Cephalosporins
- BP-S-6-Medicinal Chemistry III
- Mar 28
- 1 min read
Updated: Mar 29
Chemical Structure / Formula of Cephalosporins
Core Structure: β-lactam ring fused to a dihydrothiazine ring (unlike penicillins, which have a thiazolidine ring).
Different generations have variable side chains affecting their spectrum of activity.

Mechanism of Action
Similar to penicillins: inhibit bacterial cell wall synthesis by targeting penicillin-binding proteins (PBPs), leading to bacterial lysis.
More resistant to β-lactamases compared to penicillins.
Uses
First-generation: Gram-positive coverage (Staphylococcus, Streptococcus).
Second-generation: Increased Gram-negative activity (Haemophilus, Enterobacter).
Third generation: Broad-spectrum, effective against resistant Gram-negative bacteria (Pseudomonas, Neisseria).
Fourth/Fifth generation: Advanced activity against MDR bacteria and MRSA (Fifth generation).
Side Effects
Common: Diarrhea, nausea, rash.
Serious: Hypersensitivity reactions, C. difficile infection, nephrotoxicity (rare).