Cholesterol medication: When is treatment started and what medications are available for cholesterol management?

Cholesterol medications are a key part of the prevention and treatment of cardiovascular diseases. High cholesterol, particularly high LDL cholesterol, is one of the most significant risk factors for cardiovascular diseases. While lifestyle changes are the primary treatment option, sometimes medication is needed to lower cholesterol levels. In this article, we will examine when cholesterol medication is necessary and what medications are available for cholesterol treatment.

Cholesterol medication is usually started when lifestyle changes are insufficient to lower cholesterol levels or when a person has a high risk of developing cardiovascular diseases.Risk assessment takes into account several factors, such as:

•  LDL cholesterol level: If the LDL cholesterol level is clearly elevated (over 3.0 mmol/l) and lifestyle changes do not achieve the target level, medication may be considered.

•  Risk of cardiovascular diseases: Individuals with a high risk of cardiovascular diseases, such as diabetes, high blood pressure, or a previous heart attack, will start medication at a lower cholesterol level.

•  Genetic predisposition: Some individuals have a genetic tendency to high cholesterol, such as familial hypercholesterolemia, where medication may be initiated at an early stage.

•  The effectiveness of lifestyle changes: If sufficient results in managing cholesterol levels are not achieved through diet, exercise, and weight management, medication may be necessary.

It is the doctor's responsibility to assess the patient's overall risk and determine when medication is necessary. Risk calculators for cardiovascular diseases are often used in decision-making, taking into account age, gender, smoking, blood pressure, and cholesterol levels.

There are several different types of cholesterol medications, and they work in various ways. Here are the most common medications for cholesterol treatment:

Statins are the most commonly used cholesterol medications. They work by inhibiting an enzyme that is important for cholesterol production in the liver. This leads to a reduction in LDL cholesterol in the blood. Statins also reduce inflammation in the walls of blood vessels and stabilize cholesterol plaques, which decreases the risk of heart attacks.

The most common statins are:

•  Atorvastatin (Lipitor)

•  Simvastatin (Zocor)

•  Rosuvastatin (Crestor)

•  Pravastatin (Pravachol)

Statins are very effective, but some patients may experience side effects such as muscle pain, elevated liver function tests, or in rare cases, muscle tissue breakdown (rhabdomyolysis). A doctor will assess the benefits and potential risks before starting statin therapy.

Ezetimibe is a medication that prevents the absorption of cholesterol from the intestine. It reduces the amount of cholesterol that enters the bloodstream through diet. Ezetimibe is often used in conjunction with statins if statin therapy alone is not sufficient to lower LDL cholesterol adequately.

Ezetimibe is generally well tolerated, and its side effects are rare. It is a good option for those who cannot tolerate statins or need additional power to lower cholesterol.

PCSK9 inhibitors are a newer class of medications that effectively lower LDL cholesterol. These drugs inhibit the action of a protein called PCSK9, which increases the liver's ability to remove LDL cholesterol from the bloodstream.

PCSK9 inhibitors are generally used in patients with a very high risk of cardiovascular diseases or those with familial hypercholesterolemia. The medications are administered by injection every few weeks. 

The most common PCSK9 inhibitors are:

•  Alirocumab (Praluent)

•  Evolocumab (Repatha)

The advantage of using these medications is their effectiveness, but they are also significantly more expensive than other cholesterol medications.

 Fibraates are medications that specifically reduce triglyceride levels and may slightly increase HDL cholesterol. They work by increasing the oxidation of fatty acids in the liver and other tissues, leading to a decrease in triglycerides in the blood.

Fibraates are often used in patients with high triglyceride levels or low HDL cholesterol. They can also be used in conjunction with statins in patients with mixed dyslipidemia (high triglycerides and low HDL).

The most common fibrates are:

•  Gemfibrozil (Lopid)

•  Fenofibrate (Tricor)

Care should be taken when using fibrates in conjunction with statins, as this may increase the risk of muscle damage.

Resins (bile acid sequestrants) are medications that bind bile acids in the intestine, preventing their reabsorption back into the liver. This forces the liver to use more cholesterol for the production of new bile acids, which lowers LDL cholesterol in the blood.

Resins are not as effective as statins, but they can be used as an adjunct therapy or in patients who cannot tolerate other medications. 

The most common resins are:

•  Cholestyramine (Questran)

•  Colesevelam (Welchol)

Resins can cause gastrointestinal symptoms, such as gas and constipation, which may limit their use.