Pirfenidone 801mg Tablets
It is used to treat idiopathic pulmonary fibrosis.
Drug Class
Antifibrotic agent
Pharmacologic Class
Pyridone derivative
Pregnancy Category
Category C
FDA Approved
Oct 2014
DEA Schedule
Not Controlled
Overview
What is this medicine?
Pirfenidone is a medication used to treat a serious lung disease called Idiopathic Pulmonary Fibrosis (IPF). IPF causes scarring in the lungs, making it hard to breathe. Pirfenidone works by helping to slow down the scarring process in the lungs, which can help preserve lung function.
How to Use This Medicine
Taking Your Medication Correctly
To get the most benefit from your medication, follow your doctor's instructions carefully. Read all the information provided with your prescription and follow the instructions closely. Take your medication with food to help your body absorb it properly. Establish a routine by taking your medication at the same time every day. Continue taking your medication as directed by your doctor or healthcare provider, even if you start feeling well.
Storing and Disposing of Your Medication
Store your medication at room temperature in a dry location, such as a closet or cupboard. Avoid storing it in a bathroom, where moisture and humidity can affect the medication. Keep the lid tightly closed to protect the medication from air and moisture. Keep all medications out of the reach of children and pets to prevent accidental ingestion. When disposing of unused or expired medication, do not flush it down the toilet or pour it down the drain unless instructed to do so by your pharmacist or healthcare provider. Instead, check with your pharmacist for guidance on the best way to dispose of your medication. You may also want to explore drug take-back programs in your area.
What to Do If You Miss a Dose
If you miss a dose, take it as soon as you remember, with food. However, if it's close to the time for your next scheduled dose, skip the missed dose and resume your regular dosing schedule. Do not take two doses at the same time or take extra doses to make up for the missed one. Additionally, 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 treatment to ensure it's safe to do so.
To get the most benefit from your medication, follow your doctor's instructions carefully. Read all the information provided with your prescription and follow the instructions closely. Take your medication with food to help your body absorb it properly. Establish a routine by taking your medication at the same time every day. Continue taking your medication as directed by your doctor or healthcare provider, even if you start feeling well.
Storing and Disposing of Your Medication
Store your medication at room temperature in a dry location, such as a closet or cupboard. Avoid storing it in a bathroom, where moisture and humidity can affect the medication. Keep the lid tightly closed to protect the medication from air and moisture. Keep all medications out of the reach of children and pets to prevent accidental ingestion. When disposing of unused or expired medication, do not flush it down the toilet or pour it down the drain unless instructed to do so by your pharmacist or healthcare provider. Instead, check with your pharmacist for guidance on the best way to dispose of your medication. You may also want to explore drug take-back programs in your area.
What to Do If You Miss a Dose
If you miss a dose, take it as soon as you remember, with food. However, if it's close to the time for your next scheduled dose, skip the missed dose and resume your regular dosing schedule. Do not take two doses at the same time or take extra doses to make up for the missed one. Additionally, 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 treatment to ensure it's safe to do so.
Lifestyle & Tips
- Take pirfenidone with food to reduce stomach upset and improve absorption.
- Avoid or minimize exposure to sunlight and artificial UV light (e.g., tanning beds) while taking this medication, as it can cause severe sunburn (photosensitivity). Use sunscreen (SPF 50 or higher), wear protective clothing, and a hat when outdoors.
- Do not smoke while taking pirfenidone, as smoking can reduce the effectiveness of the medication.
- Limit or avoid alcohol consumption, especially if you have liver problems, as pirfenidone can affect the liver.
Available Forms & Alternatives
Dosing & Administration
Adult Dosing
Standard Dose:
801 mg three times daily (2403 mg/day)
Dose Range:
267 - 801 mg
Condition-Specific Dosing:
idiopathicPulmonaryFibrosis:
Initial titration: Day 1-7: 267 mg TID; Day 8-14: 534 mg TID; Day 15 onwards: 801 mg TID. Take with food.
Pediatric Dosing
Neonatal:
Not established
Infant:
Not established
Child:
Not established
Adolescent:
Not established
Dose Adjustments
Renal Impairment:
Mild:
No dose adjustment required (CrCl 50-80 mL/min).
Moderate:
Use with caution (CrCl 30-49 mL/min). Consider dose reduction or interruption if intolerance occurs.
Severe:
Not recommended (CrCl <30 mL/min).
Dialysis:
Not recommended.
Hepatic Impairment:
Mild:
No dose adjustment required (Child-Pugh A).
Moderate:
Use with caution (Child-Pugh B). Consider dose reduction or interruption if intolerance occurs. Monitor closely.
Severe:
Not recommended (Child-Pugh C).
Confidence:
High
Pharmacology
Mechanism of Action
The exact mechanism of action of pirfenidone in idiopathic pulmonary fibrosis (IPF) is not fully elucidated. However, it is believed to exert its antifibrotic and anti-inflammatory effects through multiple pathways. It inhibits the synthesis of TGF-beta (transforming growth factor-beta) and PDGF (platelet-derived growth factor), which are key mediators in fibrosis. It also reduces fibroblast proliferation, collagen synthesis, and the production of pro-fibrotic proteins and cytokines. Pirfenidone may also have antioxidant properties.
Pharmacokinetics
Absorption:
Bioavailability:
Approximately 50%
Tmax:
0.5-4 hours (fasted); 2-4 hours (with food)
FoodEffect:
Food significantly decreases Cmax (by 50%) and increases Tmax, but increases AUC (by 20-30%), leading to reduced peak-related side effects and improved tolerability. Should be taken with food.
Distribution:
Vd:
Approximately 70 L
ProteinBinding:
Approximately 50-80%
CnssPenetration:
Limited
Elimination:
HalfLife:
Approximately 2-3 hours
Clearance:
Not available
ExcretionRoute:
Primarily renal (approximately 80% as metabolite)
Unchanged:
Less than 1% (in urine)
Pharmacodynamics
OnsetOfAction:
Gradual (clinical effects observed over weeks to months)
PeakEffect:
Not applicable (chronic disease modifying drug)
DurationOfAction:
Not applicable (chronic disease modifying drug)
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. Warning signs include:
+ 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 have mild ones, it's essential to discuss any concerns with your doctor. If you experience any of the following side effects, contact your doctor for advice:
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 further guidance. This is not an exhaustive list of possible side effects. If you have questions or concerns, don't hesitate to reach out to your doctor for medical advice.
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. Warning signs include:
+ 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 have mild ones, it's essential to discuss any concerns with your doctor. If you experience any of the following side effects, contact your doctor for advice:
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 further guidance. This is not an exhaustive list of possible side effects. If you have questions or concerns, don't hesitate to reach out to your doctor for medical advice.
Seek Immediate Medical Attention If You Experience:
- Signs of liver problems: yellowing of the skin or eyes (jaundice), dark urine, pain in the upper right side of your stomach, unusual tiredness, loss of appetite.
- Severe skin rash or blistering.
- Severe nausea, vomiting, or diarrhea that does not go away.
- Unexplained weight loss.
- Signs of severe sunburn (redness, blistering, pain) after sun exposure.
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.
If you have kidney disease or liver disease, as these conditions may affect how your body processes the medication.
If you are taking any medications that may increase your skin's sensitivity to light, as this can lead to adverse reactions. There are numerous medications that can cause this interaction, so consult your doctor or pharmacist if you are unsure.
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:
Inform your doctor and pharmacist about all medications you are taking, including prescription and over-the-counter drugs, natural products, and vitamins.
Disclose any health problems you have, as they may affect the safety and efficacy of this medication.
Verify with your doctor that it is safe to take this medication in combination with your other medications and health conditions.
* Never start, stop, or modify the dosage of any medication without first consulting 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.
If you have kidney disease or liver disease, as these conditions may affect how your body processes the medication.
If you are taking any medications that may increase your skin's sensitivity to light, as this can lead to adverse reactions. There are numerous medications that can cause this interaction, so consult your doctor or pharmacist if you are unsure.
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:
Inform your doctor and pharmacist about all medications you are taking, including prescription and over-the-counter drugs, natural products, and vitamins.
Disclose any health problems you have, as they may affect the safety and efficacy of this medication.
Verify with your doctor that it is safe to take this medication in combination with your other medications and health conditions.
* Never start, stop, or modify the dosage of any medication without first consulting your doctor.
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. Additionally, use a broad-spectrum sunscreen with a high sun protection factor (SPF) and wear protective clothing and eyewear that shields you from the sun.
Quitting smoking is highly recommended before initiating this medication, and it is advisable to avoid smoking throughout the treatment period. Smoking can decrease the effectiveness of this drug, so it is crucial to discuss this with your doctor.
Regular blood tests and other laboratory assessments are necessary to monitor your condition. Ensure that you undergo these tests as scheduled by your doctor.
If you are pregnant, planning to become pregnant, or are breast-feeding, it is vital to consult your doctor. You and your doctor will need to discuss the potential benefits and risks of this medication to both you and your baby to make an informed decision.
When taking this drug, you may be more susceptible to sunburn. To minimize this risk, avoid exposure to direct sunlight, sunlamps, and tanning beds. Additionally, use a broad-spectrum sunscreen with a high sun protection factor (SPF) and wear protective clothing and eyewear that shields you from the sun.
Quitting smoking is highly recommended before initiating this medication, and it is advisable to avoid smoking throughout the treatment period. Smoking can decrease the effectiveness of this drug, so it is crucial to discuss this with your doctor.
Regular blood tests and other laboratory assessments are necessary to monitor your condition. Ensure that you undergo these tests as scheduled by your doctor.
If you are pregnant, planning to become pregnant, or are breast-feeding, it is vital to consult your doctor. You and your doctor will need to discuss the potential benefits and risks of this medication to both you and your baby to make an informed decision.
Overdose Information
Overdose Symptoms:
- Severe nausea
- Vomiting
- Diarrhea
- Dizziness
- Fatigue
- Rash
- Liver enzyme elevations
What to Do:
In case of suspected overdose, seek immediate medical attention or call a poison control center (1-800-222-1222). Management is supportive.
Drug Interactions
Contraindicated Interactions
- Fluvoxamine (strong CYP1A2 inhibitor)
Major Interactions
- Ciprofloxacin (moderate CYP1A2 inhibitor) - requires dose reduction of pirfenidone
- Amiodarone (CYP1A2 inhibitor)
- Propafenone (CYP1A2 inhibitor)
- Strong CYP1A2 inducers (e.g., Rifampin, Phenytoin, Carbamazepine, St. John's Wort) - may significantly reduce pirfenidone exposure and efficacy
Moderate Interactions
- Other moderate CYP1A2 inhibitors (e.g., Enoxacin, Mexiletine, Zileuton) - monitor for adverse effects
- Smoking (induces CYP1A2) - may reduce pirfenidone exposure
Minor Interactions
- Not specifically identified as minor, but caution with any CYP1A2 modulators.
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 baseline kidney function, as pirfenidone is primarily renally eliminated and dose adjustments may be needed in severe impairment.
Timing: Prior to initiation of therapy.
Pulmonary Function Tests (FVC, DLCO)
Rationale: To establish baseline lung function and monitor disease progression.
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 from baseline.
Action Threshold: Discontinue pirfenidone if ALT/AST >5 x ULN or if ALT/AST >3 x ULN with concomitant hyperbilirubinemia (>2 x ULN). Consider dose reduction or interruption if ALT/AST >3 to <5 x ULN.
Weight
Frequency: Periodically
Target: Stable
Action Threshold: Significant unexplained weight loss should be investigated.
Signs and symptoms of liver injury
Frequency: At each visit
Target: Absence of symptoms
Action Threshold: Report jaundice, dark urine, right upper quadrant pain, or unexplained fatigue.
Symptom Monitoring
- Nausea
- Diarrhea
- Dyspepsia
- Vomiting
- Abdominal pain
- Fatigue
- Headache
- Dizziness
- Insomnia
- Rash
- Photosensitivity reaction (sunburn-like rash)
- Unexplained weight loss
- Signs of liver injury (jaundice, dark urine, right upper quadrant pain)
Special Patient Groups
Pregnancy
Pirfenidone is classified as Pregnancy Category C. Animal studies have shown adverse effects on fetal development (e.g., increased fetal loss, reduced fetal weight, skeletal variations) at exposures higher than those achieved clinically. There are no adequate and well-controlled studies in pregnant women.
Trimester-Specific Risks:
First Trimester:
Potential for developmental toxicity based on animal data.
Second Trimester:
Potential for developmental toxicity based on animal data.
Third Trimester:
Potential for developmental toxicity based on animal data.
Lactation
It is not known whether pirfenidone or its metabolites are excreted in human milk. Due to the potential for serious adverse reactions in breastfed infants, a decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother.
Infant Risk:
Risk is unknown; potential for serious adverse effects. L3 (Moderately Safe) is a common classification, but caution is advised.
Pediatric Use
The safety and effectiveness of pirfenidone in pediatric patients have not been established. It is not indicated for use in children.
Geriatric Use
No overall differences in safety or effectiveness were observed between elderly patients (âĨ65 years) and younger patients. No specific dose adjustment is required based on age alone.
Clinical Information
Clinical Pearls
- Pirfenidone is one of two FDA-approved medications (the other being nintedanib) for Idiopathic Pulmonary Fibrosis (IPF), a progressive and fatal lung disease.
- Strict adherence to the titration schedule is crucial to improve tolerability and reduce gastrointestinal side effects.
- Always advise patients to take pirfenidone with food to minimize GI upset and improve drug exposure.
- Emphasize the importance of sun protection (sunscreen, protective clothing) due to the high risk of photosensitivity reactions.
- Regular monitoring of liver function tests is critical, especially during the first 6 months of therapy, as drug-induced liver injury can occur.
- Patients should be educated on symptoms of liver injury and advised to report them immediately.
- Smoking cessation is strongly recommended as smoking induces CYP1A2 and can reduce pirfenidone efficacy.
Alternative Therapies
- Nintedanib (another antifibrotic agent for IPF)
- Supportive care (oxygen therapy, pulmonary rehabilitation)
- Lung transplantation (for eligible patients with advanced disease)
Cost & Coverage
Average Cost:
Extremely high (e.g., $10,000 - $15,000+) per 30 tablets (801mg)
Generic Available:
Yes
Insurance Coverage:
Specialty Tier (requires prior authorization, often subject to high co-pays or co-insurance)
General Drug Facts
If your symptoms or health issues persist or worsen, it's essential to contact your doctor for further guidance. To ensure your safety, never share your medication with others or take someone else's medication. Some medications may come with an additional patient information leaflet, so be sure to check with your pharmacist for more information. If you have any questions or concerns about your medication, don't hesitate to reach out to 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 medication taken, the amount, and the time it occurred.