PHARMACO - Chloramphenicol Flashcards
?S ribosomes in bacteria
70
?S ribosomes in mammalians
80
Basis for selective toxicity against microorganisms without causing major effects on mammalian cells
3 Differences
Ribosomal subunits
Chemical composition
Functional specificities of component nucleic acids and proteins
General MoA
Bactericidal
General binding at what ribosome
50S except for tetracycline
Inhibits transpeptidation (catalyzed by peptidyl transferase)
chloramphenicol
Blocks the binding of aminoacyl moiety of tRNA to mRNA complex so the peptide at the donor site cannot be transferred to the amino acid acceptor
chloramphenicol
Bind at 50S-block translocation of peptidyl-tRNA from the acceptor site to the donor site
Macrolides, telithromycin, and clindamycin
Bind to 30S
Tetracyclines
Blocks the binding of amino-acid-charged tRNA to the acceptor site
Tetracyclines
Constrict the exit channel on the ribosome through which polypeptides are extruded tRNA synthase activity is inhibited
Streptogramins
inhibits tRNA synthase activity
Streptogramins
bactericidal AB which bind to the 50S
Streptogramins
Bacteriostatic
Binds to a unique site at 50S
Blocks formation of tRNA-ribosome-mRNA complex
Linezolid
Broad spectrum
chloramphenicol
tetracycline
moderate spectrum
macrolides
ketolides
narrow spectrum
lincosamides
streptogramins
linezolid
newer antibiotics
streptogramins
linezolid
Are there other antimicrobial drugs in chloramphenicol class
No
RoA of Chloramphenicol
Oral as well as parenteral
Tissue distribution of Chloramphenicol
Distributed throughout all tissues
Crosses placental and blood-brain barriers
Chloramphenicol
Undergoes enterohepatic cycling
Chloramphenicol
tetracycline
Enzyme that inactivates chloramphenicol
hepatic glucoronosyltransferase
Does Chloramphenicol undergo enterohepatic cycling
Yes
Fraction excreted in urine unchanged or changed in chloramphenicol?
unchanged
MoA of Chloramphenicol
Bacteriostatic
When does Chloramphenicol become bactericidal
H. influenzae
N. meningitidis
Bacteroides
Is chloramphenicol effective for chlamydia
No
Resistance to chloramphenicol
Plasmid mediated-formation of acetyl- transferases that inactivate the drug
chloramphenicol is Rarely used as a systemic drug because
of its toxicity
Backup drug for severe infections caused by salmonella
chloramphenicol
Treatment of pneumococcal and meningococcal meningitis in beta-lactam-sensitive persons
chloramphenicol
Commonly used as topical agent
chloramphenicol