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We report two cases of lupus miliaris disseminatus faciei (LMDF) in which oral tranilast was effective. In case 1, the patient was a 33-year-old woman who had developed pale red papules on her face, especially around her eyes and lower jaw, approximately 7 months previously. Examination of a skin biopsy specimen revealed epithelioid cell granulomas accompanied by caseous necrosis, and a diagnosis of LMDF was made. The patient was treated successively with azithromycin, roxithromycin and minocycline hydrochloride, but there was no improvement. When we tried oral tranilast therapy, flattening of the papules was observed 2 weeks after the start of treatment, and by 1 month the papules had almost disappeared. In case 2, the patient was a 39-year-old man who had broken out in erythematous papules on both upper and lower eyelids, with some accompanied by scaling, 2 years before the initial examination. Pathological specimen revealed epithelioid cell granulomas accompanied by caseous necrosis, and a diagnosis of LMDF was made. There was no improvement when treated orally with minocycline hydrochloride or doxycycline hydrochloride, and treatment was switched to oral tranilast therapy. After 1 month of treatment, the papules had almost disappeared. We concluded that oral tranilast therapy should be tried as a treatment for intractable LMDF.
Bacterial biofilm (BF) was established and was influenced by RXM and FLRX with different concentrations. The samples were detected with scanning electron microscope and by a rapid method after BF was stained with AgNO3 solution. The synergism of antibacterial activities of RXM and FLRX to P. Aeruginosa was studied by computer image analysis and MTT method.
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Our data suggest that oral administration of roxithromycin suppresses ovalbumin-induced airway inflammation and AHR by regulating the inflammatory cytokines via MAP kinases/NF-κB pathway in inflammatory cells. Based on these results, we suggest that roxithromycin may be used as a therapeutic agent for allergy-induced asthma.
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High biodegradation efficiencies of different emerging micropollutants were obtained with nitrifying activated sludge (NAS) working at high nitrogen loading rates (NLR), that boosted the development of biomass with high nitrifying activities (>1 g N-NH(4)(+)/g VSS d). Come-tabolic biodegradation seemed to be responsible for the removal of most compounds due to the action of the ammonium monooxygenase enzyme. NAS showed a different affinity for each compound, probably due to steric hindrance, activation energy limitations or the presence of specific functional groups. Increasing loading rates of micropollutants were removed at shorter hydraulic retention times, although the biodegradation efficiencies of compounds with slow/intermediate kinetics, such as fluoxetine, erythromycin, roxithromycin and trimethoprim, diminished due to kinetic and/or stoichiometric limitations. Solids retention time, always above the minimum to avoid the washout of nitrifiers, did not enhance the biodegradation of any of the selected compounds, with the exception of diclofenac. Regarding sorption, the solid-liquid distribution coefficients (K(d)) obtained in NAS were very similar to those found in conventional activated sludge by other authors. No correlation between K(d) values and any of the operational parameters was found for the selected substances.
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After the discovery of erythromycin and other natural compounds, including oleandomycin, spiramycin, josamycin and midecamycin, much research has been devoted to synthesizing derivatives or analogues with improved chemical, biological and pharmacokinetic properties. These new macrolides are semisynthetic molecules that differ from the original compounds in their substitution pattern of the lactone ring system. The chemical structure of macrolides is characterized by a large lactone ring containing from 12 to 16 atoms to which are attached, via glycosidic bonds, one or more sugars. The lactone ring is substituted by hydroxyl or alkyl groups, one ketone at C7 in 12-membered macrolides and at C9 in 14-membered macrolides, and one aldehyde group in 16-membered macrolides. The only compound with a 15-membered ring contains a tertiary amino group. Although the 12-membered macrolides have never become important in clinical practice, in recent years numerous new 14-membered macrolide derivatives of erythromycin A have shown improved pharmacokinetics due to chemical modifications of a hydroxyl group at C6, a proton at C8, or a ketone at C9. Derivatives, such as dirithromycin, roxithromycin, clarithromycin and flurithromycin, have all been synthesized with the aim of inhibiting their decomposition under acidic conditions to inactive anhydrohemiketal derivatives. A new 15-membered macrolide, azithromycin, with a methylated nitrogen inserted into the lactone ring shows good activity against Gram-negative bacteria. The efforts expended in chemical and biochemical modifications of 16-membered macrolides have been less successful, with only a few new molecules, such as rokitamycin and miocamycin, showing improved bioavailability and activity against some resistant micro-organisms.(ABSTRACT TRUNCATED AT 250 WORDS)
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Preincubation of Haemophilus influenzae with antibiotics may influence opsonophagocytosis as studied by chemiluminescence. Two strains of H. influenzae (strain 1 [type b] and strain 2 [uncapsulated]) were pretreated with erythromycin, roxithromycin, clarithromycin, and azithromycin for 1 h in Haemophilus test medium (the last 25 min was either without serum or with 10% fresh serum or 10% decomplemented serum). Human neutrophils were stimulated with a pretreated or control inoculum at four different bacterium/neutrophil ratios and tested for luminol chemiluminescence with an LKB luminometer. The results were normalized for bacterium/neutrophil ratio and compared by the two-sided Wilcoxon test. Pretreatment of bacteria with one-half of the MICs of erythromycin, clarithromycin, and roxithromycin produced nonsignificant (P > 0.05) increases in the chemiluminescence response (means of 23% for strain 1 and 4% for strain 2). Pretreatment with azithromycin at one-half of the MIC produced an increase in the chemiluminescence response induced by serum-opsonized strain 1 (320% +/- 36% [mean +/- standard error of the mean]) and strain 2 (107% +/- 20%) (P < 0.05). This increase was concentration dependent: for strain 1, 60% +/- 18% at one-fourth of the MIC to 440% +/- 41% at the MIC; for strain 2, 10% +/- 5% at one-fourth of the MIC to 300% +/- 20% at the MIC. For strain 1, the maximal increase with azithromycin pretreatment (at the MIC) required opsonization with fresh serum. Opsonization with decomplemented serum was associated with a 53% +/- 21% increase; this increase was 28% +/- 3% in the absence of serum. For strain 2, azithromycin reduced the lag phase of the chemiluminescence response induced by the absence of serum but did not alter the chemiluminescence response in the presence of decomplemented serum. A significant contribution of soluble factors in the enhanced response observed with bacteria preincubated with azithromycin was excluded. The increase of the chemiluminescence response with azithromycin pretreatment was probably due to improvement in complement-dependent opsonization for strain 1 and to improvement in both serum-independent and serum-dependent opsonization for strain 2.
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To examine the potential anti-androgenic activity of anti-acne therapeutic agents, nadifloxacin (NDFX), RXM, all-trans retinoic acid (atRA), and glycolic acid (GA), we carried out the transient transfection assays using the CV-1 cells as a more sensitive assay system.
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Some recently introduced macrolides have several clinical advantages over erythromycin. Azithrommcin, a prototype of these new macrolides could be a good alternative for the treatment of streptococcal pharyngitis, even over penicillin, whose failure rate can be as high as 30%. The aim of this study was to evaluate the in vitro susceptibility of 120 strains of S pyogenes isolated between 1990 and 1992 (40 per year), from diverse infections (specially tonsillitis). We determined Minimal Inhibitory Concentrations (MIC) of azithromycin, clarithromycin, roxithromycin, erythromycin and penicillin using the agar dilution method and the Minimal Bactericidal Concentration (MBC) by tube dilution for azythromycin and erythromycin. The MIC 90 for the new macrolides ranged from 0.03 to 0.12 microgram/ml, and was 0.03 microgram/ml for erythromycin and penicillin (not different). All strains were susceptible to all antibiotics and the date of isolation did not influence susceptibility. The MBC for azithromycin was 0.12 microgram/ml (identical to its MIC), which demonstrates the bactericidal effect of this antibiotic. It is concluded that this in vitro data supports the potential role of these new macrolides in the treatment of streptococcal infections.
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Cytochrome P450 (CYP) 3A4 is the most prevalent metabolising enzyme in the human liver and is also a target for various drug interactions of significant clinical concern. Even though there are numerous reports regarding drug interactions involving CYP3A4, it is far from easy to estimate all potential interactions, since too many drugs are metabolised by CYP3A4. For this reason, a comprehensive framework for the prediction of CYP3A4-mediated drug interactions would be of considerable clinical importance.
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A total of 60 isolates of A. actinomycetemcomitans recovered from 43 individuals with gingivitis or periodontitis were tested. In addition, laboratory strains UP-6 and JP2 were analysed. The E-test was employed in order to determine minimal inhibitory concentrations (MIC) of antibiotics ampicillin/sulbactam, roxithromycin, azithromycin, doxycycline, metronidazole, ciprofloxacin, and moxifloxacin.