Pirfenidone 267mg Tablets
It is used to treat idiopathic pulmonary fibrosis.
Drug Class
Antifibrotic agent
Pharmacologic Class
Pyridone derivative
Pregnancy Category
Not available
FDA Approved
Oct 2014
DEA Schedule
Not Controlled
Overview
What is this medicine?
Pirfenidone is a medicine used to treat a lung disease called idiopathic pulmonary fibrosis (IPF). IPF causes scarring in the lungs, making it harder to breathe. Pirfenidone helps slow down the progression of this scarring.
How to Use This Medicine
Taking Your Medication
To get the most benefit from your medication, follow these steps:
Take your medication exactly as directed by your doctor.
Read all the information provided with your medication and follow the instructions carefully.
Take your medication with food to help your body absorb it properly.
Take your medication at the same time every day to establish a routine.
Continue taking your medication as prescribed by your doctor or healthcare provider, even if you start to feel better.
Storing and Disposing of Your Medication
To keep your medication safe and effective:
Store your medication at room temperature in a dry place, away from the bathroom.
Keep the lid tightly closed to protect the medication from moisture and other environmental factors.
Keep all medications in a safe and secure location, out of the reach of children and pets.
Dispose of unused or expired medications properly. Do not flush them down the toilet or pour them down the drain unless instructed to do so by your pharmacist or healthcare provider. Check with your pharmacist for guidance on the best way to dispose of your medication, and consider participating in a drug take-back program in your area.
What to Do If You Miss a Dose
If you miss a dose of your medication:
Take the missed dose as soon as you remember, with food.
If it's close to the time for your next dose, skip the missed dose and resume your regular schedule.
Do not take two doses at the same time or take extra doses.
Do not take more than three doses in a 24-hour period.
If you miss 14 or more days of taking your medication, contact your doctor before restarting your medication regimen.
To get the most benefit from your medication, follow these steps:
Take your medication exactly as directed by your doctor.
Read all the information provided with your medication and follow the instructions carefully.
Take your medication with food to help your body absorb it properly.
Take your medication at the same time every day to establish a routine.
Continue taking your medication as prescribed by your doctor or healthcare provider, even if you start to feel better.
Storing and Disposing of Your Medication
To keep your medication safe and effective:
Store your medication at room temperature in a dry place, away from the bathroom.
Keep the lid tightly closed to protect the medication from moisture and other environmental factors.
Keep all medications in a safe and secure location, out of the reach of children and pets.
Dispose of unused or expired medications properly. Do not flush them down the toilet or pour them down the drain unless instructed to do so by your pharmacist or healthcare provider. Check with your pharmacist for guidance on the best way to dispose of your medication, and consider participating in a drug take-back program in your area.
What to Do If You Miss a Dose
If you miss a dose of your medication:
Take the missed dose as soon as you remember, with food.
If it's close to the time for your next dose, skip the missed dose and resume your regular schedule.
Do not take two doses at the same time or take extra doses.
Do not take more than three doses in a 24-hour period.
If you miss 14 or more days of taking your medication, contact your doctor before restarting your medication regimen.
Lifestyle & Tips
- Take pirfenidone with food to help reduce stomach upset.
- Avoid or minimize exposure to sunlight and artificial UV light (e.g., tanning beds) while taking this medicine, as it can make your skin very sensitive to light. Use sunscreen (SPF 50 or higher) and wear protective clothing (hat, long sleeves, pants) when outdoors.
- Do not smoke while taking pirfenidone, as smoking can reduce the effectiveness of the medication.
Available Forms & Alternatives
Dosing & Administration
Adult Dosing
Standard Dose:
Initial titration: 267 mg orally three times daily for 7 days. Increase to 534 mg orally three times daily for days 8-14. Maintenance dose: 801 mg orally three times daily (total 2403 mg/day). Take with food.
Dose Range:
267 - 801 mg
Condition-Specific Dosing:
Dose reduction for adverse events:
If significant adverse events (e.g., GI intolerance, rash, liver enzyme elevations) occur, reduce dose to 534 mg TID or 267 mg TID, or temporarily interrupt treatment. Re-escalate dose as tolerated.
Pediatric Dosing
Neonatal:
Not established
Infant:
Not established
Child:
Not established
Adolescent:
Not established
Dose Adjustments
Renal Impairment:
Mild:
No dose adjustment required.
Moderate:
No dose adjustment required.
Severe:
Not recommended (CrCl <30 mL/min).
Dialysis:
Not recommended in patients with end-stage renal disease requiring dialysis.
Hepatic Impairment:
Mild:
No dose adjustment required (Child-Pugh A).
Moderate:
Consider dose reduction or interruption. Monitor closely (Child-Pugh B).
Severe:
Not recommended (Child-Pugh C).
Pharmacology
Mechanism of Action
Pirfenidone is an antifibrotic agent. Its precise mechanism of action in idiopathic pulmonary fibrosis (IPF) is not fully understood, but it is believed to exert its effects by reducing fibroblast proliferation, inhibiting the production of pro-fibrotic proteins and cytokines (e.g., transforming growth factor-beta [TGF-β], tumor necrosis factor-alpha [TNF-ι], interleukin-1 beta [IL-1β], platelet-derived growth factor [PDGF]), and decreasing collagen synthesis. These actions contribute to reducing fibrosis and inflammation in the lungs.
Pharmacokinetics
Absorption:
Bioavailability:
Approximately 50%
Tmax:
0.5-4 hours
FoodEffect:
Food significantly decreases Cmax (by 50%) and increases Tmax, but increases AUC (by 20-30%), which may improve tolerability.
Distribution:
Vd:
Approximately 70 L
ProteinBinding:
Approximately 50-80%
CnssPenetration:
Limited (crosses blood-brain barrier in animal studies)
Elimination:
HalfLife:
Approximately 2-3 hours
Clearance:
Not available
ExcretionRoute:
Renal (primarily as metabolites)
Unchanged:
<1%
Pharmacodynamics
OnsetOfAction:
Not acutely defined for chronic antifibrotic effect
PeakEffect:
Not acutely defined for chronic antifibrotic effect
DurationOfAction:
Not acutely defined for chronic antifibrotic effect
Safety & Warnings
Side Effects
Urgent Side Effects: Seek Medical Help Right Away
Although rare, some people may experience severe and potentially life-threatening side effects while taking this medication. If you notice any of the following symptoms, contact your doctor or seek immediate medical attention:
Signs of an allergic reaction, such as:
+ Rash
+ Hives
+ Itching
+ Red, swollen, blistered, or peeling skin with or without fever
+ Wheezing
+ Tightness in the chest or throat
+ Trouble breathing, swallowing, or talking
+ Unusual hoarseness
+ Swelling of the mouth, face, lips, tongue, or throat
Chest pain or pressure
Sunburn
Unexplained bruising or bleeding
Liver problems, which can be rare but potentially deadly. Be aware of signs such as:
+ Dark urine
+ Tiredness
+ Decreased appetite
+ Upset stomach or stomach pain
+ Light-colored stools
+ Vomiting
+ Yellow skin or eyes
Other Possible Side Effects
Like all medications, this drug can cause side effects. While many people may not experience any side effects or only minor ones, it's essential to discuss any concerns with your doctor. If you experience any of the following side effects, contact your doctor for guidance:
Feeling dizzy, tired, or weak
Signs of a common cold
Sinus pain
Headache
Joint pain
Change in taste
Trouble sleeping
Weight loss
Stomach pain or heartburn
* Diarrhea, vomiting, upset stomach, and decreased appetite (common side effects that can often be managed with your doctor's guidance)
If any of these side effects bother you, do not improve, or are severe, contact your doctor for advice. This list is not exhaustive, and if you have questions or concerns about side effects, consult your doctor for medical guidance.
Although rare, some people may experience severe and potentially life-threatening side effects while taking this medication. If you notice any of the following symptoms, contact your doctor or seek immediate medical attention:
Signs of an allergic reaction, such as:
+ Rash
+ Hives
+ Itching
+ Red, swollen, blistered, or peeling skin with or without fever
+ Wheezing
+ Tightness in the chest or throat
+ Trouble breathing, swallowing, or talking
+ Unusual hoarseness
+ Swelling of the mouth, face, lips, tongue, or throat
Chest pain or pressure
Sunburn
Unexplained bruising or bleeding
Liver problems, which can be rare but potentially deadly. Be aware of signs such as:
+ Dark urine
+ Tiredness
+ Decreased appetite
+ Upset stomach or stomach pain
+ Light-colored stools
+ Vomiting
+ Yellow skin or eyes
Other Possible Side Effects
Like all medications, this drug can cause side effects. While many people may not experience any side effects or only minor ones, it's essential to discuss any concerns with your doctor. If you experience any of the following side effects, contact your doctor for guidance:
Feeling dizzy, tired, or weak
Signs of a common cold
Sinus pain
Headache
Joint pain
Change in taste
Trouble sleeping
Weight loss
Stomach pain or heartburn
* Diarrhea, vomiting, upset stomach, and decreased appetite (common side effects that can often be managed with your doctor's guidance)
If any of these side effects bother you, do not improve, or are severe, contact your doctor for advice. This list is not exhaustive, and if you have questions or concerns about side effects, consult your doctor for medical guidance.
Seek Immediate Medical Attention If You Experience:
- Signs of liver problems: yellowing of the skin or eyes (jaundice), dark urine, unusual tiredness, nausea, vomiting, pain in the upper right side of your stomach, itching.
- Severe skin rash or blistering.
- Severe or persistent nausea, vomiting, diarrhea, or stomach pain.
- Unexplained weight loss.
Before Using This Medicine
Before Taking This Medication: Important Information to Share with Your Doctor
It is essential to inform your doctor about the following:
Any allergies you have, including allergies to this medication, its components, or other substances, such as foods or drugs. Be sure to describe the symptoms you experienced.
Existing health conditions, including kidney disease or liver disease.
If you are taking any medications that may increase your skin's sensitivity to light, as several drugs can cause this reaction. If you are unsure, consult your doctor or pharmacist.
Please note that this is not an exhaustive list of all potential interactions between this medication and other substances or health conditions.
To ensure your safety, it is crucial to discuss all of the following with your doctor and pharmacist:
All prescription and over-the-counter medications you are taking
Any natural products or vitamins you are using
Your existing health problems
Before starting, stopping, or changing the dose of any medication, including this one, you must consult with your doctor to confirm that it is safe to do so in conjunction with your other medications and health conditions.
It is essential to inform your doctor about the following:
Any allergies you have, including allergies to this medication, its components, or other substances, such as foods or drugs. Be sure to describe the symptoms you experienced.
Existing health conditions, including kidney disease or liver disease.
If you are taking any medications that may increase your skin's sensitivity to light, as several drugs can cause this reaction. If you are unsure, consult your doctor or pharmacist.
Please note that this is not an exhaustive list of all potential interactions between this medication and other substances or health conditions.
To ensure your safety, it is crucial to discuss all of the following with your doctor and pharmacist:
All prescription and over-the-counter medications you are taking
Any natural products or vitamins you are using
Your existing health problems
Before starting, stopping, or changing the dose of any medication, including this one, you must consult with your doctor to confirm that it is safe to do so in conjunction with your other medications and health conditions.
Precautions & Cautions
It is essential to inform all your healthcare providers, including doctors, nurses, pharmacists, and dentists, that you are taking this medication.
When taking this drug, you may be more susceptible to sunburn. To minimize this risk, avoid exposure to direct sunlight, sunlamps, and tanning beds. Use a broad-spectrum sunscreen with a high sun protection factor (SPF) and wear protective clothing and eyewear that shields you from the sun.
If you smoke, it is recommended that you quit before starting this medication. Continue to avoid smoking while taking this drug, as it may decrease the medication's effectiveness. Discuss smoking cessation strategies with your doctor if needed.
Regular blood tests and other laboratory evaluations will be necessary to monitor your condition. Adhere to the schedule outlined by your doctor for these tests.
If you are pregnant, planning to become pregnant, or are breastfeeding, notify your doctor. It is crucial to discuss the potential benefits and risks of this medication to both you and your baby, allowing for an informed decision about treatment.
When taking this drug, you may be more susceptible to sunburn. To minimize this risk, avoid exposure to direct sunlight, sunlamps, and tanning beds. Use a broad-spectrum sunscreen with a high sun protection factor (SPF) and wear protective clothing and eyewear that shields you from the sun.
If you smoke, it is recommended that you quit before starting this medication. Continue to avoid smoking while taking this drug, as it may decrease the medication's effectiveness. Discuss smoking cessation strategies with your doctor if needed.
Regular blood tests and other laboratory evaluations will be necessary to monitor your condition. Adhere to the schedule outlined by your doctor for these tests.
If you are pregnant, planning to become pregnant, or are breastfeeding, notify your doctor. It is crucial to discuss the potential benefits and risks of this medication to both you and your baby, allowing for an informed decision about treatment.
Overdose Information
Overdose Symptoms:
- Nausea
- Vomiting
- Diarrhea
- Abdominal pain
- Dizziness
- Fatigue
- Rash
What to Do:
In case of suspected overdose, contact a poison control center immediately (e.g., call 1-800-222-1222 in the US) or seek emergency medical attention. Management is supportive.
Drug Interactions
Contraindicated Interactions
- Fluvoxamine (strong CYP1A2 inhibitor)
- Other strong CYP1A2 inhibitors (e.g., ciprofloxacin, enoxacin)
Major Interactions
- Amiodarone (moderate CYP1A2 inhibitor)
- Propafenone (moderate CYP1A2 inhibitor)
- Other moderate CYP1A2 inhibitors
Moderate Interactions
- Omeprazole (CYP1A2 inducer)
- Smoking (CYP1A2 inducer)
Monitoring
Baseline Monitoring
Liver Function Tests (ALT, AST, bilirubin)
Rationale: To establish baseline liver function and identify pre-existing hepatic impairment, as pirfenidone can cause liver injury.
Timing: Prior to initiation of therapy
Renal Function (CrCl)
Rationale: To assess kidney function, as pirfenidone is primarily renally eliminated and is not recommended in severe renal impairment.
Timing: Prior to initiation of therapy
Routine Monitoring
Liver Function Tests (ALT, AST, bilirubin)
Frequency: Monthly for the first 6 months, then every 3 months thereafter, or as clinically indicated.
Target: Within normal limits or stable baseline values.
Action Threshold: Discontinue pirfenidone if ALT/AST >5 x ULN or if ALT/AST >3 x ULN with concomitant hyperbilirubinemia (>2 x ULN). Reduce dose or interrupt if ALT/AST >3 to <5 x ULN.
Signs and symptoms of photosensitivity/rash
Frequency: Regularly, especially during initial treatment and sun exposure.
Target: Absence of severe rash or photosensitivity.
Action Threshold: Reduce dose or interrupt therapy for severe rash or photosensitivity reaction.
Gastrointestinal symptoms (nausea, diarrhea, dyspepsia)
Frequency: Regularly, especially during initial titration.
Target: Tolerable GI symptoms.
Action Threshold: Reduce dose or interrupt therapy for severe or persistent GI intolerance.
Symptom Monitoring
- Nausea
- Diarrhea
- Dyspepsia
- Vomiting
- Abdominal pain
- Fatigue
- Dizziness
- Headache
- Rash
- Photosensitivity reaction
- Signs of liver injury (e.g., jaundice, dark urine, right upper quadrant pain, pruritus)
Special Patient Groups
Pregnancy
Based on animal data, pirfenidone may cause fetal harm. There are no adequate and well-controlled studies in pregnant women. Use during pregnancy only if the potential benefit justifies the potential risk to the fetus.
Trimester-Specific Risks:
First Trimester:
Potential for fetal harm based on animal studies.
Second Trimester:
Potential for fetal harm based on animal studies.
Third Trimester:
Potential for fetal harm based on animal studies.
Lactation
It is unknown if pirfenidone is excreted in human milk. Due to the potential for serious adverse reactions in breastfed infants, advise women not to breastfeed during treatment with pirfenidone and for 1 week after the last dose.
Infant Risk:
High (potential for serious adverse reactions)
Pediatric Use
Safety and effectiveness in pediatric patients have not been established. Pirfenidone is not indicated for use in pediatric patients.
Geriatric Use
No specific dose adjustment is required based on age alone. However, geriatric patients may be more susceptible to adverse effects, particularly gastrointestinal and photosensitivity reactions. Monitor closely for adverse events.
Clinical Information
Clinical Pearls
- Always take pirfenidone with food to minimize gastrointestinal side effects.
- Strict adherence to sun protection measures (sunscreen, protective clothing) is crucial due to the high risk of photosensitivity.
- Regular liver function monitoring is essential, especially during the first 6 months of treatment.
- Dose titration is important for tolerability; do not start at the full maintenance dose.
- If a dose is missed, do not take extra doses to make up for the missed dose. Continue with the next scheduled dose.
Alternative Therapies
- Nintedanib (another antifibrotic approved for IPF)
Cost & Coverage
Generic Available:
Yes
Insurance Coverage:
Specialty Tier (requires prior authorization)
General Drug Facts
If your symptoms or health issues persist or worsen, it is essential to contact your doctor promptly. To ensure safe and effective treatment, never share your medication with others or take someone else's medication. Some medications may come with an additional patient information leaflet, so it's a good idea to check with your pharmacist for more information. If you have any questions or concerns about this medication, don't hesitate to discuss them with your doctor, nurse, pharmacist, or other healthcare provider. In the event of a suspected overdose, immediately call your local poison control center or seek emergency medical attention. When seeking help, be prepared to provide details about the overdose, including the medication taken, the amount, and the time it occurred.