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Lovastatin
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DRUG INFO
Lovastatin
Drug Name:
Lovastatin
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
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.
Drug Category: Antineoplastic Agents; Anticholesteremic Agents; HMG-CoA Reductase Inhibitors; ATC:C10AA02
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
Dosage Forms: Tablet
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
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
Half Life: 5.3 hours
Drug Type: Approved Drug
# Accession No: APRD00370
CAS Registry Number: 75330-75-5
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Lovastatin News
(When available)
Studies: Statins Don't Cut Risk of Colon, Other Cancers Jan 9, 2006
ACS News Center, ...statins studied included atorvastatin (Lipitor, Caduet), cerivastatin (Baycol), fluvastatin (Lescol), lovastatin (Advicor, Altoprev, Mevacor), pravastatin ...
Drug companies, scientists head back to nature Jan 12, 2006
Pittsburgh Post Gazette, It was the first statin. Dr. Endo almost immediately ran into a problem: The substance, soon to be dubbed compactin, barely worked in rats. ...
UK and Japanese Scientists Named as Laureates of the 2006(22nd) ... Jan 11, 2006
PR Newswire (press release), In 1973 Dr. Akira Endo isolated from penicillium a ground-breaking substance called ML-236B (currently known as compactin) that lowers blood cholesterol levels ...
UK and Japanese Scientists Named as Laureates of the 2006(22nd) ... Jan 11, 2006
PR Newswire (press release), Development OUTLINE In 1973 Dr. Akira Endo isolated from penicillium a ground-breaking substance called ML-236B (currently known as compactin) that lowers ...
Statin drugs must carry health warning Jan 13, 2006
Toronto Star, The makers of all the drugs, which include Lipitor, Zocor, Pravachol, Mevacor and Crestor, must include a warning and description of the risk in patient safety ...
Health Canada Mandates New Warnings on Statins Regarding Risk of ... Jan 14, 2006
Newsinferno.com, The manufacturers of Lipitor, Zocor, Pravachol, Mevacor, and Crestor are now required to include an enhanced warning about the potential risks posed to ...
Drug firms, scientists go back to nature Jan 10, 2006
Napa Valley Register, ...that Dr. Endo originally discovered shares the same basic chemical structure as three of the biggest-selling anticholesterol drugs: Zocor, Pravachol and Mevacor ...
Statins' anti-cancer benefit discounted Jan 15, 2006
Sun-Sentinel.com, ...of drugs includes such well-known drugs as Lipitor (atorvastatin), Pravachol (pravastatin), Zocor (simvastatin), Lescol (fluvastatin) and Mevacor (lovastatin). ...
MRI SCAN'S ROLE IN DIAGNOSING MULTIPLE SCLEROSIS Jan 5, 2006
Charlotte Sun-Herald, DEAR DR. DONOHUE: I had been on Mevacor for about two years to lower my cholesterol. ... Both Mevacor and Lipitor are similar medicines. ...
Two Studies Show Statins Don't Cut Cancer Risk Jan 4, 2006
Los Angeles Times, Statins are the most commonly prescribed medications in the United States and include Lipitor, Zocor, Mevacor, Crestor, Pravachol and Lescol. ...
Statins ineffective on cancer, studies say Jan 8, 2006
Indianapolis Star, Statins are the most commonly prescribed medications in the US, and as a result possess unrivaled name recognition: Lipitor, Zocor, Mevacor, Crestor, Pravachol ...
Lovastatin reverses learning and attention deficits in a mouse ... Jan 1, 2006
Xagena.it, Researchers have reported evidence that a statin, Lovastatin ( Mevacor ), already shown to be safe for use in humans has proven effective at correcting cell ...
Greater focus on artery disease needed globally Jan 11, 2006
Reuters ...undertreated with medications shown to reduce the risk of heart attack and stroke, such as the popular cholesterol-lowering statin drugs, like Zocor and Mevacor ...
Studies: Statins Don't Cut Risk of Colon, Other Cancers Jan 9, 2006
ACS News Center, ...studied included atorvastatin (Lipitor, Caduet), cerivastatin (Baycol), fluvastatin (Lescol), lovastatin (Advicor, Altoprev, Mevacor), pravastatin (Pravachol ...
Anti-obesity drug may go OTC Dec 20, 2005
Asbury Park Press, ...up.". This past January, an FDA advisory panel voted 20-3 against recommending approval of OTC Mevacor, a cholesterol-lowering drug. ...
Statins do not affect cancer risk, researchers say Jan 3, 2006
Reuters ...the most prescribed drugs in the world, include Pfizer Inc.'s Lipitor, Merck & Co Inc.'s Zocor, Bristol-Myers Squibb's Pravachol, Merck's Mevacor and Novartis ...
Statins do not affect cancer risk, researchers say Jan 3, 2006
Reuters Merck & Co Inc.'s (MRK.N: Quote, Profile, Research) Zocor, Bristol-Myers Squibb's (BMY.N: Quote, Profile, Research) Pravachol, Merck's Mevacor and Novartis ...
Statins don't appear to lower cancer risk Jan 3, 2006
Newsday, ...the most commonly prescribed medications in the United States and as a result possess unrivaled name recognition: Lipitor, Zocor, Mevacor, Crestor, Pravachol ...
Getting the Specifics on Generic Drugs Jan 5, 2006
Forbes Some pharmaceutical blockbusters have already lapsed into generic status. The anti-cholesterol drug Mevacor (lovastatin) has long been generic, Hoey said. ...
No Link Found Between Cholesterol Lowering Drugs and Colorectal ... Jan 3, 2006
BlackHillsPortal.com, ...almost 50 percent. Some of the more commonly prescribed statins are Lipitor, Zocor, Pravachol, Lescol, Mevacor and Crestor. For the ...
Statins and Cancer Prevention: Questions and Answers Jan 4, 2006
Food Consumer, For years, Satins, that include drugs such as Zacor, Crestor, Lipitor, Mevacor, Pravachol and Lescol, were believed to reduce cancer because they reduced ...
Meta-Analysis Rules Out Statin Cancer Prevention Jan 3, 2006
MedPage Today, The studies examined six statins - Mevacor (lovastatin), Lipitor (atorvastatin), Vytorin (simvastatin), Baycol (cerivastatin), Lescol (fluvastatin), and ...
CHOLESTEROL DRUG MAY BE A LOT MORE Dec 25, 2005
Chicago Tribune, ...cancer. The first statin, Mevacor, was marketed in 1987, but doctors were nervous about prescribing it, fearing side effects. Those ...
Jury gets teachers' Rx case Dec 15, 2005
Cincinnati Enquirer, ...ship" - supplied 18 percent of the name drugs sold by Medco to retirement system members, including Medco's top three sellers in 1997 - Zocor, Mevacor and Vioxx ...
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