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Progress quinolone antibacterial drugs


Gram-negative bacteria with high activity, but also significantly enhanced anti-Gram-positive bacteria activity, and anaerobic bacteria, mycoplasma, etc. there is a strong role; in which the half-life of moxifloxacin over 10h, the rest of the 5h or more; have A structure of 8-methoxy quinolone increases glomerular filtration, excretion from the urine, the average half-life of 8 ~ lOh4.3 moxifloxacin for one of 8-methoxy-substituted fluoroquinolone, photosensitive reaction less. Foreign clinical data show that live Streptococcus pneumoniae of Health} is the strongest in the fluoroquinolones. However, methicillin-resistant Staphylococcus aureus are less effective. 4.4 gemifloxacin against methicillin-resistant Staphylococcus aureus and bacteria (including Streptococcus pneumoniae) was stronger. Low incidence of adverse reactions. However, the activity of anaerobic bacteria is less than other new compounds. 4.5 West Sand Star he has a strong broad-spectrum activity against Helicobacter pylori MIC90 of 0.025mg / L, almost the same as amoxicillin: Mycobacterium tuberculosis MIC90 of 0.2mg / L, anti-Pseudomonas Pseudomonas Fu is also stronger than other varieties. Phase III clinical trials have been completed. But light toxicity and other adverse reactions and low blood sugar with the widespread use of quinolone antibiotics, bacterial resistance increased year by year. Mechanism of quinolones by bacterial cells with DNA gyrase and topoisomerase Iv interact to form a quinolone of a DNA enzyme complex. Blocking DNA replication. Quinolone-resistant bacteria on one of the reasons the two subunits of the target enzyme mutations in the amino acid substitution. A DNA enzyme complex reduces the affinity of quinolone drugs, the emergence of resistance. In both target enzymes, the higher the sensitivity of the preferred target enzyme often can be caused by bacteria, the drug varies. Most of the early development of quinolone inhibition of enzyme activity of the two targets are different, to G-bacteria, for example, the preferred target enzymes gyrase, while the G strain of choice for the topoisomerase IV. Under the action of the quinolones. Variation of the preferred target enzymes, bacteria that gain resistance. The second variation of the target enzyme, can continue to strengthen the resistance level Gan students, fewer students were u crying fewer Palestinian rule I rather keep on the death of eight-dimethyl sigh o} j Ke Wu a storm basket (ore ') and more on Velvet reduce the harmonic large photosensitive reactions. 4.6 Ge Pasha Star and clinafloxacin (due to mutation of bacteria can reduce the intake of drugs, but also cutting sand 4.1 stars,[link widoczny dla zalogowanych], in September 1997 8 - bit chlorine atoms),[link widoczny dla zalogowanych], respectively, lead to drug resistance because of severe . In addition, many bacterial cell membranes in the United States, it is resistant Staphylococcus aureus, multiple cardiac toxicity and phototoxicity, have been withdrawn from the market. Drug efflux pump on quinolone resistance of live pneumococcal, mycoplasma, anaerobes and other parties look at the development of quinolones, the main side affect is also more effective than ciprofloxacin, close to the MIC concentration to direction : 1) enhance certain bacteria (including the degree of clinical application of quinolones that have a bactericidal effect, but not for resistance, including MRSA, Enterococcus, Streptococcus, anaerobic, should pay close attention to two issues. a certain ciprofloxacin-resistant Staphylococcus aureus and multiple bacteria, Pseudomonas,[link widoczny dla zalogowanych], Aeromonas,[link widoczny dla zalogowanych], Legionella monocytogenes) and post-marketing surveillance of quinolones in enterococci during the period, because of the lack of Mycobacterium tuberculosis activity; 2) to improve the pharmacokinetic properties, increased by the discovery of several serious adverse reactions. The role of such activity, but also has severe liver toxicity bioavailability, longer half-life, as following oxyfluoride QT interval prolongation, cardiac toxicity and liver toxicity, has limited use. Mainly for the treatment of sand stars, music stars cutting sand; 3) reduce the photosensitivity and sex, suggesting the discovery of these rare but serious respiratory infections caused by susceptible strains (including increased security community, such as c an access by the methoxy adverse reactions, areas for monitoring of the new quinolones acquired pneumonia and nosocomial pneumonia), abdominal generation of gatifloxacin and moxifloxacin; 4) explore the matter is required. Second, there is globally a cavity infections (including surgical complications and the activity of the new structure: 1 is found to have the characteristics of the increasing trend of quinolone resistance after infection), gynecological and pelvic infections and meningitis-bit non- N, 6 位 replaced and seven non-F connection potential, which gives even the most active fluoroquinolone and so on. Allah is the song cutting song Sha Sha Star Star CC bond dipropyl new quinolone; 5) explore the microbial ketone has also brought a threat, so they requested the medical workers acid derivatives, to improve the water-soluble, can be used to generate a new quinolone, If found false Nocardia of dedication to work, a clear indication, so that prospective intravenous infusion, but also because of liver toxicity, and CJ coli produced 13,[link widoczny dla zalogowanych],136 pairs a secluded f-3 screw do drugs in order to extend their use of time . Restricted. Bacteria have a strong selective antibacterial effect; 6) Exploration (20,021,129 Received) plus ∞ _ Nang