Tìm theo
Rimexolone
corticosteroids
Thuốc Gốc
Small Molecule
CAS: 49697-38-3
ATC: H02AB12, S01BA13
ĐG : Alcon Laboratories , http://www.alcon.com
CTHH: C24H34O3
PTK: 370.525
Rimexolone is a glucocorticoid steroid used to treat inflammation in the eye. It is marketed as a 1% eye drop solution under the trade name Vexol
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C24H34O3
Phân tử khối
370.525
Monoisotopic mass
370.250794954
InChI
InChI=1S/C24H34O3/c1-6-20(27)24(5)14(2)11-18-17-8-7-15-12-16(25)9-10-22(15,3)21(17)19(26)13-23(18,24)4/h9-10,12,14,17-19,21,26H,6-8,11,13H2,1-5H3/t14-,17?,18?,19+,21?,22+,23+,24-/m1/s1
InChI Key
InChIKey=QTTRZHGPGKRAFB-PAIWTFDUSA-N
IUPAC Name
(2R,13R,14S,15S,17S)-17-hydroxy-2,13,14,15-tetramethyl-14-propanoyltetracyclo[8.7.0.0^{2,7}.0^{11,15}]heptadeca-3,6-dien-5-one
Traditional IUPAC Name
(2R,13R,14S,15S,17S)-17-hydroxy-2,13,14,15-tetramethyl-14-propanoyltetracyclo[8.7.0.0^{2,7}.0^{11,15}]heptadeca-3,6-dien-5-one
SMILES
CCC(=O)[C@@]1(C)[C@H](C)CC2C3CCC4=CC(=O)C=C[C@]4(C)C3[C@@H](O)C[C@]12C
Độ hòa tan
Insoluble
logP
4.2
logS
-4.5
pKa (strongest acidic)
18.76
pKa (Strongest Basic)
-0.21
PSA
54.37 Å2
Refractivity
109.07 m3·mol-1
Polarizability
43.03 Å3
Rotatable Bond Count
2
H Bond Acceptor Count
3
H Bond Donor Count
1
Physiological Charge
0
Number of Rings
4
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Rimexolone is a glucocorticoid corticosteroid for systemic use. Corticosteroids suppress the inflammatory response to a variety of inciting agents of a mechanical, chemical, or immunological nature. They inhibit edema, cellular infiltration, capillary dilatation, fibroblastic proliferation, deposition of collagen and scar formation associated with inflammation.
Cơ Chế Tác Dụng : Rimexolone is a glucocorticoid steroid used to treat inflammation in the eye. It is marketed as a 1% eye drop solution under the trade name Vexol Rimexolone is a glucocorticoid receptor agonist. The antiinflammatory actions of corticosteroids are thought to involve lipocortins, phospholipase A2 inhibitory proteins which, through inhibition of arachidonic acid, control the biosynthesis of prostaglandins and leukotrienes. By binding to the glucocorticoid receptor, this drug ultimately leads to changes in genetic transcription involving the lipocortins and prostaglandins.
Dược Động Học :
▧ Absorption :
Systemically absorbed.
▧ Metabolism :
Undergoes extensive metabolism. Following intravenous administration of radiolabeled rimexolone in rats, more than 80% of the dose was excreted in the feces as rimexolone and metabolites. Metabolites have been shown to be either less active than rimexolone or inactive in human glucocorticoid receptor binding assays.
▧ Route of Elimination :
Following IV administration of radio-labelled rimexolone to rats, greater than 80% of the dose is excreted via the feces as rimexolone and metabolites.
▧ Half Life :
The serum half-life of rimexolone could not be reliably estimated due to the large number of samples below the quantitation limit of the assay (80 pg/mL). However, based on the time required to reach steady-state, the half-life appears to be short (1-2 hours).
Độc Tính : Symptoms of overdose include retinal toxicity, glaucoma, and subcapsular cataract.
Chỉ Định : For the treatment of postoperative inflammation following ocular surgery and in the treatment of anterior uveitis.
Liều Lượng & Cách Dùng : Suspension - Ophthalmic
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Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00896
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=39507
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46504820
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D05729
ChemSpider
http://www.chemspider.com/Chemical-Structure.36120.html
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0065-0627-07
PharmGKB
http://www.pharmgkb.org/drug/PA164752251
Wikipedia
http://en.wikipedia.org/wiki/Rimexolone
RxList
http://www.rxlist.com/cgi/generic3/rimexol.htm
Drugs.com
http://www.drugs.com/cdi/rimexolone.html
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