Statins Mechanism of Action and Pharmacological Applications

Health care providers are concerned about hyperlipidemia because it is a significant reason behind several cardiovascular diseases and the leading cause of morbidity. Hyperlipidemia is defined as excessive cholesterol in the blood.

Cholesterol is the essential fat which is required for normal cell and body functioning. It is necessary for several metabolic processes including the production of bile, hormones, vitamin D. But a high level of cholesterol can lead to atherosclerosis in which cholesterol-containing plaques build-up and deposits in the arteries for the blockage of blood flow. There are different forms of cholesterol (good and bad), which plays a significant role. Increase in bad cholesterol and a decrease in the amount of good cholesterol can leads to various health complications.

Cholesterol is carried in the bloodstream within the little carriers called lipoproteins. The LDL (low-density lipoproteins) are the bad cholesterol which can stick with the walls of blood vessels. It plays a significant role in clogging the arteries of the heart that leads to atherosclerosis narrowing of arteries of the heart can develop sudden blood clots and causing a heart attack. People with high LDL cholesterol may increase the risk of cardiovascular disease.

Lifestyle changes such as regular exercise and eating a healthy diet are the first line of defence against high cholesterol (hyperlipidemia). These changes include bodyweight reduction, eating a healthy diet which includes plant-based foods, limit intake of saturated fats in your diet, which is found in full-fat dairy products, red meat and in many processed foods. Include monosaturated fats found in olive and canola oil in your diet. Smoking is also a cause for the aggravation of hyperlipidemia. So try to avoid it. Lifestyle changes are beneficial to manage hyperlipidemia. If you make all the necessary lifestyle changes, but still your cholesterol level remains high, then it is essential to take medications.

Statins
Statins are the most common and widely prescribed class of medications for the management of hyperlipidemia. It is the class of drugs which decreases the level of cholesterol in the blood. These are used in the treatment of atherosclerosis and various cardiovascular diseases. Statins block the substance which is required to make the cholesterol. It helps in the removal of cholesterol from the blood. Statins have the potential to reverse coronary artery disease.

Different types of statins
There are various types of statins like atorvastatin, lovastatin, fluvastatin, pravastatin, pitavastatin, simvastatin and rosuvastatin. Out of these statins, Atorvastatin and Rosuvastatin are the most potent drug, while fluvastatin is the least potent.
Sometimes, statins are combined with another medication for the treatment of CVS (cardiovascular) disorder. Statins do more than just decreasing the Low-density lipoprotein (bad cholesterol).

Statins mechanism of action
Statins block the action of a liver enzyme known as HMG-CoA reductase, which is responsible for producing cholesterol. Too much deposition of the cholesterol in the walls of the arteries can build-up the plaque. Statins decrease the low-density lipoprotein as well as total cholesterol level. At the same time, it lowers the triglycerides level and increases the HDL (High-density lipoprotein) – good cholesterol.
It decreases the level of triglycerides and helps to stabilize the plaque in the arteries.

Benefits of statins
Statins are useful to decrease the cholesterol level and protect against the stroke as well as a heart attack. It lowers the LDL (Low-density lipoproteins) cholesterol levels by 50%.
Statins play a significant role in raising the High-density lipoprotein. Also, they have anti-inflammatory properties which have a positive impact on the blood vessels and heart. This effect also decreases the risk of blood clots and heart attack.
These drugs decrease the chance of rejection after organ transplant.

Dosage of statins
These are well tolerated with a convenient once in a day dosing schedule and available in the form of tablets. The dose of the medication depends upon the various factors like age, your health, personal risk factors etc.
The dose for statins is 10-80 mg for Atorvastatin, 10-60 mg for Lovastatin, 80 mg for Fluvastatin, 10-80 mg for Pravastatin and 5-40 mg for Rusavastatin once daily.
Statin decreases cholesterol by 30-60%. But the dose may be increased if the target is not achieved. Even after achieving the target cholesterol level, the treatment with statins gets continuous to prevent atherosclerosis.

Side effects of statins
Generally, the statins are safe and well-tolerated with minor side effects which include abdominal pain, nausea, headache, vomiting, feeling sick, bloating and diarrhoea.
The severe side effects of statins include liver failure and skeletal muscle damage. The muscle damage presents as muscle pain from which you can find relief by switching to a different statin.

Warnings and Precautions
There are some drugs like ketoconazole, itraconazole (antifungal), clarithromycin, Telaprevir which inhibits the CYP3A4 metabolic pathway, through which plasma level of statins may increase and leads to the risk of myopathy as well as rhabdomyolysis. These drugs can be a concern due to their crossover effects on metabolism that alters the statins concentration.

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