Sparfloxacin
Mean, 67.7 years ; , with weights ranging between 34 and 57 kg mean, 47.2 kg ; and heights ranging between 151 and 163 cm mean, 156.7 cm ; . All were receiving chronic theophylline therapy for asthma. Known metabolic inhibitors or inducers 15 ; were withheld from the subjects during the study period. Informed consent was obtained from each patient after a full explanation of the procedures. Drugs. Theophylline tablets in a sustained-release formulation Theo-Dur; 100 mg of theophylline per tablet; Nikken Kagaku, Tokyo, Japan ; were used in this study. Likewise, the tablet form of sparfloxacin was used; each tablet contained 100 mg of 5-amino-1-cyclopropyl-6, 8-difluoro-1.4-dihydro - 7 cis - 3, 5 - dimethyl -1- piperazinyl ; - 4 - oxoquinoline - 3 carboxylic acid Dainippon Pharmaceutical Co., Ltd., Osaka, Japan ; . The tetrabutylammonium hydrogen sulfate used for the determination of theophylline and its metabolites in urine was obtained from Aldrich Chemical Co. Inc. All other reagents used were of analytical grade. Study design. The patients were studied during their hospitalization at Nagoya University Hospital. The study type was a single crossover with each patient serving as his own control. Each patient received theophylline at 400 to 600 mg day twice daily at 12-h intervals 9: 00 a.m. and 9: 00 p.m. ; . i ; Control study. The control study was started on the day after the patients had attained steady-state conditions. Blood samples were collected at time zero just before the start of theophylline administration ; and every 2 h from 9: 00 a.m. to 9: 00 p.m. after the start of theophylline administration. Urine samples were collected at the same times. Xanthinecontaining foods and drinks were excluded for 48 h before the day on which sampling was begun. ii ; Coadministration study. From the day after the start of the control study, 200 mg of sparfloxacin was coadministered with theophylline as a once-daily dose in the morning for 7 days. On day 8, the last morning dose of theophylline.
Consequently, sparfloxacin is contraindicated for individuals receiving these drugs as well as other qt c -prolonging antiarrhythmic drugs reported to cause torsade de pointes, such as class ia antiarrhythmic agents e, g!
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Study objective: Comparison of efficacy and safety of sparfloxacin vs ofloxacin for treatment of acute bacterial exacerbations of chronic bronchitis ABECB ; . Design: Multicenter, double-blind, randomized study. Setting: Sixty-eight private offices and outpatient clinics in the United States and Canada. Patients: Seven hundred ninety-eight adults with ABECB, as confirmed by the acute onset of new or worsened from the immediate premorbid state ; cough and sputum production. Interventions: Bandomization 1: to sparfloxacin, 400 mg on day 1, then 200 mg once daily, or ofloxacin, 400 mg twice daily, with matching comparator placebos, given concurrently for 10 consecutive days. Results: The primary efficacy parameter was overall response in the bacteriologically evaluable population. Overall success rates in this population were 85.3% and 89.3% for sparfloxacin and ofloxacin, respectively. The two-sided 95% confidence interval was .9.9, 1.9, indicating that sparfloxacin was statistically equivalent to ofloxacin. The all-treated population analysis was similar to that in the evaluable population. Bacterial eradication rates were similar in both treatment groups for Haemophilus influenzae, Streptococcus pneumoniae, Moraxella catarrhalis, Chlamydia pneumoniae, Haemophilus parainfluenzae, Klebsiella pneumoniae, Enterobacter cloacae, and Staphylococcus aureus. The frequency of adverse events overall was comparable in the two treatment groups. The sparfloxacin group had a lower frequency of digestive and nervous system adverse events, but a higher frequency of photosensitivity reactions than the ofloxacin group. Conclusions: Once-daily oral treatment with 200 mg sparfloxacin after initial 400 mg dose ; is as effective as twice-daily treatment with 400 mg ofloxacin in patients with ABECB.
Activity of AM-1155 against anaerobes Table I. The activity of AM-1155 and other agents against anaerobic bacteria and Gardnerella vaginalis Range B. fragilis n 66 ; AM-1155 temafloxacin sparfloxacin tosufloxacin ciprofloxacin ofloxacin cefmetazole Bacteroides ovatus n 8 ; AM-1155 temafloxacin sparfloxacin tosufloxacin ciprofloxacin ofloxacin cefmetazole MIC50 0.78 1.56 0.78 MIC90 6.25 12.5 6.25 gingivalis n 20 ; AM-1155 temafloxacin sparfloxacin tosufloxacin ciprofloxacin ofloxacin cefmetazole Range MIC50 0.10 0.20 MIC90 0.10 0.39.
In transformations of R6 with QRDR gene fragments of gyrB, parC, and parE from strain 4571, only parE transformants E474K ; could be selected on levofloxacin as single mutants. Introduction of the gyrB gene fragment D435E ; into R6 4571parE resulted in R6 4571parE, gyrB transformants for which the MICs increased fourfold for gatifloxacin and twofold for each of the other fluoroquinolones. Transformants with the 4571 parC mutation A63T ; could be selected only after the parE and gyrB mutations were introduced. For this final transformation, sparfloxacin was used for selection of R6 4571parE, gyrB, parC because the MICs of levofloxacin for the donor strain, 4571, and the recipient, R6 4571parE, gyrB, were the same. In addition, alternative PCR primers were used to shift the position of the parC mutation farther downstream from the 5 end of the gene fragment. Numerous transformations using the 329-bp fragment of parC amplified with oligonucleotide primers PNC10 and PNC11 ; were successful for introducing mutations in codons for S79 and D83, located 130 to 145 bp from the 5 end of the gene fragment. However, efforts to introduce the mutation in the codon for ParC A63, located at nucleotide position 83, were unsuccessful. This problem was resolved by increasing the size of the amplified gene fragment, shifting the mutation downstream to a position 181 bp from the 5 end. For the resulting R6 4571parE, gyrB, parC transformants, the MIC of sparfloxacin increased fourfold and MICs of gatifloxacin, gemifloxacin, moxifloxacin, and trovafloxacin increased twofold. The fluoroquinolone susceptibility profiles of all R6 4571parE, gyrB, parC transformants were identical to that of the donor strain, 4571, and of R6 4571chr. No active drug efflux was detected in growth inhibition assays of strain 4571 with reserpine data not shown ; . DISCUSSION The increasing prevalence of penicillin- and multidrug-resistant pneumococci has resulted in extensive use of fluoroquinolones for antimicrobial therapy of pneumococcal infections. However, the emergence of fluoroquinolone-resistant isolates 8, 21 ; threatens to further limit the number of agents available for effective treatment of pneumococcal disease. A more thorough understanding of the molecular mechanisms of resistance will aid in designing strategies to minimize the emergence of resistant strains and to predict patterns of cross-resistance among this class of antimicrobial agents. Thus, the purpose of this study was to characterize recent clinical isolates of fluoroquinolone-resistant pneumococci, determine the activity and patterns of cross-resistance of newer fluoroquinolones against these isolates, and investigate the contribution of selected gyrA, gyrB, parC, and parE mutations to fluoroquinolone resistance. Analysis of the susceptibility profiles revealed an association of multidrug resistance, but not fluoroquinolone resistance, with specific serotypes of S. pneumoniae. Four of the five MDR strains in this study were serotype 23F, which is consistent with a previous report that MDR is associated with pneumococcal serotypes 6, 14, 19, and 23 in U.S. isolates 46 ; . However, 11 serotypes and one nontypeable strain were represented among the 16 isolates with high-level resistance to fluoroquinolones, precluding any correlation between serotype and fluoroquinolone resistance. There was also no correlation between resistance to fluoroquinolones and resistance to other classes of and spectinomycin.
The addition of a third eye primordium to the forebrain region of a Rana pipiens embryo invariably results in the development of a series of periodic, mutually exclusive eyespecific bands in tectal lobes dually innervated by the host and supernumerary fibers. A number of investigators have proposed that such source-specific segregation arises as a compromise between two mechanisms that are normally involved in retinotectal map formation: one which is dependent on cell surface affinities to align the map and produce a rough retinotopy and a second that "fine tunes" the map by stabilizing adjacent terminals from neighboring retinal ganglion cell bodies at the expense of terminals from nonneighboring cells. In this study we have tested the idea that this second "fine-tuning" mechanism is dependent on neural activity by blocking impulse activity in the optic nerves of three-eyed tadpoles. To assess the requirement for activity on the formation of bands, both normal optic nerves of 17 three-eyed tadpoles were crushed intraorbitally. Two weeks after this operation, the supernumerary retinal projection had debanded and spread to cover the entire tectum in a continuous fashion. By 4 weeks, however, the host optic fibers regenerated back to the tecta and began to form segregated stripes with the fibers from the third eye. Six to 7 weeks after the optic nerve crush the periodic pattern of eye-specific segregation characteristic of dually innervated tecta was again pronounced. When activity in all three optic nerves was eliminated with tetrodotoxin TTX; embedded in a slow release plastic ; during the last 3 weeks of this process, the fibers from the two competing eyes failed to segregate and, instead, formed two completely overlapping, continuous projections across the tectal surface. To test for the requirement of activity in the maintenance of segregation, we also subjected three-eyed tadpoles without optic nerve crush to TTX blockade for 2, 3, and 4 weeks. Animals sacrificed at 2 weeks show overlap of the projections in the rostra1 tectum but distinct interdigitating stripes in.
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Resistance to ciprofloxacin in methicillin-resistant Staphylococcus aureus emerges more rapidly than to ofloxacin, levofloxacin, or sparfloxacin 1, 2 ; . We compared emergence of resistance to trovafloxacin with that to ciprofloxacin. We examined 13 methicillin-resistant S. aureus isolates for which the ciprofloxacin and trovafloxacin MICs were 1 and 2 g ml, respectively, and for which unique genotypes were found by pulsed-field gel electrophoresis. Spontaneous single-step mutation rates were determined by growing bacteria in antibiotic-free broth and plating 0.1-ml aliquots on Mueller-Hinton agar containing four or eight times the MIC of ciprofloxacin or trovafloxacin. The resistance frequency was calculated by dividing the number of colonies at 48 h the inoculum. The emergence of resistance during serial transfer was studied by growing bacteria in antibioticfree medium, adjusting the cultures to 108 CFU ml, and range, 3.3 10 to 1.1 10 7 ; , respectively P 0.05 ; Table 1 ; . In serial transfer experiments, for all strains the mean MIC of ciprofloxacin increased 6.7 0.9-fold, and the MIC of trovafloxacin increased 3.3 0.9-fold P 0.05 ; . The MICs for all strains exposed to ciprofloxacin increased by fourfold after a single transfer; the strains became resistant MIC, 4 g ml ; 3 ; within 4 transfers, and the MIC was 32 g ml after 10 transfers. In contrast, the MIC was 4 g ml for only one strain exposed to trovafloxacin. The mean MIC for the remaining strains was 2 g ml after 10 transfers. Single-step resistance and the emergence of resistance with serial transfer appear to be more common with ciprofloxacin than with trovafloxacin.
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Prevented the expansion of bacillary load between weeks 3 and 7, whereas there was an apparent reduction in counts within the control group. Because only 50% four of eight mice ; of the mice in the control group survived to week 7, it is likely that death of the most heavily infected control mice resulted in a falsely low mean bacillary load in this group at week 7. Serum moxifloxacin concentrations. Serum drug concentration-time profiles and pharmacokinetic parametric values of moxifloxacin after a single oral administration in mice are shown in Table 4. The parameters for moxifloxacin derived from this study are shown with previously published values for ofloxacin and sparfloxacin. The values for maximum serum drug concentration Cmax ; of moxifloxacin were similar to those of sparfloxacin and lower than those reported for equivalent doses of ofloxacin. Dose dependency was investigated with Cmax values of moxifloxacin. When the MIC of moxifloxacin for the CSU93 strain determined in this study 0.25 g ml and stadol.
Teric gram-negative bacilli, although it was substantially less than that against members of the family Enterobacteriaceae. Ciprofloxacin, CI-960, and PD 131, 628 were comparably active against Pseudomonas aeruginosa, each having a MIC90 of 1.0 p.g ml. Xanthomonas maltophilia was the organism most resistant to all four drugs, but CI-960 had the lowest MIC90 2.0 , ug ml ; . The MIC75s for these species were .2.0 p.g ml for ciprofloxacin, 1.0 jig ml for sparfloxacin and PD 131, 628, and 0.5 p.g ml for CI-960. CI-960 was most active against Acinetobacter anitratus MIC90, 0.13 [xg ml ; , and ciprofloxacin was least active MIC90, 1.0 p.g ml ; . The relative activities of these four quinolones against nonenteric gram-negative bacilli as a group were as follows: CI-960 PD 131, 628 ciprofloxacin sparfloxacin. Only two-thirds of enterococcal isolates were susceptible to '1.0 pLg of ciprofloxacin per ml, the MIC90 for which was 2.0 , ug ml. Sparfloxacin and PD 131, 628 exhibited comparable activities against enterococci and Streptococcus agalactiae, and their MIC90s were half of those of ciprofloxacin. CI-960 was at least twice as active as the other quinolones against enterococci and S. agalactiae. The staphylococci exhibited some species variability in their susceptibilities to these four compounds. Although Staphylococcus aureus was generally susceptible to ciprofloxacin MIC90, 1.0 p.g ml ; , the MIC90s of the other three drugs were 8- to 16-fold lower. Whereas 66 6.7% ; of 984 S. aureus isolates were resistant MIC, -4.0 Rg ml ; to ciprofloxacin, 56 5.7% ; and 55 5.6% ; were resistant to sparfloxacin and PD 131, 628, respectively, and only 1 ; required -4.0 pLg of CI-960 per ml for inhibition. Sparfloxacin, ciprofloxacin, and PD 131, 628 had MIC90s of 2.0 pLg ml for Staphylococcus epidermidis and Staphylococcus haemolyticus, and for S. haemolyticus the MIC50s of these three drugs were also 2.0 Fg ml. But all isolates of these two species were susceptible to .1.0 , ug of CI-960 per ml. Other staphylococcal species were susceptible to all four drugs, but ciprofloxacin MICs were generally higher than those of the other compounds. These four quinolone compounds exhibit potent broadspectrum antibacterial activities against routine clinical bac.
Pharmacokinetics and tissue penetration of temafloxacin. Journal of Antimicrobial Chemotherapy 24, 415-24. Ofrila, J. & Haider, F. 1991 ; . In vitro susceptibility of Chlamydia pneumoniae strain 10L 207 to temafloxacin and other antimicrobial agents. In Program and Abstracts of the Thirty-First Intersdence Conference on Antimicrobial Agents and Chemotherapy, Chicago, IL, 1991. Abstract 679, p. 212. American Society for Microbiology, Washington, D C Perronne, C , Gikas, A., Truffot-Pemot, C , Grosset, J., Vilde, J. L. & Pocidalo, J. J. 1991 ; . Activities of sparfloxacin, azithromycin, temafloxacin and rifapentine compared with that of clarithromycin against multiplication of Mycobacterhan arium complex within human macrophages. Antimicrobial Agents and Chemotherapy 35, 1356-9. Piddock, L. J. V. & Zhu, M. 1991 ; . Mechanism of action of sparfloxacin against and mechanism of mJntBiKf in Gram-negative and Gram-positive bacteria. Antimicrobial Agents and Chemotherapy 35, 2423-7. Piercy, E. A., Barbara, D., Luby, J. P. A Mackowiak, P. A. 1989 ; . Ciprofloxacin for methicillin-resistant Staphylococcus aureus infections. Antimicrobial Agents and Chemotherapy 33, 128-30. Raoult, D., Bres, P., Drancourt, M. & Vestris, G. 1991 ; . In vitro susceptibilities of Coxiella bumetii, Rickettsia rickettsii, and Ricketuia conorii to the fluoroqirinolone sparfloxacin. Antimicrobial Agents and Chemotherapy 35, 88-91. Rastogi, N. & Goh, K. S. 1991J ; . In vitro activity of the new difluorinated quinolone sparfloxacin AT-4140 ; against Mycobacterium tuberculosis compared with activities of ofloxacin and ciprofloxacin. Antimicrobial Agents and Chemotherapy 35, 1933-6. Rastogi, N., Labrousse, V., Goh, K. S. & DeSousa, J. P. C. 19916 ; . Antimycobacterial spectrum of sparfloxacin and its activities alone and in association with other drugs against Mycobacterium arium complex growing extracellularly and intraceOularly in murine and human macrophages. Antimicrobial Agents and Chemotherapy 35, 2473-80. Rolston, K. V. I., Nguyen, H., Messer, M., Leblanc, B., Ho, D. H. &. Bodey, J. P. 1990 ; . In vitro activity of sparfloxacin CI-978; AT-4140 ; against clinical isolates from cancer patients. Antimicrobial Agents and Chemotherapy 34, 2263-6. Soejima, R., Shimada, K., Matsumoto, F., Mild, F. & Saito, A. 1991 ; . A multicenter double blind comparative study of sparfloxacin and ofloxacin in the treatment of bacterial pneumonia. In Program and Abstracts of the Thirty-First Interscience Conference on Antimicrobial Agents and Chemotherapy, Chicago, IL. 1991. Abstract 877, p. 245. American Society for Microbiology, Washington, DC. Swanson, R. N., Hardy, D. J., Chu, D. T. W and stanozolol.
Borrowing, a sparfloxacin purchaser are sparfloxacin some operate nationally and which.
In a double-blind, randomized, multicenter study, 428 patients with cap received 10 days of either 200 mg of sparfloxacin once daily following a single 400 mg loading dose ; , or 500 mg of erythromycin every six hours and stelazine.
Like it ; is going to completely change the way we write, read, teach, and learn. Biography C. Sidney Burrus received his PhD from Stanford University in 1965 and has been on the faculty at Rice University since then. He was a visiting professor at the University of Erlangen in Germany in 1975 and again in 1980 and was a visiting professor at MIT in 1990. He received a Humboldt Award, a Fulbright Fellowship, and various research awards from the IEEE over the years. He is a Fellow of the IEEE. He received teaching awards from Rice in 1975 etc. was department chair for ten years, and was the Dean of Engineering at Rice for seven years. Currently, he is the Maxfield and Oshman Emeritus Professor of Electrical Engineering. He has published 5 books and over 200 research articles, mostly in digital signal processing, and has been involved with the use of technology for education which resulted in the Connexions Project which started in 1999 and sparfloxacin.
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