药品详细
Cerivastatin (Cerivastatin )
化学结构式图
中文名
Cerivastatin
英文名
Cerivastatin
分子式
Not Available
化学名
(3R,5S,6E)-7-[4-(4-fluorophenyl)-5-(methoxymethyl)-2,6-bis(propan-2-yl)pyridin-3-yl]-3,5-dihydroxyhept-6-enoic acid
分子量
Average: 459.5503
Monoisotopic: 459.242101408
Monoisotopic: 459.242101408
CAS号
145599-86-6
ATC分类
C10A 未知
药物类型
small molecule
阶段
商品名
Baycol;Lipobay;Rivastatin;
同义名
Cerivastatin sodium;Cerivastatin, sodium salt;
基本介绍
On August 8, 2001 the U.S. Food and Drug Administration (FDA) announced that Bayer Pharmaceutical Division voluntarily withdrew Baycol from the U.S. market, due to reports of fatal Rhabdomyolysis, a severe adverse reaction from this cholesterol-lowering (lipid-lowering) product. It has also been withdrawn from the Canadian market.
生产厂家
- Bayer pharmaceuticals corp
封装厂家
参考
| Synthesis Reference | Not Available |
| General Reference |
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剂型
| Form | Route | Strength |
|---|---|---|
| Tablet | Oral |
规格
化合物类型
| Type | small molecule |
| Classes |
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| Substructures |
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适应症
hyperlipidemi 高血脂;
药理
| Indication | Used as an adjunct to diet for the reduction of elevated total and LDL cholesterol levels in patients with primary hypercholesterolemia and mixed dyslipidemia (Fredrickson Types IIa and IIb) when the response to dietary restriction of saturated fat and cholesterol and other non-pharmacological measures alone has been inadequate. | ||||||||||||||||||||
| Pharmacodynamics | Cerivastatin, a competitive HMG-CoA reductase inhibitor effective in lowering LDL cholesterol and triglycerides, is used to treat primary hypercholesterolemia and mixed dyslipidemia (Fredrickson types IIa and IIb). | ||||||||||||||||||||
| Mechanism of action | Cerivastatin competitively inhibits hydroxymethylglutaryl-coenzyme A (HMG-CoA) reductase, the hepatic enzyme responsible for converting HMG-CoA to mevalonate. As mevalonate is a precursor of sterols such as cholesterol, this results in a decrease in cholesterol in hepatic cells, upregulation of LDL-receptors, and an increase in hepatic uptake of LDL-cholesterol from the circulation. | ||||||||||||||||||||
| Absorption | The mean absolute oral bioavailability 60% (range 39 - 101%). | ||||||||||||||||||||
| Volume of distribution | Not Available | ||||||||||||||||||||
| Protein binding | More than 99% of the circulating drug is bound to plasma proteins (80% to albumin). | ||||||||||||||||||||
| Metabolism |
Hepatic. Biotransformation pathways for cerivastatin in humans include the following: demethylation of the benzylic methyl ether to form Ml and hydroxylation of the methyl group in the 6'-isopropyl moiety to form M23.
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| Route of elimination | Not Available | ||||||||||||||||||||
| Half life | 2-3 hours | ||||||||||||||||||||
| Clearance | Not Available | ||||||||||||||||||||
| Toxicity | Rhabdomyolysis, liver concerns | ||||||||||||||||||||
| Affected organisms |
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| Pathways |
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理化性质
| Properties | |||||||||||||||||||||||||||||||||||||
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| State | solid | ||||||||||||||||||||||||||||||||||||
| Melting point | Not Available | ||||||||||||||||||||||||||||||||||||
| Experimental Properties |
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| Predicted Properties |
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药物相互作用
| Drug | Interaction |
|---|---|
| Bezafibrate | Increased risk of myopathy/rhabdomyolysis |
| Bosentan | Bosentan may decrease the serum concentration of cerivastatin by increasing its metabolism. Monitor for changes in the therapeutic and adverse effects of cerivastatin if bosentan is initiated, discontinued or dose changed. |
| Clarithromycin | The macrolide, clarithromycin, may increase the toxicity of the statin, cerivastatin. |
| Colchicine | Increased risk of rhabdomyolysis with this combination |
| Cyclosporine | Possible myopathy and rhabdomyolysis |
| Diltiazem | Diltiazem may increase the serum concentration of cerivastatin. Cerivastatin may increase the serum concentration of diltiazem. Monitor for changes in the therapeutic and adverse effects of both agents if concomitant therapy is initiated, discontinued or if doses are changed. |
| Erythromycin | The macrolide, erythromycin, may increase the toxicity of the statin, cerivastatin. |
| Fenofibrate | Increased risk of myopathy/rhabdomyolysis |
| Gemfibrozil | Increased risk of myopathy/rhabdomyolysis |
| Imatinib | Imatinib, a strong CYP3A4 inhibitor, may increase the serum concentration of cerivastatin by decreasing its metabolism. Monitor for changes in the therapeutic and adverse effects of cerivastatin if imatinib is initiated, discontinued or dose changed. |
| Itraconazole | Increased risk of myopathy/rhabdomyolysis |
| Josamycin | The macrolide, josamycin, may increase the toxicity of the statin, cerivastatin. |
| Ketoconazole | Increased risk of myopathy/rhabdomyolysis |
| Nefazodone | Nefazodone, a strong CYP3A4 inhibitor, may increase the serum concentration of cerivastatin by decreasing its metabolism. Monitor for changes in the therapeutic and adverse effects of cerivastatin if nefazodone is initiated, discontinued or dose changed. |
| Quinupristin | This combination presents an increased risk of toxicity |
| Rifabutin | Rifabutin may decrease the effect of cerivastatin by increasing its metabolism. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of cerivastatin if rifabutin is initiated, discontinued or dose changed. |
| Rifampin | Rifampin may decrease the effect of cerivastatin by increasing its metabolism. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of cerivastatin if rifampin is initiated, discontinued or dose changed. |
食物相互作用
- Grapefruit and grapefruit juice should be avoided throughout treatment as grapefruit can significantly increase serum levels of this product.
- Take without regard to meals.
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