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A new alternative medicine to effectively reduce blood lipid levels

A new alternative medicine to effectively reduce blood lipid levels
 

What is hyperlipidemia

Hyperlipidemia (or high levels of lipids in the blood) refers to a condition where the body has elevated levels of lipids beyond normal limits. We can easily divide the types of lipids in the blood into 2 types:

  1. Cholesterol 
    Cholesterol is the lipid that can be synthesized from our liver. It is also from the food you eat. There are two main types of cholesterol.
  •  Low-density lipoprotein or LDL, also known as “bad cholesterol”
    LDL is a type of unhealthy lipid that results from consuming high-fat foods. If the body has excessive levels of LDL, this type of lipid will accumulate along the walls of blood vessels, leading to blockages. This impairs blood flow and the flexibility of blood vessels, increasing the risk of cardiovascular diseases.
  • High-density lipoprotein or HDL, also known as “good cholesterol”
    HDL is a type of healthy lipid that helps transport LDL cholesterol from various parts of the body back to the liver for elimination. This results in a reduction of cholesterol level, helping to lower the risk of cardiovascular diseases
  1. Triglycerides
    Triglycerides come from high-fat dietary habits or excessive consumption of carbohydrates and sweet foods. If these lipids are present in excessive amounts, they are converted into triglycerides and accumulate in various tissues of the body, leading to conditions such as fatty liver disease or obesity

 

How dangerous is hyperlipidemia?

Hyperlipidemia may not always cause symptoms, but having too much lipids in your body can be a problem. Cholesterol, along with triglycerides and other lipids, can build up on the walls of your blood vessels and form plaque. Plaque causes the arteries to become hardened and narrowed, which slows down or blocks the flow of blood and oxygen supply to your heart and brain. This increases your risk of cardiovascular events such as heart attack and stroke.

 

How to treat hyperlipidemia??

  1. Non-pharmacologic treatment

  • To regulate dietary intake, it is advisable to steer clear of foods rich in saturated fats, including organ meats, fatty meat, shellfish such as oyster, squid, and shrimp.

  • Avoid using oils with high saturated fatty acids such as palm oil, coconut oil, and coconut milk.

  • Use methods of steaming, boiling, or baking food instead of frying or stir-frying.

  • Take more vegetables and fruits.

  • Eliminate tobacco and limit alcohol intake.

  • Exercise regularly and continuously at least 3-4 times/week.

  • Lose body weight or control body weight.

 

  1. Pharmacologic treatment

For certain patients with comorbidities or those who have made lifestyle modifications but are still unable to manage their lipid levels within the desired range, pharmacological intervention may be considered by their physician. Presently, there are two main types of medications available for treating hyperlipidemia:

Oral lipid lowering agents, including drugs for high LDL cholesterol and drugs for high triglycerides

  • Drugs for high LDL cholesterol
Group of medicines รายการยา
Statins
Mechanism of action: Inhibit HMG-CoA reductase which is an enzyme used in the process of cholesterol synthesis by the liver
  • Simvastatin
  • Atorvastatin
  • Rosuvastatin
  • Fluvastatin
  • Pitavastatin
  • Pravastatin
Bile acid sequestrants (BAS)
Mechanism of action: Bind with bile acid and excreted through feces, causing the liver to use cholesterol to produce more bile.
  • Cholestyramine
Ezetimibe
Mechanism of action: Inhibit the absorption of cholesterol from the digestive tract.
  • Ezetimibe


  • Drugs for high triglycerides
 
Group of medicines Medication
Fibrates
Mechanism of action: Increase the excretion of fat that has triglycerides as the main component.
  • Fenofibrate
  • Gemfibrozil
  • Pemafibrate
Omega-3 fatty acid
Mechanism of action: Inhibit the absorption of triglycerides from the digestive tract and reduces their synthesis in the liver.
  • Ethyl icosapentate
  • Omega-3 fatty acid
Nicotinic acids
Mechanism of action: Reduce triglyceride production from the liver.
  • Niacin
 

Injectable lipid lowering agents
Injectable lipid lowering agents are a new type of treatment. It may be used for some patients who have used other lipid-lowering drugs and their lipid levels have not reached the desired target even after using high doses. This group of drugs has advantages: patients do not need to use the injections every day but still able to control their blood lipid levels to the desired criteria. Examples of these drugs include protein convertase subtilisin/kexin type 9 inhibitors (PCSK9 inhibitors) such as alirocumab, evolocumab, and inclisiran.


Get to know PCSK9 inhibitors:


New lipid lowering agent. Besides its high efficiency, it does not need to be used every day.

In the body, there is a PCSK-9 (proprotein convertase subtilisin kexin type 9), which is an enzyme that plays a role in reducing the number of LDL cholesterol receptors as a mechanism for regulating blood lipid balance. If PCSK-9 is working a lot, it will cause high LDL cholesterol in the blood. Therefore, drugs that have the effect of blocking the activity of this enzyme “PCSK9 inhibitors” can help reduce LDL cholesterol in the blood. They are divided into two subgroups: monoclonal antibodies and synthetic RNA (small interfering RNA or siRNA).
 
Generic name Alirocumab Evolocumab Inclisiran
Class of medicines PCSK9 inhibitors antibody PCSK9 inhibitors antibody Small interfering ribonucleic acid (siRNA) agent
Administration and frequency Subcutaneous injection
every 2 or 4 weeks
Subcutaneous injection
every 2 or 4 weeks
Subcutaneous injection
as a single injection, again at 3 months, and then every 6 months thereafter
Efficacy Reduce LDL cholesterol from baseline 60-61% after 24 weeks Reduce LDL cholesterol from baseline 62% after 12 weeks Reduce LDL cholesterol from baseline 62% after 150 days
Side effects ▪ Pain, swelling, redness or itching around the site of injection
▪ Flu-like illness
▪ Muscle spasm
▪ Muscle pain
▪ Diarrhea
 
▪ Pain, swelling, redness or itching around the site of injection
▪ Signs of a common cold
▪ Flu-like illness
▪ Headache
▪ Back pain
▪ Joint pain
▪ Nausea
▪ Pain, swelling, redness or itching around the site of injection
▪ Joint pain
▪ Bronchitis

 
 
 

Who could benefit from PCSK9 inhibitors?

Anyone with high LDL cholesterol levels could benefit potentially. The recent focus is on three groups:

  1. Those with familial hypercholesterolemia (FH), a genetic condition. It causes LDL cholesterol level to be very high. Statins and other treatments do not lower LDL cholesterol enough for these people.

  1. Those who have had a cardiovascular disease such as a heart attack, unstable angina or stroke; this is often called secondary prevention.

  1. Those who have statin intolerance — typically muscle pain that prevent statin use or restrict use to lower-intensity statins.

 
References:
  1. ยาลดไขมันในเลือดชนิดฉีด | โดยคณะเภสัชฯ ม.มหิดล [อินเทอร์เน็ต]. 2565 [เข้าถึงเมื่อ 24 เม.ษ. 2567]. เข้าถึงได้จาก: https://pharmacy.mahidol.ac.th/th/service-knowledge-article-info-old.php?id=590
  2. UpToDate; Patient education: High cholesterol and lipids (Beyond the Basics) [Internet].2021 [cited 2024 Apr 24]. Available from: https://www.uptodate.com/contents/high-cholesterol-and-lipids-beyond-the-basics
  3. American Heart Association. Prevention and Treatment of High Cholesterol (Hyperlipidemia). American Heart Association [Internet]. 2020 [cited 2024 Apr 24]. Available from: https://www.heart.org/en/health-topics/cholesterol/prevention-and-treatment-of-high-cholesterol-hyperlipidemia
  4.  High Cholesterol . Mayo clinic [Internet]. 2023 [cited 2024 Apr 24]. Available from: https://www.mayoclinic.org/diseases-conditions/high-blood-cholesterol/symptoms-causes/syc-20350800
  5. Alirocumab: Drug information. UpToDate [Internet]. 2024 [cited 2024 Apr 24]. Available from: Alirocumab: Drug information - UpToDate
  6. Evolocumab: Drug information. UpToDate [Internet]. 2024 [cited 2024 Apr 24]. Available from: Evolocumab: Drug information - UpToDate
  7. Inclisiran: Drug information. UpToDate [Internet]. 2024 [cited 2024 Apr 24]. Available from: Inclisiran: Drug information - UpToDate
  8. Jennifer G, et al. Efficacy and Safety of Alirocumab in Reducing Lipids and Cardiovascular Events. N Engl J Med. 2015;372:1489-1499.
  9. Sabatine MS, et al. Efficacy and Safety of Evolocumab in Reducing Lipids and Cardiovascular Events. N Engl J Med. 2015;372:1500-1509.
  10. Raal F, et al. Efficacy, Safety, and Tolerability of Inclisiran in Patients With Homozygous Familial Hypercholesterolemia: Results From the ORION-5 Randomized Clinical Trial. Circulation. 2024;149:354–362.



 
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Last modify: June 13, 2024

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