Deferasirox 500mg Tablets For Susp

Manufacturer ASCENDLABS Active Ingredient Deferasirox Tablets For Oral Suspension(de FER a sir ox) Pronunciation de FER a sir ox
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.
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Drug Class
Chelating Agent
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Pharmacologic Class
Triazole Derivative Iron Chelator
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Pregnancy Category
Category C
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FDA Approved
Nov 2005
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DEA Schedule
Not Controlled

Overview

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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.
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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 to you and follow the instructions precisely.

Take your medication on an empty stomach, 30 minutes before a meal.
To take your medication, mix the tablet with a small amount of fruit juice (such as orange or apple juice) or water until it is fully dissolved. Drink the mixture immediately. Do not chew or swallow the tablet whole.
After drinking the mixture, rinse the glass with more juice or water to ensure you get the full dose, and then drink the rinse liquid.

Take 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 place, away from the bathroom.
Keep all medications in a safe and 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. 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. However, if it is 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.
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Lifestyle & Tips

  • Take the medicine once daily, preferably at the same time each day.
  • For tablets for oral suspension (Exjade): Dissolve the tablet completely by stirring in a small amount of water, orange juice, or apple juice (100-200 mL) until a fine suspension is obtained. Drink immediately. Do not chew the tablets or swallow them whole.
  • Take on an empty stomach or with a light meal to ensure consistent absorption.
  • Avoid taking with aluminum-containing antacids (e.g., Maalox, Mylanta) as they can interfere with absorption.
  • Stay well-hydrated while taking this medication to support kidney function.
  • Report any new or worsening side effects to your doctor immediately.

Dosing & Administration

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Adult Dosing

Standard Dose: Initial dose 20 mg/kg/day orally, adjusted based on serum ferritin levels. Max 40 mg/kg/day.
Dose Range: 10 - 40 mg

Condition-Specific Dosing:

transfusionalIronOverload: Initial dose 20 mg/kg/day. Adjust in 5-10 mg/kg increments every 3-6 months based on serum ferritin trends. Goal ferritin <1000 mcg/L.
nonTransfusionDependentThalassemia: Initial dose 10 mg/kg/day. Adjust in 5-10 mg/kg increments every 3-6 months based on serum ferritin trends. Goal ferritin <300 mcg/L.
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Pediatric Dosing

Neonatal: Not established (approved for â‰Ĩ2 years of age)
Infant: Not established (approved for â‰Ĩ2 years of age)
Child: Initial dose 20 mg/kg/day orally for transfusional iron overload (â‰Ĩ2 years of age). Initial dose 10 mg/kg/day for non-transfusion-dependent thalassemia (â‰Ĩ10 years of age).
Adolescent: Initial dose 20 mg/kg/day orally for transfusional iron overload. Initial dose 10 mg/kg/day for non-transfusion-dependent thalassemia.
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Dose Adjustments

Renal Impairment:

Mild: CrCl 40-60 mL/min: Consider starting at a lower dose (e.g., 10 mg/kg/day) and monitor renal function closely.
Moderate: CrCl 20-39 mL/min: Contraindicated. If CrCl decreases to <40 mL/min during treatment, interrupt therapy and re-evaluate.
Severe: CrCl <20 mL/min: Contraindicated.
Dialysis: Contraindicated.

Hepatic Impairment:

Mild: Child-Pugh A: No initial dose adjustment, but monitor closely.
Moderate: Child-Pugh B: Reduce initial dose by 50%. Monitor closely.
Severe: Child-Pugh C: Contraindicated.

Pharmacology

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Mechanism of Action

Deferasirox is an orally active chelator that is highly selective for iron. It binds iron with high affinity in a 2:1 ratio (deferasirox:iron), forming a stable, soluble complex that is excreted primarily via the feces. This process facilitates the removal of excess iron from the body, reducing iron-induced organ damage.
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Pharmacokinetics

Absorption:

Bioavailability: Exjade (oral suspension): Approximately 70% relative to an intravenous dose. Jadenu (film-coated tablet) has higher bioavailability.
Tmax: Exjade (oral suspension): 1.5 to 4 hours.
FoodEffect: Exjade (oral suspension): A high-fat meal increases AUC by 100% and Cmax by 160%. A low-fat meal increases AUC by 50% and Cmax by 80%. Should be taken on an empty stomach or with a light meal.

Distribution:

Vd: Approximately 14 L in adults.
ProteinBinding: >99% (primarily to serum albumin).
CnssPenetration: Limited

Elimination:

HalfLife: 8 to 16 hours.
Clearance: Approximately 11.6 L/h (apparent oral clearance).
ExcretionRoute: Primarily fecal (84%), with a small amount (8%) excreted renally.
Unchanged: Less than 1% renally excreted as unchanged drug.
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Pharmacodynamics

OnsetOfAction: Not acutely defined; therapeutic effects (iron chelation) are observed over weeks to months.
PeakEffect: Reduction in iron burden (e.g., serum ferritin) is gradual, typically observed over months of consistent therapy.
DurationOfAction: Effects persist as long as the drug is taken; iron re-accumulation occurs upon discontinuation.

Safety & Warnings

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BLACK BOX WARNING

Deferasirox can cause renal failure, hepatic failure, and gastrointestinal hemorrhage, sometimes fatal. Monitor renal function, liver function, and gastrointestinal bleeding. Deferasirox is contraindicated in patients with severe renal impairment (CrCl <20 mL/min) and severe hepatic impairment (Child-Pugh C).
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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
Signs of kidney problems, including:
+ Inability to pass urine
+ Changes in urine output
+ Blood in the urine
+ Sudden weight gain
Signs of liver problems, such as:
+ Dark urine
+ Fatigue
+ Decreased appetite
+ Upset stomach or stomach pain
+ Light-colored stools
+ Vomiting
+ Yellow skin or eyes
Signs of bowel problems, including:
+ Black, tarry, or bloody stools
+ Fever
+ Mucus in the stools
+ Vomiting blood or coffee ground-like material
+ Severe stomach pain, constipation, or diarrhea
Changes in hearing or eyesight
Chest pain or pressure, rapid heartbeat, or fainting
Flu-like symptoms
Rashes, which may require stopping the medication; if you develop a rash, contact your doctor immediately
Severe skin reactions, including:
+ Stevens-Johnson syndrome (SJS)
+ Toxic epidermal necrolysis (TEN)
+ Other serious reactions, which can affect body organs and be life-threatening; seek medical help immediately 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
- Swollen glands
Bone marrow suppression, which can lead to severe bleeding problems or infections; contact your doctor if you experience:
+ Signs of infection, such as fever, chills, severe sore throat, ear or sinus pain, cough, increased or changed sputum, painful urination, mouth sores, or unhealing wounds
+ Bruising or bleeding
+ Extreme fatigue or weakness

Other Possible Side Effects

Like all medications, this drug can cause side effects, although many people may not experience any or may only have mild symptoms. If you are bothered by any of the following side effects or if they persist, contact your doctor or seek medical help:

Diarrhea
Stomach pain
Upset stomach
Vomiting

This is not an exhaustive list of possible side effects. If you have questions or concerns about side effects, contact your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
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Seek Immediate Medical Attention If You Experience:

  • Severe stomach pain, black or tarry stools, vomiting blood (signs of GI bleeding)
  • Yellowing of skin or eyes (jaundice), dark urine, unusual tiredness (signs of liver problems)
  • Decreased urination, swelling in legs or feet, unusual weight gain (signs of kidney problems)
  • Sudden decrease in hearing or vision changes (blurred vision, difficulty seeing)
  • Severe skin rash or blistering
  • Persistent nausea, vomiting, or diarrhea
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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. Describe the allergic reaction and its symptoms.
Existing health conditions, such as:
+ Cancer
+ Blood or bone marrow disorders (e.g., low platelet count, high-risk myelodysplastic syndrome/MDS)
+ Kidney disease
+ Liver disease
Any instances of dehydration, including:
+ 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, terminate, or modify any medication regimen without consulting your doctor.
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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 tests, other laboratory tests, eye exams, and hearing tests as directed by your doctor to monitor your health. Do not take antacids containing aluminum while using this medication, as it may interfere with its effectiveness.

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 higher in pediatric patients. If your child's weight changes while taking this medication, consult your doctor, as their 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. To minimize the risk of unintended pregnancy, use an additional form of birth control, such as a condom, in conjunction with your regular birth control method.

If you are pregnant or planning to become pregnant, consult your doctor to discuss the potential benefits and risks associated with taking this medication during pregnancy.
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Overdose Information

Overdose Symptoms:

  • Nausea
  • Vomiting
  • Diarrhea
  • Abdominal pain
  • Headache
  • Increased liver enzymes
  • Renal dysfunction

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

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Contraindicated Interactions

  • Aluminum-containing antacids (e.g., aluminum hydroxide)
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Major Interactions

  • UGT inducers (e.g., rifampin, phenytoin, phenobarbital, ritonavir)
  • CYP3A4 inducers (e.g., rifampin)
  • Oral contraceptives (estrogen/progestin combinations)
  • Irinotecan (UGT1A1 substrate)
  • Theophylline (CYP1A2 substrate)
  • Repaglinide (UGT1A1 substrate)
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Moderate Interactions

  • NSAIDs (e.g., ibuprofen, naproxen)
  • Corticosteroids (e.g., prednisone)
  • Oral bisphosphonates (e.g., alendronate)
  • Proton pump inhibitors (e.g., omeprazole)
  • H2-receptor antagonists (e.g., ranitidine)
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Minor Interactions

  • Cholestyramine (may decrease deferasirox exposure)

Monitoring

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Baseline Monitoring

Serum ferritin

Rationale: To establish baseline iron burden and guide initial dosing.

Timing: Prior to initiation of therapy.

Serum creatinine and estimated creatinine clearance (CrCl)

Rationale: To assess renal function, as deferasirox is associated with renal toxicity and dose adjustments are needed for impairment.

Timing: Prior to initiation of therapy.

Liver function tests (LFTs: AST, ALT, alkaline phosphatase, bilirubin)

Rationale: To assess hepatic function, as deferasirox can cause hepatic toxicity and dose adjustments are needed for impairment.

Timing: Prior to initiation of therapy.

Urinalysis (proteinuria)

Rationale: To screen for renal tubular dysfunction.

Timing: Prior to initiation of therapy.

Audiometry

Rationale: To establish baseline hearing, as deferasirox can cause hearing loss.

Timing: Prior to initiation of therapy.

Ophthalmologic examination (slit lamp, fundoscopy)

Rationale: To establish baseline vision, as deferasirox can cause ocular disturbances.

Timing: Prior to initiation of therapy.

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Routine Monitoring

Serum ferritin

Frequency: Monthly

Target: Goal <1000 mcg/L for transfusional iron overload; <300 mcg/L for non-transfusion-dependent thalassemia.

Action Threshold: If consistently >2500 mcg/L, consider dose increase. If consistently <500 mcg/L, consider dose reduction or interruption.

Serum creatinine and CrCl

Frequency: Weekly for the first month, then monthly thereafter.

Target: Stable, within normal limits for age.

Action Threshold: If increase >33% above baseline on two consecutive measurements, or if CrCl falls below 40 mL/min, interrupt therapy and re-evaluate.

Liver function tests (AST, ALT)

Frequency: Bi-weekly for the first month, then monthly thereafter.

Target: Within normal limits.

Action Threshold: If persistently elevated (e.g., >5 times ULN), interrupt therapy. If >10 times ULN, discontinue.

Urinalysis (proteinuria)

Frequency: Monthly

Target: Negative or trace protein.

Action Threshold: If persistent or increasing proteinuria, investigate and consider dose adjustment or interruption.

Audiometry

Frequency: Annually

Target: Stable hearing.

Action Threshold: If hearing impairment detected, consider dose reduction or interruption.

Ophthalmologic examination

Frequency: Annually

Target: Stable vision.

Action Threshold: If visual disturbances (e.g., cataracts, retinal toxicity) detected, consider dose reduction or interruption.

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Symptom Monitoring

  • Gastrointestinal symptoms (nausea, vomiting, diarrhea, abdominal pain)
  • Skin rash
  • Hearing changes (decreased hearing, tinnitus)
  • Vision changes (blurred vision, decreased acuity, cataracts)
  • Signs of renal dysfunction (decreased urine output, edema)
  • Signs of hepatic dysfunction (jaundice, dark urine, fatigue)
  • Signs of bleeding (black/tarry stools, blood in vomit, easy bruising)

Special Patient Groups

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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 show developmental toxicity (skeletal malformations, reduced fetal weight) at doses higher than human therapeutic doses. Risk in humans is unknown.
Second Trimester: Risk in humans is unknown. Continued monitoring of maternal iron burden is important.
Third Trimester: Risk in humans is unknown. Consider potential for neonatal iron overload if maternal iron burden is not controlled.
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Lactation

It is not known whether deferasirox is 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 is unknown but cannot be ruled out. Monitor infant for adverse effects.
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Pediatric Use

Approved for children 2 years of age and older for transfusional iron overload. For non-transfusion-dependent thalassemia, approved for children 10 years of age and older. Dosing is weight-based. Close monitoring of renal and hepatic function, and growth parameters is crucial.

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Geriatric Use

Increased incidence of adverse reactions, particularly renal, hepatic, and gastrointestinal (including hemorrhage), has been observed in elderly patients. Use with caution and monitor closely. Consider lower initial doses and slower titration.

Clinical Information

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Clinical Pearls

  • Deferasirox is available as tablets for oral suspension (Exjade) and film-coated tablets (Jadenu). Ensure the correct formulation is prescribed and dispensed, as their bioavailability and dosing differ.
  • For tablets for oral suspension, proper preparation is crucial: fully dissolve in water, orange juice, or apple juice and drink immediately. Do not chew or swallow whole.
  • Strict adherence to monitoring protocols (renal, hepatic, ferritin, audiometry, ophthalmology) is essential due to potential serious adverse effects.
  • Maintain adequate hydration to minimize the risk of renal toxicity.
  • Patients should be educated on the signs and symptoms of serious adverse events (e.g., GI bleeding, liver/kidney failure) and instructed to seek immediate medical attention if they occur.
  • Dose adjustments are frequently needed based on serum ferritin levels and tolerability.
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Alternative Therapies

  • Deferoxamine (parenteral iron chelator)
  • Deferiprone (oral iron chelator)
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Cost & Coverage

Average Cost: Varies widely, typically $1,000 - $5,000+ per 30 tablets (500mg)
Generic Available: Yes
Insurance Coverage: Tier 4 (Specialty Drug) or Tier 5 (Specialty Drug) for most commercial and Medicare Part D plans.
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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. 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.