Altocor: profile and news

Health matters: 'Combination diet' can help cholesterol Jan 18, 2006
We have several classes of medications for high cholesterol: statins (Altocor, Crestor, Lescol, Lipitor, Pravachol and Zocor), bile acid sequestrants, fibrates ... - Billings Gazette,

In strategy shift, Andrx sells off 2 drug brands Mar 30, 2005
Altoprev formerly was called Altocor, but Andrx was forced to change the name last year after Kos Pharmaceuticals Inc., which markets the cholesterol drug ... - Sun-Sentinel.com,

Other information

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