Trovafloxacin/alatrofloxacin

CH4O3S 75-75-2) see Alatrofloxacin mesilate Alendronate sodium Dolasetron mesilate Glaziovine Nelfinavir mesylate Tirilazad mesilate Trovafloxacin mesilate... 

Hall, I. H., Schwab, U. E., Ward, E. S., and Ives, T. J. Effects of alatrofloxacin, the parental prodrug of trovafloxacin, on phagocytic, anti-inflammatory and immunomod-ulation events of human THP-1 monocytes. Biomed. Pharmacother. 57(8) 359—365, 2003. 

Alatrofloxacin is a fluoronaphthyridone that is hydrolysed to the active moiety, trovafloxacin, after intravenous administration. This fourth-generation broad-spectrum fluoroquinolone has activity against Gram-positive, Gram-negative, anerobic, and atypical respiratory pathogens. Because it has significant hepato-toxicity, the list of appropriate indications for trovafloxacin has been restricted. 

Seizures are rare but have occurred during treatment with other fluoroquinolones. This is the first report of a case of seizures associated with slow infusion of alatrofloxacin. However, as of 21 June 2000, the manufacturers had received 53 reports of seizures through worldwide postmarketing surveillance. In rat hippocampus slices, trovafloxacin had significant convulsive potential the underlying mechanism is hitherto incompletely understood. 

During clinical trials, thrombocytopenia occurred in under 1% of more than 7000 patients who received alatrofloxacin or trovafloxacin. 

The pharmacokinetics of a single intravenous dose of alatrofloxacin have been determined in six infants aged 3-12 months and in 14 children aged 2-12 years (14). The peak trovafloxacin concentration at the end of the infusion was 4.3 pg/ml the volume of distribution at steady state was 1.61/kg, clearance 2.5 ml/min/kg, and the half-life 9.8 hours, with no age-related differences. Less than 5% of the administered dose was excreted in the urine over 24 hours. 

The pharmacokinetics of trovafloxacin after the administration of alatrofloxacin were not substantially altered in seven critically ill patients (three men, four women) with APACHE II scores of 27 (range 15-32) and normal or mildly impaired hepatic function (15). 

Bradley JS, Kearns GL, Reed MD, Capparelli EV, Vincent J. Pharmacokinetics of a fluoronaphthyridone, trovafloxacin (CP 99,219), in infants and children following administration of a single intravenous dose of alatrofloxacin. Antimicrob Agents Chemother 2000 44(5) 1195-9. 

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