Tìm theo
gabapentin enacarbil
Các tên gọi khác (7 ) :
  • Gabapentina enacarbilo
  • Gabapentine enacarbil
  • Gabapentinum enacarbilum
  • Horizant
  • XP 13512
  • XP-13512
  • XP13512
Thuốc Gốc
Small Molecule
CAS: 478296-72-9
Gabapentin enacarbil is marketed under the name Horizant®. It is a prodrug of gabapentin, and indicated in adults for the treatment of Restless Legs Syndrome (RLS) and postherpetic neuralgia (PHN).
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Độ tan chảy
Melting onset of about 64°C.
Độ hòa tan
Solubility of 0.5 mg/mL in water
pKa
pKa 5.0
Dược Lực Học : Since gabapentin enacarbil is a prodrug of gabapentin, it's physiological effects are the same as gabapentin. Concerning PHN, gabapentin prevents allodynia and hyperalgesia.
Cơ Chế Tác Dụng : Gabapentin enacarbil is marketed under the name Horizant®. It is a prodrug of gabapentin, and indicated in adults for the treatment of Restless Legs Syndrome (RLS) and postherpetic neuralgia (PHN). Although the exact mechanism of action of gabapentin in RLS and PHN is unknown, it is presumed to involve the descending noradrenergic system, resulting in the activation of spinal alpha2-adrenergic receptors.
Dược Động Học :
▧ Absorption :
Gabapentin enacarbil is absorbed in the intestines by active transport through the proton-linked monocarboxylate transporter, MCT-1.
▧ Volume of Distribution :
The volume of distribution is 76L.
▧ Protein binding :
Gabapentin plasma protein binding is less than 3%.
▧ Metabolism :
Gabapentin enacarbil does not interact with any of the major cytochrome P450 enzymes.
▧ Route of Elimination :
Gabapentin enacarbil is eliminated primarily in the urine (94%) and to a lesser extent in the feces (5%).
▧ Half Life :
The elimination half-life of gabapentin is 5.1 to 6.0 hours.
▧ Clearance :
Renal clearance of gabapentin is 5 to 7 L/hr.
Độc Tính : Most common adverse reactions are headache, dizziness, and somnolence.
Chỉ Định : For the treatment of adult Restless Legs Syndrome (RLS) and postherpetic neuralgia (PHN).
Tương Tác Thuốc :
  • Azelastine Avoid combination due to increased CNS depression.
  • Ethanol Avoid combination due to ethanol induced increased absorption of gabapentin enacarbil and increased CNS depression.
Liều Lượng & Cách Dùng : Tablet, extended release - Oral - 300MG
Tablet, extended release - Oral - 600MG
Dữ Kiện Thương Mại
Nhà Sản Xuất
  • Công ty : GLAXO GRP LTD
    Sản phẩm biệt dược : HORIZANT
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB08872
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D09539
Wikipedia
http://en.wikipedia.org/wiki/Gabapentin_enacarbil
RxList
http://www.rxlist.com/horizant-drug.htm
Drugs.com
http://www.drugs.com/sfx/gabapentin-enacarbil-side-effects.html
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