药品详细
Cilostazol(西洛他唑)
化学结构式图
中文名
西洛他唑
英文名
Cilostazol
分子式
C20H27N5O2
化学名
6-[4-(1-cyclohexyl-1H-1,2,3,4-tetrazol-5-yl)butoxy]-1,2,3,4-tetrahydroquinolin-2-one
分子量
Average: 369.4607
Monoisotopic: 369.216475133
Monoisotopic: 369.216475133
CAS号
73963-72-1
ATC分类
B01A 抗血栓药
药物类型
small molecule
阶段
approved
商品名
同义名
基本介绍
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]
生产厂家
- Actavis totowa llc
- Alphapharm party ltd
- Apotex inc etobicoke site
- Breckenridge pharmaceutical inc
- Corepharma llc
- Ivax pharmaceuticals inc sub teva pharmaceuticals usa
- Mutual pharmaceutical co inc
- Mylan pharmaceuticals inc
- Otsuka pharmaceutical co ltd
- Pliva hrvatska doo
- Roxane laboratories inc
- Sandoz inc
- Teva pharmaceuticals usa inc
封装厂家
- Alphapharm Party Ltd.
- Apotex Inc.
- Breckenridge Pharmaceuticals
- Corepharma LLC
- Diversified Healthcare Services Inc.
- Eon Labs
- Heartland Repack Services LLC
- Murfreesboro Pharmaceutical Nursing Supply
- Mylan
- Otsuka America
- Physicians Total Care Inc.
- Prasco Labs
- Resource Optimization and Innovation LLC
- Roxane Labs
- Stat Rx Usa
- Teva Pharmaceutical Industries Ltd.
- UDL Laboratories
- United Research Laboratories Inc.
- Vangard Labs Inc.
参考
| Synthesis Reference | Not Available |
| General Reference | Not Available |
剂型
规格
化合物类型
| Type | small molecule |
| Classes |
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适应症
药理
| Indication | For the reduction of symptoms of intermittent claudication (pain in the legs that occurs with walking and disappears with rest). | ||||||
| Pharmacodynamics | 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. | ||||||
| Mechanism of action | 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. | ||||||
| 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. | ||||||
| Volume of distribution | Not Available | ||||||
| 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.
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| 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. | ||||||
| Clearance | Not Available | ||||||
| Toxicity | 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. | ||||||
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理化性质
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| State | solid | ||||||||||||||||||||||||||||||||||||||||||
| Experimental Properties |
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药物相互作用
| Drug | Interaction |
|---|---|
| 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. |
食物相互作用
- Grapefruit and grapefruit juice should be avoided throughout treatment, grapefruit can significantly increase serum levels of this product.
- Take on an empty stomach, a lipid rich meal will increase absorption.
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