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Pharmacology of Cephalosporins : General Overview

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

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Pharmacology of Cephalosporins : General Overview

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  1. Pharmacology of Cephalosporins:General Overview Flavio Guzmán, M.D. http://pharmamotion.com.ar

  2. β- lactams: cellwallinhibitors

  3. β-lactam ring • Theβ-lactam ring is a commonstructurefor: • Penicillins • Cephalosporins • Monobactams • Carbapenems • Bacteria will target this ring togainresistance.

  4. Cellwallinhibitors: importantfeatures • Cellwallinhibitorshavebacericidaleffect. • Theyactsinergisticallywithamynoglycosides • Time-dependentkinetics: the more time thedrugbindsthe bacteria, the more effectiveitis.

  5. Mechanism of action 1 • Beta-lactams bind PBP (Penicillin Binding Proteins). • Some PBP havetranspeptidaseactivity. • Transpeptidaseactivityisessential in cellwallsynthesis.

  6. Mechanism of action 2

  7. Cephalosporins

  8. Cephalosporins: characteristics

  9. Chemicalstructure of cephalosporins • Derived from 7-aminocephalosporanic acid. • They suffer the “attack” of bacteria at their beta-lactam ring.

  10. First gen. cephalosporins.:

  11. 1st Generationcephalosporins: antibacterialcoverage Active mainly against Gram positive cocci. Less active against Gram negative.

  12. Clinical uses of first gen. cephalosporins

  13. 2nd generation cephalosporins

  14. 2nd generationcephalosporins. Antibioticcoverage Increased coverage against Gram negatives, while keeping coverage against Gram +.

  15. 3rd generation cephalosporins

  16. 3rd generationcephalosporinsCoverage Increased coverage against Gram negatives. Decreased coverage against Gram +

  17. 3rd generationcephalosporinsClinical uses

  18. Ceftriaxone and meningitis

  19. 4th generation cephalosporins

  20. 4th generationcephalosporinsAntibacterialcoverage Coverage against Gram + and Gram -, good activity against β-lactamase producing bacteria.

  21. http://pharmamotion.com.ar

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