Esbriet 267mg 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?
Esbriet (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. Esbriet helps slow down the progression of this scarring and can help you breathe better.
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. Consistency is key, so take your medication at the same time every day. Even if you start to feel better, continue taking your medication as directed by your doctor or healthcare provider.
Storing and Disposing of Your Medication
To keep your medication effective and safe, store it at room temperature in a dry place, away from the bathroom. Make sure to keep the lid tightly closed. Keep all medications out of the reach of children and pets to avoid accidents. When you're finished with your medication or it's expired, dispose of it properly. Do not flush it down the toilet or pour it down the drain unless instructed to do so by your pharmacist. If you're unsure about how to dispose of your medication, ask your pharmacist for guidance. You may also want to check if there are any 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 dose, skip the missed dose and return to your regular schedule. Do not take two doses at the same time or take extra doses. Be careful not to 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 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. Consistency is key, so take your medication at the same time every day. Even if you start to feel better, continue taking your medication as directed by your doctor or healthcare provider.
Storing and Disposing of Your Medication
To keep your medication effective and safe, store it at room temperature in a dry place, away from the bathroom. Make sure to keep the lid tightly closed. Keep all medications out of the reach of children and pets to avoid accidents. When you're finished with your medication or it's expired, dispose of it properly. Do not flush it down the toilet or pour it down the drain unless instructed to do so by your pharmacist. If you're unsure about how to dispose of your medication, ask your pharmacist for guidance. You may also want to check if there are any 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 dose, skip the missed dose and return to your regular schedule. Do not take two doses at the same time or take extra doses. Be careful not to 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.
Lifestyle & Tips
- Take Esbriet with food to help reduce side effects like nausea and dizziness.
- Avoid or minimize exposure to sunlight (including sunlamps and tanning beds) while taking Esbriet, as it can make your skin very sensitive to the sun (photosensitivity). Use sunscreen (SPF 50 or higher) and wear protective clothing (hat, long sleeves, pants) when outdoors.
- Do not smoke while taking Esbriet, as smoking can reduce the effectiveness of the medication.
Available Forms & Alternatives
Available Strengths:
Generic Alternatives:
Dosing & Administration
Adult Dosing
Standard Dose:
801 mg orally three times daily (total 2403 mg/day) after titration
Dose Range:
267 - 801 mg
Condition-Specific Dosing:
titration_schedule:
Days 1-7: 267 mg TID; Days 8-14: 534 mg TID; Day 15 onwards: 801 mg TID (maintenance)
missed_dose:
If a dose is missed, take the next dose at the regularly scheduled time. Do not take two doses at one time.
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:
No dose adjustment required (CrCl 30-50 mL/min)
Severe:
Not recommended (CrCl <30 mL/min)
Dialysis:
Not recommended
Hepatic Impairment:
Mild:
No dose adjustment required (Child-Pugh A)
Moderate:
Use with caution; dose reduction or interruption may be necessary based on adverse reactions. Monitor closely (Child-Pugh B)
Severe:
Not recommended (Child-Pugh C)
Confidence:
High
Pharmacology
Mechanism of Action
Pirfenidone is an antifibrotic agent. Its precise mechanism of action in idiopathic pulmonary fibrosis (IPF) is not fully elucidated, but it is thought to exert its effects through anti-inflammatory and antifibrotic properties. It inhibits the synthesis of TGF-beta (transforming growth factor-beta), a pro-fibrotic cytokine, and TNF-alpha (tumor necrosis factor-alpha), a pro-inflammatory cytokine. It also reduces fibroblast proliferation and the production of collagen and other fibrotic proteins.
Pharmacokinetics
Absorption:
Bioavailability:
Not explicitly stated as a percentage, but well absorbed orally.
Tmax:
0.5-4 hours (fasted); 2-4 hours (fed)
FoodEffect:
Food significantly decreases Cmax (by approximately 50%) but has minimal effect on AUC. Taking with food reduces the incidence of nausea and dizziness.
Distribution:
Vd:
Approximately 70 L
ProteinBinding:
Approximately 50-80%
CnssPenetration:
Limited
Elimination:
HalfLife:
Approximately 2.4-3.1 hours
Clearance:
Not available
ExcretionRoute:
Primarily renal (approximately 80% as metabolites, <1% as unchanged drug)
Unchanged:
<1%
Pharmacodynamics
OnsetOfAction:
Not acutely defined for chronic antifibrotic therapy
PeakEffect:
Not acutely defined for chronic antifibrotic therapy
DurationOfAction:
Not acutely defined for chronic antifibrotic therapy
Confidence:
Medium
Safety & Warnings
Side Effects
Urgent Side Effects: Seek Medical Attention Immediately
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 medical help right away:
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 or seek medical help if they bother you or do not go away:
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 are common side effects of this medication. If you experience any of these, talk to your doctor about ways to manage them. Seek medical attention if they are severe, do not improve, or worsen over time.
Remember
This list is not exhaustive, and you may experience other side effects not mentioned here. If you have questions or concerns about side effects, contact 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 medical help right away:
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 or seek medical help if they bother you or do not go away:
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 are common side effects of this medication. If you experience any of these, talk to your doctor about ways to manage them. Seek medical attention if they are severe, do not improve, or worsen over time.
Remember
This list is not exhaustive, and you may experience other side effects not mentioned here. If you have questions or concerns about side effects, contact your doctor for medical advice.
Seek Immediate Medical Attention If You Experience:
- Signs of liver problems: yellowing of your skin or the whites of your eyes (jaundice), dark or brown urine, pain on the upper right side of your stomach area, unusual tiredness, nausea, or vomiting.
- Severe skin rash or blistering.
- Severe nausea, vomiting, or diarrhea that does not go away.
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 sensitivity, 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 these may interact with the medication.
Verify that it is safe to take this medication with all your other medications and health conditions.
* Never start, stop, or change the dose 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 sensitivity, 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 these may interact with the medication.
Verify that it is safe to take this medication with all your other medications and health conditions.
* Never start, stop, or change the dose 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. 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 recommended before initiating this medication, and it is advisable to avoid smoking during treatment. Smoking may decrease the effectiveness of this drug. Discuss the implications of smoking with your doctor.
Regular blood tests and other laboratory assessments should be conducted as directed by your doctor to monitor your condition.
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 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. 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 recommended before initiating this medication, and it is advisable to avoid smoking during treatment. Smoking may decrease the effectiveness of this drug. Discuss the implications of smoking with your doctor.
Regular blood tests and other laboratory assessments should be conducted as directed by your doctor to monitor your condition.
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 to make an informed decision.
Overdose Information
Overdose Symptoms:
- Nausea
- Vomiting
- Diarrhea
- Dizziness
- Fatigue
- Rash
- Potential for severe liver injury
What to Do:
Seek immediate medical attention or call a Poison Control Center at 1-800-222-1222. Treatment is supportive.
Drug Interactions
Contraindicated Interactions
- Fluvoxamine (strong CYP1A2 inhibitor)
Major Interactions
- Other strong CYP1A2 inhibitors (e.g., enoxacin, cimetidine)
Moderate Interactions
- Moderate CYP1A2 inhibitors (e.g., ciprofloxacin, amiodarone, propafenone, omeprazole): Reduce pirfenidone dose to 267 mg TID if co-administered.
- Smoking (induces CYP1A2, reduces pirfenidone exposure)
Confidence Interactions
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
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
Action Threshold: Discontinue pirfenidone if ALT or AST >5 x ULN or if ALT or AST >3 x ULN with concomitant hyperbilirubinemia or symptoms of liver injury. Consider dose reduction or interruption if ALT or AST >3 to â¤5 x ULN.
Signs and symptoms of photosensitivity/rash
Frequency: Regularly throughout therapy
Target: Absence of severe rash or photosensitivity
Action Threshold: Manage with dose reduction, interruption, or discontinuation based on severity.
Gastrointestinal symptoms (nausea, diarrhea, dyspepsia)
Frequency: Regularly throughout therapy
Target: Tolerable symptoms
Action Threshold: Manage with dose reduction, interruption, or discontinuation based on severity.
Symptom Monitoring
- Nausea
- Diarrhea
- Dyspepsia
- Fatigue
- Rash
- Photosensitivity (sunburn-like reaction)
- Signs of liver injury (e.g., yellowing of skin/eyes, dark urine, right upper quadrant abdominal pain, unusual tiredness)
Special Patient Groups
Pregnancy
Category C. There are no adequate and well-controlled studies of pirfenidone in pregnant women. Use only if the potential benefit justifies the potential risk to the fetus.
Trimester-Specific Risks:
First Trimester:
Animal studies have shown developmental toxicity (reduced fetal weight, increased skeletal variations) at doses higher than human therapeutic exposure.
Second Trimester:
Animal studies have shown developmental toxicity (reduced fetal weight, increased skeletal variations) at doses higher than human therapeutic exposure.
Third Trimester:
Animal studies have shown developmental toxicity (reduced fetal weight, increased skeletal variations) at doses higher than human therapeutic exposure.
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:
Unknown; potential for serious adverse reactions.
Pediatric Use
Safety and effectiveness in pediatric patients have not been established.
Geriatric Use
No specific dose adjustment is required based on age. However, elderly patients may be more susceptible to adverse reactions, and monitoring for side effects is important.
Clinical Information
Clinical Pearls
- Always advise patients to take pirfenidone with food to minimize gastrointestinal side effects.
- Emphasize strict sun protection measures due to significant photosensitivity risk.
- Regular liver function monitoring is crucial, especially during the first 6 months of therapy.
- Counsel patients on the importance of not smoking, as it can reduce pirfenidone efficacy.
- Pirfenidone requires a gradual dose titration over 2 weeks to improve tolerability.
Alternative Therapies
- Nintedanib (Ofev)
Cost & Coverage
Average Cost:
Highly variable, typically >$10,000 per 30 tablets
Generic Available:
Yes
Insurance Coverage:
Specialty Tier (requires prior authorization, often subject to step therapy)
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 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 happened.