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

# Oxacillin

An intravenous penicillinase-resistant penicillin for serious infections by methicillin-susceptible Staphylococcus aureus.

Updated 2026-11-01

- Class: [Beta-lactams](https://durgical.com/en/pharmacology/classes/beta-lactams/)
- Enzyme: Penicillin-binding proteins (bacterial transpeptidases)
- ATC code: J01CF04

✂**Penicillin-binding proteins (bacterial transpeptidases)**Oxacillin

ⓘ The figure shows Staphylococcus aureus PBP1 inhibited by oxacillin, bonded to the active-site serine.

**Target in 3D:** Penicillin-binding proteins (bacterial transpeptidases). PDB structure 8VBU (RCSB PDB, public domain). [View the structure at RCSB PDB](https://www.rcsb.org/structure/8VBU) · Drag to rotate · pinch to zoom

## Mechanism of action

Oxacillin is a parenteral isoxazolyl penicillin. It belongs to the penicillins resistant to staphylococcal β-lactamase: its bulky side chain keeps penicillinase from opening the β-lactam ring, so it acylates the PBPs of penicillinase-producing staphylococci. It does not work against MRSA, whose PBP2a has low affinity for β-lactams.

- Staphylococcal penicillinase cannot open its ring
- Acylates the staphylococcal PBPs
- Peptidoglycan cross-linking stops
- The staphylococcus lyses

## Pharmacokinetics

**Absorption**
Intravenous or intramuscular.

**Elimination**
By the kidney and by liver inactivation and bile; usually no adjustment in kidney failure.

**Half-life**
Short, under one hour.

## Indications

- Skin and soft-tissue infections due to penicillinase-producing staphylococci. [Cellulitis of the leg →](https://durgical.com/en/conditions/cellulitis-of-the-leg/)
- Staphylococcal osteomyelitis and septic arthritis. [Osteomyelitis →](https://durgical.com/en/conditions/osteomyelitis/)
- Bacteraemia and endocarditis due to methicillin-susceptible S. aureus. [Infective endocarditis →](https://durgical.com/en/conditions/infective-endocarditis/)

## Adverse effects

### Common

- Phlebitis at the infusion site
- Rash, fever
- Raised transaminases

### Serious (rare, important)

- Anaphylaxis
- Renal tubular damage and interstitial nephritis
- Liver dysfunction with fever, nausea and raised transaminases; blood disorders
- Clostridioides difficile diarrhoea, from mild to severe colitis

## Contraindications

- History of a hypersensitivity reaction to any penicillin
- Dextrose-containing solutions may be contraindicated with corn allergy

## Key interactions

**Tetracyclines**
Bacteriostatic: they can antagonise the bactericidal effect; the combination is avoided.

**Probenecid**
Reduces tubular secretion: higher and longer-lasting β-lactam levels.

## What is monitored

- Periodic kidney and liver function and blood count in long courses
- Cultures and susceptibility

## Administration and safety

- Intravenous; premixed bags are for intravenous use only.
- Do not confuse oxacillin with other similarly named antistaphylococcal penicillins.

## Nursing care

- Before the first dose: ask about allergy to penicillins, cephalosporins and other β-lactams, and what the reaction was.
- Watch for fever, rash, urine changes and creatinine (interstitial nephritis).
- Check the IV site for phlebitis.
- Teach the patient to report watery or bloody diarrhoea, even weeks after the course ends.

## Pregnancy and breastfeeding

Animal studies showed no fetal harm and there are no controlled studies in pregnant women; used if clearly needed.

## Memory aid

'OXA-cillin: OK for MSSA, eXit for MRSA': MRSA's PBP2a does not let it work.

## Test yourself

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

## Why does oxacillin not work against MRSA?

Because MRSA carries PBP2a, a PBP with low affinity for β-lactams.

## Which kidney toxicity is linked to oxacillin?

Tubular damage and interstitial nephritis, both uncommon.

## Does oxacillin need adjustment in kidney failure?

Generally not, because it is also cleared by the liver and bile.

[Add to my cards (3)](https://durgical.app/estudiar/?add=/en/pharmacology/oxacillin/)

## Related drugs

- [Nafcillin](https://durgical.com/en/pharmacology/nafcillin/)
- [Cloxacillin](https://durgical.com/en/pharmacology/cloxacillin/)
- [Dicloxacillin](https://durgical.com/en/pharmacology/dicloxacillin/)
- [Cefazolin](https://durgical.com/en/pharmacology/cefazolin/)

## Related conditions

- [Cellulitis of the leg](https://durgical.com/en/conditions/cellulitis-of-the-leg/)
- [Osteomyelitis](https://durgical.com/en/conditions/osteomyelitis/)
- [Infective endocarditis](https://durgical.com/en/conditions/infective-endocarditis/)

[← 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: [Oxacillin Injection: MedlinePlus Drug Information](https://medlineplus.gov/druginfo/meds/a685020.html) (MedlinePlus (U.S. National Library of Medicine), 2026); [DailyMed - OXACILLIN injection, solution](https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=d893e45b-7f18-4c67-b10c-1e2e52a6b3ef) (DailyMed (U.S. National Library of Medicine), 2026); [RCSB PDB - 8VBU: Structure of the monofunctional Staphylococcus aureus PBP1 in its beta-lactam (Oxacillin) inhibited form](https://www.rcsb.org/structure/8VBU) (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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