Tìm theo
Travoprost
Các tên gọi khác (5 ) :
  • Isopropyl (Z)-7-((1R,2R,3R,5S)-3,5-dihydroxy-2-{(1e,3R)-3-hydroxy-4-[(alpha,alpha,alpha-trifluoro-m-tolyl)oxy]-1-butenyl}cyclopentyl)-5-heptenoate
  • Travatan
  • Travatan Z
  • Travoprost
  • Travoprostum
prostaglandins synthetic, anti glaucoma agents, ophthalmics
Thuốc Gốc
Small Molecule
CAS: 157283-68-6
ATC: S01EE04
ĐG : Alcon Laboratories , http://www.alcon.com
CTHH: C26H35F3O6
PTK: 500.5477
Travoprost ophthalmic solution is a topical medication used for controlling the progression of glaucoma or ocular hypertension, by reducing intraocular pressure. It is a synthetic prostaglandin F2alpha analogue. [Wikipedia]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
Phân tử khối
500.5477
Monoisotopic mass
500.238573467
InChI
InChI=1S/C26H35F3O6/c1-17(2)35-25(33)11-6-4-3-5-10-21-22(24(32)15-23(21)31)13-12-19(30)16-34-20-9-7-8-18(14-20)26(27,28)29/h3,5,7-9,12-14,17,19,21-24,30-32H,4,6,10-11,15-16H2,1-2H3/b5-3-,13-12+/t19-,21-,22-,23+,24-/m1/s1
InChI Key
InChIKey=MKPLKVHSHYCHOC-AHTXBMBWSA-N
IUPAC Name
propan-2-yl (5Z)-7-[(1R,2R,3R,5S)-3,5-dihydroxy-2-[(1E,3R)-3-hydroxy-4-[3-(trifluoromethyl)phenoxy]but-1-en-1-yl]cyclopentyl]hept-5-enoate
Traditional IUPAC Name
travoprost
SMILES
CC(C)OC(=O)CCC\C=C/C[[email protected]]1[[email protected]@H](O)C[[email protected]@H](O)[[email protected]@H]1\C=C\[[email protected]@H](O)COC1=CC=CC(=C1)C(F)(F)F
Độ hòa tan
>16 mg/ml at 25.0°C
logP
4.6
logS
-4.8
pKa (strongest acidic)
13.95
pKa (Strongest Basic)
-2.9
PSA
96.22 Å2
Refractivity
127.86 m3·mol-1
Polarizability
51.61 Å3
Rotatable Bond Count
14
H Bond Acceptor Count
5
H Bond Donor Count
3
Physiological Charge
0
Number of Rings
2
Bioavailability
0
Dược Lực Học : Travoprost, an isopropyl ester prodrug, is a synthetic prostaglandin F2 alpha analogue that is rapidly hydrolyzed by esterases in the cornea to its biologically active free acid. The travoporst free acid is potent and highly selective for the FP prostanoid receptor.
Cơ Chế Tác Dụng : Travoprost ophthalmic solution is a topical medication used for controlling the progression of glaucoma or ocular hypertension, by reducing intraocular pressure. It is a synthetic prostaglandin F2alpha analogue. [Wikipedia] Travoprost free acid is a selective FP prostanoid receptor agonist and is believed to reduce intraocular pressure by increasing the drainage of aqueous humor, which is done primarily through increased uveoscleral outflow and to a lesser extent, trabecular outflow facility.
Dược Động Học :
▧ Absorption :
Systemically absorbed when administered to the eye.
▧ Metabolism :
Travoprost, an isopropyl ester prodrug, is hydrolyzed by esterases in the cornea to its biologically active free acid. Systemically, travoprost free acid is metabolized to inactive metabolites via beta-oxidation of the α(carboxylic acid) chain to give the 1,2-dinor and 1,2,3,4-tetranor analogs, via oxidation of the 15-hydroxyl moiety, as well as via reduction of the 13,14 double bond.
▧ Route of Elimination :
Less than 2% of the topical ocular dose of travoprost was excreted in the urine within 4 hours as the travoprost free acid.
▧ Half Life :
Terminal elimination half-life of travoprost free acid is 45 minutes.
Độc Tính : Symptoms of overexposure include irritation to the skin, eyes, nose, throat, and respiratory tract.
Chỉ Định : Ophthalmic solution used for the reduction of elevated intraocular pressure in patients with open-angle glaucoma or ocular hypertension who are intolerant of other intraocular pressure lowering medications or insufficiently responsive (failed to achieve target IOP determined after multiple measurements over time) to another intraocular pressure lowering medication.
Liều Lượng & Cách Dùng : Solution - Ophthalmic
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Travatan
  • Công ty :
    Sản phẩm biệt dược : Travatan Z
  • Công ty :
    Sản phẩm biệt dược : Travo-Z
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