Tìm theo
Flucytosine
Các tên gọi khác (10 ) :
  • 5-FC
  • 5-Fluorocystosine
  • 5-Fluorocytosin
  • 5-Fluorocytosine
  • 5-Flurocytosine
  • Ancobon (tn)
  • Flucytosin
  • Flucytosine
  • Fluocytosine
  • Fluorcytosine
antifungal agents, antimetabolites
Thuốc Gốc
Small Molecule
CAS: 2022-85-7
ATC: D01AE21, J02AX01
ĐG : Cardinal Health , http://www.cardinal.com
CTHH: C4H4FN3O
PTK: 129.0925
A fluorinated cytosine analog that is used as an antifungal agent. [PubChem]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C4H4FN3O
Phân tử khối
129.0925
Monoisotopic mass
129.03383997
InChI
InChI=1S/C4H4FN3O/c5-2-1-7-4(9)8-3(2)6/h1H,(H3,6,7,8,9)
InChI Key
InChIKey=XRECTZIEBJDKEO-UHFFFAOYSA-N
IUPAC Name
6-amino-5-fluoro-1,2-dihydropyrimidin-2-one
Traditional IUPAC Name
flucytosine
SMILES
NC1=C(F)C=NC(=O)N1
Độ tan chảy
296 °C
Độ hòa tan
1.5E+004 mg/L (at 25 °C)
logP
-1.1
logS
-1.8
pKa (strongest acidic)
8.16
pKa (Strongest Basic)
1.06
PSA
67.48 Å2
Refractivity
38.22 m3·mol-1
Polarizability
9.97 Å3
Rotatable Bond Count
0
H Bond Acceptor Count
3
H Bond Donor Count
2
Physiological Charge
0
Number of Rings
1
Bioavailability
1
Rule of Five
true
pKa
3.26
Dược Lực Học : Flucytosine is an antimetabolite that acts as an antifungal agent with in vitro and in vivo activity against Candida and Cryptococcus. Flucytosine enters the fungal cell via cytosine permease; thus, flucytosine is metabolized to 5-fluorouracil within fungal organisms. The 5-fluorouracil is extensively incorporated into fungal RNA and inhibits synthesis of both DNA and RNA. The result is unbalanced growth and death of the fungal organism. Antifungal synergism between Ancobon and polyene antibiotics, particularly amphotericin B, has been reported.
Cơ Chế Tác Dụng : A fluorinated cytosine analog that is used as an antifungal agent. [PubChem] Although the exact mode of action is unknown, it has been proposed that flucytosine acts directly on fungal organisms by competitive inhibition of purine and pyrimidine uptake and indirectly by intracellular metabolism to 5-fluorouracil. Flucytosine enters the fungal cell via cytosine permease; thus, flucytosine is metabolized to 5-fluorouracil within fungal organisms. The 5-fluorouracil is extensively incorporated into fungal RNA and inhibits synthesis of both DNA and RNA. The result is unbalanced growth and death of the fungal organism. It also appears to be an inhibitor of fungal thymidylate synthase.
Dược Động Học :
▧ Absorption :
Rapidly and virtually completely absorbed following oral administration. Bioavailability 78% to 89%.
▧ Protein binding :
28-31%
▧ Metabolism :
Flucytosine is deaminated, possibly by gut bacteria or by the fungal targets, to 5-fluorouracil, the active metabolite.
▧ Route of Elimination :
Flucytosine is excreted via the kidneys by means of glomerular filtration without significant tubular reabsorption. A small portion of the dose is excreted in the feces.
▧ Half Life :
2.4 to 4.8 hours.
Độc Tính : Oral, rat: LD50 = >15 gm/kg.
Chỉ Định : For the treatment (in combination with amphotericin B) of serious infections caused by susceptible strains of Candida (septicemia, endocarditis and urinary system infections) and/or Cryptococcus (meningitis and pulmonary infections).
Liều Lượng & Cách Dùng : Capsule - Oral
Solution - Intravenous
Dữ Kiện Thương Mại
Giá thị trường
  • Biệt dược thương mại : Ancobon 250 mg capsule
    Giá bán buôn : USD >23.09
    Đơn vị tính : capsule
  • Biệt dược thương mại : Ancobon 500 mg capsule
    Giá bán buôn : USD >45.54
    Đơn vị tính : capsule
Nhà Sản Xuất
  • Công ty : Valeant
    Sản phẩm biệt dược : Ancobon
  • Công ty : Meda
    Sản phẩm biệt dược : Ancotil
  • Công ty : TTY Biopharm
    Sản phẩm biệt dược : Flusine
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB01099
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=3366
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46504735
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D00323
ChemSpider
http://www.chemspider.com/Chemical-Structure.3249.html
BindingDB
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=50241247
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0187-3554-10
PharmGKB
http://www.pharmgkb.org/drug/PA449654
Wikipedia
http://en.wikipedia.org/wiki/Flucytosine
RxList
http://www.rxlist.com/cgi/generic3/flucytosine.htm
Drugs.com
http://www.drugs.com/cdi/flucytosine.html
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