Abstract
Chloramphenicol (CAP) and nitrosochloramphenicol (NO-CAP) were metaboli-cally reduced to aromatic amines by rat liver microsomes in vitro. The reduction required anaerobic conditions and was mediated by a NADPH-dependent reductase system. Both CAP and NO-CAP reduction were time and concentration dependent. Compared to CAP, NO-CAP (0.5 mM) reduction was rapid with complete conversion occurring in 90–120 min. At 2.5 mM NO-CAP reduction was depressed. In the presence of NO-CAP (0.05–2.5 mM) CAP metabolism was inhibited from 17 to 91 %. These results indicate that CAP and NO-CAP are metabolized by similar microsomal reductase systems and NO-CAP is unstable, readily reduced further to the aromatic amine.
| Original language | English (US) |
|---|---|
| Pages (from-to) | 58-64 |
| Number of pages | 7 |
| Journal | Pharmacology |
| Volume | 27 |
| Issue number | 1 |
| DOIs | |
| State | Published - Jan 1 1983 |
Keywords
- Chloramphenicol
- Enzymatic reduction
- Nitrosochloramphenicol
- Rat liver microsomes
ASJC Scopus subject areas
- Pharmacology
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Cite this
Lim, L. O., & Yunis, A. A. (1983). Enzymatic reduction of chloramphenicol and nitrosochloramphenicol by rat liver microsomal preparations. Pharmacology, 27(1), 58-64. https://doi.org/10.1159/000137830