Lipid-lowering drugs: classification, mechanism of action, indications for use, comparative characteristics
Diseases of the cardiovascular system, pathologies of the circulatory system occupy a leading position in the medical statistics of the whole world. Every year, the proportion of people suffering from heart disease is growing. A high mortality rate is due to many factors - unbalanced nutrition, lack of stress-resistance, polluted environment, genetic aspect.
Among cardiovascular diseases, the main are ischemic heart disease and hypertension( high blood pressure).The main prerequisite for the development of these ailments is hypercholesterolemia, which is also called hyperlipoproteinemia. This factor of the development of diseases is often detected with the progressive development of these.
Cholesterol - good or bad?
Very many medical luminaries still about ten years ago the only cause of heart disease was considered an imbalance of cholesterol in the body. Today, after numerous studies and evidence, it became clear that in the body of sick people and predisposed to the development of heart diseases, it is necessary to track not only the specific index of cholesterol, but also triglycerides, and phospholipids, and lipoproteins, which play not the least role in ensuring the uninterrupted functioning of the cardiovascular system,cardiovascular system.
The main carriers of these elements in the human body are still lipoproteins. They are divided into LDL-low-density lipoproteins that transport cholesterol into cells;VLDL is a very low-density lipoprotein that transports triglycerides;HDL - lipoproteins, transporting cholesterol and phospholipids.
LDL and VLDL move cholesterol to tissue cells and mostly lay it on the walls of the vessels, but the HDL does not allow it to settle there.
Thus, the former are a harmful factor, and the latter are useful. Therefore, the cause of cardiovascular diseases is not hidden in the index of cholesterol. To some extent it is useful for the human body as a component of the right metabolic processes. You should know that just as our body itself produces cholesterol, and in large quantities, than a person absorbs with food.
In connection with this discovery, physicians began to reduce not the cholesterol index in the blood in the treatment of cardiovascular ailments, but to regulate the imbalance between LDL, VLDL and HDL, that is, to inhibit the first and increase the latter.
Imbalance is called in the medical language a violation of lipid metabolism. It can be regulated with the help of medicines included in the group of lipid-lowering.
Lipid-lowering drugs - what is it?
There are many lipid-lowering drugs on the domestic pharmaceutical market. Lipid-lowering drugs are medicines that normalize lipid metabolism. How? How lipid-lowering drugs work, namely what is the mechanism of their effect on the patient's body, is discussed below.
Features of lipid-lowering agents
This group includes medicines of varying degrees of effectiveness. They primarily affect the total cholesterol index, reduce it, but at the same time ensure that the body regulates the proportions of LDL and HDL.
When studying hypolipidemic drugs, the mechanism of action of these, in particular, becomes clear that the decrease in the cholesterol index is achieved by inhibiting the processes responsible for its absorption in the intestine, the creation of a barrier to release fatty acids from adipose tissue, activating the processes of catabolism of cholesterol and inhibiting lipid synthesis inliver.
Various mechanisms of influence on the level of useful and harmful cholesterol are the main feature of drugs, depending on which they are included in certain subgroups of hypolipidemic drugs. This will be discussed below.
The choice of a particular drug for treatment depends on the type of diagnosed hyperlipoproteinemia. So, there are five types: the first one shows an increase in cholesterol in the blood, the second one - the increase in LDL, the third - the appearance of pathological lipoproteins, the fourth - the increase in VLDL, the fifth - the increase in cholesterol and VLDL.
In each specific case, a certain complex therapy is envisaged.
Lipid-lowering drugs are also applicable for the prevention of complex cardiovascular diseases, in particular, heart attacks and atherosclerosis. The use of these drugs in practice helped to reduce the death rate among people suffering from cardiovascular ailments. A large evidence base of medical luminaries is confirmed by the fact that lipid-lowering drugs are effective in the treatment of hypertension of various origin.
Drugs of this group have long been used in European countries in the elimination of cardiovascular diseases, while in the domestic market they have appeared relatively recently, and a large number of them are in doubt.
Today you can buy lipid-lowering drugs both domestic and foreign production. Since not all sick people have the same picture of the diagnosis, each receives individual recommendations on the use of a medication from this group.
Basic classification of
If we consider generalized hypolipidemic agents, the mechanism of their action is understandable. However, each specific drug has its own characteristics. Before describing them, let's see how the distribution of lipid-lowering drugs was classified by experienced specialists.
Thus, drugs sold in modern pharmacies that affect the level of cholesterol in the body can be divided into three types:
- depleting cholesterol in the liver, inhibiting the absorption of this in the intestines;
- inhibitory synthesis of lipoproteins;
- accelerating metabolic processes and removing lipids from the body.
The first type include sequestrants of bile acids. To the second - statins, fibrates, nicotinic acid. To the third - "Probuson", cholagogue preparations.
As noted above, lipid-lowering drugs are a special group of drugs that can increase the presence of useful cholesterol and depress harmful.
Bile acid sequestrants: characteristics, examples
The hypolipidemic drugs of this subgroup are pharmacologically related to anion exchange resins. They contain in their composition an element such as a chlorine ion. They are not absorbed in the intestines, they absorb bile acids in exchange for chlorine and they are removed naturally.
Since there is a shortage of bile acids in the intestine, fats are poorly absorbed, including the processes of absorption of cholesterol by the intestine. Thus, the body begins to respond to its shortage and reproduces HDL, which transport cholesterol from the blood vessels to the liver.
Examples of sequestrants are such drugs as "Cholestyramin" and "Cholestipol", as well as "Holestid."
Statins: characteristics, examples
These are lipid-lowering agents, the mechanism of action of which is to block the work of the enzyme that takes part in the synthesis of cholesterol. They create conditions for a significant reduction in cholesterol reproduction in the liver, which results in a decrease in its concentration in the blood.
It is generally accepted that statins can prevent heart attacks and strokes. These drugs not only reduce cholesterol, but also effectively remove inflammation of blood vessels. Liquefying blood, they inhibit the development of atherosclerosis, expand the vessels at elevated pressure, contributing to its rapid normalization. Do not allow atherosclerotic plaques to expand.
In turn, statins are lipid-lowering drugs, which are divided by their effectiveness for four generations.
First-rate statins affect the lowering of cholesterol in the blood weaker than newer drugs. Medicines "Lovastatin", "Simvastatin", "Pravastatin" refer to this group of drugs. They are made from penicillin fungi and are considered natural in origin.
Second-generation statins are drugs that have a prolonged mechanism of affecting the body of a sick person due to an increased concentration of the active component in the blood. They include a drug such as "Fluvastatin."
Statins of the third generation are an improved version of the first and second generations, which regulates the body's balance of harmful cholesterol and the beneficial, and also reduces the level of triglycerides. The most common example is the drug "Atorvastatin".
The fourth-generation statins are innovative developments that do not cause side effects and are characterized by increased efficiency. The main drug of this subgroup is Rosuvastatin.
Statins of the second, third and fourth generations are medicines of synthetic origin.
Which hypolipidemic agent in the statin group is the most effective and does not cause any side effects? There are none among them. All statins are capable of causing certain harm to the human body by side effects along with their high ability to remove inflammation of blood vessels and to remove harmful cholesterol from the body.
Fourth generation statins are the most popular and acceptable. But if we take into account the moment that every core and hypertensive patient has its own, individual picture of the disease and predispositions to complications, then the drugs are prescribed exclusively by the treating doctor, and not simply accepted because the patient so desires.
Fibrates: characteristics, examples
These hypolipidemic drugs( classification classifies them as the fourth group), which effectively cope with the task of lowering LDL and triglycerides in the blood. They activate lipoprotein lipase in blood plasma and liver. Due to this, LDL is cleaved from LDL and reproduced by HDL, which also removes cholesterol from the blood vessels.
Despite the fact that these are effective hypolipidemic drugs, the comparative characteristics with other groups of such drugs showed that they are significantly inferior in statin utility value.
Examples of fibrates are such drugs as "Clofibrate", "Gemfibrozil", "Bezafibrate", "Fenofibrate".
Nicotinic acid, its properties
Very often cores and hypertensives pay special attention to vitamins. Let's find out the drug, what vitamin refers to lipid-lowering drugs. This is just the same as nicotinic acid. Her in the medical field is called vitamin PP, or B3.
Nicotinic acid shows its lipid-lowering properties in the case of taking a dose that is larger than the human body requires as a vitamin. This drug inhibits the synthesis of VLDL in the liver, thereby reducing the concentration of LDL and TG, with TG more than cholesterol.
This drug is administered to patients in a strictly defined dose, nicotinic acid can not be administered alone. Each missed reception is fraught with deterioration in the treatment of heart disease.
This drug is an antioxidant. It moderately affects the indices of useful and harmful cholesterol in the blood. In particular, this hypolipidemic drug works a little differently compared to the above. It does not increase the concentration of HDL, but reduces it. Activation of non-receptor pathways for the induction from the blood of LDL during the reception of "Probulus" is thus a hypolipidemic property.
This drug is more experimental than curative, but there is still application of it in medical practice. Many properties of the "Probulus" have not yet been studied. He is well tolerated by patients, but without a solid evidence base of his benefits, physicians still prefer to prescribe to their patients other lipid-lowering medications for long-term and safe therapy.
Which hypolipidemic drugs are more effective?
This article discusses hypolipidemic agents. What is it is now clear. Once again, these medications help to remove harmful cholesterol from the body and increase the concentration in the blood of the beneficial. If the proportion of these substances is disrupted, the patient is at risk of developing heart attacks, strokes and atherosclerosis.
The main indications for the use of lipid-lowering drugs are the genetic predisposition for the development of atherosclerosis, hyperlipoproteinemia.
It should be noted that complex therapy does not involve the simultaneous administration of several lipid-lowering drugs. The luminary of medicine today does not distinguish among the general mass the best lipid-lowering drugs. Their pharmacology varies considerably. In each specific case a certain drug is prescribed.
If you take into account the quality before using the funds of this group, then a greater confidence is still caused by medicines of foreign production. But it is also worth noting that the domestic market today is filled with all sorts of foreign-made generics, which are also no less qualitative than the original. The undoubted advantage is that they are cheaper.
Not such a high quality is not in low efficiency, but in the slow action of the drug itself.
Lipid-lowering drugs are medicines that can fight with a high mortality rate in a group of patients suffering from cardiovascular diseases or predisposed to their development.
Now you know what are hypolipidemic agents, the indications for admission are discussed above. We do not say anything about the specific dosage of these medicines, because it is individual for each patient, it is prescribed only by the attending physician after a full diagnosis of the patient's body.
In search of lipid-lowering medications, people are faced with a situation where pharmacists recommend the purchase of hepatoprotective drugs. What is common between them?
Hepatoprotective agents are useful in the treatment of the liver. Since the hypolipidemic effect is associated with the metabolic processes in which cholesterol is involved, and which occur in the liver, many hepatoprotective drugs are characterized by a hypolipidemic effect. And this, in turn, means that UDC of hepatoprotective and lipid-lowering agents can be identical, often it is a question of one drug that is applicable in the treatment of both liver and cardiovascular diseases.
The theoretical description of the hypolipidemic properties of new generation drugs is not as complex as the practice of taking them. Achieved positive effect does not mean that these drugs are safe for the general condition of patients.
Absolutely all groups and subgroups of drugs that have hypolipidemic properties can cause serious side effects. The main thing is increasing the concentration of sugar in the blood. Therefore, they are contraindicated for use by most diabetics. But nevertheless some group of patients with diabetes mellitus passes therapy with the appointment of these. In this case, the attending physician assesses the possible risks of worsening the patient's condition.
Every person is an individually functioning organism with its own characteristics, which are both genetically inherent and physically acquired. Gipolipidemic drugs of any group from the above classification are assigned to patients after a thorough examination of the picture of deterioration of health.
Self-medication is unacceptable. Only the competent physician in the questions of metabolic processes can give a specific recommendation on what is still the drug at a certain stage of the disease is more acceptable.
It should also be understood that these drugs can be taken as the main therapy in the treatment of a progressive ailment, as well as for the prevention. In each case, a specific dose is appointed, which acts sparingly on the human body, taking it for a specific purpose( to stabilize their health).
Description for each drug indicates that lipid-lowering medications are not taken without the advice of a doctor. However, in practice, buy any of them in the pharmacy is not difficult. So be careful with the desire to take them on your own. Prescribed lipid-lowering medications often mean a constant reception.
Original lipid-lowering drugs of foreign origin are not low-budget, so many people want to take cheaper medicines from domestic manufacturers. Only the attending physician should select a replacement and adjust the dose of admission.
The effectiveness of the prevention of cardiovascular diseases and their treatment depends not only on the drug chosen, but also on its proper administration, in particular, on the prescribed dosage and the absence of omissions during therapy. Be healthy!