Tìm theo
Cilostazol
Các tên gọi khác (6 ) :
  • 3,4-dihydro-6-(4-(1-Cyclohexyl-1H-tetrazol-5-yl)butoxy)-2(1H)-quinolinone
  • 6-(4-(1-Cyclohexyl-1H-tetrazol-5-yl)butoxy)-3,4-dihydro-2(1H)-quinolinone
  • 6-(4-(1-Cyclohexyl-1H-tetrazol-5-yl)butoxy)-3,4-dihydrocarbostyril
  • 6-[4-(1-Cyclohexyl-1H-tetrazol-5-yl)-butoxy]-3,4-dihydro-1H-quinolin-2-one
  • Cilostazole
  • Cilostazolum
Thuốc tác dụng đối với máu
Thuốc Gốc
Small Molecule
CAS: 73963-72-1
ATC: B01AC23
ĐG : Alphapharm Party Ltd. , http://www.alphapharm.com.au
CTHH: C20H27N5O2
PTK: 369.4607
Cilostazol is a medication used in the alleviation of the symptom of intermittent claudication in individuals with peripheral vascular disease. It is manufactured by Otsuka Pharmaceutical Co. under the trade name Pletal. Although drugs similar to cilostazol have increased the risk of death in patients with congestive heart failure, studies of significant size have not addressed people without the disease. [Wikipedia]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C20H27N5O2
Phân tử khối
369.4607
Monoisotopic mass
369.216475133
InChI
InChI=1S/C20H27N5O2/c26-20-12-9-15-14-17(10-11-18(15)21-20)27-13-5-4-8-19-22-23-24-25(19)16-6-2-1-3-7-16/h10-11,14,16H,1-9,12-13H2,(H,21,26)
InChI Key
InChIKey=RRGUKTPIGVIEKM-UHFFFAOYSA-N
IUPAC Name
6-[4-(1-cyclohexyl-1H-1,2,3,4-tetrazol-5-yl)butoxy]-1,2,3,4-tetrahydroquinolin-2-one
Traditional IUPAC Name
cilostazol
SMILES
O=C1CCC2=C(N1)C=CC(OCCCCC1=NN=NN1C1CCCCC1)=C2
Độ tan chảy
160 °C
Độ hòa tan
3.24e-02 g/l
logP
2.3
logS
-4.1
pKa (strongest acidic)
14.42
pKa (Strongest Basic)
-0.51
PSA
81.93 Å2
Refractivity
117.13 m3·mol-1
Polarizability
41.15 Å3
Rotatable Bond Count
7
H Bond Acceptor Count
5
H Bond Donor Count
1
Physiological Charge
0
Number of Rings
4
Bioavailability
1
Rule of Five
true
Ghose Filter
true
MDDR-Like Rule
true
Dược Lực Học : Cilostazol is a quinolinone derivative indicated for the reduction of symptoms of intermittent claudication, as indicated by an increased walking distance. Intermittent claudication is pain in the legs that occurs with walking and disappears with rest. The pain occurs due to reduced blood flow to the legs.
Cơ Chế Tác Dụng : Cilostazol is a medication used in the alleviation of the symptom of intermittent claudication in individuals with peripheral vascular disease. It is manufactured by Otsuka Pharmaceutical Co. under the trade name Pletal. Although drugs similar to cilostazol have increased the risk of death in patients with congestive heart failure, studies of significant size have not addressed people without the disease. [Wikipedia] Cilostazol and several of its metabolites are cyclic AMP (cAMP) phosphodiesterase III inhibitors (PDE III inhibitors), inhibiting phosphodiesterase activity and suppressing cAMP degradation with a resultant increase in cAMP in platelets and blood vessels, leading to inhibition of platelet aggregation and vasodilation.
Dược Động Học :
▧ Absorption :
Cilostazol is absorbed after oral administration. A high fat meal increases absorption, with an approximately 90% increase in Cmax and a 25% increase in AUC. Absolute bioavailability is not known.
▧ Protein binding :
95-98%
▧ Metabolism :
Hepatic. Cilostazol is extensively metabolized by hepatic cytochrome P-450 enzymes, mainly 3A4, and, to a lesser extent, 2C19, with metabolites largely excreted in urine. Two metabolites are active, with one metabolite appearing to account for at least 50% of the pharmacologic (PDE III inhibition) activity after administration of cilostazol.
▧ Route of Elimination :
Cilostazol is extensively metabolized by hepatic cytochrome P-450 enzymes, mainly 3A4, and, to a lesser extent, 2C19, with metabolites largely excreted in urine. Cilostazol is eliminated predominately by metabolism and subsequent urinary excretion of metabolites. The primary route of elimination was via the urine (74%), with the remainder excreted in feces (20%). No measurable amount of unchanged cilostazol was excreted in the urine, and less than 2% of the dose was excreted as 3,4-dehydro-cilostazol. About 30% of the dose was excreted in urine as 4'-trans-hydroxy-cilostazol.
▧ Half Life :
11-13 hours.
Độc Tính : Information on acute overdosage with cilostazol in humans is limited. The signs and symptoms of an acute overdose can be anticipated to be those of excessive pharmacologic effect: severe headache, diarrhea, hypotension, tachycardia, and possibly cardiac arrhythmias. The oral LD50 of cilostazol is >5.0 g/kg in mice and rats and >2.0 g/kg in dogs.
Chỉ Định : For the reduction of symptoms of intermittent claudication (pain in the legs that occurs with walking and disappears with rest).
Tương Tác Thuốc :
  • Diltiazem Diltiazem, a moderate CYP3A4 inhibitor, may increase the serum concentration of cilostazol by decreasing its metabolism. Monitor for changes in the therapeutic and adverse effects of cilostazol if diltiazem is initiated, discontinued or dose changed.
  • Erythromycin Erythromycin increases the effect of cilostazol
  • Fluconazole Fluconazole may decrease the effect of cilostazol.
  • Fluoxetine Fluoxetine, a moderate CYP2C19 inhibitor, may decrease the metabolism of cilostazol. Monitor for changes in the therapeutic and adverse effects of cilostazol if fluoxetine is initiated, discontinued or dose changed.
  • Fluvoxamine Fluvoxamine increases the effect of cilostazol
  • Ginkgo biloba Additive anticoagulant/antiplatelet effects may increase bleed risk. Concomitant therapy should be avoided.
  • Itraconazole Itraconazole may increase the effect of cilostazol.
  • Josamycin Erythromycin increases the effect of cilostazol
  • Ketoconazole Ketoconazole may increase the effect of cilostazol.
  • Nefazodone Nefazodone increases the effect of cilostazol
  • Omeprazole Omeprazole increases the effect of cilostazol
  • Sertraline Sertraline increases the effect of cilostazol
  • Telithromycin Telithromycin may reduce clearance of Cilostazol. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Cilostazol if Telithromycin is initiated, discontinued or dose changed.
  • Ticlopidine Ticlopidine may decrease the metabolism and clearance of Cilostazol. Consider alternate therapy or monitor for adverse/toxic effects of Cilostazol if Ticlopidine is initiated, discontinued or dose changed.
  • Treprostinil The prostacyclin analogue, Treprostinil, increases the risk of bleeding when combined with the antiplatelet agent, Cilostazol. Monitor for increased bleeding during concomitant thearpy.
  • Voriconazole Voriconzole may increase the serum concentration of cilostazol by decreasing its metabolism. Monitor for increased therapeutic/adverse effects of cilostazol and consider reducing the dose during concomitant therapy.
Liều Lượng & Cách Dùng : Tablet - Oral
Dữ Kiện Thương Mại
Giá thị trường
  • Biệt dược thương mại : Cilostazol 100 mg tablet
    Giá bán buôn : USD >1.86
    Đơn vị tính : tablet
  • Biệt dược thương mại : Cilostazol 50 mg tablet
    Giá bán buôn : USD >1.86
    Đơn vị tính : tablet
  • Biệt dược thương mại : Pletal 50 mg tablet
    Giá bán buôn : USD >2.39
    Đơn vị tính : tablet
  • Biệt dược thương mại : Pletal 100 mg tablet
    Giá bán buôn : USD >2.51
    Đơn vị tính : tablet
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Pletaal
  • Công ty :
    Sản phẩm biệt dược : Pletal
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB01166
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=2754
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46506317
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D01896
ChemSpider
http://www.chemspider.com/Chemical-Structure.2652.html
BindingDB
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=50070490
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0378-2979-91
PharmGKB
http://www.pharmgkb.org/drug/PA164746334
Wikipedia
http://en.wikipedia.org/wiki/Cilostazol
RxList
http://www.rxlist.com/cgi/generic/cilostaz.htm
Drugs.com
http://www.drugs.com/cdi/cilostazol.html
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