Deferasirox 180mg Tablets
WARNING: This drug may cause kidney problems. Some people have needed dialysis. Sometimes, these kidney problems have been deadly. The risk of kidney problems may be higher if you already have kidney problems or other health problems. You will need to have your kidney function checked as you have been told by your doctor. If you have questions, talk with your doctor.If you are dehydrated or are taking any drugs that can raise the chance of kidney problems, talk with your doctor. There are many drugs that can raise the chance of kidney problems. Ask your doctor or pharmacist if you are not sure.This drug may cause liver problems. Sometimes, this has been deadly. The risk of liver problems may be higher if you are older than 55 years or if you already have liver problems or other health problems. You will need to have your liver function checked as you have been told by your doctor. If you have questions, talk with your doctor.If you have kidney or liver problems, talk with your doctor. This drug may need to be avoided or the dose may need to be changed with certain types of kidney or liver problems.This drug may raise the chance of severe and sometimes deadly stomach or bowel problems like ulcers or bleeding. The risk is greater in older people, and in people who have had stomach or bowel ulcers or bleeding before. These problems may occur without warning signs. @ COMMON USES: It is used to get rid of iron when too much is in the body.
Drug Class
Iron Chelator
Pharmacologic Class
Iron Chelator
Pregnancy Category
Category B
FDA Approved
Mar 2015
DEA Schedule
Not Controlled
Overview
What is this medicine?
Deferasirox is a medicine used to remove extra iron from your body. Too much iron can build up from frequent blood transfusions or certain blood disorders, and it can harm your organs. This medicine helps your body get rid of the excess iron, mainly through your stool.
How to Use This Medicine
Taking Your Medication
To take this medication correctly, follow your doctor's instructions and read all the information provided. Take the medication on an empty stomach or with a light meal. Swallow the tablet whole with water or another liquid. If you have difficulty swallowing tablets, you can crush the tablet and mix it with a small amount of soft food. However, be sure to consume the mixture immediately and do not store it for later use.
Important Note: If you need to crush the 90 mg tablet, consult with your doctor or pharmacist first, as certain types of tablet crushers should not be used.
Take your medication at the same time every day, as directed by your doctor or healthcare provider. Continue taking the medication even if you feel well, unless your doctor instructs you to stop.
Storing and Disposing of Your Medication
Store your medication at room temperature in a dry place, avoiding the bathroom. Keep all medications in a safe 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 with your pharmacist, who may be aware of drug take-back programs in your area.
Missing a Dose
If you miss a dose, take it as soon as you remember. However, if it is 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 a missed dose.
To take this medication correctly, follow your doctor's instructions and read all the information provided. Take the medication on an empty stomach or with a light meal. Swallow the tablet whole with water or another liquid. If you have difficulty swallowing tablets, you can crush the tablet and mix it with a small amount of soft food. However, be sure to consume the mixture immediately and do not store it for later use.
Important Note: If you need to crush the 90 mg tablet, consult with your doctor or pharmacist first, as certain types of tablet crushers should not be used.
Take your medication at the same time every day, as directed by your doctor or healthcare provider. Continue taking the medication even if you feel well, unless your doctor instructs you to stop.
Storing and Disposing of Your Medication
Store your medication at room temperature in a dry place, avoiding the bathroom. Keep all medications in a safe 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 with your pharmacist, who may be aware of drug take-back programs in your area.
Missing a Dose
If you miss a dose, take it as soon as you remember. However, if it is 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 a missed dose.
Lifestyle & Tips
- Take the tablet whole or crushed and mixed with soft food (e.g., applesauce, yogurt) or orange juice/apple juice. Do NOT chew the tablet.
- Take on an empty stomach or with a light meal at the same time each day.
- Maintain good hydration, especially in hot weather or during exercise.
- Avoid aluminum-containing antacids (e.g., Maalox, Mylanta) as they can interfere with deferasirox absorption.
- Report any new or worsening side effects to your doctor immediately.
Available Forms & Alternatives
Available Strengths:
- Deferasirox 90mg Tablets
- Deferasirox 360mg Tablets
- Deferasirox 125mg Tablets For Susp
- Deferasirox 500mg Tablets For Susp
- Deferasirox 250mg Tablets For Susp
- Deferasirox 180mg Tablets
- Deferasirox 90mg Oral Granules
- Deferasirox 180mg Granules
- Deferasirox 360mg Granules
- Deferasirox 180mg Granules
- Deferasirox 360mg Granules
- Deferasirox 90mg Oral Granules
Dosing & Administration
Adult Dosing
Standard Dose:
Initial dose for chronic iron overload: 14 mg/kg orally once daily. Adjust dose based on serum ferritin trends and patient response, typically in increments of 3.5 to 7 mg/kg. Max dose 28 mg/kg/day.
Dose Range:
14 - 28 mg
Condition-Specific Dosing:
Transfusional Iron Overload:
Initial dose 14 mg/kg/day. May increase to 21 mg/kg/day if needed. Max 28 mg/kg/day.
Non-transfusion-dependent Thalassemia Syndromes:
Initial dose 7 mg/kg/day. May increase to 14 mg/kg/day if needed. Max 14 mg/kg/day.
Pediatric Dosing
Neonatal:
Not established (safety and efficacy not established in pediatric patients <2 years of age).
Infant:
Not established (safety and efficacy not established in pediatric patients <2 years of age).
Child:
âĨ2 years: Same as adult dosing (14 mg/kg/day for transfusional iron overload, 7 mg/kg/day for non-transfusion-dependent thalassemia syndromes).
Adolescent:
Same as adult dosing.
Dose Adjustments
Renal Impairment:
Mild:
CrCl 60-90 mL/min: No initial dose adjustment. Monitor renal function closely.
Moderate:
CrCl 30-59 mL/min: Reduce initial dose by 50% (e.g., 7 mg/kg/day for transfusional iron overload). Monitor renal function closely.
Severe:
CrCl <30 mL/min: Contraindicated.
Dialysis:
Contraindicated in patients with severe renal impairment or end-stage renal disease (ESRD) on dialysis.
Hepatic Impairment:
Mild:
Child-Pugh A: No initial dose adjustment.
Moderate:
Child-Pugh B: Reduce initial dose by 50% (e.g., 7 mg/kg/day for transfusional iron overload). Monitor liver function closely.
Severe:
Child-Pugh C: Contraindicated.
Pharmacology
Mechanism of Action
Deferasirox is an orally active chelator that is highly selective for iron. It forms a stable 2:1 complex with iron (Fe3+), thereby promoting the excretion of iron from the body, primarily via the feces. It has a low affinity for other metals like zinc and copper.
Pharmacokinetics
Absorption:
Bioavailability:
Approximately 70% (relative to deferasirox oral suspension for tablets)
Tmax:
2-4 hours
FoodEffect:
High-fat meal increases AUC and Cmax by 70% and 50% respectively. Low-fat meal increases AUC and Cmax by 30% and 20% respectively. Should be taken on an empty stomach or with a light meal to avoid significant increase in exposure.
Distribution:
Vd:
14 L (adults)
ProteinBinding:
>99% (primarily to serum albumin)
CnssPenetration:
Limited
Elimination:
HalfLife:
8-16 hours
Clearance:
Not readily quantifiable due to enterohepatic recirculation
ExcretionRoute:
Fecal (84%), Renal (8%)
Unchanged:
Not available (primarily excreted as glucuronide conjugates)
Pharmacodynamics
OnsetOfAction:
Not precisely defined, but iron excretion begins shortly after administration.
PeakEffect:
Reduction in iron burden is gradual, observed over weeks to months of therapy.
DurationOfAction:
Daily dosing maintains continuous iron chelation.
Safety & Warnings
BLACK BOX WARNING
Deferasirox can cause renal impairment, hepatic impairment and failure, and gastrointestinal hemorrhage. Renal impairment, including renal failure requiring dialysis, has occurred. Hepatic failure, sometimes fatal, has occurred. Gastrointestinal hemorrhages, sometimes fatal, have occurred, especially in elderly patients with advanced hematologic malignancies and/or low platelet counts. Monitor renal and hepatic function and gastrointestinal bleeding.
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 immediately or seek emergency medical attention:
Signs of an allergic reaction: rash, hives, itching, red, swollen, blistered, or peeling skin (with or without fever), wheezing, tightness in the chest or throat, difficulty breathing, swallowing, or talking, unusual hoarseness, or swelling of the mouth, face, lips, tongue, or throat.
Signs of kidney problems: inability to urinate, changes in urine output, blood in the urine, or significant weight gain.
Signs of liver problems: dark urine, fatigue, decreased appetite, stomach upset or pain, light-colored stools, vomiting, or yellowing of the skin or eyes.
Signs of bowel problems: black, tarry, or bloody stools, fever, mucus in the stool, vomiting blood or coffee ground-like material, severe stomach pain, constipation, or diarrhea.
Changes in hearing or vision.
Chest pain or pressure, rapid heartbeat, or fainting.
Flu-like symptoms.
Rashes, which may require discontinuation of the medication. If you develop a rash, contact your doctor promptly to determine the best course of action.
Severe skin reactions, including Stevens-Johnson syndrome (SJS), toxic epidermal necrolysis (TEN), and other serious conditions, which can be life-threatening. Seek immediate medical attention if you experience red, swollen, blistered, or peeling skin; red or irritated eyes; sores in the mouth, throat, nose, eyes, genitals, or skin; fever; chills; body aches; shortness of breath; or swollen glands.
Bone marrow suppression, which can lead to severe bleeding or infections. Contact your doctor right away if you experience signs of infection, such as fever, chills, severe sore throat, ear or sinus pain, cough, increased or discolored sputum, painful urination, mouth sores, or unhealing wounds; bruising or bleeding; or excessive fatigue or weakness.
Other Possible Side Effects
Like all medications, this drug can cause side effects, although not everyone will experience them. If you encounter any of the following side effects or any other symptoms that concern you or persist, contact your doctor:
* Diarrhea, stomach pain, upset stomach, or vomiting.
This is not an exhaustive list of potential side effects. If you have questions or concerns, consult your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
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 immediately or seek emergency medical attention:
Signs of an allergic reaction: rash, hives, itching, red, swollen, blistered, or peeling skin (with or without fever), wheezing, tightness in the chest or throat, difficulty breathing, swallowing, or talking, unusual hoarseness, or swelling of the mouth, face, lips, tongue, or throat.
Signs of kidney problems: inability to urinate, changes in urine output, blood in the urine, or significant weight gain.
Signs of liver problems: dark urine, fatigue, decreased appetite, stomach upset or pain, light-colored stools, vomiting, or yellowing of the skin or eyes.
Signs of bowel problems: black, tarry, or bloody stools, fever, mucus in the stool, vomiting blood or coffee ground-like material, severe stomach pain, constipation, or diarrhea.
Changes in hearing or vision.
Chest pain or pressure, rapid heartbeat, or fainting.
Flu-like symptoms.
Rashes, which may require discontinuation of the medication. If you develop a rash, contact your doctor promptly to determine the best course of action.
Severe skin reactions, including Stevens-Johnson syndrome (SJS), toxic epidermal necrolysis (TEN), and other serious conditions, which can be life-threatening. Seek immediate medical attention if you experience red, swollen, blistered, or peeling skin; red or irritated eyes; sores in the mouth, throat, nose, eyes, genitals, or skin; fever; chills; body aches; shortness of breath; or swollen glands.
Bone marrow suppression, which can lead to severe bleeding or infections. Contact your doctor right away if you experience signs of infection, such as fever, chills, severe sore throat, ear or sinus pain, cough, increased or discolored sputum, painful urination, mouth sores, or unhealing wounds; bruising or bleeding; or excessive fatigue or weakness.
Other Possible Side Effects
Like all medications, this drug can cause side effects, although not everyone will experience them. If you encounter any of the following side effects or any other symptoms that concern you or persist, contact your doctor:
* Diarrhea, stomach pain, upset stomach, or vomiting.
This is not an exhaustive list of potential side effects. If you have questions or concerns, consult your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
Seek Immediate Medical Attention If You Experience:
- Severe stomach pain, black or bloody stools, vomiting blood (signs of GI bleeding)
- Yellowing of skin or eyes, dark urine, severe nausea/vomiting (signs of liver problems)
- Swelling in legs or feet, decreased urination, unusual tiredness (signs of kidney problems)
- Sudden changes in vision or hearing
- Severe skin rash, blistering, or peeling skin
- Fever, chills, sore throat, or other signs of infection (may indicate low white blood cell count)
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. Describe the allergic reaction you experienced, including the symptoms that occurred.
Certain health conditions, including:
+ Cancer
+ Blood or bone marrow disorders, such as low platelet count or high-risk myelodysplastic syndrome (MDS)
+ Kidney disease
+ Liver disease
Any instances of dehydration, such as:
+ Inability to eat or drink normally
+ Diarrhea
+ Vomiting
+ Other illnesses that may cause dehydration
Use of similar medications. If you are unsure, consult your doctor or pharmacist.
Concurrent use of the following medications:
+ Cholestyramine
+ Colesevelam
+ Colestipol
+ Phenobarbital
+ Phenytoin
+ Rifampicin
+ Ritonavir
+ Theophylline
+ Tizanidine
Breast-feeding. Note: You should not breast-feed while taking this medication.
This list is not exhaustive. It is crucial to discuss all your medications (prescription, over-the-counter, natural products, and vitamins) and health conditions with your doctor and pharmacist to ensure safe use. Do not initiate, discontinue, or modify the dosage of any medication without 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. Describe the allergic reaction you experienced, including the symptoms that occurred.
Certain health conditions, including:
+ Cancer
+ Blood or bone marrow disorders, such as low platelet count or high-risk myelodysplastic syndrome (MDS)
+ Kidney disease
+ Liver disease
Any instances of dehydration, such as:
+ Inability to eat or drink normally
+ Diarrhea
+ Vomiting
+ Other illnesses that may cause dehydration
Use of similar medications. If you are unsure, consult your doctor or pharmacist.
Concurrent use of the following medications:
+ Cholestyramine
+ Colesevelam
+ Colestipol
+ Phenobarbital
+ Phenytoin
+ Rifampicin
+ Ritonavir
+ Theophylline
+ Tizanidine
Breast-feeding. Note: You should not breast-feed while taking this medication.
This list is not exhaustive. It is crucial to discuss all your medications (prescription, over-the-counter, natural products, and vitamins) and health conditions with your doctor and pharmacist to ensure safe use. Do not initiate, discontinue, or modify the dosage of any medication without 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. Until you understand how this drug affects you, avoid operating a vehicle or engaging in activities that require alertness. Regularly undergo blood work, other laboratory tests, eye exams, and hearing tests as directed by your doctor.
To avoid potential interactions, do not take antacids containing aluminum while using this medication. If you are 55 years or older, exercise caution when taking this drug, as you may be more susceptible to side effects. Similarly, when administering this medication to a child, use it with caution, as the risk of certain side effects may be increased in pediatric patients. If your child's weight changes while taking this medication, consult with your doctor, as the dosage may need to be adjusted.
When using this medication, be aware that birth control pills and other hormone-based contraceptives may be less effective in preventing pregnancy. Therefore, consider using an additional form of birth control, such as a condom, to minimize the risk of pregnancy. If you are pregnant or plan to become pregnant, inform your doctor to discuss the potential benefits and risks of using this medication during pregnancy.
To avoid potential interactions, do not take antacids containing aluminum while using this medication. If you are 55 years or older, exercise caution when taking this drug, as you may be more susceptible to side effects. Similarly, when administering this medication to a child, use it with caution, as the risk of certain side effects may be increased in pediatric patients. If your child's weight changes while taking this medication, consult with your doctor, as the dosage may need to be adjusted.
When using this medication, be aware that birth control pills and other hormone-based contraceptives may be less effective in preventing pregnancy. Therefore, consider using an additional form of birth control, such as a condom, to minimize the risk of pregnancy. If you are pregnant or plan to become pregnant, inform your doctor to discuss the potential benefits and risks of using this medication during pregnancy.
Overdose Information
Overdose Symptoms:
- Nausea
- Vomiting
- Diarrhea
- Abdominal pain
- Headache
- Dizziness
- Elevated liver transaminases
- Renal impairment
What to Do:
Seek immediate medical attention. Call 911 or Poison Control at 1-800-222-1222. Treatment is supportive.
Drug Interactions
Contraindicated Interactions
- Patients with severe renal impairment (CrCl <30 mL/min) or ESRD on dialysis
- Patients with severe hepatic impairment (Child-Pugh C)
- Patients with high-risk myelodysplastic syndromes (MDS) or advanced malignancies who may not benefit from chelation due to rapidly progressing disease
Major Interactions
- Aluminum-containing antacids (e.g., aluminum hydroxide): Concomitant use is not recommended due to potential for increased deferasirox exposure.
- Midazolam (CYP3A4 substrate): Deferasirox is a moderate CYP3A4 inducer; may decrease midazolam exposure.
- Repaglinide (CYP2C8 substrate): Deferasirox is a CYP2C8 inhibitor; may increase repaglinide exposure (monitor blood glucose).
- Theophylline (CYP1A2 substrate): Deferasirox is a CYP1A2 inducer; may decrease theophylline exposure (monitor levels).
- Oral contraceptives (CYP3A4 substrates): Deferasirox may decrease efficacy of hormonal contraceptives (advise alternative birth control).
Moderate Interactions
- UGT inducers (e.g., rifampin, phenytoin, phenobarbital, ritonavir): May decrease deferasirox exposure (consider dose increase of deferasirox).
- UGT inhibitors (e.g., fluconazole): May increase deferasirox exposure (consider dose reduction of deferasirox).
- Vitamin C: Concomitant use with deferasirox should be initiated cautiously and monitored, as high doses of vitamin C may increase iron toxicity, especially in patients with severe iron overload and cardiac dysfunction.
Minor Interactions
- Not specifically categorized as minor, but general caution with drugs affecting renal or hepatic function.
Monitoring
Baseline Monitoring
Serum ferritin
Rationale: To establish baseline iron overload and guide initial dosing.
Timing: Prior to initiation of therapy.
Serum creatinine and estimated GFR (eGFR)
Rationale: To assess baseline renal function and rule out severe impairment.
Timing: Prior to initiation of therapy.
Liver function tests (ALT, AST, bilirubin)
Rationale: To assess baseline hepatic function and rule out severe impairment.
Timing: Prior to initiation of therapy.
Urinalysis (for proteinuria)
Rationale: To assess for baseline renal tubular dysfunction.
Timing: Prior to initiation of therapy.
Audiometry and Ophthalmologic examination
Rationale: To establish baseline for potential sensory organ toxicities.
Timing: Prior to initiation of therapy.
Routine Monitoring
Serum ferritin
Frequency: Monthly
Target: Goal is typically <1000 mcg/L, but individualized based on clinical need.
Action Threshold: Increase dose if ferritin >2500 mcg/L and well-tolerated; decrease dose if ferritin <500 mcg/L or if iron burden is adequately reduced.
Serum creatinine and eGFR
Frequency: Weekly for the first month, then monthly thereafter.
Target: Stable within normal limits or baseline.
Action Threshold: If creatinine increases by >33% above baseline on two consecutive measurements, or if it exceeds the age-appropriate upper limit of normal, interrupt therapy or reduce dose. Re-evaluate if creatinine returns to baseline.
Liver function tests (ALT, AST, bilirubin)
Frequency: Weekly for the first month, then monthly thereafter.
Target: Stable within normal limits or baseline.
Action Threshold: If transaminases increase to >5 times the upper limit of normal (ULN), interrupt therapy. If transaminases increase to >2 times ULN and are progressive, consider dose reduction or interruption.
Urinalysis (for proteinuria)
Frequency: Monthly
Target: Negative or stable.
Action Threshold: If persistent proteinuria develops, consider dose reduction or interruption.
Audiometry and Ophthalmologic examination
Frequency: Annually
Target: Stable vision and hearing.
Action Threshold: If disturbances occur, consider dose reduction or interruption and refer to specialist.
Symptom Monitoring
- Signs of renal dysfunction (e.g., decreased urine output, swelling, fatigue)
- Signs of hepatic dysfunction (e.g., jaundice, dark urine, abdominal pain, nausea, vomiting)
- Gastrointestinal symptoms (e.g., severe abdominal pain, melena, hematemesis, dyspepsia, nausea, vomiting, diarrhea)
- Skin rash
- Hearing or vision changes
- Fever, sore throat, or other signs of infection (due to potential for agranulocytosis)
Special Patient Groups
Pregnancy
Deferasirox (Jadenu tablets) is Pregnancy Category B. Animal studies have shown no evidence of teratogenicity, but there are no adequate and well-controlled studies in pregnant women. Use only if clearly needed.
Trimester-Specific Risks:
First Trimester:
Limited human data. Animal studies suggest no increased risk of major birth defects.
Second Trimester:
Limited human data.
Third Trimester:
Limited human data. Consider potential for iron deficiency in the fetus if maternal iron levels become too low.
Lactation
Deferasirox is excreted in the milk of lactating rats. It is not known whether deferasirox is excreted in human milk. Due to the potential for serious adverse reactions in the breastfed infant, 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 serious adverse effects in the infant).
Pediatric Use
Safety and efficacy have not been established in pediatric patients younger than 2 years of age. Close monitoring of renal and hepatic function is crucial in all pediatric patients, as they may be more susceptible to adverse effects.
Geriatric Use
Elderly patients (âĨ65 years) may be at increased risk of adverse reactions, particularly gastrointestinal hemorrhage, renal impairment, and bone marrow suppression. Use with caution and monitor closely.
Clinical Information
Clinical Pearls
- Deferasirox tablets (Jadenu) offer improved patient convenience compared to the dispersible tablets (Exjade) due to being swallowed whole or crushed, eliminating the need for mixing in liquid.
- Strict adherence to monitoring protocols (renal, hepatic, ferritin, sensory) is critical due to potential for serious adverse effects.
- Patients should be educated on the importance of hydration to minimize renal toxicity.
- Dose adjustments are frequently needed based on serum ferritin trends and tolerability.
- Consider alternative contraception for women of childbearing potential due to potential interaction with oral contraceptives.
Alternative Therapies
- Deferoxamine (Desferal) - parenteral iron chelator
- Deferiprone (Ferriprox) - oral iron chelator
Cost & Coverage
Average Cost:
Not available per 30 tablets
Generic Available:
Yes
Insurance Coverage:
Tier 3 or 4 (Specialty Drug)
General Drug Facts
If your symptoms or health issues persist or worsen, it is essential to contact your doctor promptly. To ensure safe use, never share your medication with others or take someone else's medication. This medication is accompanied by a Medication Guide, which provides crucial information for patients. Please read this guide carefully and review it again whenever you receive a refill of this medication. If you have any questions or concerns about this medication, consult your doctor, pharmacist, or other healthcare provider for guidance. 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 quantity, and the time it occurred.