Cholesterol-reducing drugs

This procedure was used in the synthesis of the cholesterol-reducing drug lescol.131 The diethylmethoxyboron can be prepared in situ from triethylboron and one equivalent of methanol. 

Calfee, Winston, and Stempski (2002), using national U.S. monthly data on retail prescriptions, as well as for cholesterol-reducing drugs, in 1995-2000, found little if any impact from DTCA on the pattern of statin... 

Calfee, John E., Clifford Winston, and Randolph Stempski. 2002. Direct-to-Consumer Advertising and the Demand for Cholesterol-Reducing Drugs. Journal of Lave and Economics 14(2) 673-690. 

The high-value HMG-CoA reductase inhibitor Simvastatin (8) is marketed by Merck under the name Zocor. The active ingredient is obtained from a fermentation approach. It is very similar in structure to lovastatin, which has fallen from the top-sellers list. Lovastatin (9) is also a cholesterol-reducing drug that is isolated from Aspergillus terreus.51-60 It is still obtained by fermentation,61 and with the current advances in molecular biology,62 64 chemical approaches are not able to compete in a cost-effective manner.65-67 The usage of lipases allows for the manipulation of the butyric acid sidechain to access other HMG-CoA reductase inhibitors such as simvastatin.68 A number of routes to various portions of lovastatin have been reported.69... 

Ahrer, W., Schoftner, R. and Buchberger, W. Identification of unknown degradation products in a new cholesterol-reducing drug by ion-chromatography coupled to mass spectrometry. J. Chromatogr., A 912 91-98, 2001. 

Statins are the newest class of cholesterol-reducing drugs. Statins reduce serum cholesterol levels by inhibiting the enzyme that catalyzes the reduction of hydroxymethylglu-taryl-CoA to mevalonic acid (Section 26.8). Decreasing the mevalonic acid concentration decreases the isopentenyl pyrophosphate concentration, so the biosynthesis of all terpenes, including cholesterol, is diminished. As a consequence of diminished cholesterol synthesis in the liver, the liver expresses more LDL receptors— the receptors that help clear LDL from the bloodstream. Studies show that for every 10% that choles-... 

To date, the studies that have tried to link dietary fat to increased risk of coronary heart disease have remained ambiguous. Studies have shown that cholesterol-lowering drugs help reduce the risk of heart (45) disease, but whether a diet low in cholesterol can do the same is still questionable. While nutrition experts are debating whether a low-fat, carbohydrate-based diet is the healthiest diet for Americans, nearly all agree that the anti-fat message of the last twenty years has been oversimplified. For example, some fats and oils like those found in olive oil... 

Sdringola S, Nakagawa K, Nakagawa Y, Yusuf SW, Boccalandro F, Mullani N et al. Combined intense lifestyle and pharmacologic lipid treatment further reduce coronary events and myocardial perfusion abnormalities compared with usual-care cholesterol-lowering drugs in coronary artery disease. J Am Coll Cardiol 2003 41 263-272... 

Statins are a group of cholesterol lowering drugs that have been shown to be beneficial as published in 1997. In patients with ischaemic heart disease, the number of stroke events was reduced by 30% compared with placebo. 

The current therapy leaders are the anti-ulcerants such as Omeprazole (Prilosec ) or Lansoprazole (Prevacid ), which accounted for US 19.5 billion in 2001, thus claiming a market share of 6%. The anti-ulcerants are closely followed by the cholesterol reducers, e.g., Atorvastatin (lipitor ) and Simvastatin (Zocor ), totaling US 18.9 billion, the antidepressants (US 15.9 billion), and the NSAIDs (nonsteroidal anti-inflammatory drugs US 10.9 billion). Calcium antagonists, antipsychotics, oral antidiabetics, ACE inhibitors, cephalosporins, and antihistamines complete the list of the best-selling therapy classes, with sales between US 9.9 and 6.7 billion. It is interesting to note that four classes grew more than 20% in 2001, namely the cholesterol reducers (22%), the antipsychotics (30%), the oral antidiabetics (30%), and the antihistamines (22%) [4],... 

Peripheral neuropathy occurs with statins, and perhaps with all cholesterol-lowering drugs, and may be related to reduced production of ubiquinone, as suggested in a review (5). Moreover, it appears that once a statin produces a neuropathy, rechallenge with any other statin is likely to cause a recurrence. This is reported to occur 1-3 weeks after rechallenge, whereas the resolution takes 4—6 weeks after withdrawal (5). 

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