[Durgical](https://durgical.com/en/) › [DurgiPedia](https://durgical.com/en/durgipedia/) › [Pharmacology](https://durgical.com/en/pharmacology/) › [Beta-lactams](https://durgical.com/en/pharmacology/classes/beta-lactams/) › Ceftaroline

[Pharmacology](https://durgical.com/en/pharmacology/) · [Beta-lactams](https://durgical.com/en/pharmacology/classes/beta-lactams/)

# Ceftaroline

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

Updated 2026-11-01

- Class: [Beta-lactams](https://durgical.com/en/pharmacology/classes/beta-lactams/)
- Enzyme: MRSA PBP2a and other PBPs
- ATC code: J01DI02

Also called: ceftaroline fosamil

✂**MRSA PBP2a and other PBPs**Ceftaroline

ⓘ 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](https://www.rcsb.org/structure/3ZG0) · Drag to rotate · pinch to zoom

## 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 →](https://durgical.com/en/conditions/cellulitis-of-the-leg/)
- Community-acquired bacterial pneumonia. [Community-acquired pneumonia →](https://durgical.com/en/conditions/community-acquired-pneumonia/)

## Adverse effects

### Common

- Diarrhoea, nausea, rash
- Positive direct Coombs test, common

### Serious (rare, important)

- Anaphylaxis
- Clostridioides difficile diarrhoea, from mild to severe colitis
- Haemolytic anaemia (rare)
- Encephalopathy and seizures, especially with kidney failure

## 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.

## Memory aid

'Ceftaroline rolls over MRSA': the cephalosporin in this group that unlocks PBP2a.

## 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)](https://durgical.app/estudiar/?add=/en/pharmacology/ceftaroline/)

## Related drugs

- [Cefazolin](https://durgical.com/en/pharmacology/cefazolin/)
- [Nafcillin](https://durgical.com/en/pharmacology/nafcillin/)
- [Ceftriaxone](https://durgical.com/en/pharmacology/ceftriaxone/)

## Related conditions

- [Cellulitis of the leg](https://durgical.com/en/conditions/cellulitis-of-the-leg/)
- [Community-acquired pneumonia](https://durgical.com/en/conditions/community-acquired-pneumonia/)

[← Back to the class: Beta-lactams](https://durgical.com/en/pharmacology/classes/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](https://medlineplus.gov/druginfo/meds/a611014.html) (MedlinePlus (U.S. National Library of Medicine), 2026); [DailyMed - CEFTAROLINE FOSAMIL injection, powder, lyophilized, for solution](https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=9ec2cc88-fbec-a5aa-df85-ecff7350d813) (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](https://www.rcsb.org/structure/3ZG0) (RCSB Protein Data Bank, 2026); Farmacología básica y clínica (Katzung), cap. 43 (McGraw Hill, 2025).

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Representative model, for educational purposes only.

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Source: https://durgical.com/en/pharmacology/ceftaroline/
License: CC BY 4.0 (https://creativecommons.org/licenses/by/4.0/). Cite as: DurgiPedia (durgical.com), https://durgical.com/en/pharmacology/ceftaroline/