Tìm theo
Flutamide
Các tên gọi khác (11 ) :
  • 4'-Nitro-3'-trifluoromethylisobutyranilide
  • alpha,alpha,alpha-Trifluoro-2-methyl-4'-nitro-m-propionotoluidide
  • Eulexin
  • Flutamid
  • Flutamida
  • Flutamide
  • Flutamidum
  • FTA
  • NFBA
  • Niftolid
  • Niftolide
Thuốc chống ung thư và tác động vào hệ thống miễn dịch
Thuốc Gốc
Small Molecule
CAS: 13311-84-7
ATC: L02BB01
ĐG : Barr Pharmaceuticals
CTHH: C11H11F3N2O3
PTK: 276.2118
An antiandrogen with about the same potency as cyproterone in rodent and canine species.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C11H11F3N2O3
Phân tử khối
276.2118
Monoisotopic mass
276.072176843
InChI
InChI=1S/C11H11F3N2O3/c1-6(2)10(17)15-7-3-4-9(16(18)19)8(5-7)11(12,13)14/h3-6H,1-2H3,(H,15,17)
InChI Key
InChIKey=MKXKFYHWDHIYRV-UHFFFAOYSA-N
IUPAC Name
2-methyl-N-[4-nitro-3-(trifluoromethyl)phenyl]propanamide
Traditional IUPAC Name
flutamide
SMILES
CC(C)C(=O)NC1=CC(=C(C=C1)[N+]([O-])=O)C(F)(F)F
Độ tan chảy
111.5-112.5
Độ hòa tan
9.45 mg/L
logP
3.35
logS
-4.7
pKa (strongest acidic)
13.17
pKa (Strongest Basic)
-3.7
PSA
74.92 Å2
Refractivity
63.42 m3·mol-1
Polarizability
23.2 Å3
Rotatable Bond Count
4
H Bond Acceptor Count
3
H Bond Donor Count
1
Physiological Charge
0
Number of Rings
1
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Flutamide is a nonsteroidal antiandrogen. In animal studies, flutamide demonstrates potent antiandrogenic effects. It exerts its antiandrogenic action by inhibiting androgen uptake and/or by inhibiting nuclear binding of androgen in target tissues or both. Prostatic carcinoma is known to be androgen-sensitive and responds to treatment that counteracts the effect of androgen and/or removes the source of androgen, e.g. castration. Elevations of plasma testosterone and estradiol levels have been noted following flutamide administration.
Cơ Chế Tác Dụng : An antiandrogen with about the same potency as cyproterone in rodent and canine species. Flutamide is a nonsteroidal antiandrogen that blocks the action of both endogenous and exogenous testosterone by binding to the androgen receptor. In addition Flutamide is a potent inhibitor of testosterone-stimulated prostatic DNA synthesis. Moreover, it is capable of inhibiting prostatic nuclear uptake of androgen.
Dược Động Học :
▧ Absorption :
Rapidly and completely absorbed.
▧ Protein binding :
94-96%
▧ Metabolism :
Flutamide is rapidly and extensively metabolized, with flutamide comprising only 2.5% of plasma radioactivity 1 hour after administration.
▧ Route of Elimination :
Flutamide and its metabolites are excreted mainly in the urine with only 4.2% of a single dose excreted in the feces over 72 hours.
▧ Half Life :
The plasma half-life for the alpha-hydroxylated metabolite of flutamide (an active metabolite) is approximately 6 hours.
Độc Tính : In animal studies with flutamide alone, signs of overdose included hypoactivity, piloerection, slow respiration, ataxia, and/or lacrimation, anorexia, tranquilization, emesis, and methemoglobinemia.
Chỉ Định : For the management of locally confined Stage B2-C and Stage D2 metastatic carcinoma of the prostate
Tương Tác Thuốc :
  • Telithromycin Telithromycin may reduce clearance of Flutamide. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Flutamide if Telithromycin is initiated, discontinued or dose changed.
  • Thiabendazole The strong CYP1A2 inhibitor, Thiabendazole, may increase the effects and toxicity of Flutamide by decreasing Flutamide metabolism and clearance. Monitor for changes in the therapeutic and adverse effects of Flutamide if Thiabendazole is initiated, discontinued or dose changed.
  • Voriconazole Voriconazole, a strong CYP3A4 inhibitor, may increase the serum concentration of flutamide by decreasing its metabolism. Monitor for changes in the therapeutic and adverse effects of flutamide if voriconazole is initiated, discontinued or dose changed.
Liều Lượng & Cách Dùng : Tablet - Oral
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty : CSC
    Sản phẩm biệt dược : Andraxan
  • Công ty : Medicamerc
    Sản phẩm biệt dược : Antipros
  • Sản phẩm biệt dược : Curestat
  • Công ty : Cipla
    Sản phẩm biệt dược : Cytomid
  • Công ty : Ivax
    Sản phẩm biệt dược : Dedile
  • Công ty : Bayer
    Sản phẩm biệt dược : Drogenil
  • Công ty : Genepharm
    Sản phẩm biệt dược : Elbat
  • Công ty : Nolver
    Sản phẩm biệt dược : Etaconil
  • Công ty : Schering-Plough
    Sản phẩm biệt dược : Euflex
  • Công ty : Schering-Plough
    Sản phẩm biệt dược : Eulexin
  • Công ty : Orion
    Sản phẩm biệt dược : Farostat
  • Công ty : Cryopharma
    Sản phẩm biệt dược : Flimutal
  • Sản phẩm biệt dược : Flucinom
  • Công ty : Teva
    Sản phẩm biệt dược : Flulem
  • Công ty : Nippon Kayaku
    Sản phẩm biệt dược : Odyne
  • Công ty : Sanofi-Aventis
    Sản phẩm biệt dược : Prostadirex
  • Công ty : Pharmachemie
    Sản phẩm biệt dược : Prostanon
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00499
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=3397
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46508874
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C07653
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D00586
ChemSpider
http://www.chemspider.com/Chemical-Structure.3280.html
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0555-0870-01
PharmGKB
http://www.pharmgkb.org/drug/PA449685
Wikipedia
http://en.wikipedia.org/wiki/Flutamide
RxList
http://www.rxlist.com/cgi/generic2/flutam.htm
PDRhealth
http://www.pdrhealth.com/drug_info/rxdrugprofiles/drugs/eul1168.shtml
Drugs.com
http://www.drugs.com/cdi/flutamide.html
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