Tìm theo
Nebivolol
Các tên gọi khác (5 ) :
  • 1,1'-[Bis(6-fluoro-3,4-dihydro-2H-1-benzopyran-2-yl)]-2,2'-iminodiethanol
  • 1,1'-Bis(6-fluoro-3,4-dihydro-2H-1-benzopyran-2-yl)-2,2'-iminodiethanol
  • alpha,Alpha'-(iminobismethylene)bis-(6-fluoro-3,4-dihydro-2H-1-benzopyran-2-methanol)
  • alpha,Alpha'-(iminodimethylene)bis-(6-fluoro-2-chromanmethanol)
  • Nebivololum
antihypertensive agents, adrenergic beta 1 receptor antagonists, vasodilator agents
Thuốc Gốc
Small Molecule
CAS: 99200-09-6
ATC: C07AB12
ĐG : Forest Laboratories Inc. , http://www.frx.com
CTHH: C22H25F2NO4
PTK: 405.435
Nebivolol is a highly cardioselective vasodilatory beta1 receptor blocker used in treatment of hypertension. In most countries, this medication is available only by prescription. [Wikipedia]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C22H25F2NO4
Phân tử khối
405.435
Monoisotopic mass
405.175164703
InChI
InChI=1S/C22H25F2NO4/c23-15-3-7-19-13(9-15)1-5-21(28-19)17(26)11-25-12-18(27)22-6-2-14-10-16(24)4-8-20(14)29-22/h3-4,7-10,17-18,21-22,25-27H,1-2,5-6,11-12H2
InChI Key
InChIKey=KOHIRBRYDXPAMZ-UHFFFAOYSA-N
IUPAC Name
1-(6-fluoro-3,4-dihydro-2H-1-benzopyran-2-yl)-2-{[2-(6-fluoro-3,4-dihydro-2H-1-benzopyran-2-yl)-2-hydroxyethyl]amino}ethan-1-ol
Traditional IUPAC Name
nebivolol
SMILES
OC(CNCC(O)C1CCC2=C(O1)C=CC(F)=C2)C1CCC2=C(O1)C=CC(F)=C2
Độ hòa tan
4.03e-02 g/l
logP
3.21
logS
-4
pKa (strongest acidic)
13.52
pKa (Strongest Basic)
8.9
PSA
70.95 Å2
Refractivity
103.32 m3·mol-1
Polarizability
41.98 Å3
Rotatable Bond Count
6
H Bond Acceptor Count
5
H Bond Donor Count
3
Physiological Charge
1
Number of Rings
4
Bioavailability
1
Rule of Five
true
Ghose Filter
true
MDDR-Like Rule
true
Dược Lực Học : Nebivolol is a competitive and highly selective beta-1 receptor antagonist with mild vasodilating properties, possibly due to an interaction with the L-arginine/nitric oxide pathway. In preclinical studies, nebivolol has been shown to induce endothelium-dependent arterial relaxation in a dose dependent manner, by stimulation of the release of endothelial nitric oxide. Nitric oxide acts to relax vascular smooth muscle cells and inhibits platelet aggregation and adhesion.
Cơ Chế Tác Dụng : Nebivolol is a highly cardioselective vasodilatory beta1 receptor blocker used in treatment of hypertension. In most countries, this medication is available only by prescription. [Wikipedia] Nebivolol is a selective β1-receptor antagonist. Activation of β1-receptors by epinephrine increases the heart rate and the blood pressure, and the heart consumes more oxygen. Nebivolol blocks these receptors which reverses the effects of epinephrine, lowering the heart rate and blood pressure. In addition, beta blockers prevent the release of renin, which is a hormone produced by the kidneys which leads to constriction of blood vessels. At high enough concentrations, this drug may also bind beta 2 receptors.
Dược Động Học :
▧ Absorption :
The absorption of nebivolol is rapid and not affected by food.
▧ Protein binding :
98%
▧ Metabolism :
Hepatic (CYP2D6-mediated)
▧ Half Life :
10 hours
Độc Tính : The most common signs and symptoms associated with nebivolol overdosage are bradycardia and hypotension. Other important adverse events reported with nebivolol overdose include cardiac failure, dizziness, hypoglycemia, fatigue and vomiting. Other adverse events associated with β-blocker overdose include bronchospasm and heart block. The largest known ingestion of nebivolol worldwide involved a patient who ingested up to 500 mg of nebivolol along with several 100 mg tablets of acetylsalicylic acid in a suicide attempt. The patient experienced hyperhydrosis, pallor, depressed level of consciousness, hypokinesia, hypotension, sinus bradycardia, hypoglycemia, hypokalemia, respiratory failure and vomiting. The patient recovered.
Chỉ Định : For the treatment of essential hypertension.
Tương Tác Thuốc :
  • Terazosin Increased risk of hypotension. Initiate concomitant therapy cautiously.
  • Treprostinil Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Liều Lượng & Cách Dùng : Tablet - Oral - 10 mg
Tablet - Oral - 2.5 mg
Tablet - Oral - 5 mg
Dữ Kiện Thương Mại
Giá thị trường
  • Biệt dược thương mại : Bystolic 2.5 mg tablet
    Giá bán buôn : USD >2.06
    Đơn vị tính : tablet
  • Biệt dược thương mại : Bystolic 5 mg tablet
    Giá bán buôn : USD >2.06
    Đơn vị tính : tablet
  • Biệt dược thương mại : Bystolic 10 mg tablet
    Giá bán buôn : USD >2.09
    Đơn vị tính : tablet
  • Biệt dược thương mại : Bystolic 20 mg tablet
    Giá bán buôn : USD >2.09
    Đơn vị tính : tablet
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Bystolic
  • Công ty :
    Sản phẩm biệt dược : Lobivon
  • Công ty :
    Sản phẩm biệt dược : Nebicard
  • Công ty :
    Sản phẩm biệt dược : Nebilet
  • Công ty :
    Sản phẩm biệt dược : Nebilong
  • Công ty :
    Sản phẩm biệt dược : Nodon
  • Công ty :
    Sản phẩm biệt dược : Nubeta
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB04861
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=71301
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=99443225
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D05127
ChemSpider
http://www.chemspider.com/Chemical-Structure.64421.html
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/54868-5944-0
PharmGKB
http://www.pharmgkb.org/drug/PA151958426
Wikipedia
http://en.wikipedia.org/wiki/Nebivolol
RxList
http://www.rxlist.com/bystolic-tablets-drug.htm
PDRhealth
http://www.pdrhealth.com/drugs/rx/rx-mono.aspx?contentFileName=bys1940.html&contentName=Bystolic&contentId=732
Drugs.com
http://www.drugs.com/cdi/nebivolol.html
... loading
... loading