Pharmacology · Antimicrobials (Cell Wall Inhibitors, Protein Synthesis Inhibitors, Fluoroquinolones)

Ceftaroline, a 5th-generation cephalosporin, is unique among cephalosporins because it is active against MRSA. Its mechanism of action against MRSA is:

  • A Inhibition of the mecA gene expression via transcriptional repression
  • B Direct inhibition of beta-lactamase enzyme produced by MRSA strains
  • C Disruption of the MRSA cell membrane through a mechanism similar to polymyxins
  • D High affinity binding to PBP2a (PBP2'), the altered penicillin-binding protein that confers MRSA resistance
Correct answer: D. High affinity binding to PBP2a (PBP2'), the altered penicillin-binding protein that confers MRSA resistance

Explanation

Ceftaroline is a cephalosporin with the ability to bind and inhibit PBP2a (PBP2') — the modified penicillin-binding protein encoded by mecA that normally evades all standard beta-lactams. Structural studies show ceftaroline's bulky side chain can interact with the allosteric and active sites of PBP2a, unlike older beta-lactams. It is not a beta-lactamase inhibitor, does not affect mecA gene expression, and has no membrane-disrupting (polymyxin-like) activity.

Reference: KD Tripathi, Essentials of Medical Pharmacology, 8th ed.

High-yield for: NEET PGINI-CETNExTFMGEUSMLEPLABMRCP

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