7 best cholesterol pills

*Overview of the best according to the editors of Healthy Food Near Me. About selection criteria. This material is subjective, is not an advertisement and does not serve as a guide to the purchase. Before buying, you need to consult with a specialist.

In this material, we will not just give an overview of drugs that in one way or another help to lower the fraction of “bad” cholesterol in the blood plasma, and thereby reduce the risk of cardiovascular disasters – heart attack and stroke. Let’s talk about the novelties of the pharmaceutical market in this area, and how they work. Indeed, many of these drugs are no longer prescribed because they have demonstrated their inefficiency (niacin, nicotinic acid), some are used in other dosages, and whole classes of new drugs are being introduced, which are still little known to doctors, and therefore they are poorly prescribed in the Russian Federation. .

Yes, indeed, drugs from the statin group are still considered the basis of lipid-lowering therapy. But sometimes a doctor who sets a specific goal – achieving certain cholesterol levels after a certain period of time, sometimes fails. Not all patients manage to achieve the planned values, and even if they are chosen correctly, without excessive requirements, and if other patients quite manage to achieve the desired indicators. What could cause such a series of failures? As it turned out, a special protein is produced in the human liver, the so-called proprotein convertase subtilisin / kexin type 9 (PCSK9).

Those readers who are diagnosed with atherosclerosis, or hypercholesterolemia, and who are forced to take statins, should remember this new abbreviation – PCSK9. It is this substance, or rather, its inhibitors, that are now beginning to play one of the leading roles in the treatment of atherosclerosis.

And now, before talking about new, modern and highly effective means to reduce the level of “bad” cholesterol in the blood, let’s remember who needs these drugs, and the key point for this will be a comprehensive assessment of cardiovascular risk in patients – high and very high risk. After all, it is precisely in order to reduce this risk that statins and other “cholesterol” pills are used. True, cholesterol injections have already appeared, but first things first.

Let’s evaluate the risk: high and very high

There have been some innovations in cardiovascular risk assessment. If earlier they were guided by the level of bad cholesterol fractions, the presence of bad habits, metabolic syndrome, age, and all this was understandable, but a little vague, now there are some new, more stringent criteria for at least high cardiovascular risk. We remind you that the very high risk group is 10% or more to die over the next few years from cardiovascular pathology associated with atherosclerosis, and the high risk group is from 5 to 10%. Let’s list them:

1. conducting multislice computed tomography of the coronary arteries of the myocardium. These are the very arteries in which blood flow stops during a heart attack – one of the main cardiovascular disasters. This study shows the severity of atherosclerosis directly in the coronary bed, and such people who, according to this study, have stenosis, or narrowing of at least two arteries by more than 50%, are classified as very high cardiovascular risk. Accordingly, they are prescribed statins in fairly high doses;

2. Also, when performing computed tomography of the heart, it is important to calculate coronary calcium, or determine the corresponding calcium index. This index shows how much calcium salts are deposited in soft tissues, and above all in the tissues of the coronary arteries. Such coronary calcium is very closely associated with the presence of atherosclerotic plaques, atherosclerosis, and vascular disease. Calcium retains X-rays very well, therefore, when conducting non-magnetic resonance, namely X-ray computed tomography (XCT), you can easily calculate the amount of this mineral. Therefore, if a patient with a coronary calcium index exceeds 100, the so-called Agatson index, then these are high-risk patients. Previously, such patients included only those with an index above 400;

3. There were changes in 2019 in patients with diabetes. Previously, all of them, regardless of target organ damage, were classified as high or even very high risk, but now even some patients with diabetes can be classified as moderate risk. These are people younger than 35 with insulin-dependent diabetes, or younger than 50 with type XNUMX diabetes. The main condition is that they do not have an additional risk, and diabetes mellitus has been less than ten years old.

4. But in the event that a patient has high cholesterol, and there is damage to target organs, such as kidney vessels, then this patient is at a very high risk. Under the defeat of target organs is meant retinopathy, that is, damage to the retinal vessels, diabetic polyneuropathy and the presence of protein in the urine by the type of microalbuminuria. If we are talking about people with type 1 diabetes mellitus, and the duration of the disease is more than 20 years, then this is a very high risk, regardless of other data and diagnoses;

5. Separately, it should be said about hereditary forms of familial hypercholesterolemia, which, of course, are at least at high risk. But the structure of these patients is also heterogeneous. Therefore, the new guidelines suggest that such patients should be classified as very high risk only if they already have cardiovascular disease and are diagnosed with atherosclerosis. At very high risk are those who do not yet have atherosclerosis, but have additional risk factors, such as high blood pressure, smoking, obesity, and so on;

6. the very high risk group would include all those patients who have atherosclerotic plaques in the carotid or femoral arteries. To do this, you can not carry out computed tomography, but rather a conventional ultrasound. If such plaques exist, but patients were at low or moderate risk on various questionnaires and scales, then they are now automatically transferred to at least a high cardiovascular risk group. It became known from the data of large studies that their presence is closely associated with the risk of developing major cardiovascular accidents, and this risk increases with the degree of damage to the carotid arteries;

7. no longer uses total cholesterol to assess high cardiovascular risk, it uses low-density lipoprotein cholesterol. And if in such patients their blood level is higher than 4,9 millimoles per liter, then even if they do not have any cardiovascular diseases and atherosclerosis, then they are classified as high-risk, and lipid-lowering drugs are prescribed;

8. the same applies to lipoprotein A. if it is higher than 180 mg / dl, then in such a patient the risk of developing cardiovascular diseases and severe atherosclerosis is about the same as if this patient had hereditary, familial hypercholesterolemia. Such patients are at least at high risk and treated.

By the way, lipoprotein A is partially composed of cholesterol, and its increase does not allow adequate use of statins. If low-density lipoprotein, LDL-C is effectively reduced with the use of statins, and the patient responds to treatment, then lipoprotein A shows stability and resistance, and resists treatment with statins, especially at usual dosages.

This fact may also explain the patient’s lack of response to conventional statin treatment. However, lipoprotein A is reduced quite well if PCSK9 inhibitors are added to therapy, on average, its concentration drops by 30%. Currently, you can take an analysis for lipoprotein A in any private laboratory in one working day, on average for 1000 rubles.

This substance may be considered normal at a concentration of less than 0,5 g per liter, or 50 mg/dL. High lipoprotein A is also closely associated with risk factors. It increases in the case of early development of coronary vascular disease, as well as cerebral vessels, it increases with smoking, various infectious diseases, as well as with a diagnosis of osteoporosis and treatment with bisphosphonates. High lipoprotein A occurs with nephrotic syndrome, chronic renal failure and advanced myxedema, or lack of thyroid hormones. By the way, it also increases during pregnancy, as well as during intense physical exercise, but the last two conditions do not belong to high cardiovascular risk factors.

Strategy: how are we treated?

Naturally, even new recommendations will convince and ask patients to change their lifestyle, normalize their weight, stop smoking, and begin actively and correctly treat existing diseases, or use medications for primary prevention. However, it is always necessary to start the treatment of “high cholesterol” with a diet that should be applied for 1-2 months. Sometimes just the right diet already gives an excellent result, and then, adding statins to it, you can already count on a completely different target cholesterol level.

In secondary prevention, when there have already been heart attacks, strokes, and the patient is compromised regarding cardiovascular accidents, it is necessary to apply lipid-lowering therapy to all patients whose low-density lipoprotein (LDL) level exceeds 1,4 mmol per liter.

The main component of this therapy is indeed still statins. At the same time, in order to achieve the target level of cholesterol, depending on the risk, it is necessary to use statins that act with high intensity, and moreover, at the maximum tolerated doses. What are the drugs that can provide the level of low-density lipoprotein by 50% or lower from the original, and, moreover, in the highest possible doses with good tolerance? They, first of all, will be atorvastatin and rosuvastatin. Atorvastatin is prescribed in dosages of 40 to 80 mg per day, and Rosuvastatin in doses of 20 to 40 mg per day. Quality statins from this group will be discussed below.

What if statin therapy, that is, the appointment of a single drug in the highest possible doses, could not lead to the desired reduction in cholesterol? Then the therapy is combined, and ezetimibe is added to the drug, which is also described in detail below. If this combination is not entirely effective, then a third group of drugs is added to the treatment, and the patient will eventually receive the selected statin, ezetimibe, and a drug from the PCSK9 inhibitor group. This powerful combination reduces baseline cholesterol and low-density lipoprotein levels in 85% of all patients and brings their risk to an acceptable population level.

What if the patient is intolerant of statins and develops side effects, preventing a dose increase? Then you need to immediately use ezetimibe, for example, after the liver “reacted” to statins with an increase in enzymes and bilirubin. If ezetimibe, as a primary drug, did not lead to the desired effect, then we add a PCSK9 inhibitor.

However, a modern strategy for reducing atherogenic fractions can also be formed with the appointment of other drugs. Thus, it is important to indicate the level of total triglycerides in the blood plasma. If the patient is at high or very high risk and triglycerides are approaching 5 mM per liter, then statins should be combined with eicosapentaenoic acid, at a dose of 4 g per day, along with the chosen statin. If we are talking about primary prevention (that is, when there has not yet been a cardiovascular accident), and the target level for triglycerides is 2,3 mmol / l or higher, then fenofibrate and bezafibrate can be used together with statins. These are also drugs from the group of lipid-lowering drugs, but only those belonging to the fibrate group, they will also be discussed below.

Review of the best cholesterol pills

Modern pills for high cholesterol and not only

Starting the list of modern drugs for the treatment of high cholesterol, we will first call them INN, that is, the international non-proprietary name. Then the first representative will be the original drug, which is equal to all other trade names of this drug, they are also commercial copies, or generics. A range of prices will also be given for the original drug, and for some of the more popular generics. Prices will be relevant for pharmacies of all forms of ownership in the Russian Federation for the end of April 2020.

The inclusion of certain drugs in the list is dictated by international clinical guidelines, as well as the decisions of the Congress of the International Society for Atherosclerosis, adopted in 2019. For obvious reasons, in 2020 all in-person congresses are canceled due to the epidemic and even pandemic of coronavirus infection, so the decisions and recommendations of this congress can be considered the latest scientific achievement in the treatment of atherosclerosis and lipid-lowering therapy.

And we will start the review with the recommended rosuvastatin and simvastatin, then we will look at ezetimibe, then the combined forms of statins along with ezetimibe in one tablet, and then we will look at PCSK9 inhibitors. In conclusion, we will analyze eicosapentaenoic acid, as well as some drugs from the fibrate group. Thus, in this review there will be no unnecessary drugs that can confuse the patient if he does not have a competent and thoughtful doctor.

Rosuvastatin (Crestor, Mertenil, Rosart, Rosistark, Rosucard, Rosulip, Rosufast, Roxera, Rustor, Suvardio)

Rating: 4.9

The original Crestor is really an expensive drug, and especially in a high dose. One package of medicine in tablets of 40 mg, calculated for a month (that is, 28 tablets) will cost from 5500 to 7300 rubles. The manufacturer of the drug is Astrazeneca. Fortunately, this is the maximum dosage, but such a package cannot be used for 2 months. It will not be possible to break a 40 mg tablet in half, and get 2 halves of 20 mg each: the tablets are convex, and are not intended for division.

If we talk about a package of 20 mg, then its price is from 3850 to 4950 rubles. There are also “decent” generics. So, Mertenil, which is produced by the Hungarian company Gedeon Richter, and under its control at a Russian plant, will cost from 20 to 762 rubles in the case of 1000 mg, and from 40 to 1400 rubles in a dose of 2020 mg.

Some Russian rosuvastatins are the cheapest on the market. So, rosuvastatin 40 mg, produced by Izvarino Pharma, will cost from 1400 to 1800 rubles per package of 30 tablets. And the Russian rosuvastatin weighing 20 mg, in a package of 30 tablets, manufactured by Vial LLC, will cost from 360 to 680 rubles.

We will not talk about the mechanism of action of Crestor, we will talk about important points for the patient. Cholesterol begins to decrease already one week after the start of treatment, and after 2 weeks the decrease is 90% of the desired effect, and after 2 weeks analysis can be carried out. The maximum effect develops in a month, and with regular use of the drug, it is maintained for a long time.

How to take Crestor? The tablet must be swallowed whole and can be taken at any time of the day, regardless of the meal. An important point: before starting treatment, the patient must begin to change his diet, and be on a hypocholesterolemic diet. He must follow the principles of the diet while taking Crestor. The recommended initial dose is 5 or 10 mg, once a day, and the dosage can be increased only after a month. Large doses should not be given immediately. Therefore, only a patient with a high or very high risk, or with a lower risk, but if the desired result was not achieved when taking a dose of up to 40 mg, can switch to a dosage of 20 mg a month after taking it. Such patients should be closely monitored, especially if the patient has chronic liver or kidney disease.

Advantages and disadvantages

Before starting therapy, a number of contraindications must be considered. In addition to individual intolerance, this is an active liver disease, high ALT and AST transaminases, severe chronic renal failure, muscle damage or myopathy, and the simultaneous use of cyclosporine. Crestor should not be taken during pregnancy. Also, patients on high doses must be aware of the risk of developing myopathy or rhabdomyolysis, or muscle breakdown. This leads to severe hypothyroidism, the presence of muscle diseases in the family, excessive alcohol consumption, and the simultaneous intake of fibrates. Also, 40 mg tablets are contraindicated in patients of Asian races.

There are also a large number of diseases in which Crestor and other rosuvastatins are prescribed with caution: this is a high risk of muscle damage, active liver disease. Among the side effects, sugar often rises, up to drug-induced type 2 diabetes (therefore, sugar monitoring is mandatory), headache, constipation and nausea, and muscle pain appear. In some cases, patients receiving rosuvastatin may have elevated protein in the urine.

In any case, a patient on high doses, 20 or 40 mg, must be observed by a doctor, and take regular tests for sugar, liver enzymes and “bad cholesterol”.

However, with all the disadvantages, the undeniable advantage of high-quality rosuvastatin, or Crestor, will be the ability to lower cholesterol, achieve its target values, and reduce cardiovascular risk. The high price of the original Crestor can be offset by the selection of a quality generic.

Atorvastatin (Liprimar, Atoris, Liprinorm, Torvacard, Tulip)

Rating: 4.8

Liprimar, or the original atorvastatin, is produced by the American company Pfizer, and one pack of 30 pieces of 40 mg each will cost an average of 600 rubles. This is much more profitable than using the original rosuvastatin. If we take the dosage half as much, then it can generally be bought at a price starting from 390 rubles. If we take the same package, but in the amount of 100 pieces, then we can completely meet 1300 rubles. If we assume that the maximum dosage of atorvastatin is 80 mg per day, then this is four tablets. Such packaging can be used for a whole month.

But, there are other atorvastatins, for example, Torvacard, manufactured by the Czech company Zentiva. In this case, a package of 90 tablets of 40 mg will cost from 1400 to 1800 rubles, in the case of the maximum dosage, it will last for a month and a half, with a European quality manufacturer and excellent pharmaceutical traditions. Finally, domestic atorvastatins, which are produced by the Russian pharmaceutical plant Ozon LLC, can be purchased at prices ranging from 400 to 500 rubles. for a pack of 30 tablets of 80 mg. In this case, this amount is enough for a month of taking at the maximum dosage. The question of the quality of the cheapest drug on the market always remains open.

Any atorvastatin is indicated for disorders of lipoprotein metabolism, for angina pectoris and infarction as a means of secondary prevention, and for chronic ischemic heart disease. All tablets are unmarked, film-coated and indivisible. According to international data, atorvastatin (naturally, the original Liprimar), in dosages up to 80 milligrams, reduces:

1. the content of total cholesterol by 30-46%;

2. Cs-LDLN — by 41–61%;

3. apolipoprotein-B (apo-B) — at 34–50%;

4. triglycerides – by 14-33%.

These are very good indicators, and at a dose of 80 mg it reduces the risk of myocardial ischemia and mortality by 16% after a course of four months, and the risk of repeated emergency hospitalization for angina pectoris threatening a heart attack – reduces by almost 26%.

Liprimar can be taken at any time of the day, regardless of meals. Before starting treatment, and during treatment, high cholesterol should be controlled by diet, exercise, and weight loss. Only under these conditions will any statin “work”. You also need to treat the underlying disease.

Advantages and disadvantages

The risk of overdose and complications is dose related. The higher the dose, the more the activity of liver enzymes can confidently increase, and usually when the dose is reduced, the enzymes return to normal. Therefore, a strict contraindication to taking Liprimar will be an active liver disease, such as hepatitis, or an increase in the activity of ALT and AST by more than 3 times compared to the norm.

Do not use the drug for pregnant, lactating women, as well as under the age of 18 years. It is forbidden to take it together with fusidic acid (a natural antibiotic of fungal origin). Patients with a history of liver disease and a risk of developing rhabdomyolysis, or muscle breakdown, should be taken with great caution.

There are also various side effects, of which headache, sore throat, constipation and nausea, muscle and joint pain, back and limb pain are common. Also, quite often, liver tests, serum creatine phosphokinase (CPK) increase, skin allergic reactions occur, and blood sugar rises. But in general, since the patient is treated under the control of various tests, and at high doses – under the constant supervision of a doctor, it is usually possible to avoid both side effects and the risk of overdose. From an economic point of view, the use of the original Liprimar is more justified than the more expensive Crestor.

Ezetimibe (Zetia, Ezetrol, Otrio)

Rating: 4.7

The original drug Ezetrol with the best quality is produced either by Merck Sharp and Dome, or Schering-Plough from Belgium. For 28 tablets, designed for a monthly course, you will have to spend from 1800 to 2500 rubles. in metropolitan pharmacies. There is also the drug Otrio, which is produced by the Russian Akrikhin. In it, exactly the same dosage of 10 mg, in the amount of 30 tablets, will cost from 430 to 560 rubles. How does ezetimibe work?

The drug works in the intestines, inhibiting the absorption of cholesterol. As a result, less cholesterol enters the liver, respectively, less cholesterol accumulates in the liver, and therefore the body, trying to increase its reserves in the liver, removes it from the blood to the liver, and its concentration in the blood decreases. This drug, unlike statins, does not reduce the synthesis of hepatic cholesterol and does not increase the excretion of bile acids. This remedy is used, according to modern treatment tactics, together with statins, but ezetimibe can also be used independently if statins are contraindicated. Ezetrol, or Otrio, just like statins, should be taken against the background of a lipid-lowering diet and non-drug treatments: normalizing body weight, increasing physical activity and giving up bad habits. You need to use the medicine one tablet once a day for a long time.

Advantages and disadvantages

There are not so many generics of ezetimibe, and it is difficult to get it in small towns: perhaps only in cities with a population of over a million there is either a generic or an original drug. He has few contraindications, this is hypersensitivity, as well as chronic, severe liver failure. It is also not advised to take this remedy with fibrates, but only because there were no relevant studies on this topic. If the patient is receiving cyclosporine, then care must be taken, and the drug is also not indicated for persons under 18 years of age, pregnant and lactating women.

Side effects are also possible: if one ezetimibe (monotherapy) is taken, then there may be a headache, abdominal pain or diarrhea. And if there is a combination with statins, then the effects characteristic of statins are also noted, for example, myalgia and an increase in liver enzymes. Therefore, before you start taking the drug, you need to know whether it can be bought continuously in pharmacies. In addition, the cost of the original remedy can be considered quite high, especially if Crestor is co-administered in a high dose, then the monthly course will cost about 6-8 thousand rubles. But if we take into account that the patient will save on sausages, canned food, buns and alcohol while on a diet, move more, and spend less money on travel or gasoline, then you can also save.

Rosulip plus

Rating: 4.6

Above, we said that if monotherapy with statins does not achieve an effect, then ezetimibe is added to the statin. Since both drugs are available in tablets, it was not difficult to establish a combined production of rosuvastatin with ezetimibe. Rosulip plus ezetimibe is available in capsules, 20 + 10 mg. There is also a dosage of 10 + 10. For a pack of 30 tablets (20 + 10), you will pay from 1200 to 1600 rubles. Accordingly, this packaging is convenient for those patients who do not require higher doses of rosuvastatin, and they will “go” well on 20 mg if the regimen is strengthened with ezetimibe.

Rosulip plus is produced by the Hungarian pharmaceutical company Egis, and this is a good choice: two products instead of one, and of European quality. Accordingly, it is supposed to take one tablet once a day, instead of two. The economic efficiency of such a combination is indisputable, and we will not list the contraindications and side effects for Rosulip plus separately, since they are described above for each of the components of the drug separately. You just need to sum them together.

Alirocumab (Praluent) and evolocumab (Repata)

Rating: 4.5

Finally, we proceed to describe the “heavy artillery” in the world of hypocholesterolemic therapy. At the beginning of the article, we wrote that there is a special protein, PCSK9, which regulates the consumption of lipoproteins from the blood by cells, and statins taken by patients can involuntarily increase the concentration of this protein themselves. As a result, a situation arises that taking statins by itself, “with its own hands” blocks its own effect, expected from statins. Therefore, an increase in the plasma concentration of this protein may be an important reason for the failure of statin treatment in many groups of patients.

How to deal with a high concentration of protein, or block its effect? The answer is well known. These are monoclonal antibodies that inhibit the active groups of enzymes, or turn off the function of individual proteins. Alirocumab is used parenterally, like any drugs from the antibody group, and is available in syringe pens. It is technologically quite difficult to obtain this medicine: molecular genetic production is necessary here. Praluent produces a culture of Chinese hamster ovary cells into which recombinant DNA is introduced that carries a specific amino acid sequence. They are needed to create antibodies, weighing 146 kilodaltons. Praluent’s task is to suppress the activity of PCSK9, and allow statins to work “as expected”.

It is necessary to administer the drug in doses of 75 or 150 mg every 2 weeks. A disposable, pre-filled syringe pen is placed subcutaneously in the thigh, abdomen or upper arm. Praluent is initially given at a dosage of 75 mg once every 2 weeks, but the dose is adjusted and then it can be increased, up to 150 mg also every 2 weeks, or a dose of 300 mg once a month.

How much will this treatment cost? In the case of 75 mg, there are just 2 syringe pens in one package, and one monthly course will cost starting from 29000 rubles. If the dosage is 150 mg, then you can purchase the drug in the capital’s pharmacies, starting from the cost of 33000 rubles. for a monthly course.

There is another drug from this group, which has a similar mechanism of action. This is Repata, but it needs to be administered 140 mg every 2 weeks, and this will cost from 14000 rubles, however, just for one syringe. Therefore, the monthly rate will again be about 30000 rubles.

We will not give the advantages and disadvantages of monoclonal antibodies here, since not all readers will be able to purchase this drug for themselves, because even at a very high risk, this is a 3rd line drug. Recall that at first they try to cope with diet and physical activity, modification of lifestyle. Then statins are prescribed, brought to the maximum dosage, then ezetimibe is added, and only then, with a very high cardiovascular risk, these very, very expensive (for Russians) drugs can be used. Abroad, in countries where the cost of living is above 100 thousand rubles, they are quite affordable. The official instructions for monoclonal antibodies are very specific, they are very long, overloaded with very important information for the doctor, and we will leave the explanation of these very important details for specialists who will prescribe monoclonal antibodies to patients.

Eicosapentaenoic acid

Rating: 4.4

It was mentioned above that in patients of special groups with a certain level of triglycerides, this eicosapentaenoic acid can also be used in combination therapy. In fact, this is a food supplement, not a medicine in the usual sense. This is a fatty acid that is found in fish oil, and the remedy, in principle, can be successfully replaced with oily fish. It can be salmon, cod liver, or herring, but not smoked, as this is contrary to the principles of a hypocholesterolemic diet.

After all, it has long been found out that the peoples living along the coast and who feed mainly on fish suffer much less from coronary heart disease. This acid belongs to the omega-3 family of acids, and is successfully produced in capsules, protecting against myocardial ischemia. At the same time, the systematic use of fatty fish contributes to an increase in high-density lipoproteins, which, on the contrary, protects a person from atherosclerosis, and belong to anti-atherogenic lipoproteins.

According to international recommendations, the required amount of omega-3 ranges from 0,5-2 to 3 g / day. But it is unlikely that you will consume a large amount of fish, because you can buy fish oil in the form of various omega-3 unsaturated acids in capsules. However, fish oil can help fight high levels of bad cholesterol. The choice of such capsules is very large, they are sold without a prescription, and any pharmacy will pick them up for you.

Fenofibrate (Tricor, Exlip, Grofibrate, Lipantil)

Rating: 4.3

Finally, consider Tricor, or the original fibrate drug: fenofibrate. The second representative, whose name was given at the beginning of the article, namely bezafibrate, or Holestenorm, currently does not have a registration certificate in Russia, and you cannot buy it. Therefore, consider Trikor. It is produced by the French Fournier Laboratory, and you can buy 30 tablets of 145 mg at a price of 800 to 900 rubles. for packing.

Fibrates have a common mechanism, they activate lipoprotein lipase, which breaks down fat and removes lipids from adipose tissue into the blood. As a result, dietary fats are broken down, including not only triglycerides, but also alimentary cholesterol. The use of fibrates improves the biochemical characteristics of the blood and reduces the concentration of lipids in it.

Traykor and its analogues have the ability not only to reduce total blood cholesterol by 20-25%, but also triglycerides by 40-45%, and reduce the concentration of uric acid in the blood plasma: that is, reduce the severity of uricosemia by 25%. If treated with the drug for a long time, it helps to effectively reduce cholesterol deposits in the form of plaques.

Indications for use are hereditary hypercholesterolemia, and the presence of concomitant risk factors, including high and very high risk. The medicine is used orally, at the rate of 1 tablet 1 time per day.

Advantages and disadvantages

Traykor and its analogues are contraindicated in severe renal and hepatic insufficiency, in diseases of the gallbladder, with severe phototoxicity, if ketoprofen from the NSAID group was previously prescribed. The drug is not prescribed for children and young men under 18 years of age, as well as women during lactation and pregnant women. With caution, Traykor requires an appointment for cholelithiasis or urolithiasis (by reducing uric acid in the blood plasma, it increases its output in the urine, and if the patient has urinary stones, the drug can provoke their growth), as well as in case of alcoholism.

The agent may cause side effects. These are abdominal pain, nausea and flatulence, symptoms of exacerbation of pancreatitis, increased activity of liver enzymes, and many other effects. Plasma creatinine and urea may also be elevated. In the event that Traykor is combined with anticoagulants, such as warfarin, the possibility of bleeding increases. However, this drug is considered a sufficiently powerful hypocholesterolemic agent that can be combined with statins.

About nicotinic acid: long-term delusions of doctors

Rating: 4.2

We all know that there is nicotinic acid, which is designed to lower the concentration of “bad” cholesterol, and increase the concentration of “good”. Nicotinic acid, or niacin, or PP, or B3 is a representative of B vitamins, which, among other things, is found in food. Nicotinic acid reduces the breakdown of fats, that is, spontaneous lipolysis. This leads to a decrease in the concentration of lipids in the blood, with a decrease in the concentration of low-density lipoproteins (bad), and an increase in the concentration of high-density lipoproteins (antiatherogenic, “good”).

Also, nicotinic acid reduces the synthesis of cholesterol in the liver, and dilates blood vessels. Nicotinic acid has even been shown to reduce existing cholesterol plaques and lower blood sugar, which is very important in type XNUMX diabetes, which often accompanies hypercholesterolemia in old age. Along with increased body weight, the so-called metabolic syndrome is formed.

A small concentration of acid exhibits a vitamin-like effect, and does not affect the level of lipids in the blood, but only in a large dosage, from one and a half grams to 6 g daily, it has this distinct hypolipidemic effect, although it is less pronounced than from taking statins. According to classical data, before the era of evidence-based medicine, it:

1. reduces cholesterol in the form of low-density lipoprotein up to 18%;

2. neutral fat triglycerides up to 26%;

3. increases good cholesterol levels by 15 to 30%.

At the same time, nicotinic acid is produced both in tablets and in solutions for injection, and its price is quite low: a package of 10 ampoules can cost 50 rubles, and a can of 50 tablets does not exceed the price of 78 rubles.

However, the disadvantages of nicotinic acid are a continuation of its advantages. This vitamin dilates blood vessels so well that the skin can turn red, hot flashes occur, intense skin itching, and a headache appear. From the gastrointestinal tract, heartburn and nausea, flatulence and bloating, diarrhea may occur.

If the drug is parenterally administered quickly enough, then a sharp drop in blood pressure may occur due to vasodilation, orthostatic hypotension, that is, lightheadedness and fainting when standing up abruptly, a collaptoid state.

If this medicine is used for a long time (namely, such use is necessary for the treatment of high cholesterol), then signs of fatty degeneration of the liver, an increased concentration of uric acid in the blood plasma, and an increased activity of liver enzymes may appear. These are quite severe side effects, which are usually managed by gradually increasing the dose.

A person gets used to nicotinic acid, and with addiction, the vasodilating effect gradually decreases. Therefore, treatment was started with small doses, and then little by little, over the course of a month, they reached average therapeutic dosages – 2-3, and sometimes up to 6 g per day, in order to lower cholesterol. Also widely used and prolonged tablet form of nicotinic acid, 500 mg per tablet, called Enduracin.

Thus, nicotinic acid has been used to normalize cholesterol levels since the fifties of the last century, with natural limitations due to the development of side effects. Then came the era of evidence-based medicine: randomized, double-blind, placebo-controlled studies, meta-analyses, the era of Cochrane reviews and protocols. And then, with respect to nicotinic acid, an unexpected, evidential surprise arose.

It all started with the attempts of Western companies to somehow neutralize the side effects, and the reddening of the face and upper half of the torso, the feeling of a rush, was especially annoying. New preparations of nicotinic acid were needed to lower cholesterol.

For this, another component, laropiprant, was added to nicotinic acid, and as a result, the complex drug Tredaptive was launched on the market. As a result, he was supposed to retain the effects of nicotinic acid, but not have such pronounced side effects. “Tredaptive” was registered in Russia in November 2011, but it never went on sale.

Large-scale studies have been carried out in Europe, which have shown that, nevertheless, its safety is inferior to the effectiveness of this medicine. What happened? Merck itself, which brought this drug to the market, was interested in reliable information about its effectiveness, and conducted a large-scale study together with experts from Oxford University.

The results were amazing: this drug did not lower the risk of death, and it remained exactly the same, as if no cure for atherosclerosis had been prescribed. It turned out that if you add “nicotine” to statins, then there was no reduction in the risk of coronary death, as well as stroke, but at the same time, patients had significantly more frequent adverse reactions than on statins alone. At the time of the publication of the study, “Tredaktiv” was sold in 40 countries, but by the time the study was published in our country, they decided to abandon it, and it never went on sale.

The study was quite impressive in scope. It involved about 15000 people from Europe and 11000 patients from China. At the same time, 50% of them received only statins, and the second half received a combination of a statin along with Tredaptive. The follow-up period for patients was 4 years. Studies did not reveal any significant difference in risk. Nicotinic acid with high cholesterol did not work on the “end points”, and this is the most important thing.

In addition, Cochrane Reviews identified an additional 23 studies on this topic, which were conducted up to August 2016. In total, about 40000 people took part in these studies. After all, maybe it’s not nicotinic acid that is to blame, but its interaction with a statin, or is the second component of Tredaptive, laropiprant, to blame? Therefore, these studies compared pure nicotinic acid itself versus placebo.

The average age of the patients was about 65 years, all of these individuals were compromised by atherosclerosis, some of them had a heart attack, and the period of taking nicotinic acid in this large number of subjects lasted from six months to 5 years. As a result of painstaking processing of the research results, it turned out that nicotinic acid did not affect the end point in any way: the reduction in the number of heart attacks, strokes or deaths did not exceed the average statistical error.

And there was no difference in the number of heart attacks and strokes: before the start of taking nicotinic acid, or after its long-term use, a catastrophe occurred.

Thus ended the glorious age of nicotinic acid, which has long been used to lower cholesterol. There is no point in her. Nicotinic acid and cholesterol were incompatible.

On the other hand, this does not mean at all that nicotinic acid has left the stage. She retained a remarkable vasodilating effect, which is still successfully used in the treatment of diseases, which were mentioned in the general indications for the drug. As for the Tredaptive drug, there is still information about it on pharmaceutical sites, for example, on the Vidal website. But at the same time, the drug itself is not available in pharmacies, and the information still remains, like the light from a long-extinguished star.

Attention! This material is subjective, is not an advertisement and does not serve as a guide to the purchase. Before buying, you need to consult with a specialist.