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Microbiology  ` microbiology—aNtimicrobials      Microbiology  ` microbiology—aNtimicrobials          SEcTioN ii       191




                  Protein synthesis inhibitors                                    Specifically target smaller bacterial ribosome
                   Aminoglycosides (30S)  Initiation complex formation             (70S, made of 30S and 50S subunits), leaving
                               50S                                                 human ribosome (80S) unaffected.
                    Linezolid                    70S
                     (50S)             30S                                        All are bacteriostatic, except aminoglycosides
                                                 M
                                                                                   (bactericidal) and linezolid (variable).
                             Initiation  M
                           Initiator tRNA       U A  C
                                               5´  A U G C  A U G  A U  3´        30S inhibitors
                              mRNA  U A  C    E  P  A
                                                                                  Aminoglycosides
                                                                                  Tetracyclines
                                                     H
                                                 M
                                                                                  50S inhibitors
                                                    G U A
                                                U A  C  A-site tRNA binding  Tetracyclines (30S)  Chloramphenicol, Clindamycin
                                                A U G C  A U G  A U               Erythromycin (macrolides)
                                               5´            3´
                                              E  P  A                             Linezolid
                                                          Peptidyl transferase  Chloramphenicol
                                                                         (50S)
                                                                                  “Buy AT 30, CCEL (sell) at 50.”
                                                              M
                                      M                       H
                                       H      Elongation   M
                                   U A  C
                                      G U  A              U A  C G U  A
                    5´      U  G A  3´  A U G C  A U  G A U  A U G C  A U G  A U
                                  5´            3´       5´            3´
                       Termination  E  P  A             E  P  A
                                                                     Macrolides and
                                                Translocation
                                                                     Clindamycin (50S)
                  Aminoglycosides        Gentamicin, Neomycin, Amikacin,          “Mean” (aminoglycoside) GNATS caNNOT
                                          Tobramycin, Streptomycin.                 kill anaerobes.
                   mecHaNism             Bactericidal; irreversible inhibition of initiation
                                          complex through binding of the 30S subunit.
                                          Can cause misreading of mRNA. Also block
                                          translocation. Require O 2  for uptake; therefore
                                          ineffective against anaerobes.
                   cliNical Use          Severe gram ⊝ rod infections. Synergistic with
                                          β-lactam antibiotics.
                                         Neomycin for bowel surgery.
                   aDVerse eFFects       Nephrotoxicity, Neuromuscular blockade
                                          (absolute contraindication with myasthenia
                                          gravis), Ototoxicity (especially with loop
                                          diuretics), Teratogenicity.
                   mecHaNism oF resistaNce  Bacterial transferase enzymes inactivate the
                                          drug by acetylation, phosphorylation, or
                                          adenylation.

























          FAS1_2019_03-Microbiology.indd   191                                                                         11/14/19   12:22 PM
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