Ceftobiprole
Beta-lactams
Beta-lactams
IV anti-MRSA cephalosporin that also covers Pseudomonas: it binds PBP2a. For pneumonia, bacteraemia and skin infections.
Also called: ceftobiprole medocaril
Quick facts
- Group
- Beta-lactams
- Target
- MRSA PBP2a and other PBPs
- Used for
- Certain bacterial pneumonias
- Key effects
- Nausea · Headache and insomnia
- Monitor
- Kidney function · Neurological status in people
- ATC
- J01DI01
No doses: the clinician sets them by the current guideline.
Mechanism of action
The figure shows methicillin-resistant Staphylococcus aureus PBP2a acylated by ceftobiprole in the active site.
Ceftobiprole medocaril is a prodrug rapidly converted to ceftobiprole. It acylates the PBPs, including PBP2a, which makes S. aureus methicillin-resistant and which other cephalosporins barely inhibit. Against gram-positives it resembles ceftaroline; against gram-negatives, including Pseudomonas, it resembles ceftazidime.
- The medocaril prodrug releases ceftobiprole in the blood
- Acylates MRSA PBP2a and other PBPs
- Wall cross-linking halts
- The bacterium lyses (bactericidal)
Indications
- Certain bacterial pneumonias
- Certain bloodstream infections (bacteraemia)
- Certain bacterial skin infections
Adverse effects
Common
- Nausea, vomiting, diarrhoea and abdominal pain
- Headache and insomnia
- Unusual taste in the mouth
- Infusion-site reactions
Contraindications
- Allergy to ceftobiprole or other cephalosporins
Key interactions
- Laboratory tests
- It may alter some results; the laboratory is told.
What is monitored
- Kidney function
- Neurological status in people with epilepsy or kidney failure
- Follow-up blood cultures in bacteraemia
Administration and safety
- Slow IV infusion of about 2 hours
- Name looks like ceftaroline and ceftazidime: the label is checked
Nursing care
- Ask about beta-lactam allergy, epilepsy and kidney disease
- Watch for seizures or changes in consciousness
- Watch the infusion site
- Ask the patient to report severe diarrhoea
Pharmacokinetics
- Absorption
- IV only.
- Metabolism
- The prodrug is rapidly converted to active ceftobiprole.
- Elimination
- Renal, like ceftaroline.
Test yourself
Think of the answer, then tap the question to see it.
Which protein lets ceftobiprole act against MRSA?
PBP2a, encoded by mecA, which ceftobiprole acylates and other cephalosporins barely inhibit.
How does ceftobiprole's spectrum differ from ceftaroline's?
Besides MRSA, it covers Pseudomonas aeruginosa, with a gram-negative spectrum similar to ceftazidime.
Which neurological adverse effect is watched with ceftobiprole?
Seizures, above all in people with epilepsy or kidney disease.
Connections
← 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: Ceftobiprole Medocaril Injection: MedlinePlus Drug Information (MedlinePlus (U.S. National Library of Medicine), 2026); Structural Insights into the Anti- Methicillin-Resistant Staphylococcus aureus (MRSA) Activity of Ceftobiprole (RCSB Protein Data Bank, 2026).
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Representative model, for educational purposes only.