Fleroxacin
Anti-Infective Agents
Pefloxacin
Quinolones
Probenecid
The pharmacokinetics of oral fleroxacin and ciprofloxacin in plasma and sputum during acute and chronic dosing. (1/97)
AIMS: To examine the pharmacokinetics of ciprofloxacin and fleroxacin in plasma and sputum of patients with an acute exacerbation of chronic bronchitis or bronchiectasis following the first dose and again during the third day of treatment. METHODS: Twelve patients, aged >35 years, with acute infective exacerbation of bronchitis or bronchiectasis were allocated randomly to treatment with either fleroxacin 400 mg daily or ciprofloxacin 500 mg twice daily in an open, parallel group design. Plasma and sputum were collected during the first and third days of treatment. The time course of concentrations in sputum was modelled assuming that it acted as a negligibly small compartment of distribution. RESULTS: The mean sputum to plasma ratios of both ciprofloxacin and fleroxacin were approximately 1 on both days 1 and 3. Peak concentrations of ciprofloxacin in sputum were achieved 1.6 (95% CI on mean difference 0.8-2.3) and 1.2 (0.4-1.9) h later than in plasma on day 1 and day 3, respectively (mean difference +/- 95% confidence interval). For fleroxacin, the corresponding delay in time to peak concentrations was less marked and not significant. Fleroxacin accumulated in plasma (accumulation index 1.52+/-0.07) and sputum (accumulation index 1.79+/-0.39) from day 1 to day 3. Accumulation did not occur for ciprofloxacin because the dose interval (12 h) was considerable longer than its half life (3-4 h). CONCLUSIONS: The sputum to plasma ratio of ciprofloxacin and fleroxacin is approximately 1. The time to peak concentrations of ciprofloxacin in sputum is slightly delayed compared with plasma. Fleroxacin accumulates over time in both plasma and sputum consistent with its longer half-life. (+info)Formation of antigenic quinolone photoadducts on Langerhans cells initiates photoallergy to systemically administered quinolone in mice. (2/97)
Quinolone antibacterial agents are well known to cause photoallergy as a side-effect. Murine photoallergy to fluoroquinolones is a T cell-mediated immune response, evoked either by systemic fluoroquinolone and subsequent exposure of skin to ultraviolet A light or by subcutaneous injection of fluoroquinolone-photomodified epidermal cells. In this photosensitivity, epidermal Langerhans cells may be photomodified initially with the drug and thus present photohaptenic moieties to sensitize and restimulate T cells. Although we have shown that Langerhans cells photocoupled in vitro with fluoroquinolones are capable of stimulating sensitized T cells, it remains unclear whether systemically given fluoroquinolone photomodifies Langerhans cells upon ultraviolet A irradiation of the skin and the Langerhans cells become photohapten-bearing, T cell-stimulatory cells. In a murine model of fleroxacin photoallergy induced by intraperitoneal injection of the drugs plus ultraviolet A irradiation of skin, we found that Langerhans cells as well as keratinocytes are photoderivatized with fleroxacin as demonstrated with a fluoroquinolone-specific monoclonal antibody. Langerhans-cell-enriched epidermal cells prepared from mice treated with fleroxacin and ultraviolet A induced proliferation of sensitized T cells, indicating that photomodified Langerhans cells are functional. There was an optimal range of ultraviolet A dose to quantitatively and qualitatively form fleroxacin-photomodified Langerhans cells, as excess ultraviolet A rather reduced the photoantigen-presenting capacity of Langerhans cells presumably because of drug phototoxicity. Our study suggests that Langerhans cells serve as photoantigen-presenting cells in drug photoallergy. (+info)Protective effect of fleroxacin against the nephrotoxicity of isepamicin in rats. (3/97)
The protective effect of fleroxacin on isepamicin-induced nephrotoxicity was investigated. Wistar rats were administered either fleroxacin 100 mg/kg orally, isepamicin 300 mg/kg subcutaneously, or fleroxacin and isepamicin in combination for 14 d. The animals given 300 mg/kg of isepamicin showed a significant increase in urine N-acetyl-beta-D-glucosaminidase (NAG) levels as compared with the control animals which received saline (p<0.01). However, the increase in NAG level was markedly less when isepamicin was administered in combination with fleroxacin (p<0.01). Fleroxacin alone had no effect on urine NAG activity. Serum creatinine and blood urea nitrogen (BUN) levels were significantly higher in animals treated with isepamicin alone than in the control animals (p<0.01) or animals receiving the isepamicin fleroxacin combination (p<0.01). Histopathologically, fleroxacin induced very few cellular alterations, but considerably reduced the manifestation of typical signs of isepamicin nephrotoxicity. This investigation demonstrates that fleroxacin protects animals against isepamicin-induced nephrotoxicity. (+info)MIC quality control guidelines for Haemophilus susceptibility tests using cefdinir (FK482), cefepime, cefetamet, cefpirome, ceftibuten, fleroxacin, temafloxacin, clarithromycin, RP59500, and trospectomycin. (4/97)
A multilaboratory study was performed to establish broth microdilution MIC quality control (QC) guidelines for 10 investigational drugs which previously demonstrated significant activity against Haemophilus influenzae. MIC QC ranges for H. influenzae ATCC 49247 with Haemophilus test medium were determined by using multiple contemporary lots of Haemophilus test medium and the National Committee for Clinical Laboratory Standards' recommended numbers of replicate tests. On the basis of these results, QC ranges (generally modal MIC +/- one log2 dilution) are proposed for cefdinir, cefepime, cefetamet, cefpirome, ceftibuten, fleroxacin, temafloxacin, clarithromycin, RP59500, and trospectomycin. The proposed QC guidelines for clarithromycin and temafloxacin were recently accepted by the National Committee for Clinical Laboratory Standards. (+info)Disk diffusion quality control guidelines for Haemophilus susceptibility tests using cefdinir, CI-960, fleroxacin, temafloxacin, and trospectomycin. (5/97)
A multilaboratory study to determine disk diffusion quality control ranges for Haemophilus influenzae ATCC 49247 and five investigational drugs was performed. Multiple lots of Haemophilus Test Medium and antibiotic disks were used for replicate testing in conformance with the recommendations of the National Committee for Clinical Laboratory Standards. Quality control disk zone diameter ranges were proposed for cefdinir, CI-960, fleroxacin, temafloxacin, and trospectomycin. (+info)Interpretive criteria for susceptibility testing of CI-960 (PD127391, AM-1091), fleroxacin, lomefloxacin, and temafloxacin against Neisseria gonorrhoeae, including drug stability in GC agar medium. (6/97)
CI-960, fleroxacin, lomefloxacin, and temafloxacin were tested against over 100 strains of Neisseria gonorrhoeae. Each organism was tested in triplicate by using agar dilution and disk diffusion methods recommended by the National Committee for Clinical Laboratory Standards. CI-960 was the most potent compound, with a MIC against 90% of the strains tested of 0.008 microgram/ml, and the least active was fleroxacin (MIC against 90% of strains, 0.12 microgram/ml). Only the susceptible interpretive category was recommended for the CI-960 tests as follows: 5-micrograms disk, greater than or equal to 39 mm (MIC correlate, less than or equal to 0.12 microgram/ml). Three interpretive categories were proposed for the other fluoroquinolones as follows: fleroxacin, 5-micrograms disk susceptible at greater than or equal to 33 mm (MIC correlate, less than or equal to 0.25 microgram/ml), intermediate at 28 to 32 mm (MIC correlate, 0.5 microgram/ml), and resistant at less than or equal to 27 mm (MIC correlate, greater than 0.5 microgram/ml); lomefloxacin, 10-micrograms disk susceptible at greater than or equal to 35 mm (MIC correlate, less than or equal to 0.12 microgram/ml), intermediate at 28 to 34 mm (MIC correlates, 0.25 to 0.5 microgram/ml), and resistant at less than or equal to 27 mm (MIC correlate, greater than 0.5 microgram/ml); and temafloxacin, 5-micrograms disk susceptible at greater than or equal to 36 mm (MIC correlate, less than or equal to 0.06 microgram/ml), intermediate at 28 to 35 mm (MIC correlates 0.12 to 0.25 microgram/ml), and resistant at less than or equal to 27 mm (greater than 0.25 microgram/ml). Interpretive agreement between disk diffusion results and the MICs was 100% for each agent, with the exception of lomefloxacin, which had a 0.9% minor error. All drugs were stable in GC agar medium for at least 21 days when stored at 2 to 5 degrees C. (+info)MIC and disk diffusion quality control guidelines for Neisseria gonorrhoeae susceptibility tests of cefdinir, cefetamet, CI-960, fleroxacin, lomefloxacin, and temafloxacin. (7/97)
Cefdinir (FK482), cefetamet (Ro 15-8074), CI-960, fleroxacin, lomefloxacin, and temafloxacin have potent activities against Neisseria gonorrhoeae. They were tested in a multilaboratory study to establish quality control guidelines. Quality control ranges for N. gonorrhoeae ATCC 49226 were determined by using multiple GC agar lots, three disk lots, and a number of test replicates consistent with the M23-T guidelines of the National Committee for Clinical Laboratory Standards. The MIC ranges included 2 to 4 log2 dilution steps. The recommended inhibition zone diameter ranges were generally 7 to 8 mm and included greater than or equal to 91.3% of all recorded study results. (+info)Antibacterial activity of sparfloxacin against experimental renal infections in mice. (8/97)
In a murine model of renal infection (Staphylococcus aureus and Escherichia coli), sparfloxacin was compared with ciprofloxacin and fleroxacin. After intrarenal inoculation, mice were treated orally for 5 days. The drugs were administered at five different dosages, ranging from 3.125 to 50 mg/kg of body weight per day for S. aureus and from 0.78 to 12.5 mg/kg/day for E. coli. Evaluation of efficacy was based on the proportional reduction of bacterial counts in the kidney tissues of treated animals compared with those of untreated control animals. For S. aureus, the doses required to clear the infection in 50% of mice were as follows: sparfloxacin, 10 mg/kg/day; ciprofloxacin, 33 mg/kg/day; and fleroxacin, 16 mg/kg/day. For E. coli renal infection, the corresponding dosages were as follows: sparfloxacin, 1.5 mg/kg/day; ciprofloxacin, 2.45 mg/kg/day; and fleroxacin, 1.8 mg/kg/day. Sparfloxacin and fleroxacin have a lower effective dose than ciprofloxacin in these models, probably because ciprofloxacin has a shorter serum half-life than the other two compounds. (+info)Fleroxacin is a fluoroquinolone antibiotic that is used to treat various types of bacterial infections, including respiratory, urinary tract, and skin infections. It works by inhibiting the DNA gyrase enzyme in bacteria, which is necessary for their replication and survival.
Fleroxacin has a broad spectrum of activity against both gram-positive and gram-negative bacteria, making it useful for treating a variety of infections caused by these organisms. However, like other fluoroquinolones, fleroxacin carries a risk of serious side effects, including tendinitis, tendon rupture, nerve damage, and other central nervous system effects. Therefore, its use is generally reserved for situations where other antibiotics are not effective or appropriate.
Fleroxacin is available in oral tablet form and is typically taken twice daily with a full glass of water. It should be taken on an empty stomach, at least one hour before or two hours after meals. The dosage and duration of treatment will depend on the type and severity of the infection being treated, as well as the patient's overall health status.
It is important to note that fleroxacin, like all antibiotics, should only be used under the guidance of a healthcare professional, and should not be used for viral infections such as the common cold or flu. Misuse of antibiotics can lead to antibiotic resistance, which makes it more difficult to treat bacterial infections in the future.
Ciprofloxacin is a fluoroquinolone antibiotic that is used to treat various types of bacterial infections, including respiratory, urinary, and skin infections. It works by inhibiting the bacterial DNA gyrase, which is an enzyme necessary for bacterial replication and transcription. This leads to bacterial cell death. Ciprofloxacin is available in oral and injectable forms and is usually prescribed to be taken twice a day. Common side effects include nausea, diarrhea, and headache. It may also cause serious adverse reactions such as tendinitis, tendon rupture, peripheral neuropathy, and central nervous system effects. It is important to note that ciprofloxacin should not be used in patients with a history of hypersensitivity to fluoroquinolones and should be used with caution in patients with a history of seizures, brain injury, or other neurological conditions.
Anti-infective agents are a class of medications that are used to treat infections caused by various microorganisms such as bacteria, viruses, fungi, and parasites. These agents work by either killing the microorganism or inhibiting its growth, thereby helping to control the infection and alleviate symptoms.
There are several types of anti-infective agents, including:
1. Antibiotics: These are medications that are used to treat bacterial infections. They work by either killing bacteria (bactericidal) or inhibiting their growth (bacteriostatic).
2. Antivirals: These are medications that are used to treat viral infections. They work by interfering with the replication of the virus, preventing it from spreading and causing further damage.
3. Antifungals: These are medications that are used to treat fungal infections. They work by disrupting the cell membrane of the fungus, killing it or inhibiting its growth.
4. Antiparasitics: These are medications that are used to treat parasitic infections. They work by either killing the parasite or inhibiting its growth and reproduction.
It is important to note that anti-infective agents are not effective against all types of infections, and it is essential to use them appropriately to avoid the development of drug-resistant strains of microorganisms.
Pefloxacin is a fluoroquinolone antibiotic that is primarily used to treat various types of bacterial infections, such as respiratory tract infections, urinary tract infections, skin and soft tissue infections, and sexually transmitted diseases. It works by inhibiting the DNA gyrase enzyme in bacteria, which is necessary for their replication and survival.
The medical definition of Pefloxacin can be stated as follows:
Pefloxacin (INN, USAN) - a fluoroquinolone antibiotic with bactericidal activity against a wide range of gram-positive and gram-negative bacteria. It is used to treat various types of infections caused by susceptible organisms, including respiratory tract infections, urinary tract infections, skin and soft tissue infections, and sexually transmitted diseases. Pefloxacin is available as an oral tablet or injection for intravenous use.
It's important to note that the use of fluoroquinolones like pefloxacin should be reserved for treating serious bacterial infections that are unresponsive to other antibiotics, due to concerns about their potential side effects and the risk of developing antibiotic resistance.
Fluoroquinolones are a class of antibiotics that are widely used to treat various types of bacterial infections. They work by interfering with the bacteria's ability to replicate its DNA, which ultimately leads to the death of the bacterial cells. Fluoroquinolones are known for their broad-spectrum activity against both gram-positive and gram-negative bacteria.
Some common fluoroquinolones include ciprofloxacin, levofloxacin, moxifloxacin, and ofloxacin. These antibiotics are often used to treat respiratory infections, urinary tract infections, skin infections, and gastrointestinal infections, among others.
While fluoroquinolones are generally well-tolerated, they can cause serious side effects in some people, including tendonitis, nerve damage, and changes in mood or behavior. As with all antibiotics, it's important to use fluoroquinolones only when necessary and under the guidance of a healthcare provider.
Quinolones are a class of antibacterial agents that are widely used in medicine to treat various types of infections caused by susceptible bacteria. These synthetic drugs contain a chemical structure related to quinoline and have broad-spectrum activity against both Gram-positive and Gram-negative bacteria. Quinolones work by inhibiting the bacterial DNA gyrase or topoisomerase IV enzymes, which are essential for bacterial DNA replication, transcription, and repair.
The first quinolone antibiotic was nalidixic acid, discovered in 1962. Since then, several generations of quinolones have been developed, with each generation having improved antibacterial activity and a broader spectrum of action compared to the previous one. The various generations of quinolones include:
1. First-generation quinolones (e.g., nalidixic acid): Primarily used for treating urinary tract infections caused by Gram-negative bacteria.
2. Second-generation quinolones (e.g., ciprofloxacin, ofloxacin, norfloxacin): These drugs have improved activity against both Gram-positive and Gram-negative bacteria and are used to treat a wider range of infections, including respiratory, gastrointestinal, and skin infections.
3. Third-generation quinolones (e.g., levofloxacin, sparfloxacin, grepafloxacin): These drugs have enhanced activity against Gram-positive bacteria, including some anaerobes and atypical organisms like Legionella and Mycoplasma species.
4. Fourth-generation quinolones (e.g., moxifloxacin, gatifloxacin): These drugs have the broadest spectrum of activity, including enhanced activity against Gram-positive bacteria, anaerobes, and some methicillin-resistant Staphylococcus aureus (MRSA) strains.
Quinolones are generally well-tolerated, but like all medications, they can have side effects. Common adverse reactions include gastrointestinal symptoms (nausea, vomiting, diarrhea), headache, and dizziness. Serious side effects, such as tendinitis, tendon rupture, peripheral neuropathy, and QT interval prolongation, are less common but can occur, particularly in older patients or those with underlying medical conditions. The use of quinolones should be avoided or used cautiously in these populations.
Quinolone resistance has become an increasing concern due to the widespread use of these antibiotics. Bacteria can develop resistance through various mechanisms, including chromosomal mutations and the acquisition of plasmid-mediated quinolone resistance genes. The overuse and misuse of quinolones contribute to the emergence and spread of resistant strains, which can limit treatment options for severe infections caused by these bacteria. Therefore, it is essential to use quinolones judiciously and only when clinically indicated, to help preserve their effectiveness and prevent further resistance development.
Probenecid is a medication that is primarily used to treat gout and hyperuricemia (high levels of uric acid in the blood). It works by decreasing the production of uric acid in the body and increasing its excretion through the kidneys.
In medical terms, probenecid is a uricosuric agent, which means it increases the urinary excretion of urate, the salt form of uric acid. It does this by inhibiting the reabsorption of urate in the proximal tubules of the kidneys, thereby promoting its elimination in the urine.
Probenecid is also used in conjunction with certain antibiotics, such as penicillin and cephalosporins, to increase their concentration in the body by reducing their excretion by the kidneys. This is known as probenecid-antibiotic interaction.
It's important to note that probenecid should be used under the supervision of a healthcare provider, and its use may be contraindicated in certain medical conditions or in combination with specific medications.
Sucralfate is a medication that belongs to a class of drugs called aluminum complexes. It's often used in the treatment of gastrointestinal ulcers, including duodenal and gastric ulcers, as well as in the prevention of stress-induced mucosal damage in critically ill patients.
Sucralfate works by forming a protective barrier over the ulcer site, which helps to prevent further damage from acid and digestive enzymes. It's not absorbed into the bloodstream, so it acts locally in the gastrointestinal tract. The medical definition of Sucralfate is:
A synthetic basic aluminum salt of sucrose octasulfate, which is used in the treatment of gastro duodenal ulcers and as a protectant against stress-induced mucosal damage in critically ill patients. It exerts its therapeutic effect by forming a complex, adhesive protective coating over ulcerated areas, thereby preventing further erosion from gastric acid and pepsin.
Fleroxacin - Wikipedia
Fleroxacin
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