A prodrug form of chloramphenicol
Chloramphenicol succinate is a water-soluble prodrug form of the antibiotic chloramphenicol.1 It is a substrate for succinate dehydrogenase (SDH) and is oxidized by human liver and rat liver and kidney mitochondria to release chloramphenicol in vitro.2 Chloramphenicol succinate reduces human leukocyte migration in vitro.3 In vivo, chloramphenicol succinate reduces E. coli growth in rabbit and rat models of pyelonephritis when administered at doses of 150 and 200 mg/kg, respectively.4 Chloramphenicol succinate (20 mg/kg) reduces infarct size in a porcine model of myocardial ischemia-reperfusion injury.5 Formulations containing chloramphenicol succinate have been used in the treatment of severe bacterial infections.
1.Ceriotti, G., Defranceschi, A., De Carneri, I., et al.Chloramphenicol succinate, a water-soluble derivative of chloramphenicolFarmaco Sci.9(1)21-38(1954) 2.Ambekar, C.S., Lee, J.S., Cheung, B.M., et al.Chloramphenicol succinate, a competitive substrate and inhibitor of succinate dehydrogenase: Possible reason for its toxicityToxicol. In Vitro18(4)441-447(2004) 3.Forsgren, A., and Schmeling, D.Effect of antibiotics of chemotaxis of human leukocytesAntimicrob. Agents Chemother.11(4)590-584(1977) 4.Prat, V., Konickova, L., Ritzerfeld, W., et al.Effect of chloramphenicol against different E. coli strains in vitro and in experimental pyelonephritisArzneimittelforschung18(9)1123-1127(1968) 5.Sala-Mercado, J.A., Wider, J., Undyala, V.V., et al.Profound cardioprotection with chloramphenicol succinate in the swine model of myocardial ischemia-reperfusion injuryCirculation122(11 Suppl)S179-S184(2010)
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