Tìm theo
Bimatoprost
Các tên gọi khác (2) :
  • (Z)-7-((1R,2R,3R,5S)-3,5-Dihydroxy-2-((1e,3S)-3-hydroxy-5-phenyl-1-pentenyl)cyclopentyl)-N-ethyl-5-heptenamide
  • Bimatoprostum
anti glaucoma agents
Thuốc Gốc
Small Molecule
CAS: 155206-00-1
ATC: S01EE03
ĐG : Allergan Inc. , http://www.allergan.com
CTHH: C25H37NO4
PTK: 415.5656
Bimatoprost ophthalmic solution is a topical medication used for controlling the progression of glaucoma or ocular hypertension, by reducing intraocular pressure. It is a prostaglandin analogue that works by increasing the outflow of aqueous fluid from the eyes. It binds to the prostanoid FP receptor.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C25H37NO4
Phân tử khối
415.5656
Monoisotopic mass
415.272258677
InChI
InChI=1S/C25H37NO4/c1-2-26-25(30)13-9-4-3-8-12-21-22(24(29)18-23(21)28)17-16-20(27)15-14-19-10-6-5-7-11-19/h3,5-8,10-11,16-17,20-24,27-29H,2,4,9,12-15,18H2,1H3,(H,26,30)/b8-3-,17-16+/t20-,21+,22+,23-,24+/m0/s1
InChI Key
InChIKey=AQOKCDNYWBIDND-FTOWTWDKSA-N
IUPAC Name
(5Z)-7-[(1R,2R,3R,5S)-3,5-dihydroxy-2-[(1E,3S)-3-hydroxy-5-phenylpent-1-en-1-yl]cyclopentyl]-N-ethylhept-5-enamide
Traditional IUPAC Name
bimatoprost
SMILES
CCNC(=O)CCC\C=C/C[C@H]1[C@@H](O)C[C@@H](O)[C@@H]1\C=C\[C@@H](O)CCC1=CC=CC=C1
Độ hòa tan
Slightly soluble
logP
3.2
logS
-4.3
pKa (strongest acidic)
14.35
pKa (Strongest Basic)
-0.23
PSA
89.79 Å2
Refractivity
122.83 m3·mol-1
Polarizability
48.99 Å3
Rotatable Bond Count
12
H Bond Acceptor Count
4
H Bond Donor Count
4
Physiological Charge
0
Number of Rings
2
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Bimatoprost is a prostamide, a synthetic structural analog of prostaglandin with ocular hypotensive activity, that is chemically related to prostamide F. It selectively mimics the effects of naturally occurring substances, prostamides. Bimatoprost lowers intraocular pressure (IOP) in humans. Elevated IOP presents a major risk factor for glaucomatous field loss. The higher the level of IOP, the greater the likelihood of optic nerve damage and visual field loss.
Cơ Chế Tác Dụng : Bimatoprost ophthalmic solution is a topical medication used for controlling the progression of glaucoma or ocular hypertension, by reducing intraocular pressure. It is a prostaglandin analogue that works by increasing the outflow of aqueous fluid from the eyes. It binds to the prostanoid FP receptor. Bimatoprost is believed to lower intraocular pressure (IOP) in humans by increasing outflow of aqueous humor through both the trabecular meshwork and uveoscleral routes. Bimatoprost reduces the pressure in the eye by mimicking the action of a naturally-occuring prostaglandin. Prostaglandins are a group of chemicals found in many places in the body. In the eye, they increase the drainage of the aqueous humour out of the eyeball. Bimatoprost is a synthetic compound related to one of the natural prostaglandins, and works by increasing the drainage of aqueous humour out of the eyeball. Bimatoprost may also lower the rate of aqueous formation in the eye. Both these effects decrease the pressure within the eye.
Dược Động Học :
▧ Absorption :
Systemically absorbed when administered to the eye.
▧ Volume of Distribution :
* 0.67 L/kg
▧ Protein binding :
Approximately 88% of bimatoprost is bound in human plasma.
▧ Metabolism :
Bimatoprost undergoes oxidation, N-deethylation and glucuronidation to form a variety of metabolites.
▧ Route of Elimination :
Up to 67% of the administered dose was excreted in the urine while 25% of the dose was recovered in the feces.
▧ Half Life :
Elimination half-life is approximately 45 minutes.
▧ Clearance :
* 1.5 L/hr/kg [Healthy subjects receiving IV administration of 3.12 ug/kg]
Độc Tính : In oral (by gavage) mouse and rat studies, doses up to 100 mg/kg/day did not produce any toxicity. This dose expressed as mg/m2 is at least 70 times higher than the accidental dose of one bottle of bimatoprost for a 10 kg child.
Chỉ Định : 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.
Tương Tác Thuốc :
  • Latanoprost The concomitant use of bimatoprost and latanoprost may result in increased intraocular pressure. Consider avoiding this combination of therapy. Monitor for paradoxical increases in intraocular pressure during concomitant use.
Liều Lượng & Cách Dùng : Solution - Ophthalmic
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Lumigan
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00905
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=5311027
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46505334
ChemSpider
http://www.chemspider.com/Chemical-Structure.4470565.html
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0023-3616-03
PharmGKB
http://www.pharmgkb.org/drug/PA164748867
Wikipedia
http://en.wikipedia.org/wiki/Bimatoprost
RxList
http://www.rxlist.com/cgi/generic2/bimatoprost.htm
PDRhealth
http://www.pdrhealth.com/drug_info/rxdrugprofiles/drugs/lum1578.shtml
Drugs.com
http://www.drugs.com/cdi/bimatoprost-drops.html
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