Tìm theo
Deferiprone
Các tên gọi khác (14 ) :
  • 1,2-Dimethyl-3-hydroxypyrid-4-one
  • 3-Hydroxy-1,2-dimethyl-4(1H)-pyridone
  • APO-066
  • CP-20
  • Deferipron
  • Deferiprona
  • Défériprone
  • Deferiproni
  • Deferipronum
  • Deferypron
  • Dimethylhydroxypyridone
  • DN-180-01-AF
  • Ferriprox
  • PL-1
chelating agents, iron chelating agents
Thuốc Gốc
Small Molecule
CAS: 30652-11-0
ATC: V03AC02
CTHH: C7H9NO2
PTK: 139.1519
Deferiprone is an oral iron chelator used as a second line agent in thalassemia syndromes when iron overload from blood transfusions occurs. Thalassemias are a type of hereditary anaemia due a defect in the production of hemoglobin. As a result, erythropoiesis, the production of new red blood cells, is impaired. FDA approved on October 14, 2011.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C7H9NO2
Phân tử khối
139.1519
Monoisotopic mass
139.063328537
InChI
InChI=1S/C7H9NO2/c1-5-7(10)6(9)3-4-8(5)2/h3-4,10H,1-2H3
InChI Key
InChIKey=TZXKOCQBRNJULO-UHFFFAOYSA-N
IUPAC Name
3-hydroxy-1,2-dimethyl-1,4-dihydropyridin-4-one
Traditional IUPAC Name
deferiprone
SMILES
CN1C=CC(=O)C(O)=C1C
Độ tan chảy
272-278
Độ hòa tan
Maximum water solubility of 16–18 g/L at 24°
logP
0.61
logS
0.29
pKa (strongest acidic)
11.82
pKa (Strongest Basic)
0.52
PSA
40.54 Å2
Refractivity
40.7 m3·mol-1
Polarizability
14.05 Å3
Rotatable Bond Count
0
H Bond Acceptor Count
3
H Bond Donor Count
1
Physiological Charge
0
Number of Rings
1
Bioavailability
1
Rule of Five
true
pKa
3.5
Cơ Chế Tác Dụng : Deferiprone is an oral iron chelator used as a second line agent in thalassemia syndromes when iron overload from blood transfusions occurs. Thalassemias are a type of hereditary anaemia due a defect in the production of hemoglobin. As a result, erythropoiesis, the production of new red blood cells, is impaired. FDA approved on October 14, 2011. Deferiprone is an iron chelator that binds to ferric ions (iron III) and forms a 3:1 (deferiprone:iron) stable complex and is then eliminated in the urine. Deferiprone is more selective for iron in which other metals such as zinc, copper, and aluminum have a lower affinity for deferiprone.
Dược Động Học :
▧ Absorption :
Deferiprone is absorbed in the upper gastrointestinal tract. Absorption is rapid with maximum plasma concentrations occurring after 1 hour in the fasted state and after 2 hours in the fed state.
▧ Volume of Distribution :
In healthy patients, the volume of distribution is 1L/kg, and in thalassemia patients, the volume of distribution is 1.6L/kg.
▧ Protein binding :
Plasma protein binding is less than 10%.
▧ Metabolism :
Deferiprone is mainly metabolized by UGT1A6 to the 3-O-glucuronide metabolite. This metabolite cannot chelate iron.
▧ Route of Elimination :
Within 5-6 hours of administration, more than 90% of deferiprone is eliminated from the plasma. 75 to 90% of deferiprone is excreted in the urine as the metabolite.
▧ Half Life :
The half-life is 1.9 hours.
Độc Tính : Agranulocytosis and neutropenia may occur, which can lead to fatal infections. Hepatoxicity is also possible. Most common side effects that lead to discontinuation of therapy were the gastrointestinal adverse effects (diarrhea, ulcer, nausea, gastrointestinal disturbances)
Chỉ Định : Deferiprone is indicated in thalassemia syndromes when first line chelation agents are not adequate to treat transfusional iron overload.
Tương Tác Thuốc :
  • Aluminum hydroxide Deferiprone may decrease gastrointestinal absorption by chelating to other ions. Interaction is significant so monitor closely.
  • Calcium Deferiprone serum concentrations may be decreased by calcium salts.
  • Iron Deferiprone serum concentrations may be decreased by iron salts except for ferric gluconate, ferumoxytol, iron dextran complex, and iron sucrose.
  • Iron Dextran Deferiprone may decrease gastrointestinal absorption by chelating to other ions. Interaction is significant so monitor closely.
  • Iron sucrose Deferiprone may decrease gastrointestinal absorption by chelating to other ions. Interaction is significant so monitor closely.
  • Magnesium Deferiprone serum concentrations may be decreased by magnesium salts.
  • Sodium bicarbonate Deferiprone may decrease gastrointestinal absorption by chelating to other ions. Interaction is significant so monitor closely.
  • Zinc Deferiprone serum concentrations may be decreased by zinc salts except for zinc chloride.
Liều Lượng & Cách Dùng : Tablet - Oral - 500MG
Dữ Kiện Thương Mại
Nhà Sản Xuất
  • Công ty : APOPHARMA INC
    Sản phẩm biệt dược : Ferriprox
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB08826
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D07416
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/52609-0006-1
Wikipedia
http://en.wikipedia.org/wiki/Deferiprone
RxList
http://www.rxlist.com/ferriprox-drug.htm
Drugs.com
http://www.drugs.com/mtm/deferiprone.html
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