High blood cholesterol levels are first approached by lifestyle changes. When it fails, and the risk of developing heart disease due to atherosclerosis increases, your physician will prescribe statin drugs.
How do Statins Work?
cholesterol in our body forms by a process called the Mevalonate Pathway, where an enzyme called the HMG-CoA reductase catalyzes the first and the rate-limiting step of the pathway. Statin medications such as lovastatin and Lipitor competitively inhibit this enzyme and stop the production of excess cholesterol in the body. They are hence called HMG-CoA reductase inhibitors because statins block the access of the substrate to the active site of the enzyme.
By inhibiting the first and the rate-limiting step of the pathway of cholesterol production in the liver, statins considerably reduce the total amount of cholesterol in the body, especially the low-density lipoprotein cholesterol. But cholesterol is also needed for some beneficial tasks inside the body such as absorption of fat-soluble vitamins, hormone production, and digestion.
To compensate for that, statin drugs can also help dissolve the built-up cholesterol in the arteries and reabsorb it.
This, in turn, has two effects:
- cholesterol in the arteries which is a risk factor for heart disease gets dissolved
- The body gets an internal source of cholesterol for its essential mechanisms such as lipid hormone production
What are Statin Drugs Prescribed for?
A statin drug is prescribed for any disease or condition that can benefit from a reduction in the total cholesterol levels of the body.
High cholesterol levels, mainly the ‘bad cholesterol’, directly relates to the development and progression of cardiovascular disease. Cardiovascular disease or CVD is a general term that refers to the conditions affecting the heart and blood vessels, such as heart attack or stroke.
Patients with a condition called familial hypercholesterolemia, a condition with too much cholesterol in the blood, also benefit from the LDL lowering effects of statin. But it is a rare genetic disease and statin drugs are mostly prescribed in CVD or those at risk for developing CVD.
The main types of CVD benefiting from the statin drugs are:
1. Coronary Heart Disease
Coronary heart disease is any condition where the blood flow to the heart is restricted. The most common reason is the hardening of the arteries due to the deposition of excess cholesterol. Excess cholesterol can also cause clot or plaque formation called thrombosis which can damage the arteries and reduce the blood supply.
Chronically, taking statins is usually the first choice in such conditions.
Due to compromised blood supply to the heart, the heart muscle begins to die because the supply of oxygen is not enough for them to survive. The heart becomes weak and unable to pump the blood sufficiently.
Compensatory mechanisms in our body stimulate the heart to push or pump harder. This squeezes the end arteries of the heart, and the blood supply is reduced even more.
This increased strain on the heart can precipitate any of the following conditions:
- Angina – constricting heart pain due to restricted blood flow to the heart
- Heart Attack- blood supply to the heart suddenly stops
- Heart Failure- the heart is too weak to pump blood throughout the body sufficiently
Stroke is another disease of the arteries that is similar to coronary heart disease but applies to the brain. When the blood supply to the brain is reduced or restricted, brain tissue begins to die.
Stroke is a form of CVD but has variable symptoms depending upon the area of the brain affected. But frequently, and almost invariably the person becomes unconscious, and without immediate medical aid, he may die.
3. Aortic Disease
Taking statins has been seen to reduce the growth of an aortic aneurysm, and hence the chances of its ruptures which have life-endangering consequences.
4. Peripheral Arterial Disease
Peripheral arterial disease is a condition where the blood supply to the lower or the upper limbs is restricted. This is again a slowly progressing disease and slowly cripples the patient.
Increased buildup of fats along the arteries narrows them. This condition called atherosclerosis chronically increases blood pressure. This is beacuse the hardened and the narrowed arteries are unable to adapt to the change in the flow of blood. This damages the blood vessels as well, resulting in thrombosis, and increased risk of heart attack or stroke.
Statins are considered chronically in hypertensive patients, who also have a familial history of cardiovascular problems.
The Bottom Line
Your physician may prescribe you statins if:
- You have been diagnosed with any of the above-mentioned forms of CVD
- You have a lifestyle or familial tendency to develop CVD in the later years of life. Statin treatment is chronic cholesterol-lowering therapy and can improve or stop the progression of CVD and related disorders considerably.
Relationship of the Cholesterol Levels and the Cardiovascular Disease
It’s not just the circulating cholesterol level in your body that impacts the development and progression of cardiovascular disease. Instead, the levels of LDL cholesterol or the ‘bad cholesterol’ are involved in CVD more than anything.
Mainly, there are two types of cholesterol:
LDL cholesterol is the form most involved in the deposition of cholesterol in the walls of the arteries. Whereas HDL is the one involved in the clearing and uptake of the bad cholesterol from the blood. So, you see, the target is to increase HDL and reduce LDL.
The deposition of cholesterol along the walls of the arteries hardens them. The blood vessels are then unable to adapt their diameter to changing blood flow. This causes hypertension, a condition with high blood pressure. High blood pressure damages the small vessels such as those in the kidneys and the heart.
Apart from the damage, it also reduces the lumen of the arteries so that now the narrowed arteries carry less blood. People with a genetic tendency of developing cardiovascular disease, develop these symptoms sooner and more easily.
Dosage Regimen of Statins
Statins come as tablets and should be taken as advised by the doctor.
For adults, the appropriate potency is taken once a day. It should be taken at an interval of 24 hours.
Statins are contraindicated in pregnancy and breastfeeding.
Statins are the drugs used for chronic conditions such as to reduce the progression of the disease. So, you have to take them almost for the rest of your life, if, of course, you don’t replace them with other drugs that draw cholesterol out of your body and increase high density lipoprotein (HDL).
How Effective is Statin Treatment for Cardiovascular Disease?
Statins have been shown to reduce the LDL-cholesterol levels by 20-40 % and result in resuced mortality rates due to coronary heart disease (CHD). It has shown more beneficial effects in women and the elderly.
The occurrence of major cardiovascular events reduced within two years of starting the therapy. This shows that statins have remarkable effects when used for long-term results.
Research does not show any beneficial effects when total cholesterol levels are reduced below 100 mg/dL. At the same time, when cholesterol levels are maintained within the range of 120 and 130 mg/dL, mortality rates show a significant decrease.
Are there any Alternatives before Resorting to Statins?
Statin medications such as lovastatin are the first line of drugs when it comes to managing the bad and good cholesterol levels in the blood. There are other drug options too such as niacin, but they have their own specific applications.
Statin medications are prescribed to lower blood cholesterol levels over time. But if your condition is on a very initial stage, your doctor may suggest you bring some important lifestyle changes in your life.
- Avoiding cholesterol and foods containing high-lipid content
- Regular exercise
- Maintain a healthy weight
- Avoid smoking
- Take more soluble fiber and fresh fruits
- Avoid trans fats
- Focus on monounsaturated fatty acids such as olive oil that increase the good cholesterol
Are there any Side Effects of Statin Therapy?
Any drug that helps combat a condition such as a heart attack, comes with its risk factors. With statins, major adverse effects are the following:
Muscle Pain and Injury
People taking statins report muscle aches due to muscle damage, a condition called rhabdomyolysis. This is not very common, though. And because statins are prescribed chronically, people often get used to or stop experiencing muscle aches.
However, muscle pain is not a limiting factor to taking statins.
Statins are metabolized by the liver and act on the liver enzyme HMG-CoA reductase. Liver enzyme tests of the people prescribed statin therapy often reveal an increase in the liver enzymes in the plasma.
This is the reason why the patients who have some kind of liver disease are only prescribed statins only under strict monitoring.
Increased Blood Glucose Levels
Research does not confirm the increase in blood sugar levels but some patients have reported so.
At the same time, statins are also prescribed to diabetic patients when diabetes has progressed to blood vessel and heart damage.
Patients taking statins may experience dizziness, confusion, cognitive impairment, and short-term memory loss. And these side effects go away when statin therapy is stopped.
If you experience any of these adverse effects, there is nothing to worry about. You can take a rest, and manage these. If they get severe, you can contact your physician. Do not stop taking your statin drugs without the advice of your doctor.
How to Manage Statin Side Effects?
If the side effects of your cholesterol medications are getting more noticeable, you should discuss this with your physician. He will weigh your specific risks and cholesterol levels and advise you on the right thing to do.
Common methods you can use to manage the side effects of the statin medications are:
Coenzyme Q10 Supplements
Coenzyme Q10 reduces muscle breakdown. Thus, it can help manage muscle injury and damage as a side effect of these drugs.
Stop Taking Statins for a Short While
Your physician may prescribe you some other drug for lowering cholesterol. After the side effects subside, you can continue the statin medication as advised by the doctor.
Lower the Dose
These drugs are metabolized by the liver enzymes which are genetically regulated. Some people exhibit larger amounts of these enzymes than others. Hence, some people may experience more side effects due to statin intolerance. Lowering the dosage can help reduce the side effects.
Switch to Another Statin medication
Rarely, but a certain statin may be causing your side effects. Switching to another statin drug with a consultation with your doctor may help relieve the side effects.
What should you Avoid when Taking a Statin Medication?
When on statin therapy, you should avoid taking the following:
1. High Cholesterol and Lipid-containing Foods
Statin therapy will be rendered ineffective if you don’t limit your cholesterol and lipid intake.
2. Grapefruit and Grapefruit Juice
Alcohol causes liver damage. And as we have discussed above, one of the most important statin side effects is increased Liver Function Tests (LFTs). Combining both can severely damage the liver.
Risk Factors for Statin Use
Conditions, where statin use should be carefully monitored, are:
- Active hepatic disease
- Age more than 80
- Alcohol intake problem
- Taking other cholesterol-lowering drugs
- Neuromuscular disorders such as multiple sclerosis and rhabdomyolysis
- Pregnant and breast-feeding females
- Kidney Failure
Other risk factors may include dementia, several kinds of muscle problems, and kidney or liver disease.
Some Common Statins
The Bottom Line
Statins decrease the risk of developing heart disease in people with a familial tendency, including conditions such as heart attack or stroke. Hence, these drugs have the importance of primary prevention of mortality from heart disease. Clinical pharmacology and clinical trials have proved this over and over.
A healthy lifestyle goes a long way, with these medications to keep your cholesterol numbers in check. The mild side effects should be weighed against the benefits.
Always consult your doctor before you start or stop taking these drugs.