Comparative Bioavailability of Intravenous and Oral Chloramphenicol in Adults

Abstract

The comparative bioavailability of chloramphenicol from intravenous succinate, oral palmitate, and oral base preparations was studied in a crossover manner in 12 adult patients. Chloramphenicol was administered at a dose of 1 Gm every 6 hours, and blood samples were collected at steady state. For the succinate study, total urine output was also collected. The bioavailability of active chloramphenicol from the succinate preparation averaged 85.8 +/- 42.3 and 78.8 +/- 50.1 per cent of the free base and palmitate forms, respectively. This lower availability appeared to be due to variable excretion of unchanged succinate in the urine, averaging 27 +/- 11 per cent of the dose. Regardless of dosage form or route of administration, plasma chloramphenicol concentrations remained in the therapeutic range (5 to 25 mg/liter) for the entire dosage interval, implying that no change needs to be made when changing dosage form or route of administration. The interpatient variability, however, supports the need for monitoring of plasma chloramphenicol concentrations, especially in newborn infants, persons with liver disease, or those receiving other medications that alter chloramphenicol metabolism.

Contribution of the Antibiotic Chloramphenicol and Its Analogues as Precursors of Dichloroacetamide and Other Disinfection Byproducts in Drinking Water

“…However, CAP is still widely used in livestock aquaculture as feed additives to control outbreaks of disease 21 . Previous studies have indicated that CAPs are stable and difficult to be metabolized after intake 22 and are ineffectively removed by wastewater treatment plants (WWTP) that apply conventional treatment processes. 23,24 Therefore, CAPs eventually reach surface waters that may be used as inputs to drinking water treatment plants.…”

Scientific Opinion on Chloramphenicol in food and feed

“…The hydrolysis of chloramphenicol succinate to chloramphenicol has been recently demonstrated to occur also in the bone marrow (Ambekar et al, 2000). Serum protein binding has been reported to be around 53 % in healthy adults, while only about 32 % in premature neonates (Koup et al, 1979 (Kramer et al, 1984).…”

“…Maximum concentration values ranging from 16.6 ± 4.23, 22.3 ± 7.64 and 22.8 ± 11.8 mg/L have been found in adults patients receiving chloramphenicol succinate i.v., chloramphenicol crystalline per os (p.o. ), or chloramphenicol palmitate p.o., respectively (Kramer et al, 1984).…”

“…or i.v. dosing results in variable percentages (up to 25-30 %) of the drug escaping hydrolysis to the active (de-esterified) form and undergoing prompt renal excretion (Kramer et al, 1984), likely by active tubular secretion (Ambrose, 1984). The hydrolysis of chloramphenicol succinate to chloramphenicol has been recently demonstrated to occur also in the bone marrow (Ambekar et al, 2000).…”

Hydrothermal Enhanced Nanoscale Zero-Valent Iron Activated Peroxydisulfate Oxidation of Chloramphenicol in Aqueous Solutions: Fe-Speciation Analysis and Modeling Optimization

“…Since the 1950s chloramphenicol (CAP) has acted as a widely applied broad-spectrum antibiotic with excellent antibacterial properties [1][2][3]. Approximately 16% to 38% of CAP potentially leaves organisms as a form of parent compound through feces or urine before being discharged into sewage [4]. It was reported that CAP was not effectively removed by traditional wastewater plants and largely reached surface waters, causing notable ecological risks [5,6].…”