Why is nicotinic acid used for cholesterol and what is it? Nicotinic acid is a B vitamin and is one of the water-soluble vitamins. Its use as a pharmacological drug began quite recently, at the end of the twentieth century, when its properties of reducing cholesterol and triglycerides in the blood were discovered.
Nicotinic acid is often prescribed to patients for diseases characterized by disorders of the blood lipid profile, especially for the treatment of cardiovascular pathology, for example, in atherosclerotic disease, when a lipid-lowering diet is either ineffective or insufficient.
Nicotinic acid and cholesterol are still subjects of debate among experts. The prevailing opinion is that cholesterol levels at which additional therapy with nicotinic acid should be prescribed are 6.5 mmol/l and higher. The peculiarity of the use of nicotinic acid or niacin, in contrast to other anti-atherosclerotic drugs, is that it can reduce cholesterol levels not only in the blood plasma, but also in tissues.
The following types of acid are distinguished:
- Immediate-release nicotinic acid, which is quickly released into the blood and gives an immediate but short-term effect;
- Long-acting nicotinic acid, which is released into the blood over a certain period of time and acts for a long time.
Mechanism of action and use in medicine
The chemical effect of niacin is quite diverse in relation to organs and systems:
- Its main property is that it is able to block spontaneous lipolysis and thereby reduce the amount of free fatty acids released into the blood;
- B vitamins are also used to reduce cholesterol produced by the liver;
- In addition to its direct effect on the processes of cholesterol metabolism in the body, nicotinic acid is capable of dilating spasmodic vessels, which is the prevention of atherosclerosis and tissue ischemia;
- The use of nicotinic acid has a beneficial effect on the rheological properties of blood, making it more fluid, increasing the speed and volume of blood flow, enhancing microcirculation and, as a consequence, blood supply in tissues and organs;
- It is capable of lysing atherosclerotic plaques in high concentrations, therefore it is used as a method of treating atherosclerosis;
- It enhances the motor function of the gastrointestinal tract and the secretory function of the gastric glands;
- Stimulates the production of serotonin in the brain, thereby improving mood and vitality;
- Nicotinic acid also has an anabolic effect, regulating the level of growth hormone in the blood, thereby having a hypoglycemic effect, since growth hormone indirectly increases the level of glucose in the blood and is an insulin antagonist.
Thus, the use of nicotinic acid in medical practice is quite wide: it is used not only for high cholesterol, which prevents the development of heart and vascular diseases, but can also regulate blood circulation in the body, which serves as a treatment method for existing pathologies, for example, atherosclerosis.
In addition, niacin is widely used in psychiatric practice to treat depression, schizophrenia, alcohol and nicotine addiction.
The effect of nicotinic acid on cholesterol and the cardiovascular system
The properties of nicotinic acid as a vasodilator have been known for a long time: it has been successfully used for spasms and atherosclerosis. It is noteworthy that nicotinic acid gently lowers cholesterol levels, sparing the blood vessels - this is a direct answer to the question of whether this component affects plaques.
Niacin or vitamin PP, as the active ingredient is also called, effectively counteracts fats and fatty acids entering the body, regulates lipid levels, participating in their metabolism.
When taking nicotine-based drugs, you don’t have to worry about worsening your cardiovascular system. The use of such treatment will also help normalize blood pressure, since cleaned vessels better cope with their task of supplying organs and tissues with blood.
Combination of nicotinic acid with other substances
You can and should take nicotinic acid with the following vitamins and microelements:
- Substances with antioxidant effects: vitamin C, E, beta-carotene and selenium;
- Chromium, since it additionally has a hypoglycemic effect and neutralizes the increase in glucose levels with niacin;
- Zinc, as it promotes the synthesis of its own nicotinic acid.
It is not recommended to combine the use of the vitamin with the following substances:
- Herbs: borage, comfrey, mint, as they negatively affect liver function;
- Spices: cloves, ginger, ginseng, garlic - since they reduce blood clotting, and this is an additional risk of bleeding.
Nicotinic acid preparations
On the modern market, nicotinic acid is represented by the following drugs:
- "Acipimox";
- "Niceritrol";
- "Enduracin".
Nicotinic acid preparations belong to the vitamin B group. Their pharmacological effect is that they increase the concentration of low-density lipoproteins and very low-density lipoproteins, which are antiatherogenic. Also, these medications act as activators of the fibrinolysis system and are used to prevent thrombosis.
Nicotinic acid is available both in tablet form and in the form of a solution for intravenous, intramuscular or subcutaneous administration.
Today, the most preferred nicotinic acid preparation is Enduracin. Its peculiarity lies in the content of tropical wax, which ensures long-term absorption of the medicinal substance by the gastrointestinal mucosa, and therefore a prolonged smooth effect.
Interesting
For a long time, important attention was paid to the fight against “bad cholesterol”. Drugs were used that could destroy low-density compounds. But at the same time, the level of good cholesterol often decreased. The way out of this situation was to study the effect of nicotinic acid.
About 500 patients suffering from various forms of heart and vascular diseases were recruited to participate. Mainly attention was paid to the presence of cholesterol plaques on the walls of blood vessels. For four years, statins were used for treatment, which cleared the walls of blood vessels from plaques and reduced the level of LDL production.
But at the same time, the level of protein compounds also decreased or remained at the same level. The study group was divided into two parts. Continuing the usual treatment, some of them were given drugs based on nicotinic acid, while others were given pacifiers. After a six-month experiment, we summed up the results and found out that the use of vitamin PP increased the level of good cholesterol to the required norm.
Dosing
The drug should be prescribed at minimum dosages to avoid adverse reactions. The first dose should be no more than 50 mg, then it should be gradually increased to the optimal dose. The dose should be increased once a week with constant monitoring of the patient's condition and his response to therapy.
It has been established that the maximum effect of nicotinic acid is observed at a daily dose of 2000 – 3000 mg. Maximum doses of niacin are prescribed only to patients with high blood cholesterol levels, and for preventive purposes, a drug dosage of up to 1000 mg per day is used.
In psychiatric practice, in the treatment of severe forms of schizophrenia, a daily dose of 12 grams is used for intravenous administration, which is the maximum. Exceeding it can lead to psychological and physical dependence on the drug.
Review of drugs to control cholesterol levels
Hypercholesterolemia is the most important risk factor in the development of severe diseases of the cardiovascular system, such as myocardial infarction and stroke. At the same time, diet correction and lifestyle changes do not always allow you to control blood cholesterol levels. In such cases, and if the patient has severe diseases, drugs are used to lower cholesterol levels. On the pharmaceutical market there are several groups of drugs used to treat patients with hypercholesterolemia with different mechanisms of action. What is the best cholesterol medicine? And is it possible to identify among them the most effective cholesterol-lowering drugs?
- Cholesterol and its effect on the body
- Cholesterol-lowering drugs
- Statins to combat high cholesterol
- Generations of statins
- How to use statins?
- Use of fibrates
- Drugs that interfere with cholesterol absorption
- Bile acid sequestrants
- Nicotinic acid and preparations based on it
Cholesterol and its effect on the body
Cholesterol, or cholesterol, is an essential component of cell membranes, participating in maintaining their integrity and the synthesis of steroid hormones. Therefore, it is impossible to say unequivocally that cholesterol plays only a negative role. However, in certain situations, hypercholesterolemia can lead to the development and progression of atherosclerotic vascular damage.
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Very often, people distinguish between “bad” and “good” cholesterol. This division has no biochemical confirmation, since all cholesterol is a substance homogeneous in chemical structure. There are other differences. All lipids in our body are insoluble in the blood, therefore, in order to transport them to the organs, they must first be bound to protein molecules - apolipoproteins. It is at this stage that differences in cholesterol fractions arise. High-density lipoproteins (HDL) transport cholesterol from tissues to the liver, which reduces the risk of developing atherosclerosis in blood vessels. In turn, low and very low density lipoproteins (LDL and VLDL) lead to an increase in the delivery of cholesterol and other fats to the vessels and tissues of the body, which increases the risk of developing atherosclerotic changes.
Cholesterol-lowering drugs
Drugs for lowering blood cholesterol can be divided into several groups, depending on their chemical composition and mechanism of action:
- Exchange resins and agents for reducing the absorption of cholesterol in the intestine.
- Statins, which inhibit the activity of an enzyme necessary for cholesterol synthesis.
- Fibrates to lower blood cholesterol levels.
- A nicotinic acid.
The choice of a specific medication for lowering cholesterol is made only by the attending physician, after a preliminary examination and interview of the patient, as well as additional examination methods.
Never prescribe medications yourself.
Statins to combat high cholesterol
Statins are one of the most commonly used groups of drugs to treat high cholesterol. This is due to its high efficiency and low risk of side effects. Statins block the key enzyme in cholesterol synthesis - HMG-CoA reductase, which actively works in liver tissue. This allows you to reduce the formation of endogenous cholesterol, which is two to three times greater than exogenous cholesterol, that is, coming from food.
The use of statins for high cholesterol is indicated for the following categories of patients:
- With previous strokes and myocardial infarctions.
- After major surgical operations on large vessels.
- For acute coronary syndrome and myocardial infarction.
- For coronary heart disease with a high risk of stroke or myocardial infarction.
A cardiologist or therapist should determine the indications for prescribing statins as cholesterol-lowering medications.
Generations of statins
The widespread use of statins in the treatment of patients with hypercholesterolemia and the rapid development of medical science have led to the emergence of several generations of these drugs.
- The first generation of medications (Pravastatin, Simvastatin and others) can increase the content of high-density lipoproteins and cleanse blood vessels of low and very low-density lipoproteins. The most popular is Simvastatin, the most harmless first-generation statin.
- Second generation statins (Fluvastatin and others) have a similar effect on liver enzymes and reduce blood cholesterol. They have a milder effect on the patient’s body.
- Third generation drugs (Atorvastatin and Cerivastatin) have been most fully studied for use in humans for high cholesterol. Cerivastatin is prohibited for use due to documented episodes of significant harm to the body, including death. Taking Atorvastatin is completely safe.
- Fourth generation statins are called Rosuvastatin and Pitavastatin. Recommended for use in most patients as the main remedy for cholesterol. The best drugs among statins.
The use of any statins has a positive effect on cholesterol metabolism, however, in patients taking the drugs for a long time, side effects may occur:
- Disorders of the liver due to the impact on the functioning of its enzymes.
- Mood changes with swings.
- Chronic renal failure.
- Visual impairment such as myopia.
The development of side effects can be prevented by following the doctor’s recommendations and instructions for use of medications, as well as by analyzing the effectiveness of drugs during treatment and their effect on the body.
How to use statins?
Taking statins is very convenient - it needs to be done only once in the evening, which is associated with an increase in cholesterol synthesis at night. The starting dosage of the drug is always lower than the therapeutic dosage. Gradually, the attending physician may increase the dose.
Statins can be used as a single drug to combat high cholesterol, as well as as part of a comprehensive treatment. However, simultaneous use of these drugs with fibrates can lead to the development of liver failure, muscle pain and loss of appetite.
Complex therapy for hypercholesterolemia is becoming the gold standard of treatment.
In clinical practice, there are special combined forms of drugs that reduce the amount of cholesterol in the blood. For this purpose, you can drink ready-made combinations of Lovastatin and Nicotinic acid, Rosuvastatin and Ezetimibe. In most cases, this allows the patient to increase adherence to treatment due to a decrease in the number of tablets that need to be taken, as well as increase the effectiveness of therapy due to a combination of several mechanisms of action.
Use of fibrates
In addition to statins, fibrates, which are derivatives of fibric acid, are used to reduce blood cholesterol. This acid binds to bile acids and affects the metabolism of cholesterol, HDL and LDL. Studies have shown that drugs in this group reduce the amount of lipid deposits in the vascular wall.
Fibrates include the following tablets - Lipantil, Lipanor, Gemfibrozil and others. All of them have proven themselves in clinical practice, including as medicines that cleanse blood vessels of cholesterol and other fats.
When using fibrates, the following side effects may develop:
- Dyspeptic symptoms such as nausea, vomiting, diarrhea, loss of appetite.
- Symptoms of pancreatitis are pain in the left hypochondrium, digestive disorders.
- Muscle weakness and decreased strength.
- Headaches, decreased libido.
- Some patients may experience allergic reactions such as urticaria, Quincke's edema and others.
Fibrates are prohibited for use in patients with liver disease, gallbladder disease, and in cases of disruption of the hematopoietic system. As noted above, the use of fibrate with statins can lead to the development of side effects from the liver. However, in this case it is important to select the correct reduced dosages of medications.
Cholesterol levels can quickly decrease when taking fibrates, but their prescription should be carried out by the attending physician with constant biochemical monitoring of liver function (determining the concentration of liver enzymes in the blood).
Drugs that interfere with cholesterol absorption
How to reduce cholesterol in the blood without interfering with its formation in the body?
This can be achieved by taking drugs from the group of inhibitors of cholesterol absorption in the intestine. For this purpose, such means as Ezetrol and others are used. It is safe to take the drug, since it is not absorbed into the blood from the intestinal lumen and is completely eliminated from the body. However, the effect of such drugs against cholesterol is not very great, since most of this lipid is synthesized in the body itself, and does not come with food. Therefore, there are special combination forms of drugs - Ezetimibe with various statins. This combination has an increasing effect on efficiency.
You need to take Ezetrol once a day. The average therapeutic dosage is 10 mg.
Bile acid sequestrants
Medicines from this pharmacological group can bind bile acids, converting them into water-insoluble compounds, which leads to their relative deficiency in the body. In this regard, the body tries to increase the content of bile acids and directs a large amount of cholesterol to their synthesis, which ultimately has a reducing effect on its concentration in the blood.
The effect of such drugs occurs after 2-3 weeks of regular use. At the same time, the drugs have virtually no side effects on the body, and only affect bile acids. If you use bile acid sequestrants for a long time, malabsorption syndrome may occur, which consists of impaired absorption of nutrients and various vitamins.
Sequestrants must be taken in large enough doses to bind bile acids in the intestinal lumen. However, impaired digestion of lipids and other food components can lead to the development of dyspeptic symptoms - nausea, constipation, diarrhea and bloating.
This group includes two drugs:
- Cholestipol is the best remedy from this group, containing the substance of the same name in its composition. Allows you to lower cholesterol and LDL levels in the body when taken regularly.
- Cholestyramine is sold in the form of a purified powder, which must be taken for several weeks until significant changes in cholesterol levels appear.
Nicotinic acid and preparations based on it
Nicotinic acid and drugs based on it disrupt the transport of fatty acids into the blood and inhibit the formation of cholesterol in the liver tissue. Ideal for use in patients with diabetes, as it can reduce blood glucose levels. This group of drugs includes: Enduracin, Niceritrol, Acipimox and others.
It is better to combine nicotinic acid preparations with other vitamins to reduce the risk of side effects.
What side effects may occur when taking these drugs? Since the dose of the drug is very large - from 1.5 to 3 g. per day, the appearance of various undesirable effects is possible: headache, sensations of heat and hot flashes, the development of fatty hepatosis with the replacement of functional liver tissue with fatty tissue.
It is impossible to say unequivocally that one group of drugs for lowering cholesterol is better than another. However, in modern medicine, the combination of 3-4th generation statins with inhibitors of cholesterol absorption from the intestinal lumen has earned particular popularity in the treatment of hypercholesterolemia. The use of such means makes it possible to comprehensively influence the intake of cholesterol into the body: block its absorption from food, and block its formation in the liver. This leads to a persistent decrease in the concentration of cholesterol in the blood, which is the main goal of treatment. The choice of medications should always be made by the attending physician due to the possibility of side effects and the need for constant monitoring of the progress of therapy.
Indications
Indications for the use of nicotinic acid are the following conditions:
- High level of atherogenic substances in the blood: cholesterol, high-density lipoproteins, triglycerides;
- Lack of nicotinic acid in the body;
- Gastrointestinal motility disorders, intestinal malabsorption syndrome and other gastrointestinal diseases;
- Neuritis of the facial nerve;
- Cardiovascular diseases;
- Ischemic cerebral circulatory disorders;
- Dermatitis, pellagra;
- The body’s increased need for niacin during cancer, pregnancy, infectious diseases, stress, etc.
Side effects
Despite all the positive aspects, nicotinic acid has a number of side effects, so its improper use without medical supervision is prohibited.
Due to its vasodilating effect, nicotinic acid can promote the development of bleeding in patients, so it should be taken with caution in diseases such as gastric and duodenal ulcers, gastritis, bleeding disorders, and during menstruation in girls.
Nicotinic acid preparations have a pronounced hypotensive effect, as they dilate blood vessels. Therefore, immediately after administration, patients may experience a feeling of heat, increased sweating, facial redness, itching and hives; fog and loss of consciousness are also possible in response to low blood pressure.
In patients with diabetes mellitus, the use of the drug may provoke a worsening of the underlying disease due to inhibition of the action of insulin and hyperglycemic niacin in the body.
Nicotinic acid increases appetite and may cause fatty liver degeneration.
Action of the substance
Nicotinic acid for atherosclerosis began to be used several decades ago, after clinical studies. The action of the substance manifests itself as:
- blocking spontaneous lipolysis;
- decreased production of lipoproteins in the liver;
- vasodilating effect, which is especially important in the presence of atherosclerosis;
- blood thinning, which restores blood flow.
Vitamin injections help improve the functioning of the adrenal glands, which helps stop an asthma attack. With regular intake of niacin (according to the recommended dosage), inflammation and allergic manifestations are eliminated.
Nicotinic acid is effective for hypertension - it helps stabilize blood pressure, preventing its increase in the future. After taking the drug, a person feels cheerful, the feeling of fatigue is eliminated, and endurance increases. Since niacin helps produce serotonin, the drug is used in the treatment of depression and other mental disorders. Nicotinic acid preparations are used to speed up metabolism, which helps reduce excess weight.
Thanks to niacin, cellular metabolism is improved, the formation of cholesterol plaques is inhibited, and their dissolution and elimination are accelerated. The substance helps reduce bad cholesterol and increase good cholesterol, which helps cleanse the arteries. “Bad” fats are utilized in the liver without affecting the functioning of the body.
Nicotinic acid, which is prescribed to lower cholesterol, is included in many vitamin-mineral complexes for daily use. You can get it along with some food products. People who eat well and nutritiously often do not need to take additional vitamins in the form of capsules or injections. A deficiency of the substance is observed with poor nutrition, alcoholism, and the presence of carcinomas.
Features of application
Lipotropic medications such as cholite or vitamin B12 should be used simultaneously with the prescription of the vitamin, since one of the side effects of niacin is increased appetite and impaired weight control in patients. Control of physical activity and diet are also recommended, a set of physical exercises and a split diet with plenty of low-fat dairy products, vegetables and fruits, and control of the consumption of simple carbohydrates and fats are prescribed.
To avoid redness, itching and heat, you should take Aspirin at a dose of 325 mg simultaneously with taking nicotinic acid, with a difference of half an hour, while Aspirin is drunk first. You should also not drink hot drinks such as tea or coffee while taking the drug.
According to some data, the daily dose for lowering cholesterol should not be more than 2000 mg, since exceeding it is fraught with the development of toxic hepatitis. Additional monitoring of liver function is carried out and inclusion of “Methionine” or products that contain it, for example, cottage cheese, in the therapeutic list.
Indications for discontinuation of the drug
If the patient begins to notice breathing difficulties, shortness of breath, or difficulty swallowing, this is a reason to urgently consult a doctor to consider discontinuing the nicotinic acid drug. Also alarming symptoms will be changes in the color of urine and urination disorders, signs of bleeding (overt or hidden symptoms), for example, weakness, pallor of the skin.
Important! If you experience any symptoms of physical distress in response to taking the drug, you should consult a doctor.
Enduracin
Produced (USA) in the form of tablets containing the active component of nicotinic acid 0.5 g in plastic packages.
No prescription required upon purchase.
Recommended:
- As a prophylactic for pellagra.
- Used as a vitamin preparation for diet imbalances.
- Normalizes cholesterol levels.
- Used in the complex treatment of heart and vascular diseases.
Contraindications to the use of the drug are based on the negative effects of nicotinic acid and are absolutely similar to all analogues that do not contain other components.
The production of nicotinic acid is established in almost all pharmaceutical companies in the world. Differences can only be in the form of release of the drug and the price of the product.
It is not recommended to self-medicate even for prevention. Despite the fact that the product is made on the basis of a vitamin, it is dangerous to take it uncontrollably. If you experience diseases associated with high cholesterol, you should consult a doctor and undergo a detailed examination. You need to find out your blood cholesterol levels before trying to lower or raise them.
