Inhibitors of bacterial protein synthesis 2 Flashcards
Nitrobenzene antibiotic
Chloramphenicol
Chloramphenicol - MoA
It binds reversibly to the 50S subunit of the bacterial ribosome and inhibits peptide bond formation
Chloramphenicol - Clinical use
Broad-spectrum antibiotic that is active against pathogens causing meningitis, including pneumococci, meningococci, and H. influenzae Salmonella Bacteroides Brain abcess Rickettsiae (typhus, rocky mountain spotted fever) Neiserria meningitidis
Chloramphenicol - Special considerations
High concentrations in CNS Lipophilic, well absorbed from gut Partly metabolized by glucoronate conjugation (neonates obs)
Chloramphenicol - Adverse effects
Gray baby syndrome characterized by cyanosis, weakness, respiratory depression, and shock Reversible, dose-dependent anemia caused by blockade of iron incorporation into heme Aplastic anemia (rare) Nausea, vomiting, diarrhea, Oral/vaginal candidiasis
Chloramphenicol and Clindamycin: Administration Elimination
Clindamycin: Oral, IV or Topical Hepatic metabolism; renal excretion Chloramphenicol: IV Hepatic metabolism; renal, biliary and fecal excretion
Streptogramin antibiotic
Quinupristin-Dalfopristin
Quinupristin-Dalfopristin - MoA
Binds to 50S ribosomal subunit. Inhibits tRNA synthesis + inhibits peptidyl transferase Inhibits protein synthesis when administered in 30:70.
Quinupristin-Dalfopristin - Clinical use
Bactericidal against susceptible strains of staphylococci and streptococci but bacteriostatic against Enterococcus faecium Active against many gram-postitive bacteria, including multidrug-resistant straphylococci, penicillin-resistant pneumococci, and vancomycin-resistant E. faecium, but not E. fecalis Bacteremia Pneumonia Skin and soft tissue infections Peritonitis Endocarditis Aortic graft infections
Quinupristin-Dalfopristin - Adverse effects
Infusion site reactions Arthralgia Myalgia Diarrhea Nausea
Linezolid - MoA
Binds to 23S ribosomal RNA of the 50S subunit, preventing formation of 70S initiation complex
Linezolid - Clinical use
Active against aerobic gram-positive bacteria Bactericidal against most strains of streptococci Bacteriostatic against enterococci and staphylococci Vancomycin-resistant E. faecium; pneumonia caused by methicillin-sensitive S. aureus and MRSA; and skin and soft tissue infections caused by methicillin-sensitive or methicillin-resistant staphylococci and Streptococcus pyogenes, or Steptococcus agalactiae Given IV for serious infections such as necrotizing fasciits and pneumonia Orally for mild to moderate skin and soft tissue infections
Linezolid - Adverse effects
serotonin toxicity with fluoxetine Thrombocytopenia Anemia Neutropenia in patients with renal insufficiency or during prolonged therapy
Mupirocin - MoA
Competetive inhibition of isoleucine, preventing addition of isoleucine to protein
Mupirocin - Clinical use
Active against gram-positive cocci, including most strains of methicillin-resistant staphylococci Impetigo by streptococci and staphylococci Nasal colonization of methicillin-resistant staphylococci