Generic Medicine Info
Indications and Dosage
Idiopathic pulmonary fibrosis
Adult: Initially, 267 mg tid for 7 days, then increase dose to 534 mg tid for 7 days, then to usual maintenance dose: 801 mg tid. Max: 2403 mg daily. Adjust dosage according to toxicity.
Special Patient Group
Patient concomitantly using strong CYP1A2 inhibitors (e.g. enoxacin, fluvoxamine): 267 mg tid.
Patient concomitantly using ciprofloxacin at a dosage of 750 mg bid: 534 mg tid.
Renal Impairment
ESRD requiring haemodialysis: Contraindicated.
CrCl (mL/min) Dosage
<30 Contraindicated.
Hepatic Impairment
Severe (Child-Pugh class C): Contraindicated.
Severe hepatic and renal impairment, ESRD requiring haemodialysis.
Special Precautions
Smokers. Mild to moderate hepatic and renal impairment. Pregnancy and lactation. Patient taking fluvoxamine and ciprofloxacin.
Adverse Reactions
Significant: Nausea, vomiting, diarrhoea, dyspepsia, GERD, abdominal pain, photosensitivity, weight loss, dizziness, increased ALT/AST, angioedema. Rarely, hyperbilirubinaemia.
Gastrointestinal disorders: Constipation, flatulence, gastritis.
General disorders and administration site conditions: Fatigue, asthenia, lethargy, non-cardiac chest pain.
Investigations: Increased γ-glutamyl transferase.
Metabolism and nutrition disorders: Anorexia, decreased appetite.
Musculoskeletal and connective tissue disorders: Myalgia, arthralgia.
Nervous system disorders: Headache, dysgeusia.
Psychiatric disorders: Insomnia, somnolence.
Renal and urinary disorders: UTI.
Respiratory, thoracic and mediastinal disorders: Dyspnoea, cough, upper respiratory tract infection.
Skin and subcutaneous tissue disorders: Rash, pruritus, erythema, dry skin, sunburn.
Vascular disorders: Hot flush.
Patient Counseling Information
Avoid smoking. This drug may cause dizziness and fatigue, if affected, do not drive or operate machinery. Avoid excessive exposure to sun and UV light.
Monitoring Parameters
Perform LFT before initiation of treatment, monthly for the 1st 6 months and quarterly, thereafter. Monitor weight; signs and symptoms of gastrointestinal and photosensitivity reactions.
Drug Interactions
Increased toxicity with strong (e.g. fluvoxamine) and moderate (e.g. ciprofloxacin) CYP1A2 inhibitors. Decreased efficacy with CYP1A2 inducers (e.g. omeprazole).
Food Interaction
Decreased absorption with food. May increase toxicity with grapefruit juice.
Mechanism of Action: Pirfenidone, a synthetic pyridone, is an antifibrotic agent. Its exact mechanism of action is still unknown. In idiopathic pulmonary fibrosis, it may decrease the amount of pro-inflammatory cells [e.g. interleukin-1-β (IL-1β), IL-6, tumour necrosis factor-α (TNF-α)] and the production of fibroblast and of fibrosis-associated proteins and cytokines. It may also decrease accumulation of extracellular matrix and lung fibrosis due to transforming growth factor-β (TGF-β) and platelet derived growth factor (PDGF).
Absorption: Absorbed from the gastrointestinal tract. Decreased absorption with food. Time to peak plasma concentration: 30 minutes to 4 hours.
Distribution: Volume of distribution: Approx 59-71 L. Plasma protein binding: 50-58% mainly to albumin.
Metabolism: Metabolised in the liver mainly by CYP1A2 and to a lesser extent by CYP2C9, 2C19, 2D6 and 2E1 into metabolites including 5-carboxy-pirfenidone.
Excretion: Mainly via urine (approx 80%; >95% as 5-carboxy-pirfenidone and <1% as unchanged drug). Terminal elimination half-life: Approx 3 hours.
Chemical Structure

Chemical Structure Image

Source: National Center for Biotechnology Information. PubChem Database. Pirfenidone, CID=40632, https://pubchem.ncbi.nlm.nih.gov/compound/Pirfenidone (accessed on Jan. 22, 2020)

Store at 25°C.
MIMS Class
ATC Classification
L04AX05 - pirfenidone ; Belongs to the class of other immunosuppressants.
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Esbriet 267 mg Hard Capsules (Roche Products Limited). eMC. https://www.medicines.org.uk/emc/. Accessed 30/01/2018.

Esbriet 801 mg Film-coated Tablets (Roche Products Limited). eMC. https://www.medicines.org.uk/emc/. Accessed 30/01/2018.

Esbriet Capsule; Esbriet Tablet, Coated (Genentech, Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 30/01/2018.

Joint Formulary Committee. Pirfenidone. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 30/01/2018.

McEvoy GK, Snow EK, Miller J et al (eds). Pirfenidone. AHFS Drug Information (AHFS DI) [online]. American Society of Health-System Pharmacists (ASHP). https://www.medicinescomplete.com. Accessed 30/01/2018.

Rossi S (ed). Pirfenidone. Australian Medicines Handbook [online]. Adelaide. Australian Medicines Handbook Pty Ltd. https://amhonline.amh.net.au. Accessed 30/01/2018.

Disclaimer: This information is independently developed by MIMS based on Pirfenidone from various references and is provided for your reference only. Therapeutic uses, prescribing information and product availability may vary between countries. Please refer to MIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, MIMS shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise. Copyright © 2024 MIMS. All rights reserved. Powered by MIMS.com
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