Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C31H48O2S2
Monoisotopic mass
516.30957216
InChI
InChI=1S/C31H48O2S2/c1-27(2,3)21-15-19(16-22(25(21)32)28(4,5)6)34-31(13,14)35-20-17-23(29(7,8)9)26(33)24(18-20)30(10,11)12/h15-18,32-33H,1-14H3
InChI Key
InChIKey=FYPMFJGVHOHGLL-UHFFFAOYSA-N
IUPAC Name
2,6-di-tert-butyl-4-({2-[(3,5-di-tert-butyl-4-hydroxyphenyl)sulfanyl]propan-2-yl}sulfanyl)phenol
Traditional IUPAC Name
probucol
SMILES
CC(C)(SC1=CC(=C(O)C(=C1)C(C)(C)C)C(C)(C)C)SC1=CC(=C(O)C(=C1)C(C)(C)C)C(C)(C)C
pKa (strongest acidic)
10.29
pKa (Strongest Basic)
-5.1
Refractivity
159.26 m3·mol-1
Dược Lực Học :
Probucol lowers the level of cholesterol in the bloodstream by increasing the rate of LDL catabolism. Additionally, probucol may inhibit cholesterol synthesis and delay cholesterol absorption. Probucol is a powerful antioxidant drug normally used to prevent vascular disease caused by the free radicals in the body.
Cơ Chế Tác Dụng :
A drug used to lower LDL and HDL cholesterol yet has little effect on serum-triglyceride or VLDL cholesterol. (From Martindale, The Extra Pharmacopoeia, 30th ed, p993).
Probucol lowers serum cholesterol by increasing the fractional rate of low-density lipoprotein (LDL) catabolism in the final metabolic pathway for cholesterol elimination from the body. Additionally, probucol may inhibit early stages of cholesterol biosynthesis and slightly inhibit dietary cholesterol absorption. Recent information suggests that probucol may inhibit the oxidation and tissue deposition of LDL cholesterol, thereby inhibiting atherogenesis. It appears to inhibits ABCA1-mediated cellular lipid efflux.
Dược Động Học :
▧ Absorption :
Absorption from the gastrointestinal tract is limited and variable (about 7%).
▧ Half Life :
Ranges from 12 hours to more than 500 hours, the longest half-life probably being in adipose tissue.
Chỉ Định :
Used to lower LDL and HDL cholesterol.
Tương Tác Thuốc :
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Artemether
Additive QTc-prolongation may occur. Concomitant therapy should be avoided.
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Cyclosporine
Probucol decreases the effect of cyclosporine
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Lumefantrine
Additive QTc-prolongation may occur. Concomitant therapy should be avoided.
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Tacrolimus
Additive QTc-prolongation may occur increasing the risk of serious ventricular arrhythmias. Concomitant therapy should be used with caution.
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Thiothixene
May cause additive QTc-prolonging effects. Increased risk of ventricular arrhythmias. Consider alternate therapy. Thorough risk:benefit assessment is required prior to co-administration.
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Toremifene
Additive QTc-prolongation may occur, increasing the risk of serious ventricular arrhythmias. Consider alternate therapy. A thorough risk:benefit assessment is required prior to co-administration.
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Trimipramine
Additive QTc-prolongation may occur, increasing the risk of serious ventricular arrhythmias. Concomitant therapy should be used with caution.
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Voriconazole
Additive QTc prolongation may occur. Consider alternate therapy or monitor for QTc prolongation as this can lead to Torsade de Pointes (TdP).
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Vorinostat
Additive QTc prolongation may occur. Consider alternate therapy or monitor for QTc prolongation as this can lead to Torsade de Pointes (TdP).
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Ziprasidone
Additive QTc-prolonging effects may increase the risk of severe arrhythmias. Concomitant therapy is contraindicated.
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Zuclopenthixol
Additive QTc prolongation may occur. Consider alternate therapy or use caution and monitor for QTc prolongation as this can lead to Torsade de Pointes (TdP).
Liều Lượng & Cách Dùng :
Tablet - Oral
Tablet - Oral
Dữ Kiện Thương Mại
Giá thị trường
-
Giá bán buôn : USD >2.45
Đơn vị tính : g