Deferasirox 500mg Tablets For Susp
Overview
What is this medicine?
How to Use This Medicine
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.
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.
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
Condition-Specific Dosing:
Pediatric Dosing
Dose Adjustments
Renal Impairment:
Hepatic Impairment:
Pharmacology
Mechanism of Action
Pharmacokinetics
Absorption:
Distribution:
Elimination:
Pharmacodynamics
Safety & Warnings
BLACK BOX WARNING
Side Effects
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.
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
Before Using This Medicine
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.
Precautions & Cautions
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.
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
Contraindicated Interactions
- Aluminum-containing antacids (e.g., aluminum hydroxide)
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)
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)
Minor Interactions
- Cholestyramine (may decrease deferasirox exposure)
Monitoring
Baseline Monitoring
Rationale: To establish baseline iron burden and guide initial dosing.
Timing: Prior to initiation of therapy.
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.
Rationale: To assess hepatic function, as deferasirox can cause hepatic toxicity and dose adjustments are needed for impairment.
Timing: Prior to initiation of therapy.
Rationale: To screen for renal tubular dysfunction.
Timing: Prior to initiation of therapy.
Rationale: To establish baseline hearing, as deferasirox can cause hearing loss.
Timing: Prior to initiation of therapy.
Rationale: To establish baseline vision, as deferasirox can cause ocular disturbances.
Timing: Prior to initiation of therapy.
Routine Monitoring
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.
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.
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.
Frequency: Monthly
Target: Negative or trace protein.
Action Threshold: If persistent or increasing proteinuria, investigate and consider dose adjustment or interruption.
Frequency: Annually
Target: Stable hearing.
Action Threshold: If hearing impairment detected, consider dose reduction or interruption.
Frequency: Annually
Target: Stable vision.
Action Threshold: If visual disturbances (e.g., cataracts, retinal toxicity) detected, consider dose reduction or interruption.
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
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:
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.
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.
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
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.
Alternative Therapies
- Deferoxamine (parenteral iron chelator)
- Deferiprone (oral iron chelator)