections difficult to manage and very costly to treat. (biomedcentral.com)
The emergence of multidrug-resistant strains of Mycobacterium tuberculosis has resulted in increased interest in the fluoroquinolones (FQs) as antituberculosis agents. (omicsdi.org)

It is commonly used against Gonococcal species and to induce achilles tendon toxicity in rodents. (goldbio.com)
What is Fluoroquinolone Toxicity? (hormonesmatter.com)
Even though I knew why I was sick, I was still left wondering, what does fluoroquinolone toxicity mean? (hormonesmatter.com)
Is fluoroquinolone toxicity syndrome a result of mitochondrial damage? (hormonesmatter.com)
Fluoroquinolone toxicity symptoms resemble those of autoimmune diseases, neurodegenerative diseases, and mysterious diseases. (hormonesmatter.com)

They can occur with fluoroquinolones for systemic use given by mouth or through an injection. (kpaddock.com)
Negative culture results occur for various reasons, including insufficient sample volume, initiation of antibiotics prior to obtaining an expressed prostatic specimen (EPS) sample, and the presence of fastidious organisms. (medscape.com)

The response to local changes induced by fluoroquinolone antibiotics, which target DNA gyrase subunit A and/or topoisomerase IV, involves an increase in oxygen radicals which reduces cell viability, while the induction of global supercoiling changes by novobiocin (a DNA gyrase subunit B inhibitor), or by seconeolitsine (a topoisomerase I inhibitor), has revealed the existence of topological domains that specifically respond to such changes. (ucm.es)
One of these hypothesis suggests the inhibition of subunit A of DNA-gyrase in presence of ATP [ 5 - 7 ]. (hindawi.com)

In fact, biofilms were resistant to antibiotics at concentrations 10-1000 times greater than the ones required to kill free-living or planktonic cells. (biomedcentral.com)

Notably, the drug has 100 times higher affinity for bacterial DNA gyrase than for mammalian. (illnesshacker.com)
It is also noted in an article in Science Translational Medicine entitled "Bactericidal Antibiotics Induce Mitochondrial Dysfunction and Oxidative Damage in Mammalian Cells" that fluoroquinolones, and other bactericidal antibiotics, "damage mammalian tissues by triggering mitochondrial release of reactive oxygen species (ROS). (hormonesmatter.com)

The physiopathology of diabetic foot infections (DFI) is complex, but its severity and prevalence are a consequence of host-related disorders and pathogens-factors, as virulence and antibiotic resistance traits [ 1 ]. (biomedcentral.com)

Drug is removed by induced emesis, gastric lavage, and administration of activated charcoal &use of cathartics. (medicineindia.org)

Second-generation fluoroquinolones, such as gatifloxacin and moxifloxacin, have excellent cerebrospinal fluid (CSF) penetration, and animal models suggest that they are effective in penicillin- and ceftriaxone-resistant pneumococcal meningitis. (medscape.com)

Without treatment, some infections can spread and lead to serious health problems (see List of Currently Available FDA-Approved Systemic Fluoroquinolones). (kpaddock.com)
Systemic fluoroquinolones have been associated with hypersensitivity reactions, even following a single dose. (medico-labs.com)

ASTs decrease the risk of using an antibiotic against bacteria exhibiting resistance to it, and the results are used in clinical settings to determine which antibiotic(s) to prescribe for various infections. (goldbio.com)
Prescribe fluoroquinolones to these patients only when no other treatment options are available. (kpaddock.com)

Molecular cloning of the gyrA and gyrB genes of Bacteroides fragilis encoding DNA gyrase. (omicsdi.org)

This demonstrates that the primary structure of gyrase determines intrinsic quinolone resistance and was supported by a three-dimensional model of N-terminal GyrA. (omicsdi.org)

Several fluoroquinolones are also available as otic and ophthalmic formulations. (msdmanuals.com)

After oral and parenteral administration, fluoroquinolones are widely distributed in most extracellular and intracellular fluids and are concentrated in the prostate, lungs, and bile. (msdmanuals.com)

The results suggest that the antibiotic susceptibility patterns cannot be applied to biofilm established infections. (biomedcentral.com)
Analogously, the proteins induced in bacterial cells exposed to antibiotics are believed to affect the organisms' susceptibility to these agents. (biomedcentral.com)

Gemifloxacin is a fourth generation, an oral fluoroquinolone antibiotic used in the therapy of mild-to-moderate respiratory tract infections caused by susceptible organisms. (illnesshacker.com)
Gemifloxacin is a quinolone/fluoroquinolone antibiotic. (illnesshacker.com)
Whereas LPS induced a rapid increase in NF-kappa B activation, gemifloxacin alone did not. (illnesshacker.com)

The sequence of the DNA gyrase gyrA gene of Serratia marcescens ATCC 14756 was determined. (omicsdi.org)

Additionally, biofilm cells display increased tolerance to antibiotics [ 8 ]. (biomedcentral.com)

DNA gyrase is the main target of the FQs. (omicsdi.org)

Fluoroquinolone antibiotics are approved to treat certain bacterial infections and have been used for more than 30 years. (kpaddock.com)
Levofla is a kind of antibiotic that is used to treat bacterial infections. (healthsoothe.com)

Antibiotic-resistant Neisseria gonorrhoeae (Ng ) are an emerging public health threat due to increasing numbers of multidrug resistant (MDR) organisms. (elifesciences.org)

One way to tell a fluoroquinolone apart from other antimicrobials is that they all have the suffix "-floxacin. (osmosis.org)

Perfloxacin is a fluoroquinolone antibiotic and is an analog of norfloxacin. (goldbio.com)

Fluoroquinolones should not be used in patients at increased risk unless there are no other treatment options available. (kpaddock.com)
Stop fluoroquinolone treatment immediately if a patient reports side effects suggestive of aortic aneurysm or dissection. (kpaddock.com)
In such cases, patients often have symptom improvement after antibiotic treatment. (medscape.com)
Because fluoroquinolones, including CIPRO XR, have been associated with serious adverse reactions [see WARNINGS AND PRECAUTIONS ] and for some patients uncomplicated UTI (acute cystitis) is self-limiting, reserve CIPRO XR for treatment of uncomplicated UTIs (acute cystitis) in patients who have no alternative treatment options. (globalrph.com)

7 However, antibiotic resistance usually occurs in the environment where antibiotics are frequently used. (researchsquare.com)

Topoisomerase II plays a role in condensing the chromosomes by making a double strand break in the DNA so that it can be more tightly wound, causing a supercoil. (osmosis.org)

It act by inhibiting the enzyme DNA gyrase (Topoisomerase 2) and Topoisomerase 4.DNA gyrase helps in the formation of a highly condensed three dimensional structure of the DNA by its nicking and closing activity and also by introducing negative supercoil in to the DNA double helix. (medicineindia.org)
Older fluoroquinolones have poor activity against streptococci and anaerobes. (msdmanuals.com)

After the so-called "Golden Age" of antibiotic discovery (from the 1940s to the 1960s) [ 10 ] , researchers had to realize the progressive increase of microorganisms that are not susceptive to the action of these drugs. (encyclopedia.pub)
Some quinolone and fluoroquinolone drugs chemical structures. (hindawi.com)
Levofla belongs to a class of drugs known as fluoroquinolone antibiotics. (healthsoothe.com)

Organisms29

Diseases26

Chemicals and Drugs82

Analytical, Diagnostic and Therapeutic Techniques and Equipment15

Phenomena and Processes33

Information Science3

Health Care3

Levofloxacin9

Antimicrobial6

Ciprofloxacin10

Quinolones7

Antibacterial1

Synthesis7

Isolates5

Mechanism2

Replication8

Subunits4

Gram-negative6

Evaluated in vitro1

Patients with myasthenia gravis1

Enzymes3

Escherichia1

Vitro1

Ofloxacin1

Carbapenems1

Pneumoniae3

Broad spectrum2

Oxidative stress2

Strains3

Toxicity5

Occur2

Subunit2

Concentrations1

Mammalian2

Virulence1

Emesis1

Moxifloxacin1

Systemic2

Prescribe2

GyrB1

Quinolone resistance1

Ophthalmic1

Widely1

Susceptibility2

Gemifloxacin3

Gene1

Cells1

Target1

Infections2

Organisms1

Antimicrobials1

Norfloxacin1

Treatment4

Occurs1

Chromosomes1

Activity2

Drugs3