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.
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Ceorins

Editor's Notes

  • #5 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.