Tìm theo
Bezafibrate
Các tên gọi khác (8 ) :
  • 2-(P-(2-(P-Chlorobenzamido)ethyl)phenoxy)-2-methylpropionic acid
  • Befizal
  • Bezafibrat
  • Bezafibrato
  • Bezafibratum
  • Bezalip
  • Bezatol sr (tn)
  • Cedur
Thuốc tác dụng đối với máu
Thuốc Gốc
Small Molecule
CAS: 41859-67-0
ATC: C10AB02
CTHH: C19H20ClNO4
PTK: 361.819
Antilipemic agent that lowers cholesterol and triglycerides. It decreases low density lipoproteins and increases high density lipoproteins. [PubChem]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C19H20ClNO4
Phân tử khối
361.819
Monoisotopic mass
361.10808584
InChI
InChI=1S/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)
InChI Key
InChIKey=IIBYAHWJQTYFKB-UHFFFAOYSA-N
IUPAC Name
2-(4-{2-[(4-chlorophenyl)formamido]ethyl}phenoxy)-2-methylpropanoic acid
Traditional IUPAC Name
bezafibrate
SMILES
CC(C)(OC1=CC=C(CCNC(=O)C2=CC=C(Cl)C=C2)C=C1)C(O)=O
Độ tan chảy
186 °C
Độ hòa tan
1.55e-03 g/l
logP
3.99
logS
-5.4
pKa (strongest acidic)
3.83
pKa (Strongest Basic)
-0.84
PSA
75.63 Å2
Refractivity
95.96 m3·mol-1
Polarizability
37.53 Å3
Rotatable Bond Count
7
H Bond Acceptor Count
4
H Bond Donor Count
2
Physiological Charge
-1
Number of Rings
2
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : 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.
Cơ Chế Tác Dụng : Antilipemic agent that lowers cholesterol and triglycerides. It decreases low density lipoproteins and increases high density lipoproteins. [PubChem] Like the other fibrates, bezafibrate is an agonist of PPARα; some studies suggest it may have some activity on PPARγ and PPARδ as well.
Dược Động Học :
▧ Absorption :
Bezafibrate is almost completely absorbed after oral administration. The relative bioavailability of bezafibrate retard compared to the standard form is about 70%.
▧ Protein binding :
94-96% of bezafibrate is bound to protein in human serum.
▧ Metabolism :
Hepatic.
▧ Half Life :
1-2 hours
Chỉ Định : For the treatment of primary hyperlipidaemia types IIa, IIb, III, IV and V (Fredrickson classification) corresponding to groups I, II and III of the European Atherosclerosis Society guidelines - when diet alone or improvements in lifestyle such as increased exercise or weight reduction do not lead to an adequate response. Also for the treatment of secondary hyperlipidaemias, e.g. severe hypertriglyceridemias, when sufficient improvement does not occur after correction of the underlying disorder (e.g. diabetes mellitus).
Tương Tác Thuốc :
  • Atorvastatin Increased risk of myopathy/rhabdomyolysis
  • Cerivastatin Increased risk of myopathy/rhabdomyolysis
  • Cholestyramine Bile acid sequestrants like cholestyramine may decrease the absorption of fibric acid derivatives like bezafibrate. Therapy modification should be considered. If concomitant therapy is used, separate doses by at least 2 hours to minimize this interaction. Fenofibric acid labeling recommends administration one hour prior to or 4-6 hours after a bile acid sequestrant.
  • Conivaptan Conivaptan may increase the serum concentration of CYP3A4 substrates like bezafibrates. Consider therapy modification. Conivaptan may increase the serum concentration of CYP3A4 substrates.
  • Cyclosporine Cyclosporine may enhance the nephrotoxic effect of fibric acid derivatives like bezafibrate. Fibric acid derivatives may decrease the serum concentration of cyclosporine. Extra monitoring of renal function and cyclosporine concentrations will likely be required. Adjustment of cyclosporine dose may be necessary.
  • Fluvastatin Increased risk of myopathy/rhabdomyolysis
  • Isocarboxazid MAO Inhibitors may enhance the adverse/toxic effect of Bezafibrate. Avoid concomitant use of bezafibrate with monoamine oxidase inhibitors (MAOIs) like isocarboxazid.
  • Linezolid MAO Inhibitors may enhance the adverse/toxic effect of Bezafibrate. Avoid concomitant use of bezafibrate with monoamine oxidase inhibitors (MAOIs) like linezolid.
  • Lovastatin Increased risk of myopathy/rhabdomyolysis
  • Moclobemide MAO Inhibitors may enhance the adverse/toxic effect of Bezafibrate. Avoid concomitant use of bezafibrate with monoamine oxidase inhibitors (MAOIs) like moclobemide.
  • Phenelzine MAO Inhibitors may enhance the adverse/toxic effect of Bezafibrate. Avoid concomitant use of bezafibrate with monoamine oxidase inhibitors (MAOIs) like phenelzine.
  • Pravastatin Increased risk of myopathy/rhabdomyolysis
  • Procarbazine MAO Inhibitors may enhance the adverse/toxic effect of Bezafibrate. Avoid concomitant use of bezafibrate with monoamine oxidase inhibitors (MAOIs) like procarbazine.
  • Rasagiline MAO Inhibitors may enhance the adverse/toxic effect of Bezafibrate. Avoid concomitant use of bezafibrate with monoamine oxidase inhibitors (MAOIs) rasagiline.
  • Selegiline MAO Inhibitors may enhance the adverse/toxic effect of Bezafibrate. Avoid concomitant use of bezafibrate with monoamine oxidase inhibitors (MAOIs) like selegiline.
  • Tranylcypromine MAO Inhibitors may enhance the adverse/toxic effect of Bezafibrate. Avoid concomitant use of bezafibrate with monoamine oxidase inhibitors (MAOIs) like tranylcypromine.
  • Warfarin Bezafibrate may increase the anticoagulant effect of warfarin. Monitor prothrombin time and therapeutic and adverse effects of warfarin if bezafibrate is initiated, discontinued or dose changed.
Liều Lượng & Cách Dùng : Tablet - Oral
Tablet - Oral - 200mg
Tablet, extended release - Oral
Tablet, film coated, extended release - Oral - 400mg
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Befizal
  • Công ty :
    Sản phẩm biệt dược : Bezalip
  • Công ty :
    Sản phẩm biệt dược : Bezalip retard
  • Công ty :
    Sản phẩm biệt dược : Bezatol
  • Công ty :
    Sản phẩm biệt dược : Bezatol SR
  • Công ty :
    Sản phẩm biệt dược : Cedur
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB01393
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=39042
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46509188
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D01366
ChemSpider
http://www.chemspider.com/Chemical-Structure.35728.html
BindingDB
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=28701
PharmGKB
http://www.pharmgkb.org/drug/PA162364313
Wikipedia
http://en.wikipedia.org/wiki/Bezafibrate
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