Mechanism of Action

Natural Cholesterol Guide

Lower Cholesterol By Scott Davis

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The statin family of six closely related hypocholesterolemic drugs are all potent competitive inhibitors of the enzyme 3-hydroxy-3-methylglutaryl coenzyme A re-ductase (HMG CoA reductase), the rate-limiting enzyme in cholesterol biosynthesis. The liver is their target organ, and decreased hepatic cholesterol synthesis ultimately leads to increased removal of LDL particles from the circulation. As a consequence, all other hypocholes-terolemic drugs have been relegated to secondary status.

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

Age Adjusted 6-Year Death Rate per 1000 Men

Age Adjusted 6-Year Death Rate per 1000 Men

140 160 180 200 220 240 260 280 300 Serum Cholesterol mg/dl

Key points

(1) The risk increases steadily and particularly above 200 mg/dl.

(2) The magnitude of the increased risk is large—fourfold at the top 10% as compared to the bottom 10%.

140 160 180 200 220 240 260 280 300 Serum Cholesterol mg/dl

Key points

(1) The risk increases steadily and particularly above 200 mg/dl.

(2) The magnitude of the increased risk is large—fourfold at the top 10% as compared to the bottom 10%.

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