What are HMG-CoA Reductase Inhibitors?

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  • Written By: D. Jeffress
  • Edited By: Jenn Walker
  • Last Modified Date: 29 September 2019
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High cholesterol is one of the leading causes of heart attack, stroke, and other major arterial diseases among middle-aged people and older adults. In addition to maintaining a healthy diet and exercise routine, taking prescription drugs can help lower cholesterol levels and prevent clogged arteries. HMG-CoA reductase inhibitors, also called statins, have been found to be very effective at stopping the synthesis of new cholesterol in the body and enhancing the liver's ability to remove existing deposits from the bloodstream.

Body cells go through a multiple-step process when synthesizing natural cholesterol. The first step is initiated by an enzyme called 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase. The enzyme triggers chemical and physical responses that eventually lead to lipid production. HMG-CoA reductase inhibitors work by blocking the activity of the enzyme, thereby stopping cholesterol production before it even starts.

HMG-CoA reductase inhibitors also have an impact on existing cholesterol. When the liver senses that natural production is decreased, it begins drawing dietary cholesterol out of the bloodstream to make up for the perceived deficiency. By dieting and exercising in addition to taking medications, both natural lipids and dietary cholesterol can be reduced significantly.


It is possible to experience unwanted side effects when taking HMG-CoA reductase inhibitors. The most common problems include diarrhea, abdominal pain, stomach cramps, dizzy spells, and headaches, though problems are usually mild and go away in a matter of hours. Some people also experience slight fevers, muscle cramps, and feelings of weakness or fatigue after taking a dose. Insomnia, erectile dysfunction, and allergic reactions are possible but rare.

A doctor can determine if HMG-CoA reductase inhibitors are a good treatment option after performing a thorough physical screening. Most physicians suggest that people who are at risk of high cholesterol complications try to make lifestyle changes before they prescribe medications. Avoiding smoking, fatty foods, and alcohol while exercising regularly are enough to reduce cholesterol in many people. If problems persist, a low initial dose of medication may be given to see if it has an effect.

Frequent checkups are important when starting a course of HMG-CoA reductase inhibitors so a doctor can determine the best dosage amount and continue to monitor results. Most patients are instructed to take one tablet or capsule daily, usually at bedtime. If cholesterol levels fail to reach normal levels after several months, other drugs or surgery may be considered to prevent potentially life-threatening complications.


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