Pirfenidone (Esbriet) is a pyridone-based medication used for the treatment of idiopathic pulmonary fibrosis (IPF). Its use must strictly follow the dose titration protocol, and the dosage should be adjusted based on liver function, drug interactions, and specific patient populations.

How to Use Pirfenidone (Esbriet)

Administration Method

Pirfenidone must be taken with food to reduce gastrointestinal adverse reactions (such as nausea and dizziness).

The total daily dose is 2403 mg (3 capsules of 267 mg each, taken three times a day).

Dose Titration

Days 1–7: 1 capsule (267 mg) three times a day, with a total daily dose of 801 mg.

Days 8–14: 2 capsules (534 mg) three times a day, with a total daily dose of 1602 mg.

From Day 15 onwards: 3 capsules (801 mg) three times a day, maintaining a total daily dose of 2403 mg.

If treatment is interrupted for <14 days, the original dose can be resumed directly; if the interruption lasts ≥14 days, dose titration must be repeated.

Dosage Adjustment of Pirfenidone (Esbriet)

Adjustment for Hepatic Impairment

ALT/AST > 3×ULN (asymptomatic): Discontinue concurrent hepatotoxic medications, monitor closely, and reduce the dose or discontinue pirfenidone as appropriate.

ALT/AST > 3×ULN with symptoms or hyperbilirubinemia: Permanently discontinue pirfenidone.

ALT/AST > 5×ULN: Immediately discontinue pirfenidone permanently.

Gastrointestinal Reactions

In case of persistent nausea, diarrhea, or dyspepsia, the dose can be temporarily reduced to 1602 mg per day or treatment can be paused. After symptoms resolve, the dose should be gradually resumed.

Adjustment for Drug Interactions

Strong CYP1A2 inhibitors (e.g., fluvoxamine): Concomitant use is contraindicated; if unavoidable, reduce the dose to 1 capsule (267 mg) three times a day.

Moderate CYP1A2 inhibitors (e.g., ciprofloxacin 750 mg twice daily): Reduce the dose to 2 capsules (534 mg) three times a day.

Use in Special Populations for Pirfenidone (Esbriet)

Patients with Hepatic Impairment

Mild to moderate impairment (Child-Pugh Class A/B): Use with caution, monitor liver function, and reduce the dose if necessary.

Severe impairment (Child-Pugh Class C): Contraindicated.

Patients with Renal Impairment

Mild to moderate impairment (CLcr 30–80 mL/min): Monitor for adverse reactions and adjust the dose in a timely manner.

Severe impairment (CLcr < 30 mL/min) or dialysis patients: Use is not recommended.

Smokers

Smoking can reduce the plasma concentration of pirfenidone, thereby affecting its therapeutic effect. It is recommended that patients quit smoking before starting treatment and avoid smoking during treatment.

Pregnant and Lactating Women

Pregnancy: Pirfenidone should be used only if the potential benefit outweighs the potential risk (animal studies have not shown teratogenicity, but data in humans are limited).

Lactation: Pirfenidone may be excreted in breast milk; it is recommended that either the medication be discontinued or breastfeeding be stopped.