Mevacor

The primary transporter of cholesterol in the blood is low density Hpoprotein (LDL). Once transported intraceUularly, cholesterol homeostasis is controlled primarily by suppressing cholesterol synthesis through inhibition of P-hydroxy-P-methyl gluterate-coenzyme A (HMG—CoA) reductase, acyl CoA—acyl transferase (ACAT), and down-regulation of LDL receptors. An important dmg in the regulation of cholesterol metaboHsm is lovastatin, also known as mevinolin, MK-803, and Mevacor, which is an HMG—CoA reductase inhibitor (Table 5). 

Scheme 1. Sites of inhibition of cholesterol biosynthesis by Mevacor and zaragozic acid A.

The search for inhibitors of this pathway began with the first key regulatory enzyme, HMG CoA reductase. Several clinically useful inhibitors of HMG CoA reductase are now known. One of the most successful, Mevacor, produced by Merck, is one of the pharmaceutical industry s best selling products. However, the problem with inhibiting a branched biosynthetic pathway at an early point is that the biosynthesis of other crucial biomolecules may also be inhibited. Indeed, there is some evidence that levels of ubiquinone and the dolichols are affected by some HMG CoA reductase inhibitors. Consequently, efforts have recently been directed towards finding inhibitors of squalene synthase, the enzyme controlling the first step on the route to cholesterol after the FPP branch point. 

D Mevinacor (Merck Sharp USA Mevacor (Merck Sharp ... 

Metropolis Monte Carlo (MMC) method, 26 1035-1036 Met-spar, 4 577 Metsulfuron-methyl, 13 322 Mettler dropping point, 10 827 Mevacor, 5 142... 

Baycol (cerivastatin, sold as Lipobay in Europe, Bayer) is a statin, a class of cholesterol-lower drugs. Statins are the most prescribed drugs in the United States, with more than 12 million people taking them, and more than 700,000 people in the United States taking cerivastatin. It received marketing approval on June 26, 1997 and was voluntarily removed from the market on August 8, 2001 because of its link to 100 deaths and several injuries from potentially the muscle disease rhabdomyolysis. The other statins — lovas-tatin (Mevacor Merck) pravastatin (Pravachol Bristol-Myers Squibb) simvastatin (Zocor Merck) fluvastatin (Lescol Novartis) atorvastatin (Lipitor Parke-Davis) rosuvastatin... 

A number of cholesterol-lowering drugs (Pravachol, zocor, and mevacor) are prepared by enzymatic processes. Penicillin antibiotics that have been on the market for decades are produced in large quantities by the enzymatic process. 

The most important class of cholesterol-lowering agents is the statins. These include lovastatin (Mevacor), simvastatin (Zocor), pravastatin (Pravachol), and atorvastatin (Lipitor), among others. These molecules work, in modest part, by inhibiting biosynthesis of cholesterol and, in larger part, by increasing the rate at which cholesterol is eliminated by the body. Let s have a look at this in more detail. 

Subsequently, a second, closely related molecule—lovastatin—was discovered by scientists at Merck in the United States in another fungal fermentation broth and by Sankyo in Japan. Lovastatin, marketed as Mevacor in the United States, proved both safe and efficacious for the intended nse and was the first statin to be approved for human use. Several others, some mentioned above, followed. The history of discovery and development of HMGR inhibitors has been pnUed together by Jonathan Tobert, who led the lovastatin and simvastatin clinical development effort at Merck. ... 

Fenofibrate (Anatra, Lipofen, Lofibra, TriCor, Triglide) Fluvastatin (Lescol) Gemfibrozil (Lopid) Lovastatin (Mevacor, Altocor)... 

Lovastatin (Mevacor/ Altocor) [Antilipemic/HMG-CoA Reductase Inhibitor] Uses Hypercholesterolemia Action HMG-CoA reductase inhibitor Dose 20 mg/d PO w/ PM meal may T at 4-wk intervals to 80 mg/d max or 60 mg ER tab take w/ meals Caution [X, -] Avoid w/ grapefruit juice, gemfibrozil. Contra Active liver Dz Disp Tabs SE HA GI intolerance common promptly report any unexplained muscle pain, tenderness, or weakness (myopathy) Interactions T Effects W/ grapefruit juice T risk of severe myopathy W/ azole antifungals, cyclosporine, erythromycin, gemfibrozil, HMG-CoA inhibitors, niacin T effects OF warfarin >1 effects W/ isradipine, pectin EMS t Risk of photosensitivity Rxns T effects of warfarin concurrent EtOH use t risk of liver tox diltiazem and verapamil can T risk of lovastatin tox OD Unlikely to cause life-threatening Sxs... 

Clinical trials with lovastatin (Mevacor), simvastatin (Zocor) and pravastatin (Pravachol) provided much of the evidence supporting the observation that lowering... 

Blood/gout/ mevinolin (= lovastatin = methylcompactin)/polyket. Mevacor/ inflammation... 

MEVACOR (Merck) (Lovastatin) tablets June 2002 labeling... 

AccessMedicine Print Chapter 35. Agents Used in Dyslipidemia Oral 600 mg tablets Lovastatin (generic, Mevacor)... 

Brand Name Mevacor (lovastatin) Pravachol (pravastatin)... 

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