药品详细
Gemfibrozil (吉非罗齐 )
化学结构式图
中文名
吉非罗齐
英文名
Gemfibrozil
分子式
Not Available
化学名
5-(2,5-dimethylphenoxy)-2,2-dimethylpentanoic acid
分子量
Average: 250.3334
Monoisotopic: 250.156894570
Monoisotopic: 250.156894570
CAS号
25812-30-0
ATC分类
C10A 未知
药物类型
small molecule
阶段
商品名
Apo-Gemfibrozil;Bolutol;Cholespid;Decrelip;Fibratol;Fibrocit;Gemfibril;Gemfibromax;Gemlipid;Gen-Fibro;Genlip;Gevilon;Hipolixan;Jezil;Lipozid;Lipur;Lopid;Novo-Gemfibrozil;Nu-Gemfibrozil;
同义名
基本介绍
A lipid-regulating agent that lowers elevated serum lipids primarily by decreasing serum triglycerides with a variable reduction in total cholesterol. These decreases occur primarily in the VLDL fraction and less frequently in the LDL fraction. Gemfibrozil increases HDL subfractions HDL2 and HDL3 as well as apolipoproteins A-I and A-II. Its mechanism of action has not been definitely established. [PubChem]
生产厂家
- Apotex inc
- Dava pharmaceuticals inc
- Impax pharmaceuticals
- Invagen pharmaceuticals inc
- Mylan pharmaceuticals inc
- Perrigo r and d co
- Pfizer pharmaceuticals ltd
- Purepac pharmaceutical co
- Sandoz inc
- Sun pharmaceutical industries inc
- Teva pharmaceuticals usa inc
- Watson laboratories inc
封装厂家
参考
| Synthesis Reference | Not Available |
| General Reference | Not Available |
剂型
| Form | Route | Strength |
|---|---|---|
| Capsule | Oral | |
| Tablet | Oral |
规格
| Unit description | Cost | Unit |
|---|---|---|
| Gemfibrozil powder | 2.88 USD | g |
| Lopid 600 mg tablet | 2.07 USD | tablet |
| Gemfibrozil 600 mg tablet | 1.8 USD | tablet |
| Apo-Gemfibrozil 600 mg Tablet | 0.65 USD | tablet |
| Mylan-Gemfibrozil 600 mg Tablet | 0.65 USD | tablet |
| Novo-Gemfibrozil 600 mg Tablet | 0.65 USD | tablet |
| Nu-Gemfibrozil 600 mg Tablet | 0.65 USD | tablet |
| Pms-Gemfibrozil 600 mg Tablet | 0.65 USD | tablet |
| Lopid 300 mg Capsule | 0.58 USD | capsule |
| Apo-Gemfibrozil 300 mg Capsule | 0.31 USD | capsule |
| Mylan-Gemfibrozil 300 mg Capsule | 0.31 USD | capsule |
| Novo-Gemfibrozil 300 mg Capsule | 0.31 USD | capsule |
| Nu-Gemfibrozil 300 mg Capsule | 0.31 USD | capsule |
| Pms-Gemfibrozil 300 mg Capsule | 0.31 USD | capsule |
化合物类型
| Type | small molecule |
| Classes |
|
| Substructures |
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适应症
hyperlipidemi 高血脂;
药理
| Indication | For treatment of adult patients with very high elevations of serum triglyceride levels (types IV and V hyperlipidemia) who are at risk of developing pancreatitis (inflammation of the pancreas) and who do not respond adequately to a strict diet. |
| Pharmacodynamics | Gemfibrozil, a fibric acid antilipemic agent similar to clofibrate, is used to treat hyperlipoproteinemia and as a second-line therapy for type IIb hypercholesterolemia. It acts to reduce triglyceride levels, reduce VLDL levels, reduce LDL levels (moderately), and increase HDL levels (moderately). |
| Mechanism of action | Gemfibrozil increases the activity of extrahepatic lipoprotein lipase (LL), thereby increasing lipoprotein triglyceride lipolysis. It does so by activating Peroxisome proliferator-activated receptor-alpha (PPARα) 'transcription factor ligand', a receptor that is involved in metabolism of carbohydrates and fats, as well as adipose tissue differentiation. This increase in the synthesis of lipoprotein lipase thereby increases the clearance of triglycerides. Chylomicrons are degraded, VLDLs are converted to LDLs, and LDLs are converted to HDL. This is accompanied by a slight increase in secretion of lipids into the bile and ultimately the intestine. Gemfibrozil also inhibits the synthesis and increases the clearance of apolipoprotein B, a carrier molecule for VLDL. |
| Absorption | Well absorbed from gastrointestinal tract (within 1-2 hours). |
| Volume of distribution | Not Available |
| Protein binding | 95% |
| Metabolism |
Hepatic. Gemfibrozil mainly undergoes oxidation of a ring methyl group to successively form a hydroxymethyl and a carboxyl metabolite. |
| Route of elimination | Approximately seventy percent of the administered human dose is excreted in the urine, mostly as the glucuronide conjugate, with less than 2% excreted as unchanged gemfibrozil. |
| Half life | 1.5 hours |
| Clearance | Not Available |
| Toxicity | Oral, mouse: LD50 = 3162 mg/kg. Symptoms of overdose include abdominal cramps, diarrhea, joint and muscle pain, nausea, and vomiting. |
| Affected organisms |
|
| Pathways | Not Available |
理化性质
| Properties | |||||||||||||||||||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| State | solid | ||||||||||||||||||||||||||||||||||||
| Melting point | 61-63 oC | ||||||||||||||||||||||||||||||||||||
| Experimental Properties |
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| Predicted Properties |
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药物相互作用
| Drug | Interaction |
|---|---|
| Acenocoumarol | Gemfibrozil may increase the anticoagulant effect of acenocoumarol. |
| Anisindione | Gemfibrozil may increase the anticoagulant effect of anisindione. |
| Atorvastatin | Increased risk of myopathy/rhabdomyolysis |
| Cerivastatin | Increased risk of myopathy/rhabdomyolysis |
| Dicumarol | Gemfibrozil may increase the anticoagulant effect of dicumarol. |
| Fluvastatin | Increased risk of myopathy/rhabdomyolysis |
| Glimepiride | Gemfibrozil increases the effect and toxicity of rosiglitazone/pioglitazone |
| Lovastatin | Increased risk of myopathy/rhabdomyolysis |
| Pioglitazone | Gemfibrozil may increase the effect and toxicity of pioglitazone. |
| Pravastatin | Increased risk of myopathy/rhabdomyolysis |
| Repaglinide | Gemfibrozil may increase the effect and toxicity of repaglinide. |
| Rosiglitazone | Increases the effect and toxicity of rosiglitazone/pioglitazone |
| Rosuvastatin | Gemfibrozil may increase the therapeutic and toxic effects of rosuvastatin. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of rosuvastatin if gemfibrozil is initiated, discontinued or dose changed. |
| Simvastatin | Increased risk of myopathy/rhabdomyolysis |
| Tacrine | The metabolism of Tacrine, a CYP1A2 substrate, may be reduced by Gemfibrozil, a CYP1A2 inhibitors. Monitor the efficacy and toxicity of Tacrine if Gemfibrozil is initiated, discontinued or if the dose is changed. |
| Tamoxifen | Gemfibrozil may reduce clearance rate of Tamoxifen. Monitor for changes in therapeutic/adverse effects of Tamoxifen if Gemfibrozil is initiated, discontinued or dose changed. |
| Tizanidine | Gemfibrozil may decrease the metabolism and clearance of Tizanidine. Consider alternate therapy or use caution during co-administration. |
| Tolbutamide | Gemfibrozil, a strong CYP2C9 inhibitor, may decrease the metabolism and clearance of Tolbutamide, a CYP2C9 substrate. Consider alternate therapy or monitor for changes in Tolbutamide therapeutic and adverse effects if Gemfibrozil is initiated, discontinued or dose changed. |
| Torasemide | Gemfibrozil, a strong CYP2C9 inhibitor, may increase the serum concentration of Torasemide, a CYP2C9 substrate, by decreasing Torasemide metabolism and clearance. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of Torasemide if Gemfibrozil is initiated, discontinued or dose changed. |
| Tretinoin | The strong CYP2C8 inhibitor, Gemfibrozil, may decrease the metabolism and clearance of oral Tretinoin. Consider alternate therapy or monitor for changes in Tretinoin effectiveness and adverse/toxic effects if Gemfibrozil is initiated, discontinued to dose changed. |
| Trimethoprim | The strong CYP2C9 inhibitor, Gemfibrozil, may decrease the metabolism and clearance of Trimethoprim, a CYP2C9 substrate. Consider alternate therapy or monitor for changes in therapeutic and adverse effects of Trimethoprim if Gemfibrozil is initiated, discontinued or dose changed. |
| Trimipramine | The strong CYP2C19 inhibitor, Gemfibrozil, may decrease the metabolism and clearance of Trimipramine, a CYP2C19 substrate. Consider alternate therapy or monitor for changes in therapeutic and adverse effects of Trimipramine if Gemfibrozil is initiated, discontinued or dose changed. |
| Ursodeoxycholic acid | The fibric acid derivative decreases the effect of ursodiol |
| Voriconazole | Gemfibrozil, a strong CYP2C9 inhibitor, may increase the serum concentration of voriconazole by decreasing its metabolism. Monitor for changes in the therapeutic and adverse effects of voriconazole if gemfibrozil is initiated, discontinued or dose changed. |
| Warfarin | Gemfibrozil, a strong CYP2C9 inhibitor, may decrease the metabolism of warfarin. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of warfarin if gemfibrozil is initiated, discontinued or dose changed. |
| Zafirlukast | Gemfibrozil, a strong CYP2C9 inhibitor, may decrease the metabolism and clearance of zafirlukast. Consider alternate therapy or monitor for changes in zafirlukast therapeutic and adverse effects if gemfibrozil is initiated, discontinued or dose changed. |
食物相互作用
- Take 30 minutes before meals.
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