药品详细

Probucol(普罗布考)

基本信息
剂型规格
适应症
药理
临床
理化性质
相互作用
文档
专利
Pathway
文献
序列

化学结构式图

中文名

普罗布考

英文名

Probucol

分子式

C₃₁H₄₈O₂S₂

化学名

2,6-di-tert-butyl-4-({2-[(3,5-di-tert-butyl-4-hydroxyphenyl)sulfanyl]propan-2-yl}sulfanyl)phenol

分子量

Average: 516.842
Monoisotopic: 516.30957216

CAS号

23288-49-5

ATC分类

C10A 未知

药物类型

small molecule

阶段

approved

商品名

同义名

基本介绍

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).

生产厂家

Sanofi aventis us llc

封装厂家

参考

Synthesis Reference	Not Available
General Reference	Not Available

剂型

规格

化合物类型

Type	small molecule

Classes

Phenols and Derivatives
Cumenes and Derivatives

Substructures

Hydroxy Compounds
Phenols and Derivatives
Benzene and Derivatives
Cumenes and Derivatives
Aromatic compounds
Acetals and Derivatives
Phenyl Esters

适应症

药理

Indication	Used to lower LDL and HDL cholesterol.
Pharmacodynamics	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.
Mechanism of action	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.
Absorption	Absorption from the gastrointestinal tract is limited and variable (about 7%).
Volume of distribution	Not Available
Protein binding	Not Available
Metabolism	Not Available
Route of elimination	Not Available
Half life	Ranges from 12 hours to more than 500 hours, the longest half-life probably being in adipose tissue.
Clearance	Not Available
Toxicity	Not Available
Affected organisms	Humans and other mammals
Pathways	Not Available

理化性质

Properties

State

solid

Experimental Properties

Property	Value	Source
melting point	125 °C	PhysProp

Predicted Properties

Property	Value	Source
water solubility	4.18e-05 g/l	ALOGPS
logP	8.92	ALOGPS
logP	10.57	ChemAxon
logS	-7.1	ALOGPS
pKa (strongest acidic)	10.29	ChemAxon
pKa (strongest basic)	-5.1	ChemAxon
physiological charge	0	ChemAxon
hydrogen acceptor count	2	ChemAxon
hydrogen donor count	2	ChemAxon
polar surface area	40.46	ChemAxon
rotatable bond count	8	ChemAxon
refractivity	159.26	ChemAxon
polarizability	62.37	ChemAxon

药物相互作用

Drug	Interaction
Artemether	Additive QTc-prolongation may occur. Concomitant therapy should be avoided.
Cyclosporine	Probucol decreases the effect of cyclosporine
Lumefantrine	Additive QTc-prolongation may occur. Concomitant therapy should be avoided.
Tacrolimus	Additive QTc-prolongation may occur increasing the risk of serious ventricular arrhythmias. Concomitant therapy should be used with caution.
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.
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.
Trimipramine	Additive QTc-prolongation may occur, increasing the risk of serious ventricular arrhythmias. Concomitant therapy should be used with caution.
Voriconazole	Additive QTc prolongation may occur. Consider alternate therapy or monitor for QTc prolongation as this can lead to Torsade de Pointes (TdP).
Vorinostat	Additive QTc prolongation may occur. Consider alternate therapy or monitor for QTc prolongation as this can lead to Torsade de Pointes (TdP).
Ziprasidone	Additive QTc-prolonging effects may increase the risk of severe arrhythmias. Concomitant therapy is contraindicated.
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).

食物相互作用

Take with food. Food increases availability.

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