What Is Deferoxamine?

This product is a hydroxamic acid complexing agent. The hydroxamic acid group is combined with free or protein-bound trivalent iron (Fe3 +) and aluminum (Al3 +) to form a stable, non-toxic water-soluble iron amine and aluminum amine complex (in acid The binding effect is enhanced under pH conditions) and excreted by urine. This product can remove iron ions in ferritin and hemosiderin, but it does not have a strong effect on removing iron ions in transferrin, and it cannot remove iron ions in hemoglobin, myosin, and cytochromes. This product is mainly used as a rescue drug for acute iron poisoning. Because of its low affinity with other metals, this product is not suitable for detoxification of other metal poisoning. This product is rarely absorbed in the gastrointestinal tract, can be absorbed subcutaneously, intramuscularly or intravenously, and is quickly distributed to various tissues. It is quickly metabolized by enzymes in plasma tissues.

Chinese name: Deferoxamine
Foreign name: desferrioxamine B

Former name: To Tiemin
Preparation: Injection
CAS: 70-51-9

Deferoxamine Basic Information

Chinese name: deferoxamine

Chinese alias: In addition to iron spirit, to iron

English name: desferrioxamine B

English alias: Desferrioxamine; desferrioxamine mesylate; Deferoxamin; Desferal; Deferrioxamine B;

CAS number: 70-51-9

Molecular formula: C25H48N6O8

Molecular weight: 560.68400

Exact mass: 560.35300

PSA: 205.84000

LogP: 2.40420

Deferoxamine physical data

Traits: white-nearly white, crystal-pink
Density: 1.212g / cm3
Refractive index: 1.537 ^[1]

Deferoxamine Ecological Data

The substance has certain hazards to water bodies, preventing leakage into sewers, watercourses or low areas.

Deferoxamine molecular structure data

1. Molar refractive index: 144.51

2. Molar volume (m3 / mol): 462.3

3. Isometric Zhang Rongrong (90.2K): 1264.2

4. Surface tension (dyne / cm): 55.8

5. Polarizability (10-24cm3): 57.28

Deferoxamine Computational Chemical Data

1. Hydrophobic parameter calculation reference value (XlogP): -2.1

2.Number of hydrogen-bonded donors: 6

3.Number of hydrogen bond acceptors: 9

4.Number of rotatable chemical bonds: 23

5.Number of tautomers: 4

6. Topological molecular polar surface area 206

7.Number of heavy atoms: 39

8.Surface charge: 0

9.Complexity: 739

10.Number of isotope atoms: 0

11. Determine the number of atomic stereocenters: 0

12. Uncertain number of atomic stereocenters: 0

13. Determine the number of chemical bond stereocenters: 0

14. Uncertain number of chemical bond stereocenters: 0

15.Number of covalent bond units: 1

Deferoxamine Properties and Stability

Cannot coexist with oxidants

Deferoxamine storage method

Storage method; Keep away from sunlight in a cold "(<-20 = -4) ventilated and dry place. Keep container tightly closed. ^[2]

Deferoxamine Related Information

Deferoxamine pharmacology and toxicology

This product is a chelating agent, which mainly complexes with trivalent iron ions and trivalent aluminum ions to form a complex, and the complex formation constants are 1031 and 1025, respectively. However, it has low affinity for divalent ions such as iron (Fe ++), copper (Cu ++), zinc (Zn ++), and calcium (Ca ++), and its complex formation constant is 1014 or less. Chelation is performed on a 1: 1 gram basis. Therefore, theoretically 1 g of deferoxamine can bind 85 mg of trivalent iron or 41 mg of trivalent aluminum ion (Al +++). Due to its chelating properties, whether it is free or ferritin and hemagglutinin bound iron ions can be complexed with it to form a ferric amine complex. This product can also mobilize and chelate aluminum ions bound to tissues. Formation of an aluminum amine complex. Because the two compounds, ferric amine and aluminum amine, can be excreted from urine and feces, it can reduce the pathological deposition of iron and aluminum in organs. However, this product cannot remove iron ions from transferrin, hemoglobin or other substances containing methemoglobin, so it does not produce iron deficiency anemia.

Deferoxamine pharmacokinetics

This product is a metabolite of Stryptomyces pilosis. It is made by chemically treating some iron-containing amines and removing iron. It has a large number of hydroxamic acid groups, and has a very strong complexation effect on Fe2 +. Its stability constant (k = 1031) is much larger than that on calcium (k = 102), and its complexing force on most other ions Very small. The complexes formed with iron in ferritin, ferritin and transferring have a stability constant greater than 1030; however, this is not the case with hemoglobin, muscle protein, and iron in ferritin, so this product It can make patients with iron accumulation disease discharge iron and produce negative iron balance. Gastrointestinal absorption of oral administration is below 15%. 30 minutes after intramuscular injection of DFO to healthy volunteers at 10 mg / kg body weight, the plasma concentration reached a peak of 5.5 mol / L (8.7 ug / ml). 1 hour after injection, the peak concentration of ferriamine (FO) was 3.7 mol / L (2.3 g / ml). In vitro tests showed that DFO binds to less than 10% of serum proteins. Four DFO metabolites have been isolated and detected from the urine of patients with heavy iron. Studies on healthy volunteers have shown that both DFO and FO are cleared biphasically. In the first phase (fast), the half-life of DFO is 1 hour and the FO is 2.4 hours; in the second phase (slow), the half-life of both is 6 hours. The absorbed product is metabolized by plasma enzymes and quickly excreted from the urine.

Deferoxamine drug interactions

Vitamin C combined with this product can promote iron depletion, because vitamin C can mobilize more iron into complexable iron, but if the complexable iron exceeds the amount that this product can complex, excess complexable iron Will promote lipid peroxidation and cause tissue damage.

Deferoxamine dosage forms and specifications

1. Tablets: 0.1g, 0.5g each. 2. Injection: 0.5g each.

Deferoxamine indications

Diseases caused by acute iron poisoning and chronic iron accumulation.

Deferoxamine contraindications

Those who are allergic to this product and those with renal insufficiency are prohibited. Use with caution in pregnant women (especially within 3 months of pregnancy).

Deferoxamine considerations

1. Prohibited in patients allergic to active substances, excluding patients treated after desensitization. 2. Use with caution in pregnant and lactating women. 3. The solution concentration of this product is greater than 10% can cause kidney damage, vision and hearing impairment, stunting, and acute respiratory distress signs. 4. Use of this product in large doses can worsen neurological dysfunction in patients with aluminum-related brain diseases. 5. There is local pain in the injection, and there may be diarrhea, abdominal discomfort and leg muscle tremor.

Deferoxamine adverse reactions

Oral administration of this product may have symptoms of gastrointestinal irritation, such as nausea and abdominal discomfort. Intramuscular injection can cause local pain, hearing and hearing disorders, lens opacity, redness throughout the body, urticaria, etc. In addition to the above-mentioned reactions given intravenously, occasionally hypotension, palpitations, accelerated breathing, hypoxemia, convulsions, shock, and the like. If the dose is controlled below 15 mg / (kg · h) or 50 mg / (kg · d), adverse reactions rarely occur.

Desferrioxamine dosage

1. Acute poisoning caused by ingestion of a large number of ferrous salts (such as ferrous sulfate and ferric ammonium citrate, etc.): adult dose, 0.5 to 1 g intramuscular injection for the first time, and then every 4 to 12 hours depending on the condition 0.5g was injected. If the patient is in shock, in addition to anti-shock therapy, the same dose can be added to 500ml of 5% or 10% glucose injection, intravenous drip, the drip rate should be controlled below 15mg / (kg The dose does not exceed 5g. 2. Treatment of chronic iron accumulation diseases, such as primary and secondary hemosiderinosis: intramuscular injection, 1.0g for the first time, 0.5g / h afterwards, twice. Thereafter, 0.5 g is given every 4 to 10 hours, and the total amount does not exceed 5 g / d. The method and dose of intravenous drip are the same as 1. Oral: 0.5g, 2 times / d.

Deferoxamine Expert Reviews

Hearing and vision tests should be performed before and during the medication. Oral symptoms of gastrointestinal irritation. Intravenous injection should be slow, otherwise it may cause blood pressure drop or even shock. Intramuscular injection may have local pain and allergies. The combination of deferoxamine and vitamin C should be used with caution. ^[3]