deferoxamine

Action and Spectrum

Actions and Spectrum: 

• deferoxamine is a chelating agent which can form stable complexes with metal ions. In the case of iron overload, excess iron can accumulate in tissues and organs, leading to damage and dysfunction.  
• deferoxamine works by binding to the excess iron in the body to form a stable complex called ferrioxamine, which can then be excreted through urine. By chelating iron, deferoxamine helps reduce the body’s iron burden and prevent iron-related complications such as organ damage and oxidative stress. 
• deferoxamine primarily targets iron overload conditions and is not used for other purposes. It is commonly used in patients with conditions that result in chronic or repeated blood transfusions, such as thalassemia major, sickle cell disease, and certain other anemias. These conditions can lead to excessive iron accumulation in various organs, including the heart, liver, and endocrine glands. 

Drug Interaction

Adverse Reaction

Frequency not defined 

pain 

erythema 

arthralgia 

asthma 

headache 

blood dyscrasia 

thrombocytopenia 

abdominal pain 

fever 

localized irritation 

infiltration 

Black Box Warning

Black box warning: 

None 

Contraindication / Caution

Contraindications/caution: 

• Hypersensitivity: deferoxamine should not be used in individuals who are hypersensitive (allergic) to deferoxamine or any of its components.  
• Renal Impairment: Individuals with severe renal impairment may not be suitable candidates for deferoxamine treatment, as the drug is primarily eliminated through the kidneys. In patients with compromised kidney function, deferoxamine levels could increase and lead to potential toxicity. 
• Ocular and Auditory Toxicity: deferoxamine has been associated with ocular (eye) and auditory (ear) toxicity, mainly when used at high doses or for extended periods. Patients with pre-existing visual or auditory impairments may be at higher risk for these adverse effects. 
• Neurological Disorders: deferoxamine should be cautiously approached in patients with pre-existing neurological disorders, as it has been linked to rare neurological side effects such as encephalopathy and optic neuritis. 

Pregnancy / Lactation

Pregnancy consideration: Insufficient data available 

Lactation: Excretion of the drug in human breast milk is unknown 

Pregnancy category: 

Category A: well-controlled and Satisfactory studies show no risk to the fetus in the first or later trimester. 

Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women. 

Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.    

Category D: adequate data with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.    

Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.    

Category N: There is no data available for the drug under this category 

Pharmacology

Pharmacology: 

deferoxamine acts as an iron-chelating agent, forming stable complexes with iron ions. Its primary mechanism of action involves binding to ferric iron (Fe3+) to form a chelate complex called ferrioxamine. This complex is water-soluble and can be excreted through the urine, effectively removing excess iron from the body. By chelating iron, deferoxamine helps prevent iron-related complications such as tissue damage, oxidative stress, and organ dysfunction. 

Pharmacodynamics:  

The pharmacodynamics of deferoxamine involve its ability to chelate excess ferric iron, form stable ferrioxamine complexes, and facilitate the excretion of these complexes through the urine. By reducing iron overload, deferoxamine helps mitigate the risks associated with iron-related complications. 

Pharmacokinetics: 

Absorption 

deferoxamine is not well-absorbed when taken orally due to its large size and polarity. As a result, it is primarily administered parenterally, either subcutaneously (under the skin) or intramuscularly (into muscle tissue) and intravenously (directly into a vein). Parenteral administration ensures direct delivery into the bloodstream, bypassing the need for absorption through the digestive tract. 

Distribution 

Once in the bloodstream, deferoxamine is distributed throughout the extracellular fluid compartment. It does not readily cross cell membranes, so its primary action is within the extracellular space. The drug does not have significant binding to plasma proteins. 

Metabolism 

deferoxamine is known to be metabolized by plasma enzymes to some extent. The specific enzymes involved and the resulting metabolites have yet to be extensively characterized. 

Elimination and Excretion 

deferoxamine is primarily excreted unchanged in the urine. The formation of ferrioxamine complexes (formed when deferoxamine binds to iron) allows these complexes to be filtered by the kidneys and excreted in the urine. Some portion of deferoxamine is also excreted in the feces. 

Adminstartion

Administration: 

• Subcutaneous (SC) Administration: deferoxamine is often administered subcutaneously, injected just under the skin. This route is convenient and can be performed by the patient or a caregiver after proper training. The injection is usually given in areas with a good amount of subcutaneous tissue, such as the upper arms, thighs, or abdomen. Rotating injection sites helps prevent local irritation. 
• Intramuscular (IM) Administration: Intramuscular administration involves injecting deferoxamine into a muscle. This route is less commonly used compared to subcutaneous and intravenous administration. It might be used in cases where subcutaneous administration is not feasible or tolerated. 
• Intravenous (IV) Administration: Intravenous administration involves injecting deferoxamine into a vein. Healthcare professionals typically administer IV in clinical settings, such as hospitals or infusion centers. It allows for rapid delivery of the medication into the bloodstream. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: deferoxamine 

Why do we use deferoxamine? 

deferoxamine is primarily used to treat conditions characterized by iron overload in the body. It works as a chelating agent to bind excess iron and facilitate its excretion from the body. Here are the primary uses of deferoxamine: 

• Iron Overload Conditions: deferoxamine is most used to treat iron overload conditions, particularly those resulting from chronic blood transfusions. It is used in conditions such as: 

Thalassemia: Thalassemia patients require frequent blood transfusions, which can lead to iron overload. 

Sickle Cell Disease: Individuals with sickle cell disease who receive regular blood transfusions can also develop iron overload. 

Other Anemias: Conditions associated with frequent transfusions or increased iron absorption can lead to iron accumulation. 

• Iron Poisoning: deferoxamine can be used in cases of acute iron poisoning, where a person has ingested a significant amount of iron-containing substances. The drug helps chelate the ingested iron, preventing its absorption and reducing toxicity. 
• Aluminum Chelation: While not primarily used, deferoxamine has also been investigated for its potential to chelate aluminum. It can help reduce the aluminum burden in patients with aluminum toxicity, such as those with chronic kidney disease who may accumulate aluminum from medications or dialysis solutions.