Drug information of Deferoxamine

Deferoxamine

Drug group:

Natural product isolated from Streptomyces pilosus. It forms iron complexes and is used as a chelating agent, particularly in the mesylate form.

Mechanism of effect

Deferoxamine works in treating iron toxicity by binding trivalent (ferric) iron (for which it has a strong affinity), forming ferrioxamine, a stable complex which is eliminated via the kidneys. 100 mg of deferoxamine is capable of binding approximately 8.5 mg of trivalent (ferric) iron. Deferoxamine works in treating aluminum toxicity by binding to tissue-bound aluminum to form aluminoxamine, a stable, water-soluble complex. The formation of aluminoxamine increases blood concentrations of aluminum, resulting in an increased concentration gradient between the blood and dialysate, boosting the removal of aluminum during dialysis. 100 mg of deferoxamine is capable of binding approximately 4.1 mg of aluminum.

Pharmacodynamic

Deferoxamine, otherwise known as desferrioxamine or desferal, is a chelating agent used to remove excess iron or aluminum from the body. It acts by binding free iron or aluminum in the bloodstream and enhancing its elimination in the urine.
By removing excess iron or aluminum, the agent reduces the damage done to various organs and tissues, such as the liver.

Pharmacokinetics

  • Absorption: Deferoxamine is rapidly absorbed after intramuscular or subcutaneous administration, but only poorly absorbed from the gastrointestinal tract in the presence of intact mucosa.
  • Volume of distribution: Not Available
  • Protein binding: Less than 10% bound to serum proteins in vitro.
  • Metabolism: Deferoxamine is mainly metabolised in the plasma and hepatic metabolism is minimal. A number of metabolites have been isolated but not characterised. Some metabolites of deferoxamine, most notably the product of oxidative deamination, also chelate iron, and thus the antidotal effect of the drug appears unaffected by hepatic metabolism.
  • Route of elimination: Deferoxamine mesylate is metabolized principally by plasma enzymes, but the pathways have not yet been defined. Some is also excreted in the feces via the bile.
  • Half life: Biphasic elimination pattern in healthy volunteers with a first rapid phase half life of 1 hour and a second slow phase half-life of 6 hours.

Dosage

Usual Adult Dose for Iron Poisoning - Acute

Initial dose: 1000 mg, IM or IV (maximum IV rate: 15 mg/kg/hour)

Maintenance dose: 500 mg, IM or IV, every 4 hours, for 2 doses; additional 500 mg doses every 4 to 12 hours may be given based on clinical response

Maximum dose: 6000 mg per 24 hour period.

Usual Adult Dose for Iron Poisoning - Chronic

1000 to 2000 mg, subcutaneously over 8 to 24 hours, daily

or

40 to 50 mg/kg/day, IV over 8 to 12 hours (maximum IV rate: 15 mg/kg/hour), 5 to 7 days per week

Maximum IV dose: 60 mg/kg/day

or

500 to 1000 mg, IM,

Maximum IM dose: 1000 mg/day

Usual Pediatric Dose for Iron Poisoning - Acute

3 years and older:

Initial dose: 1000 mg, IM or IV (maximum IV rate: 15 mg/kg/hour)

Maintenance dose: 500 mg, IM or IV, every 4 hours, for 2 doses; additional 500 mg doses every 4 to 12 hours may be given based on clinical response

Maximum dose: 6000 mg per 24 hour period

Usual Pediatric Dose for Iron Poisoning - Chronic

3 years and older:

1000 to 2000 mg, subcutaneously over 8 to 24 hours, daily

or

20 to 40 mg/kg/day, IV over 8 to 12 hours (maximum IV rate: 15 mg/kg/hour), 5 to 7 days per week

Maximum IV dose: 40 mg/kg/day (until growth has ceased)

or

500 to 1000 mg, IM,

Maximum IM dose: 1000 mg/day

Alerts

  • Acute respiratory distress syndrome (ARDS): Deferoxamine has been associated with ARDS following excessively high-dose IV treatment of acute iron intoxication or thalassemia; has been reported in children and adults.
  • Auditory effects: Auditory disturbances (tinnitus and high frequency hearing loss) have been reported following prolonged administration, at high doses, or in patients with low ferritin levels; effects are generally reversible with early detection and immediate discontinuation. Elderly patients are at increased risk for hearing loss. Audiology exams are recommended with long-term treatment.
  • Growth retardation: High deferoxamine doses and concurrent low ferritin levels are also associated with growth retardation. Growth velocity may partially resume to pretreatment rates after deferoxamine dose reduction.
  • Infection: Patients with iron overload are at increased susceptibility to infection with Yersinia enterocolitica and Yersinia pseudotuberculosis; treatment with deferoxamine may enhance this risk; if infection develops, discontinue therapy until resolved.
  • Infusion reactions: Flushing of the skin, hypotension, urticaria, and shock are associated with rapid IV infusion; administer by slow IV infusion, IM, or slow subcutaneous infusion only.
  • Mucormycosis: Rare and serious cases of mucormycosis (including fatalities) have been reported with use; withhold treatment with signs and symptoms of mucormycosis.
  • Ocular effects: Ocular disturbances (blurred vision; cataracts; corneal opacities; decreased visual acuity; impaired peripheral, color, and night vision; optic neuritis; retinal pigment abnormalities; retinopathy; scotoma; visual loss/defect) have been reported following prolonged administration, at high doses, or in patients with low ferritin levels; effects are generally reversible with early detection and immediate discontinuation. Elderly patients are at increased risk for ocular disorders. Periodic ophthalmic exams are recommended with long-term treatment.
  • Renal effects: Increases in serum creatinine, acute renal failure and renal tubular disorders have been reported; monitor for changes in renal function. Deferoxamine is readily dialyzable. When iron is chelated with deferoxamine, the chelate is water-soluble and is excreted renally.
  • Urine discoloration: Patients should be informed that urine may have a pink, reddish, or orange discoloration.
  • Aluminum toxicity: Treatment with deferoxamine in patients with aluminum toxicity may cause hypocalcemia and aggravate hyperparathyroidism. Deferoxamine may cause neurological symptoms (including seizure) in patients with aluminum-related encephalopathy receiving dialysis and may precipitate dialysis dementia onset.
  • Hemochromatosis: Deferoxamine is not indicated for the treatment of primary hemochromatosis (treatment of choice is phlebotomy).

Points of recommendation

To make sure this medicine is safe for you, tell your doctor if you have:

  • If you have an allergy to deferoxamine or any other part of deferoxamine.
  • If you are allergic to any drugs like this one, any other drugs, foods, or other substances. Tell your doctor about the allergy and what signs you had, like rash; hives; itching; shortness of breath; wheezing; cough; swelling of face, lips, tongue, or throat; or any other signs.
  • If you are not able to pass urine.
  • If you have kidney disease.

Avoid driving and doing other tasks or actions that call for you to be alert until you see how deferoxamine affects you.

Have an eye exam as you have been told by your doctor.

Have blood work checked as you have been told by the doctor. Talk with the doctor.

Have a hearing test before starting deferoxamine and while you take deferoxamine.

This medicine may affect certain lab tests. Tell all of your health care providers and lab workers that you take deferoxamine.

If you take vitamin C, talk with your doctor.

Talk with your doctor before taking multivitamins, natural products, and diet aids. These may have vitamin C in them.

Very bad and sometimes deadly fungal infections have rarely happened in patients taking deferoxamine. Tell your doctor right away if you have fever, runny nose, eye changes, cough, or shortness of breath.

This medicine may affect growth in children and teens in some cases. They may need regular growth checks. Talk with the doctor.

If you are 65 or older, use deferoxamine with care. You could have more side effects.

Tell your doctor if you are pregnant or plan on getting pregnant. You will need to talk about the benefits and risks of using deferoxamine while you are pregnant.

Tell your doctor if you are breast-feeding. You will need to talk about any risks to your baby.

Pregnancy level

C

Related drugs

Deferiprone , Deferasirox , Succimer


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