Cephains
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Cephains

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  • or instance, certain antibiotics, like beta-lactams (penicillins, cephalosporins, carbapenems, monobactams), clindamycin, macrolides (erythromycin, clarithromycin), oxazolidinones (linezolid), can be effective because of the extensive amount of time the antibiotic binds to the microorganism. The inhibitory effect can be effective because their concentration exceeds the MIC for the microorganism.

Cephains Cephains Presentation Transcript

  • Pharmacology of Cephalosporins: General Overview Flavio Guzmán, M.D. http://pharmamotion.com.ar
  • β - lactams: cell wall inhibitors
  • β -lactam ring
    • The β -lactam ring is a common structure for:
      • Penicillins
      • Cephalosporins
      • Monobactams
      • Carbapenems
      • Bacteria will target this ring to gain resistance.
  • Cell wall inhibitors: important features
    • Cell wall inhibitors have bacericidal effect.
    • They act sinergistically with amynoglycosides
    • Time-dependent kinetics: the more time the drug binds the bacteria, the more effective it is.
  • Mechanism of action 1
    • Some PBP have transpeptidase activity.
    • Transpeptidase activity is essential in cell wall synthesis .
    • Beta-lactams bind PBP (Penicillin Binding Proteins).
  • Mechanism of action 2
  • Cephalosporins
  • Cephalosporins: characteristics
  • Chemical structure of cephalosporins
    • Derived from 7-aminocephalosporanic acid.
    • They suffer the “attack” of bacteria at their beta-lactam ring.
  • First gen. cephalosporins.:
  • 1st Generation cephalosporins: antibacterial coverage Active mainly against Gram positive cocci. Less active against Gram negative.
  • Clinical uses of first gen. cephalosporins
  • 2nd generation cephalosporins
  • 2nd generation cephalosporins. Antibiotic coverage
    • Increased coverage against Gram negatives, while keeping coverage against Gram +.
  • 3rd generation cephalosporins
  • 3rd generation cephalosporins Coverage Increased coverage against Gram negatives. Decreased coverage against Gram +
  • 3rd generation cephalosporins Clinical uses
  • Ceftriaxone and meningitis
  • 4th generation cephalosporins
  • 4th generation cephalosporins Antibacterial coverage Coverage against Gram + and Gram -, good activity against β -lactamase producing bacteria.
    • http://pharmamotion.com.ar