Pirfenidone

Pirfenidone is a prescription medication used to treat the symptoms of Idiopathic Pulmonary Fibrosis. 

• Pirfenidone is available under the following different brand names: Esbriet

Dosages of Pirfenidone:

Adult dosage

Capsule

• 267 mg

Tablet

• 267 mg
• 801 mg

Idiopathic Pulmonary Fibrosis

Initial dose titration

Take with food

• Days 1-7: 267 mg orally three times daily (801 mg/day)
• Days 8-14: 534 mg orally three times daily (1602 mg/day)
• Day 15 and thereafter (maintenance): 801 mg orally three times daily; not to exceed 2403 mg/day)
• Pediatric use: safety and efficacy not established 

Dosage Considerations – Should be Given as Follows: 

• See “Dosages”.

Common side effects of Pirfenidone include:

• nausea, 
• vomiting, 
• loss of appetite, 
• stomach pain, 
• heartburn, 
• upset stomach, 
• diarrhea, 
• headache, 
• dizziness, 
• tiredness, 
• weight loss, 
• stuffy nose, 
• sneezing, 
• sore throat, 
• joint pain, and 
• sleep problems (insomnia)

Serious side effects of Pirfenidone include:

• hives, 
• difficulty breathing, 
• swelling of the face, lips, tongue, or throat, 
• severe ongoing stomach pain, 
• vomiting, 
• diarrhea, 
• burning or pain in the esophagus or throat, 
• stomach pain (upper right side), 
• easy bruising, 
• unusual bleeding, 
• tiredness, 
• dark urine, 
• clay-colored stools, and
• yellowing of the skin or eyes

Rare side effects of Pirfenidone include:

• none 

If your medical doctor is using this medicine to treat your pain, your doctor or pharmacist may already be aware of any possible drug interactions and may be monitoring you for them.  Do not start, stop, or change the dosage of any medicine before checking with your doctor, health care provider, or pharmacist first

• Pirfenidone has severe interactions with the following drugs:
  • carbamazepine
  • phenobarbital
  • primidone
  • rifampin
• Pirfenidone has serious interactions with at least 22 other drugs.
• Pirfenidone has moderate interactions with the following drugs:
  • cannabidiol
  • fexinidazole
  • rucaparib
  • stiripentol
• Pirfenidone has minor interactions with no other drugs

This information does not contain all possible interactions or adverse effects. Visit the RxList Drug Interaction Checker for any drugs interactions. Therefore, before using this product, tell your doctor or pharmacist of all the products you use.  Keep a list of all your medications with you, and share this information with your doctor and pharmacist.  Check with your health care professional or doctor for additional medical advice, or if you have health questions, concerns.

Contraindications

• None

Effects of drug abuse

• None

Short-Term Effects

• See “What Are Side Effects Associated with Using Pirfenidone?”

Long-Term Effects

• See “What Are Side Effects Associated with Using Pirfenidone?”

Cautions

• Photosensitivity and rash reported; avoid or minimize exposure to sunlight (including sunlamps), to use a sunblock (SPF 50 or higher), and to wear clothing that protects against sun exposure; additionally, instruct patients to avoid concomitant medications known to cause photosensitivity; dosage reduction or discontinuation may be necessary in some cases of photosensitivity reaction or rash
• Nausea, vomiting, diarrhea, dyspepsia, gastroesophageal reflux disease, and abdominal pain reported; incidence of gastrointestinal events reported to be highest early in the course of treatment (with the highest incidence occurring during initial 3 months); may decrease over time; temporary dosage reductions or discontinuations may be required

Drug-induced liver injury

• Conduct liver function tests (ALT, AST, and bilirubin) before initiating, monthly for 6 months, and then q3months thereafter and as clinically indicated
• Patients treated with 2403 mg/day reported having a higher incidence of elevated ALT/AST in clinical trials
• Measure liver function tests promptly in patients who report symptoms that may indicate liver injury, including fatigue, anorexia, right upper abdominal discomfort, dark urine, or jaundice
• Dosage modifications, interruption, or discontinuation may be necessary to reverse liver enzyme elevation

Drug interaction overview

• Pirfenidone is a CYP1A2 substrate; discontinue moderate or strong CYP1A inhibitors before initiating pirfenidone and avoid use during therapy; if unable to avoid, pirfenidone dose reduction required
• Discontinue strong CYP1A2 inducers before initiating pirfenidone and avoid use during therapy; likely to decrease exposure and lead to loss of pirfenidone efficacy
• Smoking associated with decreased systemic exposure; encourage patient to quit smoking

Pregnancy and Lactation

• Pregnancy: Data in pregnant women are insufficient to inform on drug-associated risks for major birth defects and miscarriage
• Lactation: No information is available on the presence of pirfenidone in human milk, effects of the drug on the breastfed infant, or effects of the drug on milk production; lack of clinical data during lactation precludes clear determination of the risk of pirfenidone to infant during lactation; developmental and health benefits of breastfeeding should be considered along with mother’s clinical need for therapy and potential adverse effects on the breastfed child from pirfenidone or underlying maternal condition