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Lovastatin
drug data and news
Lovastatin drug data, resources, and news articles (when available). Onconews.org provides news on cancer research. This section, which includes profiles on medicines that may or not be cancer-related is in beta form. If things run smoothly we will be releasing a new format late in the summer of 2006.
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| Generic name | Lovastatin | ||
| Brand Names/Synonyms | 6alpha-Methylcompactin; Altocor; Altoprev; Artein; Belvas; Cholestra; Closterol; Colevix; Compactin; HSDB 6534; Hipolip; Hipovastin; Lestatin; Lipdip; Lipivas; Lipofren; Lovalip; Lovalord; Lovastatin; Lovastatin [Usan:Ban:Inn]; Lovastatina [Spanish]; Lovastatine [French]; Lovastatinum [Latin]; Lovasterol; Lovastin; Lozutin; MK 803; MK-803; ML-530B; MSD 803; Mevacor; Mevastatin; Mevinacor; Mevinolin; Mevlor; Monacolin K; Nergadan; Paschol; Pravastatin; Rodatin; Rovacor; Sivlor; Taucor; Tecnolip; Teroltrat | ||
| 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 | ||
| Sponsored links | Description | Not Available | |
| Pharmacology | 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. | ||
| Lovastatin News (When available) |
Multimedia News Release - Heart Failure Society Supports the Use ... Feb 23, 2006 NitroMed Reports Financial Results for Fourth Quarter and Full ... Mar 2, 2006 NitroMed to Present at the SG Cowen & Co. Health Care Conference ... Feb 28, 2006 Rotarix Approved In Europe; Avant Due $40M At Launch Feb 27, 2006 NitroMed to Host Fourth Quarter and Year End 2005 Earnings Call ... Feb 22, 2006 New Guidelines Released for Heart Failure Treatment Feb 16, 2006 New Guidelines Released for Heart Failure Treatment Feb 16, 2006 What is Viagra Feb 13, 2006 Smoking Out Cliches About Race Feb 2, 2006 NitroMed to Present at BIO CEO & Investor Conference; February 14 ... Feb 7, 2006 Smoking Out Cliches About Race Feb 2, 2006 NitroMed Announces Sale of Common Stock Jan 25, 2006 NitroMed Sells Stock Jan 25, 2006 Gerald W. Bruce Joins NitroMed as Vice President, Sales Jan 17, 2006 NitroMed $62.5M Placement Supporting Growth Of BiDil Jan 25, 2006 NitroMed Announces Optimization of BiDil(R) Contract Sales Force Jan 20, 2006 NitroMed Promotes Michael Sabolinski, MD to the Position of Chief ... Jan 7, 2006 FDA Approves Heart Drug for Black Patients Dec 10, 2005 Columbia doctor supports heart medication that is aimed at blacks Dec 11, 2005 BiDil(R) Data to be Presented at American Heart Association ... Nov 11, 2005 Burrell Named Consumer Agency of Record for NitroMed; Account ... Nov 27, 2005 Researchers Seek to Determine Whether Genetic Variations May ... Sep 21, 2005 NitroMed Presents BiDil(R) Data on Reverse Remodeling in Heart ... Sep 21, 2005 Medicine stocks abysmal at Bengal public hospitals Oct 5, 2005 New Research: Sticky Liquids Could Help Treat Gut Problems Sep 26, 2005 Welton O'Neal, Jr., Pharm.D. Joins NitroMed as Vice President ... Sep 12, 2005 NitroMed to Present at UBS Global Life Sciences Conference ... Sep 20, 2005 | ||
| Dosage Forms | Tablet | ||
| Drug_Category | Antineoplastic Agents; Anticholesteremic Agents; HMG-CoA Reductase Inhibitors; ATC:C10AA02 | ||
| Absorption | 30% | ||
| Interactions | DRUG INTERACTIONS CYP3A4 Interactions Lovastatin is metabolized by CYP3A4 but has no CYP3A4 inhibitory activity; therefore it is not expected to affect the plasma concentrations of other drugs metabolized by CYP3A4. Potent inhibitors of CYP3A4 (below) increase the risk of myopathy by reducing the elimination of lovastatin. Pharmacokinetics. Itraconazole Ketoconazole Erythromycin Clarithromycin Telithromycin HIV protease inhibitors Nefazodone Cyclosporine Large quantities of grapefruit juice (>1 quart daily) Interactions with lipid-lowering drugs that can cause myopathy when given alone. The risk of myopathy is also increased by the following lipid-lowering drugs that are not potent CYP3A4 inhibitors, but which can cause myopathy when given alone. See WARNINGS, Myopathy/Rhabdomyolysis. Gemfibrozil Other fibrates Niacin (nicotinic acid) (=1 g/day) Other drug interactions Danazol: The risk of myopathy/rhabdomyolysis is increased by concomitant administration of danazol particularly with higher doses of lovastatin (see WARNINGS, Myopathy/Rhabdomyolysis). Amiodarone or Verapamil: The risk of myopathy/rhabdomyolysis is increased when either amiodarone or verapamil is used concomitantly with a closely related member of the HMG-CoA reductase inhibitor class (see WARNINGS, Myopathy/Rhabdomyolysis). Coumarin Anticoagulants: In a small clinical trial in which lovastatin was administered to warfarin treated patients, no effect on prothrombin time was detected. However, another HMG-CoA reductase inhibitor has been found to produce a less than two-second increase in prothrombin time in healthy volunteers receiving low doses of warfarin. Also, bleeding and/or increased prothrombin time have been reported in a few patients taking coumarin anticoagulants concomitantly with lovastatin. It is recommended that in patients taking anticoagulants, prothrombin time be determined before starting lovastatin and frequently enough during early therapy to insure that no significant alteration of prothrombin time occurs. Once a stable prothrombin time has been documented, prothrombin times can be monitored at the intervals usually recommended for patients on coumarin anticoagulants. If the dose of lovastatin is changed, the same procedure should be repeated. Lovastatin therapy has not been associated with bleeding or with changes in prothrombin time in patients not taking anticoagulants. Propranolol: In normal volunteers, there was no clinically significant pharmacokinetic or pharmacodynamic interaction with concomitant administration of single doses of lovastatin and propranolol. Digoxin: In patients with hypercholesterolemia, concomitant administration of lovastatin and digoxin resulted in no effect on digoxin plasma concentrations. Oral Hypoglycemic Agents: In pharmacokinetic studies of MEVACOR in hypercholesterolemic noninsulin dependent diabetic patients, there was no drug interaction with glipizide or with chlorpropamide | ||
| Toxicity | LD50>1000 mg/kg (orally in mice) | ||
| Organisms Affected | Humans and other mammals | ||
| Chemical IUPAC Name | [8-[2-(4-hydroxy-6-oxo-oxan-2-yl)ethyl]-3,7-dimethyl-1,2,3,7,8,8a-hexahydronaphthalen-1-yl] 2-methylbutanoate | ||
| Chemical Formula | C24H36O5 | ||
| Molecular Weight | 404.54 g/mol | ||
| Smiles String | CCC(C)C(=O)OC1CC(C=C2C1C(C(C=C2)C)CCC3CC(CC(=O)O3)O)C | ||
| Melting Point | 174.5 °C | ||
| Water Solubility | 0.0004 mg/mL | ||
| State | white, nonhygroscopic crystalline powder | ||
| LogP/Hphobicity | 4 | ||
| Isoelectric Point | Not Available | ||
| Biotransformation | hepatic | ||
| Half Life | 5.3 hours | ||
| Protein Binding [%] | >95% | ||
| RxList Link | RXlist | ||
| Sponsored links | |||
| Drug Reference |
http://www.drugs.com/cons/Lovastatin.html http://www.rxlist.com/cgi/generic3/altocor.htm | ||
| Drug Type | Approved Drug | ||
| Accession No | APRD00370 | ||
| CAS Registry Number | 75330-75-5 | ||
| KEGG Compound ID | D00359 | ||
| PubChem ID | SID:191104 | ||
| PharmGKB ID | PA450272 | ||
| SwissProt ID | Not Available | ||
| GenBank ID | Not Available | ||
| Drug ID Number [DIN] | 2243127 |
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