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192         SEcTioN ii    Microbiology  ` microbiology—aNtimicrobials                                                                                           Microbiology  ` microbiology—aNtimicrobials





               Tetracyclines         Tetracycline, doxycycline, minocycline.
                mecHaNism            Bacteriostatic; bind to 30S and prevent attachment of aminoacyl-tRNA. Limited CNS penetration.
                                       Doxycycline is fecally eliminated and can be used in patients with renal failure. Do not take
                                                                            2+
                                       tetracyclines with milk (Ca ), antacids (eg, Ca  or Mg ), or iron-containing preparations
                                                                                   2+
                                                            2+
                                       because divalent cations inhibit drugs’ absorption in the gut.
                cliNical Use         Borrelia burgdorferi, M pneumoniae. Drugs’ ability to accumulate intracellularly makes them very
                                       effective against Rickettsia and Chlamydia. Also used to treat acne. Doxycycline effective against
                                      community-acquired MRSA.
                aDVerse eFFects      GI distress, discoloration of teeth and inhibition of bone growth in children, photosensitivity.
                                       Contraindicated in pregnancy.
                mecHaNism oF resistaNce   uptake or  efflux out of bacterial cells by plasmid-encoded transport pumps.



               Tigecycline
                mecHaNism            Tetracycline derivative. Binds to 30S, inhibiting protein synthesis. Generally bacteriostatic.
                cliNical Use         Broad-spectrum anaerobic, gram ⊝, and gram ⊕ coverage. Multidrug-resistant organisms (MRSA,
                                       VRE) or infections requiring deep tissue penetration.
                aDVerse eFFects      GI symptoms: nausea, vomiting.


               Chloramphenicol

                mecHaNism            Blocks peptidyltransferase at 50S ribosomal subunit. Bacteriostatic.
                cliNical Use         Meningitis (Haemophilus influenzae, Neisseria meningitidis, Streptococcus pneumoniae) and
                                      rickettsial diseases (eg, Rocky Mountain spotted fever [Rickettsia rickettsii]).
                                     Limited use due to toxicity but often still used in developing countries because of low cost.
                aDVerse eFFects      Anemia (dose dependent), aplastic anemia (dose independent), gray baby syndrome (in premature
                                       infants because they lack liver UDP-glucuronosyltransferase).
                mecHaNism oF resistaNce  Plasmid-encoded acetyltransferase inactivates the drug.


               Clindamycin

                mecHaNism            Blocks peptide transfer (translocation) at 50S
                                       ribosomal subunit. Bacteriostatic.
                cliNical Use         Anaerobic infections (eg, Bacteroides spp.,   Treats anaerobic infections above the diaphragm
                                       Clostridium perfringens) in aspiration   vs metronidazole (anaerobic infections below
                                       pneumonia, lung abscesses, and oral      diaphragm).
                                       infections. Also effective against invasive
                                       group A streptococcal infection.
                aDVerse eFFects      Pseudomembranous colitis (C difficile
                                       overgrowth), fever, diarrhea.





















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