Tìm theo
Metipranolol
Các tên gọi khác (4 ) :
  • (+-)-Metipranolol
  • Acetic acid 4-(2-hydroxy-3-isopropylamino-propoxy)-2,3,6-trimethyl-phenyl ester
  • Metipranolol
  • Metipranololum
antihypertensive agents, sympatholytics, anti arrhythmia agents, adrenergic beta antagonists
Thuốc Gốc
Small Molecule
CAS: 22664-55-7
ATC: S01ED04
ĐG : Alcon Laboratories , http://www.alcon.com
CTHH: C17H27NO4
PTK: 309.4006
A beta-adrenergic antagonist effective for both beta-1 and beta-2 receptors. It is used as an antiarrhythmic, antihypertensive, and antiglaucoma agent. [PubChem]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C17H27NO4
Phân tử khối
309.4006
Monoisotopic mass
309.194008357
InChI
InChI=1S/C17H27NO4/c1-10(2)18-8-15(20)9-21-16-7-11(3)17(22-14(6)19)13(5)12(16)4/h7,10,15,18,20H,8-9H2,1-6H3
InChI Key
InChIKey=BQIPXWYNLPYNHW-UHFFFAOYSA-N
IUPAC Name
4-{2-hydroxy-3-[(propan-2-yl)amino]propoxy}-2,3,6-trimethylphenyl acetate
Traditional IUPAC Name
metipranolol
SMILES
CC(C)NCC(O)COC1=C(C)C(C)=C(OC(C)=O)C(C)=C1
Độ tan chảy
105-107 °C
Độ hòa tan
589 mg/L
logP
2.66
logS
-3.2
pKa (strongest acidic)
14.09
pKa (Strongest Basic)
9.67
PSA
67.79 Å2
Refractivity
86.63 m3·mol-1
Polarizability
35.85 Å3
Rotatable Bond Count
8
H Bond Acceptor Count
4
H Bond Donor Count
2
Physiological Charge
1
Number of Rings
1
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Metipranolol is a beta1 and beta2 (non-selective) adrenergic receptor-blocking agent that does not have significant intrinsic sympathomimetic, direct myocardial depressant, or local anesthetic (membrane-stabilizing) activity. Metipranolol is indicated in the treatment of elevated intraocular pressure in patients with ocular hypertension or open-angle glaucoma. Metipranolol, when applied topically to the eye, has the action of reducing elevated, as well as normal, intraocular pressure, whether or not accompanied by glaucoma. Elevated intraocular pressure is a major risk factor in the pathogenesis of glaucomatous visual field loss and optic nerve damage. Metipranolol reduces intraocular pressure with little or no effect on pupil size or accommodation in contrast to the miosis which cholinergic agents are known to produce.
Cơ Chế Tác Dụng : A beta-adrenergic antagonist effective for both beta-1 and beta-2 receptors. It is used as an antiarrhythmic, antihypertensive, and antiglaucoma agent. [PubChem] Although it is known that metipranolol binds the beta1 and beta2 adrenergic receptors, the mechanism of metipranolol's action is not known. It has no significant intrinsic sympathomimetic activity, and has only weak local anesthetic (membrane-stabilizing) and myocardial depressant activity. It appears that the ophthalmic beta-adrenergic blocking agents reduce aqueous humor production, as demonstrated by tonography and fluorophotometry. A slight increase in aqueous humor outflow may be an additional mechanism.
Chỉ Định : Indicated in the treatment of elevated intraocular pressure in patients with ocular hypertension or open angle glaucoma.
Tương Tác Thuốc :
  • Treprostinil Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Liều Lượng & Cách Dùng : Solution / drops - Ophthalmic
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Betanol
  • Công ty :
    Sản phẩm biệt dược : Disorat
  • Công ty :
    Sản phẩm biệt dược : OptiPranolol
  • Công ty :
    Sản phẩm biệt dược : Trimepranol
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB01214
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=31477
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46505935
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C07915
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D02374
ChemSpider
http://www.chemspider.com/Chemical-Structure.29193.html
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/24208-275-07
PharmGKB
http://www.pharmgkb.org/drug/PA164748727
Wikipedia
http://en.wikipedia.org/wiki/Metipranolol
RxList
http://www.rxlist.com/cgi/generic3/optipran.htm
Drugs.com
http://www.drugs.com/cdi/metipranolol-drops.html
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