What medications and when should you take to lower blood cholesterol?

“High cholesterol” does not hurt, but it can lead to the development of atherosclerosis. Atherosclerosis affects the cardiovascular system, leading to the formation of atherosclerotic plaques and blood supply disorders. This often ends in heart attacks and strokes.

Today there are many drugs from the statin group. They have been shown to be effective in reducing mortality from cardiovascular disease, but debate continues about their safety. To achieve and maintain the desired levels of lipid metabolism, long-term use of drugs is required, but many patients do not follow the recommendations, causing the effectiveness of treatment to sharply decrease. What to say about patients when doctors have different opinions on this matter.

General information

Cholesterol is a fatty alcohol, an organic compound found in the cell membranes of living organisms.
Two concepts are often used - cholesterol and cholesterol . What is the difference between them? In fact, this is the name of the same substance, only in the medical literature the term “cholesterol” is used, since the ending “-ol” indicates its relationship to alcohols. This substance is responsible for giving strength to cell membranes .

Sources of cholesterol

But if the level of cholesterol in the body is elevated, cholesterol plaques form in the walls of blood vessels, which, when cracked, create a favorable environment for the formation of blood clots . Plaques narrow the lumen of the vessel.

Therefore, after a cholesterol test, the doctor, if necessary, decides what to do if you have high cholesterol. If the interpretation of the cholesterol test indicates high levels, the specialist often prescribes expensive medications - statins , which are designed to prevent diseases of the cardiovascular system. It is important that the doctor explains that after prescription, the patient needs to take such tablets constantly, as the instructions for use suggest.

But anti-cholesterol drugs have certain side effects, which doctors should warn patients about, explaining how to take the pills correctly.

Therefore, every person who has elevated cholesterol levels must decide whether to take such medications.

There are two main groups of cholesterol medications currently offered: statins and fibrates . In addition, experts recommend that patients consume Lipoic acid and Omega 3 . The drugs used to lower cholesterol are described below. However, their use is advisable only after examination and prescription by a doctor.

Reviews

Evgeniy, 55 years old, Rostov: About 6 months ago I had a myocardial infarction. After rehabilitation at the sanatorium, I took a cholesterol test and found it was elevated. The attending physician prescribed Crestor in the minimum therapeutic dosage. I took it for a month and my cholesterol dropped to normal. The drug is effective, but the downside is a side effect in the form of diarrhea. I dealt with it with the help of bifidobacteria.

Irina, 39 years old, Moscow: I took Torvacard for almost a year. Prescribed for high cholesterol and increased risk of heart ischemia. While taking it, constant headaches appeared. The doctor prescribed the latest generation drug - Rosuvastatin, and Torvacard was noted. I have not seen any side effects from the new medicine yet. Judging by the blood test, cholesterol decreased by 30%. I will continue to take it.

Mikhail, 45 years old, Stavropol: I weigh almost 100 kg, a blood sugar test showed prediabetes. In addition, cholesterol levels are elevated. The attending physician recommended following a diet without fatty and fried foods and prescribed statins. We chose Rosucard and decided on the dosage. I’ve been taking it for almost 2 months, and my cholesterol levels have dropped by a third. The body accepted the medicine without any problems.

Statins to lower cholesterol

Before taking such drugs, you need to know what statins are - what they are, the benefits and harms of such drugs, etc. Statins are chemicals that in the body reduce the production of enzymes necessary for the process of cholesterol synthesis.

In the instructions for such drugs you can read the following:

• They reduce the concentration of cholesterol in plasma due to inhibition of HMG-CoA reductase , as well as a decrease in cholesterol synthesis in the liver.
• Reduce cholesterol concentrations in people suffering from homozygous familial hypercholesterolemia , which is not amenable to treatment with lipid-lowering drugs.
• Their mechanism of action makes it possible to reduce total cholesterol levels by 30-45%, and “harmful” cholesterol levels by 40-60%.
• When taking statins, HDL cholesterol and apolipoprotein A increase.
• The drugs reduce the likelihood of ischemic complications by 15%, in particular, according to cardiologists, the risk of angina pectoris and myocardial infarction is reduced by 25%.
• No mutagenic or carcinogenic effects are observed.

Mechanism of action

How do statins help lower blood cholesterol? 80% of this organic substance is produced by the human liver from the component mevalonic acid. In order for this acid to be intensively produced, an enzyme called HMG-CoA reductase is required.

It is precisely to reduce its production that the action of statins is aimed. The more the production of the enzyme and, as a result, mevalonic acid decreases, the lower the cholesterol level will be. In such a situation, the only source of organic matter is food, if your own cholesterol ceases to be produced.

Having lost the ability to produce cholesterol, the liver seizes the opportunity to obtain it through other methods. For example, it increases the uptake of cholesterol from the blood, where it ends up after being taken in with food. To achieve this, the synthesis of receptors sensitive to “bad” cholesterol increases. The liver produces a large amount of fats, which are excreted in bile, and these functions require enormous resources from the organ.

Instead of removing toxins and harmful substances from the body, the liver has to constantly replenish cholesterol reserves, as a result of which the concentration of the compound in the blood decreases. According to statin manufacturers, such processes stop the growth of atherosclerotic plaques and serve to prevent the formation of blood clots in capillaries.

Side effects

Numerous negative effects may occur after administration:

• Frequent side effects: asthenia , insomnia , headache , constipation , nausea , abdominal pain, diarrhea , myalgia , flatulence .
• Digestive system: diarrhea, vomiting, hepatitis, pancreatitis , cholestatic jaundice, anorexia .
• Nervous system: dizziness , amnesia, hypoesthesia, malaise, paresthesia, peripheral neuropathy.
• Allergic manifestations: rash and itching of the skin , urticaria , anaphylaxis , exudative erythema, Lyell's syndrome.
• Musculoskeletal system: back pain, myositis , cramps , arthritis , myopathy .
• Hematopoiesis: thrombocytopenia .
• Metabolic processes: hypoglycemia , diabetes mellitus , weight gain, obesity , impotence , peripheral edema.
• The most severe complication of statin treatment is rhabdomyolysis , but this occurs in rare cases.

Drawing conclusions

Statins are a group of drugs created to reduce the concentration of cholesterol in the blood, prevent the serious consequences of heart and vascular diseases, surgical operations and diabetes.

Despite a lot of rumors about these drugs, if the attending physician considers it appropriate to prescribe statins, this recommendation should not be neglected. You can supplement therapy at home by eating healthy foods, but it is unreasonable to perceive this as the only correct method of treatment.

Who needs to take statins?

Informing what statins are, advertising stories and instructions for the drugs indicate that statins are effective drugs for lowering cholesterol, which significantly improve the overall quality of life, and also reduce the likelihood of developing strokes and myocardial infarction . Accordingly, taking these pills every day is a safe method to lower your cholesterol levels.

But in fact, until today there is no accurate information about whether treating patients with such medications is really so safe and effective. After all, some researchers claim that the potential harm and side effects outweigh the benefits of statins as a prophylactic drug used to prevent cardiovascular diseases. Experts are still arguing whether it is worth taking statins, weighing the pros and cons. Doctors' forums almost always contain debates on the topic “Statins - pros and cons.”

But, nevertheless, there are certain groups of patients for whom statins are required.

The latest generation statins must be used:

• for the purpose of secondary prevention after a stroke or heart attack ;
• for reconstructive surgical interventions on large vessels and the heart;
• in case of myocardial infarction or acute coronary syndrome ;
• with ischemic disease with an increased likelihood of stroke or heart attack.

That is, anticholesterol drugs are indicated for coronary patients in order to increase their life expectancy. In this case, to reduce side effects, the doctor must select the appropriate medicine and monitor biochemical parameters. If there is a 3-fold increase in transaminases, statins are discontinued.

The advisability of prescribing medications from this group for such patients is questionable:

• at low risks;
• for diabetes mellitus ;
• in women before menopause.

If statins are prescribed to people with diabetes, they may need additional tablets to lower their blood , since statins raise their blood sugar in such patients. Medicines to lower blood sugar should only be prescribed and their dosage adjusted by a doctor.

Currently in Russia, the treatment standards for most cardiac pathologies include the use of statins. But although medical prescription reduces mortality, this is not a prerequisite for prescribing drugs to all people with coronary artery disease or hypertension. They should not be used by anyone over 45 years of age or by anyone with high cholesterol levels.

It is important to consider the compatibility of these drugs with other drugs.

If necessary, together with anticholesterol drugs, the doctor prescribes other drugs for the treatment of cardiovascular diseases: Diroton , Concor , Propanorm , etc.

Diroton (active ingredient - lisinopril ) is used to treat arterial hypertension.

Concor (active component - bisoprolol hemifumarate ) is used for the treatment of arterial hypertension , heart failure, angina pectoris .

Representatives of the latest generation statins

The latest generation of statins can effectively normalize blood lipid levels while taking medications in a minimal dose. Their undeniable advantage is the minimum of side effects. This fact allows them to be prescribed for the treatment of elderly patients.

New generation statins are significantly superior to other generations of medications in terms of effectiveness and safety. When taking them, the level of low-density lipoproteins decreases, along with a simultaneous increase in the content of good cholesterol.

List of drugs related to new generation statins:

• Rosuvastatin,
• Tevastor,
• Rozulip,
• Mertenil,
• Akorta,
• Rosecard,
• Crestor.

They are presented in tablet form and have different dosages. Some of them, for example, Akorta and Rosuvastatin, are produced by Russian manufacturers. The names of the drugs are different, but the active ingredient in them is the same - rosuvastatin. This is a selective inhibitor of coareductase, which is the “ancestor” of cholesterol itself.

Tablets based on it help increase low-density lipoprotein receptors in hepatocytes. This allows you to enhance the capture and stimulate the breakdown of low-density cholesterol. As a result of the action of these drugs, there is a simultaneous decrease in the level of bad cholesterol and triglycerides.

The therapeutic effect of modern statins appears gradually. In the first 7 days from the start of treatment, it is practically unnoticeable. But already from the 2nd week their effectiveness reaches 90%. Their maximum effect appears in the 4th week of continuous use and remains stable thereafter.

New generation cholesterol-lowering drugs have the least side effects. At the same time, they cannot be completely excluded. Basically, a negative reaction affects the functioning of the liver and kidneys. Therefore, in severe pathologies of these organs, careful prescription of statins is required, taking into account their benefits and possible risks.

Latest generation statins effectively reduce bad cholesterol levels

Statin drugs, which belong to the latest generation of drugs, have good reviews from those who took them to lower cholesterol levels. The greatest pronounced effect from taking new generation statins can be achieved when treatment is combined with an anti-cholesterol diet.

List of statin drugs

Which drugs are statins, and what their cholesterol-lowering activity is, can be found in the table below.

Classification of statins

In medicine, certain parameters are taken into account for classification.

Origin:

• Synthetic: Cerivastatin , pitavastatin , Rosuvastatin , Fluvastatin , Atorvastatin ).
• Semi-synthetic: Simvastatin , Pravastatin .
• Natural: Lovastatin .

By generation:

• First generation: lovastatin ( Choletar , Cardiostatin );
• Second generation: simvastatin ( Vasilip , Simvacard , Simvastatin , Simvor , Simvastol , Simgal , Zocor , Owencor , Sincard , etc.), pravastatin ;
• Third generation: atorvastatin ( Atomax , Tulip , Liprimar , Atoris , Torvacard , Liptonorm , Lipitor ), cerivastatin , fluvastatin .
• Fourth generation: pitavastatin , rosuvastatin ( Crestor , Akorta , Mertenil , Roxera , Rosuvastatin , Rozulip , Rosucard , Rozart , Tevastor ).

How to replace statins

The question of how to replace statins at home in order to minimize the side effects of medications worries many people with high cholesterol. There are natural substances that help reduce this organic substance in the blood:

• ascorbic acid - natural products that contain large quantities of vitamin C include rose hips, currants, sauerkraut, bell peppers, citrus fruits, etc.;
• soy enzymes present in Asian products - tofu, miso, tempeh;
• pectins – present in apples, cabbage, bran, buckwheat and rolled oats, beans, carrots, lentils;
• resveratrol – dark grapes and cranberries;
• polyunsaturated fatty acids – vegetable oils, red fish, caviar, chicken eggs;
• curcumin

The only side effect of this diet is overeating. In everything you need to observe moderation, consuming a variety of foods containing natural statins every day. Garlic also contains them. By regularly eating the root vegetable, the capillaries are cleansed and the level of lipophilic alcohol in the body naturally decreases.

Natural statins

How to choose statins?

Despite all the reviews about statins for lowering cholesterol, the patient must decide whether to take such medications, but this should be done only on the basis of the recommendation of a specialist. What is important, first of all, is not the reviews, but the doctor’s prescription.

If a person nevertheless decides to take statins, then the choice factor should not be the price of the drug, but, first of all, the presence of chronic diseases.

Self-treatment if cholesterol is elevated cannot be carried out with any medications. Treatment for high cholesterol and lipid metabolism disorders is prescribed by a cardiologist or therapist. In this case, the specialist must assess the following risks:

• age;
• floor;
• weight;
• presence of bad habits;
• diseases of the cardiovascular system, other diseases (diabetes, etc.).

It is important to take statins in the dose prescribed by your doctor, and it is important to take a biochemical blood test as often as prescribed by a specialist.

If too expensive pills were prescribed, you can ask the doctor to replace them with drugs that are cheaper. However, it is recommended to use original drugs, since domestically produced generics are of lower quality than the original drug and generics offered by imported manufacturers.

Those who, before taking them, are interested in what the real benefits and harms of statins against cholesterol are, need to consider several important factors in order to minimize the harm of these drugs.

If the medicine is prescribed to elderly patients, it must be taken into account that the risk of myopathy doubles if taken together with medications for hypertension , gout , diabetes .

For chronic liver diseases, it is advisable to take Rosuvastatin in low doses; Pravastatin ( Pravaxol ) can also be used. These drugs provide liver protection, but when using them, you should absolutely not drink alcohol or practice antibiotic .

If there is constant muscle pain or there is a risk of muscle damage, it is also advisable to use Pravastatin, since it is not so toxic to the muscles.

People with chronic kidney disease should not take Fluvastin Lescol , nor should they take Atorvastatin calcium ( Lipitor ), as these medications are toxic to the kidneys.

If a patient seeks to lower low-density cholesterol, it is recommended to use different types of statins.

Currently, there is no clear evidence that it is advisable to take a combination of statins plus nicotinic acid. When taking nicotinic acid, people with diabetes may have a decrease in blood sugar, attacks of gout, bleeding from the gastrointestinal tract are also possible, and the likelihood of rhabdomyolysis and myopathies .

Contraindications to treatment

Like other medicines, statins have contraindications, in the presence of which they should not be taken:

• pregnancy and breastfeeding - the active substances of statins penetrate the placental barrier and can cause congenital malformations and fetal death. There is no specific data on whether the drugs change the composition of mother's milk, so it is better to refrain from using them during lactation;
• severe liver diseases - hepatitis, cirrhosis;
• alcohol abuse;
• special sensitivity to the components of the drug;
• severe dysfunction of the nervous system;
• osteoporosis;
• thyroid diseases;
• high risk of developing myopathy.

At the stage of prescribing statins, it is important what drugs the patient is already taking. The specialist must take into account the cross-interaction of drugs in order to avoid a sharp negative reaction of the body to their simultaneous use.

Research on the effects of statins on the body

Previously, cardiologists prescribed statins to people suffering from coronary artery disease , arterial hypertension , and those with low risks of cardiovascular pathologies.

Currently, the attitude towards this type of drugs among some specialists has changed. Although in Russia there have not yet been full-fledged independent studies of the effects of statins on the body.

Meanwhile, Canadian scientists claim that after using statins, the risk of cataracts in patients increased by 57%, and if the person had diabetes , by 82%. Such alarming data were confirmed by statistical analysis.

Experts analyzed the results of fourteen clinical studies that were conducted to study the effect of statins on the body. Their conclusion was that this type of medication reduces the likelihood of strokes and heart attacks, but given the serious side effects, they are not prescribed to people who have not previously suffered strokes or heart disease. According to researchers, people who regularly take such medications develop the following side effects:

• renal failure;
• cataract;
• liver dysfunction;
• depression , mood swings;
• myopathy;
• memory losses.

But in general, there are different points of view on whether these drugs are harmful or relatively safe.

• Scientists from Germany have proven that with low cholesterol levels, the likelihood of developing cancer , liver disease and a number of other serious ailments, as well as early mortality and suicide, increases, thereby confirming that low cholesterol levels are more dangerous than high ones.
• Researchers from the USA claim that heart attacks and strokes do not develop due to high cholesterol, but due to low levels of magnesium in the body.
• Statins can inhibit the important function of cholesterol in repairing disorders in body tissues. In order for the body to grow muscle mass, and for its normal functioning in general, low-density fat cells, that is, “bad” cholesterol, are needed. If its deficiency is noted, myalgia and muscular dystrophy .
• When taking such drugs, cholesterol production is suppressed, and accordingly, the production of mevalonate , which is not only a source of cholesterol, but also a number of other substances. They perform important functions in the body, so their deficiency can provoke the development of diseases.
• This group of medications increases the likelihood of developing diabetes mellitus , and this disease leads to increased cholesterol levels. Various sources claim that if you take statins for a long time, the risk of diabetes ranges from 10 to 70%. Under the influence of these drugs, the concentration of the GLUT4 protein in the cell, which is responsible for blood glucose levels, decreases. British researchers have proven that taking such medications increases the risk of diabetes in women by 70% after a menstrual break.
• Negative side effects develop slowly; accordingly, the patient may not immediately notice this, which is dangerous with prolonged use.
• When using statins, there is an effect on the liver. Those who are obese or lead a sedentary lifestyle note an improvement in their vascular condition for a period of time. But over time, complex processes in the body are disrupted, which can lead to a deterioration in mental processes, especially in older people.

When a person under 50 years of age has elevated cholesterol levels, this indicates that serious disorders are developing in the body that need to be treated. In some countries, programs are being implemented at the national level to promote lowering cholesterol levels by promoting an active lifestyle, changing dietary principles, quitting nicotine addiction, and using statins.

As a result, this method “worked” in many countries: mortality from cardiovascular diseases decreased significantly. However, there is an opinion that quitting smoking, physical activity and changing the menu are a better way to prolong life than using medications that have contraindications and side effects.

Statins for older patients

Among the arguments in favor of the fact that older people should take statins only after carefully weighing the harm and benefits, we can recall a study that involved more than 3 thousand people aged 60 years and older who took statin medications. Approximately 30% noted muscle pain, as well as decreased energy, high fatigue, and weakness.

Muscle pain is most severe in those who have just started taking such medications. As a result, this condition reduces the intensity of physical activity - it is difficult for people to exercise and walk, which ultimately leads to an increased risk of strokes and heart attacks. In addition, a person who moves little begins to gradually increase body weight, which is also a risk of cardiovascular disease.

Myths about the drugs of the group

Today, there are many ways to lower cholesterol levels, from following a diet, normalizing your lifestyle, giving up bad habits, to taking various medications. Many drugs are under development, but 99% of doctors' prescriptions come down to statins. What explains this?

The fact is that drugs of the statin group are hypolipidemic, that is, they lower the level of bad cholesterol in the blood and increase the level of good cholesterol. Medicines also prevent complications, reduce the level of vascular inflammation (this is key in the development of atherosclerosis), and reduce the risk of heart attack and stroke.

Statins stabilize atherosclerotic plaques that have already formed in the capillary cavities, which is why the life expectancy of patients who take the drugs as prescribed by a specialist increases. But this particular group of drugs is surrounded by a lot of myths common among people.

We need to figure out whether the rumors about statins are true, based on the opinions of practicing doctors:

• If you constantly use statins, it will no longer be possible to quit them. Indeed, people with elevated levels of lipophilic alcohol in the blood will have to take statins to lower cholesterol constantly. When the drugs are discontinued, especially in patients with a hereditary form of hypercholesterolemia, the indicators return to their original levels. But statins are not addictive in the drug sense.
• In addition to their benefits, statins also cause irreparable harm to health. With the constant use of lipid-lowering drugs, the capillaries are cleared, but the risk of developing cancer, liver and muscle tissue diseases, and diabetes increases. But when prescribing this or that drug, experts weigh the pros and cons. And for one new case of diabetes to occur, 250 patients must be treated over 4 years. Without treatment, 6 patients will simply die from a heart attack. Thus, an increase in the activity of liver transaminases during therapy with standard doses is recorded in two out of a thousand people. Much greater damage to the liver is caused by drinking alcohol and fatty foods.
• Cholesterol drugs do not have a positive effect on the body, they are just a ploy by pharmaceutical companies. Yes, taking statins does not directly affect a person’s well-being. But it is much more effective to take drugs with a long-term effect, which improve the prognosis of survival, rather than giving a momentary insignificant result.

Also, many believe that there are no drugs in medicine that can reduce high cholesterol levels. And to maintain a normal level of lipophilic alcohol in the blood, it is enough to consume certain foods daily.

Of course, proper nutrition is a good help in cleansing blood vessels, but no product or dietary supplement can effectively prevent the progression of atherosclerosis as well as medications prescribed by a doctor. Therefore, if a specialist recommends taking statins, you should not neglect the prescription.

Fibrates: what is it?

Fibrates are also used to lower cholesterol. These drugs are fibric acid . They bind to bile acid, thereby reducing the active production of cholesterol by the liver.

Fenofibrates medicinally lower lipid , which in turn leads to lower cholesterol. According to clinical studies, the use of fenofibrates lowers cholesterol by 25%, triglycerides by 40-50%, and also increases the level of so-called “good” cholesterol by 10-30%.

Instructions for the use of fenofibrates and ciprofibrates indicate that with high cholesterol levels, these drugs reduce the amount of extravascular deposits, and also reduce cholesterol and triglyceride levels in patients with hypercholesterolemia .

List of fenofibrate drugs:

• Thaicolor;
• Lipantil;
• Exlip 200;
• Ciprofibrate Lipanor;
• Gemfibrozil.

But, before you buy and take such medications, you should keep in mind that taking them leads to certain side effects. As a rule, various digestive disorders most often occur: flatulence , dyspepsia , diarrhea , vomiting .

The following side effects have been reported after taking fenofibrates:

• Digestive system: pancreatitis , hepatitis, vomiting, abdominal pain, nausea, diarrhea, flatulence, the appearance of gallstones.
• Musculoskeletal system: muscle weakness, rhabdomyolysis, diffuse myalgia, myositis, spasms.
• Nervous system: headache, sexual dysfunction.
• Heart and blood vessels: pulmonary embolism, venous thromboembolism.
• Allergic manifestations: skin itching and rash, photosensitivity, urticaria .

Combining statins with fibrates is practiced to reduce the dosage and, accordingly, the negative effects of statins.

Beneficial features

It is impossible to do without prescribing statins for some conditions, often life-threatening. The drugs help not only in treatment, but also in the prevention of various pathologies that often accompany high cholesterol levels. The pleiotropic effects of statins represent an effect on several targets at once, triggering different biochemical processes in the body.

Doctors identify the following pleiotropic properties of lipid-lowering drugs:

• are an addition to diet and a healthy lifestyle in patients with severe heart and vascular diseases;
• help to recover after a heart attack - during this period, elevated cholesterol levels are most dangerous, and statins prevent the re-development of a life-threatening condition for the patient;
• prevent implant rejection and deterioration in the well-being of a patient who has just undergone stenting or coronary bypass surgery by lowering con-cholesterol in the blood;
• serve as a stroke prevention - they help restore normal blood flow after a hemorrhage and prevent the formation of cholesterol plaques in the vessels;
• prevent blockage of blood vessels with severe circulatory disorders in obese people;
• stop progressive atherosclerosis.

With a hereditary form of hypercholesterolemia, many children need to take statins daily. This is necessary to prevent the development of coronary disease. Scientists have found that such a measure can prevent premature death by 93%.

All other medications

Your doctor may recommend taking dietary supplements (dietary supplements).

However, natural remedies such as Omega 3 , Tykveol , flaxseed oil , and lipoic acid lower cholesterol levels slightly.

It should be borne in mind that dietary supplements are not drugs, therefore such drugs are inferior to statin drugs in terms of preventing cardiovascular diseases.

List of dietary supplements that are used for this purpose and contain natural components:

• Omega Forte;
• Doppelhertz Omega;
• Tykveol;
• Lipoic acid;
• SitoPren.

Omega 3

Tablets containing fish oil ( Omega 3 , Oceanol , Omacor ) are recommended for people who want to lower cholesterol. Fish oil protects the body from the development of vascular and heart diseases, as well as from depression and arthritis. But you need to drink fish oil very carefully, since taking it increases the risk of chronic pancreatitis .

Tykveol

Pumpkin seed oil is indicated for use by those who suffer from cholecystitis , cerebral atherosclerosis hepatitis . The product provides choleretic, anti-inflammatory, antioxidant, hepatoprotective effects.

Lipoic acid

This remedy is an endogenous antioxidant , it is used for the prevention and treatment of coronary atherosclerosis. There is a positive effect of the drug on carbohydrate metabolism. When taken, the trophism of neurons improves, and glycogen levels in the liver increase.

Vitamins

Vitamins help normalize cholesterol levels, increase hemoglobin , etc. The body needs vitamin B12 and folic acid , nicotinic acid . At the same time, it is very important that these are natural vitamins, that is, it is important to eat those foods that contain these vitamins.

SitoPren

Dietary supplement – ​​fir foot extract, it contains beta-sitosterol, polyprenols. Should be taken for hypertension , atherosclerosis , high levels of triglycerides and cholesterol.

Policosanol

Dietary supplement – ​​plant wax extract. Helps reduce low-density cholesterol levels and helps prevent atherosclerosis.

Other means

Bile acid sequestrants ( Kolesevelam , etc.) are medications that are used in complex treatment as an auxiliary component for lowering cholesterol. They suppress its synthesis in plasma.

Ciprofibrate Lipanor - suppresses cholesterol synthesis in the liver, lowers its level in the blood, reducing the level of atherogenic lipoproteins.

Indications

Drugs in this group are prescribed only by a doctor and he selects which active ingredient is suitable and its dosage. Usually, for this purpose, the risk of cardiovascular events is determined using a special scale, questionnaire, and tests are taken to determine the lipid spectrum and biochemical blood parameters. Today, statins are prescribed not only after heart attacks and strokes as secondary prevention. Under certain high-risk conditions, a doctor may use statins in the primary prevention of cardiovascular disease.

Use in children and pregnancy

Children should not be given statins: their effect on a growing body has not been studied enough, and the benefits may be offset by complications. Such tablets are prohibited for use before the age of 18 and can only be prescribed in cases of familial hypercholesterolemia. Even in such cases, not all drugs are indicated for prescription.

Separately, it is worth noting the impossibility of treating pregnant women with statins; Even the safest medications are not prescribed in the absence of adequate contraception. This is due to the fact that changes in cholesterol synthesis can deprive the child of substances necessary for development. When planning a pregnancy, you need to stop taking statins a month before pregnancy, and you cannot feed your baby breast milk while the mother is taking statins.

Drugs that inhibit the absorption of cholesterol in the intestine

The first and so far only drug in this subgroup was ezetimibe. It works primarily in the villous epithelium of the brush border of the small intestine.

The mechanism of action is based on inhibition of the cholesterol transporter in intestinal enterocytes. This reduces cholesterol absorption by approximately 50%. The level of LDL and VLDL also decreases by 20–25% and the HDL content slightly increases.

The maximum effect of the drug develops after two weeks. When used as monotherapy at a standard dose of 10 mg per day, ezetimibe provides a reduction in LDL concentrations by no more than 17–18%, so it is more often used in combination with statins [3].

Side effects

Generally, ezetimibe is well tolerated. In rare cases, it can cause changes in the level of liver enzymes, as well as back pain, arthralgia, and weakness [1, 3].

What should I warn the client about?

If your doctor has prescribed a combination of ezetimibe and a statin, it is important to follow the recommendations and take both drugs to achieve optimal lipid-lowering effects.

Summarizing

The choice of appropriate drugs for high cholesterol is the prerogative of the attending physician. Only a specialist is able to assess the patient’s health and select pills for him depending on the indications and taking into account existing contraindications. When choosing medications, you cannot focus only on cost.

Cheap products may not always be of high quality, although a high price does not guarantee a quick and long-lasting effect. It is better to stick to the golden mean, follow the doctor's instructions and take the pills strictly according to the plan. Then the prescribed drug will be beneficial and will not have side effects on the body.

National Society for the Study of Atherosclerosis

The mechanism of action of statins is well studied. Statins inhibit the activity of the enzyme hydroxymethylglutaryl-coenzyme A reductase (HMG-CoA reductase), which converts acetyl coenzyme A into mevalonate, that is, they interrupt the first link in the chain of cholesterol synthesis:

Acetyl coenzyme A → mevalonate → 5 pyrophosphomevalonate → isopectyl pyrophosphate → 3,3 dimethyl pyrophosphate → geranyl pyrophosphate → farnesyl pyrophosphate → squalene → lanosterol → cholesterol

There is no generally accepted classification of statins; usually statins are listed in chronological order, according to their appearance. Statins can be classified according to their hydrophilicity, their metabolism by the cytochrome P450 system, and the strength of their lipid-lowering effect. Tables 1 and 2 show the main characteristics of statins [1,2].

Table 1.

Table 2.

Classification according to the strength of influence on the lipid spectrum of the blood

According to the severity of the lipid-lowering effect, statins can be arranged in order of weakening effect (Fig. 4).

Figure 4. Severity of the lipid-lowering effect of statins

The severity of the lipid-lowering effect of statins was studied by direct comparison in the MERCURY I study (as part of the GALAXY program). The effect of statins on LDL and HDL cholesterol levels was assessed [3]. Another study that directly compared the effects of rosuvastatin and atorvastatin was the STELLAR study. It demonstrated that a 10 mg dose of rosuvastatin was 3-4% more effective in lowering LDL cholesterol than a 20 mg dose of atorvastatin. Therapy with rosuvastatin at a dose of 10-40 mg led to a decrease in LDL cholesterol by 46-55%, therapy with atorvastatin at a dose of 10-80 mg led to a decrease in LDL cholesterol by 37-51% [4].

A comparative analysis showed that rosuvastatin at a dose of 10-40 mg/day. allowed to achieve the target lipid level in 82-89% of cases, while atorvastatin at a dose of 10-80 mg/day - in 69-85% of cases (Fig. 5) [4].

Figure 5. Effect of statin therapy on LDL and HDL cholesterol levels (STELLAR study results) [4]

In addition to the lipid-lowering effect, statins have an effect on atherosclerotic plaque, inflammatory factors and endothelial function (pleiotropic effects).

Effect of statin therapy on atherosclerotic plaque size

The correlation of LDL cholesterol levels with angiographic findings has been shown in several studies (Fig. 6) [5-10].

Figure 6. Correlation of LDL cholesterol levels with atherosclerotic arterial disease

The effect of intensive rosuvastatin therapy on the size of atherosclerotic plaque was convincingly demonstrated in the recently completed ASTEROID study [11]. This study examined the effect of rosuvastatin on the course of coronary atherosclerosis using intravascular ultrasound. The study included 507 patients with atherosclerosis of the coronary arteries (reduction of the lumen by no more than half the diameter for at least 40 mm). Treatment with rosuvastatin at a dose of 40 mg lasted 2 years.

Endpoints were changes in relative, absolute, and normalized plaque volume (RPV, AVP, and NPV). As a result, a decrease in AOB in the most affected segment of the coronary artery was shown by 6.8%, a decrease in AOB in the assessed segment of the coronary artery by 0.79%, a decrease in AOB in the most affected segment of the coronary artery by 9.1% (p

Figure 7. Reduction of atherosclerotic plaque during therapy with rosuvastatin 40 mg/day. for 2 years (ASTEROID study). Sonograms provided by Cleveland Clinic Core Laboratory (EEM - outer elastic membrane)

Effect of statins on inflammatory factors

In patients with atherosclerosis, certain cellular and humoral changes occur. The activity of cytokines, acute phase proteins, growth factors, and adhesion molecules increases. It has been established that the main factor initiating the synthesis of C-reactive protein (CRP) by hepatocytes is cytokines, primarily interleukin-6 (IL-6) [12]. Since CRP, interleukins and adhesion molecules are markers of inflammation, a decrease in their levels can be regarded as a positive effect. The mechanism of CRP reduction under the influence of statins is currently being actively studied [13]. Statins help weaken the expression of the IL-1 family of interleukins (IL-1?, IL-1?), which have a pro-inflammatory effect [14], and reduce the level of soluble protein (sCD40L) associated with the tumor necrosis factor TNF-?. High levels of sCD40L are associated with an increased incidence of recurrent cardiovascular events [15,16]. The anti-inflammatory effects of statins are also known, for example, their effect on the activation of leukocytes and the reduction of CRP levels [17,18]. It has been shown that the proinflammatory cytokine tumor necrosis factor, which impairs endothelial function, can be inhibited in macrophages by statin therapy [19].

The fact that statin therapy leads to a decrease in CRP levels has been established based on the results of large-scale studies. The analysis included studies with all statin drugs, including rosuvastatin. The anti-inflammatory effect of statins was discovered after studying their lipid-lowering effect. The ANDROMEDA study compared the effect of rosuvastatin and atorvastatin in reducing LDL cholesterol and CRP concentrations in patients with diabetes mellitus. Although the decrease in CRP concentration when taking rosuvastatin at doses of 10 and 20 mg exceeded the effect of atorvastatin at the same doses by 6-13%, these differences were not significant [20]. However, it can be said that rosuvastatin therapy has a pronounced effect on the level of CRP and other indicators of inflammation [18].

The results of the PROVE-IT TIMI 22 study [21] show that, given the same lipid levels during statin therapy, patients with low CRP values ​​had better outcomes after myocardial infarction or less progression of atherosclerosis according to intravascular ultrasound.

The target level for CRP reduction in the REVERSAL study [22] was 2.0 mg/l; this level of CRP is approaching the population level. Pravastatin (40 mg/day) and atorvastatin (80 mg/day) were compared. During pravastatin therapy, the absolute volume of atheroma increased by 2.7%; during atorvastatin therapy, cessation of atheroma growth was achieved (-0.4%, p = 0.98). Patients who simultaneously decreased plasma concentrations of both CRP and LDL-C had slower progression of coronary atherosclerosis as measured by intravascular ultrasound, as shown in this study [22].

The effect of statins on inflammatory factors continues to be studied in the ongoing JUPITER trial. JUPITER is a large, prospective, placebo-controlled study of rosuvastatin in patients without apparent hyperlipidemia (LDL-C 2.0 mg/L) [23].

Effect of statins on endothelial function

Dysfunction of the endothelium also plays an important role in the pathogenesis of IHD [24,25]. Endothelial dysfunction may serve as a marker for the early stages of cardiovascular disease [26]. Stimulation of nitric oxide synthesis or reduction of peroxide levels restores endothelial function. Drugs with similar properties include statins and angiotensin-converting enzyme (ACE) inhibitors [27].

Although the main effect of statins is a positive effect on the lipid spectrum, it is reliably known that reducing LDL cholesterol levels improves endothelial function [28,29]. Restoration of endothelial function [30,31] during treatment with statins leads to a reduction in cardiovascular risk [32,33]. Clinical studies confirm that a similar effect appears after 16 weeks of treatment [34], and it is not associated only with a decrease in LDL cholesterol levels [35]. This so-called pleiotropic effect of statins is explained by the fact that statins inhibit the synthesis of geranylgeranyl pyrophosphate, which activates the Rho protein (effector proteins, which are kinases that control cellular functions) [36]. This protein, based on guanosine triphosphate, regulates a large number of specific cellular reactions [37], changing the permeability of the vessel wall [38], causing adhesion and migration of monocytes through the endothelium [39]. Other mechanisms of action of statins are less clear; It is believed that statins may improve endothelial function directly and indirectly. For example, lovastatin and simvastatin have been shown to induce transcription of eNOS (endothelial nitric oxide synthase) genes in endothelial cells [40]. Thus, the pleiotropic effects of statins are no less important than the lipid-lowering ones.

Other possible effects of statins

In addition to those mentioned above, other effects of statins are discussed [41], but it should be noted that these effects have not been proven in large studies, so we recommend treating them with some skepticism.

1. Dilation of the coronary arteries.
2. Preventing spasm of the coronary arteries.
3. Stimulation of coronary angiogenesis.
4. Inhibition of vascular smooth muscle cell proliferation.
5. Inhibition of platelet aggregation, reduction in the number of platelets and red blood cells, due to which blood viscosity decreases.
6. Reducing thrombin levels and stimulating fibrinolysis, reducing the level of plasminogen activator inhibitor.
7. Increased NO synthesis by endothelium.
8. Inhibition of macrophage migration into the vascular wall.
9. Antioxidant action.
10. Immunosuppressive effect.
11. Reducing albuminuria in diabetes mellitus.
12. Reduction of left ventricular hypertrophy.
13. Antiarrhythmic effect.
14. Slows the progression of Alzheimer's disease and dementia.

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Choosing the best product

The effectiveness of drugs of different generations differs significantly: this becomes especially noticeable if a comparison is made immediately between the first and fourth. The quality of Crestor's work is 4 times higher than the capabilities of the best of the first drugs - Simvastatin. The higher the generation, the lower the likelihood that the treatment will cause harm, and the better the tolerability. Therefore, the search for the best medicine should be carried out between the leaders of the last two groups.

Liprimar wins on price: treatment is relatively inexpensive. In general, atorvastatin has been used more widely and has a greater track record of predictable results. Since the patient must take statins daily for many months, the choice of Liprimar helps to reconcile the effectiveness of treatment, safety and budget. Nevertheless, the drug takes a long time to start working: the rate of development of the initial effect is almost 2 times behind that of rosuvastatin.

Crestor, on the other hand, is more effective and can help in difficult cases. Most often, rosuvastatin is better tolerated, and the high rate of influence on cholesterol synthesis allows it to win the competition for the quality of the result and the reduction of consequences. The only question remains is the price.

Reception features

Despite the unpleasant effects of treatment, statins are quite capable of extending a patient’s life by ten years. For each patient, the dosage is selected individually: it is important to find the line between benefits and side effects. When trying to understand how to take statins correctly, at what time and under what conditions, patients can follow certain tips.

For better absorption, tablets should be taken once a day, a couple of hours before bedtime.

Statins are swallowed with water or any juice other than fresh grapefruit: this can cause serious complications.

Another important recommendation is to avoid alcohol. Sometimes, to reduce the chances of a side effect, the doctor may recommend a course of treatment with short breaks.

SUMMARY

• Statins are a relatively safe group of drugs. The risk of adverse events requiring drug discontinuation is comparable to placebo. The most common pathological increase in liver enzyme activity (0.3-5%, often at the beginning of treatment, is dose-dependent. The incidence of severe liver damage in patients taking statins does not exceed that in the general population (Cohen DE, Anania FA, Chalasani N , An assessment of statin safety by hepatologists. Am J Cardiol. 2006;97(8A):77C.)
• Assessment of liver function is required only before initiating statin therapy, with further follow-up studies only if clinically indicated [].
• The myotoxic effect of statins is rare: the frequency of myalgia is 2-11%, myositis 0.5%, rhabdomyolysis 0.1%. Routine measurement of the activity of the muscle-specific enzyme, creatine kinase, over time is not recommended, however, assessment of its level is advisable at the beginning of statin treatment and when the patient complains of muscle pain and muscle weakness.
• However, these symptoms can also occur in patients without pathologically elevated enzyme activity.
• Statins are more likely to cause muscle tissue damage in patients with chronic renal failure, liver disease with biliary tract obstruction, and in patients with hypothyroidism. In connection with the latter fact, before starting treatment it is also necessary to evaluate the level of thyroid-stimulating hormone (TSH) [].
• Statin use has been poorly studied for several decades. Prescribing statins to patients 20-30 years old requires individual consideration of each case.
• Statin therapy is contraindicated in pregnant women.
• When prescribing statins to elderly patients, it is necessary to take into account life expectancy and the range of chronic somatic diseases. If there is a serious pathology, prescribing drugs from this group is not advisable.