Tìm theo
Hydroxyurea
Các tên gọi khác (14 ) :
  • Carbamohydroxamic Acid
  • Carbamohydroximic Acid
  • Carbamoyl Oxime
  • Carbamyl Hydroxamate
  • Hidroxicarbamida
  • Hydrea
  • Hydroxycarbamid
  • Hydroxycarbamide
  • Hydroxycarbamidum
  • Hydroxyharnstoff
  • Hydroxyurea
  • N-Carbamoylhydroxylamine
  • N-Hydroxyurea
  • Oxyurea
Thuốc chống ung thư và tác động vào hệ thống miễn dịch
Thuốc Gốc
Small Molecule
CAS: 127-07-1
ATC: L01XX05
ĐG : Amerisource Health Services Corp. , http://www.amerisourcebergen.com
CTHH: CH4N2O2
PTK: 76.0547
An antineoplastic agent that inhibits DNA synthesis through the inhibition of ribonucleoside diphosphate reductase. [PubChem]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
CH4N2O2
Phân tử khối
76.0547
Monoisotopic mass
76.027277382
InChI
InChI=1S/CH4N2O2/c2-1(4)3-5/h5H,(H3,2,3,4)
InChI Key
InChIKey=VSNHCAURESNICA-UHFFFAOYSA-N
IUPAC Name
hydroxyurea
Traditional IUPAC Name
hydroxyurea
SMILES
NC(=O)NO
Độ tan chảy
133-136
Độ hòa tan
1E+006 mg/L (at 25 °C)
logP
-1.80
logS
1.12
pKa (strongest acidic)
10.14
pKa (Strongest Basic)
-4.9
PSA
75.35 Å2
Refractivity
14.91 m3·mol-1
Polarizability
5.94 Å3
Rotatable Bond Count
0
H Bond Acceptor Count
2
H Bond Donor Count
3
Physiological Charge
0
Number of Rings
0
Bioavailability
1
Rule of Five
true
Dược Lực Học : Hydroxyurea has dose-dependent synergistic activity with cisplatin in vitro. In vivo Hydroxyurea showed activity in combination with cisplatin against the LX-1 and CALU-6 human lung xenografts, but minimal activity was seen with the NCI-H460 or NCI-H520 xenografts. Hydroxyurea was synergistic with cisplatin in the Lewis lung murine xenograft. Sequential exposure to Hydroxyurea 4 hours before cisplatin produced the greatest interaction.
Cơ Chế Tác Dụng : An antineoplastic agent that inhibits DNA synthesis through the inhibition of ribonucleoside diphosphate reductase. [PubChem] Hydroxyurea is converted to a free radical nitroxide (NO) in vivo, and transported by diffusion into cells where it quenches the tyrosyl free radical at the active site of the M2 protein subunit of ribonucleotide reductase, inactivating the enzyme. The entire replicase complex, including ribonucleotide reductase, is inactivated and DNA synthesis is selectively inhibited, producing cell death in S phase and synchronization of the fraction of cells that survive. Repair of DNA damaged by chemicals or irradiation is also inhibited by hydroxyurea, offering potential synergy between hydroxyurea and radiation or alkylating agents. Hydroxyurea also increases the level of fetal hemoglobin, leading to a reduction in the incidence of vasoocclusive crises in sickle cell anemia. Levels of fetal hemoglobin increase in response to activation of soluble guanylyl cyclase (sGC) by hydroxyurea-derived NO.
Dược Động Học :
▧ Absorption :
Well absorbed from the gastrointestinal tract.
▧ Metabolism :
Hepatic.
▧ Route of Elimination :
Renal excretion is a pathway of elimination.
▧ Half Life :
3-4 hours
Độc Tính : Oral, mouse: LD50 = 7330 mg/kg; Oral, rat: LD50 = 5760 mg/kg Teratogenicity: Teratogenic effects have occurred in experimental animals.Hydroxyurea use during a small number of human pregnancies has been reported. Adverse effects have not been observed in any of the exposed newborns. Reproductive Effects: Adverse reproductive effects have occurred in experimental animals. Mutagenicity: Mutagenic effects have occurred in experimental animals.Mutagenic effects have occurred in humans.
Chỉ Định : For management of melanoma, resistant chronic myelocytic leukemia, and recurrent, metastatic, or inoperable carcinoma of the ovary and Sickle-cell anemia.
Tương Tác Thuốc :
  • Belimumab Belimumab increases the immunosupressive effect. Interaction is significant so monitor closely.
  • Bendamustine May increase risk of myelosuppression.
  • Trastuzumab Trastuzumab may increase the risk of neutropenia and anemia. Monitor closely for signs and symptoms of adverse events.
Liều Lượng & Cách Dùng : Capsule - Oral
Dữ Kiện Thương Mại
Giá thị trường
  • Biệt dược thương mại : Hydrea 500 mg capsule
    Giá bán buôn : USD >1.49
    Đơn vị tính : capsule
  • Biệt dược thương mại : Hydroxyurea powder
    Giá bán buôn : USD >2.75
    Đơn vị tính : g
  • Biệt dược thương mại : Hydroxyurea 500 mg capsule
    Giá bán buôn : USD >0.9
    Đơn vị tính : capsule
  • Biệt dược thương mại : Droxia 200 mg capsule
    Giá bán buôn : USD >0.91
    Đơn vị tính : capsule
  • Biệt dược thương mại : Droxia 300 mg capsule
    Giá bán buôn : USD >0.94
    Đơn vị tính : capsule
  • Biệt dược thương mại : Droxia 400 mg capsule
    Giá bán buôn : USD >0.97
    Đơn vị tính : capsule
Nhà Sản Xuất
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB01005
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=3657
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46506927
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C07044
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D00341
ChemSpider
http://www.chemspider.com/Chemical-Structure.3530.html
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0555-0882-02
PharmGKB
http://www.pharmgkb.org/drug/PA449942
Wikipedia
http://en.wikipedia.org/wiki/Hydroxyurea
RxList
http://www.rxlist.com/cgi/generic2/hydroxyurea.htm
Drugs.com
http://www.drugs.com/cdi/hydroxyurea.html
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