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Mechanism of Action
Bezafibrate¿¡ ´ëÇÑ Mechanism_Of_Action Á¤º¸ Like the other fibrates, bezafibrate is an agonist of PPAR¥á; some studies suggest it may have some activity on PPAR¥ã and PPAR¥ä as well.
Pharmacology
Bezafibrate¿¡ ´ëÇÑ Pharmacology Á¤º¸ Bezafibrate is an antilipemic agent that lowers cholesterol and triglycerides. It decreases low density lipoproteins and increases high density lipoproteins. Bezafibrate lowers elevated blood lipids (triglycerides and cholesterol). Elevated VLDL and LDL are reduced by treatment with bezafibrate, whilst HDL-levels are increased. The activity of triglyceride lipases (lipoprotein lipase and hepatic lipoproteinlipase) involved in the catabolism of triglyceride-rich lipoproteins is increased by bezafibrate. In the course of the intensified degradation of triglyceride-rich lipoproteins (chylomicrons, VLDL) precursors for the formation of HDL are formed which explains an increase in HDL. Furthermore, cholesterol biosynthesis is reduced by bezafibrate, which is accompanied by a stimulation of the LDL-receptor-mediated lipoprotein catabolism. Elevated fibrinogen appears to be an important risk-factor, alongside the lipids, smoking and hypertension, in the development of atheroma. Fibrinogen plays an important role in viscosity, and therefore blood flow, and also appears to play an important role in thrombus development and lysability. Bezafibrate exerts an effect on thrombogenic factors. A significant decrease in elevated plasma fibrinogen levels can be achieved. This may lead, amongst other things, to a reduction in both blood and plasma viscosity. Inhibition of platelet aggregation has also been observed. A reduction in blood glucose concentration due to an increase in glucose tolerance has been reported in diabetic patients. In the same patients, the concentration of fasting and postprandial free fatty acids was reduced by bezafibrate.
Metabolism
Bezafibrate¿¡ ´ëÇÑ Metabolism Á¤º¸ # Phase_1_Metabolizing_Enzyme:Liver carboxylesterase
Protein Binding
Bezafibrate¿¡ ´ëÇÑ ´Ü¹é°áÇÕ Á¤º¸ 94-96% of bezafibrate is bound to protein in human serum.
Half-life
Bezafibrate¿¡ ´ëÇÑ ¹Ý°¨±â Á¤º¸ 1-2 hours
Absorption
Bezafibrate¿¡ ´ëÇÑ Absorption Á¤º¸ Bezafibrate is almost completely absorbed after oral administration. The relative bioavailability of bezafibrate retard compared to the standard form is about 70%.
Biotransformation
Bezafibrate¿¡ ´ëÇÑ Biotransformation Á¤º¸ Hepatic.
CYP450 Drug Interaction
[CYP450 TableÁ÷Á¢Á¶È¸]
Drug Target
[Drug Target]
Description
Bezafibrate¿¡ ´ëÇÑ Description Á¤º¸ Antilipemic agent that lowers cholesterol and triglycerides. It decreases low density lipoproteins and increases high density lipoproteins. [PubChem]
Dosage Form
Bezafibrate¿¡ ´ëÇÑ Dosage_Form Á¤º¸ Tablet OralTablet OralTablet, extended release OralTablet, film coated, extended release Oral
Drug Category
Bezafibrate¿¡ ´ëÇÑ Drug_Category Á¤º¸ Antilipemic Agents
Smiles String Canonical
Bezafibrate¿¡ ´ëÇÑ Smiles_String_canonical Á¤º¸ CC(C)(OC1=CC=C(CCNC(=O)C2=CC=C(Cl)C=C2)C=C1)C(O)=O
Smiles String Isomeric
Bezafibrate¿¡ ´ëÇÑ Smiles_String_isomeric Á¤º¸ CC(C)(OC1=CC=C(CCNC(=O)C2=CC=C(Cl)C=C2)C=C1)C(O)=O
InChI Identifier
Bezafibrate¿¡ ´ëÇÑ InChI_Identifier Á¤º¸ InChI=1/C19H20ClNO4/c1-19(2,18(23)24)25-16-9-3-13(4-10-16)11-12-21-17(22)14-5-7-15(20)8-6-14/h3-10H,11-12H2,1-2H3,(H,21,22)(H,23,24)/f/h21,23H
Chemical IUPAC Name
Bezafibrate¿¡ ´ëÇÑ Chemical_IUPAC_Name Á¤º¸ 2-[4-[2-[(4-chlorobenzoyl)amino]ethyl]phenoxy]-2-methylpropanoic acid
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