Statin drugs have been synthesized as a means to lower serum cholesterol and reduce cardiovascular risks. For a long time, researchers and doctors worked only with the drugs "Lovastatin", "Pravastatin", "Simvastatin", "Fluvastatin". Then, Atorvastatin and Rosuvastatin were synthesized - these are the latest generation of statins, or rather, the most effective drugs in this category. Also, new, that is, even safer and more effective statins are being developed, among which Pitavastatin is the most popular.
General pharmacological characteristics of statins
All statins belong to the category of drugs that affect lipid metabolism in the human body. In the anatomical, therapeutic and chemical classification of drugs, they are indicated by the code C10AA and are classified as HMG-CoA reductase inhibitors. Inhibiting the activity of this enzyme, they disrupt the synthesis of cholesterol, significantly reducing its serum amount. This action of statins allows reaching the recommended concentrations of low density lipids in the blood.
Such effects can significantly reduce the rate of development of atherosclerotic plaques. Also, drugs prevent its occurrence. Even with its presence, statins have a valuable effect: they stabilize the endothelium over an atherosclerotic plaque, and therefore significantly reduce the likelihood of coronary thrombosis, acting by a different mechanism than antiplatelet agents. Moreover, the combined use of these funds can further reduce the likelihood of a heart attack. Therefore, the price set for statins is fully justified.
Features of the classification of statins
There are several approaches to the division of drugs into classes. They can be considered from the point of view of synthesis features. Also, since treatment with different statins requires different doses, it is prudent to introduce a classification based on recommended dosages. Generational classification is as follows:
- I generation: "Simvastatin", "Pravastatin", "Lovastatin".
- II generation: "Fluvastatin."
- III 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. All other drugs are synthetic: Fluvastatin, Atorvastatin, Rosuvastatin and Pitavastatin.
Classification of statins by dose
It is reasonable to divide all class drugs, including statins of the latest generation, into low-dose (up to 8 mg), medium-dose (10-40 mg) and high-dose (40-80 mg). In particular:
- high-dose drugs (Atorvastatin, Lovastatin, Fluvastatin);
- medium-dose drugs ("Simvastatin", "Pravastatin", "Rosuvastatin");
- low-dose drugs ("Pitavastatin").
This classification reflects the possibilities of prescribing drugs and their therapeutic breadth. In particular, high-dose drugs have an effect in high quantities, while being well tolerated. Medium-dose drugs, except for “Rosuvastatin”, are worse tolerated in high doses, but have a good effect.
Medium-dose statin “Rosuvastatin”, if necessary, can be prescribed in a high dosage (80 mg), although this is often not required due to a sufficiently complete decrease in total cholesterol and its low-density fraction. Pitavastatin does require the appointment of minimal amounts, which is why the risks of its adverse reactions are many times lower than that of class analogues.
History of the development and implementation of statins
The history of statins is very mixed. Initially, their development was severely inhibited due to ignorance of cholesterol metabolism and the likelihood of developing atherosclerosis depending on blood lipid levels. Moreover, gopocholesterolemic agents were immediately synthesized in order to inhibit microflora in molds of fungi intended to produce pure penicillins. The discovery of the anticholesterol action of a number of substances produced by mushrooms, and made it possible to study statins.
The first statin was compactin, which was never introduced into clinical practice due to many opposing opinions about its effects. It was isolated from a Penicillium cetrinium culture. Then, Monacolin K, patented in February 1979, was isolated from the Monascus ruber culture. In June 79th, Mevinolin, which later became known as Lovastatin, was also patented. This drug was used in the clinic, after which statins of the last generation were isolated or synthesized.
Many opposing opinions hindered the development of statins, after which it was decided to conduct large-scale clinical tests. To date, the largest and most useful study has become 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 the life expectancy and reduces the frequency of acute coronary pathologies.
Theses in favor of statins
With an initial concentration of total cholesterol of 7.4 mmol / L, statin therapy and reaching a level of 5.4 mmol / L significantly reduces the risk of fatal cardiovascular events by 40% in the next 5 years. In a number of other studies, it was proved that a decrease in total cholesterol of only 1 mmol / l by one fifth reduces the likelihood of coronary thrombosis and, consequently, heart attack or stroke.
Considering statins, for and against which many specialists and patients speak out, one can understand the following facts: you can prescribe drugs already at the age of 40 and older, and reducing the risks of heart disease is a rational tactic for prolonging life. And since the price for statins is reasonably affordable, these drugs, which have proven their effectiveness, can be taken without sacrificing your own budget. Of course, the latest generation of statins is much more expensive, although the same "Rosuvastatin", in principle, is quite affordable for the patient. And its cheapest form is the drug Mertenil.
Comparative characteristic: pros and cons
Evaluating statins, it is very easy to speak for and against them. The arguments for are the features of their therapeutic effect: lowering blood cholesterol and its low-density fraction, preventing the risks of acute events and helping to treat them. However, drugs like statins also have contraindications. There are also side effects mediating arguments against use.
With statin therapy, there is a risk of myopathy. It is probably mediated by the inhibition of cholesterol synthesis, which is needed by the muscles. The frequency of this effect is extremely low, although it increases when taken together with other lipid-lowering drugs. There is also a risk of developing liver cancer, although the likelihood of such a disease, as recent studies have shown, is extremely low. At the same time, the fact that oncological diseases were provoked by other factors was proved. So, for drugs of the "statins" group, contraindications should prohibit the combined use of these drugs with other drugs that help to reduce the concentration of fats in cells.
The cost of the latest generation of statins
For statins of the latest generation, prices are different, although their effects are worth the price. Another question is that the results of their action can be achieved with the use of cheaper class analogues of earlier generations. In particular, the most common IV generation statin “Rosuvastatin” is approximately the price:
- 600 rubles for tablets of 40 mg;
- 400-450 per tablet of 20 mg;
- 300-350 per tablet of 10 mg;
- 200 rubles for 5 mg.
The package contains 30 tablets, which are enough for a monthly course of therapy, while for a monthly treatment with Pitavastatin the prices are approximately the following:
- 1 mg tablets cost about 700-750 rubles;
- 2 mg tablets - about 1000 rubles;
- 4 mg tablets - about 1,500 rubles.
The choice between Pitavastin and Rosuvastatin is based on four criteria: price factor, rate of decrease in low density lipoproteins, completeness of increase in high density lipoproteins, and safety. According to the rate of lowering cholesterol and increasing HDL, as well as the price, “Rosuvastatin” looks the best, while “Pitavastatin” is theoretically safer.
The latter is twice as expensive compared to Rosuvastatin. Nevertheless, there is the possibility of using other, cheaper statins. The most cost-effective previously was Simvastatin. Now he was replaced by Atorvastatin, which is naturally replaced by Rosuvastatin (its value will necessarily fall). And if the prices for statins of the latest generation are unbearable for patients, then it is worth considering the possibility of treatment with Atorvastatin or Simvastatin. By the way, most studies have been conducted with Atorvastatin.
The case for using statins by older people
Clinicians have previously been reluctant to prescribe statins for patients over 75 years of age. The reason was the following factors:
- taking several drugs of other classes;
- mutual unwillingness to add another class of drugs;
- lack or low treatment compliance;
- the patient’s reluctance to buy and use statins due to a lack of understanding of their effects.
A number of studies with Simvastatin, Pravastatin, and Atorvastatin have shown a significant reduction in mortality in patients over 75 years of age. 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), the reviews of experts unequivocally confirm one fact.
These drugs can and should be taken at a young age, regardless of whether acute vascular disorders have occurred before. And patients who really care about reducing the risk of their death from myocardial infarction or stroke need to understand that if the drug is effective and safe, then it is definitely worth taking. Moreover, statin treatment has become more accessible and will continue to be so.
Description of reviews from statins of recent generations
Patient reviews when evaluating the quality of a particular generic statin are not indicative, because they do not feel any significant changes from taking the drugs. Improving the lipid profile of the blood does not manifest itself on health and does not have external signs. It is recognized only by lipid profile. Therefore, when evaluating a statin, it is reasonable to be guided by the reviews of specialists. Moreover, about drugs in which the active substance is pitavastatin, domestic experts can not respond.
In clinical practice in the CIS, Pitavastatin is not used because of its high cost and because of the presence of Rosuvastatin and its generics. The drugs "Rosuvastatin", which are indicated above, have a quick effect: the lipid profile normalizes in 1-2 months. Atorvastatin’s time is one and a half times longer. Also, generics of "Rosuvastatin" are safer, as they are metabolized by two types of cytochrome. At the moment, this information, taken from expert reviews, plays a crucial role in the choice of statin in specific clinical situations.
General findings on statins of recent generations
The preparations Pitavastatin and Rosuvastatin are the most modern among the representatives of the class of statins, for which a large evidence base has been collected. Their effects are generally similar to those of Atorvastatin, but there are differences. "Pitavastatin" and "Rosuvastatin" allow you to achieve target levels of cholesterol, as well as low density lipoproteins at a lower dosage than "Atorvastatin".
In addition to the above advantages of statins of recent generations, another aspect is important. Namely: during treatment with Pitavastatin 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 using statins is higher than the cardioform of acetylsalicylic acid. Nevertheless, the presence of contraindications prohibits their use by a certain contingent of patients (see general contraindications).
Drug Examples
Medicines containing Rosuvastatin are available under the following trade names: Akorta, Rosistark, Rosucard, Rosart, Mertenil, Rosulip, Roxer, Rustor, Tevastor. All of these drugs are generic "Crestor", which became the first rosuvastatin. The drug, in which the active substance is pitavastatin, is registered as "Livalo". Its generics are Pitavas and Pivasta. They do not occur in the CIS, although they are registered in the pharmacopeia.
Summary
In accordance with the effects of class drugs and the analysis of the effectiveness of their administration, the use of statins is justified to stabilize the atherosclerotic plaque and prevent its breakdown. They are also used to reduce the intensity of atherosclerosis, affecting the lipid profile of serum. As a result, this class of drugs is really necessary in cardiology. And high-quality statins of the latest generation are already effective in preventing fatal coronary thrombosis.