Tìm theo
Dalfampridine
Các tên gọi khác (15 ) :
  • 4-Aminopyridine
  • 4-AP
  • 4-Pyridinamine
  • 4-Pyridylamine
  • Ampyra
  • Avitrol
  • Dalfampridine
  • EL-970
  • Fampridina
  • Fampridine
  • Fampridine-SR
  • Fampridinum
  • gamma-Aminopyridine
  • N07XX07
  • P-Aminopyridine
potassium channel blockers
Thuốc Gốc
Small Molecule
CAS: 504-24-5
ATC: N07XX07
CTHH: C5H6N2
PTK: 94.1145
Dalfampridine is a potassium channel blocker used to help multiple sclerosis patients walk. This is the first drug that was specifically approved to help with mobility in these patients. FDA approved on January 22, 2010.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C5H6N2
Phân tử khối
94.1145
Monoisotopic mass
94.053098202
InChI
InChI=1S/C5H6N2/c6-5-1-3-7-4-2-5/h1-4H,(H2,6,7)
InChI Key
InChIKey=NUKYPUAOHBNCPY-UHFFFAOYSA-N
IUPAC Name
pyridin-4-amine
Traditional IUPAC Name
4 aminopyridine
SMILES
NC1=CC=NC=C1
Độ tan chảy
157-161°C
Độ sôi
273°C
Độ hòa tan
74 g/L
logP
-0.073
logS
0.46
pKa (Strongest Basic)
8.95
PSA
38.91 Å2
Refractivity
28.6 m3·mol-1
Polarizability
9.62 Å3
Rotatable Bond Count
0
H Bond Acceptor Count
2
H Bond Donor Count
1
Physiological Charge
1
Number of Rings
1
Bioavailability
1
Rule of Five
true
pKa
11
Dược Lực Học : Dalfampridine is a board-spectrum lipophillic potassium channel blocker and binds favourably to the open state than closed state of the potassium channel in the CNS. Its pharmacological target are the potassium channels exposed in MS patients. Does not prolong the QTc interval.
Cơ Chế Tác Dụng : Dalfampridine is a potassium channel blocker used to help multiple sclerosis patients walk. This is the first drug that was specifically approved to help with mobility in these patients. FDA approved on January 22, 2010. In MS, axons are progressively demyelinated which exposes potassium channels. As a result, there is a leak of potassium ions which results in the repolarization of cells and a decrease in neuronal excitability. The overall impact is the impairment of neuromuscular transmission as it is harder to trigger an action potential. Dalfampridine inhibits voltage-gated potassium channels in the CNS to maintain the transmembrane potential and prolong action potential. In other words, dalfampridine works to make sure that the current available is high enough to stimulate conduction in demyelinated axons that are exposed in MS patients. Furthermore, it facilitates neuromuscular and synaptic transmission by relieving conduction blocks in demyelinated axons.
Dược Động Học :
▧ Absorption :
Orally-administered dalfampridine is rapidly and completely absorbed from the gastrointestinal tract. Tmax, immediate release form = 1 hour; Tmax, extended release form = 3.5 hours; Cmax, 10 mg extended release = 17.3 - 21.6 ng/mL; Relative bioavailability of 10 mg extended-release tablets compared to aqueous oral solution = 96%
▧ Volume of Distribution :
10 mg extended release = 2.6 L/kg
▧ Protein binding :
10 mg extended release = 1-3% protein bound
▧ Metabolism :
Not extensively metabolized by the liver therefore drugs effecting the cytochrome P450 enzyme system that are concomitantly administered with dalfampridine are not expected to interact with each other. Metabolites include 3-hydroxy-4-aminopyridine and 3-hydroxy-4-aminopyridine sulfate and both are inactive. CYP2E1 is the enzyme responsible for 3-hydroxylation of dalfampridine.
▧ Route of Elimination :
Almost all of the dose and its metabolites are completely eliminated by the kidneys after 24 hours. Urine (96%; 90% of total dose as unchanged drug); Feces (0.5%)
▧ Half Life :
Immediate release form = 3.5 hours; Extended release form = 5.47 hours;
Độc Tính : LD50, oral, mouse = 19 mg/kg LD50, oral, rat = 21 mg/kg
Chỉ Định : Dalfampridine is a neurofunctional modifier that helps improve walking speed in patients with multiple sclerosis (MS).
Liều Lượng & Cách Dùng : Tablet, extended release - Oral - 10 mg
Dữ Kiện Thương Mại
Nhà Sản Xuất
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB06637
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C13728
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D04127
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/10144-427-60
Wikipedia
http://en.wikipedia.org/wiki/4-Aminopyridine
RxList
http://www.rxlist.com/ampyra-drug.htm
Drugs.com
http://www.drugs.com/ampyra.html
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