Tìm theo
Deferoxamine
Các tên gọi khác (10 ) :
  • Deferoxamin
  • Deferoxamina
  • Déferoxamine
  • Deferoxaminum
  • Deferrioxamine
  • Deferrioxamine b
  • Desferrioxamine
  • DFO
  • DFOA
  • DFOM
chelating agents, siderophores
Thuốc Gốc
Small Molecule
CAS: 70-51-9
ATC: V03AC01
ĐG : APP Pharmaceuticals , http://www.apppharma.com
CTHH: C25H48N6O8
PTK: 560.684
Natural product isolated from Streptomyces pilosus. It forms iron complexes and is used as a chelating agent, particularly in the mesylate form. [PubChem]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C25H48N6O8
Phân tử khối
560.684
Monoisotopic mass
560.353362542
InChI
InChI=1S/C25H48N6O8/c1-21(32)29(37)18-9-3-6-16-27-22(33)12-14-25(36)31(39)20-10-4-7-17-28-23(34)11-13-24(35)30(38)19-8-2-5-15-26/h37-39H,2-20,26H2,1H3,(H,27,33)(H,28,34)
InChI Key
InChIKey=UBQYURCVBFRUQT-UHFFFAOYSA-N
IUPAC Name
N-(5-aminopentyl)-N-hydroxy-N'-[5-(N-hydroxy-3-{[5-(N-hydroxyacetamido)pentyl]carbamoyl}propanamido)pentyl]butanediamide
Traditional IUPAC Name
deferoxamine
SMILES
CC(=O)N(O)CCCCCNC(=O)CCC(=O)N(O)CCCCCNC(=O)CCC(=O)N(O)CCCCCN
Độ tan chảy
140 °C
Độ hòa tan
1.2E+004 mg/L (at 20 °C)
logP
-2.2
logS
-3.8
pKa (strongest acidic)
7.92
pKa (Strongest Basic)
10.23
PSA
205.84 Å2
Refractivity
144.95 m3·mol-1
Polarizability
62.41 Å3
Rotatable Bond Count
23
H Bond Acceptor Count
9
H Bond Donor Count
6
Physiological Charge
1
Number of Rings
0
Bioavailability
0
Dược Lực Học : 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.
Cơ Chế Tác Dụng : Natural product isolated from Streptomyces pilosus. It forms iron complexes and is used as a chelating agent, particularly in the mesylate form. [PubChem] 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.
Dược Động Học :
▧ Absorption :
Deferoxamine is rapidly absorbed after intramuscular or subcutaneous administration, but only poorly absorbed from the gastrointestinal tract in the presence of intact mucosa.
▧ 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.
Độc Tính : Intravenous LD50 in mouse, rat, and rabbit is 340 mg/kg, 520 mg/kg, and 600 mg/kg, respectively. Subcutaneous LD50 in mouse and rat is 1600 mg/kg and >1000 mg/kg, respectively. Oral LD50 in mouse and rat is >3000 mg/kg and >1000 mg/kg, respectively. Nephrotoxicity, ototoxicity and retinal toxicity have been reported following long-term administration for chronic iron overload.
Chỉ Định : Used to treat acute iron or aluminum toxicity (an excess of aluminum in the body) in certain patients. Also used in certain patients with anemia who must receive many blood transfusions.
Tương Tác Thuốc :
  • Vitamin C Vitamin C may increase the adverse effects of deferoxamine. Transient deterioration of left ventricular function has been observed during concomitant therapy. Use caution during concomitant therapy.
Liều Lượng & Cách Dùng : Powder, for solution - Intramuscular
Powder, for solution - Intraperitoneal
Powder, for solution - Intravenous
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty : Novartis
    Sản phẩm biệt dược : Desferal
  • Công ty : Novartis
    Sản phẩm biệt dược : Desféral
  • Công ty : Novartis
    Sản phẩm biệt dược : Desferin
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00746
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=2973
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46506395
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C06940
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D03670
ChemSpider
http://www.chemspider.com/Chemical-Structure.2867.html
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0409-2336-10
PharmGKB
http://www.pharmgkb.org/drug/PA164746490
Wikipedia
http://en.wikipedia.org/wiki/Deferoxamine
Drugs.com
http://www.drugs.com/cdi/deferoxamine.html
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