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药品详细

Lovastatin (洛伐他汀 )

化学结构式图
中文名
洛伐他汀
英文名
Lovastatin
分子式
Not Available
化学名
(1S,3R,7S,8S,8aR)-8-{2-[(2R,4R)-4-hydroxy-6-oxooxan-2-yl]ethyl}-3,7-dimethyl-1,2,3,7,8,8a-hexahydronaphthalen-1-yl (2S)-2-methylbutanoate
分子量
Average: 404.5396
Monoisotopic: 404.256274262
CAS号
75330-75-5
ATC分类
C10A 未知
药物类型
small molecule
阶段
商品名
Altocor;Altoprev;Artein;Belvas;Cholestra;Closterol;Colevix;Hipolip;Hipovastin;Lestatin;Lipdip;Lipivas;Lipofren;Lovalip;Lovalord;Lovasterol;Lovastin;Lozutin;Mevacor;Mevinacor;Mevlor;Monacolin K;Nergadan;Paschol;Rodatin;Rovacor;Sivlor;Taucor;Tecnolip;Teroltrat;
同义名
6 alpha-Methylcompactin;lovastatin;Lovastatina [Spanish];Lovastatine [French];Lovastatinum [Latin];
基本介绍

A fungal metabolite isolated from cultures of Aspergillus terreus. The compound is a potent anticholesteremic agent. It inhibits 3-hydroxy-3-methylglutaryl coenzyme A reductase (hydroxymethylglutaryl COA reductases), which is the rate-limiting enzyme in cholesterol biosynthesis. It also stimulates the production of low-density lipoprotein receptors in the liver. [PubChem]

生产厂家
  • Actavis elizabeth llc
  • Andrx labs llc
  • Apotex inc
  • Carlsbad technology inc
  • Lupin ltd
  • Merck research laboratories div merck co inc
  • Mutual pharmaceutical co inc
  • Mylan pharmaceuticals inc
  • Sandoz inc
  • Teva pharmaceuticals usa inc
封装厂家
参考
Synthesis Reference Not Available
General Reference
  1. Bobek P, Ozdin L, Galbavy S: Dose- and time-dependent hypocholesterolemic effect of oyster mushroom (Pleurotus ostreatus) in rats. Nutrition. 1998 Mar;14(3):282-6. Pubmed
剂型
Form Route Strength
Tablet Oral
规格
Unit description Cost Unit
Altoprev 60 mg 24 Hour tablet 7.99 USD tablet
Altoprev 60 mg tablet 7.74 USD tablet
Altoprev 20 mg 24 Hour tablet 6.88 USD tablet
Altoprev 20 mg tablet 6.61 USD tablet
Mevacor 40 mg tablet 4.57 USD tablet
Altoprev 40 mg tablet 4.41 USD tablet
Lovastatin 40 mg tablet 4.36 USD tablet
Altoprev 10 mg 24 Hour tablet 3.07 USD tablet
Mevacor 20 mg tablet 2.53 USD tablet
Lovastatin 20 mg tablet 2.42 USD tablet
Altocor 20 mg 24 Hour tablet 2.36 USD tablet
Apo-Lovastatin 40 mg Tablet 2.11 USD tablet
Co Lovastatin 40 mg Tablet 2.11 USD tablet
Mylan-Lovastatin 40 mg Tablet 2.11 USD tablet
Novo-Lovastatin 40 mg Tablet 2.11 USD tablet
Pms-Lovastatin 40 mg Tablet 2.11 USD tablet
Ran-Lovastatin 40 mg Tablet 2.11 USD tablet
Ratio-Lovastatin 40 mg Tablet 2.11 USD tablet
Sandoz Lovastatin 40 mg Tablet 2.11 USD tablet
Mevacor 10 mg tablet 1.65 USD tablet
Lovastatin 10 mg tablet 1.37 USD tablet
Apo-Lovastatin 20 mg Tablet 1.14 USD tablet
Co Lovastatin 20 mg Tablet 1.14 USD tablet
Mylan-Lovastatin 20 mg Tablet 1.14 USD tablet
Novo-Lovastatin 20 mg Tablet 1.14 USD tablet
Pms-Lovastatin 20 mg Tablet 1.14 USD tablet
Ran-Lovastatin 20 mg Tablet 1.14 USD tablet
Ratio-Lovastatin 20 mg Tablet 1.14 USD tablet
Sandoz Lovastatin 20 mg Tablet 1.14 USD tablet
化合物类型
Type small molecule
Classes
  • Statins
Substructures
  • Statins
  • Carboxylic Acids and Derivatives
  • Hydroxy Compounds
  • Alkanes and Alkenes
  • Pyrans
  • Acetates
  • Lactones
  • Ethers
  • Isoprenes
  • Heterocyclic compounds
  • Alcohols and Polyols
  • Cyclohexenes and Derivatives
适应症
hyperlipidemi 高血脂;
药理
Indication For management as an adjunct to diet to reduce elevated total-C, LDL-C, apo B, and TG levels in patients with primary hypercholesterolemia and mixed dyslipidemia; For primary prevention of coronary heart disease
Pharmacodynamics Lovastatin, an antilipemic agent produced by fermentation of Aspergillus terreus, is the first of a class of lipid-lowering agents known as the HMG-CoA reductase inhibitors. Lovastatin is used to treat hypercholesterolemia, to slow coronary atherosclerosis, and to prevent myocardial infarction and stroke. Lovastatin, like simvastin and unlike pravastatin, is a prodrug, concentrating active drug in the liver during first-pass circulation.
Mechanism of action Lovastatin is a lactone that is readily hydrolyzed in vivo to the corresponding b-hydroxyacid, a potent inhibitor of HMG-CoA reductase, the enzyme that catalyzes the conversion of HMG-CoA to mevalonate. The conversion of HMG-CoA to mevalonate is an early step in the biosynthetic pathway for cholesterol.
Absorption 30%
Volume of distribution Not Available
Protein binding >95%
Metabolism

hepatic
Route of elimination Lovastatin undergoes extensive first-pass extraction in the liver, its primary site of action, with subsequent excretion of drug equivalents in the bile.
Half life 5.3 hours
Clearance Not Available
Toxicity LD50>1000 mg/kg (orally in mice)
Affected organisms
  • Humans and other mammals
Pathways
Pathway Name SMPDB ID
Smp00099 Lovastatin Pathway SMP00099
理化性质
Properties
State solid
Melting point 174.5 oC
Experimental Properties
Property Value Source
water solubility 0.0004 mg/mL PhysProp
logP 4.5 PhysProp
Predicted Properties
Property Value Source
water solubility 2.43e-02 g/l ALOGPS
logP 4.11 ALOGPS
logP 3.90 ChemAxon Molconvert
logS -4.22 ALOGPS
pKa ChemAxon Molconvert
hydrogen acceptor count 3 ChemAxon Molconvert
hydrogen donor count 1 ChemAxon Molconvert
polar surface area 72.83 ChemAxon Molconvert
rotatable bond count 7 ChemAxon Molconvert
refractivity 113.18 ChemAxon Molconvert
polarizability 46.11 ChemAxon Molconvert
药物相互作用
Drug Interaction
Acenocoumarol Lovastatin may increase the anticoagulant effect of acenocoumarol. Monitor for changes in the therapeutic and adverse effects of acenocoumarol if lovastatin is initiated, discontinued or dose changed.
Amprenavir Amprenavir may increase the serum concentration of the lovastatin. Concomitant therapy is contraindicated.
Anisindione Lovastatin may increase the anticoagulant effect of anisindione. Monitor for changes in the therapeutic and adverse effects of anisindione if lovastatin if initiated, discontinued or dose changed.
Atazanavir Atazanavir may increase the effect and toxicity of lovastatin. Concomitant therapy is contraindicated.
Azithromycin The macrolide antibiotic, azithromycin, may increase the serum concentration of lovastatin by decreasing its metabolism. Monitor for changes in the therapeutic and adverse effects of lovastatin if azithromycin is initiated, discontinued or dose changed.
Bezafibrate Increased risk of myopathy/rhabdomyolysis
Bosentan Bosentan may decrease the serum concentration of lovastatin by increasing its metabolism. Monitor for changes in the therapeutic and adverse effects of lovastatin if bosentan is initiated, discontinued or dose changed.
Carbamazepine Carbamazepine, a p-glycoprotein inducer and strong CYP3A4 inducer, may decrease the effect of lovastatin by increasing its efflux and metabolism. Monitor for changes in the therapeutic and adverse effects of lovastatin if carbamazepine is initiated, discontinued or dose changed.
Clarithromycin The macrolide, clarithromycin, may increase the toxicity of the statin, lovastatin.
Colchicine Increased risk of rhabdomyolysis with this combination
Cyclosporine Possible myopathy and rhabdomyolysis
Danazol Risk of severe myopathy/rhabdomyolysis with this combination
Darunavir Darunavir may increase the effect and toxicity of lovastatin. Concomitant therapy is contraindicated.
Delavirdine Delavirdine, a strong CYP3A4 inhibitor, may increase the serum concentration of lovastatin by decreasing its metabolism. Monitor for changes in the therapeutic and adverse effects of lovastatin if delavirdine is initiated, discontinued or dose changed.
Dicumarol Lovastatin may increase the anticoagulant effect dicumarol. Monitor for changes in the therapeutic and adverse effects of dicumarol if lovastatin is initiated, discontinued or dose changed.
Diltiazem Diltiazem may increase the serum concentration of lovastatin. Lovastatin 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.
Efavirenz Efavirenz may decrease the serum concentration of lovastatin by increasing its metabolism. Monitor for changes in the therapeutic and adverse effects of lovastatin if efavirenz is initiated, discontinued or dose changed.
Erythromycin The macrolide, erythromycin, may increase the toxicity of the statin, lovastatin.
Fenofibrate Increased risk of myopathy/rhabdomyolysis
Fluconazole Increased risk of myopathy/rhabdomyolysis
Fosamprenavir Fosamprenavir, a strong CYP3A4 inhibitor, may increase the effect and toxicity of lovastatin by decreasing its metabolism. Concomitant therapy is contraindicated.
Gemfibrozil Increased risk of myopathy/rhabdomyolysis
Imatinib Imatinib, a strong CYP3A4 inhibitor, may increase the effect and toxicity of lovastatin by decreasing its metabolism. Monitor for changes in the therapeutic and adverse effects of lovastatin if imatinib is initiated, discontinued or dose changed.
Indinavir Indinavir may increase the effect and toxicity of lovastatin. Concomitant therapy is contraindicated.
Itraconazole Increased risk of myopathy/rhabdomyolysis
Josamycin The macrolide, josamycin, may increase the toxicity of the statin, lovastatin.
Ketoconazole Increased risk of myopathy/rhabdomyolysis
Nefazodone Nefazodone, a strong CYP3A4 inhibitor, may increase the serum concentration of lovastatin by decreasing its metabolism. Monitor for changes in the therapeutic and adverse effects of lovastatin if nefazodone is initiated, discontinued or dose changed.
Nelfinavir Nelfinavir may increase the effect and toxicity of lovastatin. Concomitant therapy is contraindicated.
Nevirapine The strong CYP3A4 inducer, nevirapine, may decrase the effect of lovastatin by increasing its metabolism. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of lovastatin if nevirapine is initiated, discontinued or dose changed.
Niacin Risk of severe myopathy/rhabdomyolysis with this combination
Quinupristin This combination presents an increased risk of toxicity
Rifabutin Rifabutin may decrease the effect of lovastatin by increasing its metabolism. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of lovastatin if rifabutin is initiated, discontinued or dose changed.
Rifampin Rifampin may decrease the effect of lovastatin by increasing its metabolism. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of lovastatin if rifampin is initiated, discontinued or dose changed.
Ritonavir Ritonavir may increase the effect and toxicity of lovastatin. Concomitant therapy is contraindicated.
Saquinavir Saquinavir may increase the effect and toxicity of lovastatin. Concomitant therapy is contraindicated.
Telithromycin Telithromycin may increase the adverse effects of lovastatin by decreasing its metabolism. Concomitant therapy should be avoided.
Tipranavir Tipranavir, co-administered with Ritonavir, may increase the plasma concentration of Lovastatin. Concomitant therapy is contraindicated.
Verapamil Verapamil, a moderate CYP3A4 inhibitor, may increase the serum concentration of Lovastatin by decreasing its metabolism. Avoid concurrent use if possible or reduce lovastatin dose during concomitant therapy. Monitor for changes in the therapeutic/adverse effects of Lovastatin if Verapamil is initiated, discontinued or dose changed.
Voriconazole Voriconazole, a strong CYP3A4 inhibitor, may increase the serum concentration of lovastatin by decreasing its metabolism. Monitor for changes in the therapeutic and adverse effects of lovastatin if voriconazole is initiated, discontinued or dose changed.
Warfarin Lovastatin may increase the anticoagulant effect warfarin. Monitor for changes in the therapeutic and adverse effects of warfarin if lovastatin is initiated, discontinued or dose changed .
食物相互作用
  • Avoid alcohol.
  • Avoid drastic changes in dietary habit.
  • Avoid taking with grapefruit juice.
  • Take with food, 50% increase in bioavailability when taken with food.

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