Tìm theo
Riluzole
Các tên gọi khác (3) :
  • Riluzol
  • Riluzole
  • Riluzolum
Thuốc Gốc
Small Molecule
CAS: 1744-22-5
ATC: N07XX02
ĐG : Inyx Usa Ltd.
CTHH: C8H5F3N2OS
PTK: 234.198
A glutamate antagonist (receptors, glutamate) used as an anticonvulsant (anticonvulsants) and to prolong the survival of patients with amyotrophic lateral sclerosis. Riluzole is marketed as Rilutek by Sanofi.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C8H5F3N2OS
Phân tử khối
234.198
Monoisotopic mass
234.007468097
InChI
InChI=1S/C8H5F3N2OS/c9-8(10,11)14-4-1-2-5-6(3-4)15-7(12)13-5/h1-3H,(H2,12,13)
InChI Key
InChIKey=FTALBRSUTCGOEG-UHFFFAOYSA-N
IUPAC Name
6-(trifluoromethoxy)-1,3-benzothiazol-2-amine
Traditional IUPAC Name
riluzole
SMILES
NC1=NC2=C(S1)C=C(OC(F)(F)F)C=C2
Độ tan chảy
119 °C
Độ hòa tan
3.95e-02 g/l
logP
2.3
logS
-3.8
pKa (strongest acidic)
16.44
pKa (Strongest Basic)
4.57
PSA
48.14 Å2
Refractivity
44.37 m3·mol-1
Polarizability
18.59 Å3
Rotatable Bond Count
2
H Bond Acceptor Count
3
H Bond Donor Count
1
Physiological Charge
0
Number of Rings
2
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Riluzole, a member of the benzothiazole class, is indicated for the treatment of patients with amyotrophic lateral sclerosis (ALS). Riluzole extends survival and/or time to tracheostomy. It is also neuroprotective in various in vivo experimental models of neuronal injury involving excitotoxic mechanisms. The etiology and pathogenesis of amyotrophic lateral sclerosis (ALS) are not known, although a number of hypotheses have been advanced. One hypothesis is that motor neurons, made vulnerable through either genetic predisposition or environmental factors, are injured by glutamate. In some cases of familial ALS the enzyme superoxide dismutase has been found to be defective.
Cơ Chế Tác Dụng : A glutamate antagonist (receptors, glutamate) used as an anticonvulsant (anticonvulsants) and to prolong the survival of patients with amyotrophic lateral sclerosis. Riluzole is marketed as Rilutek by Sanofi. The mode of action of riluzole is unknown. Its pharmacological properties include the following, some of which may be related to its effect: 1) an inhibitory effect on glutamate release (activation of glutamate reuptake), 2) inactivation of voltage-dependent sodium channels, and 3) ability to interfere with intracellular events that follow transmitter binding at excitatory amino acid receptors.
Dược Động Học :
▧ Absorption :
Riluzole is well-absorbed (approximately 90%), with average absolute oral bioavailability of about 60% (CV=30%). A high fat meal decreases absorption, reducing AUC by about 20% and peak blood levels by about 45%.
▧ Protein binding :
96% bound to plasma proteins, mainly to albumin and lipoprotein over the clinical concentration range.
▧ Metabolism :
Riluzole is extensively metabolized to six major and a number of minor metabolites, which have not all been identified to date. Metabolism is mostly hepatic, consisting of cytochrome P450–dependent hydroxylation and glucuronidation. CYP1A2 is the primary isozyme involved in N-hydroxylation; CYP2D6, CYP2C19, CYP3A4, and CYP2E1 are considered unlikely to contribute significantly to riluzole metabolism in humans.
▧ Half Life :
The mean elimination half-life of riluzole is 12 hours (CV=35%) after repeated doses.
Chỉ Định : For the treatment of amyotrophic lateral sclerosis (ALS, Lou Gehrig's Disease)
Liều Lượng & Cách Dùng : Tablet, coated - Oral - 50 mg
Dữ Kiện Thương Mại
Giá thị trường
  • Biệt dược thương mại : Rilutek 50 mg tablet
    Giá bán buôn : USD >18.77
    Đơn vị tính : tablet
Nhà Sản Xuất
  • Công ty : Actavis
    Sản phẩm biệt dược : Fanizan
  • Công ty : Sun Pro
    Sản phẩm biệt dược : Laidec
  • Công ty : Actavis
    Sản phẩm biệt dược : Lizolorol
  • Công ty : ratiopharm
    Sản phẩm biệt dược : Lizorolol
  • Công ty : STADA
    Sản phẩm biệt dược : Rilustad
  • Công ty : Sanofi-Aventis
    Sản phẩm biệt dược : Rilutek
  • Công ty : Actavis
    Sản phẩm biệt dược : Sclefic
  • Công ty : Lunan Pharm
    Sản phẩm biệt dược : Xie Yi Li
  • Công ty : Actavis
    Sản phẩm biệt dược : Zolerilis
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00740
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=5070
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46508094
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C07937
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D00775
ChemSpider
http://www.chemspider.com/Chemical-Structure.4892.html
BindingDB
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=30705
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0075-7700-60
PharmGKB
http://www.pharmgkb.org/drug/PA451251
Wikipedia
http://en.wikipedia.org/wiki/Riluzole
RxList
http://www.rxlist.com/cgi/generic3/riluzole.htm
Drugs.com
http://www.drugs.com/cdi/riluzole.html
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