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Fidaxomicin

  • MacrolidesMacrolides

Oral macrocyclic antibiotic that is hardly absorbed and acts in the gut against Clostridioides difficile, with few relapses.

Updated

Quick facts

Group
Macrolides
Target
Bacterial RNA polymerase (Clostridioides difficile)
Used for
Clostridioides difficile diarrhoea
Key effects
Nausea and vomiting · Abdominal pain · Constipation
Monitor
Number and look of stools · Signs of allergy
ATC
A07AA12

No doses: the clinician sets them by the current guideline.

Mechanism of action

The figure shows Clostridioides difficile RNA polymerase with fidaxomicin bound.

Target in 3D: Bacterial RNA polymerase (Clostridioides difficile). PDB structure 7L7B (RCSB PDB, public domain). View the structure at RCSB PDB

Fidaxomicin binds bacterial RNA polymerase and stops transcription from starting, so the bacterium makes no RNA. It is bactericidal against C. difficile and largely spares the normal gut flora. It barely reaches the blood, so it only works for infection of the colon.

  1. Taken by mouth, it stays in the gut lumen
  2. Binds C. difficile RNA polymerase
  3. Blocks the start of transcription
  4. Kills the bacterium and spares much of the flora

Indications

Adverse effects

Common

  • Nausea and vomiting
  • Abdominal pain
  • Constipation

Contraindications

  • Hypersensitivity to fidaxomicin or its ingredients

Key interactions

Ciclosporin and other P-glycoprotein inhibitors
Raise fidaxomicin blood levels, which stay very low; treatment is not changed.

What is monitored

  • Number and look of stools
  • Signs of allergy, above all with a history of macrolide allergy
  • Signs of relapse after treatment ends

Administration and safety

  • Oral, with or without food; a suspension also exists and is kept refrigerated
  • Does not treat infections outside the gut: it never replaces a systemic antibiotic

Pregnancy and breastfeeding

Data in pregnancy are not enough to know the risk; animal studies showed no fetal harm.

Nursing care

  • Ask about macrolide allergy
  • Reinforce hand washing with soap and water and contact precautions
  • Teach to finish the course
  • Ask the patient to report diarrhoea that comes back after treatment

Pharmacokinetics

Absorption
Minimal systemic absorption; blood levels are very low.
Metabolism
Hydrolysed to an active metabolite (OP-1118), without cytochrome P450.
Elimination
In the faeces: more than 92% of the dose is recovered there.
Half-life
About 12 hours for the drug and its metabolite (healthy adults).

Test yourself

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

Which enzyme does fidaxomicin act on?

Bacterial RNA polymerase: it stops transcription from starting in C. difficile.

Why is fidaxomicin useless for pneumonia?

It is hardly absorbed; it stays in the gut lumen and does not reach useful tissue levels.

What advantage does fidaxomicin have over oral vancomycin for C. difficile?

It spares more of the normal gut flora and is linked to fewer relapses.

Which allergy history calls for closer watch in someone receiving fidaxomicin?

Macrolide allergy: some people who reacted to fidaxomicin had it.

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Connections

← Back to the class: Macrolides

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

Sources: DailyMed - FIDAXOMICIN tablet, coated (DailyMed (U.S. National Library of Medicine), 2026); Fidaxomicin: MedlinePlus Drug Information (MedlinePlus (U.S. National Library of Medicine), 2026); Clostridioides difficile RNAP with fidaxomicin (RCSB Protein Data Bank, 2026).

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Representative model, for educational purposes only.