Esbriet 267mg Capsules
It is used to treat idiopathic pulmonary fibrosis.
Drug Class
Antifibrotic Agent
Pharmacologic Class
Pyridone derivative, antifibrotic
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 worsening 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.
Establish a routine by taking your medication at the same time every day.
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 ensure your medication remains effective and safe:
Store your medication at room temperature in a dry place, away from the bathroom.
Keep the lid tightly closed to maintain the medication's potency.
Keep all medications in a 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.
If you have questions about disposing of your medication, consult your pharmacist. You may also have access to drug take-back programs 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 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.
Do not exceed 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.
Establish a routine by taking your medication at the same time every day.
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 ensure your medication remains effective and safe:
Store your medication at room temperature in a dry place, away from the bathroom.
Keep the lid tightly closed to maintain the medication's potency.
Keep all medications in a 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.
If you have questions about disposing of your medication, consult your pharmacist. You may also have access to drug take-back programs 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 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.
Do not exceed 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 Esbriet with food to help reduce side effects like nausea and dizziness.
- Take the capsules whole; do not crush, chew, or open them.
- Protect your skin from the sun (even on cloudy days) and avoid tanning beds. Use sunscreen (SPF 50 or higher), wear protective clothing (hat, long sleeves), and limit sun exposure, as this medication can make your skin very sensitive to sunlight.
- Do not smoke while taking Esbriet, as smoking can make the medication less effective.
- Avoid grapefruit and grapefruit juice, as they can increase pirfenidone levels.
Available Forms & Alternatives
Available Strengths:
Generic Alternatives:
Dosing & Administration
Adult Dosing
Standard Dose:
Initial titration: Day 1-7: 267 mg TID; Day 8-14: 534 mg TID; Day 15 onwards: 801 mg TID. Maintenance dose: 801 mg TID (total 2403 mg/day)
Dose Range:
267 - 801 mg
Condition-Specific Dosing:
Idiopathic Pulmonary Fibrosis (IPF):
Titrate over 14 days to a target maintenance dose of 801 mg three times daily (2403 mg/day) 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 âĨ50 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) or End-Stage Renal Disease requiring dialysis.
Dialysis:
Not recommended in patients with ESRD requiring dialysis.
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 liver function closely.
Severe:
Not recommended (Child-Pugh C).
Confidence:
High
Pharmacology
Mechanism of Action
Pirfenidone is an antifibrotic agent. Its mechanism of action is not fully elucidated but is thought to involve inhibition of transforming growth factor-beta (TGF-β) and tumor necrosis factor-alpha (TNF-ι), both of which are pro-fibrotic cytokines. It also has antioxidant properties and may reduce fibroblast proliferation and collagen synthesis.
Pharmacokinetics
Absorption:
Bioavailability:
Not available (relative bioavailability is high)
Tmax:
0.5-4 hours (median 1 hour)
FoodEffect:
Food significantly decreases Cmax (by 50%) but has a minimal effect on AUC. Taking with food reduces nausea and dizziness.
Distribution:
Vd:
70-80 L
ProteinBinding:
Approximately 50-80%
CnssPenetration:
Limited
Elimination:
HalfLife:
Approximately 2-3 hours
Clearance:
Not available
ExcretionRoute:
Renal (approximately 80% as metabolites, primarily 5-carboxy-pirfenidone)
Unchanged:
Less than 1%
Pharmacodynamics
OnsetOfAction:
Not acutely defined for antifibrotic effect; clinical benefit observed over months.
PeakEffect:
Not acutely defined for antifibrotic effect.
DurationOfAction:
Not acutely defined for antifibrotic effect; requires continuous dosing.
Safety & Warnings
Side Effects
Urgent Side Effects: Seek Medical Help Right Away
While rare, some people may experience severe and potentially life-threatening side effects when taking this medication. Immediately contact your doctor or seek medical attention if you experience any of the following symptoms:
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
Most people experience either no side effects or only mild ones. However, if you encounter any of the following side effects, or if they persist or bother you, consult your doctor:
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 these, discuss ways to manage them with your doctor. Seek immediate medical attention if these effects are severe, persistent, or worsen over time.
Remember
This list is not exhaustive, and you may experience other side effects not mentioned here. If you have concerns or questions about side effects, consult your doctor for personalized advice and guidance.
While rare, some people may experience severe and potentially life-threatening side effects when taking this medication. Immediately contact your doctor or seek medical attention if you experience any of the following symptoms:
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
Most people experience either no side effects or only mild ones. However, if you encounter any of the following side effects, or if they persist or bother you, consult your doctor:
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 these, discuss ways to manage them with your doctor. Seek immediate medical attention if these effects are severe, persistent, or worsen over time.
Remember
This list is not exhaustive, and you may experience other side effects not mentioned here. If you have concerns or questions about side effects, consult your doctor for personalized advice and guidance.
Seek Immediate Medical Attention If You Experience:
- Signs of liver problems: yellowing of skin or eyes (jaundice), dark urine, pain in the upper right side of your stomach, unusual tiredness, nausea, vomiting.
- Severe rash or skin reaction, especially after sun exposure.
- Severe nausea, vomiting, or diarrhea that does not improve.
- 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. There are numerous drugs 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 discuss 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 complete medical history, including any health problems
Before starting, stopping, or modifying the dosage 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. There are numerous drugs 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 discuss 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 complete medical history, including any health problems
Before starting, stopping, or modifying the dosage 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.
Quitting smoking is recommended before initiating this medication, and you should also avoid smoking during treatment. Smoking can decrease the effectiveness of this drug, so it is crucial to discuss smoking cessation with your doctor.
Regular blood tests and other laboratory evaluations 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 immediately. 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. 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 you should also avoid smoking during treatment. Smoking can decrease the effectiveness of this drug, so it is crucial to discuss smoking cessation with your doctor.
Regular blood tests and other laboratory evaluations 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 immediately. 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:
- Nausea
- Vomiting
- Diarrhea
- Dizziness
- Fatigue
- Rash
- Liver enzyme elevations
What to Do:
There is no specific antidote for pirfenidone overdose. Management should be supportive and symptomatic. Contact a poison control center immediately (e.g., 1-800-222-1222) or seek emergency medical attention.
Drug Interactions
Contraindicated Interactions
- Fluvoxamine (strong CYP1A2 inhibitor)
Major Interactions
- Other strong CYP1A2 inhibitors (e.g., ciprofloxacin, amiodarone, propafenone, mexiletine) - concomitant use should be avoided or dose reduced with close monitoring.
- Smoking (induces CYP1A2, significantly reduces pirfenidone exposure)
Moderate Interactions
- Moderate CYP1A2 inhibitors (e.g., enoxacin) - consider dose reduction or interruption of pirfenidone if intolerance occurs.
- CYP1A2 inducers (e.g., omeprazole, rifampin) - may reduce pirfenidone exposure.
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 (eGFR, CrCl)
Rationale: To assess baseline renal function, as pirfenidone is primarily renally eliminated and dose adjustments may be needed in severe 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
Action Threshold: Discontinue pirfenidone if ALT/AST >5 x ULN or if ALT/AST >3 x ULN with concomitant hyperbilirubinemia or symptoms of liver injury. Consider dose reduction or interruption if ALT/AST >3 to <5 x ULN.
Signs and symptoms of photosensitivity/rash
Frequency: Regularly, at each clinical visit
Target: Absence of severe rash
Action Threshold: Manage with sun protection. For severe rash, consider dose reduction, interruption, or discontinuation.
Gastrointestinal symptoms (nausea, diarrhea, dyspepsia)
Frequency: Regularly, at each clinical visit
Target: Tolerable
Action Threshold: Manage with symptomatic treatment, taking with food, or dose reduction/interruption if severe.
Symptom Monitoring
- Nausea
- Diarrhea
- Dyspepsia
- Abdominal pain
- Vomiting
- Fatigue
- Dizziness
- Headache
- Rash
- Photosensitivity reaction
- Weight decrease
- Anorexia
- Signs of liver injury (e.g., jaundice, dark urine, right upper quadrant pain)
Special Patient Groups
Pregnancy
Pirfenidone is Pregnancy Category C. 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:
Animal studies showed developmental toxicity (reduced fetal weight, increased skeletal variations) at doses associated with maternal toxicity.
Second Trimester:
Animal studies showed developmental toxicity (reduced fetal weight, increased skeletal variations) at doses associated with maternal toxicity.
Third Trimester:
Animal studies showed developmental toxicity (reduced fetal weight, increased skeletal variations) at doses associated with maternal toxicity. Pirfenidone has been shown to prolong gestation and increase dystocia in rats.
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:
L3 - Moderate risk. Potential for adverse effects on the infant due to unknown excretion and potential for serious adverse reactions.
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 and younger patients. No specific dose adjustment is required based on age alone, but monitor for age-related decline in renal or hepatic function.
Clinical Information
Clinical Pearls
- Always titrate the dose gradually over 14 days to the full maintenance dose to improve tolerability and reduce gastrointestinal side effects.
- Instruct patients to take pirfenidone with food to minimize nausea and dizziness.
- Emphasize strict sun protection measures (sunscreen, protective clothing, avoiding peak sun hours) due to the high risk of photosensitivity reactions.
- Regular liver function monitoring is crucial, especially during the first 6 months of therapy.
- Counsel patients to report any signs of liver injury (e.g., jaundice, dark urine, abdominal pain) immediately.
- Smoking cessation is strongly recommended as it significantly reduces pirfenidone exposure and efficacy.
Alternative Therapies
- Nintedanib (Ofev)
Cost & Coverage
Average Cost:
$9,000 - $12,000 per 30 days supply (270 capsules of 267mg)
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'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 reporting the incident, be prepared to provide details about the medication taken, the amount, and the time it occurred.