Statins of the last generation: advantages, prices, reviews

Preparations of the class of statins have been synthesized as a means to reduce serum cholesterol and reduce cardiovascular risks. For a long time, researchers and doctors worked only with drugs "Lovastatin", "Pravastatin", "Simvastatin", "Fluvastatin." Then, "Atorvastatin" and "Rosuvastatin" were synthesized - these are statins of the last generation, or rather, the most effective drugs in this category. Also, the development of new, that is, even safer and more effective statins, is underway, among which the greatest popularity belongs to Pitavastatin.

General pharmacological characteristics of statins

All statins belong to the category of drugs that affect the lipid metabolism in the human body. In the anatomical-therapeutic-chemical classification of drugs, they are designated code C10AA and refer to inhibitors of HMG-CoA reductase. Inhibiting the activity of this enzyme, they disrupt the synthesis of cholesterol, significantly reducing its serum amount. This action of statins makes it possible to achieve the recommended concentrations of low density lipids in the blood.

Such effects can significantly reduce the rate of atherosclerotic plaque development. Also, drugs prevent its appearance. Even with its presence, statins have a valuable effect: they stabilize the endothelium over the atherosclerotic plaque, and therefore significantly reduce the likelihood of coronary thrombosis, acting by a different mechanism than antiplatelet agents. Moreover, the joint use of these agents allows even more to reduce the likelihood of a heart attack. Because the price set on statins is fully justified.

Features of classification of statins

There are several approaches to the separation of drugs into classes. They can be considered from the point of view of the synthesis features. Also, since treatment with various statins requires administration at different doses, it is prudent to introduce a classification based on the recommended dosages. The classification by generation looks as follows:

• I generation: "Simvastatin", "Pravastatin", "Lovastatin".
• 2nd generation: "Fluvastatin".
• Third generation: "Cerivastatin", "Atorvastatin".
• IV generation: "Pitavastatin", "Rosuvastatin".

All statins are divided into artificial, synthesized from raw materials, and natural. The latter include Lovastatin, Pravastatin and Simvastatin. Synthetic are all other drugs: "Fluvastatin", "Atorvastatin", "Rosuvastatin" and "Pitavastatin".

Classification of statins depending on doses of administration

All drugs class, including the latest generation of statins, it is reasonable to divide into low-dose (up to 8 mg), medium-dose (10-40 mg) and high-dose (40-80 mg). In particular:

• High-dose preparations ("Atorvastatin", "Lovastatin", "Fluvastatin");
• Medications (Simvastatin, Pravastatin, Rosuvastatin);
• Low-dose drugs ("Pitavastatin").

This classification reflects the possibilities of prescribing drugs and their therapeutic breadth. In particular, high-dosage drugs have an effect in high amounts, and are well tolerated. Medications other than "Rosuvastatin" are worse tolerated in high doses, but have a good effect.

The moderate-dose statin "Rosuvastatin" can be given at a high dosage (80 mg) if necessary, although it is often not required because of a fairly complete decrease in total cholesterol and its low-density fraction. "Pitavastatin" and does require the appointment in minimum quantities, because of which the risks of its adverse reactions are many times lower than in class analogues.

History of development and introduction of statins

The history of statins is very ambiguous. Initially, their development was severely hampered by the lack of knowledge of cholesterol metabolism and the likelihood of developing atherosclerosis, depending on blood lipid levels. Moreover, gepoholesterinemic agents were synthesized immediately in order to inhibit microflora in cultures of molds intended for the production of pure penicillins. The discovery of the anticholesterol effect of a number of substances produced by fungi, and made it possible to study statins.

The first statin was compactin, and not introduced into clinical practice because of the many opposing opinions about its effects. It was isolated from the culture of Penicillium cetrinium. Then Monaclin K, patented in February 1979, was isolated from Monascus ruber culture. In June, 79th, they patented mevinolin, which later became known as "Lovastatin". This drug was used in the clinic, after which the statins of the last generation were isolated or synthesized.

A lot of opposing opinions hampered the development of statins, after which it was decided to conduct large-scale clinical tests. To date, the largest and most useful was the study of the Scandinavian Simvastatin Survival Study. Its abbreviated name is "4S". It fully refuted the possibility of developing carcinogenic diseases associated with taking drugs, and proved that their use significantly increases life expectancy and reduces the incidence of acute coronary pathologies.

Abstracts in favor of statins

With an initial total cholesterol concentration of 7.4 mmol / L, statin therapy and achieving a level of 5.4 mmol / L significantly reduces the risk of a fatal cardiovascular event by 40% in the next 5 years. In a number of other studies, it has been shown that lowering the total cholesterol level by as little as 1 mmol / L by one-fifth reduces the likelihood of coronary thrombosis and therefore of a heart attack or stroke.

Considering statins for and against which many experts and patients speak, it is possible to understand the following facts: prescribing drugs can be already at the age of 40 years and older, and reducing the risk of heart disease is a rational tactic of prolonging life. And since the price is quite affordable for statins, these medicines that have proved their effectiveness can be taken without damage to their own budget. Of course, the statins of the last generation are much more expensive, although the same "Rosuvastatin", in principle, is quite affordable for the patient. And the cheapest form is the drug "Mertenil".

Comparative characteristics: pros and cons

Evaluating statins, for and against them to speak very simply. Arguments for are the features of their therapeutic effect: reduction of blood cholesterol and its low-density fraction, prevention of risks of acute events and assistance in their treatment. However, such drugs as statins, there are also contraindications. There are also side effects that mediate arguments against use.

With statin therapy, there is a risk of myopathy. Probably, it is mediated by the inhibition of the synthesis of cholesterol, which the muscles need. The frequency of this effect is extremely low, although it increases with joint admission with other lipid-lowering agents. There is also a risk of developing oncological pathology of the liver, although the probability of such a disease, as shown by recent studies, is extremely low. Moreover, the fact that oncological diseases were provoked by other factors was also proved. Hence, in the "statin" group drugs, contraindications should prohibit the joint intake of these drugs with other agents that contribute to reducing the concentration of fats in the cells.

The cost of statins of the latest generation

The statins of the last generation are different, although their effects are worth paying for. The only other issue is that the results of their action can be achieved with the use of cheaper class analogues of the early generations. In particular, for the most common statin of the IV generation, "Rosuvastatin", the price is approximately as follows:

• 600 rubles for pills of 40 mg;
• 400-450 per tablet of 20 mg;
• 300-350 for 10 mg tablets;
• 200 rubles for 5 mg.

The package contains 30 tablets, which is sufficient for a monthly course of therapy, whereas for a monthly treatment of Pitavastatin, the prices are approximately the following:

• Tablets of 1 mg cost about 700-750 rubles;
• Tablets of 2 mg - about 1000 rubles;
• Tablets of 4 mg - about 1500 rubles.

The choice between "Pitavastin" and "Rosuvastatin" is based on four criteria: the price factor, the rate of decrease in low-density lipoproteins, the completeness of high-density lipoproteins, safety. The speed of cholesterol reduction and the increase in HDL, as well as the best price, looks like "Rosuvastatin", whereas the more safe theoretically is "Pitavastatin".

The latter is twice as expensive in comparison with "Rosuvastatin". Nevertheless, it is possible to use other, cheaper statins. The most economically viable was Simvastatin. Now it was replaced by "Atorvastatin", which is regularly replaced by "Rosuvastatin" (its value will necessarily fall). And if prices for statins of the last generation are too high for patients, then it is worth considering the possibility of treatment with "Atorvastatin" or "Simvastatin." By the way, most of the research was done with "Atorvastatin".

Arguments in favor of statin use by elderly people

Previously, clinicians reluctantly prescribed statins to patients older than 75 years. The reason for this were the following factors:

• Taking several drugs of other classes;
• Mutual reluctance to add another class of medicines;
• Absence or low compliance of treatment;
• Unwillingness of patients themselves to buy statins and use them because of a lack of understanding of their effects.

A number of studies conducted with "Simvastatin", "Pravastatin" and "Atorvastatin" have shown a significant reduction in mortality in patients older than 75 years. Moreover, the decrease in mortality rates was even higher than in patients in the age groups 55-65 and 65-75 years. Therefore, for drugs of this category (statins), experts' reviews unequivocally confirm one fact.

These drugs can and should be taken at a later age, regardless of whether there have been previously acute vascular disorders. And patients who really care about reducing the risk of their death from myocardial infarction or stroke, you need to understand that if the drug is effective and safe, then it is definitely worth taking. Moreover, the treatment with statins has become more accessible and will continue to be so.

Characteristics of reviews from statins of recent generations

Reviews of patients when assessing the quality of a particular generic statin are not indicative, because they do not feel significant changes from taking medications. Improving the lipid profile of the blood does not manifest itself on the health and has no external signs. It is recognized only by a lipidogram. Therefore, when evaluating a statin, it is reasonable to be guided by the opinions of specialists. And about the drugs in which the active substance is Pitavastatin, domestic specialists can not respond.

In clinical practice in the CIS, "Pitavastatin" because of the high cost and because of the presence of "rosuvastatin" and its generics is not applied. The "Rosuvastatin" preparations, which are indicated above, have a quick action: the lipid profile normalizes within 1-2 months. In "Atorvastatin" this time is one and a half times more. Also, the generics of "Rosuvastatin" are safer, as they are metabolized by two types of cytochrome. At the moment, this information, taken from the opinions of specialists, plays a crucial role in the choice of statin in specific clinical situations.

General conclusions about statins of recent generations

Preparations "Pitavastatin" and "Rosuvastatin" are the most modern among representatives of the class of statins, for which a large evidence base is collected. Their effects are generally similar to those of Atorvastatin, but there are also differences. "Pitavastatin" and "Rosuvastatin" can achieve the target cholesterol levels, as well as low-density lipoprotein at a lower dosage than "Atorvastatin."

In addition to the above superiority of statins of recent generations, another aspect is also important. Namely: in the treatment of "Pitavastatinom" and "Rosuvastatin", a more rapid normalization of blood lipids and the elimination of homocysteinemia are observed. This is important both in the case of acute coronary pathology, and in chronic ischemic disease, provoked by coronary atherosclerosis. The safety of statin use is higher than that of acetylsalicylic acid. Nevertheless, the presence of contraindications prohibits their use by a certain contingent of patients (see general contraindications).

Examples of drugs

Medicines containing "Rosuvastatin" are produced under the following trade names: "Akorta", "Rosistark", "Rosukard", "Rosart", "Mertenil", "Rosulip", "Roxera", "Rustor", "Tevastor". All these preparations are generics of "Crestor", which became the first rosuvastatin. The drug, in which the active ingredient is Pitavastatin, is registered as "Livalo". Its generics are "Pitavas" and "Pivasta". In the CIS, they do not occur, although they are registered in the pharmacopeia.

Summary

In accordance with the effects of class drugs and performed analysis of the effectiveness of their appointment, the use of statins is justified for stabilizing atherosclerotic plaque and preventing its tearing. They are also used to reduce the intensity of atherosclerosis, affecting the lipid profile of blood serum. As a result, this class of drugs is really needed in cardiology. And qualitative statins of the last generation are already effective means of preventing fatal coronary thromboses.