Generic
Pirfenidone
15 brands available in the market
At a glance
Pirfenidone is an antifibrotic medication used for the treatment of idiopathic pulmonary fibrosis (IPF). It reduces fibrosis (scarring) and swelling in the lungs, making breathing easier.
Description
Pirfenidone is a novel agent with anti-inflammatory, antioxidant, and anti-fibrotic properties. It may improve lung function and reduce acute exacerbations in IPF patients. A key anti-fibrotic mechanism involves suppression of TGF-β1, a key cytokine involved in fibrogenesis and extracellular matrix production. It also downregulates pro-inflammatory cytokines including TNF-α, interleukin-1, and interferon-gamma.
Indications
- Idiopathic Pulmonary Fibrosis (IPF) (mild to moderate)
Therapeutic class
Immunosuppressant
Pharmacological class
Antifibrotic Agent
Pharmacology
Pirfenidone suppresses TGF-β1, a key cytokine involved in fibrogenesis and extracellular matrix production. It also downregulates pro-inflammatory cytokines including TNF-α, interleukin-1, and interferon-gamma. In animal models, it inhibits inflammatory cell influx and bleomycin-induced pulmonary vascular permeability.
Mechanism of action
Reduces fibrosis and inflammation by suppressing TGF-β1 and pro-inflammatory cytokines.
Dosage
Adult Dose (Oral):
- Days 1-7: 267 mg (1 capsule) three times daily
- Days 8-14: 534 mg (2 capsules) three times daily
- Day 15 and thereafter: 801 mg (3 capsules) three times daily with food
- Max 2403 mg/day (9 capsules/day)
- Hepatic impairment (mild-moderate): Use caution; consider dosage modification or discontinuation
- Severe hepatic impairment: Not recommended
- If 14+ consecutive days missed, re-initiate with titration regimen
Administration
- Take with food
- Swallow tablet whole; do not chew, crush or break
Missed dose
If you miss a dose, take it as soon as you remember; skip if it's almost time for next dose; do not double the dose.
Side effects
Common Side Effects:
- Nausea
- Rash
- Abdominal pain
- Upper respiratory tract infection
- Diarrhea
- Fatigue
- Headache
- Dyspepsia
- Dizziness
- Vomiting
- Anorexia
- GERD
- Sinusitis
- Insomnia
- Weight loss
- Arthralgia
Precautions & warnings
- Elevated liver enzymes (ALT, AST, bilirubin) may occur; monitor before and during treatment
- Photosensitivity and rash may occur; avoid sun exposure and sunlamps; use sunscreen and protective clothing
- Gastrointestinal disorders (nausea, vomiting, diarrhea, dyspepsia) may occur; temporary dose reduction or discontinuation
- May affect driving ability; do not drive if drowsy or dizzy
- Smoking reduces treatment efficacy; quit smoking
Contraindications
- Hypersensitivity to pirfenidone or any excipient
- Concomitant use with fluvoxamine
- Severe hepatic impairment or end-stage liver disease
- Severe renal impairment (CrCl <30 mL/min) or ESRD requiring dialysis
Drug interactions
- CYP1A2 inhibitors (ciprofloxacin, fluvoxamine): Increase systemic exposure of pirfenidone; discontinue fluvoxamine or reduce dose to 267 mg three times daily
- Omeprazole, rifampicin: Lowered plasma levels
- Grapefruit juice: Inhibition of CYP1A2
Food interactions
Take with food for better absorption and reduced adverse reactions; it is not known whether it is safe to consume alcohol.
Use in pregnancy
Use in Pregnancy: No data for use in pregnant women; high doses in animals prolonged gestation and reduced fetal viability; avoid during pregnancy.
Pregnancy Category: C — always consult a doctor before taking during pregnancy.
Use in lactation
Use in Lactation: Unknown if pirfenidone or its metabolites are excreted in human milk; animal data shows excretion in milk; decide whether to discontinue breastfeeding or therapy.
Pediatric use
Safety and efficacy not established in children and adolescents.
Geriatric use
No dose adjustment required in elderly patients.
Renal / hepatic impairment
Renal Impairment: Use caution; consider dose modification or discontinuation; not recommended in dialysis patients.
Hepatic Impairment: Use caution; consider dose modification or discontinuation; not recommended in severe hepatic impairment.
Overdose effects
Limited clinical experience with overdose; at doses up to 4806 mg/day, adverse reactions were mild, transient, and consistent with common side effects.
Storage conditions
Store in a cool and dry place, protected from light and moisture; keep out of reach of children.
Chemical structure
Pirfenidone