Protein synthesis inhibitors - Lincosamides

Question 1

Clindamycin

Answer 1

• Bacteriostatic
• most G+ aerobes, G+ and G- anaerobes
  
  • ​NOT G- aerobes
  • **MRSA **
• ​indicated = serious infections by anaerobic bacteriodes, mixed infections of anaerobes
• **PO and parenteral **
• penetrates into tissue (NO CNS)
• metabolized in liver
• **renal and hepatic excretion **
• MOA = binds L15 protein of 50S and inhibits protein synthesis by inhibiting translocation; premature release of polypetides by preventing exit of the nascent polypeptide chain
• adverse effects =
  
  • **pseudomembranous colitis (C diff) **(tx w/ PO metronidazole or PO vanc)
• resistance = **only constitutive methylase producing strains are resistant **(does not induce the inducible form of methylase - which adds methly group to binding site so decreases affinity for drug)
  
  • Clinda is NOT a substrate for macrolide efflux pumps
  • cross resistance to other macrolides
  • G - are intrinsically resistant due to poor perm of OMM