Tìm theo
Betahistine
Các tên gọi khác (7 ) :
  • [2-(2-Pyridyl)ethyl]methylamine
  • 2-(beta-Methylaminoethyl)pyridine
  • 2-[2-(Methylamino)ethyl]pyridine
  • Betahistina
  • Betahistinum
  • N-Methyl-2-(2-pyridinyl)ethanamine
  • N-Methyl-2-pyridineethanamine
Thuốc điều trị về tâm thần
Thuốc Gốc
Small Molecule
CAS: 5638-76-6
ATC: N07CA01
CTHH: C8H12N2
PTK: 136.1943
Betahistine is an antivertigo drug first used for treating vertigo assosicated with Ménière's disease. It is also commonly used for patients with balance disorders.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C8H12N2
Phân tử khối
136.1943
Monoisotopic mass
136.100048394
InChI
InChI=1S/C8H12N2/c1-9-7-5-8-4-2-3-6-10-8/h2-4,6,9H,5,7H2,1H3
InChI Key
InChIKey=UUQMNUMQCIQDMZ-UHFFFAOYSA-N
IUPAC Name
methyl[2-(pyridin-2-yl)ethyl]amine
Traditional IUPAC Name
betahistine
SMILES
CNCCC1=CC=CC=N1
Độ hòa tan
4.93e+01 g/l
logP
0.68
logS
-0.44
pKa (Strongest Basic)
9.77
PSA
24.92 Å2
Refractivity
41.33 m3·mol-1
Polarizability
15.85 Å3
Rotatable Bond Count
3
H Bond Acceptor Count
2
H Bond Donor Count
1
Physiological Charge
1
Number of Rings
1
Bioavailability
1
Rule of Five
true
pKa
10.1 (at 10 °C)
Dược Lực Học : Betahistine primarily acts as a histamine H1-agonist with 0.07 times the activity of histamine. Stimulating the H1-receptors in the inner ear causes a vasodilatory effect and increased permeability in the blood vessels which results in reduced endolymphatic pressure. Betahistine is believed to act by reducing the asymmetrical functioning of sensory vestibular organs as well as by increasing vestibulocochlear blood flow. Doing so aids in decreasing symptoms of vertigo and balance disorders. Betahistine also acts as a histamine H3-receptor antagonist which causes an increased output of histamine from histaminergic nerve endings which can further increase the direct H1-agonist activity. Furthermore, H3-receptor antagonism increases the levels of neurotransmitters such as serotonin in the brainstem, which inhibits the activity of vestibular nuclei, helping to restore proper balance and decrease in vertigo symptoms.
Dược Động Học :
▧ Absorption :
When given orally, betahistine is rapidly absorbed from the gastrointestinal tract.
▧ Protein binding :
Very low.
▧ Metabolism :
Betahistine is metabolized primarily into 2-pyridylacetic acid and is subsequently excreted in the urine.
▧ Route of Elimination :
Renal
▧ Half Life :
3-4 hours
Độc Tính : Symptoms of overdose (< 640 mg) include mild to moderate nausea, dry mouth, dyspepsia, abdominal pain and somnolence. More serious complications such as convulsions, pulmonary or cardiac complications, may occur with higher intentional overdoses (> 640 mg).
Chỉ Định : For the reduction of episodes of vertigo association with Ménière's disease.
Liều Lượng & Cách Dùng : Tablet - Oral - 8mg, 16mg, 24mg
Dữ Kiện Thương Mại
Nhà Sản Xuất
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB06698
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=2366
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=99443252
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D07522
ChemSpider
http://www.chemspider.com/Chemical-Structure.2276.html
PharmGKB
http://www.pharmgkb.org/drug/PA165958372
Wikipedia
http://en.wikipedia.org/wiki/Betahistine
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