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Teriflunomide
Các tên gọi khác (8 ) :
  • (Z)-2-Cyano-alpha,alpha,alpha-trifluoro-3-hydroxy-P-crotonotoluidide
  • a 77-1726
  • a 771726
  • Aubagio
  • HMR 1726
  • HMR1726
  • Teriflunomida
  • Teriflunomidum
Thuốc Gốc
Small Molecule
CAS: 163451-81-8
Teriflunomide is the active metabolite of leflunomide, and it acts as an immunomodulatory agent by inhibiting pyrimidine synthesis. It is marketed under the name Aubagio® and is indicated for the treatment of multiple sclerosis, specifically relapsing forms. The FDA label states an important warning about the risk of hepatoxicity and teratogenicity for patients using teriflunomide.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Độ hòa tan
Soluble in DMSO (practically insoluble in water).
Dược Lực Học : Teriflunomide is an immunomodulatory agent that decreases the amount of activated CNS lymphocytes, which results in anti-inflammatory and antiproliferative effects.
Cơ Chế Tác Dụng : Teriflunomide is the active metabolite of leflunomide, and it acts as an immunomodulatory agent by inhibiting pyrimidine synthesis. It is marketed under the name Aubagio® and is indicated for the treatment of multiple sclerosis, specifically relapsing forms. The FDA label states an important warning about the risk of hepatoxicity and teratogenicity for patients using teriflunomide. The exact mechanism by which teriflunomide acts in MS is not known. What is known is that teriflunomide prevents pyrimidine synthesis by inhibiting the mitochondrial enzyme dihydroorotate dehydrogenase, and this may be involved in its immunomodulatory effect in MS.
Dược Động Học :
▧ Absorption :
After oral administration of teriflunomide, maximum plasma concentrations are reached, on average, in 1-4 hours.
▧ Volume of Distribution :
After a single intravenous dose, the volume of distribution is 11 L.
▧ Protein binding :
Teriflunomide is extensively plasma protein bound(>99%).
▧ Metabolism :
Teriflunomide mainly undergoes hydrolyis to minor metabolites. Other minor metabolic pathways include oxidation, N-acetylation and sulfate conjugation. Teriflunomide is not metabolized by CYP450 or flavin monoamine oxidase.
▧ Route of Elimination :
Teriflunomide is eliminated unchanged and mainly through bile. Specifically 37.5% is eliminated in the feces and 22.6% in urine.
▧ Half Life :
The median half-life is 18 to 19 days.
▧ Clearance :
After a single IV dose, teriflunomide has a total body clearance of 30.5 mL/h.
Độc Tính : Teriflunomide is contraindicated in pregnant women or women of childbearing age due to the risk of teratogenicity. Teriflunomide is also contraindicated in severe hepatic impairment due to reports of hepatotoxicity, hepatic failure, and death.
Chỉ Định : Used in the treatment of relapsing forms of multiple sclerosis (MS).
Tương Tác Thuốc :
  • Leflunomide Avoid combination due to increased adverse effects of teriflunomide.
  • Natalizumab Avoid combination due to the increased risk of infection.
  • Pimecrolimus Avoid combination due to the increased toxic effects of immunosuppressants.
  • Tacrolimus Avoid combination due to the increased toxic effects of immunosuppressants.
Liều Lượng & Cách Dùng : Tablet - Oral - 14MG
Tablet - Oral - 7MG
Dữ Kiện Thương Mại
Nhà Sản Xuất
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB08880
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D10172
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/58468-0210-1
Wikipedia
http://en.wikipedia.org/wiki/Teriflunomide
RxList
http://www.rxlist.com/aubagio-drug.htm
Drugs.com
http://www.drugs.com/mtm/teriflunomide.html
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