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Medically reviewed by Fedorchenko Olga Valeryevna, PharmD. Last updated on 28.04.2022
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Desferal 0.5 g Mesylate for Injection, USP is indicated for the treatment of acute iron intoxication and of chronic iron overload due to transfusion-dependent anemias.
Acute Iron Intoxication
Desferal 0.5 g mesylate is an adjunct to, and not a substitute for, standard measures used in treating acute iron intoxication, which may include the following: induction of emesis with syrup of ipecac; gastric lavage; suction and maintenance of a clear airway; control of shock with intravenous fluids, blood, oxygen, and vasopressors; and correction of acidosis.
Chronic Iron Overload
Desferal 0.5 g mesylate can promote iron excretion in patients with secondary iron overload from multiple transfusions (as may occur in the treatment of some chronic anemias, including thalassemia). Long-term therapy with Desferal 0.5 g mesylate slows accumulation of hepatic iron and retards or eliminates progression of hepatic fibrosis.
Iron mobilization with Desferal 0.5 g mesylate is relatively poor in patients under the age of 3 years with relatively little iron overload. The drug should ordinarily not be given to such patients unless significant iron mobilization (e.g., 1 mg or more of iron per day) can be demonstrated.
Desferal 0.5 g mesylate is not indicated for the treatment of primary hemochromatosis, since phlebotomy is the method of choice for removing excess iron in this disorder.
Desferal 0.5 g injection is used to remove excess iron from the body in anemia or thalassemia patients who have many blood transfusions. It is also used with other medicines to treat acute iron poisoning, especially in small children.
Desferal 0.5 g combines with iron in the blood. The combination of iron and Desferal 0.5 g is then removed from the body by the kidneys. If you have too much iron in the body, it can damage various organs and tissues.
Desferal 0.5 g is to be administered only by or under the immediate supervision of your doctor.
Once a medicine has been approved for marketing for a certain use, experience may show that it is also useful for other medical problems. Although this use is not included in product labeling, Desferal 0.5 g is used in certain patients with the following medical condition:
- Aluminum toxicity (too much aluminum in the body).
Dosage Forms
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Solution Reconstituted, Injection, as mesylate [preservative free]:
Desferal 0.5 g: 500 mg (1 ea)
Generic: 500 mg (1 ea); 2 g (1 ea)
Dosing: Adult
Acute iron toxicity: Note: The IV route is preferred and is used when severe toxicity is evidenced by cardiovascular collapse or systemic symptoms (coma, shock, metabolic acidosis, or gastrointestinal bleeding) or potentially severe intoxications (peak serum iron level >500 mcg/dL) (Perrone 2015). The IM route may be used (per the manufacturer) but is not preferred and rarely indicated. The use of Desferal 0.5 g in situations in which the peak serum iron concentration is <500 mcg/dL or when severe toxicity is not evident is a subject of clinical debate (Howland 2015; Perrone 2015).
IM, IV: Initial: 1,000 mg, may be followed by 500 mg every 4 hours for 2 doses; subsequent doses of 500 mg have been administered every 4 to 12 hours based on clinical response (maximum recommended dose: 6,000 mg/day [per manufacturer])
Chronic iron overload:
IM: 500 to 1,000 mg/day (maximum: 1000 mg/day)
IV: 40 to 50 mg/kg/day (maximum: 60 mg/kg/day) over 8 to 12 hours for 5 to 7 days per week
SubQ: 1,000 to 2,000 mg/day or 20 to 40 mg/kg/day over 8 to 24 hours
Off-label dosing: IV, SubQ: 25 to 50 mg/kg over 8 to 10 hours 5 to 7 days per week (Brittenham, 2011)
Diagnosis of aluminum-induced toxicity with CKD (off-label use) (K/DOQI guidelines 2003): IV: Test dose: 5 mg/kg during the last hour of dialysis if baseline serum aluminum concentrations are 60 to 200 mcg/L, or clinical signs/symptoms of toxicity, or aluminum exposure prior to parathyroid surgery. Measure aluminum just prior to Desferal 0.5 g; remeasure 2 days later (test is positive if serum aluminum increases by ≥50 mcg/L). Do not use if unstimulated aluminum serum concentrations are >200 mcg/L to avoid Desferal 0.5 g-induced neurotoxicity.
Treatment of aluminum toxicity with CKD (off-label use) (K/DOQI guideline, 2003): IV:
Administer after diagnostic Desferal 0.5 g test dose. Note: The risk for Desferal 0.5 g-associated neurotoxicity is increased if unstimulated aluminum serum concentrations are >200 mcg/L; do not perform the Desferal 0.5 g-stimulation test and administer intensive dialysis until <200 mcg/L.
If the serum aluminum concentration rises to ≥300 mcg/L two days after the Desferal 0.5 g test dose or there are side effects after the Desferal 0.5 g-stimulation test: 5 mg/kg once a week 5 hours before dialysis for 4 months. Then discontinue Desferal 0.5 g for one month and perform the Desferal 0.5 g-stimulation test again.
If the serum aluminum concentration is <300 mcg/L two days after the Desferal 0.5 g test dose and there are no side effects after the Desferal 0.5 g-stimulation test: 5 mg/kg once a week during the last hour of dialysis for 2 months. The discontinue Desferal 0.5 g for one month and perform the Desferal 0.5 g-stimulation test again.
Dosing: Geriatric
Refer to adult dosing. May initiate at the lower end of the dosing range.
Dosing: Pediatric
Acute iron intoxication: Limited data available: Children and Adolescents: Note: The IV route is used when severe toxicity is evidenced by cardiovascular collapse or systemic symptoms (coma, shock, metabolic acidosis, or gastrointestinal bleeding) or potentially severe intoxications (peak serum iron level >500 mcg/dL) (Perrone 2011). When severe symptoms are not present, then IM may be used.
Continuous IV infusion: Initial: 15 mg/kg/hour and reduce rate as clinically indicated; maximum daily dose: 80 mg/kg/day and not to exceed 6 g/day (Desferal 0.5 g prescribing information [Canada; UK] 2010)
IV: Initial: 20 mg/kg (maximum dose: 1,000 mg) administered no faster than 15 mg/kg/hour followed by 10 mg/kg (maximum dose: 500 mg) over 4-hour intervals for 2 doses; subsequent doses of 10 mg/kg (maximum dose: 500 mg) over 4 to 12 hours may be repeated depending upon the clinical response; maximum dose: 6 g/day; this dosing may also be used IM if symptoms not severe
IM: 90 mg/kg/dose for one dose, then 45 mg/kg/dose every 4 to 12 hours as needed; maximum single dose: Children: 1,000 mg; Adults: 2,000 mg; maximum daily dose: 6 g/day (Desferal 0.5 g prescribing information [Canada; UK] 2010); others have used 50 mg/kg/dose every 6 hours with maximum daily dose: 6 g/day (Chang 2011); may also use intermittent IV dosing
Chronic iron overload:
General dosing: Manufacturer's labeling: Children ≥3 years and Adolescents:
IV:
Children and Growing Adolescents: 20 to 40 mg/kg/day over 8 to 12 hours, 5 to 7 days per week, usual maximum daily dose: 40 mg/kg/day
Adolescents once growth has ceased: 40 to 50 mg/kg/day over 8 to 12 hours, 5 to 7 days per week, usual maximum daily dose: 60 mg/kg/day
SubQ infusion via a portable, controlled infusion device: 20 to 40 mg/kg/day over 8 to 12 hours 3 to 7 days per week; maximum daily dose: 2,000 mg/day. Doses >60 mg/kg/day have not been shown to provide additional benefit (Vlachos 2008).
Sickle cell disease, chronic iron overload: Children and Adolescents: SubQ infusion: 25 mg/kg/day over 8 hours; dose and duration may be increased as needed (NHLBI 2005)
Thalassemia, chronic iron overload: Note: A lower dose may be required if the ferritin levels are low. In general, the therapeutic index should be kept <0.025 at all times. Therapeutic index = mean daily Desferal 0.5 g dose (mg/kg)/ferritin (mcg/L) (Cappellini 2008):
Children and Growing Adolescents: SubQ infusion: 20 to 40 mg/kg/day over 8 to 12 hours, 6 to 7 nights per week, maximum daily dose: 40 mg/kg/day
Adolescents once growth has ceased:
SubQ infusion (preferred): 40 to 60 mg/kg/day over 8 to 12 hours, 6 to 7 nights per week, maximum daily dose: 2,000 mg/day
SubQ bolus: 45 mg/kg/dose, 5 times per week
Aluminum-induced bone disease in chronic renal failure: Limited data available: Children and Adolescents: Note: Intended for predialysis serum aluminum concentration of 60 to 200 mcg/L; do not start chelation therapy if serum aluminum concentration >200 mcg/L; intensive dialysis (6 days per week with a high flux dialysis membrane) should be used until serum aluminum concentration decreases below 200 mcg/L (National Kidney Foundation 2003):
Test (diagnostic) dose: IV: 5 mg/kg as a single dose infused over the last hour of dialysis; measure serum aluminum concentration 2 days later; depending upon the change in serum aluminum concentration, treatment with Desferal 0.5 g may be indicated
Treatment: Monitor serum aluminum levels closely. See National Kidney Foundation guidelines for additional details on treatment algorithms.
Aluminum serum concentration rise to ≥300 mcg/L or adverse effects with test dose: IV: 5 mg/kg once a week 5 hours before dialysis for 4 months
Aluminum serum concentration rise to <300 mcg/L: IV: 5 mg/kg once a week during the last hour of dialysis for 2 months
See also:
What is the most important information I should know about Desferal 0.5 g?
You should not use this medication if you are allergic to Desferal 0.5 g, if you have severe kidney disease, or if you are unable to urinate.
Before using Desferal 0.5 g, tell your doctor if you have kidney disease, heart disease, liver disease, vision or hearing problems, asthma or other breathing disorder, low levels of calcium in your blood (hypocalcemia), or a parathyroid disorder.
Your doctor may tell you to take a vitamin C supplement after you have been using Desferal 0.5 g for 1 month. Follow your doctor's instructions about how much vitamin C to take and when to start taking it. Using too much vitamin C while you are using Desferal 0.5 g can cause heart problems. Do not take vitamin C supplements without your doctor's advice if you have heart failure.
To be sure this medication is not causing harmful effects, your kidney and heart function will need to be tested often. You may also need eye exams. Do not miss any follow up visits to your doctor for blood tests or eye exams.
Long-term use of Desferal 0.5 g can slow a child's growth. Tell your doctor if the child using this medication is not growing or gaining weight properly. A doctor should check the child's growth every 3 months.
This medication may cause blurred vision and may impair your thinking or reactions. Be careful if you drive or do anything that requires you to be alert and able to see clearly.
If you need to have any type of x-ray or CT scan using a dye that is injected into a vein, you may need to temporarily stop using Desferal 0.5 g. Be sure the doctor knows ahead of time that you are using this medication.
Use exactly as prescribed by your doctor. Do not use in larger or smaller amounts or for longer than recommended. Follow the directions on your prescription label.
Desferal 0.5 g is sometimes injected into a vein through an IV. The medicine must be given slowly through an IV infusion, and may be given for several hours in a row.
Desferal 0.5 g is also sometimes injected into a muscle using an infusion pump.
You may be shown how to use Desferal 0.5 g at home. Do not self-inject this medicine if you do not fully understand how to give the injection and properly dispose of used needles, IV tubing, and other equipment used in giving the medicine.
Desferal 0.5 g must be mixed with a liquid (diluent) before injecting it. The mixed solution should be clear with a colorless or slightly yellow appearance.
Do not use the medication if it has changed colors or has any particles in it. Call your doctor for a new prescription.
It is best to use Desferal 0.5 g within 3 hours after mixing it, but you must use it within 24 hours. Throw away the medicine if it has been longer than 24 hours since it was mixed with the liquid.
Your doctor may tell you to take a vitamin C supplement after you have been using Desferal 0.5 g for 1 month. Follow your doctor's instructions about how much vitamin C to take and when to start taking it. Using too much vitamin C while you are using Desferal 0.5 g can cause heart problems.
Do not take vitamin C supplements without your doctor's advice if you have heart failure.
To be sure this medication is not causing harmful effects, your kidney and heart function will need to be tested often. You may also need eye exams. Do not miss any follow up visits to your doctor for blood tests or eye exams.
If a child is using Desferal 0.5 g, a doctor should check the child's growth every 3 months. Do not miss any scheduled visits to your child's doctor.
Each dose of this medication is for one use only. Throw away any mixed medicine that is leftover after giving the injection.
Use a disposable needle only once. Throw away used needles in a puncture-proof container (ask your pharmacist where you can get one and how to dispose of it). Keep this container out of the reach of children and pets.
Store unmixed Desferal 0.5 g at room temperature. You may store mixed medicine at room temperature for up to 24 hours, but do not refrigerate it.
There are specific as well as general uses of a drug or medicine. A medicine can be used to prevent a disease, treat a disease over a period or cure a disease. It can also be used to treat the particular symptom of the disease. The drug use depends on the form the patient takes it. It may be more useful in injection form or sometimes in tablet form. The drug can be used for a single troubling symptom or a life-threatening condition. While some medications can be stopped after few days, some drugs need to be continued for prolonged period to get the benefit from it.Use: Labeled Indications
Acute iron toxicity: Adjunct in the treatment of acute iron intoxication
Chronic iron overload: Treatment of chronic iron overload secondary to multiple transfusions (often due to the presence of thalassemia major or sickle cell disease [Borgna-Pignatti 2015; Marsella 2015])
Off Label Uses
Diagnosis or treatment of aluminum-induced toxicity associated with chronic kidney disease (CKD)
Based on the KDOQI Clinical Practice Guidelines for Bone Metabolism and Disease in Chronic Kidney Disease, Desferal 0.5 g is effective and recommended for the diagnosis or treatment of aluminum-induced toxicity in patients with CKD.
See also:
What other drugs will affect Desferal 0.5 g?
Vitamin C: Patients with iron overload usually become vitamin C deficient, probably because iron oxidizes the vitamin. As an adjuvant to iron chelation therapy, vitamin C in doses up to 200 mg for adults may be given in divided doses, starting after an initial month of regular treatment with Desferal 0.5 g. Vitamin C increases availability of iron for chelation. In general, 50 mg daily suffices for children under 10 years old and 100 mg daily for older children. Larger doses of vitamin C fail to produce any additional increase in excretion of iron complex.
Prochlorperazine: Concurrent treatment with Desferal 0.5 g and prochlorperazine, a phenothiazine derivative, may lead to temporary impairment of consciousness.
Gallium-67: Imaging results may be distorted because of the rapid urinary excretion of Desferal 0.5 g-bound gallium-67. Discontinuation of Desferal 0.5 g 48 hours prior to scintigraphy is advisable.
See also:
What are the possible side effects of Desferal 0.5 g?
Applies to Desferal 0.5 g: injection powder for solution
In addition to its needed effects, some unwanted effects may be caused by Desferal 0.5 g (the active ingredient contained in Desferal 0.5 g). In the event that any of these side effects do occur, they may require medical attention.
If any of the following side effects occur while taking Desferal 0.5 g, check with your doctor or nurse immediately:
More common:
- Bluish fingernails, lips, or skin
- blurred vision or other problems with vision
- convulsions (seizures)
- difficulty with breathing or fast breathing
- fast heartbeat
- hearing problems
- redness or flushing of the skin
- Diarrhea
- difficult urination
- fever
- leg cramps
- nausea
- stomach and muscle cramps
- stomach discomfort
- unusual bleeding or bruising
- vomiting
- Agitation
- coma
- confusion
- cough
- decreased urine output
- depression
- difficulty with swallowing
- dizziness
- headache
- hives
- hostility
- irritability
- itching
- large, hive-like swelling on the face, eyelids, lips, tongue, throat, hands, legs, feet, or sex organs
- lethargy
- muscle twitching
- puffiness or swelling of the eyelids or around the eyes, face, lips, or tongue
- rapid weight gain
- shortness of breath
- skin rash
- stupor
- swelling of the face, ankles, or hands
- tightness in the chest
- unusual tiredness or weakness
- wheezing
Minor Side Effects
Some of the side effects that can occur with Desferal 0.5 g may not need medical attention. As your body adjusts to the medicine during treatment these side effects may go away. Your health care professional may also be able to tell you about ways to reduce or prevent some of these side effects. If any of the following side effects continue, are bothersome or if you have any questions about them, check with your health care professional:
Incidence not known:
- Bleeding, blistering, burning, coldness, discoloration of the skin, feeling of pressure, hives, infection, inflammation, itching, lumps, numbness, pain, rash, redness, scarring, soreness, stinging, swelling, tenderness, tingling, ulceration, or warmth at the injection site
Natural product isolated from Streptomyces pilosus. It forms iron complexes and is used as a chelating agent, particularly in the mesylate form. [PubChem]