Ceftaroline is a novel cephalosporin active against MRSA. Its mechanism of anti-MRSA activity involves:
- A Inhibiting the mecA gene transcription via a novel efflux pump blockade
- B Synergistic action with vancomycin against the cell wall D-Ala-D-Lac terminus
- C Irreversible binding to PBP2a with higher affinity than other beta-lactams ✓
- D Forming a dual inhibitor complex with both PBP2a and beta-lactamase
Explanation
Ceftaroline has a unique R1 side chain that allows it to bind PBP2a (encoded by mecA), the low-affinity PBP responsible for MRSA resistance, with sufficient affinity to inhibit cell wall cross-linking and produce bactericidal activity. Conventional beta-lactams have negligible affinity for PBP2a. Ceftaroline does not affect mecA gene expression, does not form dual complexes with beta-lactamases, and its mechanism is independent of vancomycin's action on D-Ala-D-Lac termini (which is relevant to vancomycin-resistant enterococci).
Reference: KD Tripathi, Essentials of Medical Pharmacology, 8th ed.
High-yield for: NEET PGINI-CETNExTFMGEUSMLEPLABMRCP
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