Tìm theo
Perampanel
Các tên gọi khác (6 ) :
  • 3-(2-Cyanophenyl)-5-(2-pyridyl)-1-phenyl-1,2-dihydropyridin-2-one
  • e 2007
  • e2007
  • ER-155055-90
  • Fycompa
  • Perampanelum
Thuốc Gốc
Small Molecule
CAS: 380917-97-5
ATC: N03AX22
Perampanel is a noncompetitive AMPA glutamate receptor antagonist. It is marketed under the name Fycompa™ and is indicated as an adjunct in patients over 12 years old for the treatment of partial-onset seizures that may or may not occur with generalized seizures. The FDA label includes an important black-boxed warning of serious or life-threatening behavioral and psychiatric reactions in patients taking Fycompa™.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Độ hòa tan
Practically insoluble in water.
Dược Lực Học : Perampanel is involved in inhibiting neuronal excitation in the central nervous system leading to such effects as decreased pyschomotor performance.
Cơ Chế Tác Dụng : Perampanel is a noncompetitive AMPA glutamate receptor antagonist. It is marketed under the name Fycompa™ and is indicated as an adjunct in patients over 12 years old for the treatment of partial-onset seizures that may or may not occur with generalized seizures. The FDA label includes an important black-boxed warning of serious or life-threatening behavioral and psychiatric reactions in patients taking Fycompa™. The exact mechanism of action of perampanel in seizures is not yet determined, but it is known that perampanel decreases neuronal excitation by non-competitive ihibition of the AMPA receptor.
Dược Động Học :
▧ Absorption :
After oral adminitration, perampanel is absorbed rapidly and completely.
▧ Volume of Distribution :
The volume of distribution of perampanel was not quantified.
▧ Protein binding :
Perampanel is 95-96% plasma protein bound with most binding to the plasma proteins α1-acid glycoprotein and albumin.
▧ Metabolism :
Perampanel is highly metabolized by CYP3A4 and/or CYP3A5 primary oxidation and by sequential glucuronidation.
▧ Route of Elimination :
Perampanel is eliminated mostely in the feces (48%) and to a lesser exten in the urine (22%).
▧ Half Life :
Perampanel has a long elmination half-life of about 105 hours.
▧ Clearance :
In healthy patients, perampanel has a clearance of about 12 mL/min.
Độc Tính : The FDA label includes an important warning of serious or life-threatening behavioral and psychiatric adverse reactions including aggression, hostility, irritability, anger, and homicidal thoughts in patients taking perampanel.
Chỉ Định : Used in patients over 12 years old for the treatment of partial-onset seizures that may or may not occur with generalized seizures.
Tương Tác Thuốc :
  • Axitinib Avoid combination with axitinib or other major CYP3A4 drug susbtrates due to the potential decrease in the drug's concentration by perampanel induction of CYP3A4.
  • Azelastine Avoid combination with azelastine or other CNS depressants due to the combined increase of CNS depression.
  • Dihydrocodeine Enhanced CNS depressant effects. Consider therapy modification, and avoid performing complex and high risk activities like driving until side effects are known.
  • Ethanol Avoid combination due to the enhanced central nervous system depression, and likely worse behavioral and psychiatric adverse reactions.
  • Etravirine Perampanel, when used concomitantly with etravirine (a strong CYP3A4 inducer), may experience a decrease in serum concentration. It is recommended to avoid concurrent therapy.
  • Phenytoin Avoid combination with phenytoin or other strong CYP3A4 inducers due to the likely decrease of perampanel concentration. If the combination must be used, an increase in perampanel dose is necessary.
  • St. John's Wort Avoid combination due to the potential decrease in perampanel concentration.
Liều Lượng & Cách Dùng : Tablet - Oral - 10 mg
Tablet - Oral - 12 mg
Tablet - Oral - 2 mg
Tablet - Oral - 4 mg
Tablet - Oral - 6 mg
Tablet - Oral - 8 mg
Dữ Kiện Thương Mại
Nhà Sản Xuất
  • Công ty : EISAI INC
    Sản phẩm biệt dược : FYCOMPA
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB08883
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D08964
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/62856-282-30
Wikipedia
http://en.wikipedia.org/wiki/Perampanel
RxList
http://www.rxlist.com/fycompa-drug.htm
Drugs.com
http://www.drugs.com/mtm/perampanel.html
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