ANTIBIOTICS-1

Anmerkungen:

• bind to cyto PBP, inh. transpeptidation, inh. cross-linking of bacterial cell wall

1. PENICILLINS, CEPHALOSPORINS,
   1. IMIPENEM, MEROPENEM, ASTREONAM VANCOMYCIN

      Anmerkungen:

      • vancomycin - Inhibits peptidoglycan synthases bind to D-Alanine
   2. B-lactamase cleavage of drugs B-lactam ring

1. Interfere with formation of initiation complex
   1. BACTERICIDAL

      Anmerkungen:

      • misread genetic code carried by mRNA resulting in the incorperatino of wrong aa
      1. AMINOGLYCOSIDE (30S), LINEZOLID (50S)
         1. production of conjugatingenzymes that increase drugs clearance
2. Interfere with incorporation of next aa
   1. BACTERIOSTATIC

      Anmerkungen:

      • inh. insertion of aminoacyl t-RNA into "A" site
      1. TETRACYCLINS (30S), DILFOPRISTIN & QUINUPRISTIN (50S)
         1. production of active transport systems that push drugs out of the cell

            Anmerkungen:

            • tetracyclins
3. Interfere with formation of peptide bond
   1. BACTERIOSTATIC

      Anmerkungen:

      • inh. peptidyltransferase
      1. CHLORAMPHENICOL
         1. formation of acetylating ensymes that inactivate drugs

            Anmerkungen:

            • chloramphenicol
4. Interfere with translocation
   1. BACTERIOSTATIC

      Anmerkungen:

      • Inh. translocation of peptidyl-tRNA from acceptor donor site
      1. MACROLIDE (50S), CLINDAMYCIN(50S)
         1. methylation of base in RNA that alter drugs binding

            Anmerkungen:

            • macrolides

1. SULFONAMIDE

   Anmerkungen:

   • inh. duhydropteroate synthetase
   1. formation of a PABA, increase resistance to inhibition of dihydropteroate synthetase
2. TRIMETHOPRIN & PYRIMETHAMINE

   Anmerkungen:

   • inh. dihydrofolate reductase

1. FLUOROQUINOLONES

   Anmerkungen:

   • inh. DNA gyrase (topiosomerase 2)
   1. increase transport systems to push drugs out. increase resistance to inh. of topio. 2

      Anmerkungen:

      • antibiotic resistance.  R-factor plasmid-mediated transmission. selection of resistance cells 
2. RIFAMPIN

   Anmerkungen:

   • inh. DNA-dep RNA polymerase