Chopramphenicol
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This document discusses the pharmacokinetics of the antibiotic chloramphenicol. It is well absorbed in the gastrointestinal tract and widely distributed throughout the body, including into the central nervous system. It is metabolized in the liver. Chloramphenicol is effective against both gram-positive and gram-negative bacteria but has more effect on gram-negatives. Its uses are now limited due to its toxicity, especially in newborn infants where it can cause a potentially fatal gray baby syndrome.
Chopramphenicol
- 2. CONTENTS • Pharmacokinetics • Absorption • Distribution • Fate and excretion
- 3. INTRODUCTION Although an effective broad-spectrum antibiotics, its uses are limited by its serious toxicity. Now is rarely used except for severe infective diseases. It is well absorbed and widely distributed, including to the CNS. It is metabolized by glucuroni-dation in the liver.
- 4. PHARMACOLOGIC EFFECTS Chloramphenical is active against a broad range of organisms, including G+and G- bacteria (including anaerobes). But, its effects on G-bacteria is better than on G+ bacteria, especially Salmonella typhi.
- 6. ABSORPTION Absorbed from the GIT tract. Peak con. Of 10 to 13ug/ml occurs with in 2 to 3 hr after the administration of 1g dose . The hydrolysis of cholremphenicol succinate is due to the esterases enzyme present in kidney, liver and lungs. Poor renal function in the neonates and other state of renal insufficiency result in increased plasma conc. Of chloremphinicol succinate
- 10. CHLORAMPHENICOL Mechanisms of action Mechanisms of resistance Clinical uses Adverse effects
- 11. MECHANISMS OF ACTION inhibits bacterial protein synthesis. CAP binds 50S subunit and block elongation by inhibiting the formation of initiation complexes and peptidyltransferase; CAP is primarily bacteriostatic, but it may be bactericidal to some strains of microorganisms even at lower concentration:
- 14. MECHANISMS OF RESISTANCE reduced membrane permeability mutation of the 50S ribosomal subunit elaboration of chloramphenicol acetyltransferase
- 15. ADVERSE EFFECTS
- 16. . Toxicity for Newborn Infants (Gray-baby syndrome) Be seen in neonates, especially premature infants, who have been given relatively large doses of CAP. The inadequate renal elimination mechanism of neonate and the inactive metabolites also contributes to the occurrence of the syndrome.
- 17. . Gastrointestinal reaction. nausea, vomiting,diarrhea . Hypersensitivity reactions . A rare anemia, probably immunological in origin but often fatal
- 20. DRUG INTERACTION Irreversibly inhibit the microsomal enzyme p-450. Conversely other drug may alter the elimination of chloremphenicol