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Anticholesterol

Introduction

Anticholesterol is a group of medicine used to reduce high cholesterol levels in the blood. Cholesterol is produced by the liver from fats in our diet. Cholesterol doesn’t dissolve in the blood instead, it bonds to carriers called lipoproteins which transport it between cells. Certain amount of cholesterol is needed by our body for the formation of cell membranes, production of some hormones and vitamin D.

Low-density lipoproteins (LDL) cholesterol makes up the majority of the body’s cholesterol. LDL is known as “bad” cholesterol because having high levels can lead to a buildup in the arteries and resulted in heart disease. High-density lipoproteins (HDL) cholesterol absorbs cholesterol and carries it back to the liver, where it is flushed from the body. High levels of HDL or “good” cholesterol, reduce the risk of heart disease and stroke.

Total cholesterol count is determined by the level of LDL cholesterol, HDL cholesterol and triglyceride, whereby a high count indicates abnormal levels of the cholesterol complexes.

Types of anticholesterol

Anticholesterol drug acts through different functions according to its type, in lowering the blood cholesterol level.

The types of anticholesterol drug:

  1. Hydroxy-Methylglutaryl Coenzyme A Inhibitors (statins)
  2. Bile Acid Binding Resin
  3. Nicotinic Acid
  4. Fibric Acid Derivatives
  5. Cholesterol Absorption Inhibitors

Function

Hydroxy-Methylglutaryl Coenzyme A Inhibitors (HMG Co A) is also known as the statins. Its function is to reduce the production of cholesterol in our body by inhibiting or blocking HMG Co A. HMG Co A is an enzyme that is responsible for the production of cholesterol in the liver.

Bile acid binding resin acts by binding to the bile acid which resulted in reduced amount of this acid for digestion process. The reduction of bile acid will promote more production of this acid by the liver. Since the liver uses cholesterol to produce bile acid, this process will help in lowering the excessive cholesterol level in the blood.

Nicotinic acid or Niacin reduces cholesterol synthesis in the body through several pathways, resulting in lower LDL and Triglyceride level and increased HDL level.

Fibric Acid Derivatives is used for the treatment of high triglyceride level in the blood. Fibric acid derivatives will reduce the production of Very Low-density lipoproteins (VLDL) and speeds up the removal of triglyceride from our body.

Cholesterol Absorption Inhibitors acts by restricting the absorption of dietary cholesterol from the intestine without affecting the absorption of Triglyceride and fat soluble vitamin.

Combinations of anticholesterol are also available in current treatment. These combination treatments proved useful in patients who failed to achieve optimal blood cholesterol level despite being compliant to initial anticholesterol medication.

Formulation of anticholesterol drug available in the market.

No.
Type of Anticholesterol
Drug Name
Dose
1. Hydroxy-Methylglutaryl Coenzyme A Inhibitors Lovastatin 20-80 mg
Pravastatin 20-40 mg
Simvastatin 20-80 mg
Atorvastatin 10-80 mg
Fluvastatin 20-80 mg
Rosuvastatin 10-40 mg
2. Bile acid binding resin Cholestyramine Not available in Malaysia
Colestipol
Colesevelam
3. Nicotinic acid Immediate release Nicotinic Acid 50-250mg
Extended release Nicotinic Acid 375-1000mg
4. Fibric Acid Derivatives Gemfibrozil 300,600 mg
Fenofibrate 100-300mg
5. Cholesterol Absorption Inhibitor Ezetimibe 10 mg
6. Combination therapy Ezetimibe and Simvastatin 10/10mg, 10/40mg, 10/80mg

How to take the medication and side effect

Patient might experience several common side effects from statin such as headache, nausea, constipation, itchiness/rashes and tiredness which usually go away after the body had adjusted. Muscle problems and liver abnormalities are rare, but may need regular liver function monitoring.

Major side effect of bile acid binding resin is constipation. This side effect can be reduced by increasing fluid intake. Several other side effects that can occur are nausea, bloating / flatulence and indigestion. Since this group of drug will interfere with the absorption of various medications, patient is advised to take this medication 1 hour before or 4 hours after taking other medications.

Flushing is a very common side effect that patient will experience when consuming nicotinic acid. This side effect can be reduced by taking nicotinic acid at night and avoid consuming alcoholic and hot drink.

Among the usual side effect of Fibric acid derivatives are neuromuscular disturbance (headache, tiredness and vertigo), diarrhea, nausea, rashes and eczema. Patient is advised to take this anticholesterol drug with food to avoid gastrointestinal intolerance. Patient also needs to inform their doctor if they experience muscle or joint pain after starting treatment with this medication.

Monitoring

Statins, Gemfibrozil and Niacin can affect the liver normal function due to their action in the liver. Therefore, patient who is taking these anticholesterol drugs will be asked to do a scheduled laboratory test for liver function to ensure the liver is in good condition. If the result of the test showed abnormality in liver function, the doctor will do adjustment in the anticholesterol drug treatment.

Additional information

Effectiveness of the anticholesterol treatment differs between individual. Patient needs to comply in taking their medication to achieve their treatment target. They need to report to their doctor about any side effect that occurs when taking the anticholesterol medication.

While patient on drug therapy, patient also need to :

  1. Eat balance diet and practice a healthy life style
  2. Exercise frequently
  3. Quit smoking
  4. Reduce and avoid alcohol intake

References

  1. Anonymus (2013).High cholesterol. Retrived November 1,2013, from http://www.mayoclinic.com/health/high-blood-cholesterol/DS00178/DSECTION=treatments-and-drugs
  2. Hochholzer,W.Berg,D.D, Giugliano,R.P.(2011). The facts behind niacin. Retrieved November 2,2013, from http://www.medscape.com/viewarticle/750937_3
  3. Joint Formulary Committee (2008-2009). British National Formulary. 58th edition. London: British Medical Association and Royal Pharmaceutical Society of Great Britain.
  4. Moll.J (April 13,2009).Niacin effect can lower your cholesterol.Retrived October 29,2013, from http://cholesterol.about.com/od/nicotinicacid/
  5. Moll.J (December 19,2007).What is niacin and how does it work ?.Retrived October 29,2013, from http://cholesterol.about.com/od/nicotinicacid/
  6. Ogbru,O. (n.d.). Statins. Retrived October 31,2013, from http://www.medicinenet.com/statins/article.htm
  7. Safeer,R.S & Lacivita,C.L (2000).Choosing drug therapy for patients with hyperlipidemia.Retrived October 29,2013, from http://www.aafp.org/afp/2000/0601/
  8. Simon,H.,Zieve.D (2012). High blood cholesterol level in-depth report. Retrived November 1,2013, from http://health.nytimes.com/health/guides/disease/high-blood-cholesterol-and-triglycerides/background.html
Last Reviewed : 11 August 2014
Writer/Translator : Mazuin bt. Mahmud Taridi
Accreditor : Najwa bt. Ahmad Hamdi