Cholesterol-lowering drugs: statins and other drugs

Atherosclerosis, which is based on a complex of complex disorders of lipid metabolism, is one of the most important risk factors for the development of vascular accidents. Closely associated with it, hypercholesterolemia is detected in more than 60% of hospitalized patients aged 30–69 years [1]. Therefore, drugs that help normalize lipid parameters are in steady demand in pharmacies. In all likelihood, it will only grow: after all, the average age of the Russian population is growing and the number of patients with cardiovascular diseases is increasing. And in order to conduct high-quality pharmaceutical consultations, it is important for primary care providers to remember how lipid-lowering drugs work, what side effects they exhibit, and what the client needs to be warned about with the appropriate prescription.

General information

Cholesterol is a fatty alcohol, an organic compound found in the cell membranes of living organisms.
Two concepts are often used - cholesterol and cholesterol . What is the difference between them? In fact, this is the name of the same substance, only in the medical literature the term “cholesterol” is used, since the ending “-ol” indicates its relationship to alcohols. This substance is responsible for giving strength to cell membranes .

Sources of cholesterol

But if the level of cholesterol in the body is elevated, cholesterol plaques form in the walls of blood vessels, which, when cracked, create a favorable environment for the formation of blood clots . Plaques narrow the lumen of the vessel.

Therefore, after a cholesterol test, the doctor, if necessary, decides what to do if you have high cholesterol. If the interpretation of the cholesterol test indicates high levels, the specialist often prescribes expensive medications - statins , which are designed to prevent diseases of the cardiovascular system. It is important that the doctor explains that after prescription, the patient needs to take such tablets constantly, as the instructions for use suggest.

But anti-cholesterol drugs have certain side effects, which doctors should warn patients about, explaining how to take the pills correctly.

Therefore, every person who has elevated cholesterol levels must decide whether to take such medications.

There are two main groups of cholesterol medications currently offered: statins and fibrates . In addition, experts recommend that patients consume Lipoic acid and Omega 3 . The drugs used to lower cholesterol are described below. However, their use is advisable only after examination and prescription by a doctor.

Drug combinations

In addition to using the drugs separately, they can be combined together to enhance the lipid-lowering effect. Sometimes statins need help fighting high cholesterol. Taking statins can be combined with the use of drugs that intensively remove bile acids from the body. Statins are also combined with drugs that inhibit cholesterol absorption or a PCSK9 inhibitor. Statins are the base drug in all drug combinations. The decision to use drugs together is made by the doctor[2].

Statins to lower cholesterol

Before taking such drugs, you need to know what statins are - what they are, the benefits and harms of such drugs, etc. Statins are chemicals that in the body reduce the production of enzymes necessary for the process of cholesterol synthesis.

In the instructions for such drugs you can read the following:

• They reduce the concentration of cholesterol in plasma due to inhibition of HMG-CoA reductase , as well as a decrease in cholesterol synthesis in the liver.
• Reduce cholesterol concentrations in people suffering from homozygous familial hypercholesterolemia , which is not amenable to treatment with lipid-lowering drugs.
• Their mechanism of action makes it possible to reduce total cholesterol levels by 30-45%, and “harmful” cholesterol levels by 40-60%.
• When taking statins, HDL cholesterol and apolipoprotein A increase.
• The drugs reduce the likelihood of ischemic complications by 15%, in particular, according to cardiologists, the risk of angina pectoris and myocardial infarction is reduced by 25%.
• No mutagenic or carcinogenic effects are observed.

A nicotinic acid

Nicotinic acid (niacin or vitamin PP) has a multidirectional effect on fat metabolism in the human body. This substance is an important part of some enzymes, without which they will not be able to carry out their function - redox processes in the cells of our body [1].

Under the influence of nicotinic acid, the breakdown of lipids in adipose tissue decreases, the level of “bad” cholesterol decreases and the content of “good” cholesterol increases [3]. This reduces the risk of atherosclerotic vascular damage.

Side effects

Numerous negative effects may occur after administration:

• Frequent side effects: asthenia , insomnia , headache , constipation , nausea , abdominal pain, diarrhea , myalgia , flatulence .
• Digestive system: diarrhea, vomiting, hepatitis, pancreatitis , cholestatic jaundice, anorexia .
• Nervous system: dizziness , amnesia, hypoesthesia, malaise, paresthesia, peripheral neuropathy.
• Allergic manifestations: rash and itching of the skin , urticaria , anaphylaxis , exudative erythema, Lyell's syndrome.
• Musculoskeletal system: back pain, myositis , cramps , arthritis , myopathy .
• Hematopoiesis: thrombocytopenia .
• Metabolic processes: hypoglycemia , diabetes mellitus , weight gain, obesity , impotence , peripheral edema.
• The most severe complication of statin treatment is rhabdomyolysis , but this occurs in rare cases.

Who needs to take statins?

Informing what statins are, advertising stories and instructions for the drugs indicate that statins are effective drugs for lowering cholesterol, which significantly improve the overall quality of life, and also reduce the likelihood of developing strokes and myocardial infarction . Accordingly, taking these pills every day is a safe method to lower your cholesterol levels.

But in fact, until today there is no accurate information about whether treating patients with such medications is really so safe and effective. After all, some researchers claim that the potential harm and side effects outweigh the benefits of statins as a prophylactic drug used to prevent cardiovascular diseases. Experts are still arguing whether it is worth taking statins, weighing the pros and cons. Doctors' forums almost always contain debates on the topic “Statins - pros and cons.”

But, nevertheless, there are certain groups of patients for whom statins are required.

The latest generation statins must be used:

• for the purpose of secondary prevention after a stroke or heart attack ;
• for reconstructive surgical interventions on large vessels and the heart;
• in case of myocardial infarction or acute coronary syndrome ;
• with ischemic disease with an increased likelihood of stroke or heart attack.

That is, anticholesterol drugs are indicated for coronary patients in order to increase their life expectancy. In this case, to reduce side effects, the doctor must select the appropriate medicine and monitor biochemical parameters. If there is a 3-fold increase in transaminases, statins are discontinued.

The advisability of prescribing medications from this group for such patients is questionable:

• at low risks;
• for diabetes mellitus ;
• in women before menopause.

If statins are prescribed to people with diabetes, they may need additional tablets to lower their blood , since statins raise their blood sugar in such patients. Medicines to lower blood sugar should only be prescribed and their dosage adjusted by a doctor.

Currently in Russia, the treatment standards for most cardiac pathologies include the use of statins. But although medical prescription reduces mortality, this is not a prerequisite for prescribing drugs to all people with coronary artery disease or hypertension. They should not be used by anyone over 45 years of age or by anyone with high cholesterol levels.

It is important to consider the compatibility of these drugs with other drugs.

If necessary, together with anticholesterol drugs, the doctor prescribes other drugs for the treatment of cardiovascular diseases: Diroton , Concor , Propanorm , etc.

Diroton (active ingredient - lisinopril ) is used to treat arterial hypertension.

Concor (active component - bisoprolol hemifumarate ) is used for the treatment of arterial hypertension , heart failure, angina pectoris .

Classification of cholesterol-lowering drugs

The following drugs are used to lower blood cholesterol:

• statins;
• fatty acid sequestrants;
• drugs that suppress cholesterol absorption;
• a nicotinic acid;
• fibrates;
• unsaturated fatty acids;
• monoclonal antibodies – PCSK9 inhibitors[2].

The drugs on this list act in different ways. Some medications reduce the supply of lipids from the food you eat. The fewer lipids that enter the bloodstream through the intestinal wall, the lower the cholesterol level in the blood will be. Other representatives from the group of cholesterol-lowering drugs affect the synthesis and utilization of their own lipids[2].

List of statin drugs

Which drugs are statins, and what their cholesterol-lowering activity is, can be found in the table below.

Classification of statins

In medicine, certain parameters are taken into account for classification.

Origin:

• Synthetic: Cerivastatin , pitavastatin , Rosuvastatin , Fluvastatin , Atorvastatin ).
• Semi-synthetic: Simvastatin , Pravastatin .
• Natural: Lovastatin .

By generation:

• First generation: lovastatin ( Choletar , Cardiostatin );
• Second generation: simvastatin ( Vasilip , Simvacard , Simvastatin , Simvor , Simvastol , Simgal , Zocor , Owencor , Sincard , etc.), pravastatin ;
• Third generation: atorvastatin ( Atomax , Tulip , Liprimar , Atoris , Torvacard , Liptonorm , Lipitor ), cerivastatin , fluvastatin .
• Fourth generation: pitavastatin , rosuvastatin ( Crestor , Akorta , Mertenil , Roxera , Rosuvastatin , Rozulip , Rosucard , Rozart , Tevastor ).

Latest generations of statins

If you choose very good cholesterol pills, it is worth buying 3-4 generation medications. The third is represented by drugs with atorvastatin:

1. Atoris (from 370 rubles);
2. Torvacard (from 266 rubles);
3. Novostat (from 560 rubles), or Novostatin;
4. Tulip (from 660 rubles).

Atorvastatin

lowers the level of low-density fats in the blood. It inhibits an enzyme that is involved in the early stages of cholesterol synthesis. Next, the activity of receptors is activated, increasing the rate of binding of fats and their removal from the plasma. The substance also prevents the destruction of the inner lining of blood vessels and promotes the growth of “good” cholesterol.

The effect of all medications is achieved within 2 weeks from the start of administration.

The patient can also be prescribed Atomax, Anvistat, Lipitor - they have the same active ingredient.

4th generation drugs are very effective, but quite expensive. These are drugs with rosuvastatin, pitavastatin. The group includes Crestor, Akorta, Livazo, Mertenil, Rozart. The price for a month of admission varies from 1000 rubles. up to 3000 rub. Usually in the first month they take 5-10 mg, then the dose is increased to 40 mg.

How to choose statins?

Despite all the reviews about statins for lowering cholesterol, the patient must decide whether to take such medications, but this should be done only on the basis of the recommendation of a specialist. What is important, first of all, is not the reviews, but the doctor’s prescription.

If a person nevertheless decides to take statins, then the choice factor should not be the price of the drug, but, first of all, the presence of chronic diseases.

Self-treatment if cholesterol is elevated cannot be carried out with any medications. Treatment for high cholesterol and lipid metabolism disorders is prescribed by a cardiologist or therapist. In this case, the specialist must assess the following risks:

• age;
• floor;
• weight;
• presence of bad habits;
• diseases of the cardiovascular system, other diseases (diabetes, etc.).

It is important to take statins in the dose prescribed by your doctor, and it is important to take a biochemical blood test as often as prescribed by a specialist.

If too expensive pills were prescribed, you can ask the doctor to replace them with drugs that are cheaper. However, it is recommended to use original drugs, since domestically produced generics are of lower quality than the original drug and generics offered by imported manufacturers.

Those who, before taking them, are interested in what the real benefits and harms of statins against cholesterol are, need to consider several important factors in order to minimize the harm of these drugs.

If the medicine is prescribed to elderly patients, it must be taken into account that the risk of myopathy doubles if taken together with medications for hypertension , gout , diabetes .

For chronic liver diseases, it is advisable to take Rosuvastatin in low doses; Pravastatin ( Pravaxol ) can also be used. These drugs provide liver protection, but when using them, you should absolutely not drink alcohol or practice antibiotic .

If there is constant muscle pain or there is a risk of muscle damage, it is also advisable to use Pravastatin, since it is not so toxic to the muscles.

People with chronic kidney disease should not take Fluvastin Lescol , nor should they take Atorvastatin calcium ( Lipitor ), as these medications are toxic to the kidneys.

If a patient seeks to lower low-density cholesterol, it is recommended to use different types of statins.

Currently, there is no clear evidence that it is advisable to take a combination of statins plus nicotinic acid. When taking nicotinic acid, people with diabetes may have a decrease in blood sugar, attacks of gout, bleeding from the gastrointestinal tract are also possible, and the likelihood of rhabdomyolysis and myopathies .

Research on the effects of statins on the body

Previously, cardiologists prescribed statins to people suffering from coronary artery disease , arterial hypertension , and those with low risks of cardiovascular pathologies.

Currently, the attitude towards this type of drugs among some specialists has changed. Although in Russia there have not yet been full-fledged independent studies of the effects of statins on the body.

Meanwhile, Canadian scientists claim that after using statins, the risk of cataracts in patients increased by 57%, and if the person had diabetes , by 82%. Such alarming data were confirmed by statistical analysis.

Experts analyzed the results of fourteen clinical studies that were conducted to study the effect of statins on the body. Their conclusion was that this type of medication reduces the likelihood of strokes and heart attacks, but given the serious side effects, they are not prescribed to people who have not previously suffered strokes or heart disease. According to researchers, people who regularly take such medications develop the following side effects:

• renal failure;
• cataract;
• liver dysfunction;
• depression , mood swings;
• myopathy;
• memory losses.

But in general, there are different points of view on whether these drugs are harmful or relatively safe.

• Scientists from Germany have proven that with low cholesterol levels, the likelihood of developing cancer , liver disease and a number of other serious ailments, as well as early mortality and suicide, increases, thereby confirming that low cholesterol levels are more dangerous than high ones.
• Researchers from the USA claim that heart attacks and strokes do not develop due to high cholesterol, but due to low levels of magnesium in the body.
• Statins can inhibit the important function of cholesterol in repairing disorders in body tissues. In order for the body to grow muscle mass, and for its normal functioning in general, low-density fat cells, that is, “bad” cholesterol, are needed. If its deficiency is noted, myalgia and muscular dystrophy .
• When taking such drugs, cholesterol production is suppressed, and accordingly, the production of mevalonate , which is not only a source of cholesterol, but also a number of other substances. They perform important functions in the body, so their deficiency can provoke the development of diseases.
• This group of medications increases the likelihood of developing diabetes mellitus , and this disease leads to increased cholesterol levels. Various sources claim that if you take statins for a long time, the risk of diabetes ranges from 10 to 70%. Under the influence of these drugs, the concentration of the GLUT4 protein in the cell, which is responsible for blood glucose levels, decreases. British researchers have proven that taking such medications increases the risk of diabetes in women by 70% after a menstrual break.
• Negative side effects develop slowly; accordingly, the patient may not immediately notice this, which is dangerous with prolonged use.
• When using statins, there is an effect on the liver. Those who are obese or lead a sedentary lifestyle note an improvement in their vascular condition for a period of time. But over time, complex processes in the body are disrupted, which can lead to a deterioration in mental processes, especially in older people.

When a person under 50 years of age has elevated cholesterol levels, this indicates that serious disorders are developing in the body that need to be treated. In some countries, programs are being implemented at the national level to promote lowering cholesterol levels by promoting an active lifestyle, changing dietary principles, quitting nicotine addiction, and using statins.

As a result, this method “worked” in many countries: mortality from cardiovascular diseases decreased significantly. However, there is an opinion that quitting smoking, physical activity and changing the menu are a better way to prolong life than using medications that have contraindications and side effects.

Statins for older patients

Among the arguments in favor of the fact that older people should take statins only after carefully weighing the harm and benefits, we can recall a study that involved more than 3 thousand people aged 60 years and older who took statin medications. Approximately 30% noted muscle pain, as well as decreased energy, high fatigue, and weakness.

Muscle pain is most severe in those who have just started taking such medications. As a result, this condition reduces the intensity of physical activity - it is difficult for people to exercise and walk, which ultimately leads to an increased risk of strokes and heart attacks. In addition, a person who moves little begins to gradually increase body weight, which is also a risk of cardiovascular disease.

Fibrates: what is it?

Fibrates are also used to lower cholesterol. These drugs are fibric acid . They bind to bile acid, thereby reducing the active production of cholesterol by the liver.

Fenofibrates medicinally lower lipid , which in turn leads to lower cholesterol. According to clinical studies, the use of fenofibrates lowers cholesterol by 25%, triglycerides by 40-50%, and also increases the level of so-called “good” cholesterol by 10-30%.

Instructions for the use of fenofibrates and ciprofibrates indicate that with high cholesterol levels, these drugs reduce the amount of extravascular deposits, and also reduce cholesterol and triglyceride levels in patients with hypercholesterolemia .

List of fenofibrate drugs:

• Thaicolor;
• Lipantil;
• Exlip 200;
• Ciprofibrate Lipanor;
• Gemfibrozil.

But, before you buy and take such medications, you should keep in mind that taking them leads to certain side effects. As a rule, various digestive disorders most often occur: flatulence , dyspepsia , diarrhea , vomiting .

The following side effects have been reported after taking fenofibrates:

• Digestive system: pancreatitis , hepatitis, vomiting, abdominal pain, nausea, diarrhea, flatulence, the appearance of gallstones.
• Musculoskeletal system: muscle weakness, rhabdomyolysis, diffuse myalgia, myositis, spasms.
• Nervous system: headache, sexual dysfunction.
• Heart and blood vessels: pulmonary embolism, venous thromboembolism.
• Allergic manifestations: skin itching and rash, photosensitivity, urticaria .

Combining statins with fibrates is practiced to reduce the dosage and, accordingly, the negative effects of statins.

Rating of cholesterol pills

The rating of medications that are aimed at treating and preventing high cholesterol was based on the results of comparative tests, as well as after analyzing the properties and composition of each drug. Additionally, customer reviews were also taken into account, as well as the opinions of doctors who reviewed all medications. The rating was also determined by checking each drug individually; during the check, we looked at the following nuances:

• Compound;
• Release form;
• Dosage;
• Price;
• Action;
• Side effects;
• Contraindications.

Testing each drug allowed us to rank the best cholesterol-lowering pills. They are characterized by rapid action, do not cause negative manifestations, and quickly neutralize the problem.

The best drugs for dizziness

All other medications

Your doctor may recommend taking dietary supplements (dietary supplements).

However, natural remedies such as Omega 3 , Tykveol , flaxseed oil , and lipoic acid lower cholesterol levels slightly.

It should be borne in mind that dietary supplements are not drugs, therefore such drugs are inferior to statin drugs in terms of preventing cardiovascular diseases.

List of dietary supplements that are used for this purpose and contain natural components:

• Omega Forte;
• Doppelhertz Omega;
• Tykveol;
• Lipoic acid;
• SitoPren.

Omega 3

Tablets containing fish oil ( Omega 3 , Oceanol , Omacor ) are recommended for people who want to lower cholesterol. Fish oil protects the body from the development of vascular and heart diseases, as well as from depression and arthritis. But you need to drink fish oil very carefully, since taking it increases the risk of chronic pancreatitis .

Tykveol

Pumpkin seed oil is indicated for use by those who suffer from cholecystitis , cerebral atherosclerosis hepatitis . The product provides choleretic, anti-inflammatory, antioxidant, hepatoprotective effects.

Lipoic acid

This remedy is an endogenous antioxidant , it is used for the prevention and treatment of coronary atherosclerosis. There is a positive effect of the drug on carbohydrate metabolism. When taken, the trophism of neurons improves, and glycogen levels in the liver increase.

Vitamins

Vitamins help normalize cholesterol levels, increase hemoglobin , etc. The body needs vitamin B12 and folic acid , nicotinic acid . At the same time, it is very important that these are natural vitamins, that is, it is important to eat those foods that contain these vitamins.

SitoPren

Dietary supplement – ​​fir foot extract, it contains beta-sitosterol, polyprenols. Should be taken for hypertension , atherosclerosis , high levels of triglycerides and cholesterol.

Policosanol

Dietary supplement – ​​plant wax extract. Helps reduce low-density cholesterol levels and helps prevent atherosclerosis.

Other means

Bile acid sequestrants ( Kolesevelam , etc.) are medications that are used in complex treatment as an auxiliary component for lowering cholesterol. They suppress its synthesis in plasma.

Ciprofibrate Lipanor - suppresses cholesterol synthesis in the liver, lowers its level in the blood, reducing the level of atherogenic lipoproteins.

Which brand of cholesterol pills is better to choose?

There are different medications for lowering cholesterol; they are produced by various pharmacological companies. The rating describes the manufacturers of the best cholesterol pills that are worth paying attention to:

• Teva is a pharmaceutical company in Israel that has been creating medicines since 1901. Its funds are aimed at treating diseases and preventing various pathologies. The composition contains natural and safe ingredients, each capsule and tablet has a good dosage.
• Pierre Fabre Medicine Production is a French pharmaceutical company that produces drugs for treatment and prevention. Tablets are created after conducting scientific research and determining their effectiveness.
• Lekpharm is a pharmaceutical company that creates medicines using modern technologies. Certified equipment is used in production; only professionals work in the company.
• Novartis is a pharmaceutical corporation that creates tablets that are supplied to many countries in Europe and the USA. The company was founded in 1996 in Switzerland. It produces medicines for the treatment of diseases associated with various systems and organs.
• Aktavis is a pharmaceutical company that produces tablets for various diseases related to the cardiovascular system. Medicines are supplied to different countries; more than 60 countries around the world sell medicines under the brand.
• Sandoz is a pharmaceutical company that creates medicinal tablets for the treatment of infectious, respiratory, and cardiovascular diseases. Medicines improve the functioning of the nervous and cardiovascular systems and have a rapid effect.
• Pfizer is an American pharmaceutical company that has been creating medical products since 1997. The main headquarters is located in New York, the research center is in Groton. The company creates more than 20 items of different release forms.
• Dr. Reddy’s is an Indian company that, since 2015, has been creating a large volume of medicines aimed at treating various diseases. The company itself was founded in 1984; it works with international markets and supplies medicines to developed countries.
• Pharmascience Inc. is a company founded in 1983, it creates medicines from various fields. Medicines are created not only for treatment, but also for the prevention of viral diseases. In total, the company created more than 40 types of medicines.
• Evalar is a pharmaceutical company that creates dietary supplements for the treatment of diseases and prevention. The preparations contain only natural herbal ingredients; the products are available in different forms.