Alatrofloxacin Mesylate - CAS 157605-25-9
Catalog number: 157605-25-9
Category: Inhibitor
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Antibacterial | Topoisomerase
The mesylate salt form of alatrofloxacin, a fluoroquinolone derivative, has been found to be a Type II DNA topoisomerase inhibitor that was once developed to be an antibacterial agent.
Alatrofloxacin mesylate; UNII-2IXX802851; Alatrofloxacin mesylate [USAN]; 2IXX802851; 7-[(1S,5R)-6-[[(2S)-2-[[(2S)-2-aminopropanoyl]amino]propanoyl]amino]-3-azabicyclo[3.1.0]hexan-3-yl]-1-(2,4-difluorophenyl)-6-fluoro-4-oxo-1,8-naphthyridine-3-carboxylic; CP 116,517; CP 116517; CP-116,517; CP-116517;
Store in a cool and dry place and at 0 - 4 °C for short term (days to weeks) or -20 °C for long term (months to years).
Quality Standard:
In-house standard
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1.Activity of trovafloxacin (CP-99,219) against Legionella isolates: in vitro activity, intracellular accumulation and killing in macrophages, and pharmacokinetics and treatment of guinea pigs with L. pneumophila pneumonia.
Edelstein PH;Edelstein MA;Ren J;Polzer R;Gladue RP Antimicrob Agents Chemother. 1996 Feb;40(2):314-19.
The activity of trovafloxacin against 22 clinical Legionella isolates was determined by broth microdilution susceptibility testing. The trovafloxacin concentration required to inhibit 90% of strains tested was < or = 0.004 micrograms/ml, in contrast to 0.032 micrograms/ml for ofloxacin. In guinea pig alveolar macrophages, trovafloxacin achieved intracellular levels up to 28-fold over the extracellular concentration, which was similar to the levels obtained with erythromycin. Trovafloxacin (0.25 micrograms/ml) reduced bacterial counts of two L. pneumophila strains grown in guinea pig alveolar macrophages by > 2 log10 CFU/ml, without regrowth, under drug-free conditions over a 3-day period; trovafloxacin was significantly more active than ofloxacin or erythromycin (0.25 to 1 microgram/ml) in this assay. Single-dose (10 mg of prodrug CP-116,517-27 per kg of body weight given intraperitoneally [i.p.], equivalent to 7.5 mg of trovafloxacin per kg) pharmacokinetic studies performed in guinea pigs with L. pneumophila pneumonia revealed peak serum and lung trovafloxacin levels to be 3.8 micrograms/ml and 5.0 micrograms/g, respectively, at 0.5 h and 4.2 micrograms/ml and 2.9 micrograms/g, respectively, at 1 h.
2.Stability of alatrofloxacin mesylate in 5% dextrose injection and 0.45% sodium-chloride injecion.
Gupta VD;Bailey RE Int J Pharm Compd. 2000 Jan-Feb;4(1):66-8.
A high-performance liquid chromatographic assay method for the quantitation of alatrofloxacin in intravenous (IV) admixtures has been developed. The method is accurate and precise, with a percent relative standard deviation of 1.2% based on five injections. The method is stability indicating since the product of decomposition, trovafloxacin, did not interfere with the assay procedure. The IV admixtures of alatrofloxacin (1.88 mg/mL) in 5% dextrose and 0.45% sodium-chloride injections were stable for at least nine days when stored at room themperature. The pH values of the admixtures did not change and they remained clear throughout this study.
3.Trovafloxacin-associated leukopenia.
Mitropoulos FA;Angood PB;Rabinovici R Ann Pharmacother. 2001 Jan;35(1):41-4.
OBJECTIVE: ;To report a case of trovafloxacin-associated leukopenia, which occurred in a trauma patient shortly after administration and resolved following discontinuation of the drug.;CASE SUMMARY: ;A 79-year-old white man was admitted to Yale New Haven Hospital after sustaining partial amputation of his right lower leg by an industrial lawn mower. After successful resuscitation, he underwent complete right lower amputation and was treated with intravenous alatrofloxacin mesylate. He developed leukopenia that resolved after discontinuation of the drug.;DISCUSSION: ;Trovafloxacin is a broad-spectrum synthetic fluoroquinolone used for a wide variety of bacterial infections. We report, for the first time in the English-language literature, a case of trovafloxacin-associated leukopenia. The leukopenia resolved promptly after discontinuation of the drug. This association is further supported by the exclusion of other potential causes for this adverse effect.;CONCLUSIONS: ;Leukopenia is a well-recognized adverse effect of several drugs. We report a case of trovafloxacin-associated leukopenia during treatment of a trauma patient. Healthcare personnel should be aware of this possible adverse reaction in patients treated with trovafloxacin.
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