Pharmacology of Cephalosporins:

General Overview
Flavio Guzmán, M.D.
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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

•Beta-lactams bind PBP (Penicillin

Binding Proteins).

•Some PBP have

transpeptidase activity.
• Transpeptidase activity is
essential in cell wall
synthesis.
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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