MOA: Bhave

  1. PCN MOA
    • ● Bind transpeptidases (PBPs) and block catalysis of crosslinking of peptidoglycan residues resulting in weak cell walls and bacterial lysis if bacteria are actively growing
    • ● Bactericidal
  2. β-lactamase Inhibitors MOA
    • ● Contain b-lactam ring, which:
    • → Act as decoy
    • → Binding to and inhibit β-lactamases
  3. Vancomycin MOA
    • ● Cell wall synthesis inhibitor
    • → Binds to D-Ala-D-Ala building block of peptidoglycan
    • → Blocks transpeptidase binding (peptidoglycan cross linking)
  4. Bacitracin MOA
    • ● Bactoprenol transfers peptidoglycan subunits to the growing cell wall
    • ● Bacitracin inhibits dephosphorylation in cycling of the lipid carrier
  5. Fosfomycin MOA
    • ● Drug is transported to the bacterial cell by glycerolphosphate or glucose 6-phosphate transport system
    • ● Inhibits the cytoplasmic enzyme enolpyruvate transferase and eventually inhibits synthesis of N-acetylmuramic acid (NAM)
  6. Daptomycin MOA
    • ● Lipid portion (tail) of molecule inserts into bacterial cell membrane forming a channel
    • → Depolarization of cell membrane
    • → Potassium efflux
    • → Rapid cell lysis
  7. Sulfonamides MOA
    • ● Inhibits Dihydropteroate synthase from forming dihydrofolic acid
    • ● Bacteriostatic
  8. Pyrimidines MOA
    • ● Selectively inhibits bacterial dihydrofolate reductase, which converts dihydrofolic acid to tetrahydrofolic acid, a step leading to the synthesis of purines and ultimately to DNA
    • ● Bacteriostatic
  9. Fluoroquinolones MOA
    • ● Block bacterial DNA synthesis by inhibiting
    • → Bacterial topoisomerase II (DNA gyrase- Inhibition of DNA gyrase prevents the relaxation of positively supercoiled DNA that is required for normal transcription and replication)
    • → Topoisomerase IV (Inhibition of topoisomerase IV interferes with separation of replicated chromosomal DNA into the respective daughter cells during cell division)
  10. Aminoglycosides MOA
    • ● Ribosomal protein synthesis inhibitor (irreversible binding to 30s ribosomal subunit)
    • → Block the formation of the initiation complex
    • → Miscoding of amino acids in the emerging peptide chain due to misreading of the mRNA
    • → Block the translocation on mRNA
    • ● Block of movement of the ribosome may occur after the formation of a single initiation complex, resulting in an mRNA chain with only a single ribosome on it, a so-called monosome
  11. Tetracyclines MOA
    • ● Bind reversibly to 30S
    • ● Bacteriostatic
  12. Macrolides MOA
    Binding to 50S
  13. Oxazolidine MOA
    Binds to the 23S ribosomal RNA of 50S
  14. Clindamycin MOA
    Binding to 50S
  15. Metronidizole MOA
    • ● Taken up by diffusion selectively absorbed by anaerobic bacteria and sensitive protozoa
    • ● It is non-enzymatically reduced by pyruvate:ferredoxin oxido-reducatase system
    • ● Reduced nitroso intermediates from linkages with cysteine bearing enzymes deactivating various cellular enzymes
    • ● Metronidazole metabolites are taken up into bacterial DNA, strand breakage, destabilization
  16. Muporicin MOA
    • ● Blocks the activity of isoleucyl-tRNA synthetase
    • ● Blocks protein synthesis
  17. Nitrofurantoin MOA
    Reduced by falvoproteins (nitrofurantoin redutase) to multiple reactive intermediates that attack ribosomal proteins, DNA, metabolic processes and other macromolecules
  18. Isoniazid MOA
    • ● Inhibits synthesis of mycolic acids of the cell wall (FAS II)
    • ● [Low] bacteriostatic
    • ● [High] bactericidal
  19. Rifampicin MOA
    • Inhibition of RNA synthesis by binding to the subunit of RNA polymerase (transcription)
    • Bactericidal
  20. Ethambutol MOA
    • ● Inhibits mycobacterial cell wall synthesis by inhibiting arabinosyl transferase
    • ● Bacteriostatic
  21. Pyrazinamide MOA
    • ● Inhibits fatty acid (FAS I) synthetase, involved in synthesis of short chain mycolic acid
    • ● Bacteriostatic and bactericidal
  22. Ethionamide MOA
    Blocks synthesis of mycolic acid (FAS II)
  23. Capreomycin MOA
    Inhibition of protein synthesis (blocking translation)
  24. Aminosalicylic Acid (PAS) MOA
    Inhibit folate synthesis (Dihydropteroate synthase preventing synthesis of dihydrofolic acid from PABA)
Card Set
MOA: Bhave
ID 1 (Final): MOA (Bhave)