Atherosclerotic cardiovascular disease is the leading cause of morbidity and mortality around the world. It is a common problem associated with ageing. As you get older, fats, calcium and cholesterol start depositing in the arteries and form plaque, due to which there is a restriction in the blood flow. Restricted blood flow can cause severe complications like stroke and heart attack.
Hyperlipidemia: What is it?
Hyperlipidemia (excessive cholesterol in the blood) is the primary cause of progressive atherosclerosis. Although cholesterol is essential for several metabolic processes, including the production of vitamin D, bile and hormones,. But an increase in the level of cholesterol can lead to atherosclerosis, in which cholesterol deposits in the arteries for the blockage of blood flow.
There are different forms of cholesterol (LDL, VLDL, and HDL), which play a significant role. Elevated low-density lipoproteins (LDL) and reduced high-density lipoproteins (HDL) lead to the risk of various cardiac health complications.
Lifestyle changes such as intake of a healthy diet, regular exercise, and weight loss if overweight are the primary treatment against high cholesterol. Smoking aggravates hyperlipidemia, so try to quit it. In addition to including a healthy diet, it is necessary to take medications to control the level of Cholesterol and triglycerides.
Lifestyle changes along with hypolipidemic drugs primarily Statins are ideal management of atherosclerotic cardiovascular disease, which assist in preventing the deposition of cholesterol in the arteries and reduces the risk of acute coronary events. Statins decrease cholesterol by 30–60%, but their dose may be increased if the target is not achieved.
It lowers the LDL (Low-density lipoproteins) cholesterol levels by 50%. Since statins contribution to reducing the triglyceride level is limited. Although it may lead to muscle pain and rarely liver failure, it is better to co-administer the statins with fibrates in combination, which ultimately causes fewer adverse effects. Fenofibrate is another class of lipid-lowering drugs that reduces cholesterol as well as triglycerides in the blood. However, it is also useful in the case of statin-resistant patients.
Statins and Fibrates: Combination therapy for Hyperlipidemia
Monotherapy with statins is the gold standard treatment for hyperlipidemia, but more significant benefits may be achieved through the combination therapy. Due to the combination, low doses of statins are administered, which causes fewer adverse effects.
To avoid serious complications from atherosclerotic cardiovascular disease, it is important to start the combination therapy to achieve the goals in less time with minimum side effects:
- A combination of atorvastatin and fenofibrate is used to decrease high cholesterol as well as triglyceride levels in the blood.
- It also increases the level of high-density lipoproteins (good cholesterol), due to which the risk of heart attacks decreases.
- Regular monitoring of liver and kidney functions are required during the treatment.
Mechanism of action
Atorvastatin prevents the body from making low-density lipoproteins (bad cholesterol), while fenofibrates decrease the level of triglycerides in the blood and increase the level of high-density lipoproteins (good cholesterol).
Atorvastatin blocks the action of a liver enzyme known as HMG-CoA reductase, which produces Cholesterol. Fibrates reduce the triglyceride synthesis in the liver and increase the clearance of triglycerides from the blood. It works by increasing the enzyme, which is responsible for the breakdown of fats in the blood. It activates the peroxisome proliferator-activated receptor-α (PPARα). Fibrates also promote the action of lipoprotein lipase, which mediates lipolysis by PPAR. It modulates the low-density lipoprotein receptor-ligand interaction. The hypotriglyceridemic effects of statins and fibrates are induced by PPARα signal pathway.
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Benefits of Atorvastatin + Fenofibrate
- Due to the combination, low doses of statins are administered, which causes fewer adverse effects (skeletal muscle damage).
- In the presence of severe hypertriglyceridemia and hyperlipidaemia, the combination therapy with statins and fibrates is beneficial because it provides a greater reduction in triglycerides.
- It is used in the treatment of mixed dyslipidemia.
- Along with proper diet, it decreases the bad Cholesterol (low-density lipoproteins) along with fats and increases the level of good Cholesterol (High-density lipoproteins) in the blood.
- It lowers triglycerides and decreases the risk of pancreatitis.
Dosage and administration
The combination is well tolerated with a convenient once-a-day dosing schedule. It is available in the form of tablets.
The dose of the medication depends upon several factors like age, patient’s health, personal risk factors, etc. The dose for various Atorvastatin is 20–80 mg, and the dose for fenofibrate is 150 mg once in a day. While in the combination, the dose of Atorvastatin is reduced to 10 mg and 160 mg for Fenofibrate. The recommended dose of this combination product is one tablet per day.
Important Information and Precautions
- Do not take this if you are suffering from severe kidney, liver and gallbladder disease.
- The risk of myopathy as well as rhabdomyolysis is increased due to the coadministration of the statin with fusidic acid
- During the treatment with this combination product, grapefruit juice must be avoided.
- Statin+Fibrates are contraindicated during pregnancy. So it is not advised to take this product during pregnancy as well as breastfeeding.
Side effects of Statins + Fenofibrate
Generally, this combination is safe and well tolerated with minor side effects, which include nausea, headache, stomach pain, constipation, muscle pain and increased glucose level in blood.
The serious side effects of this combination include myopathy (skeletal muscle damage) and rhabdomyolysis.
Conclusion
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