Tìm theo
Levobunolol
Các tên gọi khác (4 ) :
  • (-)-Bunolol
  • (S)-5-(3-((1,1-Dimethylethyl)amino)-2-hydroxypropoxy)-3,4-dihydro-1(2H)-naphthalenone
  • Levobunolol
  • Levobunololum
Thuốc dùng điều trị mắt, tai mũi họng
Thuốc Gốc
Small Molecule
CAS: 47141-42-4
ATC: S01ED03
ĐG : Alcon Laboratories , http://www.alcon.com
CTHH: C17H25NO3
PTK: 291.3853
A nonselective beta-adrenoceptor antagonist used in the treatment of glaucoma. [PubChem]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
Phân tử khối
291.3853
Monoisotopic mass
291.183443671
InChI
InChI=1S/C17H25NO3/c1-17(2,3)18-10-12(19)11-21-16-9-5-6-13-14(16)7-4-8-15(13)20/h5-6,9,12,18-19H,4,7-8,10-11H2,1-3H3/t12-/m0/s1
InChI Key
InChIKey=IXHBTMCLRNMKHZ-LBPRGKRZSA-N
IUPAC Name
5-[(2S)-3-(tert-butylamino)-2-hydroxypropoxy]-1,2,3,4-tetrahydronaphthalen-1-one
Traditional IUPAC Name
levobunolol
SMILES
CC(C)(C)NC[C@H](O)COC1=CC=CC2=C1CCCC2=O
Độ tan chảy
209-211 °C
Độ hòa tan
2.51e-01 g/l
logP
2.40
logS
-3.1
pKa (strongest acidic)
14.09
pKa (Strongest Basic)
9.66
PSA
58.56 Å2
Refractivity
83.28 m3·mol-1
Polarizability
33.38 Å3
Rotatable Bond Count
6
H Bond Acceptor Count
4
H Bond Donor Count
2
Physiological Charge
1
Number of Rings
2
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Levobunolol is an ophthalmic beta-blocker, equally effective at β(1)- and β(2)-receptor sites. Levobunolol reduces both elevated and normal IOP in patients with or without glaucoma. In patients with elevated IOP, levobunolol reduces mean IOP by approximately 25-40% from baseline. As the drug is a nonselective &beta-adrenergic blocking agent, it can produce both systemic pulmonary and cardiovascular effects following topical application to the eye. These effects include adverse pulmonary effects (eg. bronchoconstriction, increased airway resistance), and a decrease in blood pressure and heart rate.
Cơ Chế Tác Dụng : A nonselective beta-adrenoceptor antagonist used in the treatment of glaucoma. [PubChem] Levobunolol's mechanism of action in reducing IOP is not clearly defined, but is believed to be due to a reduction of the production of aqueous humor via blockage of endogenous catecholamine-stimulated increases in cyclic adenosine monophosphate (AMP) concentrations within the ciliary processes.
Dược Động Học :
▧ Absorption :
80%
▧ Metabolism :
Hepatic
▧ Half Life :
20 hours
Độc Tính : Bradycardia, hypotension, bronchospasm, and acute cardiac failure, LD50=700 mg/kg (orally in rat).
Chỉ Định : For lowering intraocular pressure (IOP) and may be used in patients with chronic open-angle glaucoma or ocular hypertension.
Tương Tác Thuốc :
  • Treprostinil Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Liều Lượng & Cách Dùng : Liquid - Ophthalmic
Solution - Ophthalmic
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Akbeta
  • Công ty :
    Sản phẩm biệt dược : Betagan
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