Esbriet 801mg 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 medication 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, but it does not cure the disease. It's important to take it exactly as prescribed, usually with food, to help reduce side effects.
How to Use This Medicine
Taking Your Medication Correctly
To get the most benefit from your medication, follow these guidelines:
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 feeling 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.
Check with your pharmacist for guidance on the best way to dispose of your medication, and consider participating in a local drug take-back program.
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 the maximum of three doses in a 24-hour period.
* If you miss 14 or more days of taking your medication, consult your doctor before restarting your medication regimen.
To get the most benefit from your medication, follow these guidelines:
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 feeling 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.
Check with your pharmacist for guidance on the best way to dispose of your medication, and consider participating in a local drug take-back program.
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 the maximum of three doses in a 24-hour period.
* If you miss 14 or more days of taking your medication, consult your doctor before restarting your medication regimen.
Lifestyle & Tips
- Take pirfenidone with food to help reduce stomach upset (nausea, diarrhea).
- Avoid or minimize exposure to sunlight and artificial UV light (e.g., tanning beds) while taking this medication, as it can cause severe sunburn or rash. 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 and worsen IPF.
- Limit or avoid grapefruit and grapefruit juice, as they may increase pirfenidone levels.
Available Forms & Alternatives
Available Strengths:
Generic Alternatives:
Dosing & Administration
Adult Dosing
Standard Dose:
Initial titration: 267 mg orally three times daily for 7 days, then 534 mg orally three times daily for 7 days, then 801 mg orally three times daily (maintenance dose). Total daily dose: 2403 mg.
Dose Range:
267 - 801 mg
Condition-Specific Dosing:
Idiopathic Pulmonary Fibrosis (IPF):
Maintenance dose is 801 mg three times daily (2403 mg/day).
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 adverse effects occur.
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:
Reduce dose to 801 mg/day (267 mg three times daily). Monitor closely for adverse effects. Consider further dose reduction or interruption if needed (Child-Pugh B).
Severe:
Not recommended (Child-Pugh C).
Pharmacology
Mechanism of Action
The exact mechanism of action of pirfenidone in idiopathic pulmonary fibrosis (IPF) is not fully elucidated. However, it is thought to exert antifibrotic effects through inhibition of various pro-fibrotic cytokines and growth factors, including transforming growth factor-beta (TGF-β), tumor necrosis factor-alpha (TNF-ι), platelet-derived growth factor (PDGF), and fibroblast growth factor (FGF). It reduces fibroblast proliferation, collagen synthesis, and the production of mediators associated with inflammation and fibrosis.
Pharmacokinetics
Absorption:
Bioavailability:
Approximately 50%
Tmax:
0.5-4 hours (fasted state)
FoodEffect:
Food significantly decreases Cmax (by approximately 50%) and increases Tmax, but increases AUC by approximately 20%. Taking with food improves tolerability and is recommended.
Distribution:
Vd:
Approximately 70 L
ProteinBinding:
Approximately 50-80%
CnssPenetration:
Limited
Elimination:
HalfLife:
Approximately 2.4-3.8 hours
Clearance:
Not available
ExcretionRoute:
Primarily renal (approximately 80% of dose excreted in urine as metabolites)
Unchanged:
<1%
Pharmacodynamics
OnsetOfAction:
Not well-defined for chronic antifibrotic effects; clinical benefits observed over months.
PeakEffect:
Not well-defined for chronic antifibrotic effects.
DurationOfAction:
Not well-defined for chronic antifibrotic effects.
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 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 list is not exhaustive, and if you have questions or concerns about side effects, 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. 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 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 list is not exhaustive, and if you have questions or concerns about side effects, 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 your skin or the whites of your eyes (jaundice), dark urine, unusual tiredness, severe nausea or vomiting, pain in the upper right side of your stomach.
- Severe skin rash or blistering, especially after sun exposure.
- Unexplained weight loss.
- New or worsening shortness of breath.
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 a history of 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 currently taking
Any natural products or vitamins you are using
Your complete medical history, including any health problems you have
Before starting, stopping, or adjusting 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.
If you have a history of 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 currently taking
Any natural products or vitamins you are using
Your complete medical history, including any health problems you have
Before starting, stopping, or adjusting 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. 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 smoking cessation 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 breastfeeding, 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 smoking cessation 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 breastfeeding, 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:
- Nausea
- Vomiting
- Diarrhea
- Dizziness
- Fatigue
- Rash
What to Do:
In case of overdose, seek immediate medical attention or call a Poison Control Center (1-800-222-1222). Management is supportive and symptomatic.
Drug Interactions
Contraindicated Interactions
- Fluvoxamine (strong CYP1A2 inhibitor)
Major Interactions
- Strong CYP1A2 inhibitors (e.g., ciprofloxacin, amiodarone, propafenone, mexiletine, enoxacin, grepafloxacin, levofloxacin, norfloxacin, ofloxacin)
- Strong CYP1A2 inducers (e.g., rifampin)
Moderate Interactions
- Moderate CYP1A2 inhibitors (e.g., cimetidine, oral contraceptives)
Minor Interactions
- Not available
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 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 or stable.
Action Threshold: Discontinue pirfenidone if ALT or AST >5 x ULN, or if ALT or AST >3 x ULN with concomitant hyperbilirubinemia or clinical symptoms of liver injury. Consider dose reduction or interruption if ALT or AST >3 to â¤5 x ULN without hyperbilirubinemia or symptoms.
Signs and symptoms of photosensitivity/rash
Frequency: Regularly, especially during sun exposure.
Target: Absence of severe rash or photosensitivity.
Action Threshold: Consider dose reduction or interruption for severe rash or photosensitivity reaction. Advise patients to use sunscreen and protective clothing.
Symptom Monitoring
- Nausea
- Diarrhea
- Dyspepsia
- Abdominal pain
- Fatigue
- Headache
- Dizziness
- Insomnia
- Weight decrease
- Anorexia
- Rash
- Photosensitivity reaction
- Signs of liver injury (e.g., jaundice, dark urine, severe nausea/vomiting, right upper quadrant pain)
Special Patient Groups
Pregnancy
Pirfenidone is not recommended for use during pregnancy unless the potential benefit justifies the potential risk to the fetus. Animal studies have shown developmental toxicity (e.g., reduced fetal weight, increased skeletal variations). 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 unknown if pirfenidone or its metabolites are excreted in human milk. Due to the potential for serious adverse reactions in breastfed infants, breastfeeding is not recommended during treatment with pirfenidone.
Infant Risk:
Risk cannot be ruled out; potential for serious adverse effects.
Pediatric Use
The safety and effectiveness of pirfenidone in pediatric patients have not been established. It is not indicated for use in this population.
Geriatric Use
No specific dose adjustment is required for elderly patients. However, elderly patients may be more susceptible to adverse effects, and monitoring for liver function and other side effects should be diligent.
Clinical Information
Clinical Pearls
- Pirfenidone should always be taken with food to minimize gastrointestinal side effects (nausea, diarrhea, dyspepsia).
- Strict adherence to sun protection measures (sunscreen SPF 50+, protective clothing) is crucial due to the high risk of photosensitivity reactions.
- Regular liver function monitoring is essential, especially during the first 6 months of therapy, to detect potential drug-induced liver injury.
- Patients should be educated on the titration schedule to minimize initial side effects and improve adherence.
- If a dose is missed, patients should take the next scheduled dose; they should not take two doses to make up for a missed dose.
- Smoking cessation is strongly advised for patients with IPF, as it can impact disease progression and potentially reduce pirfenidone efficacy.
Alternative Therapies
- Nintedanib (Ofev) - another antifibrotic agent approved for Idiopathic Pulmonary Fibrosis (IPF).
Cost & Coverage
Average Cost:
Typically >$10,000 - $15,000 per 30 tablets (801mg)
Generic Available:
Yes
Insurance Coverage:
Specialty tier, often requires prior authorization and may have specific criteria for coverage.
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. If you have any questions or concerns about your 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 reporting the incident, be prepared to provide detailed information, including the type of medication taken, the amount, and the time it occurred.