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deferasirox

   Also found in: Wikipedia 0.01 sec.
deferasirox,
a rarely used heavy metal chelating agent.
indication This drug is used to treat chronic iron overload.
contraindications Lactation, severe hepatic or renal disease, and known hypersensitivity to this drug prohibit its use. Its use is also contraindicated in children.

deferasirox

Exjade

Pharmacologic class: Iron-chelating agent

Therapeutic class: Antidote

Pregnancy risk category B

Action

Binds selectively to iron

Availability

Tablets for oral suspension: 125 mg, 250 mg, 500 mg

Indications and dosages

Chronic iron overload caused by blood transfusions

Adults and children ages 2 and older: Initially, 20 mg/kg (calculated to nearest whole tablet) P.O. daily on empty stomach at least 30 minutes before a meal, preferably at same time each day. Don't exceed 30 mg/kg daily.

Dosage adjustment

• Serum creatinine elevation
• Severe, persistent liver enzyme elevations

Contraindications

• Hypersensitivity to drug or its components

Precautions

Use cautiously in:
• serum creatinine elevation, liver enzyme elevation, severe rash
• pregnant or breastfeeding patients.

Administration

Make sure patient doesn't swallow tablets whole.
• Disperse tablets completely in water, orange juice, or apple juice; have patient consume suspension immediately. If residue remains, resuspend it in small amount of liquid and have patient swallow it. Disperse doses lower than 1 g in 3.5 oz liquid; disperse doses higher than 1 g in 7 oz liquid.
• Adjust dosage every 3 to 6 months in increments of 5 to 10 mg/kg based on ferritin levels, treatment goals, and response.

RouteOnsetPeakDuration
P.O.Unknown1.5-4 hrUnknown

Adverse reactions

CNS: headache, fatigue, dizziness

EENT: cataract, retinal disorder, increased intraocular pressure, ear infection, hearing loss, rhinitis, nasopharyngitis, pharyngolaryngeal pain, pharyngitis, acute tonsillitis

GI: nausea, vomiting, diarrhea, abdominal pain

Musculoskeletal: arthralgia, back pain

Respiratory: cough, respiratory tract infection, bronchitis

Skin: rash, urticaria

Other: fever, influenza

Interactions

Drug-drug. Aluminum-containing antacids: possible binding with antacid

Drug-diagnostic tests. Liver function tests, serum creatinine: increased

Drug-food. Any food: increased deferasirox bioavailability

Patient monitoring

• Perform baseline auditory and ophthalmic testing; repeat every 12 months.
• Monitor serum ferritin levels monthly.
• Monitor renal and hepatic function frequently.

Patient teaching

• Instruct patient to place tablets in water, orange juice, or apple juice and stir until completely dissolved. Tell him not to chew or swallow them.
• Advise patient not to take aluminum-containing antacids during therapy.
• Tell patient drug may cause vision and hearing disturbances, necessitating routine ophthalmic and auditory testing.
• Caution patient to avoid driving and other hazardous activities until drug effects are known.
• As appropriate, review all other significant adverse reactions and interactions, especially those related to the drugs, tests, and foods mentioned above.



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The team used two FDA-approved iron chelators, deferoxamine and deferasirox, that can remove excess iron from the system by binding to the metal in a process called chelation.
One of the latest drugs available for this treatment in tablet form is deferasirox, but on cost grounds this is only being made available to around 35 of the 600 patients receiving iron chelation therapy.
The MDS panel strongly recommends the consideration of deferasirox as an iron chelating agent for patients who have received greater than 20-30 red blood cell transfusions.
 
 
 
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