Ceftaroline, a fifth-generation cephalosporin, is active against MRSA because of which unique pharmacological property?

• A Resistance to beta-lactamase hydrolysis by ESBL-producing organisms
• B High affinity for PBP2a (PBP2'), the altered penicillin-binding protein encoded by mecA gene ✓
• C Inhibition of transpeptidase and transglycosylase simultaneously
• D Efflux pump inhibition restoring susceptibility to older cephalosporins

Explanation

MRSA resistance to beta-lactams is conferred by acquisition of the mecA gene encoding PBP2a (PBP2'), an altered penicillin-binding protein with very low affinity for most beta-lactams. Ceftaroline's unique chemical structure allows it to bind and inhibit PBP2a with high affinity, making it the only cephalosporin with anti-MRSA activity. This is structurally distinct from earlier cephalosporins that cannot bind PBP2a. It does not work via efflux inhibition or dual enzyme inhibition.

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

High-yield for: NEET PGINI-CETNExTFMGEUSMLEPLABMRCP

Written and medically reviewed by the StethoPrep medical team.