How does cholesterol medication work

Cholesterol medications are one of the most important means to prevent and treat cardiovascular diseases, especially when blood cholesterol levels are persistently elevated. But what exactly does a cholesterol medication do in the body? How does it affect the liver, blood vessels, and fat metabolism?

This article reviews the mechanisms of action of cholesterol medications, the effects of different drug classes, and what happens when the medication starts to take effect. At the end, there are answers to five frequently asked questions.

Cholesterol is an essential fatty compound for the body, needed for the production of cell membranes, hormones, and vitamin D. Most cholesterol is produced in the liver, and the rest is obtained from food.

Excess cholesterol – particularly LDL cholesterol – can accumulate in the walls of blood vessels and cause narrowing of the arteries. This increases the risk of heart attack and stroke.

The goal of cholesterol medications is:

• To lower the amount of LDL cholesterol in the blood
  
  

• Possibly raise HDL cholesterol
  
  

• To reduce the amount of triglycerides
  
  

• To reduce inflammation in blood vessels
  
  

• To prevent the progression of atherosclerosis, or hardening of the arteries
  
  

Different medications work through different mechanisms, but the most common target is the liver's cholesterol synthesis and circulation

• Inhibit HMG-CoA reductase enzyme, which is central to cholesterol production in the liver
  
  

• Increase the number of LDL receptors in the liver → the liver removes more cholesterol from the bloodstream
  
  

• Are the primary treatment for managing high cholesterol

• Inhibits cholesterol absorption in the small intestine
  
  

• Complements the effect of statins, as it works through a different mechanism
  
  

• Effective as a combination medication, especially in severe cases

• Biological drugs that inhibit the action of the PCSK9 protein
  
  

• This improves the lifespan and efficiency of liver LDL receptors
  
  

• Reduces LDL levels by up to 60%, especially in hereditary cholesterol disorders

• Bind bile acids in the intestine
  
  

• More bile acids are produced in the liver from cholesterol → cholesterol is removed from the bloodstream
  
  

• Sometimes used as an adjunct medication, especially with statins

The onset of action depends on the medication:

• Statins: effect begins in 3–5 days, peak at 4–6 weeks
  
  

• Ezetimibe : visible effect in about 2–4 weeks
  
  

• PCSK9 inhibitors : first effect within a few days
  
  

• Resins : results usually within 2–4 weeks
  
  

Blood lipid levels are usually checked about 4–8 weeks after starting the medication.

Successful cholesterol medication:

• Reduces LDL cholesterol by several tens of percentage points
  
  

• May raise HDL cholesterol slightly
  
  

• Can reduce triglycerides
  
  

• Slows down or even stops the growth of arterial plaques
  
  

• In the long term, significantly reduces the risk of heart and brain attacks
  

Cholesterol medications do not replace:

• A healthy diet
  
  

• Exercise
  
  

• Quitting smoking
  
  

They also do not automatically guarantee protection if other risk factors – such as high blood pressure, diabetes, or inflammation – are untreated.

Cholesterol medications work by inhibiting cholesterol production, reducing its absorption, or improving its removal from the bloodstream. Their effects often begin within a few days, but the full benefit is usually seen within 4–6 weeks.

The most common class of drugs, statins, enhance the liver's ability to remove cholesterol from circulation. Other medications are used in situations where statins are not effective enough or cannot be used. Although the medications are effective, lifestyle changes are always necessary alongside them to achieve long-term benefits.

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