Pills for high cholesterol

In the complex therapy of hypercholesterolemia, medications are used that help reduce the level of cholesterol and lipoprotein in the blood - hypolipidemic agents with different pharmacological characteristics or, as they are often called, pills for high cholesterol. This review examines the drugs that are usually prescribed by doctors.

Indications for the use of tablets for high cholesterol

The main indications for the use of tablets for high cholesterol are its level in the blood above 5.5-6 mmol per liter against the background of existing diseases of the cardiovascular system, including atherosclerosis, arterial hypertension, coronary heart disease and myocardial infarction.

In addition, drugs of this group are intended to reduce excess cholesterol levels in cases of adipose tissue adipose tissue (obesity), liver and pancreas pathologies, diabetes mellitus and chronic renal failure, and various types of hyperlipoproteinemia and hypertriglyceridemia.

The names of the high cholesterol pills most often prescribed to patients with the above mentioned diseases are as follows:

• Atorvastatin (Atoris, Liprimar, Torvacard), Lovastatin (Lovasterol, Mevacor, Mefacor), Simvastatin (Actalipid, Zocor, Zorstat), Rosuvastin (Crestor) - statins;
• Gemfibrozil (Gevilon, Hypolixan, Ipolipid, Clopidogrel), Fenofibrate (Benprofibrate, Lipidil, Lipofen, Nolipax, Protolipan) are lipid modifiers of the fibrate group (fibrates);
• Nicotinamide (Niacinamide, Nicamide, Nikofort, Nikovit) nicotinic acid (vitamin PP) and its derivatives;
• Cholestipol (Cholestid) drugs that bind bile acids;
• Fenbutol (Lorelcol, Lesterol, Sinlestan, etc.) derivatives of butylphenols;
• Ezetimibe (Ezetrol) is a selective cholesterol uptake inhibitor.

Pharmacodynamics of high cholesterol tablets

Different groups of hypolipidemic drugs have different mechanisms of action. The pharmacodynamics of pills for high cholesterol, related to the statin group, is based on the inactivation of the enzyme that regulates one of the first stages of cholesterol biosynthesis in the liver and intestines. Firstly, due to the decrease in the activity of this enzyme, the production of cholesterol in the body is reduced. Secondly, on the membranes of liver cells, the number of receptors for protein-fat compounds with a high cholesterol content of low-density lipoproteins (LDL) increases, binding cholesterol and ensuring its transportation with the bloodstream to the tissues of the body.

In the pharmacodynamics of Gemfibrozil and other fibrates, the main task of facilitating lipid metabolism and breaking down fats (triglycerides) and LDL is performed by fenofibric acid compounds (belonging to the class of amphipathic carboxylic acids). These substances activate LPL (lipoprotein lipase), an enzyme that regulates the content of fats in the blood. And LPL affects intracellular alpha receptors (PPAR-α), which modulate carbohydrate-lipid metabolism and differentiation of adipose tissue.

Nicotinic acid functions as a non-protein enzyme involved in the body's oxidation-reduction processes, including the breakdown of carbohydrates and fats to obtain energy. An increase in nicotinic acid leads to the activation of lipoprotein lipase and, as a consequence, to an increase in lipid utilization and a decrease in the content of triglycerides and lipoproteins in blood plasma.

The pharmacological action of the bile acid binder Cholestipol is provided by high-molecular anion-exchange resins of microheterogeneous structure that are insoluble in the gastrointestinal tract and prevent the reabsorption of bile and cholesterol in the intestine. This leads to the removal of cholesterol from the body through the intestine and a decrease in its content in the blood.

Butylphenol derivatives (Phenbutol, etc.) not only inhibit cholesterol production, but also reduce its absorption during digestion. And the pharmacodynamics of drugs that selectively inhibit the absorption of cholesterol from the intestine (Ezetimibe) is due to the blocking of a specific protein that is responsible for transporting cholesterol to liver cells.

Pharmacokinetics of high cholesterol tablets

The active substances of the high cholesterol tablets Atorvastatin, Lovastatin and other statins after oral administration are absorbed in the gastrointestinal tract and enter the bloodstream, reaching their highest concentration in the plasma after 90-120 minutes. When statins bind to plasma proteins by almost 96%, their systemic bioavailability does not exceed 30%, which is explained by the process of formation of active metabolites in the liver at the first stage of transformation of the active component of the drugs. In the liver, statins undergo oxidation, after which secondary metabolites are excreted through the intestines (approximately within 24 hours).

The pharmacokinetics of Gemfibrozil and all lipid-modifying drugs differ from statins in that the liver metabolism of the active substance is faster; after 2 hours, the kidneys remove half of the dose taken from the body (the rest is excreted with bile by the intestines).

Due to slow absorption in the gastrointestinal tract, Fenbutol tablets for high cholesterol act gradually, which provides the drugs of this group with a prolonged (about six months after stopping regular use) therapeutic effect in the form of antioxidant and anti-sclerotic action - reducing the oxidation of blood lipids and their deposition on the walls of blood vessels in the form of atherosclerotic plaques.

The pharmacokinetics of cholesterol-absorbing Ezetimibe are characterized by active binding to glucuronic acid phenols formed in the small intestine and liver during the body's self-cleansing of foreign and harmful substances. The pharmacologically active conjugate ezetimibe-glucuronide binds to plasma proteins and is eliminated from the blood via the kidneys and intestines within approximately 10 days.

Method of administration and dosage

The only way to use pills for high cholesterol is orally. It should be remembered that individual doses of any hypolipidemic drug are determined only by the attending physician - based on a blood test for cholesterol levels.

The standard daily dose of statins is 0.01 g (taken once a day, at the same time each day), with a subsequent increase to a maximum of 0.08 g as prescribed by a doctor.

The usual single dose of Gemfibrozil is 0.3 g (twice a day, half an hour before meals); Fenofibrate is also taken twice a day at 0.1 g (during meals, in the morning and in the evening).

The optimal single dose of nicotinic acid is 20-50 mg (2-3 times during the day); simultaneous intake of methionine will protect the liver from fat accumulation.

Cholestipol (1 g tablets) is recommended to be taken 5 tablets per day, after 1-2 months the daily dose is doubled. Fenbutol is prescribed one tablet (0.25 g) twice a day, during meals. The recommended daily dose of tablets for high cholesterol is Ezetimibe 10 mg (single dose).

An overdose of the listed medications, as noted in the instructions for the drugs, may occur when the dosage prescribed by the doctor is exceeded, however, there is no information about such cases.

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Contraindications for use

Tablets for high cholesterol, in addition to individual hypersensitivity to the active substances of the drugs, have the following contraindications for use:

• statins: severe or existing history of liver and kidney pathologies, diseases of the musculoskeletal system;
• fibrates: bile duct problems, autoimmune biliary cirrhosis;
• nicotinic acid and its derivatives: acute gastric and duodenal ulcers, kidney stones, hepatitis;
• bile acid binders: impaired absorption of fats in the intestine (steatorrhea), childhood;
• butylphenol derivatives: liver and/or kidney disease, age under 14 years;
• selective cholesterol absorption inhibitors: liver failure of any etiology, age under 18 years.

The use of cholesterol pills during pregnancy is included in the list of contraindications for lipid-lowering drugs of all pharmacological subgroups, including nicotinic acid.

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Side effects

Cholesterol pills from the statin group can have the following side effects: headaches and dizziness, dry mouth, heartburn, nausea, diarrhea, abdominal pain; liver dysfunction (increased concentration of liver enzymes transaminases), pancreas and heart (tachycardia); diabetes, insomnia, cramps and muscle pain; decreased visual acuity (up to the development of cataracts), impotence, cognitive impairment.

The use of Gemfirosil may be accompanied by nausea, stomach discomfort and diarrhea; skin reactions (dermatitis); pain - headaches, muscle pain, joint pain, stomach pain; dysfunction of the liver and gall bladder; anemia, leukopenia, anemia, as well as a decrease in the number of cellular elements (hypoplasia) of the bone marrow. Another drug in this group - Fenofibrate - in addition to the listed side effects, there is a risk of developing gallstone disease.

When using nicotinic acid preparations to lower cholesterol, a drop in blood pressure, the appearance of excess uric acid in the blood, an increase in intracellular liver enzymes and its fatty degeneration are possible. Taking Cholestipol tablets can cause nausea and vomiting, constipation or diarrhea, urticaria and skin inflammation. In case of prolonged treatment with this drug, a lack of vitamins (A, D, E, K) in the body is possible.

Digestive problems and cardiac arrhythmia are side effects of Fenbutol, and the drug Ezitimibe can cause headaches, nausea, muscle and abdominal pain, diarrhea and flatulence, as well as allergic skin rashes.

Interactions with other drugs

The interactions with other drugs identified by the manufacturers of Atorvastatin, Lovastatin, Simvastatin tablets consist of increasing their concentrations in blood plasma with the simultaneous use of antibiotics and fungicides. The combination of statins with hormonal contraceptives contributes to an increase in the concentration of the latter in plasma, and with indirect anticoagulants - reduces the blood clotting time.

Absolute incompatibility of Gemfibrozil with Lovastatin: acute renal failure and muscular dystrophy may develop. And in patients using hormonal drugs for contraception, a serious lipid metabolism disorder is possible. Fenofibrate enhances the effect of coumarin anticoagulants and phenylindanedione derivatives, as well as drugs containing salicylates and diabetes tablets.

Cholestipol, by binding bile acids in the intestine, disrupts the normal absorption of other oral medications, to avoid which all other medications must be taken 1-2 hours earlier.

All of the above-mentioned tablets for high cholesterol have the same storage conditions: a dry place, protected from bright light and out of reach of children, at normal room temperature (no more than +25-28°C).

The shelf life is also standard: two years from the production date indicated on the packaging.

See also the article Treatment of high cholesterol: the most common methods