Ceftaroline !

An intravenous cephalosporin active against methicillin-resistant Staphylococcus aureus (MRSA), for skin infections and pneumonia.

Updated 2026-11-01

Class: Beta-lactams
Enzyme: MRSA PBP2a and other PBPs
ATC code: J01DI02

Also called: ceftaroline fosamil

MRSA PBP2a and other PBPsCeftaroline

The figure shows MRSA PBP2a acylated by ceftaroline in the active site; the crystal holds another ceftaroline molecule in the allosteric site.

Target in 3D: MRSA PBP2a and other PBPs. PDB structure 3ZG0 (RCSB PDB, public domain). View the structure at RCSB PDB

Mechanism of action

Ceftaroline fosamil is a prodrug that releases ceftaroline in the blood. Ceftaroline binds with high affinity to PBP2a, the mecA-encoded transpeptidase that makes MRSA resistant to almost every β-lactam, and inactivates it, restoring bactericidal action against these strains. It also covers pneumococci and many enteric bacteria, but not Pseudomonas, and ESBLs destroy it.

The fosamil prodrug releases ceftaroline in the blood
Binds MRSA PBP2a with high affinity
Acylates PBP2a so MRSA cannot cross-link its wall
The wall fails and the staphylococcus lyses

Pharmacokinetics

Absorption: Intravenous only; the prodrug is rapidly converted to active ceftaroline.
Elimination: Mainly by the kidney; adjusted in kidney failure.

Indications

Acute bacterial skin and skin-structure infections, including those due to MRSA. Cellulitis of the leg →
Community-acquired bacterial pneumonia. Community-acquired pneumonia →

Adverse effects

Common

Diarrhoea, nausea, rash
Positive direct Coombs test, common

Contraindications

Known serious hypersensitivity to ceftaroline or other cephalosporins

Key interactions

Direct Coombs test: May turn positive without haemolysis; if anaemia appears, drug-induced haemolytic anaemia is investigated.

What is monitored

Blood count if anaemia appears (rule out haemolysis)
Kidney function

Administration and safety

Intravenous infusion only.
Do not confuse ceftaroline with ceftriaxone or ceftazidime.

Nursing care

Before the first dose: ask about allergy to penicillins, cephalosporins and other β-lactams, and what the reaction was.
Watch for pallor, jaundice or dark urine (haemolysis).
In kidney failure, watch for confusion, myoclonus or seizures (drug accumulation).
Teach the patient to report watery or bloody diarrhoea, even weeks after the course ends.

Pregnancy and breastfeeding

There are no adequate studies in pregnant women; animal studies showed no malformations.

Test yourself

Think of the answer, then tap the question to see it.

How does MRSA resist almost every β-lactam, and why does ceftaroline work?

It expresses PBP2a (mecA gene), with low affinity for β-lactams; ceftaroline binds it with high affinity and inactivates it.

Which lab finding is common with ceftaroline, and what does it mean?

A positive direct Coombs test; if anaemia appears, drug-induced haemolytic anaemia is investigated.

Does ceftaroline cover Pseudomonas aeruginosa?

No; its gram-negative spectrum is broad but does not include Pseudomonas.

Add to my cards (3)

← Back to the class: Beta-lactams

Educational content on how drugs work; not a prescribing guide and no substitute for a health professional's advice. No doses are given.

Sources: Ceftaroline Injection: MedlinePlus Drug Information (MedlinePlus (U.S. National Library of Medicine), 2026); DailyMed - CEFTAROLINE FOSAMIL injection, powder, lyophilized, for solution (DailyMed (U.S. National Library of Medicine), 2026); RCSB PDB - 3ZG0: Crystal structure of ceftaroline acyl-PBP2a from MRSA with non- covalently bound ceftaroline and muramic acid at allosteric site obtained by cocrystallization (RCSB Protein Data Bank, 2026); Farmacología básica y clínica (Katzung), cap. 43 (McGraw Hill, 2025).

Spotted a mistake?We are always improving for the community. Tell us what is wrong and our team will review it.Report a mistake

Representative model, for educational purposes only.