Deferasirox 125mg Tablets For Susp

Manufacturer BIONPHARMA 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
Iron Chelator
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Pharmacologic Class
Tridentate Ligand
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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 that extra 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 with your prescription and follow the instructions closely.

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 a small amount of juice or water to ensure you get all of the medication, and then drink the rinse.

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 to feel better.

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 any unused or expired medication properly. Do not flush medication down the toilet or pour it 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 ask about any local drug take-back programs.

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 to make up for a missed dose.
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Lifestyle & Tips

  • Take the medicine once daily, preferably at the same time each day.
  • For tablets for oral suspension (Exjade), disperse the tablet in water, orange juice, or apple juice (100-200 mL) until a fine suspension is formed. Drink immediately. Do not chew or swallow the tablets whole.
  • Take on an empty stomach or with a light meal to ensure consistent absorption.
  • Avoid taking with aluminum-containing antacids.
  • Maintain good hydration.
  • Report any new or worsening side effects to your doctor immediately.

Dosing & Administration

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Adult Dosing

Standard Dose: Transfusional Iron Overload: Initial dose 20 mg/kg/day orally. Non-Transfusion-Dependent Thalassemia (NTDT) Syndromes: Initial dose 10 mg/kg/day orally.
Dose Range: 10 - 40 mg

Condition-Specific Dosing:

transfusionalIronOverload: Initial: 20 mg/kg/day. Adjust in 5-10 mg/kg/day increments every 3-6 months based on serum ferritin trends and patient response. Max: 40 mg/kg/day.
nonTransfusionDependentThalassemia: Initial: 10 mg/kg/day. Adjust in 5-10 mg/kg/day increments every 3-6 months based on serum ferritin trends and patient response. Max: 20 mg/kg/day.
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Pediatric Dosing

Neonatal: Not established
Infant: Not established for <2 years old (transfusional) or <10 years old (NTDT).
Child: Transfusional Iron Overload (â‰Ĩ2 years): Initial 20 mg/kg/day. NTDT Syndromes (â‰Ĩ10 years): Initial 10 mg/kg/day. Dosing adjustments similar to adults.
Adolescent: Transfusional Iron Overload (â‰Ĩ2 years): Initial 20 mg/kg/day. NTDT Syndromes (â‰Ĩ10 years): Initial 10 mg/kg/day. Dosing adjustments similar to adults.
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Dose Adjustments

Renal Impairment:

Mild: No initial dose adjustment. Monitor serum creatinine closely.
Moderate: Consider reducing initial dose by 50% (e.g., 10 mg/kg/day for transfusional iron overload). Monitor serum creatinine closely. Avoid if CrCl <40 mL/min.
Severe: Contraindicated if CrCl <40 mL/min or serum creatinine >2 times the age-appropriate upper limit of normal.
Dialysis: Not recommended. Deferasirox is highly protein-bound and not dialyzable.

Hepatic Impairment:

Mild: No initial dose adjustment (Child-Pugh A).
Moderate: Reduce initial dose by 50% (Child-Pugh B). Monitor liver function closely. Avoid if Child-Pugh C.
Severe: Contraindicated (Child-Pugh C).

Pharmacology

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Mechanism of Action

Deferasirox is an orally active tridentate chelator with a high affinity for iron. It forms a stable 2:1 complex with iron, promoting its excretion primarily via the feces. It binds to iron in a 2:1 ratio (two molecules of deferasirox to one atom of iron).
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Pharmacokinetics

Absorption:

Bioavailability: Approximately 70% (oral suspension formulation)
Tmax: 1.5-4 hours
FoodEffect: High-fat meals increase AUC by 70% and Cmax by 50%. Low-fat meals increase AUC by 29% and Cmax by 15%. Should be taken on an empty stomach or with a light meal to avoid significant increases in exposure.

Distribution:

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

Elimination:

HalfLife: 8-16 hours
Clearance: Not specifically quantified, but primarily hepatic.
ExcretionRoute: Fecal (84%), Renal (8%)
Unchanged: Not available
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Pharmacodynamics

OnsetOfAction: Not acutely defined; therapeutic effects (iron chelation) are observed over weeks to months.
PeakEffect: Reduction in serum ferritin levels typically observed within months of consistent therapy.
DurationOfAction: Daily dosing required due to half-life.

Safety & Warnings

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BLACK BOX WARNING

Renal Impairment: Deferasirox can cause acute renal failure, which may require dialysis. Monitor serum creatinine and creatinine clearance. Hepatic Impairment: Deferasirox can cause hepatic failure, sometimes fatal. Monitor liver function tests. Gastrointestinal Hemorrhage: Fatal GI hemorrhage has been reported. Monitor for signs and symptoms of GI bleeding. Agranulocytosis, Thrombocytopenia, and Cytopenias: Fatal agranulocytosis, thrombocytopenia, and worsening anemia have been reported. Monitor blood counts.
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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, such as:
+ Rash or hives
+ Itching or red, swollen, blistered, or peeling skin (with or without fever)
+ Wheezing or 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, including:
+ Inability to urinate or changes in urine output
+ Blood in the urine or significant weight gain
Signs of liver problems, such as:
+ Dark urine
+ Fatigue or decreased appetite
+ Upset stomach or stomach pain
+ Light-colored stools or vomiting
+ Yellow skin or eyes
Signs of bowel problems, including:
+ Black, tarry, or bloody stools
+ Fever or mucus in the stools
+ 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 (this medication may need to be discontinued in some cases; consult your doctor if you develop a rash)
Severe skin reactions, including:
+ Stevens-Johnson syndrome (SJS)
+ Toxic epidermal necrolysis (TEN)
+ Other serious reactions that may affect internal organs and can be life-threatening
+ Symptoms may include: 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
Blood cell production problems, which can lead to severe bleeding or infections; seek medical help if you experience:
+ Fever, chills, or severe sore throat
+ Ear or sinus pain, cough, or changes in sputum
+ Painful urination or mouth sores
+ Unhealing wounds or bruising
+ Fatigue or weakness

Other Possible Side Effects

Like all medications, this drug can cause side effects. While many people may not experience any side effects or only mild ones, it's essential to discuss any concerns with your doctor. If you experience any of the following side effects or any other symptoms that bother you or do not resolve, contact your doctor:

Diarrhea
Stomach pain or upset stomach
* 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.
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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, dark urine, severe fatigue (signs of liver problems)
  • Decreased urination, swelling in legs/feet, unusual tiredness (signs of kidney problems)
  • Fever, sore throat, easy bruising or bleeding (signs of blood count problems)
  • Changes in hearing or vision
  • Severe skin rash
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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. Be sure to describe the allergic reaction and its symptoms.
Certain 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 that you should not breast-feed while taking this medication.

This list is not exhaustive, and it is crucial to discuss all your medications (prescription, over-the-counter, natural products, and vitamins) and health conditions with your doctor and pharmacist. They will help determine the safety of taking this medication with your other medications and health conditions. Do not initiate, stop, or modify the dosage of any medication 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. Before engaging in activities that require alertness, such as driving, wait until you understand how this drug affects you.

Regular monitoring is crucial; therefore, follow your doctor's instructions for scheduled blood work, lab tests, eye exams, and hearing tests.

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 children, use it with caution, as they may have a higher risk of experiencing certain side effects. If your child's weight changes while taking this medication, consult your doctor, as their dose may need to be adjusted.

When using this medication, be aware that birth control pills and other hormone-based contraceptives may be less effective. To prevent 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 plan to become pregnant, inform your doctor to discuss the potential benefits and risks of using this medication during pregnancy.
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Overdose Information

Overdose Symptoms:

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

What to Do:

Seek immediate medical attention. There is no specific antidote. Treatment is supportive. Call 1-800-222-1222 (Poison Control).

Drug Interactions

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Major Interactions

  • Aluminum-containing antacids (e.g., aluminum hydroxide): Concomitant use is contraindicated due to increased deferasirox exposure and potential for aluminum toxicity.
  • Midazolam (CYP3A4 substrate): Deferasirox is a moderate CYP3A4 inducer; may decrease exposure of CYP3A4 substrates.
  • Repaglinide (UGT1A1 substrate): Deferasirox is a UGT1A1 inducer; may decrease exposure of UGT1A1 substrates.
  • Oral Contraceptives: May decrease efficacy of hormonal contraceptives due to enzyme induction.
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Moderate Interactions

  • Cholestyramine: May decrease deferasirox exposure.
  • Vitamin C (Ascorbic Acid): Concomitant use with deferasirox may increase iron excretion, but high doses of vitamin C (>500 mg/day) may lead to cardiac toxicity in iron-overloaded patients. Use with caution and monitor cardiac function.
  • Drugs metabolized by CYP2C8 (e.g., paclitaxel, pioglitazone, rosiglitazone): Deferasirox is a weak CYP2C8 inhibitor; may increase exposure of these drugs.
  • Drugs that cause nephrotoxicity (e.g., NSAIDs, aminoglycosides): Increased risk of renal adverse events.

Monitoring

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Baseline Monitoring

Serum Ferritin

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

Timing: Prior to initiation

Serum Creatinine and Creatinine Clearance (CrCl)

Rationale: To assess baseline renal function and guide dosing, as deferasirox is associated with renal impairment.

Timing: Prior to initiation (and in duplicate prior to initiation for children)

Liver Function Tests (LFTs: AST, ALT, ALP, Bilirubin)

Rationale: To assess baseline hepatic function and guide dosing, as deferasirox is associated with hepatic impairment.

Timing: Prior to initiation

Urinalysis (proteinuria)

Rationale: To assess for baseline renal tubular dysfunction.

Timing: Prior to initiation

Audiometry

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

Timing: Prior to initiation

Ophthalmological Examination (slit lamp, fundoscopy)

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

Timing: Prior to initiation

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Routine Monitoring

Serum Ferritin

Frequency: Monthly

Target: Goal is to maintain serum ferritin between 500-1000 ng/mL or as clinically indicated to prevent further iron accumulation.

Action Threshold: Dose adjustment if ferritin trends upward or downward significantly; consider discontinuation if ferritin <500 ng/mL.

Serum Creatinine

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

Target: Within normal limits for age.

Action Threshold: If serum 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. Discontinue if persistent or progressive.

Liver Function Tests (LFTs)

Frequency: Every 2 weeks for the first month, then monthly thereafter.

Target: Within normal limits.

Action Threshold: If transaminases (AST/ALT) increase to >5 times the upper limit of normal (ULN) or >3 times ULN with bilirubin >2 times ULN, interrupt therapy. Re-evaluate and restart at lower dose if LFTs normalize.

Urinalysis (proteinuria)

Frequency: Monthly

Target: Negative or trace protein.

Action Threshold: If persistent proteinuria develops, consider dose reduction or interruption.

Audiometry

Frequency: Annually

Target: Stable hearing.

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

Ophthalmological Examination

Frequency: Annually

Target: Stable vision.

Action Threshold: If visual disturbances develop, consider dose reduction or interruption.

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Symptom Monitoring

  • Signs of renal impairment (e.g., decreased urine output, edema)
  • Signs of hepatic impairment (e.g., jaundice, dark urine, fatigue, right upper quadrant pain)
  • Gastrointestinal symptoms (e.g., nausea, vomiting, diarrhea, abdominal pain, GI hemorrhage - black/tarry stools, coffee-ground emesis)
  • Skin rash
  • Hearing changes (e.g., tinnitus, decreased hearing)
  • Vision changes (e.g., blurred vision, decreased acuity)
  • Signs of bone marrow suppression (e.g., fever, sore throat, easy bruising/bleeding, unusual fatigue)

Special Patient Groups

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Pregnancy

Use only if the potential benefit justifies the potential risk to the fetus. Animal studies show adverse effects on development. Limited human data.

Trimester-Specific Risks:

First Trimester: Potential for adverse developmental effects based on animal data.
Second Trimester: Potential for adverse developmental effects based on animal data.
Third Trimester: Potential for adverse developmental effects based on animal data.
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Lactation

Not recommended. It is unknown if 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: Potential for serious adverse reactions (e.g., renal/hepatic toxicity, cytopenias) in the infant.
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Pediatric Use

Approved for transfusional iron overload in patients â‰Ĩ2 years old and for NTDT syndromes in patients â‰Ĩ10 years old. Dosing is weight-based. Close monitoring of renal and hepatic function is crucial, especially in younger children.

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Geriatric Use

Increased risk of adverse reactions, particularly renal, hepatic, and GI hemorrhage. Use with caution and monitor closely. Start at the lower end of the dosing range.

Clinical Information

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Clinical Pearls

  • Deferasirox (Exjade) tablets for oral suspension must be fully dispersed in liquid (water, orange juice, or apple juice) and taken immediately. Do not chew or swallow whole.
  • Jadenu (film-coated tablets) can be swallowed whole or dispersed in liquid, offering more flexibility.
  • Strict adherence to monitoring protocols (renal, hepatic, ferritin, vision, hearing) is critical due to significant potential toxicities.
  • Patients should be educated on signs of serious adverse events, especially GI bleeding, and instructed to seek immediate medical attention.
  • Dose adjustments are frequently needed based on serum ferritin trends and tolerability.
  • Avoid concomitant use with aluminum-containing antacids.
  • Consider vitamin C supplementation only under strict medical supervision due to potential for cardiac toxicity in iron-overloaded patients.
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Alternative Therapies

  • Deferoxamine (parenteral iron chelator)
  • Deferiprone (oral iron chelator, often used in combination or for specific indications)
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Cost & Coverage

Average Cost: Varies widely, typically several thousand dollars per 30 tablets
Generic Available: Yes
Insurance Coverage: Specialty Tier (requires prior authorization, often subject to step therapy)
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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 is a valuable patient fact sheet. 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, we encourage you to discuss them with 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 seeking help, be prepared to provide detailed information about the overdose, including the substance taken, the amount, and the time it occurred.