Deferoxamine mesylate

Description

Deferoxamine is a bacterial siderophore that chelates iron. It is used to experimentally inhibit iron-dependent prolyl hydroxylases (EC₅₀ = 17.8 μM), thus preventing the degradation of isoforms of hypoxia inducible factor during normoxia. Deferoxamine has applications in diseases that are characterized by high levels of circulating iron, such as thalassemia major.

Chemical Properties

DEFEROXAMINE MESYLATE is white or almost white powder.

Uses

chelating agent (Fe & Al)

Uses

DEFEROXAMINE MESYLATE is an iron chelating agent used in therapy for patients with sickle cell diseases and iron overload. Studies suggest that it can exert potential antioxidant neuroprotective effects in stroke patients

brand name

Desferal (Novartis).

reaction suitability

reagent type: chelator

Biochem/physiol Actions

An iron chelator used often in the studies of cell proliferation and apoptosis. Has been shown to have anti-proliferative effects on vascular smooth muscle cells in vitro and in vivo and to arrest cells in the G1 phase. Also reported to induce p53. Induces apoptosis in HL-60 cells by chelating iron. After 48 hrs treatment with 1μM deferoxamine, DNA fragmentation was apparent. Cells treated with 0.1 μM deferoxamine for as little as 24 hours were committed to apoptosis; by 48 hrs nuclear collapse was observed. In some studies it has been shown to have antioxidant properties and to protect cells against H2O2-induced damage.

Clinical Use

Chelating agent:
Acute iron poisoning
Chronic iron or aluminium overload

Veterinary Drugs and Treatments

Deferoxamine is used for the treatment of either acute or chronic iron toxicity. It is being evaluated as an iron chelator for adjunctive treatment of acute cardiac ischemia and as a chelator for aluminum toxicity. Its efficacy in treating reperfusion injuries has been disappointing.

Drug interactions

Potentially hazardous interactions with other drugs
Avoid prochlorperazine, levomepromazine and methotrimeprazine (prolonged unconsciousness).
Do not administer with blood.

Metabolism

When given parenterally desferrioxamine forms chelates with iron and aluminium ions to form ferrioxamine and aluminoxamine, respectively. The chelates are excreted in the urine and faeces via the bile. Desferrioxamine is metabolised, mainly in the plasma. Four metabolites of desferrioxamine were isolated from urine of patients with iron overload. The following biotransformation reactions were found to occur with desferrioxamine: transamination and oxidation yielding an acid metabolite, beta-oxidation also yielding an acid metabolite, decarboxylation and N-hydroxylation yielding neutral metabolites.

storage

Store at -20°C

References

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